Composition, form of production and packaging
Tablets from light pink with marbling to pink with a touch of orange with marbling, round, with chamfers, with a smooth surface and a risk on one side; on the side of the risks the plane of the tablet is chamfered inside.
1 tab.
spirapril hydrochloride monohydrate 6.21 mg,
in t.ch. spirapril hydrochloride 6 mg
Auxiliary substances: lactose monohydrate - 99.77 mg, corn starch - 22.5 mg, povidone K30 - 3 mg, glycine hydrochloride - 3 mg, alginic acid - 13 mg, silicon dioxide colloid - 1.5 mg, magnesium stearate - 1.2 mg, iron dye oxide red (E172) 0.03 mg.
10 pieces. - blisters (3) - packs of cardboard.
Tablets from light pink with marbling to pink with a touch of orange with marbling, round, with chamfers, with a smooth surface and a risk on one side; on the side of the risks the plane of the tablet is chamfered inside.
1 tab.
spirapril hydrochloride monohydrate 6.21 mg,
in t.ch. spirapril hydrochloride 6 mg
Auxiliary substances: lactose monohydrate - 99.77 mg, corn starch - 22.5 mg, povidone K30 - 3 mg, glycine hydrochloride - 3 mg, alginic acid - 13 mg, silicon dioxide colloid - 1.5 mg, magnesium stearate - 1.2 mg, iron dye oxide red (E172) 0.03 mg.
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2010.
PHARMACHOLOGIC EFFECT
ACE inhibitor - an enzyme that catalyzes the conversion of angiotensin I into angiotensin II. Angiotensin II shows a powerful vasoconstrictor effect, increases the excretion of potassium and delays the excretion of sodium.
Spirapril has antihypertensive, vasodilating, cardioprotective and natriuretic effects, primarily affecting the renin-angiotensin-aldosterone system; it also promotes the release of biologically active substances that have natriuretic and vasodilating effects (prostaglandins E1 and E2, endothelial relaxation factor, atrial natriuretic factor) and reduces the formation of arginine-vasopressin and endothelin-1, which have vasoconstrictive properties.
The effect of the drug develops within 1 hour after administration, reaches a maximum after 4-8 hours and lasts about 24 hours.
PHARMACOKINETICS
Suction
After taking the drug, the absorption from the gastrointestinal tract is 45%. Absolute bioavailability of spirapril is approximately 50%, spiraprilata - 70%. C max in blood plasma spirapril achieved after 45-90 min, spiraprilata - after 2-3 hours.
Distribution
The binding with plasma proteins of spirapril and its active metabolite is 90%.
Metabolism
Biotransformiruetsya in the liver with the formation of an active metabolite - spiraprilata.
Excretion
It is excreted in the urine (40%) and feces (51%) unchanged and in the form of metabolites. T 1/2 is 2 hours for the first phase of excretion and 40 hours for the second phase.
INDICATIONS
- arterial hypertension;
- chronic heart failure (as part of combination therapy).
DOSING MODE
The drug is taken orally, regardless of food intake, with a sufficient amount of liquid, without chewing.
With arterial hypertension and chronic heart failure, the initial daily dose of the drug is 3 mg (1/2 tab.). If necessary, the daily dose can be increased to 6 mg (1 tab.).The maintenance dose is, on average, 6 mg (1 tab.) Per day. The maximum daily dose is 6 mg.
The duration of the course of treatment is determined by the doctor individually.
For patients with impaired renal function ( KK 10-30 ml / min), the recommended daily dose is 3 mg (1/2 tab.), Which is taken in the morning. Treatment begins only under the condition of careful medical supervision of the patient. Depending on the parameters of kidney function, the daily dose of the drug can be maximally increased in single reasonable cases up to 6 mg (1 tab.), Which is taken in the morning.
In patients with moderate renal dysfunction (CK 30-60 ml / min), a violation of liver function , as well as in elderly patients, dose reduction is not required.
SIDE EFFECT
From the side of the cardiovascular system : a decrease in blood pressure, orthostatic hypotension; rarely - faint; in isolated cases - tachycardia, arrhythmias, angina pectoris, myocardial infarction, increased manifestations of peripheral circulatory insufficiency, exacerbation of Raynaud's disease.
From the side of the urinary system: hypercreatininaemia, development or strengthening of chronic renal failure, proteinuria.
From the central nervous system and peripheral nervous system: cerebral stroke, dizziness, headache, weakness; when used in high doses - insomnia, anxiety, depression, confusion, paresthesia, sleep disorders, imbalance.
On the part of the sense organs : violations of the vestibular apparatus, hearing and vision impairment, noise in the ears, changes in taste or temporary loss of taste.
On the part of the digestive system : nausea, diarrhea, cholestatic jaundice, dyspepsia, constipation, decreased appetite, stomatitis, glossitis, dry mouth, increased activity of hepatic transaminases, hyperbilirubinemia; in isolated cases - intestinal obstruction, violations of liver function, hepatitis, pancreatitis and progressive necrosis of the liver (up to a lethal outcome).
On the part of the respiratory system: dry cough, pulmonary infiltrates, bronchospasm, dyspnea, rhinitis, rhinorrhea, sinusitis, pharyngitis, dysphonia.
Allergic reactions : skin rash, itching, urticaria, photosensitivity, angioedema, facial edema, extremities, lips, tongue, glottis and / or larynx, erythema multiforme, exfoliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis ( Lyell's syndrome); in isolated cases - angioedema of the intestine.
On the part of the hematopoiesis system: anemia, leukopenia, thrombocytopenia; rarely - eosinophilia; in isolated cases - agranulocytosis, pancytopenia, hemolysis.
On the part of metabolism: increased urea, hyperkalemia, hyponatremia.
Other : alopecia, onycholysis, decreased potency; in isolated cases - increased titer of antinuclear antibodies.
CONTRAINDICATIONS
- angioedema in history on the background of the administration of ACE inhibitors;
- hereditary or idiopathic angioedema;
- Pregnancy;
- lactation period (breastfeeding);
- age under 18 years (efficiency and safety not established);
- Hypersensitivity to the components of the drug.
Caution should be given to the drug with bilateral renal artery stenosis, single-kidney artery stenosis, pronounced renal dysfunction (KC <10 ml / min), condition after kidney transplantation, stenosis of the aortic or mitral valve, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism, systemic connective diseases tissue (eg SLE, scleroderma), impaired liver function, cerebrovascular and cardiovascular diseases (including cerebral circulatory insufficiency, coronary heart disease, coronary artery disease rnaya failure), inhibition of bone marrow hematopoiesis, diabetes, hyperkalemia, a diet with sodium restriction, for conditions involving reduction bcc (including diarrhea, vomiting), and elderly patients.
PREGNANCY AND LACTATION
Quadropril В® is contraindicated in pregnancy.
If you need to use Quadropril during lactation, breastfeeding should be discontinued.
If on a background of treatment Квадроприлом there was a pregnancy, therapy should be canceled, since. when taking Quadropril, intrauterine damage to the fetus may occur (renal impairment, fetal and newborn blood pressure lowering, renal dysfunction, hyperkalemia, skull hypoplasia, oligohydramnion, limb contracture, skull deformity, lung hypoplasia).
APPLICATION FOR FUNCTIONS OF THE LIVER
With care Quadropril В® should be used for severe kidney damage (KK 10-30 ml / min). The drug is contraindicated for use with QC less than 10 ml / min.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With care, Quadropril В® should be used for violations of liver function.
APPLICATION FOR CHILDREN
The effectiveness and safety of the use of the drug to 18 years are not established.
APPLICATION IN ELDERLY PATIENTS
In elderly patients, dose reduction is not required.
SPECIAL INSTRUCTIONS
Arterial hypotension, which occurred after taking the first dose, is not a contraindication for the further use of Quadropril (after normalization of blood pressure, subsequent regular administration does not lead to arterial hypotension).
In patients with renovascular hypertension, it is necessary to systematically monitor the creatinine and urea levels in the plasma.
Patients with autoimmune diseases need regular monitoring of the number of leukocytes in the blood.
The appointment on the background of hyperkalemia should be carried out under the control of the concentration of potassium in the blood plasma.
When performing surgical interventions using general anesthesia in patients taking Quadropril В® , there may be a marked decrease in blood pressure. Before general anesthesia, an anesthesiologist should be warned about the use of ACE inhibitors.
During treatment Quadropril can not be used for hemodialysis or hemofiltration membranes containing polyacrylonitrile-metal-sulfonate (for example, AN69), since there is a risk of reactions of hypersensitivity up to the development of shock, threatening the life of the patient. In case of emergency dialysis or hemofiltration, before the procedure, the patient is prescribed another antihypertensive drug (not an ACE inhibitor) or another dialysis membrane is used.
During the conduct of plasmapheresis with dextran sulfate, concomitant therapy with an ACE inhibitor may lead to hypersensitivity reactions that threaten the patient's life.
During desensitizing therapy aimed at eliminating the symptoms caused by the poison of insects (bee or wasp stings), anaphylactic reactions can sometimes develop against the background of an ACE inhibitor, sometimes threatening the patient's life (lowering blood pressure, dyspnea, vomiting, allergic skin rash).
The treatment is carried out under constant medical supervision.
In patients with reduced bcc in the body (due, for example, to vomiting, diarrhea, diuretics), weakening of the contractility of the heart or malignant hypertension at the beginning of treatment Quadropril may experience a sharp drop in blood pressure. If possible, before beginning treatment with Quadropril, you should make up for the deficiency of BCC in the body or limit the therapy with diuretics and, if necessary, cancel them.
To avoid an unpredictable sharp drop in blood pressure after taking the first dose, as well as after increasing the dose of diuretics and / or increasing the dose of Quadropril, these patients are prescribed medical supervision for at least 6 hours.
Due to the fact that angioedema of the face, extremities, lips, tongue, larynx or pharynx is observed with ACE inhibitors in rare cases, the appearance of this adverse reaction is possible when taking Quadropril. In this case, treatment with QUADROIPLE should be stopped immediately and the patient's condition monitored until the edema completely disappears. Even in the case of swelling of the tongue without breathing, it may take a long time to monitor the patient's condition and take emergency measures, as in very rare cases, the edema of the tongue and larynx were fatal.
When swelling of tissues involving the larynx, pharynx and / or tongue, epinephrine should be injected urgently at a dose of 0.3-0.5 mg or slowly iv in a dose of 0.1 mg under the control of ECG and AD, then prescribe SCS. After this, the administration of antihistamines (blockers of histamine H 1 -receptors) is recommended.
In patients with malignant arterial hypertension or with heart failure, Quadrapril therapy is started in the hospital.
During the treatment it is necessary to refrain from taking ethanol.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: marked decrease in blood pressure, bradycardia, collapse, shock, disturbance of water-electrolyte balance, acute renal failure.
Treatment: symptomatic (gastric lavage, the appointment of adsorbent substances). In severe cases - hospitalization and maintenance of vital body functions in a hospital.
To remove the drug from the body, you can conduct a hemodialysis session. With arterial hypotension, first of all, replenish BCC in / in infusion of physiological solution. If necessary, in addition to / in catecholamines are administered. With a pronounced bradycardia, which is not stopped with the help of drugs, an artificial pacemaker is implanted. It is necessary to control the concentration of electrolytes and creatinine in the blood.
DRUG INTERACTION
Antihypertensive drugs (especially in combination with diuretics), hypnotics, means for general anesthesia intensify the hypotensive effect of Quadropril.
NSAIDs (eg, acetylsalicylic acid, indomethacin), incl. and COX-2 inhibitors, can weaken the hypotensive effect of Quadropril.
With the simultaneous use of Quadropril with potassium preparations, potassium-sparing diuretics (eg, spironolactone, amiloride, triamterene), as well as heparin, the risk of hyperkalemia increases.
Quadropril В®, when used simultaneously with lithium salts, causes an increase in the concentration of lithium in the blood plasma (a systematic control of the concentration of lithium in the blood serum is necessary).
When joint application of Quadropril with allopurinol, procainamide, as well as drugs that suppress the protective reactions of the body (cytostatic, immunosuppressive agents, GCS for systemic use), the risk of developing leukopenia increases.
Quadropril В® enhances the hypoglycemic action of insulin, oral hypoglycemic agents (biguanides, sulfonylurea derivatives).
When applied simultaneously with estrogens or table salt, the antihypertensive effect of Quadropril is reduced.
Simultaneous administration of quadropril and ethanol leads to an increase in the action of ethanol.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
