クロルゾキサゾン

1.6

2.11

2.96e+00 g/L

>25.4 [ug/mL] (The mean of the results at pH 7.4)

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

Pharmaceuticals

191-191.5

191.5 °C

Warning

H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]

P261, P264, P264+P265, P270, P271, P280, P301+P317, P302+P352, P304+P340, P305+P351+P338, P319, P321, P330, P332+P317, P337+P317, P362+P364, P403+P233, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 54 reports by companies from 11 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

There have been no adequate prospective studies demonstrating the rates ofALT or AST elevations on chlorzoxazone therapy. Rare instances of clinicalapparent liver disease due to chlorzoxazone have appeared, including fatalcases. While case reports have been few, in many instances chlorzoxazone wasclearly implicated; furthermore, a related muscle relaxant with similarstructure (zoxazolamine) was withdrawn from use in 1961, largely because ofhepatotoxicity. The usual latency period to onset of liver injury is 1 to 4weeks, and the pattern of disease is typically hepatocellular with markedelevations in ALT levels and jaundice, but minimal increases in alkalinephosphatase. Cholestatic enzyme elevations after exposure to chlorzoxazonehave also been described. Allergic manifestations (rash and fever) arecommon, particularly in cases with a short latency (Case 1); autoantibodiesare rare. Recovery is rapid once chlorzoxazone is stopped, but fatal caseshave been reported, with disease progression despite early discontinuationof the agent (Case 2). There is rapid recurrence of injury with reexposure,often accompanied by fever.

M - Musculo-skeletal system

QM - Musculo-skeletal system

Chlorzoxazone is a centrally-acting agent for painful musculoskeletal conditions. Data available from animal experiments as well as human study indicate that chlorzoxazone acts primarily at the level of the spinal cord and subcortical areas of the brain where it inhibits multisynaptic reflex a.c. involved in producing and maintaining skeletal muscle spasm of varied etiology. The clinical result is a reduction of the skeletal muscle spasm with relief of pain and increased mobility of the involved muscles.

Chlorzoxazone inhibits degranulation of mast cells, subsequently preventing the release of histamine and slow-reacting substance of anaphylaxis (SRS-A), mediators of type I allergic reactions. Chlorzoxazone also may reduce the release of inflammatory leukotrienes. Chlorzoxazone may act by inhibiting calcium and potassium influx which would lead to neuronal inhibition and muscle relaxation. Data available from animal experiments as well as human study indicate that chlorzoxazone acts primarily at the level of the spinal cord and subcortical areas of the brain where it inhibits multisynaptic reflex arcs involved in producing and maintaining skeletal muscle spasm

Chlorzoxazone is rapidly metabolized in the liver and is excreted in the urine, primarily in a conjugated form as the glucuronide.

Chlorzoxazone has known human metabolites that include 6-Hydroxychlorzoxazone.

H0DE420U8G

CHLORZOXAZONE

Physiologic Effects [PE] - Centrally-mediated Muscle Relaxation

Established Pharmacologic Class [EPC] - Muscle Relaxant

Chlorzoxazone is a Muscle Relaxant. The physiologic effect of chlorzoxazone is by means of Centrally-mediated Muscle Relaxation.

CHLORZOXAZONE