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Enablex

Enablex - General Information

Enablex (Enablex®, Novartis) is a medication used to treat urinary incontinence.
Enablex works by blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions. It thereby decreases the urgency to urinate. It should not be used in people with urinary retention.
It is not known whether this selectivity for the M3 receptor translates into any clinical advantage when treating symptoms of overactive bladder syndrome.

 

Pharmacology of Enablex

Enablex is a competitive muscarinic receptor antagonist. In vitro studies using human recombinant muscarinic receptor subtypes show that darifenacin has greater affinity for the M3 receptor than for the other known muscarinic receptors (9 and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4). Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of the urinary bladder smooth muscle and stimulation of salivary secretion. Adverse drug effects such as dry mouth, constipation and abnormal vision may be mediated through effects on M3 receptors in these organs.

 

Enablex for patients

Patients should be informed that anticholinergic agents, such as ENABLEX, may produce clinically significant adverse effects related to anticholinergic pharmacological activity including constipation, urinary retention and blurred vision. Heat prostration (due to decreased sweating) can occur when anticholinergics such as ENABLEX are used in a hot environment. Because anticholinergics, such as ENABLEX, may produce dizziness or blurred vision, patients should be advised to exercise caution in decisions to engage in potentially dangerous activities until the drug's effects have been determined. Patients should read the patient information leaflet before starting therapy with ENABLEX.

ENABLEX extended-release tablets should be taken once daily with liquid. They may be taken with or without food, and should be swallowed whole and not chewed, divided or crushed.


PATIENT INSERT

ENABLEX® (darifenacin)
Extended-release tablets 7.5 mg or 15 mg

Read the Patient Information that comes with ENABLEX before you start taking it and each time you get a refill. There may be new information. This leaflet does not take the place of talking to your doctor or other healthcare professional about your medical condition or your treatment. Only your doctor or healthcare professional can determine if treatment with ENABLEX is right for you.

What is ENABLEX?

ENABLEX is a prescription medicine used in adults to treat the following symptoms due to a condition called overactive bladder:

  • having a strong need to go to the bathroom right away (also called "urgency")
  • leaking or wetting accidents (also called "urinary incontinence")
  • having to go to the bathroom too often (also called "urinary frequency")

What is overactive bladder?

Overactive bladder happens when you cannot control your bladder contractions. When these muscle contractions happen too often or cannot be controlled, you get symptoms of overactive bladder, which are urinary urgency, urinary incontinence (leakage) and urinary frequency.

Who should not take ENABLEX?

Do not take ENABLEX if you:

  • are not able to empty your bladder (also called "urinary retention")
  • have delayed or slow emptying of your stomach (also called "gastric retention")
  • have an eye problem called "uncontrolled narrow-angle glaucoma"
  • are allergic to ENABLEX or to any of its ingredients. See the end of this leaflet for a complete list of ingredients.

ENABLEX has not been studied in children.

What should I tell my doctor before starting ENABLEX?

Before starting ENABLEX, tell your doctor or healthcare professional about all of your medical conditions including if you:

  • have any stomach or intestinal problems, or problems with constipation
  • have trouble emptying your bladder or if you have a weak urine stream
  • have an eye problem called narrow-angle glaucoma
  • have liver problems
  • are pregnant or planning to become pregnant. It is not known if ENABLEX can harm your unborn baby.
  • are breastfeeding. It is not known if ENABLEX passes into breast milk and if it can harm your baby.

Tell your doctor about all the medicines you take, including prescription and nonprescription medicines, vitamins, and herbal supplements. ENABLEX and certain other medicines can interact with each other, causing side effects. Especially tell your doctor if you take:

  • ketoconazole (Nizoral) or itraconazole (Sporonox), antifungal medicines
  • clarithromycin (Biaxin), an antibiotic medicine
  • ritonivir or nelfinavir (Viracept), antiviral medicines
  • nefazadone (Serzone), a depression medicine
  • flecainide (Tambocor), an abnormal heartbeat (antiarrhythmia) medicine
  • thioridazine (Mellaril), a mental disorder (antipsychotic) medicine
  • a medicine called a tricyclic antidepressant

Know all the medicines you take. Keep a list of them with you to show your doctor and pharmacist each time you get a new medicine.

How should I take ENABLEX?

Take ENABLEX exactly as prescribed. Your doctor will prescribe the dose that is right for you. Your doctor may prescribe the lowest dose if you have certain medical conditions such as liver problems.

  • You should take ENABLEX once daily with liquid.
  • ENABLEX should be swallowed whole and not chewed, divided or crushed.
  • ENABLEX may be taken with or without food.
  • If you miss a dose of ENABLEX, begin taking ENABLEX again the next day. Do not take two doses of ENABLEX in the same day.
  • If you take too much ENABLEX, call your local Poison Control Center or emergency room right away.

What are the possible side effects of ENABLEX?

The most common side effects with ENABLEX are:

  • dry mouth
  • constipation.

ENABLEX may cause other less common side effects, that include:

  • blurred vision. Use caution while driving or doing dangerous activities until you know how ENABLEX affects you.
  • heat prostration. Heat prostration (due to decreased sweating) can occur when drugs such as ENABLEX are used in a hot environment.

These are not all the side effects with ENABLEX. For more information, ask your doctor, healthcare professional or pharmacist.

How do I store ENABLEX?

  • Keep ENABLEX and all medicines out of the reach of children.
  • Store ENABLEX at room temperature, 59 to 86° F (15 to 30° C). Protect from light.
  • Safely dispose of ENABLEX that is out of date or no longer needed.

General information about ENABLEX

Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not give ENABLEX to other people, even if they have the same symptoms you have. It may harm them.

This leaflet summarizes the most important information about ENABLEX. If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about ENABLEX that is written for health professionals. You can also call the product information department at 1-888-44 ENABLEX (1 888-443-6225) or visit the website at www.ENABLEX.com.

What are the ingredients in ENABLEX?

Active Ingredient: darifenacin

Inactive Ingredients: dibasic calcium phosphate anhydrous, hydroxypropyl methylcellulose (hypromellose), lactose monohydrate, magnesium stearate, titanium dioxide and triacetin. The 15 mg tablet also contains FD&C Yellow No. 6 Aluminum Lake.

Appearance

The 7.5-mg tablet is round and white-colored with "DF" on one side and "7.5" on the other side

The 15-mg tablet is round and peach-colored with "DF" on one side and "15" on the other side.

*Mellaril is a registered trademark of Novartis Inc. The other brands listed are the trademarks of their respective owners and not trademarks of Novartis Inc.

Manufactured by: Pfizer Incorporated Brooklyn, New York 11206, Distributed by: Novartis Pharmaceuticals Corporation East Hanover, New Jersey 07936,

 

Enablex Interactions

The daily dose of ENABLEX should not exceed 7.5 mg when coadministered with potent CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, nelfinavir, clarithromycin and nefazadone) . Caution should be taken when ENABLEX is used concomitantly with medications that are predominantly metabolized by CYP2D6 and which have a narrow therapeutic window, such as flecainide, thioridazine and tricyclic antidepressants (see CLINICAL PHARMACOLOGY). The concomitant use of ENABLEX with other anticholinergic agents may increase the frequency and/or severity of dry mouth, constipation, blurred vision and other anticholinergic pharmacological effects. Anticholinergic agents may potentially alter the absorption of some concomitantly administered drugs due to effects on gastrointestinal motility.

Drug Laboratory Test Interactions

Interactions between darifenacin and laboratory tests have not been studied.

 

Enablex Contraindications

ENABLEX (darifenacin) extended-release tablets are contraindicated in patients with urinary retention, gastric retention or uncontrolled narrow-angle glaucoma and in patients who are at risk for these conditions. ENABLEX is also contraindicated in patients with known hypersensitivity to the drug or its ingredients.

 

Additional information about Enablex

Enablex Indication: For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.
Mechanism Of Action: Enablex selectively antagonizes the muscarinic M3 receptor. M3 receptors are involved in contraction of human bladder and gastrointestinal smooth muscle, saliva production, and iris sphincter function.
Drug Interactions: Clarithromycin This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
Itraconazole This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
Ketoconazole This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
Nefazodone This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
Nelfinavir This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
Ritonavir This potent CYP3A4 inhibitor slows darifenacin/solifenacin metabolism
Rivastigmine Possible antagonism of action
Food Interactions: Take without regard to meals.
Generic Name: Darifenacin
Synonyms: Not Available
Drug Category: Urinary antispasmodics
Drug Type: Small Molecule; Approved

Other Brand Names containing Darifenacin: Enablex;
Absorption: The mean oral bioavailability at steady state is estimated to be 15% and 19% for 7.5 mg and 15 mg tablets, respectively.
Toxicity (Overdose): Overdosage can potentially result in severe central anticholinergic effects.
Protein Binding: Darifenacin is approximately 98% bound to plasma proteins (primarily to alpha-1-acid-glycoprotein).
Biotransformation: Hepatic. Primarily mediated by the cytochrome P450 enzymes CYP2D6 and CYP3A4.
Half Life: The elimination half-life of darifenacin following chronic dosing is approximately 13-19 hours.
Dosage Forms of Enablex: Tablet, extended release Oral
Chemical IUPAC Name: 2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-di(phenyl)acetamide
Chemical Formula: C28H30N2O2
Darifenacin on Wikipedia: https://en.wikipedia.org/wiki/Darifenacin
Organisms Affected: Humans and other mammals