Bronopol API Manufacturers

General Description:

Bronopol, identified by CAS number 52-51-7, is a notable compound with significant therapeutic applications. Bronopol, or 2-Bromo-2-nitro-1,3-propanediol, is an organic compound with wide-spectrum antimicrobial properties. First synthesized in 1897, bronopol was primarily used as a preservative for pharmaceuticals and was registered in the United States in 1984 for use in industrial bactericides, slimicides and preservatives . Bronopol is used as a microbicide or microbiostat in various commercial and industrial applications, including oil field systems, air washer systems, air conditioning or humidifying systems, cooling water systems, papermills, absorbent clays, metal working fluids, printing inks, paints, adhesives and consumer products . Compared to other aliphatic halogen-nitro compounds, bronopol is more stable to hydrolysis in aqueous media under normal conditions . The inhibitory activity against various bacteria, including _Pseudomonas aeruginosa_, was demonstrated _in vitro_ . The agent is largely available commercially as an antibacterial for a variety of industrial purposes while it is predominantly available for purchase as a pet animal litter antibacterial at the domestic consumer level . Nevertheless, ongoing contemporary re-evaluations of bronopol use in large markets such as Canada now place various compositional and product restrictions on the use of the agent in cosmetic products and in other products where it may not primarily be used in the role of a non-medicinal preservative antimicrobial .

Indications:

This drug is primarily indicated for: Bronopol as an active ingredient is registered as a commercial biocide and preservative in many industrial processes. Registered biocidal uses include pulp and paper mills, water cooling towers, waste water treatment, evaporative condensers, heat exchangers, food pasteurizing plants, metalworking fluids, and oilfield applications . In addition, preservative uses include household products (e.g, dishwashing liquids, laundry products), latex emulsions, polymer lattices, pigments, leather and milk samples for analysis . Bronopol is also formulated into granular domestic end-use products in the form of cat litter . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Bronopol undergoes metabolic processing primarily in: Bronopol undergoes degradation in aqueous medium to form bromonitroethanol from a retroaldol reaction with the liberation of an equimolar amount of formaldehyde . Formaldehyde is a degradation product of bronopol, which may cause sensitization . Bromonitroethanol further decomposes to formaldehyde and bromonitromethane. Bromonitroethanol may also break down to release a nitrite ion and 2-bromoethanol . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Bronopol are crucial for its therapeutic efficacy: Bronopol was rapidly absorbed in animal studies. It may be absorbed via aerosol inhalation, dermal contact, and ingestion . In rats, approximately 40% of the topically applied dose of bronopol was absorbed through the skin within 24 hr . Following oral administration of 1 mg/kg in rats, the peak plasma concentrations of bronopol were reached up to 2 hours post-dosing . The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Bronopol is an important consideration for its dosing schedule: The half-life of bronopol in the biological systems is not reported in the literature. The half-life value reported for bronopol reflects the environment fate of the compound. When released into the air as vapours, bronopol is degraded in the atmosphere by reaction with photochemically-produced hydroxyl radicals where the half life for this reaction is approximately 11 days . The photolysis half-life is 24 hours in water but may be up to 2 days under natural sunlight . This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Bronopol exhibits a strong affinity for binding with plasma proteins: No data available. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Bronopol from the body primarily occurs through: Metabolism studies indicate that bronopol is primarily excreted in the urine . In rats, about 19% of dermally-applied bronopol was excreted in the urine, feces and expired air . Following oral administration of 1 mg/kg radiolabelled bronopol in rats, approximately 81% and 6% of the administered radioactivity was recovered in the urine and expired air, respectively, within a period of 24 hours . Following intravenous administration in rat, the recoveries in the urine and expired air were 74% and 9% of the dose, respectively . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Bronopol is distributed throughout the body with a volume of distribution of: The highest concentrations of bronopol were detected in the excretory organs of rat such as kidney, liver, and lung . The lowest concentration was in the fat . This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Bronopol is a critical factor in determining its safe and effective dosage: No data available. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Bronopol exerts its therapeutic effects through: At concentrations of 12.5 to 50 μg/mL, bronopol mediated an inhibitory activity against various strains of Gram negative and positive bacteria _in vitro_ . The bactericidal activity is reported to be greater against Gram-negative bacteria than against Gram-positive cocci . Bronopol was also demonstrated to be effective against various fungal species, but the inhibitory action is reported to be minimal compared to that of against bacterial species . The inhibitory activity of bronopol decreases with increasing pH of the media . Bronopol also elicits an anti-protozoal activity, as demonstrated with _Ichthyophthirius multifiliis_ _in vitro_ and _in vivo_ . It is proposed that bronopol affects the survival of all free-living stages of _I. multifiliis_ . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Bronopol functions by: It is proposed that bronopol generates biocide-induced bacteriostasis followed by a growth at an inhibited rate in bacteria, via two distinct reactions between bronopol and essential thiols within the bacterial cell . Under aerobic conditions, bronopol catalyzes the oxidation of thiol groups, such as cysteine, to disulfides. This reaction is accompanied by rapid consumption of oxygen, where oxygen acts as the final oxidant. During the conversion of cysteine to cystine, radical anion intermediates such as superoxide and peroxide are formed from bronopol to exert a direct bactericidal activity. The oxidation of excess thiols alters the redox state to create anoxic conditions, leading to a second reaction involving the oxidation of intracellular thiols such as glutathione to its disulfide. The resulting effects are inhibition of enzyme function, and reduced growth rate following the bacteriostatic period . Under the anoxic conditions, the reaction between thiol and bronopol decelerates without the involvement of oxygen and the consumption of bronopol predominates. Bronopol is ultimately removed from the reaction via consumption and resumption of bacterial growth occurs . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Categories:

Bronopol is categorized under the following therapeutic classes: Alcohols, Anti-Infective Agents, Anti-Infective Agents, Local, Cell-mediated Immunity, Compounds used in a research, industrial, or household setting, Drugs that are Mainly Renally Excreted, Glycols, Increased Histamine Release, Indicators and Reagents, Laboratory Chemicals, Preservatives, Pharmaceutical, Standardized Chemical Allergen. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Bronopol include:

• Water Solubility: 25-25g/100mL at 22°C
• Melting Point: 123-130
• Boiling Point: 130
• logP: -0.6