KANARB®PLUS FILM COATED TABLETS 120 MG/12.5 MG

Fimasartan
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.

Active Ingredient / Synonyms

Fimasartan | Fimasartan |

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.

Pharmacodynamics

Fimasartan is a selective angiotensin receptor 1 (AR1) inhibitor [A20319]. It acts to lower blood pressure by inhibiting vasoconstriction

Pharmacokinetics

Absorption:

Tmax is 0.5-1.3 h [A20319].

Distribution:

Not Available

Metabolism:

Not Available

Elimination:

Most is eliminated unchangd in bile with less than 3% in the urine [A20319].

Half-life

The half life of elimination is 7-10 h [A20319].

Clearance

Not Available

Toxicity

Not Available

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

HCTZ | Hydrochlorothiazide |

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.

Pharmacodynamics

Thiazides such as hydrochlorothiazide promote water loss from the body (diuretics). They inhibit Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

Pharmacokinetics

Absorption:

50-60%

Distribution:

Not Available

Metabolism:

Hydrochlorothiazide is not metabolized.

Elimination:

Hydrochlorothiazide is not metabolized but is eliminated rapidly by the kidney. Hydrochlorothiazide crosses the placental but not the blood-brain barrier and is excreted in breast milk.

Half-life

5.6 and 14.8 hours

Clearance

Not Available

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.

References

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

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Approval Information

KANARB®PLUS FILM COATED TABLETS 120 MG/12.5 MG was registered with Health Science Authority of Singapore by ZUELLIG PHARMA PTE LTD. It is marketed with the registration number of SIN15819P with effective from 2019-09-26.

This product contains 120 mg of Fimasartan, and 12.5MG of Hydrochlorothiazide in the form of TABLET, FILM COATED.

The medicine was manufactured by BORYUNG PHARMACEUTICAL CO. in KOREA, and LTD. in REPUBLIC OF

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

ATC Code: C03AA03, C

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