DescriptionSources: http://www.drugbank.ca/drugs/DB00602Curator's Comment: Description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2008/050742s022lbl.pdf
Sources: http://www.drugbank.ca/drugs/DB00602
Curator's Comment: Description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2008/050742s022lbl.pdf
Ivermectin is a broad-spectrum anti-parasite medication. It was first marketed under the name Stromectol® and used against worms (except tapeworms), but, in 2012, it was approved for the topical treatment of head lice infestations in patients 6 months of age and older, and marketed under the name Sklice™ as well. Ivermectin is mainly used in humans in the treatment of onchocerciasis but is also effective against other worm infestations (such as strongyloidiasis, ascariasis, trichuriasis, and enterobiasis). 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 the normal intrauterine development of O. volvulus microfilariae and may inhibit their release from the uteri of gravid female worms. It is sold under brand names Heartgard, Sklice and Stromectol in the United States, Ivomec worldwide by Merial Animal Health, Mectizan in Canada by Merck, Iver-DT in Nepal by Alive Pharmaceutical and Ivexterm in Mexico by Valeant Pharmaceuticals International. In Southeast Asian countries, it is marketed by Delta Pharma Ltd. under the trade name Scabo 6.
CNS Activity
Curator's Comment: Some penetration of the blood-brain barrier does occur at relatively high doses, with brain levels peaking between two and five hours after administration. Symptoms seen in a range of mammalian species are CNS depression, and consequent ataxia, as might be expected from potentiation of inhibitory GABA-ergic synapses. However, at therapeutic doses cannot cross the blood-brain barrier into the mammalian CNS https://www.ncbi.nlm.nih.gov/pubmed/21321478
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16126457
Curator's Comment: Ivermectin, the first commercially available macrocyclic lactone endectocide, was discovered in a screening program at Merck in the mid-1970s # Merck
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL1075092 Sources: https://www.drugbank.ca/drugs/DB00602 |
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Target ID: CHEMBL5845 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11278873 |
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Target ID: CHEMBL2094121 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11082440 |
33.0 nM [IC50] | ||
Target ID: CHEMBL613135 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14592480 |
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Target ID: CHEMBL613142 |
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Target ID: CHEMBL2363050 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14639007 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Curative | STROMECTOL Approved UseSTROMECTOL is indicated for the treatment of the following infections:
Strongyloidiasis of the intestinal tract. STROMECTOL is indicated for the treatment of intestinal (i.e., nondisseminated) strongyloidiasis due to the nematode parasite Strongyloides stercoralis.
Onchocerciasis. STROMECTOL is indicated for the treatment of onchocerciasis due to the nematode
parasite Onchocerca volvulus. Launch Date1998 |
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Curative | STROMECTOL Approved UseSTROMECTOL is indicated for the treatment of the following infections:
Strongyloidiasis of the intestinal tract. STROMECTOL is indicated for the treatment of intestinal (i.e., nondisseminated) strongyloidiasis due to the nematode parasite Strongyloides stercoralis.
Onchocerciasis. STROMECTOL is indicated for the treatment of onchocerciasis due to the nematode
parasite Onchocerca volvulus. Launch Date1998 |
PubMed
Title | Date | PubMed |
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P-gp modulating drugs greatly potentiate the in vitro effect of ivermectin against resistant larvae of Haemonchus placei. | 2014 Oct 15 |
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Liposomal Systems as Nanocarriers for the Antiviral Agent Ivermectin. | 2016 |
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Increased expression of ATP binding cassette transporter genes following exposure of Haemonchus contortus larvae to a high concentration of monepantel in vitro. | 2016 Sep 29 |
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In vitro susceptibility of nematophagous fungi to antiparasitic drugs: interactions and implications for biological control. | 2017 Jul-Sept |
Patents
Sample Use Guides
The recommended dosage of STROMECTOL for the treatment of strongyloidiasis is a single oral dose
designed to provide approximately 200 mcg of ivermectin per kg of body weight.
The recommended dosage of STROMECTOL for the treatment of onchocerciasis is a single oral dose
designed to provide approximately 150 mcg of ivermectin per kg of body weight.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24998875
10 uM ivermectin up-regulated mRNA expression of Abcb1a, Abcb1b, Abcc2, Cyp1a1 and Cyp2b10 by 2.1-, 1.9-, 2.1-, 4.0 and 2.9-fold. resp. in mouse intestinal epithelial CMT-93 cell line.
Substance Class |
Mixture
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CFR |
21 CFR 524.1195
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CFR |
21 CFR 520.1194
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CFR |
21 CFR 520.1197
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WHO-ATC |
D11AX22
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CFR |
21 CFR 520.1195
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CFR |
21 CFR 520.1193
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WHO-ATC |
P02CF01
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EPA PESTICIDE CODE |
628811
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CFR |
21 CFR 524.1140
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CFR |
21 CFR 524.1193
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WHO-ESSENTIAL MEDICINES LIST |
6.1.2
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NDF-RT |
N0000175484
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CFR |
21 CFR 520.1199
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CFR |
21 CFR 522.1192
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NDF-RT |
N0000181811
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CFR |
21 CFR 556.344
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CFR |
21 CFR 520.1192
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WHO-VATC |
QP54AA01
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NCI_THESAURUS |
C250
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CFR |
21 CFR 520.1196
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CFR |
21 CFR 520.1200
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CFR |
21 CFR 558.300
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CFR |
21 CFR 520.1198
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WHO-VATC |
QP54AA51
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WHO-VATC |
QS02QA03
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CFR |
21 CFR 522.1193
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LIVERTOX |
NBK548921
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D007559
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DB00602
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IVERMECTIN
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Ivermectin
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CHEMBL1200633
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m6566
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ivermectin
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755843
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All of the following components must be present:
Related Record | Type | Details | ||
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TRANSPORTER -> INHIBITOR | |||
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TRANSPORTER -> SUBSTRATE | |||
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TARGET ORGANISM->INHIBITOR | |||
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BINDER->LIGAND |
BINDING
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TARGET ORGANISM->INHIBITOR | |||
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TRANSPORTER -> SUBSTRATE |
Collies were observed to have severe neurological signs after oral administration of ivermectin attributable to an inherited ABCB1-1Δ mutation and its effect on the integrity of the blood–brain barrier.
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METABOLIC ENZYME -> SUBSTRATE | |||
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TRANSPORTER -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE |
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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