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• 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 depressionControl anxietyControl obsessions
Nausea, agitation, headache, sexual dysfunction
Tricyclic antidepressants
Inhibit reuptake of seretonoinInhibit reuptake of norepinephrine (NE)Block NE receptorBlock ACh receptorBlock histamine receptor
Reduce depressionRelief of severe painPrevent 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/
ReceptorPhysiological effects
Side effects
MAO inhibitors Increase NE & 5 – HT by inhibiting the enzyme that degrades them (MAO – A)
Reduce depressionControl anxiety
Sedation, dizzinessSexual dysfunctionHypertensive crisis (interaction with tyramine)
Trazodone & nefazadone
5 – HT2 receptor antagonismAdrenergic receptor blockade
Reduce depressionReduce anxiety
Nausea, sedation, orthostasis, priapism
SSNRI’s: venlafaxine and duloxetine
Potent inhibitor of seretonin & norepinephrine reuptakeWeak inhibitor of dopamine reuptake
Reduce depressionRelieve 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
Cont…Medication Action on NT/
ReceptorPhysiological effects Side effects
Antipsychotics: phenothiazines and haloperidol
Strong D, receptor blockadeWeaker blockade of ACh, H1, alpha adrenergic & 5-HT2 receptors
Relief of psychosisRelief of anxiety(Some) provide relief from nausea and vomitting and intractable hiccoughs
Blurred vision, dry mouth, decreased sweating, constipation, urinary retention. TachycardiaEPS, 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 anxietySedation
Dependency (with long term use)Confusion, memory impairment, motor incoordination
Cont…Medication Action on NT/
ReceptorPhysiological effects
Side effects
Antipsychotics (novel): clozapine, olanzapine, arip[iprazole, quetiapine, risperidone, ziprasidone
Receptor antagonism of 5-HTD1 – D5 (varies with drug)H1, alpha 1 adrenergic, muscarinic (ACh)
Relief of psychosis (with minimal or no EPS)Relief of anxietyRelief of acute mania
Potential with some of the drugs for mild EPS (D2)Sedation, weight gain (H1)Orthostasis & dizzinessBlurred vision, dry mouth, decreased sweating, constipation, urinary retention, tachycardia (ACh)
Antianxiety: buspirone
5-HT agonistD2 agonistD2 antagonist
Relief of anxiety Nausea, headache, dizzinessRestlessness
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 AGENTSANTIMANIC:
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 crisisTardive dyskinesiaNeuroleptic malignant syndromeHyperglycemia 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
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