Universal reference book for medicines
Name of the drug: AKRIPAMID В® (AKRIPAMIDE)

Active substance: indapamide

Type: Diuretic.
Antihypertensive drug
Manufacturer: Chemical-Pharmaceutical Plant Akrihin (Russia)
Composition, form of production and packaging
Tablets covered with a film coating of
white or white with a cream or grayish hue of color, round, biconcave;
roughening is allowed; on the bend - white or almost white.
1 tab.

indapamide 2.5 mg

Excipients: lactose (milk sugar), potato starch, povidone, sodium lauryl sulfate, talc, magnesium stearate.

Sheath composition: hypromellose (hydroxypropylmethylcellulose), macrogol 6000 (polyethylene glycol 6000), glycerol (glycerin), titanium dioxide, talc.

10 pieces.
- packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

The product description was approved by the manufacturer for the 2009 print edition.

PHARMACHOLOGIC EFFECT

Antihypertensive drug, diuretic, has vasodilating activity.
By pharmacological properties close to thiazide diuretics - causes a disruption of the reabsorption of sodium ions in the cortical segment of the Henle loop. Increases excretion in the urine of sodium and chlorine ions and to a lesser extent potassium and magnesium ions.Possessing the ability to selectively block slow calcium channels, increases the elasticity of the walls of the arteries and reduces the OPSS. Helps reduce hypertrophy of the left ventricle of the heart.
Does not affect the content of lipids in plasma (TG, HDL and LDL) and carbohydrate metabolism (including in patients with concomitant diabetes mellitus).

Reduces the sensitivity of the vascular wall to noradrenaline and angiotensin II, stimulates the synthesis of PgE 2 and prostacyclin PgI 2 , reduces the production of free and stable oxygen radicals.

At appointment in high doses does not influence a degree of depression of a BP, despite of an increase in a diuresis.
After repeated administration, the therapeutic effect is observed after 1-2 weeks, reaches a maximum by 8-12 weeks and lasts up to 8 weeks. After taking the drug in a single dose, the maximum effect is observed after 24 hours.
PHARMACOKINETICS

Suction

After oral administration, it is quickly and completely absorbed from the digestive tract.
Bioavailability is high (93%). Eating somewhat slows down the speed, but does not affect the final amount of absorbed drug. C max in the blood is achieved in 1-2 hours.
After taking the drug inside C max at a dose of 5 mg is 260 ng / l.
At repeated receptions of fluctuation of concentration of a preparation in plasma in an interval between receptions of two doses decrease. C ss is achieved after 7 days of regular admission.
Distribution and Metabolism

Binding to plasma proteins is 70-80%.
It also binds to the elastin of the smooth muscles of the vascular wall. Has a large V d .
Penetrates through histohematological (including placental) barriers, excreted in breast milk.

Metabolised in the liver.

Do not cumulate.

Excretion

T 1/2 of indapamide is an average of 14 hours. It is excreted from the body by the kidneys (up to 70%) mainly in the form of metabolites, through the intestine - 20-23%.

Pharmacokinetics in special clinical cases

In patients with renal insufficiency, pharmacokinetics does not change.

INDICATIONS

- arterial hypertension.

DOSING MODE

The drug is administered orally, preferably in the morning, regardless of food intake.

The daily dose is 2.5 mg (1 tab.) If after 4-8 weeks of therapy the desired therapeutic effect is not achieved, the dose of the drug should not be increased (an increased risk of side effects without increasing the antihypertensive effect).
In such cases, it is recommended that another antihypertensive drug that is not a diuretic be included in the drug treatment regimen. In the case of starting treatment with two antihypertensive drugs, the dose of Acrypamide remains 2.5 mg 1 time / day in the morning.
Tablets are taken with a sufficient amount of liquid.

SIDE EFFECT

From the cardiovascular system: orthostatic hypotension, arrhythmia, palpitations.

From the central nervous system and peripheral nervous system: headache, dizziness, nervousness, asthenia, drowsiness, vertigo, insomnia, depression, fatigue, malaise, tension, irritability, anxiety.

On the part of the digestive system: constipation or diarrhea, dyspepsia (including nausea, vomiting), anorexia, dry mouth, abdominal pain, hepatic encephalopathy (against liver failure), pancreatitis.

From the urinary system: nocturia, polyuria.

On the part of the respiratory system: rhinitis, cough, pharyngitis, sinusitis.

Allergic reactions: skin itching, maculopapular rash, hives, hemorrhagic vasculitis.

From the hemopoietic system: thrombocytopenia, leukopenia, agranulocytosis, bone marrow aplasia, hemolytic anemia.

Laboratory indicators: hypercalcemia, hyperuricemia, hypochloraemia, hypokalemia, hyponatremia, hyperglycemia, increased blood urea nitrogen, hypercreatininaemia, glucosuria.

Other: muscle spasm, exacerbation of SLE.

CONTRAINDICATIONS

anuria;

- severe hepatic insufficiency (including with encephalopathy);

- severe renal failure;

- hypokalemia;

- simultaneous reception of drugs that extend the QT interval;

- Pregnancy;

- lactation period (breastfeeding);

- age under 18 years (effectiveness and safety not established);

- lactose intolerance, galactosemia, glucose / galactose absorption disorder syndrome;

- hypersensitivity to the components of the drug;

- hypersensitivity to other sulfonamide derivatives.

Caution should be applied to the preparation for violations of water-electrolyte metabolism, mild and moderate hepatic and / or renal failure, lengthening of the QT interval, hyperuricemia (especially in gout or urate nephrourolythiasis), hyperparathyroidism.

PREGNANCY AND LACTATION

The drug is contraindicated for use in pregnancy and lactation (breastfeeding).

APPLICATION FOR FUNCTIONS OF THE LIVER

Contraindicated in patients with severe renal failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated use in severe hepatic insufficiency (including with encephalopathy).

APPLICATION FOR CHILDREN

Contraindication: age under 18 years (efficacy and safety not established).

APPLICATION IN ELDERLY PATIENTS

The most thorough control is shown in the elderly.

SPECIAL INSTRUCTIONS

Patients receiving cardiac glycosides, laxative drugs, against hyperaldosteronism, as well as elderly patients, are shown careful control of the content of potassium and creatinine ions.

Against the background of the drug Acrypamide should be systematically monitor the concentration of ions of potassium, sodium, magnesium in the plasma (possibly the development of electrolyte disorders), pH, the concentration of glucose, uric acid and residual nitrogen.
The most careful control is indicated in patients with cirrhosis of the liver (especially with edema or ascites - the risk of developing metabolic alkalosis, enhancing the manifestation of hepatic encephalopathy), IHD, chronic heart failure, and also in the elderly. Patients with an increased QT interval on the ECG (congenital or developing against a pathological process) also belong to the high-risk group.
The first determination of the concentration of potassium ions in the blood should be performed during the first week of treatment.

Hypercalcemia on the background of taking the drug Acrypamide may be a consequence of previously undiagnosed hyperparathyroidism.

In patients with diabetes, it is extremely important to monitor blood glucose levels, especially when hypokalemia is present.

Significant dehydration can lead to the development of acute renal failure (reduced glomerular filtration).
It is necessary to compensate for the loss of water and at the beginning of the treatment carefully monitor the kidney function.
On the background of the reception of Acrypamide, positive results are possible during doping control.

Patients with arterial hypertension and hyponatremia (due to taking diuretics) need to stop taking diuretics 3 days before the start of taking ACE inhibitors (if necessary, diuretics can be taken a little later) or they are given initial low doses of ACE inhibitors.

OVERDOSE

Symptoms: nausea, vomiting, weakness, arterial hypotension, dizziness, drowsiness, confusion, respiratory depression, dysfunction of the gastrointestinal tract;
in patients with impaired liver function, hepatic coma may develop.
Treatment: gastric lavage and / or the appointment of activated charcoal, correction of water-electrolyte balance, symptomatic therapy.
There is no specific antidote.
DRUG INTERACTION

Acrypamide increases the concentration of lithium ions in the blood plasma (decreased excretion in the urine), lithium has a nephrotoxic effect.

Increases the risk of kidney dysfunction when using iodine-containing contrasting drugs in high doses (dehydration of the body).
Before using iodine-containing contrast agents, it is necessary to restore the loss of fluid in the body.
Reduces the effect of indirect anticoagulants (coumarin or indanedione derivatives) due to an increase in the concentration of coagulation factors as a result of a decrease in BCC and increase in their production by the liver (dose adjustment may be required).

Strengthens the blockade of the neuromuscular transmission, which develops under the action of nondepolarizing muscle relaxants.

"Loopback" and thiazide diuretics, cardiac glycosides, GCS and mineralocorticoids, tetracosactide, amphotericin B (with iv introduction), laxative drugs increase the risk of hypokalemia.
With simultaneous admission with cardiac glycosides, the likelihood of developing digitalis intoxication increases; with preparations of calcium ions - hypercalcemia; with metformin, aggravation of lactic acidosis is possible.
Astemizole, erythromycin (with iv introduction), pentamidine, sultopride, terfenadine, vincamine, antiarrhythmic drugs of the IA class (quinidine, disopyramide) and III class (amiodarone, brethil tosylate, sotalol) can lead to the development of pirouette-type arrhythmias for a synergistic account for the increase in the QT interval.

NSAIDs, GCS, tetracosactide, adrenostimulators are reduced, baclofen increases the hypotensive effect of indapamide.

Combination with potassium-sparing diuretics can be effective in some patients, but the possibility of hypo- or hyperkalemia, especially in patients with diabetes and renal insufficiency, is not completely excluded.

ACE inhibitors increase the risk of arterial hypotension and / or acute renal failure (especially with existing renal artery stenosis).

Imipramine (tricyclic) antidepressants and antipsychotic drugs (neuroleptics) increase the hypotensive effect and increase the risk of developing orthostatic hypotension.

Cyclosporine increases the risk of hypercreatininaemia.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored in a dry, dark place at a temperature of no higher than 25 В° C.
Shelf life - 4 years.

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