ANTI PSYCHOTIC DRUGS (NEUROLEPTIC)
INTRODUCTION
The word neuroleptic originates from a Greek word “lepsis “(“to take “or to “seize
“ ). Antipsychotic drugs are prescribed drugs used to treat psychotic disorders
such as schizophrenia, affective disorders or psychotic depression.Anti psychotic
drugs regulate certain brain chemicals called neurotransmitter and these are
Dopamine, Serotonin, Catecholamine etc.
There are two classifications of Antipsychotic drugs.
TYPICAL OR FIRST GENERATION ANTIPSYCHOTIC DRUGS
This is further subdivided into Phenothiazines and
Butyrephenones.
These drugs were developed in 1950s. Traditionally, it was thought that these
mediations were more likely than the newer ones to cause extra pyramidal
symptoms like rigidity (muscle stiffness), unusual body or facial movements,
persistent muscle spasms, tremors, restlessness etc.
However, recent research suggests that these medications can just be safe and
tolerated just like the newer medications, although much controversy still exists
on the topic. In the past, these medications were often used at much higher doses
than are used currently which explains why they appear to cause more side
effects. It was also thought that these older medications were not very effective
for negative symptoms of schizophrenia including lack of speech, apathy, flat
facial expression or personality.
Researches seem to support the conclusion that newer medications are better for
negative symptoms although there is significant controversy
EXAMPLE OF TYPICAL MEDICATIONS.
Chlorpromazine ( thorazine )
Fluphenazine ( prollxin )
Haloperidol ( Haldol )
Loxapine ( adauve , loxitane )
Molldone ( moban )
Periphenazine ( trllafon )
Pimozide ( orap )
Prochlorperazine ( Compazine , compro )
Thioridazine (mellaril, melleril)
Trifluoperazine (stelazine)
ATYPICAL MEDICATIONS (SECOND GENERATION ANTIPSYCHOTIC DRUGS)
These are the newer Antipsychotic medications; they have largely replaced older
medications due to the supposedly lower risk of side effects particularly
extrapyramidal side effects. These medications are rather expensive and carry a
significant risk of weight gain and diabetes.
However, they may be more effective than older medications of negative
symptoms of schizophrenia. Both generations tend to block receptors in the
brain’s dopamine pathways, but atypical tend to act on serotonin receptors as
well.
EXAMPLES OF ATYPICAL MEDICATIONS
Aripirazole ( abilify )
Aserapine ( saphils )
Clozapine (clozaril, fazaclo )
Iioperidone ( fancipt )
Lurasidone ( Latuda)
Olanzapine (Zyprexa)
Palloperidone (lnvega)
Risperidone (Risperdal)
Ziprasidone (Geodan)
A number of adverse side effects have been observed on patients taking
Antipsychotic drugs ranging from mild to life threatening effects. The following
are general side effects of Antipsychotic medications.
SEDATION
Sedation is common with Antipsychotic medication and it is dose related. It can
be a cause of poor compliance and if it persists, can interfere with social and
vocational functioning. Many patients become tolerant to the sedative effect over
time. This can be prevented by changing to a single bed time dose or switching to
less sedative medications.
HYPOTENSION
Orthostatic hypotension can occur with most of the Antipsychotic medications.
This effect is more common in older adults, those on Antihypertensive and those
with the cardiovascular diseases. To prevent this, treatment options including
decreasing or dividing doses or switching to a drug with lesser Anti adrenergic
effects.
ANTICHOLINERGIC EFFECTS
Anticholinergic effects include constipation, urinary retention, dry mouth, blurred
vision and at times cognitive impairement.These symptoms can lead to other
problems like, tooth decay, falls and intestinal obstruction. Drugs that are likely to
cause these are clozapine, olanzapine and quetiapine.
EXTRAPYRAMIDAL SYMPTOMS
Antipsychotic medications cause four main extrapyramidal symptoms,
pseudoparkinisonism, akathisia, acute dystonia and tardive dyskinesia, especially
the typical Antipsychotics.
PSEUDOPARKINSONIM
This is a reversible syndrome that includes tremulousness of hands and arms,
rigidity in the arms and shoulders, masked face and shuffine giant.
AKATHISIA
Is described subjectively as a feeling of inner restlessness as that can be
manifested as excessive pacing or inability to remain for any length of time
Treatment of akathisia includes: dosage reduction when possible or addition of a
low dose beta blockers e.g. propranolol.
TARDIVE DYSKINESIA
This is an involuntary movement disorder that can occur in long term
Antipsychotic treatment and may not be reversible even when treatment is
discontinued. It usually involves the oro-facial region, but all parts of the body can
be involved. The symptoms are more present especially when the patient is
awake than during sleep. Attempts to treat tardive Dyskinesia usually begins by
discontinuing the offending agent or switching to one with lower risk but
evidence is sufficient to show marked reduction in symptoms.
HYPERPIOCACTINEMID
This is increased levels of prolactin in the blood. This can be asymptomatic but
may cause gynecomastia, oligaamenorrhoea, amenorrhea, sexual dysfunction,
acne and loss of bone density (osteoporosis).
SEXUAL DYSFUNCTION
Up to 43% of patients taking Antipsychotic drugs report problems with sexual
dysfunctions. Both typical and atypical drugs can impair arousal and orgasm in
men and women. First generation Antipsychotics can cause erectile and
ejaculation dysfunction in men including spontaneous pain or retrograde
ejaculation as well as priapism.
AGRANULOCYTOSIS
In rare cases clozapine causes neutropenia (neutrophil count below 1500 cells per
mm3 and agranulocytosis which can lead to potentially fatal infections. This can
occur in less than 1% of patients. Medication is to be discontinued if white blood
cell count drops below 3000mm3.
CARDIAC ARRHYTHIMIAS
Antipsychotic drugs can lead to prolongation of ventricular repolarization which
leads to sudden cardiac death .To avoid this, physicians should be vigilant in
assessing the patients’ cardiac symptoms.
SEIZURES
All Antipsychotics can lower seizures threshold. They should be used with caution
in patients who have a history of seizure and those with organic brain disorder.
They lower the seizure threshold most common in typical Antipsychotic drugs
especially clozapine in higher doses. Depot Antipsychotic should not be used in
patients with epilepsy.
METABOLIC SYNDROME
Weight gain is a common adverse effect of using Antipsychotic drugs. It can be
rapid and difficult to control. It is worse in clozapine and olanzapine.
Antipsychotics can contribute to a wide range of glycemic abnormalities, from
mild insulin resistance to diabetic ketoacidosis as well as worsening of glycemic
control in patients with pre-existing diabetes. The greatest risk is with clozapine
and olanzapine.
WITHDRAWAL EFFECTS
Temporary withdrawal symptoms may occur following lowering the dosage or
discontinuing the drug, e.g. .Insomnia, agitation, psychosis and motor disorder
and can be mistaken for return of the underlying condition.
In conclusion, close monitoring by the physician is important when the patient is
taking Antipsychotic as this will promote early detection and treatment of the
adverse side effects, because this may cause discomfort to the patient and
sometimes become fatal. Education of the patient and care givers about the drug
is vital.
