PSYCHOPHARMACOLOGY
Terms
• Psychotropic medication:
– Medications that affects psychic function,
behavior or experience
• Neurotransmitter:
– A chemical that is stored in the axon terminals of
the presynaptic neuron
• Receptor:
– Molecules situated on the cell membrane that are
binding sites for neurotransmitters
Effects of psychotropic medications on
neurotransmitters
Medication
Action on NT/
Receptor
Physiological effects Side effects
SSRI’s
Inhibit reuptake of
seretonin
Reduce depression
Control anxiety
Control obsessions
Nausea, agitation,
headache, sexual
dysfunction
Tricyclic
antidepressants
Inhibit reuptake of
seretonoin
Inhibit reuptake of
norepinephrine (NE)
Block NE receptor
Block ACh receptor
Block histamine
receptor
Reduce depression
Relief of severe pain
Prevent panic
attacks
Sexual dysfunction
(NE & 5 – HT)
Sedation, weight
gain (H1)
Dry mouth,
constipation,
blurred vision,
urinary retention
(ACh), postural
hypotension and
tachycardia
Cont…
Medication
Action on NT/
Receptor
Physiological
effects
Side effects
MAO inhibitors
Increase NE & 5 –
HT by inhibiting the
enzyme that
degrades them
(MAO – A)
Reduce depression
Control anxiety
Sedation, dizziness
Sexual dysfunction
Hypertensive crisis
(interaction with
tyramine)
Trazodone &
nefazadone
5 – HT2 receptor
Reduce depression
antagonism
Reduce anxiety
Adrenergic receptor
blockade
Nausea, sedation,
orthostasis,
priapism
SSNRI’s: venlafaxine Potent inhibitor of
and duloxetine
seretonin &
norepinephrine
reuptake
Weak inhibitor of
dopamine reuptake
Reduce depression
Relieve pain of
neuropathy
(duloxetine)
Relieve anxiety
(venlafaxine)
Nausea, increased
sweating, insomnia,
tremors, sexual
dysfunction
Bupropion
Reduce depression,
aid in smoking
cessation, reduce
symptoms of ADHD
Insomnia, dry
mouth, tremor,
seizures
Inhibits reuptake of
5-HT. NE &
dopamine
Cont…
Medication
Action on NT/
Receptor
Physiological effects Side effects
Antipsychotics:
phenothiazines and
haloperidol
Strong D, receptor
blockade
Weaker blockade of
ACh, H1, alpha
adrenergic & 5-HT2
receptors
Relief of psychosis
Relief of anxiety
(Some) provide
relief from nausea
and vomitting and
intractable
hiccoughs
Blurred vision, dry
mouth, decreased
sweating,
constipation, urinary
retention.
Tachycardia
EPS, increased
plasma prolactin
(D2), sedation,
weight gain (H1),
ejaculatory difficulty
(5-HT2), orthostatic
hypotension
Antianxiety:
benzodiazepines
Binds to BZ receptor
sites on the GABA
receptor complex,
increases receptor
affinity for GABA
Relief of anxiety
Sedation
Dependency (with
long term use)
Confusion, memory
impairment, motor
incoordination
Cont…
Medication
Action on NT/
Receptor
Physiological
effects
Side effects
Antipsychotics
(novel): clozapine,
olanzapine,
arip[iprazole,
quetiapine,
risperidone,
ziprasidone
Receptor
antagonism of 5-HT
D1 – D5 (varies with
drug)
H1, alpha 1
adrenergic,
muscarinic (ACh)
Relief of psychosis
(with minimal or no
EPS)
Relief of anxiety
Relief of acute
mania
Potential with some
of the drugs for
mild EPS (D2)
Sedation, weight
gain (H1)
Orthostasis &
dizziness
Blurred vision, dry
mouth, decreased
sweating,
constipation,
urinary retention,
tachycardia (ACh)
Antianxiety:
buspirone
5-HT agonist
D2 agonist
D2 antagonist
Relief of anxiety
Nausea, headache,
dizziness
Restlessness
ANTIANXIETY AGENTS
• Indications
– These are also called anxiolytics and minor
tranquilizers.
– These are used in the treatment of anxiety
disorders, anxiety symptoms, acute alcohol
withdrawal, skeletal muscle spasms, convulsive
disorders, status epilepticus and preoperative
sedation.
Cont…
• Side effects:
–
–
–
–
–
–
–
–
–
–
Drowsiness, confusion, lethargy
Tolerance; physical & psychological dependence
Ability to potentiate the effects of other CNS depressants
Possibility of aggravating symptoms in depressed persons
Orthostatic hypotension
Paradoxical excitement
Dry mouth
Nausea & vomiting
Blood dyscrasias
Delayed onset
Examples
Chemical class
Generic (trade) name
Antihistamines
Hydroxyzine (Atarax, Vistaril)
Benzodiazepines
Alprazolam (Xanax)
Chlordiazepoxide (Librium)
Clonazepam (Klonopin)
Clorazepate (Traxene)
Diazepam (Valium)
Lorazepam (Ativan)
Oxazepam (Serax)
Propanediols
Meprobamate (Miltown)
Azaspirodecanediones
Buspirone (BuSpar)
ANTIDEPRESSANTS
• Indications:
– It is used in the treatment of dysthymic disorder,
major depression with melancholia or psychotic
symptoms, depression associated with organic
disease, alcoholism, schizophrenia or mental
retardation, depressive phase of bipolar disorder
and depression accompanied by anxiety.
– These drugs elevate mood and alleviate other
symptoms associated with moderate-to-severe
depression
Cont…
• Side effects with all chemical classes:
– Dry mouth
– Sedation
– Nausea
– Discontinuation syndrome
– Hepatic failure
• Side effects with MAOI’s:
– Hypertensive crisis
Cont…
• Side effects with tricyclics:
– Blurred vision
– Constipation
– Urinary retention
– Orthostatic hypotension
– Reduction of seizure threshold
– Tachycardia; arrhythmias
– Photosensitivity
– Weight gain
Cont…
• Side effects with SSRI’s:
– Insomnia, agitation
– Headache
– Weight loss
– Sexual dysfunction
– Seretonin syndrome
Examples
Chemical class
Generic (trade) name
Tricyclics
Amitriptyline, Amoxapine, Clomipramine, Desipramine,
Doxepin, Imipramine, Nortriptyline, Protriptyline,
Trimipramine
SSRI’s
Citralopram, Fluoxetine, Fluvoxamine, Escitalopram,
Paroxetine, Sertraline
MAOI
Isocarboxazid, Phenelzine, Tranylcypromine
Others
Bupropion, Maprotiline, Mirtazapine, Trazodone,
Nefazodone, Venlafaxine, Duloxetine
MOOD STABILIZING AGENTS
ANTIMANIC:
Prevention and treatment of manic episodes of
bipolar disorder, alcohol dependence, major
depression
ANTICONVULSANTS:
All stages of seizures
CALCIUM CHANNEL BLOCKERS:
Angina, arrhytmias, hypertension, bipolar mania,
migraine headache
ANTIPSYCHOTICS:
Schizophrenia, bipolar mania
Cont…
Chemical class
Generic (trade) name
Antimanic
Lithium carbonate
Anticonvulsants
Clonazepam, carbamazepine, valporic acid, lamotrigine,
gabapentin, topiramate
Calcium channel blocker
Verapamil
Antipsychotics
Olanzapine, aripiprazole, chlorpromazine, quetiapine,
risperidone, ziprasidone
Cont…
• Side effects of antimanic:
–
–
–
–
–
–
–
Drowsiness, dizziness, headache
Dry mouth, thirst
GI upset, nausea/ vomiting
Fine hand tremors
Hypotension, arrhythmias, pulse irregularities
Polyuria, dehydration
Weight gain
• Side effects of calcium channel blockers:
–
–
–
–
drowsiness, dizziness
Hypotension, bradycardia
Nausea
constipation
Cont…
• Side effects of anticonvulsants:
–
–
–
–
–
–
Nausea/ vomitting
Drowsiness, dizziness
Blood dyscrasias
Prolonged bleeding time
Risk of severe rash
Decreased efficacy with oral contraceptives
• Side effects of antipsychotics:
–
–
–
–
–
–
Drowsiness, dizziness
Dry mouth, constipation
Increased appetite, weight gain
ECG changes
Extra Pyramidal Symptoms
Hyperglycemia & diabetes
ANTIPSYCHOTIC AGENTS
• Indications:
– These are also called major tranquilizers and
neuroleptics.
– They are used in the treatment of acute and chronic
psychoses particularly when accompanied by
increased psychomotor activity
– Selected agents are used as antiemetics in the
treatment of intractable hiccoughs and for the control
of tics and vocal utterances in Tourette’s disorder
Examples
Chemical class
Generic (trade) name
Phenothiazines
Chlorpromazine, Fluphenazine, Perphenazine,
Prochlorperazine, Thioridazine, Trifluoperazine
Thioxanthene
Thiothixene
Benzisoxazole
Risperidone
Dibenzoxazepine
Loxapine
Dihydroindolone
Molindone
Dibenzodiazepine
Clozapine
Diphenylbutylpiperidine
Pimozide
Thienobenzodiazepine
Olanzapine
Dibenzothiazepine
Quetiapine
Benzothiazolylpiperazine
Ziprasidone
Dihydrocarbostyril
Aripiprazole
Cont…
• Side effects of antipsychotics:
– Anticholinergic effects such as dry mouth, blurred vision,
constipation, urinary retention
– Nausea, GI upset
– Skin rash
– Sedation
– Orthostatic hypotension
– Photosensitivity
– Hormonal effects
– ECG Changes
– Reduction of seizure threshold
– Agranulocytosis
– Hypsersalivation
Cont…
• Extrapyramidal symptoms (EPS)
– Pseudoparkinsonism
– Akinesia
– Akathisia
– Dystonia
– Oculogyric crisis
Tardive dyskinesia
Neuroleptic malignant syndrome
Hyperglycemia and diabetes
SEDATIVE HYPNOTICS
• Indications:
– They are used in the short term management of
various anxiety states and to treat insomnia.
– Selected agents are used as anticonvulsants and
preoperative sedatives and to reduce anxiety
associated with drug withdrawal
Examples
Chemical class
Generic (trade) name
Barbiturates
Amobarbital, Butabarbital, Mephobarbital,
Pentobarbital, Phenobarbital, Secobarbital
Benzodiazipines
Estazolam, Flurazepam, Quazepam, Temazepam,
Triazolam
Miscellaneous
Chloral hydrate, Eszopiclone, Zaleplon, Zolpidem
Cont…
• Side effects:
–
–
–
–
–
–
–
–
–
–
Drowsiness, confusion, lethargy
Tolerance; physical & psychological dependence
Ability to potentiate the effects of other CNS depressants
Possibility of aggravating symptoms in depressed persons
Orthostatic hypotension
Paradoxical excitement
Dry mouth
Nausea & vomiting
Blood dyscrasias
Delayed onset
Newer trends – agents for ADHD
• Indications:
– These are used for ADHD in children and adults
• Side effects:
–
–
–
–
–
–
–
Overstimulation, restlessness, insomnia
Palpitations, tachycardia
Anorexia, weight loss
Tolerance, physical and psychological dependence
Nausea and vomiting
Constipation
Potential for seizures
Examples
Chemical class
Generic (trade) name
Amphetamines
Dextroamphetamine sulfate, Methamphetamine
Amphetamine mixtures
Dextroamphetamine/ amphetamine
Miscellaneous
Methylphenidate, Dexmethylphenidate, Pemoline,
Atomoxetine, Bupropion