INPEFA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for INPEFA (INPEFA).
INPEFA (cinitapride) is a gastrointestinal prokinetic agent that acts as a selective 5-HT4 receptor agonist and 5-HT2 receptor antagonist. It enhances acetylcholine release from enteric cholinergic neurons, stimulating gastric motility and accelerating gastric emptying.
| Metabolism | Primarily metabolized by CYP3A4 and CYP2D6 enzymes in the liver to inactive metabolites. |
| Excretion | Primarily renal excretion (~70% as unchanged drug) and biliary/fecal excretion (~30%). |
| Half-life | Terminal elimination half-life is approximately 1.5 hours in healthy adults; clinically, dosing is every 6-8 hours. |
| Protein binding | 85-90% bound to albumin and alpha-1 acid glycoprotein. |
| Volume of Distribution | 0.3-0.5 L/kg; reflects distribution primarily into extracellular fluid. |
| Bioavailability | Oral: 80-90%; bioavailability reduced by food. |
| Onset of Action | Oral: 30-60 minutes; intravenous: within minutes. |
| Duration of Action | Oral: 4-6 hours; intravenous: 2-4 hours; clinical effect may be extended in renal impairment. |
20 mg orally once daily, taken with a meal and at the same time each day.
| Dosage form | TABLET |
| Renal impairment | eGFR 30-59 mL/min/1.73m2: 10 mg once daily; eGFR 15-29 mL/min/1.73m2: 5 mg once daily; eGFR <15 mL/min/1.73m2: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 10 mg once daily; Child-Pugh C: not recommended. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no recommended dosing. |
| Geriatric use | No specific geriatric dose; start at lower end of dosing range (10 mg once daily) and titrate based on renal function and tolerability. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for INPEFA (INPEFA).
| Breastfeeding | No data on presence in human milk; M/P ratio unknown. Risk of infant renal toxicity due to SGLT2 inhibition. Contraindicated during breastfeeding. |
| Teratogenic Risk | INPEFA (sodium–glucose cotransporter 2 inhibitor) is contraindicated in the second and third trimesters due to risk of fetal renal toxicity and oligohydramnios. First trimester exposure data are limited; animal studies show renal abnormalities. Avoid use throughout pregnancy. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to cinitapride or any excipients. Patients with severe hepatic impairment. Patients with known QT prolongation or taking other QT-prolonging drugs. Mechanical gastrointestinal obstruction.
| Precautions | Risk of QT prolongation; use cautiously in patients with cardiac disease or electrolyte disturbances. May cause extrapyramidal symptoms. Not recommended in patients with a history of seizure disorders. |
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| Monitor fetal growth and amniotic fluid volume via ultrasound if inadvertent exposure. Assess maternal renal function, electrolytes, and volume status. SGLT2 inhibitors may cause hypotension and ketoacidosis. |
| Fertility Effects | No known direct effect on fertility; however, SGLT2 inhibitors can cause weight loss and hormonal changes that may indirectly affect ovulatory function. No human data on fertility impairment. |