Trifluoperazine

407.5

407.50

204-219-4

214IZI85K3

DTXSID1046928

C62084

N - Nervous system

2934300000

35

4.9

Solid

1.2060 (estimate)

25.0 °C

202-210 °C @ Press: 0.6 Torr

8.76e-03 g/L

Trifluoperazine HCl should be stored at controlled room temperature and protected from light and freezing. Exposure to light may result in discoloration. /Trifluoperazine HCl/

LD50 orally in rats, mice: 542.7, 424.0 mg/ml (Fowler)

pKa1= 3.9; pKa2= 8.1 /Dihydrochloride/

188.1 Ų [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]

PRACTICALLY ODORLESS & HAS BITTER TASTE; MELTS @ ABOUT 242 °C WITH DECOMP WHITE TO PALE-YELLOW, CRYSTALLINE POWDER /HYDROCHLORIDE/

In aqueous solution, trifluoperazine HCl is readily oxidized by atmospheric oxygen. /Trifluoperazine HCl/

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).

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.

Liver test abnormalities have been reported to occur in a high proportion of patients on long term phenothiazine therapy, but elevations are uncommonly above 3 times the upper limit of normal. The aminotransferase abnormalities are usually mild, asymptomatic and transient, reversing even with continuation of medication. Rare instances of clinically apparent acute liver injury, resembling that due to chlorpromazine, have been reported with trifluoperazine therapy. The onset of jaundice is usually within 1 to 4 weeks, and the pattern of serum enzyme elevations is typically cholestatic or mixed. Immunoallergic features (rash, fever and eosinophilia) were present in some cases but were mild and self-limited; autoantibodies were rare.

Additive QT interval prolongation may increase the risk of ventricular tachycardia when /probucol is used with phenothiazines/. /Phenothiazines/|Concurrent use /of other photosensitizing medications/ with phenothiazines may cause additive photosensitizing effects. In addition, concurrent use of systemic methoxsalen, trixsalen, or tetracyclines with phenothiazines may potentiate intraocular photochemical damage to the choroid, retina, or lens. /Phenothiazines/|Prior administration of phenothiazines may decrease the pressor effect and shorten the duration of action of phenylephrine. /Phenothiazines/|In addition to increased CNS and respiratory depression, concurrent use /of opiod (narcotic) analgesics/ with phenothiazines increases orthostatic hypotension and increases the risk of severe constipation, which may lead to paralytic ileus, and/or urinary retention. /Phenothiazines/|For more Interactions (Complete) data for TRIFLUOPERAZINE (29 total), please visit the HSDB record page.

LD50 Mouse ip 175 mg/kg

... TRIFLUOPERAZINE HAS A HIGH TENDENCY TO PRODUCE EXTRAPYRAMIDAL EFFECTS ... EXTRAPYRAMIDAL SYMPTOMS PRESENTING AS TORTICOLLIS, STIFFENING OF THE BODY, SPASTICITY, IMPAIRED SPEECH, AND OPISTHOTONOS MAY OCCUR. THESE SYMPTOMS MAY OCCUR FREQUENTLY IN CHILDREN WHO HAVE BEEN ADMINISTERED PROCHLORPERAZINE (cOMPAZINE) FOR THE TREATMENT OF NAUSEA AND VOMITING. /PHENOTHIAZINES/

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

For the treatment of anxiety disorders, depressive symptoms secondary to anxiety and agitation.

Trifluoperazine is a phenothiazine and antipsychotic agent that no longer commonly used in clinical practice. Trifluoperazine is a rare cause of clinically apparent acute cholestatic liver injury.

Antipsychotic Agents

Antiemetics; Antipsychotic Agents, Phenothiazine; Dopamine Antagonists|IN THE TREATMENT OF ACUTE PSYCHOSES, THE DOSE OF ANTIPSYCHOTIC DRUG IS INCREASED DURING THE FIRST FEW DAYS TO ACHIEVE CONTROL OF SYMPTOMS. THE DOSE IS THEN ADJUSTED DURING THE NEXT SEVERAL WEEKS AS THE PATIENT'S CONDITION WARRANTS. /PHENOTHIAZINES/|The use of antipsychotic drugs in mania and depression has met with some success. /PHENOTHIAZINES/|...TRIFLUOPERAZINE...REPORTED EFFECTIVE IN SEVERELY IMPAIRED AUTISTIC CHILDREN, & DIFFERENTIAL DIAGNOSIS OF THIS GROUP FROM SO-CALLED MINIMAL-BRAIN-DAMAGE (MBD) SYNDROME IN CHILDREN IS ESSENTIAL.|For more Therapeutic Uses (Complete) data for TRIFLUOPERAZINE (10 total), please visit the HSDB record page.

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/|...FEW PT WITH ANGINA PECTORIS HAVE REPORTED INCR PAIN DURING THERAPY WITH TRIFLUOPERAZINE. THEREFORE, PT WITH ANGINA SHOULD BE OBSERVED CAREFULLY & DRUG WITHDRAWN IF UNFAVORABLE RESPONSE OCCURS. /HYDROCHLORIDE/|SAFE USE...DURING PREGNANCY HAS NOT BEEN ESTABLISHED WITH RESPECT TO POSSIBLE ADVERSE EFFECTS ON FETAL DEVELOPMENT. ...PHENOTHIAZINES... SHOULD BE USED WITH EXTREME CAUTION IN PT WITH HISTORY OF GLAUCOMA OR PROSTATIC HYPERTROPHY. /PHENOTHIAZINES/|ROUTINE ADMIN OF ANTIPARKINSONISM AGENTS SHOULD BE AVOIDED WITH MOST ANTIPSYCHOTIC DRUG REGIMENS. /PHENOTHIAZINES/|For more Drug Warnings (Complete) data for TRIFLUOPERAZINE (28 total), please visit the HSDB record page.

Lethal dose: 0.3-0.8 mg/dL /From table/

Therapeutic or normal dose: 80 ug/dL; Toxic dose: 120-300 ug/dL /From table/

Trifluoperazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Trifluoperazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.

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 used to prevent NAUSEA or VOMITING. (See all compounds classified as Antiemetics.)|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.)

ULTIMATE SOJOURN OF PHENOTHIAZINE DRUGS IN BODY IS EXCEEDINGLY LONG. /PHENOTHIAZINES/

Hepatic.|AFTER CHRONIC ADMIN OF PIPERAZINE-SUBSTITUTED PHENOTHIAZINE DRUGS...TO RATS, TISSUES CONTAINED DRUG METABOLITES, IN WHICH PIPERAZINE RING FISSION BY MULTIPLE OXIDATIVE N-DEALKYLATION HAD OCCURRED TO GIVE SUBSTITUTED ETHYLENEDIAMINE. ...2-TRIFLUOROMETHYL ANALOGUE WAS FORMED SIMILARLY FROM TRIFLUPERAZINE.|IN VIVO DEGRADATION OF PIPERAZINE RING OF TRIFLUOPERAZINE LEADS TO FORMATION OF GAMMA-(PHENOTHIAZINYL-10)-PROPYLAMINE & ITS RING SUBSTITUTED ANALOGS CF3- & CL-. SULFOXIDES OF THESE METABOLITES HAVE BEEN IDENTIFIED AS URINARY BIOTRANSFORMATION PRODUCTS IN RATS (CHRONIC).

10-20 hours

Trifluoperazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.|...PHENOTHIAZINES, BLOCK DOPAMINE RECEPTORS & INCR TURNOVER RATE OF DOPAMINE IN CORPUS STRIATUM. INCR TURNOVER RATE IS BELIEVED TO BE RESULT OF NEURONAL FEEDBACK MECHANISM. ...OF IDENTIFIED DOPAMINERGIC NEURONS IN SUBSTANTIA NIGRA & VENTRAL TEGMENTAL AREAS. SPONTANEOUS FIRING OF THESE CELLS IS INCR... /PHENOTHIAZINES/

EXTRAPYRAMIDAL SYMPTOMS...RELIEVED WITH BARBITURATES, METHYLPHENIDATE HYDROCHLORIDE...ANTI-PARKINSON DRUGS...BENZTROPINE MESYLATE...TRIHEXYPHENIDYL HYDROCHLORIDE...DIPHENHYDRAMINE HYDROCHLORIDE...IN SEVERE CASES, SUPPORTIVE THERAPY...MAINTAINING CLEAR AIRWAY & ADEQUATE HYDRATION. /HYDROCHLORIDE/

EPITHELIAL KERATOPATHY OFTEN IS OBSERVED IN PATIENTS ON LONG-TERM THERAPY WITH CHLORPROMAZINE, AND OPACITIES IN THE CORNEA AND IN THE LENS OF THE EYE ALSO HAVE BEEN NOTED. ... PIGMENTARY RETINOPATHY HAS BEEN REPORTED, PARTICULARLY FOLLOWING DOSES OF THIORIDAZINE IN EXCESS OF 1000 MG/DAY; A MAXIMUM DAILY DOSE OF 800 MG CURRENTLY IS RECOMMENDED. /PHENOTHIAZINES/|...OCULOGYRIC CRISES CAN BE PRODUCED... BLURRING OF VISION HAS BEEN MENTIONED OCCASIONALLY, ASSOC WITH DRYNESS OF MOUTH, WHICH SUGGESTS THAT BLURRING MIGHT BE DUE TO ANTICHOLINERGIC MYDRIASIS & CYCLOPLEGIA. ...SUSPICIONS...THAT TRIFLUOPERAZINE PRODUCES DEPOSITS IN LENS OR CORNEA.|LARGE DOSES (80 MG TRIFLUOPERAZINE) ARE MORE LIKELY TO PRODUCE OR AGGRAVATE DYSKINESIA IN PT AGE 40-55 THAN ARE CONVENTIONAL DOSES. RISK OF PERSISTENT MOTOR ABNORMALITIES RISES SHARPLY IN OLDER PERSONS WITH CHRONIC DOSING OF 100-200 MG CHLORPROMAZINE OR EQUIV.|Most studies indicate the phenothiazines are nonteratogenic but there are reports of defects in infants exposed to these drugs during the first trimester. /Phenothiazines/|For more Human Toxicity Excerpts (Complete) data for TRIFLUOPERAZINE (7 total), please visit the HSDB record page.

Apo Trifluoperazine

TABLET: 1, 2, 5, 10 MG; CAPSULE: 10 MG/ML; VIAL: 2 MG/ML IN 10 ML. /FROM TABLE, HYDROCHLORIDE/|SYRUP NF: 10 MG/ML /HYDROCHLORIDE/

THE NATURE OF SUBSTITUENT @ POSITION 10 ALSO INFLUENCES PHARMACOLOGICAL ACTIVITY. ... SEVERAL POTENT PHENOTHIAZINE ANTIPSYCHOTIC COMPOUNDS HAVE A PIPERAZINE (OR PIPERAZINYL) GROUP IN THE SIDE CHAIN; ... TRIFLUOPERAZINE /IS AN/ EXAMPLE.|Phenothiazine has a three-ring structure in which two benzene rings are linked by a sulfur and a nitrogen atom. If the nitrogen at position 10 is replaced by a carbon atom with a double bond to the side chain, the compound is a thioxanthene. /PHENOTHIAZINES/

THIN-LAYER CHROMATOGRAPHY.|DIFFERENCE UV SPECTROMETRIC TECHNIQUE BASED ON ABSORBANCE OF SULFOXIDE DERIVATIVE OF PHENOTHIAZINES.|DETECTION LIMIT 10-1000 PPB.

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