CARDIBLOC-SR CAPSULE 40mg

Nicardipine

Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.

Active Ingredient / Synonyms

Nicardipino | Nicardipinum | Nicardipine |

Description

A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. [PubChem]

Indication

Used for the management of patients with chronic stable angina and for the treatment of hypertension.

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.

Pharmacodynamics

Nicardipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nicardipine is similar to other peripheral vasodilators. Nicardipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. 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.

Pharmacokinetics

Absorption:

While nicardipine is completely absorbed, it is subject to saturable first pass metabolism and the systemic bioavailability is about 35% following a 30 mg oral dose at steady state.

Distribution:

* 8.3 L/kg

Metabolism:

Nicardipine HCl is metabolized extensively by the liver.

Elimination:

Nicardipine has been shown to be rapidly and extensively metabolized by the liver.

Half-life

8.6 hours

Clearance

* 0.4 L/hr∙kg [Following infusion]

Toxicity

Oral LD50 Rat = 184 mg/kg, Oral LD50 Mouse = 322 mg/kg

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

CARDIBLOC-SR CAPSULE 40mg was registered with Health Science Authority of Singapore by ZUELLIG PHARMA PTE LTD. It is marketed with the registration number of SIN10226P with effective from 1998-10-10.

This product contains 40mg of Nicardipine in the form of CAPSULE.

The medicine was manufactured by ASTELLAS PHARMA TECH CO. LTD in JAPAN

It is a Presciption Only Medicine which can only be obtained from a doctor or a dentist, or from a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Anatomical Therapeutic Chemical (ATC) Classification

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44 APO-DIAZEPAM TABLET 5mg Diazepam POM PHARMAFORTE SINGAPORE PTE LTD Active
45 APO-DIAZEPAM TABLET 10mg Diazepam POM PHARMAFORTE SINGAPORE PTE LTD Active
46 APO-PROPRANOLOL TABLET 10mg Propranolol POM PHARMAFORTE SINGAPORE PTE LTD Active
55 APO-ISDN TABLET 10mg Isosorbide Dinitrate POM PHARMAFORTE SINGAPORE PTE LTD Active
63 DIAPO TABLET 10mg Diazepam POM BEACONS PHARMACEUTICALS PTE LTD Active
64 FURMIDE TABLET 40mg Furosemide POM BEACONS PHARMACEUTICALS PTE LTD Active

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508 APO-SULFATRIM PEDIATRIC TABLET Sulfamethoxazole|Trimethoprim POM PHARMAFORTE SINGAPORE PTE LTD Active
526 B.S. SUSPENSION Sulfamethoxazole|Trimethoprim POM APEX PHARMA MARKETING PTE LTD Active
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