Dosing & Uses
Dosage Forms & Strengths
50-75 mg qD PO for 1-3 weeks, THEN
25-37.5 mg qD PO for 4-5 weeks
P jiroveci Pneumonia (Off-label)
Prophylaxis p P jiroveci pneumonia (formerly Pneumocystis pneumonia); administer with dapsone
50-75 mg PO once/week
Tay-Sachs & Sandhoff Disease (Orphan)
Treatment of GM-2 gangliosidoses (Tay-Sachs disease and Sandhoff disease)
Orphan indication sponsor
- ExSAR Corporation; 11 Deer Park Drive; Monmouth Junction, NJ 08852
Other Indications & Uses
Treatment & prevention of toxoplasmosis (with sulfadiazine, clindamycin, or atovaquone); malaria
Off-label: prophylaxis of P. jiroveci pneumonia (with dapsone), isosporiasis
Dosage Forms & Strengths
>2 Months Old
- Loading dose: 2 mg/kg/d divided q12hr PO for 3 days
- Maintenance: 1 mg/kg PO qD for 4 weeks
< 2 months old: Safety and efficacy not established
Serious - Use Alternative
Significant - Monitor Closely
Frequency Not Defined
Abnormal skin pigmentation
Arrhythmias (large doses)
Megaloblastic or folate-deficiency anemia
Severe renal dz
Hepatic/renal dz, anemia, myelosuppression, epilepsy
No longer recommended for malaria prevention or acute Tx if used alone
Use w/ leucovorin, esp. at high doses
Pregnancy & Lactation
Pregnancy Category: C
Lactation: enters breast milk, do not nurse
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Onset: ~1 hr
Absorption: well absorbed
Distribution: widely, mainly in blood cells, kidneys, lungs, liver, & spleen; crosses into CSF; crosses placenta; enters breast milk
Protein Bound: 80-87%
Half-life elimination: 80-95 hr
Peak Plasma Time: 1.5-8 hr
Excretion: urine (20-30% as unchanged drug)
Mechanism of Action
Folic acid antagonist
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.
|1||This drug is available at the lowest co-pay. Most commonly, these are generic drugs.|
|2||This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.|
|3||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.|
|4||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|5||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|6||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|NC||NOT COVERED – Drugs that are not covered by the plan.|
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
Select a box to add or remove a plan.
Select a class to view formulary status for similar drugs