Nitrendipine

Nitrendipine is an antihypertensive belonging to Calcium channel blocker.

Nitrendipine is a calcium channel blocker indicated in the treatment of arterial hypertension.

Nitrendipine well absorbed from the GI tract. The Absolute bioavailability of Nitrendipine is about 10-30%. Time to peak plasma concentration is approximately within 1-3 hours.

Nitrendipine is about 98% of protein binding. The volume of distribution of Nitrendipine is approximately 6 L/kg. Nitrendipine metabolized in the liver. It Undergoes extensive first-pass metabolism. Terminal elimination half-life is approximately 10-22 hours. Nitrendipine excreted via urine and feces (as inactive metabolites, <0.1% as unchanged drug).

Nitrendipine shows common side effects like Headache, Palpitations, Edema, Flatulence, Diarrhea, Nausea, Hypotension, Vomiting, Constipation, Dry mouth, Chest pain, Dizziness, etc.

Nitrendipine is available in the form of Oral Tablets.

Nitrendipine is available in India, US, Germany, Spain, Switzerland, Poland, Japan, China, and France.

Nitrendipine belonging to the Calcium Channel Blocker, acts as an antihypertensive agent.

Nitrendipine 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.

The Onset of action of Nitrendipine is within 1-3 hours.

The Tmax and Duration of Action for Nitrendipine in the body is not known.

Nitrendipine is available in the form of Oral Tablet.

Nitrendipine Tablet is taken orally, usually once or twice a day.

Nitrendipine is a dihydropyridine calcium channel blocker indicated in the treatment of arterial hypertension.

Nitrendipine is an antihypertensive agent belonging to calcium channel blocker.

Nitrendipine relaxes coronary vascular smooth muscles by inhibiting Calcium ions. It lowers BP primarily by arteriolar dilation.

Nitrendipine is approved for use in the following clinical indications

● Hypertension

Nitrendipine is indicated in the treatment of arterial hypertension.

● Hypertension

● Adult: 20 mg daily as a single dose or in 2 divided doses, may be increased to 20 mg two times a day as necessary to control resistant Hypertension.

Elderly: Initially, 10 mg daily.

Nitrendipine is available in various strengths as 10mg and 20mg.

Nitrendipine is available in the form of Oral Tablet.

Dosage Adjustment in Kidney Patient

Information is not available.

Dosage Adjustment in Hepatic impairment Patient

Initially: 5–10 mg once daily.

Avoid grapefruit juice while taking Nitrendipine.

 Nitrendipine is contraindicated in patients with

● Hypersensitivity to other calcium channel blocking agents, hypotension, advanced aortic stenosis.

● Patients with severe aortic stenosis, poor cardiac reserve, heart failure.

● Use with caution in Pregnancy and lactation.

● Use with caution in patients with liver insufficiency, digital ischemia, nonobstructive hypertrophic cardiomyopathy, Duchenne muscular dystrophy, or in combination with beta-blockers.

Information is not available.

Nitrendipine is not recommended for use in breastfeeding women unless absolutely necessary. All the risks and benefits should be considered before Nitrendipine.

Nitrendipine is not recommended for use in pregnant women unless necessary. All the risks and benefits should be considered before taking Nitrendipine.

Avoid grapefruit juice while taking Nitrendipine.

 Avoid grapefruit juice while taking Nitrendipine.

● Atenolol: Increased hypotensive effect.

● Carteolol: Increased hypotensive effect.

● Digoxin: At nitrendipine doses exceeding 20 mg daily, increased digoxin levels and toxicity can occur.

● Metoprolol: Increased hypotensive effect.

● Ranitidine: Decrease in clearance of nitrendipine probably of little clinical significance

The common side effect of Nitrendipine include the following

● Headache, Palpitations, Edema, Flatulence, Diarrhea, Nausea, Hypotension, Vomiting, Constipation, Dry mouth, Chest pain, Dizziness.

● Pregnancy

Pregnancy Category

Nitrendipine is not recommended for use in pregnant women unless necessary. All the risks and benefits should be considered before taking Nitrendipine.

● Nursing Mothers

Nitrendipine is not recommended for use in breastfeeding women unless absolutely necessary. All the risks and benefits should be considered before Nitrendipine.

● Pediatric Use

Information is not available.

● Geriatric Use

Information is not available.

Information is not available.

● 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 like 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

Nitrendipine well absorbed from the GI tract. The Absolute bioavailability of Nitrendipine is about 10-30%. Time to peak plasma concentration is approximately within 1-3 hours.

Distribution

Nitrendipine is about 98% of protein binding. The volume of distribution of Nitrendipine is approximately 6 L/kg.

Metabolism and Excretion

Nitrendipine metabolized in the liver. It Undergoes extensive first-pass metabolism.

Terminal elimination half-life is approximately 10-22 hours. Nitrendipine excreted via urine and feces (as inactive metabolites, <0.1% as unchanged drug).

1. Vanov SK, Pun EF, Taylor RJ. The Safety of Nitrendipine in the Treatment of Essential Hypertension--A Review of 61 Clinical Studies. Angiology. 1988 Jan 15;39(1).

2. Goa KL, Sorkin EM. Nitrendipine. Drugs. 1987 Feb;33(2):123-55.

3. Voruganti S, Yamsani SK, Ravula SK, Gannu R, Yamsani MR. Effect of pomegranate juice on intestinal transport and pharmacokinetics of nitrendipine in rats. Phytotherapy Research. 2012 Aug;26(8):1240-5.

https://go.drugbank.com/drugs/DB01054

https://www.practo.com/medicine-info/nitrendipine-1074-api

https://www.mims.com/india/drug/info/nitrendipine?type=full&mtype=generic#mechanism-of-action

https://www.syrianclinic.com/med/en/ProfDrugs/Nitrendipinepd.html