Indapamid

General characteristics. Structure:

Active agent: индапамид (in the form of a hydrochloride) - 2,5 mg; excipients - lactoses monohydrate, povidone (To 30), кросповидон, magnesium stearate, sodium lauryl sulfate, talc, metilgidroksipropiltsellyuloza, makrogol, titanium dioxide.

Pharmacological properties:

Pharmacodynamics. Antihypertensive (diuretic, vazodilatator). On pharmacological properties it is close to thiazide diuretics (disturbance of a reabsorption of Na + in a cortical segment of a Henle's loop). Increases removal with urine Na+, Cl-and to a lesser extent K+ and Mg2+. Having ability to selectively block "slow" calcium channels, increases elasticity of walls of arteries and reduces OPSS. Promotes reduction of a hypertrophy of LZh of heart. Does not influence the maintenance of lipids in plasma (TG, LPNP, LPVP); does not influence carbohydrate metabolism (including at patients with the accompanying diabetes mellitus). Reduces sensitivity of a vascular wall to noradrenaline and angiotensin II, stimulates synthesis of PgE2 and PgI2 prostacyclin, reduces products of free and stable oxygen radicals. At appointment in high doses does not influence extent of decrease in the ABP, despite increase in a diuresis. After multiple dose the therapeutic effect is noted in 1-2 weeks, reaches a maximum to 8-12 weeks and remains to 8 weeks; after reception of a single dose the maximum effect is noted in 24 h.

Pharmacokinetics. It is quickly and completely soaked up from a GIT; bioavailability - high. Meal slows down absorption speed a little, but does not influence final amount of the soaked-up drug. TCmax is 1-2 h after reception of a usual dosage form and 12 h after reception of tablets ретард. Cmax after intake in a dose of 5 mg - 260 ng/ml. At repeated methods of fluctuation of concentration of drug in plasma in an interval between receptions of 2 doses decrease. Css is established in 7 days of regular reception. Communication with proteins of plasma - 71-79%. Contacts also elastin of unstriated muscles of a vascular wall. Has the high volume of distribution, passes through gistogematichesky barriers (including placental). It is metabolized in a liver. T1/2 is 14 h, final T1/2 - 26 h. Kidneys remove 60-70% in the form of metabolites (in not changed look about 5-7% are removed), through intestines - 20-23%. At patients with a renal failure the pharmacokinetics does not change. Does not kumulirut.

Indications to use:

Arterial hypertension.

Route of administration and doses:

Inside, more preferably in the morning. At arterial hypertension in an initial dose - on 1.25-2.5 mg (not prolonged form) of 1 times a day or 1.5 mg (a tablet ретард) in the morning. At insufficient efficiency in 4-8 weeks it is reasonable to add to therapy HP with other mechanism of action (increase in a dose is inexpedient - in the absence of essential increase in effect growth of side effects is noted).

Features of use:

At the patients accepting cardiac glycosides, HP laxatives against the background of a hyper aldosteronism, and also at elderly people careful control of maintenance of K+ and creatinine is shown. Against the background of reception of an indapamid it is necessary to control systematically concentration of K+, Na+, Mg2 + in plasma (electrolytic disturbances can develop), pH, concentration of glucose, uric acid and residual nitrogen. The most careful control is shown at patients with cirrhosis (especially with hypostases or ascites - risk of development of the metabolic alkalosis strengthening displays of hepatic encephalopathy), IBS, HSN, and also at elderly people. Patients with the increased Q-T interval on an ECG also treat group of the increased risk (inborn or developed against the background of any pathological process). The first measurement of concentration of K+ in blood should be taken during 1 week of treatment. The hypercalcemia against the background of reception of an indapamid can be a consequence of earlier not diagnosed hyperparathyreosis. At patients with a diabetes mellitus it is extremely important to control glucose level in blood, especially in the presence of a hypopotassemia. Considerable dehydration can lead to development of an acute renal failure (decrease in glomerular filtering). Patients need to offset loss of water and in an initiation of treatment carefully to control function of kidneys. Indapamid can yield a positive take when carrying out a drug test. It is necessary for patients with arterial hypertension and a hyponatremia (owing to reception of diuretics) in 3 days prior to reception of APF inhibitors to stop reception of diuretics (if necessary reception of diuretics can be resumed a bit later) лЙбо by it appoint initial low doses of APF inhibitors. Can aggravate a current of hard currency. Efficiency and safety at children are not established. With care. A hyponatremia, etc. disturbances of water and electrolytic exchange, a moderate liver and/or renal failure, ascites, IBS, HSN, lengthening of an interval of Q-T, the hyperuricemia (which is especially shown gout or an uratny nefrourolitiaz), a hyperparathyreosis, pregnancy, the lactation period, advanced age and age up to 18 years (lack of sufficient experience). Acute disorder of cerebral circulation, dekompensirovanny diabetes mellitus with ketoacidosis - for the low doses which are required for treatment of arterial hypertension.

Side effects:

Frequency of development of side effects of a dozozavisim.

From the alimentary system: when using in a dose of 1.25 mg: more than 5% - locks or diarrhea, dyspepsia, nausea, an abdominal pain. In a dose of 2.5-5 mg (in addition): more than 5% - vomiting, a gastralgia, a loss of appetite, dryness in a mouth.

From a nervous system: when using in a dose of 1.25 mg: more than 5% - an adynamy, nervousness; less than 5% - a headache, dizziness. In a dose of 2.5-5 mg (in addition): more than 5% - slight dizziness, drowsiness, вертиго, sleeplessness, a depression; less than 5% of cases - increased fatigue, an adynamy, a lethargy, slackness, an indisposition, a spasm of muscles, nervousness, tension, uneasiness, irritability, agitation.

From sense bodys: when using in a dose of 1.25 mg: more than 5% - conjunctivitis. In a dose of 2.5-5 mg (in addition): more than 5% - a vision disorder.

Others: when using in a dose of 1.25 mg: more than 5% - a grippopodobny syndrome, thorax pain; less than 5% - infections, a dorsodynia. In a dose of 2.5-5 mg (in addition): more than 5% - decrease in a potentiality and/or libido, a rhinorrhea, the increased sweating, decrease in body weight, paresthesia in extremities.

From respiratory system: when using in a dose of 1.25 mg: less than 5% - cough, pharyngitis, sinusitis; more than 5% - rhinitis.

From CCC: more than 5% - orthostatic hypotension, changes on an ECG (hypopotassemia), arrhythmia, heartbeat.

From an urinary system: more than 5% - frequent infections, a nocturia, a polyuria. Allergic reactions: more than 5% - rash, urticaria, an itch, a vasculitis.

Laboratory indicators: more than 5% - a hyperuricemia, a hyperglycemia, a hyponatremia, a hypochloraemia, increase in an urea nitrogen in plasma, a giperkreatininemiya, a glucosuria, a hypercalcemia.

Interaction with other medicines:

Increases concentration of Li + in plasma (decrease in removal with urine), lithium has nephrotoxic effect. Increases risk of development of renal failures when using iodinated contrast HP in high doses (organism dehydration). Before use of iodinated contrast HP by the patient it is necessary to recover liquid loss. Reduces effect of indirect anticoagulants (derivative coumarin or an indandion) owing to increase in concentration of factors of coagulation as a result of reduction of OTsK and increase in their products liver (dose adjustment can be required). Strengthens the neuromuscular transmission blockade developing under the influence of not depolarizing muscle relaxants. Saluretics (loopback, thiazide), cardiac glycosides, GKS and ISS, тетракозактид, Amphotericinum In (in/in), HP laxatives increase risk of development of a hypopotassemia. At a concomitant use with cardiac glycosides the probability of development of digitalis intoxication increases; with the drugs Ca2 + - hypercalcemias; with Metforminum aggravation of lactic acidosis is possible. Astemizol, erythromycin in/in, pentamidine, сультоприд, терфенадин, Vincaminum, antiarrhytmic HP of Ia of a class (quinidine, Disopyramidum) and the III class (Amiodaronum, a bretylium tosylate, соталол) can lead to development of arrhythmia in the pirouette type due to sinergidny influence (lengthening) on Q-T interval duration. NPVP, GKS, тетракозактид, adrenostimulyator reduce hypotensive effect, Baclofenum strengthens. The combination with kaliysberegayushchy diuretics can be effective at some category of patients, however at the same time the possibility of development hypo - or hyperpotassemias, especially at patients with a diabetes mellitus and a renal failure completely is not excluded. APF inhibitors increase risk of development of arterial hypotension and/or acute renal failure (especially at the available renal artery stenosis). Imipraminovy (tricyclic) antidepressants and antipsychotic HP (neuroleptics) strengthen hypotensive action and increase risk of development of orthostatic hypotension. Cyclosporine increases risk of development of a giperkreatininemiya.

Contraindications:

Hypersensitivity, heavy hepatic (including with encephalopathy) and/or a renal failure (anury), a hypopotassemia. An acute disorder of cerebral circulation, a dekompensirovanny diabetes mellitus with ketoacidosis - for the high doses which are required for treatment of an edematous syndrome. A lactose intolerance, a galactosemia, a syndrome of disturbance of absorption of a glucose/galactose - for the dosage forms containing lactose.

Overdose:

Symptoms: nausea, vomiting, weakness, dysfunction of a GIT, water and electrolytic disturbances, in certain cases - an excessive snyzheniye of the ABP, respiratory depression. At patients with cirrhosis development of a hepatic coma is possible. Treatment: gastric lavage, correction of water and electrolytic balance, symptomatic therapy. There is no specific antidote.

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe