Aliskiren + Amlodipine (Aliskirenum + Amlodipinum)

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

Renin inhibitors

Calcium channel blockers

Included in the formulation
  • Racilam
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    Novartis Pharma AG     Switzerland
    • АТХ:

    C.09.X.A.53   Aliskiren and amlodipine

    Pharmacodynamics:

    Combined antihypertensive drug.

    Aliskiren

    Selective inhibitor of renin of non-peptide structure, blocks the conversion of angiotensin into angiotensin I, reducing the plasma renin level, angiotensin I and angiotensin II.

    Renin is excreted by the kidneys with a decrease in renal perfusion and the volume of circulating blood. Once in the bloodstream, renin cleaves angiotensin to an inactive decapeptide of angiotensin I, which, in turn, with the help of an angiotensin-converting enzyme is converted into active octapeptide angiotensin II, which causes vasoconstriction and stimulates the release of adrenal catecholamines from the adrenal medulla, also enhances the reabsorption of sodium and aldosterone ions, which increases blood pressure. By increasing the level of angiotensin II there is an expression of markers and mediators of inflammation and fibrosis of the organ. In addition, angiotensin II inhibits the release of renin, adversely affecting the system. As a result, increased activity of renin leads to an increased risk of cardiovascular complications.

    The action of inhibitors of renin leads to a compensatory increase in the concentration of renin in the blood plasma. The action of aliskiren neutralizes the feedback effect, which leads to a persistent decrease in plasma renin activity.

    Amlodipine

    Selective calcium channel blocker II class. Has antianginal and antihypertensive effect. Prevents the entry of extracellular calcium into the muscle cells of the coronary and peripheral arteries. In high doses, it inhibits the release of calcium ions from intracellular stores. Does not affect the tone of the veins.

    Strengthens the coronary blood flow, improving the blood supply of ischemic zones of the myocardium, does not cause a "robbery syndrome". Expands peripheral arteries, reduces overall peripheral resistance, postnagruzku and the need for myocardium in oxygen. Does not affect the drivers of rhythm: sinoatrial and atrioventricular nodes. Has a weak antiarrhythmic effect.

    It enhances kidney blood flow, causes a moderate natriuresis.

    Pharmacokinetics:

    Aliskiren

    After oral ingestion, up to 2.5% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 1-3 hours.The equilibrium concentration in blood plasma is reached within 5-7 days after the start of the administration once a day, the equilibrium level is approximately 2 times higher than at the initial dose. The connection with plasma proteins is up to 50%.

    Metabolism in the liver.

    The half-life is 40 hours. Elimination with feces, mostly unchanged.

    Amlodipine

    After oral administration up to 80% absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 6-12 hours. It binds to plasma proteins by 97.5%. Penetrates through the blood-brain barrier. Metabolised in the liver.

    The half-life is 30-50 hours.

    Elimination by the kidneys in the form of metabolites. It is not removed during hemodialysis.

    Indications:

    It is used for the treatment of arterial hypertension.

    ICD-10

    IX.I10-I15.I15   Secondary Hypertension

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

    Contraindications:

    Acute myocardial infarction, aortic stenosis, arterial hypotension, anuria, severe renal failure, hereditary angioedema, shock, individual intolerance, children under 18 years of age.

    Carefully:

    Hypokalemia, hyponatremia, Renovascular hypertension, elderly age.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside, 1 tablet a day, regardless of food intake and time.

    The highest daily dose: 150 mg of aliskiren and 50 mg of amlodipine (1 tablet).

    The highest single dose: 150 mg of aliskiren and 50 mg of amlodipine (1 tablet).

    Side effects:

    Aliskiren

    Central and peripheral nervous system: dizziness.

    The cardiovascular system: hypotension, peripheral edema.

    Digestive system: diarrhea.

    Dermatological reactions: hyperemia, toxic epidermal necrolysis, Stevens-Johnson syndrome, skin itching.

    urinary system: impaired renal function.

    Allergic reactions.

    Amlodipine

    Central and peripheral nervous system: dizziness, headache, with prolonged use - paresthesia of the extremities, depression.

    The cardiovascular system: possible exacerbation of angina in the first days of taking the drug, flushing of the blood to the skin of the face, tachycardia.

    Digestive system: nausea, gingival hyperplasia.

    Musculoskeletal system: myalgia, convulsions of the upper and lower extremities.

    urinary system: rarely - polyuria.

    Reproductive system: gynecomastia, erectile dysfunction.

    Allergic reactions.

    Overdose:

    Aliskiren

    Arterial hypotension.

    Treatment is symptomatic.

    Amlodipine

    Headache, arrhythmia. In severe cases - loss of consciousness, coma.

    Treatment is symptomatic. Antidotes are calcium preparations. Hemodialysis is ineffective, plasmapheresis is recommended.

    Interaction:

    Aliskiren

    Clinically significant interactions are not described.

    Amlodipine

    Incompatible with alcohol. The intake of grapefruit juice slows the absorption of the drug.

    With the simultaneous use of the drug with antihypertensive drugs, as well as inhalational anesthetics, tricyclic antidepressants, nitrates, cimetidine, diuretics, the hypotensive effect intensifies.

    Incompatible with rifampicin, as it accelerates the metabolism of slow calcium channel blockers.

    Increases the concentration of indirect anticoagulants in blood plasma.

    Special instructions:

    Stop taking the drug should be gradual.

    Before an operative intervention it is necessary to inform the anesthesiologist about taking the drug by the patient.

    Instructions
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