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Tolterodine; Uses, Dosage, Side Effects, Drug Interactions

Tolterodine is a benzhydryl compound and a muscarinic receptor antagonist possessing both antimuscarinic and antispasmodic properties. Both tolterodine and its active metabolite, 5-hydroxymethyl tolterodine, competitively blocks muscarinic receptors, thereby inhibiting acetylcholine binding. This antagonistic action results in an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, indicating an antimuscarinic action on the lower urinary tract. The 5-hydroxymethyl metabolite appears to contribute significantly to the therapeutic effects.

Tolterodine is an antimuscarinic drug that is used for symptomatic treatment of urinary incontinence. 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.

Mechanism of Action of Tolterodine

Both tolterodine and its active metabolite, 5-hydroxymethyl tolterodine, act as competitive antagonists at muscarinic receptors. This antagonism results in inhibition of bladder contraction, a decrease in detrusor pressure, and an incomplete emptying of the bladder.nBoth urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine are an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, consistent with an antimuscarinic action on the lower urinary tract.

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Indications of Tolterodine

Overactive Bladder
Urinary Incontinence
Treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).
For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).

Contra-Indications of Tolterodine

Disorder of mental processes due to a brain disease
Myasthenia gravis
closed angle glaucoma
Worsening of glaucoma
Very rapid heartbeat – torsades de pointes
prolonged QT interval on EKG
Abnormal EKG with QT changes from birth
Narrowing of the opening between the stomach and small intestine
severe liver disease
severe renal impairment
Blockage of urinary bladder
Cannot empty bladder
Problem emptying stomach contents
Decreased motility function of stomach or intestines

Dosages of Tolterodine

Strengths: 1 mg; 2 mg; 4 mg

Urinary Incontinence

Immediate release tablets

Initial dose: 2 mg orally 2 times a day
Maintenance dose: 1 to 2 mg orally 2 times a day, depending on patient response and tolerability

Extended release capsules

Initial dose: 4 mg orally once a day
Maintenance dose: 2 to 4 mg orally once a day, depending on patient response and tolerability

Urinary Frequency

Immediate release tablets

Initial dose: 2 mg orally 2 times a day
Maintenance dose: 1 to 2 mg orally 2 times a day, depending on patient response and tolerability

Extended release capsules

Initial dose: 4 mg orally once a day
Maintenance dose: 2 to 4 mg orally once a day, depending on patient response and tolerability

Side Effects of tolterodine

The most common

xerostomia (dry mouth)
decreased gastric motility (upset stomach)
Headache
constipation
dry eyes
sleepiness
urinary retention
chest pain, fast or uneven heart rate;
confusion, hallucinations;
urinating less than usual or not at all; or
painful or difficult urination.

More common

Abnormal vision, including difficulty with adjusting to distances
bloody or cloudy urine
difficult, burning, or painful urination
frequent urge to urinate
Sensation of pins and needles in the fingers and toes
Allergic reactions
Nervousness
Aware of the heartbeat (palpitations)
Heart failure
Irregular heartbeat
Heart burn
Memory impairment

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Less common

Chest pain
cough
diarrhea
fever
general feeling of discomfort or illness
headache
joint pain
loss of appetite
muscle aches and pains
nausea
pain or tenderness around the eyes and cheekbones
shortness of breath or troubled breathing
sore throat
stuffy or runny nose
sweating
the tightness of the chest or wheezing
trouble with sleeping

Drug Interactions of tolterodine

Toltaradin may interact with following drugs, supplements & may change the efficacy of drugs

arsenic trioxide
chloroquine or halofantrine
cyclosporine
droperidol
narcotic medication such as levomethadyl or methadone ;
pentamidine
antibiotics such as azithromycin , clarithromycin , erythromycin , or telithromycin ;
medicines to treat psychiatric disorders, such as chlorpromazine , haloperidol mesoridazine pimozide , or thioridazine ; or
heart rhythm medicine such as amiodarone , dofetilide , disopyramide , procainamide , quinidine , or sotalol .

Pregnancy & Lactation of tolterodine

FDA Pregnancy Category C

Pregnancy

You should not use Tolterodine tablets when you are pregnant. Tell your doctor immediately if you are pregnant, think you are pregnant or are planning to become pregnant.

Breast-feeding

It is not known if tolterodine is excreted in the mother’s breast milk. Breastfeeding is not recommended during administration of Tolterodine tablets.