Chlorobutanol hemihydrate
Chlorobutanol hemihydrate Uses, Dosage, Side Effects, Food Interaction and all others data.
Chlorobutanol hemihydrate, 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 hemihydrate is a common detergent preservative in eye drops and other ophthalmic therapeutic formulations .
| Trade Name | Chlorobutanol hemihydrate |
| Generic | Chlorobutanol |
| Chlorobutanol Other Names | Chloretone, Chlorobutanol |
| Type | |
| Formula | C4H7Cl3O |
| Weight | Average: 177.45 Monoisotopic: 175.9562479 |
| Protein binding | The binding to plasma proteins was 57 ± 3% . |
| Groups | Approved, Investigational, Vet approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
No approved therapeutic indications on its own.
Chlorobutanol hemihydrate is also used to associated treatment for these conditions: Acute Rhinosinusitis, Acute Sinusitis, Infective otitis externa, Pollen Allergy, Rhinitis, Acute Rhinitis
How Chlorobutanol hemihydrate works
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 hemihydrate also inhibits oxygen use by the cornea, which increases susceptibility to infection .
Toxicity
Oral LD50 of anhydrous chlorobutanol in rat is 510 mg/kg . Chlorobutanol hemihydrate was shown to induce conjunctival and corneal cell toxicity in vitro
Food Interaction
No interactions found.Volume of Distribution
The volume of distribution was approximately 233 ± 141 L in healthy individuals receiving oral chlorobutanol .
Elimination Route
Following oral administration in healthy subjects, the plasma concentration fell by 50% in 24 hours post-administration .
Half Life
Following oral administration, the terminal elimination half life in healthy subjects was 10.3 ± 1.3 days .
Clearance
In healthy subjects, the clearance was approximately 11.6 ± 1.0 mL/min following oral administration .
Elimination Route
Under physiological conditions, chlorobutanol is unstable. The mean urinary recovery accounts for 9.6% of the dose orally administered .
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