Drug information of Nitrendipine

Nitrendipine


Nitrendipine is a calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.

Mechanism of effect

By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Nitrendipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

Pharmacodynamic

Nitrendipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nitrendipine is similar to other peripheral vasodilators. Nitrendipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

Pharmacokinetics

Absorption: Well absorbed from the GI tract. Absolute bioavailability: 10-30%. Time to peak plasma concentration: 1-3 hr.
Distribution: Plasma protein binding: Approx 98%.
Metabolism: Metabolised in the liver. Undergoes extensive first-pass metabolism.
Excretion: Via urine and faeces 

Drug indications

Hypertension

Dosage

Dosage Details
Oral
Hypertension
Adult: 20 mg daily as a single dose or in 2 divided doses, may be increased to 20 mg bid as necessary to control resistant HTN.
Elderly: Initially, 10 mg daily.
Hepatic Impairment
Initially, 5-10 mg once daily.

Drug contraindications

• in patients with known hypersensitivity to nitrendipine or to any of the excipients
in patients with unstable angina pectoris and after acute myocardial infarction within the first 4 weeks
during pregnancy and lactation
in cases of decompensated heart failure

Side effects

The most common ADRs (frequency common: ≥1/100 to < 1/10) are headache, palpitations, vasodilation, oedema, flatulence, feeling unwell, and anxiety reactions. None of these ADRs is considered severe from the overall experience. Except from ‘feeling unwell’ and ‘anxiety reactions’ the ADRs are attributable to the mode of action of nitrendipine. The most severe ADRs are hypotension, angina pectoris (chest pain), and allergic reaction including angioedema (all frequency uncommon: ≥ 1/1,000 to < 1/100). These ADRs, dependent on their course, might require immediate medical intervention. ADRs listed under “common” were observed with a frequency below 3 % with the exception of oedema (6.2 %), headache (4.7 %) and vasodilatation (3.0 %)

macrolide antibiotics (e.g., erythromycin), • anti-HIV protease inhibitors (e.g., ritonavir), • azole antimycotics (e.g., ketoconazole), • the antidepressants nefazodone and fluoxetine, • quinupristin/dalfopristin, • valproic acid, • cimetidine and ranitidine
• diuretics, • beta-blockers, • ACE-inhibitors, • Angiotensin 1 (AT1) receptor-antagonists, • other calcium antagonists, • alpha-adrenergic blocking agents, • PDE5 inhibitors, • alpha-methyldopa

Points of recommendation

Should be taken with food
Protect from light.

Pregnancy level

X

contraindication

Breast feeding warning

contraindication

Related drugs

Amlodipine , Nifedipine , Nimodipine


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