Anti-Diarrheals

Crofelemer - fulyzaq ™

Drug UPDATES: FULYZAQ ™ (crofelemer) delayed-release tablets for oral use

Dosing: Click (+) next to Dosage and Administration section (drug info link)
ABBREVIATED MONOGRAPH - SEE PACKAGE INSERT.

Initial U.S. Approval: 2012

Mechanism of Action: Crofelemer is an inhibitor of both the cyclic adenosine monophosphate (cAMP)-stimulated cystic fibrosis transmembrane conductance regulator (CFTR) chloride ion (Cl-) channel, and the calcium-activated Cl- channels (CaCC) at the luminal membrane of enterocytes. The CFTR Cl- channel and CaCC regulate Cl- and fluid secretion by intestinal epithelial cells. Crofelemer acts by blocking Cl- secretion and accompanying high volume water loss in diarrhea, normalizing the flow of Cl- and water in the GI tract.

INDICATIONS AND USAGE: FULYZAQ is an anti-diarrheal indicated for the symptomatic relief of non-infectious diarrhea in adult patients with HIV/AIDS on anti-retroviral therapy.

DOSAGE AND ADMINISTRATION
The recommended dose of FULYZAQ is one 125 mg delayed-release tablet taken orally two times a day, with or without food. FULYZAQ tablets should not be crushed or chewed. Tablets should be swallowed whole.

HOW SUPPLIED: Delayed-Release Tablets: 125 mg

Kaopectate®

IMPORTANT:
In 2003, the active ingredient in Kaopectate was reformulated to contain bismuth subsalicylate, replacing attapulgite as the active ingredient. The FDA found attapulgite efficacy data to be inadequate.

INDICATIONS:
Symptomatic treatment of mild, nonspecific diarrhea; control of traveler's diarrhea (enterotoxigenic Escherichia coli ); as part of a multidrug regimen for H. pylori eradication to reduce the risk of duodenal ulcer recurrence

Mechanism of Action: not completely understood. Antimicrobial and antisecretory action.

DOSING:
Oral:
Treatment of nonspecific diarrhea, control/relieve traveler's diarrhea: Subsalicylate (doses based on 262 mg/15 mL liquid or 262 mg tablets):

Children >12 years and Adults: 2 tablets or 30 mL every 30 minutes to 1 hour as needed up to 8 doses/24 hours

SUPPLIED:
Caplet, as subsalicylate (Pepto-Bismol®): 262 mg [sugar free; contains sodium 2 mg]

Liquid, as subsalicylate: 262 mg/15 mL (240 mL, 360 mL, 480 mL); 525 mg/15 mL (240 mL, 360 mL)

Lomotil® (diphenoxylate + atropine)

Adults: DOSING: Diarrhea: Oral: The initial oral dose of diphenoxylate is 2 tablets (5 mg) or (10 ml) 4 times daily. Most patients will require this dosage until control has been attained, after which the dose may be adjusted according to the individual response. Control may be maintained with 2 tablets or 10 mL daily

Diphenoxylate:
Onset of action: Antidiarrheal: 45-60 minutes
Peak effect: Antidiarrheal: ~2 hours
Duration: Antidiarrheal: 3-4 hours.
Half-life: 2.5 hours.

If there is no response with 48 hours, the drug is unlikely to be effective and should be discontinued; if chronic diarrhea is not improved symptomatically within 10 days at maximum dosage of 20 mg/day, control is unlikely with further use.

Supplied
Solution, oral: Diphenoxylate hydrochloride 2.5 mg and atropine sulfate 0.025 mg per 5 mL. Tablet (Lomotil®, Lonox®): Diphenoxylate hydrochloride 2.5 mg and atropine sulfate 0.025 mg.

Loperamide ( imodium® )

Adults: DOSING: [2 mg capsule /tablet]
Acute diarrhea: Oral: Initial: 4 mg, followed by 2 mg after each loose stool, up to 16 mg/day

Chronic diarrhea: Oral: Initial: Follow acute diarrhea; maintenance dose should be slowly titrated downward to minimum required to control symptoms (typically, 4-8 mg/day in divided doses)

Traveler's diarrhea: Oral: Initial: 4 mg after first loose stool, followed by 2 mg after each subsequent stool (maximum dose: 8 mg/day)

Pepto-bismol® (bismuth subsalicylate)

DOSING: ADULTS
Treatment of nonspecific diarrhea, control/relieve traveler's diarrhea: Oral: Subsalicylate (doses based on 262 mg/15 mL liquid or 262 mg tablets): 2 tablets or 30 mL every 30 minutes to 1 hour as needed up to 8 doses/24 hours.

Helicobacter pylori eradication: Oral: 524 mg 4 times/day with meals and at bedtime; requires combination therapy.

Control of fecal odor in ileostomy or colostomy: Oral: Subgallate: 200-400 mg up to 4 times/day.

Telotristat ethyl - xermelo ™

Drug UPDATES: XERMELO ™ (telotristat ethyl) tablets
[Drug information / PDF] REVIEW PACKAGE INSERT FOR POSSIBLE UPDATES
PACKAGE INSERT -Dosing: Click (+) next to Dosage and Administration section (drug info link)

Initial U.S. Approval: 2017

Mechanism of Action:
Telotristat, the active metabolite of telotristat ethyl, is an inhibitor of tryptophan hydroxylase, which mediates the rate limiting step in serotonin biosynthesis. The in vitro inhibitory potency of telotristat towards tryptophan hydroxylase is 29 times higher than that of telotristat ethyl. Serotonin plays a role in mediating secretion, motility, inflammation, and sensation of the gastrointestinal tract, and is over-produced in patients with carcinoid syndrome. Through inhibition of tryptophan hydroxylase, telotristat and telotristat ethyl reduce the production of peripheral serotonin, and the frequency of carcinoid syndrome diarrhea.

INDICATIONS AND USAGE:
Xermelo is a tryptophan hydroxylase inhibitor indicated for the treatment of carcinoid syndrome diarrhea in combination with somatostatin analog (SSA) therapy in adults inadequately controlled by SSA therapy.

DOSAGE AND ADMINISTRATION: PDF
The recommended dosage of Xermelo in adult patients is 250 mg three times daily for patients whose diarrhea is inadequately controlled by SSA therapy.

Administration
Take Xermelo with food.
When short-acting octreotide is used in combination with Xermelo, administer short-acting octreotide at least 30 minutes after administering Xermelo [see Clinical Pharmacology (12.3), Clinical Studies (14)].
If a dose is missed, take the next dose at the regular time. Do not take 2 doses at the same time to make up for a missed dose.
Discontinue Xermelo if severe constipation develops

HOW SUPPLIED:
Tablets: 250 mg telotristat ethyl

Reference(s)

National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates. A local search option of this data can be found here.