alosetron

Contraindicated in:

Hypersensitivity;
Constipation;
History of chronic/severe constipation or complications due to constipation;
History of GI obstruction, stricture, toxic megacolon, perforation, and/or adhesions;
History of ischemic colitis, ↓ intestinal circulation, thrombophlebitis, or coagulation defects;
History of Crohn disease/ulcerative colitis/diverticulitis;
Severe hepatic impairment;
Concurrent use of fluvoxamine.

Use Cautiously in:

Mild or moderate hepatic impairment;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children;
Geri: ↑risk of constipation in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

GI:

, abdominal discomfort, abdominal distention, ACUTE ISCHEMIC COLITIS , flatulence, nausea, GI viral infections, hemorrhoids, regurgitation or reflux, TOXIC MEGACOLON

Interactions ⬆ ⬇

Drug-drug:

Fluvoxamine can ↑ levels and risk of toxicity; concurrent use contraindicated.
Amiodarone, cimetidine, ciprofloxacin, clarithromycin, itraconazole, ketoconazole, ofloxacin, protease inhibitors, and voriconazole may ↑ levels and risk of toxicity; use concurrently with caution.

Availability ⬆ ⬇

(Generic available)

Tablets: 0.5 mg; 1 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 0.5 mg twice daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

5-HT₃ receptors are nonselective cation channels responsible for regulation of visceral pain, colonic transit, and GI secretions. Alosetron inhibits the activation of these channels.

Therapeutic effects:

Increased colonic transit time without affecting orocecal transit time, resulting in decreased pain/discomfort and diarrhea associated with IBS.

Classifications ⬆ ⬇

Therapeutic Classification: anti irritable bowel syndrome agents

Pharmacologic Classification: five ht3 antagonists

Pharmacokinetics ⬆ ⬇

Absorption: 50–60% absorbed following oral administration.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Extensively metabolized by the liver; 13% excreted unchanged in urine.

Half-Life: 1.5 hr.

Time/Action Profile ⬆ ⬇

(pain/discomfort, diarrhea)

ROUTE	ONSET	PEAK	DURATION
PO	within 1–2 wk	up to 6 wk	1 wk‡

‡Following discontinuation.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take alosetron exactly as directed. If a dose is missed, skip the dose and return to regular schedule; do not double doses. Counsel patients about the risks and benefits of alosetron and the impact of IBS symptoms on their life. Patients should read the Medication Guide before starting alosetron and each time they refill their prescription.
Caution patient to stop taking alosetron and report constipation or signs of ischemic colitis to health care professional immediately. Immediately contact health care professional again if constipation does not resolve after discontinuation of alosetron. Alosetron should be resumed only after constipation has resolved and on the advice of their health care professional. Treatment with alosetron should not be resumed in patients who develop ischemic colitis.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Rep: Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

45963- Actavis Pharma, Inc.
- 45963-479- Alosetron Hydrochloride
  - 45963-479-03- 1 BOTTLE in 1 CARTON (45963-479-03) / 30 TABLET in 1 BOTTLE

45963- Actavis Pharma, Inc.
- 45963-480- Alosetron Hydrochloride
  - 45963-480-03- 1 BOTTLE in 1 CARTON (45963-480-03) / 30 TABLET in 1 BOTTLE

53104- Cipla Ltd.
- 53104-7658-
  - 53104-7658-1- 1 kg in 1 DRUM (53104-7658-1)

53746- Amneal Pharmaceuticals of New York LLC
- 53746-248- Alosetron Hydrochloride
  - 53746-248-30- 30 TABLET, FILM COATED in 1 BOTTLE (53746-248-30)

53746- Amneal Pharmaceuticals of New York LLC
- 53746-249- Alosetron Hydrochloride
  - 53746-249-30- 30 TABLET, FILM COATED in 1 BOTTLE (53746-249-30)

54766- Sebela Pharmaceuticals Inc.
- 54766-894- LOTRONEX
  - 54766-894-03- 30 TABLET in 1 BOTTLE (54766-894-03)

54766- Sebela Pharmaceuticals Inc.
- 54766-895- LOTRONEX
  - 54766-895-03- 30 TABLET in 1 BOTTLE (54766-895-03)

58159- NURAY CHEMICALS PRIVATE LIMITED
- 58159-032-
  - 58159-032-01- 35 kg in 1 DRUM (58159-032-01)

63629- Bryant Ranch Prepack
- 63629-2518- Alosetron
  - 63629-2518-1- 30 TABLET in 1 BOTTLE (63629-2518-1)

65162- Amneal Pharmaceuticals LLC
- 65162-248- Alosetron Hydrochloride
  - 65162-248-03- 30 TABLET, FILM COATED in 1 BOTTLE (65162-248-03)

65162- Amneal Pharmaceuticals LLC
- 65162-248- Alosetron Hydrochloride
  - 65162-248-50- 500 TABLET, FILM COATED in 1 BOTTLE (65162-248-50)

65162- Amneal Pharmaceuticals LLC
- 65162-249- Alosetron Hydrochloride
  - 65162-249-03- 30 TABLET, FILM COATED in 1 BOTTLE (65162-249-03)

65162- Amneal Pharmaceuticals LLC
- 65162-249- Alosetron Hydrochloride
  - 65162-249-50- 500 TABLET, FILM COATED in 1 BOTTLE (65162-249-50)

70756- Lifestar Pharma LLC
- 70756-701- Alosetron
  - 70756-701-30- 30 TABLET in 1 BOTTLE (70756-701-30)

70756- Lifestar Pharma LLC
- 70756-702- Alosetron
  - 70756-702-30- 30 TABLET in 1 BOTTLE (70756-702-30)

76055- Sionc Pharmaceutical Private Limited
- 76055-0009-
  - 76055-0009-1- 25 kg in 1 DRUM (76055-0009-1)

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Indications ⬇

Contraind./Precautions ⬆ ⬇