Monograph
N06BA02 - Dexamfetamine |
Propably not porphyrinogenic |
PNP |
Rationale
Dexamfetamine is partially metabolized in the liver, and the main isoenzyme involved is CYP 2D6. No relevant interactions of amfetamine or dexamfetamine indicating CYP-induction or inhibition of CYP 3A4 or 2C9. Anorexia is a common side effect of amfetamine that may be potentially porphyrinogenic through reduction in caloric intake.
Chemical description
Dexamphetamine is the dextrorotatory (S) isomer of amphetamine.
Therapeutic characteristics
Dexamphetamine (dextroamphetamine sulfate) alone and in fixed-combination preparations with dextroamphetamine saccharate, amphetamine aspartate, and amphetamine sulfate is used in the treatment of narcolepsy and as an adjunct to psychological, educational, social, and other remedial measures in the treatment of ADHD in children, adolescents, and adults. Administered orally. Common adverse reactions of dexamfetamine that can be confused with an acute porphyric attack are anorexia, abdominal cramps and other gastrointestinal disturbances, tachycardia, and increased blood pressure. Also nervousness, restlessness and irritability that can be followed by depression and fatigue. Anorexia is a common side effect of amfetamine that may be potentially porphyrinogenic through reduction in caloric intake.
Metabolism and pharmacokinetics
Amphetamines are partially metabolised in the liver but a considerable fraction may be excreted in the urine unchanged. Elimination is increased in acidic urine. After high doses, elimination in the urine may take several days. Amphetamine is listed by Rendic (2002) and de la Torre (2004) as a substrate and an inhibitor of CYP 2D6. Observed drug-drug interactions are reported to be primarily pharmacodynamic interactions (Markowitz, 1999).
IPNet drug reports
No.
References
# | Citation details | PMID |
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* | Scientific articles | |
1. | de la Torre, R., Farre, M. et al. Clinical pharmacokinetics of amfetamine and related substances: monitoring in conventional and non-conventional matrices. Clin Pharmacokinet 2004;43(3):157-85.
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2. | Markowitz, J.S., Morrison, S.D., et al. Drug interactions with psychostimulants.
Int Clin Psychopharmacol. 1999;14(1):1-18. |
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3. | Rendic, S. Summery of information on human CYP enzymes: human P450 metabolism. Drug metabolism reviews 2002; 34(1&2), 83-448.
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* | Drug reference publications | |
4. | McEvoy, G.K., editor. Dextroamphetamine Saccharate, Dextroamphetamine Sulfate. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (02.03.10).
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5. | Sweetman, S.C., editor. Martindale: The complete drug reference. Dexamfetamine Sulfate. Pharmaceutical Press 2009.
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