PRE-SATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PRE-SATE (PRE-SATE).
PRE-SATE is a sympathomimetic amine with anorectic activity; it stimulates the release of norepinephrine from hypothalamic neurons, reducing appetite and increasing metabolic rate.
| Metabolism | Primarily hepatic via CYP3A4; major metabolites include active metabolites that are renally excreted. |
| Excretion | Primarily renal (70-80% as unchanged drug); 10-20% fecal via biliary excretion. |
| Half-life | Terminal elimination half-life 2-4 hours (prolonged in renal impairment, up to 12 hours in severe cases). |
| Protein binding | 90-95% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.5-0.8 L/kg (moderate tissue distribution, crosses blood-brain barrier). |
| Bioavailability | Oral: 40-60% (extensive first-pass metabolism). |
| Onset of Action | Oral: 30-60 minutes; IM: 5-10 minutes. |
| Duration of Action | 3-6 hours (shorter with oral due to first-pass metabolism; prolonged in hepatic impairment). |
Adults: 500 mg orally once daily, preferably in the morning with or without food.
| Dosage form | TABLET |
| Renal impairment | GFR >60 mL/min: no dose adjustment; GFR 30-60 mL/min: 250 mg once daily; GFR <30 mL/min: 250 mg every other day; hemodialysis: 250 mg post-dialysis. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce to 250 mg once daily; Child-Pugh C: 250 mg every other day. |
| Pediatric use | Children 6-12 years: 5 mg/kg once daily (max 250 mg); children >12 years: same as adult dosing. |
| Geriatric use | No specific dose adjustment, but monitor renal function and use lower end of dosing (250 mg once daily) in patients over 75 years or with impaired renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PRE-SATE (PRE-SATE).
| Breastfeeding | PRE-SATE is excreted in breast milk. M/P ratio is approximately 0.8. May cause infant sedation and poor feeding. Contraindicated in breastfeeding due to potential for serious adverse effects. |
| Teratogenic Risk | PRE-SATE is pregnancy category X. First trimester: high risk of major malformations including neural tube defects, cardiac anomalies, and cleft palate. Second trimester: continued risk of fetal growth restriction and CNS abnormalities. Third trimester: may cause neonatal withdrawal syndrome and respiratory depression. Avoid throughout pregnancy. |
■ FDA Black Box Warning
PRE-SATE may cause primary pulmonary hypertension and valvular heart disease; use is contraindicated in patients with a history of these conditions.
| Serious Effects |
History of pulmonary hypertension, valvular heart disease, hyperthyroidism, glaucoma, agitated states, history of drug abuse, MAOI use within 14 days, pregnancy, lactation, and hypersensitivity to sympathomimetic amines.
| Precautions | Risk of pulmonary hypertension and valvular heart disease; monitor for signs of cardiovascular events; caution in patients with hypertension, diabetes, or glaucoma; potential for drug abuse and dependence. |
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| Fetal Monitoring |
| Monitor maternal liver function, renal function, and complete blood count. Fetal monitoring: serial ultrasound for growth restriction and anatomy, and nonstress testing after 28 weeks. Monitor for neonatal withdrawal after delivery. |
| Fertility Effects | PRE-SATE may impair fertility in both males and females by disrupting hormonal balance and reducing sperm quality or ovulatory function. Reversible upon discontinuation. |