General Description
Haldol, also referred to as Haloperidol is a first-generation antipsychotic (FGA) drug that
is commonly used to treat schizophrenia. Besides schizophrenia, the drug has also been
confirmed to treat other psychological health and disposition disorders such as schizoaffective
disorder, tourette’s condition, hyperactivity, and bipolar disorder. According to a report by the
U.S. National Library of Medicine (NIH, 2016), Haloperidol is also prescribed for serious
behavioral disorders, for instance, impulsiveness, violent behavior or, hyperactivity among
minors who cannot be treated with psychotherapy or with other treatments. Haldol works by
reducing atypical arousal in the brain.
Mechanism of Action
Haldol bars the dopamine and serotonin type 2 receptors at the nerve spot. Moreover,
Haldol is a phenylbutylpiperadine derivative with antipsychotic, neuroleptic, and antiemetic
actions (National Center for Biotechnology Information, 2017). Haloperidol aggressively
obstructs postsynaptic dopamine (D2) receptors thata re located in the brain’s mesolimbic
structure, thus eliminating dopamine neurotransmission. This process results in anti-delusionary
and anti-hallucinogenic outcomes. According to the National Center for Biotechnology
Information (2017), antagonistic action that is facilitated through D2 dopamine receptors in the
chemoreceptive trigger zone (CTZ) is responsible for its antiemetic action.
Dosage, Administration, Absorption, and Metabolism
Haloperidol can be taken orally in tablet form or through an injection. Dosage for the
drug depends on the patient’s symptomology. The oral drug can be administered two to three
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times a day, while the patient can receive the injection after every four to eight hours. The drug
administration is prescribed by a trained medical practitioner, and medication should always be
taken as directed.
Glucuronidation entails the route of haloperidol metabolism that is accountable for
almost 50-60% of absorption in vivo. Different from other medications, this procedure cannot be
reversed by enzymes from gut bacteria, and it is expelled as haloperidol glucuronide. Whereas
O-glucuronidation is the main site of modification, N-glucuronidation is exhibited in vitro
though at much lower intensities. Around 25% of haloperidol experiences reduction, which is a
reversible progression. Nonetheless, the reverse oxidation reaction ensues about one-quarter of
the reduction reaction. The two oxidative routes are responsible for the remaining 15-30%
oxidative N-alkylation to CPHP and FBPA and oxidation to haloperidol pyridinium. Oxidative
N-alkylation cuts the link between the piperidine two ring areas and single ring with a carbon
pillar and fundamentally separates the drug into two developing CPHP and FBPA. Whirl-
Carrillo et al. (2016) affirm that though CYP3A4 is the main enzyme in the lessening of
Haloperidol, investigations have shown this process can impact metabolism. Overall, Haldol is
significantly absorbed in the liver.
Side Effects and Contraindications
Haloperidol bears an impact on dopamine, sigma, serotonin, histamine, and adrenergic
receptors. The drug’s possible side effects include quick heart rate, faintness, drowsiness,
biliousness, and hyperactivity. Patients can also develop a disorder referred to as tardive
dyskinesia, which is the reflex movement of the tongue, hands, feet, and neck. The brain’s
sensitivity to dopamine is the primary cause of tardive dyskinesia. The other side effect of
Haloperidol is a condition called akathisia, which is characterized by muscle stiffness. Other
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notable side effects are weight gain, erectile dysfunction, insomnia, dry mouth, variations in
menstruation, and constipation.
Since tardive dyskinesia is at times a permanent side effect that leads to impairment,
medical scholars are pursuing an alternative treatment to reduce the risk of the disorder. The eon
going research at the moment is determining if Gingko Biloba or Vitamin E can be used as a
substitute to Haldol; nonetheless, this exploration is in its initial stages. Additional severe side
effects that call for urgent attention are seizures, speedy heartbeat, high or low blood pressure,
fever, and inability to control the bladder. Taking the drug alongside other prescribed
medications can also lead to dangerous side effects. Therefore, patients should not take
Haloperidol with sedatives, painkillers, narcotics, and anxiety medications.
Haloperidol involves a conservative antipsychotic agent to treat acute and chronic
psychosis (Cowling, Covington, Roehmer, & Musey, 2019). Haloperidol therapy is generally
linked to slight serum aminotransferase elevations and on rare occasions connected to clinically
apparent acute liver injury” (National Center for Biotechnology Information, 2017). Therefore,
Haloperidol should not be prescribed to people who are sensitive to this drug, those diagnosed
with Parkinson’s ailment, in a coma or, those experiencing CNS dejection.
Furthermore, a patient should never cease to take the drug as prescribed without consulting a
medical practitioner. Possible withdrawal indications entail spontaneous motion of the mouth,
tongue, jaw, hands, and tremors. In case an individual experiences the withdrawal, seeking
medical attention is commended.
Overdose
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In case of an overdose, the patient would require instant medical attention. An overdose's
signs include serious breathing difficulties, faintness, feeling confused, drowsiness, reflex
movements, for instance, trembling, and muscle arduousness or jerking.
Conclusion
Haldol is an antipsychotic drug that is applied in the treatment of mental health
conditions. The medication is also administered to individuals with behavioral disorders such as
violent conduct and impulsiveness. The drug can be taken orally or through an injection. Similar
to other medications, Haldol is associated with numerous side effects. In case a patient takes an
overdose, instant medical attention is recommended.
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References
Cowling, M., Covington, S., Roehmer, C., & Musey, P. (2019). Characterizing the role of
Haloperidol for analgesia in the emergency department. Journal of Pain Management,
34(2/3), 141–146.
National Center for Biotechnology Information. (2017). Haloperidol. PubChem. Retrieved from
https://pubchem.ncbi.nlm.nih.gov/compound/Haloperidol.
U.S. National Library of Medicine (NIH). (2016). Haloperidol: MedlinePlus drug
information. MedlinePlus. Retrieved from
https://medlineplus.gov/druginfo/meds/a682180.html.
Whirl-Carrillo, M., McDonagh, E. M., Hebert, J. M., Gong, L., Sangkuhl, K., Thorn, C. F.,
Klein, T. E. (2012). Pharmacogenomics knowledge for personalized medicine. Clinical
Pharmacology & Therapeutics, 92(4), 414-417.