Cilnidipine
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Cilnidipine is a
calcium channel blocker Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are a group of medications that disrupt the movement of calcium () through calcium channels. Calcium channel blockers are used as antihypertensive drugs, i.e., as ...
. Cilnidipine is approved for use in Japan, China, India, Nepal, and Korea for
hypertension Hypertension, also known as high blood pressure, is a Chronic condition, long-term Disease, medical condition in which the blood pressure in the artery, arteries is persistently elevated. High blood pressure usually does not cause symptoms i ...
. It is a calcium antagonist accompanied with L-type and N-type calcium channel blocking functions. Unlike other calcium antagonists, cilnidipine can act on the N-type calcium channel in addition to acting on the L-type calcium channel. It was patented in 1984 and approved for medical use in 1995. Cilnidipine is currently being repurposed and developed for use in patients with
Raynaud's phenomenon Raynaud syndrome, also known as Raynaud's phenomenon, is a medical condition in which the spasm of small arteries causes episodes of reduced blood flow to end arterioles. Typically the fingers, and, less commonly, the toes, are involved. Rare ...
and
systemic sclerosis Systemic scleroderma, or systemic sclerosis, is an autoimmune rheumatic disease characterised by excessive production and accumulation of collagen, called fibrosis, in the skin and internal organs and by injuries to small arteries. There are tw ...
by Aisa Pharma, a US biopharma development company.


Medical uses

Cilnidipine decreases blood pressure and is used to treat hypertension and its
comorbidities In medicine, comorbidity refers to the simultaneous presence of two or more medical conditions in a patient; often co-occurring (that is, concomitant or concurrent) with a primary condition. It originates from the Latin term (meaning "sickness" ...
. Due to its blocking action at the N-type and L-type calcium channel, cilnidipine dilates both
arteriole An arteriole is a small-diameter blood vessel in the microcirculation that extends and branches out from an artery and leads to capillary, capillaries. Arterioles have vascular smooth muscle, muscular walls (usually only one to two layers of smoo ...
s and
venule A venule is a very small vein in the microcirculation that allows blood to return from the capillary beds to drain into the venous system via increasingly larger veins. Post-capillary venules are the smallest of the veins with a diameter of ...
s, reducing the pressure in the
capillary bed A capillary is a small blood vessel, from 5 to 10 micrometres in diameter, and is part of the microcirculation system. Capillaries are microvessels and the smallest blood vessels in the body. They are composed of only the tunica intima (the inn ...
. Cilnidipine is vasoselective and has a weak direct
dromotropic The term ''dromotropic'' derives from the Greek word δρόμος ''drómos'', meaning "running", a course, a race. A dromotropic agent is one which affects the conduction speed (in fact the magnitude of delay) in the AV node, and subsequently th ...
effect, a strong vasodepressor effect, and an arrhythmia-inhibiting effect. Blood pressure control with cilnidipine treatment in Japanese post-stroke hypertensive patients
he CA-ATTEND study He or HE may refer to: Language * He (letter), the fifth letter of the Semitic abjads * He (pronoun), a pronoun in Modern English * He (kana), one of the Japanese kana (へ in hiragana and ヘ in katakana) * Ge (Cyrillic), a Cyrillic letter cal ...
- the results of a large-scale prospective post-marketing surveillance study of post-stroke hypertensive patients (n = 2667, male 60.4%, 69.0 ± 10.9 years) treated with cilnidipine indicate that cilnidipine was effective in treating uncontrolled blood pressure and was well tolerated in post-stroke hypertensive patients. The Ambulatory Blood Pressure Control and Home Blood Pressure (Morning and Evening) Lowering By N-Channel Blocker Cilnidipine (ACHIEVE-ONE) trial is a large-scale (n=2319) clinical study on blood pressure (BP) and pulse rate (PR) in the real world with use of cilnidipine - this study revealed that Cilnidipine significantly reduced BP and PR in hypertensive patients at the clinic and at home, especially with higher BP and PR in the morning. Cilnidipine is currently being studied in the RECONNOITER study in Australia for its effect on Raynaud's and other manifestations of disease in patients with Systemic Sclerosis.


Side effects

The side effects could be severe dizziness, fast heartbeat, and swelling of face, lips, tongue, eyelids, hands and feet. Lesser side effects include stomach pain, diarrhea and hypotension.
Peripheral edema Peripheral edema is edema (accumulation of fluid causing swelling) in tissues perfused by the peripheral vascular system, usually in the lower limbs. In the most dependent parts of the body (those hanging distally), it may be called dependent ede ...
, a common side effect from the use of
amlodipine Amlodipine, sold under the brand name Norvasc among others, is a calcium channel blocker medication used to treat hypertension, high blood pressure, coronary artery disease (CAD) and variant angina (also called Prinzmetal angina or coronary ar ...
, was reduced when patients were shifted to cilnidipine.


Brand names

In India, it is sold under the brand name Cinod, Cilacar, Clinblue, Cilaheart, and among others at doses of 5mg–10mg–20mg.


History

It was jointly developed by Fuji Viscera Pharmaceutical Company and
Ajinomoto is a Japanese multinational food and biotechnology corporation which produces seasonings, cooking oils, frozen food Freezing food Food preservation, preserves it from the time it is prepared to the time it is eaten. Since early times, farm ...
, and was approved to enter the market and be used as an anti-hypertensive in 1995.


References


Further reading

* {{refend Calcium channel blockers Dihydropyridines 3-Nitrophenyl compounds Carboxylate esters Ethers