Ivermectol: A Potent Antiparasitic for Systemic Infestations
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Synonyms | |||
Ivermectol represents a significant advancement in antiparasitic therapy, offering broad-spectrum efficacy against a range of nematode and arthropod infestations. As a semi-synthetic derivative of avermectin B1, it operates through a unique mechanism of action, selectively binding to glutamate-gated chloride ion channels in invertebrate nerve and muscle cells. This leads to increased cell permeability to chloride ions, resulting in hyperpolarization and subsequent paralysis or death of the parasite. Its high therapeutic index and favorable pharmacokinetic profile make it a cornerstone in both human and veterinary parasitology, particularly for conditions where traditional anthelmintics demonstrate limited efficacy or unacceptable toxicity profiles.
Features
- Contains ivermectin as the active pharmaceutical ingredient (typically 3mg, 6mg, or 12mg tablets)
- Exhibits high bioavailability when administered orally on an empty stomach
- Demonstrons a broad spectrum of activity against nematodes (roundworms) and ectoparasites
- Manufactured under strict GMP (Good Manufacturing Practice) guidelines
- Available in scored tablets for accurate dose splitting when required
- Stable at room temperature with a prolonged shelf life when stored properly
Benefits
- Effectively eliminates a wide range of parasitic infections, reducing morbidity and transmission rates
- Single-dose regimens for many indications improve patient compliance and treatment adherence
- Demonstrates a high safety margin in humans at therapeutic doses
- Contributes to mass drug administration programs for controlling neglected tropical diseases
- Reduces parasite load in communities, decreasing the overall burden of parasitic diseases
- Provides an alternative treatment option for cases resistant to other anthelmintic agents
Common use
Ivermectol is primarily indicated for the treatment of various parasitic infestations. Its most significant application is in the management of onchocerciasis (river blindness), where it effectively kills microfilariae and reduces transmission by decreasing the number of larvae available to black flies. It is also approved for strongyloidiasis caused by Stronglyoides stercoralis, particularly in immunocompromised patients where disseminated disease can be fatal. Additionally, it shows efficacy against cutaneous larva migrans, scabies (especially crusted/norwegian variant), ascariasis, trichuriasis, enterobiasis, and filariasis including lymphatic filariasis (often co-administered with albendazole). Off-label uses include treatment for head lice, demodicosis, and certain mite infestations when standard therapies prove ineffective.
Dosage and direction
Dosage is weight-based and varies according to the specific parasitic infection being treated. For onchocerciasis, the standard dose is 150mcg/kg orally as a single dose, repeated every 6-12 months until asymptomatic. For strongyloidiasis, 200mcg/kg orally as a single dose is typically administered. Tablets should be taken with a full glass of water on an empty stomach (at least 1 hour before or 2 hours after food) to maximize absorption. Dosing may need adjustment in patients with hepatic impairment, though no specific dosage adjustment is required for renal impairment as ivermectin is primarily metabolized in the liver and excreted in feces. For children weighing less than 15kg, specialized formulations or compounding may be necessary.
Precautions
Patients should be screened for concomitant loiasis (African eye worm) due to the risk of serious encephalopathic reactions in those with high Loa loa microfilarial loads. Use with caution in elderly patients who may have decreased hepatic function. Breastfeeding should be interrupted for approximately 72 hours after administration due to secretion in milk. While not typically sedating, patients should be cautioned about potential dizziness and advised against operating machinery until they know how the medication affects them. Those with asthma may experience worsening symptoms due to the inflammatory response to dying parasites. Regular monitoring of liver function tests may be warranted during repeated dosing regimens.
Contraindications
Ivermectol is contraindicated in patients with known hypersensitivity to ivermectin or any component of the formulation. It should not be administered to children weighing less than 15kg unless specifically indicated and under close medical supervision. Contraindicated in patients with meningitis or other conditions that may increase the permeability of the blood-brain barrier due to potential neurotoxicity. Avoid use in pregnancy, especially during the first trimester, unless the potential benefit justifies the potential risk to the fetus. Not recommended for patients with untreated tuberculosis or other severe immunosuppressive conditions due to theoretical risk of disseminated strongyloidiasis.
Possible side effect
Most adverse reactions are mild and transient, often related to the death of parasites rather than direct drug toxicity. Common effects include dizziness, pruritus, fever, and skin rash (in up to 10-30% of patients with filarial infections). Gastrointestinal disturbances such as nausea, diarrhea, and abdominal pain may occur. Less frequently, patients may experience orthostatic hypotension, tachycardia, or edema. Ocular side effects include conjunctival hemorrhage and anterior uveitis, particularly in onchocerciasis patients. Severe but rare reactions include the Mazzotti reaction (fever, urticaria, lymphadenopathy) in onchocerciasis, and encephalopathy in patients with heavy Loa loa infections. Hepatotoxicity and neutropenia have been reported in isolated cases.
Drug interaction
Ivermectin is primarily metabolized by CYP3A4 enzymes and may interact with potent inhibitors of this system (e.g., ketoconazole, ritonavir, clarithromycin) leading to increased ivermectin levels. Inducers of CYP3A4 (e.g., rifampin, carbamazepine, St. John’s wort) may decrease ivermectin concentrations. Concurrent use with other medications that enhance GABA activity (e.g., benzodiazepines, barbiturates) may theoretically potentiate CNS depression, though clinical significance is uncertain. Warfarin efficacy may be reduced due to induction of metabolism. Vaccines may have reduced efficacy if administered shortly after ivermectin treatment due to its immunomodulatory effects.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Doubling the dose to make up for a missed dose is not recommended. For mass drug administration programs where single-dose regimens are standard, a missed dose typically requires administration at the next available opportunity, which may be during the next treatment cycle (often 6-12 months later).
Overdose
Symptoms of overdose are primarily extensions of its pharmacological effects and may include gastrointestinal distress, dizziness, nausea, vomiting, and pupillary dilation. Severe overdose may lead to hypotension, respiratory depression, and coma. There is no specific antidote for ivermectin overdose. Management is supportive and symptomatic, including gastric lavage if presented early, activated charcoal to prevent further absorption, and maintenance of vital functions. Hemodialysis is not effective due to high protein binding and extensive tissue distribution. Cases of significant human overdose are rare due to the drug’s wide safety margin.
Storage
Store at controlled room temperature between 15-30°C (59-86°F). Protect from light and moisture. Keep in the original container with the lid tightly closed. Do not store in bathroom or other humid areas. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the packaging. Properly discard any unused medication after treatment completion to prevent accidental ingestion or misuse.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Ivermectol is a prescription medication that should only be used under the supervision of a qualified healthcare professional. The prescribing physician should be consulted for diagnosis and appropriate treatment recommendations. Never self-medicate with antiparasitic agents. The efficacy and safety profile may vary based on individual patient factors, parasitic load, and regional parasite resistance patterns. Always follow local treatment guidelines and regulatory approvals for specific indications.
Reviews
Clinical studies have consistently demonstrated ivermectin’s efficacy, with microfilarial load reduction exceeding 90% within months of treatment in onchocerciasis patients. A systematic review of 18 randomized controlled trials confirmed its superiority over placebo for scabies treatment (RR 6.61, 95% CI 3.17 to 13.78). In strongyloidiasis, cure rates approach 85-100% after single-dose therapy. The World Health Organization includes ivermectin on its List of Essential Medicines, noting its significant public health impact in reducing transmission of neglected tropical diseases. Long-term surveillance data from mass drug administration programs show sustained reductions in disease prevalence with minimal development of resistance despite decades of use.