NIMOTOP
Clinical safety rating
cautionComprehensive clinical and safety monograph for NIMOTOP (NIMOTOP).
Nimodipine is a dihydropyridine calcium channel blocker that selectively inhibits calcium influx into vascular smooth muscle cells, leading to vasodilation. It has a preferential effect on cerebral arteries, reducing the incidence of vasospasm following subarachnoid hemorrhage.
| Metabolism | Nimodipine is extensively metabolized in the liver primarily by the CYP3A4 isoenzyme, with no significant first-pass effect. Metabolites are excreted mainly in bile (about 80%) and urine (about 20%). |
| Excretion | Primarily hepatic metabolism; 50% excreted in urine as metabolites, 30% in feces via biliary elimination. Less than 1% excreted unchanged in urine. |
| Half-life | Terminal elimination half-life is approximately 8–9 hours (range 3–12 hours) in adults, with clinical context of twice-daily dosing for continuous cerebral vasodilation in subarachnoid hemorrhage. |
| Protein binding | 97–99% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 0.9–1.6 L/kg (average 1.2 L/kg), indicating extensive tissue distribution and high lipophilicity. |
| Bioavailability | Oral: 13% (range 3–30%) due to extensive first-pass metabolism. Intravenous: 100%. |
| Onset of Action | Oral: 1–3 hours. Intravenous: within minutes, with peak effect at 1 hour after infusion initiation. |
| Duration of Action | Oral: 12–24 hours with twice-daily dosing. Intravenous: 4–8 hours post-infusion; clinical effect may persist longer due to cerebrovascular selectivity. |
| Molecular Weight | 418.44 |
60 mg orally every 4 hours for 21 days, initiated within 96 hours of subarachnoid hemorrhage. If unable to swallow, 0.5 mg/h continuous IV infusion via central line; increase to 1 mg/h after 2 hours if tolerated, continue for up to 21 days.
| Dosage form | CAPSULE |
| Renal impairment | No dose adjustment required for renal impairment. Use caution in severe renal failure due to risk of accumulation of metabolites. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh C). In mild to moderate (Child-Pugh A or B), reduce oral dose to 30 mg every 4 hours or decrease IV infusion rate to 0.5 mg/h; monitor blood pressure closely. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no recommended dosing. |
| Geriatric use | No specific dose adjustment required, but elderly patients may be more sensitive to hypotensive effects; monitor blood pressure closely and consider starting at lower end of dosing range. |
| 1st trimester | No adequate studies in pregnant women; animal studies show fetal toxicity. Use only if benefit outweighs risk. |
| 2nd trimester | May cause maternal hypotension and reduced uteroplacental perfusion. Use with caution. |
| 3rd trimester | May cause uterine relaxation and delay labor. Use only if clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for NIMOTOP (NIMOTOP).
| Placental transfer | Nimodipine crosses the placenta; documented in animal studies and human case reports. |
| Breastfeeding | Nimodipine is excreted into breast milk in small amounts. Because of potential for serious adverse reactions in nursing infants, decide whether to discontinue nursing or discontinue drug, taking into account importance of drug to mother. |
| Lactation Rating | L3 |
| Teratogenic Risk | Teratogenicity not established in humans; animal studies show no fetal harm. Use only if maternal benefit outweighs risk. First trimester: avoid unless essential. Second/third trimesters: potential for maternal hypotension and reduced uteroplacental perfusion. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and neurologic status. Fetal heart rate monitoring and ultrasound for growth and placental perfusion. |
| Fertility Effects | No evidence of impaired fertility in animal studies. Human data lacking. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to nimodipine or any componentConcurrent use with rifampinConcurrent use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin)
| Precautions | Hypotension: May cause systemic hypotension, especially in patients with compromised cardiovascular function, Hepatic impairment: Reduce dose in patients with liver cirrhosis due to increased bioavailability, Intestinal pseudo-obstruction: Rare cases reported; monitor for decreased bowel sounds or abdominal distension |
| Food/Dietary | Avoid grapefruit juice and grapefruit products as they inhibit CYP3A4 and increase nimodipine levels. Avoid high-fat meals as they may decrease absorption. |
| Clinical Pearls | Administer via central line to avoid phlebitis; titrate slowly to avoid hypotension; monitor for bradycardia and heart block; use nifedipine (dihydropyridine) with caution in patients with hepatic impairment due to CYP3A4 metabolism. |
| Patient Advice | Take exactly as prescribed, do not skip doses. · Avoid grapefruit juice and grapefruit products during treatment. · Report any unusual bleeding, bruising, or signs of infection immediately. · Do not drive or operate heavy machinery if you feel dizzy or lightheaded. · Store capsules at room temperature away from moisture and heat. |
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