Cilnidipine

Cilnidipine is a dihydropyridine belonging to the calcium channel blocker

Cilnidipine is indicated for the management of hypertension for end-organ protection.

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. Cilnidipine is mainly metabolized in the liver. Its metabolites are N-dephenylated Cilnidipine(DPH), deaminated Cilnidipine(AL), and N-debenzylated Cilnidipine(DBZ). Both metabolites behave as calcium antagonists. Cilnidipine is also referred to as NZ-105 and has been found to be mainly eliminated by the biliary system.

The Tmax of Cilnidipine was about 1.50-3.67 hours, and Cmax was about 9.66-66.91 ng/ml.

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

Cilnidipine is available in dosage forms, such as tablets.

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

Cilnidipine acts on the L-type calcium channels of blood vessels by blocking the incoming calcium and suppressing the contraction of blood vessels, thereby reducing blood pressure. Cilnidipine also works on the N-type calcium channel located at the end of the sympathetic nerve, inhibiting the emission of norepinephrine and suppressing the increase in stress blood pressure.

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

Cilnidipine tablets were taken orally with or without food.

Cilnidipine is indicated for the management of hypertension for end-organ protection.

Cilnidipine is a calcium channel blocker. It lowers blood pressure by relaxing blood vessels, which makes the heart more efficient at pumping blood throughout the body.

Cilnidipine 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.

Cilnidipine is available in various dosage strengths: 5 mg, 10 mg, 20 mg.

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

• Dose Adjustment in Pediatric Patients.

Cilnidipine is not recommended to Pediatric Patient.

Cilnidipine is indicated for the management of hypertension for end-organ protection.

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).

Cilnidipine may be contraindicated in the following.

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

• Aortic stenosis

Aortic stenosis is narrowing or blockage of the aortic valve (it is a branch of a larger blood vessel in your heart) that regulates blood flow in the chambers of your heart. This medicine slows down the blood flow, which may increase the risk of very low blood pressure.

• Liver disease

Use Cilnidipine with caution if one has liver problems as this medicine is broken down and absorbed in the liver. An impaired liver can lead to the accumulation of this medicine and cause serious side effects.

• Kidney diseases

Use Cilnidipine with caution if one has severe kidney problems as this medicine is filtered and excreted through the kidneys. It may lead to the accumulation of this medicine in your blood and increase the risk of side effects.

The adverse reactions related to molecule Cilnidipine can be categorized as

• Common Adverse effects: Swelling of feet, Tiredness, Headache, Depression, Nausea, Dizziness, Stomach pain, Palpitations, flushing and excessive fall in blood pressure are observed as serious side effects along with male sexual dysfunction and allergic reactions.
• 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

Pharmacodynamics:

Cilnidipine is a calcium channel blocker that works by normalizing the blood pressure by relaxing the blood vessels and improves blood flow and oxygen in the body, thereby reducing the risk of getting chest pain. It prevents the entry of calcium from entering into the muscles, leading to muscle relaxation.

Pharmacokinetics:

• Absorption

Cilnidipine presents a very rapid absorption with a maximum peaked concentration after 2 hours. Its distribution tends to be higher in the liver as well as in kidneys, plasma and other tissues. Cilnidipine does not present a high accumulation in the tissue after repeated oral administration.

• Distribution

Cilnidipine is reported to present very low bioavailability determined to be approximately 13%. This low bioavailability is suggested to be due to its low aqueous solubility and high permeability. Hence, efforts have been made in order to find an innovative formulation that can significantly improve the bioavailability of this drug. One of these formulations corresponds to the generation of polymeric nanoparticles which enhance the bioavailability by 2.5-3-fold.

• Metabolism:

Cilnidipine is metabolized by both liver and kidney. It is rapidly metabolized by liver microsomes by a dehydrogenation process. The major enzymatic isoform involved in Cilnidipine dehydrogenation of the dihydropyridine ring is CYP3A.

• Elimination

Cilnidipine gets eliminated through the urine in a proportion of 20% of the administered dose and 80% is eliminated by the feces.

1. https://www.google.com/amp/s/www.practo.com/medicine-info/amp/cilnidipine-10-mg-tablet-19662
2. https://www.apollopharmacy.in/salt/CILNIDIPINE
3. https://www.1mg.com/generics/cilnidipine-209598
4. https://go.drugbank.com/drugs/DB09232