Proguanil


Concise Prescribing Info
Indications/Uses
Malaria prophylaxis.
Dosage/Direction for Use
Adult : PO 200 mg/day. Start 1 wk before exposure to malaria or 1-2 days prior to travel. Continue throughout exposure and for at least 4 wk after leaving a malaria-infested area.
Dosage Details
Oral
Prophylaxis of malaria
Adult: 200 mg daily. Start chemoprophylaxis for travellers 1 wk before exposure to malaria, or 1-2 days prior to travel. Continue admin throughout exposure and for at least 4 wk (or 1 wk if given w/ atovaquone) after leaving a malaria-infested area.
Child: <1 yr 25 mg daily; 1-4 yr 50 mg daily; 5-8 yr 100 mg daily; 9-14 yr 150 mg daily; >14 yr Same as adult dose. Start at least 2 days before entering the malarious area and continue for the whole period of stay and 4 wk after leaving the area.
Renal Impairment
CrCl (mL/min) Dosage
<10 50 mg once wkly.
10-19 50 mg every other day.
20-59 100 mg daily.
Administration
Should be taken with food. Tab may be crushed & mixed w/ milk, honey or jam just before swallowing.
Special Precautions
Renal impairment. Childn. Pregnancy and lactation.
Adverse Reactions
Mild gastric intolerance, diarrhoea, constipation, aphthous ulceration, stomatitis; urticaria, angioedema, vasculitis, reversible hair loss; drug fever, cholestasis; seizures, psychotic events; haematological changes in patients w/ severe renal impairment.
Drug Interactions
Reduced absorption by antacids. May potentiate anticoagulant effect of warfarin and related anticoagulants through a possible interference w/ their metabolic pathways.
Action
Description: Proguanil is a biguanide derivative, metabolised in the body to its active metabolite, cycloguanil. Cycloguanil acts by inhibiting plasmodial dihydrofolate reductase, thus, preventing nucleic acid synthesis in the parasite. It is active against pre-erythrocytic forms and is a slow-acting blood schizontocide.
Pharmacokinetics:
Absorption: Readily absorbed from the GI tract. Time to peak plasma concentration: W/in approx 4 hr.
Distribution: Distributed into breast milk (small amounts). Plasma protein binding: Approx 75%.
Metabolism: Undergoes hepatic metabolism to its active metabolite, cycloguanil by CYP2C19 isoenzyme.
Excretion: Via faeces and principally, in the urine (approx 40-60%) as unchanged drug (60%) and cycloguanil (30%). Elimination half-life: Approx 20 hr.
Chemical Structure

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Storage
Store below 30°C.
MIMS Class
ATC Classification
P01BB01 - proguanil ; Belongs to the class of biguanide antimalarials.
Disclaimer: This information is independently developed by MIMS based on Proguanil from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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