Bendazac API Manufacturers

General Description:

Bendazac, identified by CAS number 20187-55-7, is a notable compound with significant therapeutic applications. Bendazac is an oxyacetic acid . Despite possessing anti-inflammatory, anti-necrotic, choleretic, and anti-lipidemic characteristics, most research has revolved around studying and demonstrating the agent's principal action in inhibiting the denaturation of proteins - an effect that has primarily proven useful in managing and delaying the progression of ocular cataracts . Bendazac, however, has since been withdrawn or discontinued in various international regions due to its capability or risk for eliciting hepatotoxicity in patients although a small handful of regions may continue to have the medication available for purchase and use either as a topical anti-inflammatory/analgesic cream or eye drop formulation.

Indications:

This drug is primarily indicated for: Prior to the withdrawal of bendazac from various international regions of use due to concerns for hepatotoxicity the chemical had demonstrated potential usefulness predominantly as the prescription medication bendazac lysine for the indication of managing the level of vision in patients with mild to moderate cataracts to facilitate delaying the need for surgical intervention . Elsewhere bendazac may still be available in a limited capacity as a non-prescription topical cream product for treating conditions like local pain, inflammation, dermatitis, eczema, pruritis, hives, insect bites, burns, erythema, and others - although such products may also be facing general discontinuation . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Bendazac undergoes metabolic processing primarily in: Bendazac is largely eliminated by metabolism, where more than 60% of an administered dose is excreted in the urine as the hydroxylated primary metabolite 5-hydroxybendazac and its glucuronide while up to approximately 15% of a bendazac dose is also excreted in the urine unchanged and as a glucuronide . Unfortunately, there is little data available regarding the specific enzymes responsible for bendazac's metabolism . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Bendazac are crucial for its therapeutic efficacy: Administered as its lysine salt, a 500 mg oral tablet of bendazac is well absorbed into the human body with maximum plasma concentrations Cmax ranging from 35 to 55 mg/L being attained within 0.5 to 1 hour in healthy volunteers after oral administration of a single 500 mg dose . The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Bendazac is an important consideration for its dosing schedule: The plasma elimination half-life recorded for bendazac is given as 1.7 to 5.2 hours, with a mean of 3.5 hours . This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Bendazac exhibits a strong affinity for binding with plasma proteins: Bendazac is >99% highly bound to plasma albumin protein in healthy subjects . This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Bendazac from the body primarily occurs through: About 60% of a dose of bendazac is eliminated via the urine as its primary metabolite, 5-hydroxybendazac . Approximately 15% of a dose is eliminated as unchanged drug and bendazac glucuronide in the urine as well. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Bendazac is distributed throughout the body with a volume of distribution of: The volume of distribution documented for bendazac is 0.16 L/kg . This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Bendazac is a critical factor in determining its safe and effective dosage: The plasma clearance recorded for bendazac is given as 0.018 to 0.054 L/h/kg with a mean of 0.033 L/h/kg . It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Bendazac exerts its therapeutic effects through: Bendazac principally demonstrates an antidenaturant action on proteins . This effect has been shown to inhibit the denaturation of various proteins like ocular lens proteins by heat, ultraviolet radiation, free radicals, and other chemicals . The medication may be administered to patients via a number of different formulations, including orally as the lysine salt, as eye drops, or even topical applications for the skin . Some preliminary studies have suggested that an apparent improvement of the blood-retinal barrier had been observed in diabetic patients using bendazac lysine 500 mg three times a day for three to six months . Moreover, the use of topical bendazac has also been shown to demonstrate anti-inflammatory effects in animal models and clinical studies to effectively treat varied dermatoses, especially those involving a necrotic component . Additionally, bendazac has also demonstrated choleretic and antilipidaemic activities that have resulted in substantial reductions in beta/alpha lipoprotein ratio, and total lipid, total cholesterol, and triglyceride levels in patients with dyslipidaemia using oral bendazac lysine 500 mg three times daily . The medication has also elicited the inhibition of phytohaemagglutinin induced lymphocyte transformation in vitro . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Bendazac functions by: Bendazac seems to elicit an anticataract action by inhibiting the denaturation of ocular lens proteins, although the precise mechanisms by which this action occurs has not yet been formally elucidated - despite there being many proposed mechanisms . In particular, the denaturation of lens proteins may in part be prevented by inhibiting the binding of certain chemicals like cyanates or sugars and 5-hydroxybendazac - the major metabolite of bendazac - has been shown to be capable of inhibiting the glycosylation of lens proteins by sugars like galactose or glucose-6-phosphate in a dose-dependent manner . Moreover, the apparent ability for administered bendazac to elicit free radical scavenger activities due to interactions with protein molecules suggests that the medication may also be able to prevent the oxidation of lens proteins by free radicals in the development of cataracts . Furthermore, bendazac may also be capable of reducing the sulfhydryl group oxidation of lens proteins by the saliva, serum, or urine from patients with cataracts following single dose administration and reduce biological liquid oxidant activity (BLOA) in doing so . Otherwise, it is believed that bendazac also possesses non-steroidal anti-inflammatory actions, as well as analgesic, antipyretic, and platelet-inhibitory effects These effects may be accounted for in part by the substance's capability to inhibit prostaglandin synthesis by inhibiting cyclooxygenase activity in converting arachidonic acid to cyclic endoperoxides - the precursors of prostaglandins . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Bendazac belongs to the class of organic compounds known as indazoles. These are compounds containing an indazole, which is structurally characterized by a pyrazole fused to a benzene, classified under the direct parent group Indazoles. This compound is a part of the Organic compounds, falling under the Organoheterocyclic compounds superclass, and categorized within the Benzopyrazoles class, specifically within the Indazoles subclass.

Categories:

Bendazac is categorized under the following therapeutic classes: Agents causing hyperkalemia, Agents that produce hypertension, Analgesics, Analgesics, Non-Narcotic, Anti-Inflammatory Agents, Anti-Inflammatory Agents, Non-Steroidal, Antiinflammatory Preparations, Non-Steroids for Topical Use, Antimetabolites, Antirheumatic Agents, Heterocyclic Compounds, Fused-Ring, Hypolipidemic Agents, Lipid Regulating Agents, Musculo-Skeletal System, Nephrotoxic agents, Non COX-2 selective NSAIDS, Ophthalmologicals, Peripheral Nervous System Agents, Pyrazoles, Sensory Organs, Sensory System Agents, Topical Products for Joint and Muscular Pain. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.