Urispas
Urispas
Generic Name
Urispas
Mechanism
- Competitive antagonist of muscarinic M3 receptors in the detrusor smooth muscle.
- Inhibits acetylcholine‑mediated detrusor contraction, reducing involuntary bladder activity.
- Limited systemic absorption results in minimal anticholinergic side‑effects compared with oral agents.
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Pharmacokinetics
| Parameter | Data | Comments |
| Absorption | Rapid local absorption from the urethral mucosa; peak plasma levels < 50 ng/mL. | Limited systemic exposure. |
| Distribution | Primarily confined to the bladder wall; negligible crossing of the blood‑brain barrier. | Reduces CNS side effects. |
| Metabolism | Minimal hepatic metabolism; primarily excreted unchanged. | CYP450 involvement negligible. |
| Elimination | Renal excretion (≈70 %) and urinary excretion (≈20 %). | Dose adjusted in severe renal impairment. |
| Half‑life | Local effect lasts 6–8 h; systemic half‑life < 2 h. | Supports once‑daily dosing. |
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Indications
- Overactive bladder (OAB) – urge incontinence and urinary frequency.
- Idiopathic urge‑to‑urinate – patients with bladder hypersensitivity not responsive to behavioral therapy.
- Adjunctive therapy – when oral antimuscarinics are poorly tolerated.
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Contraindications
- Absolute Contraindications
- Severe bladder outlet obstruction (e.g., benign prostatic hyperplasia).
- Acute urinary retention.
- Known hypersensitivity to any component of the formulation.
- Warnings
- Ocular disease – potential to exacerbate narrow‑angle glaucoma.
- Cognitive impairment – careful use in elderly patients due to risk of confusion, though minimal systemic absorption mitigates risk.
- Pregnancy & Lactation – classification C; use only if benefits outweigh risks.
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Dosing
- Initial Dose: 2 mg (1 × ½ tablet) applied intravaginally at bedtime.
- Maintenance Dose: 2 mg once daily, preferably at bedtime.
- Maximum: 4 mg/day (two tablets).
- Administration Tips
- Keep the applicator away from the urethral opening.
- Avoid coughing or straining during insertion to reduce retrograde migration.
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Monitoring
| Parameter | Frequency | Rationale |
| Urinary frequency & urgency | Baseline, 1 month, 3 months | Assess therapeutic response. |
| Renal function | Baseline & 6‑month review | Adjust dose if eGFR < 30 mL/min. |
| Blood pressure | Baseline & 2‑month review | Antimuscarinics can lower BP. |
| Ophthalmologic exam | Baseline & 6‑month if symptoms | Monitor potential angle‑closure. |
| Adverse event reporting | Continuous | Detect rare systemic effects. |
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Clinical Pearls
- Start Low, Go Slow – Begin with 2 mg nightly; increase only if symptoms persist after 4 weeks.
- Topical Advantage – Urispas offers effective local action with fewer dry‑mouth and constipation side‑effects common to oral antimuscarinics.
- Patient Selection – Ideal for patients who are elderly, have difficulty swallowing pills, or experienced intolerable anticholinergic side‑effects from oral therapy.
- Use with Behavioral Therapy – Combine with bladder training and pelvic floor exercises for maximal benefit.
- Storage – Keep at ≤ 20 °C; protection from frost and direct sunlight.
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• Note: This drug card is intended for educational purposes. Always refer to the most recent prescribing information and clinical guidelines before initiating therapy.