ivermectin Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
antiparasitics, ivermectin derivatives 3972 70288-86-7

Description:

MoleculeDescription

Synonyms:

  • ivermectin
  • noramectin
  • noromectin
  • zimecterin
A mixture of mostly avermectin H2B1a (RN 71827-03-7) with some avermectin H2B1b (RN 70209-81-3), which are macrolides from STREPTOMYCES avermitilis. It binds glutamate-gated chloride channel to cause increased permeability and hyperpolarization of nerve and muscle cells. It also interacts with other CHLORIDE CHANNELS. It is a broad spectrum antiparasitic that is active against microfilariae of ONCHOCERCA VOLVULUS but not the adult form.
  • Molecular weight: 1736.19
  • Formula: C95H146O28
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
12 mg O

Approvals:

DateAgencyCompanyOrphan
Nov. 22, 1996 FDA MERCK SHARP DOHME

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Asthenia 1836.54 79.16 467 946 65198 3319248
Headache 1547.14 79.16 439 974 91541 3292905
Conjunctival haemorrhage 1407.00 79.16 201 1212 968 3383478
Ocular hyperaemia 1370.43 79.16 240 1173 4913 3379533
Pyrexia 1244.29 79.16 363 1050 80752 3303694
Coma 913.40 79.16 198 1215 12354 3372092
Vertigo 791.87 79.16 174 1239 11458 3372988
Back pain 582.88 79.16 173 1240 37832 3346614
Gait disturbance 496.50 79.16 143 1270 27849 3356597
Encephalopathy 496.35 79.16 110 1303 7352 3377094
Urinary incontinence 485.63 79.16 104 1309 5908 3378538
Malaria 397.32 79.16 55 1358 187 3384259
Depressed level of consciousness 388.64 79.16 98 1315 11367 3373079
Diarrhoea 309.43 79.16 142 1271 104206 3280240
Arthralgia 303.52 79.16 120 1293 60741 3323705
Pruritus 292.86 79.16 109 1304 46724 3337722
Abnormal behaviour 253.31 79.16 68 1345 9960 3374486
Myalgia 227.05 79.16 82 1331 31993 3352453
Language disorder 213.67 79.16 34 1379 346 3384100
Chills 204.49 79.16 69 1344 21953 3362493
Strongyloidiasis 171.83 79.16 28 1385 334 3384112
Agitation 141.28 79.16 51 1362 19655 3364791
Anal incontinence 134.40 79.16 31 1382 2409 3382037
Loss of consciousness 133.91 79.16 54 1359 28093 3356353
Logorrhoea 130.58 79.16 25 1388 781 3383665
Vomiting 130.02 79.16 76 1337 89455 3294991
Neck pain 120.07 79.16 37 1376 8730 3375716
Hypotension 113.48 79.16 57 1356 49457 3334989
Dysstasia 106.09 79.16 28 1385 3788 3380658
Erythema 105.79 79.16 46 1367 28764 3355682
Nuchal rigidity 102.98 79.16 17 1396 220 3384226
Drug ineffective 100.00 79.16 71 1342 116019 3268427
Speech disorder 97.94 79.16 32 1381 9100 3375346
Decubitus ulcer 96.45 79.16 23 1390 2059 3382387
Disorientation 90.90 79.16 31 1382 10048 3374398
Pain 86.13 79.16 54 1359 71503 3312943
Skin irritation 84.84 79.16 20 1393 1703 3382743
Decreased appetite 84.00 79.16 44 1369 41446 3343000
Rosacea 81.29 79.16 16 1397 577 3383869
Skin burning sensation 81.27 79.16 20 1393 2041 3382405

Pharmacologic Action:

SourceCodeDescription
ATC D11AX22 DERMATOLOGICALS
OTHER DERMATOLOGICAL PREPARATIONS
OTHER DERMATOLOGICAL PREPARATIONS
Other dermatologicals
ATC P02CF01 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ANTHELMINTICS
ANTINEMATODAL AGENTS
Avermectines
FDA EPC N0000175484 Antiparasitic
FDA EPC N0000181811 Pediculicide
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000977 Antiparasitic Agents
MeSH PA D007306 Insecticides
MeSH PA D010575 Pesticides
CHEBI has role CHEBI:73333 scabicide
CHEBI has role CHEBI:35443 anthelminthic drug
CHEBI has role CHEBI:35820 antiprotozoal drug
CHEBI has role CHEBI:35444 antinematodal drug
CHEBI has role CHEBI:24852 insecticide

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Infection by Strongyloides indication 1214006 DOID:10955
Infection by Onchocerca volvulus indication 38539003 DOID:11678
Infection by Loa loa contraindication 44250009 DOID:13523
Liver function tests abnormal contraindication 166603001

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 5952372 Sept. 18, 2018 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 6133310 April 26, 2019 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 7550440 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 8080530 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 8093219 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 8415311 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 8470788 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 8815816 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
0.5% SKLICE ARBOR PHARMS LLC N202736 Feb. 7, 2012 RX LOTION TOPICAL 8927595 Oct. 12, 2027 FOR HEAD LICE INFESTATIONS
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 9089587 March 13, 2034 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 9233117 March 13, 2034 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 9233118 March 13, 2034 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 9782425 March 13, 2034 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium-dependent noradrenaline transporter Transporter Ki 5.41 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 6.12 DRUG MATRIX
Muscarinic acetylcholine receptor M1 GPCR Ki 5.92 DRUG MATRIX
Muscarinic acetylcholine receptor M3 GPCR Ki 5.89 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 5.59 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 6.24 DRUG MATRIX
Sodium-dependent dopamine transporter Transporter Ki 5.45 DRUG MATRIX
Adenosine receptor A3 GPCR Ki 6.54 DRUG MATRIX
Multidrug resistance protein 1 Transporter IC50 7 WOMBAT-PK
Neuronal acetylcholine receptor subunit alpha-7 Ion channel ALLOSTERIC MODULATOR EC50 5.10 IUPHAR
Glycine Receptor Ion channel AGONIST EC50 6.40 IUPHAR
Bile acid receptor Nuclear hormone receptor IC50 6.59 CHEMBL
D(1A) dopamine receptor GPCR Ki 5.65 DRUG MATRIX
Alpha-2A adrenergic receptor GPCR Ki 5.66 DRUG MATRIX
Glutamate-gated chloride channel Ion channel MODULATOR CHEMBL CHEMBL
Glutamate-gated chloride channel Ion channel MODULATOR CHEMBL CHEMBL
Sodium/potassium-transporting ATPase subunit alpha-1 Unclassified IC50 5.08 CHEMBL
Sarcoplasmic/endoplasmic reticulum calcium ATPase 2 Unclassified IC50 5.17 CHEMBL
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 Unclassified IC50 4.77 CHEMBL
P2X purinoceptor 4 Unclassified ALLOSTERIC MODULATOR EC50 6.60 IUPHAR

External reference:

IDSource
2373 IUPHAR_LIGAND_ID
4021046 VUID
N0000148510 NUI
C0022322 UMLSCUI
D00804 KEGG_DRUG
DB00602 DRUGBANK_ID
6069 RXNORM
387559003 SNOMEDCT_US
96138006 SNOMEDCT_US
4941 MMSL
d04101 MMSL
4021046 VANDF
71965 MMSL
N0000148510 NDFRT
N0000006374 NDFRT
005266 NDDF
8883YP2R6D UNII
4828 INN_ID
CHEMBL1200633 ChEMBL_ID
D007559 MESH_DESCRIPTOR_UI
6321424 PUBCHEM_CID
CHEBI:6078 CHEBI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
STROMECTOL HUMAN PRESCRIPTION DRUG LABEL 1 0006-0032 TABLET 3 mg ORAL NDA 11 sections
SOOLANTRA HUMAN PRESCRIPTION DRUG LABEL 1 0299-3823 CREAM 10 mg TOPICAL NDA 16 sections
Sklice HUMAN PRESCRIPTION DRUG LABEL 1 24338-183 LOTION 5 mg TOPICAL NDA 17 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 42799-806 TABLET 3 mg ORAL ANDA 12 sections
Sklice HUMAN PRESCRIPTION DRUG LABEL 1 49281-183 LOTION 0.59 g TOPICAL NDA 16 sections
STROMECTOL HUMAN PRESCRIPTION DRUG LABEL 1 55695-019 TABLET 3 mg ORAL NDA 11 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 63629-7275 TABLET 3 mg ORAL ANDA 12 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 76413-155 TABLET 3 mg ORAL ANDA 12 sections