Darifénacine
Darifénacine Uses, Dosage, Side Effects, Mechanism of Action, How Long Does it Take to Work? Darifénacine is a brand name. Its generic name is Darifenacin.
Introduction
Darifénacine is an oral antimuscarinic agent approved for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and frequency. Darifénacine is a selective and competitive antagonist of muscarinic M3-receptors in the smooth muscle of the bladder and the urinary tract.
Uses
Darifénacine is used to treat overactive bladder (a condition in which the bladder muscles contracts uncontrollably and causes frequent urination, urgent need to urinate, and inability to control urination). It works by relaxing the bladder muscles.
Mechanism of Action
Darifénacine is an orally active quaternary ammonium antimuscarinic. It binds to M3-muscarinic receptors, decreasing acetylcholine release from the parasympathetic nerves, thus decreasing bladder contractions and urinary urgency and frequency.
How Long Does it Take to Work?
Darifénacine generally begins to work within 1-3 days, with the peak effects usually seen around 2-4 weeks.
Absorption
Darifénacine is poorly absorbed from the gastrointestinal tract, with an oral bioavailability of about 40%.
Route of Elimination
Darifénacine is metabolized in the liver by cytochrome P450 enzymes and then eliminated mainly via the feces.
Dosage
The usual dose of Darifénacine is 7.5 mg orally once daily, although it can be increased to 15 mg once daily in certain patients or in certain clinical cases. The effects of the drug last for about 24 hours, so the drug must be taken each day.
Administration
Darifénacine should be taken with water, either with or without food. Swallow the tablet whole, without crushing or chewing.
Side Effects
Common side effects of Darifénacine include dry mouth, constipation, dizziness, drowsiness, blurred vision, difficulty urinating, nausea, and confusion.
Toxicity
The LD50 of Darifénacine for mice is 7000 mg/kg. Symptoms of overdose include dry mouth, confusion, exhaustion, dizziness, and blurred vision.
Precaution
Darifénacine is not recommended for people with narrow-angle glaucoma or blockage of the gut or urinary tract. It should also be used with caution in people with a history of urinary retention, hypertension, or cardiac dysrhythmias. Darifénacine should also be used with caution in pregnant and breastfeeding women.
Interactions
Darifénacine may interact with other medications, such as antacids, antibiotics, antidepressants, or antipsychotics. Therefore, it is important to inform your doctor of any medications you are taking prior to starting Darifénacine.
Disease Interactions
Darifénacine may worsen the symptoms of narrow-angle glaucoma, so it is important to inform your doctor if you have this condition. Darifénacine may also worsen urinary obstruction, so it is important to inform your doctor if you have any signs or symptoms of this condition.
Drug Interaction
Darifénacine may interact with other drugs which increase the risk of side effects such as drowsiness, dizziness, dry mouth, confusion, difficulty urinating, and blurred vision. Examples include antacids, tricyclic antidepressants, MAOIs, and certain antipsychotics.
Food Interactions
It is recommended to take Darifénacine with a full glass of water, either with or without food.
Pregnancy Use
Darifénacine should be used with caution in women who are pregnant. It is not known if it is safe for use in pregnant women.
Lactation Use
Darifénacine should be used with caution in women who are breastfeeding. It is not known if it is safe for use in lactating women.
Acute Overdose
Symptoms of an overdose may include dry mouth, confusion, exhaustion, dizziness, and blurred vision. If an overdose is suspected, seek medical attention immediately.
Contraindication
Darifénacine should not be used in people with narrow-angle glaucoma, blockage of the gut or urinary tract, or urinary retention. It should also not be used in people who are hypersensitive to Darifénacine or any of its ingredients.
Use Directions
Darifénacine should be taken exactly as prescribed. Do not take more or less than the recommended dose. You may take Darifénacine with or without food.
Storage Condition
Store Darifénacine at room temperature between 15°C and 30°C (59°F and 86°F). Keep Darifénacine away from light, moisture, and heat.
Volume of Distribution
The volume of distribution for Darifénacine is approximately 18L.
Half Life
The elimination half-life of Darifénacine is about 11 hours.
Clearance
The clearance of Darifénacine in healthy volunteers is approximately 3.5 mL/min/kg.
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