📋 Indications & Clinical Dosage
*Treatment of susceptible infections of respiratory tract, gastro-intestinal, urinary tracts, skin & soft-tissues:*
ORAL: Adult & Children above 12 years: 960 mg twice daily.
Children 6 weeks-5 months: 120 mg twice daily, alternatively 24 mg/kg twice daily; 6 months-5 yrs: 240 mg twice daily, alternatively 24 mg/kg twice daily; 6-11 yrs: 480 mg twice daily, alternatively24 mg/kg twice daily.
BY IV INF: Adult: 960 mg every 12 hours, increased to 1.44 g every12 hours, increased dose used in severe infection.
*Treatment of Pneumocystis jirovecii (Pneumocystis carinii) infections:*
ORAL OR BY IV INF: Adult: 120 mg/kg daily in 2-4 divided doses for14-21 days. Prophylaxis: 960 mg once daily (oral), reduced if not tolerated to 480 mg once daily, alternatively 960 mg once daily on alternate days, 3 times weekly.
Children: 120 mg/kg daily in 2-4 divided doses for 14-21 days, oral route preferred for children. Prophylaxis: 450 mg/m2 twice daily (max. per dose 960 mg twice daily) for 3 days of the week (either consecutively or on alternate days).
💊 Mode of Administration
Infuse over 60-90 min, must dilute well before giving. May be given less diluted in a central line. Not for IM injection. Maintain adequate fluid intake to prevent crystalluria. Administer around-the-clock every 6-12 hours.
⛔ Contraindications
Neonates, severe renal or hepatic insufficiency, blood dyscrasias.
⚠️ Precautions & Warnings
Avoid in blood disorders, avoid in infants under 6 weeks (except for treatment or prophylaxis of pneumocystis pneumonia) because of the risk of kernicterus, elderly, G6PD deficiency (risk of haemolytic anaemia), maintain adequate fluid intake, predisposition to folate deficiency, predisposition to hyperkalaemia (in adults), hepatic and renal impairment (reduce or space out dosage), severe allergy or asthma, perform regular haematological tests during long term therapy. Discontinue if rash develops.
🔄 Drug Interactions
Folate inhibitors, anticoagulants, anticonvulsants, hypoglycaemics, cyclosporin, procainamide, aman-tadine, lamivudine, thiazides, pyrimethamine, digoxin.
⚠️ Adverse Reactions / Side Effects
Abdominal discomfort, diarrhoea, headache, Hyperkalaemia, nausea, rash, vomiting, glossitis, blood dyscrasias, folate deficiency, liver changes. Rarely: erythema multiforme, Lyell syndrome, exfoliative dermatitis, Stevens-Johnson syndrome, convulsions, peripheral neuritis, ataxia, granulocytosis and bone marrow depression
🤰 Pregnancy & Lactation Safety
Pregnancy Risk:
Contraindicated in pregnancy.
Lactation / Breastfeeding:
Contraindicated or not recommended.
🧪 Compatibility & Storage Stability
Compatibility: Stable in 05 1/2NS, LR, 0.45% NS. At Y-site administration, incompatible with fluconazole, midazolam, vinorelbine. When admixed, incompatible with fluconazole, verapamil
Stability & Storage: Do not refrigerate injection, less soluble in more alkaline pH. Protect from light.