Description
Ivermectin is a semi-synthetic derivative of avermectins isolated from Streptomyces bacteria. The development of Ivermectin by William Campbell and Satoshi Omura was awarded the Nobel Prize in Medicine in 2015 - the substance has massive significance in the global fight against onchocerciasis (river blindness) and filariasis.
Per study reports Ivermectin binds to glutamate-gated chloride channels in nematodes and arthropods. Activation of these channels leads to hyperpolarization and paralysis of parasites. In mammals (including humans) this action is minimal due to blood-brain barrier protection - Ivermectin is considered very well tolerated in standard doses.
Clinically Ivermectin is used for treatment of strongyloidiasis, onchocerciasis, filariasis, scabies, and crusted scabies. Off-label research applications include rosacea and experimental antiviral research (2020-2022 in discussion for COVID-19, with mixed data).
Pharmacokinetically orally bioavailable with about 18-hour half-life. Single-dose application is clinical standard for most indications.
Known effects: in standard doses very well tolerated. At very high doses or in users with blood-brain barrier defects (e.g., certain Collie dog breeds) CNS effects possible.
You can order Ivermectin as oral tablets in one bottle with 5mg per tablet.
This information is for research and educational purposes only. No medical recommendations.
Risks & Safety
Ivermectin is considered very well tolerated at the documented standard doses; in mammals the underlying mechanism at glutamate-gated chloride channels affects the nervous system only to a small degree because of blood-brain barrier protection.
Documented in clinical studies:
- Good tolerability at standard doses: at the documented antiparasitic doses only minor effects are described, which is why the compound has been used broadly for decades.
- Neurological effects with excess dosing: at very high doses, CNS effects are documented in the literature, since the blood-brain barrier protection can then be exceeded.
- Blood-brain barrier deficit: with weakened blood-brain barrier protection, described in the literature for example in certain dog breeds, neurological effects are possible even at lower doses.
- Interaction with P-glycoprotein inhibitors: combination with P-glycoprotein inhibitors can weaken the protective mechanism and favor neurological effects.
Monitoring via bloodwork is recommended. This classification does not replace medical advice. Risk and responsibility for any actual use lie entirely with the buyer.
Studies
- Ivermectin, ‘Wonder drug’ from Japan: the human use perspective - Proceedings of the Japan Academy 2011, Crump & Omura: comprehensive review of discovery, mechanism, and global use.
- The Pharmacokinetics and Interactions of Ivermectin in Humans - A Mini-review - AAPS Journal 2008, Gonzalez Canga et al: mini-review of pharmacokinetics and interactions in humans.
- Superiority of ivermectin 1% cream over metronidazole 0.75% cream in treating inflammatory lesions of rosacea: a randomized, investigator-blinded trial - British Journal of Dermatology 2015, Taieb et al: RCT of topical ivermectin in rosacea.
- Ivermectin: enigmatic multifaceted ‘wonder’ drug continues to surprise and exceed expectations - Journal of Antibiotics 2017, Crump: recent mechanism and use review after Nobel Prize award.
- Ivermectin for preventing and treating COVID-19 - Cochrane Database of Systematic Reviews 2022, Popp et al: Cochrane review of ivermectin in COVID-19 without robust evidence of efficacy.
