Cilnidipine is approved for use in countries like Japan, China, India, Korea, and also in some European countries to treat hypertension. It decreases blood pressure and is used to treat hypertension. Due to its blocking action at the N-type and L-type calcium channel, cilnidipine dilates both arterioles and venules, which reduces the pressure in the capillary bed.
Cilnidipine 5 MG Tablet is known to be channel blocker of calcium. It helps in treating high blood pressure. Cilnidipine Tablet stops the calcium activity on the blood vessels and the heart.It results in increase in the supply of blood to the heart. This in turn helps lower blood pressure as well as slows down the heart rate.
The route of administration of drug is orally and the dosge may vary from 5mg to 10 mg.In some cases, dosage as high as 20 mg may also be prescribed. This drug should be consumed once or even twice daily depending on the dosage and intensity of the condition. As such there are no side effects of this medication.
Indications:
Cilnidipine is indicated for the treatment of hypertension for end-organ protection.It is reported to bevery useful in elderly patients and in those with diabetes and albuminuria. Cilnidipine has been also used in chronic kidney disease patients.It decreases blood pressure which helps to treat hypertension.
Mechanism of action:
Cilnidipine acts on the L-type calcium channels of blood vessels it blocks the incoming calcium and suppressing the contraction of blood vessels, thereby reducing blood pressure. Cilnidipine 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.
Pharmacodynamics:
Administration of cilnidipine has been shown to present an antisympathetic profile in vitro and in vivo. It decreases blood pressure safely and effectively without excessive blood pressure reduction or tachycardia. It is a dihydropyridine class of calcium-channel blocker. Cilnidipine prevents intracellular calcium influx and results in vasodilatation. Cilnidipine possesses superior selectivity for vascular smooth muscle cells.
Pharmacokinetics:
Absorption: Cilnidipine have 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 tissues. Cilnidipine does not present a high accumulation in the tissue after it is orally administrated.
Cilnidipine is reported to present very low bioavailability determined to be approximately 13%. This low bioavailability is due to its low aqueous solubility and high permeability. One of these formulations corresponds to the generation of polymeric nanoparticles which enhance the bioavailability by 2.5-3-fold.
Drugs which are in group of dihydropyridines like cilnidipine tend to have a large volume of distribution.Liver and kidney both are metabolized by Cilnidipine . 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
The route of elimination of Cilnidipine is through the urine in a proportion of 20% of the administered dose and rest of 80% is eliminated by the feces.
Side Effects:
● Dizziness,sleepiness
● Fatigue
● Eye pain
● Palpitation
● Hypotension
● Swelling Of Face, Lips, Eyelids, Tongue, Hands And Feet
● Fast Heartbeat
● Muscle Pain
● Shaking Of Hands Or Feet
● Skin Rash
● Decrease In Libido
● Increased Urination Frequency
● Stomach Pain
● Diarrhoea
Contraindications & Precaution:
Cilnidipine is contraindicated in patients who are suffering from severe aortic stenosis, cardiogenic shock, recent history of unstable angina or MI, heart failure and hypotension.
Cilnidipine should not be discontinued abruptly to avoid withdrawal symptoms.