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Haloperidol


 
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Haloperidol oral tablet is only available as a generic drug. There is no brand-name version. Haloperidol is available as an oral tablet, an oral solution, and an injectable form. Haloperidol oral tablet is used to treat a range of disruptive disorders, behavior problems, and motion problems.

A phenyl-piperidinyl-butyrophenone, traditional antipsychotic drug that is used primarily to treat schizophrenia and other psychoses. It is also used for the management of schizoaffective disorder, delusional disorders, ballism, and Tourette syndrome (a drug of choice) and occasionally as adjunctive therapy in mental retardation and the chorea associated with Huntington's disease. It is a potent antiemetic and is used in the treatment of intractable hiccups



Uses

Haloperidol is used to treat certain mental/mood disorders (e.g., schizophrenia, schizoaffective disorders). This medicine helps you to think more clearly, feel less nervous, and take part in everyday life. It can also help prevent suicide in people who are likely to harm themselves. It also reduces aggression and the desire to hurt others. It can decrease negative thoughts and hallucinations.
Haloperidol can also be used to treat uncontrolled movements and outbursts of words/sounds related to Tourette's disorder. 

Haloperidol is also used for severe behavior problems in hyperactive children when other treatments or medications have not worked.
Haloperidol is a psychiatric medication (antipsychotic-type) that works by helping to restore the balance of certain natural substances in the brain (neurotransmitters).

Indications

·         For the treatment of schizophrenia
·         For the treatment of acute psychosis in acutely agitated schizophrenic patients with moderately severe to very severe symptoms
·         For the treatment of severe behavioral or psychological symptoms of dementia
·         For the treatment of delirium in the pediatric intensive care unit
·         For the treatment of agitation or delirium
·         For agitation† or delirium in adult patients with no underlying psychiatric illness
·         For use as a second-line agent for rescue treatment of chemotherapy-induced nausea/vomiting
·         For the treatment of irritability associated with autistic disorder
·         For the treatment of tics and vocal utterances associated with Tourette's syndrome
·         For the treatment of severe behavioral problems associated with oppositional defiant disorder or other disruptive behavioral disorders, or for the treatment of attention-deficit hyperactivity disorder (ADHD) in pediatric patients who show excessive motor activity with accompanying conduct disorders

Mechanism of action

Haloperidol inhibits the effects of dopamine and increases its turnover, however, the exact mechanism of action is not fully understood. Dopamine overactivity can be presynaptic (an excess of dopamine release from dopamine nerve terminals) or post-synaptic (an increase in the density of D2 receptors or an increase in post-receptor action). Traditional antipsychotics, such as haloperidol, bind more tightly than dopamine itself to the dopamine D2 receptor, with dissociation constants that are lower than that for dopamine

It is believed that haloperidol competitively blocks post-synaptic dopamine (D2) receptors in the brain, eliminating dopamine neurotransmission and leading to the relief of delusions and hallucinations that are commonly associated with psychosis. It acts primarily on the D2-receptors and has some effect on 5-HT2 and α1-receptors, with negligible effects on dopamine D1-receptors. 

The drug also exerts some blockade of α-adrenergic receptors of the autonomic system
Antagonistic activity regulated through dopamine D2 receptors in the chemoreceptive trigger zone (CTZ) of the brain renders its antiemetic activity. Of the three D2-like receptors, only the D2 receptor is blocked by antipsychotic drugs in direct relation to their clinical antipsychotic abilities. The optimal clinical efficacy of antipsychotics is associated with the blockade of approximately 60 % - 80 % of D2 receptors in the brain

Clinical brain-imaging findings show that haloperidol remains tightly bound to D2 dopamine receptors in humans undergoing 2 positron emission tomography (PET) scans with a 24h pause in between scans. A common adverse effect of this drug is the development of extrapyramidal symptoms (EPS), due to the tight binding of haloperidol to the dopamine D2 receptor. Further information is found in the "Toxicity" section of this drug profile.

Due to the risk of unpleasant and sometimes lifelong extrapyramidal symptoms, newer antipsychotic medications than haloperidol have been discovered and formulated. Rapid dissociation of drugs from dopamine D2 receptors is a plausible explanation for the improved EPS profile of atypical antipsychotics such as Risperidone. This is also consistent with the theory of a lower affinity for D2 receptors for these drugs. As mentioned above, haloperidol binds tightly to the dopamine receptor, potentiating the risk of extrapyramidal symptoms, and therefore should only been used when necessary.

Bipolar disorder drug

Using lithium with haloperidol can lead to encephalopathic syndrome. This condition can result in brain damage. Symptoms may include weakness, fever, tremor, confusion, muscle spasms, and abnormal blood test results. If you experience any of these symptoms, tell your doctor right away.

Irregular heart rate drugs

Don’t take haloperidol with these drugs. The combination can increase the effects that both drugs may have on your heart. This can cause the irregular heart rate called torsades de pointes, which can be fatal. Examples of these drugs include:
  • dofetilide
  • quinidine
  • dronedarone

Anticoagulant, blood thinner

Taking warfarin with haloperidol may make warfarin less effective.

Parkinson’s disease drugs

Taking haloperidol with these medications can make the Parkinson’s medications less effective. It may also increase pressure of the fluid in your eyes. If you’re taking these drugs together and they need to be stopped, the haloperidol should be stopped first to prevent muscle side effects. Examples of these drugs include:
  • levodopa
  • pramipexole
  • ropinirole

Anti-seizure drugs

Haloperidol increases your risk of seizure. Your doctor should use caution in prescribing haloperidol for you if you’re taking anti-seizure drugs. Examples of these drugs include:
  • carbamazepine
  • phenytoin
  • valproic acid
  • oxcarbazepine

Antibiotic

Taking rifampin with haloperidol may lower the amount of haloperidol in your body. Your haloperidol dose may need to be changed or stopped when you start taking rifampin.

Low blood pressure drug

Taking epinephrine with haloperidol may block the action of epinephrine and cause a condition called epinephrine reversal. Symptoms of epinephrine reversal may include a serious decrease of blood pressure, fast heart rate, and heart attack.

Side Effects

Dizziness, lightheadedness, drowsiness, difficulty urinating, sleep disturbances, headache, and anxiety may occur. If these effects persist or worsen, notify your doctor or pharmacist promptly.
Dizziness and lightheadedness can increase the risk of falling. Get up slowly when rising from a sitting or lying position.

In rare cases, haloperidol may increase your level of a certain chemical made by the body (prolactin). For females, this increase in prolactin may result in unwanted breast milk, missed/stopped periods, or difficulty becoming pregnant. For males, it may result in decreased sexual ability, inability to produce sperm, or enlarged breasts. If you develop any of these symptoms, tell your doctor right away.

For males, in the unlikely event you have a painful or prolonged erection (lasting more than 4 hours), stop using this drug and seek immediate medical attention, or permanent problems may occur.
This medication may rarely cause a condition known as tardive dyskinesia. In some cases, this condition may be permanent. Tell your doctor right away if you develop any facial/muscle twitching such as tongue thrusting, chewing movements, puffing or puckering of your mouth, or uncontrollable shaking.

    Alcohol interaction warning

    Avoid using alcohol while taking haloperidol. Drinking alcohol while taking haloperidol can make the side effects of both the drug and alcohol stronger. Taking alcohol and haloperidol together may also cause your blood pressure to decrease.

    For people with dementia: If you’re aged 65 years or older and have psychosis related to dementia, taking haloperidol may increase your risk of death. You shouldn’t use haloperidol if you have this condition.

    For people with cerebrovascular disease: These are serious diseases of the blood vessels to the heart and brain. Haloperidol may cause a temporary drop in blood pressure or cause chest pain. If you have symptoms of a drop in your blood pressure level, contact your doctor. Symptoms include:
    • dizziness
    • fainting
    • blurred vision, especially when standing up
    For people with seizures: If you have a history of seizures or are taking anti-seizure drugs, your doctor may lower your dose of haloperidol or stop your treatment with this drug. Taking haloperidol may make you have a seizure more easily.

    For people with Parkinson’s disease: Haloperidol works on a chemical in your brain called dopamine. It may make your Parkinson’s disease much worse.

    For people with low white blood cell counts: Haloperidol may cause the number of your white blood cells to drop. You doctor will need to check your white blood cell count often. If your blood cell counts become too low, you may have to stop taking haloperidol.

    For people with mania: When haloperidol is used to control mania in mania cyclic disorder, you may have a fast mood swing to depression.

    For people with thyrotoxicosis: This is a condition that happens when your body makes too much thyroid hormone. Too much thyroid hormone in your body can be toxic to your nervous system. Haloperidol may increase your chance of having this condition. Symptoms may include rigidity and the inability to walk and talk.

    For people with low potassium or magnesium: Having low potassium or magnesium levels and taking haloperidol may increase your risk of cardiovascular side effects. These include Q–T syndrome and an irregular heart rate called torsades de pointes, which can be fatal.

    For pregnant women: There are no well-controlled studies with haloperidol in pregnant women. There are reports of birth defects, but it’s not certain if haloperidol was the cause.
    You should only use haloperidol during pregnancy if the potential benefit outweighs the potential risk to the fetus.
    Call your doctor if you become pregnant while taking this drug.

    For women who are breastfeeding: Avoid breastfeeding while taking haloperidol. Haloperidol passes through breast milk and may harm your child.

    For seniors: The effects of haloperidol in people aged 65 years and older may be much stronger.
    Seniors are more at risk for a side effect called tardive dyskinesia. This condition can cause movement disorders of your mouth and legs. Women who have been taking this medication for a long time are at higher risk.

    For children: Haloperidol is not approved for children younger than 3 years.
    Haloperidol Haloperidol Reviewed by gafacom on May 10, 2019 Rating: 5

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