Composition
of 1 tab. | |
telmisartan | 80 mg |
Auxiliary substances:
sodium hydroxide-6.8 mg,
povidone (K-30) – 24 mg,
meglumine-24 mg,
mannitol-330.4 mg,
magnesium stearate-4.8 mg,
talc-10 mg
.10 pcs. – contour cell packages (3) – cardboard packs.
Pharmacological action
Antihypertensive agent, angiotensin II receptor antagonist (type AT 1). It has a very high affinity for this receptor subtype. Telmisartan selectively and permanently binds to receptors and displaces angiotensin II from binding to AT1 receptors. It shows no affinity for other AT receptor subtypes. The functional significance of other receptor subtypes and the effect of elevated (as a result of telmisartan) angiotensin II levels on them is not known. Telmisartan reduces the level of aldosterone in blood plasma, does not inhibit plasma renin, does not block ion channels, does not inhibit ACE (kinase II), which also destroys bradykinin. Therefore, there are no side effects associated with bradykinin.
Indications
Arterial hypertension.
Recommendations for use
For adults, the daily dose is 20-40 mg (1 time/day). In some patients, a hypotensive effect can be achieved at a dose of 20 mg / day. If necessary, the dose can be increased to 80 mg / day.
Patients with impaired renal function, as well as elderly patients, do not need to adjust the dose.
For patients with impaired liver function, the daily dose is 40 mg.
Contraindications
Biliary tract obstruction, severe hepatic and renal dysfunction, pregnancy, lactation (breast-feeding), hypersensitivity to telmisartan.
Side effects
From the central nervous system: Â headache, dizziness, fatigue, insomnia, anxiety, depression, seizures.
From the digestive system: Â abdominal pain, dyspepsia, nausea, diarrhea, increased activity of hepatic transaminases.
Respiratory system disorders: Â cough, pharyngitis, upper respiratory tract infections.
From the hematopoietic system: Â reduced hemoglobin levels.
Allergic reactions: Â rash; in a single case – angioedema.
From the urinary system: Â peripheral edema, urinary tract infections, increased uric acid levels, hypercreatininemia.
From the cardiovascular system: Â marked decrease in blood pressure, palpitations, chest pain.
Musculoskeletal disorders: Â low back pain, myalgia, arthralgia.
From the side of laboratory parameters: Â hyperkalemia, anemia, hyperuricemia.
Other services: Â flu-like syndrome.
Interaction
When used concomitantly with antihypertensive drugs, it is possible to increase the antihypertensive effect.
When used concomitantly with potassium-sparing diuretics, heparin, dietary supplements, salt substitutes containing potassium, hyperkalemia may develop.
When used concomitantly with lithium preparations, it is possible to increase the concentration of lithium in blood plasma.
With simultaneous use, it is possible to increase the concentration of digoxin in blood plasma.
Description
Tablets are white or almost white in color, round, flat-cylindrical, with a chamfer and risk.
Functional features
When taken orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is 50%. When taken simultaneously with food, the decrease in AUC ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg).3 hours after ingestion, the plasma concentration is equalized, regardless of whether it is taken with food or on an empty stomach.
Binding to plasma proteins is 99.5%. The average apparent Vd atthe equilibrium stage is 500 liters. It is metabolized by conjugation with glucuronic acid. The metabolites are pharmacologically inactive.
T1/2 – more than 20 hours. It is excreted unchanged through the intestines. Cumulative renal excretion is less than 1%. Total plasma clearance-1000 ml / min (renal blood flow-1500 ml / min).
Special instructions
telmisartan should be used with caution in patients with impaired liver function, acute gastric and duodenal ulcers, other gastrointestinal diseases, aortic and mitral valve stenosis, obstructive hypertrophic cardiomyopathy, coronary heart disease, and heart failure.
In patients with bilateral renal artery stenosis or renal artery stenosis of a single functioning kidney, the use of telmisartan increases the risk of severe hypotension and renal failure. Therefore, telmisartan should be used with caution in this category of patients.
During the use of telmisartan in patients with impaired renal function, it is necessary to monitor the content of potassium and creatinine in blood plasma.
Currently, there are no data on the use of telmisartan in patients with a recent kidney transplant.
Patients with reduced BCC and/or hyponatremia may experience symptomatic hypotension, especially after the first dose of telmisartan. Therefore, before conducting therapy, correction of such conditions is necessary.
It is not recommended to use telmisartan in patients with primary aldosteronism, since such patients are insensitive to drugs that affect the renin-angiotensin system.
The use of telmisartan is possible in combination with thiazide diuretics, since this combination provides an additional reduction in blood pressure.
When considering increasing the dose of telmisartan, it should be remembered that the maximum antihypertensive effect is usually achieved 4-8 weeks after the start of treatment.
Use in pediatrics
There are no data on the safety and efficacy of telmisartan in children and adolescents.
Influence on the ability to drive motor vehicles and manage mechanisms
The question of the possibility of engaging in potentially dangerous activities that require increased attention and rapid psychomotor reactions should be resolved only after evaluating the individual response to telmisartan.
Active ingredient
Telmisartan
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Description
For adults as directed by your doctor
Indications
Hypertension
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