Telsartan, tablets 40 mg 30 pcs

Pharmacodynamics

Telmisartan is a specific angiotensin II receptor antagonist (ARA) type AT1, effective when taken orally. It has high affinity for the AT1 subtype of angiotensin II receptors, through which angiotensin II action is realized. It displaces angiotensin II from binding to the receptor, having no agonist effect against this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptor.

Binding is long lasting. It has no affinity for other receptors, including AT2 receptor and other less studied angiotensin receptors. The functional significance of these receptors and the effect of their possible overstimulation by angiotensin II, the concentration of which increases with telmisartan administration, have not been studied. It reduces the blood concentration of aldosterone, does not inhibit plasma renin and does not block ion channels. Telmisartan does not inhibit angiotensin-converting enzyme (kininase II), which also degrades bradykinin. Therefore, an increase in bradykinin-induced side effects is not expected.

In patients with arterial hypertension, telmisartan at a dose of 80 mg completely blocks the hypertensive effects of angiotensin II. Initiation of antihypertensive action is observed within 3 hours after the first oral administration of telmisartan. The drug action lasts for 24 hours and remains significant up to 48 hours.

Distinct antihypertensive effect usually develops in 4 weeks after regular drug intake.
In patients with arterial hypertension telmisartan reduces systolic and diastolic blood pressure (BP) without affecting heart rate (HR).

In the case of abrupt telmisartan withdrawal, BP gradually returns to baseline levels without the development of “withdrawal” syndrome.

Pharmacokinetics

absorption

When taken orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 50%. When taken concomitantly with food, the area under the pharmacokinetic curve “concentration-time” (AUC) decreases from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). Three hours after intake, plasma concentrations level off regardless of food intake.

Distribution

The binding to plasma proteins is 99.5% (mainly to albumin and alpha-1 glycoprotein). The average apparent volume of distribution at equilibrium concentration is 500 liters.

Metabolism

Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive.

Elimation

The half-life (T1/2) is more than 20 hours. Excreted intestinally unchanged, renal excretion – less than 2% of the dose taken. Total plasma clearance is high (900 ml/min) compared to “hepatic blood flow” (about 1500 ml/min).

Pharmacokinetics in special patient groups

Gender differences

There is a difference in plasma concentrations of telmisartan in men and women. Maximum plasma concentration (Cmax) is approximately 3 times and AUC approximately 2 times higher in women compared to men with no significant effect on efficacy. No dosage adjustment is required.

Elderly patients

Telmisartan pharmacokinetics in elderly patients does not differ from that in younger patients. No dose adjustment is required.

Patients with impaired renal function

In patients with mild to moderate impaired renal function no dose adjustment of telmisartan is required.
Patients with severe renal impairment and patients on hemodialysis are recommended a lower starting dose of 20 mg per day.

Telmisartan is not excreted by hemodialysis.

Patients with impaired hepatic function

Pharmacokinetic studies in patients with hepatic impairment have shown increased absolute bioavailability of telmisartan to almost 100%. The T1/2 is unchanged in hepatic insufficiency. In patients with mild to moderate hepatic impairment (Child-Pugh class A and B), the daily dose of the drug should not exceed 40 mg.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Telsartan may increase the hypotensive effect of other antihypertensive agents. Other clinically significant interactions have not been identified.

The co-administration of Telmisartan with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine does not lead to clinically significant interaction. When concomitant use with digoxin an increase of 20% (in a single case by 39%) in mean minimal plasma concentrations of digoxin was observed, therefore plasma levels of digoxin should be monitored.

A 2.5-fold increase in AUC0-24 and Cmax of ramipril and ramiprilat has been observed with concomitant use of telmisartan and ramipril. The clinical significance of this phenomenon has not been established.

There have been reports of reversible increases in serum lithium concentrations and toxicity when lithium is coadministered with angiotensin II receptor antagonists, including telmisartan. In this case, monitoring of plasma lithium levels is recommended and patients should be under close medical supervision.

Concomitant treatment with nonsteroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid, cyclooxygenase-2 [COX-2] inhibitors and non-selective NSAIDs, is associated with the risk of acute renal failure in patients with dehydration.

Drugs acting on the renin-angiotensin system may have a synergistic effect. Patients receiving concomitant NSAIDs and telmisartan should adequately replenish water loss and monitor renal function at the start of treatment.

Some reduction in the antihypertensive effect of telmisartan has been reported when used concomitantly with NSAIDs.

The concomitant treatment of telmisartan with corticosteroid drugs decreases the antihypertensive effect

.

Special Instructions

Contraindications

Side effects

Overdose

The data on overdose in humans is very limited.

Symptoms: The most likely signs of overdose may be hypotension and tachycardia; the development of bradycardia is also not excluded.

Treatment: The recommended treatment is symptomatic. Telmisartan is not removed from the blood by hemodialysis.

Pregnancy use

Similarities