Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.Opioid-Related Disorders: Disorders related or resulting from abuse or mis-use of opioids.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Opiate Substitution Treatment: Medical treatment for opioid dependence using a substitute opiate such as METHADONE or BUPRENORPHINE.Narcotics: 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.Analgesics, Opioid: Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.Administration, Sublingual: Administration of a soluble dosage form by placement under the tongue.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3)Morphinans: 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.Heroin Dependence: Strong dependence, both physiological and emotional, upon heroin.Neonatal Abstinence Syndrome: Fetal and neonatal addiction and withdrawal as a result of the mother's dependence on drugs during pregnancy. Withdrawal or abstinence symptoms develop shortly after birth. Symptoms exhibited are loud, high-pitched crying, sweating, yawning and gastrointestinal disturbances.Methadyl Acetate: A narcotic analgesic with a long onset and duration of action.Heroin: 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)Naltrexone: 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.Substance Withdrawal Syndrome: 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.Receptors, Opioid: 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.Receptors, Opioid, mu: 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.Opiate Alkaloids: Alkaloids found in OPIUM from PAPAVER that induce analgesic and narcotic effects by action upon OPIOID RECEPTORS.Levorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection.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.Substance Abuse Detection: Detection of drugs that have been abused, overused, or misused, including legal and illegal drugs. Urine screening is the usual method of detection.ThiazinesPrescription Drug Diversion: The transfer of prescription drugs from legal to illegal distribution and marketing networks.Prescription Drug Misuse: Improper use of drugs or medications outside the intended purpose, scope, or guidelines for use. This is in contrast to MEDICATION ADHERENCE, and distinguished from DRUG ABUSE, which is a deliberate or willful action.Nalbuphine: 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.Analgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.Substance Abuse Treatment Centers: Health facilities providing therapy and/or rehabilitation for substance-dependent individuals. Methadone distribution centers are included.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.Drug and Narcotic Control: Control of drug and narcotic use by international agreement, or by institutional systems for handling prescribed drugs. This includes regulations concerned with the manufacturing, dispensing, approval (DRUG APPROVAL), and marketing of drugs.Street Drugs: Drugs obtained and often manufactured illegally for the subjective effects they are said to produce. They are often distributed in urban areas, but are also available in suburban and rural areas, and tend to be grossly impure and may cause unexpected toxicity.Analgesia: Methods of PAIN relief that may be used with or in place of ANALGESICS.

*  Buprenorphine for Drug Dependence

You take buprenorphine by placing pills under your tongue. How It Works. Buprenorphine is an opioid medicine similar to ... In some cases, buprenorphine may be used as an alternative to methadone, which also is given to treat opioid addiction. ... Buprenorphine may have less severe side effects than methadone. Talk to your doctor about what might work best for you. ... Buprenorphine can help treat addiction to opioid drugs, including heroin and narcotic painkillers. It prevents or reduces ...

*  Transtec patches (buprenorphine)

Buprenorphine is a strong painkiller related to morphine. ... Buprenorphine is in the same class of medicines as some of the ... Transtec patches contain the active ingredient buprenorphine, which is a type of medicine called an opioid analgesic ( ... Transtec patches (buprenorphine). Transtec patches contain the active ingredient buprenorphine, which is a type of medicine ... Subutex, Gabup, Prefibin and unbranded buprenorphine sublingual tablets also contain buprenorphine, but these are used to treat ...

*  FDA approves first buprenorphine implant for treatment of opioid dependence

Probuphine is designed to provide a constant, low-level dose of buprenorphine for six months in patients who are already stable ... the first buprenorphine implant for the maintenance treatment of opioid dependence. ... on low-to-moderate doses of other forms of buprenorphine, as part of a complete treatment program. ... Until today, buprenorphine for the treatment of opioid dependence was only approved as a pill or a film placed under the tongue ...

*  Buprenorphine and naloxone Uses, Side Effects & Warnings - Drugs.com

... includes buprenorphine and naloxone description, dosage and directions. ... buprenorphine and naloxone. Generic Name: buprenorphine and naloxone (BUE pre NOR feen and nal OX one). Brand Name: Bunavail, ... Buprenorphine and naloxone dosing information. Usual Adult Dose for Opiate Dependence:. Buprenorphine monotherapy is generally ... Buprenorphine and naloxone is not for use as a pain medication.. Buprenorphine and naloxone may also be used for purposes not ...

*  Buprenorphine and Integrated HIV Care Evaluation - Full Text View - ClinicalTrials.gov

Buprenorphine and Integrated HIV Care Evaluation. The recruitment status of this study is unknown. The completion date has ... Drug: Buprenorphine Behavioral: Integrated HIV care and office-based opioid dependence treatment Phase 4 ... Buprenorphine. Narcotics. Central Nervous System Depressants. Physiological Effects of Drugs. Analgesics. Sensory System Agents ... The Drug Addiction Treatment Act of 2000 and the approval of buprenorphine for the office-based treatment of opioid addiction ...

*  Buprenorphine Suite of Blending Products | National Institute on Drug Abuse (NIDA)

To address this problem, the Buprenorphine Treatment Blending Team (also referred to as: "Buprenorphine Awareness Team") ... Buprenorphine Treatment for Young Adults. Highlights the findings of the NIDA CTN study that compared longer term versus short- ... Buprenorphine Treatment: Training for Multidisciplinary Addiction Professionals. Opioid abuse and addiction (e.g., heroin, ... Primary results indicated that young adults in the longer term buprenorphine treatment were less likely to inject drugs or ...

*  Buprenorphine Maintenance vs. Detoxification in Prescription Opioid Dependence - Full Text View - ClinicalTrials.gov

In Mtn, buprenorphine/naloxone will continue unchanged for the remainder of the study. In Dtx, the dosage of buprenorphine/ ... Buprenorphine. Buprenorphine, Naloxone Drug Combination. Naloxone. Analgesics, Opioid. Narcotics. Central Nervous System ... Behavioral: Behavioral: Buprenorphine/naloxone maintenance (Mtn) Behavioral: Behavioral: Buprenorphine/naloxone detoxification ... The aim of the study is to determine whether buprenorphine/naloxone maintenance versus detoxification using buprenorphine/ ...

*  We Speak Methadone (and buprenorphine) • Login

We Speak Methadone (and buprenorphine). A NAMA Recovery Forum for Medication Assisted Treatment patients, family and advocates ...

*  Buprenorphine / Naloxone - Suboxone Addiction Treatment | Addict Help

Buprenorphine can be used as a patch or implant to treat pain or addiction it is part of Suboxone as buprenorphine / naloxone ... Is Treatment with Buprenorphine for an Opioid Addiction Always Successful?. Approved by the FDA in 2002, buprenorphine is now ... Buprenorphine For Pain Relief. For individuals that are not opioid tolerant, buprenorphine, in low dosages, works well for ... Side Effects of Buprenorphine. People taking buprenorphine or Suboxone may experience side effects similar to opioids side ...

*  We Speak Methadone (and buprenorphine) • Index page

Buprenorphine (Suboxone, Subutex, Zubsolv and Bunavail) Buprenorphine and Buprenorphine/Naloxone - specific discussions, topics ... We Speak Methadone (and Buprenorphine) Message Boards. Medication Assisted Treatment Main Forum Information on treatment and ... We Speak Methadone (and buprenorphine). A NAMA Recovery Forum for Medication Assisted Treatment patients, family and advocates ...

*  Dr. Seth Thompson M.D. in Abingdon, VA 24210 | Buprenorphine Treatment Program

Here at BuprenorphineTreatmentProgram.com, we list over 14,000+ doctors and treatment centers all across the U.S. that specialize in treating patients with Buprenorphine for drug addiction or severe chronic pain.. Buprenorphine (or Bupe) is a prescription drug in Suboxone and Subutex. If you live in Abingdon, Virginia and need help with detoxification and addiction treatment for heroin or other opioid drugs like oxycodone and hydrocodone included in prescription pain pills such as Percocet, OxyContin, Lortab and Vicodin, please contact one of the doctors or treatment facilities on our site.. ...

*  CHMP Positive Opinion for Opioid Dependence Treatment With Zubsolv® (buprenorphine and naloxone) in

CAMBRIDGE, England and UPPSALA, Sweden, Sept. 15, 2017 /PRNewswire/ -- CHMP Positive Opinion for Opioid Dependence Treatment With Zubsolv® (buprenorphine...

*  Buprenorphine/Naloxone Treatment for Opioid Dependence-Experiment II-3 - 6 - Full Text View - ClinicalTrials.gov

Inclusion Criteria:. Individuals must be healthy, non-drug dependent volunteers, be at least 18 years of age, and have no prior history of drug or alcohol abuse or dependence. Subjects must have had some minimal experience with opioids (e.g. at least two prior exposures). Exclusion Criteria:. Individuals with evidence of an active Diagnostic and Statistical Manual of Mental Disorders (DSM-IV) Axis I psychiatric disorder (e.g. psychosis, manic-depressive illness, organic psychiatric disorders), significant medical illness (e.g., liver or cardiovascular disease) or pregnant female subjects are excluded from study participation. ...

*  Treating Chronic Pain in Buprenorphine Patients in Primary Care Settings - Michael Stein

Nearly half a million Americans receive buprenorphine for opioid dependence treatment. Approximately 40% of those seeking treatment with buprenorphine have pain...

*  Plus it

The effects of buprenorphine on behavior reinforced by smoked cocaine base and orally delivered phencyclidine (PCP), ethanol and saccharin were compared. There were six groups of four to five rhesus monkeys. Group 1 contained four monkeys that had been trained to smoke cocaine base under progressive ratio (PR) or fixed ratio (FR) schedules. Up to eight smoke deliveries (2 mg/kg) were available during daily 3-hr sessions. Each delivery was separated by a 15-min timeout. The remaining groups received concurrent access to different combinations of orally delivered liquids as follows: group 2, PCP (0.25 mg/ml) and water; group 3, saccharin (0.03% w/v) and water; group 4, PCP and saccharin; group 5, ethanol (8% w/v) and water; and group 6, ethanol and PCP. Saline or buprenorphine (0.003, 0.012, 0.05, 0.2 and 0.8 mg/kg) injections were given i.m. 30 min before each session for 5 consecutive days. Buprenorphine produced a dose-dependent reduction in behavior ...

*  Trends in Receipt of Buprenorphine and Naltrexone for Opioid Use Disorder Among Adolescents and Young Adults, 2001-2014. |...

Among 20 822 youth diagnosed with OUD (0.2% of the 9.7 million sample), 13 698 (65.8%) were male and 17 119 (82.2%) were non-Hispanic white. Mean (SD) age was 21.0 (2.5) years at the first observed diagnosis. The diagnosis rate of OUD increased nearly 6-fold from 2001 to 2014 (from 0.26 per 100 000 person-years to 1.51 per 100 000 person-years). Overall, 5580 (26.8%) youth were dispensed a medication within 6 months of diagnosis, with 4976 (89.2%) of medication-treated youth receiving buprenorphine and 604 (10.8%) receiving naltrexone. Medication receipt increased more than 10-fold, from 3.0% in 2002 (when buprenorphine was introduced) to 31.8% in 2009, but declined in subsequent years (27.5% in 2014). In multivariable analyses, younger individuals were less likely to receive medications, with adjusted probability for age 13 to 15 years, 1.4% (95% CI, 0.4%-2.3%); 16 to 17 years, 9.7% (95% CI, 8.4%-11.1%); 18 to 20 years, 22.0% (95% CI, 21.0%-23.0%); and 21 to 25 years, 30.5% ...

*  Buprenorphine Injection Information

The buprenorphine injection is a prescription medication used to treat moderate-to-severe pain. This eMedTV article provides some basic drug information on the buprenorphine injection, such as common side effects. A link to more details is also provided.

*  A Bioavailability and Safety Study of Probuphine Versus Sublingual Buprenorphine in Patients With Opioid Dependence - Full Text...

Presence of aspartate aminotransferase (AST) levels greater than or equal to 3 X upper limit of normal and/or alanine aminotransferase (ALT) levels greater than or equal to 3 X upper limit of normal and/or total bilirubin greater than or equal to 1.5 X upper limit of normal and/or creatinine greater than or equal to 1.5 X upper limit of ...

*  A Phase 3 Study to Evaluate the Safety, Tolerability, and Efficacy of Naltrexone for Use in Conjunction With Buprenorphine in...

This study will evaluate the safety, effectiveness and tolerance of low doses of oral naltrexone along with buprenorphine to treat opioid use disorder prior to

*  A Better Today First Treatment Center to Offer Buprenorphine Implant to Clients

Scottsdale, AZ (PRWEB) November 08, 2016 -- In a groundbreaking treatment expansion, the FDA-approved Probuphine (Buprenorphine) implants have been

*  Suboxone & Weightlifting | LIVESTRONG.COM

Suboxone is an oral medication used to treat opiate addiction. It consists of a combination of buprenorphine and naloxone. Buprenorphine is a half opiate...

*  A Phase 1, Multiple-dose, Parallel Group Study to Evaluate the Safety and Pharmacodynamic Effects of RDC-0313-buprenorphine ...

The purpose of this study is to assess the safety and tolerability of ALKS33-BUP when administered to opioid-experienced cocaine abusers.

Agonist–antagonistUniform State Narcotic Drug Act: The National Conference of Commissioners on Uniform State Laws developed the Uniform State Narcotic Drug Act in 1934 due to the lack of restrictions in the Harrison Act of 1914. The act was a revenue-producing act and, while it provided penalties for violations, it did not give authority to the states to exercise police power regarding either seizure of drugs used in illicit trade or punishment of those responsible.Opioid: Opioids are substances that act on the nervous system in a similar way to opiates such as morphine and codeine. In a medical context the term usually indicates medications that are artificially made rather than extracted from opium.Hydrophile: A hydrophile is a molecule or other molecular entity that is attracted to, and tends to be dissolved by, water.Liddell, H.Methadone clinic: A methadone clinic is a clinic which has been established for the dispensing of methadone (Dolophine), a schedule II opioid analgesic, to those who abuse heroin and other opioids. The focus of these clinics is the elimination or reduction of opioid usage by putting the patient on methadone.Cyclorphan: Cyclorphan is an opioid compound that is a δ-opioid receptor agonist, a κ-opioid receptor agonist, and a μ-opioid receptor antagonist. Chemically, it is a morphinan and is related to levorphanol.Comfort Food (novel): Comfort Food: A Novel by Noah Ashenhurst contains a cast of characters: a romantic academic, a self-assured young writer, an enigmatic musician, a slacker, a wealthy mountaineer, and a former heroin addict—characters whose lives intersect in the unique, award-winning debut novel.Neonatal withdrawalNoracymethadolLow-dose naltrexone: Low-dose naltrexone (LDN) describes the off-label use of the medication naltrexone at low doses for diseases such as multiple sclerosis. Naltrexone is typically prescribed for opioid dependence or alcohol dependence, as it is a strong opioid antagonist.Benzodiazepine withdrawal syndromeOpioid receptor: Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin.SC-17599Morphia (disambiguation): Morphia, also called morphine, is a highly potent opiate analgesic drug.Drug test: A drug test is a technical analysis of a biological specimen, for example urine, hair, blood, breath, sweat, or oral fluid/saliva—to determine the presence or absence of specified parent drugs or their metabolites. Major applications of drug testing include detection of the presence of performance enhancing steroids in sport, employers screening for drugs prohibited by law (such as cannabis, cocaine and heroin) and police officers testing for the presence and concentration of alcohol (ethanol) in the blood commonly referred to as BAC (blood alcohol content).Azure ADrug diversion: Drug diversion is a medical and legal concept involving the transfer of any legally prescribed controlled substance from the individual for whom it was prescribed to another person for any illicit use. Safe Healthcare Blogs CDC|url = http://blogs.Polysubstance dependence: A person with polysubstance dependence is psychologically addicted to being in an intoxicated state without a preference for one particular substance. Although any combination of three drugs can be used, studies have shown that alcohol is commonly used with another substance.NalbuphineCompound analgesic: Compound analgesics are those with multiple active ingredients; they include many of the stronger prescription analgesics.Shanghai Drug Abuse Treatment Centre: The Shanghai Drug Abuse Treatment Centre, or SDATC (), is a governmental organization providing drug abuse treatment and rehabilitation services in Shanghai, China. SDATC is the only government-supported centre in Shanghai and was established in 1997 on the approval of Shanghai Narcotic Control Commission and Shanghai Public Health Bureau.Concentration effect: In the study of inhaled anesthetics, the concentration effect is the increase in the rate that the Fa(alveolar concentration)/Fi(inspired concentration) ratio rises as the alveolar concentration of that gas is increased. In simple terms, the higher the concentration of gas administered, the faster the alveolar concentration of that gas approaches the inspired concentration.HydromorphoneList of Drug Enforcement Administration operations: The following is a list of major operations undertaken by the United States Drug Enforcement Administration, in reverse chronological order.List of drug interactions: The following is a list of interactions with various prescription and over-the counter drugs:Preventive analgesia: Preventive analgesia is a practice aimed at reducing short- and long-term post-surgery pain. Activity in the body's pain signalling system during surgery produces "sensitization"; that is, it increases the intensity of post-operative pain.

(1/597) Rapid detoxification of heroin dependence by buprenorphine.

AIM: To evaluate the clinical efficacy of buprenorphine (Bup) in treatment of acute heroin withdrawal. METHODS: Bup was given sublingually daily to 60 cases of heroin addicts in 3 groups: low, medium, and high doses. Withdrawal signs and symptoms of heroin were rated by Clinical Institute Narcotic Assessment. Craving for heroin during detoxification was assessed by Visual Analogue Scale. The side effects of Bup was assessed by Treatment Emergent Symptom Scale. RESULTS: The mean daily consumption of Bup in low, medium, and high group was 2.0, 2.9, and 3.6 mg, respectively. Bup not only suppressed objective signs and withdrawal symptoms for heroin withdrawal, but also reduced the duration for heroin detoxification over 7-8 d. CONCLUSION: Bup is an effective and rapid detoxification agent with fewer side effects for treatment of acute heroin withdrawal.  (+info)

(2/597) Nonselective coupling of the human mu-opioid receptor to multiple inhibitory G-protein isoforms.

The human mu-opioid receptor was expressed in Saccharomyces cerevisiae. Binding of [3H]diprenorphine to yeast spheroplasts was specific and saturable (Kd = 1 nm, Bmax = 0.2-1 pmol x mg-1 of membrane proteins). Inhibition of [3H]diprenorphine binding by antagonists and agonists with varying opioid selectivities (mu, delta and kappa) occurred with the same order of potency as in mammalian tissues. Affinities of antagonists were the same with yeast spheroplasts as in reference tissues whereas those of agonists, except etorphine and buprenorphine, were 10-fold to 100-fold lower. Addition of heterotrimeric Gi,o-proteins purified from bovine brain shifted the mu-opioid receptor into a high-affinity state for agonists. Using individually purified Galpha-subunits re-associated with betagamma-dimers, we showed that alphao1, alphao2, alphai1, alphai2 and alphai3 reconstituted high-affinity agonist binding with equal efficiency. This suggests that the structural determinants of the mu-opioid receptor responsible for G-protein coupling are not able to confer a high degree of specificity towards any member of the Gi,o family. The selective effects of opioid observed in specialized tissues upon opioid stimulation may be a result of regulation of G-protein activity by cell-specific factors which should conveniently be analysed using the reconstitution assay described here.  (+info)

(3/597) Assessment of opioid partial agonist activity with a three-choice hydromorphone dose-discrimination procedure.

The discriminative stimulus and subjective effects of opioid mixed agonist-antagonists were assessed in volunteer nondependent heroin users trained in a three-choice drug discrimination procedure to discriminate among the effects of i.m. administration of 2 ml of saline, 1 mg of hydromorphone, and 4 mg of hydromorphone (a morphine-like mu agonist). Other subjective, behavioral, and physiological measures were concurrently collected. The discrimination was readily learned by six of the eight subjects. After training, generalization curves were determined for the following i.m. drug conditions: hydromorphone (0.375-4.0 mg), pentazocine (7.5-60 mg), butorphanol (0.75-6 mg), nalbuphine (3-24 mg), and buprenorphine (0.075-0.6 mg). All five of the test drugs were discriminated significantly or showed trends toward being discriminated as hydromorphone 1 mg-like at one or more dose levels. Hydromorphone showed an inverted U-shaped dose-effect function on the hydromorphone 1 mg-like discrimination. Subjective effect measures produced clearer differentiation among the test drugs than did drug discrimination performance. The present results differ from those of a previous study that observed a close relationship between the results of the discrimination measure and subjective effect measures. The previous study used similar methods and test drugs but different training drugs (e.g., 3 mg of hydromorphone versus 6 mg of butorphanol versus saline). It appears that both the sensitivity of drug discrimination performance to between-drug differences and the relationship between discriminative and subjective effects depends upon the specific discrimination that is trained (e.g., two-choice or three-choice). The present high dose-low dose-saline discrimination procedure appears useful for assessing partial agonist activity. The present data are consistent with partial agonist activity for pentazocine, butorphanol, nalbuphine, and buprenorphine.  (+info)

(4/597) Agonistic effect of buprenorphine in a nociceptin/OFQ receptor-triggered reporter gene assay.

The role of the opioid-like receptor 1 (ORL1) and its endogenous ligand, nociceptin/orphanin FQ (N/OFQ), in nociception, anxiety, and learning remains to be defined. To allow the rapid identification of agonists and antagonists, a reporter gene assay has been established in which the ORL1 receptor is functionally linked to the cyclic AMP-dependent expression of luciferase. N/OFQ and N/OFQ(1-13)NH(2) inhibited the forskolin-induced luciferase gene expression with IC(50) values of 0.81 +/- 0.5 and 0.87 +/- 0.16 nM, respectively. Buprenorphine was identified as a full agonist at the ORL1 receptor with an IC(50) value of 8.4 +/- 2.8 nM. Fentanyl and 7-benzylidenenaltrexone displayed a weak agonistic activity. The ORL1 antagonist [Phe(1)Psi(CH(2)-NH)Gly(2)]N/OFQ((1-13))NH(2) clearly behaved as an agonist in this assay with an IC(50) value of 85 +/- 47 nM. Thus, there is still a need for antagonistic tool compounds that might help to elucidate the neurophysiological role of N/OFQ.  (+info)

(5/597) Determination of buprenorphine and norbuprenorphine in urine and hair by gas chromatography-mass spectrometry.

Buprenorphine, which is used in France as a substitution drug for opioid addiction, is widely abused, and several fatal cases have been reported. In order to confirm a recent intoxication or to establish retrospectively chronic abuse, a simple and reliable gas chromatographic-mass spectrometric method was developed and validated for quantitation of buprenorphine and its active metabolite norbuprenorphine in urine and hair. Two milliliters of urine or 50 mg of pulverized hair was submitted to a pretreatment (enzymatic hydrolysis for urine and decontamination with dichloromethane followed by incubation in 0.1 M HCI for hair). Buprenorphine-d4 was chosen as the internal standard. Selective solid-phase extraction with Bond Elut Certify columns provided recoveries higher than 85% for urine and 43% for hair. By using a mixture of MSTFA/TMSIM/TMCS (100:2:5), buprenorphine and norbuprenorphine produced stable silylated derivatives. The detection was carried out with a quadrupole mass detector working in El selected ion monitoring mode. Ions at m/z 450 and 468 were chosen for the quantitation of buprenorphine and norbuprenorphine, respectively (m/z 454 was used for the internal standard). Limits of quantitation were 0.25 and 0.20 ng/mL, respectively, for buprenorphine and norbuprenorphine in urine and 0.005 ng/mg for the two compounds in hair. Calibration curves were linear from 0 to 50 ng/mL in urine and from 0 to 0.4 ng/mg in hair. Between-day and within-day precisions were less than 8.4% in hair and 6.1% in urine for both molecules in all cases. This method was applied to urine and hair samples collected from patients in a withdrawal treatment program and demonstrated its good applicability in routine analysis and its benefit for clinicians. This technique, which requires instruments already available to many toxicology laboratories, offers an attractive alternative to more sophisticated techniques.  (+info)

(6/597) A retrospective study of buprenorphine and norbuprenorphine in human hair after multiple doses.

The analysis of hair has been proposed as a tool for monitoring drug-treatment compliance. This study was performed to determine if buprenorphine (BPR) and norbuprenorphine (NBPR) could be detected in human hair after controlled administration of drug and to determine if segmental analysis of hair was an accurate record of the dosing history. Subjects with dark hair (six males, six females) received 8 mg sublingual BPR for a maximum of 180 days. Single hair collections were made once after BPR treatment and stored at -20 degrees C until analysis. Hair was aligned scalp-end to tip and then segmented in 3-cm sections. For this study, it was assumed that the mean hair growth rate was 1.0 cm/month. Deuterated internal standard was added to hair segments (2-20 mg of hair) and digested overnight at room temperature with 1 N NaOH. Specimens were extracted with a liquid-liquid procedure and analyzed by liquid chromatography-tandem mass spectrometry. The limits of quantitation for BPR and NBPR were 3 pg/mg and 5 pg/mg, respectively, for 20 mg of hair. BPR and NBPR concentrations were highest for all subjects in hair segments estimated to correspond to the subject's period of drug treatment. With one exception, NBPR was present in higher concentrations in hair than was the parent compound. BPR concentrations in hair segments ranged from 3.1 pg/mg to 123.8 pg/mg. NBPR concentrations ranged from 4.8 pg/mg to 1517.8 pg/mg. In one subject, BPR and NBPR were not detected in any hair segment. In some subjects, BPR and NBPR were detected in hair segments that did not correspond to the period of drug treatment, suggesting that drug movement may have occurred by diffusion in sweat and other mechanisms. The data from this study also indicate that there is a high degree of intersubject variability in measured concentration of BPR and NBPR in hair segments, even when subjects receive the same dose for an equivalent number of treatment days. Future prospective studies involving controlled drug administration will be necessary to evaluate whether hair can serve as an accurate historical record of variations in the pattern of drug use.  (+info)

(7/597) Ring-constrained orvinols as analogs of buprenorphine: differences in opioid activity related to configuration of C(20) hydroxyl group.

The relative positions of the C(20) substituents in buprenorphine, particularly the hydroxyl group, have been implicated in its actions as a partial mu-agonist and a kappa-antagonist. This hypothesis has been examined by the synthesis and pharmacological characterization of five orvinols in which the C(20) carbon atom of buprenorphine is constrained in a five-membered ring, fixing the hydroxyl group above (beta) or below (alpha) the plane of the ring. All five compounds were nonselective in binding assays with similar, low nanomolar affinities. The compounds acted as delta-agonists in the mouse vas deferens and kappa-agonists in the myenteric plexus-longitudinal muscle of the guinea pig ileum and in Chinese hamster ovary (CHO) cells expressing the human kappa-opioid receptor (CHO-hkor). All were lower efficacy mu-agonists than buprenorphine as measured by the [(35)S]guanosine-5'-O-(3-thio)triphosphate assay in SH-SY5Y cells. The major difference between the isomers was an 11- to 12-fold higher potency of the beta-OH isomer (BU46) compared with the alpha-OH isomer (BU47) at the kappa-receptor in the guinea pig ileum and CHO-hkor cells and a somewhat higher efficacy of BU46 in CHO-hkor cells. BU46 and BU47 were evaluated in vivo. BU46 was a full agonist in the mouse writhing assay and antinociception was prevented by norbinaltorphimine, showing a kappa-mechanism of action. In contrast, BU47 acted as an antagonist of mu-, delta-, and kappa-mediated antinociception in the writhing assay. The results show that the configuration of the hydroxyl group is not important in binding affinity at mu-, delta-, or kappa-receptors but does influence kappa-potency and kappa-efficacy, particularly in vivo.  (+info)

(8/597) Opiate drugs and delta-receptor-mediated myocardial protection.

BACKGROUND: Hypothermic myocardial arrest is necessary to complete most cardiac surgery, which limits the success of such operations. Similarly, cold, inhospitable environments limit the survival of warm-blooded animals. Animals have successfully adapted to this challenge through hibernation. Hibernation is an energy-conserving state, now known to be governed by cyclical variation in endogenous opiate compounds. It may also be induced in nonhibernators via hibernating animal serum factors or delta-opiate peptides. Furthermore, hibernation-induction triggers extend organ preservation in many models. This study examined whether opiate drugs with an affinity for the delta-opiate receptor confer similar protection. METHODS AND RESULTS: Isolated hearts harvested from New Zealand White rabbits were treated with either cardioplegia alone or delta-opiate drugs (fentanyl, morphine, buprenorphine, pentazocine) followed by 2 hours of 34 degrees C ischemia. Hearts were then reperfused, and functional and metabolic indices of treated groups were compared with untreated controls. Isovolumic developed pressure, coronary flow, and oxygen consumption were compared as a percent of preischemia versus 45 minutes after reflow. Developed pressure and oxygen consumption were better preserved in the morphine, buprenorphine, and pentazocine groups when compared with cardioplegia alone. CONCLUSIONS: Drugs with delta-opiate activity confer myocardial protection, which is additive to cardioplegia. Use of delta-opiate drugs in this context may have important clinical implications.  (+info)


  • Containing both naloxone (Narcan) and buprenorphine, Suboxone treats opioid addiction by reducing the intensity of cravings and withdrawal symptoms. (addict-help.com)
  • Suboxone is typically prescribed during the maintenance stage of treatment, after the addict has taken another medication called Subutex (oral buprenorphine) for several weeks. (addict-help.com)
  • Suboxone, a combination of buprenorphine / naloxone drug is the most commonly prescribed drug for opiate addiction withdrawal treatment, in part because it is specifically designed to combat abuse of buprenorphine. (addict-help.com)
  • Buprenorphine and Buprenorphine/Naloxone - specific discussions, topics, patient experiences and anything else related to the maintenance treatment of opioid addiction with Suboxone, Subutex, Zubsolv, Bunavail or any of their generic formulations in an opioid treatment program OR an office based setting! (methadone.org)


  • MAT is a comprehensive approach that combines approved medications (currently, methadone, buprenorphine or naltrexone) with counseling and other behavioral therapies to treat patients with opioid use disorder. (fda.gov)
  • Research indicates that when used in combination with behavioral and addiction counseling therapies , buprenorphine supports a "whole patient" method of successfully treating and managing opioid dependence. (addict-help.com)
  • A randomized clinical trial evaluating whether Behavioral Drug and HIV Risk Reduction Counseling (BDRC), abstinence-contingent take-home buprenorphine (ACB), or the combination of the two improve efficacy and cost-effectiveness of standard buprenorphine treatment for opiate-dependent individuals in Malaysia. (clinicaltrials.gov)


  • Buprenorphine can cause side effects similar to other opioids and also can cause physical dependence. (webmd.com)
  • The U.S. Food and Drug Administration today approved Probuphine, the first buprenorphine implant for the maintenance treatment of opioid dependence. (fda.gov)
  • Until today, buprenorphine for the treatment of opioid dependence was only approved as a pill or a film placed under the tongue or on the inside of a person's cheek until it dissolved. (fda.gov)
  • Expanding the use and availability of medication-assisted treatment (MAT) options like buprenorphine is an important component of the FDA's opioid action plan and one of three top priorities for the U.S. Department of Health and Human Services' Opioid Initiative aimed at reducing prescription opioid and heroin related overdose, death and dependence. (fda.gov)
  • The purpose of this study is to assess the feasibility, cost and effectiveness of interventions designed to integrate buprenorphine treatment for opioid dependence into HIV primary care in ten HIV care centers in the U.S. (clinicaltrials.gov)
  • Buprenorphine for the Treatment of Opioid Dependence in Preg. (lww.com)

dose of buprenorphine

  • Probuphine is designed to provide a constant, low-level dose of buprenorphine for six months in patients who are already stable on low-to-moderate doses of other forms of buprenorphine, as part of a complete treatment program. (fda.gov)

shown that buprenorphine

  • Research has shown that buprenorphine is effective for treating opioid addiction . (webmd.com)
  • Some research has shown that buprenorphine lessens the neonatal abstinence syndrome when compared to methadone. (clinicaltrials.gov)

Methadone and Buprenorphine

  • The subjects in this study are women enrolled in a large, multi-site, double blind study that looks at the effects of methadone and buprenorphine treatment during pregnancy. (clinicaltrials.gov)
  • Additionally, infant neurobehavioral assessments and measurements of infant vagal tone will be collected to see how methadone and buprenorphine differentially affect the neonatal abstinence syndrome, or 'withdrawal' in exposed neonates. (clinicaltrials.gov)
  • The differential effects of methadone and buprenorphine on the neonatal abstinence syndrome will also be explored. (clinicaltrials.gov)

take buprenorphine

  • You take buprenorphine by placing pills under your tongue . (webmd.com)
  • How should I take buprenorphine and naloxone? (drugs.com)
  • Wear a medical alert tag or carry an ID card stating that you take buprenorphine and naloxone. (drugs.com)

naloxone treatment

  • Highlights the findings of the NIDA CTN study that compared longer term versus short-term buprenorphine/naloxone treatment in an outpatient setting. (drugabuse.gov)
  • Findings from a study conducted by NIDA's National Drug Abuse Treatment Clinical Trials Network (CTN) indicated that prescription opioid-dependent patients are most likely to reduce opioid use during buprenorphine/naloxone treatment with relatively brief weekly medical management visits. (drugabuse.gov)


  • Subutex and Cizdol are trade names for medications given to heroin and prescription pain killer addicts while buprenorphine-based Temgesic, Buprenex and Norspan are normally prescribed relieve acute chronic pain. (addict-help.com)


  • In our original RCT, buprenorphine (BUP) was superior to naltrexone and placebo in treatment retention, weeks of consecutive abstinence and time to heroin use. (clinicaltrials.gov)
  • Trends in Receipt of Buprenorphine and Naltrexone for Opioid Use Disorder Among Adolescents and Young Adults, 2001-2014. (populationmedicine.org)
  • To identify time trends and disparities in receipt of buprenorphine and naltrexone among youth with OUD in the United States. (populationmedicine.org)
  • Dispensing of a medication (buprenorphine or naltrexone) within 6 months of first receiving an OUD diagnosis. (populationmedicine.org)
  • Overall, 5580 (26.8%) youth were dispensed a medication within 6 months of diagnosis, with 4976 (89.2%) of medication-treated youth receiving buprenorphine and 604 (10.8%) receiving naltrexone. (populationmedicine.org)
  • In this first national study of buprenorphine and naltrexone receipt among youth, dispensing increased over time. (populationmedicine.org)

opiate-dependent individuals

  • Buprenorphine is a new therapy for opiate dependent individuals, and its use during pregnancy is currently being evaluated. (clinicaltrials.gov)


  • Buprenorphine can help treat addiction to opioid drugs, including heroin and narcotic painkillers. (webmd.com)
  • In some cases, buprenorphine may be used as an alternative to methadone , which also is given to treat opioid addiction. (webmd.com)
  • Buprenorphine and naloxone is a combination medicine used to treat narcotic (opiate) addiction. (drugs.com)
  • Buprenorphine and naloxone may cause breathing problems, behavior changes, or life-threatening addiction and withdrawal symptoms in your newborn if you use the medication during pregnancy. (drugs.com)
  • The Drug Addiction Treatment Act of 2000 and the approval of buprenorphine for the office-based treatment of opioid addiction provide a new opportunity to integrate addiction treatment and medical care for people with HIV. (clinicaltrials.gov)
  • To address this problem, the Buprenorphine Treatment Blending Team (also referred to as: "Buprenorphine Awareness Team") developed a training package to disseminate information and enhance awareness among multi-disciplinary addiction professionals about buprenorphine treatment. (drugabuse.gov)
  • Buprenorphine is a partially synthetic opioid derived from thebaine, a lesser component of opium and similar chemically to codeine and morphine, buprenorphine is used to help opioid abusers beat their addiction. (addict-help.com)
  • Buprenorphine has a number of legitimate uses, including being prescribed as a painkiller for individuals with chronic pain and to provide an alternative treatment for individuals that have developed an opioid addiction. (addict-help.com)
  • Due to the highly addictive qualities of buprenorphine, it is a prescription drug that is often abused by individuals who are prescribed it to treat an opioid addiction, in a similar manner to how methadone is often abused. (addict-help.com)
  • When treating opioid addiction, buprenorphine effectively works as a stepping stone drug. (addict-help.com)
  • High levels of the drug are prescribed, resulting in an addiction to buprenorphine, which is also an opioid. (addict-help.com)
  • The buprenorphine portion of the drug works exactly as described above when used to treat opiate addiction. (addict-help.com)
  • Is Treatment with Buprenorphine for an Opioid Addiction Always Successful? (addict-help.com)
  • Approved by the FDA in 2002, buprenorphine is now considered an essential component of medication assisted treatment (MAT) for an opioid addiction. (addict-help.com)

neonatal abstinen

  • In addition, prenatal use of buprenorphine appears to decrease the severity and duration of neonatal abstinence syndrome as compared with methadone maintenance. (lww.com)

opioid receptors

  • Buprenorphine mimicks the action of natural endorphins by stimulating the opioid receptors in the brain and spinal cord. (netdoctor.co.uk)
  • Unusual pharmacological properties found in buprenorphine helps reduce its potential for abuse by addicts, diminishes severity of cravings and withdrawal symptoms and exerts partial agonist properties on opioid receptors in the brain. (addict-help.com)


  • Medication receipt increased more than 10-fold, from 3.0% in 2002 (when buprenorphine was introduced) to 31.8% in 2009, but declined in subsequent years (27.5% in 2014). (populationmedicine.org)


  • You should not use this medicine if you are allergic to buprenorphine or naloxone (Narcan). (drugs.com)


  • Buprenorphine and naloxone may also be habit-forming, even at regular doses. (drugs.com)
  • Lower than normal doses of buprenorphine are given during the first few days, with a gradual increase in dosage occurring over a period of several weeks. (addict-help.com)


  • Buprenorphine is an opioid medicine similar to morphine , codeine, and heroin . (webmd.com)
  • Buprenorphine is a strong painkiller related to morphine. (netdoctor.co.uk)


  • Research has demonstrated the effectiveness of buprenorphine in reducing illicit drug use among opioid dependent people. (clinicaltrials.gov)
  • Instructs treatment providers about a unique, 13-day buprenorphine intervention for opioid dependent patients. (drugabuse.gov)
  • The aim of the study is to determine whether buprenorphine/naloxone maintenance versus detoxification using buprenorphine/naloxone, in prescription opioid dependent patients receiving primary care management and drug counseling in an office-based setting, leads to decreased illicit opioid use. (clinicaltrials.gov)
  • The purpose of this study is to assess the abuse liability and examine the reinforcing effects of intravenous buprenorphine and buprenorphine/naloxone combinations in healthy, non-drug dependent volunteers. (clinicaltrials.gov)
  • The purpose is to study the relation between pupillary diameter measured under scotopic conditions, and the pain thresholds measured at the time of peak and residual effect of methadone/buprenorphine in opiate-dependent patients following a substitution program. (clinicaltrials.gov)


  • This study will measure the amount of buprenorphine found in the blood after taking sublingual buprenorphine tablets versus after implantation with 4 Probuphine (buprenorphine implants). (clinicaltrials.gov)
  • This is an open-label study intended to evaluate the relative bioavailability of 4 Probuphine implants versus 16mg QD sublingual buprenorphine, as determined by plasma BPN AUC(0-24), during 24 hours at steady state. (clinicaltrials.gov)


  • However, as an implant, Probuphine provides a new treatment option for people in recovery who may value the unique benefits of a six-month implant compared to other forms of buprenorphine, such as the possibility of improved patient convenience from not needing to take medication on a daily basis. (fda.gov)
  • Comparisons: All eleven programs will compare a group of patients who receive integrated buprenorphine treatment and HIV care to a group of patients who receive an alternate intervention. (clinicaltrials.gov)
  • To test its effectiveness, the NIDA CTN protocol compared this 13-day buprenorphine taper intervention to an alternative treatment (clonidine detoxification) in both inpatient and outpatient settings. (drugabuse.gov)
  • In contrast with the clonidine treatment group, patients who received buprenorphine provided more opioid negative urine samples upon completion of the intervention. (drugabuse.gov)
  • Primary results indicated that young adults in the longer term buprenorphine treatment were less likely to inject drugs or abuse opioids, cocaine, and marijuana, and were more likely to remain in treatment than those young adults who received short-term detoxification. (drugabuse.gov)
  • Training program and manual, PowerPoint presentation, buprenorphine treatment research and resources. (drugabuse.gov)
  • Buprenorphine maintenance treatment is emerging as a treatment during pregnancy with distinct benefits for the neonate and the pregnant woman. (lww.com)
  • Management of buprenorphine includes initiation and maintenance treatment as well as careful planning for pain control during and after delivery and prevention of postpartum relapse risk. (lww.com)
  • There is evidence that emerging collaborative care models are effective ways to deliver buprenorphine maintenance treatment, although more investigation is needed to generalize this to the obstetric setting. (lww.com)


  • Buprenorphine/naloxone detoxification (Dtx) is identical to Mtn for the first 4 weeks (stabilization) following randomization. (clinicaltrials.gov)


  • Weaning from buprenorphine is generally safer and easier to control than weaning away from illegal opioids. (addict-help.com)

breast milk

  • Buprenorphine can pass into breast milk and may harm a nursing baby. (drugs.com)
  • Only very small amounts of buprenorphine enter breast milk, making it a good option for those who elect to breast-feed. (lww.com)


  • Buprenorphine is effective in decreasing the risk of relapse in pregnant women. (lww.com)

withdrawal symptoms

  • Regular adherence to MAT with buprenorphine reduces opioid withdrawal symptoms and the desire to use, without causing the cycle of highs and lows associated with opioid misuse or abuse. (fda.gov)
  • Do not stop using buprenorphine and naloxone suddenly, or you could have unpleasant withdrawal symptoms. (drugs.com)


  • Although buprenorphine does produce opioid-like side effects, such as respiratory depression, drowsiness and euphoria, its effects are significantly weaker than those produced by heroin and prescription pain pills. (addict-help.com)


  • Never use buprenorphine and naloxone in larger amounts, or for longer than prescribed. (drugs.com)


  • Never crush or break a buprenorphine and naloxone pill to inhale the powder or mix it into a liquid to inject the drug into your vein. (drugs.com)
  • Buprenorphine/naloxone maintenance (Mtn) is designed to reflect usual care by primary care physicians and includes weekly drug counseling (DC) and referral to ancillary services. (clinicaltrials.gov)
  • Implantable formulation of buprenorphine made of buprenorphine HCl/ethylene vinyl acetate, considered a drug. (clinicaltrials.gov)


  • When injected, though, it is absorbed and that absorption results side effects that are nearly identical to buprenorphine withdrawal effects. (addict-help.com)


  • Buprenorphine may have less severe side effects than methadone. (webmd.com)
  • These side effects can help limit the most common form of abuse in ways that buprenorphine alone simply can't. (addict-help.com)


  • Transtec patches contain the active ingredient buprenorphine, which is a type of medicine called an opioid analgesic (painkiller). (netdoctor.co.uk)



  • Buprenorphine and naloxone is not for use as a pain medication. (drugs.com)


  • This practice has resulted in death with the misuse of buprenorphine and naloxone and similar prescription drugs. (drugs.com)


  • Thirty methadone and 30 buprenorphine maintained women will be evaluated at 24, 28, 32 and 36 weeks gestation using a state-of-the-art computerized fetal actocardiograph and data analysis program to simultaneously evaluate fetal movement and heart rate and maternal physiologic parameters. (clinicaltrials.gov)