트리플루프로마진

Pharmaceuticals -> Listed in ZINC15

Pharmaceuticals -> Nervous system -> Antipsychotics

5.2

5.17

SOL IN WATER, ALC, & ACETONE; INSOL IN ETHER /HCL/

PRACTICALLY INSOL IN WATER

1.80e-03 g/L

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

Pharmaceuticals

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/

Danger

H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]

P203, P261, P262, P264, P270, P271, P280, P301+P316, P302+P352, P304+P340, P316, P318, P321, P330, P361+P364, P403+P233, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 38 reports by companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

...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.

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).

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.

N - Nervous system

QN - Nervous system

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.

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/

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/

Hepatic.

Drugs used to prevent NAUSEA or VOMITING.

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.

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.

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/

MEDICATION (VET)

MEDICATION

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

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/