Peringatan Keamanan

Used appropriately, topically applied ivermectin lotions and creams are unlikely to cause significant toxicity. With accidental or intentional significant exposure to unknown quantities of veterinary formulations of ivermectin (by ingestion, inhalation, injection, or significant body surface area exposure) patients have reported rash, edema, headache, dizziness, asthenia, nausea, vomiting, and diarrhea. Other less common effects include seizure, ataxia, dyspnea, abdominal pain, paresthesia, urticaria, and contact dermatitis.L31453 Overdosage with orally administered ivermectin was lethal in mice and rats (at doses several-fold higher than the recommended dose), with death preceded by significant ataxia, bradypnea, tremors, ptosis, decreased activity, emesis, and mydriasis.L31453

If overdosage of ivermectin is suspected, initiate supportive therapy as clinically indicated, including the use of parenteral fluids and electrolytes, respiratory support, and pressor agents to manage hypotension. Induction of emesis and/or gastric lavage may be considered alongside other purgatives and routine anti-poison measures if clinically indicated.L31453

Ivermectin

DB00602

small molecule approved investigational vet_approved

Deskripsi

Ivermectin is a semi-synthetic antiparasitic medication derived from avermectins, a class of highly-active broad-spectrum antiparasitic agents isolated from the fermentation products of Streptomyces avermitilis.L31453 Ivermectin itself is a mixture of two avermectins, comprising roughly 90% 5-O-demethyl-22,23-dihydroavermectin A1a (22,23-dihydroavermectin B1a) and 10% 5-O-demethyl-25-de(1-methylpropyl)-22,23-dihydro­-25-(1-methylethyl)avermectin A1a (22,23-dihydroavermectin B1b).L31453

Ivermectin is mainly used in humans in the treatment of onchocerciasis, but may also be effective against other worm infestations (such as strongyloidiasis, ascariasis, trichuriasis and enterobiasis). Applied topically, it may be used in the treatment of head lice infestation.

With the advent of 2020 and the COVID-19 pandemic, ivermectin began garnering notoriety due to its off-label use for the prophylaxis and treatment of COVID-19. While studies are still ongoing, much of the evidence for ivermectin in COVID-19 relies on pre-print in vitro data, and the clinical utility of this data remains unclear. Due to a number of factors - for example, the relatively low number of patients per trial and the speed at which these trials were conducted - studies on the use of ivermectin in COVID-19 have been fraught with statistical errors and accusations of plagiarism.L36763,A238929 In addition, the use of aggregate patient data in large-scale meta-analyses (as opposed to individual patient data (IPD)) has been shown to disguise otherwise blatant data errors, such as extreme terminal digit bias and the duplication of blocks of patient records.A238929

Until high-quality, peer-reviewed data regarding both the safety and efficacy of ivermectin for COVID-19 in humans becomes available, the use of ivermectin for these purposes should be avoided in favour of thoroughly-vetted therapies (e.g. COVID-19 vaccines like Comirnaty(https://go.drugbank.com/drugs/DB15696)).

Struktur Molekul 2D

Berat 1736.185
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following oral administration, the half-life of ivermectin is approximately 18 hours.[L31453]
Volume Distribusi The volume of distribution is 3 to 3.5 L/kg and it does not cross the blood-brain barrier.
Klirens (Clearance) -

Absorpsi

Moderately well absorbed. Improved absorption with high fat meal.

Metabolisme

Primarily hepatic. Ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1 % of the administered dose excreted in the urine.

Rute Eliminasi

Ivermectin is metabolized in the liver, and ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1% of the administered dose excreted in the urine.

Interaksi Makanan

1 Data
  • 1. Take on an empty stomach. Oral ivermectin should be taken on an empty stomach with a glass of water.

Interaksi Obat

351 Data
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Ivermectin.
Azithromycin The serum concentration of Ivermectin can be increased when it is combined with Azithromycin.
Dicoumarol Ivermectin may increase the anticoagulant activities of Dicoumarol.
Phenindione Ivermectin may increase the anticoagulant activities of Phenindione.
Warfarin Ivermectin may increase the anticoagulant activities of Warfarin.
Phenprocoumon Ivermectin may increase the anticoagulant activities of Phenprocoumon.
Acenocoumarol Ivermectin may increase the anticoagulant activities of Acenocoumarol.
4-hydroxycoumarin Ivermectin may increase the anticoagulant activities of 4-hydroxycoumarin.
Coumarin Ivermectin may increase the anticoagulant activities of Coumarin.
(R)-warfarin Ivermectin may increase the anticoagulant activities of (R)-warfarin.
Ethyl biscoumacetate Ivermectin may increase the anticoagulant activities of Ethyl biscoumacetate.
Fluindione Ivermectin may increase the anticoagulant activities of Fluindione.
Clorindione Ivermectin may increase the anticoagulant activities of Clorindione.
Diphenadione Ivermectin may increase the anticoagulant activities of Diphenadione.
Tioclomarol Ivermectin may increase the anticoagulant activities of Tioclomarol.
(S)-Warfarin Ivermectin may increase the anticoagulant activities of (S)-Warfarin.
Pitolisant The serum concentration of Ivermectin can be decreased when it is combined with Pitolisant.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Novobiocin Novobiocin may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Hesperetin Hesperetin may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Rabeprazole Rabeprazole may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Topiroxostat Topiroxostat may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Daidzin Daidzin may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Fusidic acid The metabolism of Ivermectin can be decreased when combined with Fusidic acid.
Naringenin Naringenin may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Eltrombopag Eltrombopag may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Simeprevir The metabolism of Ivermectin can be decreased when combined with Simeprevir.
Safinamide Safinamide may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Teriflunomide Teriflunomide may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Cannabidiol Cannabidiol may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Fostamatinib Fostamatinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Gilteritinib Gilteritinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Nabiximols Nabiximols may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Fedratinib The serum concentration of Ivermectin can be increased when it is combined with Fedratinib.
Istradefylline Istradefylline may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Caffeine Caffeine may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Afatinib Afatinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Pravastatin Pravastatin may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Pantoprazole Pantoprazole may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Diethylstilbestrol Diethylstilbestrol may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Gefitinib Gefitinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Beclomethasone dipropionate Beclomethasone dipropionate may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Lansoprazole Lansoprazole may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Estradiol Estradiol may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Buprenorphine Buprenorphine may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Telmisartan Telmisartan may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Genistein Genistein may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Quercetin Quercetin may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Taurocholic acid Taurocholic acid may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Elacridar Elacridar may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Dovitinib Dovitinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Vismodegib Vismodegib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Daclatasvir Daclatasvir may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Dasabuvir Dasabuvir may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Rolapitant Rolapitant may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Paritaprevir Paritaprevir may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Velpatasvir Velpatasvir may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Glasdegib Glasdegib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Voxilaprevir Voxilaprevir may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Letermovir The excretion of Letermovir can be decreased when combined with Ivermectin.
Rucaparib Rucaparib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Pibrentasvir Pibrentasvir may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Glecaprevir Glecaprevir may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Estradiol acetate Estradiol acetate may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Estradiol benzoate Estradiol benzoate may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Estradiol cypionate Estradiol cypionate may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Estradiol dienanthate Estradiol dienanthate may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Estradiol valerate Estradiol valerate may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Rilpivirine Rilpivirine may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Ripretinib Ripretinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Fostemsavir Fostemsavir may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Imatinib Imatinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Isavuconazole The metabolism of Ivermectin can be decreased when combined with Isavuconazole.
Clofazimine Clofazimine may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Cyclosporine The metabolism of Ivermectin can be decreased when combined with Cyclosporine.
Erlotinib Erlotinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Dasatinib Dasatinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Sunitinib Sunitinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Vandetanib Vandetanib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Vemurafenib Vemurafenib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Regorafenib Regorafenib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Ponatinib Ponatinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Dabrafenib The serum concentration of Ivermectin can be decreased when it is combined with Dabrafenib.
Palbociclib Palbociclib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Alectinib Alectinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Venetoclax The metabolism of Ivermectin can be decreased when combined with Venetoclax.
Dacomitinib Dacomitinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Abemaciclib Abemaciclib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Brigatinib Brigatinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Enasidenib Enasidenib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Dexamethasone acetate Dexamethasone acetate may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Avanafil The serum concentration of Avanafil can be increased when it is combined with Ivermectin.
Tepotinib Tepotinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Tivozanib Tivozanib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Osimertinib Osimertinib may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Belumosudil Belumosudil may decrease the excretion rate of Ivermectin which could result in a higher serum level.
Valsartan The excretion of Valsartan can be decreased when combined with Ivermectin.
Torasemide The excretion of Torasemide can be decreased when combined with Ivermectin.

Target Protein

Glutamate-gated chloride channel subunit beta glc-2
Glutamate-gated chloride channel alpha glc-1

Referensi & Sumber

Synthesis reference: Shuet-Hing L. Chiu, Josephine R. Carlin, Rae Taub, "Ivermectin derivative compounds and process for preparing the same." U.S. Patent US4963667, issued June, 1982.
Artikel (PubMed)
  • PMID: 32824399
    El-Saber Batiha G, Alqahtani A, Ilesanmi OB, Saati AA, El-Mleeh A, Hetta HF, Magdy Beshbishy A: Avermectin Derivatives, Pharmacokinetics, Therapeutic and Toxic Dosages, Mechanism of Action, and Their Biological Effects. Pharmaceuticals (Basel). 2020 Aug 17;13(8). pii: ph13080196. doi: 10.3390/ph13080196.
  • PMID: 34430453
    Mathachan SR, Sardana K, Khurana A: Current Use of Ivermectin in Dermatology, Tropical Medicine, and COVID-19: An Update on Pharmacology, Uses, Proven and Varied Proposed Mechanistic Action. Indian Dermatol Online J. 2021 Jul 14;12(4):500-514. doi: 10.4103/idoj.idoj29821. eCollection 2021 Jul-Aug.
  • PMID: 34220503
    Alam S, Kamal TB, Sarker MMR, Zhou JR, Rahman SMA, Mohamed IN: Therapeutic Effectiveness and Safety of Repurposing Drugs for the Treatment of COVID-19: Position Standing in 2021. Front Pharmacol. 2021 Jun 14;12:659577. doi: 10.3389/fphar.2021.659577. eCollection 2021.
  • PMID: 34281149
    Bestetti RB, Furlan-Daniel R, Silva VMR: Pharmacological Treatment of Patients with Mild to Moderate COVID-19: A Comprehensive Review. Int J Environ Res Public Health. 2021 Jul 5;18(13). pii: ijerph18137212. doi: 10.3390/ijerph18137212.
  • PMID: -
    Lawrence JM, Meyerowitz-Katz G, Heathers JAJ, et al.: The lesson of ivermectin: meta-analyses based on summary data alone are inherently unreliable. Nat Med.

Contoh Produk & Brand

Produk: 38 • International brands: 20
Produk
  • 171083 Ivermectin 1% / Metronidazole 1% / Niacinamide 4%
    Gel • - • Topical • US
  • Brimonidine Tartrate 0.25% / Ivermectin 1% / Metronidazole 1% / Niacinamide 4%
    Gel • - • Topical • US
  • Ivermectin
    Tablet • 3 mg/1 • Oral • US • Generic • Approved
  • Ivermectin
    Tablet • 3 mg/1 • Oral • US • Generic • Approved
  • Ivermectin
    Tablet • 3 mg/1 • Oral • US • Generic • Approved
  • Ivermectin
    Powder • 1 kg/1kg • Not applicable • US
  • Ivermectin
    Cream • 10 mg/1g • Topical • US • Generic • Approved
  • Ivermectin
    Cream • 10 mg/1g • Topical • US • Generic • Approved
Menampilkan 8 dari 38 produk.
International Brands
  • Ascapil — Abbott
  • Detebencil — Roux-Ocefa
  • Ermetin — Unipharm
  • Gotax — Metlen
  • Imectin — Pulse
  • Ivectin — Aristopharma
  • Ivera — Beximco
  • Ivergot — Licol
  • Ivermec — UCI
  • Ivexterm — Valeant

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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