What Is Perphenazine?

4- [3- (2-chlorophenothiazine-1o-yl) propyl] -1-piperazine ethanol

Fenaijing is used to treat paranoid psychosis, reactive psychosis, symptomatic mental illness, simple type and chronic schizophrenia. It is also used for the treatment of nausea, vomiting, hiccups, etc. Those with neurosis with anxiety and tension symptoms can also be treated with small doses and other drugs.
Drug name
Perennial
Drug type
Essential medicines
English name
Perphenazine
Chinese alias
Dropericin; Perphenazine; Panfenazine
English alias
Perphenan; Trilafon; Trilifan

Perphenazine chemical name

4- [3- (2-chlorophenothiazine-1o-yl) propyl] -1-piperazine ethanol

Molecular structure of perphenazine

Perphenazine molecular formula

C21H26ClN30S

Perphenazine molecular weight

403

Physiochemical Properties

This product is white to light yellow crystalline powder; almost odorless, slightly bitter. This product is very soluble in chloroform, easily soluble in methanol, soluble in ethanol, and almost insoluble in water; soluble in dilute hydrochloric acid. Melting point The melting point of this product (Appendix VI C) is 94 ~ 100 ° C.

Perphenazine Pharmacology

This product is a piperazine derivative of phenothiazines. The pharmacological effect is similar to chlorpromazine, but its antipsychotic and antiemetic effects are strong, while its sedative effects are weak. Low toxicity. Effective on symptoms such as hallucinations, delusions, anxiety, nervousness, agitation, etc .: The effect on dopamine receptors is the same as that of chloropropane, and its extrapyramidal adverse reactions are more obvious; the effect on norepinephrine receptors is smaller, so the effect on blood pressure Not big. Intramuscular injection of this product is effective for 10 minutes in the treatment of acute psychosis, the maximum effect is 1 to 2 hours, and the effect can last for 6 hours. Oral absorption is slow and irregular, bioavailability is 20%, and the peak time is 4-8 hours. It is mainly metabolized in the liver. There is a clear first pass effect in the liver and there is enterohepatic circulation.

Perphenazine indications

For the treatment of paranoid psychosis, reactive psychosis, symptomatic psychosis, simple type and chronic schizophrenia. It is also used for the treatment of nausea, vomiting, hiccups, etc. Those with neurosis with anxiety and tension symptoms can also be treated with small doses and other drugs.

Perphenazine Usage and Dosage

Due to different dosage forms and specifications, please read the drug instructions carefully or follow the doctor's advice.

Perphenazine adverse reactions

Common extrapyramidal reactions are usually relieved by taking benzetholide. Tardive dyskinesia can also occur with long-term use. Few patients have palpitations, tachycardia, dry mouth, nausea, vomiting, constipation, frequent urination, changes in appetite, and weight gain. Orthostatic collapse can sometimes occur. Occasionally, rash, allergic dermatitis, obstructive jaundice, and ST-T wave changes in electrocardiogram.

Perphenazine contraindications

Those who are allergic to phenothiazines, those with liver dysfunction, those with hematological disease, myelosuppression, glaucoma, Parkinson's disease and Parkinson's syndrome are prohibited.

Perennial cautions

Use with caution in pregnant women and lactating women.

Perphenazine drug interactions

Combined with pethidine can strengthen the sedative or analgesic effect of this product. It can enhance the adverse reactions of monoamine oxidase inhibitors, tricyclic antidepressants, propranolol and phenytoin. In combination with fluoxetine, paroxetine, sertraline, severe acute Parkinson's syndrome may occur. Combined with lithium, it can lead to weakness, dyskinesia, enhanced extrapyramidal response, encephalopathy and brain damage. can reduce the efficacy of amphetamine, guanethidine, anticonvulsants and levodopa. Combination with tramadol can cause seizures. can reverse the effects of adrenaline and cause severe hypotension.

Perphenazine

Tablet: 2mg, 4mg; Injection: 1ml: 5mg

Introduction of Perphenazine Pharmacopoeia

[Identification] (1) Take 5mg of this product, add 1ml each of hydrochloric acid and water, heat to 80 , add a few drops of hydrogen peroxide solution, it will be dark red; after standing, the red gradually fades. (2) Take this product, add methanol to dissolve and dilute it to make a solution containing 10 µg per ml. According to ultraviolet-visible spectrophotometry (Appendix IV A), it has the maximum absorption at the wavelengths of 258nm and 313nm. The ratio of absorbance at 258nm should be 0.12 to 0.13. (3) The infrared light absorption spectrum of this product should be consistent with the control spectrum (spectrum set 243). [Inspection] Clarity and color of methanol solution: 0.20g of this product. After dissolving in 10ml of methanol, the solution should be clear and colorless; if color develops, compare with yellow standard colorimetric solution No. 2 (Appendix A first method), Must not be deeper. Related substances are protected from light. Take an appropriate amount of this product, add methanol to dissolve and dilute it to make a solution containing 1mg per lml as the test solution; take 1ml of precise amount, place it in a 100ml volumetric flask, dilute to the mark with methanol, shake well, and use it as a control solution. According to the high performance liquid chromatography (Appendix VD) test, octadecylsilane bonded silica gel was used as the filler; methanol was used as the mobile phase A, and 0.03mol / L ammonium acetate solution was used as the mobile phase B. Gradient elution, detection wavelength is 254nm. Take 25mg of perphenazine reference product, place it in a 25ml volumetric flask, add 15ml of methanol to dissolve, add 2ml of 30% hydrogen peroxide solution, shake well, dilute to the mark with methanol, shake and place. 1.5 hours, as the system suitability test solution; take 20µl of the system suitability test solution and inject it into the liquid chromatograph, so that the retention time of perphenazine peak is about 27 minutes, and the resolution of the peak of degradation impurities with a relative retention time of about 0.73 should be Greater than 7.0. Take 20l of the control solution and inject it into the liquid chromatograph, adjust the detection sensitivity so that the peak height of the main component chromatographic peak is about 20% of the full range; and then accurately measure 20l each of the test solution and the control solution, and inject them into the liquid chromatography. Instrument, record the chromatogram. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak must not be greater than 0.5 times (0.5%) the main peak area of the control solution, and the sum of the peak areas of each impurity must not be greater than 2 times (2.0%) the main peak area of the control solution . Any chromatographic peak in the chromatogram of the test solution that is less than 0.01 times the area of the main peak of the control solution can be ignored.
Take this product after losing weight, put it in a phosphorus pentoxide dryer, and dry it under reduced pressure to constant weight. The weight loss should not exceed 0.5% (Appendix L). The ignition residue shall not exceed 0.1% (Appendix N). [Content determination] Take about 0.15g of this product, weigh it accurately, add 20ml of glacial acetic acid to dissolve, add 1 drop of crystal violet indicator solution, and titrate with perchloric acid titration solution (0.1mol / L) until the solution is blue-green, The results of the titration are corrected with a blank test. Each 1ml of perchloric acid titration solution (0.1mol / L) is equivalent to 20.20mg of C21H26C1N30S. [Category] Antipsychotics. [Storage] shading and sealed.
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