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Encyclopedia > Haloperidol
Haloperidol
Systematic (IUPAC) name
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-
1-(4-fluorophenyl)-butan-1-one
Identifiers
CAS number 52-86-8
ATC code N05AD01
PubChem 3559
DrugBank APRD00538
Chemical data
Formula C21H23ClFNO2 
Mol. mass 375.90 (plain haloperidol)
Pharmacokinetic data
Bioavailability approx. 60 to 70% (tablets and liquid)
Metabolism hepatic
Half life 12 to 36 hours
Excretion biliar/urine
Therapeutic considerations
Pregnancy cat.

C Image File history File links Haloperidol. ... Image File history File links Download high-resolution version (1100x433, 131 KB) File links The following pages on the English Wikipedia link to this file (pages on other projects are not listed): Tourette syndrome Haloperidol Wikipedia:Featured article candidates/Featured log Wikipedia:Featured article candidates/Tourette syndrome Wikipedia:Featured article... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... This article does not cite its references or sources. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Standard atomic weight 12. ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, Symbol, Number chlorine, Cl, 17 Chemical series halogens Group, Period, Block 17, 3, p Appearance yellowish green Standard atomic weight 35. ... General Name, Symbol, Number fluorine, F, 9 Chemical series halogens Group, Period, Block 17, 2, p Appearance Yellowish brown gas Atomic mass 18. ... General Name, Symbol, Number nitrogen, N, 7 Chemical series nonmetals Group, Period, Block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... General Name, Symbol, Number oxygen, O, 8 Chemical series nonmetals, chalcogens Group, Period, Block 16, 2, p Appearance colorless (gas) very pale blue (liquid) Standard atomic weight 15. ... The molecular mass (abbreviated MM) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... It has been suggested that Effective half-life be merged into this article or section. ... Excretion is the process of eliminating waste products of metabolism and other materials that are of no use. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ...

Legal status

Prescription only The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ...

Routes oral, IM, IV, decanoate

Haloperidol (sold under the tradenames Aloperidin, Bioperidolo, Brotopon, Dozic, Duraperidol (Germany), Einalon S, Eukystol, Haldol, Halosten, Keselan, Linton, Peluces, Serenace, Serenase, Sigaperidol) is a conventional, or typical, butyrophenone antipsychotic drug. It was developed in 1957 by the Belgian company Janssen Pharmaceutica and submitted to first clinical trials in Belgium in the same year. After being rejected by U.S. company Searle due to side effects, it was later marketed in the U.S. by McNeil Laboratories. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... Look up IM, im, Im in Wiktionary, the free dictionary. ... Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... The decanoate ion is the conjugate base of decanoic acid, with formula C9H19COO−. Decanoate compounds include salts and esters of decanoic acid, such as sodium decanoate or methyl decanoate. ... Typical antipsychotics (sometimes referred to as conventional antipsychotics or conventional neuroleptics) are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis (in particular, schizophrenia), and are generally being replaced by atypical antipsychotic drugs. ... The most successful treatment approaches combine the use of drugs, psychotherapy, and supportive therapy. ... The term antipsychotic is applied to a group of drugs used to treat psychosis. ... Oral medication A medication is any drug taken to cure or reduce the symptoms of an illness or ongoing medical condition. ... Johnson & Johnson NYSE: JNJ is an international pharmaceutical, medical devices and consumer packaged goods manufacturer founded in 1885. ... Motto: (Out Of Many, One) (traditional) In God We Trust (1956 to date) Anthem: The Star-Spangled Banner Capital Washington D.C. Largest city New York City None at federal level (English de facto) Government Federal constitutional republic  - President George Walker Bush (R)  - Vice President Dick Cheney (R) Independence from... G.D. Searle & Company was a company focusing on life sciences, specifically pharmaceuticals, agriculture, and animal health. ... The company was founded on March 17, 1879 by 23 year old Robert McNeil, who paid US $167 for a drugstore complete with fixtures, inventory and soda fountain, as a retail pharmacy, in the Kensington section of Philadelphia, PA, USA. Robert McNeil was a graduate of the Philadelphia College of...

Contents

Chemistry

Haloperidol is an odourless white to yellow crystalline powder. Its chemical name is 4-[4-(p-chlorophenyl)-4-hydroxypiperidino]-4'-fluorobutyrophenone and its empirical formula is C21H23ClFNO2


Pharmacology

Haloperidol is a neuroleptic and a butyrophenone. Due to its strong central antidopaminergic action, it is classified as a highly potent neuroleptic. It is approximately 50 times more potent than chlorpromazine on a weight basis (50mg chlorpromazine are equivalent to 1mg haloperidol). Haloperidol possesses a strong activity against delusions and hallucinations, most likely due to an effective dopaminergic receptor blockage in the mesocortex and the limbic system of the brain. It blocks the dopaminergic action in the nigrostriatal pathways, which is the probable reason for the high frequency of extrapyramidal-motoric side-effects (dystonias, akathisia, pseudoparkinsonism). It has minor antihistaminic and anticholinergic properties, therefore cardiovascular and anticholinergic side-effects such as hypotension, dry mouth, constipation, etc., are seen quite infrequently, compared with less potent neuroleptics such as chlorpromazine. Haloperidol also has sedative properties and displays a strong action against psychomotor agitation, due to a specific action in the limbic system. It therefore is an effective treatment for mania and states of agitation. Additionally, it can be given as an adjuvant in the therapy of severe chronic pain. The term antipsychotic is applied to a group of drugs used to treat psychosis. ... The most successful treatment approaches combine the use of drugs, psychotherapy, and supportive therapy. ... Chlorpromazine was the first antipsychotic drug, used during the 1950s and 1960s. ... A delusion is commonly defined as a false belief, and is used in everyday language to describe a belief that is either false, fanciful or derived from deception. ... A hallucination is a false sensory perception in the absence of an external stimulus, as distinct from an illusion, which is a misperception of an external stimulus. ... Dopamine is a phenethylamine naturally produced by the human body. ... The limbic system within the brain. ... The nigrostriatal pathway is a neural pathway which connects the substantia nigra with the striatum. ... In human anatomy, the extrapyramidal system is a neural network located in the brain that is part of the motor system involved in the coordination of movement. ... This article or section does not cite its references or sources. ... // Choline is a nutrient, essential for cardiovascular and brain function, and for cellular membrane composition and repair. ... The circulatory system or cardiovascular system is the organ system which circulates blood around the body of most animals. ... In physiology and medicine, hypotension refers to an abnormally low blood pressure. ... Xerostomia is the medical term for a dry mouth due to a lack of saliva. ... Constipation or irregularity, is a condition of the digestive system where a person (or animal) experiences hard feces that are difficult to egest; it may be extremely painful, and in severe cases (fecal impaction) lead to symptoms of bowel obstruction. ... A sedative is a substance which depresses the central nervous system (CNS), resulting in calmness, relaxation, reduction of anxiety, sleepiness, slowed breathing, slurred speech, staggering gait, poor judgment, and slow, uncertain reflexes. ... The limbic system within the brain. ... Mania is a severe medical condition characterized by extremely elevated mood, energy, and thought patterns. ... In medicine, adjuvants are agents which modify the effect of other agents while having few if any direct effects when given by themselves. ...


The peripheral antidopaminergic effects of haloperidol account for its strong antiemetic activity. There, it acts at the chemoreceptor trigger zone (CTZ). Haloperidol is useful to treat severe forms of nausea/emesis such as those resulting from chemotherapy. The peripheral effects lead also to a relaxation of the gastric sphincter muscle and an increased release of the hormone prolactin, with the possible emergence of breast enlargement and secretion of milk (lactation) in both sexes. The Chemoreceptor trigger zone (CTZ) is an area of the brain which receives inputs from blood-borne drugs or hormones, and communicates with the Vomit Centre, to initiate vomiting. ... Chemotherapy is the use of chemical substances to treat disease. ... Look up Sphincter in Wiktionary, the free dictionary. ... Prolactin (PRL) is a peptide hormone primarily associated with lactation. ... Kittens nursing Lactation describes the secretion of milk from the mammary glands, the process of providing that milk to the young, and the period of time that a mother lactates to feed her young. ...


Pharmacokinetics

Intramuscular injections

The drug is well and rapidly absorbed and has a high bioavailability. Plasma-levels reach their maximum within 20 minutes after injection. The decanoate injectable formulation is for intramuscular administration only and should never be used intraveneously.


Intravenous injections

The bioavailability is 100% and the very rapid onset of action is seen within about ten minutes. The duration of action is 3 to 6 hours. If haloperidol is given as slow IV infusion, the onset of action is retarded, but the duration prolonged compared to IV injection.


Therapeutic concentrations

Plasma levels of 4 micrograms per liter to 20 (up to 25) micrograms per liter are required for therapeutic action. The determination of plasma levels can be used to decide about dose adjustments and to check compliance, particular in long-term patients. Plasma levels in excess of the therapeutic range may lead to a higher incidence of side-effects or even pose the risk of haloperidol intoxication.


Uses

Haloperidol is used in the control of the symptoms of:

  • Acute psychosis, such as drug psychosis (LSD, amphetamines, PCP), psychosis associated with high fever or metabolic disease
  • Acute and chronic schizophrenia
  • Acute manic phases until the concomitantly given first-line drugs such as lithium or valproate are effective
  • Hyperactivity, aggression.
  • Acute delirium
  • Otherwise uncontrollable severe behavioral disorders in children and adolescents
  • Agitation and confusion associated with cerebral sclerosis
  • Adjunctive treatment of alcohol and opioid withdrawal
  • Treatment of neurological disorders such as tics, Tourette syndrome, and chorea
  • Treatment of severe nausea/emesis (postoperative, side-effects of radiation and cancer chemotherapy)
  • Adjunctive treatment of severe chronic pain, always together with analgesics
  • Therapeutic trial in personality disorders such as borderline personality disorders
  • Also used in the treatment of Intractable hickups

Some weeks or even months of treatment may be needed before a remission of schizophrenia is evident. Psychosis is a generic psychiatric term for a mental state often described as involving a loss of contact with reality. Stedmans Medical Dictionary defines psychosis as a severe mental disorder, with or without organic damage, characterized by derangement of personality and loss of contact with reality and causing deterioration... Mania is a severe medical condition characterized by extremely elevated mood, energy, and thought patterns. ... Hyperactivity can be described as a state in which a person is abnormally easily excitable and exuberant. ... Aggression is sometimes used to intimidate and coerce during extremely rigorous physical training. ... “Delirious” redirects here. ... Multiple sclerosis (MS) is a demyelinating disease, a non-contagious chronic autoimmune disorder of the central nervous system which can present with a variety of neurological symptoms occurring in attacks or slowly progressing over time. ... Tourette syndrome (also called Tourettes syndrome, Tourettes disorder, Gilles de la Tourette syndrome, GTS or, more commonly, simply Tourettes or TS) is an inherited neurological disorder with onset in childhood, characterized by the presence of multiple physical (motor) tics and at least one vocal (phonic) tic; these... Chorea may refer to: Chorea, an ancient Greek round dance accompanied by singing. ... This article or section does not adequately cite its references or sources. ...


In some clinics the use of atypical neuroleptics (e.g. clozapine, risperidone, olanzapine, ziprasidone) is generally preferred over haloperidol, because these drugs have an appreciably lower incidence of extrapyramidal side-effects. Each of these drugs, however, has its own spectrum of potentially serious side-effects (e.g. agranulocytosis with clozapine, weight gain with increased risk of diabetes and of stroke). Atypical neuroleptics are also much more expensive and have recently been the subject of increasing controversy regarding their efficacy in comparison to older products and side effects. The atypical antipsychotics (also known as second generation antipsychotics) are a class of prescription medications used to treat psychiatric conditions. ... Clozapine (sold as Clozaril®, Leponex®, Fazaclo®) was the first of the atypical antipsychotics to be developed. ... Risperdal tablets Risperidone (sold under the trade names Belivon, Rispen and Risperdal in the United States) is an atypical antipsychotic medication developed by Janssen Pharmaceutica. ... Olanzapine (oh-LAN-za-peen, sold as Zyprexa®, Zyprexa Zydis®, or in combination with fluoxetine, as Symbyax®) was the third atypical antipsychotic to gain approval by the Food and Drug Administration (FDA) and has become one of the most commonly used atypical antipsychotics. ... Ziprasidone (marketed as Geodon®, Zeldox®) was the fifth atypical antipsychotic to gain FDA approval. ...


Haloperidol is considered indispensable for treating psychiatric emergency situations. It is enrolled in the World Health Organization List of Essential Medicines. The World Health Organization (WHO) is a specialized agency of the United Nations that acts as a coordinating authority on international public health, headquartered in Geneva, Switzerland. ... It has been suggested that this article or section be merged into Essential medicines. ...


As is common with typical neuroleptics, haloperidol is by far more active against "positive" psychotic symptoms (delusions, hallucinations etc.) than against "negative" symptoms (social withdrawal, autism etc.). The effectiveness of haloperidol against positive symptoms has not been outperformed by newer antipsychotics.


Contraindications

Absolute

  • Preexisting coma
  • Severe intoxication with alcohol or other central depressant drugs
  • Known allergy against haloperidol or other butyrophenones or other drug ingredients

In medicine, a coma (from the Greek koma, meaning deep sleep) is a profound state of unconsciousness. ...

Special caution needed

  • Preexisting Parkinson's disease
  • Patients at special risk for the development of QT prolongation (hypokalemia, concomitant use of other drugs causing QT prolongation)
  • Compromised liver-function (as haloperidol is metabolized and eliminated mainly by the liver, dose reductions and/or spaced intervals may be needed)
  • Haloperidol may decrease the seizure-threshold. Treat patients with epilepsy and those with risk factors for the development of seizures (alcohol withdrawal, encephalopathy) with caution. Maintain existing anticonvulsive therapy.
  • Patients with hyperthyreosis; the action of haloperidol is intensified and side-effects are more likely. Initiate an effective therapy of hyperthyreosis.
  • IV injections: inject slowly to avoid hypotension or orthostatic collapse. Avoid IV injections in cardiovascular unstable patients (preexisting hypotension, shock, concomitant antihypertensive therapy, heart insufficiency). Prefer in these cases moderate oral or IM doses.

The long QT syndrome (LQTS) is a heart disease in which there is an abnormally long delay between the electrical excitation (or depolarization) and relaxation (repolarization) of the ventricles of the heart. ... Hypokalemia is a potentially fatal condition in which the body fails to retain sufficient potassium to maintain health. ... The liver is an organ present in vertebrates and some other animals. ...

Side-effects

The drug is noted for its strong early and late extrapyramidal side-effects. The risk of tardive dyskinesia is around 4% per year in younger patients, higher than with most other antipsychotic drugs. In patients over the age of 45, the percentage of those afflicted can be even higher. Other predispositive factors may be female gender, prexisting affective disorder and cerebral dysfunction. See chlorpromazine for further details. In human anatomy, the extrapyramidal system is a neural network located in the brain that is part of the motor system involved in the coordination of movement. ... Tardive dyskinesia is a serious neurological disorder caused by the long-term and/or high-dose use of dopamine antagonists, usually antipsychotics and among them especially the typical antipsychotics. ... Chlorpromazine was the first antipsychotic drug, used during the 1950s and 1960s. ...


Other side effects include dry mouth, lethargy, muscle-stiffness, muscle-cramping, restlessness, tremors, and weight-gain; side effects like these are more likely to occur when the drug is given in high doses and/or during long-term treatment. Depression, severe enough to result in suicide, is quite often seen during long-term treatment. Care should be taken to detect and treat depression early in course. Sometimes the change from haloperidol to a mildly potent neuroleptic (e.g. chlorprothixene or chlorpromazine), together with appropriate antidepressant therapy, does help. Sedative and anticholinergic side-effects occur more frequently in the elderly. Xerostomia is the medical term for a dry mouth due to a lack of saliva. ... Fatigue is a feeling of excessive tiredness or lethargy, with a desire to rest, perhaps to sleep. ... A top-down view of skeletal muscle Muscle (from Latin musculus little mouse [1]) is contractile tissue of the body and is derived from the mesodermal layer of embryonic germ cells. ... For the film see Tremors (film). ... A spring scale measures the weight of an object In the physical sciences, weight is a measurement of the gravitational force acting on an object. ... Clinical depression (also called major depressive disorder, or sometimes unipolar when compared with bipolar disorder, which is sometimes called manic depression) is a state of intense sadness, melancholia or despair that has advanced to the point of being disruptive to an individuals social functioning and/or activities of daily... It has been suggested that Suicide method be merged into this article or section. ... Chlorprothixene is a typical antipsychotic drug of the thioxanthine class. ... Chlorpromazine was the first antipsychotic drug, used during the 1950s and 1960s. ...


Neuroleptic malignant syndrome (NMS) is a significant possible side effect. Haloperidol and fluphenazine are the two drugs which cause NMS most often. Allergic and toxic side-effects are uncommon. Skin rash and photosensitivity both occur in less than 1% of patients. Neuroleptic malignant syndrome (NMS) is a life-threatening, neurological disorder most often caused by an adverse reaction to neuroleptic or antipsychotic drugs. ... Fluphenazineis a typical antipsychoticdrug. ...


Children and adolescents are particularly sensitive to the early and late extrapyramidal side-effects of haloperidol. It is recommended to treat pediatric patients only if clearly needed and if the psychiatric or neurologic disorder is substantial.


QT prolongation with sudden death is rarely seen. Likewise, the development of thromboembolic complications are also rare. The long QT syndrome (LQTS) is a heart disease in which there is an abnormally long delay between the electrical excitation (or depolarization) and relaxation (repolarization) of the ventricles of the heart. ... Thrombosis is the formation of a clot or thrombus inside a blood vessel, obstructing the flow of blood through the circulatory system. ...


Haloperidol has a negative impact on vigilance and decreases the ability of the patient to drive or operate a machine, particularly initially.


Abuse and dependence

Haloperidol is completely devoid of any potential psychological dependence. A greater problem is that psychiatric patients prescribed this drug may seek to avoid taking it and consequently risk relapse of their symptoms.


Unpleasant withdrawal symptoms, if haloperidol is stopped abruptly after long-term treatment, are commonly noted. These are usually agitation, anxiety, insomnia, and nausea. Rebound of psychotic symptoms and mood swing into mania are also seen. These symptoms are not indicative of dependence. Instead of terminating treatment with haloperidol abruptly, decrease its dose, if possible, by 20 to 25% weekly. If haloperidol has to be stopped at once for medical reasons, give tranquilizers like Diazepam or Alprazolam for a few weeks, as needed, for effective alleviation of withdrawal symptoms.


Other Remarks

During long-term treatment of chronic psychiatric disorders, it should be tried - in regular intervals - to reduce the daily dose to the lowest level needed for maintenance of remission. Sometimes, it may be indicated to terminate haloperidol treatment gradually.


Other forms of therapy (psychotherapy, occupational therapy/ergotherapie, social rehabilitation) should be instituted properly.


Pregnancy and lactation

Data from animal experiments indicate haloperidol is not teratogenic, but is embryotoxic in high doses. In humans, no controlled studies exist. Unconfirmed studies in pregnant women revealed possible damage to the fetus, although most of the women were exposed to multiple drugs during pregnancy. Following accepted general principles, haloperidol should only be given during pregnancy if the benefit to the mother clearly outweighs the potential fetal risk. Enos the space chimp before insertion into the Mercury-Atlas 5 capsule in 1961. ... Teratogenesis is a medical term from the Greek, literally meaning monster making. ...


Haloperidol, when given to lactating women, is found in significant amounts in their milk. Breastfed children sometimes show extrapyramidal symptoms. If the use of haloperidol during lactation seems indicated, the benefit for the mother should clearly outweigh the risk for the child. Consider termination of breastfeeding.


Carcinogenicity

So far, no statistically acceptable evidence is found to associate long-term use of haloperidol with the potential for increased breast cancer risk in female patients. In an unconfirmed study, relative risks of breast cancer, in inmates of the Buffalo Psychiatric Center undergoing long-term treatment with haloperidol, were 3.5 (compared to patients hospitalized in general or internal medicine facilities) and 9.5 (general population), respectively (authors: U. Halbreich et al, loc. cit.: 'American Journal of Psychiatry', 1996). These results need confirmation by larger studies. If true, carcinogenity is most probably related to the strong increase in plasma-levels of prolactin under long-term treatment with haloperidol. This news is another good reason to avoid any unnecessary use of haloperidol. Prolactin (PRL) is a peptide hormone primarily associated with lactation. ...


Interactions

  • Other central depressants (alcohol, tranquilizers, narcotics): actions and side-effects of these drugs (sedation, respiratory depression) are increased. In particular, the doses of concomitantly used opioids for chronic pain can be reduced by 50%.
  • Methyldopa: increased risk of extrapyramidal side-effects and other unwanted central effects
  • Levodopa: decreased action of levodopa
  • Tricyclic antidepressants: metabolism and elimination of tricyclics significantly decreased, increased toxicity noted (anticholinergic and cardiovascular side-effcts, lowering of seizure-threshold)
  • Quinidine, buspirone, and fluoxetine: increased plasma-levels of haloperidol, decrease haloperidol dose, if necessary
  • Carbamazepine, phenobarbital, and rifampicin: plasma-levels of haloperidol significantly decreased, increase haloperidol dose, if necessary.
  • lithium: rare cases of the following symptoms have been noted: encephalopathy, early and late extrapyramidal side-effects, other neurologic symptoms and coma. Check lithium plasma levels regularly and keep the dose of haloperidol as low as possible.
  • Guanethidine: antihypertensive action antagonized
  • Epinephrine: action antagonized, paradoxical decrease in blood pressure may result

Methyldopa or alpha-methyldopa (brand names Aldomet, Apo-Methyldopa, Dopamet, Novomedopa) is a centrally-acting antiadrenergic antihypertensive medication. ... L-DOPA (levodopa, 3,4-dihydroxy-L-phenylalanine). ... Chemical structure of the tricyclic antidepressant amitriptyline Tricyclic antidepressants are a class of antidepressant drugs first used in the 1950s. ... Quinidine is a pharmaceutical agent that acts as a class I antiarrhythmic agent in the heart. ... Buspirone (brand-names Ansial®, Ansiced®, Anxiron®, Axoren®, Bespar®, BuSpar®, Buspimen®, Buspinol®, Buspisal®, Narol®, Spitomin®) is an anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. ... Fluoxetine hydrochloride (Prozac) is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. ... Carbamazepine (sold under the brand-names Biston, Calepsin, Carbatrol, Epitol, Equetro, Finlepsin, Sirtal, Stazepine, Tegretol, Telesmin, Timonil, sometimes abbreviated CBZ) is an anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy and bipolar disorder. ... Phenobarbital (also phenobarbitone) (Luminal®) is a weak acid with the chemical formula C12H12N2O3. ... Rifampicin (INN) (IPA: ) or rifampin (USAN) is a bacteriocidal antibiotic drug of the rifamycin group. ... Lithium salts are chemical salts of lithium used primarily in the treatment of bipolar disorder as mood stabilizing drugs. ... Encephalopathy is a container term for various conditions affecting the brain. ... Guanethidine is an antihypertensive drug. ... Adrenaline redirects here. ...

Doses

As directed by the physician, depends on the condition to be treated, age and weight of patient:

  • Acute problems: single doses of 1 mg to 5 mg (up to 10mg) oral or i.m., usually repeated every 4 to 8 hours. Do not exceed an oral dose of 100 mg daily. Doses used for IV injection are usually 5 to 10 mg as a single dose; not exceeding 50 mg daily.
  • Chronic conditions: 0.5 to 20 mg daily oral, rarely more. The lowest dose that maintains remission should be employed.
  • Experimental doses: In resistant cases of psychosis small studies with oral doses of up to 300 mg daily have been conducted (in most cases together with an anticholinergic antiparkinsonian drug (Biperiden, Benzatropine, etc.) to avoid severe early extrapyramidal side-effects. These studies showed no superior results and led to severe side-effects. Also, the frequency of otherwise unusual side-effects (hypotension, QT-time prolongation, and serious cardiac arrhythmias) was dramatically increased. The clinical use of haloperidol in these doses is discouraged now and it is recommended to switch the patient gradually to a different neuroleptic (e.g. clozapine, olanzapine, aripiprazole).

Depot forms are also available; these are injected deeply i.m. at regular intervals. The depot forms are not suitable for initial treatment. Cardiac arrhythmia is a group of conditions in which the muscle contraction of the heart is irregular or is faster or slower than normal. ...


Overdose

Experimental evidence from animal studies indicates that doses needed for acute poisoning are quite high in relation to therapeutic doses.


Symptoms are usually due to exaggerated side-effects. Most often encountered are:

  • Severe extrapyramidal side-effects with muscle rigidity and tremors, akathisia etc. (inject 5 mg biperiden (Akineton®) slowly IV, repeat after some hours if necessary). Sometimes oral or IM treatment with biperiden is needed for several days or even weeks. If the patient is very upset about extrapyramidal side-effects, small doses of lorazepam (0.5 to 1 mg orally, repeated every 4 to 6 hours if necessary) can be given. Lorazepam has an intrinsic action against upset, anxiety, and extrapyramidal side-effects.
  • Hypotension or hypertension
  • Sedation
  • Anticholinergic side-effects (dry mouth, constipation, paralytic ileus, difficulties in urinating, massive sweating). Cautious doses of physostigmine may be given repeatedly. N.B. Physostigmine may increase the risk of seizures!
  • Coma in severe cases, accompanied by respiratory depression and massive hypotension, shock
  • Rarely serious ventricular arrhythmia (torsades de pointes) with or without prolonged QT-time
  • Epileptic seizures, give careful doses of diazepam 5 mg to 10 mg by slow IV injection, repeatedly if needed, until seizures subside. Take care not to worsen central depression or respiratory depression caused by haloperidol. The treatment facility should be able to institute artificial respiration readily. Valproate first given as slow IV infusion and later orally may also be effective.

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. Avoid epinephrine for treatment of hypotension and shock, because its action might be reversed.


Generally, the prognosis of overdose is good and lasting damage is not known, provided that the patient has survived the initial phase.


Overdoses with depot injections are uncommon, because almost always experienced personnel administer them to patients.


Other formulations

The decanoate ester of haloperidol (Haloperidol decanoate, trade names Haldol decanoate®, Halomonth®, Neoperidole®) has a much longer duration of action, and therefore is used in noncompliant people. A dose of 25 to 250 mg. is given by intramuscular injection once every two to four weeks.[1] The decanoate ion is the conjugate base of decanoic acid, with formula C9H19COO−. Decanoate compounds include salts and esters of decanoic acid, such as sodium decanoate or methyl decanoate. ...


The structural formula of haloperidol decanoate is 4-(4-chlorophenyl)-1-1[4-(4-fluorophenyl)-4-oxobutyl]-4 piperidinyl decanoate (see image below).


haloperidol decanoate chemical structure, public domain This image is ineligible for copyright and therefore in the public domain, because it consists entirely of information that is common property and contains no original authorship. ...


Veterinary use

Haloperidol is also used on many different kinds of animals. It appears to be particularly successful when given to birds; e.g. a parrot that will not otherwise stop plucking its feathers out.


Dose forms

  • Liquid: 2 mg/mL, also 10 mg/mL
  • Tablets: 0,5 mg, 1 mg, 2 mg, 5 mg, 10 mg, 20 mg
  • Injection: 5 mg (1 mL)
  • Depot injection forms
  • The original drug Haldol® and many generics are available

References

  • B. Bandelow, S. Bleich, S. Kropp: Handbuch Psychopharmaka (German), 2nd. edition, 2004
  • Benkert, Hippius: Kompendium der Psychiatrischen Pharmakotherapie (German), 4th. edition, 2003
  • Schweizer Arzneimittelkompendium (German): Scientific Information on Haldol®

See also

Biological psychiatry, or biopsychiatry is an approach to psychiatry that aims to understand mental disorder in terms of the biological function of the nervous system. ... President George W. Bush established the controversial President’s New Freedom Commission on Mental Health in April, 2002, to conduct a comprehensive study of the United States mental health service delivery system and make recommendations based on their findings. ... A number of people considered ill and needing treatment by specific psychiatrists or psychiatric doctrine in general do not perceive benefit from the services offered or forced upon them. ... The international headquarters of the Citizens Commission on Human Rights on Sunset Boulevard in Hollywood, California. ...

External links

  • Rx-List.com - Haloperidol
  • Medline plus - Haloperidol
  • Swiss scientific information on Haldol
  • WHO List of Essential Drugs
  • German antipsychiatry comments regarding cancerogenity
  • Links to external chemical sources

  Results from FactBites:
 
Haloperidol Photos (69 words)
Back photo of yellow Haloperidol with “H 2” imprinted on the tablet.
Mailing envelope in which tablets were shipped to consumers
The ruler was placed for size comparison purposes.
Haloperidol for agitation in dementia (627 words)
In the present study haloperidol treatment was associated with a lower degree of aggression than was placebo.
Evidence suggests that haloperidol was useful in reducing aggression, but was associated with adverse effects; there was no evidence to support the routine use of this drug for other manifestations of agitation in dementia.
Variations in degree of dementia, dosage and length of haloperidol treatment, and in ways of assessing response to treatment suggested caution in the interpretation of reported effects of haloperidol in the management of agitation in dementia.
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