ivermectin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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. In vitro data suggest evidence of activity against SARS-CoV-2, but to date available data are insufficient to recommend either for or against the use of ivermectin for the treatment of COVID-19. FDA issued a warning concerning possi-ble inappropriate use of ivermectin products intended for animals as an attempt to self-medicate for the treat-ment of COVID-19.
  • Molecular weight: 1736.19
  • Formula: C95H146O28
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
12 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 4 mg/mL Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.17 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Nov. 22, 1996 FDA MERCK SHARP DOHME

FDA Adverse Event Reporting System (Female)

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
Conjunctival haemorrhage 277.01 34.75 60 3399 2921 46679682
Ocular hyperaemia 183.77 34.75 65 3394 19645 46662958
Asthenia 162.15 34.75 153 3306 310922 46371681
Headache 146.07 34.75 177 3282 478175 46204428
Vertigo 134.50 34.75 69 3390 51979 46630624
Strongyloidiasis 118.36 34.75 24 3435 841 46681762
Malaria 106.48 34.75 18 3441 224 46682379
Skin irritation 83.21 34.75 28 3431 7259 46675344
Pyrexia 80.67 34.75 113 3346 348689 46333914
Somatic delusion 77.91 34.75 16 3443 597 46682006
Coma 72.15 34.75 48 3411 58301 46624302
Acarodermatitis 58.53 34.75 13 3446 707 46681896
Logorrhoea 56.48 34.75 16 3443 2343 46680260
Depressed level of consciousness 51.33 34.75 36 3423 47533 46635070
Skin burning sensation 48.68 34.75 21 3438 10671 46671932
Erythema 48.19 34.75 56 3403 142764 46539839
Abnormal faeces 47.96 34.75 16 3443 4033 46678570
Encephalopathy 47.28 34.75 30 3429 33559 46649044
Gastrointestinal motility disorder 46.38 34.75 16 3443 4462 46678141
Urine odour abnormal 44.78 34.75 16 3443 4946 46677657
Pruritus 42.22 34.75 69 3390 242283 46440320
Oral discomfort 40.86 34.75 17 3442 7901 46674702
Rosacea 38.39 34.75 13 3446 3428 46679175

FDA Adverse Event Reporting System (Male)

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
Conjunctival haemorrhage 896.71 39.56 179 4798 2521 29944980
Ocular hyperaemia 662.14 39.56 175 4802 8868 29938633
Asthenia 511.24 39.56 361 4616 220929 29726572
Headache 485.45 39.56 325 4652 181981 29765520
Coma 401.73 39.56 174 4803 40275 29907226
Vertigo 311.16 39.56 123 4854 22512 29924989
Pyrexia 284.63 39.56 292 4685 294197 29653304
Urinary incontinence 250.08 39.56 97 4880 16843 29930658
Malaria 222.69 39.56 38 4939 203 29947298
Back pain 179.80 39.56 143 4834 102453 29845048
Gait disturbance 156.64 39.56 116 4861 74661 29872840
Encephalopathy 156.04 39.56 85 4892 32120 29915381
Strongyloidiasis 113.97 39.56 33 4944 2313 29945188
Depressed level of consciousness 107.17 39.56 71 4906 38151 29909350
Language disorder 94.29 39.56 25 4952 1263 29946238
Abnormal behaviour 85.14 39.56 53 4924 25570 29921931
Myalgia 74.69 39.56 77 4900 76590 29870911
Arthralgia 72.06 39.56 100 4877 135691 29811810
Nuchal rigidity 71.60 39.56 15 4962 267 29947234
Logorrhoea 65.61 39.56 21 4956 2061 29945440
Pruritus 61.09 39.56 86 4891 118118 29829383
Filariasis 53.92 39.56 7 4970 0 29947501
Anal incontinence 53.18 39.56 25 4952 6897 29940604
Chills 48.72 39.56 60 4917 72278 29875223
Stupor 47.36 39.56 18 4959 2935 29944566
Adverse event 46.59 39.56 30 4947 15311 29932190
Blood smear test abnormal 46.22 39.56 6 4971 0 29947501

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
CHEBI has role CHEBI:24852 insecticides
CHEBI has role CHEBI:35443 anthelminthic
CHEBI has role CHEBI:35444 antinematodals
CHEBI has role CHEBI:35820 antiprotozoal agent
CHEBI has role CHEBI:73333 scabicides
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000977 Antiparasitic Agents
MeSH PA D007306 Insecticides
MeSH PA D010575 Pesticides
FDA EPC N0000181811 Pediculicide

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)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Alpha-2A adrenergic receptor GPCR Ki 5.66 DRUG MATRIX
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
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
SARS-CoV-2 Virus INHIBITOR IC50 5.69 SCIENTIFIC LITERATURE
P2X purinoceptor 4 Unclassified ALLOSTERIC MODULATOR EC50 6.60 IUPHAR

External reference:

IDSource
4021046 VUID
N0000148510 NUI
D00804 KEGG_DRUG
4021046 VANDF
C0022322 UMLSCUI
CHEBI:6078 CHEBI
IVM PDB_CHEM_ID
CHEMBL1200633 ChEMBL_ID
D007559 MESH_DESCRIPTOR_UI
DB00602 DRUGBANK_ID
2373 IUPHAR_LIGAND_ID
4828 INN_ID
8883YP2R6D UNII
3085416 PUBCHEM_CID
6069 RXNORM
4941 MMSL
71965 MMSL
d04101 MMSL
005266 NDDF
387559003 SNOMEDCT_US
96138006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
STROMECTOL HUMAN PRESCRIPTION DRUG LABEL 1 0006-0032 TABLET 3 mg ORAL NDA 26 sections
SOOLANTRA HUMAN PRESCRIPTION DRUG LABEL 1 0299-3823 CREAM 10 mg TOPICAL NDA 26 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 0574-2107 CREAM 10 mg TOPICAL NDA authorized generic 26 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 0591-4052 CREAM 10 mg TOPICAL ANDA 25 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 42799-806 TABLET 3 mg ORAL ANDA 25 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 51672-4211 LOTION 5 mg TOPICAL ANDA 27 sections
Ivermectin HUMAN OTC DRUG LABEL 1 51672-4230 LOTION 5 mg TOPICAL ANDA 17 sections
STROMECTOL HUMAN PRESCRIPTION DRUG LABEL 1 55695-019 TABLET 3 mg ORAL NDA 26 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 63629-7275 TABLET 3 mg ORAL ANDA 24 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 66993-948 CREAM 10 mg TOPICAL NDA authorized generic 26 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 68071-2242 TABLET 3 mg ORAL ANDA 25 sections
BRIMONIDINE TARTRATE 0.25% / IVERMECTIN 1% / METRONIDAZOLE 1% / NIACINULLMIDE 4% HUMAN PRESCRIPTION DRUG LABEL 4 72934-1028 GEL 1 g TOPICAL unapproved drug other 4 sections
IVERMECTIN 1% / METRONIDAZOLE 1% HUMAN PRESCRIPTION DRUG LABEL 2 72934-1130 GEL 1 g TOPICAL unapproved drug other 4 sections
IVERMECTIN 1% / METRONIDAZOLE 1% / NIACINULLMIDE 4% HUMAN PRESCRIPTION DRUG LABEL 3 72934-1131 GEL 1 g TOPICAL unapproved drug other 4 sections
171083 IVERMECTIN 1% / METRONIDAZOLE 1% / NIACINULLMIDE 4% HUMAN PRESCRIPTION DRUG LABEL 3 72934-1237 GEL 1 g TOPICAL unapproved drug other 4 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 76413-155 TABLET 3 mg ORAL ANDA 24 sections