Santos Flashcards

1
Q

main excitatory NT

A

glutamate -> depolarization

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2
Q

main inhibitory NT

A

GABA and glycine -> hyper polarization

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3
Q

Ion channels (ionotropic)

A
  • FAST neurotransmission

- ligand or voltage gated

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4
Q

GPCR (metabotropic)

A
  • SLOW neurotransmission

- Gq, Gs, Gi

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5
Q

GABAa receptors

A
  • ionotropic -> FAST transmission

- where most drugs bind

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6
Q

GABAb receptors

A

-metabotropic -> SLOW transmission

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7
Q

glutamate decarboxylase

A
  • converts glutamate to GABA

- requires vit. B6 cofactor

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8
Q

low vit. B6

A

decrease GABA synthesis -> seizures

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9
Q

ACh NT

A
  • alpha-1 or beta receptors -> excitatory

- alpha-2 receptors -> inhibitory

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10
Q

Serotonin NT

A
  • synthesized from Tryptophan
  • 5-HT3R -> ionotropic -> FAST excitatory
  • 5-HT1A -> metabotropic -> SLOW inhibitory
  • 5-HT2 or 5-HT4 -> metabotropic -> SLOW excitatory
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11
Q

D1-class - D1, D5 receptors

A

increase AC -> excitatory (Gs)

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12
Q

D2-class: D2, D3, D4 receptors

A

decrease AC -> inhibitory (Gi)

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13
Q

Histamine: H1, H2 receptors

A
  • metabotropic -> slow EXCITATORY
  • H1R -> Gq (PLC)
  • H2R -> Gs (AC)
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14
Q

Histamine: H3, H4 receptors

A

-metabotropic -> slow INHIBITORY

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15
Q

bipolar effective disorder

A

-high risk of SUICIDE

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16
Q

Lithium

A
  • 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)
17
Q

other drugs for bipolar disorder

A

Valproic acid, Carbamezapine, Lamotrigine

  • Carbamezapine -> induce CYP3A4 and not used w/ other drugs
  • Lamotrigene -> maintenance only
18
Q

Schizophrenia

A
  • most common psychotic disorder
  • Pos Sx: hallucinations, delusions, disorganized thoughts
  • Neg Sx: avolition, apathy, alogia
19
Q

Monamine hypothesis

A

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

20
Q

1st Gen (typical) antipsychotics

A

Chlorpromazine, Haloperidol

  • D2R antagonists -> MORE EPS effects
  • treat only positive Sx
21
Q

2nd Gen (atypical) antipsychotics

A

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
22
Q

Quetiapine

A
  • 2nd gen

- block D1R > 5-HT2AR

23
Q

Aripiprazole

A
  • 2nd gen

- PARTIAL D2 AGONIST

24
Q

side effects of antipsychotics

A
  • EPS due to D2R blockade
  • NEUROLEPTIC MALIGNANT SYNDROME
  • hyperprolactinemia
  • QT prolongation (torsades) -> block Ikr rectifier K+ channels
25
Q

major depressive disorder (MDD)

A
  • recurrent depressive episodes WITHOUT mania ( >2wks)

- SUICIDE RISK

26
Q

SSRIs

A

Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Citalopram, Escitalopram, Vilazodone

MOA: inhibit SERT and stimulate 5-HT1A, 5-HT7 auto receptors

27
Q

Fluoxetine and Paroxetine

A
  • inhibit CYP2D6 -> drug interactions

- fluvoxamine -> inhibit CYP3A4

28
Q

SNRIs

A

Duloxetine, Venlafaxine, Desvenlafaxine, Milnacipran, Levomilnacipran

-MOA: inhibit both SERT and NET and stimulate 5-HT1A, 5-HT1D, 5-HT7 auto receptors

29
Q

TCA

A

Imipramine**, Desipramine, Clomipramine, Trimipramine, Amitriptyline, Protriptyline, Doxepin

  • MOA: inhibit SERT and NET; antimuscarinic, antihistaminic, alpha-blockade
  • AE: LETHAL OVERDOSE*** -> CARDIOTOXICITY
30
Q

5-HT2 Antagonists

A

Trazodone, Nifazodone, Vortioxetine

  • MOA: 5-HT2R antagonist; antimuscarinic, antihistaminic, alpha-blockade
  • AE: sedation, orthostatic hypotension, PRIAPISM
31
Q

MOA inhibitors

A

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

32
Q

which drug is specific for blocking MAO-B?

A

Selegiline

33
Q

Atypical antidepressants

A

Buproprion, Mirtazapine, Buspirone

  • Buproprion -> inhibit NET and DAT
  • Mirtazapine -> cause sedation & treat insomnia
34
Q

what is associated with ALL antidepressants?

A

RISK OF SUICIDE