Tablet Presentation

Each Tablet Contains:
Cilnidipine IP 5/10/20 mg

Cilnidipine is a dihydropyridine calcium antagonist. Compared with other calcium antagonists, cilnidipine can act on the N-type calcium channel that existing sympathetic nerve end besides acting on L-type calcium channel that similar to most of the calcium antagonists.

Indication

• Management of hypertension for end-organ protection
• Chronic kidney disease

Mechanism of action

Administration of cilnidipine has been shown to present an antisympathetic profile. It decreases blood pressure safely and effectively without excessive blood pressure reduction or tachycardia. 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.

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 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.
Volume of distribution: Drugs on the group of dihydropyridines such as cilnidipine tend to have a large volume of distribution. Cilnidipine presents a very high protein binding that represents to even 98% of the administered dose.
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. The half-life of the hypotensive effect for cilnidipine is of about 20.4 min

Side Effects

The common side effects include stomach pain, diarrhea and hypotension.
Severe side effects include dizziness, fast heartbeat, and swelling of face, lips, tongue, eyelids, hands and feet.

Contraindication

Cilnidipine is contraindicated in patients with severe aortic stenosis, cardiogenic shock, recent history of unstable angina or MI, heart failure and hypotension. Do not discontinue Cilnidipine abruptly to avoid withdrawal symptoms. Caution should be exercised during Cilnidipine use in pregnancy.

Interaction

Cilnidipine can interact with aldesleukin, quinidine, phenytoin, rifampicin, erythromycin, other anti-hypertensive drugs and anti-psychotic drugs.