tolterodine (Detrol, Detrol LA)
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Introduction
Tradename: Detrol.
Indications
- treatment of urinary frequency & urinary urgency due to urge incontinence & overactive bladder
Contraindications
Dosage
Tabs: 1,2 mg; 2,4 mg (Detrol LA)
Pharmacokinetics
- oral absorption increased by food
- bioavailability 77%
- peak concentration 1-2 hours after oral dose
- metabolized in liver by cyt P450 2D6 & cyt P450 3A4 to active 5-hydroxymethyl derivative
- highly bound to plasma proteins (alpha-1 acid glycoprotein)
elimination via liver
protein binding = 96 %
Adverse effects
- anticholinergic effects:
- GI: dry mouth, dyspepsia
- respiratory: bronchitis, cough
- psychiatric: somnolence
- cardiovascular: hypertension, chest pain
- infection (especially fungal)
- increase in urine residual volume
- central nervous system
- give activated charcoal
- electrocardiogram (ECG) monitor
Drug interactions
- fluoxetine inhibits tolterodine metabolism
- cyt P450 2D6 & cyt P450 3A4 inhibitors (no data, use caution)
- macrolides, antifungal agents
- maximum dose of tolterodine: 1 mg BID if administered concurrently[5]
Mechanism of action
- muscarinic receptor antagonist
- presumptive muscle relaxant
- newer agent allegedly better tolerated than oxybutynin (Ditropan)
- allegedly some bladder selectivity[3]
- primarily antagonizes muscarinic M2 receptors & muscarininc M3 receptors[6]
- bladder selectivity vs salivary gland in animal model[5]
More general terms
Additional terms
- cytochrome P450 2D6 (cytochrome P450 2D, cytochrome P450 DB1, debrisoquine-4-hydroxylase, CYP2D6)
- cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
References
- ↑ Physician's Desk Reference (PDR), volume 102, 1999, Medical Economics, 1999
- ↑ Pharmacia & Upjohn
- ↑ 3.0 3.1 Eslami M. In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 12-15, 2001
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 5.0 5.1 5.2 Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
- ↑ 6.0 6.1 Prescriber's Letter 12(2): 2005 Antimuscarinic Medications for Overactive Bladder Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=210209&pb=PRL (subscription needed) http://www.prescribersletter.com