Telmisar

Rx                  TELMISAR

                                                                               

COMPOSITION:

Each tablet contains

Telmisartan……..20mg

Telmisartan …….40mg

DESCRIPTION:

TELMISAR(Telmisartan) is chemically designated as (2-(4-{[4-methyl-6-(1-methyl-1H-1,3-benzodiazol-2-yl)-2-propyl-1H-1,3-benzodiazol-1-yl]methyl}phenyl)benzoic acid).

Its molecular formula is C33H30N402 & its molecular weight is 514.62

Telmisartan is a non-peptide angiotensin II receptor antagonist (angiotensin receptor blocker, ARB) used in the management of hypertension.

It is used for hypertension at once daily dosing.

Telmisartan lowers systolic/diastolic blood pressure in patients with hypertension by up to 12/9mm Hg at 40mg once daily, and up to 13/10mm Hg at 80mg once daily.

Like other angiotensin II antagonists, it has low incidence of adverse effects.

Telmisartan gives better 24-hour control of blood pressure than amlodipine and losartan, particularly for the 18 to 24 hour period after dosing when serum levels are lowest and the risk of cardiovascular events is likely to be greatest.

PHARMACODYNAMICS:

Telmisartan is a nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits angiotensin II AT₁ receptor subtype without affecting other systems involved in cardiovascular regulation, with a binding affinity 3000 times greater for AT₁ than AT₂.

Telmisartan blocks the vasoconstriction and aldosteron secretion effect of angiotensin II by selectively blocking the binding of angiotensin II to the AT₁ receptor in many tissues. Its action is therefore independent of the pathways for angiotensin II synthesis.

In patients with hypertension, telmisartan reduces both systolic and diastolic blood pressure without affecting pulse rate.

After the first dose of Telmisartan, the antihypertensive activity gradually becomes evident within 3 hours. The maximum reduction in blood pressure is generally attained 4 to 8 weeks after the start of treatment and is sustained during long term therapy.

The antihypertensive effect of Telmisartan is not influenced by patient’s age, weight or body mass index.

In addition to blocking the RAs, Telmisartan acts as a selective modulator of peroxisome proliferator-activated receptor gamma (PPAR-γ), a central regulator of insulin and glucose metabolism.

It is believed that telmisartan’s dual mode of action may provide protective benefits against the vascular and renal damage caused by diabetes and cardiovascular disease (CVD).

PHARMACOKINETICS:

The oral bioavailability of telmisartan is dose dependent. Administration with food reduces bioavailability of 40 mg dose by 6%, hence Telmisartan may be taken with or without food.

Absorption:

Absorption of telmisartan is rapid although the amount absorbed varies. The mean absolute bioavailability for telmisartan is about 50 %.

When telmisartan is taken with food, the reduction in the area under the plasma concentration-time curve (AUC0-∞) of telmisartan varies from approximately 6 % (40 mg dose) to approximately 19 % (160 mg dose). By 3 hours after administration plasma concentrations are similar whether telmisartan is taken fasting or with food.

Distribution:

Telmisartan is largely bound to plasma protein (> 99.5 %).

Metabolism:

Telmisartan is metabolized by conjugation with Glucuronic acid to form an acylglucuronide of Telmisartan.

The CYP 450 isoenzyme are not responsible for Telmisartan metabolism.

Elimination:

The primary route of elimination of telmisartan and its metabolite is billiary-faceal excretion. More than 90% of 40mg single oral or intravenous dose of [14C] telmisartan was excreted within 120 hrs in healthy male volunteers, while <1% was recovered in urine.

Plasma concentrations were higher in females than in males, without relevant influence on efficacy.

INDICATION;

TELMISAR (Telmisartan) is indicated for the treatment of ;

·         Essential hypertension.

·         Cardiovascular prevention

·         Reduction of cardiovascular morbidity in patients with:

Ø  Manifest atherothrombotic cardiovascular disease (history of coronary heart disease, stroke, or peripheral arterial disease) or

Ø  Type 2 diabetes mellitus with documented target organ damage

CONTRAINDICATION:

TELMISAR is contraindicated in patients who are hypersensitive to any of the component in this product, during second and third trimesters of pregnancy, lactation, and in children. It is also contraindicated in biliary obstructive disorders and severe hepatic impairment.

DRUG INTERACTIONS:

Other antihypertensives: increases risk of hypotension.

NSAID’s: reduces antihypertensive effects of Telmisartan.

Corticosteroids: reduction of antihypertensive effects.

Warfarin: no change in INR value.

Digoxin: increase in digoxin plasma concentration.

Other: no significant interaction with acetaminophen, glyburide, hydrochlorthiazide.

WARNING & PRECAUTIONS:

TELMISAR should not be given to patients with cholestasis, biliary obstructive disorders or severe hepatic impairment. There is risk of hypotension in patients with artery stenosis or single functioning kidney.

In patients with impaired renal function, telmisartan is associated with oliguria or progressive azotemia.

Telmisartan extracts have shown its presence in milk, so nursing mothers need to be cautioned on avoiding its adverse effects in infant.

 Safety on pediatric patients has not yet been established, so special caution is to be followed.

ADVERSE EFFECTS:

Cardiovascular: edema, palpitation, bradycardia.

Nervous : headache, dizziness, insomnia, anxiety.

Gastri-intestinal: diarrhea, dyspepsia, nausea, flatulence, dry mouth, anorexia.

Ocular: visual disturbance (rare).

General effects: fatigue, influenza like symptoms.

DOSE & ADMINISTRATION:

 The effective dose range is 20-80 mg once daily, with the usual starting dose of 40 mg once daily. Some patients may be benefit at a dosage of 20 mg/day. Maximum antihypertensive effect is generally attained at 4 to 8 weeks after start of treatment.

Renal impairment: No dosage adjustment necessary in mild to moderate   impairment, i.e. Creatinine clearance between 30-80 ml/min.

Hepatic impairment: Dose should not exceed 40mg once daily in mild to moderate impairment.

Elderly: No dosage adjustment necessary.

Children: Safety and efficacy of Telmisartan not established.

If dose is missed: should not be double dosed, if dose is missed, same dose should be taken on the following day.

TELMISAR can be administered with other hypertensive agents.

TELMISAR can be administered with or without food.

PRESENTATION:

TELMISAR 20:

TELMISAR 40: