Monograph
P02CF01 - Ivermectin |
Propably not porphyrinogenic |
PNP |
Side effects
Ivermectin has no physiological actions or side effects of relevance to acute porphyria.
Rationale
Ivermectin is not an inhibitor or an inducer of any major CYP enzymes, and therefore no pharmacokinetic porphyrinogenic effects are suspected.
Chemical description
Macrocyclic lactone, a semisynthetic derivative of avermectins produced by Streptomyces avermitilis.
Therapeutic characteristics
Ivermectin is used in the treatment of strongyloidiasis of the intestinal tract and of onchocerciasis. It is also used in the treatment of scabies or pediculosis in patients where topical skin treatment is met with difficulties.
It is administered orally usually as a single dose that may be repeated after 14 days.
Metabolism and pharmacokinetics
Ivermectin is highly lipid soluble and is widely distributed within the body. It has an elimination half-life of about 18 hours. Ivermectin is a substrate of P-glycoprotein and of CYP 3A4 (Zeng 1998, Kiki-Mvouaka 2010), and to a minor degree CYP 2D6 and CYP 2E1 (Prescribing information, Merck & Co).
The findings of in vitro studies using human liver microsomes suggest that clinically relevant concentrations of ivermectin do not significantly inhibit the metabolizing activities of CYP3A4, CYP2D6, CYP2C9, CYP1A2, and CYP2E1 (Prescribing information, Merck & Co).
Ivermectin did not induce the expression of CYP 1A2, 2B6, 2C9 or 3A4 in cultured human hepatocytes (SPC Soolantra).
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | The pharmacokinetics and interactions of ivermectin in humans--a mini-review.
Canga A G, Prieto AMS et al. AAPS J. 2008;10(1):42-6. |
18446504 |
| 2. | Role of P-glycoprotein in the disposition of macrocyclic lactones: A comparison between ivermectin, eprinomectin, and moxidectin in mice.
Kiki-Mvouaka S, Menez C et al. Drug Metab Dispos. 2010 Apr;38(4):573-80. |
20089736 |
| 3. | Identification of cytochrome P4503A4 as the major enzyme responsible for the metabolism of ivermectin by human liver microsomes.
Zeng Z, Andrew NW et al. Xenobiotica. 1998 Mar;28(3):313-21. |
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| * | Drug reference publications | |
| 4. | Micromedex 2.0 (electronic version). Ivermectin. (Drugdex System). (11.02.2014).
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| * | Summary of Product Characteristics | |
| 5. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Soolantra.
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| * | Other sources | |
| 6. | Prescribing information. STROMECTOL(R) oral tablets, ivermectin oral tablets. Merck & Co, Inc, Whitehouse Station, NJ, 2009.
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