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Haloperidol; Uses, Dosage, Side Effects, Drug Interactions

Haloperidol is a diphenylbutylpiperidine derivative with antipsychotic, neuroleptic, and antiemetic activities. Haloperidol competitively blocks postsynaptic dopamine (D2) receptors in the mesolimbic system of the brain, thereby eliminating dopamine neurotransmission and leading to antidelusionary and antihallucinagenic effects. Antagonistic activity mediated through D2 dopamine receptors in the chemoreceptive trigger zone (CTZ) accounts for its antiemetic activity.

A phenyl-piperidinyl-butyrophenone that is used primarily to treat schizophrenia and other psychoses. It is also used in schizoaffective disorder, delusional disorders, ballism, and Tourette syndrome (a drug of choice) and occasionally as adjunctive therapy in mental retardation and the chorea of Huntington disease. It is a potent antiemetic and is used in the treatment of intractable hiccups. 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. It may be used by mouth, as an injection into a muscle, or intravenously. Haloperidol typically works within thirty to sixty minutes.

Mechanism of Action of Haloperidol

The precise mechanism whereby the therapeutic effects of haloperidol are produced is not known, but the drug appears to depress the CNS at the subcortical level of the brain, midbrain, and brain stem reticular formation. Haloperidol seems to inhibit the ascending reticular activating system of the brain stem (possibly through the caudate nucleus), thereby interrupting the impulse between the diencephalon and the cortex. The drug may antagonize the actions of glutamic acid within the extrapyramidal system, and inhibitions of catecholamine receptors may also contribute to haloperidol’s mechanism of action. Haloperidol may also inhibit the reuptake of various neurotransmitters in the midbrain, and appears to have a strong central antidopaminergic and weak central anticholinergic activity. The drug produces catalepsy and inhibits spontaneous motor activity and conditioned avoidance behaviors in animals. The exact mechanism of antiemetic action of haloperidol has also not been fully determined, but the drug has been shown to directly affect the chemoreceptor trigger zone (CTZ) through the blocking of dopamine receptors in the CTZ.

Although the complex mechanism of the therapeutic effect is not clearly established, haloperidol is known to produce a selective effect on the central nervous system (CNS) by competitive blockade of postsynaptic dopamine (D2) receptors in the mesolimbic dopaminergic system and an increased turnover of brain dopamine to produce its tranquilizing effects. With subchronic therapy, depolarization blockade, or diminished firing rate of the dopamine neuron (decreased release) along with D2 postsynaptic blockade results in the antipsychotic action.

Indications of Haloperidol

Acute psychosis, such as drug-induced psychosis caused by LSD, psilocybin, amphetamines, ketamine, and phencyclidine, and psychosis associated with high fever or metabolic disease
Adjunctive treatment of alcohol and opioid withdrawal
Agitation and confusion associated with cerebral sclerosis
Alcohol-induced psychosis
Hallucinations in alcohol withdrawal
Borderline personality disorder
Aggressive behavior
Dementia
ICU agitation
Mania
Hyperactive delirium (to control the agitation component of delirium)
Hyperactivity, aggression
Aggressive Behavior
Delirium
Gilles de la Tourette’s syndrome
Huntington’s disease
Obsessive-compulsive disorder
Prophylaxis against postoperative nausea and vomiting
Psychosis
Psychotic disorder
Schizophrenic disorders
Prophylaxis of acute chemotherapy-induced nausea and vomiting
Severe disruptive behavior disorder
Otherwise uncontrollable, severe behavioral disorders in children and adolescents
Schizophrenia
The therapeutic trial in personality disorders, such as borderline personality disorder
Treatment of intractable hiccups
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 therapy and chemotherapy in oncology.
It is a potent antiemetic and is used in the treatment of intractable hiccups

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Contra-Indications of Haloperidol

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 a cardiac arrest.

Dosage of Haloperidol

Strengths: 0.5 mg; 1 mg; 2 mg; 5 mg; 10 mg; 20 mg; 2 mg/mL;

Psychosis

Oral Haloperidol Formulations

Moderate symptomology: 0.5 to 2 mg orally 2 to 3 times a day
Severe symptomology: 3 to 5 mg orally 2 to 3 times a day
Initial doses of up to 100 mg/day have been necessary in some severely resistant cases.
Maintenance dose: After achieving a satisfactory response, the dose should be adjusted as practical to achieve optimum control

Haloperidol Lactate for Injection

Prompt control acute agitation: 2 to 5 mg IM every 4 to 8 hours
The frequency of IM administration should be determined by patient response and may be given as often as every hour.
Maximum dose: 20 mg/day

Schizophrenia

Oral Haloperidol Formulations

Moderate symptomology: 0.5 to 2 mg orally 2 to 3 times a day
Severe symptomology: 3 to 5 mg orally 2 to 3 times a day
Initial doses of up to 100 mg/day have been necessary in some severely resistant cases.
Maintenance dose: After achieving a satisfactory response, the dose should be adjusted as practical to achieve optimum control

Haloperidol Lactate for Injection

Prompt control acute agitation: 2 to 5 mg IM every 4 to 8 hours
The frequency of IM administration should be determined by patient response and may be given as often as every hour.
Maximum dose: 20 mg/day

Agitated State

Oral Haloperidol Formulations

Moderate symptomology: 0.5 to 2 mg orally 2 to 3 times a day
Severe symptomology: 3 to 5 mg orally 2 to 3 times a day
Initial doses of up to 100 mg/day have been necessary in some severely resistant cases.
Maintenance dose: After achieving a satisfactory response, the dose should be adjusted as practical to achieve optimum control

Haloperidol Lactate for Injection

Prompt control acute agitation: 2 to 5 mg IM every 4 to 8 hours
The frequency of IM administration should be determined by patient response and may be given as often as every hour.
Maximum dose: 20 mg/day

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Agitation

Oral Haloperidol Formulations

Moderate symptomology: 0.5 to 2 mg orally 2 to 3 times a day
Severe symptomology: 3 to 5 mg orally 2 to 3 times a day
Initial doses of up to 100 mg/day have been necessary in some severely resistant cases.
Maintenance dose: After achieving a satisfactory response, the dose should be adjusted as practical to achieve optimum control

Haloperidol Lactate for Injection

Prompt control acute agitation: 2 to 5 mg IM every 4 to 8 hours
The frequency of IM administration should be determined by patient response and may be given as often as every hour.
Maximum dose: 20 mg/day

Pediatric Psychosis

3 to 12 years and 15 to 40 kg

Initial dose: 0.5 mg/day orally in 2 to 3 divided doses
Adjust in increments of 0.5 mg every 5 to 7 days until the desired effect is achieved
Maintenance dose: 0.05 to 0.15 mg/kg/day in 2 to 3 divided doses

13 years and older and greater than 40 kg , Initial dose

Moderate symptomology: 0.5 to 2 mg orally 2 to 3 times a day
Severe symptomology: 3 to 5 mg orally 2 to 3 times a day
Maintenance dose: After achieving a satisfactory response, the dose should be adjusted as practical to achieve optimum control

Pediatric Aggressive Behavior

3 to 12 years and 15 to 40 kg

Initial dose: 0.5 mg/day orally in 2 to 3 divided doses
Maintenance dose: 0.05 to 0.075 mg/kg/day

Side Effects of Haloperidol

The most common

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

More common

Difficulty with speaking or swallowing
inability to move the eyes
loss of balance control
mask-like face
muscle spasms, especially of the neck and back
restlessness or need to keep moving (severe)
shuffling walk
stiffness of the arms and legs
trembling and shaking of the fingers and hands
twisting movements of the body
weakness of the arms and legs

Less common

Decreased thirst
difficulty in urination
dizziness, lightheadedness, or fainting
hallucinations (seeing or hearing things that are not there)
lip smacking or puckering
puffing of the cheeks
rapid or worm-like movements of the tongue
skin rash
uncontrolled chewing movements

Drug Interactions of Haloperidol

Heloperidol may interact with following drug, supplements, & may change the efficacy of drugs

antihistamines (e.g,. cetirizine, doxylamine, diphenhydramine, hydroxyzine,loratadine)
antiseizure medications e.g., clobazam, levetiracetam, phenobarbital, phenytoin, , valproic acid, zonisamide)
aripiprazole
“azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
captopril
celecoxib
chloroquine
cholecalciferol
cyclosporine
dantrolene
domperidone
“gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
gabapentin
H2 antagonists (e.g., famotidine, ranitidine)
mirabegron
montelukast
non-steroidal anti-inflammatory medications (NSAIDs;e.g., diclofenac, ibuprofenserotonin antagonists (anti-emetic medications;, naproxen)
phosphodiesterase 5 inhibitors (e.g., sildenafil, tadalafil, vardenafil)
quinolone antibiotics (e.g., levofloxacin, norfloxacin, moxifloxacin)
selective serotonin reuptake inhibitors (SSRIs; e.g., paroxetine, fluoxetine,citalopram)
e.g., granisetron,ondansetron)
“statin” anti-cholesterol medications (e.g., atorvastatin, lovastatin,simvastatin)
theophylline
thiazide diuretics (water pills; e.g., hydrochlorothiazide, indapamide, metolazone)
tramadol
tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine,
tapentadol
tetracycline
(water pills; e.g., hydrochlorothiazide, indapamide, metolazone)
tramadol
tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
zafirlukast

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Pregnancy & Lactation of Haloperidol

FDA Pregnancy Category C

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

This medication passes into breast milk. If you are a breast-feeding mother and are taking haloperidol, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.