Azelnidipine

Azelnidipine is a Dihydropyridine belonging to the calcium channel blocker

Azelnidipine is used in the treatment of hypertension.

The oral ingestion of azelnidipine demonstrates rapid and dose-dependent absorption. The volume of distribution was found to be 1749 +/- 964. Azelnidipine is metabolized by hepatic cytochrome P450 (CYP) 3A4 and has no active metabolite product. It may interact with other drugs or compounds that are substrates for this enzyme. Azelnidipine is lipophilic and has a potent affinity for membranes of vascular smooth muscle cells. It gets excreted via urine and feces.

The common side effects are dizziness, drowsiness, headache, weakness, Nausea, strong irregular heartbeat, swelling, and dizziness upon standing.

Azelnidipine is available in dosage forms, such as tablets.

Azelnidipine is available in Europe, Japan, China, the USA, and India.

Azelnidipine inhibits trans-membrane Ca2+ influx through the voltage-dependent channels of smooth muscles in vascular walls. Ca2+ channels are classified into various categories, including L-type, T-type, N-type, P/Q-type, and R-type Ca2+ channels. The L-type Ca2+ channels. Normally, calcium induces smooth muscle contraction, contributing to hypertension. When calcium channels are blocked, the vascular smooth muscle does not contract, resulting in the relaxation of vascular smooth muscle walls and decreased blood pressure.

Azelnidipine is available in the form of dosage forms, such as tablets.

Azelnidipine tablets were taken orally with or without food.

Azelnidipine is used in the treatment of hypertension.

Azelnidipine is used to cure high blood pressure, also known as hypertension. The active constituent of this medicine belongs to the class of calcium channel-blocking agents. It reduces blood pressure by blocking the calcium channels, thus relaxing the blood vessels. This medication also works by reducing the pressure on blood vessels to make it for the heart to pump more blood in the body.

Azelnidipine is approved for its use in the following clinical indications:

Hypertension

This medicine is used in the treatment of hypertension which is an elevation of the blood pressure caused by genetic and/or environmental factors.

Azelnidipine is available in various dosage strengths: 8 mg and 16 mg

Azelnidipine is available in the form of dosage forms, such as tablets.

Azelnidipine is approved for the treatment of Hypertension.

Eat plenty of fruits, vegetables, and whole grains. Choose lean proteins, such as skinless chicken, fish, and beans. Eat non-fat or low-fat dairy products, such as skim milk and low-fat yogurt. Avoid foods that contain high levels of sodium (salt).

Azelnidipine may be contraindicated in the following.

Hypersensitivity, Severe hypotension, Cardiogenic shock, Left ventricular outflow tract obstruction, Heart failure after acute myocardial infarction.

The adverse reactions related to molecule Azelnidipine can be categorized as

• Common Adverse effects: Headache (usually transitory), flushing, dizziness, nausea, vomiting and weakness
• Less Common adverse effects: Red, itchy or watery eyes – these can be signs of conjunctivitis or a corneal ulcer, Painful sores (ulcers) on the eyes, skin or the lining of your mouth
• Rare Adverse effects: Tinnitus, Thrombocytopenia, Visual disturbances, Insomnia, Gynecomastia, Elevated hepatic enzymes, Anxiety and depression

The clinically relevant drug interactions of Azelnidipine are briefly summarized here.

• Hypotensive interaction may occur with alcohol, TCAs, antihypertensives and other vasodilators.

• Potentially Fatal: Enhanced hypotensive effect with sildenafil and other phosphodiesterase type-5 inhibitors.

Pharmacodynamics:

Azelnidipine is a vasodilator that induces a gradual decrease in blood pressure in hypertensive patients. Unlike other members of its drug class, azelnidipine does not induce reflex tachycardia due to vasodilation. This is likely due to the fact that it elicits a gradual fall in blood pressure.

It also exhibits a prolonged hypotensive effect and has been shown to have a strong anti-arteriosclerotic action in vessels due to its high affinity for vascular tissue and antioxidative activity

Pharmacokinetics:

• Absorption

The absorption ratio of radioactivity estimated from the sum of biliary and urinary excretions was found to be approximately 62% . The radioactivity was high in the gastrointestinal tract and liver, followed by the adrenal glands, suggesting high rates of metabolism in these regions.

• Metabolism

Azelnidipine is mainly metabolized in the liver. Its metabolites are N-dephenylated Azelnidipine (DPH), deaminated Azelnidipine (A.L.) and N-debenzylated Azelnidipine (DBZ). Both metabolites behave as calcium antagonists. In one study, the vasodilating capabilities of DBZ and DPH were about two-thirds and one-third respectively than that of the unmetabolized drug. Research suggests that the majority of the pharmacological effect after oral dosing of Azelnidipine hydrochloride is due to unchanged drug and its metabolites play little role in its therapeutic effect.

• Elimination

Azelnidipine is also referred to as NZ-105 and has been found to be mainly eliminated by the biliary system

1. https://go.drugbank.com/drugs/DB09235
2. https://www.apollopharmacy.in/salt/AZELNIDIPINE
3. https://pubchem.ncbi.nlm.nih.gov/compound/Azelnidipine #section=MeSH-Pharmacological-Classification
4. https://www.medplusmart.com/product/efnocar-40mg-tab_efno0001