Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antihypertensive agent, angiotensin II receptor antagonist (type AT1). Has a very high affinity for this receptor subtype. Selectively and permanently binding to the receptors, telmisartan displaces angiotensin II from the bond with the AT1 receptors. Does not show affinity for other subtypes of AT receptors. The functional significance of other receptor subtypes and the effect of increased (as a result of telmisartan administration) levels of angiotensin II on them is not known. Telmisartan reduces aldosterone levels in blood plasma, does not inhibit blood 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.
PHARMACOKINETICS
When ingested quickly absorbed from the digestive tract. Bioavailability is 50%. When taken concomitantly with food, the decrease in AUC ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). After 3 hours after administration, the concentration in the plasma is equalized, independently, whether it is taken with food or on an empty stomach. The connection with plasma proteins is 99.5%. The average values ​​of the apparent V d in the equilibrium stage are 500 liters. Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive.
T 1/2 - more than 20 hours. It is excreted through intestines in unchanged form. Cumulative renal excretion is less than 1%. The total plasma clearance is 1000 ml / min (renal blood flow - 1500 ml / min).
INDICATIONS
Arterial hypertension.
DOSING MODE
For adults, the daily dose is 20-40 mg (1 time / day). In some patients, the 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 patients of advanced age, do not need dose adjustment.
For patients with impaired liver function, the daily dose is 40 mg.
SIDE EFFECT
From the side of the central nervous system: headache, dizziness, fatigue, insomnia, anxiety, depression, convulsions.
On the part of the digestive system: abdominal pain, indigestion, nausea, diarrhea, increased activity of hepatic transaminases.
On the part of the respiratory system: cough, pharyngitis, upper respiratory tract infections.
From the hemopoietic system: a decrease in the level of hemoglobin.
Allergic reactions: rash; in a single case - angioedema.
On the part of the urinary system: peripheral edema, urinary tract infection, increased uric acid, hypercreatininaemia.
From the cardiovascular system: a marked decrease in blood pressure, palpitations, and chest pain.
From the musculoskeletal system: pain in the lower back, myalgia, arthralgia.
On the part of laboratory indicators: hyperkalemia, anemia, hyperuricemia.
Other: influenza-like syndrome.
CONTRAINDICATIONS
Obstruction of bile ducts, severe violations of liver and kidney function, pregnancy, lactation (breastfeeding), hypersensitivity to telmisartan.
PREGNANCY AND LACTATION
Telmisartan is contraindicated in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal dysfunction.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.
APPLICATION FOR CHILDREN
Data on the safety and efficacy of telmisartan in children and adolescents are not available.
APPLICATION IN ELDERLY PATIENTS
Older patients are not required to adjust the dose.
SPECIAL INSTRUCTIONS
Cautiously used telmisartan for violations of liver function, peptic ulcer of the stomach and duodenal ulcer in the acute stage, other gastrointestinal diseases, stenosis of the aorta and mitral valve, obstructive hypertrophic cardiomyopathy, coronary heart disease, 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 arterial hypotension and renal failure. Therefore, caution should be used telmisartan in this category of patients.
In the period of using telmisartan in patients with impaired renal function, it is necessary to control the content of potassium and creatinine in the blood plasma.
Currently, there is no data on the use of telmisartan in patients with a recent kidney transplant.
In patients with reduced BCC and / or hyponatremia, symptomatic arterial hypotension may occur, especially after taking the first dose of telmisartan. Therefore, before the treatment, correction of such conditions is necessary.
It is not recommended to use telmisartan in patients with primary aldosteronism. such patients are insensitive to drugs that have an effect on the renin-angiotensin system.
The use of telmisartan is possible in combination with thiazide diuretics. a similar combination provides an additional reduction in blood pressure.
When considering the possibility of increasing the dose of telmisartan, remember that the maximum hypotensive effect is usually achieved in 4-8 weeks after the start of treatment.
Use in Pediatrics
Data on the safety and efficacy of telmisartan in children and adolescents are not available.
Impact on the ability to drive vehicles and manage mechanisms
The question of the possibility of practicing potentially hazardous activities requiring increased attention and rapid psychomotor reactions should be addressed only after evaluating the individual response to telmisartan.
DRUG INTERACTION
With simultaneous use with antihypertensive drugs may increase the antihypertensive effect.
With simultaneous application with potassium-sparing diuretics, heparin, biologically active additives, salt substitutes containing potassium, it is possible to develop hyperkalemia.
With simultaneous use with lithium preparations, an increase in the concentration of lithium in the blood plasma is possible.
With simultaneous use, an increase in the concentration of digoxin in the blood plasma is possible.
