Haloperidol; Uses, Dosage, Side Effects, Drug Interactions

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.

or

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

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

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

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.

References