Exforge tablets 5 mg + 80 mg, 28 pcs. (amlodipine, Valsartan)

Release form

Tablets.

Packaging

28 pcs

Pharmacological action

Exforge is a combined antihypertensive drug containing active substances with a complementing mechanism of blood pressure control.

Amlodipine, a derivative of dihydropyridine, belongs to the class of slow calcium channel blockers (BMCC), valsartan belongs 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 with that of monotherapy with each drug.

Amlodipine

Amlodipine, part of Exforge, inhibits the transmembrane intake of calcium ions in cardiomyocytes and vascular smooth muscle cells. The mechanism of the antihypertensive effect of amlodipine is associated with a direct relaxing effect on vascular smooth muscle, causing a decrease in OPSS and a decrease in blood pressure.

After administration in therapeutic doses in patients with arterial hypertension, amlodipine causes vasodilation, leading to a decrease in blood pressure (in the patient’s position, lying and standing). 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 plasma correlates with the clinical effect in both young and elderly patients.

With arterial hypertension in patients with normal renal function, amlodipine in therapeutic doses leads to a decrease in renal vascular resistance, increase the glomerular filtration rate and effective plasma renal blood flow without changing the filtration fraction and the level of proteinuria.

As with other BMCC, the administration of amlodipine in patients with normal left ventricular function caused a change in the hemodynamic parameters of cardiac function at rest and during physical activity: a slight increase in the cardiac index was observed without significant effect on the maximum rate of increase in LV pressure, of course, diastolic LV pressure and volume. Hemodynamic studies in intact animals and humans have shown that a decrease in blood pressure under the influence of amlodipine in the range of therapeutic doses is not accompanied by a negative inotropic effect, even when used with beta-blockers.

Amlodipine does not alter the function of the sinoatrial node or AV conduction in intact animals and in humans. When using amlodipine in combination with beta-blockers in patients with arterial hypertension or with angina pectoris, a decrease in blood pressure is not accompanied by undesirable changes in ECG parameters.

Clinical efficacy of amlodipine in patients with chronic stable angina pectoris, vasospastic angina pectoris, and angiographically confirmed coronary artery disease has been proven.

Valsartan

Valsartan is an active and specific angiotensin II receptor antagonist intended for oral administration. It acts selectively on AT 1 subtype receptors, which are responsible for the known effects of angiotensin II. An increase in the plasma concentration of free angiotensin II due to blockade of AT 1 receptors under the influence of valsartan can stimulate unblocked AT 2 receptors, which counteract the effects of stimulation of AT 1 receptors. Valsartan does not have any pronounced agonistic activity against AT 1 receptors. The affinity of valsartan for AT 1 subtype receptors is approximately 20,000 times higher than for AT 2 subtype receptors.

Valsartan does not inhibit ACE, also known as kininase II, which converts angiotensin I to angiotensin II and causes the destruction of bradykinin.

Since the use of angiotensin II antagonists does not inhibit ACE and the accumulation of bradykinin or substance P, the development of a dry cough is unlikely.

In comparative clinical studies of valsartan with an ACE inhibitor, the incidence of dry cough was significantly lower (p <0.05) in patients receiving valsartan (2.6% of patients receiving valsartan and 7.9% receiving an ACE inhibitor). In a clinical study, which included patients who had previously developed a dry cough during treatment with an ACE inhibitor, this complication was noted in 19.5% of cases with valsartan treatment, and in 19% of cases with thiazide diuretic treatment. At the same time, in the group of patients treated with an ACE inhibitor, cough was observed in 68.5% of cases (p <0.05). Valsartan does not interact and does not block receptors of other hormones or ion channels, which are important for regulating the functions of the cardiovascular system.

When treating patients with arterial hypertension with valsartan, a decrease in blood pressure is noted, 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 after 4-6 hours. After taking the drug, the duration of the hypotensive effect lasts more than 24 hours. With repeated use, the maximum decrease in blood pressure, regardless of the dose taken, is usually achieved within 2-4 weeks. and maintained at a consistent level during long-term therapy. A sharp cessation 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 (class II-IV according to NYHA classification) leads to a significant decrease in the number of hospitalizations. This effect is most pronounced in patients not receiving ACE inhibitors or beta-blockers. When taking valsartan in patients with left ventricular failure (stable clinical course) or with impaired LV function after myocardial infarction, a decrease in cardiovascular mortality is noted.

Amlodipine / Valsartan

In patients with arterial hypertension who received Exforge 1 time / day, the antihypertensive effect persisted for 24 hours.

Exforge at a dose of 10/160 mg normalizes blood pressure (a decrease in diastolic blood pressure in the sitting position is less than 90 mm Hg. at the end of the study) in 62% of patients with inadequate blood pressure control with 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 control of blood pressure on the background of monotherapy with amlodipine at a dose of 10 mg. In patients with arterial hypertension with a combination of valsartan at a dose of 160 mg with amlodipine at a dose of 10 mg, an additional decrease in systolic and diastolic blood pressure by 6.0 mm RT is achieved. Art. and 3.9 mmHg. Art. respectively, compared with patients who continued to receive only valsartan at a dose of 160 mg or only amlodipine at a dose of 10 mg.

When titrating an Exforge dose of 5/160 mg to 10/160 mg in patients with arterial hypertension with diastolic blood pressure> 110 mm Hg. Art. and less than 120 mm RT. Art. there is a decrease in blood pressure in the sitting position at 36/29 mm RT. Art., comparable to a decrease in blood pressure when titrating a dose of a combination of an ACE inhibitor and a thiazide diuretic.

In two long-term studies with a long observation period, the Exforge effect persisted for 1 year. The sudden cessation of Exforge is not accompanied by a sharp increase in blood pressure.

In patients with adequate blood pressure control, but who developed severe edema with amlodipine monotherapy, when using combination therapy, a comparable blood pressure control was achieved with a lower likelihood of developing edema.

Exforge's therapeutic efficacy is independent of the patient’s age, gender, and race.

Contraindications

Pregnancy.

Hypersensitivity to the drug.

The safety of Exforge has not been established for the following categories:

Patients with unilateral or bilateral renal artery stenosis or stenosis of a single kidney artery.

Patients after a recent kidney transplant.

Children and adolescents under 18 years of age.

Precautions:

Impaired liver function (especially with obstructive biliary tract disease).

Severe renal impairment (creatinine clearance <10 ml / min).

Mitral or aortic stenosis.

Hypertrophic obstructive cardiomyopathy.

Hyperkalemia.

Deficiency in sodium and / or a decrease in bcc.

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 wish 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 of the possible risk to the fetus associated with the use of drugs that affect RAAS.

Given the mechanism of action of angiotensin II receptor antagonists, the risk to the fetus cannot be ruled out. It is known that the appointment of ACE inhibitors that affect RAAS in pregnant women in the II and III trimesters leads to damage or death of the developing fetus. According to a retrospective analysis of the use of ACE inhibitors in the first trimester of pregnancy was accompanied by the development of pathology of the fetus and newborn. With the unintended use of valsartan in pregnant women, cases of the development of spontaneous abortion are described, oligohydramnios and impaired renal function in newborns.

It is not known whether valsartan and / or amlodipine is excreted in breast milk. Since valsartan with breast milk is noted in experimental studies, it is not recommended to use Exforge during lactation (breastfeeding).

Special instructions

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

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

If necessary, cancel beta-blockers before starting Exforge therapy the dose of beta-blockers should be reduced gradually.As amlodipine is not a beta-blocker, the use of Ek Forge not prevent the development of withdrawal syndrome, which occurs when a dramatic treatment of beta-blockers.

In a placebo-controlled study in patients with uncomplicated arterial hypertension, pronounced arterial hypotension was observed in 0.4% of cases. In patients with activated RAAS (for example, with a deficiency of BCC and / or sodium in patients receiving high doses of diuretics), when taking angiotensin receptor blockers, symptomatic arterial hypotension may develop. Before starting Exforge treatment, a correction of the sodium content in the body and / or BCC should be carried out or therapy should be started under close medical supervision.

If arterial hypotension develops, the patient should be laid with raised legs, and if necessary, be infused with saline. After stabilization of blood pressure, Exforge treatment can be continued.

While using the drug with biologically active additives containing potassium, potassium-sparing diuretics, potassium-containing salt substitutes, or with other drugs that can cause an increase in the concentration of potassium in the blood (for example, with heparin), caution should be exercised and regular monitoring of the concentration of potassium in blood.

Effect on the ability to drive vehicles and control mechanisms

There is 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.

Composition of

Active ingredients: amlodipine, valsartan

Excipients: microcrystalline cellulose, crospovidone, magnesium stearate, colloidal silicon dioxide, hypromellose (hydroxypropylmethyl cellulose), titanium dioxide (E171, yellow polyol, 250 g, yellow polyol, (oxol), yellow carbon dioxide (yellow), , talc.

Dosage and administration of

The drug should be taken orally with a small amount of water, 1 time / day, regardless of the meal time.

Recommended daily dose is 1 tablet.

When prescribed to elderly patients, patients with initial or moderate impaired renal function (creatinine clearance> 30 ml / min), with impaired liver function or with liver diseases, with cholestasis, changes in dosing regimen are not required.

Side effects

From the respiratory system: often - nasopharyngitis, flu sometimes - cough, pain in the throat and larynx.

On the part of the sensory organs: rarely - visual impairment, tinnitus sometimes - dizziness associated with impaired function of the vestibular apparatus.

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

On the part of the cardiovascular system: sometimes - tachycardia, palpitations, orthostatic hypotension, rarely - syncope, marked reduction in blood pressure.

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

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

From the musculoskeletal system: sometimes - swelling of the joints, back pain, arthralgia rarely - muscle cramps, a feeling of heaviness throughout the body.

From the urinary system: rarely - pollakiuria, polyuria.

From the reproductive system: rarely - erectile dysfunction.

Other: often - pastiness, facial edema, peripheral edema, fatigue, flushing, asthenia, a feeling of heat.

Drug interaction

Amlodipine

When monotherapy with amlodipine, there is no clinically significant interaction with thiazide diuretics, beta-adrenergic blocking agents, ACE inhibitors, long-acting nitrates, nitroglycerin, varisiloxin, dihydroxylamine, dihydroxylamine, dihydroxinomax, hydroxycarboxylic acid hydroxycarboxylic acid hydroxycarboxylic acid, magnesium hydroxide, simethicone), cimetidine, NSAIDs, antibiotics and oral hypoglycemic drugs.

Valsartan

It has been established that monotherapy with valsartan has no clinically significant interaction with the following drugs: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine, glibenclamide.

When used with dietary supplements containing potassium, potassium-sparing diuretics, potassium-containing salt substitutes, or with other drugs that can cause an increase in the concentration of potassium in the blood (for example, with heparin), caution should be exercised and frequent monitoring of the concentration of potassium in the blood .

overdose

Symptoms: There are currently no cases of overdose with the drug. With an overdose of valsartan, a marked decrease in blood pressure and dizziness can be expected. An overdose of amlodipine can lead to excessive peripheral vasodilation and possible reflex tachycardia. The occurrence of pronounced and prolonged systemic arterial hypotension up to the development of lethal shock has also been reported.

Treatment: if you accidentally overdose, you should induce vomiting (if the drug was recently taken) or wash your stomach, appoint activated charcoal. The use of activated charcoal in healthy volunteers immediately or 2 h after administration of amlodipine significantly reduced its absorption. At clinically expressed arterial hypotension caused by Exforge, it is necessary to conclude the patient with the raised legs, to take active measures for maintenance of activity of cardiovascular system, including frequent monitoring of heart and respiratory function, BCC and urinary output. In the absence of contraindications to restore vascular tone and blood pressure can be used (with caution) vasoconstrictor. In / in the introduction of calcium gluconate may be effective for eliminating calcium channel blockade. Withdrawal of valsartan and amlodipine during hemodialysis is unlikely.

Storage conditions

Store in a dry place at a temperature not exceeding 30 ° C.

Shelf life

2 years.

Deystvuyushtee substance

Amlodipine, Valsartan

Terms of sale from

pharmacies Prescription

dosage form



Possible product names

EXFORGE 0.005 / 0.08 N28 TABLE P / O

Exforge 5 mg + 80 mg No. 28 tab s / pl srlkp Exforge 5mg + 80mg Tab. p / pl / rev X28

Exforge 5mg + 80mg No. 28 tab

EXFORGE 5MG / 80MG. No. 28 TAB. P / O

Novartis Farma Stein AG, Switzerland



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