Pharmacology Exam Iv (Fall 2006) (Card Set #2)

Front 1

Tricyclics and heterocyclics, reuptake inhibitors, MAOi's, etc

Back 1

Antidepressant Agents

Front 2

What is used to treat Mania?

Back 2

Lithium

Front 3

What are benzodiazepines used for?

Back 3

Antianxiety

Front 4

Barbituates are sedative-hypnotics, what are these used for?

Back 4

Panic and phobic disorders

Front 5

What are some anti-psychotic agents?

Back 5

Phenothiazines and Non-phenothiazines

Front 6

Rank the 3 types of depression from least to most common...

Back 6

3. Bipolar Affective
2. Major Depression
1. Reactive Depression

Front 7

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

Back 7

Tricyclic Antidepressants

Front 8

What is the mechanism of action for TCAs?

Back 8

-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

Front 9

What are some TCAs?

Back 9

Impramine, amitriptyline, mixed NE and 5HT reuptake inhibitors

Front 10

What are TCA clincial characteristics?

Back 10

Produce immediate increases in neurotransmitter levels. Significant delay in clinical efficacy (2-4 weeks).
Chronic treatment maintained for 6 months.

Front 11

What are the adverse reactions for TCAs?

Back 11

Sympathomimetic (tremor, insomnia)
Anticholinergic (orthostatic hypotension, sedation)
Confusion, disorientation, anxiety, delerium, altered appetite, nausea, gastric distress

Front 12

What are some SSRIs?

Back 12

Paroxetine, sertraline, Fluvoxamine, Citalopram

Front 13

What are side effects of SSRIs?

Back 13

Less severe than TCAs (anticholinergic/cardiovascular) others include: nausea, headache, decrease appetite, diarrhea, nervousness, anxiety)

Front 14

True or False?
SSRIs are often used with MAOi's?

Back 14

False

Front 15

What are some second generation antidepressants?

Back 15

Maprotiline, amoxapine, Bupropion, Trazodone

Front 16

What drug is this?

Tetracycic
Inhibits NET
Associated with increased risk of tonic-clonic seizures
resembles TCA, desipramine

Back 16

Maprotiline

Front 17

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

Back 17

Amoxapine

Front 18

What drug is this?

Stucturally similiar to amphetamines
Blocks DAT
Weak 5HTT and NET blocker
can precipitate seizures

Back 18

Bupropion

Front 19

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

Back 19

Trazodone

Front 20

"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

Back 20

Venlafaxine

Front 21

Third generation Antidepressant

Analog of widely used European antidepressant
Tetracyclic
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

Back 21

Mirtazpine

Front 22

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

Back 22

Nefazodone

Front 23

What are the classes of MAOIs?

Back 23

Tranylcypromine and Hydrazides (Phenelzine and Isocarboxazid)

Front 24

What is the MOA for MAOIs?

Back 24

Inhibits MAO enzyme leading to increased concentration in synapse.

Front 25

How long does inhibition of MAO persist after secassion?

Back 25

7 days for tranylcypromine
2-3 weeks for Phenelzine

Front 26

What is tyramine?

Back 26

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)

Front 27

What are some adverse reactions of MAOIs?

Back 27

CNS stimulant
Cardiovascular hypertension
tyramine cause release of catecholamines (cheese syndrome)
General hypotension
Blood dyscrasias
Jaundice
Food interactions
Sexual disturbances

Front 28

What are some drug-drug interactions of MAOi's?

Back 28

Amphetamines, nasal decongestants, appetite suppressants, TCA and MAO inhibitors

Front 29

What are the therapeutic uses of MAOIs?

Back 29

Adult major depression
ADD
tourette's syndrome
Axiety Disorder
Post-traumatic stree Syndrome
Psychosomatic disorders

Front 30

What is the treatment of MAOI overdose?

Back 30

Phenothiazines, with alpha2 blocking (i.e. chlorpromazine)

Front 31

What are some Antimanic Agents?

Back 31

Lithium, Carbamazepine, and Valproic acid

Front 32

What drugs is Lithium given in conjunction with because of time-delay?

Back 32

Phenothiazine or Haloperidol

Front 33

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?

Back 33

Antimanic properties
-GABA increase
-DA decrease

Antidepressive properties
-5HT increase

Interferes with G-proteins and adenylate cyclase activity.

Front 34

What are some adverse reactions to Lithium?

Back 34

1. Toxicity greater than 2.0 mEq/L
2. GI distress
3. Neuromuscular and CNS distrubances
4. Cardiovascular
5. Renal
6. Thyroid

Front 35

The half life of Lithium is approximately 24 hours...What are some methods to treat Lithium toxicity?

Back 35

-NaCl in high volume to flush kidneys
-Osmotic diuresis using mannitol and Aminophylline
-Hemodialysis if experiencing renal failure

Front 36

What are some symptoms of Psychosis?

Back 36

-Impaired behavior
-Distorted thinking
-Inability to comprehend reality
-Impaired reasoning
-Agitation
-Delusion and hallucination

Front 37

How do most but not all antipsychotic drugs work?

Back 37

Most antipsychotic drugs block post synaptic D2 receptors.

Front 38

If an antipsychotic drug does not block dopamine, what other neurotransmitters are sometimes affected?

Back 38

Serotonin, Glutamate, and other treatments

Front 39

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.

Back 39

Phenothiazines (PZ)

Front 40

What are the three chemical classes of Phenothiazines based on substitution at position 10?

Back 40

Aliphatic, Piperdine, and Piperazine

Front 41

Antipsychotic activity is Structure Directed. What are some requirements of the structures for activity to occur?

Back 41

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

Front 42

How is the potency of antipsychotic drugs related to the adverse effects?

Back 42

In general, typical high potency antipsychotic drugs show greater EPRs.
Low potency antipsychotic drugs show greater sedative effects, hypotension and autonomic side effects.