Darifenacin

Darifenacin Brand Name– Enablex

What is Darifenacin

Darifenacin hydrobromide is an oral competitive, selective M3 muscarinic receptor antagonist administered once daily to treat overactive bladder (OAB) and its symptoms in adults.

Both M2 and M3 receptors are located in the detrusor muscle; even though M2 receptors are much more prevalent, it appears that M3 receptors are more important in mediating direct detrusor contractions.

The M3 receptor is also involved in gastrointestinal smooth muscle function, salivary production, and iris sphincter function.

Treatment with darifenacin for OAB results in significant reductions in the frequency of urinary incontinence, reductions in the number of micturitions per day, and improvements in the frequency and severity of symptoms including urgency. In addition, darifenacin has been shown to be as effective as oxybutynin in reducing the incidence of incontinent episodes and symptoms of urgency.

When compared with oxybutynin, the incidence of dry mouth was found to be significantly lower with darifenacin (13% for darifenacin vs. 36% for oxybutynin, p less than 0.05).

Darifenacin was FDA-approved in 2004.

Indications

  1. overactive bladder (OAB)
  2. urinary incontinence

For the treatment of an overactive bladder (OAB) with symptoms of urinary frequency, urinary urgency, or urge-related urinary incontinence

Side Effects

  1. abdominal pain
  2. anaphylactoid reactions
  3. angioedema
  4. arthralgia
  5. asthenia
  6. back pain
  7. confusion
  8. constipation
  9. diarrhea
  10. dizziness
  11. drowsiness
  12. dyspepsia
  13. erythema multiforme
  14. hallucinations
  15. headache
  16. hypertension
  17. nausea
  18. palpitations
  19. peripheral edema
  20. pharyngitis
  21. pruritus
  22. rash
  23. rhinitis
  24. urinary retention
  25. vaginitis
  26. vomiting
  27. weight gain
  28. xerophthalmia
  29. xerostomia

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • anticholinergic medications
  • autonomic neuropathy
  • bladder obstruction
  • breast-feeding
  • children
  • closed-angle glaucoma
  • constipation
  • contact lenses
  • driving or operating machinery
  • gastroparesis
  • geriatric
  • GI obstruction
  • hepatic disease
  • history of angioedema
  • ileus
  • infants
  • myasthenia gravis
  • pregnancy
  • prostatic hypertrophy
  • pyloric stenosis
  • ulcerative colitis
  • urinary retention
  • urinary tract obstruction

Interactions

  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Codeine
  • Acetaminophen; Dextromethorphan
  • Acetaminophen; Dextromethorphan; Doxylamine
  • Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
  • Acetaminophen; Dextromethorphan; Phenylephrine
  • Acetaminophen; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Tramadol
  • Alfentanil
  • Amantadine
  • Amiloride
  • Amiloride; Hydrochlorothiazide, HCTZ
  • Amiodarone
  • Amitriptyline
  • Amitriptyline; Chlordiazepoxide
  • Amlodipine; Celecoxib
  • Amobarbital
  • Amoxapine
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amprenavir
  • Apalutamide
  • Aprepitant, Fosaprepitant
  • Aripiprazole
  • Artemether; Lumefantrine
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atropine; Difenoxin
  • Atropine; Diphenoxylate
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Barbiturates
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Belladonna; Opium
  • Benzhydrocodone; Acetaminophen
  • Boceprevir
  • Bosentan
  • Brexpiprazole
  • Brigatinib
  • Brompheniramine; Dextromethorphan; Guaifenesin
  • Brompheniramine; Dextromethorphan; Phenylephrine
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Bumetanide
  • Bupropion
  • Bupropion; Naltrexone
  • Butabarbital
  • Caffeine
  • Caffeine; Ergotamine
  • Carbamazepine
  • Carbidopa; Levodopa
  • Carbidopa; Levodopa; Entacapone
  • Carbinoxamine; Dextromethorphan; Pseudoephedrine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Celecoxib
  • Cenobamate
  • Ceritinib
  • Chloramphenicol
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dextromethorphan
  • Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Cimetidine
  • Ciprofloxacin
  • Cisapride
  • Citalopram
  • Clarithromycin
  • Clomipramine
  • Clozapine
  • Cobicistat
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Conivaptan
  • Dabrafenib
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Delavirdine
  • Desipramine
  • Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Dextromethorphan
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Dextromethorphan; Guaifenesin
  • Dextromethorphan; Guaifenesin; Phenylephrine
  • Dextromethorphan; Guaifenesin; Potassium Guaiacolsulfonate
  • Dextromethorphan; Guaifenesin; Pseudoephedrine
  • Dextromethorphan; Promethazine
  • Dextromethorphan; Quinidine
  • Digoxin
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diltiazem
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Doxepin
  • Doxorubicin
  • Dronedarone
  • Duloxetine
  • Dutasteride; Tamsulosin
  • Duvelisib
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elbasvir; Grazoprevir
  • Eliglustat
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Encorafenib
  • Enzalutamide
  • Escitalopram
  • Ethacrynic Acid
  • Fedratinib
  • Fentanyl
  • Fesoterodine
  • Flecainide
  • Fluconazole
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fosamprenavir
  • Fosphenytoin
  • Furosemide
  • grapefruit juice
  • Green Tea
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Haloperidol
  • Homatropine; Hydrocodone
  • Hydrochlorothiazide, HCTZ; Propranolol
  • Hydrochlorothiazide, HCTZ; Spironolactone
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Ibuprofen; Oxycodone
  • Idelalisib
  • Imatinib
  • Imipramine
  • Indinavir
  • Isavuconazonium
  • Itraconazole
  • Ivosidenib
  • Ketoconazole
  • Lefamulin
  • Letermovir
  • Levodopa
  • Loop diuretics
  • Loperamide
  • Loperamide; Simethicone
  • Lopinavir; Ritonavir
  • Lorlatinib
  • Lumacaftor; Ivacaftor
  • Maprotiline
  • Meperidine
  • Meperidine; Promethazine
  • Mephobarbital
  • Methadone
  • Methohexital
  • Mexiletine
  • Midazolam
  • Mifepristone
  • Mirabegron
  • Mitotane
  • Morphine
  • Morphine; Naltrexone
  • Nebivolol
  • Nebivolol; Valsartan
  • Nefazodone
  • Nelfinavir
  • Nortriptyline
  • Olanzapine
  • Ombitasvir; Paritaprevir; Ritonavir
  • Oritavancin
  • Orphenadrine
  • Oxycodone
  • Oxymorphone
  • Paroxetine
  • Pazopanib
  • Peginterferon Alfa-2b
  • Pentobarbital
  • Perphenazine; Amitriptyline
  • Pexidartinib
  • Phenobarbital
  • Phenytoin
  • Pimozide
  • Posaconazole
  • Potassium-sparing diuretics
  • Primidone
  • Propafenone
  • Propranolol
  • Protriptyline
  • Quetiapine
  • Quinidine
  • Remifentanil
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifamycins
  • Ritonavir
  • Rolapitant
  • Saquinavir
  • Secobarbital
  • Sertraline
  • Simeprevir
  • Spironolactone
  • Sufentanil
  • Tamsulosin
  • Tapentadol
  • Telaprevir
  • Telithromycin
  • Telotristat Ethyl
  • Terbinafine
  • Thiopental
  • Thioridazine
  • Tipranavir
  • Torsemide
  • Tramadol
  • Trandolapril; Verapamil
  • Triamterene
  • Tricyclic antidepressants
  • Trimipramine
  • Tucatinib
  • Vemurafenib
  • Verapamil
  • Voriconazole
  • Zafirlukast
  • Zileuton

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