Psychotropic Drugs

Bryan Mae H. Degorio

Review on Neurobiological Theory

A.Neurotransmitters
- are the chemical substances that are being
manufactured in the neuron that aid in the
transmission of information throughout the body.

 They either excite or stimulate an action in the

cells (excitatory) or inhibit or stop an action
(inhibitory).
 After neurotransmitters are released into the
synapse (point of contact between the dendrites
and the next neuron) and relay the message to
the receptor cells, they are either transported
back from the synapse to the axon to be stored
for later use (reuptake) or are metabolized and
inactivated by enzymes, primarily monoamine
oxidase (MAO).
1. Dopamine
- a neurotransmitter located primarily in the brain
stem. Dopamine is generally excitatory and is
synthesized from tyrosine, a dietary amino acid.

 Antipsychoticmedications work by blocking

dopamine receptors and reducing dopamine
activity.
2. Norepinephrine and Epinephrine
- Norepinephrine, the most prevalent
neurotransmitter, is located primarily in the brain
stem. It plays a role in mood regulation.

 Epinephrine is also known as noradrenaline and

adrenaline. Epinephrine has limited distribution in
the brain but controls the fight-or-flight response in
the peripheral nervous system.
3. Serotonin
 A neurotransmitter found only in the brain, is
derived from tryptophan, a dietary amino acid.
 The function of serotonin is mostly inhibitory,
involved in the control of food intake, sleep and
wakefulness, temperature regulation, pain control,
sexual behavior, and regulation of emotions.
 Some antidepressants block serotonin reuptake, thus
leaving it available longer in the synapse, which
results in improved mood.
4. Histamine
 The role of histamine in mental illness is under
investigation.  
5. Acetylcholine
 Acetylcholine is a neurotransmitter found in the brain,
spinal cord, and peripheral nervous system. It can be
excitatory or inhibitory. It is synthesized from dietary
choline found in red meat and vegetables and has been
found to affect the sleep-wake cycle and to signal
muscles to become active.
 Studies have shown that people with Alzheimer’s
disease have decreased acetylcholine secreting neurons.
6. Glutamate
 Glutamate is an excitatory amino acid that at high
levels can have major neurotoxic effects.
7. Gamma-Aminobutyric Acid (GABA)
 GABA is a major inhibitory neurotransmitter in the
brain and has been found to modulate other
neurotransmitter systems rather than to provide
a direct stimulus.
 Drugs that increase GABA function such as
benzodiazepines are used to treat anxiety and to
induce sleep.
Theories of Psychopharmacology
 Efficacy refers to the maximal therapeutic effect that a
drug can achieve.
 Potency describes the amount of the drug needed to
achieve that maximum effect; low-potency drugs require
higher doses to achieve efficacy, whereas high-potency
drugs achieve efficacy at lower doses.
 Half Life is the time it takes for half of the drug to be
removed from the bloodstream. Drugs with shorter half-
life may need to be given three or four times a day, but
drugs with a longer half-life may be given once a day.
 The FDA may issue a black-box warning when a drug is
found to have serious or life-threatening side effects. This
means that package inserts must have a highlighted box,
separate from the text, which contains a warning about the
serious side-effects.
 
Sedative Hypnotics and Anti-anxiety Drugs
- these drugs are use to treat anxiety and anxiety
disorders, OCD, depression, post-traumatic
stress disorder, and alcohol withdrawal
- it induces sedation, relax muscles and inhibit
convulsion
- previously called: Minor tranquilizer
- 2 Major Groups:
a. Benzopdiazipines
b. Barbiturates
Benzodiazepines
- mediates the action of actions of the amino acid GABA,
the major inhibitory neurotransmitter in the brain
- it increases the action of the GABA thus opening the
chloride channel rendering the neurons in
hyperpolarized state which reduces the neurons
excitability
- Indications:
a. Anxiolytic d. Anesthetics
b. Hypnotics e. Muscle Relaxant
c. Anticonvulsant
- Adverse Reaction:
a. Physical dependence or psychological dependence
b. CNS: drowsiness, sedation, poor coordination, and
impaired memory or clouded sensorium
c. When used for sleep, may complain of next-day
sedation or a hangover effect
d. Use cautiously among elderly
e. CI: Among pregnant client and are not recommended among
nursing mothers
- Drug Interaction
a. Alcohol and other CNS depressant- respiratory
depression
 b. Tobacco, caffeine and sympathomimetics-
decrease the effect of benzodiazipines
Examples:
a. Chlodiazepoxide (librium)
b. Diazepam (Valium)
c. Lorazepam (Ativan)
d. Oxazepam (Serax)
e. Alprazolam (Xanax)
f. Prazepam (Xentrax)
d. Chlorazepate (Tranxene)
Non-Benzodiazipines
- often used for the relief of anxiety
 acts as partial agonist at serotonin receptors, which
decreases serotonin turnover
 Has a lesser CNS side effects
 Examples: Buspirone
Nursing Implication
1. Administer IM route slowly in large muscles
2. Observe for S.E.
3. Monitor vitals signs (hypotension and bradycardia)
4. Do not mix diazepam with other drugs
5. For Benzodiazepines overdose
- Antagonist: flumazenil IV (Romazicon)
- if conscious: administer emetic (follow with
activated charcoal
- if unconscious: Gastric lavage
- Maintain airway, give O2
7. Client teaching
- do not drive or operate machine
- do not consume alcohol, CNS depressant
- Effective response may take 1-2 weeks
- strictly follow drug regimen- prevent withdrawal
symptoms
Barbiturates
- are drugs use to treat insomnia, anxiety, tension and
apprehension
- Mechanism of Action:
a. Depress the reticular activating system by
promoting the inhibitory synaptic action of the
GABA
- Indications
a. Sedative hypnotics
b. Anesthetics
c. Anti-convulsant
- Adverse Reaction:
a. Mild side effect:
- confusion and irritability
- Rare: agranulocytosis, thrombocyopenia and
megaloblastic anemia
Allergic reaction
b. Withdrawal symptoms
- nightmares, daytime agitation and shaky feelings
c. Overdose: Respiratory and cardiovascular
depression
Examples:
a. Amobarbital (amytal)
b. Aprobarbital (Alurate)
c. Butabarbetal (Butisol)
d. Pentobarbital (Nembutal)
e. Phenobarbital (Luminal)
f. Secobarbital (Seconal)
Barbiturates are classified in four categories

1. Long acting- Phenobarbital

2. Short acting- Butobarbital , Pentobarbital
3. Ultra short acting- Thiopental, Methohexitone
Anti-Psychotic
- also known as Neuroleptic or Major Tranquilizer
- used to treat symptoms of psychosis, such as
delusions and hallucinations seen in
schizophrenia, schizoaffective disorder, and
manic phase of bipolar disorder
- work by blocking receptors of the
neurotransmitter dopamine
- 2 Categories:
A. Classic/Typical Antipsychotic
B. Atypical Antipsychotic
Classic/Typical Antipsychotic
- the largest group under this category are the
Phenotiazines
Mechanism of Action
a. As Dopamine Receptor Agonist
- it blocks dopamine receptor in various parts of the brain
- Dopamine receptors are classified into 5
(D1, D2, D3, D4, D5)
- it blocks : D2, D3, D4
- relieving psychotic manifestation
- blocking of D2 leads to EPS manifestations
b. As Adrenergic and Cholinergic Receptor Antagonist
- it blocks the receptors of norepinephrine and
dopamine
c. CNS effect and Adrenergic Receptors
- neurons containing norepinephrine in the reticular
activating system of the brain is associated
with alertness
- blockade can lead to sedative effect
- blockade of norepinephrine receptor in the center
can lead to hypotension
 Indications:
- to treat manifestations associated by the Dopamine
theory of pscyhosis
- Gilles de la Tourette’s Syndrome
- Emesis and dopamine
Adverse Reaction:
1. Extrapyramidal Syndrome (EPS)
- this is the most important side effect of the
antipsychotic drugs
- it arises from the blockade of the D2 receptors in
the certain nuclei of the basal ganglia which is
responsible for the coordinated movement
 - can be manifested by:
 Acute dystonia
 Akathisia
 Tardive dyskinesia
 Pseudoparkinsonism

Acute Dystonia
- is a spasm of the muscles of the tongue, face, neck or back
and may mimic seizures
- can be manifested by: torticollitis, oculygric crises and
opisthonos posture
- can be treated by anticholinergic drugs
Akathisia
- is a motor restlessness
- is reported by the client as an intense need to
move about
- The client appears restless or anxious and agitated
often with a rigid posture or gait and a lack of
spontaneous gestures.
- can be treated with : anticholinergic drugs or
muscle relaxant
Pseudoparkinsonism
- is marked by motor retardation and rigidity
- often referred to by the generic label of EPS
- symptoms resemble those of Parkinson’s disease and
include:
a. A stiff and stooped posture
b. Mask-like faces, decreased arm swing, a shuffling,
festinating gait, cogwheel rigidity,
drooling, tremors,
c. Bradycardia, and coarse pill-rolling movements of the
thumb and fingers while at rest
 - can be treated by: oral anticholinergic drugs or
amantidine (a dopamine agonist)
Tardive Dyskinesia
- is associated with long term, high doses of
antipsychotic therapy
- syndrome of permanent involuntary movements
commonly caused by the long-term use of
conventional antipsychotic drugs
- symptoms of TD include involuntary movements of the
tongue , facial and neck muscles, and upper and
lower extremities
- tongue thrusting and protruding, lip smacking, blinking,
grimacing, and other excessive, unnecessary facial
movements are characteristic
- once it has developed, TD is irreversible, although
decreasing or discontinuing antipsychotic
medication can arrest its progression
Neuroleptic Malignant Syndrome
 Potentially fatal reaction to antipsychotic drugs
 major symptoms of NMS are rigidity, high fever,
autonomic instability (such as unstable BP,
diaphoresis, and pallor), delirium, and
elevated levels of enzymes
(particularly creatinine phosphokinase)
 clients with NMS usually are confused and often
mute, may fluctuate from agitation to
stupor
Anticholinergic Action
- atropine like effects
- dry mouth, blurred vision, delayed micturation, and
constipation
- CNS reaction: is beneficial because it used to treat
pseudoparkinsonism manifestations
Seizure Potential
- it lowers the convulsive threshold
Endocrine Disturbances
- blockade of the dopamine receptors can lead to
hypersecretion of prolactin and endocrine disturbances in
the reproductive system
 - can lead to:
 increase blood prolactin levels causing breast enlargement
and tenderness (both in men and women)
 diminished libido
 erectile and orgasmic dysfunction
 menstrual irregularities
 weight gain (obesity common in schizophrenic clients,
increasing risk for DM II and CVD)
 minor cardiovascular adverse effects such as postural
hypotension, palpitations, and tachycardia
 Allergic Reaction:
- photosensitivity and cholestatic hepatitis
Drug Interaction
a. It potentiates the action of drugs that depresses
the CNS: sedative-hypnotics, narcotic
analgesic and anesthetic agent
Nursing Implication:
1. Informclient of side effects and encourage to report
problems instead of discontinuing medication
2. teach client methods of managing or avoiding
unpleasant side effects and maintaining medication
regimen:
 dry mouth – sugar-free fluids and sugar-free hard candy
* client should avoid calorie-laden beverages and
candy
 constipation – exercise, increase water and bulk-forming
foods; stool softener permissible but avoid laxatives
 photosensitivity – sunscreen
3. Client should monitor amount of sleepiness and
drowsiness they feel; avoid driving and potentially
dangerous activities until response time and reflexes
seem normal
Examples of Drugs:
A. Phenothiazine
 Alipathic
- Chlorpromazine (thorazine)
- Promazine (Sparine)
- Trifulpromazine (Vesporin)
 Piperazines
- Fluphenazine (Prolixin)
- Perphenazine (Trilafon)
  Piperidines
- Thioridazine (Meliaril)
- Mesoridazine (Serentil)
B. Non-Phenothiazide
 Haloperidol (haldol)
 Loxapine (loxatane)
 Molindone (Moban)
 Pimozide (Orap)
Atypical Antipsychotic
- are new agents used of treatment of severe
schizophrenia
- they have minimal EPS side effects
- are effective in treating negative symptoms of
schizophrenia (apathy, social withdrawal,
blunted affect
- Mechanism of action:
a. Blocks the Dopamine D2 but not as effective as the
traditional antipsychotic
b. Block the serotonine 5-HT2A receptors
Indication:
a. Patients who are unresponsive to typical
antipsychotic drugs
Adverse Reaction:
a. Increase risk for seizure
b. Clozapine
- CV: orthostatic hypotension and tacycardia
- agranulocytosis
- dizziness and sedation
Examples:
a. Olanzapine (Clorazil)
b. Olanzapine (Zyprexia)
c. Respiridone (Risperdal)
Nursing Implication:
 Monitor VS
 Remain with client while he takes the medication.
 Avoid skin contact with liquid concentrates.
 Protect liquid prep from light & dilute with juice.
 Administer oral dose with food or milk.
 Administer IM drug deep.
 Observe for EPS.
 Monitor for signs of neuroleptic malignant syndrome.
 Client teachings:
- take drug exactly as ordered.
- Meds take 6 wks or longer to achieve full clinical
effect.
- WBC monitored for 3 months. (WOF signs of
infection)
- Avoid driving & operating machineries.
 Avoid driving & operating machineries.
 Avoid direct sunlight.
 Avoid extremes in temperatures & increased exercise.
 Change positions slowly.
 Alipathic phenothiazines  pink-red brown urine.
 Suggest lozenges, hard candy for dry mouth.
 Changes to sexual functioning & menstruation.
Antidepressant Drugs
- primarily used in the treatment of major depressive
illness, anxiety disorders, depressed phase of bipolar
disorder, and psychotic depression
- somehow interact with norephinephrine and
serotonin which regulate mood, arousal, attention, sensory
processing, and appetite
- Theories of the Development of Mood Disorders:
a. Deficiency of brain neurotransmitter norepinephrine is
associated with depression
b. Reserpine depletes norepinephrine causes depression
c. Inhibition on MAO has antidepressant effect
Classification of Anti-Depressant:
a. Selective Serotonine Reuptake Inhibitor (SSRI)
b. Tricyclic Anti-depressant
c. Monoamine Oxidase Inhibitor
Selective Serotonine Reuptake Inhibitor
- newest category of antidepressant with fewer side
effects and minimal potential lethal overdose
- Mechanism of action:
1. Blocks the neuronal reuptake of serotonin but have
little effect on norepinephrine and dopamine
Indication:
a. major depression (unipolar)
b. Obsessive Compulsive Disorders and eating
disorders
Adverse Reaction:
a. Headaches, tremors, anxiety and drowsiness, dry mouth,
sweating and diarrhea
b. Use cautiously in patient with:
- liver and renal impairment
- patients with seizure disorders
- nursing mothers is not recommended
Drug Interaction:
a. Other anti-depressant drug may be potentiated by
SSRI: MOA and tryptophan
b. Use cautiously with anticoagulant and phenytoin
Examples:
 Flouxetine (Prozac)
 Sertraline (zoloft)
 Paroxatine (Plaxil)
 Fluvoxamine (Luvox)
 Citalopram (Celexa)
Tricyclic Antidepressant
- Have a more pronounced side effects compared to
SSRI
- Mechanism of Action:
a. Blocks the reuptake of norepinephrine or
serotonin in the presynaptic cleft causing an
increase concentration of these
neurotransmitter
b. Block cholinergic receptors leading to
anticholinergic side effects
c. Takes 2-3 weeks before the effects can be seen among
patients
Indications:
1. major depression and bipolar disorders
2. clomipramine- obsessive compulsive disorders
3. Imipramine- enuresis
Adverse Reactions:
a. Anticholinergic Side Effects:
- dry mouth, blurring of vision and constipation
- cautiously among client with glaucoma
- pt with urinary retention and obstruction
b. Cardiac Effects
- increase in heart rate (anticholinergic effects)
- postural hypotension (adrenolytic effect)
- decrease myocardial contractility and coronary blood
flow (Quinidine like effect)
c. Weight gain
d. Toxicity:
1. Not addicting
2. Overdose of Tricyclic antidepressant
- anticholinergic poisoning
- delerium, seizures, hallucination, pupillary dilation and
hyperactive reflexes
 - Antidote: Physostigmine (antilirium)
Drug Interaction:
a. Can potentiate CNS depression
b. Cemitidine and methylpenidate- inhibit its
metabolism
Examples:
 Amytriptyline (elavil)
 Trimipramine (Surmontil)
 Doxepin (Sinequan)
 Imipramine (Tofranil)
Monoamine Oxidase Inhibitor
- are less commonly used because of poor safety
profile that requires strict adherence to
dietary limitations and potential for drug
interaction
- Mechanism of Action:
a. It inhibits the enzyme MAO thus preventing the
degradation of epinephrine and serotonin so that its
concentration in CNS is increased
Indications:
a. Effective in treatment of depression exhibit as phobias
Side Effects:
a. Anticholinegic effects
b. Sedation
c. insomnia
Toxicity:
a. Reflects adrenergic activity:
- tachycardia, anxiety, insomnia and restlessness
Interactions:
1. Foods containing Tyramine
- Avocados, Bananas, Beer, Chocolates,
Cheese, Liver, Meat extracts, Papaya extracts,
Raisins, Salami, Yogurt
- can be manifested by:
a. Hypertensive crises- due to
accumulated release of
norepinephrine
- Pentholamine- can be given
Examples:
 Isocarboxacid (Marplan)
 Phenelzine (Nardil)
 Tranylcypromine (Parnate)
Mood Stabilizer/Antimanic Drugs
- used for treatment of manic episodes in bipolar
disorder
- Example: Lithium
- Lithium- the most established mood stabilizer
- Mechanism of Action
- it normalizes the reuptake of serotonin,
norepinephrine, acetylcholine, and
dopamine
- has a narrow therapeutic range: 0.6-1.5 mEq/L
 - excreted in the kidney
- Na deficiency- increaser lithium absorption
- Na Excess- lower lithium below therapeutic
range
- may reverse manic episode in 1-3 weeks
- Indication: Treatment of the manic phase in bipolar
disorders
- Adverse Reaction:
a. CI among pregnant client
b. Inhibit thyroxine release
c. Nephrotoxic
Toxicity:
a. 1.5-2.0 mEq/L- persistent diarrhea, n and v,
muscle weakness, blurred of
vision and tinnitus
b. 2.0- 3.5 mEq/L- excessive urination, tremors and
mental confusion
d. > 3.5 mEq/L- seizure, coma, oliguria/anuria,
nystagmus, MI and cardiac dys.
Treatment: Gastric lavage, correction of fluid imbalance
and mannitol
Interaction:
a. NASIDS, diuretics, tetracyclines- increases the risk
of lithium toxicity
b. Caffeine product (coffe and tea cole)- aggravate
manic phase