U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Description
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

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

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
STROMECTOL

Approved Use

STROMECTOL 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 Date

1998
Curative
STROMECTOL

Approved Use

STROMECTOL 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 Date

1998
PubMed

PubMed

TitleDatePubMed
P-gp modulating drugs greatly potentiate the in vitro effect of ivermectin against resistant larvae of Haemonchus placei.
2014 Oct 15
Liposomal Systems as Nanocarriers for the Antiviral Agent Ivermectin.
2016
Evaluation of the in vitro expression of ATP binding-cassette (ABC) proteins in an Ixodes ricinus cell line exposed to ivermectin.
2016 Apr 18
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
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
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.
Name Type Language
IVERMECTIN
EP   GREEN BOOK   INN   JAN   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD  
INN   USAN  
Official Name English
L 640471
Code English
HYVERMECTIN
Brand Name English
IVOMEC
Brand Name English
EQUIMEC
Brand Name English
NOROMECTIN
Brand Name English
IVERMECTIN [USAN]
Common Name English
CD-5024
Code English
ORAMEC
Brand Name English
CD5024
Code English
L-640471
Code English
IVERMECTIN [ORANGE BOOK]
Common Name English
CARDOMEC
Brand Name English
22,23-DIHYDROABAMECTIN
Common Name English
NORAMECTIN
Brand Name English
BOVINET
Brand Name English
ACAREXX
Brand Name English
CEVAMEC
Brand Name English
A MIXTURE OF NOT LESS THAN 80% IVERMECTIN COMPONENT B1A AND NOT MORE THAN 20% IVERMECTIN COMPONENT B1B
Common Name English
NSC-755843
Code English
MK-933
Code English
IVOSINT
Brand Name English
Ivermectin [WHO-DD]
Common Name English
IVERMECTIN [USP-RS]
Common Name English
IVERTIN
Brand Name English
A MIXTURE OF AVERMECTIN A1A, 5-O-DEMETHYL-22,23-DIHYDRO-(COMPONENT H2B1A), AND AVERMECTIN A1A, 5-O-DEMETHYL-25-DE(1-METHYLPROPYL)-22,23-DIHYDRO-25-(1-METHYLETHYL)-(COMPONENT H2B1B)
Common Name English
IVERMECTIN [EP MONOGRAPH]
Common Name English
IVECTIN
Brand Name English
IVERMECTIN [GREEN BOOK]
Common Name English
ZIMECTERIN
Brand Name English
UVEMEC
Brand Name English
VERMIC
Brand Name English
HEARTGARD
Brand Name English
EQVALAN
Brand Name English
JETAMEC
Brand Name English
IVERMECTIN [USP MONOGRAPH]
Common Name English
SKLICE
Brand Name English
IVERMECTIN [VANDF]
Common Name English
VETMEC
Brand Name English
PANDEX
Brand Name English
MECTIZAN
Brand Name English
22,23-DIHYDROAVERMECTIN B1
Common Name English
IVERMECTIN [JAN]
Common Name English
CARDOTEK 30
Brand Name English
BIMECTIN
Brand Name English
MK 933
Code English
IVERMECTIN [MI]
Common Name English
ivermectin [INN]
Common Name English
STROMECTOL
Brand Name English
SOOLANTRA
Brand Name English
22,23-DIHYDRO C-076B1
Common Name English
PHOENECTIN
Brand Name English
IVERMECTIN [MART.]
Common Name English
Classification Tree Code System Code
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
Created by admin on Fri Dec 15 15:59:11 GMT 2023 , Edited by admin on Fri Dec 15 15:59:11 GMT 2023
LIVERTOX NBK548921
Created by admin on Fri Dec 15 15:59:11 GMT 2023 , Edited by admin on Fri Dec 15 15:59:11 GMT 2023
Code System Code Type Description
NCI_THESAURUS
C61796
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PRIMARY
EVMPD
SUB12089MIG
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PRIMARY
RS_ITEM_NUM
1354309
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PRIMARY
RXCUI
6069
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PRIMARY RxNorm
MESH
D007559
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PRIMARY
DRUG BANK
DB00602
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PRIMARY
IUPHAR
2373
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PRIMARY
EPA CompTox
DTXSID7040235
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PRIMARY
WIKIPEDIA
IVERMECTIN
Created by admin on Fri Dec 15 15:59:11 GMT 2023 , Edited by admin on Fri Dec 15 15:59:11 GMT 2023
PRIMARY
FDA UNII
8883YP2R6D
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PRIMARY
DRUG CENTRAL
3972
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PRIMARY
ECHA (EC/EINECS)
274-536-0
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PRIMARY
CHEBI
6078
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PRIMARY
CAS
70288-86-7
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PRIMARY
INN
4828
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PRIMARY
LACTMED
Ivermectin
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PRIMARY
ChEMBL
CHEMBL1200633
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PRIMARY
MERCK INDEX
m6566
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PRIMARY Merck Index
DAILYMED
8883YP2R6D
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PRIMARY
ALANWOOD
ivermectin
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PRIMARY
NSC
755843
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PRIMARY
All of the following components must be present:
Definition References