Tolterodine (Detrol and Detrolla). (Medication Update).MODE OF ACTION Competitive muscarinic muscarinic /mus·ca·rin·ic/ (mus?kah-rin´ik) denoting the cholinergic effects of muscarine on postganglionic parasympathetic neural impulses. receptor antagonist. EFFECTS ON OVERACTIVE BLADDER Antagonism of cholinergic cholinergic /cho·lin·er·gic/ (ko?lin-er´jik) 1. parasympathomimetic; stimulated, activated, or transmitted by choline (acetylcholine); said of the sympathetic and parasympathetic nerve fibers that liberate acetylcholine at a muscarinic receptors in the overactive bladder reduces urinary frequency and urgency. CONTRAINDICATIONS Known hypersensitivity to tolterodine or other formulation components. Urinary or gastric retention. Uncontrolled narrow-angle glaucoma. Pregnancy Category C Pregnancy category C No adequate human or animal studies; or adverse fetal effects in animal studies, but no available human data. Mentioned in: Antianxiety Drugs . ADVERSE EFFECTS Abdominal pain (4-5%), constipation (67%), diarrhea (4%), dyspepsia dyspepsia: see indigestion. (3-4%), dry eyes (3%), dry mouth (23-34.8%), fatigue (24%), headache (6-7%), and vertigo (2-5%). DRUG-DRUG INTERACTIONS Azole antifungals, cyclosporine, macrolide antibiotics, and vinblastine vinblastine /vin·blas·tine/ (vin-blas´ten) an antineoplasticvinca alkaloid used as the sulfate salt in the palliative treatment of a variety of malignancies. may increase tolterodine levels. DRUG-FOOD INTERACTIONS Food increases the bioavailability bioavailability /bio·avail·a·bil·i·ty/ (bi?o-ah-val?ah-bil´i-te) the degree to which a drug or other substance becomes available to the target tissue after administration. bi·o·a·vail·a·bil·i·ty n. of tolterodine, but this may not be clinically significant. RECOMMENDED DOSE Immediate-release: 2 mg BID initially, but may be reduced to 1 mg BID. Extended-release: 4 mg QD initially, but may be reduced to 2 mg QD. DOSAGE FORMS AVAILABLE Immediate-release: 1 mg and 2 mg tablets. Extended-release: 2 mg and 4 mg capsules. MANUFACTURER Pharmacia. OTHER POINTS OF INTEREST Patients who have impaired renal or hepatic function or who are taking cytochrome P450 3A4 inhibitors (see Drug-Drug Interactions above) should be started on a lower dose. References (1.) Hutchison TA, Shahan DR (eds): DRUGDEX System. MIcROMEDEX, Inc, Greenwood Village, Col (Edition expires 3/2002) (2.) Hebel SK, Katstrup EK (eds): Drug Facts and Comparisons. St. Louis, Mo, 2001 |
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