Triflupromazine

352.4170696

352.42

205-673-6

RO16TQF95Y

DTXSID9023704

VISCOUS, LIGHT AMBER-COLORED, LIQ, WHICH CRYSTALLIZES ON PROLONGED STANDING INTO LARGE IRREGULAR CRYSTALS

N - Nervous system

2934300000

31.8

5.2

Solid

1.2198 (estimate)

316.0 °C

176 °C @ Press: 0.7 Torr

212.4ºC

nD23 1.5780

1.80e-03 g/L

SLIGHT, CHARACTERISTIC ODOR; MELTS BETWEEN 170 & 178 °C /HYDROCHLORIDE/|PH OF 2% AQ SOLN 4.1, IF PH IS RAISED TO 6.4, PPT OF FREE BASE RESULTS /HYDROCHLORIDE/|WHITE TO PALE TAN, CRYSTALLINE POWDER /HYDROCHLORIDE/|CRYSTALS FROM XYLENE /HYDROCHLORIDE/

SOLN ARE SENSITIVE TO AIR & LIGHT /HYDROCHLORIDE/

P201, P202, P261, P264, P270, P271, P280, P281, P301+P310, P302+P352, P304+P340, P308+P313, P311, P312, P321, P322, P330, P361, P363, P403+P233, P405, P501

H301

Symptoms of overdose include agitation, coma, convulsions, difficulty breathing, difficulty swallowing, dry mouth, extreme sleepiness, fever, intestinal blockage, irregular heart rate, low blood pressure, and restlessness.

...ANTIPSYCHOTIC DRUGS...MAY BLOCK ANTIHYPERTENSIVE EFFECTS OF GUANETHIDINE. PT BEING TREATED WITH PHENOTHIAZINES SHOULD BE ADVISED THAT THEIR SUSCEPTIBILITY TO ALCOHOL MAY BE INCR. /PHENOTHIAZINES/|ADDITIVE TO ACTION OF OTHER DEPRESSANTS & WILL POTENTIATE ANESTHETICS.|MAY INCR TOXICITY OF ORGANOPHOSPHORUS OR OTHER ACETYLCHOLINESTERASE INHIBITORS & PROCAINE. DO NOT USE EPINEPHRINE TO COMBAT ITS HYPOTENSIVE OR DEPRESSANT EFFECTS AS IT POTENTIATES THEM.|CONCURRENT ADMIN OF PHENOTHIAZINES & TRICYCLIC ANTIDEPRESSANTS MAY RESULT IN INCR IN SERUM LEVEL OF EITHER AGENT. /PHENOTHIAZINES/|For more Interactions (Complete) data for TRIFLUPROMAZINE (7 total), please visit the HSDB record page.

Very high (90% or more).

Used mainly in the management of psychoses. Also used to control nausea and vomiting.

Antiemetics; Antipsychotic Agents, Phenothiazine; Dopamine Antagonists|THIS PHENOTHIAZINE IS EFFECTIVE IN MGMNT OF POSTOPERATIVE NAUSEA & VOMITING, RADIATION SICKNESS, & NAUSEA & VOMITING CAUSED BY TOXINS. /HYDROCHLORIDE/|TREATMENT OF ORG BRAIN SYNDROMES, BOTH CHRONIC & ACUTE, IS ANOTHER USE...USE... IN /TREATMENT OF/ MANIA & DEPRESSION HAS MET WITH SOME SUCCESS... ANXIETY IS CONSIDERED...INDICATION FOR USE... /PHENOTHIAZINES/|PHENOTHIAZINES...FAVORABLY MODIFY PATHOGNOMONIC SYMPTOMS OF SCHIZOPHRENIA, THAT IS, THOUGHT DISORDER; BLUNTED AFFECT, WITHDRAWAL, & RETARDATION; & AUTISTIC BEHAVIOR & MANNERISMS. FAVORABLE CHANGES IN BELLIGERENCE, RESISTIVENESS, PERCEPTUAL DISTURBANCES, & PARANOID PROJECTION ALSO OCCUR... /PHENOTHIAZINES/|For more Therapeutic Uses (Complete) data for TRIFLUPROMAZINE (6 total), please visit the HSDB record page.

TRIFLUPROMAZINE PRODUCES LESS SEDATION THAN SOME OTHER PHENOTHIAZINES (EG, PROMAZINE), BUT IT PROLONGS POSTANESTHESIA SLEEPING TIME. EXTRAPYRAMIDAL REACTIONS HAVE BEEN OBSERVED FOLLOWING EVEN SINGLE DOSES OF THIS ALIPHATIC COMPD. /HYDROCHLORIDE/|PHENOTHIAZINES ARE BEST UTILIZED IN CONTROL OF NAUSEA & VOMITING OF SHORT DURATION, SINCE WITH PROLONGED USE INCIDENCE OF MOST OF THEIR ADVERSE EFFECTS INCR. /PHENOTHIAZINES/|...PRECAUTIONS SHOULD BE OBSERVED IN USE OF PHENOTHIAZINES FOR NAUSEA & VOMITING...BECAUSE THEY MAY MASK DIAGNOSTIC SYMPTOMS IN ACUTE SURGICAL CONDITIONS OR NEUROLOGICAL SYNDROMES. /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. /PHENOTHIAZINES/|For more Drug Warnings (Complete) data for TRIFLUPROMAZINE (8 total), please visit the HSDB record page.

4. 4= VERY TOXIC: PROBABLE ORAL LETHAL DOSE (HUMAN) 50-500 MG/KG, BETWEEN 1 TEASPOON & 1 OZ FOR 70 KG PERSON (150 LB). /HYDROCHLORIDE/

TOLERANCE TO VARIOUS ANTIPSYCHOTIC DRUGS & CROSS-TOLERANCE AMONG AGENTS... DEMONSTRABLE IN BEHAVIORAL & BIOCHEM EXPT IN ANIMALS, /ESP/...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 (DEVELOPMENT OF CHOREOATHETOSIS ON ABRUPT DISCONTINUATION OF ANTIPSYCHOTIC DRUGS, ESP FOLLOWING PROLONGED USE OF HIGH DOSES... /PHENOTHIAZINES/

Triflupromazine is a member of a class of drugs called phenthiazines, which are dopamine D1/D2 receptor antagonists. Phenothiazines are used to treat serious mental and emotional disorders, including schizophrenia and other psychotic disorders. It reduces anxiety, emotional withdrawal, hallucinations, disorganized thoughts, blunted mood, and suspiciousness. Triflupromazine is used particularly to control violent behavior during acute episodes of psychotic disorders. It can also be used to control severe nausea and vomiting, severe hiccups, and moderate to severe pain in some hospitalized patients. Triflupromazine acts on the central nervous system.

Drugs used to prevent NAUSEA or VOMITING. (See all compounds classified as Antiemetics.)|Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)|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.)

Absorption may be erratic and peak plasma concentrations show large interindividual differences.|FATE OF SEVERAL (14)C QUATERNARY PHENOTHIAZINES, SUCH AS...TRIFLUPROMAZINE METHIODIDE...HAVE BEEN STUDIED IN RAT. ...MORE OF IP DOSE OF PHENOTHIAZINE WAS EXCRETED IN FECES (VIA BILE). WHERE EXAMINED, NO N-DEALKYLATION OF QUATERNARY NITROGEN WAS DETECTED. /METHIODIDE/

Hepatic.|...METAB...BY OXIDATIVE PROCESSES MEDIATED LARGELY BY HEPATIC MICROSOMAL & OTHER DRUG-METABOLIZING ENZYMES. CONJUGATION WITH GLUCURONIC ACID...PROMINENT ROUTE.../PRC: REACTIONS INCL HYDROXYLATION, DEMETHYLATION, SULFOXIDE FORMATION; METABOLIC ALTERATIONS IN SIDE CHAIN MAY ALSO OCCUR/. /PHENOTHIAZINES/

Triflupromazine binds to the dopamine D1 and dopamine D2 receptors and inhibits their activity. The mechanism of the anti-emetic effect is due predominantly to blockage of the dopamine D2 neurotransmitter receptors in the chemoreceptor trigger zone (CTZ) and vomiting centre. Triflupromazine blocks the neurotransmitter dopamine and the vagus nerve in the gastrointestinal tract. Triflupromazine also binds the muscarinic acetylcholine receptors (M1 and M2) and the tryptamine D receptors (5HT_2B).|...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/|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/

MILD ELEVATION OF TEMP...IF...GIVEN PARENTERALLY. ...HYPOTHERMIA CAN OCCUR & MAY BE DUE BOTH TO ACTION ON HEAT-REGULATING CENTER & TO DIRECT PERIPHERAL VASODILATATION. SENSITIVITY & ADAPTATION TO ENVIRONMENTAL TEMP CHANGE ARE IMPAIRED...FATAL HYPERTHERMIA & HEAT STROKE ARE POSSIBLE COMPLICATIONS. /PHENOTHIAZINES/|...JAUNDICE FOLLOWING PHENOTHIAZINE ADMIN IS HYPERSENSITIVITY MANIFESTATION. ... LEUKOCYTOSIS, LEUKOPENIA, & EOSINOPHILIA OCCUR WITH PHENOTHIAZINE MEDICATION. /PHENOTHIAZINES/|...SKIN DISORDERS ARE ASSOC WITH USE OF PHENOTHIAZINES. FIRST IS HYPERSENSITIVITY REACTION THAT MAY BE URTICARIAL, MACULOPAPULAR, PETECHIAL, OR EDEMATOUS. ...PHOTOSENSITIVITY OCCURS... /PHENOTHIAZINES/|ABNORMAL PIGMENTATION INDUCED BY LONG-TERM ADMIN OF PHENOTHIAZINES IN HIGH DOSES TO CHRONIC SCHIZOPHRENICS HAS BEEN REPORTED. ... PIGMENTARY RETINOPATHY...MAY BE CLOSELY RELATED TOXIC EFFECT OF PHENOTHIAZINES... /PHENOTHIAZINES/|For more Human Toxicity Excerpts (Complete) data for TRIFLUPROMAZINE (9 total), please visit the HSDB record page.

Fluopromazine

TABLET-10, 25, 50 MG; SYRUP-50 MG/5 ML; VIAL-10 MG/ML IN 10 ML; SYRINGE-10 MG/ML.|ORAL SUSPENSION NF: 50 MG/5 ML (HYDROCHLORIDE EQUIVALENT).|ADAZINE, FLUOMAZINA, FLUOROFEN, NIVOMAN, PSYQUIL, SIQUIL, VESPRAL, VESPRIN. /HYDROCHLORIDE/

IDENTIFICATION OF PHENOTHIAZINES & THEIR CORRESPONDING SULFOXIDES & SULFONES BY IN SITU HYDROLYSIS FOLLOWED BY THIN-LAYER CHROMATOGRAPHY.|CHEM IONIZATION BY METHANE; GAS CHROMATOGRAPHY-MASS SPECTROSCOPY OF PURE SAMPLES OF TRIFLUPROMAZINE.|ISOCRATIC MULTI-COLUMN HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY AS TECHNIQUE FOR QUALITATIVE ANALYSIS & ITS APPLICATION TO CHARACTERIZATION OF BASIC DRUGS USING AN AQUEOUS METHANOL SOLVENT.

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