Antidepressants and Anxiolytics Med Chem

Question 1

What is the most common mood disorder in adults?

Answer 1

Major depressive disorder

Question 2

Criteria required for diagnosis of major depressive disorder

Answer 2

One or more depressive episodes without a history of manic, mixed or hypomanic episodes

Question 3

Monoamine hypothesis

Answer 3

Deficiency or imbalances in the monoamine neurotransmitters (serotonin, norepinephrine, dopamine) causes depression

Question 4

Based on the monoamine hypothesis, increasing which two neurotransmitters could alleviate depression?

Answer 4

Serotonin and norepinephrine

Question 5

Drugs that selectively increase which neurotransmitter decrease depression?

Answer 5

Serotonin

Question 6

Hypercholinergic hypothesis of depression

Answer 6

Hyperactivity of cholinergic system and excessive nicotinic receptor activity can lead to depression

Question 7

Examples of antidepressants with nicotinic acetylcholine receptor inhibitory activity

Answer 7

Bupropion
Nicotinic transdermal patch

Question 8

Which amino acid is a precursor for serotonin?

Answer 8

Tryptophan

Question 9

Which enzyme is responsible for serotonin synthesis?

Answer 9

Tryptophan hydroxylase

Question 10

Which amino acid is a precursor for norepinephrine?

Answer 10

Tyrosine

Question 11

Which enzyme is responsible for norepinephrine synthesis?

Answer 11

Tyrosine hydroxylase

Question 12

True or false: For all monoamines, the first synthetic step is rate limiting

Answer 12

True

Question 13

Serotonin is transported into the vesicles via what?

Answer 13

Vesicular monoamine transporter (VMAT)

Question 14

Reserpine binds irreversibly to what to inhibit packaging of DA, NE, EPI, and 5-HT into vesicles?

Answer 14

VMAT

Question 15

What two compounds degrade serotonin?

Answer 15

Monoamine oxidase (MAO) and catechol-O-methyl-transferase (COMT)

Question 16

MAO inhibitor MOA

Answer 16

Increase serotonin and norepinephrine available in the cytoplasm by blocking the deamination of monoamines via MAO

Question 17

MAOi contrindications

Answer 17

Concomitant use of: sympathomimetic drugs, other MAOIs, L-DOPA, L-tryptophan, phenylalanine, bupropion, excessive coffee, chocolate intake, high tyramine containing foods, heart failure, general anesthesia, local anesthesia with vasoconstrictors, liver disease

Question 18

What is the result of MAOi use with high levels of tyramine?

Answer 18

Hypertension

Question 19

Between tertiary and secondary amines, which exhibit more selectivity?

Answer 19

Secondary amines selectively inhibit norepinephrine reuptake (still have some serotonin reuptake activity)

Question 20

Examples of tertiary amine TCAs

Answer 20

Clomipramine
Imipramine
Doxepin
Amitriptyline

Question 21

Fluoxetine 20mg target plasma level

Answer 21

200 ng/mL

Question 22

SSRI contraindication

Answer 22

Concomitant use of MAOi

Question 23

Concomitant use of SSRIs and MAOis can lead to what?

Answer 23

Serotonin syndrome

Question 24

SSRI monotherapy in bipolar patients can lead to what?

Answer 24

Mania

Question 25

SSRI examples

Answer 25

Fluoxetine Paroxetine Sertraline Fluvoxamine Citalopram Escitalopram

Question 26

SNRI contraindication

Answer 26

Concomitant use of MAOi

Question 27

SNRI examples

Answer 27

Venlafaxine Desvenlafaxine Duloxetine Milnacipran Levomilnacipran

Question 28

Bupropion (NDRI) contraindications

Answer 28

Concomitant use of MAOi Seizure disorders Eating disorders Patients undergoing abrupt discontinuation of alcohol or sedatives

Question 29

Common adverse effects of agents with mixed serotonergic effects

Answer 29

Nausea, vomiting, diarrhea, constipation, dizziness

Question 30

Examples of mood stabilizers

Answer 30

Carbamazepine Valproic acid Lithium carbonate

Question 31

Lithium MOA

Answer 31

Therapeutic plasma levels of lithium deplete inositol pool available for resynthesis, reducing neuronal activity in the brain

Question 32

The R-enantiomer of ketamine has a (higher/lower) affinity for NMDA receptors than the S-enantiomer

Answer 32

Lower

Question 33

Esketamine contraindications

Answer 33

Ketamine hypersensitivity, aneurysmal vascular disease, intracerebral hemorrhage

Question 34

Ketamine MOA

Answer 34

NMDA receptor antagonist; increases synaptic glutamate activity

Question 35

Generalized anxiety disorder

Answer 35

Persistent and excessive anxiety and worry

Question 36

Panic disorder

Answer 36

Recurrent unexpected panic attacks and is persistently concerned or worried about having more panic attacks or changes their behavior in maladaptive ways because of panic attacks

Question 37

Social anxiety disorder

Answer 37

Fearful or anxious about or avoidant of social interactions and situations

Question 38

Substance/medication-induced anxiety disorder

Answer 38

Substance intoxication or withdrawal or to a medication treatment

Question 39

(Ionotropic/Metabotropic) GABA receptors bind GABA and open intrinsic Cl- channels

Answer 39

Ionotropic (GABAa)

Question 40

Which drug class is most effective and most commonly prescribed drugs for rapid relief of anxiety symptoms?

Answer 40

Benzodiazepines

Question 41

Benzodiazepine MOA

Answer 41

Positive allosteric modulators that enhance GABAa receptor channels in the presence of GABA

Question 42

Benzodiazepine antagonist

Answer 42

Flumazenil (Romazicon)

Question 43

What pharmacokinetic property of benzodiazepines explains their rapid and complete absorption?

Answer 43

Highly lipophilic

Question 44

Classify and explain reaction between benzodiazepines and alcohol

Answer 44

Pharmacodynamic. Additive CNS depressive effects

Question 45

Classify and explain reaction between benzodiazepines and CYP450 inhibitors (ketoconazole, ritonavir, etc.)

Answer 45

Pharmacokinetic. Increase concentration of benzodiazepines

Question 46

Which class of agents are considered first line in managing generalized anxiety disorder?

Answer 46

Antidepressants

Question 47

What is the place of therapy of buspirone in managing generalized anxiety disorder?

Answer 47

Second line agent