Exforge, pills 5mg+80mg, 28pcs

Composition

Active ingredients:

Amlodipine,

valsartanmedical substances:

microcrystalline cellulose,

crospovidone, magnesium stearate,

colloidal silicon dioxide,

hypromellose (hydroxypropylmethylcellulose),

titanium dioxide (E 171),

yellow iron oxide (E 172),

macrogol 4000 (polyethylene glycol 4000),

talc.

Pharmacological action

Exforge is a combined antihypertensive drug containing active substances with a complementary mechanism for controlling blood pressure. Amlodipine, a dihydropyridine derivative, belongs to the class of slow calcium channel blockers (BMCC), valsartan – to the class of angiotensin II receptor antagonists. The combination of these components has a mutually complementary antihypertensive effect, which leads to a more pronounced decrease in blood pressure compared to that on the background of monotherapy with each drug. Amlodipinamlodipine, which is part of Exforge, inhibits the transmembrane supply of calcium ions to cardiomyocytes and vascular smooth muscle cells. The mechanism of antihypertensive action of amlodipine is associated with a direct relaxing effect on vascular smooth muscles, causing a decrease in OPSS and a decrease in blood pressure. After taking therapeutic doses in patients with arterial hypertension, amlodipine causes vasodilation, leading to a decrease in blood pressure (in the supine and standing position of the patient). A decrease in blood pressure is not accompanied by a significant change in heart rate and catecholamine levels with prolonged use. The concentration of the drug in blood plasma correlates with the clinical effect in both young and elderly patients. In hypertensive patients with normal renal function, amlodipine in therapeutic doses leads to a decrease in renal vascular resistance, an increase in glomerular filtration rate and effective renal plasma blood flow without changing the filtration fraction and level of proteinuria. As with other BMCs, taking amlodipine in patients with normal left ventricular function caused changes in the hemodynamic parameters of heart function at rest and during exercise: a slight increase in the cardiac index was noted without significant influence on the maximum rate of increase in LV pressure, end-diastolic pressure and LV volume. Hemodynamic studies in intact animals and humans have shown that lowering blood pressure under the influence of amlodipine in the therapeutic dose range is not accompanied by a negative inotropic effect, even when used simultaneously with beta-blockers. Amlodipine does not alter sinoatrial node function or AV conduction in intact animals or humans. When using amlodipine in combination with beta-blockers in patients with arterial hypertension or angina, a decrease in blood pressure is not accompanied by undesirable changes in ECG parameters. The clinical efficacy of amlodipine has been demonstrated in patients with chronic stable angina, vasospastic angina and angiographically confirmed coronary artery disease. Valsartan Valsartan is an active and specific angiotensin II receptor antagonist intended for oral use. It acts selectively on AT1 subtype receptors, which are responsible for the known effects of angiotensin II. An increase in the plasma concentration of free angiotensin II due to AT1-receptor blockade under the influence of valsartan can stimulate unblocked AT2-receptors, which counteract the effects of AT1-receptor stimulation. Valsartan does not have any pronounced agonistic activity against AT1 receptors. The affinity of valsartan for the AT 1 subtype receptors is approximately 20,000 times higher than for the AT 2 subtype receptors. Valsartan does not inhibit ACE, also known as kininase II, which converts angiotensin I to angiotensin II and causes the breakdown of bradykinin. T. k. when using angiotensin II antagonists, ACE inhibition does not occur and the accumulation of bradykinin or substance P, the development of dry cough is unlikely. In comparative clinical trials of valsartan with an ACE inhibitor, the incidence of dry cough was significantly lower (p In a clinical study that included patients who had previously developed a dry cough during treatment with an ACE inhibitor, this complication was noted in 19.5% of cases when treated with valsartan, and in 19% of cases when treated with a thiazide diuretic. At the same time, in the group of patients treated with an ACE inhibitor, cough was observed in 68.5% of cases (pWhen treating patients with arterial hypertension with valsartan, there is a decrease in blood pressure, not accompanied by a change in heart rate. The antihypertensive effect is manifested within 2 hours in most patients after a single dose of the drug. The maximum decrease in blood pressure develops in 4-6 hours. After taking the drug, the duration of the antihypertensive effect persists for more than 24 hours. With repeated use, the maximum reduction in blood pressure, regardless of the dose taken, is usually achieved within 2-4 weeks. and it is maintained at the achieved level during long-term therapy. Abrupt discontinuation of valsartan is not accompanied by a sharp increase in blood pressure or other undesirable clinical consequences. The use of valsartan in patients with chronic heart failure (NYHA class II-IV) leads to a significant reduction in the number of hospitalizations. This effect is most pronounced in patients who do not receive ACE inhibitors or beta-blockers. When taking valsartan in patients with left ventricular insufficiency (stable clinical course) or with impaired LV function after a myocardial infarction, a decrease in cardiovascular mortality is noted. Amlodipine/Valsartan in hypertensive patients treated with Exforge 1 time / day, the antihypertensive effect was maintained for 24 hours. Exforge at a dose of 10/160 mg normalizes blood pressure (a decrease in diastolic blood pressure in a sitting position of less than 90 mm Hg at the end of the study) in 62% of patients with inadequate blood pressure control on the background of monotherapy with valsartan at a dose of 160 mg / day. Exforge at a dose of 10/160 mg normalizes blood pressure in 78% of patients with inadequate blood pressure control on the background of monotherapy with amlodipine at a dose of 10 mg. In patients with arterial hypertension, the combination of valsartan 160 mg with amlodipine 10 mg resulted in an additional reduction in systolic and diastolic blood pressure by 6.0 mm Hg and 3.9 mm Hg, respectively, compared to patients who continued to receive only valsartan 160 mg or only amlodipine 10 mg. When titrating the Exforge dose from 5/160 mg to 10/160 mg in hypertensive patients with diastolic blood pressure > 110 mm Hg and less than 120 mm Hg, there is a decrease in blood pressure in the sitting position by 36/29 mm Hg, comparable to the decrease in blood pressure when titrating the dose of a combination of an ACE inhibitor and a thiazide diuretic. In two long-term studies with a long follow-up period, the Exforge effect persisted for 1 year. Sudden discontinuation of Exforge is not accompanied by a sharp increase in blood pressure. In patients who achieved adequate blood pressure control, but developed severe edema on the background of amlodipine monotherapy, when using combination therapy, comparable blood pressure control was achieved with a lower probability of edema development. The therapeutic effectiveness of Exforge does not depend on the age, gender and race of the patient.

Indications

Arterial hypertension (for patients who are indicated for combination therapy).

Use during pregnancy and lactation

Exforge, like any other drug that has a direct effect on the renin-angiotensin-aldosterone system (RAAS), should not be prescribed during pregnancy and women who want to become pregnant. If pregnancy is detected during Exforge treatment, the drug should be discontinued as soon as possible. Patients of childbearing age should be informed about the possible risk to the fetus associated with the use of drugs that affect the RAAS. Given the mechanism of action of angiotensin II receptor antagonists, the risk to the fetus cannot be excluded. It is known that the use of ACE inhibitors that affect the RAAS to pregnant women in the second and third trimesters leads to damage or death of the developing fetus. According to a retrospective analysis, the use of ACE inhibitors in the first trimester of pregnancy was accompanied by the development of fetal and newborn pathology. Cases of spontaneous abortions, lack of water supply, and impaired renal function in newborns have been reported with unintentional use of valsartan in pregnant women. It is not known whether valsartan and/or amlodipine are excreted in breast milk. Since the isolation of valsartan in breast milk has been noted in experimental studies, Exforge is not recommended to be used during lactation (breastfeeding).

Contraindications

Pregnancy. Hypersensitivity to the components of the drug. The safety of using Exforge is not established for the following categories: : Patients with unilateral or bilateral renal artery stenosis or stenosis of the artery of a single kidney. Patients after a recent kidney transplant. Children and teenagers under 18 years of age. With caution: Disorders of liver function (especially in obstructive diseases of the biliary tract). Severe renal impairment ( creatinine clearance Mitral or aortic stenosis. Hypertrophic obstructive cardiomyopathy. Hyperkalemia. Lack of sodium in the body and/or a decrease in BCC.

Side effects

Respiratory system disorders:  often-nasopharyngitis, flu; sometimes-cough, pain in the pharynx and larynx.

From the side of the senses: rarely-visual disturbances, tinnitus; sometimes-dizziness associated with impaired function of the vestibular apparatus.

From the central nervous system and peripheral nervous system: often – headache; sometimes-dizziness, drowsiness, orthostatic vertigo, paresthesia; rarely-anxiety.

From the cardiovascular system: sometimes-tachycardia, palpitation, orthostatic hypotension; rarely-syncopal state, marked decrease in blood pressure.

From the digestive system: sometimes – diarrhea, nausea, abdominal pain, constipation, dry mouth.

Dermatological reactions: sometimes-skin rash, erythema; rarely-hyperhidrosis, exanthema, pruritus.

Musculoskeletal disorders: sometimes-swelling of the joints, back pain, arthralgia; rarely-muscle spasms, a feeling of heaviness throughout the body.

From the urinary system: rarely-pollakiuria, polyuria.

From the side of the reproductive system: rarely-erectile dysfunction.

Other services: often-pastyness, facial edema, peripheral edema, increased fatigue, flushes of blood to the face, asthenia, a feeling of heat.

Interaction

Amlodipine: No clinically significant interactions with thiazide diuretics, beta-blockers, ACE inhibitors, long-acting nitrates, sublingual nitroglycerin, digoxin, warfarin, atorvastatin, sildenafil, maalox (aluminum hydroxide gel, magnesium hydroxide, simethicone ), cimetidine, NSAIDs, antibiotics, etc. have been observed with amlodipine monotherapy. oral hypoglycemic medications. Valsartan Monotherapy with valsartan was found to have no clinically significant interaction with the following drugs: cimetidine, warfarin, furosemide, digoxin, atenolol, Indometacin, hydrochlorothiazide, amlodipine, glibenclamide. When used concomitantly with dietary supplements containing potassium, potassium-sparing diuretics, potassium-containing salt substitutes, or with other drugs that may cause an increase in the concentration of potassium in the blood (for example, with heparin), care should be taken and frequent monitoring of the concentration of potassium in the blood should be carried out.

How to take, course of use and dosage

The drug should be taken orally, washed down with a small amount of water,1 time / day, regardless of the time of food intake. The recommended daily dose is 1 tablet. When prescribing to elderly patients, patients with initial or moderate renal impairment (creatinine clearance > 30 ml / min), with impaired liver function or with liver diseases, with cholestasis, no dosage changes are required.

Overdose

Symptoms: There are currently no data on overdose cases. With an overdose of valsartan, you can expect the development of a pronounced decrease in blood pressure and dizziness.

Overdose of amlodipine can lead to excessive peripheral vasodilation and possible reflex tachycardia. Severe and prolonged systemic hypotension, up to fatal shock, has also been reported.

Treatment: in case of accidental overdose, you should induce vomiting (if the drug was taken recently) or perform gastric lavage, prescribe activated charcoal. The use of activated charcoal in healthy volunteers immediately or 2 hours after taking amlodipine significantly reduced its absorption.

In case of clinically expressed hypotension caused by Exforge, the patient should be placed with raised legs, take active measures to maintain the activity of the cardiovascular system, including frequent monitoring of the function of the heart and respiratory system, BCC and the amount of urine released.

In the absence of contraindications, a vasoconstrictor may be used (with caution) to restore vascular tone and blood pressure. Intravenous use of calcium gluconate may be effective in eliminating calcium channel blockage. Elimination of valsartan and amlodipine during hemodialysis is unlikely.

Special instructions

Caution should be exercised when prescribing Exforge to patients with liver disease (especially obstructive biliary tract diseases). Valsartan is mainly excreted unchanged in the bile, while amlodipine is extensively metabolized in the liver.

Patients with initial and moderate renal impairment (creatinine clearance 30-50 ml/min) do not need to adjust the dose of Exforge. Caution should be exercised when prescribing the drug to patients with severe renal impairment (CC) As well as when using other vasodilators, special care should be taken when prescribing the drug to patients with mitral or aortic stenosis, hypertrophic obstructive cardiomyopathy.

If it is necessary to cancel beta-blockers before starting Exforge therapy, the dose of beta-blockers should be reduced gradually. Since amlodipine is not a beta-blocker, the use of Exforge does not prevent the development of withdrawal syndrome that occurs when treatment with beta-blockers is abruptly discontinued.

In placebo-controlled studies, patients with uncomplicated arterial hypertension experienced severe hypotension in 0.4% of cases. In patients with activated RAAS (for example, with BCC and/or sodium deficiency in patients receiving high doses of diuretics), when taking angiotensin receptor blockers, symptomatic hypotension may develop. Before starting treatment with Exforge, the body’s sodium content and/or BCC should be corrected, or therapy should be initiated under close medical supervision.

If arterial hypotension develops, the patient should be placed with raised legs, if necessary, an intravenous infusion of saline solution should be performed. After blood pressure stabilizes, treatment with Exforge can be continued.

When using the drug concomitantly with dietary supplements containing potassium, potassium-sparing diuretics, potassium-containing salt substitutes, or with other drugs that may cause an increase in the concentration of potassium in the blood (for example, with heparin), care should be taken and regular monitoring of the concentration of potassium in the blood should be carried out.

Influence on the ability to drive motor vehicles and manage mechanisms

There are no data on the effect of the drug on the ability to drive vehicles and work with mechanisms. Due to the possible occurrence of dizziness or increased fatigue, care should be taken when driving vehicles or working with mechanisms.

Form of production

Pills.

Storage conditions

In a dry place, at a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Amlodipine, Valsartan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension