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Chlorobutanol
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Looking for Chlorobutanol API 57-15-8?
- Description:
- Here you will find a list of producers, manufacturers and distributors of Chlorobutanol. You can filter on certificates such as GMP, FDA, CEP, Written Confirmation and more. Send inquiries for free and get in direct contact with the supplier of your choice.
- API | Excipient name:
- Chlorobutanol
- Synonyms:
- Chloretone , Chlorobutanol
- Cas Number:
- 57-15-8
- DrugBank number:
- DB11386
- Unique Ingredient Identifier:
- HM4YQM8WRC
General Description:
Chlorobutanol, identified by CAS number 57-15-8, is a notable compound with significant therapeutic applications. Chlorobutanol, or chlorbutol, is an alcohol-based preservative with no surfactant activity . It also elicits sedative-hypnotic and weak local anesthetic actions in addition to antibacterial and antifungal properties. Similar in nature to chloral hydrate, it is formed by the simple nucleophilic addition of chloroform and acetone. As a long-term stabilizer of multi-ingredient preparations, chlorobutanol is normally used at a concentration of 0.5%. At this concentration, it also conserves its antimicrobial activity. Due to the long terminal half-life of 37 days, the use of chlorobutanol as a sedative is limited because of the considerable accumulation which will occur following multiple dosing . Chlorobutanol is a common detergent preservative in eye drops and other ophthalmic therapeutic formulations .
Indications:
This drug is primarily indicated for: No approved therapeutic indications on its own. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.
Metabolism:
Chlorobutanol undergoes metabolic processing primarily in: Chlorobutanol is reported to undergo glucuronidation and sulphation . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.
Absorption:
The absorption characteristics of Chlorobutanol are crucial for its therapeutic efficacy: Following oral administration in healthy subjects, the plasma concentration fell by 50% in 24 hours post-administration . The drug's ability to rapidly penetrate into cells ensures quick onset of action.
Half-life:
The half-life of Chlorobutanol is an important consideration for its dosing schedule: Following oral administration, the terminal elimination half life in healthy subjects was 10.3 ± 1.3 days . This determines the duration of action and helps in formulating effective dosing regimens.
Protein Binding:
Chlorobutanol exhibits a strong affinity for binding with plasma proteins: The binding to plasma proteins was 57 ± 3% . This property plays a key role in the drug's pharmacokinetics and distribution within the body.
Route of Elimination:
The elimination of Chlorobutanol from the body primarily occurs through: Under physiological conditions, chlorobutanol is unstable. The mean urinary recovery accounts for 9.6% of the dose orally administered . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.
Volume of Distribution:
Chlorobutanol is distributed throughout the body with a volume of distribution of: The volume of distribution was approximately 233 ± 141 L in healthy individuals receiving oral chlorobutanol . This metric indicates how extensively the drug permeates into body tissues.
Clearance:
The clearance rate of Chlorobutanol is a critical factor in determining its safe and effective dosage: In healthy subjects, the clearance was approximately 11.6 ± 1.0 mL/min following oral administration . It reflects the efficiency with which the drug is removed from the systemic circulation.
Pharmacodynamics:
Chlorobutanol exerts its therapeutic effects through: Chlorobutanol is a detergent preservative with a broad spectrum of antimicrobial activity . _In vitro_, chlorobutanol demonstrated to inhibit platelet aggregation and release via unknown mechanisms . A study proposes that the antiplatelet effect of chlorobutanol may occur from inhibition of the arachidonic acid pathway . It attenuated thromboxane B2 formation, elevation of cytosolic free calcium, and ATP release, and additionally exhibited a significant inhibitory activity toward several aggregation inducers in a time- and concentration-dependent manner . Chlorobutanol may exert a direct negative inotropic effect on myocardial cells to isometric tension produced by the heart . Chlorobutanol was shown to induce conjunctival and corneal cell toxicity _in vitro_: at a concentration of 0.1%, Cbl caused near depletion of the squamous layer while degeneration of corneal epithelial cells, generation of conspicuous membranous blebs, cytoplasmic swelling, and occasional breaks in the external cell membrane were observed at a concentration of 0.5% . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.
Mechanism of Action:
Chlorobutanol functions by: As a detergent, chlorobutanol disrupts the lipid structure of the cell membrane and increases the cell permeability, leading to cell lysis . It induces conjunctival and corneal cell toxicity via causing cell retraction and cessation of normal cytokines, cell movement, and mitotic activity . It disrupts the barrier and transport properties of the corneal epithelium as well as inhibits the utilization of oxygen by the cornea . Chlorobutanol also inhibits oxygen use by the cornea, which increases susceptibility to infection . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.
Toxicity:
Classification:
Chlorobutanol belongs to the class of organic compounds known as tertiary alcohols. These are compounds in which a hydroxy group, -OH, is attached to a saturated carbon atom R3COH (R not H ), classified under the direct parent group Tertiary alcohols. This compound is a part of the Organic compounds, falling under the Organic oxygen compounds superclass, and categorized within the Organooxygen compounds class, specifically within the Alcohols and polyols subclass.
Categories:
Chlorobutanol is categorized under the following therapeutic classes: Alcohols, Alimentary Tract and Metabolism, Antiemetics and Antinauseants, Butanols, Chlorohydrins, Compounds used in a research, industrial, or household setting, Fatty Alcohols, Lipids, Pharmaceutic Aids, Pharmaceutical Preparations, Preservatives, Pharmaceutical. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.
Experimental Properties:
Further physical and chemical characteristics of Chlorobutanol include:
- Melting Point: 99
- Boiling Point: 167
Chlorobutanol is a type of Antiemetics
Antiemetics are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) used to alleviate and prevent nausea and vomiting, also known as emesis. They play a vital role in managing these distressing symptoms, which can be caused by various factors such as chemotherapy, postoperative recovery, motion sickness, or gastrointestinal disorders.
Antiemetics work by targeting specific pathways in the body that trigger emesis. One common mechanism involves blocking dopamine receptors in the brain, as dopamine plays a significant role in triggering the vomiting reflex. This class of antiemetics is known as dopamine antagonists. Another mechanism involves inhibiting serotonin receptors, which are associated with nausea and vomiting. These agents, called serotonin antagonists, effectively reduce these symptoms.
In addition to dopamine and serotonin antagonists, other types of antiemetics include neurokinin-1 receptor antagonists, antihistamines, and anticholinergics. Each of these classes acts on different pathways in the body to provide relief from nausea and vomiting.
Pharmaceutical companies manufacture antiemetic APIs in accordance with strict quality control guidelines and regulations. These APIs serve as the active ingredients in various formulations, such as tablets, capsules, injections, or suppositories, designed to deliver the desired therapeutic effects.
Overall, antiemetic APIs form an essential category in the pharmaceutical industry, addressing the significant need for effective management of nausea and vomiting. Their development and availability greatly contribute to enhancing patient comfort and quality of life during various medical treatments and conditions.
