2010/09/17

Akripamide Retard

Composition, structure and packing

Long-acting tablets, coated white or white with kremovatym or grayish tint, round, biconvex.

1 tab. indapamide 1.5 mg.

Excipients: ludipress, hydroxypropylmethylcellulose (gipromelloza), colloidal silicon dioxide (aerosil), magnesium stearate, polyethylene glycol (macrogol), glycerol, titanium dioxide, talc, lactose.

Clinico-pharmacological group: diuretics. Antihypertensives.

Pharmacological action

Antihypertensive drugs, diuretic, vasodilating activity. By pharmacologically similar to thiazide diuretics. Violates the reabsorption of sodium ions in the cortical segment of the loop of Henle. Increases urinary excretion of sodium, chlorine, and, to a lesser extent - ions of potassium and magnesium. With the ability to selectively block the slow calcium channels, increases the elasticity of arterial walls and reduces TPVR. Helps reduce the hypertrophy of the left ventricle of the heart.

It has no effect on lipid and carbohydrate exchanges (including patients with diabetes mellitus), does not violate the sensitivity of peripheral tissues to the action of insulin.

Reduces the sensitivity of the vascular wall to noradrenaline and angiotensin II, stimulates the synthesis of prostaglandin E2 and reduces the production of free and stable oxygen radicals.

The hypotensive effect develops at the end of the first week, kept for 24 h on the background of a single administration.

Pharmacokinetics

Absorption

Once inside quickly and completely absorbed from the gastrointestinal tract. High Bioavailability - 93%. Eating a slow rate of absorption, but does not affect the number has grown deep substance. Once inside the blood plasma Cmax is achieved within 12 h. In repeated receptions fluctuations in the concentration of the drug in blood plasma in the interval between doses of two doses are reduced.

Distribution

The equilibrium state is established within 7 days of regular use. Linking to plasma proteins - 79%. Also been associated with elastin smooth muscles of the vascular wall. It has a high Vd, passes through histohematogenous barriers (including placenta), is excreted in breast milk. Not cumulative.

Metabolism and excretion

Metabolised in liver. T1 / 2 - 18 hours urinary recovery of 60-80% in the form of metabolites, unchanged - about 5%, through the intestines - 20%.

Pharmacokinetics in special clinical situations

In patients with renal insufficiency pharmacokinetics unchanged.

Statement
hypertension.

Dosage regimen

The drug is prescribed oral dose of 1.5 mg (mainly in the morning). Tablets should be taken without chewing, drinking plenty of fluids.

Side effect

On the part of the digestive system: nausea, anorexia, dry mouth, stomachalgia, vomiting, diarrhea, constipation, abdominal pain, may develop hepatic encephalopathy, rare - pancreatitis.

From the CNS: asthenia, nervousness, headache, dizziness, drowsiness, vertigo, insomnia, depression, rarely - fatigue, weakness, malaise, muscle spasm, tension, irritability, anxiety.

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

Since the cardiovascular system: orthostatic hypotension, ECG changes (hypokalemia), arrhythmia, palpitations. From the urinary system: frequent infections, nocturia, polyuria.

On the part of the hemopoietic system: rarely - thrombocytopenia, leukopenia, agranulocytosis, bone marrow aplasia, hemolytic anemia.

Allergic reactions: rash, urticaria, pruritus, hemorrhagic vasculitis.

Laboratory indicators: hyperuricemia, hyperglycemia, hypokalemia, chloropenia, hyponatremia, hypercalcemia, increase in blood plasma urea nitrogen, hypercreatininemia, Glycosuria.

Other: exacerbation of systemic lupus erythematosus.

Contraindications
hypokalemia;
severe renal insufficiency (stage anuria);
marked hepatic impairment (including those with encephalopathy);
simultaneous reception of drugs prolong the QT interval;
lactose;
galactosemia;
malabsorption syndrome glucose / galactose;
Pregnancy
Lactation (breastfeeding);
the age of 18 years (effectiveness and safety have not been established);
Hypersensitivity to the drug and other sulfonamide derivatives.

With caution is prescribed for disorders of liver function and / or kidney disease, disruption of water and electrolyte balance, hyperparathyroidism, patients with an increased QT interval on ECG or receiving concomitant therapy of diabetes in decompensation stage, hyperuricemia (especially accompanied by gout and urate nephrolithiasis).

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding).

Application for violations of liver function

Contraindicated in marked hepatic failure (including those with encephalopathy).

With caution is prescribed for violations of liver function.

Application for violations of renal function

With caution is prescribed for violations of kidney function. Contraindicated in severe renal insufficiency (stage anuria).

Cautions

Note that patients receiving cardiac glycosides, laxatives, and hyperaldosteronism, as well as in the elderly shows a regular control of the content of potassium ions and creatinine.

During the course of Akripamida retard should systematically monitor the concentration of potassium ions, sodium, magnesium in blood plasma (can develop electrolyte disturbances), pH, glucose, uric acid and residual nitrogen.

The most careful control is shown in patients with liver cirrhosis (especially with edema or ascites, as there is a risk of developing metabolic alkalosis, enhances the manifestation of hepatic encephalopathy), myocardial ischemia, heart failure, as well as in the elderly.

High-risk groups also include patients with an increased QT interval on ECG (congenital or developed in the presence of any pathological process).

The first measurement of the concentration of potassium in the blood should be carried out during the first week of treatment. Hypercalcemia against reception Akripamida retard may be due to previously undiagnosed hyperparathyroidism.

Patients with diabetes should monitor blood glucose levels, especially in the presence of hypokalemia. Significant dehydration can lead to acute renal failure (decrease in glomerular filtration). Patients need to compensate for the loss of water and the beginning of treatment carefully monitor renal function.

Patients with hypertension and hyponatremia (due to receiving diuretics) should be 3 days before receiving ACE inhibitors stop taking diuretics (if necessary, diuretics can be resumed later) or they prescribe ACE inhibitors in low initial doses. In the application of indapamide possible positive results during the doping control.

Effects on ability to drive vehicles and management mechanisms

In some cases, individual reactions associated with changes in blood pressure, especially in the beginning of treatment and with the addition of another antihypertensive drug. As a result, may decrease the ability to drive a car and work with mechanisms that require attention.

Overdose

Symptoms: nausea, vomiting, weakness, gastrointestinal dysfunction, fluid and electrolyte disturbances, in some cases - the excessive lowering of blood pressure, respiratory depression. Patients with cirrhosis may develop hepatic coma.

Treatment: gastric lavage, correction of water and electrolyte balance, symptomatic therapy. No specific antidote.

Drug Interactions

At the same time.The Akripamida retard saluretikami, cardiac glycosides, gluco-and mineralocorticoid, tetrakozaktidom, amphotericin B (for B / administration), laxatives increases the risk of hypokalemia.

At the same time.The Akripamida retard with cardiac glycosides increases the likelihood of digitalis intoxication.

At the same time.The Akripamida retard calcium supplementation increases the risk of hypercalcemia.

At the same time.The Akripamida retard with metformin may be worsening lactic acidosis. Akripamid retard increases the concentration of lithium in blood plasma (by reducing the excretion of urine), which increases the risk of nephrotoxicity of the latter.

At the same time receiving a Akripamidom retard astemizola, erythromycin (for in / introduction), pentamidine, sultoprida, terfenadina, vinkamina, antiarrhythmics class IA (quinidine, dizopiramid) and class III (amiodarone, bretilium, sotalol) may develop arrhythmias such as "pirouette .

At the same time.The Akripamida retard with NSAIDs, GCS tetrakozaktidom, sympathomimetics reduced hypotensive effect.

At the same time.The Akripamida retard baklofenom increased hypotensive effect. Combination Akripamida retard with potassium-sparing diuretics may be effective in a certain category of patients, but it is not completely exclude the possibility of hypo-or hyperkalaemia, especially in patients with diabetes and renal insufficiency.

At the same time.The Akripamida retard ACE inhibitors increase the risk of arterial hypotension and / or acute renal failure (especially when existing renal artery stenosis).

At the same time.The Akripamida retard with iodine contrast medium in high doses may develop dehydration and increase risk of renal dysfunction. Before using iodine-contrast substances patients to restore lost fluids. Imipraminovye (tricyclic) antidepressants and antipsychotics increase the hypotensive effect Akripamida retard and increase the risk of orthostatic hypotension.

At the same time.The Akripamida retard with cyclosporine increases risk of hypercreatininemia. Akripamid retard reduces the effect of indirect anticoagulants (coumarin derivatives or indandiona) due to increased concentrations of coagulation factors by reducing blood volume and improve their products liver (may require dosage adjustment).

Akripamid retard enhances blockade of neuromuscular transmission, evolving under the action of nondepolarizing muscle relaxants.

Terms and Conditions of storage

List B. The drug should be stored in dry, protected from light, away from children at or above 25 ° C. Shelf life - 2 years.