Proguanil: Indication, Dosage, Side Effect, Precaution

Generic Medicine Info Patient Medicine Information

This information is not country-specific. Please refer to the Myanmar prescribing information.

Generic Medicine Info

Indications and Dosage

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

Storage

Store below 30°C.

MIMS Class

Antimalarials

ATC Classification

P01BB01 - proguanil ; Belongs to the class of biguanide antimalarials.

References

Buckingham R (ed). Proguanil Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/02/2016.

Joint Formulary Committee. Proguanil Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/02/2016.

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