Santos

Question 1

main excitatory NT

Answer 1

glutamate -> depolarization

Question 2

main inhibitory NT

Answer 2

GABA and glycine -> hyper polarization

Question 3

Ion channels (ionotropic)

Answer 3

• FAST neurotransmission

- ligand or voltage gated

Question 4

GPCR (metabotropic)

Answer 4

• SLOW neurotransmission

- Gq, Gs, Gi

Question 5

GABAa receptors

Answer 5

• ionotropic -> FAST transmission

- where most drugs bind

Question 6

GABAb receptors

Answer 6

-metabotropic -> SLOW transmission

Question 7

glutamate decarboxylase

Answer 7

• converts glutamate to GABA

- requires vit. B6 cofactor

Question 8

low vit. B6

Answer 8

decrease GABA synthesis -> seizures

Question 9

ACh NT

Answer 9

• alpha-1 or beta receptors -> excitatory

- alpha-2 receptors -> inhibitory

Question 10

Serotonin NT

Answer 10

• synthesized from Tryptophan
• 5-HT3R -> ionotropic -> FAST excitatory
• 5-HT1A -> metabotropic -> SLOW inhibitory
• 5-HT2 or 5-HT4 -> metabotropic -> SLOW excitatory

Question 11

D1-class - D1, D5 receptors

Answer 11

increase AC -> excitatory (Gs)

Question 12

D2-class: D2, D3, D4 receptors

Answer 12

decrease AC -> inhibitory (Gi)

Question 13

Histamine: H1, H2 receptors

Answer 13

• metabotropic -> slow EXCITATORY
• H1R -> Gq (PLC)
• H2R -> Gs (AC)

Question 14

Histamine: H3, H4 receptors

Answer 14

-metabotropic -> slow INHIBITORY

Question 15

bipolar effective disorder

Answer 15

-high risk of SUICIDE

Question 16

Lithium

Answer 16

• prophylaxis for mania and depression in bipolar
• REDUCE SUICIDE RISK
• Neuroprotective (increase BDNF, bcl-2)
• not used in renal failure
• NARROW therapeutic window (0.6-1.5 mEq/L)
• AE: tremor, hypothyroidism, DI, TERATOGEN (Ebsteins)

Question 17

other drugs for bipolar disorder

Answer 17

Valproic acid, Carbamezapine, Lamotrigine

• Carbamezapine -> induce CYP3A4 and not used w/ other drugs
• Lamotrigene -> maintenance only

Question 18

Schizophrenia

Answer 18

• most common psychotic disorder
• Pos Sx: hallucinations, delusions, disorganized thoughts
• Neg Sx: avolition, apathy, alogia

Question 19

Monamine hypothesis

Answer 19

-Schizophrenia due to HIGH dopamine D2R, 5-HT2, or Glutamate neurotransmission

Question 20

1st Gen (typical) antipsychotics

Answer 20

Chlorpromazine, Haloperidol

• D2R antagonists -> MORE EPS effects
• treat only positive Sx

Question 21

2nd Gen (atypical) antipsychotics

Answer 21

Clozapine, Risperidone, Olanzapine, Quetiapine, Ziprasidone, Aripiprazole

• 5-HT2AR antagonists (some D2R blocking) -> LESS EPS effects
• INVERSE AGONISTS -> block 5-HTA2 and 5-HT2C receptors
• treat positive and negative Sx

Question 22

Quetiapine

Answer 22

• 2nd gen

- block D1R > 5-HT2AR

Question 23

Aripiprazole

Answer 23

• 2nd gen

- PARTIAL D2 AGONIST

Question 24

side effects of antipsychotics

Answer 24

• EPS due to D2R blockade
• NEUROLEPTIC MALIGNANT SYNDROME
• hyperprolactinemia
• QT prolongation (torsades) -> block Ikr rectifier K+ channels

Question 25

major depressive disorder (MDD)

Answer 25

- recurrent depressive episodes WITHOUT mania ( >2wks) | - SUICIDE RISK

Question 26

SSRIs

Answer 26

Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Citalopram, Escitalopram, Vilazodone MOA: inhibit SERT and stimulate 5-HT1A, 5-HT7 auto receptors

Question 27

Fluoxetine and Paroxetine

Answer 27

- inhibit CYP2D6 -> drug interactions | - fluvoxamine -> inhibit CYP3A4

Question 28

SNRIs

Answer 28

Duloxetine, Venlafaxine, Desvenlafaxine, Milnacipran, Levomilnacipran -MOA: inhibit both SERT and NET and stimulate 5-HT1A, 5-HT1D, 5-HT7 auto receptors

Question 29

TCA

Answer 29

Imipramine**, Desipramine, Clomipramine, Trimipramine, Amitriptyline, Protriptyline, Doxepin - MOA: inhibit SERT and NET; antimuscarinic, antihistaminic, alpha-blockade - AE: LETHAL OVERDOSE*** -> CARDIOTOXICITY

Question 30

5-HT2 Antagonists

Answer 30

Trazodone, Nifazodone, Vortioxetine - MOA: 5-HT2R antagonist; antimuscarinic, antihistaminic, alpha-blockade - AE: sedation, orthostatic hypotension, PRIAPISM

Question 31

MOA inhibitors

Answer 31

Phenelzine, Tranylcypromine, Selegiline MOA: IRREVERSIBLE inhibitors of MAO-A and MAO-B -> decrease metabolism of 5-HT, NE, DA, and tyramine -AE: TYRAMINE TOXICITY -> HTN crisis (and tachycardia/stroke) due to tyramine induced NE release

Question 32

which drug is specific for blocking MAO-B?

Answer 32

Selegiline

Question 33

Atypical antidepressants

Answer 33

Buproprion, Mirtazapine, Buspirone - Buproprion -> inhibit NET and DAT - Mirtazapine -> cause sedation & treat insomnia

Question 34

what is associated with ALL antidepressants?

Answer 34

RISK OF SUICIDE