Brands, Medical Use, Clinical Data
Drug Category
- Antidyskinetics
- Antipsychotics
- Antiemetics
- Butyrophenones
- Dopamine Antagonists
Dosage Forms
- Injection
- Oral solution
- Tablet
Brands / Synonyms
ALDO; Aloperidin; Aloperidol; Aloperidolo; Aloperidon; Apo-Haloperidol; Bioperidolo; Brotopon; Dozic; Dozix; Einalon S; Eukystol; Galoperidol; Haldol; Haldol Decanoate; Haldol La; Haldol Solutab; Halidol; Halojust; Halol; Halopal; Haloperido; Haloperidol Decanoate; Haloperidol Intensol; Haloperidol Lactate; Halopidol; Halopoidol; Halosten; Keselan; Lealgin Compositum; Linton; Mixidol; Novo-Peridol; Pekuces; Peluces; Peridol; Pernox; Pms Haloperidol; Serenace; Serenase; Serenelfi; Sernas; Sernel; Sigaperidol; Ulcolind; Uliolind; Vesalium
Indications
For the treatment of schizophrenic patients who require prolonged parenteral antipsychotic therapy also used in Tourette's syndrome and Severe hyperactivity.
Pharmacology
Haloperidol is a psychotropic agent indicated for the treatment of schizophrenia. It also exerts sedative and antiemetic activity. Haloperidol has actions at all levels of the central nervous system-primarily at subcortical levels-as well as on multiple organ systems. Haloperidol has strong antiadrenergic and weaker peripheral anticholinergic activity; ganglionic blocking action is relatively slight. It also possesses slight antihistaminic and antiserotonin activity.
Mechanism of Action
The precise mechanism whereby the therapeutic effects of haloperidol are produced is not known. Its effect on the central nervous system is thought to be associated with the competitive blockade of postsynaptic dopamine D2 receptors in the mesolimbic dopaminergic system and an increased turnover rate of brain dopamine.
Absorption
Oral-60%
Toxicity
LD50=165 mg/kg (rats, oral)
Biotrnasformation / Drug Metabolism
Hepatic
Contraindications
Since the pharmacologic and clinical actions of HALDOL Decanoate 50 and HALDOL Decanoate 100 are
attributed to HALDOL (haloperidol) as the active medication, Contraindications, Warnings, and additional information
are those of HALDOL, modified only to reflect the prolonged action. HALDOL is contraindicated in severe toxic central
nervous system depression or comatose states from any cause and in individuals who are hypersensitive to this drug or
have Parkinsonís disease.
Drug Interactions
An encephalopathic syndrome (characterized by weakness, lethargy, fever, tremulousness and confusion,
extrapyramidal symptoms, leukocytosis, elevated serum enzymes, BUN, and FBS) followed by irreversible brain damage
has occurred in a few patients treated with lithium plus HALDOL. A causal relationship between these events and the
concomitant administration of lithium and HALDOL has not been established; however, patients receiving such combined
therapy should be monitored closely for early evidence of neurological toxicity and treatment discontinued promptly
if such signs appear.
As with other antipsychotic agents, it should be noted that HALDOL may be capable of potentiating CNS
depressants such as anesthetics, opiates, and alcohol.
In a study of 12 schizophrenic patients coadministered oral haloperidol and rifampin, plasma
haloperidol levels were decreased by a mean of 70% and mean scores on the Brief Psychiatric Rating Scale were
increased from baseline. In 5 other schizophrenic patients treated with oral haloperidol and rifampin,
discontinuation of rifampin produced a mean 3.3-fold increase in haloperidol concentrations. Thus, careful monitoring
of clinical status is warranted when rifampin is administered or discontinued in haloperidol-treated patients.
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