UNODC - Bulletin on Narcotics - Issue 1 -
This pathway depicts, in a stylized human liver cell, the principal candidate pharmacogenes involved in the pharmacokinetics of codeine and morphine. Codeine (INN) C18H21NO3 or methylmorphine is an opiate used for its are occasionally encountered on the pharmaceutical market and in research. Drugs bearing resemblance to codeine in effects due to close structural relationship are. These drugs include morphine and codeine, as well as many synthetic on the black market or seeking out illegal opiates such as heroin.
Codeine - DrugBank
While codeine can be extracted from opium, most codeine is synthesized from morphine through the process of O-methylation. Codeine is marketed as the salts codeine sulphate and codeine phosphate in the United States and Canada.
Codeine hydrochloride is more commonly marketed in continental Europe and other regions, and codeine hydroiodide and codeine bitartrate round out the top five most-used codeine salts worldwide. Codeine is usually present in raw opium as free alkaloid in addition to codeine meconate, codeine pectinate, and possibly other naturally-occuring codeine salts. Dozens of other salts of codeine have been developed over the last years including some with special properties of other drug groups such as codeine salicylate and codeine-based salts of barbituric acid barbiturates.
Codeine citrate, nitrate, picrate, acetate, hydrobromide and others are occasionally encountered on the pharmaceutical market and in research. Codeine is the starting material and prototype of a large class of mainly mild to moderately strong opioids such as hydrocodone, dihydrocodeine and its derivatives such as nicocodeine, oxycodone etc.
Drugs bearing resemblance to codeine in effects due to close structural relationship are variations on the methyl groups at the 3 position including ethylmorphine a. While having no narcotic effects of its own, the important opioid precursor thebaine differs from codeine only slightly in structure. Pseudocodeine and some other similar alkaloids not currently used in medicine are found in trace amounts in opium as well.
Indications Approved indications for codeine include: Cough, though its efficacy in low dose over the counter formulations has been disputed. These combinations provide greater pain relief than either agent alone drug synergy; see synergy.
Codeine-only products can be obtained with a prescription as a time release tablet eg. Codeine Contin r mg and Perduretas 50 mg. Injectable codeine is available for subcutaneous or intramuscular injecton; intravenous injection can cause a serious reaction which can progress to anaphylaxis.
Codeine suppositories are also marketed in some countries. Caffeine, being a stimulant, tends to offset the sedative effects of codeine.
It also can increase the effectiveness and absorption rate of analgesics in some circumstances. Municipal and provincial regulations may impact the range of products which can be dispensed in the latter case. It can be used legally only by health professionals and for university research purposes.
The substance can be given by pharmacists under a prescription. However, codeine is available without prescription from licensed pharmacists in doses up to 0. It is a Schedule II controlled substance for pain-relief products containing codeine alone or more than 90 mg per dosage unit. Preparations for cough or diarrhea containing small amounts of codeine in combination with two or more other active ingredients are Schedule V in the US, and may be dispensed in amounts up to 4 fl.
In locales where dilute codeine preparations are non-prescription, anywhere from very few to perhaps a moderate percentage of pharmacists will sell these preparations without a prescription.
Drugs bearing resemblance to codeine in effects due to close structural relationship are variations on the methyl groups at the 3 position including ethylmorphine a. While having no narcotic effects of its own, the important opioid precursor thebaine differs from codeine only slightly in structure. Pseudocodeine and some other similar alkaloids not currently used in medicine are found in trace amounts in opium as well. History[ edit ] Codeine, or 3-methylmorphine, is an alkaloid found in the opium poppyPapaver somniferum var.
Opium poppy has been cultivated and utilized throughout human history for a variety of medicinal analgesic, anti-tussive and anti-diarrheal and hypnotic properties linked to the diversity of its active components, which include morphine, codeine and papaverine. Until the beginning of the 19th century, raw opium was used in diverse preparations known as laudanum see Thomas de Quincey 's Confessions of an English Opium-Eaterand paregoric elixirsa number of which were popular in England since the beginning of the 18th century; the original preparation seems to have been elaborated in Leidenthe Netherlands around by a chemist named Lemort; in the London Pharmacopoeia mentions an Elixir Asthmaticum, replaced by the term Elixir Paregoricum "pain soother" in The progressive isolation of opium's several active components opened the path to improved selectivity and safety of the opiates-based pharmacopeia.
Codeine is the most widely used opiate in the world,   and is one of the most commonly used drugs overall according to numerous reports by organizations including the World Health Organization and its League of Nations predecessor agency. It is one of the most effective orally administered opioid analgesics and has a wide safety margin. While codeine can be directly extracted from opium, its original source, most codeine is synthesized from the much more abundant morphine through the process of O- methylation  through a process first completed in the late 20th century by Robert C.
Corcoran and Junning Ma. They quickly succeeded using petroleum or coal tar and a process developed at the United States' National Institutes of Health.
Numerous codeine salts have been prepared since the drug was discovered. The most commonly used are the hydrochloride freebase conversion ratio 0. The latter was introduced as Codeonal inindicated for pain with nervousness.
- PAINKILLERS: A SHORT HISTORY
Codeine hydrochloride is more common worldwide and the citrate, hydroiodide, hydrobromide, tartrate, and other salts are also seen. Brand named as Phenergan with Codeine or in generic form as promethazine with codeine. In the s it started to be mixed with soft drinks to be used as a recreational drug and was called 'syrup', 'lean', or ' purple drank '.
Drug abuse screening programs generally test urinehairsweat or saliva. Many commercial opiate screening tests directed at morphine cross-react appreciably with codeine and its metabolites, but chromatographic techniques can easily distinguish codeine from other opiates and opioids. It is important to note that codeine usage results in significant amounts of morphine as an excretion product.
Furthermore, heroin contains codeine or acetyl codeine as an impurity and its use will result in excretion of small amounts of codeine. Poppy seed foods represent yet another source of low levels of codeine in one's biofluids.
Australia[ edit ] In Australia, Since February 1,preparations containing codeine are not available without a prescription. Schedule 8 preparations are subject to the strictest regulation of all medications available to consumers. A similar tablet called "A. Both tablets are kept behind the counter and must be dispensed by a pharmacist who may limit quantities. Names of many codeine and dihydrocodeine products in Canada tend to follow the narcotic content number system Tylenol With Codeine No.
Codeine became a prescription-only medication in the province of Manitoba on February 1, A pharmacist may issue a prescription, and all purchases are logged to a central database to prevent overprescribing.
In Austriathe drug is listed under the Suchtmittelgesetz in categories corresponding to their classification under the Single Convention on Narcotic Drugs.
Dispensing of products containing codeine and similar drugs dihydrocodeinenicocodeine, benzylmorphine, ethylmorphine etc.