Alosetron

Alosetron Brand Name– Lotronex

What is Alosetron

Alosetron is an oral selective serotonin 5-HT3 receptor antagonist. It is approved with restrictions for the treatment of women who exhibit severe diarrhea-predominant irritable bowel syndrome (IBS) and have failed conventional therapy.

Severe IBS occurs in < 5% of patients. Efficacy in men has not been established. In clinical studies, women with severe diarrhea-predominant IBS (bowel urgency >= 50% of days) had significant increases (13—16%) in the median percentage of days with urgency control vs. placebo; a retrospective analysis of the data concurred that alosetron had a beneficial effect on control of bowel urgency in these patients.

The diagnosis of IBS has been defined according to the ROME II criteria used to assess IBS subgroups (e.g., diarrhea- or constipation-predominant) as well as by a recent evidence and consensus-based guideline.

The FDA originally approved alosetron for diarrhea-predominant IBS in February 2000.

Indications

  • irritable bowel syndrome

For the treatment of severe, chronic, diarrhea-predominant irritable bowel syndrome (IBS) in women for whom conventional therapy has failed

NOTE: Diarrhea-predominant IBS is considered severe if it includes diarrhea and one or more of the following: frequent/severe abdominal pain; frequent bowel urgency or fecal incontinence; restriction of daily activities due to IBS. 

Side Effects

  1. abdominal pain
  2. alopecia
  3. anxiety
  4. atopic dermatitis
  5. bone pain
  6. cholecystitis
  7. colitis
  8. confusion
  9. constipation
  10. cough
  11. depression
  12. diuresis
  13. drowsiness
  14. dysgeusia
  15. dyspepsia
  16. elevated hepatic enzymes
  17. flatulence
  18. folliculitis
  19. gastroesophageal reflux
  20. GI bleeding
  21. GI obstruction
  22. GI perforation
  23. headache
  24. hemorrhoids
  25. hepatitis
  26. hyperglycemia
  27. hypertension
  28. hypoglycemia
  29. ileus
  30. increased urinary frequency
  31. infection
  32. laryngitis
  33. menstrual irregularity
  34. myalgia
  35. nausea
  36. photophobia
  37. polyuria
  38. rash
  39. sinus tachycardia
  40. toxic megacolon
  41. urticaria
  42. vomiting
  43. xerostomia

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • anticholinergic medications
  • bleeding
  • breast-feeding
  • children
  • constipation
  • Crohn’s disease
  • diverticulitis
  • geriatric
  • GI bleeding
  • GI disease
  • GI obstruction
  • GI perforation
  • hepatic disease
  • infants
  • ischemic colitis
  • neonates
  • pregnancy
  • renal failure
  • renal impairment
  • thrombophlebitis
  • toxic megacolon
  • ulcerative colitis

Interactions

  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Codeine
  • Acetaminophen; Dextromethorphan; Doxylamine
  • Acetaminophen; Diphenhydramine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Propoxyphene
  • Acrivastine; Pseudoephedrine
  • Alfentanil
  • Amantadine
  • Amitriptyline
  • Amitriptyline; Chlordiazepoxide
  • Amoxapine
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amprenavir
  • Anticholinergics
  • Antidiarrheals
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atropine
  • Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Atropine; Difenoxin
  • Atropine; Diphenoxylate
  • Atropine; Edrophonium
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Belladonna; Opium
  • Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Benztropine
  • Bethanechol
  • Boceprevir
  • Brompheniramine
  • Brompheniramine; Carbetapentane; Phenylephrine
  • Brompheniramine; Dextromethorphan; Guaifenesin
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Brompheniramine; Pseudoephedrine
  • Buprenorphine
  • Buprenorphine; Naloxone
  • Bupropion
  • Bupropion; Naltrexone
  • Cannabidiol
  • Carbamazepine
  • Carbetapentane; Chlorpheniramine
  • Carbetapentane; Chlorpheniramine; Phenylephrine
  • Carbetapentane; Diphenhydramine; Phenylephrine
  • Carbetapentane; Phenylephrine; Pyrilamine
  • Carbetapentane; Pyrilamine
  • Carbinoxamine
  • Carbinoxamine; Dextromethorphan; Pseudoephedrine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Carbinoxamine; Phenylephrine
  • Carbinoxamine; Pseudoephedrine
  • Ceritinib
  • Chlophedianol; Dexbrompheniramine
  • Chlophedianol; Dexchlorpheniramine; Pseudoephedrine
  • Chlorcyclizine
  • Chlordiazepoxide; Clidinium
  • Chlorpheniramine
  • 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
  • Chlorpheniramine; Phenylephrine
  • Chlorpheniramine; Pseudoephedrine
  • Chlorpromazine
  • Ciprofloxacin
  • Cisapride
  • Clarithromycin
  • Clemastine
  • Clomipramine
  • Clozapine
  • Cobicistat
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Crofelemer
  • Cyclizine
  • Cyclobenzaprine
  • Cyproheptadine
  • Dalfopristin; Quinupristin
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Delavirdine
  • Desipramine
  • Dexamethasone
  • Dexchlorpheniramine
  • Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Dextromethorphan; Promethazine
  • Dicyclomine
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Dimenhydrinate
  • Diphenhydramine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Diphenhydramine; Phenylephrine
  • Disopyramide
  • Doxepin
  • Doxylamine
  • Doxylamine; Pyridoxine
  • Eluxadoline
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Fentanyl
  • Flavoxate
  • Fluoxetine; Olanzapine
  • Fluphenazine
  • Fluvoxamine
  • Fosamprenavir
  • Givosiran
  • Glycopyrrolate
  • Glycopyrrolate; Formoterol
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Homatropine; Hydrocodone
  • Hydantoins
  • Hydralazine
  • Hydralazine; Hydrochlorothiazide, HCTZ
  • Hydralazine; Isosorbide Dinitrate, ISDN
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Hydroxyzine
  • Hyoscyamine
  • Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate
  • Ibuprofen; Oxycodone
  • Idelalisib
  • Imipramine
  • Indacaterol; Glycopyrrolate
  • Indinavir
  • Isoniazid, INH
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Ketoconazole
  • Leflunomide
  • Letermovir
  • Levorphanol
  • Lopinavir; Ritonavir
  • Lubiprostone
  • Maprotiline
  • Meclizine
  • Mepenzolate
  • Meperidine
  • Meperidine; Promethazine
  • Mephobarbital
  • Mesoridazine
  • Methadone
  • Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine
  • Methscopolamine
  • Metoclopramide
  • Mexiletine
  • Mitotane
  • Morphine
  • Morphine; Naltrexone
  • Nefazodone
  • Nelfinavir
  • Netupitant, Fosnetupitant; Palonosetron
  • Norfloxacin
  • Nortriptyline
  • Obeticholic Acid
  • Olanzapine
  • Ombitasvir; Paritaprevir; Ritonavir
  • Opiate Agonists
  • Orphenadrine
  • Oxybutynin
  • Oxycodone
  • Oxymorphone
  • Palonosetron
  • Peginterferon Alfa-2b
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenobarbital
  • Phenothiazines
  • Phenylephrine; Promethazine
  • Posaconazole
  • Pramlintide
  • Primidone
  • Procainamide
  • Prochlorperazine
  • Promethazine
  • Propantheline
  • Propoxyphene
  • Protriptyline
  • Quinine
  • Remifentanil
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifamycins
  • Ritonavir
  • Rucaparib
  • Saquinavir
  • Scopolamine
  • Sedating H1-blockers
  • St. John’s Wort, Hypericum perforatum
  • Streptogramins
  • Sufentanil
  • Telaprevir
  • Telithromycin
  • Teriflunomide
  • Thiabendazole
  • Thiethylperazine
  • Thioridazine
  • Tricyclic antidepressants
  • Trifluoperazine
  • Trihexyphenidyl
  • Trimipramine
  • Triprolidine
  • Trospium
  • Tucatinib
  • Vemurafenib
  • Voriconazole
  • Zafirlukast
  • Zileuton
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