INTRODUCTION

Nicardipine
Nicardipine is a medication used to treat hypertension and
angina. It belongs to the dihydropyridine class of class of calcium
channel blockers. It is available in by mouth and intravenous
formulations.
Brand Names:- Cardene IV, Cardene SR
Dosage Form:- Capsule, IV injection
Dosage:- Initial dose:- Treatment should start with the
continuous administration of nicardipine at a rate of 3-5 mg/h for
15 minutes. Rates can be increased by increments of 0.5 or 1 mg
every 15 minutes. The infusion rate should not exceed 15 mg/h.
Maintenance dose:- When the target pressure is reached, the dose
should be reduced progressively, usually to between 2 and 4 mg/h,
to maintain the therapeutic efficacy.
Mechanism of Action:- By deforming the channel, inhibiting
ion-control gating mechanisms, and/or interfering with the
release of calcium from the sarcoplasmic reticulum, nicardipine
inhibits the influx of extracellular calcium across the myocardial
and vascular smooth muscle cell membranes the decrease in
intracellular calcium inhibits the contractile processes of the
myocardial smooth muscle cells, causing dilation of the coronary
and systemic arteries, increased oxygen delivery to the
myocardial tissue, decreased total peripheral resistance,
decreased systemic blood pressure, and decreased afterload.

Synthesis of Nicardipine:- Methyl ester of ß-aminocrotonic

acid is reacted with 2-methyl-2-benzylaminoethyl ester of
acetoacetic acid gives nicardipine.

Side Effects:- Fever and neck pain, flushing, or swelling

ankles/feet, indigestion, Reduced platelets count, etc.
Uses:- Severe chest pain (angina), hypertension.
 SUMMARY/REPORT

Nicardipine is used to treat high blood pressure and to control

angina (chest pain). It is also used for Raynaud's phenomenon. It
has been used in percutaneous coronary intervention. Nicardipine
is a second-generation dihydroperidine calcium channel blockers.
It lowers blood pressure by relaxing the blood vessels so the heart
does not have to pump as hard. It controls chest pain by
increasing the supply of blood and oxygen to the heart. It may
help to increase your ability to exercise and decrease the
frequency of angina attacks. It has also been used in the treatment
of asthma and enhances the action of specific antineoplastic
agents. It has a role as an antihypertensive agent, a calcium
channel blocker, a vasodilator agent and an autophagy inhibitor.
It is available in by mouth and intravenous formulations.
Multiple studies and case reports have shown nicardipine to be
safe and effective in a variety of patients, including neonates,
children with postoperative hypertension, and children with
hypertensive crises. It has also been used effectively in children
with renal disease. Nicardipine is metabolized in the liver.
Nicardipine comes as a regular capsule and as an extended-
release (long-acting) capsule to take by mouth. The regular
capsule is usually taken three times a day. The extended-release
capsule is usually taken two times a day. If taken regularly,
nicardipine controls chest pain, but it does not stop chest pain
once it starts. People should not use nicardipine if they have
severe narrowing of the aortic valve in your heart (aortic
stenosis). Nicardipine may cause serious side effects like a light-
headed feeling, pounding heartbeats or fluttering in chest, severe
or ongoing chest pain. Nicardipine is not a beta-blocker and
therefore gives no protection against the dangers of abrupt beta-
blocker withdrawal. Women who wish to breastfeed should not be
given this drug. Safety and efficacy in patients under the age of 18
also have not been established. Drinking alcohol with this
medicine can cause side effects.
 REFERENCE

I. Kar Ashutosh, Medicinal chemistry, New Age international

publishers, 8th edition, page:-423-424

II. Algarsamy V., Textbook of Medicinal Chemistry, Vol 2,

CBS Publishers and Distributors Pvt Ltd., 3rd edition, Page

No:- 453-454

III. Razadan B., Medicinal Chemistry, CBS Publishers and

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IV. Narajji C., Patil V.C., Medicinal Chemistry I, Nirali

Prakashan, 6th edition, Page No:- 116-117

V. Miller P.F., Agnes F.V., McBrewster J., Medicinal

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