Product Information
Registration Status: ActiveCARDIBLOC-SR CAPSULE 40mg is approved to be sold in Singapore with effective from 1998-10-10. It is marketed by ZUELLIG PHARMA PTE LTD, with the registration number of SIN10226P.
This product contains Nicardipine 40mg in the form of CAPSULE. It is approved for ORAL use.
This product is manufactured by ASTELLAS PHARMA TECH CO. LTD in JAPAN.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
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.
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
Clearance
* 0.4 L/hr∙kg [Following infusion]
Toxicity
Oral LD50 Rat = 184 mg/kg, Oral LD50 Mouse = 322 mg/kg
Active Ingredient/Synonyms
Nicardipino | Nicardipinum | 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.