What Is Haloperidol?

1- (4-fluorophenyl) -4- [4- (4-chlorophenyl) -4-hydroxy-1-piperidinyl] -1-butanone

Haloperidol is mainly used for: various acute and chronic schizophrenia. It is particularly suitable for acute puberty and paranoid schizophrenia with hostile emotions and aggressive actions. It can also be used for other types of chronic schizophrenia that are ineffective for phenothiazine treatment. Anxiety neurosis. Children's Tourette Syndrome, also known as Tourette Syndrome (TS), is effective in treating small doses of this product, which can eliminate involuntary movements and reduce and eliminate the accompanying mental symptoms. Vomiting and stubborn hiccups.

Drug name: Haloperidol
Drug type: Essential medicines

English name: Haloperidol
Chinese alias: Haloperidol; Haloperidol; Haloperol
English alias: Serenase; Duraperidol; Halperon

Haloperidol chemical name

1- (4-fluorophenyl) -4- [4- (4-chlorophenyl) -4-hydroxy-1-piperidinyl] -1-butanone

Haloperidol molecular formula

C21H23ClFN02

Haloperidol molecular weight

375

Physicochemical Properties of Haloperidol

White or almost white crystalline powder; odorless and tasteless. Soluble in water. Dissolved in chloroform, slightly soluble in ethanol, slightly soluble in ether, almost insoluble in water.

Haloperidol pharmacology

This product is the main representative of butyrylbenzene antipsychotics. Its effect is similar to chlorpromazine, and it has a strong dopamine receptor antagonistic effect. At the same dose, its antagonism of dopamine receptors is 20 to 40 times that of chlorpromazine, so it belongs to a potent and low-dose antipsychotic. Features are: strong anti-anxiety and anti-psychotic effects, long-term, effective for manic symptoms of schizophrenia and other mental illnesses. The antiemetic effect is also strong, but the sedative effect is weak. The cooling effect is not obvious. The anticholinergic and anti-NA effects are weak, and the cardiovascular system has fewer adverse reactions. Oral absorption is rapid, and the plasma concentration reaches a peak in 3 to 6 hours. t1 / 2typically 21 hours (13 ~ 35 hours). In the liver, about 40% are excreted by the urine within 5 days after a single oral dose. Bile can also be excreted in small amounts.

Haloperidol indication

Mainly used for: various acute and chronic schizophrenia. It is particularly suitable for acute puberty and paranoid schizophrenia with hostile emotions and aggressive actions. It can also be used for other types of chronic schizophrenia that are ineffective for phenothiazine treatment. Anxiety neurosis. Children's Tourette Syndrome, also known as Tourette Syndrome (TS), is effective in treating small doses of this product, which can eliminate involuntary movements and reduce and eliminate the accompanying mental symptoms. Vomiting and stubborn hiccups.

Haloperidol usage and dosage

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

Haloperidol adverse reactions

Extrapyramidal reactions are more common, and reducing the dose can reduce or disappear. Long-term application can cause tardive dyskinesia. Can still cause insomnia, headache, dry mouth and digestive tract symptoms. Long-term use of large doses can cause arrhythmias and myocardial damage.

Haloperidol contraindications

Patients with tremor palsy or severely toxic CNS should not be used. Patients who are allergic to this drug, cardiac insufficiency, myelosuppression, and myasthenia gravis are contraindicated. There have been reports of teratogenicity, which is contraindicated in pregnant women. Not suitable for lactating women.

Haloperidol precautions

It has been reported that respiratory muscle dyskinesia is caused by intramuscular injection, and attention should be paid during application. Use with caution in patients with pulmonary insufficiency. can affect liver function, but can gradually recover after stopping the drug. Use with caution in patients with liver dysfunction. Use with caution in patients with epilepsy, heart disease, glaucoma, renal insufficiency and urinary retention, hyperthyroidism or toxic goiter. Children may cause severe dystonia after medication, so you should take special care.

Haloperidol Drug Interactions

When used in combination with anesthetics, analgesics, and hypnotics, they can be synergistic with each other, and should be reduced in combination. When combined with fluoxetine, it can aggravate extrapyramidal reactions. When used in combination with methyldopa, it can aggravate mental symptoms and should be avoided. When combined with antihypertensive drugs, blood pressure can be excessively reduced. When used in combination with epinephrine, it can cause blood pressure to drop. Use of phenobarbital can reduce the blood concentration of this product.

Haloperidol preparations

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

Haloperidol Pharmacopeia Introduction

[Identification] (1) Take about 1 ml of a saturated sulfuric acid solution of chromium trioxide, place it in a small test tube, and rotate the test tube. The solution should be evenly coated on the wall of the tube. It is applied to the wall of the tube, and similar grease is present on the wall of the tube. (2) The infrared light absorption spectrum of this product should be consistent with the control spectrum (spectrum set 281). (3) Take about 20mg of this product and perform organic destruction according to the oxygen bottle combustion method (Appendix C). Use 5ml sodium hydroxide test solution as the absorption solution. After absorption is complete, add dilute nitric acid to make it acidic, and then slowly boil 2 Minutes, the solution should show a chloride identification reaction (Appendix III). [Check] The clarity of the acidic solution is 50mg, and 10ml of lactic acid solution (0.5-100) is added. After heating and dissolving, the solution should be clear. Related substances are protected from light. Take about 50mg of this product, put it in a 50ml measuring flask, add the mobile phase to dissolve and dilute it to the mark, shake well, and use it as a test solution; precisely measure 1ml, place it in a 100ml measuring bottle, and quantitatively dilute to the mark with the mobile phase, shake As a control solution. Tested according to high performance liquid chromatography (Appendix VD), using octadecylsilane bonded silica as a filler; methanol-0.05mol / L potassium dihydrogen phosphate solution (50:50) (pH adjusted to 4.0 with phosphoric acid) ) Is a mobile phase; the detection wavelength is 220 nm. The retention time of the haloperidol peak is about 13 minutes, and the resolution of the haloperidol peak from the adjacent impurity peaks should meet the requirements. Measure 15µl 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 15µl each of the test solution and the control solution and inject them into the liquid chromatography Record the chromatogram to 2.5 times the retention time of the main component peaks. If there are impurity peaks in 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. Larger than the control solution (1.0%). Any chromatographic peak in the chromatogram of the test solution that is less than 0.05 times the main peak area of the control solution can be ignored. Take this product after losing weight and dry it at 60 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 0.2g of this product, accurately weigh, add 20ml of glacial acetic acid, dissolve at a slight temperature, let cool, add 2 drops of naphthol benzyl alcohol indicator solution, and use perchloric acid titration solution (0.1mol / L) Titrate until the solution appears green, and correct the result of the titration with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol / L) is equivalent to 37.59 mg of C21H23ClFN02. [Category] Antipsychotics. [Storage] shading and sealed. ^[1] ^[2] ^[3] ^[4]