Nicardipine

Chemical formula: C₂₆H₂₉N₃O₆  Molecular mass: 479.525 g/mol  PubChem compound: 4474

Interactions

Nicardipine interacts in the following cases:

Cardiac failure

Haemodynamic studies in patients with heart failure have shown that nicardipine reduces afterload and improves overall haemodynamics. In one study, intravenous nicardipine reduced myocardial contractility in patients with severe heart failure despite increases in cardiac index and ejection fraction noted in the same patients.

Since nicardipine has not been extensively studied in patients with severe left ventricular dysfunction and cardiac failure one must consider that worsening of cardiac failure may occur.

CYP3A4 inducers, CYP3A4 inhibitors

Nicardipine is metabolized by cytochrome P450 3A4. Concomitant administration of nicardipine with inducers (e.g. carbamazepine and rifampicin) or inhibitors (e.g. cimetidine and grapefruit juice) of cytochrome P450 3A4 may alter the plasma levels of nicardipine.

Clinical monitoring during treatment with an enzyme inducing or inhibiting agent, and after its discontinuation, is required.

Impaired liver function, impaired renal function

Since nicardipine is subject to first-pass metabolism, use with caution in patients with impaired liver function or reduced hepatic blood flow. Patients with severe liver disease showed elevated blood levels and the half-life of nicardipine was prolonged. Nicardipine blood levels may also be elevated in some renally impaired patients. Therefore the lowest starting dose and extending the dosing interval should be individually considered in these patients.

Magnesium

Due to the possible risk of pulmonary oedema or excessive decrease in blood pressure, caution should be taken if magnesium sulphate is used concomitantly.

Beta-blocking, anti-hypertensive drugs

Nicardipine may be used in combination with beta-blocking and other anti-hypertensive drugs but the possibility of an additive effect resulting in postural hypotension should be considered.

Caution should be exercised when using nicardipine in combination with a beta-blocker in patients with decreased cardiac function.

If switching from beta-blockers to nicardipine, gradually reduce the beta-blocker dose (preferably over 8-10 days) since nicardipine gives no protection against the dangers of abrupt beta-blocker withdrawal.

Ciclosporin, tacrolimus, sirolimus

Concomitant administration of nicardipine and cyclosporine, tacrolimus or sirolimus results in elevated plasma cyclosporine, tacrolimus or sirolimus levels. Cyclosporine, tacrolimus or sirolimus level should be monitored and dosage of immunosuppressant and/or nicardipine should be reduced, if required.

Dantrolene

In animal studies, administration of verapamil and intravenous dantrolene has caused fatal ventricular fibrillation. The combination of a calcium channel inhibitor and dantrolene is therefore potentially dangerous.

Digoxin

Careful monitoring of serum digoxin levels is advised in patients also receiving nicardipine as levels may be increased.

Fentanyl

Severe hypotension has been reported during fentanyl anaesthesia with concomitant use of a beta-blocker and calcium blockade. Even though such interactions have not been seen in clinical trials, such hypotensive episodes should be vigorously treated with conventional therapy such as intravenous fluids.

Pregnancy

Acute pulmonary oedema has been observed when nicardipine has been used as tocolytic during pregnancy, especially in cases of multiple pregnancy (twins or more), with the intravenous route and/or concomitant use of beta-2 agonists.

Nursing mothers

Because nicardipine was found in maternal milk, breast-feeding must be discontinued during nicardipine treatment.

Effects on ability to drive and use machines

Caution should be exercised because the hypotensive effects of this drug may cause dizziness.

Adverse reactions


Oral administration

Majority are not serious and are expected consequences of the vasodilator effects of Cardene.

The most frequent side-effects reported are headache, oedema peripheral, heat sensation and/or flushing, palpitations, nausea and dizziness.

Other side-effects noted in clinical trials include the following:

Cardiac disorders: Tachycardia

As with the use of other short-acting dihydropyridines in patients with ischaemic heart disease, exacerbation of angina pectoris may occur frequently at the start of treatment with nicardipine capsules. The occurrence of myocardial infarction has been reported although it is not possible to distinguish such an event from the natural course of ischaemic heart disease.

Gastro-intestinal disorders: Gastro-intestinal upset, Gingival hyperplasia, Vomiting

General disorders and administration site conditions: Asthenia

Hepatobiliary disorders: Hepatic function abnormal

Renal and urinary disorders: Renal function abnormal, Frequency of micturition

Nervous system disorders: Drowsiness, Insomnia, Tinnitus, Paraesthesia, Functional disorders

Respiratory, thoracic and mediastinal disorders: Dyspnoea

Frequency: unknown, Pulmonary oedema*

* cases have been also reported when used as tocolytic during pregnancy

Skin and subcutaneous tissue disorders: Erythema, Pruritis, Rash

Vascular disorders: Hypotension, Orthostatic hypotension

Immune system disorders: Anaphylactic reaction

Frequency: Unknown

Investigations: Hepatic enzyme increased

Frequency: Unknown

Rarely, depression, impotence and thrombocytopenia have been reported.

The above mentioned listed adverse reactions have been observed during clinical studies and/or during marketed use.

IV administration

Summary of the safety profile

The majority of undesirable effects are the consequence of the vasodilator effects of nicardipine. The most frequent events are headache, dizziness, peripheral oedema, palpitations and flushing

List of adverse reactions

Adverse reactions listed below have been observed during clinical studies and/or during marketed use and are based on clinical trial data and classified according to MedDRA System Organ Class. Frequency categories are defined according to the following convention: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000) and not known (cannot be estimated from the available data).

Blood and lymphatic system disorders

Not known: Thrombocytopenia

Immune system disorders

Not known: Anaphylactic reaction

Nervous system disorders

Very common: Headache

Common: Dizziness

Cardiac disorders

Common: Lower limb oedema, palpitations, hypotension, tachycardia

Not known: Atrioventricular block, angina pectoris

Vascular disorders

Common: Orthostatic hypotension

Respiratory, thoracic and mediastinal disorders

Not known: Pulmonary oedema*

Gastrointestinal disorders

Common: Nausea, vomiting

Not known: Paralytic ileus

Skin and subcutaneous tissue disorders

Common: Flushing

Not known: Erythema

General disorders and administration site conditions

Not known: Phlebitis

Investigations

Not known: Hepatic enzyme increased

* cases have been also reported when used as tocolytic during pregnancy

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