ALOSETRON HYDROCHLORIDE

×

Overview

What is ALOSETRON HYDROCHLORIDE?

The active ingredient in alosetron hydrochloride tablets is alosetron hydrochloride (HCl), a potent and selective antagonist of the serotonin 5-HT receptor type. Chemically, alosetron is designated as 2,3,4,5-tetrahydro-5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-1H-pyrido[4,3-b]indol-1-one, monohydrochloride. Alosetron is achiral and has the empirical formula CHNO•HCl, representing a molecular weight of 330.8.

Alosetron is a white to beige powder that has a solubility of 61 mg/mL in water, 42 mg/mL in 0.1M hydrochloric acid, 0.3 mg/mL in pH 6 phosphate buffer, and <0.1 mg/mL in pH 8 phosphate buffer. The chemical structure of alosetron is:

Alosetron hydrochloride tablets are supplied for oral administration as 0.5 mg (white) and 1 mg (blue) tablets. The 0.5 mg tablet contains 0.562 mg alosetron HCl equivalent to 0.5 mg alosetron, and the 1 mg tablet contains 1.124 mg alosetron HCl equivalent to 1 mg of alosetron. Each tablet also contains the inactive ingredients lactose anhydrous, magnesium stearate, microcrystalline cellulose, and pregelatinized starch. The white film-coat for the 0.5 mg tablet contains hypromellose, titanium dioxide, and triacetin. The blue film coat for the 1 mg tablet contains hypromellose, titanium dioxide, triacetin, and Fd&C Blue #2/indigo carmine aluminium lake.

What does ALOSETRON HYDROCHLORIDE look like?

What are the available doses of ALOSETRON HYDROCHLORIDE?

Tablets: 0.5 and 1 mg (3)

What should I talk to my health care provider before I take ALOSETRON HYDROCHLORIDE?

How should I use ALOSETRON HYDROCHLORIDE?

Alosetron hydrochloride tablets are indicated only for women with severe diarrhea-predominant irritable bowel syndrome (IBS) who have:

Diarrhea-predominant IBS is severe if it includes diarrhea and one or more of the following:

Because of infrequent but serious gastrointestinal adverse reactions associated with alosetron hydrochloride tablets, the indication is restricted to those patients for whom the benefit-to-risk balance is most favorable.

Clinical studies have not been performed to adequately confirm the benefits of alosetron hydrochloride tablets in men.

To lower the risk of constipation, alosetron hydrochloride tablets should be started at a dosage of 0.5 mg twice a day. Patients who become constipated at this dosage should stop taking alosetron hydrochloride tablets until the constipation resolves. They may be restarted at 0.5 mg once a day. If constipation recurs at the lower dose, alosetron hydrochloride tablets should be discontinued immediately.

Patients well controlled on 0.5 mg once or twice a day may be maintained on this regimen. If after 4 weeks the dosage is well tolerated but does not adequately control IBS symptoms, then the dosage can be increased to up to 1 mg twice a dayAlosetron hydrochloride tabletsshould be discontinued in patients who have not had adequate control of IBS symptoms after 4 weeks of treatment with 1 mg twice a day.

Alosetron hydrochloride tablets can be taken with or without food see ].

Alosetron hydrochloride tablets should be discontinued immediately in patients who develop constipation or signs of ischemic colitis. Alosetron hydrochloride tablets should not be restarted in patients who develop ischemic colitis.

Clinical trial and postmarketing experience suggest that debilitated patients or patients taking additional medications that decrease gastrointestinal motility may be at greater risk of serious complications of constipation. Therefore, appropriate caution and follow-up should be exercised if alosetron hydrochloride tablets are prescribed for these patients.

Postmarketing experience suggests that elderly patients may be at greater risk for complications of constipation; therefore, appropriate caution and follow-up should be exercised if alosetron hydrochloride tablets are prescribed for these patients .

What interacts with ALOSETRON HYDROCHLORIDE?

Sorry No Records found

What are the warnings of ALOSETRON HYDROCHLORIDE?

Sorry No Records found

What are the precautions of ALOSETRON HYDROCHLORIDE?

Sorry No Records found

What are the side effects of ALOSETRON HYDROCHLORIDE?

Sorry No records found

What should I look out for while using ALOSETRON HYDROCHLORIDE?

Do not initiate in patients with constipation (4.1)

History of chronic or severe constipation or sequelae from constipation; intestinal obstruction, stricture, toxic megacolon, gastrointestinal perforation, and/or adhesions; ischemic colitis; impaired intestinal circulation, thrombophlebitis, or hypercoagulable state; Crohn’s disease or ulcerative colitis; diverticulitis; severe hepatic impairment (4.2)

Concomitant use of fluvoxamine (4.3)

W

A

RNING: SERIOUS GASTROINTESTINAL ADVERSE REACTIONS

Infrequent but serious gastrointestinal adverse reactions have been reported with the use of

alosetron hydrochloride. These events, including ischemic colitis and serious complications of constipation, have resulted in hospitalization, and rarely, blood transfusion, surgery, and death.

What might happen if I take too much ALOSETRON HYDROCHLORIDE?

There is no specific antidote for overdose of alosetron hydrochloride. Patients should be managed with appropriate supportive therapy. Individual oral doses as large as 16 mg have been administered in clinical studies without significant adverse reactions. This dose is 8 times higher than the recommended total daily dose. Inhibition of the metabolic elimination and reduced first pass of other drugs might occur with overdoses of alosetron hydrochloride

How should I store and handle ALOSETRON HYDROCHLORIDE?

Store at controlled room temperature 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [See USP Controlled Room Temperature]. Keep bottle tightly closed and protect from moisture.Alosetron hydrochloride tablets, 0.5 mg (0.562 mg alosetron HCl equivalent to 0.5 mg alosetron) are white, oval, film-coated tablets debossed with “P” on one side and 819 on the other side.Bottles of 30 (NDC 49884-819-11) with child-resistant closures.Alosetron hydrochloride tablets, 1 mg (1.124 mg alosetron HCl equivalent to 1 mg alosetron), are blue, oval, film-coated tablets debossed with “P” on one side and 820 on the other side.Bottles of 30 (NDC 49884-820-11) with child-resistant closures.Store at 20˚ to 25˚C (68˚ to 77˚F) (USP Controlled Room Temperature). Protect from light and moisture.Alosetron hydrochloride tablets, 0.5 mg (0.562 mg alosetron HCl equivalent to 0.5 mg alosetron) are white, oval, film-coated tablets debossed with “P” on one side and 819 on the other side.Bottles of 30 (NDC 49884-819-11) with child-resistant closures.Alosetron hydrochloride tablets, 1 mg (1.124 mg alosetron HCl equivalent to 1 mg alosetron), are blue, oval, film-coated tablets debossed with “P” on one side and 820 on the other side.Bottles of 30 (NDC 49884-820-11) with child-resistant closures.Store at 20˚ to 25˚C (68˚ to 77˚F) (USP Controlled Room Temperature). Protect from light and moisture.Alosetron hydrochloride tablets, 0.5 mg (0.562 mg alosetron HCl equivalent to 0.5 mg alosetron) are white, oval, film-coated tablets debossed with “P” on one side and 819 on the other side.Bottles of 30 (NDC 49884-819-11) with child-resistant closures.Alosetron hydrochloride tablets, 1 mg (1.124 mg alosetron HCl equivalent to 1 mg alosetron), are blue, oval, film-coated tablets debossed with “P” on one side and 820 on the other side.Bottles of 30 (NDC 49884-820-11) with child-resistant closures.Store at 20˚ to 25˚C (68˚ to 77˚F) (USP Controlled Room Temperature). Protect from light and moisture.Alosetron hydrochloride tablets, 0.5 mg (0.562 mg alosetron HCl equivalent to 0.5 mg alosetron) are white, oval, film-coated tablets debossed with “P” on one side and 819 on the other side.Bottles of 30 (NDC 49884-819-11) with child-resistant closures.Alosetron hydrochloride tablets, 1 mg (1.124 mg alosetron HCl equivalent to 1 mg alosetron), are blue, oval, film-coated tablets debossed with “P” on one side and 820 on the other side.Bottles of 30 (NDC 49884-820-11) with child-resistant closures.Store at 20˚ to 25˚C (68˚ to 77˚F) (USP Controlled Room Temperature). Protect from light and moisture.Alosetron hydrochloride tablets, 0.5 mg (0.562 mg alosetron HCl equivalent to 0.5 mg alosetron) are white, oval, film-coated tablets debossed with “P” on one side and 819 on the other side.Bottles of 30 (NDC 49884-819-11) with child-resistant closures.Alosetron hydrochloride tablets, 1 mg (1.124 mg alosetron HCl equivalent to 1 mg alosetron), are blue, oval, film-coated tablets debossed with “P” on one side and 820 on the other side.Bottles of 30 (NDC 49884-820-11) with child-resistant closures.Store at 20˚ to 25˚C (68˚ to 77˚F) (USP Controlled Room Temperature). Protect from light and moisture.

×

Clinical Information

Chemical Structure

No Image found

Clinical Pharmacology

Alosetron is a potent and selective 5-HT receptor antagonist. 5-HT receptors are ligand-gated cation channels that are extensively distributed on enteric neurons in the human gastrointestinal tract, as well as other peripheral and central locations. Activation of these channels and the resulting neuronal depolarization affect the regulation of visceral pain, colonic transit, and gastrointestinal secretions, processes that relate to the pathophysiology of IBS. 5- HT receptor antagonists such as alosetron inhibit activation of non-selective cation channels, which results in the modulation of the enteric nervous system.

The cause of IBS is unknown. IBS is characterized by visceral hypersensitivity and hyperactivity of the gastrointestinal tract, which lead to abnormal sensations of pain and motor activity. Following distention of the rectum, patients with IBS exhibit pain and discomfort at lower volumes than healthy volunteers. Following such distention, alosetron reduced pain and exaggerated motor responses, possibly due to blockade of 5- HT receptors.

Non-Clinical Toxicology

Do not initiate in patients with constipation (4.1)

History of chronic or severe constipation or sequelae from constipation; intestinal obstruction, stricture, toxic megacolon, gastrointestinal perforation, and/or adhesions; ischemic colitis; impaired intestinal circulation, thrombophlebitis, or hypercoagulable state; Crohn’s disease or ulcerative colitis; diverticulitis; severe hepatic impairment (4.2)

Concomitant use of fluvoxamine (4.3)

W

A

RNING: SERIOUS GASTROINTESTINAL ADVERSE REACTIONS

Infrequent but serious gastrointestinal adverse reactions have been reported with the use of

alosetron hydrochloride. These events, including ischemic colitis and serious complications of constipation, have resulted in hospitalization, and rarely, blood transfusion, surgery, and death.

ACE-inhibitors

Reports suggest that NSAIDs may diminish the antihypertensive effect of ACE-inhibitors. This interaction should be given consideration in patients taking NSAIDs concomitantly with ACE-inhibitors.

Aspirin

When ibuprofen tablets are administered with aspirin, its protein binding is reduced, although the clearance of free ibuprofen tablets is not altered. The clinical significance of this interaction is not known; however, as with other NSAIDs, concomitant administration of ibuprofen and aspirin is not generally recommended because of the potential for increased adverse effects.

Diuretics

Clinical studies, as well as post marketing observations, have shown that ibuprofen tablets can reduce the natriuretic effect-of furosemide and thiazides in some patients. This response has been attributed to inhibition of renal prostaglandin synthesis. During concomitant therapy with NSAIDs, the patient should be observed closely for signs of renal failure (see , ), as well as to assure diuretic efficacy.

Lithium

Ibuprofen produced an elevation of plasma lithium levels and a reduction in renal lithium clearance in a study of eleven normal volunteers. The mean minimum lithium concentration increased 15% and the renal clearance of lithium was decreased by 19% during this period of concomitant drug administration. This effect has been attributed to inhibition of renal prostaglandin synthesis by ibuprofen. Thus, when ibuprofen and lithium are administered concurrently, subjects should be observed carefully for signs of lithium toxicity. (Read circulars for lithium preparation before use of such concurrent therapy).

Methotrexate

NSAIDs have been reported to competitively inhibit methotrexate accumulation in rabbit kidney slices. This may indicate that they could enhance the toxicity of methotrexate. Caution should be used when NSAIDs are administered concomitantly with methotrexate.

Warfarin-type anticoagulants

Several short-term controlled studies failed to show that ibuprofen tablets significantly affected prothrombin times or a variety of other clotting factors when administered to individuals on coumarin-type anticoagulants. However, because bleeding has been reported when ibuprofen tablets and other NSAIDs have been administered to patients on coumarin-type anticoagulants, the physician should be cautious when administering ibuprofen tablets to patients on anticoagulants. The effects of warfarin and NSAIDs on GI bleeding are synergistic, such that the users of both drugs together have a risk of serious GI bleeding higher than users of either drug alone.

H-2 Antagonists

In studies with human volunteers, co-administration of cimetidine or ranitidine with ibuprofen had no substantive effect on ibuprofen serum concentrations.

S

ome patients have experienced serious complications of constipation without warning

Serious complications of constipation, including obstruction, ileus, impaction, toxic megacolon, and secondary bowel ischemia, have been reported with use of alosetron hydrochloride during clinical trials. Complications of constipation have been reported with use of 1 mg twice daily and with lower doses. A dose response relationship has not been established for serious complications of constipation. The incidence of serious complications of constipation was approximately 0.1% (1 per 1,000 patients) in women receiving either alosetron hydrochloride tabletsor placebo.In addition, rare cases of perforation and death have been reported from postmarketing clinical practice. In some cases, complications of constipation required intestinal surgery, including colectomy. Patients who are elderly, debilitated, or taking additional medications that decrease gastrointestinal motility may be at greater risk for complications of constipation.

Alosetron hydrochloride should be discontinued immediately in patients who develop constipation

The following adverse reactions are described in more detail in other sections of the label:

×

Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

×

Review

×

Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72

×

Tips

×

Interactions

A total of 440 drugs (1549 brand and generic names) are known to interact with Imbruvica (ibrutinib). 228 major drug interactions (854 brand and generic names) 210 moderate drug interactions (691 brand and generic names) 2 minor drug interactions (4 brand and generic names) Show all medications in the database that may interact with Imbruvica (ibrutinib).

Disclaimer: