Thiethylperazine

5.41 @ 25 °C

5

4.82

WHITE TO FAINTLY YELLOW CRYSTALLINE POWDER; SLIGHT ODOR; FREELY SOL IN WATER; SOL IN METHANOL; PH (FRESHLY PREPARED 1 IN 100 SOLN) BETWEEN 2.8-3.8 /MALATE/

FAINTLY YELLOWISH, FINE, CRYSTALLINE, VOLUMINOUS POWDER; ODORLESS OR HAS VERY SLIGHT ODOR; BITTER TASTE; MELTS @ 183 °C WITH DECOMP; POORLY SOL IN WATER, METHANOL, ABSOLUTE ETHANOL; VERY POORLY SOL IN BENZENE, ETHER, CHLOROFORM /MALEATE/

4.87e-03 g/L

Breast Feeding; Lactation; Antiemetics; Phenothiazines; Gastrointestinal Agents

Pharmaceuticals

62-64 °C

62-64 °C

Crystals from ethanol; MP: 214-216 °C /Dihydrochloride/

Crystals from ethanol; MP: 139 °C /Dimalate/

62 - 64 °C

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).

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.

/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/

R - Respiratory system

QR - Respiratory system

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.

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/

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.