nimodipine (Nimotop, Nymalize)

Dosing and uses of Nimodipine (Nimotop, Nymalize)

• Adult
• Pediatric

 

Adult dosage forms and strengths

gel capsule

• 30mg

oral solution (Nymalize)

• 60mg/20mL

 

Subarachnoid Hemorrhage

Indicated for the improvement of neurological outcome by reducing the incidence and severity of ischemic deficits with subarachnoid hemorrhage from ruptured intracranial berry aneurysms regardless of their postictus neurological condition (ie, Hunt and Hess Grades I-V)

60 mg PO q4hr for 21 days; begin therapy within 96 hours of subarachnoid hemorrhage

 

Dosage modifications

Renal impairment: Supplemental dose not necessary in hemodialysis or peritoneal dialysis

Hepatic impairment: Decrease dose to 30 mg PO q4hr; closely monitor BP and Hr

 

Subarachnoid Hemorrhage (Orphan)

New dosage form

Orphan designation for intraventricular injection for treatment of subarachnoid hemorrhage

Sponsor

• Edge Therapeutics, Inc; 211 Warren Street, Newark, NJ 07103

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Nimodipine (Nimotop, Nymalize) adverse (side) effects

1-10%

Reduction in systemic blood pressure (1-8%)

Diarrhea (2-4%)

Headache (1-4%)

Abdominal discomfort (2%)

Rash (1-2%)

 

<1%

Heart failure

Arrhythmia

Anemia

ECG abnormalities

GI hemorrhage

Hepatitis

Jaundice

Thrombocytopenia

Vomiting

Thrombosis

Rebound vasospasm

 

Warnings

Black box warnings

Do not administer contents of gel capsule or oral solution IV or by other parenteral routes

Deaths and serious life-threatening adverse events (ie, significant hypotension requiring pressor support) have occurred when injected parenterally

 

Contraindications

Hypersensitivity

Parenteral administration; risk of death (see Black box warnings)

 

Cautions

Congestive heart failure

Reflex tachycardia resulting in angina and/or MI in patients with obstructive coronary disease reported

Metabolism decreased in patients with hepatic impairment

Use caution in hepatic impairment or hypertrophic subaortic stenosis

Peripheral edema may occur within 2-3 weeks of initiating therapy

Hypotension with or without syncope is possible (particularly with severe aortic stenosis)

Intestinal pseudo-obstruction and ileus have been reported rarely

A decreased dose may be required with strong CYP3A4 inhibitors

 

Pregnancy and lactation

Pregnancy category: C

Lactation: unknown; avoid

 

Pregnancy categories

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.

 

Pharmacology of Nimodipine (Nimotop, Nymalize)

Mechanism of action

Ca channel blocker with minimal effects on conduction in heart; primary effect is upon cerebral arteries to prevent vasospasm

Highly lipophilic, allowing it to cross the blood-brain barrier

 

Absorption

Bioavailability: 13%

Peak Plasma Time: 1 hr

Peak Plasma Concentration: 80 ng/mL

 

Distribution

Protein Bound: 95%

Vd: 0.43 L/kg

 

Metabolism

Hepatic P450 enzyme CYP3A4

 

Elimination

Half-Life: 1-2 hr

Total Body Clearance: 0.84 L/kg (healthy); 1.18 L/kg (SAH)

Excretion: Urine (50%); feces (32%)

 

Administration

Instructions

Gel capsule: Swallow capsule whole; if unable to swallow, may withdraw liquid content out with syringe and administer PO

Oral solution: Administer only enterally (eg, oral, nasogastric tube, or gastric tube route); for each dose, refill the syringe with 20 mL of 0.9% NaCl and then flush any remaining contents from NG or gastric tube into the stomach

Do not administer gel capsule contents or oral solution IV or any other parenteral route (see Black box warnings)

Take at least 1 hr before or 2 hr after meals

Avoid grapefruit juice