Comparative Pharmacology
Head-to-head clinical analysis: HICON versus TOLTERODINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: HICON versus TOLTERODINE.
HICON vs TOLTERODINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Unknown; possibly involves modulation of hypothalamic thermoregulatory center.
Competitive antagonist of muscarinic acetylcholine receptors (M1, M2, M3, M4, M5), with selectivity for the M3 receptor subtype involved in detrusor muscle contraction, reducing bladder smooth muscle contractility and increasing bladder capacity.
HICON (norepinephrine) 0.05-0.5 mcg/kg/min IV continuous infusion, titrated to blood pressure.
2 mg PO twice daily; may reduce to 1 mg twice daily if tolerated.
None Documented
None Documented
Terminal half-life: 12-18 hours; prolonged to 24-36 hours in renal impairment (CrCl <30 mL/min)
Clinical Note
moderateTolterodine + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Tolterodine."
Clinical Note
moderateTolterodine + Cyclosporine
"The metabolism of Cyclosporine can be decreased when combined with Tolterodine."
Clinical Note
moderateTolterodine + Fluconazole
"The metabolism of Fluconazole can be decreased when combined with Tolterodine."
Clinical Note
moderateTolterodine + Clotrimazole
Terminal elimination half-life is 2-4 hours in extensive CYP2D6 metabolizers; increased to 4-10 hours in poor metabolizers or with CYP3A4 inhibitors.
Renal: 70% as unchanged drug; biliary/fecal: 25% as metabolites; 5% other
Primarily hepatic metabolism via CYP2D6 and CYP3A4; renal excretion accounts for <5% of unchanged drug; ~80% excreted in urine as metabolites, ~20% in feces.
Category C
Category A/B
Anticholinergic
Anticholinergic
"The metabolism of Clotrimazole can be decreased when combined with Tolterodine."