Dihydrocodeine is a semi-synthetic opioid analgesic prescribed for severe pain or dyspnea, or as antitussive, either alone or compounded with paracetamol (as in co-dydramol) or aspirin. It was developed in Germany in 1908 and was first marketed in 1911.
Generally available as tablets, solutions, herbs, and other oral forms, dihydrocodeine is also available in some countries as an injection solution for deep subcutaneous and intra-muscle administration. As with codeine, intravenous administration should be avoided, as it may cause life-threatening anaphylaxis and pulmonary edema. In the past, dihydrocodeine suppositories were used. Dihydrocodeine is available in suppository form on prescription.
Dihydrocodeine is used as an alternative or addition to codeine for the aforementioned indications. It is available as the following salts, in the order of approximate use frequency sequences: bitartrate, phosphate, hydrochloride, tartrate, hydroiodide, methyliodide, hydrobromide, sulfate, and thiocyanate. Salt for free base conversion factor was 0.67 for bitartrate, 0.73 for phosphate, and 0.89 for hydrochloride.
Dihydrocodeine was developed during an intensive, more effective antitussive international search, primarily to help reduce the spread of tuberculosis, pertussis, pneumonia, and similar diseases in the air, in the years from c.a. 1895 to 1915. The chemical structure is similar to codeine. Dihydrocodeine is twice as strong as codeine. Although dihydrocodeine has a very active metabolite, in the form of dihydromorphine and dihydromorphine-6-glucuronate (one hundred times stronger), this metabolite is produced in small quantities so that it does not have a clinically significant effect.
Dihydrocodeine is also a member of the original and chemical base of a number of similar semi-synthetic opioids such as acetylcycrocin, dihydrocodeine enol acetate, dihydroisocodine, nicocodeine, and nicodicodeine.
Video Dihydrocodeine
Indication
Approved indications for dihydrocodeine are moderate to severe pain management and cough and shortness of breath. As with other drugs in this group, antitussive doses tend to be less than analgesic doses, and dihydrocodeine is a strong cough suppressant like all other members of the immediate codeine family (see below) and their cousins ​​are hydrocodone, oxycodone and ethylmorphine, intact opium preparation, and strong opioid hydromorphone.
For use against pain, dihydrocodeine is usually formulated as a tablet or capsule containing 15-16 mg or 30-32 mg with or without other active ingredients such as aspirin, paracetamol (acetaminophen), ibuprofen, or others.
Controlled-controlled dilydrocodeine is available for pain and cough, as shown below, such as wax tablets containing 60 to 120 mg of the drug. Some formulations, intended to be used against coughs and the like, have other active ingredients such as antihistamines, decongestants and more. Other oral formulations, such as effervescent powder packages, sublingual drops, elixirs and the like are also available in many locations.
Suntydrocodeine injection is most commonly given as a deep subcutaneous injection.
Maps Dihydrocodeine
Preparation and availability
Table-topped dihydrocodeine products in many European and Pacific Rim countries generally contain 2-20 mg of dihydrocodeine per unit dose combined with one or more other active ingredients such as paracetamol (acetaminophen), aspirin, ibuprofen, antihistamines, decongestants , vitamins, medicinal herbs, and other ingredients. In a subset of these countries and foreign goods, 30 mg tablets and controlled tablets of 60 mg are available on the table and chemists may be able to properly expend 90 and 120 mg strength at their discretion.
In the United States, the most common analgesic brands with dihydroxine are: DHC Plus (16 and 32 mg), Panor SS (32 mg), ZerLor (32 mg), DC Panor (16 mg) and Synalgos DC (16 mg). This combination product also includes paracetamol (acetaminophen) and caffeine. Aspirin is used in the case of DC Synalgos.
Dihydrocodeine is sometimes marketed in combination with paracetamol as co-dydramol (BAN) to provide greater pain relief than single-use agents (see synergy example).
In the UK and other countries, 30 mg tablets containing only dihydrocodeine as active ingredients are available, as well as Dihydrocodeine 40mg tablets available in the UK as DF-118 Forte.
The original dihydrocodeine product, Paracodin, is a dihydrocodeine hydroiodid herb also available as Tussionex style suspension in many European countries.
In many European countries and elsewhere in the world, the most frequently found preparation of dihydrocodeine is an extended release tablet made by wrapping granules from a mixture of ingredients, almost always using dihydrocodeine bitartrate salts, of four different sizes in wax-based binder. The usual strengths are 60, 90, and 120 mg. Common trade names for extended release tablets are Didor Continus, Codidol, Codi-Contin, Dicodin (made in France and main products containing tartrate salt), Contugesic, DHC, and DHC Continus.
Dihydrocodeine is available in Japan as a tablet containing 2.5 mg of dihydrocodeine phosphate and caffeine, decongestant d, l-methylephedrine HCl, and antihistamine chlorpheniramine, and frothy granule packages such as Alka-Seltzer with 10 mg dihidrocodeine with lysozyme and chlorpheniramine, marketed for OTC sales as New Bron Solution-ACE. Both of these formulations may have contained phenyltoloxamine citrate as an antihistamine component.
Elsewhere in Pacific Rim, Dicogesic is analogous to Glaxo/Smith-Kline DF-118.
Manufacturer of New Bron Solution-ACE; SS Pharmaceutical Co., Ltd., also markets ibuprofen with a dihydrocodeine product called S.Tac EVE, which also includes d, l-methylephedrine HCl, chlorpheniramine, anhydrous caffeine, and vitamins B1 and C.
The Panlor series is manufactured by Pan-American Laboratories of Covington, Louisiana, and they also market some of the prescription-based coughs of dihidrokodein cough in the United States.
Side effects
Like other opioids, physical and psychological tolerance and dependence develop with the use of recurrent dihydrocodeine. All opioids can impair the mental or physical abilities required for the performance of potentially hazardous tasks such as driving or operating the machine if taken in large doses.
Itching and redness and other effects of blood vessel dilation are also common side effects, due to the release of histamine in response to drugs using one or more receptor types in the CNS or other responses elsewhere in the body. First-generation antihistamines such as tripelennamine (Pyrabenzamine), clemastine (Tavist), hydroxyzine (Atarax), diphenhydramine (Benadryl), cyproheptadine (Periactin), brompheniramine (Dimetapp), chlorphenamine (Chlor-Trimeton), doxylamine (NyQuil) and phenyltoloxamine (Percofiic Original Formula) not only combats the side effects of histamine, but is analgesic (potential) in varying degrees. Promethazine antihistamines (Phenergan) may also have a positive effect on hepatic metabolism of dihydrocodeine as well as with codeine. Promethazine high doses can disrupt most other opioids with the exception of the pethidine family (Demerol and the like) by this mechanism or other unknowns.
Like all drugs, side effects depend on the person taking the drug. They can range from mild to extreme, from headaches to difficulty breathing.
Constipation is a side effect of dihydrocodeine and almost all opioids are almost universal. This results from peristaltic slowing in the intestine and is the reason for dihydrocodeine, ethylmorphine, codeine, opium preparation, and morphine used to stop diarrhea and combat irritable bowel syndrome (IBS) in the form of diarrhea and cyclic and other conditions that cause hypermotility or intestinal cramps. Opioid/opioid preparations are often used as a last resort in which severe pain and bowel are organically loosened. It is generally preferable to treat IBS with a non-psycho-tropic opioid such as loperamide hydrochloride which remains contained in the intestine, thus not causing a drowsiness effect and allowing many people to work using machinery etc. For IBS, hyoscine butylbromide (UK Buscopan)) and mebeverine hydrochloride (Colofac) can be effective with or without opium-related compounds.
Rule
- AustraliaÃ,
- In Australia, dihydrocodeine is a pharmaceutical drug 'OTC Schedule 2 when compounded with aspirin and no other therapeutic active substance, does not exceed 5mg per tablet and a recommended dose of 10mg. No more than 25 units of dose are permitted under Schedule 2 rules for dihydrocodeine. This is a pharmacist class drug alone when supplemented with one or more other therapeutic active substances and does not exceed 15mg of dihidrocodeine per dose. Schedule 3 drugs, while still OTC, can only be issued after consultation with the pharmacist. This is a Schedule 4 drug (prescribed only) when aggravated with one or more other therapeutic active substances and does not exceed 100mg dihydrocodeine per dose. The preparation of a single dihydroxinein material is included in the Schedule 8 regulation and requires a legal, official prescription from the government.
- Hong KongÃ,
- In Hong Kong, dihydrocodeine is set out under Schedule 1 of Chapter 132 of the Hong Kong Dangerous Drug Act . This can only be used legally by health professionals and for university research purposes. A pharmacist can remove Dihydrocodeine when equipped with a prescription. Anyone who supplies nonprescription substances can be fined $ 10,000 (HKD). Penalties for trading or manufacturing substance are a $ 5,000,000 (HKD) fine and life imprisonment. Ownership of substance for consumption, without license from the Ministry of Health, is illegal and carries a fine of $ 1,000,000 (HKD) or 7 years in prison.
- Japan
- In Japan, dihydrocodeine is available without a prescription; used in cough medicine such as New Bron Solution-ACE. Dihydrocodeine is used as an antitussive in many products as an alternative to Dextromethorphan. Drugs in Japan containing dihydrocodeine are combined with caffeine to offset the effects of sedatives and prevent recreational use. Hydrocodeine-containing coughs are controlled similarly to dextromethrophan in the United States, as sales are strictly limited by the number of purchases and are restricted to persons aged 20 and over to be purchased.
- United Kingdom
- In the UK, dihydrocodeine is a Class B drug; however, are available over-the-counter in small amounts (less than 8 mg), when combined with paracetamol (see co-dydramol). Dihydrocodeine is listed in List 5 of the Drug Abuse Act 2001 which is exempt from the prohibition on ownership provided that in the form of a single preparation not designed for injection and less than 100 mg (calculated as a free base) or with a total concentration of less than 2.5% (calculated as base free). The illegal possession of dihydrocodeine can lead to 5 years in prison or an unlimited fine.
- United States
- In the US, dihydrocodeine is a DEA Schedule II agent, although preparations containing small amounts of dihydrocodeine are classified as Schedule III or Schedule V, depending on the relative concentrations of dihydrocodeine with other active constituents, such as paracetamol (acetaminophen). Scheduling is similar to that in the UK. ACSCN DEA for dihydrocodeine free base and all salt is 9120. The annual aggregate production quota of 2013 is 250 kilos.
International treaties and controlled substance laws of most countries, such as Germany BetÃÆ'¤ubungsmittelgesetz , regulate dihydrocodeine at the same level as codeine. Drug-based dihydrocodeine drugs are mainly used where chronic pain patients can basically have OTC access to them provided they are registered with the provincial or national government as such patients.
Diluted-controlled dilydrocodeine is a non-prescription item in some places, especially 60 mg strength. A report by Ivo? Andor Organization in 2004 mentions Andorra, Spain, Gibraltar and Austria have varying levels of access to these products and other products such as dihydrocodeine, nicocodeine and codeine.
Chemistry
Dihydrocodeine is a parent drug of a fairly strong series of narcotics including, among others, hydrocodone, nicocodeine, nicodicodeine, thebaine and acetyldihydrocodeine.
While converting codeine into morphine is a difficult and unattractive task, dihydrocodeine can be converted to dihydromorphine with a very high yield (greater than 95%). Dihydromorphine is widely used in Japan. Dihydromorphine can be converted quantitatively into hydromorphone using potassium tert butoxide.
Dihydrocodeine may be suspected to be detected by the Froehde reagent.
Use of recreation
As dihydrocodeine can provide high euphoria when taken in higher doses than therapy, it is quite commonly abused recreation. Typical recreational doses can be anything from 70 to 500 mg, or, to users with tolerance, even more. Potentiators and adjuvants are often incorporated when dihydrocodeine is used in an unsupervised manner, especially carisoprodol, hydroxyzine and first generation antihistamines, both for enhancing effects and reducing side effects such as itching.
History
Two well-known users of dihydrocodeine are William S. Burroughs, who describes it as "twice as tough as codeine and almost as good as heroin" and Hermann GÃÆ'¶ring, which consumes up to 100 tablets (3 grams) of dihydrocodeine per day and is captured by Allied with large numbers drug in a suitcase, reportedly more than 20,000 tablets, probably most of the world's supply at the time. He also used morphine and oxycodone, starting with the use of therapeutic morphine after being injured in the groin during November 1923 Beer Hall Putsch in Munich and then using dihydrocodeine in the early 1930s for toothache.
Brand name
The brand names for dihydrocodeine products include Drocode, Paracodeine and Parzone. Many brand names include Rikodeine, Trezix, Synalgos DC, Panor DC, Panor SS, Contugesic, New Bron Solution-ACE, Huscode, Drocode, Paracodin, Codidol, Dehace, DHC Continus, Didor Continus, Dicogesic, Codhydrine, Dekacodin, DH- Codeine , Didrate, Dihydrin, Hydrocodin, Nadeine, Novicodin, Rapacodin, Fortuss, Paramol, Remedeine, Dico and DF-118.
References
External links
Media related to Dihydrocodeine on Wikimedia Commons
Source of the article : Wikipedia
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