Stem definition | Drug id | CAS RN |
---|---|---|
antiparasitics, ivermectin derivatives | 3972 | 70288-86-7 |
Molecule | Description |
---|---|
Synonyms:
|
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.
|
Dose | Unit | Route |
---|---|---|
12 | mg | O |
Property | Value | Reference |
---|---|---|
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 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Date | Agency | Company | Orphan |
---|---|---|---|
Nov. 22, 1996 | FDA | MERCK SHARP DOHME |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
Source | Code | Description |
---|---|---|
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 |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
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 |
None
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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 |
ID | Source |
---|---|
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 |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
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 |