Blockordil
Blockordil: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Blokordil
ATX code: C09AA01
Active ingredient: captopril (Captopril)
Manufacturer: KRKA d.d. (KRKA, dd) (Slovenia)
Description and photo update: 2019-11-07
Blocordil is an antihypertensive drug, an angiotensin-converting enzyme (ACE) inhibitor.
Release form and composition
The drug is produced in the form of tablets: white, round, slightly biconvex, with a chamfer, on one side of the 25 mg and 50 mg tablets there is a dividing risk (10 pieces in blisters, in a cardboard box 2 blisters and instructions for use of Blockordil).
1 tablet contains:
- active substance: captopril - 12.5; 25 or 50 mg;
- auxiliary components: corn starch, lactose monohydrate, stearic acid, microcrystalline cellulose.
Pharmacological properties
Pharmacodynamics
Blockordil is an antihypertensive drug, the active ingredient of which is captopril, which is an ACE inhibitor. The mechanism of action of the drug is due to the ability of captopril to competitively inhibit the activity of ACE, causing a decrease in the rate of conversion of angiotensin I to angiotensin II. Angiotensin II, along with a pronounced vasoconstrictor effect, stimulates the secretion of aldosterone in the adrenal cortex. Reducing the formation of angiotensin II, reduces its content in the adrenal cortex and helps to reduce the release of aldosterone. In addition, the effect of captopril on the kinin-kallikrein system is supposed, which prevents the breakdown of bradykinin. Increases coronary and renal blood flow.
The antihypertensive effect does not depend on the level of renin activity in plasma; blood pressure (BP) decreases both with normal and with a reduced concentration of the hormone. This is due to the effect of captopril on the tissue renin-angiotensin-aldosterone system (RAAS).
The vasodilating effect of Blockordil helps to reduce resistance in the pulmonary vessels, OPSS (total peripheral vascular resistance) and wedge pressure in the pulmonary capillaries, or post- and preload on the heart. Increases cardiac output and exercise tolerance. Against the background of prolonged use, the severity of left ventricular myocardial hypertrophy decreases, the progression of heart failure is prevented, the development of left ventricular dilatation slows down. In chronic heart failure, it helps to reduce sodium concentration. The arteries expand to a greater extent than the veins. It causes an improvement in the blood supply to the ischemic myocardium, a decrease in platelet aggregation.
By lowering the tone of the efferent arterioles of the renal glomeruli, captopril improves intraglomerular hemodynamics, which prevents the occurrence of diabetic nephropathy.
In a daily dose of 50 mg, Blockordil exhibits angioprotective properties against the vessels of the microvasculature, slowing down the progression of chronic renal failure (CRF) in patients with diabetic nephroangiopathy.
A decrease in blood pressure leads to a decrease in myocardial oxygen demand and is not accompanied by reflex tachycardia.
After taking Blocordil inside the maximum decrease in blood pressure occurs in 1-1.5 hours. The antihypertensive effect reaches optimal values after 14–28 days of therapy and is dose-dependent.
Pharmacokinetics
After taking Blocordil, the absorption of captopril occurs quickly, on an empty stomach the degree of absorption reaches 75%, and when taken with meals it decreases by 30-40%. Bioavailability is 35-40%. The maximum concentration in blood plasma is reached in 0.5-1.5 hours and is 114 ng / ml.
Plasma protein binding (mainly albumin) - 25-30%.
The blood-brain and placental barrier overcomes less than 1% of the dose taken. It is secreted in breast milk.
It is metabolized in the liver with the formation of pharmacologically inactive metabolites - captopril-cysteindisulfide and captopril disulfide dimer.
The half-life (T 1/2) is 3 hours.
Excreted through the kidneys 95% of the dose, including unchanged - 40-50%. After a single oral administration after 4 hours, 38% of captopril is determined unchanged in the urine and 28% in the form of metabolites, after 6 hours only metabolites are present in the urine. In daily urine, the proportion of unchanged captopril is 38%, and in the form of metabolites - 62%.
In case of impaired renal function, T 1/2 captopril increases to 33 hours. In chronic renal failure, the substance accumulates.
In elderly patients, the pharmacokinetics of captopril does not change, therefore, in the absence of impaired renal function, elderly people with hypertension are advised to take the usual doses of Blocordil.
Indications for use
- arterial hypertension (including renovascular hypertension);
- chronic heart failure (as part of combination therapy);
- impaired left ventricular function after myocardial infarction (for patients in a clinically stable state);
- diabetic nephropathy against the background of type 1 diabetes mellitus (with daily albuminuria more than 30 mg).
Contraindications
Absolute:
- hereditary angioedema or idiopathic edema;
- the presence of indications in the history of angioedema that occurs during therapy with other ACE inhibitors;
- hemodynamically significant bilateral stenosis of the renal arteries, stenosis of the artery of a single kidney with azotemia;
- porphyria;
- lactose intolerance, glucose-galactose malabsorption syndrome, lactase deficiency;
- age up to 18 years;
- period of pregnancy and lactation;
- hypersensitivity to other ACE inhibitors (including history) and drug components.
It is recommended to prescribe Blocordil tablets with caution in case of hemodynamically significant aortic stenosis, cerebrovascular diseases (including cerebral circulation insufficiency, cerebral ischemia), inhibition of bone marrow hematopoiesis, renal failure, condition after kidney transplantation, liver failure, diabetes mellitus, connective tissue diseases, limiting the consumption of table salt, reduced circulating blood volume (BCC), including in conditions such as diarrhea and vomiting, causing a decrease in BCC, as well as in old age.
Blockordil, instructions for use: method and dosage
Blockordil tablets are taken orally with a small amount of liquid, 1 hour before meals or 2 hours after meals, regularly, preferably always at the same time of day.
Recommended dosage of Blocordil:
- arterial hypertension: initial dose - 12.5 mg 2 times a day. If after 14 days of admission there is no sufficient therapeutic effect, then the initial dose is gradually (with an interval of 14-28 days) increased until the optimal effect is achieved. For mild to moderate arterial hypertension, the maintenance dose is usually 25 mg 2 times a day. The maximum dose is 50 mg 2 times a day. The maintenance dose for severe hypertension is 50 mg 3 times a day, the maximum daily dose is 150 mg;
- malignant arterial hypertension: initial dose - 12.5 mg or 25 mg 2-3 times a day;
- chronic heart failure: the initial dose is 12.5 mg 2-3 times a day. If necessary, it can be increased gradually (with an interval of 14–28 days). The average maintenance dose of Blocordil can be 25-50 mg 2-3 times a day. The maximum dose is 150 mg per day;
- dysfunction of the left ventricle, which arose against the background of a previous myocardial infarction: treatment should be started from 3 to 16 days after myocardial infarction with an initial dose of 6.25 mg once a day (captopril tablets with a risk of 12.5 mg can be used) … If necessary, the dose can be gradually increased (with an interval of at least 14 days) to 50 mg 3 times a day;
- diabetic nephropathy: 75-100 mg per day, divided into 2-3 doses. For patients with type 1 diabetes mellitus with microalbuminuria (daily release of albumin 30–300 mg), the drug is prescribed at a dose of 50 mg 2 times a day. If the total protein clearance per day is more than 500 mg, then a dose of 25 mg 3 times a day is effective.
In case of impaired renal function, the daily dose of Blocordil is determined taking into account creatinine clearance (CC):
- CC not less than 30 ml / min (moderate renal dysfunction): 75-100 mg;
- CC less than 30 ml / min: the initial daily dose is up to 12.5 mg, if necessary, its gradual increase is possible.
Recommended dosage for elderly patients: 6.25 mg 2 times a day.
If necessary, Blocordil can be used in combination with loop diuretics.
The missed intake of the next dose cannot be replenished by a one-time increase in the next dose.
Side effects
- on the part of the cardiovascular system: rarely - a pronounced decrease in blood pressure, tachyarrhythmia, tachycardia, palpitations, exertional angina, peripheral edema; very rare: Raynaud's syndrome, cardiogenic shock, cardiac arrest;
- from the nervous system: often - taste disturbances, sleep disorders, dizziness; rarely - feeling tired, drowsiness, general weakness, paresthesia, headache, asthenia; very rarely - depression, confusion, cerebrovascular disorders (including fainting, stroke);
- from the respiratory system: often - dry irritating cough (unproductive), bronchospasm, shortness of breath; very rarely - rhinitis, allergic alveolitis, eosinophilic pneumonitis;
- on the part of the hematopoietic and lymphatic system: very rarely - thrombocytopenia, eosinophilia, lymphadenopathy, neutropenia, agranulocytosis, anemia (aplastic or hemolytic), pancytopenia (more often with impaired renal function);
- from the immune system: very rarely - autoimmune diseases, increased titers of antinuclear antibodies;
- from the digestive system: often - dryness of the oral mucosa, abdominal pain, nausea, vomiting, diarrhea, constipation, gastritis; rarely - aphthous ulcers of the inner surface of the cheeks and tongue, hyperbilirubinemia; very rarely - peptic ulcers, glossitis, pancreatitis, cholestasis, jaundice, liver dysfunction, intestinal angioedema, hepatitis (including necrotizing hepatitis), increased activity of hepatic transaminases;
- from the senses: very rarely - visual impairment;
- on the part of the skin: often - itching, skin rash, alopecia; rarely - angioedema; very rarely - urticaria, exfoliative dermatitis, Stevens-Johnson syndrome, erythema multiforme, photosensitivity (erythema), pemphigoid skin reactions;
- on the part of the musculoskeletal system: very rarely - arthralgia, myalgia;
- from the urinary and reproductive systems: rarely - frequent urination, renal dysfunction, oliguria, polyuria; very rarely - nephrotic syndrome, gynecomastia, impotence;
- laboratory indicators: very rarely - increased hematocrit, proteinuria, increased levels of urea, bilirubin and creatinine, hyperkalemia, hyponatremia, increased erythrocyte sedimentation rate, leukopenia;
- others: infrequently - weakness, chest pain; very rarely - fever.
Overdose
- symptoms: severe drop in blood pressure (including sudden cardiovascular failure, loss of consciousness and the threat of death), acute cerebrovascular accident, myocardial infarction, thromboembolic complications;
- treatment: immediate gastric lavage or artificial vomiting, taking activated charcoal. The patient should be placed on his back with his legs raised. Intravenous (iv) administration of 0.9% sodium chloride solution is shown, measures are taken to increase the BCC and restore blood pressure. Symptomatic therapy involves subcutaneous or intravenous administration of epinephrine, the appointment of antihistamines. Conducting a hemodialysis session and using peritoneal dialysis are ineffective.
special instructions
Blockordil at a dose of 25 mg can be administered sublingually once to lower blood pressure in hypertensive crisis, the tablet should be chewed and left under the tongue until completely absorbed. If no sufficient hypotensive effect is observed within one hour, the drug should be taken again at a dose of 25 mg in the same way.
There is a risk of arterial hypotension after taking the first dose of Blocordil, it increases with a reduced BCC or hyponatremia due to the use of high doses of diuretics or hemodialysis. Symptoms of arterial hypotension include nausea and fainting, with a pronounced decrease in blood pressure - acute renal failure, including death.
To prevent the development of arterial hypotension, it is recommended to start treatment with Blocordil after stopping the diuretic and a salt-free diet.
If episodes of symptomatic arterial hypotension are repeated, it is necessary to reduce the dose of Blocordil or discontinue drug therapy.
Captopril can reduce renal function up to acute renal failure, therefore, treatment should be accompanied by regular monitoring of the genitourinary system.
It should be borne in mind that in elderly patients, the risk of developing side effects is increased.
While taking Blocordil, the likelihood of developing hyperkalemia is high, the risk group includes patients with chronic renal failure, diabetes mellitus, who are on concomitant therapy with potassium-sparing diuretics (including spironolactone, amiloride, triamterene) or potassium preparations. In this regard, the simultaneous reception of Blocordil with the indicated funds is not recommended. If it is necessary to combine it with potassium preparations, the patient must ensure regular studies for the content of potassium in the blood serum.
It is recommended to periodically monitor the number of leukocytes in the blood. When prescribing Blocordil, the doctor should inform the patient about the need for immediate medical attention if a sore throat, fever or other signs of an infectious disease occurs.
Patients with diabetes mellitus may need to adjust the dose of insulin or oral hypoglycemic agents for oral administration.
Before carrying out desensitizing therapy with hymenoptera venom (bees, wasps), the ACE inhibitor should be stopped at least 24 hours before the start of the procedure. This will reduce the risk of developing anaphylactoid reactions.
Temporary withdrawal of the drug is required before each procedure for apheresis of low-density lipoproteins using high-flow membranes or elective surgery. The patient must inform the anesthesiologist about the use of Blocordil.
Patients should be aware that a false positive reaction may occur when urine is analyzed for acetone while taking captopril.
Influence on the ability to drive vehicles and complex mechanisms
Given the possibility of an excessive decrease in blood pressure, the development of dizziness and other side effects that negatively affect the concentration of attention and the speed of psychomotor reactions, during the period of treatment with Blocordil, care must be taken both when driving vehicles and when performing other potentially dangerous activities.
Application during pregnancy and lactation
The use of Blockordil is contraindicated during the period of gestation and breastfeeding.
Pediatric use
The safety and efficacy of captopril under the age of 18 has not been established, therefore it is contraindicated to use Blockordil in pediatric practice.
With impaired renal function
The appointment of Blocordil is contraindicated in patients with hemodynamically significant bilateral renal artery stenosis or stenosis of an artery of a single kidney with azotemia.
The drug should be taken with caution in case of renal failure and condition after kidney transplantation. Dose adjustment of Blocordil is required based on QC indicators.
For violations of liver function
It is contraindicated to prescribe Blocordil for porphyria.
Captopril should be taken with caution in liver failure.
Use in the elderly
Care should be taken when taking Blocordil to elderly patients, they must strictly follow the recommended dosing regimen.
Drug interactions
- nonsteroidal anti-inflammatory drugs (including indomethacin, selective inhibitors of cyclooxygenase-2), estrogens: against the background of concomitant therapy with these drugs, the hypotensive effect of Blockordil is weakened;
- potassium-sparing diuretics, potassium supplements, potassium food supplements, salt substitutes: increase the risk of hyperkalemia;
- general anesthesia drugs: can cause a significant decrease in blood pressure;
- lithium preparations: the elimination of lithium preparations slows down, which leads to an increase in the level of lithium concentration in the blood;
- allopurinol, procainamide: increase the risk of neutropenia, Stevens-Johnson syndrome;
- gold preparations: intravenous administration of sodium aurothiomalate can potentiate the development of a symptom complex, including nausea, vomiting, facial flushing and lowering blood pressure;
- insulin, oral hypoglycemic agents: the interaction of captopril with hypoglycemic agents increases the risk of hypoglycemia;
- antacids: slow down the absorption of captopril in the gastrointestinal tract;
- ethanol: against the background of taking ethanol-containing drugs and drinking alcoholic beverages, the hypotensive effect of Blockordil increases;
- aldesleukin, alprostadil, alpha1-blockers, beta-blockers, diuretics, slow calcium channel blockers, cardiotonics, centrally acting alpha2-adrenergic agonists, minoxidil, nitrates, vasodilators, muscle relaxants: it should be borne in mind that the combination with the listed drugs potentiates hypotensive action;
- hypnotics, antidepressants, anxiolytics, antipsychotics: can enhance the hypotensive effect of Blockordil;
- epoetin, glucocorticosteroids, estrogens (including combined oral contraceptives), carbenoxolone, naloxone: concomitant therapy with these agents reduces the activity of Blockordil;
- probenecid: helps to reduce the renal clearance of captopril and increase its serum concentrations;
- azathioprine, cyclophosphamide: Taking these and other immunosuppressants increases the risk of hematological disorders.
Analogs
The analogues of Blockordil are Captopril, Captopril Sandoz, Captopril-AKOS, Captopril-STI, Captopril-Ferein, Captopril-FPO, Angiopril-25, Vero-Captopril, Capoten, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Blockordil
Isolated reviews of Blockordil are positive. Patients prefer to use it if it is necessary to bring down high blood pressure for a short time, but I recommend using it with not very high pressure surges.
The price of Blockordil in pharmacies
The registration of the drug has not been renewed, and therefore it is not available in the pharmacy chain, therefore the price of Blocordil is unknown.
The cost of Captopril, an analogue with the same active ingredient, depending on the dosage, can be:
- tablets 25 mg, 10 pcs. in blisters: 2 blisters in a package - 8–26 rubles; 4 blisters in the package - 12–34 rubles;
- tablets 50 mg 10 pcs. in blisters: 2 blisters in the package - 13–35 rubles; 4 blisters in the package - 28–56 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
