Antitussive Agents
Dextromethorphan
Pharmacological studies on root bark of mulberry tree (Morus alba L.) (1/196)
Pharmacological studies were done on the root bark of mulberry tree and pharmacological effects were compared with the clinical effects of "Sohakuhi" in Chinese medicine. n-Butanol- and water-soluble fractions of mulberry root had similar effects except for those on the cadiovascular system. Both fractions showed cathartic, analgesic, diuretic, antitussive, antiedema, sedative, anticonvulsant, and hypotensive actions in mice, rats, guinea pigs and dogs. There appears to be a correlation between the experimental pharmacological results and the clinical applications of mulberry root found in the literature on Chinese medicine. (+info)Influence of central antitussive drugs on the cough motor pattern. (2/196)
The present study was conducted to determine the effects of administration of centrally active antitussive drugs on the cough motor pattern. Electromyograms of diaphragm and rectus abdominis muscles were recorded in anesthetized, spontaneously breathing cats. Cough was produced by mechanical stimulation of the intrathoracic trachea. Centrally acting drugs administered included codeine, morphine, dextromethorphan, baclofen, CP-99,994, and SR-48,968. Intravertebral artery administration of all drugs reduced cough number (number of coughs per stimulus trial) and rectus abdominis burst amplitude in a dose-dependent manner. Codeine, dextromethorphan, CP-99,994, SR-48,968, and baclofen had no effect on cough cycle timing (CTtot) or diaphragm amplitude during cough, even at doses that inhibited cough number by 80-90%. Morphine lengthened CTtot and inhibited diaphragm amplitude during cough, but these effects were not dose dependent. Only CP-99,994 altered the eupneic respiratory pattern. Central antitussive drugs primarily suppress cough by inhibition of expiratory motor drive and cough number. CTtot and inspiratory motor drive are relatively insensitive to the effects of these drugs. CTtot can be controlled independently from cough number. (+info)Sigmoidal kinetics of CYP3A substrates: an approach for scaling dextromethorphan metabolism in hepatic microsomes and isolated hepatocytes to predict in vivo clearance in rat. (3/196)
The metabolism of a number of compounds by the cytochrome P-450 subfamily CYP3A does not exhibit classic Michaelis-Menten kinetics but displays a sigmoidal rate-substrate concentration relationship. Intrinsic clearance (CLint) cannot be calculated for these drugs due to the lack of a first order region in their kinetic profiles, and a suitable parameter has yet to be identified to allow such data to be scaled to predict in vivo clearance. As sigmoidal kinetics have only been observed with microsomal systems, we have investigated whether this behavior is demonstrable in freshly isolated hepatocytes. We have also evaluated the term maximum clearance (CLmax), which refers to the in vitro clearance when the enzyme is fully activated, to predict in vivo clearance. To these ends we have studied the metabolism of dextromethorphan to methoxymorphinan and dextrorphan; methoxymorphinan production is best described by sigmoidal kinetics in both hepatocytes and microsomes, dextrorphan production is best described by a two site Michaelis-Menten model in microsomes but is sigmoidal in hepatocytes. Total clearance, estimated from the CLmax and CLint terms, was scaled to give mean predictions of 127 to 319 ml/min/standard rat weight of 250 g. In vivo CLint, determined after infusion via the hepatic portal vein to steady state and correcting for plasma protein binding and blood-to-plasma concentration ratio, was 259 +/- 59.2 ml/min/standard rat weight of 250 g. These investigations show that sigmoidal kinetics is not unique to microsomes and that CLmax is a useful parameter for scaling to the in vivo situation. (+info)Characterization of cytochrome P-450 2D1 activity in rat brain: high-affinity kinetics for dextromethorphan. (4/196)
We investigated the enzymatic function, stability, and regional distribution of rat brain cytochrome P-450 (CYP) 2D1 activity. CYP2D1 is the homolog of human CYP2D6, a genetically variable enzyme that activates or inactivates many clinical drugs acting on the central nervous system (e.g., antidepressants, monoamine oxidase inhibitors, serotonin uptake inhibitors, and neuroleptics), drugs of abuse (e.g., amphetamine and codeine), neurotoxins (e.g., 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, 1,2,3, 4-tetrahydroquinoline), and endogenous neurochemicals (e.g., tryptamine). The CYP2D family has been identified in rodent, canine, and primate brain. Conversion of dextromethorphan to dextrorphan by rat brain membranes was assayed by HPLC and was dependent on NADPH, protein concentration, and incubation time. Significant loss of activity was observed in some homogenizing buffers and after freezing of whole tissues or membrane preparations. Dextromethorphan (0.5-640 microM) metabolism was mediated by high- and low-affinity enzyme systems; K(m1) was 2.7 +/- 2.6 and K(m2) was 757 +/- 156 microM (n = 3 rats, mean +/- S.E.). The enzyme activity was significantly (p <.01) and stereoselectively inhibited by CYP2D1 inhibitors quinine and quinidine (not by CYP2C or CYP3A inhibitors), and by anti-CYP2D6 peptide antiserum (not by anti-CYP2C, -CYP2B, or -CYP3A antibodies). The enzymatic activity demonstrated significant brain regional variation (n = 10 regions, p <.001). These data characterize CYP2D1-mediated dextromethorphan metabolism in rat brain and suggest that localized metabolism of other CYP2D1 substrates (drugs, neurotoxins, and possibly endogenous compounds) within the brain will occur. In humans, CYP2D6 is genetically polymorphic; the variable expression of brain CYP2D6 may result in interindividual differences in central drug and neurotoxin metabolism, possibly contributing to interindividual differences in drug effects and neurotoxicity. (+info)The role of codeine phosphate premedication in fibre-optic bronchoscopy under insufficient local anaesthesia and midazolam sedation. (5/196)
Midazolam is widely used as a sedative agent to produce amnesia in patients undergoing fibre-optic bronchoscopy. However, if a patient does not receive sufficient local anaesthesia, continuous severe cough and physical movement may interrupt the procedure and reduce its safety. We therefore examined whether codeine phosphate is a useful premedication for bronchoscopy. The study design was a randomized comparison between codeine phosphate and a placebo in patients undergoing light local anaesthesia and midazolam sedation. We used low dose local anaesthesia (5 ml of nebulized 2% xylocaine) on the assumption of insufficient local anaesthesia. Patients were allocated to receive codeine phosphate 0.4 mg kg-1 or a saline placebo 60 min before they were sedated with i.v. midazolam. If the patients exhibited severe cough during bronchoscopy, intrabronchial supplemental local anaesthesia (2% xylocaine solution in 1 ml increments) was instilled via a bronchoscope to the trachea and segmental bronchi to suppress the cough. The dose of supplemental xylocaine was assessed and the requirements were significantly lower in the codeine group compared to the placebo group: 36.4 +/- 10.2 mg vs. 95.1 +/- 24.6 mg, respectively. After bronchoscopy, patients were interviewed by a doctor to assess their willingness to undergo a repeat procedure if one was clinically indicated, but no significant difference was observed between the two groups. If local anaesthesia is insufficient, midazolam together with codeine phosphate premedication is useful for both the patient and the bronchoscopist. (+info)The antitussive effect of dextromethorphan in relation to CYP2D6 activity. (6/196)
AIMS: To test the hypothesis that inhibition of cytochrome P450 2D6 (CYP2D6) by quinidine increases the antitussive effect of dextromethorphan (DEX) in an induced cough model. METHODS: Twenty-two healthy extensive metaboliser phenotypes for CYP2D6 were studied according to a double-blind, randomised cross-over design after administration of: (1) Placebo antitussive preceded at 1 h by placebo inhibitor; (2) 30 mg oral DEX preceded at 1 h by placebo inhibitor (DEX30); (3) 60 mg oral DEX preceded at 1 h by placebo inhibitor (DEX60); (4) 30 mg oral DEX preceded at 1 h by 50 mg oral quinidine sulphate (QDEX30). Cough frequency following inhalation of 10% citric acid was measured at baseline and at intervals up to 12 h. Plasma concentrations of DEX and its metabolites were measured up to 96 h by h.p.l.c. RESULTS: Inhibition of CYP2D6 by quinidine caused a significant increase in the mean ratio of DEX to dextrorphan (DEX:DOR) plasma AUC(96) (0.04 vs 1.81, P<0.001). The mean (+/-s.d.) decrements in cough frequency below baseline over 12 h (AUEC) were: 8% (11), 17% (14.5), 25% (16.2) and 25% (16.9) for placebo, DEX30, DEX60 and QDEX30 treatments, respectively. Statistically significant differences in antitussive effect were detected for the contrasts between DEX60/placebo (P<0.001; 95% CI of difference +80, +327) and QDEX30/placebo (P<0.001, +88, +336), but not for DEX30/placebo, DEX30/DEX60 or DEX30/QDEX30 (P=0.071, -7, +241; P=0.254, -37, +211; P=0.187, -29, +219, respectively). CONCLUSIONS: A significant antitussive effect was demonstrated after 60 mg dextromethorphan and 30 mg dextromethorphan preceded by 50 mg quinidine using an induced cough model. However, although the study was powered to detect a 10% difference in cough response, the observed differences for other contrasts were less than 10%, such that it was possible only to imply a dose effect (30 vs 60 mg) in the antitussive activity of DEX and enhancement of this effect by CYP2D6 inhibition. (+info)Dextromethorphan. Extrapolation of findings from reproductive studies in animals to humans. (7/196)
QUESTION: One of my patients, who is now 8 weeks pregnant, just read in the newspaper that dextromethorphan (DM), an antitussive found in a variety of cough medicines, caused birth defects in chicken embryos. The author of the study stated that even one dose could be dangerous and that he would never allow his wife to use this drug if she were pregnant. My patient was understandably very concerned because last week she was suffering from a nasty cough and had been advised by her pharmacist to use a cough mixture containing DM, which she subsequently took for several days. ANSWER: You may reassure your patient that she did not put her baby at risk by using this substance. Dextromethorphan has been on the market for many years and has never been implicated as a human teratogen. Furthermore, chick embryos are not a good model for predicting teratogenic potential in humans and, consequently, were abandoned as such more than 30 years ago. (+info)Effect of oral mexiletine on the cough response to capsaicin and tartaric acid. (8/196)
BACKGROUND: The effect of the orally active local anaesthetic mexiletine on the cough response to two different tussive agents, a C-fibre ending stimulator capsaicin and a chemostimulant tartaric acid, was examined in normal subjects. METHODS: The cough threshold, defined as the lowest concentration of capsaicin (C(5)-CP) or tartaric acid (C(5)-TA) causing five or more coughs, and histamine induced bronchoconstriction were measured three hours after a single oral dose of 300 mg mexiletine or placebo in 14 normal subjects. RESULTS: Mexiletene in a mean (SE) serum concentration of 0.99 (0. 04) microg/ml significantly increased C(5)-TA from a geometric mean (SE) of 32.0 (1.27) mg/ml with placebo to 49.9 (1.34) mg/ml, but C(5)-CP did not differ significantly between treatment with mexiletine (12.2 (1.33) microM) and placebo (14.9 (1.23) microM). CONCLUSIONS: These results suggest that the cough response to capsaicin and tartaric acid may be mediated in part via different neural pathways. (+info)Antitussive agents are medications that are used to suppress cough. They work by numbing the throat and interrupting the cough reflex. Some common antitussives include dextromethorphan, codeine, and hydrocodone. These medications can be found in various over-the-counter and prescription cough and cold products. It is important to use antitussives only as directed, as they can have side effects such as drowsiness, constipation, and slowed breathing. Additionally, it's important to note that long term use of opioid antitussive like codeine and hydrocodone are not recommended due to the risk of addiction and other serious side effects.
Aporphine is a type of chemical compound called alkaloids, which are found in certain plants. Aporphines have a specific chemical structure and can have various pharmacological effects. They have been studied for their potential medicinal properties, including anti-inflammatory, antispasmodic, and antiasthmatic activities. Some aporphine alkaloids have also been found to have psychoactive effects and are used in traditional medicine in some cultures. However, more research is needed to fully understand the therapeutic potential and safety of aporphines.
Dextromethorphan is a medication that is commonly used as a cough suppressant in over-the-counter cold and cough remedies. It works by numbing the throat area, which helps to reduce the cough reflex. Dextromethorphan is a synthetic derivative of morphine, but it does not have the same pain-relieving or addictive properties as opioids.
Dextromethorphan is available in various forms, including tablets, capsules, liquids, and lozenges. It is often combined with other medications, such as antihistamines, decongestants, and pain relievers, to provide relief from cold and flu symptoms.
While dextromethorphan is generally considered safe when used as directed, it can have side effects, including dizziness, drowsiness, and stomach upset. In high doses or when taken with certain other medications, dextromethorphan can cause hallucinations, impaired judgment, and other serious side effects. It is important to follow the recommended dosage and to talk to a healthcare provider before taking dextromethorphan if you have any health conditions or are taking other medications.
A cough is a reflex action that helps to clear the airways of irritants, foreign particles, or excess mucus or phlegm. It is characterized by a sudden, forceful expulsion of air from the lungs through the mouth and nose. A cough can be acute (short-term) or chronic (long-term), and it can be accompanied by other symptoms such as chest pain, shortness of breath, or fever. Coughing can be caused by various factors, including respiratory infections, allergies, asthma, environmental pollutants, gastroesophageal reflux disease (GERD), and chronic lung diseases such as chronic obstructive pulmonary disease (COPD) and bronchitis. In some cases, a cough may be a symptom of a more serious underlying condition, such as heart failure or lung cancer.
Noscapine
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List of MeSH codes (D27)
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Analgesics1
- Therapy for patients with acute bronchitis is generally aimed toward alleviation of symptoms and includes the use of analgesics, antipyretics, antitussives, and expectorants. (medscape.com)
Dextromethorphan Hydrobromide1
- Pholcodine and dextromethorphan hydrobromide are antitussives that are intended to help suppress dry, unproductive (non-phlegmy) coughs, which can contribute to making your throat sore. (choice.com.au)
Centrally acting antitussiv2
- A naturally occurring opium alkaloid that is a centrally acting antitussive agent. (harvard.edu)
- Dextromethorphan, a centrally-acting antitussive agent, depresses the medullary cough center through sigma receptor stimulation, resulting to decreased sensitivity of cough receptors and interruption of cough impulse transmission.Pseudoephedrine is both an α-and β-adrenergic receptor agonist. (medeasy.health)
Opioid2
- Hydromorphone was approved for use in the United States in 1984 and is still widely used in treatment of moderate-to-severe pain not responsive to non-opioid agents. (nih.gov)
- Severe adverse events include life-threatening respiratory depression, addiction, abuse, opioid withdrawal, serotonin syndrome (when used with serotonergic agents) and adrenal insufficiency. (nih.gov)
Relieves3
- It is an antitussive agent which relieves cough as well as upper respiratory symptoms linked to cold or allergy so buy Hydrocodone online. (video-bookmark.com)
- EU] Antispasmodic: An agent that relieves spasm. (joecolgan.com)
- EU] Antitussive: An agent that relieves or prevents cough. (joecolgan.com)
Decongestant1
- This preparation is a mixture of antitussive, decongestant and antihistamine agent. (medeasy.health)
Analgesic4
- Hydrocodone is a narcotic analgesic used in combination products to relieve mild to moderate pain and an antitussive agent to relieve cough and upper respiratory symptoms associated with allergy or cold . (peacehealth.org)
- Today, opium alkaloids are used as an analgesic, antitussive (cough suppressant), and antispasmodic agents (smooth muscle relaxant). (martifarm.com)
- Dextromethorphan is an antitussive agent and, unlike the isomeric levorphanol, it has no analgesic or addictive properties. (medlibrary.org)
- By combining analgesic agents that target different receptors and pathways, we can enhance pain control by producing additive, or synergistic, effects. (medscape.com)
Mild to moderate pain1
- Codeine is used to treat mild to moderate pain and as an antitussive agent. (rehabs.com)
Codeine3
- The antitussive activity of the extract was comparable to that of codeine phosphate (10 mg), a standard antitussive agent. (wikigenes.org)
- 14. Takahama K, Shirasaki T Central and peripheral mechanisms of narcotic antitussives: codeine-sensitive and -resistant coughs. (lekwpolsce.pl)
- 17. Freestone C, Eccles R. Assessment of the antitussive efficacy of codeine in cough associated with common cold. (lekwpolsce.pl)
Coughs2
- But a wide-scale review of trials testing antitussives (mainly dextromethorphan) found that they were no more effective than a placebo for treating coughs in most cases. (choice.com.au)
- The over-the-counter cough and cold products examined in this study include these ingredients: decongestants (for unclogging a stuffy nose), expectorants (for loosening mucus so that it can be coughed up), and antitussives (for quieting coughs). (cdc.gov)
Drugs3
- Cardiovascular Drugs / Antilipemic Agents / HMG-CoA Reductase Inhibitors (i.e. (tevausa.com)
- Insomnia inducing drugs include caffeine, nicotine, weight loss preparations, and activating agents of both prescription and abuse. (springer.com)
- Different treatable traits exist with cough variant asthma (CVA)/eosinophilic bronchitis responding to anti-inflammatory treatment and non-acid reflux being treated with promotility agents rather the anti-acid drugs. (ersjournals.com)
Narcotic1
- Dextromethorphan is a safe, effective, non-narcotic antitussive agent which has a central action on the cough centre in the medulla. (medeasy.health)
Antihistamine1
- Doxylamine: A first-generation antihistamine that is commonly used as a sleeping agent due to. (bargelheuser.de)
Antimicrobial1
- Penicillin is the antimicrobial agent of choice for treatment of group A streptococcal pharyngitis. (medscape.com)
Clinical Trials1
- Our aims were to develop a health related quality of life questionnaire specifically for chronic cough that is brief, simple to administer and score, suitable to monitor individual patients, assess different aspects of health affected in patients, be sensitive enough to detect changes in health status within an adult chronic cough population, and be an outcome measure in clinical trials of new antitussive agents. (bmj.com)
Sedatives3
- In this brief overview, medications used to treat insomnia such as hypnotics, sedatives, medications inducing sedation as a side effect, medications directed at the sleep-associated circadian neuroendocrine system, and agents utilized in treating insomnia-inducing sleep diagnoses such as restless leg syndrome are discussed. (springer.com)
- Other pharmacological agents producing sedation (sedatives and agents used off-label for sedative side-effects) should be used cautiously for the treatment of insomnia due to the increased risk of next day sleepiness as well as for known toxicities and adverse side effects. (springer.com)
- Medications for treating insomnia are classified as hypnotics, sedatives, medications inducing sedation as a side effect, medications directed at the sleep-associated circadian neuroendocrine system, and agents utilized in treating insomnia-inducing sleep diagnoses such as restless leg syndrome (RLS) (Curry et al. (springer.com)
Medication2
- Noscapine is often used as an antitussive medication. (wikipedia.org)
- tetracaine) and has been associated with adverse CNS effects possibly related to a prior sensitivity to related agents or interaction with concomitant medication. (nih.gov)
Doses3
- At any one time 20% of the UK population have a troublesome cough and sufferers consume 75 million doses of over the counter antitussive medications annually. (bmj.com)
- Hydromorphone is also used, in low doses, as an antitussive. (nih.gov)
- Narcotics do play a role, but newer agents that are being used more prevalently include N-methyl-D-aspartate (NMDA) receptor antagonists, either ketamine or dextromethorphan , at doses that are well above what is used for an antitussive effect, as well as antiseizure medications like gabapentinoids, particularly gabapentin and pregabalin . (medscape.com)
Hypnotics1
- These are the agents that should be exclusively classified as hypnotics and utilized to induce sleep when medications are required to treat the complaint of insomnia. (springer.com)
Acute1
- There have been no convincing cases of idiosyncratic acute, clinically apparent liver injury attributed to either agent. (nih.gov)
Recreational2
- Dextromethorphan is a widely used antitussive agent, also showing increased recreational abuse. (erowid.org)
- Many of these substances have long been used in ritualistic medicine, and some are emerging agents of recreational use. (medscape.com)
Antagonist1
- Pretreatment with rimcazole, a σ-specific antagonist, causes a dose-dependent reduction in antitussive activity of noscapine. (wikipedia.org)
Sympathomimetic2
- Ephedrine is classified as a sympathomimetic agent that acts as an agonist at α and β receptors. (differencey.com)
- Pseudoephedrine is classified as a sympathomimetic agent that acts as an agonist at α receptors. (differencey.com)
Commonly used as a thick1
- Pectin is commonly used as a thickening agent in foods like jam and jelly. (choice.com.au)
Promethazine1
- Promethazine is an H 1 receptor blocking agent. (medlibrary.org)
Benzodiazepines1
- Benzodiazepines are the first-line agents, and should be administered liberally. (medscape.com)
Central1
- Le recueil de données sur les intoxications au moyen d'un système de registre central est nécessaire pour la mise en oeuvre de programmes de prévention et leur évaluation future. (who.int)
Effective1
- It is usually well tolerated and provides good coverage of most infectious agents, but it is not effective against Mycoplasma and Legionella species. (medscape.com)
Activity2
- Noscapine's antitussive effects appear to be primarily mediated by its σ-receptor agonist activity. (wikipedia.org)
- 0.001) antitussive activity at all tested dose levels when compared with the control. (wikigenes.org)
Bacterial2
- This agent inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins. (medscape.com)
- This agent inhibits bacterial protein synthesis by binding with the 30S and, possibly, the 50S ribosomal subunit(s). (medscape.com)
Effects3
- This agent is primarily used for its antitussive (cough-suppressing) effects. (wikipedia.org)
- Many other agents can be classified as pseudohallucinogens because they produce psychotic and delirious effects without the classic visual disturbances of true hallucinogens. (medscape.com)
- This also helps to minimize any side effects that are associated with a single agent. (medscape.com)
Review1
- 12. Morice A, Kardos P. Comprehensive evidence-based review on European antitussives. (lekwpolsce.pl)
Clinically1
- A commonly reported side-effect following inhaled administration of therapeutic dose of the current, clinically used non-selective muscarinic antagonists is dry-mouth and while this is reported as only mild in intensity it does limit the dose of inhaled agent given. (justia.com)
Management1
- In stable patients with spontaneous breathing, conservative management, including antibiotic prophylaxis, antitussive agents, and chest tube insertion if required, is considered sufficient. (silverchair.com)
Treatment1
- used as an anti-diarrheic and antitussive agent for the treatment of chronic diarrhea or dysentery, persistent cough, and hoarse voice. (tcmfans.club)
Abuse1
- Synthetic cathinone or "bath salt" abuse has emerged over the last decade and gained popularity in large part due to these agents' accessibility and ambiguous legal status. (medscape.com)
Include1
- these include the short acting agents Atrovent® (ipratropium bromide) and Oxivent® (oxitropium bromide) and the long acting agent Spiriva® (tiotropium bromide). (justia.com)