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  Darifenacin

 


Darifenacin

Darifenacin review




Darifenacin is a drug used to treat urinary incontinence or the condition where the patient experiences an inability to control urination. It works by blocking nerve receptors responsible for bladder muscle contractions and relaxes overactive bladder muscles responsible for uncontrollable spasms which make holding urine difficult. It relieves the feeling of urgency to urinate and helps the patient hold urine for a longer period of time.

It is marketed under the brand names Enablex and Emselex by Novartis and comes is extended release 7.5mg and 15mg tablets.

It is specifically used reduce the constant feeling of wanting to urinate, difficulty to hold in urine, and uncontrollable urination caused by and overactive bladder. It does this by blocking the receptors to the bladder wall called muscarinic receptors that are found on the surface of the muscle cells.

The dosage for darifenacin is 7.5 mg once a day initially, and may be increased to 15 mg once each day about two weeks into the treatment. They should be taken with fluids and may or may not be taken with food. However, being an extended-release tablets, it should not be chewed or crushed and must be swallowed whole to ensure proper release. Always follow specific instructions given by your physician and do not attempt to change dosage without the doctor’s permission.

Patients suffering from less severe hepatic impairment or when darifenacin is taken along with CYP3A4 inhibitor drugs such as ketoconazole, itraconazole or ritonavir should not take more than 7.5 mg of darifenacin daily. It is not recommended to take darifenacin for those who have severe hepatic impairment.

Taking darifenacin may cause side effects. Inform your doctor if you experience any of these symptoms for a prolonged period of time: dryness of the mouth or the eyes, stomach upsets and abdominal pain, diarrhea or constipation, or fatigue.

Other more serious side effects include difficulty in urination, burning sensation when passing urine, rashes and itching, as well as other allergic reactions. Seek immediate medical attention when experiencing any of those symptoms.

Other side effects rarely observed include palpitations, confusion and hallucinations, and hypersensitivity reactions.

Care should be taken when administering darifenacin to people with certain health conditions. These includes people with decreased kidney and liver function, cases of blockage of urine outflow, those suffering from or at risk of urinary retention, sufferers of constipation, those with stomach or intestinal obstructions, patients with weak gastrointestinal muscle contractions, those with disorders concerning the involuntary nervous system and those being treated for closed angle glaucoma. In cases of severe liver or kidney dysfunction or extremely weak stomach, actual urinary blockage or severely weakened muscle contractions in the gut, darifenacin should not be given at all.

Darifenacin may also interact with other bladder and urinary medication, and may cause adverse reactions when taken with CYP3A4 inhibitor drugs. Taking darifenacin with anticholinergic drugs may also increase intensity and frequency of anticholinergic side effects such as dryness of the mouth mouth, constipation or blurred vision.

Darifenacin has the following structural formula:

Chemical structure of darifenacin


• Molecular formula of darifenacin is C28H30N2O2
• Chemical IUPAC Name is 2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenyl-acetamide
• Molecular weight is 426.55 g/mol



Brand name(s): Enablex


Review published on: 12 July 2009

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