Creato da Codeine30mgParacetam il 14/05/2007
Codeine30mgParacetamol
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Codeine 30mg-Paracetamol (INN) or methylmorphine is an opiate used for its analgesic, antitussive and antidiarrheal properties. It is marketed as the salts Codeine 30mg-Paracetamol sulfate and Codeine 30mg-Paracetamol phosphate. Codeine 30mg-Paracetamol hydrochloride is more commonly marketed in continental Europe and other regions.
Codeine 30mg-Paracetamol is an alkaloid found in opium in concentrations ranging from 0.3 to 3.0 percent. While Codeine 30mg-Paracetamol can be extracted from opium, most Codeine 30mg-Paracetamol is synthesized from morphine through the process of O-methylation.
Approved indications for Codeine 30mg-Paracetamol include:
* Cough, though its efficacy has been disputed.
* Diarrhea
* Mild to moderate pain
Codeine 30mg-Paracetamol is sometimes marketed in combination preparations with paracetamol (acetaminophen) as co-codamol, with aspirin co-codaprin or with ibuprofen. These combinations provide greater pain relief than either agent used singly (q.v. Drug Synergy).
In the United States, Codeine 30mg-Paracetamol is regulated by the Controlled Substances Act. It is a Schedule II controlled substance for pain-relief products containing Codeine 30mg-Paracetamol alone. In combination with aspirin or acetaminophen (paracetamol/tylenol) it is listed as Schedule III. Codeine 30mg-Paracetamol is also available outside the United States as an over-the-counter drug (Schedule V) in liquid cough-relief formulations. Internationally, Codeine 30mg-Paracetamol is a Schedule II drug under the Single Convention on Narcotic Drugs.
In the United Kingdom, Codeine 30mg-Paracetamol is regulated by the Misuse of Drugs Act 1971; it is a Class B Drug, except for concentrations of less than 8mg when combined with paracetamol - or 12.5mg when combined with ibuprofen - which are available in many over the counter preparations.
In Australia, New Zealand and Canada, Codeine 30mg-Paracetamol is regulated, however it is available without prescription in combination preparations from licensed pharmacists in doses up to 15 mg/tablet (8 mg/tablet in Canada).
Codeine 30mg-Paracetamol is considered a prodrug, since it is metabolised in vivo to the principal active analgesic agent morphine. It is, however, less potent than morphine since only about 10% of the Codeine 30mg-Paracetamol is converted. It also has a correspondingly lower dependence-liability than morphine.
Theoretically, a dose of approximately 200 mg (oral) of Codeine 30mg-Paracetamol must be administered to give equivalent analgesia to 30 mg (oral) of morphine (Rossi, 2004). It is not used, however, in single doses of greater than 60mg (and no more than 240 mg in 24 hours) since there is a ceiling effect.
The conversion of Codeine 30mg-Paracetamol to morphine occurs in the liver and is catalysed by the cytochrome P450 enzyme CYP2D6. Approximately 6–10% of the Caucasian population have poorly functional CYP2D6 and Codeine 30mg-Paracetamol is virtually ineffective for analgesia in these patients (Rossi, 2004). Many of the adverse effects, however, are still experienced. Also, some medications are CYP2D6 inhibitors and reduce or even completely eliminate the efficacy of Codeine 30mg-Paracetamol. The most notorious of these are the selective serotonin reuptake inhibitors, such as fluoxetine (Prozac) and citalopram (Celexa).
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