Tolterodine; Uses, Dosage, Side Effects, Drug Interactions

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.

You Might Also Like   Management of Drug Interactions, Types, Guideline

Indications of Tolterodine

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 

More common

You Might Also Like   Uses Indications of Eluxadoline Tablet

Less common

Drug Interactions of tolterodine

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

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.

References

You Might Also Like   Nisoldipine; Uses, Dosage, Side Effects, Interactions

 

About the author

Translate »