Thiethylperazine

399.61576

399.62

215-819-0

8ETK1WAF6R

DTXSID1023651

C62081

Crystals from acetone

R - Respiratory system

60.3

5

Solid

1.1684 (rough estimate)

62-64 °C

227 °C @ Press: 0.01 Torr

292.4ºC

1.5605 (estimate)

4.87e-03 g/L

Crystals from methanol; decomp @ 188-190 °C /Dimaleate/

SP0350000

P264, P270, P273, P301+P312, P330, P391, P501

H302

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P273, P301+P312, P330, P391, and P501|Aggregated GHS information provided by 5 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Manifestations of acute overdosage of TORECAN (thiethylperazine) can be expected to reflect the CNS effects of the drug and include extrapyramidal symptoms (E.P.S), confusion and convulsions with reduced or absent reflexes, respiratory depression and hypotension.

/INTERACTS WITH/...GUANETHIDINE (BLOCKADE OF ANTIHYPERTENSIVE EFFECT); MORPHINE (POTENTIATES SEDATION); MEPERIDINE (INCR RESP DEPRESSION); BARBITURATES & OTHER CNS DEPRESSANTS INCL ALCOHOL (POTENTIATION RESULTING IN INCR SEDATIVE EFFECT OR PROLONGED POST-ANESTHETIC SLEEP TIME)... /MALATE & MALEATE/|/INTERACTS WITH/...LEVODOPA (DECR UPTAKE & EFFECTIVENESS); ANTICONVULSANTS (LOWERS SEIZURE THRESHOLD); PROCARBAZINE (POTENTIATION OF BEHAVIORAL ABNORMALITIES). /MALATE & MALEATE/

60%

PHENOTHIAZINES ... MAY APPEAR IN MILK OF NURSING MOTHERS... /PHENOTHIAZINES, HUMAN, ORAL, IM/

For the treatment or relief of nausea and vomiting.

Antiemetics; Dopamine Antagonists|EXPTL USE (VET): THE EFFECT OF THIETHYLPERAZINE ON VESTIBULAR NYSTAGMUS IN RABBITS WAS INVESTIGATED. THE NYSTAGMUS WAS PROVOKED BY MEANS OF A TORSION SWING. A CLEAR SUPPRESSIVE EFFECT BUT LESS STRONG & SHORTER THAN CINNARIZINE & SULPIRIDE WAS SEEN WITH THIETHYLPERAZINE.|EXPTL USE (VET): DOGS FED 0.4 KG DOG FOOD WERE THEN INJECTED WITH 0.86 MG/KG THIETHYLPERAZINE IM & IRRADIATED BY (60)CO TELETHERAPY UNIT. THE DOSE OF RADIATION CAUSING EMESIS IN 50% (ED50) OF CONTROL DOGS WAS 170 RAD. ED50 WAS INCR TO 320 RAD BY THIETHYLPERAZINE.|A PHENOTHIAZINE ANTIEMETIC EFFECTIVE IN RELIEF OF NAUSEA & VOMITING FROM VARIOUS CAUSES. IT IS ALSO POSSIBLY EFFECTIVE FOR MGMNT OF VERTIGO. /MALEATE/|For more Therapeutic Uses (Complete) data for ETHYLTHIOPERAZINE (12 total), please visit the HSDB record page.

IT SHOULD NOT BE USED IN PREGNANCY OR CHILDREN UNDER 12 YEARS OF AGE. OTHER CONTRAINDICATIONS & SIDE EFFECTS ARE THE SAME AS THOSE FOR OTHER PHENOTHIAZINES. /MALEATE/|THESE AGENTS SHOULD BE USED CAUTIOUSLY IN PT WITH SEVERE LIVER DISEASE & SEIZURE DISORDERS & IN ELDERLY PT. /ANTIEMETIC PHENOTHIAZINES/|... PHENOTHIAZINES ... SHOULD BE USED WITH EXTREME CAUTION, IF @ ALL, IN UNTREATED EPILEPTIC PT & IN PT UNDERGOING WITHDRAWAL FROM CENTRAL DEPRESSANT DRUGS SUCH AS ALCOHOL, BARBITURATES, AND BENZODIAZEPINES. PHENOTHIAZINES MAY BE USED IN EPILEPTICS IF MODERATE DOSES ARE ATTAINED GRADUALLY AND IF CONCOMITANT ANTICONVULSANT DRUG THERAPY IS MAINTAINED. /PHENOTHIAZINES/|...PRECAUTIONS SHOULD BE OBSERVED IN USE OF PHENOTHIAZINES FOR NAUSEA & VOMITING AS WITH USE OF POTENT ANALGESICS IN TREATMENT OF PAIN, BECAUSE THEY MAY MASK DIAGNOSTIC SYMPTOMS IN ACUTE SURGICAL CONDITIONS OR NEUROLOGICAL SYNDROMES. /PHENOTHIAZINES/|For more Drug Warnings (Complete) data for ETHYLTHIOPERAZINE (31 total), please visit the HSDB record page.

TOLERANCE TO ANTIPSYCHOTIC DRUGS & CROSS-TOLERANCE AMONG AGENTS ... DEMONSTRABLE IN BEHAVIORAL & BIOCHEM EXPT IN ANIMALS, PARTICULARLY THOSE DIRECTED TOWARD EVALUATION OF BLOCKADE OF DOPAMINERGIC RECEPTORS IN BASAL GANGLIA. /PHENOTHIAZINES/|ONE CORRELATE OF TOLERANCE ... IS DEVELOPMENT OF DISUSE SUPERSENSITIVITY IN /FOREBRAIN DOPAMINERGIC SYSTEMS/ ... THIS MECHANISM MAY UNDERLIE ... WITHDRAWAL-EMERGENT DYSKINESIAS (CHOREOATHETOSIS ON ABRUPT DISCONTINUATION OF ANTIPSYCHOTIC DRUGS, ESP FOLLOWING PROLONGED USE OF HIGH DOSES ... /PHENOTHIAZINES/

Thiethylperazine, an atypical antipsychotic agent, is used to treat both negative and positive symptoms of schizophrenia, acute mania with bipolar disorder, agitation, and psychotic symptoms in dementia. Future uses may include the treatment of obsessive-compulsive disorder and severe behavioral disorders in autism. Structurally and pharmacologically similar to clozapine, Thiethylperazine binds to alpha(1), dopamine, histamine H1, muscarinic, and serotonin type 2 (5-HT2) receptors.

Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME. (See all compounds classified as Dopamine Antagonists.)|Drugs used to prevent NAUSEA or VOMITING. (See all compounds classified as Antiemetics.)

Thiethylperazine is eliminated in the urine.|APPROX HALF OF METABOLITES OF COMMONLY USED PHENOTHIAZINES ARE FOUND IN URINE & REST IN FECES. 6 MO AFTER DISCONTINUATION OF THESE DRUGS, VARIOUS METABOLITES ARE DETECTABLE IN URINE. /PHENOTHIAZINES/|PHENOTHIAZINE TRANQUILIZERS CROSS PLACENTA RAPIDLY, & THEY HAVE BEEN MEASURED FOR MANY YR IN URINE & TISSUES OF NEONATES OF TREATED MOTHERS, BUT VERY LOW BLOOD LEVELS OF MOTHERS & FETUSES HAVE BEEN MEASURED ONLY RECENTLY... /PHENOTHIAZINES/

IN PRINCIPLE, METABOLITES OF THIETHYLPERAZINE SIMILAR TO THOSE OF THIORIDAZINE SEEM TO BE FORMED. A LARGE PROPORTION OF THE DOSE IS SECRETED INTO BILE AS GLUCURONIDES.|... METAB ... ARE OXIDATIVE PROCESSES MEDIATED LARGELY BY GENETICALLY CONTROLLED HEPATIC MICROSOMAL OXIDASES & CONJUGATION PROCESSES. /PHENOTHIAZINES/

Thiethylperazine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Thiethylperazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Thiethylperazine does not appear to block dopamine within the tubero-infundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with thiethylperazine.|THERE IS AN ADENYLATE CYCLASE IN LIMBIC SYSTEM, AS WELL AS IN CAUDATE NUCLEUS, THAT IS SPECIFICALLY ACTIVATED BY DOPAMINE. ...ACTIVATION OF...ENZYME IS... BLOCKED BY...PHENOTHIAZINES. ...THERAPEUTIC EFFICACY & SIDE EFFECTS MAY RELATE TO INHIBITION OF DOPAMINE ACTIVATION OF ADENYLATE CYCLASE. /PHENOTHIAZINES/|...PHENOTHIAZINES, BLOCK DOPAMINE RECEPTORS & INCR TURNOVER RATE OF DOPAMINE IN CORPUS STRIATUM. INCR TURNOVER RATE IS BELIEVED TO BE RESULT OF NEURONAL FEEDBACK MECHANISM. ...FIRING OF.../IDENTIFIED DOPAMINERGIC NEURONS IN SUBSTANTIA NIGRA & VENTRAL TEGMENTAL AREAS/ IS INCR BY ANTIPSYCHOTIC PHENOTHIAZINES. /PHENOTHIAZINES/

DYSKINESIA TARDA CAUSED BY LONG-TERM ADMIN OF THIETHYLPERAZINE.

Norzine

Torecan maleate, Toresten, Tresten. /Dimaleate/|TORECAN [MALATE] (BOEHRINGER INGELHEIM), INJECTION: SOLN (AQUEOUS) 5 MG/ML IN 2 ML CONTAINERS. /MALATE/

TORECAN DIMALEATE WAS EXTRACTED FROM PILLS & SUPPOSITORIES WITH 0.1 N HCL & DETERMINED BY POLAROGRAPHY.|CHEMICAL CHARACTERIZATION OF THIETHYLPERAZINE DIMALEATE BY MASS SPECTROMETRY WITH POSSIBLE FRAGMENTATION ROUTES.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals