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Neuroleptic Butyrophenones

Saturday, September 15th 2012. | Medical Treatment

Neuroleptic Butyrophenones Definition

Neuroleptic or antipsychotic class of butyrophenones are also called neuroleptics or first generation. They are used in the treatment of schizophrenia, rather today in 2 nd intention, because of their tolerance. They can cause extrapyramidal disorders (found in Parkinson’s disease, abnormal movements, rigidity, involuntary muscle contractions) anticholinergic effects (dry mouth, tachycardia, diplopia, urinary retention, constipation), rhythm disturbances, a risk convulsive and hematological disorders.

Butyrophenones antiproductifs antipsychotic effects, especially hallucinations, effects antiemetisants and sedative effects (for pipamperone) and mixed (for haloperidol, a neuroleptic considered versatile).

These drugs are in the form of tablets, drinkable drops and injections.


Neuroleptic Butyrophenones Mechanism

Antipsychotic neuroleptic butyrophenone class, possess antidopaminergic which are charged, the antipsychotic effect desired therapeutic and side effects (extrapyramidal syndrome, dyskinesia, hyperprolactinemia).

Molecules with a sedative, also have antihistamine properties, the origin of these sedative effects generally sought in the clinic, and anticholinergic and adrenergic marked the origin of orthostatic hypotension.

The gastrointestinal absorption is complete after oral administration, but the bioavailability is 60%, due to first-pass metabolism of nearly 40%, fecal and urinary elimination half-life and is about 20 hours. The maximum plasma concentration after 2 to 6 hours, with a high interindividual variability.

All these pharmacokinetic parameters are that these molecules are administered orally, at rate of 1 to 2 doses per day.

Neuroleptic Butyrophenones Therapeutic goals

Prescribing antipsychotic or neuroleptic butyrophenones aims to control symptoms and prevent complications and relapse of psychotic states, schizophrenia and behavioral disorders.

Neuroleptic Butyrophenones Indications

Butyrophenones antipsychotics are indicated in:

  • The acute and chronic psychotic states, schizophrenia and delusional disorders.
  • Severe behavioral disorders with agitation and aggression in children.
  • Anxiety in 2 nd intention and psychosomatic manifestations after failure of standard therapy.
  • Nausea and vomiting after radiotherapy

Neuroleptic Butyrophenones Side effects

These are some complications that can occur when taking the drug, knowing that induced side effects vary among individuals.

In the use of antipsychotic butyrophenones have been reported:

  • At psychic sedation, emotional numbing, depression.
  • At the neurological level: acute dyskinesia, abnormal motor activity, difficulty in achieving voluntary actions.
  • At Endocrine: weight gain, amenorrhea, impotence, frigidity.
  • Various disorders, photosensitivity, torsade de pointes (cardiac arrhythmia), hypothermia.

Neuroleptic Butyrophenones Precautions

Under treatment with antipsychotic butyrophenones must:

  • Monitor weight, blood glucose, cholesterol.
  • Suspend treatment if unexplained fever, as can malignant syndrome.
  • Prevent dry mouth.
  • Use with caution butyrophenone antipsychotics in the elderly because of the risk of hypotension, patients with Parkinson’s and epilepsy due to a decrease in the seizure threshold (threshold at which to trigger seizures) , of renal and hepatic impairment due to an overdose and in serious cardiovascular disease.

Pregnancy and lactation

The use of antipsychotic butyrophenones is not recommended during pregnancy except for haloperidol. In the newborn haloperidol is sometimes responsible for extrapyramidal disorder, if continued late pregnancy (as hypertonia and tremor)

Due to the transition in breast milk, these molecules are not recommended during lactation.

Driving and using machines

Because of the risk of drowsiness, risk decreased alertness, blurred vision, dizziness associated with taking these drugs, patients’ attention should be drawn to drive and use machines.

Neuroleptic Butyrophenones lifestyle

The medication adherence is essential. Eliminating alcohol is important.

Neuroleptic Butyrophenones drug interactions

Butyrophenones associations with alcohol, antiemetisants, lithium, apomorphine, some neuroleptics (chlorpromazine, levomepromazine, sulpiride) to levodopa, are discouraged.

Associations with anticholinergic butyrophenones, antidiabetics, antihypertensives, carbamazepine, other neuroleptics, should be used with caution.

Butyrophenones associations with other depressant drugs central nervous system, are taken into account.

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