Version May 2024
Overactive bladder: Oral: Modified release: Initial: 30 mg once daily; may increase to a maximum of 45 mg once daily.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Mild to moderate impairment: No dosage adjustment necessary; use with caution.
Severe impairment: Maximum dose: 30 mg/day.
Mild impairment: No dosage adjustments necessary.
Moderate to severe impairment: Use is contraindicated.
Overactive bladder: Children and Adolescents: Oral: Immediate release: 0.8 mg/kg/day in 2 divided doses or alternatively the following body weight adjusted dosing may be used:
12 to 16 kg: 5 mg two times daily.
17 to 22 kg: 5 mg in the morning and 10 mg in the evening.
23 to 28 kg: 10 mg two times daily.
29 to 34 kg: 10 mg in the morning and 15 mg in the evening.
≥35 kg: 15 mg two times daily (maximum: 30 mg/day).
Note: Modified-release capsules should not be used in pediatric patients.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not always defined.
Cardiovascular: Fatigue (≥0.1% to <5%), hypotension (0.1% to <5%), edema (>0.1%), hypertension (>0.1%), palpitation (> 0.1%), atrioventricular block, bradycardia, chest pain, extrasystoles, flushing, prolonged QT interval on ECG, tachycardia, ventricular tachycardia
Central nervous system: Dizziness (0.1% to <5%), fatigue (0.1% to <5%), headache (0.1% to <5%), drowsiness (<0.1%), excitability (>0.1%), insomnia (>0.1%), paralysis (>0.1%), confusion, delirium, hallucination, impaired consciousness, restlessness
Dermatologic: Pruritus (0.1% to <5%), skin rash (0.1% to <5%), urticaria (>0.1%), erythema, Stevens-Johnson syndrome
Endocrine & metabolic: Polydipsia (5%)
Gastrointestinal: Abdominal pain (0.1% to <5%), constipation (0.1% to <5%), dyspepsia (0.1% to <5%), diarrhea (0.1% to <5%), nausea (0.1% to <5%), vomiting (0.1% to <5%), xerostomia (≥1%), anorexia (>0.1%), cleft palate (>0.1%), dysgeusia (<0.1%), glossitis (>0.1%), stomatitis (>0.1%), abdominal distension, intestinal obstruction, sore throat
Genitourinary: Dysuria (0.1% to <5%), increased post-void residual urine (0.1% to <5%), urinary incontinence (>0.1%), urinary retention (<0.1%), anuria
Hematologic & oncologic: Leukopenia (0.1% to <5%), myoglobin increased, thrombocytopenia
Hepatic: Increased serum alkaline phosphatase (0.1% to <5%), increased serum transaminases (0.1% to <5%), hepatic insufficiency, jaundice
Hypersensitivity: Hypersensitivity
Neuromuscular & skeletal: Back pain (>0.1%), tremor (>0.1%), weakness (>0.1%), dyskinesia, increased creatine phosphokinase, myalgia, rhabdomyolysis
Ophthalmic: Oculomotor disturbance (0.1% to <5%), accommodation disturbances (<1%), visual disturbance (<1%), dry eye syndrome (0.1%), eye pain, glaucoma, increased intraocular pressure
Renal: Increased blood urea nitrogen (>0.1%), increased creatinine clearance (>0.1%), renal insufficiency
Respiratory: Increased bronchial secretions (>0.1%)
Miscellaneous: Fever (>0.1%)
Postmarketing, and/or case reports: Cough, dyschromia, leukocytosis, pain, reduced urine flow, tinnitus, upper respiratory tract infection
Hypersensitivity to propiverine or any component of the formulation; gastrointestinal obstructive disorder; angle-closure glaucoma (uncontrolled); intestinal atony; myasthenia gravis; tachyarrhythmias; toxic megacolon; severe ulcerative colitis; moderate or severe hepatic impairment; significant degree of bladder outflow obstruction where urinary retention may be anticipated; rare hereditary problems of galactose intolerance, glucose-galactose malabsorption, or congenital lactase deficiency; children with rare hereditary problems of fructose intolerance or sucrose-isomaltase insufficiency.
Concerns related to adverse effects:
• CNS effects: May cause drowsiness and blurred vision, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with heart failure, tachycardia, and/or cardiac arrhythmias; may exacerbate condition. Use is contraindicated in patients with tachyarrhythmias. Monitor patients at risk for QTc prolongation during therapy (have not been studied).
• Glaucoma: Use with caution in patients with glaucoma; may exacerbate condition. Use is contraindicated in patients with uncontrolled angle-closure glaucoma.
• Hepatic impairment: Use with caution in patients with mild hepatic impairment. Monitor hepatic function closely and discontinue if transaminases and/or bilirubin are above normal limits. Use is contraindicated in patients with moderate or severe hepatic impairment.
• Hiatal hernia: Use with caution in patients with hiatal hernia with reflux esophagitis.
• Neuropathy: Use with caution in patients with autonomic neuropathy; may aggravate symptoms of decreased GI motility
• Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture; may cause urinary retention
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment may be required in severe impairment.
Other warnings/precautions:
• Appropriate use: Prior to initiating therapy, rule out alternative causes of pollakiuria and nocturia (eg, organic bladder disease such as UTI or malignancy, heart failure).
Not available in the US
Yes
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule Extended Release 24 Hour, Oral:
Mictoryl: 30 mg, 45 mg
Tablet, Oral:
Mictoryl Pediatric: 5 mg
IR tablets: Administer at least 1 hour before meals particularly in patients with renal/mild hepatic impairment.
Modified-release capsules: May administer without respect to meals. Do not crush or chew.
Bariatric surgery: Capsule, modified release: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate. ER capsules should be swallowed whole. IR tablet formulation is available. If safety and efficacy can be effectively monitored, no change in formulation or administration is required after bariatric surgery.
Oral: Immediate-release tablets: Administer at least 1 hour before meals particularly in patients with renal/mild hepatic impairment.
Note: Not approved in US.
Overactive bladder: Treatment of symptoms (incontinence, frequency, urgency) due to overactive bladder
Beers Criteria: Based on pharmacologic class concerns for anticholinergics in the Beers Criteria, propiverine may be a potentially inappropriate medication to be avoided in patients ≥65 years due to its anticholinergic properties (Beers Criteria [AGS 2023]).
Substrate of CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP3A4 (weak)
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy
Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
ALPRAZolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of ALPRAZolam. Risk C: Monitor therapy
Amantadine: Propiverine may enhance the adverse/toxic effect of Amantadine. Risk C: Monitor therapy
Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy
Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy
CarBAMazepine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of CarBAMazepine. Risk C: Monitor therapy
Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy
Chlorprothixene: Anticholinergic Agents may enhance the anticholinergic effect of Chlorprothixene. Risk C: Monitor therapy
Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination
CloZAPine: Anticholinergic Agents may enhance the constipating effect of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider therapy modification
CycloSPORINE (Systemic): CYP3A4 Inhibitors (Weak) may increase the serum concentration of CycloSPORINE (Systemic). Risk C: Monitor therapy
Dofetilide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide. Risk C: Monitor therapy
Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination
Finerenone: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Finerenone. Risk C: Monitor therapy
Flibanserin: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin. Risk C: Monitor therapy
Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy
Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy
Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination
Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy
Ixabepilone: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Ixabepilone. Risk C: Monitor therapy
Lemborexant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lemborexant. Management: The maximum recommended dosage of lemborexant is 5 mg, no more than once per night, when coadministered with weak CYP3A4 inhibitors. Risk D: Consider therapy modification
Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination
Lomitapide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lomitapide. Management: Patients on lomitapide 5 mg/day may continue that dose. Patients taking lomitapide 10 mg/day or more should decrease the lomitapide dose by half. The lomitapide dose may then be titrated up to a max adult dose of 30 mg/day. Risk D: Consider therapy modification
Lonafarnib: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lonafarnib. Management: Avoid concurrent use of lonafarnib with weak CYP3A4 inhibitors. If concurrent use is unavoidable, reduce the lonafarnib dose to or continue at a dose of 115 mg/square meter. Monitor for evidence of arrhythmia, syncope, palpitations, or similar effects. Risk D: Consider therapy modification
Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Midazolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Midazolam. Risk C: Monitor therapy
Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy
NiMODipine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine. Risk C: Monitor therapy
Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy
Opioid Agonists: Anticholinergic Agents may enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. Risk C: Monitor therapy
Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Pimozide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide. Risk X: Avoid combination
Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid combination
Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium citrate. Risk X: Avoid combination
Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid combination
Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy
Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination
Rivastigmine: Anticholinergic Agents may diminish the therapeutic effect of Rivastigmine. Rivastigmine may diminish the therapeutic effect of Anticholinergic Agents. Management: Use of rivastigmine with an anticholinergic agent is not recommended unless clinically necessary. If the combination is necessary, monitor for reduced anticholinergic effects. Risk D: Consider therapy modification
Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider therapy modification
Simvastatin: CYP3A4 Inhibitors (Weak) may increase serum concentrations of the active metabolite(s) of Simvastatin. CYP3A4 Inhibitors (Weak) may increase the serum concentration of Simvastatin. Risk C: Monitor therapy
Sirolimus (Conventional): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Sirolimus (Conventional). Risk C: Monitor therapy
Sirolimus (Protein Bound): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Sirolimus (Protein Bound). Management: Reduce the dose of protein bound sirolimus to 56 mg/m2 when used concomitantly with a weak CYP3A4 inhibitor. Risk D: Consider therapy modification
Tacrolimus (Systemic): CYP3A4 Inhibitors (Weak) may increase the serum concentration of Tacrolimus (Systemic). Risk C: Monitor therapy
Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy
Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination
Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy
Triazolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Triazolam. Risk C: Monitor therapy
Ubrogepant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Ubrogepant. Management: In patients taking weak CYP3A4 inhibitors, the initial and second dose (given at least 2 hours later if needed) of ubrogepant should be limited to 50 mg. Risk D: Consider therapy modification
Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Adverse events have been reported in animal reproduction studies. Use is not recommended in pregnancy.
It is not known if propiverine is present in breast milk. Breastfeeding is not recommended by the manufacturer.
Hepatic function during long-term therapy; renal function; intraocular pressure in patients at risk of developing glaucoma; QTc interval (patients at risk for QTc prolongation)
Propiverine and three active metabolites account for pharmacologic effects; antispasmodic effect by inhibiting calcium influx and modulating intracellular calcium in bladder smooth muscle; also has anticholinergic activity leading to decreased intravesical pressure.
Absorption: Nearly complete.
Distribution: Mean: 279 L (range: 125 L to 473 L).
Protein binding: Propiverine: 90% to 95%; propiverine-N-oxide (main metabolite): 60%.
Metabolism: Extensive via hepatic and intestinal enzymes, primarily by oxidation of piperidyl-N and mediated by CYP3A4 and flavin-monooxygenases (FMO) 1 and 3; main metabolite propiverine-N-oxide.
Bioavailability: Large first-pass effect; Immediate release: 53.3% (increased with high-fat meal); Modified release: 59.5% to 60.8% ± 17.3% to 23.3%.
Half-life elimination: Immediate release: 11.4 hours (range: 7.4 to 17.7 hours); Modified release: 14.2 to 16.3 hours (range: 10.8 to 19.2 hours).
Time to peak, serum: Immediate release: ~2 hours; Modified release: ~10 hours.
Excretion: Urine (60%, <1% unchanged); Feces (21%).
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