page_title: Haloperidol
section_title: Pharmacology
hierarchical_section_title: Haloperidol / Pharmacology
caption_attribution_description: English: Drug Name: Haloperidol 10 MG Oral Tablet Ingredient(s): Haloperidol Imprint: GG126 Color(s): Green Shape: Round *Size (mm): 10.00 *Score: 1 Inactive Ingredient(s): lactose monohydrate / povidone / starch, corn / ma... lactose monohydrate / povidone / starch, corn / magnesium stearate / d&amp;c yellow no. 10 / fd&amp;c blue no. 1 Drug Label Author: Sandoz Inc DEA Schedule: Non-scheduled
context_page_description: Haloperidol, marketed under the trade name Haldol among others, is a typical antipsychotic medication. 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 or injection into a muscle or a vein. Haloperidol typically works within 30 to 60 minutes. 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.
  Haloperidol may result in a movement disorder known as tardive dyskinesia which may be permanent. Neuroleptic malignant syndrome and QT interval prolongation may occur. In older people with psychosis due to dementia it results in an increased risk of death. When taken during pregnancy it may result in problems in the infant. It should not be used in people with Parkinson's disease.
  Haloperidol was discovered in 1958 by Paul Janssen. It was made from pethidine. It is on the World Health Organization's List of Essential Medicines. It is the most commonly used typical antipsychotic.
context_section_description: Haloperidol is a typical butyrophenone type antipsychotic that exhibits high affinity dopamine D₂ receptor antagonism and slow receptor dissociation kinetics. It has effects similar to the phenothiazines. The drug binds preferentially to D₂ and α₁ receptors at low dose (ED₅₀ = 0.13 and 0.42 mg/kg, respectively), and 5-HT₂ receptors at a higher dose (ED₅₀ = 2.6 mg/kg). Given that antagonism of D₂ receptors is more beneficial on the positive symptoms of schizophrenia and antagonism of 5-HT₂ receptors on the negative symptoms, this characteristic underlies haloperidol's greater effect on delusions, hallucinations and other manifestations of psychosis. Haloperidol's negligible affinity for histamine H₁ receptors and muscarinic M₁ acetylcholine receptors yields an antipsychotic with a lower incidence of sedation, weight gain, and orthostatic hypotension though having higher rates of treatment emergent extrapyramidal symptoms.
  Haloperidol acts on these receptors: (Kᵢ)
  D₁ (silent antagonist) — Unknown efficiency
  D₅ (silent antagonist) — Unknown efficiency
  D₂ (inverse agonist) — 0.74 nM
  D₃ (inverse agonist) — 0.2 nM
  D₄ (inverse agonist) — 5–9 nM
  σ₁ (irreversible inactivation by haloperidol metabolite HPP⁺) –  3 nM
  σ₂ (agonist): 54 nM
  5HT1A receptor agonist –  1927 nM
  5HT2A (silent antagonist) –  53 nM
  5HT2C (silent antagonist) – 10,000 nM
  5HT₆ (silent antagonist) – 3666 nM
  5HT₇ (irreversible silent antagonist) — 377.2 nM
  H₁ (silent antagonist) — 1,800 nM
  M₁ (silent antagonist) — 10,000 nM
  α1A (silent antagonist) — 12 nM
  α2A (silent antagonist) — 1130 nM
  α2B (silent antagonist) — 480 nM
  α2C (silent antagonist) — 550 nM
  NR1/NR2B subunit containing NMDA receptor (antagonist; ifenprodil site): IC₅₀ — 2,000 nM
caption: Haloperidol, 10-mg oral tablet
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