Plot 1 Junaid Dosunmu Street,Central Business District, Alausa, P.0. Box 3560 Ikeja, Lagos, Nigeria.
Tel: + 234-1-774-1205
AstraZeneca, Silk Court, Silk Road Business Park, Macclesfield, Cheshire SK10 2NA, England
Dosage Form, Composition & NAFDAC Registration Number (NRN)
Tablet (NRN: 04-0364): Proguanil HCl BP 100 mg.
Paludrine is effective against the tissue forms of some strains of P. falciparum and acts through an active metabolite cycloguanil. The mechanism of action is probably due to inhibition of dihydrofolate reductase. The effect of this action is to prevent schizogony and its main effect is against the developing primary tissue schizonts.
Proguanil is well absorbed in man with peak plasma concentrations of approximately 140 ng/ml occurring around four hours after an oral dose of 200 mg to an adult.
The active triazine metabolite cycloguanil peaks at approximately 75 ng/ml one hour later. The elimination half-lives for proguanil and cycloguanil are reported to be of the order of 20 hours. There is a low degree of drug accumulation after repeat doses, leading to steady state conditions after approximately three days. When daily doses are not taken, blood levels fall sharply but do not disappear completely until at least two or three doses are missed.
Prevention and suppression of malaria.
Severe renal failure.
Pregnancy: Pregnancy increases the risks from malaria. It is generally accepted that all drug treatment should be avoided if possible during the first trimester of pregnancy. Paludrine has been widely used for more than 40 years and a casual connection between its use and any adverse effect on mother or foetus has not been established.
Lactation: Although Paludrine is excreted in breast milk, the amount is insufficient to confer any benefit on the infant. Separate chemoprophylaxis for the infant is required.
Effect on ability to drive or operate machinery: There is no evidence to suggest that Paludrine causes sedation or is likely to affect concentration.
At normal dosage levels the side effect most commonly encountered is mild gastric intolerance. This usually subsides as treatment is continued. Mouth ulceration and stomatitis have on occasion been reported. Isolated cases of skin reactions and reversible hair loss have been reported in association with the use of proguanil.
Dosage & Administration
Dosage & Administration
Adults (including the elderly): 2 tablets (200 mg) daily.
Under 1 year ¼ tablet (25 mg) daily
1 - 4 years ½ tablet (50 mg daily)
5 - 8 years 1 tablet (100 mg) daily
9 - 14 years 1½ tablets (150 mg) daily
Over 14 years Adult dose daily.
The daily dose is best taken with water, after food, at the same time each day. For a young child, the dose may be administered crushed and mixed with milk, honey or jam. Non-immune subjects entering a malarious region are advised to begin treatment with Paludrine at least 24 hours before arrival.
The daily dose of Paludrine should be continued throughout exposure to risk and for four weeks after leaving the area. The value of malaria prophylaxis in subjects with partial immunity is debatable. However, malaria prophylaxis may be of value in certain high risk groups.
Overdosage The following effects have been reported in cases of overdosage: haematuria, renal irritation, epigastric discomfort and vomiting. There is no specific antidote and symptoms should be treated as they arise
Store at room temperature.