mefloquine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
quinoline derivatives	1665	53230-10-7

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

mephloquine
mephloquine HCl
mephloquine hydrochloride
mefloquine
(+/-)-Mefloquine
lariam
mefloquin
mephaquin
mefloquine hydrochloride
mefloquine HCl

A phospholipid-interacting antimalarial drug (ANTIMALARIALS). It is very effective against PLASMODIUM FALCIPARUM with very few side effects.

Molecular weight: 378.32
Formula: C17H16F6N2O
CLOGP: 3.67
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 45.15
ALOGS: -4
ROTB: 4

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
1	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	9 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	47.20 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	80 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
fu (Fraction unbound in plasma)	0 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Approvals:

Date	Agency	Company	Orphan
May 2, 1989	FDA

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
Immune reconstitution inflammatory syndrome	80.33	43.19	15	265	6069	63482673
Product use in unapproved indication	70.42	43.19	27	253	179053	63309689
Progressive multifocal leukoencephalopathy	63.41	43.19	14	266	12957	63475785

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
Progressive multifocal leukoencephalopathy	98.35	62.82	22	322	9742	34946845

FDA Adverse Event Reporting System (Geriatric)

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
Progressive multifocal leukoencephalopathy	144.92	48.60	33	568	20567	79723220
JC virus infection	91.48	48.60	17	584	3864	79739923
Immune reconstitution inflammatory syndrome	80.30	48.60	19	582	13822	79729965

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	P01BC02	ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS ANTIMALARIALS Methanolquinolines
ATC	P01BF02	ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS ANTIMALARIALS Artemisinin and derivatives, combinations
FDA EPC	N0000175482	Antimalarial
CHEBI has role	CHEBI:38068	antimalarials
CHEBI has role	CHEBI:149553	anticoronaviral drug
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000962	Antimalarials
MeSH PA	D000977	Antiparasitic Agents
MeSH PA	D000981	Antiprotozoal Agents

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Vivax malaria	indication	27052006	DOID:12978
Chloroquine-Resistant Plasmodium Falciparum Malaria Prevention	indication
Chloroquine Resistant Plasmodium Falciparum Malaria	indication
Ataxia	contraindication	20262006
Generalized anxiety disorder	contraindication	21897009	DOID:14320
Depressive disorder	contraindication	35489007
Sinus bradycardia	contraindication	49710005
Schizophrenia	contraindication	58214004	DOID:5419
Sinus node dysfunction	contraindication	60423000
Psychotic disorder	contraindication	69322001
Prolonged QT interval	contraindication	111975006
Seizure disorder	contraindication	128613002
Atrioventricular block	contraindication	233917008	DOID:0050820
Disease of liver	contraindication	235856003	DOID:409
Psychiatric Disturbance	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.95	acidic
pKa2	8.56	Basic
pKa3	4.89	Basic

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])	Mechanism action	Bioact source	MoA source
Adenosine receptor A2a	GPCR	P29274	AA2AR_HUMAN		Ki	6.91		CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.25		WOMBAT-PK
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN					WOMBAT-PK
Adenosine receptor A1	GPCR	P30542	AA1R_HUMAN		Ki	5.91		CHEMBL
Hemoglobin subunit alpha	Secreted	P69905	HBA_HUMAN					WOMBAT-PK
Glycine receptor subunit alpha-1	Ion channel	P23415	GLRA1_HUMAN		EC50	5.60		CHEMBL
Protein kinase Pfmrk	Unclassified		P90584_PLAFA		IC50	4.92		CHEMBL

External reference:

ID	Source
4019811	VUID
N0000147900	NUI
D00831	KEGG_DRUG
51773-92-3	SECONDARY_CAS_RN
4019498	VANDF
4019811	VANDF
C0025153	UMLSCUI
CHEBI:63609	CHEBI
YMZ	PDB_CHEM_ID
CHEMBL411685	ChEMBL_ID
CHEMBL416956	ChEMBL_ID
CHEMBL411686	ChEMBL_ID
DB00358	DRUGBANK_ID
CHEMBL535650	ChEMBL_ID
D015767	MESH_DESCRIPTOR_UI
40692	PUBCHEM_CID
4252	IUPHAR_LIGAND_ID
3777	INN_ID
TML814419R	UNII
202989	RXNORM
1710	MMSL
43453	MMSL
5035	MMSL
d00286	MMSL
003537	NDDF
004873	NDDF
387505001	SNOMEDCT_US
412243001	SNOMEDCT_US
87567009	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Mefloquine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0025	TABLET	250 mg	ORAL	ANDA	24 sections
Mefloquine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0555-0171	TABLET	250 mg	ORAL	ANDA	23 sections
Mefloquine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0555-0171	TABLET	250 mg	ORAL	ANDA	23 sections
Mefloquine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	21695-449	TABLET	250 mg	ORAL	ANDA	23 sections
Mefloquine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	21695-561	TABLET	250 mg	ORAL	ANDA	26 sections
Mefloquine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-2396	TABLET	250 mg	ORAL	ANDA	23 sections
Mefloquine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-2396	TABLET	250 mg	ORAL	ANDA	23 sections
Mefloquine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	52959-803	TABLET	250 mg	ORAL	ANDA	26 sections
Mefloquine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5434	TABLET	250 mg	ORAL	ANDA	13 sections
Mefloquine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	68071-4702	TABLET	250 mg	ORAL	ANDA	23 sections