1. PSYCHOPHARMACOLOGY

2. Terms Psychotropic medication: Neurotransmitter: Receptor:
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

3. Effects of psychotropic medications on neurotransmitters
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
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

4. 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 antagonism
Adrenergic receptor blockade
Reduce anxiety
Nausea, sedation, orthostasis, priapism
SSNRI’s: venlafaxine and duloxetine
Potent inhibitor of seretonin & norepinephrine reuptake
Weak inhibitor of dopamine reuptake
Relieve pain of neuropathy (duloxetine)
Relieve anxiety (venlafaxine)
Nausea, increased sweating, insomnia, tremors, sexual dysfunction
Bupropion
Inhibits reuptake of 5-HT. NE & dopamine
Reduce depression, aid in smoking cessation, reduce symptoms of ADHD
Insomnia, dry mouth, tremor, seizures

5. 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
Sedation
Dependency (with long term use)
Confusion, memory impairment, motor incoordination

6. 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
Nausea, headache, dizziness
Restlessness

7. 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.

8. 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

9. 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)

10. 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

11. Cont… Side effects with all chemical classes:
Dry mouth
Sedation
Nausea
Discontinuation syndrome
Hepatic failure
Side effects with MAOI’s:
Hypertensive crisis

12. Cont… Side effects with tricyclics: Blurred vision Constipation
Urinary retention
Orthostatic hypotension
Reduction of seizure threshold
Tachycardia; arrhythmias
Photosensitivity
Weight gain

13. Cont… Side effects with SSRI’s: Insomnia, agitation Headache
Weight loss
Sexual dysfunction
Seretonin syndrome

14. 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

15. 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

16. 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

17. 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

18. Cont… Side effects of anticonvulsants: Side effects of antipsychotics:
Nausea/ vomitting
Drowsiness, dizziness
Blood dyscrasias
Prolonged bleeding time
Risk of severe rash
Decreased efficacy with oral contraceptives
Side effects of antipsychotics:
Dry mouth, constipation
Increased appetite, weight gain
ECG changes
Extra Pyramidal Symptoms
Hyperglycemia & diabetes

19. 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

20. 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

21. 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

22. Cont… Extrapyramidal symptoms (EPS) Pseudoparkinsonism Akinesia
Akathisia
Dystonia
Oculogyric crisis
Tardive dyskinesia
Neuroleptic malignant syndrome
Hyperglycemia and diabetes

23. 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

24. 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

25. 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

26. 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

27. Examples Chemical class Generic (trade) name Amphetamines
Dextroamphetamine sulfate, Methamphetamine
Amphetamine mixtures
Dextroamphetamine/ amphetamine
Miscellaneous
Methylphenidate, Dexmethylphenidate, Pemoline, Atomoxetine, Bupropion