Proguanil Tablets B.P.
Each Uncoated Tablet Contains:
Proguanil Hydrochloride BP 100mg
MECHANISM OF ACTION
The active triazine metabolite, inhibits plasmodial dihydrofolate reductase and thus disrupts the synthesis of nucleic acids in the parasite.
Proguanil is indicated for the causal prophylaxis of falciparum (p. falciparum) malaria, proguanil also suppresses other forms of malaria, and it is used to reduce transmission of infection. Proguanil should not be used alone in countries where chloroquine-resistant malaria has been confirmed.
Known or suspected hypersensitivity to proguanil.
DOSAGE AND ADMINISTRATION
For prophylaxis of malaria
Adults: Usual dose iS 100 mg daily. In highly endemic areas this dose may be safely increased to 200mg daily. The daily dose is best taken with water after food. Nonimmune subjects entering a malarious region are advised to begin treatment with proguanil at least 24 hours before arrival. A daily dose of proguanil should be continued for weeks after leaving the area.
Elderly: There are no special dosage recommendations for the elderly, but it may be advisable to monitor elderly patients so that optimum dosage can be individually determined.
Children: Under 1 year 25 mg daily; 1 to 4years: 50 mg daily; 5 to 8 years: 15 mg daily; 9 to 12 years: 100 mg daily; over 12 years: adult dose daily.
For a young child, the dose may be administered crushed and mixed with milk, honey or jam. For all countries with chloroquine-resistant malaria: The dose of proguanil is increased to 200 mg daily with chloroquine (base) given 300 mg once a week, i.e., approximately equivalent to 500 mg chloroquine phosphate.
For more Information on the management of overdose or unintentional ingestion, contact a Poison Control Center (sea Poison Control Center Listing). Clinical effects of overdose: The following effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate) -not necessarily inclusive: Acute Epigastric discomfort (abdominal or stomach pain); hematuria (blood in urine; lower back pain; pain or burning while urinating); renal irritation (pains or burning while urinating); or vomiting.
TREATMENT OF OVERDOSE
Because there is no specific antidote for proguanil overdose, treatment should include the following: Specific treatment – Symptomatic treatment may be given.
Supportive care – Supportive measures necessary for maintaining the vital functions of the patient may be administered. Patients in whom intentional overdose is confirmed or suspected should be referred for psychiatric consultation.
At normal therapeutic doses, the adverse effect most commonly encountered is mild gastric intolerance. This usually subsides as treatment is continued. Mouth ulceration has occasionally been reported. Large doses (1 g daily) may cause vomiting, abdominal pain, hematuria and renal irritation. Blood dyscrasias have been reported in patients with renal failure given proguanil. Selected cases of skin reactions and reversible hair loss have been reported in association with the use of proguanil.
It is generally accepted that all drug treatment should be avoided if possible during the first trimester of pregnancy. A causal connection between the use of proguanil and any adverse effect on mother and fetus has never been established, but the attending physician should carefully weigh the expected benefits against the potential risks.
Use proguanil with caution in patients with severe renal impairment.
Renal impairment, Mouth ulcers with renal impairment, other medications. Reduced dose necessary in children. The drug passes into breast milk. Safety in pregnancy not established, although benefits generally considered to outweigh risks. Folate supplements indicated.
Fluvoxamine: Fluvoxamine can virtually abolish the metabolism of proguanil to its active metabolite cycloguanil via an inhibitory effect on the cytochrome P450 lsoenzyme CYP2C19.
Warfarin: For a report of haematuria and high prothrombin ratio in a patient stabilized on warfarin who took proguanil for malaria prophylaxis.
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Lifeline Pharmaceuticals Ltd.
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