Description
Pharmacological action of
Pharmaceutical group:
ACE inhibitor.
Pharmaceutical action:
ACE inhibitor, has a hypotensive, vasodilating, diuretic and potassium-sparing effect. It reduces the formation of angiotensin II from angiotensin I, which leads to a decrease in OPSS and systemic blood pressure.
Suppresses aldosterone synthesis, inhibits tissue ACE.
The antihypertensive effect is also due to the suppression of the metabolism of bradykinin, which has a pronounced vasodilating effect. A decrease in blood pressure is not accompanied by a change in bcc, cerebral and renal blood flow, blood supply to internal organs, skeletal muscles, skin, and reflex activity of the myocardium.
With hypertension and LV hypertrophy, treatment leads to a decrease in its mass and wall thickness of the septum. Long-term treatment does not lead to metabolic disorders.
After oral administration, the hypotensive effect develops within 1 hour, reaches a maximum after 3-6 hours and persists for 24 hours.
Pharmacokinetics: Absorption – 36% (regardless of food intake). In the mucous membrane of the gastrointestinal tract and liver, it is hydrolyzed to form fosinoprilat. TCmax – 3 hours, T1 / 2 – 11.5 hours.
Communication with plasma proteins – 95%, has a relatively small volume of distribution and is sorbed to a small extent by cellular components.
Does not penetrate the BBB. It is excreted in the bile, with urine.
Indications
Arterial hypertension, CHF.
Contraindications
Hypersensitivity to fosinopril, pregnancy, lactation.
Caution. A history of angioedema during therapy with ACE inhibitors, hereditary or idiopathic angioedema, aortic stenosis,
cerebrovascular and cardiovascular diseases (including cerebrovascular insufficiency, coronary heart disease, coronary insufficiency), srdlmp including SLE, scleroderma),
inhibition of bone marrow hematopoiesis,
diabetes mellitus, hyperkalemia,
bilateral renal artery stenosis, stenosis of a single kidney artery,
consisting after kidney transplantation,
liver failure, a diet with a restriction of Na +, conditions accompanied by a decrease in BCC (including diarrhea, vomiting),
old age, age up to 18 years (safety and efficacy have not been studied).
Special instructions
Patients with malignant arterial hypertension or concomitant decompensated heart failure should begin treatment in a hospital setting.
Before starting treatment with ACE inhibitors and during treatment, they count the total number of leukocytes and determine the leukocyte formula (1 time per month in the first 3-6 months of treatment and at periodic intervals of up to 1 year in patients with an increased risk of neutropenia: in case of impaired renal function, systemic diseases of the connective tissue in those receiving high doses), as well as at the first signs of infection.
Before and during treatment, control of blood pressure, renal function, plasma K +, Hb and creatinine, urea, electrolyte concentrations and liver enzyme activity in the blood is necessary.
Based on the results of epidemiological studies, it is suggested that the simultaneous use of ACE inhibitors and insulin, as well as oral hypoglycemic drugs, can lead to the development of hypoglycemia. The greatest risk of development is observed during the first weeks of combination therapy, as well as in patients with impaired renal function. Patients with diabetes require careful glycemic control, especially during the first month of treatment with an ACE inhibitor.
Caution should be exercised when prescribing to patients on a low-salt or salt-free diet (increased risk of hypotension).
Safety and efficacy in pediatric practice: it is recommended that closely monitor newborns who have been exposed to intrauterine exposure to ACE inhibitors to detect hypotension, oliguria and hyperkalemia.
Newborns and infants have a risk of oliguria and neurological disorders, possibly due to a decrease in renal and cerebral blood flow due to a decrease in blood pressure, caused by ACE inhibitors, lower initial doses and close monitoring are recommended.
Care must be taken when driving or performing other work requiring increased attention, as dizziness is possible, especially after an initial dose of an ACE inhibitor in patients taking diuretic drugs.
Caution should be exercised when exercising or in hot weather because of the risk of dehydration and a decrease in blood pressure due to a decrease in fluid volume.
Before surgery (including dentistry), the surgeon / anesthetist should be advised of the use of ACE inhibitors.
When using ACE inhibitors in the II-III trimesters of pregnancy, oligohydroamnion, hypotension of the fetus and newborn, oliguria and deaths are possible.
Composition
fosinopril 20 mg.
Dosage and administration
Inside, at 10 mg / day, 1 time per day, if necessary, the dose can be increased to 40 mg.
The dose should be selected in accordance with the dynamics of blood pressure.
Side effects
From the CCC side: decreased blood pressure, orthostatic collapse, tachycardia, palpitations, arrhythmias, angina pectoris, myocardial infarction.
From the urinary system: development or enhancement of chronic renal failure, proteinuria.
From the nervous system: stroke, cerebral ischemia, dizziness, headache, weakness when used in high doses – insomnia, anxiety, depression, confusion, disorders of the vestibular apparatus, paresthesia.
On the part of the sensory organs: hearing and vision impairment, tinnitus.
From the digestive system: nausea, intestinal obstruction, pancreatitis, hepatitis, cholestatic jaundice, abdominal pain, vomiting, dyspepsia, constipation, loss of appetite, stomatitis, glossitis.
From the respiratory system: dry cough, pulmonary infiltrates, bronchospasm, shortness of breath, rhinorrhea, pharyngitis, dysphonia.
Allergic, toxic-allergic and immunopathological reactions, incl. angioedema of the small intestine (very rare).
Lab performance: hypercreatininemia, increased urea concentration, increased activity of hepatic transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia, decreased Hb and hematocrit, neutropenia, leukopenia, eosinophilia, increased ESR.
Cases of hypoglycemia have been reported in patients with diabetes who took insulin and oral hypoglycemic drugs.
Teratogenic, fetotoxic effect – impaired development of the kidneys of the fetus, decreased blood pressure of the fetus and newborns, impaired renal function, hyperkalemia, cranial hypoplasia, oligohydramnios, limb contracture, skull deformation, lung hypoplasia.
Overdose
Symptoms: decreased blood pressure, bradycardia, shock, disturbance of water-electrolyte balance, acute renal failure, stupor.
Treatment: place the patient in a supine position with raised legs.
In mild cases of overdose, gastric lavage, administration of adsorbents and sodium sulfate within 30 minutes after administration.
With a decrease in blood pressure – on / in the introduction of catecholamines, angiotensin II with bradycardia – the use of a pacemaker.
Not indicated during hemodialysis.
Active ingredient
Fosinopril
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