Twynsta pills 5 mg + 80 mg 28 pcs
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Active ingredients
Amlodipine + Telmisartan
Release form
Pills
Composition
1 tab. amlodipine besylate 6.935 mg, which corresponds to the content of amlodipine 5 mg telmisartan 40 mg. Excipients: sodium hydroxide - 3.
Pharmacological effect
Pharmacotherapeutic group: blocker of "slow" calcium channels + angiotensin II receptor antagonist. Combined antihypertensive drug containing two active ingredients with a complementary effect, allowing to control blood pressure in patients with arterial (essential) hypertension: angiotensin II receptor antagonist (telmisartan) and slow calcium channel blocker, dihydropyridine derivative (amlodipine). The combination of these substances has an additive antihypertensive effect, reducing blood pressure to a greater extent than each component separately. The drug Twynsta, taken 1 time / day, leads to an effective and sustained decrease in blood pressure within 24 hours. Telmisartan: Telmisartan is a specific angiotensin II receptor antagonist (type AT1) that is effective when taken orally. It has a high affinity for the AT1 receptor subtype angiotensin II, through which the action of angiotensin II is realized. Displaces angiotensin II from its association with the receptor, not having the action of an agonist on this receptor. Telmisartan binds only to the angiotensin II receptor AT1 subtype. The binding is long lasting. Does not have affinity for other receptors, incl. to the AT2 receptor. Reduces the concentration of aldosterone in the blood, does not inhibit renin in the blood plasma and does not block the ion channels. Telmisartan does not inhibit ACE (kininase II) - an enzyme that also destroys bradykinin, so an increase in side effects caused by bradykinin is not expected. In patients with telmisartan in a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of the antihypertensive effect is noted within 3 hours after the first dose of telmisartan. The effect of the drug lasts for 24 hours and remains significant until 48 hours. A pronounced antihypertensive effect usually develops after 4-8 weeks of regular use. In patients with arterial hypertension, telmisartan reduces systolic and diastolic blood pressure without affecting heart rate.In the case of abrupt cancellation of telmisartan, blood pressure gradually returns to its original level without the development of withdrawal syndrome. Amlodipine: Amlodipine, a dihydropyridine derivative, belongs to the class of slow calcium channel blockers. Inhibits transmembrane entry of calcium ions into cardiomyocytes and vascular smooth muscle cells. The mechanism of antihypertensive action of amlodipine is associated with a direct relaxing effect on vascular smooth muscle cells, which leads to a decrease in peripheral vascular resistance and a decrease in blood pressure. In patients with arterial hypertension, the use of amlodipine 1 time / day provides a clinically significant reduction in blood pressure for 24 hours. Orthostatic hypotension is not characteristic when using amlodipine due to the slow onset of the drug. In patients with arterial hypertension and normal renal function, amlodipine at therapeutic doses resulted in a decrease in renal vascular resistance, an increase in glomerular filtration rate, and effective plasma blood flow in the kidney, without changing filtration or proteinuria. Amlodipine does not cause any metabolic adverse effects or changes in plasma lipid levels, and is therefore suitable for use in patients with bronchial asthma, diabetes mellitus and gout. The use of amlodipine in patients with heart failure is not accompanied by a negative inotropic effect (exercise tolerance does not decrease, the left ventricular ejection fraction does not decrease).
Pharmacokinetics
The speed and extent of absorption of the drug Tvinsta equivalent to the bioavailability of telmisartan and amlodipine when used separately. Telmisartan: Absorption: Ingestion is rapidly absorbed from the gastrointestinal tract. Bioavailability - 50%. When taken simultaneously with food, the decrease in AUC ranges from 6% (when used at a dose of 40 mg) to 19% (when applied at a dose of 160 mg). 3 h after ingestion, the concentration in the blood plasma levels off, regardless of the meal. Cmax in plasma and, to a lesser extent, AUC increase disproportionately to the dose. Distribution: Plasma protein binding is 99.5%, mainly with albumin and alpha1-glycoprotein. The average value of the visible Vd at an equilibrium concentration of 500 l.Data on clinically significant accumulation of telmisartan is not available. Metabolism Metabolized by telmisartan by conjugation with glucuronic acid. Metabolites are pharmacologically inactive. Excretion: T1 / 2 is more than 20 hours. Excreted in unchanged form with faeces, excretion in the urine - less than 2%. Total plasma clearance is high (900 ml / min) compared with hepatic blood flow (about 1500 ml / min). Pharmacokinetics in special clinical situations: There is a difference in plasma concentrations of telmisartan in men and women. Cmax and AUC were approximately 3 and 2 times, respectively, higher in women compared to men without significant effect on efficacy. The pharmacokinetics of telmisartan in elderly patients does not differ from the pharmacokinetics in young patients. Telmisartan binds to plasma proteins and is not removed during hemodialysis in patients with renal insufficiency. Also marked lower concentrations of telmisartan in the blood plasma, T1 / 2 does not change. Pharmacokinetic studies conducted in patients with impaired liver function have shown that the absolute bioavailability of telmisartan increases to almost 100%. T1 / 2 in patients with impaired liver function does not change. Amlodipine: Absorption: After taking amlodipine by mouth in therapeutic doses, Cmax in the blood plasma is reached in 6-12 hours. The absolute bioavailability value ranges from 64% to 80%. Eating does not affect the bioavailability of amlodipine. Distribution: Amlodipine Vd is approximately 21 L / kg. In vitro studies have shown that in patients with arterial hypertension, approximately 97.5% of circulating amlodipine binds to plasma proteins. Stable plasma concentrations are achieved after continuous use of the drug for 7-8 days. Metabolism: Amlodipine is largely (approximately 90%) metabolized in the liver to form inactive metabolites. Withdrawal: The removal of amlodipine from the blood plasma occurs in two phases. T1 / 2 is approximately 30-50 hours. Amlodipine is excreted in the urine both unchanged (10%) and as metabolites (60%). Pharmacokinetics in special clinical situations: Elderly patients tend to reduce the clearance of amlodipine, which leads to an increase in AUC and T1 / 2.The pharmacokinetics of amlodipine in patients with impaired renal function does not change significantly. In patients with hepatic insufficiency, amlodipine clearance decreased, leading to an increase in the AUC value of approximately 40-60%.
Indications
- arterial hypertension (for patients whose blood pressure is not sufficiently controlled by telmisartan or amlodipine in monotherapy) - arterial hypertension (for patients who are shown combination therapy) - patients with arterial hypertension receiving telmisartan and amlodipine in separate pills as a substitute for this therapy.
Contraindications
- obstructive diseases of the biliary tract - severe arterial hypotension - obstruction of the outgoing tract of the left ventricle (including a high degree of aortic stenosis) - hemodynamically unstable heart failure after acute myocardial infarction - severe hepatic failure - shock - intolerance to fructose and syndrome of abnormal heart disease / galactose or sucrase / isomaltase deficiency - pregnancy - breastfeeding period - age up to 18 years (efficacy and safety is not established implications) - hypersensitivity to active ingredients or auxiliary substances - hypersensitivity to other dihydropyridine derivatives. The drug should be administered with caution to patients with: - obstructive biliary tract diseases or hepatic insufficiency - bilateral renal artery stenosis or single kidney artery stenosis - condition after kidney transplantation - reduced BCC and / or hyponatremia - double renin-angiotensin-aldosterone system block - other conditions characterized by RAAS activation - primary aldosteronism - aortic and mitral stenosis, obstructive hypertrophic cardio myopathy - heart failure - hyperkalemia - diabetes mellitus with additional cardiovascular risk (i.e., concomitant coronary artery disease / IHD /) - after 1 month after acute myocardial infarction and unstable stenocardia.
Use during pregnancy and lactation
Special studies of the drug Twynsta during pregnancy and during lactation have not been conducted.The effects associated with the individual components of the drug are described below. Pregnancy Telmisartan The use of angiotensin II receptor antagonists (ARA II) is contraindicated during pregnancy. When diagnosing pregnancy, the drug should be immediately discontinued. If necessary, alternative therapy should be prescribed. It is known that the use of ARA II during the II and III trimesters of pregnancy has a fetotoxic effect (reduced kidney function, oligohydramnios, delayed ossification of the fetal skull), and neonatal toxicity (renal failure, arterial hypotension and hyperkalemia) is also observed. Amlodipine Limited data available on the effects of amlodipine or other calcium receptor antagonists do not indicate the presence of adverse effects on the fetus. However, there is a risk of slowing down the process of childbirth The period of breastfeeding Special studies on the allocation of telmisartan and / or amlodipine with breast milk in women have not been conducted. Animal studies have shown that telmisartan is excreted in milk from lactating animals. Given the possible adverse reactions, the decision to continue breastfeeding or to cancel therapy should be made taking into account its importance to the mother. Studies on the effect on human fertility were not conducted.
Dosage and administration
Adults The drug Twynsta must be taken 1 time / day, inside, regardless of the meal. Twynsta can be administered to patients who receive the same doses of telmisartan and amlodipine as separate pills for ease of therapy and increased adherence to treatment. Twynsta may be prescribed to patients in whom the use of amlodipine alone or one telmisartan does not lead to adequate blood pressure control. Patients taking amlodipine at a dose of 10 mg, in which there are adverse reactions limiting the drug, for example, peripheral edema, can switch to taking Twintta at a dose of 40/5 mg 1 time / day, which will reduce the dose of amlodipine, but not reduce overall expected antihypertensive effect. Treatment of arterial hypertension in a patient may begin with the use of the drug Twynsta in the case when it is assumed that the achievement of BP control with the help of any one drug is unlikely.The usual initial dose of Twynsta is 40/5 mg 1 time per day. Patients who need a more significant reduction in blood pressure can begin taking the drug Twynsta at a dose of 80/5 mg 1 time / day. If, at least after 2 weeks of treatment, an additional reduction in blood pressure is required, the dose of the drug can be gradually increased to a maximum dose of 80/10 mg 1 time / day. Twynsta can be used with other antihypertensive drugs. Renal dysfunction In patients with impaired renal function, including in patients on hemodialysis, no changes in dosing of the drug are required. Amlodipine and telmisartan are not removed from the body during hemodialysis. Liver dysfunction In patients with mild or moderate liver dysfunction, Twynsta should be used with caution. The dose of telmisartan should not exceed 40 mg 1 time / day. Elderly patients Dosage and administration do not require changes. Features of the drug at the first dose or when it is canceled. After the first dose of telmisartan, the hypotensive effect gradually develops during the first 3 hours and the effect of the drug lasts for 24 hours and remains significant until 48 hours. baseline without the development of withdrawal syndrome.
Side effects
1) expected based on the experience of using telmisartan 2) expected based on the experience of using amlodipine 3) expected with simultaneous use of telmisartan and amlodipine Inside the system-organ classes, the following categories are used by the frequency of occurrence of side effects: very often (1/10); often (1/100, less than 1/10); infrequently (1/1000, less than 1/100); rarely (1/10 000, less than 1/1000); very rarely (less than 1/10 000); frequency unknown (cannot be calculated from available data). Systemic organ class Side effect Frequency of infection and invasion Cystitis3) Rarely Urinary tract infections1) Infrequently Upper respiratory tract infections1) Infrequently Sepsis, incl. fatal outcome1) Rarely Psychotic disorders Depression3), anxiety3), insomnia3) Rarely Lability of mood2) confused consciousness2) Frequency unknown Nervous system disorders Vertigo3) Often Drowsiness3) migraine3) headache3)paresthesia3) Infrequently Decrease in sensitivity or resistance to external factors3), impaired taste3), syncope3), tremor3), peripheral neuropathy3) Rarely Immune system disorders Anaphylactic reaction1) Rarely Hypersensitivity1), 2) Rarely1), Unknown frequency1) Disorders of the side organs of vision Violation of vision3) Rarely Violations of the organs of hearing Vertigo3) Infrequently Tinnitus2) Frequency unknown Violations of the cardiovascular system Bradycardia3), palpitations3) Infrequently Tachycardia 1) Infrequently Myocardial infarction2) Rarely Arrhythmia2), ventricular tachycardia2a), atrial fibrillation2) Frequency unknown Severe reduction in AD3), orthostatic hypotension3) Infrequently Disturbances of the respiratory system Cough 3) Infrequent Dyspnea1) 2) N),)))))))))))) Cough 3) Infrequent Dyspnea), 2) n) n) Gastrointestinal disorders Abdominal pain3), diarrhea3), nausea3), flatulence1) Infrequently Vomiting3), dyspepsia3), stomach discomfort1) Rarely Changes in the rhythm of defecation2), pancreatitis2), gastritis2) Frequency unknown liver cuts1) Rarely Hepatitis2), jaundice2) Unknown frequency Increased liver transaminase activity (mainly reflecting cholestasis) 2) Unknown frequency Increased liver enzymes3) Rarely Disorders of the skin and subcutaneous tissue Eczema3), erythema3), rash1), 3) drug rash1), toxic rash1) Rarely Pruritic itch3) Infrequently Angioedema 1), 2) Rarely1), frequency unknown2) Hyperhidrosis1), 2) Infrequent1), frequency unknown2) Krapivnitsa1), 2) Rarely1), frequency unknown2), frequency unknown 2) ), skin discoloration2), multif erythema2), exfoliative dermatitis2), Stevens-Johnson syndrome2), photosensitization reaction2), vasculitis2) Frequency unknown Arthralgia3), back pain3), muscle spasms (cramps and calf muscles) 3), pain) Lower extremity pain3), pain in tendons (symptoms resembling tendonitis) 1) Rarely Disorders of the genitourinary system Nocturia3) Rarely Renal dysfunction, including acute renal failure1), urination disorders2), frequent urination2) Frequency non-weight ectile dysfunction3) Infrequently General disorders Peripheral edema3) Often Asthenia (weakness) 3), pain in the chest3), increased fatigue3), edema3) Infrequently Ailment3), flu-like syndrome1), feeling of a rush of blood to the face3), gingival hypertrophy3)dry oral mucosa3) Rarely Pain2), increase in body mass2), decrease in body weight2), gynecomastia2) Frequency unknown Reactions identified during special studies Increase in uric acid concentration in blood3), increase in creatinine in blood1) and creatine phosphokinase (CPK) 1 ), decrease in hemoglobin1) (anemia, weakness), hypoglycemia (in patients with diabetes mellitus) 1), eosinophilia1) Rarely Leukopenia2), hyperglycemia2) Frequency unknown Hyperkalemia1) Infrequently Thrombocytopenia1), 2) Rarely1) frequency unknown 2) Information on individual components Side effects previously reported with one of the components of the drug (amlodipine or telmisartan) may increase with the use of Twynsta, even if they have not been observed in clinical studies or during the post-marketing period. Additional information regarding the combination of components Peripheral edema, a dose-dependent side effect of amlodipine, was observed in patients who received the combination of telmisartan and amlodipine, less often than in patients who received only amlodipine.
Overdose
Symptoms No overdose cases have been identified. Possible symptoms of overdose consist of symptoms from the individual components of the drug. Telmisartan - a pronounced decrease in blood pressure, tachycardia, possibly bradycardia, dizziness, increased serum creatinine levels, acute renal failure. Amlodipine - excessive peripheral vasodilation and, possibly, reflex tachycardia. There may be severe and probably prolonged systemic hypotension, up to the development of a fatal shock. Treatment Hemodialysis is not effective. Monitoring the patient's condition, therapy should be symptomatic and supportive. In order to counteract the blockade of calcium channels, intravenous administration of calcium gluconate may be useful. Overdose treatment methods can be used, such as induction of vomiting, gastric lavage, the use of activated carbon, transferring the patient to the "supine-lying position" and the introduction of plasma substituting solutions in the case of a pronounced decrease in blood pressure.
Interaction with other drugs
There were no interactions between the two active components that are included in the fixed doses of this drug in clinical studies. Special studies of drug interactions drug Twynsta with other drugs have been conducted. Combination of Active Ingredients With simultaneous use of Twynsta with the preparations listed below, the following information should be taken into account. Other antihypertensive drugs. When used concomitantly with other antihypertensive drugs, the hypotensive effect of the drug Tvinsta may increase. Drugs capable of lowering blood pressure Some drugs, such as baclofen and amifostine, can be expected, due to their pharmacological properties, to increase the hypotensive effect of all antihypertensive drugs, including Tvinsta. In addition, orthostatic hypotension may be enhanced by ethanol, barbiturates, narcotic drugs or antidepressants. Corticosteroids (systemic use) Perhaps a decrease in the hypotensive effect. Telmisartan With simultaneous use of telmisartan with: - other antihypertensive drugs: it is possible to enhance the hypotensive effect. In one study, the combined use of telmisartan and ramipril showed an increase in AUC0-24 and Cmax of ramipril and ramiprilat by a factor of 2.5. The clinical significance of this interaction has not been established. - digoxin, warfarin, hydrochlorothiazide, glibenclamide, simvastatin and amlodipine: no clinically significant interaction was found. An increase in the average concentration of digoxin in the blood plasma was noted on average by 20% (in one case by 39%). With the simultaneous appointment of telmisartan and digoxin, it is advisable to periodically determine the concentration of digoxin in the blood. - lithium preparations: there was a reversible increase in the concentration of lithium in the blood, accompanied by toxic effects when taking ACE inhibitors. In rare cases, such changes have been reported with the appointment of angiotensin II receptor antagonists, in particular, telmisartan. With the simultaneous appointment of lithium preparations and angiotensin II receptor antagonists, it is recommended to determine the content of lithium in the blood.- NSAIDs, including acetylsalicylic acid in doses, used as an anti-inflammatory agent, cyclooxygenase-2 inhibitors (COX-2) and non-selective NSAIDs can cause the development of acute renal failure in patients with reduced BCC. Preparations affecting the activity of the renin-angiotensin system, incl. telmisartan may have a synergistic effect. In patients receiving NSAIDs and telmisartan, at the beginning of treatment, BCC should be compensated and renal function should be monitored. With the simultaneous use of NSAIDs and antihypertensive drugs like telmisartan, a decrease in the antihypertensive effect by inhibiting the vasodilator effect of prostaglandins has been reported. Amlodipine In case of simultaneous use of amlodipine with: - grapefruit and grapefruit juice: simultaneous use of the drug with grapefruit or grapefruit juice is not recommended, since in some patients, as a result of the increased bioavailability of amlodipine, its antihypertensive effects may increase; - inhibitors of CYP3A4 isoenzyme: in a study in elderly patients, diltiazem was shown to inhibit amlodipine metabolism, probably affecting CYP3A4 (amlodipine plasma concentrations increase by about 50% and the effect of amlodipine increases). It is possible that more active inhibitors of CYP3A4 (such as ketoconazole, itraconazole, ritonavir) may increase plasma concentrations of amlodipine more than diltiazem. - inducers of CYP3A4 isoenzyme - anticonvulsant drugs (for example, carbamazepine, phenobarbital, phenytoin, phosphenytoin, primidone), rifampicin, St. John's wort (Hypericum perforatum): combined use can lead to a decrease in the concentrations of amlodipine in the blood plasma. Regular medical surveillance is indicated. During the use of CYP3A4 inducers, as well as after their cancellation, it is recommended (if possible) to change the dose of amlodipine; - The combined use of simvastatin in a dose of 80 mg with amlodipine, regardless of the dose, contributes to an increase in the exposure of simvastatin to 77% compared with simvastatin monotherapy. Therefore, the dose of simvastatin should not exceed 40 mg / day. With simultaneous use of the following drugs, the following information should be taken into account. The safety of combined use of amlodipine with thiazide diuretics, beta-blockers, ACE inhibitors, long-acting nitrates, nitroglycerin (used sublingually), NSAIDs,antibiotics and hypoglycemic agents for oral administration. With simultaneous use of amlodipine and sildenafil, it was shown that each drug had an independent hypotensive effect. Additional information Simultaneous use of 240 ml of grapefruit juice with a single dose of amlodipine 10 mg taken orally in 20 healthy volunteers did not lead to a significant effect on the pharmacokinetic properties of amlodipine. The simultaneous use of amlodipine with cimetidine had no significant effect on the pharmacokinetics of amlodipine. The simultaneous use of amlodipine with atorvastatin, digoxin, warfarin or cyclosporin did not significantly affect the pharmacokinetics or pharmacodynamics of these drugs. Based on the experience of using other drugs that affect the RAAS, simultaneous use of the drug Tvinsta and potassium-sparing diuretics, potassium-containing additives, potassium-containing dietary salt, other drugs that increase the content of potassium in the blood (for example, heparin) can lead to hyperkalemia, therefore this indicator should be monitored in patients. In this regard, their simultaneous use with telmisartan requires caution.
special instructions
The drug should be administered with caution if the patient has the following conditions: - abnormal liver function; - bilateral renal artery stenosis or arterial stenosis of a single kidney, severe renal dysfunction. In some patients, due to the suppression of the RAAS, especially when using a combination of agents acting on this system, renal function is impaired (including acute renal failure). Therefore, therapy, accompanied by a similar double blockade of the RAAS, should be carried out strictly individually and with careful monitoring of renal function (including periodic monitoring of the content of potassium and creatinine in blood serum). In cases of dependence of the vascular tone and kidney function, mainly on the activity of the RAAS (for example, in patients with chronic heart failure or kidney diseases, including stenosis of the renal arteries, or stenosis of the artery of a single kidney), the administration of drugs affecting this system, may be accompanied by the development of acute arterial hypotension, hyperasotemia, oliguria, andin rare cases, acute renal failure; - condition after kidney transplantation (no experience); - reduction of bcc and / or hyponatremia due to prior diuretic therapy, restriction of salt, diarrhea or vomiting; - double blockade of RAAS; - other conditions characterized by RAAS activation; - primary aldosteronism; - Aortic and mitral valve stenosis, idiopathic hypertrophic subaortic stenosis; - heart failure; - hyperkalemia; - hereditary intolerance to fructose; - in patients with diabetes mellitus and additional cardiovascular risk, i.e. Patients with diabetes mellitus and concomitant coronary artery disease (IHD), the risk of fatal myocardial infarction and sudden cardiovascular death may be increased when treated with antihypertensive drugs such as angiotensin II receptor antagonists and ACE inhibitors. In patients with diabetes, IHD may be asymptomatic, as a result of which it cannot be diagnosed. Patients with diabetes should undergo an appropriate diagnosis, for example, an exercise test, for the diagnosis and treatment of coronary artery disease, respectively, before starting treatment with Twist. Other indications Tvinst is less effective in treating patients of the Negroid race (renin activity in the blood is usually reduced in this population). There are no data on the use of the drug Twynsta in patients with unstable angina, in acute myocardial infarction and in the period of one month after the development of myocardial infarction. Impact on the ability to drive motor vehicles and control mechanisms No impact studies on the ability to drive motor vehicles and control mechanisms have been conducted. However, it should be taken into account that during treatment such undesirable effects as syncope, drowsiness or dizziness may occur. Therefore, when driving a vehicle or machinery, care should be taken. If patients experience these sensations, they should avoid performing such potentially dangerous activities as driving a car or operating machinery.