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nimodipine (Nimotop, Numalize)
Tradename: Nimotop.
Indications:
1) improvement of neurological deficits due to vasospasm following subarachnoid hemorrhage
2) acute ischemic stroke (may be of some benefit)
3) prophylactic management of migraine headache
Precautions:
1) use with caution in patients with impaired liver function
2) may increase frequency & severity of angina during initiation of therapy
3) use with caution in patients with CHF or aortic stenosis especially if concurrent use of beta blocker
Dosage:
1) 60 mg PO every 4 hours for 3 weeks
2) start therapy
a) as soon as possible [4]
b) 96 hours after subarachnoid hemorrhage
3) NOT FOR INTRAVENOUS OR PARENTERAL ADMINISTRATION [5] MAY RESULT IN DEATH
4) Nymalize oral solution for subarachnoid hemorrhage [6]
Capsules: 30 mg.
Pharmacokinetics:
1) oral bioavailability is low & variable
2) metabolized in the liver by cyt P450 3A4
-> extensive 1st pass metabolism
3) elimination 1/2life is 2-9 hours
4) eliminated in the urine
Adverse effects:
1) most common (1-10%)
- reductions in systemic blood pressure
2) uncommon (< 1%)
- hepatitis, hemorrhage, edema, diarrhea, rash, headache, nausea, dyspnea, EKG abnormalities, tachycardia, bradycardia, muscle cramps, acne, depression
3) other [4]
- heartburn, flushing
Drug interactions:
1) hypotensive agents in combination increase hypotensive effects
2) cimetidine increases plasma levels of nimodipine
3) any drug that inhibits cyt P450 3A4 may increase levels of nimodipine
4) any drug that induces cyt P450 3A4 may diminish levels of nimodipine
Mechanism of action:
1) L-type Ca+2 channel blocker
2) preferentially effects central nervous system at usual doses
Interactions
drug interactions
drug adverse effects (more general classes)
Related
cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
General
calcium channel blocker (CCB)
dihydropyridine
neurologic agent
Properties
MISC-INFO: elimination route LIVER
1/2life 2-9 HOURS
pregnancy-category C
safety in lactation -
Database Correlations
PUBCHEM correlations
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
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998 - not on National VA formulary
- 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
- 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