Auranofin
Severe
Database
Clinical effect not specified
Source: DDInter
Drug reference
Proguanil
Antimalarial
Also known as proguanil hydrochloride
Antimalarial
CDSCO approvedSchedule H
EXCRETION
—
not curated
INTERACTIONS
4 major
SEVERE in our sources
PREGNANCY
, in breastfeeding women, and in children under 12 years. All
FDA category + note
Top interactionssee all 8 →
- AuranofinSevereDatabaseDDInter
- AurothioglucoseSevereDatabaseDDInter
- EfavirenzSevereDatabaseDDInter
- Sodium AurothiomalateSevereDatabaseDDInter
Mechanism
Proguanil is a prodrug that is metabolized by CYP2C19 to its active triazine metabolite cycloguanil, which selectively inhibits plasmodial dihydrofolate reductase-thymidylate synthetase — an enzyme critical for de novo folate synthesis in the parasite but structurally distinct from the mammalian enzyme. This blocks parasite DNA synthesis and schizogony. Proguanil also has an independent antiparasitic mechanism (possibly involving mitochondrial membrane potential disruption) that synergizes with atovaquone in the fixed-dose combination Malarone.
Indications
Prophylaxis of falciparum malaria (with atovaquone)Treatment of acute, uncomplicated falciparum malaria (with atovaquone)Prophylaxis of malaria in areas of the world with little chloroquine resistance (usually with chloroquine hydrochloride)partner drug in act (atovaquone-proguanil)chemoprophylaxis (as single agent in england and europe)effective for drug-resistant p. falciparum or p. vivax when administered with atovaquonecausal prophylaxis (primarily for P. falciparum, but not used in India)prophylaxis for travellers visiting malaria endemic areas (in combination with atovaquone)Combination with atovaquone for treatment of multidrug resistant falciparum malaria (USA, Thailand, some other countries)Causal prophylactic (in combination with atovaquone) for travellers visiting CQ-resistant/multidrug-resistant P.f. endemic areasSuppressive prophylactic (in combination with CQ) in moderately CQ-resistant P.f. areas (historically in Africa)
Dosing
- Adult
- (white patches) if the dose is too large for the child’s age (taking into account the fluoride content of the local drinking water and of toothpaste). The risk of osteonecrosis of the jaw is substantially greater for patients receiving intravenous bisphosphonates in the treatment of cancer than for patients receiving oral bisphosphonates for osteoporosis or Paget’s disease.…
Pharmacokinetics
Onset
approximately 5 h
Half-life
180 to 200 h or longer
Bioavailability
extensively absorbed regardless of food intake
Protein binding
Noncumulative
Metabolism
oxidized to cycloguanil and 4-chlorophenyl biguanide by the CYP2C subfamily
Excretion
40% to 60% in urine (parent drug or active metabolite)
Contraindications
- severe renal impairment (creatinine clearance <30 ml/min)
- hypersensitivity to atovaquone or proguanil
Side effects
Common
Oral ulcerationnauseadiarrheaMild abdominal symptomsVomitingOccasional stomatitisHaematuriaRashesTransient loss of hairurticaria
Serious
- vomiting (large doses)
- abdominal pain (large doses)
- diarrhea (large doses)
- hematuria (large doses)
- transient epithelial cells and casts in urine (large doses)
- hematuria
- gi disturbances
Pregnancy & lactation
Pregnancy
, in breastfeeding women, and in children under 12 years. All
Drug interactions
Aurothioglucose
Severe
Database
Clinical effect not specified
Source: DDInter
Efavirenz
Severe
Database
Decreased plasma levels of proguanil.
Source: DDInter
Sodium Aurothiomalate
Severe
Database
Clinical effect not specified
Source: DDInter
Atazanavir
Moderate
Textbook
Decreased plasma levels of proguanil.
Source: Harrison 22e · p1743
Atovaquone
Moderate
Textbook
Enhanced antimalarial efficacy and reduced resistance development against multidrug resistant falciparum malaria.
Source: KDT 7e · p816-835
Lopinavir Ritonavir
Moderate
Textbook
Decreased plasma levels of proguanil.
Source: Harrison 22e · p1743
Pyrimethamine
Moderate
Database
Increased risk of bone marrow suppression.
Source: DDInter
4 additional low-confidence interactions hidden — those rows lack a documented mechanism or management plan in our sources.
Related guidelines
Other Antimalarial drugs
Ask House about Proguanil
Continue into a citation-backed clinical answer with the drug context already attached.
Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, BNF·Verified: 2026-05-13 · House clinical team