Dichlothiazide - instructions for use, precautions and side effects. Diuretics, their classification, pharmacological characteristics

  • Date: 12.04.2019

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Recipe

Rp: Dichlotiazidi 0.025

D. t. d. N. 20 in tab.

S. 1 tablet 1 time a day, in the morning.

pharmachologic effect

Medium strength thiazide diuretic. Reduces Na + reabsorption at the level of the cortical segment of Henle's loop, without affecting its section passing in the medulla of the kidney, which determines a weaker diuretic effect in comparison with furosemide.

Blocks carbonic anhydrase in proximal convoluted tubules, enhances urinary excretion of K + (in the distal tubules, Na + is exchanged for K +), hydrocarbons and phosphates. Virtually no effect on CBS (Na + is excreted either together with Cl- or with bicarbonate, therefore, with alkalosis, the excretion of bicarbonates increases, with acidosis - of chlorides).

Increases the excretion of Mg2 +; retains Ca2 + ions in the body and excretion of urates. The diuretic effect develops in 1-2 hours, reaches a maximum after 4 hours, lasts 10-12 hours. The effect decreases with a decrease in the glomerular filtration rate and stops at its value less than 30 ml / min. Patients do not diabetes mellitus has an antidiuretic effect (reduces the volume of urine and increases its concentration). It lowers blood pressure by reducing the BCC, changing the reactivity of the vascular wall, reducing the pressor effect of vasoconstrictor drugs (epinephrine, norepinephrine) and increasing the depressor effect on the ganglia.

Mode of application

To lower blood pressure: by mouth, 25-50 mg / day, with a slight diuresis and natriuresis noted only on the first day of admission (prescribed for a long time in combination with other antihypertensive drugs: vasodilators, ACE inhibitors, sympatholytics, beta-blockers).

With an increase in the dose from 25 to 100 mg, a proportional increase in diuresis, natriuresis and a decrease in blood pressure is observed.

In a single dose over 100 mg - an increase in diuresis and a further decrease in blood pressure are insignificant, there is a disproportionately increasing loss of electrolytes, especially K + and Mg2 +. Increasing the dose over 200 mg is inappropriate, because increased urine output does not occur.

In case of edematous syndrome (depending on the condition and reaction of the patient), it is prescribed in a daily dose of 25-100 mg, taken once (in the morning) or in 2 doses (in the morning). Elderly people - 12.5 mg 1-2 times a day. Children aged 2 months to 14 years old - 1 mg / kg / day. Maximum dose for children under the age of 6 months - 3.5 mg / kg / day, up to 2 years old - 12.5-37.5 mg / day, 3-12 years old - 100 mg / day, divided into 2-3 doses.

As a maintenance therapy at the indicated dose, it is prescribed 2 times a week.

When using an intermittent course of treatment, taken after 1-3 days or within 2-3 days with a subsequent break, the decrease in effectiveness is less pronounced and side effects develop less frequently.

Indications

Contraindications

Severe liver failure, diabetic glomerulosclerosis, chronic diseases chronic kidney renal failure With hypoisostenuria and azotemia, oliguria and anuria in the first 3 months of pregnancy. Conditionally contraindicated in patients with gout and diabetes mellitus. Should be administered with caution in patients with reduced carbohydrate tolerance.

Side effects

Arterial hypertension, congestive heart failure, diabetes insipidus, liver cirrhosis with portal hypertension and edematous-ascitic syndrome, glaucoma, nephritis, nephrosis; rarely - toxicosis of pregnant women.

Release form

Tablets of 0.025 and 0.1 g.

Instructions for use

International name

Hydrochlorothiazide

Group affiliation

Diuretic

Description of the active substance (INN)

Hydrochlorothiazide

Dosage form

Pills

pharmachologic effect

Medium strength thiazide diuretic. Reduces Na + reabsorption at the level of the cortical segment of Henle's loop, without affecting its section passing in the medulla of the kidney, which determines a weaker diuretic effect in comparison with furosemide. Blocks carbonic anhydrase in the proximal section of the convoluted tubules, enhances urinary excretion of K + (in the distal tubules, Na + is exchanged for K +), hydrocarbonates and phosphates. Virtually no effect on CBS (Na + is excreted either together with Cl- or with bicarbonate, therefore, with alkalosis, the excretion of bicarbonates increases, with acidosis - of chlorides). Increases the excretion of Mg2 +; detains Ca2 + ions in the body and excretion of urates. The diuretic effect develops after 1-2 hours, reaches a maximum after 4 hours, lasts 10-12 hours. The effect decreases with a decrease in the glomerular filtration rate and stops when it is less than 30 ml / min. In patients with diabetes insipidus, it has an antidiuretic effect (reduces the volume of urine and increases its concentration). It lowers blood pressure by reducing the BCC, changing the reactivity of the vascular wall, reducing the pressor effect of vasoconstrictor drugs (epinephrine, norepinephrine) and increasing the depressor effect on the ganglia.

Indications

Arterial hypertension; edematous syndrome of various origins(CHF, portal hypertension, nephrotic syndrome, chronic renal failure, fluid retention in obesity), gestosis (nephropathy, edema, eclampsia); diabetes insipidus; subcompensated forms of glaucoma; prevention of the formation of stones in the urinary tract.

Contraindications

Hypersensitivity, gout, diabetes mellitus ( severe forms), Chronic renal failure (CC less than 20-30 ml / min, anuria), hypokalemia, hypercalcemia, hyponatremia; pregnancy (I trimester), lactation. With caution. II-III trimesters of pregnancy.

Side effects

Dry mouth, nausea, vomiting, diarrhea; weakness, increased fatigue, dizziness, headache, palpitations, convulsions calf muscles, hypokalemia, hypomagnesemia, hyponatremia, hyperuricemia, hypercalcemia, hyperglycemia; exacerbation of gout, thrombosis, thromboembolism, hypercreatininemia, acute interstitial nephritis, vasculitis, progression of myopia, neutropenia, thrombocytopenia, hemorrhagic pancreatitis, acute cholecystitis(against the background of cholelithiasis), orthostatic hypotension, allergic dermatitis.

Application and dosage

To lower blood pressure: by mouth, 25-50 mg / day, with a slight diuresis and natriuresis noted only on the first day of admission (prescribed for a long time in combination with other antihypertensive drugs: vasodilators, ACE inhibitors, sympatholytics, beta-blockers). With an increase in the dose from 25 to 100 mg, a proportional increase in diuresis, natriuresis and a decrease in blood pressure is observed. In a single dose over 100 mg - an increase in diuresis and a further decrease in blood pressure are insignificant, there is a disproportionately increasing loss of electrolytes, especially K + and Mg2 +. Increasing the dose over 200 mg is inappropriate, because increased urine output does not occur.

In case of edematous syndrome (depending on the condition and reaction of the patient), it is prescribed in a daily dose of 25-100 mg, taken once (in the morning) or in 2 doses (in the morning). Elderly people - 12.5 mg 1-2 times a day. Children aged 2 months to 14 years old - 1 mg / kg / day. The maximum dose for children under the age of 6 months is 3.5 mg / kg / day, up to 2 years old - 12.5-37.5 mg / day, 3-12 years old - 100 mg / day, divided into 2-3 doses. After 3-5 days of treatment, it is recommended to take a break for 3-5 days. As a maintenance therapy at the indicated dose, it is prescribed 2 times a week. When using an intermittent course of treatment, taken after 1-3 days or within 2-3 days with a subsequent break, the decrease in effectiveness is less pronounced and side effects develop less frequently.

To reduce intraocular pressure, 25 mg is prescribed 1 time in 1-6 days; the effect occurs within 24-48 hours. diabetes insipidus- 25 mg 1-2 times a day with a gradual increase in the dose (daily dose - 100 mg) until reaching therapeutic effect(reduction of thirst and polyuria), further dose reduction is possible.

special instructions

For the prevention of K + and Mg2 + deficiency, a diet with a high content of these salts, potassium-sparing diuretics, K + and Mg2 + salts are prescribed.

Regular monitoring of plasma levels of K +, glucose, uric acid, lipids and creatinine.

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially dangerous species activities requiring increased concentration attention and speed of psychomotor reactions.

Interaction

Drugs that intensively bind to proteins ( indirect anticoagulants, clofibrate, NSAIDs), enhance the diuretic effect.

The antihypertensive effect is enhanced by vasodilators, beta-blockers, barbiturates, phenothiazines, tricyclic antidepressants, ethanol.

It enhances the neurotoxicity of salicylates, weakens the effect of oral hypoglycemic drugs, norepinephrine, epinephrine and anti-gout drugs, enhances the side effects of cardiac glycosides, cardiotoxic and neurotoxic effects of Li + drugs, the effect of peripheral muscle relaxants, and reduces the excretion of quinidine.

With the simultaneous administration of methyldopa, hemolysis may develop.

Cholestyramine reduces absorption.

Reduces the effect of oral contraceptives.

Hypertensive patients, do not feed pharmacies, use this cheap analog times of the USSR

Active substance:

Hydrochlorothiazide * (Hydrochlorothiazide *)

ATX

C03AA03 Hydrochlorothiazide

Pharmacological group

  • Diuretics

Nosological classification (ICD-10)

  • E23.2 Diabetes insipidus
  • I10 Essential (primary) hypertension
  • I15 Secondary hypertension
  • I15.0 Renovascular hypertension
  • I50.0 Congestive heart failure
  • K76.6 Portal hypertension
  • N00 Acute nephritic syndrome
  • N04 Nephrotic syndrome
  • N18.9 Chronic renal failure, unspecified
  • N25.1 Nephrogenic diabetes insipidus
  • R35 Polyuria
  • R60 Edema, not elsewhere classified
  • R82.9 Other and unspecified abnormalities on examination of urine
  • Y42.0 Adverse reactions in therapeutic use of glucocorticoids and their synthetic analogues

3D images

Composition and form of release


in a blister 20 pcs.; in a cardboard box 1 blister.

Description of the dosage form

White or off-white round flat tablets with an engraved "H" on one side and a notch on the other.

pharmachologic effect

Pharmacological action - diuretic.

Pharmacodynamics

The primary mechanism of action of thiazide diuretics is increased urine output
by blocking the reabsorption of sodium and chlorine ions at the beginning of the renal tubules. By doing this they increase
excretion of sodium and chlorine and therefore water. Excretion of other electrolytes, namely potassium and magnesium,
also increases.

At maximum therapeutic doses, natriuretic / diuretic effect
all thiazides are approximately the same. Natriuresis and diuresis occur within 2 hours and reach their
maximum after about 4 hours. They also reduce the activity of carbonic anhydrase by increasing the excretion
bicarbonate ion, but this effect is usually weak and does not affect the pH of the urine. Hydrochlorothiazide
also has antihypertensive properties. Thiazide diuretics have no effect on normal blood pressure.

Pharmacokinetics

Hydrochlorothiazide is incomplete, but rather rapidly absorbed from the gastrointestinal tract. This effect persists for 6-12 hours. After oral administration of a dose of 100 mg, Cmax in blood plasma is achieved after 1.5-2.5 hours.

At the maximum diuretic activity (approximately 4 hours after administration), the concentration of hydrochlorothiazide in the blood plasma is 2 μg / ml. Plasma protein binding is 40%. It is excreted mainly through the kidneys (filtration and secretion) in an unchanged form. T1 / 2 for patients with normal renal function is 6.4 hours, for patients with moderate renal insufficiency - 11.5 hours, and for patients with Cl creatinine less than 30 ml / min - 20.7 hours.

Hydrochlorothiazide crosses the placental barrier and is excreted in breast milk.

Indications of the drug Hypothiazid®

arterial hypertension (used both in monotherapy and in combination with other antihypertensive drugs);

edematous syndrome of various origins (chronic heart failure, nephrotic syndrome, premenstrual syndrome, acute glomerulonephritis, chronic renal failure, portal hypertension, corticosteroid treatment);

control of polyuria, mainly in nephrogenic diabetes insipidus;

prevention of the formation of stones in the genitourinary tract in predisposed patients (reduction of hypercalciuria).

Contraindications

hypersensitivity to the drug or to other sulfonamides;

severe renal (Cl creatinine - less than 30 ml / min) or liver failure;

difficult to control diabetes mellitus;

Addison's disease:

refractory hypokalemia, hyponatremia, hypercalcemia;

childhood up to 3 years (solid dosage form).

Use with caution in hypokalemia, hyponatremia, hypercalcemia, in patients with coronary artery disease, with cirrhosis of the liver, gout, in the elderly, in patients suffering from lactose intolerance, while taking cardiac glycosides.

Application during pregnancy and lactation

Hydrochlorothiazide crosses the placental barrier. The use of the drug in the first trimester of pregnancy is contraindicated. In the II and III trimesters of pregnancy, the drug can be prescribed only in case of urgent need, when the benefit to the mother outweighs the potential risk to the fetus and / or child. There is a risk of developing fetal or newborn jaundice, thrombocytopenia and other consequences.

The drug passes into breast milk; therefore, if the use of the drug is absolutely necessary, then breastfeeding should be discontinued.

Side effects

Electrolyte imbalance

Hypokalemia, hypomagnesemia, hypercalcemia, and hypochloremic alkalosis: dry mouth, thirst, irregular heart rhythm, changes in mood or psyche, muscle cramps and pain, nausea, vomiting, unusual tiredness or weakness. Hypochloremic alkalosis can cause hepatic encephalopathy or hepatic coma.

Hyponatremia: confusion, convulsions, lethargy, slowing down of the thinking process, fatigue, excitability, muscle cramps.

Metabolic phenomena: hyperglycemia, glucosuria, hyperuricemia with the development of a gout attack. Treatment with thiazides can reduce glucose tolerance, and latent diabetes mellitus may manifest. Serum lipid levels may increase with high doses.

From the gastrointestinal tract: cholecystitis or pancreatitis, cholestatic jaundice, diarrhea, sialadenitis, constipation, anorexia.

From the side of the cardiovascular system: arrhythmias, orthostatic hypotension, vasculitis.

From the nervous system and sensory organs: dizziness, blurry vision (temporarily), headache, paresthesia.

From the side of hematopoietic organs: very rarely - leukopenia, agranulocytosis, thrombocytopenia, hemolytic anemia, aplastic anemia.

Hypersensitivity reactions: urticaria, purpura, necrotizing vasculitis, Stevens-Johnson syndrome, respiratory distress syndrome(including pneumonitis and noncardiogenic pulmonary edema), photosensitivity, anaphylactic reactions up to shock.

Other phenomena: decreased potency, impaired renal function, interstitial nephritis.

Interaction

Avoid the simultaneous use of the drug with lithium salts (renal clearance
lithium decreases, its toxicity increases).

Use with caution with following drugs:

- antihypertensive drugs (their effect is potentiated, may appear
the need for dose adjustment);

- cardiac glycosides (hypokalemia and hypomagnesemia associated with the action
thiazide diuretics, may increase digitalis toxicity);

- amiodarone (its use simultaneously with thiazide diuretics can lead to
increased risk of arrhythmias associated with hypokalemia);

- hypoglycemic agents for oral administration (their effectiveness decreases, may
develop hyperglycemia);

- corticosteroid drugs, calcitonin (increase the degree of excretion
potassium);

- NSAIDs (can weaken the diuretic and hypotensive effect of thiazides);

- non-depolarizing muscle relaxants (their effect may be enhanced);

- amantadine (clearance of amantadine can be reduced by hydrochlorothiazide, which leads to
an increase in plasma amantadine concentration and possible toxicity);

- cholestyramine, which reduces the absorption of hydrochlorothiazide;

- ethanol, barbiturates and narcotic analgesics, which enhance the effect
orthostatic hypotension.

The effect of the drug on laboratory test data

Thiazides can reduce plasma levels of iodine bound to proteins.

Before performing analyzes of the function of the parathyroid glands, thiazides should be canceled.
The serum bilirubin concentration may be increased.

Method of administration and dosage

Inside, after eating.

The dosage should be selected individually. With constant medical
control is established the minimum effective dose.

Due to the increased loss of potassium and magnesium ions during treatment (level
serum potassium may decrease below 3.0 mmol / L), there is a need for potassium replacement and
magnesium.

Adults. As an antihypertensive agent, the usual initial
the daily dose is 25-50 mg once, as monotherapy or in combination with others
antihypertensive drugs. For some patients, an initial dose of 12.5 mg is sufficient, both in the form
monotherapy and in combination. It is necessary to use the minimum effective dose not exceeding
100 mg / day If Hypothiazid® is combined with other antihypertensive drugs, it may
it becomes necessary to reduce the dose of another drug in order to prevent an excessive decrease
HELL.

The antihypertensive effect appears within 3-4 days, however, for
it may take up to 3-4 weeks to achieve the optimal effect. After the end of treatment
the hypotensive effect lasts for 1 week.

Edematous syndrome of various origins. The usual starting dose for treatment
edema is 25-100 mg of the drug 1 time per day or 1 time per 2 days. Depending on the clinical
reactions, the dose can be reduced to 25-50 mg 1 time per day or 1 time in 2 days. In some heavy
cases at the beginning of treatment may require doses of up to 200 mg / day.

For premenstrual syndrome, the usual dose is 25 mg / day and
it is used from the onset of symptoms to the onset of menstruation.

Children. Doses should be adjusted based on the weight of the child.
Usual pediatric daily doses are 1–2 mg / kg or 30–60 mg / m2
body surfaces are prescribed once a day. Total daily dose for children aged 3 to 12 years
- 37.5-100 mg.

Overdose

The most noticeable manifestation of an overdose of hydrochlorothiazide is an acute loss of fluid and electrolytes, expressed in following signs and symptoms:

Cardiovascular: tachycardia, decreased blood pressure, shock.

Neuromuscular: weakness, confusion, dizziness and spasms of the calf muscles, paresthesia, impaired consciousness, fatigue.

Gastrointestinal: nausea, vomiting, thirst.

Renal: polyuria, oliguria, or anuria (due to hemoconcentration).

Laboratory indicators: hypokalemia, hyponatremia, hypochloremia, alkalosis, elevated level blood urea nitrogen (especially in patients with renal failure).

Treatment: there is no specific antidote for hydrochlorothiazide overdose.

Induction of vomiting, gastric lavage can be methods of drug elimination.

The absorption of the drug can be reduced by prescribing activated carbon... In case of a decrease in blood pressure or shock, the BCC and electrolytes (potassium, sodium) should be replaced.

Watch out for water and electrolyte balance(especially serum potassium) and renal function to normal.

special instructions

With prolonged course of treatment, it is necessary to carefully monitor clinical symptoms disturbances in water and electrolyte balance, primarily in high-risk patients: patients with diseases of the cardiovascular system and impaired liver function; in case of severe vomiting or when there are signs of a violation of the water and electrolyte balance, such as dry mouth, thirst, weakness, lethargy, drowsiness, anxiety, muscle pain or cramps, muscle weakness, hypotension, oliguria, tachycardia, complaints from the gastrointestinal tract.

Hypokalemia can be avoided by using potassium-containing drugs or food, rich in potassium(fruits, vegetables), especially in the case of increased loss of potassium (increased diuresis, prolonged treatment) or simultaneous treatment with digitalis glycosides or corticosteroid drugs.

It has been shown that thiazides increase the excretion of magnesium in the urine; this can lead to hypomagnesemia.

With reduced renal function, creatinine clearance must be monitored. In patients with impaired renal function, the drug can cause azotemia, and cumulative effects can also develop. If impaired renal function is obvious, with the onset of oliguria, the possibility of discontinuing the drug should be considered.

Patients with impaired liver function or with progressive liver disease are prescribed thiazides with caution, since a small change in the water-electrolyte balance, as well as the level of ammonium in the serum, can cause hepatic coma.

In the case of severe cerebral and coronary sclerosis, the administration of the drug requires special care.

Treatment with thiazide drugs may interfere with glucose tolerance. During a long course of treatment with overt and latent diabetes mellitus, systematic monitoring of carbohydrate metabolism is necessary; it may be necessary to change the dose of hypoglycemic drugs. Increased monitoring of patients with impaired uric acid metabolism is required.

Alcohol, barbiturates, narcotic analgesics increase the orthostatic hypotensive effect of thiazide diuretics.

With long-term therapy, in rare cases, a pathological change was observed parathyroid glands accompanied by hypercalcemia and hypophosphatemia. Thiazides can reduce the amount of iodine that binds to serum proteins without showing signs of thyroid dysfunction.

In patients suffering from lactose intolerance, gastrointestinal complaints may appear due to the presence of lactose in the tablets: Hypothiazid® 25 mg tablets contain 63 mg of lactose, Hypothiazid® 100 mg - 39 mg of lactose.

Impact on the ability to drive and perform work requiring increased attention. V initial stage the use of the drug (the duration of this period is determined individually), it is forbidden to drive a car and perform work requiring increased attention.

Conditions of dispensing from pharmacies

On prescription.

Storage conditions of the drug Hypothiazid®

In a dark place at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life of the drug Hypothiazid®

Do not use after the expiration date printed on the package.

Sources of

  • https://allmed.pro/drugs/dihlotiazid
  • http://www.BazaTabletok.ru/dihlotiazid
  • https://www.rlsnet.ru/tn_index_id_1025.htm

Gross formula

C 7 H 8 ClN 3 O 4 S 2

Pharmacological group of the substance Hydrochlorothiazide

Nosological classification (ICD-10)

CAS code

58-93-5

Characteristics of the substance Hydrochlorothiazide

White or yellow crystalline powder. Slightly soluble in water, hardly soluble in methanol, insoluble in ether, readily soluble in alkaline solutions. Molecular weight 297.72.

Pharmacology

pharmachologic effect- diuretic, hypotensive.

Reduces the reabsorption of sodium and chlorine ions (to a lesser extent - potassium and bicarbonates) in the proximal tubules of the kidneys, increases the excretion of magnesium ions, reduces - ions of calcium, uric acid. Inhibits the reactivity of the vascular wall in relation to the vasoconstrictor effects of mediators due to a decrease in the concentration of sodium ions in the cytoplasm of vascular myocytes, reduces the BCC, lowers blood pressure.

Incompletely, but rather quickly absorbed from the gastrointestinal tract. In the blood, it binds to proteins by 40-60%. Penetrates through the hematoplacental barrier and into breast milk. It is excreted by the kidneys. The diuretic effect develops after 30-60 minutes, reaches a maximum after 4-6 hours, and lasts for 6-12 hours.

Application of the substance Hydrochlorothiazide

Arterial hypertension (monotherapy or in combination with other antihypertensive drugs), edematous syndrome of various origins (chronic heart failure, nephrotic syndrome, premenstrual syndrome, acute glomerulonephritis, chronic renal failure, portal hypertension, treatment with corticosteroids), control of polyuria (mainly in nephrogenic non-sucrose) ), prevention of the formation of stones in the genitourinary tract in predisposed patients (reduction of hypercalciuria).

Contraindications

Hypersensitivity (including to other sulfonamides), anuria, severe renal (Cl creatinine - less than 30 ml / min) or liver failure, difficult-to-control diabetes mellitus, Addison's disease, gout, childhood (up to 3 years).

Restrictions on use

Hypokalemia, hyponatremia and hypercalcemia, ischemic heart disease, simultaneous intake of cardiac glycosides, liver and kidney dysfunctions, pregnancy, old age.

Application during pregnancy and lactation

Discontinue during treatment breast-feeding.

Side effects of the substance Hydrochlorothiazide

Electrolyte imbalance

Hypokalemia, hypomagnesemia, hypercalcemia and hypochloremic alkalosis: dry mouth, thirst, irregular heart rhythm, changes in mood or psyche, muscle cramps and pain, nausea, vomiting, unusual tiredness or weakness. Hypochloremic alkalosis can cause hepatic encephalopathy or hepatic coma.

Hyponatremia: confusion, convulsions, lethargy, slowing down of the thinking process, fatigue, excitability, muscle cramps.

Metabolic phenomena: hyperglycemia, glucosuria, hyperuricemia with the development of a gout attack. Treatment with thiazides can reduce glucose tolerance, and latent diabetes mellitus may manifest. Serum lipid levels may increase with high doses.

From the digestive tract: cholecystitis or pancreatitis, cholestatic jaundice, diarrhea, sialadenitis, constipation, anorexia.

On the part of the cardiovascular system and blood (hematopoiesis, hemostasis): arrhythmias, orthostatic hypotension, vasculitis; very rarely - leukopenia, agranulocytosis, thrombocytopenia, hemolytic anemia, aplastic anemia.

From the nervous system and sensory organs: dizziness, blurry vision (temporary), headache, paresthesia.

Hypersensitivity reactions: urticaria, purpura, necrotizing vasculitis, Stevens-Johnson syndrome, respiratory distress syndrome (including pneumonitis and noncardiogenic pulmonary edema), photosensitivity, anaphylactic reactions up to shock.

Others: decreased potency, impaired renal function, interstitial nephritis.

Updating information

The risk of developing acute transient myopia and acute angle-closure glaucoma

In the post-registration period, information appeared that hydrochlorothiazide can cause acute transient myopia and acute angle-closure glaucoma. Symptoms of these NCDs include decreased vision, eye pain, and may develop hours or weeks after starting the drug. Angle-closure glaucoma can lead to complete loss of vision. If complications develop, it is recommended to stop taking hydrochlorothiazide. Increased intraocular pressure may require surgery.

[Updated 14.02.2012 ]

Interaction

The simultaneous use of hydrochlorothiazide with lithium salts should be avoided (renal clearance of lithium decreases, its toxicity increases).

It should be used with caution with antihypertensive drugs (their effect is potentiated, it may be necessary to adjust the dose), cardiac glycosides (hypokalemia and hypomagnesemia associated with the action of thiazide diuretics can increase the toxicity of digitalis), amiodarone (its use simultaneously with thiazide diuretics can lead to increased risk of arrhythmias associated with hypokalemia), oral hypoglycemic agents (their effectiveness decreases, hyperglycemia may develop), corticosteroids, calcitonin (increase potassium excretion), NSAIDs (may weaken the diuretic and hypotensive effect of thiazides), non-depolarizing muscle relaxants (their effect may increase), amantadine (clearance of amantadine can be reduced by hydrochlorothiazide, which leads to an increase in the concentration of amantadine in plasma and possible toxicity), cholestyramine (reduces the absorption of hydrochlorothiazide), ethanol, barbiturates and narcotic analgesics, which increase effect of orthostatic hypotension.

Thiazides can reduce plasma levels of iodine bound to proteins.

Before performing analyzes of the function of the parathyroid glands, thiazides should be canceled. The serum bilirubin concentration may be increased.

Overdose

Symptoms: dehydration, pronounced electrolyte disturbances, confusion, dry mouth, lethargy, muscle weakness, drowsiness, tachycardia, hypotension, oliguria, decreased blood pressure, shock.

Treatment: induction of vomiting, gastric lavage, intravenous administration of fluids, electrolytes, symptomatic therapy. The specific antidote is unknown.

Route of administration

Inside.

Precautions for the substance Hydrochlorothiazide

With long-term course treatment, it is necessary to carefully monitor the clinical symptoms of imbalance in the water-electrolyte balance, primarily in high-risk patients: patients with diseases of the cardiovascular system and impaired liver function; in case of severe vomiting or when there are signs of a violation of the water and electrolyte balance, such as dry mouth, thirst, weakness, lethargy, drowsiness, anxiety, muscle pain or cramps, muscle weakness, hypotension, oliguria, tachycardia, complaints from the gastrointestinal tract.

Hypokalemia, especially in the case of increased potassium loss (increased diuresis, prolonged treatment) or simultaneous treatment with digitalis glycosides or corticosteroid drugs, can be avoided by using potassium-containing drugs or foods rich in potassium (fruits, vegetables). It has been shown that thiazides increase the excretion of magnesium in the urine, which can lead to hypomagnesemia.

With reduced renal function, creatinine clearance must be monitored. In patients with impaired renal function, the drug can cause azotemia, and cumulative effects can also develop. If impaired renal function is obvious, with the onset of oliguria, the possibility of discontinuing the drug should be considered.

Patients with impaired liver function or progressive liver disease should be prescribed thiazides with caution, since a small change in the water-electrolyte balance, as well as the level of ammonium in the serum, can cause hepatic coma.

Dichlothiazide is a diuretic agent containing the active ingredient hydrochlorothiazide. It is used for the treatment of edema and essential hypertension.

Dichlothiazide

Attention! In the ATC pharmacology handbook, the drug is indicated by Latin letters and numbers C03AB03. The international non-proprietary name of Dichlothiazide is hydrochlorothiazide.

Dichlothiazide acts in the same way as other thiazide-type dehydrating agents. An active chemical compound blocks transport system sodium and chloride in kidney cells. As a result, sodium chloride (NaCl) and the associated water are excreted more quickly from the body. Dichlotiaizd is similar in some situations to loop diuretics. It promotes the excretion of potassium in the urine and is effective even with impaired renal function.


Pharmacodynamics of the drug

Indications for use

Hydrochlorothiazide increases the excretion of fluids and electrolytes (sodium, chloride, potassium, and calcium through the kidneys). It is used to remove water from tissues (edema). Swelling can have different causes: heart disease, liver disease or kidney disease.

Increased fluid excretion reduces blood pressure making dichotiazide an effective antihypertensive drug in the treatment of essential hypertension.

Dichlothiazide: instructions for use

Dichlothiazide tablets are available with 12.5 mg and 25 mg of active ingredient. Several lower dose tablets can be taken to achieve the desired dosage. Conversely, the tablets in a large dosage are divided in half.

In the treatment of high blood pressure, 12.5 to 25 mg is initially prescribed active ingredient once a day.

In the treatment of edema, 25 to 50 mg of Dichlothiazide is used once a day. For long-term therapy, it is recommended to use 25 to 50 and a maximum of 100 mg per day. In chronic myocardial insufficiency, together with ACE inhibitors, 25 to 37.5 mg of dichothiazide are prescribed per day. In case of liver dysfunction or renal dysfunction, the dose should be adjusted accordingly.

It should be noted that analogs (hypothiazide) and the original drug are available with a prescription.

Important! Only the attending physician can write out a prescription form. The price of drugs containing HCT varies greatly.

Contraindications

Dichlothiazide should not be used when:

  • Hypersensitivity to sipamide, thiazides, or sulfonamides;
  • Severe liver dysfunction;
  • Low concentration of potassium in the bloodstream;
  • High concentration of calcium in the blood;
  • Concomitant therapy with spironolactone;
  • Gout;
  • Overly reduced level sodium;
  • Dehydration and anemia.

With an increase in the level of uric acid in the blood, low blood pressure, circulatory disorders of the coronary and cerebral vessels, diabetes, the use of the drug by the doctor is considered only with caution and with the ineffectiveness of safer analogues.

Pregnancy, lactation and childhood use

Dichlothiazide should not be taken during pregnancy and lactation. This can cause side effects that could harm the baby.

Children should not be treated with Dichlothiazide.

Side effects

Very common side reactions:

  • Deficiency of potassium in the blood;
  • Gastric disorders;
  • ECG changes;
  • Increased sensitivity to cardiac glycosides;
  • Cardiac arrhythmia;
  • Atony.

Common side effects:

  • Apathy;
  • Lethargy;
  • Anxiety;
  • Excitation;
  • Headache;
  • Dizziness;
  • Hyposalivation;
  • Fatigue;
  • Hyperhidrosis;
  • Orthostatic hypotension;
  • Palpitations;
  • Occlusion of blood vessels (with venous disease and high doses);
  • Stomach ache;
  • Diarrhea;
  • Constipation;
  • Muscle spasms;
  • Fluid balance disorders;
  • Metabolic disorders mineral substances in organism.

Rare side effects:

  • Allergic reactions;
  • An increase in the concentration of fats in the blood;
  • The onset of diabetes mellitus;
  • Increased blood sugar (hyperglycemia);
  • Visual impairment;
  • Bleeding in the pancreas (due to inflammation);
  • Gallstones
  • Allergic reactions skin(itching, redness, hives, chronic sensitivity to light);
  • Deficiency of magnesium in the blood (with seizures or cardiac arrhythmias).

The increased excretion of minerals and water due to treatment can generally cause or worsen acid deficiency in the body (metabolic alkalosis). The concentration of uric acid in the blood can increase and lead to gout. Severe dehydration can dry out the body.

At the same time, absorption may decrease or potassium loss may increase, for example, with vomiting, chronic diarrhea or severe hyperhidrosis of the extremities. This can manifest as muscle weakness, nerve abnormalities, and paralysis. Severe loss of potassium can cause intestinal paralysis or coma.


Hydrochlorothiazide

Increased urinary sodium excretion can lead to hyponatremia, especially if sodium chloride is not consumed in adequate amounts. Common Symptoms include apathy, angina, loss of appetite, weakness, drowsiness, vomiting, and confusion.

An increase in calcium excretion can lead to hypocalcemia. This in rare cases causes severe seizures.

Treatment with dichothiazide should be discontinued by the doctor immediately if the following side effects occur: increased myopia, pancreatitis, low blood pressure with changes in body position, gallbladder infections, anemia, uncontrolled mineral imbalance, severe stomach upset, impaired brain function, vascular inflammation and anaphylaxis.

Interactions

Dichlothiazide increases the main and side effects of digoxin and other cardiac glycosides, which can increase cardiac output due to increased potassium excretion.

The toxic effect of lithium increases when combined with Dichlothiazide.

The effect of antidiabetic substances, that is, drugs for lowering blood sugar levels, is reduced when administered simultaneously with Dichlothiazide.

Combination with diazoxide, a drug to reduce blood pressure, can lead to an excessive decrease in blood pressure and an increase in blood sugar and uric acid levels. The risk of severe hypotension exists with concomitant use ACE inhibitors, which are also prescribed to treat high blood pressure.

When combined with non-steroidal anti-inflammatory drugs (NSAIDs) such as acetylsalicylic acid, therapeutic effect Dichlothiazide decreases.

Co-administration with licorice root, which is often found in mucolytic mixtures, can lead to life-threatening hypokalemia. This also applies to the simultaneous use of Dichlothiazide with laxatives or glucocorticoids.

If calcium supplements or vitamin D derivatives are taken at the same time, there may be a sharp increase in blood calcium levels.

Precautionary measures

If Dichlothiazide is taken for a long period of time, it is necessary to monitor the concentration of blood sugar, lipids, uric acid, creatinine and electrolytes (especially potassium).

Care must be taken during treatment with Dichlothiazide and constantly drink the right amount of liquid. Otherwise, life-threatening dehydration may occur.


Potassium

The medication can affect the psychomotor response to the extent that driving can be dangerous.

Advice! Dichlothiazide can cause allergic reactions of varying severity. Therefore, when any warning signs allergies, you must immediately contact your doctor or call an ambulance.

Yet:

The mechanism of action of Ko-Renitek, composition, precautions for use, instructions for use, analogs, prices and reviews

6-chloro-7-sulphamoyl-3,4-dihydro-2-H-l, 2,4-benzothiadiazine-1,1-dioxide.

Synonyms: Hypothiazide, Dihydrochlorthiazid, Disalunil, Nefrix, Unazid, Urodiazin.

Release form... Tablets of 0.025 and 0.1 g.

Pharmacokinetics... Well absorbed (70-80%) from the digestive system. After oral administration of 0.075 g, the maximum concentration in blood plasma occurs after 1.5-3 hours, in patients with heart failure - after 8 hours. digestive tract increases in case of admission drug while eating. Half-life - 6-15 hours drug with urine decreases to 21-63%. Renal clearance is normally 330 ml / min, and in heart failure - 10-187 ml / min, and there is a direct correlation with creatinine clearance. After ingestion a drug has a diuretic effect after 2-3 hours, maximum effect occurs in 3-6 hours, its duration is 6-12 hours and more, and in the first half of the period of action, the saluretic effect predominates, and in the second, the diuretic effect. The maximum diuretic effect is manifested when administered drug at midnight, minimum - at 8 am.

Pharmacodynamics... It is excreted from the body both by filtration and glomeruli, and by secretion in the proximal tubules. Here, basically, its ability to inhibit tubular sodium reabsorption is manifested. In addition to the effect on the enzyme carbonic anhydrase, dichlothiazide can inhibit the activity of sodium, potassium, ATPase, succinate dehydrogenase, as well as oxidation enzymes of non-esterified fatty acids, etc. All this disrupts the energy supply of transport mechanisms on the basement membrane. In addition, it was shown that against the background of dichlothiazide, the permeability of the basement membrane for sodium changes, as a result of which energy consumption increases for its reabsorption. There are reports that thiazides in the distal tubules, without affecting the active transport of sodium, reduce electrical resistance, increasing the permeability to sodium chloride and promoting the return flow of already reabsorbed sodium chloride into the tubule.

The drug does not have a significant effect on the acid-base state, therefore it can be prescribed both for acidosis and for alkalosis. Chlorides are released in ratios equivalent to sodium, HCO 3 ions - in physiological amounts. The excretion of potassium increases under its influence, therefore hypokalemia may develop. This may be due to the blockade of potassium reabsorption in the proximal tubules of the nephron and a compensatory increase in its secretion in the distal ones due to the greater loading of this section of the nephron with sodium.

Dichlothiazide, secreted by the cells of the tubules of the nephron, can, by a competitive type, inhibit the secretion of uric acid and lead to an exacerbation of gout.

Hypotensive effect drug is caused not only by increased fluid loss and a decrease in the volume of intravascular fluid and a decrease in edema of the vascular wall, but mainly by a decrease in the sensitivity of smooth muscles vessels to catecholamines.

The beneficial effect of dichlothiazide in diabetes insipidus depends, apparently, on its ability to block thirst, directly affecting the thirst center, and by reducing the stimulation of this center by high plasma osmolarity. By increasing sodium excretion, a drug greatly reduces the increased osmotic pressure blood plasma accompanying this disease. By inhibiting the enzyme phosphodiesterase in the kidneys, it sensitizes the kidneys to endogenous vasopressin.

Application... With water retention in the body. Effective even in case of long-term use. With edema due to cardiovascular failure, liver cirrhosis, nephrotic syndrome, toxicosis of pregnancy, premenstrual syndrome, taking corticosteroids, obesity, with hypothalamic pathology, as well as with localized edema. Assign 0.025-0.1 g per day (in 1-2 doses), sometimes 0.2 g per day in the morning for 3-7 days with 3-4 days interruptions. When increasing daily dose more than 0.2 g, the diuretic effect increases. If necessary, long-term treatment appoint 2-3 times a week.

During the period treatment it is necessary to prescribe a potassium diet or (in case of use in large doses, long-term use) combine dichlothiazide with potassium preparations.

With hypertension and symptomatic hypertension, dichlothiazide is prescribed in slightly smaller doses(0.025-0.075 g), mainly in combination with antihypertensive and antispasmodics daily or every other day. In the absence of edema, the drug, without exerting a pronounced diuretic effect, reduces pressure due to, as it is assumed, the redistribution of sodium in the cells of the vascular walls, a decrease in blood mass and the sensitivity of cells to catecholamines.

When taking dichlothiazide, blood pressure decreases by the end of the 2nd day treatment due to a decrease in the minute volume of the heart (first phase of action), then the total peripheral resistance gradually decreases (second phase of action); clinical effect due to decreased tone vessels usually occurs after 2-3 weeks of treatment.

In patients with glaucoma, to lower intraocular pressure (more often with subcompensated forms), 0.025 g per day is prescribed. The effect occurs within 24-48 hours after administration drug and against the background of miotic drugs lasts 1-6 days, after which a drug must be re-entered.

With diabetes insipidus, under the influence of dichlothiazide, polyuria and thirst are reduced. Initially, 0.025 g is prescribed 1-2 times a day, then dose gradually increase until a therapeutic effect is achieved.

The drug can potentiate the effectiveness of antiblastoma drugs.

Side effect... For long-term use in large enough doses hypokalemia and hypochloremic alkalosis are possible. Hypokalemia, as a rule, develops in patients with liver cirrhosis and nephrotic syndrome, hypochloremic alkalosis - with a salt-free diet and chloride loss due to vomiting and diarrhea.

In the case of prolonged use, exacerbation of gout, hyperglycemia and exacerbation of diabetes mellitus are possible due to overstrain of the insular apparatus. And large doses dichlothiazide can cause general weakness, nausea, vomiting, diarrhea, and, in rare cases, dermatitis.

A decrease in glomerular filtration in the case of dichlothiazide use can be explained, on the one hand, by a decrease in tubular reabsorption, an increase in intratubular pressure, as a result of which ultrafiltration into the nephron capsule decreases, on the other hand, by a decrease in the volume of extracellular fluid, a decrease in blood pressure.

Contraindications to the appointment... Severe liver failure, diabetic glomerulosclerosis, chronic kidney disease in the stage of chronic renal failure With hypoisostenuria and azotemia, oliguria and anuria in the first 3 months of pregnancy. Conditionally contraindicated in patients with gout and diabetes mellitus. Should be administered with caution in patients with reduced carbohydrate tolerance.

Interacting with others medicines . A drug should be prescribed with caution in combination with antihypertensive drugs because of the possibility of orthostatic hypotension due to the potentiation of their effect. Combined appointment drug with cardiac glycosides, it is dangerous due to the hypokalemic effect of dichlothiazide. Dichlothiazide enhances the ototoxicity of some antibiotics, reduces the sensitivity of body tissues to adrenomimetics.

To enhance the diuretic effect, dichlothiazide can be combined with drugs acting at the level of the apical membrane (spironolactone); at the same time, the risk of hypokalemia and disorders of the acid-base state decreases.

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