What Is Trifluoperazine?

Triflurazine is an oral drug that is mainly used for the treatment of mental illness. It is better for acute and chronic schizophrenia, especially for delusional and nervous types.

Chinese name: Triflurazine
Foreign name: trifluoperazine

EINECS number: 204-219-4
CAS number: 117-89-5

Triflurazine Basic Information

Chinese name: triflurazine

Chinese alias: 10- [3- (4-methylpiperazin-1-ylpropyl] -2-trifluoromethyl-10H-phenothiazine; trifluoropyrazine

English name: Trifluoperazine

English alias: Trifluperazine; Trifluoperazina; triphthazine dihydrochloride; Flurazine; Trifluoperazine;

Triflurin; 10- [3- (4-methylpiperazin-1-yl) propyl] -2- (trifluoromethyl) phenothiazine; Triftazin; Trifluoroperazine; Triperazine; Stelazine; Trifluoperazin; NOVO-TRIFLUZINETM; trifluoroperazine hydrochloride; trifluoroperazine dihydrochloride

CAS number: 117-89-5

Molecular formula: C ₂₁ H ₂₄ F ₃ N ₃ S

Molecular weight: 407.49600

Exact mass: 407.16400

PSA: 35.02000

LogP: 4.88640

Physicochemical properties of triflurazine

Appearance and properties: white to light yellow crystalline powder

Density: 1.239g / cm ³

Boiling point: 506ºC at 760mmHg

Vapor pressure: 2.32E-10mmHg at 25 ° C

Flash point: 158.3ºC

Storage conditions: -20 ^[1]

Triflurazine Safety Information

Customs code: 2934300000

Triflurazine molecular structure data

1. Molar refractive index: 108.15

2. Molar volume (cm3 / mol): 328.7

3. Isometric Zhang Rongrong (90.2K): 828.8

4. Surface tension (dyne / cm): 40.3

5. Polarizability (10-24cm3): 42.87

Calculated Chemical Data for Triflurazine

1. Hydrophobic parameter calculation reference value (XlogP): None

2.Number of hydrogen bond donors: 0

3.Number of hydrogen bond acceptors: 7

4.Number of rotatable chemical bonds: 4

5.Number of tautomers: none

6. Topological molecular polar surface area 35

7.Number of heavy atoms: 28

8.Surface charge: 0

9.Complexity: 510

10.Number of isotope atoms: 0

11. Determine the number of atomic stereocenters: 0

12. Uncertain number of atomic stereocenters: 0

13. Determine the number of chemical bond stereocenters: 0

14. Uncertain number of chemical bond stereocenters: 0

15. Number of covalent bond units: 1 ^[2]

Triflurazine Triflurazine Related Drug Sheet Information

Pharmacological effects of triflurazine

This product is a phenothiazine with a piperazine side chain. The effect is similar to chlorpromazine, but the antipsychotic and antiemetic effects are strong, and extrapyramidal reactions are more common. It has a good effect on eliminating hallucinations, delusions, and improving the symptoms of stagnation, stiffness, apathy, and withdrawal, and it has a poor effect on the symptoms of excitement and mania. It is effective for non-psychiatric affective disorders such as anxiety and nervousness, but it is usually only used in patients who develop tolerance to benzodiazepines, and low doses should be used for short periods. This product can also control nausea and vomiting.

Triflurazine drug interactions

1. Combination with alcohol or central nervous system inhibitors (barbiturates, benzodiazepines, sedatives, muscle relaxants, anesthetics, analgesics) or tricyclic antidepressants can cause excessive sleepiness. 2. Can reduce the efficacy of amphetamine, anticonvulsants and levodopa. 3. It can aggravate the adverse reactions of adrenaline, monoamine oxidase inhibitors, metoprolol, phenytoin sodium and tricyclic antidepressants. 4. Trifluoperazine and monoamine oxidase inhibitors should be used separately at least 14 days apart. 5. Lithium salt can reduce the efficacy of triflurazine and increase adverse reactions. 6. Combined with methyldopa can increase blood pressure.

Triflurazine pharmacokinetics

The drug is easily absorbed by oral administration, and the peak time is 2 to 4 hours. A single administration can last for 24 hours. Because this drug is highly fat soluble, its concentration in the central nervous system exceeds its plasma concentration. Easily penetrates the placental barrier. The total protein binding rate was 90% to 99%. A variety of active metabolites are produced in the liver through oxidation, and these active metabolites are excreted through the urine. Partially excreted by feces. The elimination half-life of the parent compound is 24 h. Cannot be ruled out by hemodialysis.

Triflurazine dosage forms and specifications

1. Tablet: 1mg, 5mg; 2. Injection (powder): 1mg.

Triflurazine indication

1. For acute and chronic schizophrenia, especially delusional and nervous. 2. For non-psychiatric affective mood disorders: Usually only used in patients who develop tolerance to benzodiazepines, and low doses should be used short-term. 3. Used to control nausea and vomiting.

Triflurazine contraindications

1. Blood diseases. 2. Myelosuppression. 3. Coma. 4. Those with a history of liver damage are disabled.

Triflurazine precautions

1. Use with caution: (1) cardiovascular disease; (2) retinopathy and glaucoma; (3) malignant syndrome caused by nerve blockers. 2. The effects of drugs on the elderly: elderly patients should not be used. General elderly patients should reduce the amount. 3. The effects of the drug on pregnancy: This drug can penetrate the placental barrier. The FDA classifies pregnancy as Class C. 4. The effect of the drug on breastfeeding: It is unclear whether the drug can be excreted through milk. 5. The effect of the drug on the test value or diagnosis: may cause false positives in early pregnancy tests.

Triflurazine adverse reactions

1. The incidence of extrapyramidal reactions is 60%. Slight: blurred vision, constipation, less sweat, diarrhea, dizziness, drowsiness, dry mouth, fatigue, irritability, menstrual disorders, nasal congestion, restlessness, vomiting, weight gain. These adverse reactions can disappear as the body adapts to the drug. 3. Severe: Be sure to tell your doctor about any persistent or troublesome adverse reactions, such as breast swelling (including men and women), chest pain, convulsions, pigmentation, difficulty swallowing or breathing, salivation; dizziness, fever, impotence, no Voluntary movements (face, jaw, mouth, tongue), palpitations, rashes, sleep disturbances, sore throat, suicidal tendency, tremors, dyskinesias, abnormal bleeding and bruising, visual disturbances, yellowing of the skin or eyes.

Triflurazine Usage and Dosage

1. Treatment of mental illness: Start oral 5mg, 2 times a day, and then gradually increase to the usual dose of 15-20mg daily, divided into doses, severe patients can use 40mg per day. Deep intramuscular injection can alleviate the symptoms of acute psychosis, 1 ~ 3mg per day, divided into intramuscular injections. 2. Control nausea and vomiting: 1-2mg, 2 times a day, up to 6mg a day, in divided doses.

Evaluation of the efficacy of triflurazine

The stabilization effect is stronger than chlorpromazine, the effect is faster, and the maintenance time is longer; the hypnotic and sedative effects and the antihistamine and antispasmodic effects are weaker. The antipsychotic effect is more than 20 times stronger than chlorpromazine. For association disorders, mania, emotional euphoria, the effect is poor ^[3] .