Ccbest M

Uses

Cilnidipine is used for the management of hypertension for end-organ protection. It is reported to be useful in elderly patients and in those with diabetes and albuminuria. Cilnidipine has been increasingly used in patients with chronic kidney disease.

Hypertension is the term used to describe the presence of high blood pressure. The blood pressure is generated by the force of the blood pumped from the heart against the blood vessels. Thus hypertension is caused when there is too much pressure on the blood vessels and this effect can damage the blood vessel

Ccbest M is also used to associated treatment for these conditions: High Blood Pressure (Hypertension)

How Ccbest M works

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.

Dosage

Ccbest M dosage

5-10 mg once daily, increase to 20 mg once daily if necessary.

Side Effects

Dizziness; flushing; headache; hypotension; peripheral oedema; tachycardia; palpitations; GI disturbances; increased micturition frequency; lethargy; eye pain; depression; ischaemic chest pain; cerebral or myocardial ischaemia; transient blindness; rashes; fever; abnormal liver function; gingival hyperplasia; myalgia; tremor; impotence.

Toxicity

The percentage of reports of cilnidipine that express drug toxicity reported as side effects are 5.26%.

Precaution

Hypotension, poor cardiac reserve, heart failure. Sudden withdrawal may exacerbate angina. Discontinue in patients who experience ischemic pain following administration. Pregnancy, lactation.

Interaction

Other antihypertensives; aldesleukin; antipsychotics that cause hypotension; may modify insulin and glucose responses; quinidine; carbamazepine; phenytoin; rifampicin; cimetidine; erythromycin.

Volume of Distribution

Drugs on the group of dihydropyridines such as cilnidipine tend to have a large volume of distribution.

Elimination Route

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.

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.

Half Life

The half-life of the hypotensive effect for cilnidipine is of about 20.4 min.

Elimination Route

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

Pregnancy & Breastfeeding use

No specific information about USFDA pregnancy category. Caution should be exercised during Cilnidipine use in pregnancy. Nursing mothers should consult a physician before taking Cilnidipine.

Contraindication

Cardiogenic shock; recent MI or acute unstable angina; severe aortic stenosis.

Innovators Monograph

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