Amlodipine + Irbesartan (Amlodipine + Irbesartan)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Angiotensin II receptor antagonists (AT1 subtype)

Calcium channel blockers

Included in the formulation
  • Aprovask®
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    Sanofi-Aventis de Mexico SA de S.V.     Mexico
    • АТХ:

    C.09.D.B.05   Irbesartan and amlodipine

    Pharmacodynamics:

    The pharmacodynamic properties of each of the active substances that make up the combined preparation, irbesartan and amlodipine, contribute to their additive antihypertensive effect when used in combination, compared with that in the use of each of these drugs alone. Both angiotensin II receptor antagonists and slow calcium channel blockers reduce arterial pressure by decreasing peripheral vascular resistance, but calcium blockade and reduction in angiotensin II-mediated vasoconstrictor action are complementary mechanisms. Besides, irbesartan prevents the development of peripheral edema (side effect of amlodipine).

    Amlodipine blocks calcium channels Ltype of smooth musculature of the vessels, thus providing a direct vasorelaxing effect. Irbesartan is a competitive blocker of angiotensin receptors II (AT1- subtype), which are in the smooth muscles of the vessels and the adrenal cortex (it is possible to internalize the receptors), also blocks the aldosterone-secreting effect of angiotensin. In complex amlodipine and irbesartan potentiate the antihypertensive effect of each other.

    Amlodipine reduces myocardial ischemia due to the following two effects:

    1) Amlodipine expands the peripheral arterioles and thereby reduces the overall peripheral resistance of the vessels, the so-called afterload. Since the heart rate when receiving amlodipine is practically not increased, this decrease in the load on the cardiac muscle reduces the energy expenditure of the myocardium and its need for oxygen.

    2) The mechanism of antianginal action of amlodipine also appears to be associated with the expansion of the main coronary arteries and coronary arterioles, both in the zones of the myocardium with normal blood flow and in the ischemic zones of the myocardium. This dilatation of the coronary vessels increases the oxygen delivery to the myocardium in patients with spasm of the coronary arteries (with Prinzmetal angina or variant angina).

    Pharmacokinetics:

    Amlodipine: the drug binds to plasma proteins by 92-98%, undergoes biotransformation in the liver (CYP3A3/4, 3A5-7), half-life is 2 hours, excreted by the kidneys by 80% and the gastrointestinal tract by 20%.

    Irbesartan is a drug that is active when ingested, which does not need biotransformation to manifest its activity. After oral administration irbesartan quickly and completely absorbed. Maximum concentration Irbesartan in blood plasma is achieved after 1.5-2 hours after its intake. Absolute bioavailability of irbesartan when ingested is 60-80%. Eating does not affect the bioavailability of irbesartan.

    Irbesartan binds to plasma proteins by 96%, undergoes biotransformation in the liver (CYP2C9), the half-life is 11-15 hours, excreted by the kidneys by 20% and the gastrointestinal tract by 80%.

    Indications:

    Arterial hypertension.

    ICD-10

    IX.I10-I15.I10   Essential [primary] hypertension

    Contraindications:
    • Hypersensitivity.
    • Pregnancy and lactation.
    • Clinically significant aortic stenosis.
    • Age to 18 years.
    • Unstable angina.
    • Cardiogenic shock.
    • Simultaneous reception of drugs containing aliskiren, in patients with mild / severe renal insufficiency, diabetes mellitus.
    Carefully:
    • Hyponatremia, hypovolemia.
    • Patients in whom kidney function depends on the activity of the renin-angiotensin-aldosterone system.
    • Chronic heart failure.
    • Kidney Diseases.
    • Syndrome of weakness of the sinus node.
    • Stenosis of the mitral and aortic valve.
    • Hypertrophic obstructive cardiomyopathy.
    • Cardiac ischemia.
    • Clinically significant atherosclerosis of cerebral vessels.
    • Syndrome of weakness of the sinus node.
    Pregnancy and lactation:

    Category of recommendations for FDA - C. The drug is contraindicated during pregnancy and lactation. The drug should also not be taken to women with childbearing potential if they do not use effective methods of contraception.

    Dosing and Administration:

    Orally, the average dose is 1 tablet a day (5 mg of amlodipine, 150 mg of irbesartan), the maximum dose of amlodipine is 10 mg, irbesartanaa is 300 mg.

    Side effects:

    From the side kidney and urinary tract: hypercreatinemia, proteinuria, azotemia.

    From the side gastrointestinal tract: pain in the abdomen, swelling of the gums, constipation, nausea, glossitis.

    From the side metabolism: hyperkalemia.

    From the side genital organs and mammary glands: erectile disfunction.

    String of cardio-vascular system: sinus bradycardia, palpitations, orthostatic hypotension, excessive lowering of arterial pressure, tachycardia.

    From the side nervous system: vertigo, headache, drowsiness, paresthesia, dizziness.

    Violations at the place of administration: asthenia, edema, peripheral edema.

    From the side respiratory system: cough.

    From the side musculoskeletal system: arthralgia, myalgia, stiffness of joints.

    From the side immune system: allergic reactions.

    Overdose:

    Pronounced peripheral vasodilation, excessive decrease in blood pressure. Treatment is symptomatic.

    Interaction:

    Combination amlodipine + irbesartan in combination with drugs, containing aliskiren, is contraindicated in patients with diabetes mellitus or moderately severe and severe renal failure (glomerular filtration rate <60 ml / min / 1.73 m2) and is not recommended for other patients.

    Special instructions:

    The drug may cause an excessive decrease in blood pressure.

    The safety of the drug for children has not been studied.

    Impact on the ability to drive vehicles and manage mechanisms not studied, but unlikely.

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