Adult: For the symptomatic treatment of urinary frequency, urgency, and incontinence: As conventional tab: 15 mg bid, may increase to 15 mg tid, if necessary. As modified-release cap: Initially, 30 mg once daily, may increase to 45 mg once daily, if necessary. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Oral Neurogenic detrusor overactivity
Adult: For the treatment of cases from spinal cord injuries (e.g. transverse lesion paraplegia): As conventional tab: 15 mg tid. Max: 45 mg daily.
What are the brands available for Propiverine in Singapore?
Mictonorm
Special Patient Group
Patient taking potent flavin-containing monooxygenase inhibitor (e.g. thiamazole, methimazole) in combination with potent CYP3A4/5 inhibitor: As conventional tab: Initially, 15 mg once daily, carefully titrate to a higher dose thereafter.
Renal Impairment
CrCl (mL/min)
Dosage
<30
As conventional tab: Max dose: 30 mg daily.
Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Hepatic Impairment
Moderate to severe: Contraindicated.
Administration
May be taken with or without food.
Contraindications
Gastrointestinal obstructive disorder, intestinal atony, toxic megacolon, severe ulcerative colitis, tachyarrhythmias, uncontrolled angle-closure glaucoma, myasthenia gravis; significant degree of bladder outflow obstruction that may lead to urinary retention. Moderate to severe hepatic impairment.
Special Precautions
Patient with severe congestive heart failure (NYHA class IV), tachycardia, cardiac arrhythmias, hiatal hernia with reflux oesophagitis, autonomic neuropathy, prostatic hyperplasia, urinary stricture. Patient taking potent flavin-containing mono-oxygenase inhibitor (e.g. thiamazole) in combination with potent CYP3A4/5 inhibitor. Renal and mild hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Exacerbation of heart failure, tachycardia, cardiac arrhythmias, acute angle-closure glaucoma, symptoms of decreased gastrointestinal motility; urinary retention. Eye disorders: Accommodation disorder, visual impairment. Gastrointestinal disorders: Dry mouth, constipation, abdominal pain, dyspepsia, dysgeusia, nausea, vomiting. General disorders and administration site conditions: Fatigue.
Nervous system disorders: Headache, dizziness, tremor, speech disorder. Renal and urinary disorders: Urinary retention, bladder and urethral symptoms. Skin and subcutaneous tissue disorders: Pruritus. Vascular disorders: Flushing, decreased blood pressure with drowsiness.
Patient Counseling Information
This drug may cause drowsiness and blurred vision, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor LFTs (particularly during long-term therapy), renal function, IOP (patients at risk of developing glaucoma), QTc interval (patients at risk of QTc prolongation).
Overdosage
Symptoms: Nausea, dizziness, severe dry mouth, inhibition of intestinal motility, bradycardia (possibly leading to tachycardia), speech disorder, muscular weakness, restlessness, confusion, hallucination, confabulation, mydriasis and accommodation disorder, and urinary retention. Management: Symptomatic and supportive treatment. Give activated charcoal with plenty of water. May consider gastric lavage within 1 hour of ingestion. May administer physostigmine to treat severe central anticholinergic effects (e.g. hallucinations, pronounced excitation). May give benzodiazepines to treat convulsions or pronounced excitation. May administer pilocarpine eye drops and/or darken the patient’s room to treat mydriasis. Employ artificial respiration for respiratory insufficiency and catheterisation for urinary retention.
Drug Interactions
Enhanced effect with TCAs (e.g. imipramine), tranquillisers (e.g. benzodiazepines), systemic anticholinergics, amantadine, neuroleptics (e.g. phenothiazines), β-adrenoceptor agonists (e.g. β-sympathomimetics). Reduced efficacy with cholinergic agents. Decreased blood pressure with isoniazid. May decrease the effects of prokinetics (e.g. metoclopramide).
Food Interaction
Increased bioavailability with a high-fat meal (conventional tab).
Action
Description: Mechanism of Action: Propiverine is a tertiary antimuscarinic agent with similar effects to those of atropine. It prevents Ca influx and modulates intracellular Ca in urinary bladder smooth muscle cells causing musculotropic spasmolysis. Pharmacokinetics: Absorption: Almost completely absorbed from the gastrointestinal tract. Bioavailability: 53.3% (conventional tab); 59.5-60.8% ± 17.3-23.3% (modified-release cap). Time to peak plasma concentration: Approx 2 hours (conventional tab); approx 10 hours (modified-release cap). Distribution: Volume of distribution: 279 L (range: 125-473 L). Plasma protein binding: 90-95% (propiverine); 60% (propiverine-N-oxide). Metabolism: Extensively metabolised by intestinal enzymes and in the liver by CYP3A4 and flavin-monooxygenases 1 and 3 enzymes primarily via oxidation of piperidyl-N into propiverine-N-oxide metabolite; undergoes extensive first-pass metabolism. Excretion: Via urine (60%; <1% as unchanged drug); faeces (21%). Elimination half-life: Conventional tab: 11.4 hours (range: 7.4-17.7 hours). Modified-release cap: 14.2-16.3 hours (range: 10.8-19.2 hours).
Chemical Structure
Propiverine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4942, Propiverine. https://pubchem.ncbi.nlm.nih.gov/compound/Propiverine. Accessed Oct. 28, 2024.
Storage
Conventional tab/modified-release cap: Store below 30°C. Protect the modified-release cap from moisture.
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