Buy Generic Capoten (Captopril) 12,5, 25, 50 mg online

Last Updated on February 19, 2017 by Dr.Derek Fhisher

Most popular brand: Capoten
Active ingredient: Captopril
Available dosage forms: 12,5, 25, 50 mg

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Captopril general information

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Captopril (Captopril): instruction, and the use of a formula

The nosological classification (ICD – 10)

Code CAS

Feature substance Captopril

White or off-white crystalline powder with a faint odor of sulfur containing sulfhydryl residue. Soluble in water (160 mg / ml), methanol, and ethanol (96%). Poorly soluble in chloroform and ethyl acetate, insoluble in ether.

Pharmacology

Mode of action – the hypotensive, vasodilatory, cardioprotective, natriuretic.

It inhibits ACE. prevents passage of angiotensin I to angiotensin II (has socudosuzhivayuschee action, promotes the release of aldosterone) and inhibits the inactivation of endogenous vasodilators – bradykinin and PGE ₂ . Increases kallikrein activity – kinin system, increases the release of biologically active substances (PGE ₂ and PGI ₂ endothelial relaxing and atrio -. Natriuretic factor) that have natriuretic and vasodilator effect, improves renal bloodstream. It reduces the release of norepinephrine from nerve endings, education arginine – vasopressin and endothelin 1, having vasoconstrictor properties?. ACE activity is reduced by 40% after 1-3 hours after administration of a dose of 12.5 mg (50% inhibition of enzyme activity required plasma concentration 22 nmol / l). Antihypertensive action is shown in 15-60 min after oral administration, reaching a maximum after 60-90 minutes and lasts 6-12 hours. The duration of the antihypertensive effect is dose dependent and reaches optimum values ​​for several weeks with repeated use. Decreases round. pre – and afterload on the heart, pressure in the pulmonary and pulmonary vascular resistance, increases cardiac output (heart rate does not change). In patients with heart failure increases exercise tolerance, decreases pulmonary capillary wedge pressure, reduces the size of infarction dilated (long-term therapy), improves health, increases life expectancy, ie It has a cardioprotective effect. In high doses (500 mg / day) shows angioprotective properties with respect to microvascular, increasing the diameter of the major peripheral arteries (from 13% to 21%) and slow the progression of renal disease in diabetic nephropathy (reduced need for dialysis procedures, kidney transplant, postpones death). It reduces the frequency of cardio – vascular complications in hypertension combined with diabetes. In patients with moderate hypertension when used in doses of 25-50 mg 2 times a day improves the quality and duration of life, general well-being, improves sleep and emotional status.

Quickly and completely absorbed from the gastrointestinal tract. Minimal absorption is 60-75%. In the presence of food decreased the bioavailability of 30-55% without a significant change in pharmacokinetic and pharmacodynamic parameters. When taken on an empty stomach is found in the blood after 15 minutes, C _max is achieved in 30-90 minutes. By the end of the day the rest of the concentration with respect to the C _max is 7-8%. Sublingual use improves bioavailability and faster onset of action. The plasma is 25-30% associated with proteins (mainly albumin). It passes through the blood-tissue barriers, eliminating the BBB. the placenta and passes into breast milk (concentration reaches about 1% of the level in the mother’s blood). T _1/2 is 2-3 hours and is increased in patients with congestive heart failure and in patients with renal insufficiency up to 3,5-32 h The volume of distribution is 0.7 l / kg and clearance -. 56 l / h. Treated biotransformation in the liver with the formation of a disulfide dimer of captopril and captopril – tsisteindisulfida. Excreted mainly by the kidneys (2/3 dose excreted within 4 hours and more than 95% – within 24 hours) as metabolites and unaltered (40-50%).

Application of the substance Captopril

Arterial hypertension (mono – and combination therapy), congestive heart failure, cardiomyopathy, left ventricular dysfunction at steady state in patients after myocardial infarction, diabetic nephropathy and diabetes mellitus type 1 (albuminuria greater than 30 mg / day) .

Contraindications

Hypersensitivity, the presence of medical history information at the previous appointment of ACE inhibitors develop angioedema. hereditary or idiopathic angioedema, primary hyperaldosteronism, pregnancy, breast-feeding.

The combined use of aliskiren with captopril in diabetic patients is contraindicated.

Restrictions on the use

Evaluation of correlation risk – benefit in the following cases: leukopenia, thrombocytopenia, aortic stenosis or other obstructive changes complicating outflow of blood from the heart; hypertrophic cardiomyopathy with a low cardiac output; pronounced renal dysfunction; bilateral renal artery stenosis or stenosis of the artery to a solitary kidney; the presence of transplanted kidneys; hyperkalemia; children’s age.

Application of pregnancy and breastfeeding

is contraindicated in pregnancy.

Category effects on the fetus by FDA – D.

breast-feeding should be discontinued at the time of treatment.

Side effects of substance Captopril

From the nervous system and sensory organs: fatigue, dizziness, headache, depression of the central nervous system. drowsiness, confusion, depression, ataxia, seizures, numbness or tingling in the extremities, blurred vision and / or smell.

From the cardio – vascular system and blood (blood, hemostasis): hypotension, including Orthostatic, angina, myocardial infarction, cardiac arrhythmias (atrial tachycardia – or bradycardia, atrial fibrillation), palpitations, acute ischemic stroke, peripheral edema, lymphadenopathy, anemia, chest pain, pulmonary embolism, neutropenia, agranulocytosis (0, 2% – in patients with impaired renal function, 3.7% – against the background of connective tissue), thrombocytopenia, eosinophilia.

From the respiratory system: bronchospasm, dyspnea, interstitial pneumonitis, bronchitis, non-productive cough.

From the digestive tract: anorexia, taste disturbance, stomatitis, ulcerative lesions of the oral mucosa and of the stomach, dry mouth, glossitis, difficulty swallowing, nausea, vomiting, dyspepsia, flatulence, abdominal pain, constipation or diarrhea, pancreatitis, liver (cholestasis, cholestatic hepatitis, hepatocellular necrosis).

From the of the genitourinary system. impairment of renal function, oliguria, proteinuria, impotence.

For the skin: redness of skin, rash, pruritus, exfoliative dermatitis, toxic epidermal necrolysis, pemphigus, herpes zoster, alopecia, fotodermatit.

Allergic reactions: Stevens – Johnson syndrome, urticaria, angioedema, anaphylactic shock, etc..

Other: fever, chills, sepsis, arthralgia, hyperkalemia, gynecomastia, serum sickness, increase in blood liver enzymes, BUN, acidosis, positive reaction when testing for antibodies to nuclear antigen.

Interaction

Strengthens possible hypotensive effect of anesthetics. It reduces secondary hyperaldosteronism and hypokalemia caused by diuretics. Increases concentration of digoxin and lithium plasma. Effects strengthen other antihypertensives, including beta – blockers, including when systemic absorption of ophthalmic dosage forms, diuretics, clonidine, narcotic analgesics, antipsychotics, alcohol, weaken – estrogens, NSAIDs. sympathomimetics, antacids (reduced bioavailability by 45%). Potassium-sparing diuretics, cyclosporine, kalisodergaszczye medicines and supplements, salt substitutes, milk with a low salt content increases the risk of hyperkalemia. Drugs that suppress bone marrow function (immunosuppressants, cytostatics and / or allopurinol), increase the risk of neutropenia / agranulocytosis or fatal. Do dampening effect of alcohol on the central nervous system. Probenecid slows excretion of captopril in the urine.

Overdose

Symptoms: acute hypotension, cerebrovascular accident, myocardial infarction, thromboembolism, angioedema.

Treatment: a dose reduction or complete removal of the drug; gastric lavage, the patient in a horizontal position, carrying out measures to increase BCC (isotonic sodium chloride solution, transfusion, etc. blood liquids.), symptomatic therapy: epinephrine (n / c or / in), antihistamines, hydrocortisone (in / ). Hemodialysis, if necessary, use an artificial pacemaker.

Dosing and Administration

Inside, for 1 hour before meals. When hypertension: the initial dose – 12.5 mg 2 times a day, if necessary, a single dose increased to 50 mg 3 times a day at intervals of 2-4 weeks; maintenance dose of 25 mg 2-3 times a day; the maximum daily dose – 150 mg. If renovascular hypertension and renal: the initial dose – 6.25 mg 3 times a day, keeping – 25 mg 3 times a day. In chronic heart failure, post-MI: the initial dose – 6.25 mg 3 times a day with the subsequent increase (every 2-3 weeks) to a maintenance dose of 25 mg 2-3 times daily or to 50 mg 3 times a day (post-MI). The maximum daily dose – 150 mg. If the kidney function: starting dose of 6.25 mg 2-3 times a day with the subsequent increase of the maximum dose depends on creatinine clearance: the clearance 35-130 ml / min / 1.73 m 2 – 150 mg of 20-35 ml / min / 1.73 m 2 – 75 mg, less than 20 ml / min / 1.73 m 2 – 37.5 mg.

Precautions substance Captopril

The treatment is carried out under regular medical supervision. Prior to treatment (for 1 week) previous antihypertensive therapy should be discontinued. In patients with malignant hypertension over every 24 hours, gradually increase the dose until the maximum effect under the control of blood pressure. During treatment requires monitoring of blood pressure. peripheral blood (prior to treatment, during the first 3-6 months of treatment and at regular intervals thereafter until 1 year, especially in patients with an increased risk of neutropenia), protein levels, potassium in plasma urea nitrogen, creatinine, renal function, weight body, diet. With the development of hyponatremia, dehydration requires correction dosing regimen (dose reduction). Urticaria maculopapular or (rarely) a rash occurs during the first 4 weeks of treatment, disappear with decreasing doses, withdrawal of the drug and administration of antihistamines. Dose-related neutropenia develops within 3 months after initiation of therapy (the maximum decrease in the number of white blood cells is observed for 10-30 days and lasts for about 2 weeks after discontinuation of the drug). Cough (often observed in women) often appears in the first week (from 24 hours to several months) therapy is maintained during the treatment and is terminated several days after termination of therapy. Violation of taste and reversible decrease in body weight and restored after 2-3 months of therapy. Care should be taken when carrying out surgical procedures (including dental), especially when using general anesthetics that have a hypotensive effect. With the development of cholestatic jaundice and progression of fulminant hepatic necrosis treatment should be discontinued. You should avoid hemodialysis through high-performance membranes poliakrilonitrilmetaallilsulfata (eg N69), hemofiltration or LDL – apheresis (development of anaphylaxis or anaphylactoid reactions). Hyposensitization therapy can increase the risk of anaphylactic reactions. Recommended that the use of alcoholic beverages during treatment. Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention.

Cautions

When you miss a dose do not double the subsequent dose. During the test acetonuria possible positive results.