Chemical formula: C₂₆H₂₉N₃O₆ Molecular mass: 479.525 g/mol PubChem compound: 4474
Nicardipine interacts in the following cases:
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.
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.
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.
Due to the possible risk of pulmonary oedema or excessive decrease in blood pressure, caution should be taken if magnesium sulphate is used concomitantly.
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.
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.
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.
Careful monitoring of serum digoxin levels is advised in patients also receiving nicardipine as levels may be increased.
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.
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.
Because nicardipine was found in maternal milk, breast-feeding must be discontinued during nicardipine treatment.
Caution should be exercised because the hypotensive effects of this drug may cause dizziness.
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.
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
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).
Not known: Thrombocytopenia
Not known: Anaphylactic reaction
Very common: Headache
Common: Dizziness
Common: Lower limb oedema, palpitations, hypotension, tachycardia
Not known: Atrioventricular block, angina pectoris
Common: Orthostatic hypotension
Not known: Pulmonary oedema*
Common: Nausea, vomiting
Not known: Paralytic ileus
Common: Flushing
Not known: Erythema
Not known: Phlebitis
Not known: Hepatic enzyme increased
* cases have been also reported when used as tocolytic during pregnancy
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