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Carboprost tromethamine | CAS No: 58551-69-2 | GMP-certified suppliers
A medication that induces uterine contractions for second-trimester pregnancy termination and manages postpartum hemorrhage unresponsive to conventional treatments.
Therapeutic categories
Primary indications
- For aborting pregnancy between the 13th and 20th weeks of gestation as calculated from the first day of the last normal menstrual period and in the following conditions related to second trimester abortion: 1
- Failure of expulsion of the fetus during the course of treatment by another method
- 2
- Premature rupture of membranes in intrauterine methods with loss of drug and insufficient or absent uterine activity
Product Snapshot
- Carboprost tromethamine is an injectable solution formulated for intramuscular administration
- It is primarily indicated for second trimester pregnancy termination and management of postpartum hemorrhage due to uterine atony
- The product is approved for use in the US and Canadian markets
Clinical Overview
Pharmacodynamically, carboprost stimulates myometrial contractions resembling labor contractions at term, facilitating evacuation of uterine contents. This agent also contracts smooth muscle in the gastrointestinal tract, potentially causing adverse effects such as vomiting and diarrhea. Transient increases in body temperature have been observed clinically at therapeutic doses, while marked elevations in blood pressure and bronchoconstriction can occur at higher doses or in some patients.
The mechanism of action involves binding to prostaglandin E2 receptors in uterine tissue, prompting muscle contractions that induce labor or placental expulsion. Endogenous prostaglandins share this role in modulating uterine contractility and smooth muscle activity. Carboprost belongs to several pharmacological categories including nonsteroidal abortifacients, prostaglandins F, eicosanoids, and reproductive control agents.
Key ADME parameters for carboprost tromethamine include intramuscular administration with rapid onset of uterine contractions. Metabolism primarily occurs via enzymatic degradation in vivo; detailed pharmacokinetic data are limited. Safety considerations relate to contraindications in patients with active cardiovascular, pulmonary, or hepatic disease, due to possible bronchospasm and blood pressure effects. Monitoring for gastrointestinal disturbances and temperature changes is advisable during treatment.
Carboprost tromethamine is marketed under various brand names globally and is regulated as a prescription drug with strict clinical oversight. For API procurement, adherence to pharmacopeial standards and regulatory compliance is essential. Quality attributes such as purity, isomeric composition, and absence of contaminants must be rigorously controlled to ensure safety and efficacy in clinical use. Validation of manufacturing processes and supplier audits remain critical components of sourcing strategy.
Identification & chemistry
| Generic name | Carboprost tromethamine |
|---|---|
| Molecule type | Small molecule |
| CAS | 58551-69-2 |
| UNII | U4526F86FJ |
| DrugBank ID | DB00429 |
Pharmacology
| Summary | Carboprost is a synthetic prostaglandin analog that primarily targets the prostaglandin E2 receptor EP1 subtype to induce myometrial contractions. It facilitates uterine evacuation during second-trimester abortion and promotes hemostasis postpartum by enhancing uterine muscle tone. Additionally, carboprost influences smooth muscle activity in the gastrointestinal and vascular systems, contributing to its pharmacodynamic profile. |
|---|---|
| Mechanism of action | Carboprost is a synthetic prostaglandin. It binds the prostaglandin E2 receptor, causing myometrial contractions, casuing the induction of labour or the expulsion of the placenta. Prostaglandins occur naturally in the body and act at several sites in the body including the womb (uterus). They act on the muscles of the womb, causing them to contract. |
| Pharmacodynamics | Carboprost tromethamine administered intramuscularly stimulates in the gravid uterus myometrial contractions similar to labor contractions at the end of a full term pregnancy. Whether or not these contractions result from a direct effect of carboprost on the myome-trium has not been determined. Nonetheless, they evacuate the products of conception from the uterus in most cases. Postpartum, the resultant myometrial contractions provide hemostasis at the site of placentation. Carboprost tromethamine also stimulates the smooth muscle of the human gastrointestinal tract. This activity may produce the vomiting or diarrhea or both that is common when carbo-prost tromethamine is used to terminate pregnancy and for use postpartum. In laboratory animals and also in humans carboprost tromethamine can elevate body temperature. With the clinical doses of carboprost trometh-amine used for the termination of pregnancy, and for use postpartum, some patients do experience transient temperature increases. In laboratory animals and in humans large doses of carboprost tromethamine can raise blood pressure, probably by contracting the vascular smooth muscle. With the doses of carboprost tromethamine used for terminating pregnancy, this effect has not been clinically significant. In laboratory animals and also in humans carboprost tromethamine can elevate body temperature. With the clinical doses of carboprost tromethamine used for the termination of pregnancy, some patients do experience temperature increases. In some patients, carboprost tromethamine may cause transient bronchoconstriction. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Prostaglandin E2 receptor EP1 subtype | Humans | agonist |
ADME / PK
| Metabolism | Metabolized in the lungs and liver. Metabolites are excreted in urine. |
|---|
Formulation & handling
- Carboprost tromethamine is formulated for intramuscular injection due to its low oral bioavailability.
- It is a small molecule with moderate lipophilicity (LogP 2.89) and low water solubility, requiring appropriate solubilization methods for injection.
- Handling should consider its stability in aqueous solution and protection from light and extreme temperatures to maintain potency.
Regulatory status
| Lifecycle | The API's primary patents have expired in the US and Canada, allowing for generic entry and increased market competition. As a result, the market in these regions is considered mature with multiple approved products. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Carboprost tromethamine is originally manufactured and packaged by two companies, Pharmacia and Upjohn Co. and Hospira Inc., primarily serving the US and Canadian markets. The branded product presence is focused in North America, with multiple brand samples noted. Patent expiration status suggests that generic competition may exist or emerge, given the availability of multiple manufacturers and packaging sources. |
|---|
Safety
| Toxicity | Symptoms of overdose include irritation, nausea, vomiting, diarrhea, coughing, dyspnea, asthma, hypertension, flushing, and pyrexia. |
|---|
- Handle with care to avoid inhalation or ingestion
- Exposure may cause respiratory irritation, coughing, and dyspnea
- Potential systemic effects from overdose include gastrointestinal symptoms, hypertension, and pyrexia
Carboprost Tromethamine is a type of Prostaglandin Analogues
Prostaglandin analogues are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the field of medicine. These synthetic compounds mimic the effects of natural prostaglandins, which are hormone-like substances found in the body.
Prostaglandin analogues have gained significant attention in medical research due to their diverse therapeutic applications. They exhibit a wide range of physiological activities, such as regulating inflammation, blood flow, and hormone levels. These compounds are commonly used in the treatment of various conditions, including glaucoma, ocular hypertension, and certain types of cancer.
One notable application of prostaglandin analogues is in ophthalmology. These compounds effectively reduce intraocular pressure by increasing the outflow of aqueous humor, providing an effective treatment for glaucoma patients. Moreover, prostaglandin analogues offer the advantage of once-daily dosing, enhancing patient compliance and convenience.
In the field of oncology, prostaglandin analogues have shown promise as anticancer agents. They exert anti-proliferative effects on cancer cells and can induce apoptosis, making them valuable in the treatment of certain malignancies.
Overall, prostaglandin analogues represent a significant class of pharmaceutical APIs with diverse therapeutic applications. Continued research and development in this area hold great potential for the advancement of medicine and the improvement of patient care.
Carboprost Tromethamine (Prostaglandin Analogues), classified under Anti-inflammatory Agents
Anti-inflammatory agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat various inflammatory conditions. These agents play a vital role in alleviating pain, reducing swelling, and controlling inflammation in the body. They are widely employed in the management of diverse medical conditions, including arthritis, autoimmune disorders, asthma, and skin conditions like dermatitis.
Anti-inflammatory APIs primarily function by inhibiting the production of specific enzymes called cyclooxygenases (COX) and lipoxygenases (LOX). These enzymes are responsible for the synthesis of pro-inflammatory molecules known as prostaglandins and leukotrienes, respectively. By suppressing the activity of COX and LOX, anti-inflammatory agents effectively curtail the production of these inflammatory mediators, thereby mitigating inflammation.
Common examples of anti-inflammatory APIs include non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen, aspirin, and naproxen. These agents exhibit analgesic, antipyretic, and anti-inflammatory properties. Another group of anti-inflammatory APIs includes corticosteroids, such as prednisone and dexamethasone, which are synthetic hormones that modulate the body's immune response to control inflammation.
In conclusion, anti-inflammatory agents are a vital category of pharmaceutical APIs widely used to manage inflammation-related disorders. They target enzymes involved in the synthesis of pro-inflammatory molecules, effectively reducing pain and swelling. NSAIDs and corticosteroids are commonly prescribed anti-inflammatory APIs due to their efficacy in controlling inflammation.
Carboprost Tromethamine API manufacturers & distributors
Compare qualified Carboprost Tromethamine API suppliers worldwide. We currently have 6 companies offering Carboprost Tromethamine API, with manufacturing taking place in 5 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, GMP, MSDS, USDMF | 229 products |
| Aquatic Remedies Pvt Ltd | Producer | India | India | CoA | 35 products |
| Chinoin | Producer | Hungary | Hungary | CoA, GMP | 21 products |
| Chirogate International | Producer | Taiwan | Taiwan | CoA, FDA, GMP, USDMF | 17 products |
| Mahalaxmi Chemi Pharm | Producer | India | India | CoA | 13 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CoA, GMP, ISO9001, MSDS | 144 products |
When sending a request, specify which Carboprost Tromethamine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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