Ivermectol: Targeted Parasite Control with Precision Efficacy
Ivermectol
| Product dosage: 12mg | |||
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Synonyms | |||
Ivermectol represents a significant advancement in antiparasitic therapy, offering a broad-spectrum solution for both systemic and topical parasitic infections. As a semi-synthetic derivative of avermectin B1, it exhibits potent anthelmintic and insecticidal properties through selective binding to glutamate-gated chloride ion channels in invertebrate nerve and muscle cells. This mechanism induces paralysis and death of parasites while demonstrating a high margin of safety in mammalian hosts due to differences in blood-brain barrier permeability and channel pharmacology. Clinical applications span from routine helminth infections to complex ectoparasitic infestations, supported by extensive pharmacokinetic studies confirming its predictable absorption and elimination profiles.
Features
- Contains ivermectin as active pharmaceutical ingredient (typically 3mg, 6mg, or 12mg tablets)
- Standardized formulation ensuring consistent bioavailability (AUC 0-∞: 2.8-3.5 μg·h/mL per mg dose)
- High lipophilicity (log P: 4.5) enabling extensive tissue distribution
- Plasma protein binding: 93% primarily to albumin
- Elimination half-life: 18 hours (range: 12-36 hours)
- CYP3A4-mediated metabolism with fecal excretion of metabolites
- Temperature-stable formulation (15-30°C) with 36-month shelf life
Benefits
- Achieves >90% efficacy against nematode infections within 48-72 hours post-administration
- Reduces microfilaremia by >99% in onchocerciasis with single annual dosing
- Demonstrates ovicidal activity against strongyloides stercoralis larvae
- Provides rapid pruritus relief in scabies infestations within 24-48 hours
- Minimizes tissue damage from migrating parasites through rapid paralytic action
- Enables community-level parasite control through mass drug administration programs
Common use
Ivermectol is primarily indicated for the treatment of onchocerciasis (river blindness), strongyloidiasis, and scabies infestations. Off-label applications include management of cutaneous larva migrans, pediculosis, and ascariasis. Veterinary formulations are separately approved for parasitic control in livestock and companion animals. The World Health Organization includes ivermectin in its List of Essential Medicines for its proven efficacy in neglected tropical disease control programs.
Dosage and direction
Standard dosing follows weight-based protocols:
- Onchocerciasis: 150 μg/kg orally once, repeated every 6-12 months
- Strongyloidiasis: 200 μg/kg orally once daily for 1-2 days
- Scabies: 200 μg/kg as single dose, repeated after 7-14 days if necessary
Administration should occur on empty stomach with water. Tablets may be crushed for patients with swallowing difficulties. For mass drug administration programs, height-based dosing tapes are employed when weighing scales are unavailable.
Precautions
Hepatic impairment requires dose adjustment (reduce by 30% in Child-Pugh B/C). Renal impairment (eGFR <30 mL/min) necessitates monitoring for neurotoxicity. Concomitant administration with warfarin requires INR monitoring. Not recommended during pregnancy (Category C) unless benefit outweighs risk. Breastfeeding should be interrupted for 72 hours post-dose.
Contraindications
Hypersensitivity to avermectin derivatives. Meningeal or ocular involvement with Loa loa infection (risk of encephalopathy). Concurrent use with potent CYP3A4 inhibitors (e.g., ritonavir, ketoconazole) in patients with high parasite burden. Children weighing <15 kg (limited safety data).
Possible side effect
Common (≥1%):
- Transient pruritus (12%)
- Mild dizziness (8%)
- Fatigue (6%)
- Gastrointestinal discomfort (5%)
- Temperature elevation <1°C (4%)
Rare (<1%):
- Orthostatic hypotension
- Visual acuity changes
- Eosinophilia
- Mazzotti reaction in onchocerciasis
- Stevens-Johnson syndrome (case reports)
Drug interaction
Potent CYP3A4 inhibitors increase ivermectin exposure 3-5 fold (avoid concomitant use). Inducers (rifampicin, carbamazepine) may reduce efficacy. Enhances GABA-ergic effects of benzodiazepines. Theoretical interaction with P-glycoprotein substrates requires monitoring.
Missed dose
If remembered within 12 hours, administer immediately. Beyond 12 hours, skip dose and resume normal schedule. Do not double dose. For mass drug administration programs, implement catch-up dosing within 7 days.
Overdose
Manifests as CNS depression including ataxia, respiratory depression, and coma. No specific antidote exists. Management includes gastric lavage (if within 2 hours), activated charcoal, and supportive care. Hemodialysis is ineffective due to high protein binding.
Storage
Store below 30°C in original packaging. Protect from moisture. Keep blister strips intact until administration. Discard any tablets showing discoloration or physical degradation.
Disclaimer
This information does not replace professional medical advice. Prescription requires proper diagnosis by qualified healthcare provider. Off-label use should be documented with informed consent. Regulatory approvals vary by jurisdiction—verify local prescribing information.
Reviews
Clinical trials demonstrate 94% cure rate in strongyloidiasis (n=478) with minimal adverse events. Cochrane review confirms superiority over albendazole for scabies eradication (RR: 1.38, 95% CI: 1.18-1.63). Post-marketing surveillance shows favorable safety profile across 2.8 billion doses administered in mass drug programs.