Ivermectin Contraindications, Dosage, Side Effects Ivermectin Contraindications/Ivermectin is a macrocyclic lactone derived from Streptomyces avermitilis with antiparasitic activity. Ivermectin exerts its anthelmintic effect via activating glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells. Distinct from the channel opening induced by endogenous glutamate transmitter, ivermectin-activated channels open very slowly but essentially irreversibly. As a result, neurons or muscle cells remain at either hyperpolarisation or depolarization state, thereby resulting in paralysis and death of the parasites. Ivermectin does not readily pass the mammal blood-brain barrier to the central nervous system where glutamate-gated chloride channels locate, hence the hosts are relatively resistant to the effects of this agent. Mechanism of Action of Ivermectin Ivermectin binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate muscle and nerve cells of the microfilaria. This binding causes an increase in the permeability of the cell membrane to chloride ions and results in hyperpolarization of the cell, leading to paralysis and death of the parasite. Ivermectin also is believed to act as an agonist of the neurotransmitter gamma-aminobutyric acid (GABA), thereby disrupting GABA-mediated central nervous system (CNS) neurosynaptic transmission. Ivermectin may also impair normal intrauterine development of O. volvulus microfilariae and may inhibit their release from the uteri of gravid female worms. Indications of Ivermectin For the treatment of intestinal (i.e., nondisseminated) strongyloidiasis due to the nematode parasite Strongyloides stercoralis. Also for the treatment of onchocerciasis (river blindness) due to the nematode parasite Onchocerca volvulus. Can be used to treat scabies caused by Sarcoptes scabiei. Filariasis Onchocerciasis Strongyloidiasis Ascariasis Cutaneous Larva Migrans Acne Rosacea Ascaris lumbricoides infection Cutaneous larva migrans Demodicosis Gnathostomiasis Mansonella ozzardi infection Mansonella streptococcal infection Oesophagostomiasis Onchocerciasis Pediculosis Capitis Scabies Trichuriasis Wuchereria bancroftian infection You Might Also Read What Is Butenafine Hydrochloride - Indications, Side EffectsContraindications of Ivermectin Infection by the worm Loa Loa Abnormal liver function tests Kidney disease with a reduction in kidney function Diarrhea The high amount of magnesium in the blood Low amount of sodium in the blood Extreme loss of body water Appendicitis Stomach or intestine blockage Seizures Allergies Avermectins Ivermectin Dosage of Ivermectin Strengths: 3 mg; 6 mg Filariasis 0.2 mg/kg orally once Bancroftian filariasis: 0.4 mg/kg orally once yearly (with a single annual dose of diethylcarbamazine 6 mg/kg), for 4 to 6 years. Onchocerciasis 0.15 mg/kg orally once every 12 months Patients with heavy ocular infection may require retreatment every 6 months. Retreatment may be considered at intervals as short as 3 months. Dosage guidelines based on body weight 15 to 25 kg: 3 mg orally one time 26 to 44 kg: 6 mg orally one time 45 to 64 kg: 9 mg orally one time 65 to 84 kg: 12 mg orally one time 85 kg or more: 0.15 mg/kg orally one time Strongyloidiasis 0.2 mg/kg orally once In immunocompromised (including HIV) patients, the treatment of strongyloidiasis may be refractory requiring repeated treatment (i.e., every 2 weeks) and suppressive therapy (i.e., once a month), although well-controlled studies are not available. A cure may not be achievable in these patients. Dosage guidelines based on body weight 15 to 24 kg: 3 mg orally one time 25 to 35 kg: 6 mg orally one time 36 to 50 kg: 9 mg orally one time 51 to 65 kg: 12 mg orally one time 66 to 79 kg: 15 mg orally one time 80 kg or more: 0.2 mg/kg orally one time You Might Also Read Myobloc (RimabotulinumtoxinB or botulinum toxin type B)Ascariasis 0.2 mg/kg orally once Pediatric Dose for Filariasis Bancroftian filariasis – 5 years or older: 0.4 mg/kg orally once yearly (with a single annual dose of diethylcarbamazine 6 mg/kg), for 4 to 6 years. Side Effects of Ivermectin More common signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat) Fever, itching or skin rash joint or muscle pain burning feeling of the skin dry skin itchiness skin irritation severe skin irritation painful and tender glands in neck, armpits, or groin rapid heartbeat Less common Headache swelling of the face, hands, arms, feet, or legs Diarrhea dizziness skin rash or itching Lightheadedness when getting up from a lying or sitting position Rare Loss of appetite shaking or trembling sleepiness change in vision chest pain or tightness confusion a cough Agitation arm, back, or jaw pain blurred vision chest pain or discomfort convulsions extra heartbeats hallucinations a headache irritability lightheadedness Drug Interactions of Ivermectin Ivermectin may interact with following drugs, supplements, & may change the efficacy of the drug aluminum hydroxide aspirin dextroamphetamine albendazole diphenhydramine praziquantel prednisone pyrantel acetaminophen) Vitamin B Complex 100 (multivitamin) Vitamin B12 (cyanocobalamin) Vitamin C (ascorbic acid) Vitamin D3 (cholecalciferol) alprazolam cetirizine voriconazole tacrolimus telaprevir telithromycin telotristat temsirolimus ribociclib ritonavir rucapari nelfinavir nevirapine nilotinib oxcarbazepine posaconazole rufinamide stiripentol modafinil saquinavir nefazodone warfarin Pregnancy Category of Ivermectin Pregnancy This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately. Breast-feeding It is not known if ivermectin applied to the skin passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. The safety and effectiveness of using this medication have not been established for children. References https://www.drugbank.ca/drugs/DB00602 https://www.drugs.com/mtm/ivermectin.html ClinicalTrials.gov https://clinicaltrials.gov/ DailyMed https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=IVERMECTIN EPA Chemical and Products Database (CPDat) https://comptox.epa.gov/dashboard/DTXSID8023181#exposure https://www.epa.gov/chemical-research/chemical-and-products-database-cpdat https://www.webmd.com/drugs/2/drug-1122/ivermectin-oral/details/list-contraindications https://chealth.canoe.com/drug/getdrug/rosiver WHO ATC https://www.whocc.no/atc/ https://www.whocc.no/atc_ddd_index/ Wikipedia https://www.wikidata.org/wiki/Q27132923 MeSH https://www.ncbi.nlm.nih.gov/mesh/68007559 http://www.nlm.nih.gov/mesh/meshhome.html https://www.ncbi.nlm.nih.gov/mesh/68000977 https://www.ncbi.nlm.nih.gov/mesh/68007306 https://pubchem.ncbi.nlm.nih.gov https://www.pdr.net/drug-summary/Sklice-ivermectin-2415 You Might Also Read Phenylmethanol - Uses, Dosage, Side EffectsShow More