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
Chlorobutanol hemihydrate
Chlorobutanol hemihydrate

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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*** Taking medicines without doctor's advice can cause long-term problems.
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