Ramipril-SZ, 10mg pills, 30pcs

Composition

Active ingredient:

ramipril – 10 mg;

Auxiliary substances:  

lactose monohydrate 143.5 mg,

magnesium stearate 1.5 mg

Pharmacological action

Ramipril-SZ is an ACE inhibitor. It is a prodrug from which the active metabolite ramiprilate is formed in the body. It is believed that the mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of conversion of angiotensin I to angiotensin II, which is a powerful vasoconstrictor. As a result of a decrease in the concentration of angiotensin II, a secondary increase in plasma renin activity occurs due to the elimination of negative feedback during renin release and a direct decrease in aldosterone secretion. Due to its vasodilating action, it reduces OPSS (afterload), jamming pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; increases the minute volume of the heart and load tolerance.

In patients with signs of chronic heart failure after a myocardial infarction, ramipril reduces the risk of sudden death, progression of heart failure to severe/resistant failure, and reduces the number of hospitalizations for heart failure.

Ramipril is known to significantly reduce the incidence of myocardial infarction, stroke, and cardiovascular death in patients with an increased cardiovascular risk due to vascular diseases (CHD, stroke, or peripheral vascular disease) or diabetes mellitus who have at least one additional risk factor (microalbuminuria, hypertension, elevated total cholesterol, low HDL, smoking).

Reduces overall mortality and the need for revascularization procedures, and slows the onset and progression of chronic heart failure. In both diabetic and non-diabetic patients, ramipril significantly reduces existing microalbuminuria and the risk of developing nephropathy. These effects are observed in patients with both elevated and normal blood pressure.

The hypotensive effect of ramipril develops in about 1-2 hours, reaches a maximum within 3-6 hours, and lasts at least 24 hours.

Indications

• Arterial hypertension;
• congestive heart failure, including acute myocardial infarction in patients with stable haemodynamics,
• diabetic nephropathy and chronic diffuse renal disease (non-diabetic nephropathy);
• reduction in the risk of myocardial infarction, stroke, or coronary death in patients with coronary artery disease, with an increased risk of cardiovascular diseases, including patients after myocardial infarction, percutaneous transluminal coronary angioplasty, coronary artery bypass grafting (when clinically stable condition).

Use during pregnancy and lactation

Contraindicated in pregnancy. Before starting treatment, you should make sure that there is no pregnancy. If the patient becomes pregnant during treatment, it is necessary to replace ramipril drug therapy with another therapy as soon as possible. Otherwise, there is a risk of damage to the fetus, especially in the first trimester of pregnancy.

Effect on the fetus:  impaired fetal kidney development, decreased blood pressure Fetal and newborn blood pressure, renal dysfunction, hyperkalemia, cranial hypoplasia, oligohydramnion, limb contracture, cranial deformity, lung hypoplasia.

Category of action on the fetus according to the FDA-D.

Breast-feeding should be discontinued for the duration of treatment.

Contraindications

• Hypersensitivity to ramipril or other ACE inhibitors;
• a history of angioedema, including those associated with previous therapy with ACE inhibitors;
• pregnancy, breast-feeding, age after 18 years (safety and efficacy have not been determined).

Side effects

Cardiovascular and blood disorders (hematopoiesis, hemostasis):  hypotension (10.7%), including postural (2.2%), angina (2.9%), syncope (2.1%), heart failure (2%), myocardial infarction (1.7%), vertigo (1.5%), chest pain (1.1%), less than 1% — arrhythmia, palpitations, hemolytic anemia, myelodepression, pancytopenia, thrombocytopenia, eosinophilia, agranulocytosis; vasculitis.

From the digestive tract:  nausea (2.2%), vomiting (1.6%), diarrhea (1.1%), less than 1% — dry mouth or increased salivation, anorexia, dyspepsia, dysphagia, constipation, abdominal pain, gastroenteritis, pancreatitis, hepatitis, liver dysfunction (cholestatic jaundice, fulminant liver necrosis with fatal outcome), changes in the level of transaminases.

Nervous system and sensory disorders:  dizziness (4.1%), headache (1.2%), asthenia (0.3%), less than 1% — cerebrovascular disorders, amnesia, drowsiness, seizures, depression, sleep disorders, neuralgia, neuropathy, paresthesia, tremor, hearing loss, visual impairment.

Respiratory system disorders:  unproductive cough (7.6%), upper respiratory tract infections, less than 1% — dyspnoea, pharyngitis, sinusitis, rhinitis, tracheobronchitis, laryngitis, bronchospasm.

From the genitourinary system:  impaired renal function (1.2%), less than 1% — proteinuria, oliguria, edema; impotence.

From the side of the skin:  urticaria, prurigo, rash, erythema multiforme, photosensitization.

Other services:  less than 1% — weight loss, anaphylactoid reactions, increased levels of urea nitrogen and creatinine, angioedema (0.3%), arthralgia/arthritis, myalgia, fever, increased titer of antinuclear antibodies, hyperkalemia, changes in enzyme activity, bilirubin, uric acid, glucose concentrations.

Interaction

Contraindicated combinations – Use of certain high-flow membranes with a negatively charged surface (for example, polyacrylonitrile membranes) during hemodialysis or hemofiltration; use of dextran sulfate in low-density lipoprotein apheresis Risk of severe anaphylactic reactions.

Not recommended combinations

-With potassium salts, potassium-sparing diuretics (for example, amiloride, triamterene, spironolactone), a more pronounced increase in the content of potassium in the blood serum is possible (with simultaneous use, careful monitoring of the content of potassium in the blood serum is required).

Combinations that should be used with caution

– With antihypertensive agents (especially diuretics) and other drugs that reduce blood pressure (nitrates, tricyclic antidepressants) Potentiation of the antihypertensive effect; when combined with diuretics, the serum sodium content should be monitored.

– With hypnotics, narcotic and non-narcotic analgesics May be more pronounced decrease in blood pressure; – WITH vasopressor of sympathomimetika (with epinephrine) Decrease the hypotensive effect of ramipril, requires careful control of blood pressure.

– With allopurinol, a procainamide, cytostatics, immunosuppressants and systemic corticosteroids and other drugs that may affect the hematological parameters of the combined use increases the risk of leukopenia. – With lithium salts, increase the serum concentration of lithium and increase the cardio-and neurotoxic effects of lithium.

– With hypoglycemic agents for oral use (sulfonylureas, biguanides), insulin Due to a decrease in insulin resistance under the influence of ramipril, it is possible to increase the hypoglycemic effect of these drugs up to the development of hypoglycemia. Combinations to be considered

– With nonsteroidal anti-inflammatory drugs (Indometacin, acetylsalicylic acid) It is possible to weaken the effect of ramipril, increase the risk of impaired renal function and increase the content of potassium in the blood serum.

– With heparin, it is possible to increase the content of potassium in the blood serum.

– With sodium chloride, Reducing the hypotensive effect of ramipril and less effective treatment of symptoms of chronic heart failure.

– Increased vasodilation with ethanol. Ramipril may increase the adverse effects of ethanol on the body.

– With estrogens, Weakening of the hypotensive effect of ramipril (fluid retention).

– Desensitizing therapy in case of hypersensitivity to insect poisons, ACE inhibitors, including ramipril, increase the likelihood of developing severe anaphylactic or anaphylactoid reactions to insect poisons. With the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate) for intravenous use, a symptom complex has been described, including facial skin hyperemia, nausea, vomiting, and arterial hypotension.

How to take it, course of use and dosage

Tablets should be swallowed whole (not chewed), and washed down with a sufficient amount (1/2 cup) of water, regardless of the meal (that is, tablets can be taken both before, during or after a meal). The dose is selected depending on the therapeutic effect and tolerability of the drug by the patient. Treatment with Ramipril-SZ is usually long-term, and its duration is determined by the doctor on a case-by-case basis. Unless otherwise prescribed, the following dosage regimens are recommended for normal renal and hepatic function.

For essential hypertension

Usually, the initial dose is 2.5 mg once a day in the morning. If taking the drug at this dose for 3 weeks or more fails to normalize blood pressure, the dose can be increased to 5 mg ramipril per day.If the 5 mg dose is not effective enough, it can be doubled in 2-3 weeks to the maximum recommended daily dose of 10 mg per day. As an alternative to increasing the dose to 10 mg per day, if the hypotensive effectiveness of the daily dose of 5 mg is insufficient, it is possible to add other antihypertensive agents, in particular diuretics or slow calcium channel blockers, to the treatment. In case of chronic heart failure

Recommended starting dose: 1.25 mg once a day (1/2 tablet 2.5 mg). Depending on the patient’s response to the therapy, the dose may increase. It is recommended to double the dose at intervals of 1-2 weeks. If a daily dose of 2.5 mg or higher is required, it can be given either once a day or divided into 2 doses. The maximum recommended daily dose is 10 mg.

For diabetic or non-diabetic nephropathy

Recommended starting dose: 1.25 mg once a day (1/2 tablet 2.5 mg). The dose can be increased to 5 mg once a day. In these conditions, doses above 5 mg once daily have not been sufficiently studied in controlled clinical trials. To reduce the risk of myocardial infarction, stroke, or cardiovascular mortality in patients at high cardiovascular risk

Recommended starting dose: 2.5 mg once a day. Depending on the patient’s tolerance to the drug, the dose can be gradually increased. It is recommended to double the dose after 1 week of treatment, and during the next 3 weeks of treatment – increase it to the usual maintenance dose of 10 mg 1 time per day. Doses exceeding 10 mg have not been sufficiently studied in controlled clinical trials. The use of the drug in patients with creatinine clearance less than 0.6 ml / sec has not been sufficiently studied. In case of heart failure that developed during the first few days (from the 2nd to the 9th day) after acute myocardial infarction

The recommended starting dose is 5 mg per day, divided into two single doses of 2.5 mg, which are taken one in the morning and the second in the evening. If the patient does not tolerate this initial dose (there is an excessive decrease in blood pressure), then he is recommended to give 1.25 mg 2 times a day for two days (1/2 tablet 2.5 mg). Then, depending on the patient’s response, the dose can be increased. It is recommended that the dose should be doubled at intervals of 1-3 days if increased. Later, the total daily dose, which was initially divided into two doses, can be given once. The maximum recommended dose is 10 mg.

Currently, the experience of treating patients with severe heart failure (NYHA functional class III-IV) that occurred immediately after acute myocardial infarction is insufficient. If these patients decide to start treatment with Ramipril-SZ, it is recommended that treatment should start with the lowest possible dose – 1.25 mg once a day (1/2 tablet 2.5 mg) and special care should be taken with each dose increase.

Overdose

Symptoms: excessive peripheral vasodilation with the development of a pronounced decrease in blood pressure, shock; bradycardia, water and electrolyte disorders, acute renal failure, stupor.

Treatment: gastric lavage, intake of adsorbents, sodium sulfate (if possible during the first 30 minutes). In the case of a marked decrease in blood pressure, the use of alpha-1-adrenergic agonists (norepinephrine, dopamine) can be added to therapy to replenish the volume of circulating blood and restore electrolyte balance. If bradycardia is refractory to medical treatment, it may be necessary to install a temporary artificial pacemaker. In case of overdose, serum creatinine and electrolyte concentrations should be monitored.

Special instructions

Treatment is carried out with regular medical supervision. Prior to starting treatment (1 week in advance), previous antihypertensive therapy, including diuretics, should be discontinued (if it is impossible to cancel diuretics, it is necessary to reduce the dose and adjust the water-electrolyte balance). In patients with a malignant course of hypertension, the dose is increased gradually, every 24 hours, under control Blood pressure until the maximum effect is achieved.

During therapy, it is necessary to monitor blood pressure, constantly monitor the picture of peripheral blood (before starting treatment, the first 3-6 months of treatment and at periodic intervals in the future up to 1 year, especially in patients with an increased risk of neutropenia), protein levels, potassium in plasma, urea nitrogen, creatinine, kidney function, body weight, and diet. If the patient develops hyponatremia and dehydration, it is necessary to adjust the dosage regimen (reducing doses). If cholestatic jaundice develops and fulminant liver necrosis progresses, treatment is discontinued.

Hemodialysis through high-performance polyacrylonitrile metaallyl sulfate membranes (for example, AN69), hemofiltration, or LDL apheresis should be avoided (anaphylaxis or anaphylactoid reactions may occur). It should be borne in mind that when using ramipril in patients with autoimmune diseases and syndromes, the risk of developing neutropenia increases.

Hyposensitization therapy may increase the risk of anaphylactic reactions. It is recommended to exclude the use of alcoholic beverages during treatment. Use with caution when working for drivers of vehicles and people whose profession is associated with increased concentration of attention.

Form of production

Tablets

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Ramipril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Diabetic Nephropathy, Kidney damage, Heart failure, Prevention of heart attacks and strokes