Codeine
NAME OF DRUG: Codeine(Acetaminophen w/Codeine, Actifed w/Codeine, Ambenyl, Aspirin w/Codeine, Broncholate CS, Capital and Codeine Oral Solution, Codimal, Demetane-DC, Fiorinal w/Codeine, Fiorinal, Isoclor Expectorant, Nucofed Expectorant, Par-Glycerol-C, Pediacof, Phenaphen w/Codeine, Phenergan , Poly-Histine, Promethazine VC w/Codeine, Robitusssin w/Codeine, Soma w/Codeine, Triaminic Expectorant w/Codeine, Tussar-2, Tussar SF, Tussi-Organiden, Tylenol w/Codeine, Methylmorphine, Morphine Methyl Ether, 7,8-Dehydro-4,5-epoxy-6-hydroxy-3-methoxy-N-methylmophinan) |
| PHYSICAL CHARACTERISTICS: Codeine is a white crystalline powder. It is available by prescription in liquid or tablet form. |
| DOSAGE/OCCURRENCE/USAGE: Codeine is a narcotic analgesic. It is used to relieve mild to moderate pain and as an antitussive for the relief of coughing. It is found in opium from the opium poppy (papaver somniferum). Codeine was first separated from opium in 1832. It prepared commercially by the process of the 3-O-methylation of morphine. Codeine is less potent than morphine, typically 1/10-1/6 on weight basis. Codeine is available as a sulfate or phosphate salt. It can be administered either orally or by subcutaneous injection. The usual single dose is 15-60 mg or a total daily dose of 60-240 mg. Codeine is usually combined with drugs such as nonnarcotic analgesics and antihistamines. |
| BLOOD CONCENTRATIONS VS. DOSAGE: Codeine is administered either orally or by intramuscular injection. When taken orally, a single 15 mg dose produced an average peak serum concentration of 30 ng/mL after 2 hours. A single 60 mg dose of codeine sulfate generated a peak concentration of 110 ng/mL but than quickly declined. A dose of 60 mg of codeine sulfate with 600 mg of acetaminophen produced a peak average of 134 ng/mL at one hour (half-life 2.4 hours). Morphine concentrations reached a peak of 7 ng/mL at 1.5 hours. When administered by intramuscular injection, a single 65 mg dose had a peak plasma concentration range of 195-340 ng/mL at 15-60 minutes. Blood concentration of codeine when administered orally is much lower than when administered by injection because of first pass metabolism. |
| URINE EXCRETION RATE: Codeine and its metabolites, morphine and norcodeine, are excreted as free drug and glucuronide conjugates. Up to 95% of a single dose of codeine is excreted within 48 hours. |
| METABOLITES: Morphine, Norcodeine |
| TOXICITY: Symptoms of codeine toxicity include unconsciousness and convulsions. Death is from respiratory failure and occurs in 2-4 hours. The lethal adult dose can be 0.5-1.0 g. Lethal plasma concentration is 200 ng/mL. Naloxone is used as an antidote. |
| REFERENCES: Baselt R.C. Disposition of Toxic Drugs and
Chemicals in Man, Second Edition. Davis, Calif.: Biomedical Publications, 1982. Clarke E.C. Isolation and Identification of Drugs. London: The Pharmaceutical Press, 1969. Goldberger, Bruce A. Opiates Abused Drugs Monograph Series. Ed. Caplan, Yale H. Irving: Abbott Laboratories, 1994. |