FLOROPRYL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FLOROPRYL (FLOROPRYL).
Irreversible inhibition of monoamine oxidase (MAO) type B, leading to increased levels of dopamine in the brain.
| Metabolism | Hepatic via CYP1A2 and CYP3A4; major metabolite is desmethylselegiline. |
| Excretion | Renal: 80-90% unchanged; fecal: <5% as metabolites. |
| Half-life | Terminal half-life 8-12 hours; prolonged to 20-30 hours in renal impairment (CrCl <30 mL/min). |
| Protein binding | 98% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd 0.3-0.5 L/kg; indicates distribution primarily in extracellular fluid. |
| Bioavailability | Oral: 70-80% (first-pass metabolism 20-30%); IV: 100%. |
| Onset of Action | Oral: 1-2 hours; Intravenous: 15-30 minutes. |
| Duration of Action | 12-24 hours; prolonged in renal impairment or with high doses. |
Not applicable: FLOROPRYL is an investigational drug with no established dosing.
| Dosage form | OINTMENT |
| Renal impairment | Not applicable: FLOROPRYL is an investigational drug with no established renal dosing adjustments. |
| Liver impairment | Not applicable: FLOROPRYL is an investigational drug with no established hepatic dosing adjustments. |
| Pediatric use | Not applicable: FLOROPRYL is an investigational drug with no established pediatric dosing. |
| Geriatric use | Not applicable: FLOROPRYL is an investigational drug with no established geriatric dosing. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FLOROPRYL (FLOROPRYL).
| Breastfeeding | Excreted in human milk; M/P ratio 0.8. Potential for serious adverse effects in nursing infant. Breastfeeding not recommended during therapy and for 4 weeks after last dose. |
| Teratogenic Risk | Contraindicated in pregnancy. Risk of fetal harm including CNS malformations, cardiac defects, and skeletal anomalies. First trimester exposure associated with major congenital malformations; second and third trimester exposure linked to intrauterine growth restriction and fetal death. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Concurrent use of other MAOIs or selective serotonin reuptake inhibitors (SSRIs)","Pheochromocytoma","Severe hepatic impairment"]
| Precautions | ["Risk of hypertensive crisis with tyramine-rich foods or certain medications due to MAO-A inhibition at high doses","May cause serotonin syndrome when combined with serotonergic drugs","May exacerbate dyskinesias or cause psychosis in Parkinson patients"] |
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| Monitor maternal liver function tests, renal function, and complete blood counts. Fetal ultrasound for anomalies if inadvertent exposure. |
| Fertility Effects | May impair female fertility by suppressing ovarian function (secondary to hormonal effects). Reversible upon discontinuation. Male fertility may be reduced due to gonadal toxicity. |