Composition, structure and packing
Tablets are round, flat, light-orange color, with beveled edges on the surface of tablets allowed blotches of darker color on one side - the risk and engraved "APO" over "50-25", the other side is smooth.
1 tab. triamterene hydrochlorothiazide 25 mg to 50 mg.
Excipients: lactose monohydrate, magnesium stearate, colloidal silicon dioxide (aerosil), sodium croscarmellose, dye Sunset Yellow.
Clinico-pharmacological group: diuretics combined composition.
Pharmacological action
Combined medication. Has diuretic and hypotensive action.
Hydrochlorothiazide - thiazide diuretics, diuretic effect of which involves a violation of the reabsorption of sodium, chlorine, potassium, magnesium, water in the distal nephron: delayed excretion of calcium, uric acid. It has antihypertensive properties; hypotensive action develops through the expansion of arterioles. Has no effect on normal blood pressure. Diuretichesky effect of hydrochlorothiazide occurs after 1-2 h, reaches a maximum in 4 hours and lasts 6-12 hours antihypertensive effect occurs within 3-4 days, but to achieve the optimal therapeutic effect may take 3-4 weeks.
Triamterene - Potassium-sparing diuretics, reduces the permeability of cell membranes of the distal renal tubules to sodium ions and increases their excretion in the urine without increasing the excretion of potassium ions. Secretion of potassium ions in the distal tubule is reduced. In combination with hydrochlorothiazide triamterene can reduce hypokalemia, caused by thiazide diuretics, and enhance the diuretic effect of hydrochlorothiazide.
Triamterene diuretic effect after oral administration indicated after 15-20 min. The maximum effect - in 2-3 hours, duration - 12 hours
Pharmacokinetics
Hydrochlorothiazide
Absorption and distribution
After oral hydrochlorothiazide absorbed from the digestive tract quickly, but not completely (60-80% of the accepted oral dose). Cmax plasma levels of 2 mg / ml. Linking to plasma proteins is 40%, Vd - 3-4 L / kg. Hydrochlorothiazide crosses the placental barrier.
Metabolism and excretion
T1 / 2 - about 3-4 hours Hydrochlorothiazide is not exposed to significant metabolism. We derive the kidneys (mainly due to filtration and secretion) unchanged.
Triamterene
Absorption and distribution
Once inside quickly, but not completely (30-70% of applied dose) absorbed from the gastrointestinal tract. Cmax plasma levels achieved after 2-4 h. The binding to plasma proteins is 67%.
Metabolism and excretion
Biotransformiruetsya in the liver with the formation of both active and inactive metabolites. T1 / 2 in the norm of 1.5-2 h (anuria - 10 h), metabolites - up to 12 hours is derived mainly from the bile and feces, the second - by the kidneys.
Statement
edematous syndrome of different genesis (chronic heart failure, nephrotic syndrome, cirrhosis of the liver);
hypertension.
Dosage regimen
Tablets taken by mouth, without chewing, drinking small amounts of water after a meal. When edema initial dose is determined by the severity of violations of water-electrolyte metabolism and is usually on 1 tab. 2 times / day after meals. More may increase the dose to a maximum of 3 pi. / day (2 tabs. After breakfast and 1 tablet. After dinner).
With the recovery of swelling switching to maintenance therapy for 1-2 pi. within 1-2 days.
When hypertension the initial dose - 1 tab. / day (morning, after breakfast), then gradually increase the dose. The maximum daily dose - 4 pi. Patients with impaired renal function (CC 30-50 ml / min) maximum daily dose - 1 tab.
Side effect
From the CNS: fatigue, convulsions.
Since the cardiovascular system: heart rate, marked reduction of blood pressure, rarely - thrombosis, embolism.
From the urinary system: rarely - increased content of urea in the blood, nephrolithiasis, dry mouth, thirst.
On the part of the digestive system: rarely - pain or discomfort in the epigastric region, nausea, vomiting, abdominal pain, spastic nature, constipation, diarrhea, jaundice, hemorrhagic pancreatitis, acute cholecystitis.
On the part of metabolism: rarely - hyponatremia, gipomagniemiya, chloropenia, hypo-or hyperkalemia, hypercalcemia, hyperuricemia, exacerbation of gout, hypertriglyceridemia, reduced glucose tolerance, hyperglycemia.
Allergic reactions: sometimes - redness, itching, hives.
Other: muscle weakness; rare - the growth of short-sightedness, and sometimes - anemia.
Contraindications
chronic renal failure;
anuria;
acute glomerulonephritis;
marked hepatic impairment;
precoma, hepatic coma;
hyperkalaemia;
I trimester of pregnancy;
lactation;
the age of 18 years (effectiveness and safety have not been established);
Hypersensitivity to the drug's components and sulfanilamide.
With care prescribers in diabetes, gout, patients with impaired liver function and / or kidneys, with deficit of folic acid (in patients with cirrhosis of the liver).
Beremennnost and lactation
The drug is contraindicated for use in the I trimester of pregnancy and during lactation.
Application for violations of liver function
Be wary prescribers to patients with disorders of the liver.
Application for violations of renal function
Be wary prescribers to patients with impaired renal function. Contraindicated in renal failure.
Cautions
Prolonged use of Apo-Triazida need to control the blood content of potassium ions, sodium, chloride, urea, creatinine, glucose, uric acid, complete blood count (that is suspected of a lack of folic acid).
With the passage of the drug should not take two doses at once.
Effects on ability to drive vehicles and management mechanisms
At the beginning of drug treatment should be avoided classes of potentially hazardous activities that require attention and speed of psychomotor reactions (on the background of BP reduction may slow down the speed of psychomotor reactions).
Overdose
Symptoms: marked reduction of BP. Treatment: If necessary, a symptomatic therapy.
Drug Interactions
With simultaneous use of drugs extensively bound to plasma proteins of blood (indirect anticoagulants, clofibrate, NSAIDs), increase the diuretic effect of the drug.
With simultaneous application of anti-hypertensive effect of Apo-Triazida reinforce vasodilators, barbiturates, phenothiazines, tricyclic antidepressants, ethanol.
When the joint application of Apo-Triazid enhances neurotoxicity salicylates, reduces the effect of oral hypoglycemic funds, norepinephrine, epinephrine and arthrifuge, intensifies the effects (including spin), cardiac glycosides, cardiotoxic and neurotoxic effects of drugs lithium action curariform muscle relaxant, reduces excretion of quinidine.
When applied simultaneously with methyldopa increased risk of hemolysis.
At the same time.The kolestiramin reduces the absorption of Apo-Triazida. Hlorpropamid while reception with Apo-Triazidom can lead to marked hypokalemia. When combined with NSAIDs may develop acute renal failure.
Terms and Conditions of storage
List B. The drug should be stored in a dry, protected from light and away from children at a temperature of 15 ° to 25 ° C. Shelf life - 4 years.
Tablets are round, flat, light-orange color, with beveled edges on the surface of tablets allowed blotches of darker color on one side - the risk and engraved "APO" over "50-25", the other side is smooth.
1 tab. triamterene hydrochlorothiazide 25 mg to 50 mg.
Excipients: lactose monohydrate, magnesium stearate, colloidal silicon dioxide (aerosil), sodium croscarmellose, dye Sunset Yellow.
Clinico-pharmacological group: diuretics combined composition.
Pharmacological action
Combined medication. Has diuretic and hypotensive action.
Hydrochlorothiazide - thiazide diuretics, diuretic effect of which involves a violation of the reabsorption of sodium, chlorine, potassium, magnesium, water in the distal nephron: delayed excretion of calcium, uric acid. It has antihypertensive properties; hypotensive action develops through the expansion of arterioles. Has no effect on normal blood pressure. Diuretichesky effect of hydrochlorothiazide occurs after 1-2 h, reaches a maximum in 4 hours and lasts 6-12 hours antihypertensive effect occurs within 3-4 days, but to achieve the optimal therapeutic effect may take 3-4 weeks.
Triamterene - Potassium-sparing diuretics, reduces the permeability of cell membranes of the distal renal tubules to sodium ions and increases their excretion in the urine without increasing the excretion of potassium ions. Secretion of potassium ions in the distal tubule is reduced. In combination with hydrochlorothiazide triamterene can reduce hypokalemia, caused by thiazide diuretics, and enhance the diuretic effect of hydrochlorothiazide.
Triamterene diuretic effect after oral administration indicated after 15-20 min. The maximum effect - in 2-3 hours, duration - 12 hours
Pharmacokinetics
Hydrochlorothiazide
Absorption and distribution
After oral hydrochlorothiazide absorbed from the digestive tract quickly, but not completely (60-80% of the accepted oral dose). Cmax plasma levels of 2 mg / ml. Linking to plasma proteins is 40%, Vd - 3-4 L / kg. Hydrochlorothiazide crosses the placental barrier.
Metabolism and excretion
T1 / 2 - about 3-4 hours Hydrochlorothiazide is not exposed to significant metabolism. We derive the kidneys (mainly due to filtration and secretion) unchanged.
Triamterene
Absorption and distribution
Once inside quickly, but not completely (30-70% of applied dose) absorbed from the gastrointestinal tract. Cmax plasma levels achieved after 2-4 h. The binding to plasma proteins is 67%.
Metabolism and excretion
Biotransformiruetsya in the liver with the formation of both active and inactive metabolites. T1 / 2 in the norm of 1.5-2 h (anuria - 10 h), metabolites - up to 12 hours is derived mainly from the bile and feces, the second - by the kidneys.
Statement
edematous syndrome of different genesis (chronic heart failure, nephrotic syndrome, cirrhosis of the liver);
hypertension.
Dosage regimen
Tablets taken by mouth, without chewing, drinking small amounts of water after a meal. When edema initial dose is determined by the severity of violations of water-electrolyte metabolism and is usually on 1 tab. 2 times / day after meals. More may increase the dose to a maximum of 3 pi. / day (2 tabs. After breakfast and 1 tablet. After dinner).
With the recovery of swelling switching to maintenance therapy for 1-2 pi. within 1-2 days.
When hypertension the initial dose - 1 tab. / day (morning, after breakfast), then gradually increase the dose. The maximum daily dose - 4 pi. Patients with impaired renal function (CC 30-50 ml / min) maximum daily dose - 1 tab.
Side effect
From the CNS: fatigue, convulsions.
Since the cardiovascular system: heart rate, marked reduction of blood pressure, rarely - thrombosis, embolism.
From the urinary system: rarely - increased content of urea in the blood, nephrolithiasis, dry mouth, thirst.
On the part of the digestive system: rarely - pain or discomfort in the epigastric region, nausea, vomiting, abdominal pain, spastic nature, constipation, diarrhea, jaundice, hemorrhagic pancreatitis, acute cholecystitis.
On the part of metabolism: rarely - hyponatremia, gipomagniemiya, chloropenia, hypo-or hyperkalemia, hypercalcemia, hyperuricemia, exacerbation of gout, hypertriglyceridemia, reduced glucose tolerance, hyperglycemia.
Allergic reactions: sometimes - redness, itching, hives.
Other: muscle weakness; rare - the growth of short-sightedness, and sometimes - anemia.
Contraindications
chronic renal failure;
anuria;
acute glomerulonephritis;
marked hepatic impairment;
precoma, hepatic coma;
hyperkalaemia;
I trimester of pregnancy;
lactation;
the age of 18 years (effectiveness and safety have not been established);
Hypersensitivity to the drug's components and sulfanilamide.
With care prescribers in diabetes, gout, patients with impaired liver function and / or kidneys, with deficit of folic acid (in patients with cirrhosis of the liver).
Beremennnost and lactation
The drug is contraindicated for use in the I trimester of pregnancy and during lactation.
Application for violations of liver function
Be wary prescribers to patients with disorders of the liver.
Application for violations of renal function
Be wary prescribers to patients with impaired renal function. Contraindicated in renal failure.
Cautions
Prolonged use of Apo-Triazida need to control the blood content of potassium ions, sodium, chloride, urea, creatinine, glucose, uric acid, complete blood count (that is suspected of a lack of folic acid).
With the passage of the drug should not take two doses at once.
Effects on ability to drive vehicles and management mechanisms
At the beginning of drug treatment should be avoided classes of potentially hazardous activities that require attention and speed of psychomotor reactions (on the background of BP reduction may slow down the speed of psychomotor reactions).
Overdose
Symptoms: marked reduction of BP. Treatment: If necessary, a symptomatic therapy.
Drug Interactions
With simultaneous use of drugs extensively bound to plasma proteins of blood (indirect anticoagulants, clofibrate, NSAIDs), increase the diuretic effect of the drug.
With simultaneous application of anti-hypertensive effect of Apo-Triazida reinforce vasodilators, barbiturates, phenothiazines, tricyclic antidepressants, ethanol.
When the joint application of Apo-Triazid enhances neurotoxicity salicylates, reduces the effect of oral hypoglycemic funds, norepinephrine, epinephrine and arthrifuge, intensifies the effects (including spin), cardiac glycosides, cardiotoxic and neurotoxic effects of drugs lithium action curariform muscle relaxant, reduces excretion of quinidine.
When applied simultaneously with methyldopa increased risk of hemolysis.
At the same time.The kolestiramin reduces the absorption of Apo-Triazida. Hlorpropamid while reception with Apo-Triazidom can lead to marked hypokalemia. When combined with NSAIDs may develop acute renal failure.
Terms and Conditions of storage
List B. The drug should be stored in a dry, protected from light and away from children at a temperature of 15 ° to 25 ° C. Shelf life - 4 years.
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