CNS Drugs: Psyche drugs

Question 1

Mechanism: selective blockade of 5HT reuptake
• Uses:
– Major depression
– OCD
– Bulimia
– Anxiety disorders (chronic treatment/acute, benzodiazepines)
– Premenstrual dysphoric disorder (PMDD)

Answer 1

Selective Serotonin Reuptake Inhibitors (SSRIs)

ie fluoxetine, paroxetine, sertraline, citalopram, fluvoxamine

Question 2

Major S/E of SSRIs

Answer 2

anxiety, agitation, bruxism, sexual dysfunction, weight loss

Question 3

Toxicity of SSRIs

Answer 3

serotonin syndrome:sweating, rigidity, myoclonus, hyperthermia, ANS
instability, seizures

Question 4

Drug interactions with SSRIs

Answer 4

MAOIs, TCAs, and meperidine

Question 5

SSRI inhibitors of Cytochrome P450

Answer 5

fluvoxamine

and fluoxetine

Question 6

Drugs: amitriptyline, imipramine, and clomipramine

• Mechanism: nonspecific blockade of 5HT and NE reuptake
• Uses:
– Major depressions
– Phobic and panic anxiety states
– Obsessive-compulsive disorders (OCDs)
– Neuropathic pain
– Enuresis

Answer 6

Tricyclic Antidepressants (TCAs)

Question 7

TCA S/E

Answer 7

muscarinic and α blockade

Question 8

TCA toxicity

Answer 8

“3 Cs”: coma, convulsions, and cardiotoxicity”

Question 9

TCA drug interactions

Answer 9

Hypertensive crisis with MAO inhibitors
– Serotonin syndrome with SSRIs, MAO inhibitors, and meperidine
– Prevent antihypertensive action of α2 agonists

Question 10

• Drugs: phenelzine and tranylcypromine
• Mechanism: irreversible inhibition of MAOA and MAOB
• Use: atypical depressions

Answer 10

MAO Inhibitors

Question 11

MAOI drug interactions

Answer 11

Serotonin syndrome: SSRIs, TCAs, and meperidine

Question 12

Drugs: releasers (i.e., tyramine), tricyclic antidepressants (TCAs),
α1 agonists, levodopa

Answer 12

MAOIs

Question 13

MAOI symptoms

Answer 13

↑ BP, arrhythmias, excitation, hyperthermia

Question 14

Antidepressant associated with:

cardiac arrhythmias and priapism

Answer 14

Trazodone

Question 15

Antidepressant associated with:

nonselective reuptake blocker devoid of ANS side effects

Answer 15

Venlafaxine

Question 16

Antidepressant associated with:

dopamine reuptake blocker; used in smoking cessation

Answer 16

Bupropion

Question 17

Antidepressant associated with:

α2 antagonist, associated with weight gain

Answer 17

Mirtazapine:

Question 18

DOC for bipolar disorders

Prevents recycling of inositol (↓ PIP ) by blocking inositol
monophosphatase – ↓cAMP

Answer 18

Lithium

Question 19

Lithium S/E

Answer 19

Narrow therapeutic index; requires therapeutic monitoring
– Tremor, flu-like symptoms, life-threatening seizures
– Hypothyroidism with goiter (↓ TSH effects and inhibition of 5′-deiodinase)
– Nephrogenic diabetes insipidus (↓ ADH effect); manage with amiloride

Question 20

Lithium during pregnancy

Answer 20

Teratogenicity: Ebstein’s anomaly (malformed tricuspid valve)

Question 21

Other drugs used for Bipolar disorder

Answer 21

valproic acid and carbamazepine.

Question 22

DRUGS USED IN ADHD

Answer 22

Methylphenidate and Atomoxetine

Question 23

Drug for ADHD
Amphetamine-like
– Side effects: agitation, restlessness, insomnia, cardiovascular toxicity

Answer 23

Methylphenidate

Question 24

Selective NE reuptake inhibitor for ADHD

Answer 24

Atomoxetine

Question 25

Which tract is characterized by:
Cell bodies in the substantia nigra project to the striatum, where they release DA, which inhibits GABA-ergic neurons. In Parkinson disease, the loss of DA neurons in this tract leads to excessive ACh activity → extrapyramidal dysfunction.
• DA receptor antagonists → pseudo-Parkinsonism (reversible).
• DA agonists may cause dyskinesia

Answer 25

Nigrostriatal Tract

Question 26

Which tract is characterized by:
Cell bodies in midbrain project to cerebrocortical and limbic structures
• Functionsincluderegulationofaffect,reinforcement,cognitivefunctions, and sensory perception. Psychotic disorders and addiction are partly explained by ↑ DA in these pathways.
• Drugs that ↑ DA functions →↑ reinforcement and, at high doses, may cause psychoses.
• DA antagonists →↓ cognitive function

Answer 26

Mesolimbic-Mesocortical Tract

Question 27

Which tract is characterized by:
Cell bodies in hypothalamus project to anterior pituitary and release DA →↓ prolactin.
• DA agonists are used in hyperprolactinemic states.
• DA antagonists may cause endocrine dysfunction, including gynecomastia and amenorrhea/galactorrhea.

Answer 27

Tuberoinfundibular

Question 28

Prodrug converted to dopamine by aromatic amino acid decarbox-
ylase (AAAD)
– Given with carbidopa
– Side effects: dyskinesias, “on-off” effects, psychosis, hypotension, vomiting

Answer 28

Levodopa

Question 29

– COMT converts L-dopa to 3-O-methyldopa, a partial agonist at dopamine receptors.
– These drugs inhibit COMT and enhance levodopa uptake and efficacy.
– Tolcapone is hepatotoxic.

Answer 29

Tolcapone and entacapone

Question 30

Which Dopamine partial agonist is hepatotoxic

Answer 30

Tolcapone

Question 31

– MAOB-selective inhibitor (no tyramine interactions)
– Initial treatment and adjunct to levodopa
– Side effects: dyskinesias, psychosis, insomnia (metabolized to amphetamine)

Answer 31

Selegiline

Question 32

Dopamine-Receptor Agonists

Side effects: dyskinesias and psychosis

Answer 32

Pramipexole and ropinirole

Bromocriptine

Question 33

– Use: hyperprolactinemia and acromegaly

Answer 33

Bromocriptine

Question 34

Drugs Decreasing ACh Function

• muscarinic blockers
• Actions: ↓ tremor and rigidity but have little effects on bradykinesia

Side effects: atropine-like

Answer 34

Benztropine and trihexyphenidyl

Question 35

– Antiviral, which block muscarinic receptors and ↑ dopamine release
– Side effects: atropine-like and livedo reticularis

Answer 35

Amantadine

Question 36

Tx includes:

Blockade of dopamine receptors • Blockade of 5HT2 receptors

Answer 36

Schizophrenia

Question 37

Typical Antipsychotics

Answer 37

Chlorpromazine,Thioridazine, Fluphenazine, Haloperidol

Question 38

Atypical Antipsychotics

Answer 38

Clozapine, Olanzapine, Risperidone, Aripiprazole, quetiapine, ziprasidone

Question 39

Antipsychotics with parenteral formulations

Answer 39

fluphenazine, haloperidol