Haloperidol
Haldol
First-Generation AntipsychoticGeneric availableTDM data
The mechanism of action of haloperidol for the treatment of schizophrenia is unclear. However, its effect in schizophrenia could be mediated through its activity as an antagonist at central dopamine type 2 receptors. Haloperidol also binds to alpha-1 adrenergic receptors, but with lower affinity, and displays minimal binding to muscarinic cholinergic and histaminergic (H1) receptors.
Compare Haloperidol →FDA-Approved Indications
- Management of manifestations of psychotic disorders (including schizophrenia)
- Tics and vocal utterances of Tourette's disorder
- Severe behavior problems in children (combative, explosive hyperexcitability)
- Short-term treatment of hyperactive children with conduct disorders
What Sets This Drug Apart
- Prototypical high-potency FGA with D2 affinity (0.7 nM) and negligible H1/M1 binding — minimal sedation and anticholinergic effects but high EPS and prolactin liability
- Available as decanoate LAI (monthly IM) — one of the longest-established depot antipsychotic formulations; valuable for adherence-limited patients
- IV route no longer FDA-approved due to QTc prolongation risk, but oral and IM formulations are standard for acute agitation management
- QTc prolongation is dose-dependent and highest with parenteral routes; baseline ECG and periodic monitoring mandatory
- Remains a standard comparator in antipsychotic trials and the reference high-potency FGA; haloperidol equivalents used for dose comparison
- Acute dystonia risk highest in young males within first 72 hours; prophylactic anticholinergic often co-prescribed
Boxed Warning
WARNING Increased Mortality in Elderly Patients with Dementia-Related Psychosis Elderly patients with dementia-related psychosis treated wit