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Tolterodine


Tolterodine
Systematic (IUPAC) name
2-[3-[bis(1-methylethyl)amino]- 1-phenyl-propyl]-4-methyl-phenol
Identifiers
CAS number	124937-51-5
ATC code	G04BD07
PubChem	60774
DrugBank	APRD00146
Chemical data
Formula	C₂₂H₃₁N O
Mol. mass	325.488 g/mol
Pharmacokinetic data
Bioavailability	77%
Protein binding	Approximately 96.3%.
Metabolism	?
Half life	1.9-3.7 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Tolterodine is an antimuscarinic drug that is used to treat urinary incontinence. It is sold under the trade name Detrol.

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Pharmacology

Tolterodine acts on M2 and M3 subtypes of muscarinic receptors whereas most antimuscarinic treatments for overactive bladder only act on M3 receptors making them more selective.

Tolterodine, although it acts on two types of receptors, has fewer side effects than other antimuscarinics eg. oxybutynin (which is selective for M3 only) as tolterodine targets the bladder more than other areas of the body. This means that less drug needs to be given daily (due to efficient targeting of the bladder) and so there are fewer side effects.

Side effects

Known Side Effects:

Hyposalivation (Dry mouth)
Decreased gastric motility (Upset stomach)
Headache
Constipation
Dry eyes
Sleepiness

Reports of Patients’ Experiences Since Detrol Became Available:

The following reactions have been reported in patients who have taken Detrol since it has become available:

Allergic reactions including swelling
Rapid heartbeat or abnormal heartbeat
Accumulation of fluid in the arms and legs
Hallucinations

Contraindications Not to be used in patients with Myasthenia Gravis and Angle Closure Glaucoma

v • d • e Urologicals (G04)
Acidifiers	Ammonium chloride, Calcium chloride
Urinary antispasmodics (primarily antimuscarinics)	Darifenacin, Emepronium, Flavoxate, Meladrazine, Oxybutynin, Propiverine, Solifenacin, Terodiline, Tolterodine, Trospium
For erectile dysfunction	Alprostadil, Apomorphine, Moxisylyte, Papaverine, Phentolamine, Yohimbine, PDE5 inhibitors (Avanafil, Sildenafil, Tadalafil, Udenafil, Vardenafil)
Other urologicals	Acetohydroxamic acid, Collagen, Dimethyl sulfoxide, Magnesium hydroxide, Pentosan polysulfate, Phenazopyridine, Phenyl salicylate, Succinimide
For benign prostatic hypertrophy	5α-reductase inhibitors: Dutasteride, Finasteride Alpha blockers: Alfuzosin, Doxazosin, Tamsulosin, Terazosin Herbals: Pygeum africanum, Serenoa repens