Triamterene

Triamterene is a potassium-sparing diuretic. Triamterene lowers the permeability of distal tubular cell membranes for sodium ions and enhances their excretion in the urine. Triamterene does not increase the release of potassium ions. In the distal tubules, the secretion of potassium decreases. Triamterene reinforces the diuretic effect of thiazide diuretics and reduces hypokalemia, which is caused by thiazide diuretics. The diuretic effect of Triamterene upon ingestion is noted after 15 to 20 minutes, the maximum effect develops in 2 to 3 hours. The duration of the Triamterene is 12 hours.

 


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Description

Pharmacological properties.

Triamterene is a potassium-sparing diuretic. Triamterene lowers the permeability of distal tubular cell membranes for sodium ions and enhances their excretion in the urine. Triamterene does not increase the release of potassium ions. In the distal tubules, the secretion of potassium decreases. Triamterene reinforces the diuretic effect of thiazide diuretics and reduces hypokalemia, which is caused by thiazide diuretics. The diuretic effect of Triamterene upon ingestion is noted after 15 to 20 minutes, the maximum effect develops in 2 to 3 hours. The duration of the Triamterene is 12 hours.

In case of oral administration, Triamterene is absorbed very quickly in the gastrointestinal tract. The degree of absorption of Triamterene is variable (30-70% of the dose taken). The bioavailability of Triamterene is approximately 50%. It binds with plasma proteins on about 60%. The maximum concentration of Triamterene in blood plasma is reached after 2 to 4 hours. Triamterene is excreted in breast milk and penetrates the placental barrier. Triamterene is extensively metabolized with formation of active and inactive metabolites and excreted primarily in the urine primarily as metabolites, in an unmodified form is displayed in a small amount. The half-life of Triamterene is approximately 2 hours (with anuria – 10 hours), metabolites – up to 12 hours. The main way to excrete Triamterene is the intestine, the secondary way is the kidneys.
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Indication.

Arterial hypertension; edematous syndrome of various origin (including nephrotic syndrome, chronic heart failure, cirrhosis); prevention of hypoglycemia when using saluretics.

Method of application of Triamterene and dose.

Triamterene is taken internally, the dosage is set individually.
When using Triamterene in patients with cirrhosis of the hepatic, an increase in the risk of developing megaloblastic anemia is possible.

It is not recommended to use Triamterene in case of hyperkalemia, together with other potassium-sparing diuretics (including amiloride, spironolactone, combined preparations which contain Triamterene), salt substitutes that contain potassium.

Triamterene is used with caution in patients with gout, indications in the anamnesis of urolithiasis.
If you missed the next Triamterene, then you can’t take two doses of the drug at a time.
In the treatment periodic monitoring of blood levels of potassium, sodium, chlorine, urea, creatinine, glucose, uric acid, a picture of peripheral blood is necessary.

During treatment with Triamterene, potentially dangerous activities that require increased concentration and speed of psychomotor reactions (including the management of vehicles and mechanisms) should be avoided.

Contraindications.

Hypersensitivity, lactation, pregnancy, age 18 years (efficacy and safety have not been established), hepatic and / or kidney failure, anuria, acute glomerulonephritis, hyperkalemia, precoma and hepatic coma, joint use with other potassium-sparing diuretics (including spironolactone, amiloride, combined preparations that contain Triamterene), salt substitutes that contain potassium.
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Side effects of Triamterene.

Digestive system: dry mouth, dyspeptic symptoms, nausea, vomiting, diarrhea, abdominal pain and discomfort in the epigastric region, constipation, colicky abdominal pain, hemorrhagic pancreatitis, acute cholecystitis.

Nervous system and sensory organs: drowsiness, uncoordinated movements, headache, fatigue, nervousness, confusion, visual impairment, a decrease in the production of tear fluid, worsening of the already available myopia, icteric coloring of the sclera.

Musculoskeletal system: muscle weakness, muscle tension, cramps calf muscles.

Cardiovascular system and blood (hemostasis, blood formation): hypotension, heart rate, cardiovascular collapse, cardiac arrhythmias, syncope, blood clots, embolism, aplastic anemia, thrombocytopenia, leukopenia, agranulocytosis, megaloblastic anemia.

Interaction of Triamterene with other substances.

With the joint use of Triamterene with angiotensin-converting enzyme inhibitors, hyperkalemia (especially in patients with impaired renal function) is possible, because angiotensin-converting enzyme inhibitors reduce aldosterone levels, which leads to potassium retention in the body against potassium excretion.

The combined use of Triamterene with antihypertensive drugs, the antihypertensive effect of Triamterene is enhanced.

When Triamterene is used together with diclofenac, a case of impaired renal functional status is described.

The combined use of Triamterene with other potassium-sparing diuretics, potassium supplements, salt substitutes and biologically active additives to food, which contain potassium, may develop hyperkalemia.

When it is used together with Triamterene losartan, candesartan, eprosartan, enalapril, enalaprilat, cilazapril the risk of hyperkalemia increases; sharing is not recommended.
In the joint use of Triamterene with indomethacin, acute renal failure may develop.
In case of the joint use of Triamterene with ranitidine, it is possible to reduce the absorption and diuretic effect of Triamterene

Sharing Triamterene and lisinopril requires special care to avoid the development of hyperkalemia, especially with reduced renal function.

The combined use of Triamterene and losartan can increase the concentration of potassium in the blood plasma.

We do not recommend sharing Triamterene with ramipril, perindopril, indapamide, fosinopril, because the development of hyperkalemia is possible, especially in patients with renal insufficiency, diabetes mellitus, when used together, you should regularly monitor the concentration of potassium in the blood plasma, the parameters of the electrocardiogram, and adjust therapy if necessary.

Overdose

In case of overdose Triamterene develop a pronounced reduction in blood pressure, nausea, vomiting, diarrhea, dizziness, drowsiness, confusion, muscle cramps, skin rash, dehydration, disruption of water and electrolyte balance (including hyperkalemia).
Treatment: removal of preparation, gastric lavage, activated charcoal, symptomatic treatment of arterial hypotension, disorders of water and electrolyte balance, dehydration, maintenance of vital functions. There is no specific antidote.

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