Extrapyramidal symptoms:

Antipsychotic medications commonly produce extrapyramidal symptoms as side effects. The

extrapyramidal symptoms include acute dyskinesias and dystonic reactions, tardive dyskinesia,
Parkinsonism, akinesia, akathisia, and neuroleptic malignant syndrome. Extrapyramidal symptoms
are caused by dopamine blockade or depletion in the basal ganglia; this lack of dopamine often mimics
idiopathic pathologies of the extrapyramidal system. Less recognized is that extrapyramidal symptoms
are also associated with certain non-antipsychotic agents, including some antidepressants, lithium,
various anticonvulsants, antiemetics and, rarely, oral-contraceptive agents.

Restlessness and nervous energy shown by pacing, marching, shuffling, or foot-tapping

Severe, uncontrolled muscle contractions of your head, neck, trunk, and limbs that cause stiff
tongue, twisted neck, or back arching
Tremors, stiff posture, or no arm movement when you walk
Uncontrolled movements of your tongue, jaw, lips, or face, such as pursing, chewing, or
frequent eye blinking
Uncontrolled movements of your fingers or toes, head nodding, or pelvic thrusting
Fast, irregular breathing with grunts, gasping, or sighing
Weak voice, drooling, or little or no facial expression

First generation antipsychotics (TYPICAL) are D2 antagonists and are associated

with higher risk of EPS.
Second generation antipsychotics( ATYPICAL): are 5HT2A/D2 antagonists, are
associated with lower risk of EPS and with higher risk of metabolic side effects.

First generation antipsychotics are D2 antagonists, they act on different regions such as mesolimbic,
mesocortical, nigrostriatal and tuberoinfundibular pathways.

Something worth noting is that both first and second generation antipsychotics have some degree of
D2 antagonism. D2 antagonism has proven to be responsible for antipsychotic efficacy.

Besides D2 antagonism, first generation agents have effects on other receptors, such as muscarinic,
adrenergic alpha 1 and histamine-1.

Blockade of these receptors is related with their side effects profile.

Second generation antipsychotics also block D2 receptors, but what makes them different from first
generation agents is their ability to block 5HT2A receptors. As we saw in a previous slide, these
drugs are also known as serotonin-dopamine antagonists.
In fact, they have higher affinity for 5HT2a receptors than D2 receptors.
Distinction between typical and atypical groups is
not clearly defined, but rests on:

Incidence of extrapyramidal side-effects (less in

atypical group)

Efficacy in treatment resistant group of patients

Efficacy against negative symptoms

First Generation Antipsychotics

Also known as conventional or typical antipsychotics, medications in this group were the first
drugs used to treat schizophrenia. Although they can be very effective, they are often accompanied
by very challenging side effects, particularly with long term use. However, for many patients, the
benefits outweighed the risks.
Conventional antipsychotics, unfortunately, have very limited effectiveness in treating the negative
symptoms of schizophrenia, such as emotional flatness and lack of initiative. They also provide little,
if any, benefit for mood symptoms or cognitive impairment.
Despite the fact that many newer antipsychotics have been developed, many of the first generation
antipsychotics are still frequently prescribed today. Others, such as trifluoperazine and molindone,
have been discontinued.

Second Generation Antipsychotics

The early 1990s brought the development of a new group of antipsychotics, known as second
generation or atypical antipsychotics. Because they were believed to have fewer side effects, they
quickly began to replace conventional antipsychotics for the treatment of schizophrenia and related
conditions.

A dopamine agonist receptor is a compound that activates dopamine receptors in the absence of
that receptor's physiological ligand, the neurotransmitter dopamine. Dopamine agonists activate
signaling pathways through the dopamine receptor and trimeric G-proteins, ultimately leading to
changes in gene transcription.

Selective serotonin reuptake inhibitors (SSRIs), as the name suggests, inhibit the reuptake or re-
absorption of the brain chemical serotonin by the nerve cells. Serotonin is a neurotransmitter
associated with the sense of well-being and joy. When the re-absorption of this chemical is
blocked, the amount available to the brain increases. SSRIs are most commonly used in the
treatment of moderate to severe depression. They are also used in anxiety disorders, panic
disorder, obsessive compulsive disorder (OCD), and in post traumatic stress disorder (PTSD).
This medicine has helped in allaying depression and anxiety in majority of the patients with
lesser side effects as compared to the older drugs.

Serotonin-norepinephrine reuptake inhibitors (SNRIs) also inhibit the reuptake of serotonin. In

addition, they inhibit the re-absorption of another neurotransmitter called nor-epinephrine. Just
like serotonin is associated with positive feelings, nor-epinephrine is associated with alertness
and energy. Thus, this newly found group of medicines also are used in the treatment of major
depressive disorders, mood disorders, anxiety disorders, and attention deficit hyperactive
disorder (ADHD). Apart from these, SNRIs are also used to treat chronic neuropathic pains like
nerve pain from diabetes, fibromyalgia, and in relief of menopausal symptoms.

Anxiolytic-hypnotic

Description

This is the most frequently used anxiolytic drug because it can lyse or break the feeling

of anxiety without causing much sedation and are less likely to make patients physically dependent.

Therapeutic Action

By acting on the limbic system and the reticular activating system (RAS), it causes the gamma-

aminobutyric acid (GABA) to be more effective in interfering neuron firing. GABA stabilizes the

postsynaptic cell which leads to an anxiolytic effect at a dose lower than required to induce sedation and

hypnosis. However, the exact mechanism of action is not clearly understood.

Indications

Indicated for the treatment of the following conditions: anxiety disorders, alcohol withdrawal,

hyperexcitability and agitation, and preoperative relief of anxiety and tension to aid in balanced

anesthesia.
Nursing Assessment

These are the important things the nurse should include in conducting assessment, history
taking, and examination:

Assess for the mentioned cautions and contraindications (e.g. drug allergies,
hepatorenal diseases, psychosis, glaucoma, etc.) to prevent any untoward
complications.
Perform a thorough physical assessment to establish baseline data before drug
therapy begins, to determine effectiveness of therapy, and to evaluate for
occurrence of any adverse effects associated with drug therapy.
 Monitor results of laboratory tests (e.g. renal and liver functions tests, complete
blood count (CBC), etc.) to monitor effectiveness of the therapy and provide
prompt treatment to developing complications.
Monitor patient response to therapy (e.g. controlled anxiety, sleep, etc).
Monitor for adverse effects (e.g. hypotension, blood dyscrasias, hepatorenal
dysfunction, etc).
Evaluate patient understanding on drug therapy by asking patient to name the drug,
its indication, and adverse effects to watch for.
Monitor patient compliance to drug therapy.