Nimodipine

Pronunciation: nye-MOE-di-peen
Class: Calcium channel blocking agent

Trade Names

Nimodipine
- Capsules, liquid 30 mg

Pharmacology

Inhibits movement of calcium ions across cell membrane in systemic and coronary vascular smooth muscle and myocardium. Has greater effect on cerebral arteries than on other arteries.

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Pharmacokinetics

Absorption

Nimodipine is rapidly absorbed after oral administration. Bioavailability is 13% and T _max is approximately 1 h. Food decreases peak plasma concentration 68% and bioavailability 38%.

Distribution

Nimodipine protein binding is over 95%.

Metabolism

Extensive first-pass metabolism in the liver.

Elimination

Nimodipine is eliminated in urine (less than 1% unchanged), and metabolites are considerably less active than parent compound. Terminal t _{1/ 2} is 8 to 9 h, and initial t _{1/ 2} is 1 to 2 h.

Special Populations

AUC and C _max were approximately 2–fold higher; this response is not considered important.

Nimodipine bioavailability is increased, C _max almost doubles, and dosage adjustment is necessary in patients with hepatic cirrhosis.

Indications and Usage

Improvement of neurologic deficits caused by vasospasm after subarachnoid hemorrhage from ruptured intracranial berry aneurysms.

Contraindications

Standard considerations.

Dosage and Administration

PO/Nasogastric Reduce dosage to 30 mg every 4 h.

PO/Nasogastric 60 mg every 4 h for 21 consecutive days. Initiate therapy within 96 h of subarachnoid hemorrhage.

General Advice

• If capsule cannot be swallowed, make hole in both ends of capsule with 18-gauge needle and extract contents into syringe. Empty contents into patient's nasogastric tube and wash down tube with 30 mL of isotonic sodium chloride solution.
• Take 1 h before or 2 h after meals.

Storage/Stability

Store at room temperature (59° to 86°F) in original foil packaging.

Drug Interactions

May cause increased adverse reactions because of myocardial contractility or AV conduction depression.

Nimodipine plasma levels may be elevated, increasing the pharmacologic effects and adverse reactions.

May cause severe hypotension or increased fluid requirements.

May have additive effects.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension (4%); bradycardia, ECG abnormalities, tachycardia (1%); CHF, heart failure, hypertension, palpitations, rebound vasospasm (less than 1%).

CNS

Headache (4%); depression (1%); dizziness, light-headedness (less than 1%).

Dermatologic

Rash (2%); acne (1%); diaphoresis, itching (less than 1%).

GI

Diarrhea (4%); GI symptoms (2%); nausea (1%); GI hemorrhage; vomiting (less than 1%).

Hematologic-Lymphatic

Anemia, decreased platelet count, deep vein thrombosis, DIC, hematoma, thrombocytopenia (less than 1%).

Hepatic

Abnormal LFTs (1%); hepatitis, jaundice (less than 1%).

Metabolic-Nutritional

Hyponatremia (less than 1%).

Musculoskeletal

Muscle cramps/pain (1%).

Respiratory

Dyspnea (1%); wheezing (less than 1%).

Miscellaneous

Flushing (2%); edema (1%); phenytoin toxicity (less than 1%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Use with caution, reflecting greater frequency of decreased hepatic, renal, or cardiac function, and concomitant disease or other drug therapy.

Hepatic Function

Use drug with caution in patients with hepatic function impairment or reduced hepatic blood flow.

Antiplatelet effects

Calcium channel blockers may inhibit platelet function.

Overdosage

Symptoms

Symptoms of overdosage have not been reported. Symptoms would be expected to be related to CV effects such as excessive peripheral vasodilation with marked systemic hypotension.

Patient Information

• Explain that medication needs to be taken around the clock for 21 days.
• Instruct patient to report the following symptoms to health care provider: abdominal cramping, diarrhea, dizziness, faint feeling, nausea, palpitations, shortness of breath, swelling of hands or feet, unusual bruising or bleeding.

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