Proguanil is biguanide compound which has little antimalarial activity until metabolized in the body to the active antimalarial drug cycloguanil. Cycloguanil inhibits plasmodium dyhydrofolate reductase and thus disrupts synthesis of nucleic acids in the parasite. Cycloguanil is active against pre-erythrocytic forms and is a slow acting blood scizontocide.
| Pharmacokinetics: |
- Proguanil is ready absorbed from the gastro-intestinal tract
following oral doses, peak plasma concentrations occurring within
about 4 hours. Proguanil is metabolized in the liver to the active
metabolite cycloguanil. Peak plasma concentrations of cycloguanil
occur approximately one hour after those of the parent drug. The
elimination half-life for both Proguanil & cycloguanil are about
20 hours. About 40% to 60% of Proguanil is eliminated in the urine,
of which 60% is unchanged & 30% cycloguanil. There is also some
elimination via faeces. Proguanil is distributed into breast milk in
small amount.
|
| Uses |
- Proguanil is an effective antimalarial agent. It is used for the
prevention and treatment of uncomplicated malaria.
|
| Doses & Administration: |
- It is generally recommended that chemoprophylaxis for travelers
should be started about one or two weeks before exposure to malaria,
but if this is not possible, it can be started 1 to 2 days prior to
travel. Administration should continue throughout exposure and for
at least 4 weeks after leaving the malarious area.
|
| Prevention Of Malaria: |
- Adults: 200 mg [2 tablets daily]
- Children: Upto 1 Year: 25 mg [¼ tablet daily]
1 to 4 Years: 50 mg [½ tablet]
5 to 8 Years: 100 mg [1 tablet daily]
9 to 15 Years: 150 mg[1½ tablets daily]
Tablets to be taken with or after food. For children tablets may be
crushed and mixed with milk, honey or jam. |
| Contraindications & Warnings: |
- Proguanil should be used with caution in patients with renal
impairment; dosage should be reduced accordingly. Proguanil is
contraindicated in patients with known allergy or any of the
excipients used.
|
| Adversed Effects: |
- Apart from mild gastric intolerance, diarrhoea and some reports
of aphthous ulceration there appear to be few adverse effects associated with usual doses of Proguanil hydrochloride.
Haematological changes may occur in patients with severe renal
impairment.
|
| Interactions: |
- Fluvoxamine can virtually abolish the metabolism of Proguanil to
its active metabolite cycloguanil via an inhibitory effect on the
cytochrome P450 isoenzyme CYP2C19.
|
| Pharmaceutical Precautions: |
- Store in a dry & dark place below 25℃
- Protect from light and moisture.
|
| Presentation: |
- 100 Tablets packed in plastic container.
|
©
Yashica Pharmaceuticals Private Limited. All Rights Reserved (Terms
of Use)
