Chlorphenesin carbamate

245.660

245.66

212-954-7

HQC4WI89YG|G014XC07GH

82943

DTXSID5022803

CRYSTALS FROM BENZENE + TOLUENE|WHITE TO OFF-WHITE POWDER

81.78000

1.41

1.4±0.1 g/cm3

89-91 °C

481.8±40.0 °C at 760 mmHg

245.2±27.3 °C

1.564

FREELY SOL IN ALCOHOL

LD50 orally in rats: 748 mg/kg; i.v. in mice: 239 mg/kg (Cass, Frederick)

ODORLESS

PRACTICALLY TASTELESS

STABLE IN LIGHT, AIR, AND AT ORDINARY TEMP.

IT NONCOMPETITIVELY ANTAGONIZED HISTAMINE, ACETYLCHOLINE, NOREPINEPHRINE & OXYTOCIN IN ISOLATED GUINEA PIG INTESTINE & TRACHEA & IN RAT VAS DEFERENS & UTERUS.|IT POTENTIATED THE HEXOBARBITAL-INDUCED SLEEPING TIME IN MICE & ITS ED50 VALUE WAS 99 MG/KG.

IT IS EMPLOYED TO DIMINISH SKELETAL MUSCLE SPASMS RESULTING FROM TRAUMA , INFLAMMATION, VERTEBRAL DISK SYNDROME, OSTEOARTHRITIS, AND RHEUMATOID ARTHRITIS.|APPLICATION: CENTRALLY ACTIVE SKELETAL MUSCLE RELAXANT SIMILAR IN ITS ACTIONS TO METHOCARBAMOL...|IT MAY BE USEFUL AS TEMPORARY ADJUNCT TO PHYSIOTHERAPY & OTHER APPROPRIATE MEASURES IN THE TREATMENT OF THE DISCOMFORT PRODUCED BY SKELETAL MUSCLE SPASM OF LOCAL ORIGIN.|MEDICATION (VET): /USED/ AS AN ADJUNCT TO OTHER THERAPY FOR ACUTE INFLAMMATORY OR TRAUMATIC SKELETAL MUSCLE INVOLVEMENT INCLUDING SPRAINS & INTERVERTEBRAL DISC SYNDROMES.|THESE DRUGS MAY TEMPORARILY ABATE SOME OF THE SYMPTOMS OF CEREBRAL PALSY, BUT THEY HAVE MINOR ROLE IN OVERALL MGMNT OF THIS DISEASE... ALL CENTRALLY ACTING MUSCLE RELAXANTS PRODUCE SOME SEDATION, AT LEAST AT HIGHEST DOSES EMPLOYED CLINICALLY. /MUSCLE RELAXANTS/

PERSONS TAKING DRUG SHOULD NOT DRIVE, OPERATE MACHINERY, OR UNDERTAKE ACTIVITIES THAT REQUIRE ALERTNESS, JUDGMENT, OR MENTATION.|...PROBABLY HAS AN ADDICTION LIABILITY, AS DO OTHER CARBAMATES.|VET: DO NOT ADMIN TO ANY ANIMAL WITH SIGNIFICANT LIVER PATHOLOGY. LIVER FUNCTION MAY BE ADVERSELY AFFECTED DURING ITS USE.

ORAL DOSES ARE READILY ABSORBED /IN ANIMALS/.|MUCH OF DOSE OF CHLORPHENESIN CARBAMATE...IS RAPIDLY EXCRETED IN URINE OF RATS & OF MAN.|AFTER ORAL ADMIN OF (14)C-LABELED CHLORPHENESIN CARBAMATE TO RATS, IT WAS ABSORBED FROM GI TRACT; EXCRETED IN URINE ABOUT 90%; 36% IN BILE. RADIOACTIVITY WAS DISTRIBUTED IN ALMOST ALL TISSUES, HIGHEST IN LIVER, BRAIN & SPINAL CORD.

MAJOR METABOLITE (49% OF DOSE) IS ETHER GLUCURONIDE OF CHLORPHENESIN CARBAMATE...|5% APPEARED IN URINE AS P-CHLOROPHENOXYLACTIC ACID, 17% AS P-CHLOROPHENOXYACETIC ACID, AND 9% AS SULFATE CONJUGATE OF P-CHLOROPHENOL...|MAJOR METABOLITES IN A 48-HR URINE SAMPLE FROM RATS GIVEN (14)C-LABELED CHLORPHENESIN CARBAMATE WERE GLUCURONIDE, P-CHLOROPHENOXYLACTIC ACID, P-CHLOROPHENOXYACETIC ACID, & P-CHLOROPHENOL.

MUSCLE RELAXANTS CAUSE SKELETAL MUSCULAR RELAXATION, WITHOUT LOSS OF CONSCIOUSNESS, AS RESULT OF SELECTIVE ACTION UPON CNS. ... PROMINENT EFFECT OF MUSCLE RELAXANTS IS TO DEPRESS SPINAL POLYSYNAPTIC REFLEXES PREFERENTIALLY OVER MONOSYNAPTIC REFLEXES. ... MECHANISM OF ACTION...REMAIN TO BE ELUCIDATED. /MUSCLE RELAXANTS/

MOST COMMON UNTOWARD EFFECTS ARE DROWSINESS AND DIZZINESS. ADVERSE REACTIONS NOTED OCCASIONALLY INCLUDE GI DISTURBANCES, PARADOXICAL STIMULATION, NERVOUSNESS, INSOMNIA, HEADACHE, & ASTHENIA. RASH & PRURITUS OCCUR RARELY.|SIDE EFFECTS INCLUDE...EPIGASTRIC DISTRESS, NAUSEA...|CENTRALLY ACTING MUSCLE RELAXANTS COMMONLY PRODUCE...BLURRED VISION, WEAKNESS, LETHARGY, ATAXIA, & NYSTAGMUS. ...VOMITING, HEARTBURN, & ABDOMINAL DISTRESS ARE ALSO OBSERVED, ESPECIALLY AFTER LARGE ORAL DOSES. HYPERSENSITIVITY REACTIONS INCLUDE...RARELY, ANAPHYLACTOID REACTION & LEUKOPENIA. /MUSCLE RELAXANTS/

chlorphenesin carbamate

PROBABLY 100% AS SKELETAL MUSCLE RELAXANT (1975)

TLC. DAVIS, TW MCCONNEL, J CHROMATOGR 29, 286 (1967). /CHLORPHENESIN/|HIGH PRESSURE LIQUID CHROMATOGRAPHIC DETERMINATION OF CHLORPHENESISN CARBAMATE.

URINE, TLC. BUHLER DB, J PHARMACOL EXP THER 145, 232 (1964).|GLC DETERMINATION OF CHLORPHENESIN CARBAMATE IN SERUM.

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