AKRIPAMID RETARD
Active material: Indapamid
When ATH: C03BA11
CCF: Diuretic. Antihypertensive drugs
ICD-10 codes (testimony): I10
Manufacturer: Chemical-Pharmaceutical Plant JSC QUINACRINE (Russia)
PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING
Sustained-release tablets, coated white or white with kremovatam or serovatam brown color, round, lenticular.
| 1 tab. | |
| indapamid | 1.5 mg |
Excipients: ludipress, hydroxypropyl (gipromelloza), colloidal silicon dioxide (aэrosyl), magnesium stearate, polyethylene glycol (macrogol), glycerol (glycerol), Titanium dioxide, talc, lactose.
10 PC. – packings Valium planimetric (3) – packs cardboard.
10 PC. – packings Valium planimetric (6) – packs cardboard.
Pharmacological action
Antihypertensive drugs, diuretic, has vazodilatiruta activity. The pharmacological properties close to tiazidnam from other dioretikam. Violates reabsorbqiyu sodium ions in korticalnom segment hinges genle. Increases the excretion of urine sodium ions, chlorine, less, – potassium and magnesium ions. With its ability to selectively block slow calzieve channels, increases the elasticity of the walls of the arteries and reduces round. Reduces left ventricular hypertrophy.
No impact on lipid and carbohydrate exchanges (incl. patients with diabetes), does not violate the sensitivity peripheral tissues to insulin.
Reduces the sensitivity of the vascular wall to norarenalino and Angiotensin II, stimulates the synthesis of prostaglandin e2, decreases products free and stable oxygen radicals.
Gipotenzivny effect develops by the end of the first week, It persists for 24 h on the background of a single admission.
Pharmacokinetics
Absorption
Once inside quickly and completely absorbed from the gastrointestinal tract. High Bioavailability – 93%. Eating slows down the absorption rate, but does not affect the number of substances vsosavchegosa. After oral administration, Cmax plasma levels achieved after 12 no. Repeated receptions fluctuations of drug concentration in the blood plasma in the interval between meals two doses reduced.
Distribution
The equilibrium state is established through 7 regular admission days. The binding to plasma proteins – 79%. Associated with elastin and smooth muscle of the vascular wall.
Has a large Vd , It penetrates the blood-tissue barriers (incl. placental), excreted in breast milk. Not accumulates.
Metabolism and excretion
It is metabolized in the liver.
T1/2 – 18 no. The kidneys remove 60-80% as metabolites, in unchanged form – about 5%, through the intestine – 20%.
Pharmacokinetics in special clinical situations
In patients with renal insufficiency pharmacokinetics unchanged.
Testimony
- Arterial hypertension.
Dosage regimen
The drug is administered orally at a dose 1.5 mg (predominantly in the morning).
Tablets should be taken with liquid, drinking plenty of fluids.
Side effect
From the digestive system: nausea, anorexia, dry mouth, gastralgia, vomiting, diarrhea, constipation, abdominal pain, the development of hepatic encephalopathy; rarely – pancreatitis.
CNS: asthenia, nervousness, headache, dizziness, drowsiness, vertigo, insomnia, depression; seldom-fatigue, generalized weakness, malaise, muscle spasm, tension, irritability, alarm.
The respiratory system: cough, pharyngitis, sinusitis; rarely – rhinitis.
Cardio-vascular system: orthostatic hypotension, ECG changes (kaliopenia), arrhythmia, heartbeat.
From the urinary system: frequent infections, nocturia, polyuria.
From the hematopoietic system: rarely – thrombocytopenia, leukopenia, agranulocytosis, bone marrow aplasia, gemoliticheskaya anemia.
Allergic reactions: rash, hives, itch, gemorragicheskiy vasculitis.
Laboratory findings: hyperuricemia, giperglikemiâ, kaliopenia, chloropenia, giponatriemiya, hypercalcemia, increase in plasma urea nitrogen, giperkreatininemiя, glycosuria.
Other: the worsening tide of Systemic Lupus Erythematosus.
Contraindications
- Hypokalemia;
- Severe renal insufficiency (Stage anurii);
- Severe hepatic impairment (incl. encephalopathy);
- Concomitant use of drugs, extension QT interval;
- Lactose intolerance;
- Galactosemia;
malabsorption syndrome of glucose/Galactose;
- Pregnancy;
- Lactation (breast-feeding);
- Up to 18 years (efficacy and safety have not been established);
-hypersensitivity to the drug and other derivative sulfonamida.
FROM caution prescribed for violations of the liver and / or kidney, violation vodno-elektrolitnogo balance, giperparatireoze, patients with increased QT interval on the ECG or receiving combination therapy, Diabetes under decompensation, hyperuricemia (especially accompanied by gout and urate nephrolithiasis).
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation (breast-feeding).
Cautions
It should be taken into account, that patients, taking cardiac glycosides, laxatives, against the backdrop of hyperaldosteronism, as well as in the elderly shows regular monitoring of ions potassium and creatinine.
Against the backdrop of the admission Akripamida® retard should systematically monitor the concentration of potassium ions, sodium, magnesium plasma (can develop electrolyte disorders), pH, glucose, uric acid and residual nitrogen.
The most careful control shown in patients with liver cirrhosis (especially with edema or ascites, tk. There is a risk of metabolic alkalosis, increase the expression of hepatic encephalopathy), CHD, Heart Failure, as well as in the elderly.
At risk also include patients with increased QT interval on the ECG (congenital or develop on the background of a pathological process).
The first measurement of the concentration of potassium in the blood should be held during the first week of treatment.
Gipercalziemia against the backdrop of the admission Akripamida® retard may be the consequence of earlier nediagnostirovannogo hyperparathyroidism.
Diabetic patients should monitor the level of glucose in the blood, especially in the presence of hypokalemia.
Considerable dehydration may lead to acute renal failure (reduction in glomerular filtration rate). Patients need to compensate for the loss of water at the beginning of treatment carefully monitor renal function.
Patients with arterial hypertension and hyponatremia (due to diuretics) necessary for 3 the day before you start taking ACE inhibitors stop taking diuretics (If necessary, the admission dioretikov can resume later), or they prescribe ACE inhibitors in low initial doses.
In applying indapamida positive results are possible when conducting doping control.
Effects on ability to drive vehicles and management mechanisms
In some cases the individual reactions, associated with changes in blood pressure, especially at the beginning of treatment and when you add other antigipertenzivnogo tools. As a result of which may decrease the ability to driving and working with machinery, require attention.
Overdose
Symptoms: nausea, vomiting, weakness, dysfunction of the gastrointestinal tract, water and electrolyte disturbances, in some cases – excessive reduction of blood pressure, respiratory depression. Patients with cirrhosis may develop hepatic coma.
Treatment: gastric lavage, Correction fluid and electrolyte balance, simptomaticheskaya therapy. No specific antidote.
Drug Interactions
Together admission Akripamida® retard from saluretikami, cardiac glycosides, glitches- and mineralocorticoid, tetrakozaktidom, amphotericin B (for / in the), laxatives increased risk gipokaliemii.
Together admission Akripamida® retard with cardiac glycosides is increased likelihood digitalisna intoxication.
Together admission Akripamida® retard with drugs calcium increases the likelihood of developing gipercalziemii.
Together admission Akripamida® retard with metformin possible aggravation of molernkislogo azidoza.
Akripamid® retard increases lithium concentration in the blood plasma (by reducing urinary excretion), that increases the risk of nefrotoksicski action last.
Together with the admission Akripamidom® retard astemizola, Erythromycin (for / in the), pentamidine, sultoprida, Terfenadine, vinkamina, Class IA antiarrhythmics (quinidine, disopyramide) and class III (Amiodarone, bretilium, sotalol) Perhaps the type of arrhythmia. “pirouette”.
Together admission Akripamida® retard with NSAIDS, GCS, tetrakozaktidom, sympathomimetic dropping gipotenzivny effect.
Together admission Akripamida® retard with baklofenom amplified gipotenzivne effect.
Combination Akripamida® retard with kalisberegatmi dioretikami may be proved to be effective for some patients, but it is not completely ruled out the possibility of a hypo- or hyperkalemia, especially in patients with diabetes mellitus and renal failure.
Together admission Akripamida® retard ACE inhibitors increase the risk of arterial hypotension, and/or acute renal failure (especially when existing renal artery stenosis).
Together admission Akripamida® retard with are contrasting means in high doses may develop dehydration and increase the risk of violations of the kidney. Before using jodosoderžaŝih contrast patients must recover lost fluids.
Imipraminovye (tricyclic) Antidepressants and antipsychotics increase gipotenzivne effect Akripamida® retard and increase the risk orthostatic hypotension.
Together admission Akripamida® retard with ziklosporinom increases the risk giperkreatininemii.
Akripamid® retard impact proximity effect anticoagulants (coumarin derivatives or indandiona) due to the increasing concentration of coagulation factors by reducing the volume of circulating blood and increase their production by the liver (may require dose adjustment).
Akripamid® retard reinforces embargo neuromuscular transmission, evolving under the influence of nedepoliarizuth miorelaksantov.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored in a dry, protected from light, inaccessible to children at temperature not exceeding 25 ° C. Shelf life – 2 year.
