HALOPERIDOL

AKHILA V P
 MECHANISM OF ACTION

• The mechanism of action of haloperidol primarily involves its

interaction with dopamine receptors in the brain. Specifically,
haloperidol acts as a dopamine receptor antagonist, meaning it
blocks the activity of dopamine at certain receptor sites. This
blockade predominantly occurs at dopamine D2 receptors,
although haloperidol also has affinity for other dopamine
receptor subtypes.
• By blocking dopamine receptors, haloperidol inhibits the effects of
dopamine neurotransmission in certain brain regions, particularly those
implicated in the regulation of mood, behavior, and psychosis. This
antagonism of dopamine receptors is thought to contribute to
haloperidol's antipsychotic effects, as it helps normalize dopaminergic
activity in individuals with conditions such as schizophrenia and acute
psychosis.
• Additionally, haloperidol's antagonism of dopamine receptors may lead to
side effects such as extrapyramidal symptoms (EPS), which are movement
disorders characterized by dystonia, akathisia, parkinsonism, and tardive
dyskinesia. These side effects are thought to result from alterations in
dopaminergic signaling pathways within the basal ganglia and other
motor control regions of the brain.
 INDICATION

• Haloperidol is indicated for the treatment of various psychiatric and neurological

conditions. Some of the primary indications for haloperidol include:
• Schizophrenia: Haloperidol is commonly used to manage the symptoms of
schizophrenia, including hallucinations, delusions, disorganized thinking, and
emotional disturbances.
• Acute Psychosis: It is also effective in the treatment of acute episodes of
psychosis, which may occur in conditions such as schizophrenia, bipolar disorder,
or severe depression.
• Tourette Syndrome: Haloperidol can help alleviate tics and
other symptoms associated with Tourette syndrome, a
neurological disorder characterized by involuntary movements
and vocalizations.
•
 DOSAGE FORM

• Haloperidol is available in various dosage forms, and its administration

depends on the specific condition being treated. Tablets: Haloperidol is
commonly available in tablet form, typically in strengths ranging from 0.5
mg to 10 mg.
• Liquid Solution: Some formulations of haloperidol are available as oral
liquid solutions, which may be preferred for patients who have difficulty
swallowing tablets.
• Intramuscular Injection: Haloperidol may also be administered via
intramuscular injection for rapid onset of action, particularly in emergency
or acute settings.
 DOSAGE & ADMINISTRATION

• Schizophrenia and Acute Psychosis: The initial dosage of haloperidol for

adults is typically 0.5 to 2 mg orally two to three times daily. The dosage
may be gradually increased based on response and tolerability, with a
maximum recommended dose of 100 mg per day. For intramuscular
administration, the initial dose is usually 2 to 5 mg, with additional doses
administered as needed every 4 to 8 hours. Once control is achieved, the
patient may be switched to oral therapy.
• Tourette Syndrome: The initial dosage for Tourette syndrome is
often lower, starting at 0.5 mg orally two to three times daily.
The dosage may be titrated upward based on response, with a
maximum recommended dose of 20 mg per day.
• Absorption: Haloperidol is well-absorbed after oral
administration, with peak plasma concentrations reached
within 2 to 6 hours.
• Distribution: It has a large volume of distribution, indicating
extensive tissue distribution throughout the body.
•
• Metabolism: Haloperidol undergoes extensive hepatic
metabolism, primarily via cytochrome P450 enzymes,
particularly CYP3A4 and CYP2D6.
• Excretion: Metabolites of haloperidol are primarily eliminated
via the kidneys, with a small fraction excreted in the feces.
 ADVERSE EFFECT

• Extrapyramidal Symptoms (EPS): One of the most common adverse

effects of haloperidol is EPS, which includes symptoms such as
dystonia (sustained muscle contractions), akathisia (restlessness),
parkinsonism (tremor, rigidity, bradykinesia), and tardive dyskinesia
(involuntary repetitive movements). These effects are due to
haloperidol's blockade of dopamine receptors in the basal ganglia.
•
• Sedation: Haloperidol can cause sedation or drowsiness,
particularly at higher doses or when first starting treatment.
• Anticholinergic Effects: It may also exhibit anticholinergic
effects, leading to dry mouth, constipation, urinary retention,
and blurred vision.
 DRUG INTERACTION

• Haloperidol can interact with several medications, potentially leading to adverse effects
or alterations in therapeutic response. Here are some notable drug interactions
involving haloperidol:
• Central Nervous System (CNS) Depressants: Concurrent use of haloperidol with other
CNS depressants, such as benzodiazepines, opioids, or alcohol, may potentiate sedation
and respiratory depression. Caution is advised when combining these medications, and
dosage adjustments may be necessary to minimize the risk of excessive sedation or
respiratory depression.
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