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Dihydrocodeine: Difference between revisions
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Dihydrocodeine is also known as ''Drocode, Paracodeine and Parzone.'' Its many brand names include ''Synalgos DC, Panlor DC, Panlor SS, Contugesic, New Bron Solution-ACE, Huscode, Drocode, Paracodin,''<ref name=":0">https://web.archive.org/web/20190525105330/https://www.gelbe-liste.de/wirkstoffe/Dihydrocodein_1788</ref> ''Codidol, Dehace, Didor Continus, Dicogesic, Codhydrine, Dekacodin, DHC,''<ref name=":0" /> ''DH-Codeine, Didrate, Dihydrin, Hydrocodin, Makatussin, Nadeine, Novicodin, Rapacodin, Fortuss, Paramol, Remedeine, Dico and DF-118''. | Dihydrocodeine is also known as ''Drocode, Paracodeine and Parzone.'' Its many brand names include ''Synalgos DC, Panlor DC, Panlor SS, Contugesic, New Bron Solution-ACE, Huscode, Drocode, Paracodin,''<ref name=":0">https://web.archive.org/web/20190525105330/https://www.gelbe-liste.de/wirkstoffe/Dihydrocodein_1788</ref> ''Codidol, Dehace, Didor Continus, Dicogesic, Codhydrine, Dekacodin, DHC,''<ref name=":0" /> ''DH-Codeine, Didrate, Dihydrin, Hydrocodin, Makatussin, Nadeine, Novicodin, Rapacodin, Fortuss, Paramol, Remedeine, Dico and DF-118''. | ||
Dihydrocodeine is available as tablets, solutions, elixirs, and other oral forms. In some countries, the drug is available as an injectable solution for deep subcutaneous and intra-muscular administration. As with codeine, intravenous administration should be avoided as it could result in anaphylaxis and dangerous pulmonary edema. Dihydrocodeine is available in suppository form on prescription. | Dihydrocodeine is available as tablets, solutions, elixirs, and other oral forms. In some countries, the drug is available as an injectable solution for deep subcutaneous and intra-muscular administration. As with codeine, intravenous administration should be avoided as it could result in anaphylaxis and dangerous pulmonary edema. Dihydrocodeine is available in suppository form on prescription.{{citation needed}} | ||
Dihydrocodeine is used as an alternative or adjunct to [[codeine]] and is similar in chemical structure. Depending on individual metabolism, dihydrocodeine is 100 to 150 percent as strong as codeine. | Dihydrocodeine is used as an alternative or adjunct to [[codeine]] and is similar in chemical structure. Depending on individual metabolism, dihydrocodeine is 100 to 150 percent as strong as codeine.{{citation needed}} | ||
==Chemistry== | ==Chemistry== | ||
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==Pharmacology== | ==Pharmacology== | ||
Dihydrocodeine exerts its effects by binding to and activating the [[Opioid#Mu_.28.CE.BC.29|μ-opioid]] [[receptor]]. This occurs because opioids structurally mimic endogenous endorphins which are naturally found within the body and also work upon the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their [[physical euphoria|euphoria]], [[pain relief]] and [[anxiolytic]] effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement. | Dihydrocodeine exerts its effects by binding to and activating the [[Opioid#Mu_.28.CE.BC.29|μ-opioid]] [[receptor]]. This occurs because opioids structurally mimic endogenous endorphins which are naturally found within the body and also work upon the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their [[physical euphoria|euphoria]], [[pain relief]] and [[anxiolytic]] effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement.{{citation needed}} | ||
Dihydrocodeine is metabolized via CYP2D6 to the active metabolite dihydromorphine, which has a potency similar to morphine. Other weakly active metabolites include nordihydrocodeine (which is formed via CYP3A4) and dihydrocodeine-6-glucuronide.<ref>Kirkwood LC, Nation RL, Somogyi AA. Characterization of the human cytochrome P450 enzymes involved in the metabolism of dihydrocodeine. Br J Clin Pharmacol. 1997;44:549-55.</ref> Although dihydrocodeine does have extremely active metabolites in the form of dihydromorphine and dihydromorphine-6-glucuronide, these metabolites are produced in such a small amount that they do not have clinically important effects.<ref>The role of active metabolites in dihydrocodeine effects (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/12665158</ref> | Dihydrocodeine is metabolized via CYP2D6 to the active metabolite dihydromorphine, which has a potency similar to morphine. Other weakly active metabolites include nordihydrocodeine (which is formed via CYP3A4) and dihydrocodeine-6-glucuronide.<ref>Kirkwood LC, Nation RL, Somogyi AA. Characterization of the human cytochrome P450 enzymes involved in the metabolism of dihydrocodeine. Br J Clin Pharmacol. 1997;44:549-55.</ref> Although dihydrocodeine does have extremely active metabolites in the form of dihydromorphine and dihydromorphine-6-glucuronide, these metabolites are produced in such a small amount that they do not have clinically important effects.<ref>The role of active metabolites in dihydrocodeine effects (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/12665158</ref> | ||
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*'''Austria:''' Dihydrocodeine is legal for medical use under the AMG (Arzneimittelgesetz Österreich) and illegal when sold or possessed without a prescription under the SMG (Suchtmittelgesetz Österreich).{{citation needed}} | *'''Austria:''' Dihydrocodeine is legal for medical use under the AMG (Arzneimittelgesetz Österreich) and illegal when sold or possessed without a prescription under the SMG (Suchtmittelgesetz Österreich).{{citation needed}} | ||
*'''Germany:''' Dihydrocodeine is a controlled substance under Anlage III of the BtMG. It can only be prescribed on a narcotic prescription form. There is an exception for preperations, containing up to 2,5% or 100mg dihydrocodeine per unit, which can be prescripted on a regular prescription, if not prescripted to an alcohol or drug dependent person.<ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html</ref> | *'''Germany:''' Dihydrocodeine is a controlled substance under Anlage III of the BtMG. It can only be prescribed on a narcotic prescription form. There is an exception for preperations, containing up to 2,5% or 100mg dihydrocodeine per unit, which can be prescripted on a regular prescription, if not prescripted to an alcohol or drug dependent person.<ref>http://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html</ref> | ||
*'''Hong Kong''' | *'''Hong Kong:''' In Hong Kong, dihydrocodeine is regulated under Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance. It can only be used legally by health professionals and for university research purposes. A pharmacist can dispense Dihydrocodeine when furnished with a doctors prescription. Anyone who supplies the substance without a prescription can be fined $10000 (HKD). The penalty for trafficking or manufacturing the substance is a $5,000,000 (HKD) fine and life imprisonment. Possession of the substance for consumption, without a licence from the Department of Health, is illegal and carries a $1,000,000 (HKD) fine and/or 7 years imprisonment.{{citation needed}} | ||
*'''Japan''' | *'''Japan:''' In Japan, dihydrocodeine is available without a prescription; used in cough medicines such as New Bron Solution-ACE. Dihydrocodeine is used as an antitussive in many products as a Dextromethorphan alternative. Medicines in Japan which contain dihydrocodeine are coupled with caffeine to offset the sedative effects and discourage recreational use. Cough medicines containing dihydrocodeine are controlled similarly to dextromethorphan in the United States, in that its sale is strictly limited by purchase quantity and is restricted to persons 20 and older for purchase.{{citation needed}} | ||
*'''Switzerland''' | *'''Switzerland:''' In Switzerland, dihydrocodeine is legal in limited quantities if the buyer is 18 years or older. After age 30, dihydrocodeine is accessible in unlimited quantities.{{citation needed}} | ||
*'''United Kingdom''' | *'''United Kingdom:''' In the United Kingdom, dihydrocodeine is a Class B drug; but, it is available over-the-counter in small amounts (less than 8 mg), when combined with paracetamol (see co-dydramol). Dihydrocodeine is listed in Schedule 5 of the Misuse of Drugs Regulations 2001 whereby it is exempt from prohibition on possession provided that it is in the form of a single preparation not being designed for injection and less than 100 mg (calculated as free base) or with a total concentration less than 2.5% (calculated as free base). Illegal possession of dihydrocodeine can result in up to 5 years in prison and/or an unlimited fine.{{citation needed}} | ||
*'''United States''' | *'''United States:''' In the USA, dihydrocodeine is a DEA Schedule II substance, although preparations containing small amounts of dihydrocodeine are classified as Schedule III or Schedule V, depending on the concentration of dihydrocodeine relative to other active constituents, such as paracetamol (acetaminophen). This scheduling is similar to the UK's. The DEA's ACSCN for dihydrocodeine free base and all salts is 9120. The 2013 annual aggregate manufacturing quota is 250 kilos.{{citation needed}} | ||
==See also== | ==See also== | ||