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Micardis

Micardis
Micardis (Telmisartan) is an angiotensin II receptor blocker (ARB) that is used to treat hypertension.

Brand: Telmisartan

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: March 2024
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Micardis 80 mg
180 pills - 80 mg
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$359.91 $2.00 $156.03 Add to cart
120 pills - 80 mg
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$249.97 $2.08 $93.99 Add to cart
90 pills - 80 mg
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$195.95 $2.18 $62.02 Add to cart
60 pills - 80 mg
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$141.93 $2.37 $30.05 Add to cart
30 pills - 80 mg $85.99 $2.87 No Add to cart
Micardis 40 mg
360 pills - 40 mg
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$555.99 $1.54 $331.89 Add to cart
180 pills - 40 mg
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$295.95 $1.64 $147.99 Add to cart
120 pills - 40 mg
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$205.99 $1.72 $89.97 Add to cart
90 pills - 40 mg
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$163.01 $1.81 $58.96 Add to cart
60 pills - 40 mg
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$119.05 $1.98 $28.93 Add to cart
30 pills - 40 mg $73.99 $2.47 No Add to cart
Micardis 20 mg
360 pills - 20 mg
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$337.95 $0.94 $261.69 Add to cart
180 pills - 20 mg
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$174.93 $0.97 $124.89 Add to cart
120 pills - 20 mg
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$127.95 $1.07 $71.93 Add to cart
90 pills - 20 mg
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$103.99 $1.16 $45.92 Add to cart
60 pills - 20 mg $77.99 $1.30 $21.95 Add to cart
30 pills - 20 mg $49.97 $1.67 No Add to cart

Product description

Drug Title

Micardis (Telmisartan)

Pharmacological action

Antihypertensive drug.


Pharmacodynamics


Telmisartan is a specific angiotensin II receptor antagonist. It has a high affinity for the AT1 subtype of angiotensin II receptors, through which the action of angiotensin II is realized. Telmisartan displaces angiotensin II from binding to the receptor without any agonist effect on this receptor. It binds only to the AT1 subtype of angiotensin II receptor. Binding is prolonged. Telmisartan has no affinity for other receptors (including AT2 receptors) and other less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible overstimulation by angiotensin II, the concentration of which increases when telmisartan is prescribed, has not been studied. It reduces the blood concentration of aldosterone, does not inhibit plasma renin and does not block ion channels. It does not inhibit ACE (kininase II), an enzyme that also degrades bradykinin, so an increase in bradykinin-induced side effects is not expected.


Telmisartan at a dose of 80 mg completely blocks the hypertensive effects of angiotensin II. The onset of hypotensive effect is noted within 3 h after the first telmisartan administration. The action of the drug persists for 24 h and remains significant up to 48 h. A pronounced hypotensive effect usually develops after 4-8 weeks of regular use.


In patients with arterial hypertension, telmisartan reduces systolic and diastolic BP without affecting HR.


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


Pharmacokinetics

Absorption


Telmisartan is rapidly absorbed from the gastrointestinal tract when administered orally. Bioavailability is 50%.


AUC in food use ranges from 6% (in 40 mg dose) to 19% (in 160 mg dose). Three hours after the intake, plasma concentrations level off regardless of the time of ingestion.


Distribution


Binding to plasma proteins is more than 99.5%, mainly to albumin and α1-glycoprotein. Mean apparent Vd in equilibrium is 500 l.


Metabolism


Metabolized by conjugation with glucuronic acid. Metabolites are not pharmacologically active.


Excretion


T1/2 is more than 20 hours. It is excreted unchanged in the intestine, renal excretion is less than 2% of the administered dose. Total plasma clearance is high (900 ml/min) compared to hepatic blood flow (about 1500 ml/min).


Pharmacokinetics in special clinical cases


There is a difference in concentrations in men and women. In women, Cmax and AUC were approximately 3 and 2 times higher, respectively, than in men (with no significant effect on efficacy).


Pharmacokinetics of telmisartan in elderly patients does not differ from pharmacokinetics in younger patients. No dose adjustment is required.


No dose modification is required in patients with renal impairment, including patients on hemodialysis. Telmisartan is not eliminated by hemodialysis.


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.


Basic telmisartan pharmacokinetics in children and adolescents aged 6 to 18 years following telmisartan doses of 1 mg/kg or 2 mg/kg for 4 weeks are generally comparable to those of adults and confirm the non-linearity of telmisartan pharmacokinetics, especially with respect to Cmax.

Contraindications to use

  • Obstructive diseases of the biliary tract;
  • severe liver function abnormalities (class C on the Child-Pugh scale);
  • concomitant use with aliskiren in patients with diabetes mellitus or renal insufficiency (FFR <60 ml/min/1.73 m2);
  • fructose intolerance, glucose/galactose malabsorption syndrome or sucrose/isomaltase deficiency;
  • Under 18 years of age (effectiveness and safety have not been established);
  • pregnancy;
  • Breast-feeding period;
  • hypersensitivity to the active substance or excipients of the drug.

With caution


  • Bilateral stenosis of the renal arteries or stenosis of the artery of the single kidney;
  • Impaired hepatic and/or renal function;
  • Decreased RBC due to previous diuretic therapy, restriction of table salt intake, diarrhea or vomiting;
  • hyponatremia;
  • hyperkalemia;
  • conditions after kidney transplantation (no history of use);
  • chronic heart failure;
  • aortic and mitral valve stenosis;
  • Idiopathic hypertrophic subaortic stenosis;
  • primary aldosteronism (efficacy and safety not established).

Administration during pregnancy and lactation

The use of Mycardis is contraindicated in pregnancy.


The use of angiotensin II receptor antagonists in the first trimester of pregnancy is not recommended, these drugs should not be prescribed during pregnancy. If pregnancy is diagnosed, the use of the drug should be stopped immediately. If necessary, alternative therapy (other classes of hypotensive drugs approved for use in pregnancy) should be prescribed.


Angiotensin II receptor antagonists are contraindicated in II and III trimesters of pregnancy. Preclinical studies of telmisartan showed no teratogenic effects, but fetotoxicity was established. It is known that exposure to angiotensin II receptor antagonists in II and III trimesters of pregnancy causes fetotoxicity in humans (decreased renal function, oligohydramnios, delayed cranial ossification) and neonatal toxicity (renal failure, arterial hypotension, hyperkalemia).


Alternative therapy should be administered to patients planning pregnancy. If treatment with angiotensin II receptor antagonists was administered during the second trimester of pregnancy, an ultrasound examination of the fetal kidneys and skull bones is recommended.


Newborns whose mothers received angiotensin II receptor antagonists should be closely monitored for arterial hypotension.


Therapy with Mycardis is contraindicated during breastfeeding.


Studies of the effect on human fertility have not been conducted.


Administration in liver dysfunction

The drug is contraindicated in patients with biliary tract permeability disorders and marked liver dysfunction (class C of the Child-Pugh system).


In patients with mild to moderate hepatic impairment (class A and B on the Child-Pugh scale), the daily dose should not exceed 40 mg.


Administration in renal dysfunction

Patients with renal failure (including those on hemodialysis) do not need to correct the dose.


The preparation should be used with caution in bilateral renal artery stenosis or stenosis of the artery of the only kidney, renal dysfunction, conditions after kidney transplantation.


Administration in children

The drug is contraindicated in children and adolescents under 18 years old, because data about efficiency and safety in this group of patients are absent.

Indications of the drug Mycardis

arterial hypertension;

reduction of cardiovascular morbidity and mortality in patients aged 55 years and older at high risk of cardiovascular disease.


Dosing regimen

The drug is administered orally, regardless of meals.


In case of arterial hypertension, the recommended initial dose of Mycardis® is 1 tablet. (40 mg) once daily. If therapeutic effect is not achieved, the drug dose may be increased to 80 mg once daily. When deciding to increase the dose, it should be taken into account that the maximum antihypertensive effect is usually achieved within 4-8 weeks after the start of treatment.


To reduce cardiovascular morbidity and mortality, the recommended dose is 1 tablet. (80 mg) once daily. In the initial period of treatment, additional BP adjustment may be required.


Patients with renal failure (including those on hemodialysis) do not require dose adjustment.


The daily dose of this medicine should not exceed 40 mg in patients with mild to moderate liver dysfunction (class A and B according to Child-Pugh scale).


The dosing regimen in elderly patients does not require changes.