Pharmacodynamics and pharmacokinetics
Pharmacodynamics
Micardis Plus is a combination of telmisartan angiotensin type II receptor blocker hydrochlorothiazide ( diuretic ). The combined use of these components causes a stronger antihypertensive effect than using them separately. Taking the drug once a day leads to a pronounced gradual decrease in blood pressure.
Telmisartan is a selective angiotensin type 2 receptor blocker. Has high affinity for angiotensin II receptors of the AT1 subtype . It displaces angiotensin II from the receptor. The binding is long-term. Telmisartan does not block other receptors (including AT2 type receptors) of angiotensin . Telmisartan also reduces aldosterone .
In persons with arterial hypertension 80 mg of telmisartan per day completely suppresses the effects of angiotensin II . The onset of action occurs three hours after ingestion of the drug. The effect lasts for 24 hours. A permanent antihypertensive effect is observed a month after regular use of telmisartan .
Hydrochlorothiazide is diuretic . Affects the reabsorption of electrolytes in the renal tubules, directly increasing the excretion of sodium and chlorides. This causes a decrease in circulating blood volume, an increase in renin aldosterone synthesis .
After administration of hydrochlorothiazide, diuresis increases after two hours, and the maximum effect is achieved after four hours and persists for 6-12 hours.
Pharmacokinetics
Telmisartan. Quickly absorbed from the digestive tract. The maximum concentration of telmisartan occurs within an hour. Bioavailability is 50%.
Reaction with blood proteins is more than 99.5%. Metabolized by interaction with glucuronic acid . Telmisartan derivatives are pharmacologically inactive.
The half-life is approximately 20 hours. Excreted with feces in its original form and with the kidneys - up to 2%.
The pharmacokinetics of telmisartan in elderly patients does not differ from those in younger patients. No dose selection is required.
Hydrochlorothiazide. After oral administration of hydrochlorothiazide, maximum concentrations are achieved within 1-2 hours. Bioavailability reaches 60%.
Reaction with plasma proteins – 64%. It is not metabolized and is excreted unchanged through the kidneys.
pharmachologic effect
Manufacturer: Boehringer Ingelheim, Germany
Release form: tablets
Active ingredient: telmisartan
Synonyms: Telsartan, Telzap, Telmista, Telpres, Telmisartan
Mikardis consists of the synthetic substance telmisartan. Its action is to block certain receptors and eliminate their vasoconstrictive effect. Thus, systemic blood pressure and the level of aldosterone (a hormone that retains water in the body) in the blood decrease. The therapeutic effect lasts for 24 hours.
Belongs to the pharmacological group of angiotensin II receptor antagonists.
Contraindications
The drug has the following contraindications:
- obstruction of the biliary tract;
- severe liver or kidney dysfunction;
- refractory hypercalcemia, hypokalemia ;
- fructose intolerance ;
- lactase deficiency galactose or lactose intolerance ;
- age less than 18 years;
- lactation;
- pregnancy;
- allergy to the components of the drug.
Carefully:
- stenosis of both renal arteries, severe kidney damage;
- liver dysfunction or progressive liver damage;
- hyperkalemia;
- hypovolemia after treatment with diuretics , as well as after limiting salt intake, vomiting or diarrhea ;
- chronic heart failure , functional class III-IV;
- mitral and aortic valve ;
- condition after kidney transplant;
- obstructive cardiomyopathy;
- primary aldosteronism ;
- diabetes;
- gout.
Side effects
- From the respiratory system: shortness of breath, respiratory distress syndrome .
- From the circulatory system: tachycardia , arrhythmias , bradycardia , severe decrease in blood pressure.
- From the nervous system: fainting, paresthesia , dizziness, insomnia , anxiety, depression , excitability, headache.
- From the digestive system: flatulence, diarrhea, dry mouth, abdominal pain, constipation, gastritis, hypercholesterolemia, hyperglycemia, pancreatitis, jaundice, dyspepsia.
- Skin: sweating.
- From the musculoskeletal system: muscle spasms, arthralgia , myalgia , arthrosis , chest pain.
- From the hematopoietic system: leukopenia, eosinophilia, anemia, neutropenia, thrombocytopenia, thrombocytopenia.
- From the genitourinary system: renal failure, nephritis, glucosuria.
- From the eyes: visual impairment, glaucoma, xanthopsia, acute myopia .
- Infections: sepsis , respiratory tract infections ( pharyngitis, bronchitis, sinusitis ), inflammation of the salivary glands.
- Metabolic disorders: increased creatinine, liver enzymes, creatine phosphokinase, uric acid in the blood, hypertriglyceridemia, hyperkalemia, hypokalemia, hypoglycemia, hyponatremia, decreased hemoglobin .
- Allergic reactions : skin itching, angioedema , rash, erythema , anaphylactic reactions , eczema, systemic vasculitis, necrotizing vasculitis .
MicardisPlus tablets 40 mg+12.5 mg 28 pcs.
TELMISARTAN. With simultaneous use of telmisartan with: - other antihypertensive drugs: the antihypertensive effect may be enhanced. In one study, with the combined use of telmisartan and ramipril, an increase in AUC0-24 and Cmax of ramipril and ramiprilat was observed by 2.5 times. The clinical significance of this interaction has not been established. In the analysis of adverse events leading to discontinuation of treatment and the analysis of serious adverse events obtained during the clinical trial, it was found that cough and angioedema were observed more often during therapy with ramipril, while arterial hypotension occurred more often during therapy with telmisartan. Cases of hyperkalemia, renal failure, arterial hypotension and syncope were observed significantly more often with the combined use of telmisartan and ramipril; - lithium preparations: a reversible increase in the concentration of lithium in the blood was observed, accompanied by toxic effects when taking ACE inhibitors. In rare cases, such changes have been reported with the administration of angiotensin II receptor antagonists, in particular telmisartan. When prescribing lithium drugs and angiotensin II receptor antagonists simultaneously, it is recommended to determine the lithium content in the blood; - non-steroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid in doses used as an anti-inflammatory agent, cyclooxygenase-2 (COX-2) inhibitors and non-selective NSAIDs, can cause the development of acute renal failure in patients with reduced BCC. Drugs that affect the RAAS may have a synergistic effect. In patients receiving NSAIDs and telmisartan, blood volume should be compensated and renal function monitored at the beginning of treatment. A decrease in the effect of antihypertensive agents, such as telmisartan, through inhibition of the vasodilatory effect of prostaglandins has been observed when combined with NSAIDs. When telmisartan was taken simultaneously with ibuprofen or paracetamol, no clinically significant effect was observed; - digoxin, warfarin, hydrochlorothiazide, glibenclamide, simvastatin and amlodipine: no clinically significant interaction was detected. There was an increase in the average concentration of digoxin in the blood plasma by an average of 20% (in one case by 39%). When telmisartan and digoxin are prescribed simultaneously, it is advisable to periodically determine the concentration of digoxin in the blood; - aliskiren, aliskiren-containing drugs: clinical data have shown that dual blockade of the RAAS through combined use with ACE inhibitors, angiotensin II receptor blockers or aliskiren is associated with a high incidence of side effects such as hypotension, hyperkalemia, decreased renal function (including acute renal failure ) compared to the use of a single active RAAS blocker. HYDROCHLOROTHIAZIDE. When used simultaneously with: - ethanol, barbiturates or narcotic analgesics: risk of orthostatic hypotension; - hypoglycemic agents for oral administration and insulin: dose adjustment of hypoglycemic agents for oral administration and insulin may be required; — metformin: risk of developing lactic acidosis; - cholestyramine and colestipol: in the presence of anion exchange resins, the absorption of hydrochlorothiazide is impaired; - cardiac glycosides: risk of hypokalemia or hypomagnesemia caused by thiazide diuretics, development of arrhythmias caused by taking cardiac glycosides; - pressor amines (for example, norepinephrine): the effect of pressor amines may be weakened; - non-depolarizing muscle relaxants (for example, tubocurarine chloride): hydrochlorothiazide may enhance the effect of non-depolarizing muscle relaxants; - antigout drugs: the concentration of uric acid in the blood serum may increase and therefore changes in the dose of uricosuric drugs may be required. The use of thiazide diuretics increases the incidence of hypersensitivity reactions to allopurinol; - calcium supplements and vitamin D: thiazide diuretics can increase the calcium level in the blood serum due to a decrease in its excretion by the kidneys. If you need to use calcium supplements, you should regularly monitor the calcium level in the blood and, if necessary, change the dose of calcium supplements; - beta-blockers and diazoxide: thiazide diuretics may enhance hyperglycemia caused by beta-blockers and diazoxide; - m-anticholinergic blockers (for example, atropine, biperidine): decreased gastrointestinal motility, increased bioavailability of thiazide diuretics; - amantadine: the clearance of amantadine may be reduced by hydrochlorothiazide, which leads to an increase in amantadine plasma concentrations and possible toxicity; - cytotoxic drugs (for example, cyclophosphamide, methotrexate): reducing the renal excretion of cytotoxic drugs and enhancing their myelosuppressive effect; - NSAIDs: combined use with thiazide diuretics can lead to a decrease in diuretic and antihypertensive effect; - drugs that lead to potassium excretion and hypokalemia (for example, diuretics that remove potassium; laxatives; glucocorticosteroids, calcitonin, ACTH (adrenocorticotropic hormone), glycyrrhizic acid (found in licorice root), amphotericin B; carbenoxolone; benzylpenicillin; acetylsalicylic acid derivatives ): increased hypokalemic effect. Hypokalemia caused by hydrochlorothiazide is compensated by the potassium-sparing effect of telmisartan; - theophylline: increased risk of hypokalemia; - amiodarone: simultaneous use with thiazide diuretics may lead to an increased risk of arrhythmias associated with hypokalemia; - potassium-sparing diuretics, potassium preparations, other drugs that can increase the potassium content in the blood serum (for example, heparin) or replacing sodium in table salt with potassium salts can lead to hyperkalemia. Periodic monitoring of the potassium level in the blood plasma is recommended in cases where the drug MICARDISPLUS is prescribed together with drugs that can cause hypokalemia, as well as with drugs that can increase the content of potassium in the blood serum.
Interaction
When using telmisartan with:
- other antihypertensive drugs – it is possible to increase the strength of the antihypertensive effect ;
- lithium preparations – a temporary increase in lithium in the blood is possible;
- non-steroidal anti-inflammatory drugs acute renal failure may occur in patients with a reduced volume of circulating blood;
- digoxin – it is possible to increase the concentration of digoxin in the blood by 20%.
When using hydrochlorothiazide with:
- barbiturates, ethanol or opioid orthostatic hypotension may develop ;
- Metformin – possible development of lactic acidosis ;
- hypoglycemic agents and insulin - dose adjustment of hypoglycemic drugs ;
- cholestyramine and colestipol - possible inhibition of hydrochlorothiazide ;
- non-depolarizing muscle relaxants – their effect may be enhanced;
- cardiac glycosides – possible development of hypokalemia or hypomagnesemia ;
- anti-gout medications – it is possible to increase the level of uric acid in the blood.
- calcium preparations – it is possible to increase the concentration of calcium in the blood due to inhibition of its excretion by the kidneys.
- amantadine – there may be an increased risk of developing undesirable effects of amantadine ;
- m-anticholinergic blockers ( atropine , biperiden ) – possible weakening of intestinal motility, increasing the bioavailability of thiazide diuretics ;
- non-steroidal anti-inflammatory drugs - may weaken the diuretic and antihypertensive effects .
Micardis or Vamloset
Manufacturer: KRKA, Slovenia
Release form: tablets
Active ingredient: amlodipine, valsartan
Synonyms: Exforge
Vamloset is a combination drug that contains two active substances that complement each other’s healing properties. Consequently, its hypotensive effect is enhanced compared to using the drugs separately. Prescribed to patients with arterial hypertension who are indicated for treatment with several drugs.
An analogue of Mikardis is produced in three dosages in packages of 30 tablets. The dosage regimen, like that of Micardis, begins with small doses, gradually increasing to an effective maintenance dose.
Comparing these drugs, it is clear that they differ in composition. The antihypertensive property of the analogue is enhanced by two complementary substances, its cost is cheaper, and the frequency of administration is the same - once a day.
In each case, the doctor selects the appropriate medication.
special instructions
In patients with coronary heart disease, the use of any blood pressure-lowering drug, in case of a strong decrease in pressure, can lead to the development of myocardial or cerebral infarction.
Micardis Plus has a weaker therapeutic effect in people of the Negroid race.
When driving vehicles, you should be aware of the possibility of dizziness and drowsiness after taking the drug.
Analogues of Mikardis Plus
Level 4 ATX code matches:
Diokor
Gizaar
Teveten Plus
Atacand Plus
Co Diovan
Vazar N
Valz N
The following analogues of the drug are known: Atakand Plus , Valzap Plus , Valsacor , Gizaar Forte , Co-Diovan , Teveten Plus and others.
Price Mikardis Plus
In Ukraine, the price of the drug in a dosage of 80 mg/12.5 mg No. 28 averages 450 hryvnia; in Russia, such a package will cost 855-1000 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
ZdravCity
- Mikardis Plus tablets 80 mg + 12.5 mg 28 pcs. Boehringer Ingelheim
RUB 1,142 order
Pharmacy Dialogue
- Mikardis plus tablets 80mg/12.5mg No. 28Boehringer Ingelheim
1102 rub. order
- Mikardis plus (tab. 80 mg/12.5 mg No. 28)Boehringer Ingelheim
RUB 1,119 order
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Micardis - instructions for use
Tablets contain 40 mg or 80 mg of the active ingredient telmisartan. The package contains 14 or 28 tablets, 7 pieces on one blister.
The effective dose of the drug is selected together with the doctor. For some patients, 20 mg of medication per day will be enough, for others, if there is no effect, the dose can be increased to 80 mg or a diuretic can be added. The supporting therapeutic effect is achieved after 1–2 months of use. In patients with severe arterial hypertension, the maximum daily dose can reach 160 mg.
Micardis tablets are taken orally regardless of before or after meals.