Analogs or derivatives of morphine.
The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.
Strong dependence, both physiological and emotional, upon morphine.
Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.
Progressive diminution of the susceptibility of a human or animal to the effects of a drug, resulting from its continued administration. It should be differentiated from DRUG RESISTANCE wherein an organism, disease, or tissue fails to respond to the intended effectiveness of a chemical or drug. It should also be differentiated from MAXIMUM TOLERATED DOSE and NO-OBSERVED-ADVERSE-EFFECT LEVEL.
Agents that induce NARCOSIS. Narcotics include agents that cause somnolence or induced sleep (STUPOR); natural or synthetic derivatives of OPIUM or MORPHINE or any substance that has such effects. They are potent inducers of ANALGESIA and OPIOID-RELATED DISORDERS.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.
Agents inhibiting the effect of narcotics on the central nervous system.
Methods of PAIN relief that may be used with or in place of ANALGESICS.
Scales, questionnaires, tests, and other methods used to assess pain severity and duration in patients or experimental animals to aid in diagnosis, therapy, and physiological studies.
Introduction of therapeutic agents into the spinal region using a needle and syringe.
An opioid analgesic related to MORPHINE but with less potent analgesic properties and mild sedative effects. It also acts centrally to suppress cough.
Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.
Pain during the period after surgery.
Compounds capable of relieving pain without the loss of CONSCIOUSNESS.
The relationship between the dose of an administered drug and the response of the organism to the drug.
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
Relief of PAIN, without loss of CONSCIOUSNESS, through ANALGESIC AGENTS administered by the patients. It has been used successfully to control POSTOPERATIVE PAIN, during OBSTETRIC LABOR, after BURNS, and in TERMINAL CARE. The choice of agent, dose, and lockout interval greatly influence effectiveness. The potential for overdose can be minimized by combining small bolus doses with a mandatory interval between successive doses (lockout interval).
A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
A narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed)
An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.
A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078)
Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.
An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.
Central gray matter surrounding the CEREBRAL AQUEDUCT in the MESENCEPHALON. Physiologically it is probably involved in RAGE reactions, the LORDOSIS REFLEX; FEEDING responses, bladder tonus, and pain.
A semisynthetic derivative of CODEINE.
The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)
One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla.
A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.
A narcotic used as a pain medication. It appears to be an agonist at kappa opioid receptors and an antagonist or partial agonist at mu opioid receptors.

A practical approach to determine cutoff concentrations for opiate testing with simultaneous detection of codeine, morphine, and 6-acetylmorphine in urine. (1/272)

BACKGROUND: Both the Department of Defense (DoD) and the Department of Health and Human Services (DHHS) currently require two confirmation tests to verify use of heroin, one test for total morphine and a separate test for 6-acetylmorphine (6-AM). Our aim was to determine appropriate free-codeine, free-morphine, and 6-AM cutoff concentrations that could be substituted for total-morphine, total-codeine, and 6-AM cutoff concentrations and to develop a less labor-intensive method for measuring codeine, morphine, and 6-AM. METHODS: Urine samples containing opiates were extracted, derivatized, and analyzed using gas chromatography-mass spectrometry with selective ion monitoring. RESULTS: The limits of detection for codeine, morphine, and 6-AM were 6, 5, and 0.5 microg/L, respectively. Recoveries were >90%. Quantification was linear over the concentration range of 6-1000 microg/L for codeine, 5-5000 microg/L for morphine, and 0.5-800 microg/L for 6-AM. Cutoff concentrations for confirmation of opiates were 100, 100, and 10 microg/L for free codeine, free morphine, and 6-AM. CONCLUSION: The proposed cutoff concentrations for free morphine and 6-AM provide better detection windows for morphine and heroin use than the cutoff concentrations for total morphine and 6-AM used at present. Detection of free codeine, instead of total codeine, simplifies interpretation of codeine use. The single-extraction method enables simultaneous, less labor-intensive analysis of morphine, codeine, and 6-AM.  (+info)

Pharmacokinetic modeling of M6G formation after oral administration of morphine in healthy volunteers. (2/272)

BACKGROUND: Morphine is metabolized to two major metabolites, morphine-3-glucuronide and morphine-6-glucuronide (M6G). Under the conditions of long-term oral morphine administration, the accumulation of M6G may contribute to the analgesic effects, but it may also cause respiratory depression. METHODS: Five healthy male volunteers (ages 25-34 yr) received 90 mg MST (morphine sulfate 5H2O sustained-released tablet, equivalent to 67.8 mg oral morphine). Multiple plasma and urine samples were taken for as long as 14 and 36 h, respectively. Individual pharmacokinetics after intravenous administration of morphine and M6G were available from a previous investigation. A new model that considers the M6G-plasma profile as a sum of the input from the first-pass metabolism of morphine and the input from systemically available morphine was applied to the plasma concentration versus time curves of M6G. The concentrations of M6G at the effect site after long-term morphine administration were simulated. RESULTS: The fraction of morphine absorbed from the gut was 82+/-14%. Of this, 42+/-8% passed through the liver, resulting in an oral bioavailability of morphine of 34+/-9%. Of the total amount of M6G, 71+/-7% was formed during the first-pass metabolism, and 29+/-7% was formed by metabolism of systemic morphine. After 36 h, the amounts of M6G and morphine excreted in the urine were 92+/-17% and 9+/-3%, respectively. Simulation of effect-site concentrations of M6G indicated that after multiple oral dosing of morphine in patients with normal liver and renal function, M6G might reach concentrations two times greater than that of morphine. CONCLUSIONS: M6G may contribute to the analgesic and side effects seen with long-term morphine treatment. The current model of morphine and M6G pharmacokinetics after oral administration of morphine may serve as a pharmacokinetic basis for experiments evaluating the analgesic contribution of M6G with long-term oral dosing of morphine.  (+info)

Pharmacokinetics of morphine and its glucuronides following intravenous administration of morphine in patients undergoing continuous ambulatory peritoneal dialysis. (3/272)

BACKGROUND: Conjugation with glucuronic acid represents the major route of biotransformation of morphine. The glucuronides morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) are eliminated via the kidneys. Therefore, chronic renal failure should affect the disposition of M3G and M6G. Numerous patients undergoing long-term continuous ambulatory peritoneal dialysis (CAPD) require pain treatment with morphine. There are only limited data available about the disposition of morphine and its active metabolites M6G and M3G in patients on CAPD. We therefore investigated the pharmacokinetics of morphine and its metabolites in CAPD patients. METHODS: This was a single intravenous dose pharmacokinetic study in 10 CAPD patients (1 female, 9 male, age 31-69 years). Morphine-hydrochloride (Mo) (10 mg) was administered intravenously. Serum, urine, and dialysate samples were collected during 24 h. GC-MS-MS and HPLC-MS methods were used to quantify respectively morphine and morphine glucuronides. RESULTS: While systemic clearance of morphine (1246+/-240 ml/min) was in the range observed in patients with normal kidney function, both M3G and M6G showed substantial accumulation. The area under the concentration-time curve (AUC) ratio of M3G:Mo (33.4+/-7.1) and of M6G:Mo (12.2+/-3.2) was 5.5 and 13.5 times higher than in patients with normal kidney function. Renal clearances of morphine, M3G, and M6G (morphine 3.0+/-2.5 ml/min; M3G 3.9+/-2.2 ml/min; M6G 3.6+/-2.2 ml/min) and dialysate clearances (morphine 4.1+/-1.3 ml/min; M3G 3.2+/-0.7 ml/min; M6G 3.0+/-0.8 ml/min) were extremely low. Therefore the accumulation of M6G and M3G is readily explained by kidney failure which is not compensated by CAPD. CONCLUSION: Accumulation of M3G and M6G is due to the substantially lowered clearance by residual renal function and peritoneal dialysis. In view of the accumulation of potential active metabolites, subsequent investigations have to assess the frequency of side-effects in patients on CAPD.  (+info)

Detection of 6-acetylmorphine in vitreous humor and cerebrospinal fluid--comparison with urinary analysis for proving heroin administration in opiate fatalities. (4/272)

The concentrations of morphine and 6-acetylmorphine (6-AM) in urine, cerebrospinal fluid (CSF), and vitreous humor (VH) and the morphine concentrations in blood were determined by gas chromatography-mass spectrometry for 29 fatalities after abuse of heroin either alone or in combination with alcohol and other drugs. 6-AM was found above a quantitation limit of 1 ng/mL in urine in 89% of the cases, in CSF in 68% of the cases, and in VH in 75% of the cases. The 6-AM concentrations in CSF (mean, 10 ng/mL) and VH (mean, 17 ng/mL) were in general much smaller than in urine (mean, 170 ng/mL); therefore, the different pharmacokinetic behavior of the fluids is discussed. There is no uniformity between the three fluids with respect to the presence or absence of 6-AM. Therefore, CSF or VH may be used as complementary or alternative materials to urine in order to prove heroin uptake in opiate fatalities.  (+info)

GC-MS confirmation of codeine, morphine, 6-acetylmorphine, hydrocodone, hydromorphone, oxycodone, and oxymorphone in urine. (5/272)

A procedure for the simultaneous confirmation of codeine, morphine, 6-acetylmorphine, hydrocodone, hydromorphone, oxycodone, and oxymorphone in urine specimens by gas chromatography-mass spectrometry (GC-MS) is described. After the addition of nalorphine and naltrexone as the two internal standards, the urine is hydrolyzed overnight with beta-glucuronidase from E. coli. The urine is adjusted to pH 9 and extracted with 8% trifluoroethanol in methylene dichloride. After evaporating the organic, the residue is sequentially derivatized with 2% methoxyamine in pyridine, then with propionic anhydride. The ketone groups on hydrocodone, hydromorphone, oxycodone, oxymorphone, and naltrexone are converted to their respective methoximes. Available hydroxyl groups on the O3 and O6 positions are converted to propionic esters. After a brief purification step, the extracts are analyzed by GC-MS using full scan electron impact ionization. Nalorphine is used as the internal standard for codeine, morphine, and 6-acetylmorphine; naltrexone is used as the internal standard for the 6-keto-opioids. The method is linear to 2000 ng/mL for the 6-keto-opioids and to 5000 ng/mL for the others. The limit of quantitation is 25 ng/mL in hydrolyzed urine. Day-to-day precision at 300 and 1500 ng/mL ranged between 6 and 10.9%. The coefficients of variation for 6-acetylmorphine were 12% at both 30 and 150 ng/mL. A list of 38 other basic drugs or metabolites detected by this method is tabulated.  (+info)

Topical opioids in mice: analgesia and reversal of tolerance by a topical N-methyl-D-aspartate antagonist. (6/272)

In addition to its central actions, morphine has important peripheral effects. To examine peripheral analgesic mechanisms, we developed a topical opioid paradigm in which the tail was immersed in a dimethyl sulfoxide (DMSO) solution containing various drugs. Alone, DMSO was inactive in the tail-flick assay in mice. DMSO solutions containing morphine and peptides such as [D-Ala2,MePhe4, Gly(ol)5]enkephalin (DAMGO) produced a potent, dose-dependent analgesia with the radiant heat tail-flick assay. The actions of the drugs were local. Analgesia was observed only in regions of the tail exposed to the solution and not in more proximal unexposed portions of the tail. Immersion of the tail in a solution containing either 125I-labeled morphine or 125I-labeled DAMGO revealed no detectable uptake of radioactivity into the brain, spinal cord, or blood. In the tail, radioactivity was limited only to the regions actually immersed in the solutions. The topical drugs potentiated systemic agents, similar to the previously established synergy between peripheral and central sites of action. Local tolerance was rapidly produced by repeated daily exposure of the tail to morphine. Topical morphine tolerance was effectively blocked by the N-methyl-D-aspartate (NMDA) antagonist MK801 given either systemically or topically but not intrathecally. The ability of a topical NMDA antagonist to block local morphine tolerance suggests that peripheral NMDA receptors mediate topical morphine tolerance. Morphine was cross-tolerant to DAMGO, but not to morphine-6beta-glucuronide, implying different mechanisms of action. These observations are significant in the design and use of opioids clinically.  (+info)

kappa-Opioid receptor effects of butorphanol in rhesus monkeys. (7/272)

Butorphanol and nalbuphine have substantial affinity for mu and kappa-opioid receptor sites, yet their behavioral effects in monkeys are largely consistent with a mu receptor mechanism of action. Using ethylketocyclazocine (EKC) discrimination and diuresis assays in rhesus monkeys (Macaca mulatta), the purpose of the current investigation was to characterize the in vivo kappa-opioid activity of these compounds through the use of an insurmountable mu-opioid receptor antagonist, clocinnamox. Alone, butorphanol (0.001-0.032 mg/kg i.m.) failed to generalize to EKC, and pretreatment with the competitive opioid receptor antagonist quadazocine (0.1 or 0.32 mg/kg i.m.) did not alter this generalization. At 24 h after clocinnamox (0.1 mg/kg i.m.) administration, butorphanol fully generalized to EKC, and this generalization was maintained in two of three monkeys at 72 h. Parallel results were observed in diuresis: butorphanol alone and in the presence of quadazocine (1 mg/kg i.m.) did not alter urine output, and a marked diuretic effect was demonstrated 24 h to 2 weeks after clocinnamox administration. Clocinnamox did not alter the discriminative stimulus or diuretic effects of nalbuphine or of the kappa-opioid receptor agonists EKC or U69593. These results are consistent with an in vivo agonist activity of butorphanol at kappa-opioid receptors that can only be demonstrated when an insurmountable antagonist has substantially eliminated the dominant receptor population through which it exerts its action.  (+info)

Morphine and morphine-6-glucuronide in the plasma and cerebrospinal fluid of children. (8/272)

AIMS: To measure morphine and morphine-6-glucuronide in the plasma and cerebrospinal fluid of children following a single intravenous dose of morphine. METHODS: Twenty-nine paired samples of cerebrospinal fluid and plasma were collected from children with leukaemia undergoing therapeutic lumbar puncture. An intravenous dose of morphine was administered at selected intervals before the procedure. Concentrations of morphine and morphine-6-glucuronide (M6G) were measured in each sample. Morphine was measured using a specific radioimmunoassay (r.i.a.) and M6G was measured using a novel enzyme-linked immunosorbent assay (ELISA). RESULTS: The ELISA for measuring M6G was highly sensitive. The intra-and interassay variations were less than 15%. Using a two-compartment model for plasma morphine, the area under the curve to infinity (AUC, 7143 ng ml-1 min), volume of distribution (3.6 l kg-1 ) and elimination half-life (88 min) were comparable with those reported in adults. Clearance (35 ml min-1 ) was higher than that in adults. Morphine-6-glucuronide was readily synthesized by the children in this study. The elimination half-life (321 min) and AUC (35507 ng ml-1 min) of plasma M6G were much greater than those of morphine. CONCLUSIONS: Extensive metabolism of morphine to M6G in children with cancer has been demonstrated. These data provide further evidence to support the importance of M6G accumulation after multiple doses. There was no evidence that morphine passed more easily into the CSF of children than adults.  (+info)

Morphine derivatives are substances that are synthesized from or structurally similar to morphine, a natural opiate alkaloid found in the opium poppy. These compounds share many of the same pharmacological properties as morphine and are often used for their analgesic (pain-relieving), sedative, and anxiolytic (anxiety-reducing) effects.

Examples of morphine derivatives include:

1. Hydrocodone: A semi-synthetic opioid that is often combined with acetaminophen for the treatment of moderate to severe pain.
2. Oxycodone: A synthetic opioid that is used for the management of moderate to severe pain, either alone or in combination with other medications.
3. Hydromorphone: A potent semi-synthetic opioid that is used for the treatment of severe pain, typically in a hospital setting.
4. Oxymorphone: A synthetic opioid that is similar to hydromorphone in its potency and use for managing severe pain.
5. Codeine: A naturally occurring opiate alkaloid that is less potent than morphine but still has analgesic, cough suppressant, and antidiarrheal properties. It is often combined with other medications for various therapeutic purposes.
6. Fentanyl: A synthetic opioid that is significantly more potent than morphine and is used for the management of severe pain, typically in a hospital or clinical setting.

It's important to note that while these derivatives can be beneficial for managing pain and other symptoms, they also carry a risk of dependence, addiction, and potentially life-threatening side effects such as respiratory depression. As a result, their use should be closely monitored by healthcare professionals and prescribed cautiously.

Morphine is a potent opioid analgesic (pain reliever) derived from the opium poppy. It works by binding to opioid receptors in the brain and spinal cord, blocking the transmission of pain signals and reducing the perception of pain. Morphine is used to treat moderate to severe pain, including pain associated with cancer, myocardial infarction, and other conditions. It can also be used as a sedative and cough suppressant.

Morphine has a high potential for abuse and dependence, and its use should be closely monitored by healthcare professionals. Common side effects of morphine include drowsiness, respiratory depression, constipation, nausea, and vomiting. Overdose can result in respiratory failure, coma, and death.

Morphine dependence is a medical condition characterized by a physical and psychological dependency on morphine, a potent opioid analgesic. This dependence develops as a result of repeated use or abuse of morphine, leading to changes in the brain's reward and pleasure pathways. The Diagnostic and Statistical Manual of Mental Disorders, 5th Edition (DSM-5) outlines the following criteria for diagnosing opioid dependence, which includes morphine:

A. A problematic pattern of opioid use leading to clinically significant impairment or distress, as manifested by at least two of the following, occurring within a 12-month period:

1. Opioids are often taken in larger amounts or over a longer period than was intended.
2. There is a persistent desire or unsuccessful efforts to cut down or control opioid use.
3. A great deal of time is spent in activities necessary to obtain the opioid, use the opioid, or recover from its effects.
4. Craving, or a strong desire or urge to use opioids.
5. Recurrent opioid use resulting in a failure to fulfill major role obligations at work, school, or home.
6. Continued opioid use despite having persistent or recurrent social or interpersonal problems caused or exacerbated by the effects of opioids.
7. Important social, occupational, or recreational activities are given up or reduced because of opioid use.
8. Recurrent opioid use in situations in which it is physically hazardous.
9. Continued opioid use despite knowing that a physical or psychological problem is likely to have been caused or exacerbated by opioids.
10. Tolerance, as defined by either of the following:
a. A need for markedly increased amounts of opioids to achieve intoxication or desired effect.
b. A markedly diminished effect with continued use of the same amount of an opioid.
11. Withdrawal, as manifested by either of the following:
a. The characteristic opioid withdrawal syndrome.
b. The same (or a closely related) substance is taken to relieve or avoid withdrawal symptoms.

Additionally, it's important to note that if someone has been using opioids for an extended period and suddenly stops taking them, they may experience withdrawal symptoms. These can include:

- Anxiety
- Muscle aches
- Insomnia
- Runny nose
- Sweating
- Diarrhea
- Nausea or vomiting
- Abdominal cramping
- Dilated pupils

If you or someone you know is struggling with opioid use, it's essential to seek professional help. There are many resources available, including inpatient and outpatient treatment programs, support groups, and medications that can help manage withdrawal symptoms and cravings.

Analgesics, opioid are a class of drugs used for the treatment of pain. They work by binding to specific receptors in the brain and spinal cord, blocking the transmission of pain signals to the brain. Opioids can be synthetic or natural, and include drugs such as morphine, codeine, oxycodone, hydrocodone, hydromorphone, fentanyl, and methadone. They are often used for moderate to severe pain, such as that resulting from injury, surgery, or chronic conditions like cancer. However, opioids can also produce euphoria, physical dependence, and addiction, so they are tightly regulated and carry a risk of misuse.

Drug tolerance is a medical concept that refers to the decreased response to a drug following its repeated use, requiring higher doses to achieve the same effect. This occurs because the body adapts to the presence of the drug, leading to changes in the function or expression of targets that the drug acts upon, such as receptors or enzymes. Tolerance can develop to various types of drugs, including opioids, benzodiazepines, and alcohol, and it is often associated with physical dependence and addiction. It's important to note that tolerance is different from resistance, which refers to the ability of a pathogen to survive or grow in the presence of a drug, such as antibiotics.

Narcotics, in a medical context, are substances that induce sleep, relieve pain, and suppress cough. They are often used for anesthesia during surgical procedures. Narcotics are derived from opium or its synthetic substitutes and include drugs such as morphine, codeine, fentanyl, oxycodone, and hydrocodone. These drugs bind to specific receptors in the brain and spinal cord, reducing the perception of pain and producing a sense of well-being. However, narcotics can also produce physical dependence and addiction, and their long-term use can lead to tolerance, meaning that higher doses are required to achieve the same effect. Narcotics are classified as controlled substances due to their potential for abuse and are subject to strict regulations.

Naloxone is a medication used to reverse the effects of opioids, both illicit and prescription. It works by blocking the action of opioids on the brain and restoring breathing in cases where opioids have caused depressed respirations. Common brand names for naloxone include Narcan and Evzio.

Naloxone is an opioid antagonist, meaning that it binds to opioid receptors in the body without activating them, effectively blocking the effects of opioids already present at these sites. It has no effect in people who have not taken opioids and does not reverse the effects of other sedatives or substances.

Naloxone can be administered via intranasal, intramuscular, intravenous, or subcutaneous routes. The onset of action varies depending on the route of administration but generally ranges from 1 to 5 minutes when given intravenously and up to 10-15 minutes with other methods.

The duration of naloxone's effects is usually shorter than that of most opioids, so multiple doses or a continuous infusion may be necessary in severe cases to maintain reversal of opioid toxicity. Naloxone has been used successfully in emergency situations to treat opioid overdoses and has saved many lives.

It is important to note that naloxone does not reverse the effects of other substances or address the underlying causes of addiction, so it should be used as part of a comprehensive treatment plan for individuals struggling with opioid use disorders.

Opioid mu receptors, also known as mu-opioid receptors (MORs), are a type of G protein-coupled receptor that binds to opioids, a class of chemicals that include both natural and synthetic painkillers. These receptors are found in the brain, spinal cord, and gastrointestinal tract, and play a key role in mediating the effects of opioid drugs such as morphine, heroin, and oxycodone.

MORs are involved in pain modulation, reward processing, respiratory depression, and physical dependence. Activation of MORs can lead to feelings of euphoria, decreased perception of pain, and slowed breathing. Prolonged activation of these receptors can also result in tolerance, where higher doses of the drug are required to achieve the same effect, and dependence, where withdrawal symptoms occur when the drug is discontinued.

MORs have three main subtypes: MOR-1, MOR-2, and MOR-3, with MOR-1 being the most widely studied and clinically relevant. Selective agonists for MOR-1, such as fentanyl and sufentanil, are commonly used in anesthesia and pain management. However, the abuse potential and risk of overdose associated with these drugs make them a significant public health concern.

Narcotic antagonists are a class of medications that block the effects of opioids, a type of narcotic pain reliever, by binding to opioid receptors in the brain and blocking the activation of these receptors by opioids. This results in the prevention or reversal of opioid-induced effects such as respiratory depression, sedation, and euphoria. Narcotic antagonists are used for a variety of medical purposes, including the treatment of opioid overdose, the management of opioid dependence, and the prevention of opioid-induced side effects in certain clinical situations. Examples of narcotic antagonists include naloxone, naltrexone, and methylnaltrexone.

Analgesia is defined as the absence or relief of pain in a patient, achieved through various medical means. It is derived from the Greek word "an-" meaning without and "algein" meaning to feel pain. Analgesics are medications that are used to reduce pain without causing loss of consciousness, and they work by blocking the transmission of pain signals to the brain.

Examples of analgesics include over-the-counter medications such as acetaminophen (Tylenol) and nonsteroidal anti-inflammatory drugs (NSAIDs) like ibuprofen (Advil, Motrin) and naproxen (Aleve). Prescription opioid painkillers, such as oxycodone (OxyContin, Percocet) and hydrocodone (Vicodin), are also used for pain relief but carry a higher risk of addiction and abuse.

Analgesia can also be achieved through non-pharmacological means, such as through nerve blocks, spinal cord stimulation, acupuncture, and other complementary therapies. The choice of analgesic therapy depends on the type and severity of pain, as well as the patient's medical history and individual needs.

Pain measurement, in a medical context, refers to the quantification or evaluation of the intensity and/or unpleasantness of a patient's subjective pain experience. This is typically accomplished through the use of standardized self-report measures such as numerical rating scales (NRS), visual analog scales (VAS), or categorical scales (mild, moderate, severe). In some cases, physiological measures like heart rate, blood pressure, and facial expressions may also be used to supplement self-reported pain ratings. The goal of pain measurement is to help healthcare providers better understand the nature and severity of a patient's pain in order to develop an effective treatment plan.

Spinal injections, also known as epidural injections or intrathecal injections, are medical procedures involving the injection of medications directly into the spinal canal. The medication is usually delivered into the space surrounding the spinal cord (the epidural space) or into the cerebrospinal fluid that surrounds and protects the spinal cord (the subarachnoid space).

The medications used in spinal injections can include local anesthetics, steroids, opioids, or a combination of these. The purpose of spinal injections is to provide diagnostic information, therapeutic relief, or both. They are commonly used to treat various conditions affecting the spine, such as radicular pain (pain that radiates down the arms or legs), disc herniation, spinal stenosis, and degenerative disc disease.

Spinal injections can be administered using different techniques, including fluoroscopy-guided injections, computed tomography (CT) scan-guided injections, or with the help of a nerve stimulator. These techniques ensure accurate placement of the medication and minimize the risk of complications.

It is essential to consult a healthcare professional for specific information regarding spinal injections and their potential benefits and risks.

Codeine is a opiate analgesic, commonly used for its pain-relieving and cough suppressant properties. It is typically prescribed for mild to moderately severe pain, and is also found in some over-the-counter cold and cough medications. Codeine works by binding to opioid receptors in the brain and spinal cord, which helps to reduce the perception of pain. Like other opiates, codeine can produce side effects such as drowsiness, constipation, and respiratory depression, and it carries a risk of dependence and addiction with long-term use. It is important to follow your healthcare provider's instructions carefully when taking codeine, and to inform them of any other medications you are taking, as well as any medical conditions you may have.

Substance Withdrawal Syndrome is a medically recognized condition that occurs when an individual who has been using certain substances, such as alcohol, opioids, or benzodiazepines, suddenly stops or significantly reduces their use. The syndrome is characterized by a specific set of symptoms that can be physical, cognitive, and emotional in nature. These symptoms can vary widely depending on the substance that was being used, the length and intensity of the addiction, and individual factors such as genetics, age, and overall health.

The Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition (DSM-5), published by the American Psychiatric Association, provides the following diagnostic criteria for Substance Withdrawal Syndrome:

A. The development of objective evidence of withdrawal, referring to the specific physiological changes associated with the particular substance, or subjective evidence of withdrawal, characterized by the individual's report of symptoms that correspond to the typical withdrawal syndrome for the substance.

B. The symptoms cause clinically significant distress or impairment in social, occupational, or other important areas of functioning.

C. The symptoms are not better explained by co-occurring mental, medical, or other substance use disorders.

D. The withdrawal syndrome is not attributable to another medical condition and is not better accounted for by another mental disorder.

The DSM-5 also specifies that the diagnosis of Substance Withdrawal Syndrome should be substance-specific, meaning that it should specify the particular class of substances (e.g., alcohol, opioids, benzodiazepines) responsible for the withdrawal symptoms. This is important because different substances have distinct withdrawal syndromes and require different approaches to management and treatment.

In general, Substance Withdrawal Syndrome can be a challenging and potentially dangerous condition that requires professional medical supervision and support during the detoxification process. The specific symptoms and their severity will vary depending on the substance involved, but they may include:

* For alcohol: tremors, seizures, hallucinations, agitation, anxiety, nausea, vomiting, and insomnia.
* For opioids: muscle aches, restlessness, lacrimation (tearing), rhinorrhea (runny nose), yawning, perspiration, chills, mydriasis (dilated pupils), piloerection (goosebumps), nausea or vomiting, diarrhea, and abdominal cramps.
* For benzodiazepines: anxiety, irritability, insomnia, restlessness, confusion, hallucinations, seizures, and increased heart rate and blood pressure.

It is essential to consult with a healthcare professional if you or someone you know is experiencing symptoms of Substance Withdrawal Syndrome. They can provide appropriate medical care, support, and referrals for further treatment as needed.

Postoperative pain is defined as the pain or discomfort experienced by patients following a surgical procedure. It can vary in intensity and duration depending on the type of surgery performed, individual pain tolerance, and other factors. The pain may be caused by tissue trauma, inflammation, or nerve damage resulting from the surgical intervention. Proper assessment and management of postoperative pain is essential to promote recovery, prevent complications, and improve patient satisfaction.

Analgesics are a class of drugs that are used to relieve pain. They work by blocking the transmission of pain signals in the nervous system, allowing individuals to manage their pain levels more effectively. There are many different types of analgesics available, including both prescription and over-the-counter options. Some common examples include acetaminophen (Tylenol), ibuprofen (Advil or Motrin), and opioids such as morphine or oxycodone.

The choice of analgesic will depend on several factors, including the type and severity of pain being experienced, any underlying medical conditions, potential drug interactions, and individual patient preferences. It is important to use these medications as directed by a healthcare provider, as misuse or overuse can lead to serious side effects and potential addiction.

In addition to their pain-relieving properties, some analgesics may also have additional benefits such as reducing inflammation (like in the case of nonsteroidal anti-inflammatory drugs or NSAIDs) or causing sedation (as with certain opioids). However, it is essential to weigh these potential benefits against the risks and side effects associated with each medication.

When used appropriately, analgesics can significantly improve a person's quality of life by helping them manage their pain effectively and allowing them to engage in daily activities more comfortably.

A dose-response relationship in the context of drugs refers to the changes in the effects or symptoms that occur as the dose of a drug is increased or decreased. Generally, as the dose of a drug is increased, the severity or intensity of its effects also increases. Conversely, as the dose is decreased, the effects of the drug become less severe or may disappear altogether.

The dose-response relationship is an important concept in pharmacology and toxicology because it helps to establish the safe and effective dosage range for a drug. By understanding how changes in the dose of a drug affect its therapeutic and adverse effects, healthcare providers can optimize treatment plans for their patients while minimizing the risk of harm.

The dose-response relationship is typically depicted as a curve that shows the relationship between the dose of a drug and its effect. The shape of the curve may vary depending on the drug and the specific effect being measured. Some drugs may have a steep dose-response curve, meaning that small changes in the dose can result in large differences in the effect. Other drugs may have a more gradual dose-response curve, where larger changes in the dose are needed to produce significant effects.

In addition to helping establish safe and effective dosages, the dose-response relationship is also used to evaluate the potential therapeutic benefits and risks of new drugs during clinical trials. By systematically testing different doses of a drug in controlled studies, researchers can identify the optimal dosage range for the drug and assess its safety and efficacy.

Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage. It is a complex phenomenon that can result from various stimuli, such as thermal, mechanical, or chemical irritation, and it can be acute or chronic. The perception of pain involves the activation of specialized nerve cells called nociceptors, which transmit signals to the brain via the spinal cord. These signals are then processed in different regions of the brain, leading to the conscious experience of pain. It's important to note that pain is a highly individual and subjective experience, and its perception can vary widely among individuals.

Opioid receptors are a type of G protein-coupled receptor (GPCR) found in the cell membranes of certain neurons in the central and peripheral nervous system. They bind to opioids, which are chemicals that can block pain signals and produce a sense of well-being. There are four main types of opioid receptors: mu, delta, kappa, and nociceptin. These receptors play a role in the regulation of pain, reward, addiction, and other physiological functions. Activation of opioid receptors can lead to both therapeutic effects (such as pain relief) and adverse effects (such as respiratory depression and constipation).

Naltrexone is a medication that is primarily used to manage alcohol dependence and opioid dependence. It works by blocking the effects of opioids and alcohol on the brain, reducing the euphoric feelings and cravings associated with their use. Naltrexone comes in the form of a tablet that is taken orally, and it has no potential for abuse or dependence.

Medically, naltrexone is classified as an opioid antagonist, which means that it binds to opioid receptors in the brain without activating them, thereby blocking the effects of opioids such as heroin, morphine, and oxycodone. It also reduces the rewarding effects of alcohol by blocking the release of endorphins, which are natural chemicals in the brain that produce feelings of pleasure.

Naltrexone is often used as part of a comprehensive treatment program for addiction, along with counseling, behavioral therapy, and support groups. It can help individuals maintain abstinence from opioids or alcohol by reducing cravings and preventing relapse. Naltrexone is generally safe and well-tolerated, but it may cause side effects such as nausea, headache, dizziness, and fatigue in some people.

It's important to note that naltrexone should only be used under the supervision of a healthcare provider, and it is not recommended for individuals who are currently taking opioids or who have recently stopped using them, as it can cause withdrawal symptoms. Additionally, naltrexone may interact with other medications, so it's important to inform your healthcare provider of all medications you are taking before starting naltrexone therapy.

Molecular structure, in the context of biochemistry and molecular biology, refers to the arrangement and organization of atoms and chemical bonds within a molecule. It describes the three-dimensional layout of the constituent elements, including their spatial relationships, bond lengths, and angles. Understanding molecular structure is crucial for elucidating the functions and reactivities of biological macromolecules such as proteins, nucleic acids, lipids, and carbohydrates. Various experimental techniques, like X-ray crystallography, nuclear magnetic resonance (NMR) spectroscopy, and cryo-electron microscopy (cryo-EM), are employed to determine molecular structures at atomic resolution, providing valuable insights into their biological roles and potential therapeutic targets.

Patient-controlled analgesia (PCA) is a method of pain management that allows patients to self-administer doses of analgesic medication through a controlled pump system. With PCA, the patient can press a button to deliver a predetermined dose of pain medication, usually an opioid, directly into their intravenous (IV) line.

The dosage and frequency of the medication are set by the healthcare provider based on the patient's individual needs and medical condition. The PCA pump is designed to prevent overinfusion by limiting the amount of medication that can be delivered within a specific time frame.

PCA provides several benefits, including improved pain control, increased patient satisfaction, and reduced sedation compared to traditional methods of opioid administration. It also allows patients to take an active role in managing their pain and provides them with a sense of control during their hospital stay. However, it is essential to monitor patients closely while using PCA to ensure safe and effective use.

Nalorphine is defined as a morphine derivative that antagonizes the effects of opiate agonists, such as morphine and heroin, by competing for binding sites in the central nervous system. It was initially used as an analgesic but has since been replaced by other drugs due to its potential for abuse and adverse psychological effects. Currently, it is primarily used in research and to reverse opioid overdose.

A Structure-Activity Relationship (SAR) in the context of medicinal chemistry and pharmacology refers to the relationship between the chemical structure of a drug or molecule and its biological activity or effect on a target protein, cell, or organism. SAR studies aim to identify patterns and correlations between structural features of a compound and its ability to interact with a specific biological target, leading to a desired therapeutic response or undesired side effects.

By analyzing the SAR, researchers can optimize the chemical structure of lead compounds to enhance their potency, selectivity, safety, and pharmacokinetic properties, ultimately guiding the design and development of novel drugs with improved efficacy and reduced toxicity.

Sprague-Dawley rats are a strain of albino laboratory rats that are widely used in scientific research. They were first developed by researchers H.H. Sprague and R.C. Dawley in the early 20th century, and have since become one of the most commonly used rat strains in biomedical research due to their relatively large size, ease of handling, and consistent genetic background.

Sprague-Dawley rats are outbred, which means that they are genetically diverse and do not suffer from the same limitations as inbred strains, which can have reduced fertility and increased susceptibility to certain diseases. They are also characterized by their docile nature and low levels of aggression, making them easier to handle and study than some other rat strains.

These rats are used in a wide variety of research areas, including toxicology, pharmacology, nutrition, cancer, and behavioral studies. Because they are genetically diverse, Sprague-Dawley rats can be used to model a range of human diseases and conditions, making them an important tool in the development of new drugs and therapies.

Heroin is a highly addictive drug that is processed from morphine, a naturally occurring substance extracted from the seed pod of the Asian opium poppy plant. It is a "downer" or depressant that affects the brain's pleasure systems and interferes with the brain's ability to perceive pain.

Heroin can be injected, smoked, or snorted. It is sold as a white or brownish powder or as a black, sticky substance known as "black tar heroin." Regardless of how it is taken, heroin enters the brain rapidly and is highly addictive.

The use of heroin can lead to serious health problems, including fatal overdose, spontaneous abortion, and infectious diseases like HIV and hepatitis. Long-term use of heroin can lead to physical dependence and addiction, a chronic disease that can be difficult to treat.

Hydromorphone is a potent semi-synthetic opioid analgesic, which is chemically related to morphine but is approximately 8 times more potent. It is used for the relief of moderate to severe pain and is available in various forms such as tablets, extended-release tablets, solutions, and injectable formulations. Common brand names include Dilaudid and Exalgo. Hydromorphone works by binding to opioid receptors in the brain and spinal cord, reducing the perception of pain and decreasing the emotional response to pain. As with other opioids, hydromorphone carries a risk for dependence, addiction, and abuse.

Fentanyl is a potent synthetic opioid analgesic, which is similar to morphine but is 50 to 100 times more potent. It is a schedule II prescription drug, typically used to treat patients with severe pain or to manage pain after surgery. It works by binding to the body's opioid receptors, which are found in the brain, spinal cord, and other areas of the body.

Fentanyl can be administered in several forms, including transdermal patches, lozenges, injectable solutions, and tablets that dissolve in the mouth. Illegally manufactured and distributed fentanyl has also become a major public health concern, as it is often mixed with other drugs such as heroin, cocaine, and counterfeit pills, leading to an increase in overdose deaths.

Like all opioids, fentanyl carries a risk of dependence, addiction, and overdose, especially when used outside of medical supervision or in combination with other central nervous system depressants such as alcohol or benzodiazepines. It is important to use fentanyl only as directed by a healthcare provider and to be aware of the potential risks associated with its use.

Morphinans are a class of organic compounds that share a common skeletal structure, which is based on the morphine molecule. The morphinan structure consists of a tetracyclic ring system made up of three six-membered benzene rings (A, C, and D) fused to a five-membered dihydrofuran ring (B).

Morphinans are important in medicinal chemistry because many opioid analgesics, such as morphine, hydromorphone, oxymorphone, and levorphanol, are derived from or structurally related to morphinans. These compounds exert their pharmacological effects by binding to opioid receptors in the brain and spinal cord, which are involved in pain perception, reward, and addictive behaviors.

It is worth noting that while all opiates (drugs derived from the opium poppy) are morphinans, not all morphinans are opiates. Some synthetic or semi-synthetic morphinans, such as fentanyl and methadone, do not have a natural origin but still share the same basic structure and pharmacological properties.

The periaqueductal gray (PAG) is a region in the midbrain, surrounding the cerebral aqueduct (a narrow channel connecting the third and fourth ventricles within the brain). It is a column of neurons that plays a crucial role in the modulation of pain perception, cardiorespiratory regulation, and defensive behaviors. The PAG is involved in the descending pain modulatory system, where it receives input from various emotional and cognitive areas and sends output to the rostral ventromedial medulla, which in turn regulates nociceptive processing at the spinal cord level. Additionally, the PAG is implicated in the regulation of fear, anxiety, and stress responses, as well as sexual behavior and reward processing.

Oxycodone is a semi-synthetic opioid analgesic, which means it's a painkiller that's synthesized from thebaine, an alkaloid found in the poppy plant. It's a strong pain reliever used to treat moderate to severe pain and is often prescribed for around-the-clock treatment of chronic pain. Oxycodone can be found in various forms, such as immediate-release tablets, extended-release tablets, capsules, and solutions.

Common brand names for oxycodone include OxyContin (extended-release), Percocet (oxycodone + acetaminophen), and Roxicodone (immediate-release). As an opioid, oxycodone works by binding to specific receptors in the brain, spinal cord, and gut, reducing the perception of pain and decreasing the emotional response to pain.

However, it's important to note that oxycodone has a high potential for abuse and addiction due to its euphoric effects. Misuse or prolonged use can lead to physical dependence, tolerance, and withdrawal symptoms upon discontinuation. Therefore, it should be taken exactly as prescribed by a healthcare professional and used with caution.

Pentazocine is a synthetic opioid analgesic, chemically unrelated to other opiates or opioids. It acts as an agonist at the kappa-opioid receptor and as an antagonist at the mu-opioid receptor, which means it can produce pain relief but block the effects of full agonists such as heroin or morphine. Pentazocine is used for the management of moderate to severe pain and is available in oral, intramuscular, and intravenous formulations. Common side effects include dizziness, lightheadedness, sedation, nausea, and vomiting.

Enkephalins are naturally occurring opioid peptides that bind to opiate receptors in the brain and other organs, producing pain-relieving and other effects. They are derived from the precursor protein proenkephalin and consist of two main types: Leu-enkephalin and Met-enkephalin. Enkephalins play a role in pain modulation, stress response, mood regulation, and addictive behaviors. They are also involved in the body's reward system and have been implicated in various physiological processes such as respiration, gastrointestinal motility, and hormone release.

Opioid delta receptors, also known as delta opioid receptors (DORs), are a type of G protein-coupled receptor found in the nervous system and other tissues throughout the body. They belong to the opioid receptor family, which includes mu, delta, and kappa receptors. These receptors play an essential role in pain modulation, reward processing, and addictive behaviors.

Delta opioid receptors are activated by endogenous opioid peptides such as enkephalins and exogenous opioids like synthetic drugs. Once activated, they trigger a series of intracellular signaling events that can lead to inhibition of neuronal excitability, reduced neurotransmitter release, and ultimately, pain relief.

Delta opioid receptors have also been implicated in various physiological processes, including immune function, respiratory regulation, and gastrointestinal motility. However, their clinical use as therapeutic targets has been limited due to the development of tolerance and potential adverse effects such as sedation and respiratory depression.

In summary, delta opioid receptors are a type of opioid receptor that plays an essential role in pain modulation and other physiological processes. They are activated by endogenous and exogenous opioids and trigger intracellular signaling events leading to various effects, including pain relief. However, their clinical use as therapeutic targets is limited due to potential adverse effects.

Nalbuphine is a synthetic opioid analgesic, which means it is a medication used to treat pain. It works by binding to opioid receptors in the brain and spinal cord, reducing the perception of pain. Nalbuphine has both agonist and antagonist properties at different types of opioid receptors. Specifically, it acts as an agonist at kappa opioid receptors and as a partial antagonist at mu opioid receptors.

Nalbuphine is often used to manage moderate to severe pain, either alone or in combination with other medications. It can be administered through various routes, including intravenously, intramuscularly, or subcutaneously. Common side effects of nalbuphine include dizziness, sedation, sweating, and nausea.

It's important to note that opioids like nalbuphine can be habit-forming and should be used with caution under the guidance of a healthcare provider. Misuse or abuse of these medications can lead to serious health consequences, including addiction, overdose, and death.

US 2960505, Weiss U, "Morphine derivative", published 11/15/1960 Weiss U, Daum SJ (January 1965). "Derivatives of Morphine. IV. ... Hydromorphinol (RAM-320, 14-Hydroxydihydromorphine), is an opiate analogue that is a derivative of morphine, where the 14- ... It has similar effects to morphine such as sedation, analgesia and respiratory depression, but is twice as potent as morphine ... which is different at position 6 on the morphine carbon skeleton. Hydromorphinol was developed in Austria in 1932. In the ...
Nuclear-Substituted Morphine Derivatives". The Journal of Organic Chemistry. 03 (3): 204. doi:10.1021/jo01220a003. (CS1 ... McLaughlin JP, Nowak D, Sebastian A, Schultz AG, Archer S, Bidlack JM (December 1995). "Metopon and two unique derivatives: ... US Patent 2178010 Eddy NB (November 1948). "Pharmacology of metopon and other new analgesic opium derivatives". Annals of the ... Metopon (5-methylhydromorphone, CAS number 124-92-5) is an opioid analogue that is a methylated derivative of hydromorphone ...
cite book}}: ,journal= ignored (help) Rinner U, Hudlicky T (2012). "Synthesis of morphine alkaloids and derivatives". Alkaloid ... Morphine Total Syntheses @ Wilson T (2006). "Synthesis of Morphine Alkaloids" (PDF). Professor Scott E. Denmark ... Gates' total synthesis of morphine provided a proof of the structure of morphine proposed by Robinson in 1925. This synthesis ... The first morphine total synthesis, devised by Marshall D. Gates, Jr. in 1952 remains a widely used example of total synthesis ...
Morphine and codeine are opium derivatives." Opioids have led to many deaths in the United States, particularly by causing ... A popular derivative, crack cocaine is typically smoked. When transformed into its freebase form, crack, the cocaine vapour may ... LSD: A popular ergoline derivative, that was first synthesized in 1938 by Albert Hofmann. However, he failed to notice its ... For instance, in the music industry, the musical genres hip hop, hardcore rap, and trap, alongside their derivative subgenres ...
Okun R, Elliott HW (November 1958). "Acute pharmacological studies of some new morphine derivatives". The Journal of ... 6-Methylenedihydrodesoxymorphine is a potent μ-opioid agonist, 80x stronger than morphine. Compared to morphine it has a faster ... It produces around the same degree of respiratory depression as morphine, but less inhibition of gastrointestinal motility. ... 6-Methylenedihydrodesoxymorphine (6-MDDM) is an opiate analogue structurally related to desomorphine that is a derivative of ...
It is a derivative of morphine. Myrophine is substituted with a 3-benzyl group and a 6-myristyl chain. It is metabolised to ... and so is a long-acting prodrug for morphine, but with a slow onset of effects. It is weaker than morphine as an analgesic but ... In addiction studies conducted in human subjects in the 1950s, myrophine did not substitute for morphine in withdrawal, did not ... Eddy NB, Halbach H, Braenden OJ (1957). "Synthetic substances with morphine-like effect: clinical experience; potency, side- ...
"Evidence for topographical analogy between methionine-enkephalin and morphine derivatives". Biochemistry. 16 (9): 1831-8. doi: ... The tyrosine residue at position 1 is thought to be analogous to the 3-hydroxyl group on morphine. Leu-enkephalin has agonistic ...
2-Acylaminopyridine derivatives with morphine agonistic and morphine antagonistic effects]". Arzneimittel-Forschung. 24 (4): ... With about 10% of the analgesic potency of morphine, 50 mg of propiram is equivalent to about 60 mg of codeine or 50 mg of ... US3163654A Pyridine derivatives and their preparation (n-tertiary aminoalkyl-n-acyl)-amino pyridines U.S. Patent 3,163,654 Drug ...
He also experimented on barbiturates and morphine derivatives for mind control purposes. August Hirt - He was responsible for ...
The apo- prefix indicates that it is a morphine derivative. Historically, apomorphine has been tried for a variety of uses, ... The compound is historically a morphine decomposition product made by boiling morphine with concentrated acid, hence the - ... morphine suffix. Contrary to its name however, apomorphine doesn't actually contain morphine or its skeleton, nor does it bind ... Furthermore, morphine-based natural products can be heated in acid to give aporphine degradation products, like the FDA- ...
He also conducted experiments using barbiturates and morphine derivatives for mind-control purposes. He was made ...
... is an opiate analogue that is a derivative of morphine. It was developed in the early 1900s after first ... It is produced in the same fashion as other esters of morphine-treating morphine with an acid anhydride (or some acids or other ... Specifically, the original 1875 synthesis was effected by boiling morphine for 2 hours in benzoic anhydride at 130 °C, as was ... It is described as being virtually identical to heroin and morphine in its effects, and consequently was itself banned ...
... (Morphine methobromide, Morphine bromomethylate, Morphosan) a derivative of morphine. It is an opioid ... It is a quaternary ammonium salt formed by reaction of morphine with methyl bromide and a controlled substance. 21 CFR 1308.11 ...
... of which morphine-N-oxide-derivatives, like codeine-N-oxide; The isomers and stereoisomers of tetrahydrocannabinol; The ethers ... morpheridine morphine morphine-methobromide morphine-N-oxide myrophine nicocodeine nicodicodine nicomorphine noracymethadol ... and morpholine derivatives of lysergic acid, and the thereby introduction of methyl-, acetyl- or halogen groups obtained ... zipeprol The esters and derivatives of ecgonine, which can be turned into ecgonine and cocaine; The mono- and di-alkylamide-, ...
... centrally acting morphine derivative and has important analgesic properties. Houdi AA, Kottayil S, Crooks PA, Butterfield DA ( ... centrally acting morphine derivative". Pharmacology, Biochemistry, and Behavior. 53 (3): 665-71. doi:10.1016/0091-3057(95)02067 ... the other two being morphine and more active 6-monoacetylmorphine (6-MAM). Because of the acetyl-group in 3-position, 3-MAM has ...
Earlier treaties had only controlled opium, coca, and derivatives such as morphine, heroin, and cocaine. The Single Convention ... The Single Convention allows only drugs with morphine-like, cocaine-like, and cannabis-like effects to be added to the ... Consequently, in countries where underprescription is chronic due to the high prices of morphine and lack of availability and ... The council, who support licensing poppy cultivation in Afghanistan to create Afghan morphine, believe the opium supply in this ...
Armstrong, S. C.; Cozza, K. L. (2003). "Pharmacokinetic Drug Interactions of Morphine, Codeine, and Their Derivatives: Theory ... Morphine-6-glucuronide Srinivasan, V.; Wielbo, D.; Tebbett, I. R. (1997). "Analgesic effects of codeine-6-glucuronide after ... not morphine". International Journal of Clinical Practice. 54 (6): 395-398. PMID 11092114. ...
"Morphine derivative", US3254088 "Joint Nuclear Accident Co-ordinating Center: Record of Events" (PDF). United States Department ...
Eddy NB, Howes HA (1935). "Studies of Morphine, Codeine and their Derivatives X. Desoxymorphine-C, Desoxycodeine-C and their ... Dose for dose it is eight to ten times more potent than morphine. Desomorphine is a morphine analogue where the 6-hydroxyl ... "Morphine Derivative and Processes", published 1934-19-07, issued 1934-13-11 "Krokodil". New York State Office of Alcoholism and ... Early medical trials of humans taking desomorphine have resulted in the finding that as with morphine and most other analgesics ...
The amine is often an alkaloid, such as nicotine, cocaine, morphine, and ephedrine, or derivatives thereof. Freebasing is a ...
... and 3-acetyl derivatives are less potent than the corresponding derivatives of etorphine at 11,000 and 1300 times morphine, ... This molecule is biosynthetically related to the morphinane derivatives metabolism, where thebaine and morphine are implicated ... potency of morphine) and acetylation of the 3-hydroxy group of etorphine resulting in acetorphine (8700× morphine)-although ... Other notable derivatives then result from further modification of this template, with saturation of the 7,8-double bond of ...
... a 14-beta-aminomorphinone derivative, compared to fentanyl and morphine". Anesthesia and Analgesia. 69 (4): 450-6. doi:10.1213/ ... Pentamorphone (14β-pentylaminomorphinone, RX-77989) is a semi-synthetic opiate derivative related to compounds such as ...
Brugos B, Arya V, Hochhaus G (2004). "Stabilized dynorphin derivatives for modulating antinociceptive activity in morphine ... Han and Xie found dynorphin to be 6-10 times more potent than morphine on a per mole basis. In addition, morphine tolerance did ... Ren MF, Lu CH, Han JS (1985). "Dynorphin-A-(1-13) antagonizes morphine analgesia in the brain and potentiates morphine ... Dynorphin derivatives are generally considered to be of little clinical use because of their very short duration of action. Day ...
US 2062324, "Method of Extraction of Morphine and Related Derivatives" U. Zerell, B. Ahrens and P. Gerz (2005). "Documentation ... Calcium morphenate is a calcium salt of morphine which is produced by using calcium bases to raise the pH of an aqueous ... This was a method used in pharmaceutical manufacturing to separate morphine from other alkaloids and inert materials from the ... Treatment with a weak acid such as ammonium chloride then causes morphine freebase to precipitate, leaving codeine and other ...
Based on this information and examinations of victims, doctors suggested that the compound might be a morphine derivative. The ... He said that the gas was a fentanyl derivative, an extremely powerful opioid. Boris Grebenyuk, the All-Russia Disaster Relief ... If fentanyl or a fentanyl derivative was used, the hostage liberators had only minutes to inject naloxone into the hostages ... Some of the later publications in medical journals assumed that Russian special forces used aerosol of a fentanyl derivative, ...
... producing strong derivatives of morphine and codeine. Many morphine derivatives can also be manufactured using thebaine or ... also known as morphine diacetate, diamorphine, or diacetyl morphine) is an ester of morphine and a morphine prodrug, ... Morphine and its major metabolites, morphine-3-glucuronide and morphine-6-glucuronide, can be detected in blood, plasma, hair, ... Morphine is metabolized primarily into morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) via glucuronidation by ...
A Short History of the Discovery and Development of Naltrexone and Other Morphine Derivatives. Chapter 6 in Natural Products in ...
Because of this, he became addicted to morphine and heroin (a synthetic derivative of morphine, but much more potent). Sigmund ... Devastated by pain, addiction, and disease, he relapsed and began using morphine again. Ernst von Fleischl-Marxow died on ... but also as a treatment for morphine addicts. He recommended this to his friend Fleischl-Marxow, who proceeded to fall even ...
Black tar as a type holds a variable admixture morphine derivatives-predominantly 6-MAM (6-monoacetylmorphine) which is another ... Morphine, one of many alkaloids in opium, is then extracted out of the opium by acid-base extraction and turned into heroin by ... Some drugs, like cocaine and morphine, are extracted from plant sources and refined with the aid of chemicals. Semi-synthetic ...
The apo- prefix relates to it being a morphine derivative ("[comes] from morphine"). Historically, apomorphine has been tried ... In the US, the Harrison Narcotics Tax Act made working with any morphine derivatives extremely hard, despite apomorphine itself ... Several techniques exist for the creation of apomorphine from morphine. In the past, morphine had been combined with ... The compound is historically a morphine decomposition product made by boiling morphine with concentrated acid, hence the - ...
US 2960505, Weiss U, "Morphine derivative", published 11/15/1960 Weiss U, Daum SJ (January 1965). "Derivatives of Morphine. IV. ... Hydromorphinol (RAM-320, 14-Hydroxydihydromorphine), is an opiate analogue that is a derivative of morphine, where the 14- ... It has similar effects to morphine such as sedation, analgesia and respiratory depression, but is twice as potent as morphine ... which is different at position 6 on the morphine carbon skeleton. Hydromorphinol was developed in Austria in 1932. In the ...
Fluorescently Labeled Morphine Derivatives for Bioimaging Studies. Journal of medicinal chemistry. (In Press.) ...
Some street drugs, notably morphine derivatives, are analogous. Both sexes are affected, but males are more incapacitated than ... all of which is not too far removed from the way in which opium and its derivatives activate the brain by competing with the ...
Categories: Morphine Derivatives Image Types: Photo, Illustrations, Video, Color, Black&White, PublicDomain, ...
Morphine sulfate (Astramorph, Duramorph, MS Contin, Avinza, Depodur, Infumorph, Kadian, MorphaBond, Arymo ER). *View full drug ... A synthetic opioid that is 75-200 times more potent and much shorter half-life than morphine sulfate. Has less hypotensive ... For chronic severe pain unremitting to alternative therapy, oral immediate-release and extended-release morphine sulfate may be ... effects and is safer in patients with hyperactive airway disease than morphine because of minimal-to-no associated histamine ...
... a semisynthetic morphine derivative 3,4 Dextromethorphan undergoes metabolic O-demethylation to its active metabolite ...
... and its derivatives, morphine and heroin -- adequate to supply Europe and the United States for up to three years. ...
A good example of a derivative is that codeine (methylmorphine) is a derivative of morphine. The second article was in Time ... Kadian was referred to a a morphine derivative in the article. The active medication is morphine, and is encapsulated in a ... Morphine, also given to Jackson and many others in the Civil War, is still the Armys most commonly used painkilling drug. It ... Is it really necessary to compare morphine and demonize and stigmatize it more? It is a powerful medication for sure, but one ...
As a derivative of morphine, dilaudid is an opioid class drug. Dilaudid is about three to four times more powerful at relieving ... Withdrawal symptoms are similar to those experienced by people withdrawing from morphine, only much more intense. ... pain than morphine. It works by binding to opioid receptors found in the brain which prevents the body from experiencing pain. ...
As for what Vicodin is classified as, this is a drug that is based on morphine, a derivative of opium. The history of ... The iconic name that was given to the morphine derivative is impressive in its own way. According to one article on the subject ... He stumbled across a far more potent, acetylated form of morphine, now called "diacetylmorphine" or morphine diacetate, which ... Marys Hospital Medical School at the time, and he had been trying to synthesize stronger forms of morphine. ...
Safe storage of medicines that are only active as morphine and its derivatives, the cotnpound times stronger 6. Number of the ... In its simplest form, the a-hydroxyethyl derivative. Expected to reach the person would be decreased pro- duction line. ...
Morphine Derivatives (TLC) urine Rs.1450 MTB by PCR Qualitative Rs.4840 ...
Offers a list prescription drugs commonly abused, including depressants, opioids and morphine derivatives, and stimulants, and ... Describes how opiates, such as Vicodin, morphine, heroin, and codeine, affect the brain, the nervous system, and the limbic ...
HPCE analysis of hydrolysing morphine derivatives. Quantitation of decomposition rate and mobility  ...
Do not give morphine, morphine derivatives, or Demerol.. *Use ice packs or cold compresses to relieve the pain and slow the ...
In conclusion, we show that endogenous M6G can be found at higher levels than morphine in the blood of morphine-naive patients ... morphine-6-glucuronide [M6G]; morphine-3-glucuronide [M3G]) are formed by mammalian cells from dopamine. Changes in the ... Then, a M6G-specific ELISA-assay was tested to quantify M6G in the plasma of healthy donors, morphine-treated, and critically ... While endogenous morphine levels are detectable using enzyme-linked immunosorbant assay (ELISA), mass spectrometry (MS) ...
Morphine and its derivative "heroin" are opiates. Opioids are man-made narcotic analgesics. Some or everything of the chemicals ...
Heroin is a semisynthetic derivative of morphine. Mandrax is a trade name for methaqualone, a pharmaceutical depressant. ... small-scale illicit producer of opium and coca for the processing of opiates and coca derivatives; however, large quantities of ... Narcotics are drugs that relieve pain, often induce sleep, and refer to opium, opium derivatives, and synthetic substitutes. ... significant transit area for Afghan drugs, including heroin, opium, morphine, and hashish, bound for Iran, Western markets, the ...
Heroin is a semisynthetic derivative of morphine. Mandrax is a trade name for methaqualone, a pharmaceutical depressant. ... Related to heroin and common prescription opioids such as morphine. Overdose deaths among ages 15-19 have risen 23 between 2024 ...
... models were used to screen morphine derivatives binding to MRGPRX2. Furthermore, most morphine derivatives significantly ... Morphine derivatives are clinically important anesthetic and sedative drugs, which often show anaphylactic side effects. Mas- ...
member has not used morphine derivatives since documented date of morphine allergy. ... The accumulated high dose threshold is 120 mg of morphine or morphine equivalent (MME) per day for an individual agent, and 180 ... The accumulated high dose threshold is 120 mg of morphine or morphine milligram equivalent (MME) per day for an individual ... adverse reaction or contraindication to morphine sulfate extended-release that cannot be expected or managed as a part of ...
It is one of two derivatives of morphine, the other being oxycodone. (4,5-epoxy-3-hydroxy-17-methylmorphinan-6-one). http://www ... Morphine. Morphine is an opiate used in the treatment of severe pain. It occurs naturally in the opium poppy and has a long ... desomorphine is an an opiate analogue invented in 1932 in the United States that is a derivative of morphine. http://en. ... This latex contains a variety of opiates including codeine and morphine. It has a long history of use in Asia and Europe. ( ...
It is one of two derivatives of morphine, the other being oxycodone. (4,5-epoxy-3-hydroxy-17-methylmorphinan-6-one). http://www ... Morphine. Morphine is an opiate used in the treatment of severe pain. It occurs naturally in the opium poppy and has a long ... desomorphine is an an opiate analogue invented in 1932 in the United States that is a derivative of morphine. http://en. ... This latex contains a variety of opiates including codeine and morphine. It has a long history of use in Asia and Europe. ( ...
Endorphins are structurally identical to opium and its derivatives (morphine, codeine, heroin, etc.). Activities that release ...
... data from double blind studies bcz there have never been double blind studies conducted on morphine and its derivatives, "... ... it came back positive for opioids and morphine, a substance that naturally occurs in poppy seeds, which I ate on two " ... Poppy seeds have enough codeine and morphine that naturally are in them that it triggered this false positive. I am just ...
On the right side, next to the hands image, do you see "Opioids and Morphine Derivatives?" Is this a list? If so, use bullet ...
The drug is a pain medicine based on a morphine derivative that Purdue stated was non- addictive. In the 90s it was first ...
  • He stumbled across a far more potent, acetylated form of morphine, now called " diacetylmorphine " or morphine diacetate, which is the chemical name for heroin. (
  • Morphine and its derivative "heroin" are opiates. (
  • Heroin is a semisynthetic derivative of morphine. (
  • Related to heroin and common prescription opioids such as morphine. (
  • Opium derivatives (e.g. opiates such as morphine and heroin) and opioids (e.g. fentanyl) were not considered by the Working Group. (
  • Offers a list prescription drugs commonly abused, including depressants, opioids and morphine derivatives, and stimulants, and provides their common and street names, how they are generally administered, and their potential health effects. (
  • This is particularly true for highly potent synthetic opioids like fentanyl and its derivatives (shown in Figure 2). (
  • Many synthetic opioids are derivatives of fentanyl and are significantly more potent than morphine. (
  • Fentanyl is a synthetic opioid analgesic that is a full μ -opioid receptor agonist (one of the three opioid receptors through which opioids exert their pharmacologic actions) and has 100 times the potency of morphine ( 2 ). (
  • it is the D-isomer of levorphanol, a semisynthetic morphine derivative 3,4 Dextromethorphan undergoes metabolic O-demethylation to its active metabolite dextrorphan, which has similar activities to phencyclidine. (
  • Fentanyl is approximately 100-fold more potent than morphine and boasts an LD50 of 0.03 mg/kg in monkeys [5]. (
  • It has similar effects to morphine such as sedation, analgesia and respiratory depression, but is twice as potent as morphine and has a steeper dose-response curve and longer half-life. (
  • A synthetic opioid that is 75-200 times more potent and much shorter half-life than morphine sulfate. (
  • Narcotics are drugs that relieve pain, often induce sleep, and refer to opium, opium derivatives, and synthetic substitutes. (
  • Originally, it referred to drugs that caused narcosis (insensibility or stupor), particularly opioid drugs (eg, opium, opium derivatives). (
  • For chronic severe pain unremitting to alternative therapy, oral immediate-release and extended-release morphine sulfate may be warranted. (
  • Arymo ER is a morphine sulfate abuse-deterrent derivative. (
  • The specificity of this antibody was assessed against 30 morphine-related compounds. (
  • Kadian was referred to a a 'morphine derivative' in the article. (
  • He was working at St. Mary's Hospital Medical School at the time, and he had been trying to synthesize stronger forms of morphine. (
  • Safe storage of medicines that are only active as morphine and its derivatives, the cotnpound times stronger 6. (
  • The active medication is morphine, and is encapsulated in a different type of delivery system. (
  • The TUR went fine, and my doctor was very pleased (although the catheter was extremely uncomfortable, my muscles never accustomed themselves to its presence, and no medication helped - even, after the first use, a morphine derivative). (
  • Some street drugs, notably morphine derivatives, are analogous. (
  • Morphine, also given to Jackson and many others in the Civil War, is still the Army's most commonly used painkilling drug. (
  • For this reason, morphine-3-β-glucuronide (M3G), an active metabolite of morphine, was studied to provide quantitative data on disposition. (
  • As for what Vicodin is classified as, this is a drug that is based on morphine, a derivative of opium. (
  • Plant, the Production of, Internation- cocaine and the derivatives of these sub- al and Wholesale Trade in, and Use of the substances of concern while en- stances. (
  • Has less hypotensive effects and is safer in patients with hyperactive airway disease than morphine because of minimal-to-no associated histamine release. (
  • Withdrawal symptoms are similar to those experienced by people withdrawing from morphine, only much more intense. (
  • As in the adult, M3G was the primary metabolite and accounted for approximately 30% of the clearance of morphine from the fetus. (
  • Opium and its derivatives, such as laudanum, codeine, morphine, and heroin, have been used throughout our modern history and between the 16th and 19th centuries to treat pain, cough, and diarrhea. (
  • Heroin was first produced in 1874 by an English researcher C.R. Wright, who synthesized diacetylmorphine commonly known as Heroin by boiling morphine and acetic anhydride together for many hours. (
  • Like morphine, however, patients using heroin to relieve symptoms often developed a tolerance to the drug and became addicted. (
  • Morphine and its derivative "heroin" are opiates. (
  • Heroin is a semisynthetic derivative of morphine. (
  • Opium and its derivatives - particularly morphine and heroin - are the most dangerous of the habit-forming narcotic drugs"13. (
  • These derivatives, morphine and heroin, make up the chief danger in the West14. (
  • The most dangerously addicting of all the habit-forming drugs is heroin, which is derived from morphine. (
  • In 1898, heroin was invented and imported into the U.S. The drug company Bayer developed heroin as an alternative to morphine, marketing it as a less addictive painkiller. (
  • Morphine, codeine and heroin can all be made with poppy plant derivatives. (
  • Derivatives of laudanum include paregoric (a drug to treat diarrhea), morphine and heroin. (
  • Opioid usage in the U.S. first began in the late 19th Century when heroin, and its derivatives morphine, first became readily available. (
  • When patients come to the Coleman Institute for Addiction Medicine to detox off various addictive substances such as heroin, fentanyl, Percocet®, Dilaudid®, Roxicet®, or any other derivatives of morphine, they aren't feeling their best. (
  • The following article is about an opioid derivative known as codeine phosphate. (
  • Codeine phosphate UK is a morphine or opium derivative. (
  • Codeine phosphate brings its effects by acting as a selective agonist to the opioid receptors in the brain although the rate of affinity for the mu-receptor is much less as compared to the more potent morphine drug. (
  • NSAIDs, including ibuprofen and ketorolac, can be used to treat mild to moderate pain, while narcotic medications, such as morphine sulfate and oxycodone, are useful against moderate to severe pain. (
  • In the U.S., one of the oldest narcotic painkillers or opioid derivatives ever used was morphine. (
  • Our objective was to investigate whether the UGT2B7 H268Y and UGT1A1*28 polymorphisms contribute to the variability in morphine glucuronide-to-morphine plasma ratios among cancer patients undergoing analgesic therapy with morphine. (
  • Braenden, Eddy & Halbach (1955), summarizing the relationship between chemical structure and analgesic action, said "In morphine and its derivatives the methyl substituent on nitrogen seems essential because its substitution by other alkyl groups reduces or abolishes analgesic action. (
  • It is well known, of course, that substituting alkyl for methyl on the nitrogen of morphine results in a compound (nalorphine) which is antagonistic to most morphine-like effects and which retains little analgesic action as measured by various techniques in animals. (
  • Recently Winter, Orahovats & Lehman (1957) reported on analgesic activity and morphine antagonism in a large series of N-substituted derivatives of morphine. (
  • Also N-phenacyl-, N-phenoxyethyl-, and N-benzylnormorphine had less than one-tenth the analgesic potency of morphine and N-cyclohexylethylnormorphine was one-third as effective. (
  • In striking contrast they reported that N-phenethylnor-morphine was six times more effective than morphine as an analgesic in rats. (
  • Levorphanol [(-) 3-hydroxy-N-methylmorphinan], representing an incomplete synthesis of morphine, is morphine-like in its action with a greater analgesic potency. (
  • A Dupont Merck group led by Cheng resynthesized this racemic mixture along with the N-cyclopropyl methyl derivative and evaluated them for opioid receptor binding along with their analgesic properties in mice. (
  • A longstanding method of treatment for both short term and chronic pain management has been the use of opioid analgesics such as morphine and it's derivatives both natural and synthetic. (
  • Seventy patients with normal hepatic and renal function using slow-release morphine to relieve cancer pain were included. (
  • In Capital, volume 1 , he discusses opium use in Europe, where the drug and its derivatives morphine and laudanum were legal pharmaceuticals. (
  • If allyl is substituted for methyl on the nitrogen of levorphanol, the resulting compound, levallorphan, is also a morphine antagonist which dose-wise is more effective than nalorphine. (
  • Cocaine and its derivatives: Absent. (
  • For chronic severe pain unremitting to alternative therapy, oral immediate-release and extended-release morphine sulfate may be warranted. (
  • Hydromorphone and oxymorphone, close synthetic derivatives of morphine, are also metabolized primarily by UGT enzymes. (
  • Morphine, a powerful opium derivative first synthesized in the early 19th century, comes in the form of a bitter-tasting pill or solution. (
  • Studies in rats have indicated that UGT1A1 may also contribute to the formation of morphine 3-glucuronide (M3G). (
  • Morphine is still used today in clinical settings for pain management. (
  • Studies indicate that opium and morphine addiction during the Reconstruction era in the Southern states was the highest in the world. (
  • The proximity of the sources of opium and its derivatives and of other opiate drugs, that is drugs which irregardless of origin, show morphine-like properties, has really increased the facility to acquire clandestinely these internationally guarded narcotics. (
  • In many LMICs, there is limited availability of oral morphine and too few staff trained in palliative care. (
  • UDP-glucuronosyltransferase (UGT) 2B7 is the major UGT isoform responsible for the 3- and 6-glucuronidation of morphine in humans. (