Drugs codeine

Dayer P, Desmeules J, Leemann T, Stribemi R. 1988. Bioactivation of the narcotic drug codeine in human liver is mediated by the polymorphic monooxygenase catalyzing debrisoquine 4-hydroxylation (cytochrome P-450 dbl/ bufl). Biochem Biophys Res Commun 152 411-416. 

Codeine is a natural alkaloid found in the opium plant. As a pharmaceutical, codeine is used as an analgesic, antitussive, and antidiar-rheal. Codeine is also commonly combined with other cough suppressants as well as with aspirin and ibuprofen. In the United States, codeine is a Schedule III controlled substance, which means that its distribution is more tightly regulated than unscheduled drugs. Codeine has pain-relieving qualities principally because, once in the body, about 10 percent of codeine turns into morphine. This conversion occurs in the liver, where an enzyme changes codeine s... 

As with all drugs, codeine has some undesirable effects in addition to its therapeutic effects. At the usual cough suppressing doses (see below), codeine may cause nausea—the medical term for upset stomach accompanied by the sensation of queasiness— which makes you feel as if you are about to regurgitate (vomit, or throw up ). Codeine may cause vomiting... 

Heroin is a Schedule I drug morphine, codeine, fentanyl, hydrocodone, hydromorphone, and oxycodone are Schedule II drugs codeine plus aspirin or acetaminophen is Schedule III propoxyphene is Schedule IV and codeine sold over the counter is Schedule V. 

Amino group containing drugs (codeine phosphate, Bare silica Micra, 3 pm Acetonitrile-5-20 mM Tris-HC1, pH 7.5-10 (90 35-10) 270 mm x 65-75 pm i.d. 200 mm packed length 143... 

Amino group-containing drugs codeine phosphate, ephedrine hydrochroride, thebaine, berberine, hydrochloride, jatrorrizine hydrochloride, cocaine hydrochloride... 

Triplet states of the amiodarone, an antiarrhythmic drug which shows cutaneous toxicity, are involved in its photolysis. The lowest triplet states of the drugs codeine and morphine and their molecular sub units veratrole and guaiacol are. ... 

Spectra in the mid-infrared range were recorded in 70 blood serum samples representing seven classes of the drugs codeine, methamphetamine, desmethyldiazepam, oxazepam, diazepam, amphetamine sulfate, and hydromorphone. For data analysis, the absorbances at 16 wavenumbers were chosen as input to the CART algorithm. The resulting classification tree has the following shape ... 

Thomapyrin containing acetaminophen, caffeine and acetylsalicylic acid Antiviral drug suramin Amino group containing drugs codeine phosphate, ephedrine hydrochroride, thebaine, berberine, hydrochloride, jatrorrizine hydrochloride, cocaine hydrochloride Isradepin and by-products Morphine alkaloids Barbiturates (barbital, phenobarbital, secobarbital, thiopental)... 

Morphine has an LD50 i.v. in mouse of 226-318 mg/kg (Wink, 1993). Codeine (62) is also an important analgetic and antitussive drug. Codeine is the most widely used morphine type alkaloid it has an LD50 i.p. in mouse of 300 mg/kg (Wink, 1993). This alkaloid is derived from opium (0.2-0.7%) and synthesized by methylation of morphine (Tyler et al, 1981). Heroin (65) (Fig. 32.21), a synthetic diacetate of morphine, crosses the blood-brain barrier more rapidly than morphine and is highly euphoric and analgetic. 

As an oral drug, codeine is much less effective as an analgesic due to its large first-pass hepatic metabolism compared to morphine, hydrocodone and oxycodone. The plasma half-life of codeine is also shorter than many other orally available opiates such as morphine, hydromorphone, and oxymorphone. Like all opioids, continued use of codeine may result in tolerance development and physical dependence. However, when compared to potent mu agonists, codeine is less addictive and is associated with mild withdrawal symptoms. 

Estimation of Other Alkaloids in Opium. Of the other alkaloids the most important is codeine, and processes for its estimation in opium have been described by Cespari, Andrews,and Annett and co-workers methods for its assay in admixture with other drugs in tablets and other products are also available. The estimation of papaverine has been described by Issekutz,i and of narcotine by Snesarov. As to methods for the separation and estimation of two or more of these subsidiary alkaloids, codeine and narcotine have been dealt with by van der Widen,narcotine and papaverine by Annett and Bose, ( and the bromination of codeine and narceine has been studied by Vaisberg et al. with a view to estimation by this means. 

Centrally acting drugs include dextromethorphan and codeine. However the possibility that there may also be peripheral effects of these drugs has lead to the development of BW443C (see below). 

In the strict sense, opiates are drugs which are derived from opium and include the natural products morphine, codeine, thebaine and many semi-synthetic congeners derived from them. In the wider sense, opiates are morphine-like drugs with non-peptidic structures. The old term opiates is now more and more replaced by the term opioids which applies to any substance, whether endogenous or synthetic, pqrtidic or non-peptidic, that produces morphine-like effects through an action on opioid receptors. 

Cytochrome P450 2D6 Extremely high activity in about 2% of Caucasian populations and completely deficient activity in about 7%. Inefficiency in ultrarapid metabolizers and extremely heavy effects in poor metabolizers for more than 50 drugs. A few drugs requiring bioactivation by CYP have low efficacy in poor metabolizers (example codein is activated to morphine via CYP2D6). 

The physician s order reads codeine sulfate gr 1/4 (apodiecaries ). The drug container is labeled codeine sulfate 15 mg (metric). Grains must be converted to milligrams or milligrams converted to grains. 

Relief of severe, persistent cough (codeine, although the drug s use has declined)... 

Use of codeine may result in respiratory depression, euphoria, light-headedness, sedation, nausea, vomiting, and hypersensitivity reactions. The more common adverse reactions associated with the antitussives are listed in the Summary Drug Table Antitussive, Mucolytic, and Expectorant Drugs. When used as directed, nonprescription cough medicines containing two or more ingredients have few adverse reactions. However, those that contain an antihistamine may cause drowsiness. 

The term opioid refers to any exogenous substance that acts as an agonist at any of several receptors. Opioid antagonists are drugs that bind to a receptor but produce no actions. The poppy plant, Papaver somniferum, from which opium is obtained, is grown in many areas of the world. Morphine constitutes 10% of opium, and codeine can be obtained direcdy from opium. Semisynthetic opioids such as heroin and oxycodone are obtained directly or indirectly from morphine. There are other distinct chemical classes of drugs with opioid actions, including the methadones. 

Drugs (radiocontrast media, drugs used in general anesthesia, codeine morphine, dextromethorphan, aspirin, and other analgesics)... 

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