Acetamine codeine high how much


CodeineDrug groupsOpioid Codeine is a pain reliever and antitussive agent from the group of opioids for the symptomatic treatment of pain and dry coughs. Codeine can make you tired or sleepy and must not be taken with alcohol or other central depressant substances. In addition, as with other opioids, there is a potential for abuse and dependence due to the psychotropic effect. Other possible adverse effects include constipation, nausea, and shortness of breath.

Synonymous: CodeinumPhEur, Codeini phosphas hemihydricusPhEur, methylmorphine, codeine phosphate

Products

Codeine is available alone or in combination with other active ingredients in the form of tablets, effervescent tablets, capsules, dragees, syrups, drops, bronchial lozenges and suppositories. For the treatment of pain, it is also combined with paracetamol (see under Codeine Paracetamol).

Structure and properties

Codeine (C.18H21NO3, Mr = 299.36 g / mol) O-methylated morphine and comes naturally in opium from the opium poppy (Papaver somniferum) in front. It is available as a base in the form of a white powder or as crystals that are soluble in boiling water. It is usually contained in medicinal products as codeine phosphate hemihydrate (Codeini phosphas hemihydricus), codeine · H3PO4 0.5 H2O, which is easily soluble in water.

Effects

Codeine (ATC R05DA04) has central pain-relieving, cough-relieving, calming, euphoric and constipating properties. The effects are based on the binding to opioid receptors. The cough-relieving effects are attributed to an inhibition of the cough center in the brain stem.

Codeine is widely used and prominently mentioned in the WHO level scheme, but its medical use is not undisputed in the scientific literature. For example, some publications ask whether codeine is actually effective against coughs. The variable pharmacokinetics, which presumably lead to some patients responding excessively and others not at all, is also controversial (see below). There is a lack of modern admission studies.

Indications

As a cough suppressant for dry coughs and as a pain reliever for pain. Codeine can be used to treat diarrhea, but is not officially approved for it in Switzerland.

abuse

Codeine is abused as a euphoric and depressant intoxicant. Information on this topic can be found under the article → Abuse of cough syrup and opioids.

dosage

According to the medicinal product information.

Contraindications

Numerous precautions must be taken when using codeine. They can be found in the specialist information for medicinal products.

Interactions

Central depressant drugs such as sedatives, sleeping pills, antidepressants, neuroleptics or alcohol as well as anticholinergics can increase the undesirable effects of codeine. MAOIs are contraindicated. The simultaneous use of expectorants is not indicated.

According to the doctrine, codeine is demethylated as a prodrug by CYP2D6 to form the active ingredient morphine. This would mean that codeine cannot fully develop its effects in a poor metabolizer of CYP2D6. Conversely, an ultra-rapid metabolizer could suffer an overdose because it produces large amounts of morphine and drug interactions via CYP2D6 would be possible. However, it is believed by some skilled in the art that codeine-6-glucuronide, which is formed by conjugation, is the active agent (e.g. Vree et al., 2000). Codeine is also demethylated to norcodeine via CYP3A4 and partially excreted unchanged.

unwanted effects

Possible adverse effects include allergic reactions, histamine release, itching, low blood pressure, skin reactions, nausea, vomiting, constipation, dry mouth, headache, drowsiness, sleep disorders, shortness of breath, addiction and abstinence symptoms.

see also literature
  • American Academy of Pediatrics. Committee on Drugs. Use of codeine- and dextromethorphan-containing cough remedies in children. Pediatrics. 1997, 99 (6), 918-20 Pubmed
  • Armstrong S.C., Cozza K.L. Pharmacokinetic drug interactions of morphine, codeine, and their derivatives: theory and clinical reality, part I. Psychosomatics, 2003, 44 (2), 167-71 Pubmed
  • Medicinal product information (CH)
  • Bolser D.C., Davenport P.W. Codeine and cough: an ineffective gold standard. Curr Opin Allergy Clin Immunol, 2007, 7 (1), 32-6 Pubmed
  • Derry S., Moore R.A., McQuay H.J. Single dose oral codeine, as a single agent, for acute postoperative pain in adults. Cochrane Database Syst Rev, 2010, 14 (4), CD008099 Pubmed
  • European Pharmacopoeia PhEur
  • Fagerlund T.H., Braaten O. No pain relief from codeine ...? An introduction to pharmacogenomics. Acta Anaesthesiol Scand, 2001, 45 (2), 140-9 Pubmed
  • Madadi P., Koren G. Pharmacogenetic insights into codeine analgesia: implications to pediatric codeine use. Pharmacogenomics, 2008, 9 (9), 1267-84 Pubmed
  • Nauta M., Landsmeer M.L., Koren G. Codeine-acetaminophen versus nonsteroidal anti-inflammatory drugs in the treatment of post-abdominal surgery pain: a systematic review of randomized trials. Am J Surg, 2009, 198 (2), 256-61 Pubmed
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  • Smith L.A., Moore R.A., McQuay H.J., Gavaghan D. Using evidence from different sources: an example using paracetamol 1000 mg plus codeine 60 mg. BMC Med Res Methodol, 2001 Pubmed
  • Tremlett M., Anderson B.J., Wolf A. Pro-con debate: is codeine a drug that still has a useful role in pediatric practice? Pediatr Anaesth, 2010, 20 (2), 183-94 Pubmed
  • Vree T.B., van Dongen R.T., Koopman-Kimenai P.M. Codeine analgesia is due to codeine-6-glucuronide, not morphine. Int J Clin Pract, 2000, 54 (6), 395-8 Pubmed
  • Williams D.G., Hatch D.J., Howard R.F. Codeine phosphate in pediatric medicine. Br J Anaesth, 2001, 86 (3), 413-21 Pubmed
author

Conflicts of Interest: None / Independent. The author has no relationships with the manufacturers and is not involved in the sale of the products mentioned.

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