GIPOTIAZID
Active material: Gidroxlorotiazid
When ATH: C03AA03
CCF: Diuretic
ICD-10 codes (testimony): E23.2, I10, I50.0, N00, N04, N18, N20, N21, N94.3
When CSF: 01.08.02.01
Manufacturer: CHINOIN Pharmaceutical and Chemical Works Private Co. Ltd. (Hungary)
Pharmaceutical form, composition and packaging
Pills white or nearly white, round, flat, Engraved “N” on one side and Valium – another.
| 1 tab. | |
| gidroxlorotiazid | 25 mg |
| -“- | 100 mg |
Excipients: magnesium stearate, talc, gelatin, corn starch, lactose monohydrate.
20 PC. – blisters (1) – packs cardboard.
Pharmacological action
Diuretic. The primary mechanism of action of thiazide diuretics increase urine output is by blocking the reabsorption of sodium ions and chlorine in early renal tubules. Consequently, it increases the excretion of sodium and chlorine and, Consequently, water. Also increases the excretion of potassium and magnesium.
The maximum therapeutic dose diuretic / natriuretic effect of thiazides are approximately equal. Natriuresis and diuresis occurs within 2 h and reaches its maximum after about 4 no. They also reduce the activity of carbonic anhydrase by increasing excretion of bicarbonate ion, but this effect is weak and usually does not affect the pH of the urine.
Hydrochlorothiazide also has antihypertensive properties. In normal blood pressure thiazide diuretics have no effect.
Pharmacokinetics
Absorption and distribution
Less than Gidrohlorotiazid, but fairly rapidly absorbed from the gastrointestinal tract. This effect persists for 6-12 no. After oral dose 100 mg Cmax plasma levels achieved after 1.5-2.5 no. At the peak of diuretic activity (approximately 4 h after administration) hydrochlorothiazide concentration in plasma is 2 ug / ml.
Binding to plasma proteins is 40%.
Deduction
The primary route of elimination – kidney (filtration and secretion) in unmodified form. T1/2 for patients with normal renal function is 6.4 no. T1/2 for patients with mild renal insufficiency is 11.5 no. T1/2 for patients with CC<30 ml / min of 20.7 no. Hydrochlorothiazide crosses the placental barrier and is excreted in breast milk.
Testimony
- Arterial hypertension (monotherapy, in the complex antihypertensive therapy);
- Edematous syndrome of various genesis (incl. in chronic heart failure, nephrotic syndrome, premenstrual tension syndrome, acute glomerulonephritis, chronic renal failure, portal hypertension, corticosteroid treatment);
- Control of polyuria, preferably at nephrogenic diabetes insipidus;
- Prevention of stone formation in the urinary tract in susceptible patients (decrease hypercalciuria).
Dosage regimen
The dose should be selected individually. With constant medical control sets the minimum effective dose. The drug is taken orally after a meal.
Adults
At hypertension starting dose is 25-50 mg / day one, alone or in combination with other antihypertensives. Some patients enough initial dose 12.5 mg (as monotherapy, in combination). It is necessary to use the minimum effective dose, not exceeding 100 mg / day. When combined gipotiazid® with other antihypertensive agents, you may need to reduce the dose of the other drug for the prevention of excessive blood pressure lowering.
The antihypertensive effect is manifested within 3-4 days, but for optimal effect may require 3-4 of the week. After the end of therapy hypotensive effect is maintained for 1 of the week.
At edematous syndrome of various genesis starting dose is 25-100 mg / day once or 1 once every 2 day. Depending on the clinical response the dose can be reduced to 25-50 mg / day once or 1 once every 2 day. In some severe cases, early treatment may need to increase the dose to 200 mg / day.
At predmestrualnogo stress syndrome the drug is prescribed in a dose 25 mg / day and used from the start of symptoms before menstruation.
At nephrogenic diabetes insipidus recommended regular daily dose 50-150 mg (in divided doses).
Due to an increased loss of potassium and magnesium ions during treatment (serum potassium level may be <3.0 mmol / l) there is a need to substitute potassium and magnesium.
Babies
Doses should be installed, based on the weight of the child. Typical daily doses of pediatric: 1-2 mg / kg body weight or 30-60 mg / m2 body surface 1 time / day. The daily dose at the children aged 3 to 12 years amounts to 37.5-100 mg.
Side effect
From the central and peripheral nervous system: dizziness, temporary blurred vision, headache, paresthesia.
From the digestive system: cholecystitis, pancreatitis, cholestatic jaundice, diarrhea, sialadenitis, constipation, anorexia.
Cardio-vascular system: arrhythmia, orthostatic hypotension, vasculitis.
From the urinary system: impairment of renal function, interstitial nephritis.
From the hematopoietic system: rarely – leukopenia, agranulocytosis, thrombocytopenia, gemoliticheskaya anemia, aplasticheskaya anemia.
Metabolism: giperglikemiâ (reduced glucose tolerance could trigger latent manifest before diabetes), glycosuria, hyperuricemia (with the development of a gout attack), kaliopenia, gipomagniemiya, hypercalcemia, giponatriemiya (incl. confusion, convulsions, lethargy, slowing the process of thinking, fatigue, excitability, muscle cramps), hypochloraemic alkalosis (incl. dry mouth, thirst, irregular heart rhythm, changes in mood or psyche, cramping and muscle soreness, nausea, vomiting, unusual tiredness or weakness). Hypochloraemic alkalosis may cause hepatic encephalopathy, or hepatic coma. In applying the drug in high doses may increase the levels of serum lipids.
Allergic reactions: hives, purpura, Necrotizing Vasculitis, Stevens-Johnson syndrome, respiratory distress syndrome (incl. pneumonitis, nekardiogennyj Lung edema), photosensitivity, anaphylactic reactions up to shock.
Other: reduced potency.
Contraindications
- Anurija;
- Severe renal insufficiency (CC<30 ml / min);
- Severe hepatic impairment;
- Diffi- cult diabetes;
- Addison's disease;
- Refractory hypokalaemia, giponatriemiya, hypercalcemia;
- Children up to age 3 years (for solid dosage forms);
- Hypersensitivity to the drug;
- Hypersensitivity to sulfonamide derivative.
FROM caution use in patients with hypokalemia, giponatriemii, hypercalcemia, CHD, cirrhosis, podagre, lactose intolerance, application of cardiac glycosides, as well as in elderly patients.
Pregnancy and lactation
Do not use this drug in the I trimester of pregnancy. In the II and III of the third trimester use of the drug is possible only in the case, when the intended benefits to the mother outweighs the potential risk to the fetus.
Hydrochlorothiazide crosses the placental barrier. There is a risk of fetal or neonatal jaundice, thrombocytopenia and other effects of.
The drug is excreted in breast milk. If necessary, use during lactation should decide the issue of termination of breastfeeding.
Cautions
In long-term treatment should be carefully monitored clinical symptoms of disorders of water and electrolyte balance, Firstly, in patients at high risk: patients with diseases of the cardiovascular system, impaired liver function, when severe vomiting or signs of violations of water-electrolyte balance (incl. dry mouth, thirst, weakness, lethargy, drowsiness, anxiety, muscle pain or cramps, muscular weakness, gipotenziya, oligurija, tachycardia, complaints from the gastrointestinal tract).
Use of the potassium-containing drugs or foods, rich in potassium (incl. fruit, vegetables), especially the loss of potassium due to the enhanced diuresis, prolonged diuretic therapy, any simultaneous treatment of digitalis glycosides or corticosteroids, avoids hypokalaemia.
Increased urinary excretion of magnesium when used thiazides may cause hypomagnesemia.
At reduced kidney function requires monitoring of creatinine clearance. In patients with renal dysfunction drug can cause azotemia and development of cumulative effects. If dysfunction Kidney obvious, upon the occurrence of oliguria should consider discontinuation of the drug.
Patients with impaired hepatic function or progressive liver disease thiazides should be used with caution, because a small change in water and electrolyte balance, as well as the level of ammonium in serum may cause hepatic coma.
In severe cerebral and coronary sclerosis drug application requires special care.
Treatment of thiazide drugs may interfere with glucose tolerance. During the long course of treatment when the manifest and latent diabetes requires systematic monitoring carbohydrate metabolism because of the potential need to change the dose of hypoglycemic drugs.
It requires strict control of patients with impaired metabolism of uric acid.
Alcohol, barbiturates, opioid analgesics increase the orthostatic hypotensive effect of thiazide diuretics.
In rare cases, prolonged therapy observed pathological changes in the parathyroid glands, accompanied by hypercalcemia and hypophosphatemia.
Thiazides may reduce the amount of iodine, binding to serum proteins, without showing signs of disorders of the thyroid gland.
Keep in mind the possibility of gastrointestinal complaints in patients with lactose intolerance, as tablets Hypothiazid® 25 mg contain 63 Lactose mg, Gipotiazid® 100 mg – 39 Lactose mg.
Effects on ability to drive vehicles and management mechanisms
In the initial stage of the drug (the duration of this period is determined individually) It prohibited to drive a car and perform the work, requiring special attention.
Overdose
Symptoms: due to loss of fluid and electrolytes in the drug overdose may experience tachycardia, decrease in blood pressure, shock, weakness, confusion, dizziness, cramping calf muscles, paresthesia, disturbance of consciousness, fatigue, nausea, vomiting, thirst, polyuria, oliguria or anuria (due to hemoconcentration), kaliopenia, giponatriemiya, chloropenia, alkalosis, increase in blood urea nitrogen (especially in patients with renal insufficiency).
Treatment: artificial vomiting, gastric lavage, activated carbon. By reducing blood pressure or shock should compensate the BCC and electrolytes (incl. potassium, sodium). It should monitor the status of water and electrolyte balance (especially serum potassium) and renal function prior to the establishment of normal values. No specific antidote.
Drug Interactions
The simultaneous use of hydrochlorothiazide® with lithium salts should be avoided, because it reduces the renal clearance of lithium and increase its toxicity.
With simultaneous use of hydrochlorothiazide® with antihypertensive drugs and their effect is potentiated may need dose adjustment.
With simultaneous use of hydrochlorothiazide® with cardiac glycosides hypokalemia and hypomagnesemia, associated with the effect of thiazide diuretics, may increase the toxicity of digitalis.
With simultaneous use of hydrochlorothiazide® with amiodarone increases the risk of arrhythmias, associated with hypokalemia.
With simultaneous use of hydrochlorothiazide® with oral hypoglycemic agents reduced the effectiveness of the latter and may develop hyperglycemia.
With simultaneous use of hydrochlorothiazide® with corticosteroids, calcitonin increases the degree of excretion of potassium.
With simultaneous use of hydrochlorothiazide® NSAIDs attenuated diuretic and hypotensive effect of thiazides.
With simultaneous use of hydrochlorothiazide® nedepolyariziruyuschimi with muscle relaxants enhanced effect of the latter.
With simultaneous use of hydrochlorothiazide® with amantadine increases the concentration and toxicity of the latter, as a result of its reduced clearance.
With simultaneous use of hydrochlorothiazide® with decreases kolestiraminom absorption gidrohlorotiazida.
With simultaneous use of hydrochlorothiazide® ethanol, barbiturate and opioid analgesics increases risk of orthostatic hypotension.
Thiazides may reduce the plasma levels of iodine, protein-bound; increase the concentration of bilirubin in the blood serum.
Before carrying out tests for parathyroid function thiazides should be abolished.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored out of reach of children, dark place at a temperature of 15 ° to 25 ° C. Shelf life - 5 years.
