1、锥体外系反应较重且常见，急性肌张力障碍在儿童和青少年更易发生，出现明显的扭转痉挛，吞咽困难，静坐不能及类帕金森病。 2、长期大量使用可出现迟发性运动障碍。 3、可出现口干、视物模糊、乏力、便秘、出汗等。 4、可引起血浆中泌乳素浓度增加，可能有关的症状为：溢乳、男子女性化乳房、月经失调、闭经。 5、少数病人可能引起抑郁反应。 6、偶见过敏性皮疹、粒细胞减少及恶性综合征。
haloperidol
Haloperidol, marketed under the trade name Haldol among others, is a typical antipsychotic medication.[3] Haloperidol is used in the treatment of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, nausea and vomiting, delirium, agitation, acute psychosis, and hallucinations in alcohol withdrawal.[3][4][5] It may be used by mouth or injection into a muscle or a vein.[3] Haloperidol typically works within thirty to sixty minutes.[3] A long-acting formulation may be used as an injection every four weeks in people with schizophrenia or related illnesses, who either forget or refuse to take the medication by mouth.[3]
Haloperidol may result in a movement disorder known as tardive dyskinesia which may be permanent.[3] Neuroleptic malignant syndrome and QT interval prolongation may occur.[3] In older people with psychosis due to dementia it results in an increased risk of death.[3] When taken during pregnancy it may result in problems in the infant.[3][6] It should not be used in people with Parkinson's disease.[3]
Haloperidol was discovered in 1958 by Paul Janssen.[7] It was made from pethidine(meperidine).[8] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[9] It is the most commonly used typical antipsychotic.[10] The yearly cost of the typical dose of haloperidol is about £20–800 in the United Kingdom.[10][11] The annual cost in the United States is around $250.[12] In 2016 it was the 243rd most prescribed medication in the United States with more than 2 million prescriptions.[13]
Medical uses
Haloperidol is used in the control of the symptoms of:
§ Acute psychosis, such as drug-induced psychosis caused by LSD, psilocybin, amphetamines, ketamine,[14] and phencyclidine,[15] and psychosis associated with high fever or metabolic disease. Some evidence, however, has found haloperidol to worsen psychosis due to psilocybin.[16]
§ Adjunctive treatment of alcohol and opioid withdrawal
§ Agitation and confusion associated with cerebral sclerosis
§ Alcohol-induced psychosis
§ Hallucinations in alcohol withdrawal[4]
§ Hyperactive delirium (to control the agitation component of delirium)
§ Hyperactivity, aggression
§ Otherwise uncontrollable, severe behavioral disorders in children and adolescents
§ Schizophrenia[17]
§ Therapeutic trial in personality disorders, such as borderline personality disorder
§ Treatment of intractable hiccups[18][19]
§ Treatment of neurological disorders, such as tic disorders such as Tourette syndrome, and chorea
§ Treatment of severe nausea and emesis in postoperative and palliative care, especially for palliating adverse effects of radiation
Haloperidol was considered indispensable for treating psychiatric emergency situations,[20][21] although the newer atypical drugs have gained a greater role in a number of situations as outlined in a series of consensus reviews published between 2001 and 2005.[22][23][24]
In a 2013 comparison of 15 antipsychotics in schizophrenia, haloperidol demonstrated standard effectiveness. It was 13-16% more effective than ziprasidone, chlorpromazine, and asenapine, approximately as effective as quetiapine and aripiprazole, and 10% less effective than paliperidone.[25] A 2013 systematic review compared haloperidol to placeboin schizophrenia:[26]
Summary
Haloperidol often causes troublesome adverse effects. If there is no other antipsychotic drug, using haloperidol to offset the consequences of untreated schizophrenia is justified. Where a choice of drug is available, however, an alternative antipsychotic with less likelihood of adverse effects such as parkinsonism, akathisia and acute dystonias may be more desirable.[26]
Outcome Findings in words Findings in numbers Quality of evidence
General outcomes
No marked global improvement
Follow-up: >6–24 weeks Haloperidol, when compared with placebo, reduces the chance of experiencing 'no improvement'. Data are based on moderate quality evidence. RR 0.67 (0.58 to 0.78) Moderate
Not discharged from hospital
Follow-up: > 6–24 weeks Haloperidol may reduce the chance of staying in hospital, but, at present it is not possible to be confident about the difference between people receiving haloperidol and people taking placebo. Data supporting this finding are very limited. RR 0.85 (0.47 to 1.52) Very low
Relapse
Follow-up: < 52 weeks Haloperidol may reduce the chance of relapse, but, at present there is only very limited data supporting this finding. RR 0.69 (0.55 to 0.86) Very low
Leaving the study early
Follow-up: > 6–24 weeks Haloperidol probably slightly reduces the risk of loss to follow up, but the difference between the two treatments is not quite clear. Data supporting this finding are based on moderate quality evidence. RR 0.54 (0.29 to 1) Moderate
Adverse effects – movement disorders
Parkinsonism
Follow-up: 3 weeks to 3 months Haloperidol substantially increases the risk of movement disorders. Data are based on moderate quality evidence. RR 5.48 (2.68 to 11.22) Moderate
Missing outcomes
Severe adverse events, such as death, and outcomes such as satisfaction with treatment were not measured/reported in the included studies.
Contraindications
§ Pre-existing coma, acute stroke
§ Severe intoxication with alcohol or other central depressant drugs
§ Known allergy against haloperidol or other butyrophenones or other drug ingredients
§ Known heart disease, when combined will tend towards cardiac arrest[citation needed]
Adverse effects
Sources for the following lists of adverse effects[34][35][36][37]
As haloperidol is a high-potency typical antipsychotic, it tends to produce significant extrapyramidal side effects. According to a 2013 meta-analysis of the comparative efficacy and tolerability of 15 antipsychotic drugs it was the most prone of the 15 for causing extrapyramidal side effects.[25]
With more than 6 months of use 14% percent of users gain weight.[38]
Common (>1% incidence)
§ Extrapyramidal side effects including:
· Akathisia (motor restlessness)
· Dystonia (continuous spasms and muscle contractions)
· Muscle rigidity
· Parkinsonism (characteristic symptoms such as rigidity)
§ Hypotension
§ Anticholinergic side effects such as: (These adverse effects are more common than with lower-potency typical antipsychotics, such as chlorpromazine and thioridazine.)
· Blurred vision
· Constipation
· Dry mouth
§ Somnolence (which is not a particularly prominent side effect, as is supported by the results of the aforementioned meta-analysis.[25])
Unknown frequency
§ Anemia
§ Headache
§ Increased respiratory rate
§ Orthostatic hypotension
§ Prolonged QT interval
§ Visual disturbances
Rare (<1% incidence)
§ Acute hepatic failure
§ Agitation
§ Agranulocytosis
§ Anaphylactic reaction
§ Anorexia
§ Bronchospasm
§ Cataracts
§ Cholestasis
§ Confusional state
§ Depression
§ Dermatitis exfoliative
§ Dyspnea
§ Edema
§ Extrasystoles
§ Face edema
§ Gynecomastia
§ Hepatitis
§ Hyperglycemia
§ Hypersensitivity
§ Hyperthermia
§ Hypoglycemia
§ Hyponatremia
§ Hypothermia
§ Increased sweating
§ Injection site abscess
§ Insomnia
§ Itchiness
§ Jaundice
§ Laryngeal edema
§ Laryngospasm
§ Leukocytoclastic vasculitis
§ Leukopenia
§ Liver function test abnormal
§ Nausea
§ Neuroleptic malignant syndrome
§ Neutropenia
Overdose
Symptoms
Symptoms are usually due to side effects. Most often encountered are:
§ Anticholinergic side effects (dry mouth, constipation, paralytic ileus, difficulties in urinating, decreased perspiration)
§ Coma in severe cases, accompanied by respiratory depression and massive hypotension, shock
§ Hypotension or hypertension
§ Rarely, serious ventricular arrhythmia (torsades de pointes), with or without prolonged QT-time
§ Sedation
§ Severe extrapyramidal side effects with muscle rigidity and tremors, akathisia, etc.
Treatment
Treatment is merely symptomatic and involves intensive care with stabilization of vital functions. In early detected cases of oral overdose, induction of emesis, gastric lavage, and the use of activated charcoal can all be tried. Epinephrine is avoided for treatment of hypotension and shock, because its action might be reversed. In the case of a severe overdose, antidotes such as bromocriptine or ropinirole may be used to treat the extrapyramidal effects caused by haloperidol, acting as dopamine receptor antagonists.[citation needed] ECG and vital signs should be monitored especially for QT prolongation and severe arrhythmias should be treated with antiarrhythmic measures.[17]
Prognosis
In general, the prognosis of overdose is good, provided the person has survived the initial phase. An overdose of haloperidol can be fatal.[43]
