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

Description
Curator's Comment:: 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

Conditions

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

907718400000
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

907718400000
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
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
IVERMECTIN [WHO-DD]
Common Name 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 [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
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 520.1197
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
WHO-ATC D11AX22
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 520.1195
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 520.1193
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
WHO-ATC P02CF01
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
EPA PESTICIDE CODE 628811
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 524.1140
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 524.1193
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
WHO-ESSENTIAL MEDICINES LIST 6.1.2
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
NDF-RT N0000175484
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 520.1199
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 522.1192
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
NDF-RT N0000181811
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 556.344
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 520.1192
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
WHO-VATC QP54AA01
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
NCI_THESAURUS C250
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 520.1196
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 520.1200
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 558.300
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 520.1198
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
WHO-VATC QP54AA51
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
WHO-VATC QS02QA03
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
CFR 21 CFR 522.1193
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
LIVERTOX 527
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C61796
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
EVMPD
SUB12089MIG
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
RXCUI
6069
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY RxNorm
MESH
D007559
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
DRUG BANK
DB00602
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
IUPHAR
2373
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
EPA CompTox
70288-86-7
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
WIKIPEDIA
IVERMECTIN
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
FDA UNII
8883YP2R6D
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
DRUG CENTRAL
3972
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
ECHA (EC/EINECS)
274-536-0
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
USP_CATALOG
1354309
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY USP-RS
CAS
70288-86-7
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
INN
4828
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
LACTMED
Ivermectin
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
ChEMBL
CHEMBL1200633
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY
MERCK INDEX
M6566
Created by admin on Fri Jun 25 21:01:33 UTC 2021 , Edited by admin on Fri Jun 25 21:01:33 UTC 2021
PRIMARY Merck Index
All of the following components must be present:
Definition References