Darifenacina
Darifenacina Uses, Dosage, Side Effects, Mechanism of Action, How Long Does it Take to Work? Darifenacina is a brand name. Its generic name is Darifenacin.
Introduction
Darifenacina is an oral antimuscarinic agent approved for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and frequency. Darifenacina is a selective and competitive antagonist of muscarinic M3-receptors in the smooth muscle of the bladder and the urinary tract.
Uses
Darifenacina 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
Darifenacina 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?
Darifenacina generally begins to work within 1-3 days, with the peak effects usually seen around 2-4 weeks.
Absorption
Darifenacina is poorly absorbed from the gastrointestinal tract, with an oral bioavailability of about 40%.
Route of Elimination
Darifenacina is metabolized in the liver by cytochrome P450 enzymes and then eliminated mainly via the feces.
Dosage
The usual dose of Darifenacina 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
Darifenacina should be taken with water, either with or without food. Swallow the tablet whole, without crushing or chewing.
Side Effects
Common side effects of Darifenacina include dry mouth, constipation, dizziness, drowsiness, blurred vision, difficulty urinating, nausea, and confusion.
Toxicity
The LD50 of Darifenacina for mice is 7000 mg/kg. Symptoms of overdose include dry mouth, confusion, exhaustion, dizziness, and blurred vision.
Precaution
Darifenacina 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. Darifenacina should also be used with caution in pregnant and breastfeeding women.
Interactions
Darifenacina 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 Darifenacina.
Disease Interactions
Darifenacina may worsen the symptoms of narrow-angle glaucoma, so it is important to inform your doctor if you have this condition. Darifenacina 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
Darifenacina 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 Darifenacina with a full glass of water, either with or without food.
Pregnancy Use
Darifenacina 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
Darifenacina 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
Darifenacina 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 Darifenacina or any of its ingredients.
Use Directions
Darifenacina should be taken exactly as prescribed. Do not take more or less than the recommended dose. You may take Darifenacina with or without food.
Storage Condition
Store Darifenacina at room temperature between 15°C and 30°C (59°F and 86°F). Keep Darifenacina away from light, moisture, and heat.
Volume of Distribution
The volume of distribution for Darifenacina is approximately 18L.
Half Life
The elimination half-life of Darifenacina is about 11 hours.
Clearance
The clearance of Darifenacina in healthy volunteers is approximately 3.5 mL/min/kg.
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