Nicardipine hydrochloride
Nicardipine hydrochloride (Cardene)
Nicardipine hydrochloride
(nye-
KAR-dih-peen)
Pregnancy Category: C
Cardene
Cardene IV
Cardene SR
(Rx)
Classification:
Calcium channel blocking agent (antianginal, antihypertensive)
See Also:
See also
Calcium Channel Blocking Agents
[.
]
Action/Kinetics:
Moderately increases CO and significantly decreases peripheral vascular resistance.
Onset of action: 20 min.
Maximum plasma levels: 30-120 min. Significant first-pass metabolism. Food (especially fats) will decrease the amount of drug absorbed from the GI tract. Steady-state plasma levels are reached after 2-3 days of therapy.
Therapeutic serum levels: 0.028-0.050 mcg/mL.
t
1/2, at steady state: 8.6 hr.
Maximum BP-lowering effects, immediate release: 1-2 hr;
maximum BP-lowering effects, sustained release: 2-6 hr.
Duration: 8 hr. Highly bound to plasma protein ( > 95%) and metabolized by the liver with excretion through both the urine and feces.
Uses:
Immediate release: Chronic stable angina (effort-associated angina) alone or in combination with beta-adrenergic blocking agents.
Immediate and sustained released: Hypertension alone or in combination with other antihypertensive drugs.
IV: Short-term treatment of hypertension when PO therapy is not desired or possible.
Investigational: CHF.
Contraindications:
Use in advanced aortic stenosis due to the effect on reducing afterload. During lactation.
Special Concerns:
Safety and efficacy in children less than 18 years of age have not been established. Use with caution in clients with CHF, especially in combination with a beta blocker due to the possibility of a negative inotropic effect. Use with caution in clients with impaired liver function, reduced hepatic blood flow, or impaired renal function. Initial increase in frequency, duration, or severity of angina.
Side Effects:
CV: Pedal edema, flushing, increased angina, palpitations, tachycardia, other edema, abnormal ECG, hypotension, postural hypotension, syncope,
MI, AV block ventricular extrasystoles, peripheral vascular disease.
CNS: Dizziness, headache, somnolence, malaise, nervousness, insomnia, abnormal dreams, vertigo, depression, confusion, amnesia, anxiety, weakness, psychoses, hallucinations, paranoia.
GI: N&V;, dyspepsia, dry mouth, constipation, sore throat.
Neuromuscular: Asthenia, myalgia, paresthesia, hyperkinesia, arthralgia.
Miscellaneous: Rash, dyspnea, SOB, nocturia, polyuria, allergic reactions, abnormal liver chemistries, hot flashes, impotence, rhinitis, sinusitis, nasal congestion, chest congestion, tinnitus, equilibrium disturbances, abnormal or blurred vision, infection, atypical chest pain.
Overdose Management:
Symptoms: Marked hypotension, bradycardia, palpitations, flushing, drowsiness, confusion, and slurred speech following PO overdose. Lethal overdose may cause systemic hypotension, bradycardia (following initial tachycardia), and progressive AV block.
Treatment:
- Treatment is supportive. Monitor cardiac and respiratory function.
- If client is seen soon after ingestion, emetics or gastric lavage should be considered, followed by cathartics.
-
Hypotension: IV calcium, dopamine, isoproterenol, metaraminol, or norepinephrine. Also, provide IV fluids. Place client in Trendelenburg position.
-
Ventricular tachycardia: IV procainamide or lidocaine; cardioversion may be necessary. Also, provide slow-drip IV fluids.
-
Bradycardia, asystole, AV block: IV atropine sulfate (0.6-1 mg), calcium gluconate (10% solution), isoproterenol, norepinephrine; also, cardiac pacing may be indicated. Provide slow-drip IV fluids.
Drug Interactions:
-
Cimetidine /
Bioavailability of nicardipine
plasma levels
-
Cyclosporine /
Plasma levels of cyclosporine possibly leading to renal toxicity
-
Ranitidine /
Bioavailability of nicardipine
How Supplied:
Capsule: 20 mg, 30 mg;
Capsule, Extended Release: 30 mg, 45 mg, 60 mg;
Injection: 2.5 mg/mL
Dosage
?Capsules, Immediate Release
Angina, hypertension.
Initial, usual: 20 mg t.i.d. (range: 20-40 mg t.i.d.). Wait 3 days before increasing dose to ensure steady-state plasma levels.
?Capsules, Sustained Release
Hypertension.
Initial: 30 mg b.i.d. (range: 30-60 mg b.i.d.).
NOTE: Initial dose in renal impairment: 20 mg t.i.d. Initial dose in hepatic impairment: 20 mg b.i.d.
?IV
Hypertension.
Individualize dose. Initial: 5 mg/hr; the infusion rate may be increased to a maximum of 15 mg/hr (by 2.5-mg/hr increments q 15 min). For a more rapid reduction in BP, initiate at 5 mg/hr but increase the rate q 5 min in 2.5-mg/hr increments until a maximum of 15 mg/hr is reached.
Maintenance: 3 mg/hr. The IV infusion rate to produce an average plasma level similar to a particular PO dose is as follows: 20 mg q 8 hr is equivalent to 0.5 mg/hr; 30 mg q 8 hr is equivalent to 1.2 mg/hr; and 40 mg q 8 hr is equivalent to 2.2 mg/hr. |