2010/09/21

Arindap

Composition, structure and packing

Tablets, coated white, round, biconvex, on the break - a white or nearly white.

1 tab. indapamide 2.5 mg.

Excipients: microcrystalline cellulose, krospovidon, magnesium stearate.

The composition of the shell: gipromelloza, stearic acid, microcrystalline cellulose, titanium dioxide.

Clinico-pharmacological group: diuretics.

Antihypertensives.

Pharmacological action

Antihypertensive drugs. By pharmacologically similar to thiazide diuretics (the mechanism of action involves a violation of the reabsorption of sodium in the cortical segment of the loop of Henle). Increases urinary excretion of sodium and 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.

Does not affect the lipid content in blood plasma (TG, LDL, HDL) and carbohydrate metabolism (including patients with concomitant diabetes mellitus). Reduces the sensitivity of the vascular wall to norepinephrine (noradrenaline) and angiotensin II, stimulates the synthesis of prostaglandin E2 and reduces the production of free and stable oxygen radicals. Hypotensive effect persists for 24 hours while taking the drug 1 times / d, the optimal therapeutic effect develops at the end of the first week of admission.

Pharmacokinetics

Absorption

Once inside quickly and completely absorbed from the gastrointestinal tract, bioavailability - high (93%). Reception with food slows the absorption of some, but not affect its value. Cmax achieved within 1-2 hours after ingestion.

Distribution

Repeated receptions fluctuations in the concentration of the drug in blood plasma in the interval between doses of two doses are reduced. 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. Not cumulative. It has a high Vd, penetrates through histohematogenous barriers (including placenta), is excreted in breast milk.

Metabolism and excretion

Metabolised in liver. T1 / 2 - 18 hours is derived primarily by the kidneys as metabolites 60-80% (unchanged output of about 5%), through the intestines - 20%.

Pharmacokinetics in special clinical situations

In patients with renal insufficiency pharmacokinetics unchanged.

Statement
hypertension.

Dosage regimen

Tablets taken by mouth, not liquid. The recommended dose is - 2.5 mg (1 tab.) 1 times / day (morning). If after 4-8 weeks of treatment desired therapeutic effect is not achieved, the dose of the drug is not recommended to raise (increase the risk of side effects without increased antihypertensive effect).

Instead, the scheme of medical treatment is recommended to include other antihypertensive medication (not diuretics). In cases where treatment should begin with the reception of the two drugs, dose Arindapa remains equal to 2.5 mg (1 time per day, morning).

Side effect
On the part of the digestive system: nausea / anorexia, dry mouth, stomachalgia, vomiting, diarrhea, constipation, pancreatitis.
From the CNS: asthenia, nervousness, headache, dizziness, drowsiness, vertigo, insomnia, depression, rarely - fatigue, weakness, malaise, muscle spasm, tension, irritability, anxiety.
From the side of the organ of vision: conjunctivitis, visual disturbances.
On the part of the respiratory system: cough, sore throat, sinusitis, rhinorrhea, rarely - rhinitis.
Since the cardiovascular system: orthostatic hypotension, ECG changes (hypokalemia), arrhythmia, palpitations.
From the urinary system: frequent infections, nocturia, polyuria. Allergic reactions: rash, urticaria, pruritus, hemorrhagic vasculitis.
From the laboratory parameters: hyperuricemia, hypokalemia, chloropenia, hyponatremia, hypercalciuria, improvement in blood plasma urea nitrogen, hypercreatininemia, Glycosuria.
Other: flu-like syndrome, chest pain, back pain, infection, reduced potency, decreased libido, sweating, weight loss, tingling in the extremities, exacerbation of systemic lupus erythematosus.

Contraindications
anuria;
hypokalemia;
marked hepatic impairment (including those with encephalopathy);
renal failure;
Pregnancy
lactation;
the age of 18 years (effectiveness and safety have not been established);
simultaneous reception of drugs prolong the interval QT;
Hypersensitivity to the drug and other sulfonamide derivatives.

With caution is prescribed for diabetes in decompensation stage, hyperuricemia (especially accompanied by gout and urate nephrolithiasis).

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Application for violations of liver function

The drug is contraindicated in marked hepatic failure (including those with encephalopathy).

Application for violations of renal function

Contraindicated in renal failure.

Cautions

In the appointment of the drug to patients receiving cardiac glycosides, laxatives, and hyperaldosteronism, as well as the elderly shows a regular control of the content of potassium ions and creatinine level. During the course of Arindapa should systematically monitor the concentration of potassium ions, sodium, magnesium in blood plasma (may develop electrolyte disturbances), pH, glucose, uric acid and residual nitrogen.

The most careful control of selected patients with liver cirrhosis (especially those with edema or ascites due to the risk of developing metabolic alkalosis, enhances the manifestation of hepatic encephalopathy), as well as coronary heart disease, heart failure and 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 definition of the concentration of potassium ions in the blood should be carried out during the first week of the drug. Hypercalcemia against reception Arindapa may be due to previously undiagnosed hyperparathyroidism. In patients with diabetes mellitus is extremely important to 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. Arindap can give a positive result during the doping control.

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 ACE inhibitor administered in low initial doses. In the appointment of indapamide should be borne in mind that the derivatives of sulfonamides may aggravate during systemic lupus erythematosus.

Use in Pediatrics

Efficacy and safety of the drug in children has not been established.

Overdose

Symptoms: nausea, vomiting, weakness, gastrointestinal dysfunction, disruption of water and electrolyte balance, 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, if necessary, carry symptomatically. No specific antidote.

Drug Interactions

In a joint application with indapamide saluretiki, cardiac glycosides, gluco-and mineralocorticoid, tetrakozaktid, amphotericin B (for B / administration), laxatives increase the risk of hypokalemia. At the same time receiving a cardiac glycoside increases the likelihood of digitalis intoxication with calcium supplementation - hypercalcemia; with metformin - possibly worsening lactic acidosis.

When combined with the use of indapamide increases the concentration of lithium ions in the blood plasma (by reducing the excretion of urine), lithium has nephrotoxic effects.

When combined with the use of indapamide should be aware that astemizol, erythromycin / a, pentamidine, sultoprid, terfenadin, vinkamin, class Ia antiarrhythmics (quinidine, dizopiramid) and class III (amiodarone, bretilium, sotalol) may lead to arrhythmia type "pirouette".

When the joint application of NSAIDs, GCS tetrakozaktid, sympathomimetic reduce the hypotensive effect of indapamide, Baclofen - strengthens.

The combination with a potassium-sparing diuretics can 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.

When combined with the use of indapamide ACE inhibitors increase the risk of arterial hypotension and / or acute hepatic failure (especially when existing renal artery stenosis). Indapamide increases the risk of renal dysfunction using iodine contrast agents at high doses (due to dehydration).

Before using iodine contrast agents patients to restore lost fluids. Imipraminovye (tricyclic) antidepressants and antipsychotic tools enhance hypotensive effect and increase the risk of orthostatic hypotension.

When the joint application of cyclosporine increases the risk of hypercreatininemia. Indapamide reduces the effect of indirect anticoagulants (coumarin derivatives or indandiona) due to increasing concentrations of coagulation factors by reducing the BCC and increase their products gras (may require dosage adjustment). Indapamide 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 a dry, protected from light and the reach of children, at a temperature below 25 ° C. Shelf life - 3 years.