Information about Torespot
Composition:
Each tablet contains: 10 mg or 20 mg of torsemide.
Pharmacological Properties:
Clinical pharmacology studies have confirmed that torsemide acts from within the lumen of the thick ascending portion of the loop of Henle, where it inhibits the Na+/K+/2CI--carrier system. Diuretic activity thus correlates better with the rate of drug excretion in the urine than with the concentration in the blood.
Torsemide increases the urinary excretion of sodium, chloride, and water, but it does not significantly alter glomerular filtration rate, renal plasma flow, or acid-base balance.
Pharmacokinetics: The bioavailability of Torespot tablets is approximately 80%. The drug is absorbed with little first-pass metabolism, and the serum concentration reaches its peak (Cmax) within 1 hour after oral administration. Cmax and AUC after oral administration are proportional to dose over the range of 2.5 mg to 200 mg. Absorption is essentially unaffected by renal or hepatic dysfunction. The volume of distribution of torsemide is 12 liters to 15 liters in normal adults or in patients with mild to moderate renal failure or congestive heart failure. In normal subjects the elimination half-life of torsemide is approximately 3.5 hours. Torsemide is cleared from the circulation by both hepatic metabolism (approximately 80%) and excretion into the urine (approximately 20%). Torsemide is extensively bound to plasma protein (>99%).
With oral dosing, the onset of diuresis occurs within 1 hour and the peak effect occurs during the first or second hour and diuresis lasts about 6 to 8 hours.
Indications:
Torespot is indicated for the treatment of:
Edema associated with congestive heart failure, renal disease, or hepatic disease.
Edema associated with chronic renal failure. (It is effective).
Hypertension alone or in combination with other antihypertensive agents. (Chronic use of any diuretic in hepatic disease has not been studied in adequate and well-controlled trials).
Contraindications:
Hypersensitivity to Torespot or to sulfonylureas.
In patients who are anuric.
Warnings and Precautions:
Torespot should be used with caution in patients with hepatic disease with cirrhosis and ascites. (To prevent hypokalemia and metabolic alkalosis, an aldosterone antagonist or potassium-sparing drug should be used concomitantly with it).
Tinnitus and hearing loss (usually reversible) have been observed after oral Torespot. Ototoxicity has also been seen in animal studies with high plasma levels.
In patients who develop fluid and electrolyte imbalances, hypovolemia, or prerenal azotemia, Torespot should be discontinued until the situation is corrected; Torespot may be restarted at a lower dose.
Periodic monitoring of serum potassium and other electrolytes is advised in patients treated with Torespot.
No significant trends have been observed in any laboratory values.
Drug Interactions:
When the following drugs: beta-blockers, ACE inhibitors, and calcium-channel blockers have been administered together with Torespot, none of these combined uses was associated with new or unexpected adverse events. Also when administered together with digitalis glycosides, ACE inhibitors, and organic nitrates,had no interactions with any of them. Coadministrations with spironolactone, Torespot reduced its renal clearance and increases in the AUC.
Coadministration with salicylates and NSAIDs may be associated with renal dysfunction.
Indomethacin partially inhibits the natriuretic effect of Torespot.
Cimetidine does alter the pharmacokinetic profile and diuretic activity of Torespot.
Digoxin increases the AUC for Torespot by 50%, but no need for dose adjustment.
Probenecid reduces secretion of Torespot and thereby decreases its diuretic activity.
Carcinogenesis, Mutagenesis and Impairment of Fertility
No overall increase in tumor incidence, and no mutagenic activity was detected in any of a variety of in vivo and in vitro tests of torsemide and its major human metabolite.
In doses up to 25 mg/kg/day, torsemide had no adverse effect on the reproductive performance of male or female rats.
Pregnancy and Lactation:
Pregnancy Category B. This drug should be used during pregnancy only if clearly needed.
Caution should be exercised when Torespot is administered to a nursing woman. (It is not known whether Torespot is excreted in human milk).
Pediatric Use:
Safety and effectiveness in pediatric patients have not been established.
Geriatric Use
No specific age-related differences in effectiveness or safety were observed between younger patients and elderly patients.
Side Effects:
The reported side effects of Torespot were generally transient, and there is no relationship between side effects and age, sex, race, or duration of therapy.
The most common reasons for discontinuation of therapy with Torespot were: dizziness, headache, nausea, weakness, vomiting, hyperglycemia, excessive urination, hyperuricemia, hypokalemia, excessive thirst, hypovolemia, impotence, esophageal hemorrhage, and dyspepsia.
Only “excessive urination” was generally occurring significantly more frequently in patients treated with Torespot than in patients treated with placebo.
Serious adverse events were atrial fibrillation, chest pain, diarrhea, digitalis intoxication, gastrointestinal hemorrhage, hyperglycemia, hyperuricemia, hypokalemia, hypotension, hypovolemia, shunt thrombosis, rash, rectal bleeding, syncope, and ventricular tachycardia.
Dosage and Administration:
Torespot tablets may be given at any time in relation to a meal, as convenient. Special dosage adjustment in the elderly is not necessary.
The usual initial oral dose in Congestive Heart Failure is 10 mg or 20 mg once-daily. The dose may be doubled until the desired diuretic response is obtained. Single doses higher than 200 mg have not been adequately studied.
For patients with Chronic Renal Failure, the usual initial dose of Torespot is 20 mg of once-daily oral Torespot. The dose may be increased until the desired diuretic response is obtained. Single doses higher than 200 mg have not been adequately studied.
For patients with Hepatic Cirrhosis, the usual initial dose is 5 mg or 10 mg of once-daily oral Torespot, administered together with an aldosterone antagonist or a potassium-sparing diuretic. The dose may be increased until the desired diuretic response is obtained. Single doses higher than 40 mg have not been adequately studied.
For patients with Hypertension, the usual initial dose is 5 mg once daily. The dose may be increased to 10 mg once daily if the 5 mg dose does not provide adequate reduction in blood pressure within 4 to 6 weeks.
Overdosage:
There is no human experience with overdoses of Torespot, but the signs and symptoms of overdosage can be anticipated to be those of excessive pharmacologic effect: dehydration, hypovolemia, hypotension, hyponatremia, hypokalemia, hypochloremic alkalosis, and hemoconcentration. Treatment of overdosage should consist of fluid and electrolyte replacement.
No data are available to suggest to change the pH of the urine that might accelerate elimination of torsemide and its metabolites. Torsemide is not dialyzable, so hemodialysis will not accelerate elimination.
Storage:
Store the product at 15˚ to 30˚C.
Rx only.
Packing:
Package of 30 Tablets for all strength.