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42 Cards in this Set

  • Front
  • Back
Tricyclics and heterocyclics, reuptake inhibitors, MAOi's, etc
Antidepressant Agents
What is used to treat Mania?
What are benzodiazepines used for?
Barbituates are sedative-hypnotics, what are these used for?
Panic and phobic disorders
What are some anti-psychotic agents?
Phenothiazines and Non-phenothiazines
Rank the 3 types of depression from least to most common...
3. Bipolar Affective
2. Major Depression
1. Reactive Depression
Refers to 3 ring nucleus (some have 4)
Aliphatic side chain attached to N in center ring
Tertiary or secondary amines
First thought to be antihistamines with sedative properties
Tricyclic Antidepressants
What is the mechanism of action for TCAs?
-primary action: Block reuptake of NE and 5HT to increase synaptic concentrations

-secondary action: Block muscarinic, block perpheral alpha (orthostatic hypotension), block histamine, sedation and drowsiness
What are some TCAs?
Impramine, amitriptyline, mixed NE and 5HT reuptake inhibitors
What are TCA clincial characteristics?
Produce immediate increases in neurotransmitter levels. Significant delay in clinical efficacy (2-4 weeks).
Chronic treatment maintained for 6 months.
What are the adverse reactions for TCAs?
Sympathomimetic (tremor, insomnia)
Anticholinergic (orthostatic hypotension, sedation)
Confusion, disorientation, anxiety, delerium, altered appetite, nausea, gastric distress
What are some SSRIs?
Paroxetine, sertraline, Fluvoxamine, Citalopram
What are side effects of SSRIs?
Less severe than TCAs (anticholinergic/cardiovascular) others include: nausea, headache, decrease appetite, diarrhea, nervousness, anxiety)
True or False?
SSRIs are often used with MAOi's?
What are some second generation antidepressants?
Maprotiline, amoxapine, Bupropion, Trazodone
What drug is this?

Inhibits NET
Associated with increased risk of tonic-clonic seizures
resembles TCA, desipramine
What drug is this?

Metabolite of loxapine, has some antipsychotic action.
DA receptor antagonist
Useful for deression in psychotic patients
Side effects: Akathisia, parkinsonism, amenrrhe-galactorrhea syndrome
What drug is this?

Stucturally similiar to amphetamines
Blocks DAT
Weak 5HTT and NET blocker
can precipitate seizures
What drug is this?

5HT receptor agonist
Unpredictable efficacy for depression
Chronic administration leads to 5HT receptor down regulation
Side effects: drowsiness, dizziness, light headache, orthostatic hypotension, tachycardia
"Third generation" Antidepressant

-Chemically unique, short half life
Potent blocker of 5HTT and weak inhibitor of NET
Down regulates 5HT and beta receptors
Does not bind to muscarinic, alpha 1, H1
Less side effects
Low dose acts like SSRI
May produce dose related hypertension
Third generation Antidepressant

Analog of widely used European antidepressant
Greater sedation effects than other "third generation"
Does not block 5HTT or NET
Antagonist of central alpha2 presynaptic
Results in increase of NE and 5HT into synapse
Blocks 5HT2 and 5HT3 receptors
Different duration of action
Useful for non resondents to TCA and SSRI
Side effects: drowsiness, weight gain, atropine like effects, orthostatic hypotension, elevate cholestrol and triglycerides, liver effects
Third generation antidepressant

Developed on the basis of trazodone
Blocks 5HTT and NET
Converted to active metabolite which acts as 5HT receptor agonist
Potent inhibitor of CYP3A4
Less sedating than other "third generation"
Fewer adverse sexual side effects than SSRI
What are the classes of MAOIs?
Tranylcypromine and Hydrazides (Phenelzine and Isocarboxazid)
What is the MOA for MAOIs?
Inhibits MAO enzyme leading to increased concentration in synapse.
How long does inhibition of MAO persist after secassion?
7 days for tranylcypromine
2-3 weeks for Phenelzine
What is tyramine?
A monoamine derived from the decarboxylation of tyrosine during fermentation or decay. It is found in certain foods. If tyramine metabolism is compromised by MAOi, then high levels of tyramine may cause hypertensive crisis. (cheese syndrome)
What are some adverse reactions of MAOIs?
CNS stimulant
Cardiovascular hypertension
tyramine cause release of catecholamines (cheese syndrome)
General hypotension
Blood dyscrasias
Food interactions
Sexual disturbances
What are some drug-drug interactions of MAOi's?
Amphetamines, nasal decongestants, appetite suppressants, TCA and MAO inhibitors
What are the therapeutic uses of MAOIs?
Adult major depression
tourette's syndrome
Axiety Disorder
Post-traumatic stree Syndrome
Psychosomatic disorders
What is the treatment of MAOI overdose?
Phenothiazines, with alpha2 blocking (i.e. chlorpromazine)
What are some Antimanic Agents?
Lithium, Carbamazepine, and Valproic acid
What drugs is Lithium given in conjunction with because of time-delay?
Phenothiazine or Haloperidol
Lithium readily passes the BBB and also replaces intracellular Na+ and alters neurotransmitter synthesis, release, and reuptake. More specifically, how does it treat mania and depression?
Antimanic properties
-GABA increase
-DA decrease

Antidepressive properties
-5HT increase

Interferes with G-proteins and adenylate cyclase activity.
What are some adverse reactions to Lithium?
1. Toxicity greater than 2.0 mEq/L
2. GI distress
3. Neuromuscular and CNS distrubances
4. Cardiovascular
5. Renal
6. Thyroid
The half life of Lithium is approximately 24 hours...What are some methods to treat Lithium toxicity?
-NaCl in high volume to flush kidneys
-Osmotic diuresis using mannitol and Aminophylline
-Hemodialysis if experiencing renal failure
What are some symptoms of Psychosis?
-Impaired behavior
-Distorted thinking
-Inability to comprehend reality
-Impaired reasoning
-Delusion and hallucination
How do most but not all antipsychotic drugs work?
Most antipsychotic drugs block post synaptic D2 receptors.
If an antipsychotic drug does not block dopamine, what other neurotransmitters are sometimes affected?
Serotonin, Glutamate, and other treatments
First and largest group of antipsychotic agents.
Chemical structure: Characterized by a tricyclic nucleus of 2 benzene rings joined by a central ring bridged by a S atom and N atom.
Phenothiazines (PZ)
What are the three chemical classes of Phenothiazines based on substitution at position 10?
Aliphatic, Piperdine, and Piperazine
Antipsychotic activity is Structure Directed. What are some requirements of the structures for activity to occur?
1. Substitution at N (position 10) required for activity
2. Substitution on ring at position 2 enhances activity
3. N-alkyl groups required for activity
4. 3-carbon chain required for antipsychotic activity
How is the potency of antipsychotic drugs related to the adverse effects?
In general, typical high potency antipsychotic drugs show greater EPRs.
Low potency antipsychotic drugs show greater sedative effects, hypotension and autonomic side effects.