Cardionid

Nicardipine hydrochloride.

Each mL contains Nicardipine Hydrochloride 1 mg.

Pharmacology: Pharmacokinetics: Nicardipine is rapidly and completely absorbed from the gastrointestinal tract but is subject to saturable first pass hepatic metabolism. Bioavailability of about 35% has been reported after a 30-mg dose at steady state. The pharmacokinetics of nicardipine are non-linear due to the saturable first-pass hepatic metabolism and an increase in dose may produce a disproportionate increase in plasma concentration. There is also considerable interindividual variation in plasma-nicardipine concentrations. Nicardipine is more than 95% bound to plasma proteins. Nicardipine is extensively metabolized in the liver and is excreted in the urine and faeces, mainly as inactive metabolites. The terminal plasma half-life is about 8.6 hours, thus steady-state plasma concentrations are achieved after 2 to 3 days of dosing three times daily.

Nicardipine hydrochloride is indicated for the short-term treatment of hypertension when oral therapy is not feasible or not desirable.

Nicardipine hydrochloride is generally given orally although the intravenous route has been used for the short-term treatment of hypertension. An initial infusion rate of 5 mg/hour is recommended, increased, as necessary, up to a maximum of 15 mg/hour and subsequently reduced to 3 mg/hour.
Reduced doses of nicardipine hydrochloride and longer dosing intervals may be necessary in patients with hepatic or renal impairment. The US manufacturers recommend an initial dose of 20 mg twice daily by mouth in patients with hepatic impairment.
Drug Discontinuation and Transition to an Oral Antihypertensive Agent: Discontinuation of infusion is followed by a 50% offset of action in about 30 minutes.
If treatment includes transfer to an oral antihypertensive agent other than oral nicardipine, initiate therapy upon discontinuation of Cardena I.V. Premixed Injection.
If oral nicardipine is to be used, administer the first dose 1 hour prior to discontinuation of the infusion.

Contraindicated in patients with advanced aortic stenosis because part of the effect of nicardipine hydrochloride IV is secondary to reduced afterload. Reduction of diastolic pressure in these patients may worsen rather than improve myocardial oxygen balance. It is also contraindicated in patients with hypersensitivity, compensatory hypertension (i.e. in case of an arteriovenous shunt or aortic coarctation), unstable angina, within 8 days after myocardial infarction.

Nicardipine should be used with caution in patients with acute cerebral infarction or hemorrhage and systemic hypotension should be avoided in these patients. In addition, frequency, duration, and severity of angina occasionally may increase during initiation of nicardipine therapy or upward adjustment of dosage.
Nicardipine should be used with caution and dosage titrated carefully in patients with congestive heart failure, especially in those receiving concomitant β-adrenergic blocking agents, since nicardipine has a negative inotropic effect in vitro in some patients and may precipitate or worsen heat failure. Peripheral edema occurring during the course of nicardipine therapy should be investigated, especially in patients with congestive heart failure, since it may indicate deterioration in left ventricular function induced by the drug.
Nicardipine is not a β-adrenergic blocking agent and offers no protection against abrupt withdrawal of β-adrenergic blocking agents. If nicardipine is initiated in patients currently receiving a β-adrenergic blocking agent with the intent to withdraw β-adrenergic blocking agent, this should be done by a gradual reduction in dosage, preferably 8-10 day.
Since nicardipine is extensively metabolized in the liver, the drug should be used with caution and in reduced dosage in patients with hepatic impairment or reduced hepatic blood flow. Bioavailability and the elimination half-life of nicardipine are increased in patients with severe hepatic impairment, in addition, IV nicardipine should be used with caution in patients with portal hypertension since the drug reportedly increases the hepatic venous pressure gradient by 4 mmHg in patients with cirrhosis at high doses (5 mg administered over 20 minutes).
Use in Pregnancy & Lactation: There are no adequate and controlled studies to date using nicardipine in pregnant women. Nicardipine should be used during pregnancy only when the potential benefits justify the possible risks to the fetus.

There are no adequate and controlled studies to date using nicardipine in pregnant women. Nicardipine should be used during pregnancy only when the potential benefits justify the possible risks to the fetus.

The most common adverse effects are associated with its vasodilator action and often diminish on continued therapy. They include dizziness, flushing, headache, hypotension, peripheral oedema, tachycardia, and palpitations. Nausea and other gastrointestinal disturbances, increased micturition frequency, lethargy, eye pain, visual disturbances, and mental depression have also occurred. A paradoxical increase in ischaemic chest pain may occur at the start of treatment and in a few patients excessive fall in blood pressure has led to cerebral or myocardial ischaemia or transient blindness. There have been reports of rashes (including erythema multiforme), fever, and abnormalities in liver function, including cholestasis, due to hypersensitivity reactions. Gingival hyperplasia, myalgia, tremor, and impotence have been reported. Overdosage may be associated with bradycardia and hypotension; hyperglycaemia, metabolic acidosis, and coma may also occur.

Store at temperatures not exceeding 30° C. Protect from light.

Calcium Antagonists

C08CA04 - nicardipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.

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