nimodipine (Nimotop, Numalize)
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Introduction
Tradename: Nimotop.
Indications
- improvement of neurological deficits due to vasospasm following subarachnoid hemorrhage
- acute ischemic stroke (may be of some benefit)
- prophylactic management of migraine headache
Precautions:
- use with caution in patients with impaired liver function
- may increase frequency & severity of angina during initiation of therapy
- use with caution in patients with CHF or aortic stenosis especially if concurrent use of beta blocker
Dosage
- 60 mg PO every 4 hours for 3 weeks
- start therapy
- as soon as possible[4]
- 96 hours after subarachnoid hemorrhage
- NOT FOR INTRAVENOUS OR PARENTERAL ADMINISTRATION[5] MAY RESULT IN DEATH
- Nymalize oral solution for subarachnoid hemorrhage[6]
Capsules: 30 mg.
Pharmacokinetics
- oral bioavailability is low & variable
- metabolized in the liver by cyt P450 3A4
- extensive 1st pass metabolism
- elimination 1/2life is 2-9 hours
- eliminated in the urine
elimination via liver
1/2life = 2-9 hours
Adverse effects
- most common (1-10%)
- reductions in systemic blood pressure
- uncommon (< 1%)
- hepatitis, hemorrhage, edema, diarrhea, rash, headache, nausea, dyspnea, EKG abnormalities, tachycardia, bradycardia, muscle cramps, acne, depression
- other[4]
- drug adverse effects of calcium channel blockers
- drug adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of antihypertensive agents
Drug interactions
- hypotensive agents in combination increase hypotensive effects
- cimetidine increases plasma levels of nimodipine
- any drug that inhibits cyt P450 3A4 may increase levels of nimodipine
- any drug that induces cyt P450 3A4 may diminish levels of nimodipine
- drug interaction(s) of calcium channel blockers with ARBs
- drug interaction(s) of calcium channel blockers with ACE inhibitors
- drug interaction(s) of calcium channel blockers with diuretics
- drug interaction(s) of calcium channel blockers with erythromycin
- drug interaction(s) of calcium channel blockers with clarithromycin
- drug interaction(s) of renin-angiotensin-aldosterone inhibitors with trimethoprim-sulfamethoxazole
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium channel blockers
- drug interaction(s) of NSAIDs & antihypertensives
Mechanism of action
- L-type Ca+2 channel blocker
- preferentially effects central nervous system at usual doses
More general terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996.
- ↑ The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill pg 774
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 4.0 4.1 4.2 Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 - not on National VA formulary
- ↑ 5.0 5.1 FDA MedWatch http://www.fda.gov/medwatch/safety/2006/safety06.htm#Nimotop
FDA MedWatch, 08/02/10 http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm220840.htm - ↑ 6.0 6.1 FDA News Release. May 14, 2013 FDA approves Nymalize - first nimodipine oral solution for use in certain brain hemorrhage patients. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm352280.htm