Trospium Chloride 60mg Information
Trospium chloride 60mg (Trospium chloride) Description
Trospium chloride is a quaternary ammonium compound with the chemical name of Spiro[8azoniabicyclo[3,2,1]octane-8,1'-pyrrolidinium]-3-[(hydroxydiphenylacetyl)oxy]-,chloride(1α, 3β, 5α). The empirical formula of trospium chloride is CHClNO and its molecular weight is 427.97. The structural formula of trospium chloride is represented below:
Trospium chloride is a fine, colorless to slightly yellow, crystalline solid. The compound’s solubility in water is approximately 1 g/2 mL.
Each trospium chloride tablet contains 20 mg of trospium chloride and is to be given orally. Each tablet also contains the following inactive ingredients: microcrystalline cellulose, lactose monohydrate, corn starch, povidone, croscarmellose sodium, colloidal silicon dioxide, magnesium stearate, sucrose, copovidone, titanium dioxide, polyethylene glycol 6000, talc, hypromellose, macrogol, iron oxide yellow, iron oxide red.
Trospium chloride 60mg (Trospium chloride) Clinical Pharmacology
Trospium chloride is a muscarinic antagonist.
Trospium chloride antagonizes the effect of acetylcholine on muscarinic receptors in cholinergically innervated organs including the bladder. Its parasympatholytic action reduces the tonus of smooth muscle in the bladder. Receptor assays showed that trospium chloride has negligible affinity for nicotinic receptors as compared to muscarinic receptors at concentrations obtained from therapeutic doses.
Trospium chloride 60mg (Trospium chloride) Clinical Studies
Trospium chloride was evaluated for the treatment of patients with overactive bladder who had symptoms of urinary frequency, urgency, and urge incontinence in two U.S. 12-week, placebo-controlled studies and one 9-month open label extension.
Trospium chloride 60mg (Trospium chloride) Indications And Usage
Trospium chloride tablets, a muscarinic antagonist, are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency.
Trospium chloride 60mg (Trospium chloride) Contraindications
Trospium chloride is contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma and in patients who are at risk for these conditions.Trospium chloride is also contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients.
Trospium chloride 60mg (Trospium chloride) Warnings
Angioedema of the face, lips, tongue and/or larynx has been reported with trospium chloride. In one case, angioedema occurred after the first dose. Angioedema associated with upper airway swelling may be life threatening. If involvement of the tongue, hypopharynx, or larynx occurs, trospium chloride should be promptly discontinued and appropriate therapy and/or measures necessary to ensure a patent airway should be promptly provided.
Trospium chloride 60mg (Trospium chloride) Precautions
Risk of Urinary Retention:
Controlled Narrow-angle Glaucoma:
Patients should be informed that trospium chloride may produce angioedema which could result in life-threatening airway obstruction. Patients should be advised to promptly discontinue trospium chloride and seek immediate medical attention if they experience edema of the tongue, edema of the laryngopharynx, or difficulty breathing.
Patients should be informed that anticholinergic agents, such as trospium chloride, may produce clinically significant adverse effects related to anticholinergic pharmacological activity. For example, heat prostration (fever and heat stroke due to decreased sweating) can occur when anticholinergics such as trospium chloride are used in a hot environment. Because anticholinergics such as trospium chloride may also produce dizziness or blurred vision, patients should be advised to exercise caution. Patients should be informed that alcohol may enhance the drowsiness caused by anticholinergic agents.
Trospium chloride should be taken 1 hour prior to meals or on an empty stomach. If a dose is skipped, patients are advised to take their next dose 1 hour prior to their next meal.
Trospium chloride is metabolized by ester hydrolysis and excreted by the kidneys through a combination of tubular secretion and glomerular filtration. Based on data, no clinically relevant metabolic drug-drug interactions are expected with trospium. However, some drugs which are actively secreted by the kidney may interact with trospium by competing for renal tubular secretion. Co-administration of 500 mg metformin immediate release tablets twice daily with trospium chloride 60 mg extended release tablets reduced the steady-state systemic exposure of trospium by approximately 29% for mean AUCand by 34% for mean C.
The concomitant use of trospium chloride with other antimuscarinic agents that produce dry mouth, constipation, and other anticholinergic pharmacological effects may increase the frequency and/or severity of such effects. Trospium chloride may potentially alter the absorption of some concomitantly administered drugs due to anticholinergic effects on gastrointestinal motility.
Concomitant use of trospium chloride and digoxin did not affect the pharmacokinetics of either drug.
Drugs Eliminated by Active Tubular Secretion:
Coadministration of trospium chloride with these drugs may increase the serum concentration of trospium chloride and/or the coadministered drug due to competition for this elimination pathway. Careful patient monitoring is recommended in patients receiving such drugs (See ).
Carcinogenicity studies with trospium chloride were conducted in mice and rats for 78 weeks and 104 weeks, respectively, at maximally tolerated doses. No evidence of a carcinogenic effect was found in either mice or rats administered up to 200 mg/kg/day, approximately 9 times the expected clinical exposure levels at the maximum recommended human dose (MRHD) of 40 mg.
Trospium chloride was not mutagenic nor genotoxic in tests in vitro in bacteria (Ames test) and mammalian cells (L5178Y mouse lymphoma and CHO cells) or in vivo in the rat micronucleus test.
No evidence of impaired fertility was observed in rats administered doses up to 200 mg/kg/day (about 16 times the expected clinical exposure at the MRHD, based on AUC).
Trospium chloride (2 mg/kg PO and 50 μg/kg IV) was excreted, to a limited extent (
Trospium chloride should be used during lactation only if the potential benefit justifies the potential risk to the newborn.
Of the 591 patients with overactive bladder who received treatment with trospium chloride in the two U.S., placebo-controlled, efficacy and safety studies, 249 patients (42%) were 65 years of age and older.
Eighty-eight trospium chloride-treated patients (15%) were ≥75 years of age.
In these 2 studies, the incidence of commonly reported anticholinergic adverse events in patients treated with trospium chloride (including dry mouth, constipation, dyspepsia, UTI, and urinary retention) was higher in patients 75 years of age and older as compared to younger patients. This effect may be related to an enhanced sensitivity to anticholinergic agents in this patient population (See and ). Therefore, based upon tolerability, the dose frequency of trospium chloride may be reduced to 20 mg once daily in patients 75 years of age and older.
Trospium chloride 60mg (Trospium chloride) Adverse Reactions
The safety of trospium chloride was evaluated in Phase 2 and 3 controlled clinical trials in a total of 2975 patients, who were treated with trospium chloride (N=1673), placebo (N=1056) or active control medications (N=246). Of this total, 1181 patients participated in two, 12-week, Phase 3, U.S., efficacy and safety studies and a 9-month open-label extension. Of this total, 591 patients received trospium chloride 20 mg twice daily. In all controlled trials combined, 232 and 208 patients received treatment with trospium chloride for at least 24 and 52 weeks, respectively.
In all placebo-controlled trials combined, the incidence of serious adverse events was 2.9% among patients receiving trospium chloride 20 mg twice daily and 1.5% among patients receiving placebo. Of these, 0.2% and 0.3% were judged to be at least possibly related to treatment with trospium chloride or placebo, respectively, by the investigator.
Table 4 lists treatment emergent adverse events from the combined 12-week U.S. safety and efficacy trials that were judged to be at least possibly related to treatment with trospium chloride by the investigator, were reported by at least 1% of patients, and were reported more frequently in the trospium chloride group than in the placebo group.
The most common adverse events reported by patients receiving trospium chloride 20 mg twice daily were dry mouth and constipation.
The single most frequently reported adverse event for trospium chloride, dry mouth, occurred in 20.1% of trospium chloride treated patients and 5.8% of patients receiving placebo. In the two Phase 3 U.S. studies, dry mouth led to discontinuation in 1.9% of patients treated with trospium chloride 20 mg twice daily. For the patients who reported dry mouth, most had their first occurrence of the event within the first month of treatment.
Abbreviations: NOS = not otherwise specified.
Other adverse events from the Phase 3, U.S., placebo-controlled trials judged possibly related to treatment with trospium chloride by the investigator, occurring in ≥ 0.5% of trospium chloride-treated patients, and more common with trospium chloride than placebo are: tachycardia NOS, vision blurred, abdominal distension, vomiting NOS, dysgeusia, dry throat, and dry skin.
During controlled clinical studies, one event of angioneurotic edema was reported.
Trospium chloride 60mg (Trospium chloride) Dosage And Administration
The recommended dose is 20 mg twice daily.
Trospium chloride tablets should be dosed at least one hour before meals or given on an empty stomach.
Dosage modification is recommended in the following patient populations:
Trospium chloride 60mg (Trospium chloride) How Supplied
Trospium chloride tablets 20 mg (brownish yellow, round biconvex film-coated tablets, debossed with ‘L’ on one side and '1' on other side) are supplied as follows:
Bottles of 30 NDC 68462-461-30Bottles of 60 NDC 68462-461-60Bottles of 500 NDC 68462-461-05Bottles of 1000 NDC 68462-461-10
Trospium chloride 60mg (Trospium chloride)
Trospium chloride 60mg (Trospium chloride) Principal Display Panel
GlenmarkNDC 68462-461-10TROSPIUMCHLORIDETABLETS20 mgRx Only 1000 Tablets
