Spirapril (Spiraprilum)

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

ACE Inhibitors

Included in the formulation
  • Quadropril®
    pills inwards 
    Teva Pharmaceutical Enterprises Co., Ltd.     Israel
    • АТХ:

    C.09.A.A   ACE Inhibitors

    C.09.A.A.11   Spirapril

    Pharmacodynamics:

    It blocks the conversion of angiotensin I to angiotensin II, which results in the release of noradrenaline from the endings of sympathetic fibers, the vasoconstrictor effect, the secretion of aldosterone by the adrenal cortex and increases the bradykinin content by reducing its inactivation by the angiotensin converting enzyme.

    Bradykinin stimulates B2-cinin receptors of the vascular endothelium, which leads to the rapid release of prostacyclin and other vasodilating substances that cause relaxation of smooth muscles.

    Reduces the overall peripheral resistance of blood vessels, without affecting the heart rate.

    Pharmacokinetics:

    After oral administration, an empty stomach is absorbed up to 45% in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 1 hour. The connection with plasma proteins is 90%.

    Metabolism in the liver with the formation of an active metabolite - aspirin.

    Half-life of the first phase (before the formation of aspirate) is 2 h, the second phase - 40 h.Elimination with feces (51%) and kidneys (49%) in unchanged form and in the form of metabolite.

    Indications:

    It is used for the treatment of arterial hypertension.

    ICD-10

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

    Contraindications:

    Individual intolerance.

    Carefully:

    Renal failure.

    Pregnancy and lactation:

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

    Dosing and Administration:

    Inside to 6 mg 1 time / day.

    The highest daily dose: 6 mg.

    The highest single dose: 6 mg.

    Side effects:

    Central and peripheral nervous system: cerebral ischemia, headache, dizziness, anxiety, confusion, paresthesia.

    The system of hematopoiesis: anemia, leukopenia, thrombocytopenia, rarely - eosinophilia.

    Respiratory system: dry cough, bronchospasm, dyspnea, rhinorrhea, pharyngitis, dysphonia.

    Cardiovascular system: hyperkalemia, hyponatremia, orthostatic hypotension, syncope, tachycardia, angina pectoris, myocardial infarction.

    Digestive system: nausea, cholestatic jaundice, constipation, dry mouth.

    Urinary system: hypercreatinemia, proteinuria, increased urea levels, development or progression of chronic renal failure.

    Dermatological reactions: onycholysis, alopecia.

    Reproductive system: decreased potency.

    Allergic reactions.

    Overdose:

    Pronounced decrease in blood pressure, electrolyte imbalance, bradycardia, cardiovascular shock, renal failure.

    Treatment: intravenous epinephrine, blood substitution solutions, hydrocortisone.

    Interaction:

    Strengthens the hypoglycemic action of insulin and oral hypoglycemic drugs.

    Enhances the toxic effects of lithium preparations.

    Sodium chloride, non-steroidal anti-inflammatory drugs reduce the hypotensive effect of spirapril.

    With simultaneous use with potassium-sparing diuretics (amiloride, triamterene, spironolactone), products with a high content of potassium develops hyperkalemia.

    When used simultaneously with cytostatics, allopurinol, systemic glucocorticosteroids, procainamide, immunosuppressants increase the risk of developing leukopenia.

    With simultaneous use with drugs for general anesthesia and for local anesthesia, it is possible to develop arterial hypotension.

    Special instructions:

    Monitoring of blood pressure, peripheral blood.

    With caution apply to individuals whose profession requires increased concentration and attention.

    Instructions
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