Telmista 80 mg - an antihypertensive drug, a specific antagonist of angiotensin II receptors (type AT1).
1 tablet 80 mg:
Active ingredient: Telmisartan 80.00 mg
Excipients: meglumine, sodium hydroxide, povidone-KZO, lactose monohydrate, sorbitol (E420), magnesium stearate.
Tablets 80 mg: Capsule-shaped, biconvex tablets of white or almost white color.
Telmisartan is a specific angiotensin II receptor antagonist (ARA II) (type AT1), effective when taken orally. It has a high affinity for the AT1 subtype of angiotensin II receptors, through which the action of angiotensin II is realized. Displaces angiotensin II from the connection with the receptor, not possessing the action of an agonist in relation to this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptors. The connection is continuous. It does not have an 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 excessive stimulation with angiotensin II, the concentration of which increases with the use of telmisartan, has not been studied. It reduces the concentration of aldosterone in blood plasma, does not inhibit renin in blood plasma and ns blocks ion channels. Telmisartan does not inhibit the angiotensin converting enzyme (ACE) (kininase II) (an enzyme that also breaks down bradykinin). Therefore, an increase in side effects caused by bradykinin is not expected.
In patients, telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of antihypertensive action is noted within 3 hours after the first administration of telmisartan. The effect of the drug persists for 24 hours and remains significant up to 48 hours. A pronounced antihypertensive effect usually develops after 4-8 weeks of regular administration of telmisartan.
In patients with arterial hypertension, telmisartan lowers systolic and diastolic blood pressure (BP) without affecting heart rate (HR).
In the case of abrupt cancellation of telmisartan, blood pressure gradually returns to its original level without the development of "withdrawal" syndrome.
When taken orally, it is rapidly absorbed from the gastrointestinal tract (GIT). Bioavailability is 50%. The decrease in AUC (area under the concentration-time curve) with the simultaneous use of telmisartan with meals ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after ingestion, the concentration in the blood plasma is leveled, regardless of the time of eating. There is a difference in plasma concentrations in men and women. The maximum concentration (Cmax) in blood plasma and AUC in women compared with men was approximately 3 and 2 times higher, respectively (without a significant effect on effectiveness).
Communication with blood plasma proteins - 99.5%, mainly with albumin and alpha-1 glycoprotein.
The average value of the apparent volume of distribution in equilibrium concentration is 500 liters. It is metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive. The half-life (T1 / 2) is more than 20 hours. It is excreted mainly through the intestine in an unchanged form and by the kidneys - less than 2% of the dose taken. The total plasma clearance is high (900 ml / min), but compared with the "hepatic" blood flow (about 1500 ml / min).
Contraindications in the use of the Telmista drug:
- Hypersensitivity to the active substance or excipients of the drug.
- The period of breastfeeding.
- Obstructive diseases of the biliary tract.
- Severe hepatic impairment (Child-Pugh class C).
- Concomitant use with aliskiren in patients with diabetes mellitus or moderate to severe renal failure (glomerular filtration rate (GFR)
The observed cases of side effects did not correlate with the gender, age or race of the patients.
- Infectious and parasitic diseases: sepsis, including fatal sepsis, urinary tract infections (including cystitis), upper respiratory tract infections.
- Disorders from the blood and lymphatic system: anemia, eosinophilia, thrombocytopenia.
- Immune system disorders: anaphylactic reactions, hypersensitivity (erythema, urticaria, angioedema), eczema, pruritus, skin rash (including drug), angioedema (fatal), hyperhidrosis, toxic skin rash.
- Violations of the nervous system: anxiety, insomnia, depression, fainting, vertigo.
- Disorders of the organ of vision: visual disturbances.
- Violations of the heart: bradycardia, tachycardia.
- Violations of the blood vessels: a marked decrease in blood pressure, orthostatic hypotension.
- Disorders of the respiratory system, chest organs and mediastinum: shortness of breath, cough, interstitial lung disease * (* in the post-marketing period of use, cases of interstitial lung disease have been described, with a temporary relationship with telmisartan. However, there is no causal relationship with the use of telmisartan was established).
- Digestive disorders: abdominal pain, diarrhea, dry oral mucosa, dyspepsia, flatulence, stomach discomfort, vomiting, taste perversion (dysgeusia), impaired liver function / liver disease * (* according to the results of post-marketing observations in the majority cases of impaired liver function / liver disease have been identified in residents of Japan).
- Violations of the musculoskeletal and connective tissue: arthralgia, back pain, muscle spasms (cramps of the calf muscles), pain in the lower extremities, myalgia, pain in the tendons (symptoms similar to the manifestation of tendonitis).
- Disorders from the kidneys and urinary tract: impaired renal function, including acute renal failure.
- General disorders and disorders at the injection site: chest pain, flu-like syndrome, general weakness.
- Laboratory and instrumental data: a decrease in hemoglobin, an increase in the concentration of uric acid, creatinine in blood plasma, an increase in the activity of "liver" enzymes, creatine phosphokinase (CPK) in blood plasma, hyperkalemia, hypoglycemia (in patients with diabetes mellitus).
Interaction with other drugs
Telmisartan may increase the antihypertensive effect of other antihypertensive drugs. Other types of interactions of clinical significance have not been identified.
Concomitant use with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine does not lead to a clinically significant interaction. A marked increase in the average concentration of digoxin in blood plasma by an average of 20% (in one case, by 39%). With the simultaneous use of telmisartan and digoxin, it is advisable to periodically determine the concentration of digoxin in the blood plasma.
Like other drugs acting on the renin-angiotensin-aldosterone system (RAAS), the use of telmisartan can cause hyperkalemia (see section "Special instructions"). The risk may increase in case of simultaneous use with other drugs, which can also provoke the development of hyperkalemia (potassium-containing salt substitutes, potassium-sparing diuretics, ACE inhibitors, ARA II, non-steroidal anti-inflammatory drugs NSAIDs, including selective cyclooxygenase-2 | TsOGG-2 | immunosuppressants cyclosporine or tacrolimus and trimethoprim.
The development of hyperkalemia depends on concomitant risk factors. The risk is also increased in case of simultaneous use of the above combinations. In particular, the risk is especially high when used simultaneously with potassium-sparing diuretics, as well as with potassium-containing salt substitutes. For example, concomitant use with ACE inhibitors or NSAIDs is less risk if strict precautions are taken. ARA II, such as telmisartan, reduce potassium loss during diuretic therapy. The use of potassium-sparing diuretics, for example, spironolactone, eplerenone, triamteren or amiloride, potassium supplements or potassium salt substitutes can lead to a significant increase in serum potassium. The simultaneous use of documented hypokalemia should be used with caution and with regular monitoring of potassium in the blood plasma. With the simultaneous use of telmisartan and ramipril, a 2.5-fold increase in the AUC0-24 and Cmax of ramipril and ramipril was observed. The clinical significance of this phenomenon has not been established. With the simultaneous use of ACE inhibitors and lithium preparations, a reversible increase in plasma lithium content was observed, accompanied by toxic effects. In rare cases, such changes have been reported with ARA II and lithium preparations. With the simultaneous use of lithium and ARA II, it is recommended to determine the content of lithium in blood plasma. Treatment with NSAIDs, including acetylsalicylic acid, COX-2, and non-selective NSAIDs, can cause acute renal failure in dehydrated patients. Drugs acting on RAAS may have a synergistic effect. In patients receiving NSAIDs and telmisartan, bcc must be compensated at the beginning of treatment and renal function monitored. Concomitant use with aliskiren in patients with diabetes mellitus or moderate to severe renal failure (glomerular filtration rate of GFR