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ivermectin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antiparasitics, ivermectin derivatives	3972	70288-86-7

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
12	mg	O

ADMET properties:

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

Approvals:

Date	Agency	Company	Orphan
Nov. 22, 1996	FDA	MERCK SHARP DOHME

FDA Adverse Event Reporting System (Female)

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

FDA Adverse Event Reporting System (Male)

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

Pharmacologic Action:

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

Drug Use (View source of the data)

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

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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.66	DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.41	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	6.12	DRUG MATRIX
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	5.92	DRUG MATRIX
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	5.89	DRUG MATRIX
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	5.59	DRUG MATRIX
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	6.24	DRUG MATRIX
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	5.45	DRUG MATRIX
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	6.54	DRUG MATRIX
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	7	WOMBAT-PK
Neuronal acetylcholine receptor subunit alpha-7	Ion channel	P36544	ACHA7_HUMAN	ALLOSTERIC MODULATOR	EC50	5.10	IUPHAR
Glycine Receptor	Ion channel	O75311 P23415 P23416 P48167	GLRA1_HUMAN GLRA2_HUMAN GLRA3_HUMAN GLRB_HUMAN	AGONIST	EC50	6.40	IUPHAR
Bile acid receptor	Nuclear hormone receptor	Q96RI1	NR1H4_HUMAN		IC50	6.59	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	5.65	DRUG MATRIX
Glutamate-gated chloride channel	Ion channel		GLUCB_HAECO	MODULATOR			CHEMBL	CHEMBL
Glutamate-gated chloride channel	Ion channel		Q25634_ONCVO	MODULATOR			CHEMBL	CHEMBL
Sodium/potassium-transporting ATPase subunit alpha-1	Unclassified		AT1A1_RAT		IC50	5.08	CHEMBL
Sarcoplasmic/endoplasmic reticulum calcium ATPase 2	Unclassified		AT2A2_RAT		IC50	5.17	CHEMBL
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1	Unclassified		AT2A1_RAT		IC50	4.77	CHEMBL
SARS-CoV-2	Virus			INHIBITOR	IC50	5.69	SCIENTIFIC LITERATURE
P2X purinoceptor 4	Unclassified		P2RX4_RAT	ALLOSTERIC MODULATOR	EC50	6.60	IUPHAR

External reference:

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

Pharmaceutical products:

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