Absorption, Distribution and Excretion
Following oral administration in healthy subjects, plasma concentration decreased by 50% within 24 hours. Chlorobutanol is unstable under physiological conditions. The mean urinary recovery rate is 9.6% of the oral dose. The volume of distribution after oral administration of chlorobutanol in healthy subjects is approximately 233 ± 141 L. The clearance after oral administration in healthy subjects is approximately 11.6 ± 1.0 mL/min. Metabolism/Metabolites Chlorobutanol has been reported to undergo glucuronidation and sulfation. Biological Half-Life The terminal elimination half-life after oral administration in healthy subjects is 10.3 ± 1.3 days.

The binding rate of protein to plasma proteins was 57 ± 3%.

[1]. Chlorobutanol: maternal serum levels and placental transfer in the mouse. Vet Hum Toxicol. 1997 Oct;39(5):287-90.

[2]. The antibacterial stability of chlorobutanol stored in polyethylene bottles. Am J Hosp Pharm. 1971 Jul;28(7):507-12.

Chlorobutanol is a tertiary alcohol. Chlorobutanol, also known as chlorobutanol, is an alcohol preservative without surfactant activity. In addition to its antibacterial and antifungal properties, it also has sedative-hypnotic and weak local anesthetic effects. Its properties are similar to chloral hydrate, and it is formed by a simple nucleophilic addition reaction of chloroform and acetone. As a long-term stabilizer in multi-component formulations, chlorobutanol is usually used at a concentration of 0.5%. At this concentration, it also maintains its antibacterial activity. Due to its long terminal half-life of 37 days, significant accumulation occurs after repeated administration, thus limiting its use as a sedative. Chlorobutanol is a commonly used surfactant and preservative in eye drops and other ophthalmic therapeutic preparations. It is a colorless to white crystalline compound with the odor and taste of camphor. It is widely used in various drug solutions, especially injections, as a preservative. Furthermore, it is also the active ingredient in some oral sedatives and local anesthetics. See also: chlorobutanol; doxylamine succinate (ingredient).

---

Drug Indications
Currently, there are no approved indications for single treatment.Mechanism of Action
As a surfactant, chlorobutanol disrupts the lipid structure of cell membranes, increasing cell permeability and leading to cell lysis. It induces conjunctival and corneal cytotoxicity by causing cell retraction and halting normal cytokine, cell motility, and mitotic activity. It disrupts the barrier and transport functions of the corneal epithelium and inhibits corneal oxygen utilization. Chlorobutanol also inhibits corneal oxygen utilization, thereby increasing susceptibility to infection.Therapeutic Uses
Adrenergic α-receptor agonist; adrenergic drug; sympathomimetic drug; vasoconstrictor.

For topical use, dissolved in clove oil, it is used as a dental analgesic. It has mild local anesthetic efficacy and has been used as an anesthetic powder (1% to 5%) or ointment (10%).
Orally, its therapeutic uses are largely the same as chloral hydrate.
Therefore, chlorobutanol is used as a sedative and hypnotic. It has been administered orally to relieve vomiting caused by gastritis. Dosage—Topical…tablets or capsules.
Medication (Veterinary): Disinfectant and local anesthetic; can be used orally as a sedative and hypnotic. It appears to be effective for gastritis with persistent vomiting in dogs.
For more complete data on the therapeutic uses of chloromethone (7 in total), please visit the HSDB record page.

---

Drug Warnings
Veterinary Warning:…Not for use in felines for motion sickness, as repeated use in this species can lead to respiratory depression, which may even be fatal. Avoid use in animals with liver or kidney disease.
Similar to chloral hydrate, but does not cause stomach irritation.
Allergic reactions…including erythema, scarlet fever-like rash, urticaria, and eczematous dermatitis. The rash typically begins on the face or back and then spreads to the neck, chest, and arms; scaling may follow…/Chloral Hydrate/
Adverse central nervous system reactions include dizziness, malaise, ataxia, and nightmares. "Hangover" symptoms may also occur…/Chloral Hydrate/
Pharmacodynamics
Chlorobutanol is a detergent preservative with broad-spectrum antibacterial activity. In vitro studies have shown that chlorobutanol inhibits platelet aggregation and release through an unknown mechanism. One study suggests that chlorobutanol's antiplatelet effect may stem from inhibition of the arachidonic acid pathway. It attenuates thromboxane B2 production, increases in cytoplasmic free calcium, and ATP release, and exhibits significant inhibitory activity against various aggregation inducers in a time- and concentration-dependent manner. Chlorobutanol may have a direct negative inotropic effect on cardiomyocytes, thereby weakening the isometric contractile tension produced by the heart. In vitro experiments showed that chlorobutanol can induce conjunctival and corneal cell toxicity: at a concentration of 0.1%, chlorobutanol almost completely destroyed the squamous layer; at a concentration of 0.5%, corneal epithelial cell degeneration, formation of obvious vesicles, cytoplasmic swelling, and occasional rupture of the outer membrane were observed.

175.956

57-15-8

Chlorobutanol hemihydrate;6001-64-5

5977

White to off-white solid powder

1.4±0.1 g/cm3

167.0±0.0 °C at 760 mmHg

~78 °C

61.8±25.9 °C

0.6±0.6 mmHg at 25°C

1.491

2.07

1

1

0

8

83.8

0

ClC(C(C([H])([H])[H])(C([H])([H])[H])O[H])(Cl)Cl

OSASVXMJTNOKOY-UHFFFAOYSA-N

InChI=1S/C4H7Cl3O/c1-3(2,8)4(5,6)7/h8H,1-2H3

1,1,1-trichloro-2-methylpropan-2-ol

Chlortran Methaform Chlorobutanol Acetochlorone

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~563.51 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (14.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

---

Solubility in Formulation 2: ≥ 2.5 mg/mL (14.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

---

View More

Solubility in Formulation 3: ≥ 2.5 mg/mL (14.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

---

 (Please use freshly prepared in vivo formulations for optimal results.)