Mefloquine
Antimalarial — ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
Also known as: (+/-)-Mefloquine, lariam, mefloquin, mefloquine HCl, mefloquine hydrochloride, mephaquin, mephloquine, mephloquine HCl, mephloquine hydrochloride
Data last refreshed: (DrugCentral release 2024-11-01)
Key facts
Mefloquine is an ofp drug in the Antimalarial class catalogued in DrugCentral. It was first approved by the FDA in 1989. DrugCentral lists 7 molecular targets, including ADORA2A, ADORA1 and GLRA1. Recorded indications include Chloroquine Resistant Plasmodium Falciparum Malaria, Chloroquine-Resistant Plasmodium Falciparum Malaria Prevention and Vivax malaria.
- Approval status: ofp (first approved 1989 by the FDA).
- Drug class: Antimalarial.
- Molecular targets: ADORA2A, ADORA1, GLRA1 and KCNH2 (7 listed in DrugCentral).
- Indications: Chloroquine Resistant Plasmodium Falciparum Malaria, Chloroquine-Resistant Plasmodium Falciparum Malaria Prevention and Vivax malaria.
- ATC code: P01BC02 (Methanolquinolines).
- Molecular formula: C17H16F6N2O; molecular weight 378.32 g/mol.
Indications & contraindications
Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).
Indications (3)
- Chloroquine Resistant Plasmodium Falciparum Malaria
- Chloroquine-Resistant Plasmodium Falciparum Malaria Prevention
- Vivax malaria
Contraindications (12)
- Ataxia
- Atrioventricular block
- Depressive disorder
- Disease of liver
- Generalized anxiety disorder
- Prolonged QT interval
- Psychiatric Disturbance
- Psychotic disorder
- Schizophrenia
- Seizure disorder
- Sinus bradycardia
- Sinus node dysfunction
Mechanism & targets
| Established pharmacologic class | Antimalarial |
|---|
Molecular targets (7)
| Target | Gene | Action | Activity |
|---|---|---|---|
| Adenosine receptor A2a | ADORA2A | unknown | Ki 6.91 |
| Adenosine receptor A1 | ADORA1 | unknown | Ki 5.91 |
| Glycine receptor subunit alpha-1 | GLRA1 | unknown | EC50 5.60 |
| Potassium voltage-gated channel subfamily H member 2 | KCNH2 | unknown | IC50 5.25 |
| Protein kinase Pfmrk | Pfmrk | unknown | IC50 4.92 |
| Hemoglobin subunit alpha | HBA1 | unknown | — |
| Multidrug resistance protein 1 | ABCB1 | unknown | — |
Regulatory approvals (1)
| Date | Agency | Marketed as | Applicant | Orphan |
|---|---|---|---|---|
| 1989-05-02 | FDA | — | — |
ATC classification
| ATC code | Therapeutic hierarchy |
|---|---|
P01BC02 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › ANTIMALARIALS › Methanolquinolines |
P01BF02 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › ANTIMALARIALS › Artemisinin and derivatives, combinations |
Pharmacogenomics
Drug-label and guideline annotations from PharmGKB and CPIC.
- Swissmedic label: G6PD · Informative PGx
Reported adverse-event signals
Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.
| MedDRA term | LLR |
|---|---|
| Progressive multifocal leukoencephalopathy | 254.2 |
| Immune reconstitution inflammatory syndrome | 155.6 |
| JC virus infection | 140.1 |
| Product use in unapproved indication | 65.1 |
Chemical structure
| Molecular formula | C17H16F6N2O |
|---|---|
| Molecular weight | 378.32 g/mol |
| CAS number | 53230-10-7 |
| InChIKey | XEEQGYMUWCZPDN-DOMZBBRYSA-N |
| PubChem CID | 4046 |
Frequently asked questions
Answers are generated from the structured data on this page, not written by hand.
What is Mefloquine used for?
DrugCentral lists the following indications for Mefloquine: Chloroquine Resistant Plasmodium Falciparum Malaria, Chloroquine-Resistant Plasmodium Falciparum Malaria Prevention and Vivax malaria.
How does Mefloquine work?
Its molecular targets in DrugCentral include ADORA2A, ADORA1, GLRA1 and KCNH2.
When was Mefloquine first approved?
Mefloquine was first approved by the FDA in 1989.
What drug class does Mefloquine belong to?
Mefloquine is in the Antimalarial class.
What is the chemical formula of Mefloquine?
Mefloquine has the molecular formula C17H16F6N2O and a molecular weight of 378.32 g/mol.
Browse: all drugs starting with M · drug guides by category · protein targets A–Z.
Sources
- DrugCentral drug card 1665 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
- ChEMBL CHEMBL416956 — compound record and bioactivity
- PubChem CID 4046 — chemical identifiers
- DrugBank DB00358 — drug record
- FDA UNII TML814419R — substance identity
- DailyMed: FDA labels for Mefloquine — current prescribing information (label search)
- UniProt P29274 (ADORA2A) — target protein
- UniProt P30542 (ADORA1) — target protein
- UniProt P23415 (GLRA1) — target protein
- UniProt Q12809 (KCNH2) — target protein
- UniProt P69905 (HBA1) — target protein
- UniProt P08183 (ABCB1) — target protein
- FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
- PharmGKB / CPIC — pharmacogenomic label annotations
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