Monograph
N05CF03 - Zaleplon |
Propably not porphyrinogenic |
PNP |
Rationale
It is not an inhibitor or an inducer of CYP2C9 or any other major CYP enzymes in vivo.
Chemical description
Zaleplon is a pyrazolopyrimidine hypnotic.
Therapeutic characteristics
Zaleplon is indicated for the treatment of patients with insomnia who have difficulty falling asleep. It is indicated only when the disorder is severe, disabling or subjection the individual to extreme distress.
Metabolism and pharmacokinetics
Zaleplon is primarily metabolised by aldehyde oxidase with minor contribution by CYP3A4 (Dooley 2000 and SPC) to three inactive metabolites (Hesse 2003). The half-life elimination is approximately 1 hour.
When co-administered zaleplon (single-dose) did not have any significant effect on the pharmacokinetics of ibuprofen (single-dose) (Hesse 2003 and Sanchez 2000), a CYP2C9 substrate (SPC). This indicates that zaleplon is not a an inhibitor or an inducer of CYP2C9.
Zaleplon is not listed as an inducer or inhibitor of any major CYP enzymes (FDA, Hisaka 2010, Isoherranen 2009 and Pelkonen 2008) and no drug-drug interaction with zaleplon as a perpetrator has been reported in the literature (Interaksjoner and SPC). This also indicate that zaleplonis not an inhibitor or an inducer of any major CYP enzymes.
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Zaleplon: a review of its use in the treatment of insomnia.
Dooley M, Plosker GL. Drugs. 2000 Aug;60(2):413-45. |
10983740 |
| 2. | Clinically important drug interactions with zopiclone, zolpidem and zaleplon.
Hesse LM, von Moltke LL, Greenblatt DJ. CNS Drugs. 2003;17(7):513-32. |
12751920 |
| 3. | Prediction of pharmacokinetic drug-drug interaction caused by changes in cytochrome P450 activity using in vivo information.
Hisaka A, Ohno Y, et al. Pharmacol Ther. 2010 Feb;125(2):230-48. |
|
| 4. | Qualitative analysis of the role of metabolites in inhibitory drug-drug interactions: literature evaluation based on the metabolism and transport drug interaction database.
Isoherranen N, Hachad H, et al. Chem Res Toxicol. 2009 Feb;22(2):294-8. |
|
| 5. | Inhibition and induction of human cytochrome P450 enzymes: current status.
Pelkonen O, Turpeinen M, et al. Arch Toxicol. 2008 Oct;82(10):667-715. |
18618097 |
| 6. | Absence of an interaction between ibuprofen and zaleplon.
Sanchez Garcia P, Carcas A, et al. Am J Health Syst Pharm. 2000 Jun 15;57(12):1137-41. |
10911512 |
| * | Government bodies | |
| 7. | U.S Food and Drug Administration (FDA).
|
|
| * | Drug interaction databases | |
| 8. | Interaksjoner. zaleplon
|
|
| * | Summary of Product Characteristics | |
| 9. | Norwegian medicines agency. Summary of Product Characteristics (SPC). Ibuprofen.
|
|
| 10. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Zaleplon.
|
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