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Fesoterodine

Mechanism :

Fesoterodine is converted to its active metabolite 5-hydroxymethyltolterodine. It is a competitive muscarinic antagonist. It inhibits bladder contraction and lowers detrusor pressure due to its antimuscarinic action on the bladder.

Indication :

Pediatric neurogenic detrusor overactivity (NDO) in patients above 6 years of age.

Contraindications :

• Hypersensitivity to the drug

• Hypersensitivity to tolterodine

• Angle closure glaucoma

• Retention of urine

• Gastric retention

• Child Pugh class C hepatic impairment

• Creatinine clearance <30 in pediatric patients with weight 26-30kg

• Creatinine clearance 15-30 in pediatric patients with weight >35kg

• Use with caution if creatinine clearance 30-89 in pediatric patients with weight 26-35 kg

• Use with caution if creatinine clearance 15-30 in pediatric patients with weight >30 kg

• Use cautiously in patients with gastrointestinal obstruction

• Use cautiously in patients with impared gastrointestinal motility

• Use cautiously in patients with bladder obstruction

• Use cautiously in patients with myasthenia gravis

• Use cautiously in patients living in high temperatures

Dosing :

Extended release tablets available in the strengths of 4 mg and 8 mg. Do not crush/cut/chew tablet.

<6 years:

Safety and efficacy not well known.

≥6 years:

Weight ≤25 kg: Safety and efficacy not well known.

Weight 25-35 kg: 4 mg orally once daily; dose may be increased to 8 mg orally once daily if required.

Weight >35 kg: 4 mg orally once daily; increase the dose to 8 mg orally once daily after the first week.

Dose modification with concurrent use of strong CYP3A4 inhibitors ( eg, ketoconazole, itraconazole, clarithromycin):

≥6 years with weight 25-30 kg: Not recommended.

≥6 years with >30 kg: maximum daily dose = 4 mg PO.

Adverse Effect :

Diarrhea, dryness of the mouth, pain in the abdomen, urinary tract infection, constipation, weight gain, tachycardia, headache, ophthalmologic reactions, dyspepsia, Insomnia.

Interaction :

• Caffeine

• Opiate drugs

• Ethanol

• Anticholinergics

• Clarithromycin

• Amprenavir

• Atazanavir

• Cobicistat

• Difenoxin

• Ceritinib

• Chloramphenicol

• Cisapride

• Clozapine

• Guaifenesin

• Ritonavir

• Grapefruit juice

• Green tea

• Mifepristone

• Mirabegron

• Antivirals

• Voriconazole

• Salicylamide

• Phenyltoloxamine

Lactation :

Use with caution during breastfeeding. There is no human data regarding the risk to child.

Hepatic Dose :

Avoid use in Child Pugh class C

Pregnanacy :

Use cautiously during pregnancy. There is no human data regarding the risk to fetus.