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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › AGENTS AGAINST AMOEBIASIS AND OTHER PROTOZOAL DISEASES › Other agents against amoebiasis and other protozoal diseases
trimetrexate
P01AX07
Forms & Strengths
- Powder for injection: 25 mg vial
Adult Dosing
- Pneumocystis jirovecii pneumonia in AIDS: 45 mg/m2 IV once daily for 21 days
- Must be co-administered with leucovorin calcium rescue: 20 mg/m2 IV or orally every 6 hours for 24 days
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Alternative treatment of moderate-to-severe Pneumocystis jirovecii pneumonia in immunocompromised patients (e.g., AIDS) who are intolerant of or refractory to trimethoprim-sulfamethoxazole
Mechanism of Action
- Potent inhibitor of dihydrofolate reductase (DHFR)
- Blocks the reduction of dihydrofolate to tetrahydrofolate, resulting in the inhibition of purine and pyrimidine synthesis and subsequent cell death
Contraindications
- Hypersensitivity to trimetrexate or methotrexate
- Clinically significant active infection other than Pneumocystis jirovecii
- Severe myelosuppression
- Pregnancy and lactation
Adverse Reactions
- Severe myelosuppression (neutropenia, thrombocytopenia, anemia)
- Elevated transaminases and liver function tests
- Mucositis, stomatitis, nausea, vomiting, diarrhea
- Rash, fever, fatigue
Drug Interactions
- Inhibitors of CYP3A4 and CYP2C8 may increase trimetrexate plasma concentrations
- Myelosuppressive agents increase the risk of severe bone marrow toxicity
- Hepatotoxic drugs may increase the risk of liver injury
Curated Content: Needs Vetting Before Put to Clinical Use