PSYCHOTROPIC DRUGS

/PHARMACOPSYCHOTHERAPY

NRSG 362: Mental Health and Psychiatric

Nursing
CLAIRE
 Introduction
• Antipsychotics/neuroleptics denote a group of drugs used
to treat schizophrenia/other psychoses and agitated states.
• They work by blocking the receptors of the
neurotransmitter Dopamine
• Clinical use of psychotropic drugs dates back 50years i.e
chlorpromazine .
• Non medical use; self administration of
stimulants and anti anxiety agents are used to produce
stability, relief and pleasure .
• Psychotropic medications are medications that affect
cognitive function, emotion and behaviour.
 Basic guidelines for
pharmacotherapy
• a.Use well-tried drugs
• b.Change drugs only for a good reason e.g.
intolerable side effects
• c.Combine drugs only for special reasons e.g.
benzodiazepines and neuroleptics to control
acute symptoms of schizophrenia or lithium and
SSRIs to control drug resistant depressive
disorder
• d.Adjust dosage carefully
 Basic guidelines -CTN
• e.Plan the interval between doses
• f.Decide the duration of treatment e.g. if
dependency risk is there give for a short time
while others like antidepressants/antipsychotics
given for longer time to prevent relapse
• g.Advise patients before giving the drugs e.g.
initial effects , onset of action, first sign of
improvement, common side effects, any serious
effects, any restrictions while taking the drug
and how long the patient will take the drug.
 CNS neurotransmission
• Neurotransmitter-chemical that allows
transmission of signal from one neuron to
the next neuron across a synapse.
– Attaches to a receptor on cell surface
and either inhibits or excites.
– Major target of psychotropic drugs
 Sites of CNS drug action
Drugs may alter
1. The action potential in the presynaptic fiber
2. Synthesis of transmitter
3. Storage
4. Metabolism
4. Release
 Sites of CNS drug action Cont..
6. Reuptake
7. Degradation
8. Receptor for the transmitter or
9. Receptor-induced decrease or increase
in ionic conduction.
MOA
 MOA for Antipsychotic drugs
They act as antagonists at several receptor
types namely;
Acetylcholine; excitatory
Dopamine; inhibitory
Norepinephrine/epinephrine; CNS
stimulation
Glutamate; excitatory
MOA for Antipsychotic drugs Cont…
Serotonin; inhibitory
Involved in emotion and mood.
GABA; excitatory
NB: They are dopamine receptor antagonists.
• Also inhibit receptors for acetylcholine
(muscarinic), histamine (H1), noradrenaline
and serotonin (5HT).
 Dopaminergic systems
Five dopamine pathways in the brain
Mesolimbic- mesocortical pathway
Is related to behavior. Increasing activity in
the pathway may cause delusions,
hallucinations and other positive
schizophrenic symptoms
Dopaminergic systems Cont.
 Nigrostriatal pathway
Involved in the coordination of body movements.
Inhibition causes extra pyramidal side effects
 Tuberoinfundibular pathway
Is involved in physiological inhibition of prolactin
secretion and blockage leads to elevated serum
prolactin levels
 Incartohypothamic pathway
Functions not yet defined in humans.
 Medullary- periventricular pathway
It is involved in eating behavior
 Uses of psychotropic drugs
• In schizophrenic symptoms which include;
Thought disorder
Emotional withdrawal
Halluccinations
 Delusions
• In Tourette’s syndrome
• In bipolar affective disorder which include
mania and depression.
Uses of psychotropic drugs Cont..
• In narcolepsy- Characterized by daytime
sleepiness and sudden periods of loss of
wakefullness.
• In toxic psychosis caused by overdosage
of certain CNS stimulants
• In psychotic symptoms
• For non psychiatric indications;
 antiemetic effect e.g. chlorpromazine
Relieve of pruritis e.g. phenothiazines
Uses of psychotropic drugs Cont.

Preoperative sedation e.g. promethazine

Butyrophenone e.g. druperidol used in
combination with fentanyl in
neuroleptanasthesia
CLASSIFICATION
1. Antipsychotics:(neuropletics): Phenothiazines,
Butyrophenones,-substituted benzamide
2. Antidepressants:Tricyclic antidepressants, monoamine
oxidase inhibitor(MAOIs),-selective serotonin
reuptake inhibitors (SSRIs),norepinephrine
3. Mood stabilizer –Lithium and carbamazepine and
sodium valproate Lithium.
4. Anxiolytics –Benzodiazepines and Azapirones
(buspirone)
5.Hypnotics –Benzodiazepines and cyclopyrrones
(zopiclone)
6 Psycho stimulants- amphetamine
 1.ANTIPSYCHOTICS
• Antipsychotic drugs are the primary medical
treatment for Schizophrenia and are also used in
psychotic episodes of acute mania, psychotic
depression, and drug-induced psychosis.
• Persons with dementia who have psychotic
symptoms sometimes respond to low doses of
antipsychotics.
• Transient psychotic symptoms, such as those
seen in some persons with borderline
personality disorder.
 ANTIPSYCHOTICS
• They include 1st generation (typical) e.g.
chlorpromazine, fluphenazine,
haloperidol, thioridazine, trifluoperazine.
• 2nd generation (atypical) e.g. clozapine,
olanzepine, quetiapine, risperidone,
ziprasidone.
• Review doses
Chemical Classification of antipsychotics

• Phenothiazines e.g.
Aliphatic derivatives; chlorpromazine,
Piperidine derivatives; thioridazine
 Piperazine derivatives; fluphenazine
• Thiozanthones e.g. Thiothixene
 Chemical Classification Cont.

• Butyrophenomes e.g. Haloperidol

• Chemical structure types e.g.
pimozidine, olanzapine
 MECHANISM OF ACTION
• Block receptors for the neurotransmitter
dopamine.
• The typical antipsychotics are potent
antagonists (blockers) of dopamine receptors
D2, D3, and D4 but also produces many
extrapyramidal side effects. 9
• Atypical are relatively weak blockers of D2, so
lower incidence of extrapyramidal side effects.
Atypical also inhibit the reuptake of serotonin,
which makes them more effective in treating
the depressive aspects of Schizophrenia.
 Pharmacokinetics
• Readily but incompletely absorbed from
GIT when given orally- undergo significant
first pass metabolism
• Lipid soluble, readily enter CNS/ most
other body tissues
• Bound extensively to plasma proteins
• IM doses provide four to five times the
active dose as oral doses hence requires
caution of switching between routes.
 Pharmacokinetics Cont..
• Access to CNS depends on their water
solubility (polar) and is more to those of
low molecular weight e.g. lithium

• Require metabolism to more water

soluble metabolites for their elimination.
 Pharmacokinetics Cont..
• Drugs that modify the activities of drug
metabolizing enzymes may have an
impact on clearance of these drugs
• Are sequestrated in lipid compartments of
the body and have a longer clinical
duration of action.
• Metabolized in the liver by oxidation and
demethylation.
 Pharmacokinetics Cont..
• Widely distributed and stored in the tissues,
being released for up to 6 months after the
drug is stopped.
• Children metabolize these drugs faster
than adults and elderly patients tend to
metabolize them more slowly.
• Cross the placenta and are also excreted
in breast milk
 Antipsychotic drugs’ side effects
Metabolic/endocrine
•Affect metabolism causing weight gain hence risk
of diabetes
•Hyperprolactinemia syndrome and increased
peripheral conversion of androgens to estrogens.
• Amenorrhea, galactorrhea, false-positive
pregnancy tests, and increased libido have been
reported in women, whereas men have
experienced decreased libido, gynecomastia,
Impotence and infertility in men
 Antipsychotic drugs’ side effects
Cont.
Sedation
Bevioural effects
• Toxic confusional state,
pseudodepression
 Side effects -cont...
• Neuroleptic malignant syndrome(NMS)
• Is potentially fatal, idiosyncratic reaction to an
antipsychotic manifested by : Rigidity ,High fever,
Autonomic instability such as unstable blood pressure,
diaphoresis, pallor, delirium and elevated levels of
enzymes (particularly CPK), Confusion,Being
mute ,Fluctuation from agitation to stupor,seizures.
• RX-Discontinue antipsychotics immediately
• Institution of supportive care such as rehydration and
hypothermia, until the client’s physical condition is
stabilized.
 Side effects Cont.
• Extrapyramidal Symptoms (EPS) are serious
neurologic symptoms as a result of blockade of
D2 receptors in the midbrain region of the
brain stem,include: – Acute Dystonia,
Pseudoparkinsonism ,Akathisia &Tardive
Dyskinesia(TD) as below;
• Tardive Dyskinesia-Involuntary movements of
the tongue, facial and neck muscles, upper and
lower extremities, and truncal musculature –
Tongue-thrusting and protrusion, lip-smacking,
blinking.
 side effects Cont.
• Pseudoparkinsonism- bradykinesia, rigidity,
tremor, akathisia (intense need to move
around)
• Acute dystonic reactions (spastic ,
intermittent spasmodic or sustained
involuntary contractions of muscles in the
face, neck, trunk, pelvis, even larynx),
incontrollable seizures,torticollis (twisted
head and neck) .
 Antipsychotic drugs’ side effects
Cont..
• Autonomic effects
Dry mouth, constipation, urinary
retention, orthostatic hypotension,
impaired ejaculation
• Occular complications
Deposits in anterior portions of the eye;
cornea or lens
 Antipsychotic drugs’ side effects
Cont.
• Cardiac toxicity
Overdose of thioridazone associated
with major ventricular arrhythmias.
Ziprasidone prolong QT interval of ECG
• Toxic allergic reactions
Agranulocytosis, cholestatic jaundice,
skin eruptions
 Contraindications
• Should not be used during pregnancy or
lactation .
• Underlying diseases dopamine blocking
effects e.g. CNS depression, comatose
states, phaecromocytoma ( a tumour of
the adrenal medulla -(adrenaline and
noradrenaline secretion).
 CLIENT TEACHING ON
•
ANTIPSYCHOTICS
Drink sugar-free fluids to ease the anticholinergic effects of dry
mouth.
• Avoid calorie-laden beverages, contribute to weight gain
• Constipation prevented by increasing intake of water and bulk-
forming foods in the diet and by exercising.
• Use sunscreen to prevent burning and avoid long periods of time in
the sun.
• Rising slowly from a sitting or lying position will prevent falls from
orthostatic hypotension or dizziness due to a drop in blood
pressure.
• Monitor the amount of sleepiness or drowsiness you experience.
• Blood samples should be taken weekly to monitor the WBC count of
patients with agranulocytosis.
 DRUGS USED TO TREAT
EXTRAPYRAMIDAL SIDE EFFECTS
• Dopaminergic Agonists e.g
• Benztropine (Cogentin) 1- 3 bid 1mg –
2mg
• Anticholinergic Beperiden (Akineton)
2mg tid – qid or,
• Beta-blocker Trihexaphenidyl (Artane)
2mg – 5mg tid -
 2.ANTIDEPRESSANTS
Belong to four classes;
 Tricyclics e.g. amitriptylline, imipramine
 SSRI’s -selective serotonin reuptake inhibitors
and serotonin norepinephrine reuptake
inhibitors (SNRIs).; fluoxetine, fluvoxamine,
paroxetine.
 MAOI’s e.g. phenelzine, tranylcypromine
 Others e.g. bupropion, mirtazepine,
affect norepinephrine and dopamine levels in
the brain
 Anti depressant drugs Cont.
• Depression disorders result from deficiency of
norepinehrine or serotonin at synapses
• NE and serotonin are in mood expression pathways
hence decrease leads to depression and increase
leads to mania.
• Antidepressants do not cause dependence,
tolerance,
• addiction or withdrawal.
• It takes an average of 10-14 days for the beginning
effect and full effect may not be apparent for 4-6
weeks.
 i.Tricyclics
Amitriptyline (Elavil),Clomipramine
(Anafranil),Doxepine,
(Sinequan),Imipramine (Tofranil)
• Block reuptake transporters of both
norepinephrine and serotonin
Pharmacokinetics
• Well absorbed orally
• Undergo first pass metabolism
• Have high volumes of distribution
 Tricyclics Cont.
• Extensive hepatic metabolism required for their
elimination
• Plasma half lives 8-36 hrs permitting OD dosing
• Form active metabolites
Side effects:
• Most common uncomfortable side effects
– sedation
– orthostatic hypotension
– anticholinergic
 Side Effects -- TCAs
• Others
– tremors,
– restlessness, insomnia, confusion
– pedal edema, headache, and seizures
– Blood dyscrasias
– Sexual dysfunction
• Adverse
– cardiotoxicity
• Sympathomimetic – tremor, insomnia
• Antimuscarinic – blurred vision, constipation, urinary
hesitancy, confusion especially in the elderly
Contraindications -Tricyclics
Dementia
Suicidal clients
Cardiac disease
Pregnancy- category D
Seizure disorders
Alcohol
Note; dose for elderly should be 1/2 adult
dose.
 SSRI’s
Paroxetine citalopram,Fluoxetine
(Prozac),Sertraline (Zoloft),Fluvoxamine (Luvox)
• Selectively blocks the reuptake of serotonin into the
neuron
Pharmacokinetics
• Require hepatic metabolism
• Half lives of 18-24hrs
• Fluoxetine forms an active metabolite
 SSRI’s Cont..
with half live of several days hence basis
for weekly dosing
• Inhibit hepatic enzymes increasing
activity of other drugs e.g. TCA and
warfarin
Side effects
• SSRI’s increase risk of suicidal thinking in
children, adolescents and young adults
 SSRI’s side effects Cont..
• Sleep disturbances- insomnia
• Agitation
• Appetite changes, can lead to weight gain
• Sexual dysfunction
• Decreased libido
• Teratogenic potential with use of paroxetine
• Contraindication
 Cardiac dysrrthymias
 Considerations..
• Are safe and are not lethal in overdose
• Good choice for the elderly; has very few
side effects
• If used with MAOI may cause serotonin
syndrome leading to seizures and death
• If used with TCA’s may cause TCA toxicity
• Takes two weeks for effects to be seen
 MAOI’s
Senegeline, phenelzine, tranylcypromine
 MAO metabolizes/breaks down NE, 5HT,
tyramine, dopamine
• Inhibit MAO thus interfering with breakdown
of norepinephrine, dopamine and serotonin.
Pharmacokinetics
• Orally active and given daily
 MAOI’s Cont..
• Inhibit hepatic enzymes and cause drug
interactions
• Tranylcypromine has fastest onset but shorter
duration of action – one week
Toxic effects;
• Hypertensive crisis
• Sympathomimetic effects with foods
containing tyramine e.g. cheese, red wine,
beer, chocolate.
• MAOI’s cause dry mouth and constipation
 3.ANTIANXIETY/ANXIOLYTIC
DRUGS
• Used in patients who have abnormal
levels of anxiety
• Indications
• Post traumatic stress disorder
(PTSD),Generalized Anxiety Disorder
(GAD) ,Panic Disorder, Phobic Disorder ,
Obsessive Compulsive Disorder
(OCD) ,Separation Anxiety Disorder
 Anxiolytics Cont.
• Classes
• i.Benzodiazepines e.g diazepam
(Valium),lorazepam (Ativan)
&alprazolam (Xanax)
• ii.Nonbenzodiazepines e.g busipirone
(BuSpar) &zolpidem (Ambien)
• Target GABA receptors in the brain
which exerts an inhibitory effect on
neurons through increased chloride ion
conductance.
 Anxiolytics Cont.
Pharmacokinetics
Diazepam
• Phase 1 metabolites are
pharmacologically active
• Erratic bioavailability from IM injections
 Anxiolytics Cont..
Pharmacokinetics
• Rapidly absorbed orally but undergoes
extensive first pass metabolism
• Half life is 2-4 hours
• Rimfampicin decreases half life
• Inhibitors of CYP3A4, eg. erythromycin
increase its plasma level
 Anxiolytics Cont.
• Barbiturates increase the duration of
GABA mediated chloride ion channel
opening
• Also block excitatory transmitter
glutamic acid
Effects depend on dose- range from
sedation and relieve of anxiety through
hypnosis to anesthesia and coma.
 Anxiolytics Cont.
• Side effects
Drowsiness- , blurred vision, sleep
disturbances such as nightmares,
confusion, lethargy
Toxic effects; medullary depression
(depression of RS) especially high doses
of alcohol and barbiturates
Dizziness, dry mouth, nervousness’
diarrhoea, headache, excitement.
 Anxiolytics Cont.
Contraindication
 Combination with other CNS antidepresssants
 Renal/hepatic dysfunction
 History of drug abuse or addiction
 Depressive and suicidal tendencies
 Breathing related sleep disorders
 Dizziness, dry mouth, nervousness’ diarrhoea,
headache, excitement.
 Pregnancy and breastfeeding
 Toxicity and overdose
• Symptoms of toxicity include euphoria,
slurred speech,disorientation, unsteady
gait and impaired judgment.
• Symptoms of overdose include
respiratory depression, cold and clammy
skin, hypotension, weak and rapid pulse,
dilated pupils and coma
 Administration
• All antianxiety medications may be taken
orally.
• Antacids interfere with the absorption so
taken until several hours later.
• Some medications may be administered IM/IV
• Benzodiazepines should not be discontinued
abruptly because of the risk of withdrawal
symptoms,gradually reduced carefully.
4.MOOD STABILIZERS /ANTIMANICS
& ANTICONVULSANTS
• Used to treat bipolar disorders or
manic depression which leads to
mood swings- low or high
• Used in schizoaffective disorders
• Lithium is the first line of treatment,
others include carbamazepine
 Mood stabilizers Cont.
Mode of action of lithium
• Action: uncertain, crosses cell membranes,
altering sodium transport.
• Lithium normalizes REM sleep abnormalities
which are present in mood disorders.
• Mood stabilizers which increase GABA activity
seem to have an antimanic, antipanic and
antianxiety effect.
 Mood stabilizers Cont.
• Blood levels monitored (lithium toxicity -
severe diarrhea, vomiting, drowsiness,
muscular weakness, and lack of
coordination, withhold)
 Enhances some actions of serotonin
 Augments synthesis of acetylcholine by
increasing choline uptake
 Mood stabilizers Cont.
• Effects on second messenger intracellular
enzymes that mediate transmitter action
Pharmacokinetics
• Absorbed rapidly and completely from gut
• Distributed throughout body water
• Cleared by kidneys at a rate of 1/5 of
creatinine
 Mood stabilizers Cont.
• Clearance decreases about 25% with use
of thiazide diuretics and NSAID’s
• Half live is 20hrs
• Plasma level altered with changes in
body water; dehydration increases toxic
levels
• Caffeine and theophylline increase renal
clearance
 Mood stabilizers Cont.
• Side Effects: thirst, metallic taste, increased
frequency or urination, fine head and hand
tremor, drowsiness, and mild diarrhea
• Adverse effects
• Neurologic and psychiatric- tremors
• Thyroid enlargement and reduced function-
effect is reversible
• Nephrogenic diabetes insipidus due to loss of
responsiveness to ADH
 Mood stabilizers Cont.
• Oedema due to effect of lithium on
sodium retention
• Cardiac effects; bradycardia –
tachycardia
• Use in pregnancy and breastfeeding; falls
under category D
 Mood stabilizers Cont.
• Can cause toxicity in newborns leading to
lethargy, cyanosis, poor sucking and
moro reflexes and hepatomegally
• Leukocytosis
• Narrow therapeutic window hence need
to monitor blood levels; for acute
symptoms levels are 0.8-1.2meq/l while
maintainace dose is 0.4-0.7meq/l
 Administration
• The administration of lithium is oral, in capsule or
liquid form.
• Both carbamazepine and valproate are available in
tablet and liquid forms. Initially low doses are increased
gradually.
• The ultimate dosages are determined by reduction of
symptoms, blood levels and side effects.
• Patients must continuously be monitored for
hypotension and bradycardia
 Anticonvulsants
• Valporate and derivatives (divalproex sodium -
Depakote)
• Carbamazapine (Tegretol)
• Gabapentin (Neurontin) (least side effects)
• Lamotrigine (Lamictal)
• Topiramate (Topamax)
 Carbamazepine
Side Effects
• Dizziness, drowsiness, tremor, visual
disturbances, nausea, and vomiting
• Minimized by treating in low doses
• Give with food
• Weight gain
• Alopecia (hair loss)
 5.HYPNOTICS-SEDATIVES
• Sedative: A drug that subdues excitement and calms
the subject without inducing sleep, though
drowsiness may be produced
• Hypnotic: A drug that induces and/or maintains sleep,
similar to normal sleep which is can be aroused.
• Tranquilizers may be a more familiar term used to
describe sedative-hypnotic agents
• Benzodiazepines as above in anxiolytics are example
of sedatives-hypnotics
• Benzodiazepines act on the GABA system in the brain
to induce sleep.
 SEDATIVES-HYPNOTICS
• 1.Barbiturates:
Phenobarbitone ,Pentobarbitone,
Butobarbitone, Thiopentone,
• 2. Benzodiazepines: as above in Antianxiety
drugs
 Short-Term Side Effects
• Euphoria-Being in a happy world”
• Fatigue
• Feeling drowsy
• Shallow breathing
• Not being able to take full, deep, normal
breaths
• Trouble coordinating your movements
• Paranoia
• Aggression
 Long term side effects
• Rebound effects-Over use of these drugs can
cause a reversal effect
• Tolerance develops, resulting in dependence
• Withdrawal
• Memory impairment/Amnesia
• Confusion
• Sleepiness
 5.Stimulants
• Any drug that increases bodily functions,
specifically those that stimulate the brain and
nervous system.
• Stimulants stimulate alertness, increase
speech and motor activity, and as well as
decrease appetite.
• Drugs that are considered a Stimulants ●
marijuana ● cocaine ● hallucinogens ●
inhalants ● amphetamines ● tranquilizers
 INDICATIONS/USES
• ADHD ,Narcolepsy ,Prolonged depression Morbid
obesity
• THERAPEUTIC INDICATION - Obesity ,ADHD ,
Narcolepsy
CONTRAINDICATION
• Patient with anorexia
• Insomnia
• Psychopathic personality
• H/O homicidal or suicidal tendencies
 TYPES OF STIMULANTS
• 1.Psychomotor stimulants - cause excitement and euphoria and
decrease feeling of fatigue and increase motor activity E.G
i.Methylxanthines -> Xanthine is a purine base found in most
human body Tissues and flu
• ii.Nicotine -A active ingredient in tobacco. Used in smoking
cessation therapy
• iii.Cocaine
• iv.Amphetamine
• 2.Hallucinogens or Psychomimetic drugs
• .
• 9. 1. Example-Amphetamines
• Used in narcolepsy, ADHD, and obesity
 Other Biological Treatment
• Light Therapy (Phototherapy)
– Reset circadian rhythms
– Used for SAD
• Nutritional Therapies
• Electroconvulsive therapy
 MODEL FOR MANAGEMENT OF
PSYCHIATRIC & MENTAL
DISORDERS
• ALWAYS USE THE BIOPSYCHOSOCIAL MODEL
• 1.BIO-i.DRUGS(REFER TO THE RELEVANT
GROUP OF DRUGS )-MORE THAN ONE DRUG
CLASS CAN BE USED
• ii.ELECTROCONVULSIVE THERAPY(if indicated)
• iii.Nutrition
• iv.Hygiene
 BIOPSYCHOSOCIAL MODEL IN
MNGT-CT
• 2.PSYCHO
• 3.SOCIAL
 Reading assignment
• Apply the steps of the nursing process to the
administration of psychotropic medications.
• Discuss the Role of the nurse in administering
psychotropic drugs.
 ASSIGNMENTS
• READ AND WRITE NOTES ON ROLES OF
NURSE OR NURSING INTERVENTIONS IN
PSYCHOPHARMACOTHERAPY
 References

• Katzung, B. G., Masters S. B., Trevor A. J.,

(2009), Basic and clinical pharmacology,
11th McGraw- Hill companies.