Drug intelligence / Profile preview

tolterodine + tamsulosin

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

The combination of tolterodine and tamsulosin is primarily used to treat lower urinary tract symptoms (LUTS) in men, particularly those with overactive bladder (OAB) and benign prostatic hyperplasia (BPH). This combination therapy has shown significant benefits compared to either medication used alone. ## Mechanism and Efficacy Tolterodine is an antimuscarinic agent that helps control overactive bladder symptoms, while tamsulosin is an alpha1-receptor antagonist that helps relieve symptoms related to benign prostatic hyperplasia. When used together, they address both the storage and voiding symptoms that many men experience[1][2]. Clinical studies have demonstrated that the combination therapy provides superior results compared to monotherapy. In a major randomized, double-blind, placebo-controlled study, 80% of patients receiving tolterodine ER plus tamsulosin reported treatment benefit after 12 weeks, compared to only 62% of those on placebo[2][5][6]. Neither drug alone showed significant improvement over placebo, with tamsulosin monotherapy achieving 71% benefit and tolterodine monotherapy achieving 65% benefit[2][6]. The combination therapy significantly reduced: - Urgency episodes with and without incontinence - Frequency of urination (micturitions per 24 hours) - Nighttime urination (nocturia) - International Prostate Symptom Score (IPSS)[6] ## Dosage and Administration The typical dosage is: - Tolterodine ER: 4 mg once daily - Tamsulosin: 0.4 mg once daily[6][7] The medication should be taken 30 minutes after the same meal each day[7]. ## Side Effects Common side effects include: - Dry mouth - Constipation - Indigestion - Headache - Dizziness[7] ## Contraindications This combination is contraindicated in: - Patients with hypersensitivity to either drug - Severe renal or hepatic impairment - History of urinary or gastric retention - Uncontrolled narrow-angle glaucoma[7] ## Drug Interactions Tolterodine + tamsulosin may interact with: - Antibiotics (erythromycin, clarithromycin) - Antifungals (ketoconazole, itraconazole) - HIV medications - Medications for irregular heartbeat (amiodarone, sotalol, quinidine, procainamide) - Blood pressure medications (atenolol, metoprolol, prazosin, terazosin) - Pain relievers (diclofenac, ibuprofen, indomethacin) - Other alpha-1 adrenergic receptor antagonists[4][7] Patients should avoid grapefruit juice and alcohol while taking this medication[4]. ## Special Populations This medication is specifically designed for men with lower urinary tract symptoms and is not indicated for use in women, children, or adolescents[4][7]. The combination has also been studied in female patients with suspected functional bladder outlet obstruction, showing improvements in both subjective symptoms and objective urodynamic parameters[3].

02

Targets

ADRA1A (α1A)CHRM2 (M2)CHRM3 (M3)

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