TELTAS-80 TABLET 80MG

Telmisartan

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

4'-((1,4'-Dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl)methyl)-(1,1'-biphenyl)-2-carboxylic acid | 4'-((4-Methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl)methyl)-2-biphenylcarboxylic acid | 4'-[(1,4'-Dimethyl-2'propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid | 4'-[(1,7'-Dimethyl-2'-propyl-1H,3'h-2,5'-bibenzimidazol-3'-yl)methyl]biphenyl-2-carboxylic acid | BIBR 277 | Telmisartan | Telmisartan |

Description

Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. Generally, angiotensin II receptor blockers (ARBs) such as telmisartan bind to the angiotensin II type 1 (AT1) receptors with high affinity, causing inhibition of the action of angiotensin II on vascular smooth muscle, ultimately leading to a reduction in arterial blood pressure. Recent studies suggest that telmisartan may also have PPAR-gamma agonistic properties that could potentially confer beneficial metabolic effects.

Indication

Used alone or in combination with other classes of antihypertensives for the treatment of hypertension. Also used in the treatment of diabetic nephropathy in hypertensive patients with type 2 diabetes mellitus, as well as the treatment of congestive heart failure (only in patients who cannot tolerate ACE inhibitors).

Mechanism of Action

Telmisartan interferes with the binding of angiotensin II to the angiotensin II AT1-receptor by binding reversibly and selectively to the receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. Telmisartan does not inhibit the angiotensin converting enzyme, other hormone receptors, or ion channels. Studies also suggest that telmisartan is a partial agonist of PPARγ, which is an established target for antidiabetic drugs. This suggests that telmisartan can improve carbohydrate and lipid metabolism, as well as control insulin resistance without causing the side effects that are associated with full PPARγ activators.

Pharmacodynamics

Telmisartan is an orally active nonpeptide angiotensin II antagonist that acts on the AT1 receptor subtype. It has the highest affinity for the AT1 receptor among commercially available ARBS and has minimal affinity for the AT2 receptor. New studies suggest that telmisartan may also have PPARγ agonistic properties that could potentially confer beneficial metabolic effects, as PPARγ is a nuclear receptor that regulates specific gene transcription, and whose target genes are involved in the regulation of glucose and lipid metabolism, as well as anti-inflammatory responses. This observation is currently being explored in clinical trials. Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Telmisartan works by blocking the vasoconstrictor and aldosterone secretory effects of angiotensin II.

Pharmacokinetics

Absorption:

Absolute bioavailability depends on dosage. Food slightly decreases the bioavailability (a decrease of about 6% is seen when the 40-mg dose is administered with food).

Distribution:

* 500 L

Metabolism:

Minimally metabolized by conjugation to form a pharmacologically inactive acylglucuronide; the glucuronide of the parent compound is the only metabolite that has been identified in human plasma and urine. The cytochrome P450 isoenzymes are not involved in the metabolism of telmisartan.

Elimination:

Following either intravenous or oral administration of 14C-labeled telmisartan, most of the administered dose (>97%) was eliminated unchanged in feces via biliary excretion; only minute amounts were found in the urine (0.91% and 0.49% of total radioactivity, respectively).

Half-life

Bi-exponential decay kinetics with a terminal elimination half-life of approximately 24 hours.

Clearance

* >800 mL/min

Toxicity

Intravenous LD50 in rats is 150-200 mg/kg in males and 200 to 250 mg/kg in females. Acute oral toxicity is low: no deaths and no changes occurred in rats or dogs at 2000 mg/kg, the highest dose tested. Limited data are available with regard to overdosage in humans. The most likely manifestations of overdosage with telmisartan would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation.

References

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

Although best effort has been made to ensure the information provided is correct and updated, users are advised to visit HSA Official website whenever in doubt. Please see Disclaimers.
We welcome all the content error reporting/feedback. Please contact us @ Text Us!

Approval Information

TELTAS-80 TABLET 80MG was registered with Health Science Authority of Singapore by APOTHECA MARKETING PTE LTD. It is marketed with the registration number of SIN15102P with effective from 2016-10-17.

This product contains 80mg of Telmisartan in the form of ORAL TABLET.

The medicine was manufactured by INTAS PHARMACEUTICALS LTD in INDIA

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

Products Containing as Single Ingredient

Drug IDTrade NameActive IngredientsForensic ClassRegistrantStatus
1DEXTROMETHORPHAN LINCTUS 15mg/5mlDextromethorphanP OnlyDRUG HOUSES OF AUSTRALIA PTE LTDActive
22ZENMOLIN SYRUP 2mg/5mlSalbutamolP OnlyDRUG HOUSES OF AUSTRALIA PTE LTDActive
41APO-PROPRANOLOL TABLET 40mgPropranololPOMPHARMAFORTE SINGAPORE PTE LTDActive
42APO-DIAZEPAM TABLET 2mgDiazepamPOMPHARMAFORTE SINGAPORE PTE LTDActive
44APO-DIAZEPAM TABLET 5mgDiazepamPOMPHARMAFORTE SINGAPORE PTE LTDActive
45APO-DIAZEPAM TABLET 10mgDiazepamPOMPHARMAFORTE SINGAPORE PTE LTDActive
46APO-PROPRANOLOL TABLET 10mgPropranololPOMPHARMAFORTE SINGAPORE PTE LTDActive
55APO-ISDN TABLET 10mgIsosorbide DinitratePOMPHARMAFORTE SINGAPORE PTE LTDActive
63DIAPO TABLET 10mgDiazepamPOMBEACONS PHARMACEUTICALS PTE LTDActive
64FURMIDE TABLET 40mgFurosemidePOMBEACONS PHARMACEUTICALS PTE LTDActive

Products Containing as Mixture Ingredient

Drug IDTrade NameActive IngredientsForensic ClassRegistrantStatus
4DIPHENHYDRAMINE EXPECTORANTAmmonium Chloride|Diphenhydramine|Sodium CitrateP OnlyDRUG HOUSES OF AUSTRALIA PTE LTDActive
5DIPHENHYDRAMINE EXPECTORANT PAED.Ammonium Chloride|Diphenhydramine|Sodium CitrateP OnlyDRUG HOUSES OF AUSTRALIA PTE LTDActive
400FAKTU SUPPOSITORYCinchocaine|PolicresulenP OnlyTAKEDA PHARMACEUTICALS (ASIA PACIFIC) PTE LTDActive
407TRIMAXAZOLE TABLETSulfamethoxazole|TrimethoprimPOMBEACONS PHARMACEUTICALS PTE LTDActive
435APO-SULFATRIM TABLETSulfamethoxazole|TrimethoprimPOMPHARMAFORTE SINGAPORE PTE LTDActive
508APO-SULFATRIM PEDIATRIC TABLETSulfamethoxazole|TrimethoprimPOMPHARMAFORTE SINGAPORE PTE LTDActive
526B.S. SUSPENSIONSulfamethoxazole|TrimethoprimPOMAPEX PHARMA MARKETING PTE LTDActive
583CO-TRIMEXAZOLE SUSPENSIONSulfamethoxazole|TrimethoprimPOMBEACONS PHARMACEUTICALS PTE LTDActive
676BANEOCIN OINTMENTBacitracin|NeomycinPOMNOVARTIS (SINGAPORE) PTE LTDActive
678BANEOCIN POWDERBacitracin|NeomycinPOMNOVARTIS (SINGAPORE) PTE LTDActive