Product Information
Registration Status: ActiveKANARB®PLUS FILM COATED TABLETS 60 MG/12.5 MG is approved to be sold in Singapore with effective from 2019-09-26. It is marketed by ZUELLIG PHARMA PTE LTD, with the registration number of SIN15818P.
This product contains Fimasartan 60mg, and Hydrochlorothiazide 12.5MG in the form of TABLET, FILM COATED. It is approved for ORAL use.
This product is manufactured by BORYUNG PHARMACEUTICAL CO. in KOREA, and LTD. in REPUBLIC OF.
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
Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Concurrent administration of fimasartan with diuretic hydrochlorothiazide has shown to be safe in clinical trials. Fimasartan was approved for use in South Korea in September 9th, 2010 and is available under the brand name Kanarb through Boryung Pharmaceuticals, who are presently seeking worldwide partnership.
Indication
Used for the treatment of hypertension and heart failure [A20319].
Mechanism of Action
Angiotensin II activates AR1 leading to vasoconstriction and increased noradrenaline release which further increases vasoconstriction via action at α1-adrenergic receptors [A20319, T28]. It also stimulates secretion of aldosterone which acts to increase sodium and water reabsorption in the renal tubules [T28]. Fimasartan bind to and antagonizes AR1 preventing vasoconstriction and reducing aldosterone secretion to increase natriuresis leading to a reduction in blood volume. Together these effects produce an anti-hypertensive effect.
Pharmacokinetics
- Absorption
- Tmax is 0.5-1.3 h [A20319].
- Distribution
- Metabolism
- Elimination
Active Ingredient/Synonyms
Fimasartan | Fimasartan |
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.
Description
A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It has been used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism. [PubChem]
Indication
For the treatment of high blood pressure and management of edema.
Mechanism of Action
Hydrochlorothiazide, a thiazide diuretic, inhibits water reabsorption in the nephron by inhibiting the sodium-chloride symporter (SLC12A3) in the distal convoluted tubule, which is responsible for 5% of total sodium reabsorption. Normally, the sodium-chloride symporter transports sodium and chloride from the lumen into the epithelial cell lining the distal convoluted tubule. The energy for this is provided by a sodium gradient established by sodium-potassium ATPases on the basolateral membrane. Once sodium has entered the cell, it is transported out into the basolateral interstitium via the sodium-potassium ATPase, causing an increase in the osmolarity of the interstitium, thereby establishing an osmotic gradient for water reabsorption. By blocking the sodium-chloride symporter, hydrochlorothiazide effectively reduces the osmotic gradient and water reabsorption throughout the nephron.
Pharmacokinetics
- Absorption
- 50-60%
- Distribution
- Metabolism
- Hydrochlorothiazide is not metabolized.
- Elimination
Toxicity
The most common signs and symptoms observed are those caused by electrolyte depletion (hypokalemia, hypochloremia, hyponatremia) and dehydration resulting from excessive diuresis. If digitalis has also been administered, hypokalemia may accentuate cardiac arrhythmias. The oral LD50 of hydrochlorothiazide is greater than 10 g/kg in the mouse and rat.
Active Ingredient/Synonyms
HCTZ | Hydrochlorothiazide |
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.