Bromocriptine Mesylate Tablets Information Research Report

1. Basic Information

2. Domestic Market Status

2.1 Original Research Manufacturer Domestic Registration Status

2.2 Generic Drug Approval

2.3 Consistency Evaluation Application and Approval Status

2.4 Generic Drug Application Status

2.5 Clinical Filing Status

3. Reference Drug

4. Reference Drug Patent Information

5. Active Pharmaceutical Ingredient (API) Research

5.1 API Pharmacopoeia Information

5.2 API Filing Information

6. Formulation Research

6.1 Target Product Quality Overview

6.2 Formulation Pharmacopoeia Information

1. Basic Information

Opioid analgesics are commonly used for moderate to severe pain associated with various diseases but are accompanied by a range of debilitating side effects, including constipation, abdominal pain, discomfort, bloating, nausea, vomiting, urinary retention, and itching. Among these patients, approximately 40-70% experience chronic constipation.

Opioid drugs can maintain or increase the tone of intestinal smooth muscles, inhibit forward peristalsis, increase the tone of the ileocecal valve and anal sphincter, and decrease sensitivity to rectal distension, thereby causing constipation. Additionally, secretion and blood flow can also be adversely affected.

In palliative care for patients with life-threatening conditions, opioid-induced constipation may be altered and aggravated by factors related to underlying malignancies or other comorbidities, such as metabolic changes (e.g., diabetes, hypercalcemia, hypokalemia, uremia, hypothyroidism), dehydration, advanced age, reduced physical activity or immobility, low fluid and/or dietary fiber intake, mechanical obstruction, neurological diseases, and concomitant drugs like antiemetics, diuretics, anticonvulsants, and vinca alkaloids. Moreover, unlike other side effects of opioids, patients rarely develop tolerance to the constipating effects of opioid substances.

Bromocriptine Mesylate is a selective antagonist that interacts with opioid drugs at the μ-opioid receptor. As a quaternary ammonium salt, bromocriptine mesylate has limited ability to cross the blood-brain barrier. This allows bromocriptine mesylate to act as a μ-opioid receptor antagonist in peripheral tissues, such as the gastrointestinal tract, reducing opioid-induced constipation without affecting the analgesic effects mediated by opioids in the central nervous system.

In 2008, bromocriptine mesylate injection was approved for use in the United States, and in 2016, bromocriptine mesylate tablets (brand name: RELISTOR) were also approved. RELISTOR tablets have been listed by the National Medical Products Administration as a reference drug for generic formulation, with basic information provided in Table 1-1.

Table 1-1 Basic Information

2. Domestic Market Status

2.1 Original Manufacturer Domestic Registration Status

As of March 1st, the original formulation has not been imported into China.

2.2 Generic Drug Approval

As of March 1st, no companies have received approval for the generic version of this product.

2.3 Consistency Evaluation Application and Approval Status

As of March 1st, no companies have received approval for the generic version of this product.

2.4 Generic Drug Application Status

As of March 1st, only one company has submitted a clinical application for the generic version of this product, as detailed in Table 2-1.

Table 2-1 Generic Drug Application Status

2.5 Clinical Filing Status

As of March 1st, there is no clinical filing information for this product.

3. Reference Drug

Table 3-1 National Medical Products Administration Published Reference Drug Information

4. Reference Drug Patent Information

Table 4-1 Reference Drug Patent Information

 5. Active Pharmaceutical Ingredient (API) Research

5.1 API Pharmacopoeia Information

Search results show that the USP has included the quality standards for the active pharmaceutical ingredient of this product.

5.2 API Filing Information

As of March 1st, there is no filing information for the active pharmaceutical ingredient of this product.

6. Formulation Research

6.1 Target Product Quality Overview

Table 6-1 Target Product Quality Overview

6.2 Formulation Pharmacopoeia Information

Upon searching ChP, USP, EP, and JP, no quality standards for this product’s formulation have been included in these pharmacopoeias.