LOTRONEX Tablet (2019)

Βιβλιογραφική αναφορά

Συγγραφείς

Sebela Pharmaceuticals Inc.

Λέξεις κλειδιά

54766-895 54766-894

Για την προβολή της πλήρους καταχώρησης απαιτείται συνδρομή σε ισχύ.
Αποκτήστε πρόσβαση σε όλες τις πληροφορίες και τα εργαλεία του Galinos.gr δωρεάν για έναν μήνα απλά κάνοντας εγγραφή.
Δωρεάν εγγραφή

WARNING: SERIOUS GASTROINTESTINAL ADVERSE REACTIONS

Infrequent but serious gastrointestinal adverse reactions have been reported with the use of LOTRONEX. These events, including ischemic colitis and serious complications of constipation, have resulted ...

1. Indications and Usage

LOTRONEX is indicated only for women with severe diarrhea-predominant irritable bowel syndrome (IBS) who have: chronic IBS symptoms (generally lasting 6 months or longer), had anatomic or biochemical abnormalities ...

2. Dosage and Administration

2.1 Adult Patients To lower the risk of constipation, LOTRONEX should be started at a dosage of 0.5 mg twice a day. Patients who become constipated at this dosage should stop taking LOTRONEX until the ...

3. Dosage Forms and Strengths

0.5 mg and 1 mg tablets. LOTRONEX Tablets, 0.5 mg (0.562 mg alosetron HCl equivalent to 0.5 mg alosetron), are white, oval, film-coated tablets debossed with GX EX1 on one face. LOTRONEX Tablets, 1 mg ...

4. Contraindications

4.1 Constipation LOTRONEX should not be initiated in patients with constipation [see Warnings and Precautions (5.1)]. 4.2 History of Severe Bowel or Hepatic Disorders LOTRONEX is contraindicated ...

5. Warnings and Precautions

5.1 Serious Complications of Constipation Some patients have experienced serious complications of constipation without warning. Serious complications of constipation, including obstruction, ileus, ...

6. Adverse Reactions

The following adverse reactions are described in more detail in other sections of the label: Complications of constipation [see Boxed Warning, Warnings and Precautions (5.1)]. Ischemic colitis ...

6.1. Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another ...

6.2. Postmarketing Experience

In addition to events reported in clinical trials, the following events have been identified during use of LOTRONEX in clinical practice. Because they were reported voluntarily from a population of unknown ...

7. Drug Interactions

In vivo data suggest that alosetron is primarily metabolized by cytochrome P450 (CYP) 1A2, with minor contributions from CYP3A4 and CYP2C9. Therefore, inducers or inhibitors of these enzymes may ...

8.1. Pregnancy

Risk Summary The available data with LOTRONEX use in pregnant women are insufficient to draw conclusions about any drug-associated risks for major birth defects, miscarriage, or adverse maternal or fetal ...

8.2. Lactation

Alosetron and/or metabolites of alosetron are excreted in the breast milk of lactating rats. It is not known whether alosetron is excreted in human milk. Because many drugs are excreted in human milk, ...

8.4. Pediatric Use

Safety and effectiveness in pediatric patients have not been established. Use of LOTRONEX is not recommended in the pediatric population, based upon the risk of serious complications of constipation and ...

8.5. Geriatric Use

In some studies in healthy men or women, plasma concentrations were elevated by approximately 40% in individuals 65 years and older compared to young adults [see Warnings and Precautions (5.1)] ...

8.6. Hepatic Impairment

Due to the extensive hepatic metabolism of alosetron, increased exposure to alosetron and/or its metabolites is likely to occur in patients with hepatic impairment. Alosetron should not be used in patients ...

8.7. Renal Impairment

Renal impairment (creatinine clearance 4 to 56 mL/min) has no effect on the renal elimination of alosetron due to the minor contribution of this pathway to elimination. The effect of renal impairment on ...

10. Overdosage

There is no specific antidote for overdose of LOTRONEX. Patients should be managed with appropriate supportive therapy. Individual oral doses as large as 16 mg have been administered in clinical studies ...

11. Description

The active ingredient in LOTRONEX Tablets is alosetron hydrochloride (HCl), a potent and selective antagonist of the serotonin 5-HT 3 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, ...

12.1. Mechanism of Action

Alosetron is a potent and selective 5-HT3 receptor antagonist. 5-HT3 receptors are ligand-gated cation channels that are extensively distributed on enteric neurons in the human gastrointestinal ...

12.2. Pharmacodynamics

In healthy volunteers and patients with IBS, alosetron (2 mg orally, twice daily for 8 days) increased colonic transit time without affecting orocecal transit time. In healthy volunteers, alosetron also ...

12.3. Pharmacokinetics

The pharmacokinetics of alosetron have been studied after single oral doses ranging from 0.05 to 16 mg in healthy men. The pharmacokinetics of alosetron have also been evaluated in healthy women and men ...

13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility

In 2-year oral studies, alosetron was not carcinogenic in mice at doses up to 30 mg/kg/day or in rats at doses up to 40 mg/kg/day. These doses are about 60 to 160 times, respectively, the recommended human ...

14. Clinical Studies

14.1 Dose-Ranging Study Data from a dose-ranging study of women (n = 85) who received LOTRONEX 0.5 mg twice daily indicated that the incidence of constipation (14%) was lower than that experienced by women ...

15. References

1. Thompson WG, Creed F, Drossman DA, et al. Functional bowel disease and functional abdominal pain Gastroenterol Int. 1992;5:75-91.

16.1. How Supplied

LOTRONEX Tablets, 0.5 mg (0.562 mg alosetron HCl equivalent to 0.5 mg alosetron) are white, oval, film-coated tablets debossed with GX EX1 on one face. Bottles of 30 (NDC 65483-894-03) with child-resistant ...

16.2. Storage and Handling

Store at 20-25°C (68-77°F) (USP Controlled Room Temperature). Protect from light and moisture.

17. Patient Counseling Information

Advise the patient to read the FDA-approved labeling (Medication Guide). Prescriber and Patient Responsibilities Patients should be fully counseled on and understand the risks and benefits of ...