by pharmacodynamic synergism. Use Caution/Monitor. Additive anticholinergic effects, possible hypoglycemia.quinacrineMinor (1)quinacrine will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.quinidineMonitor Closely (1)quinidine will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.quinupristin/dalfopristinMonitor Closely (1)quinupristin/dalfopristin will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.ranolazineMinor (1)ranolazine will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.rapacuroniumMonitor Closely (1)rapacuronium and tolterodine both decrease cholinergic effects/transmission. Use Caution/Monitor.revefenacinSerious - Use Alternative (1)revefenacin and tolterodine both decrease cholinergic effects/transmission. Avoid or Use Alternate Drug. Coadministration may cause additive anticholinergic effects.ribociclibSerious - Use Alternative (1)ribociclib will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.rifabutinSerious - Use Alternative (1)rifabutin will decrease the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.rifampinSerious - Use Alternative (1)rifampin will decrease the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.rifapentineMonitor Closely (1)rifapentine will decrease the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.risperidoneMonitor Closely (3)tolterodine decreases levels of risperidone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. tolterodine decreases levels of risperidone by pharmacodynamic antagonism. Use Caution/Monitor. risperidone increases effects of tolterodine by pharmacodynamic synergism. Use Caution/Monitor. Additive anticholinergic effects, possible hypoglycemia.ritonavirMonitor Closely (1)ritonavir will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.Minor (1)ritonavir will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.rivastigmineMonitor Closely (1)tolterodine and rivastigmine both decrease cholinergic effects/transmission. Use Caution/Monitor.rocuroniumMonitor Closely (1)rocuronium and tolterodine both decrease cholinergic effects/transmission. Use Caution/Monitor.rolapitantMonitor Closely (1)rolapitant will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Rolapitant may increase plasma concentrations of CYP2D6 substrates for at least 28 days following rolapitant administration.rucaparibMonitor Closely (1)rucaparib will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.rufinamideMonitor Closely (1)rufinamide will decrease the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.saquinavirSerious - Use Alternative (1)saquinavir will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.scopolamineMonitor Closely (1)scopolamine and tolterodine both decrease cholinergic effects/transmission. Use Caution/Monitor.secobarbitalMonitor Closely (1)secobarbital will decrease the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.secretinSerious - Use Alternative (1)tolterodine decreases effects of secretin by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Concomitant use of anticholinergic drugs may cause a hyporesponse to stimulation testing with secretin. Discontinue anticholinergic drugs at least 5 half-lives before administering secretin.sertralineMinor (1)sertraline will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.solifenacinMonitor Closely (1)solifenacin and tolterodine both decrease cholinergic effects/transmission. Use Caution/Monitor.St John's WortSerious - Use Alternative (1)St John's Wort will decrease the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.stiripentolMonitor Closely (1)stiripentol, tolterodine. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.succinylcholineMonitor Closely (1)succinylcholine increases and tolterodine decreases cholinergic effects/transmission. Effect of interaction is not clear, use caution. Use Caution/Monitor.tazemetostatMonitor Closely (1)tazemetostat will decrease the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.tecovirimatMonitor Closely (1)tecovirimat will decrease the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.terbinafineMonitor Closely (1)terbinafine will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Assess need to reduce dose of CYP2D6-metabolized drug.thioridazineMonitor Closely (3)tolterodine decreases levels of thioridazine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. tolterodine decreases levels of thioridazine by pharmacodynamic antagonism. Use Caution/Monitor. thioridazine increases effects of tolterodine by pharmacodynamic synergism. Use Caution/Monitor. Additive anticholinergic effects, possible hypoglycemia.Minor (1)thioridazine will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.thiothixeneMonitor Closely (3)tolterodine decreases levels of thiothixene by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. tolterodine decreases levels of thiothixene by pharmacodynamic antagonism. Use Caution/Monitor. thiothixene increases effects of tolterodine by pharmacodynamic synergism. Use Caution/Monitor. Additive anticholinergic effects, possible hypoglycemia.tiotropiumMonitor Closely (1)tiotropium and tolterodine both decrease cholinergic effects/transmission. Use Caution/Monitor.tipranavirSerious - Use Alternative (1)tipranavir will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.Minor (1)tipranavir will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.topiramateMonitor Closely (1)topiramate will decrease the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.trazodoneMonitor Closely (1)tolterodine and trazodone both decrease cholinergic effects/transmission. Use Caution/Monitor.trifluoperazineMonitor Closely (3)tolterodine decreases levels of trifluoperazine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. tolterodine decreases levels of trifluoperazine by pharmacodynamic antagonism. Use Caution/Monitor. trifluoperazine increases effects of tolterodine by pharmacodynamic synergism. Use Caution/Monitor. Additive anticholinergic effects, possible hypoglycemia.trihexyphenidylMonitor Closely (1)tolterodine and trihexyphenidyl both decrease cholinergic effects/transmission. Use Caution/Monitor. Potential for additive anticholinergic effects.trimipramineMonitor Closely (1)tolterodine and trimipramine both decrease cholinergic effects/transmission. Use Caution/Monitor.trospium chlorideMonitor Closely (1)tolterodine and trospium chloride both decrease cholinergic effects/transmission. Use Caution/Monitor.tucatinibSerious - Use Alternative (1)tucatinib will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.vecuroniumMonitor Closely (1)tolterodine and vecuronium both decrease cholinergic effects/transmission. Use Caution/Monitor.venlafaxineMinor (1)venlafaxine will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Minor/Significance Unknown.verapamilMonitor Closely (1)verapamil will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.voriconazoleMonitor Closely (1)voriconazole will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.voxelotorSerious - Use Alternative (1)voxelotor will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.zafirlukastMonitor Closely (1)zafirlukast will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.ziprasidoneMonitor Closely (3)tolterodine decreases levels of ziprasidone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. tolterodine decreases levels of ziprasidone by pharmacodynamic antagonism. Use Caution/Monitor. ziprasidone increases effects of tolterodine by pharmacodynamic synergism. Use Caution/Monitor. Additive anticholinergic effects, possible hypoglycemia.zotepineMonitor Closely (2)tolterodine decreases levels of zotepine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. tolterodine decreases levels of zotepine by pharmacodynamic antagonism. Use Caution/Monitor. >10% Dry mouth (40%) 1-10% Blurred vision Constipation Dizziness Drowsiness Dyspepsia Headache Xerophthalmia Contraindications Urinary or gastric retention Uncontrolled narrow-angle glaucoma Hypersensitivity to drug or ingredients or to fesoterodine fumarate, which is metabolized to 5-hydroxymethyl tolterodine Cautions Controlled narrow-angle glaucoma, hepatic, or renal impairment Anaphylaxis and angioedema necessitating hospitalization and emergency treatment reported with first or subsequent doses; discontinue immediately if angioedema and hypotension, difficulty breathing, or airway obstruction develop Anticholinergic central nervous system effects (eg, dizziness, somnolence) reported; patients should not drive or operate heavy machinery until they adjust to therapy Use with caution in patients with myasthenia gravis, which is characterized by decreased cholinergic activity at neuromuscular junction When coadministered with strong CYP3A4 inhibitors, tolterodine should be given at reduced dosage QTc prolongation reported with high doses; use caution in patients with congenital prolonged QT or in patients receiving concurrent therapy with QTc-prolonging drugs (class Ia or III antiarrhythmics) Anticholinergics may potentially adversely affect the clinical course of alzheimer disease in patients receiving cholinesterase inhibitors; monitor for decreases in congnition, functional abilities and increased problematic behaviors in patients with dementia receiving dual therapy with an anticholinesterase inhibitor and a bladder anticholinercgic agent like tolterodine May increase risk of urinary retention in patients with bladder flow obstruction (eg, benign prostatic hypertrophy) May increase risk of gastric retention in patients with decreased GI motility or gastrointestinal obstructive disorders Pregnancy There are no available data with use in pregnant women to inform drug-associated risks; in animal reproduction studies, oral administration of tolterodine and its 5-HMT metabolite to pregnant mice during organogenesis did not produce adverse developmental outcomes at doses approximately 9 to 12 times the clinical exposure at a dose of 20 mg/kg/day; however, higher doses produced adverse developmental outcomes Lactation There is no information on presence in human milk, effects on breastfed infant, or on milk production; based on limited data, tolterodine is excreted into milk in mice in low amounts; the development and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from drug or from underlying maternal conditionPregnancy Categories A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk. B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available. Mechanism of Action Competitive muscarinic receptor antagonist; decreases bladder contractions; is more specific for bladder than oxybutynin Absorption Bioavailability: 77% Onset: Overactive bladder, 1 wk; urge incontinence, 1 hr Time to peak effect: 2-4 wk Peak plasma time: Immediate release, 1-2 hr; extended release, 2-6 hr Distribution Vd: 113 L Metabolism Metabolized in liver by CYP2D6 and (to minor extent) CYP3A4 Metabolites: 5-Hydroxymethyl, dealkylated tolterodine Elimination Half-life: Parent drug, 1.9-3.7 hr; active metabolite (5-hydroxymethyl), 3 hr (8.7 hr in cirrhosis) Total body clearance: 5.7 L/kg/hr Excretion: Urine (77%), feces (17%) BRAND FORM. UNIT PRICE PILL IMAGE Detrol oral- 2 mg tabletDetrol oral- 1 mg tablettolterodine oral- 2 mg capsuletolterodine oral- 2 mg capsuletolterodine oral- 4 mg capsuletolterodine oral- 1 mg tablettolterodine oral- 4 mg capsuletolterodine oral- 4 mg capsuletolterodine oral- 2 mg capsuletolterodine oral- 4 mg capsuletolterodine oral- 2 mg capsuletolterodine oral- 1 mg tablettolterodine oral- 4 mg capsuletolterodine oral- 2 mg capsuletolterodine oral- 4 mg capsuletolterodine oral- 2 mg tablettolterodine oral- 1 mg tablettolterodine oral- 2 mg capsuletolterodine oral- 2 mg tablettolterodine oral- 2 mg tablettolterodine oral- 1 mg tabletDetrol LA oral- 4 mg capsuleDetrol LA oral- 2 mg capsuleCopyright © 2010 First DataBank, Inc.Print Patient Educationtolterodine oral TOLTERODINE EXTENDED-RELEASE - ORAL (tol-TER-oh-deen) COMMON BRAND NAME(S): Detrol LA USES: This medication is used to treat an overactive bladder. By relaxing the muscles in the bladder, tolterodine improves your ability to control your urination. It helps to reduce leaking of urine, feelings of needing to urinate right away, and frequent trips to the bathroom. This medication belongs to the class of drugs known as antispasmodics. HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start using tolterodine and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually once a day. Swallow the medication whole with a full glass of liquid. Do not crush or chew the medication. Doing so can destroy the long action of the drug and may increase side effects.Use this medication regularly to get the most benefit from it. To help you remember, use it at the same time each day. The dosage is based on your medical condition (especially kidney and liver disease), response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products