Chemical formula: C₁₁H₁₆ClN₅ Molecular mass: 253.731 g/mol PubChem compound: 4923
Proguanil interacts in the following cases:
Based on a theoretical model derived from a single dose pharmacokinetic study, the following guidance is given for adults with renal impairment. Proguanil should be used with caution in patients with severe renal impairment.
| Creatinine clearance (ml/min 1.73 m²) | Dosage |
|---|---|
| ≥60 | 200 mg once daily (standard dose) |
| 20 to 59 | 100 mg once daily |
| 10 to 19 | 50 mg every second day |
| <10 | 50 mg once weekly |
The grade of renal impairment and/or the serum creatinine concentration may be approximately equated to creatinine clearance levels as indicated below.
| Creatinine clearance (ml/min/1.73 m²) | Approx* serum creatinine (micromol/1) | Renal Impairment Grade (arbitrarily divided for dosage purposes) |
|---|---|---|
| ≥60 | - | - |
| 20 to 59 | 150 to 300 | Mild |
| 10 to 19 | 300 to 700 | Moderate |
| <10 | >700 | Severe |
* Serum creatinine concentration is only an approximate guide to renal function unless corrected for age, weight and sex.
Antacids may reduce the absorption of proguanil, so should be taken at least 2-3 hours apart.
Proguanil can potentiate the anticoagulant effect of warfarin and related anticoagulants through a possible interference with their metabolic pathways. Caution is advised when initiating or withdrawing malaria prophylaxis with proguanil in patients on continuous treatment with anticoagulants.
When given with boosted protease-inhibitors, reduction in proguanil exposure has been observed. This combination should be avoided when possible.
There are limited data available from the use of proguanil in pregnant women.
Proguanil should not be used during pregnancy unless, in the judgement of the physician, potential benefit outweighs the risk.
Malaria in pregnant women increases the risk of maternal death, miscarriage, still-birth and low birth weight with the associated risk of neonatal death. Although travel to malarious areas should be avoided during pregnancy, if this is unavoidable effective prophylaxis is therefore strongly advised in pregnant women.
Proguanil is a dihydrofolate reductase inhibitor and adequate folate supplements should be given to pregnant women taking proguanil.
Although proguanil is excreted in breast milk, the amount is insufficient to confer any benefit on the infant. Separate chemoprophylaxis for the infant is required.
There is no evidence to suggest that proguanil causes sedation or is likely to affect concentration.
Undesirable effects are listed by MedDRA System Organ Classes.
Assessment of undesirable effects is based on the following frequency groupings:
Very common: ≥1/10
Common: ≥1/100 to <1/10
Uncommon: ≥1/1,000 to <1/100
Rare: ≥1/10,000 to <1/1,000
Very rare: <1/10,000
Not known: cannot be estimated from the available data
| System Organ Class | Undesirable Effect and Frequency |
|---|---|
| Blood and lymphatic system disorders | Not known: Haematological changes such as aplastic anaemia, anaemia megaloblastic and pancytopenia |
| Immune system disorders | Not known: Hypersensitivity, including urticaria, angioedema Vasculitis |
| Gastrointestinal disorders | Not known: Gastric disorder, including diarrhoea and constipation* Mouth ulceration Stomatitis |
| Hepatobiliary disorders | Not known Cholestasis |
| Skin and subcutaneous tissue disorders | Not known Skin reactions such as skin exfoliation, rash, pruritus and alopecia** |
| General disorders and administration site conditions | Not known Pyrexia |
* usually subsides as treatment is continued.
** reversible alopecia
© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.
