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nicardipine (Cardene, Cardene SR)
Tradename: Cardene.
Indications:
- hypertension
- Prinzmetal's angina
- Raynaud's phenomenon
Contraindications: patients with severe aortic stenosis
Precautions:
1) patients with impaired renal or hepatic function
2) patients with CHF
3) pheochromocytoma
4) may increase the frequency, severity & duration of angina during initiation of therapy
Dosage:
- start 20 mg PO TID, max 120 mg/day.
Tabs: 20, 30 mg.
- IV infusion 2-15 mg/hr.
Injection: 2.5 mg/mL (10 mL).
Sustained release: (Cardene SR)
- start 30 mg PO BID, max 120 mg/day.
Tabs: 30, 45, 60 mg
Pharmacokinetics:
-> metabolized in the liver by cyt P450 3A4
Adverse effects:
1) most common (1-10%)
- flushing, palpitations, tachycardia, pedal edema, headache, dizziness, nausea, somnolence, weakness
2) uncommon (< 1%)
- edema, tachycardia, syncope, abnormal EKG, insomnia, malaise, abnormal dreams, rash, vomiting, constipation, dyspepsia, xerostomia, nocturia, tremor
Drug interactions:
1) possible hypotensive effect when used concurrently with fentanyl
2) cimetidine increases levels of nicardipine
3) nicardipine increases levels of cyclosporine
4) increased negative inotropic effect of beta-blockers
5) any drug that inhibits cyt P450 3A4 may increase levels of nicardipine
6) any drug that induces cyt P450 3A4 may diminish levels of nicardipine
Laboratory:
- nicardipine in serum/plasma
Mechanism of action:
- nicardipine is a 2nd generation Ca+2-channel antagonist
- nicardipine is an L-type Ca+2 channel blocker
- it elicits favorable responses in both myocardial oxygen balance & renal function parameters
- nicardipine decreases renal glomerular pressure by efferent arteriolar dilatation, thus diminishing proteinuria [2]
- thus nicardipine is considered a good alternative agent for the management of myocardial ischemia/infarction & acute renal failure
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
Properties
MISC-INFO: elimination route LIVER
onset-of-action 5-20 MIN {IV}
1/2life 1.0 HOURS
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 8th ed.
Gilman et al, eds. Permagon Press/McGraw Hill pg 774
- Medical Knowledge Self Assessment Program (MKSAP) 11, American
College of Physicians, Philadelphia 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998 (Cardene IV)
- Prescriber's Letter 13(3): 2006
Cytochrome P450 drug interactions
Detail-Document#: 220233
(subscription needed) http://www.prescribersletter.com
- Deprecated Reference