A calcium channel blocker that belongs to the dihydropyridine class is cilnidipine. For the protection of end-organs, cilnidipine is recommended for the treatment of hypertension.

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December 3, 2022
Cilnidipine
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Indications, Uses, Dosage, Drugs Interactions, Side effects
Cilnidipine
Medicine Type :
Allopathy
Prescription Type:
Prescription Required
Approval :
DCGI (Drugs Controller General of India)
Schedule
Schedule H
Pharmacological Class:
Calcium channel blocker,
Therapy Class:
Dihydropyridine,
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

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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).

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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.
Food Warning
Salt Substitutes: Those who are taking Cilnidipine should avoid sodium, calcium, and
magnesium-rich foods. The salts may reduce the blood-pressure-lowering effect
of Cilnidipine.
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.

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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.
There are some clinical studies of the drug Cilnidipine mentioned below:
1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8695827/
2. https://www.clinicaltrials.gov/ct2/show/NCT00325637
3. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3538493/
4. https://ichgcp.net/amp/clinical-trials-registry/NCT00325637
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
Parthika Patel
Parthika Patel has completed her Graduated B.Pharm from SSR
COLLEGE OF PHARMACY and done M.Pharm in Pharmaceutics. She
can be contacted at editorial@medicaldialogues.in. Contact no. 011-
43720751

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Dr JUHI SINGLA
Dr JUHI SINGLA has completed her MBBS from Era’s Lucknow
Medical college and done MD pharmacology from SGT UNIVERSITY
Gurgaon. She can be contacted at editorial@medicaldialogues.in.
Contact no. 011-43720751