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Pharmacology III > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

Antidepressant Targets

A
  1. TCAs inhibit the reuptake of NE and 5-HT
  2. SSRIs selectively inhibit the reuptake of 5-HT
  3. SNRIs inhibit the reuptake of NE and 5-HT
  4. DA reuptake inhibitors - Bupropion
  5. MAOIs inhibit the metabolism of NE, DA, and 5-HT
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2
Q

Tricyclic Antidepressants (TCA) - MoA

A 
 Inhibit re-uptake of NE and 5-HT
 Also block a-adrenergic, histamine and muscarinic 
    receptors
 No euphoria/low abuse potential
 2-4 weeks to have effect
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3
Q

Tricyclic Antidepressants (TCA) - Uses

A

depression

  • chronic pain (TMJ), fibromyalgia
  • enuresis
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4
Q

TCAs

A

Amitriptyline (Elavil®)
Imipramine (Tofranil®)
Nortriptyline (Pamelor®)
Desipramine (Norpramin®)

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5
Q

Amitriptyline (Elavil®); Imipramine (Tofranil®)

A
  • Tertiary amines
  • Primary inhibit 5-HT re-uptake
  • Produce more seizures than secondary amines
  • More sedating than secondary amines
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6
Q

Nortriptyline (Pamelor®); Desipramine (Norpramin®)

A
  • Secondary amines

* Primarily block NE re-uptake

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7
Q

TCA Pharmacokinetics

A

 Well-absorbed orally
 Variable and long half-lives (10-90 hrs)
 They are generally given once a day, at bedtime.
 Metabolized by CYP2D6 - drug interactions VERY
common

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8
Q

TCA Side Effects

A

 Weight gain
 Histamine receptor blockade
• Drowsiness, fatigue, sedation
 Cholinergic blockade
• Blurred vision, tachycardia, constipation, urinary
retention, dry mouth, palpitations
• Impairment of memory and cognition
alpha1 receptor blockade
• Cardiac depression and arrhythmias
• Postural hypotension, dizziness, reflex tachycardia
Analgesia results from activation of descending
noradrenergic pathways in the spinal cord (NE acts on
α2receptors to decrease glutamate input into pain
pathway going to brain)
 Syndrome of inappropriate antidiuretic hormone secretion (SIADH) may occur. This may lead to water intoxication and hyponatremia.
 Sexual dysfunction
 Decrease in seizure threshold
 Tolerance generally develops to sedation, postural
hypotension and to the anticholinergic effects
 Can be used in pregnancy

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9
Q

TCA Toxicity and Overdose

A 
Cardiac Toxicity
 Torsadesde pointes 
 prolongedQT interval
 cardiac arrhythmias
 severe hypotension
 agitation, delirium
 seizures, hyperpyrexia
 coma, shock, metabolic acidosis
 respiratory depression
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10
Q

Treatment of TCA overdose

A

 Cardiac monitoring, supportive care
 Gastric lavage and activated charcoal
 Magnesium, isoproterenol and cardiac pacing for
Torsadesde pointes
 Lidocaine, propranolol, phenytoin to manage
arrhythmias and/or prevent seizures
 Sodium bicarbonate and potassium chloride to
restore acid/base balance

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11
Q

TCA Drug Interactions

A

 Combined with MAOIs can result in serotonin
syndrome: severe CNS toxicity manifested by
hyperpyrexia, convulsions and coma
 TCAs compete for metabolism of SSRIs, thus
combination can lead to toxic levels of TCAs
 TCAs may cause hypertension when combined with
sympathomimetic drugs such as amphetamine
 TCAs potentiate the sedative actions of alcohol/CNS
depressants
 TCAs potentiate the effects of anticholinergic drugs

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12
Q

Selective Serotonin Reuptake Inhibitors (SSRIs)

A 
Fluoxetine (Prozac®) 
Sertraline (Zoloft®)    
Paroxetine (Paxil®)     
Citalopram (Celexa®)
Escitalopram (Lexapro®)
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13
Q

Selective Serotonin Reuptake Inhibitors (SSRIs) - Uses

A
  • Depression
  • Panic disorder
  • Obsessive-compulsive disorder: Paroxetine (Paxil®)
  • Social anxiety: Paroxetine (Paxil®)
  • Bulimia
  • Alcoholism
  • Children and Teenagers
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14
Q

Fluoxetine (Prozac®)

A

• Half-life of 2-3 days; Norfluoxetine, active metabolite,
7-9 days
• Most likely to inhibit CYP450 enzymes (CYP2D6)
• More drug interactions than other SSRIs
• Impairs blood glucose levels in diabetics

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15
Q

Sertraline (Zoloft®)

A
  • Half life of 26 hours; Extensive first-pass elimination
  • Least likely SSRI to interact with other drugs
  • Preferred in elderly
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16
Q

Citalopram (Celexa®) / Escitalopram (Lexapro®)

A

• Currently the DOC for depression
• Low incidence of pharmacokinetic interactions and
side effects

17
Q

Selective Serotonin Reuptake Inhibitors (SSRIs) - MoA

A
  • Selectively inhibits 5-HT reuptake

* 2-3 weeks to be effective

18
Q

Selective Serotonin Reuptake Inhibitors (SSRIs) - Pharmacokinetics

A
  • Well absorbed by gut
  • Half life = 24-72 hours
  • Metabolized by CYP450s (2D6)
  • Inhibit CYP450s
  • Many drug interactions
19
Q

SSRI Side Effects

A

 Mild side effects; Less autonomic side effects and
chance for cardiac arrhythmias than TCAs
 GI: nausea, loss of appetite, constipation
 Weight loss or gain possible
 CNS stimulation (anxiety or insomnia) may occur with
fluoxetine or sertraline
 Sedation more likely with other drugs
 Sexual disinterest/dysfunction, impairment of
ejaculation
 Photosensitivity, limit sun exposure

20
Q

SSRI Drug Interactions

A

 Inhibition of CYP3A4 and CYP2D6
• TCAs: Inhibition of metabolism increases toxicity
• Phenytoin and carbamazepine: increased levels and
toxicity
 MAOIs: Serotonin syndrome
 St. John’s Wort or amphetamines - serotonin
syndrome
 beta-blockers: may result in heart block and
hypotension

 Opioids
• Codeine - Fluoxetine inhibits conversion to the
active compound
• Meperidine - Increases 5-HT; potential for serotonin
syndrome
• Tramadol - Increased risk of seizures

21
Q

Serotonin-norepinephrine reuptake inhibitors (SNRI)

A

 SNRIs inhibit NE & 5-HT re-uptake
 More side effects than SSRIs
 Uses: depression, neuropathic pain, post
menopausal hot flashes

 Venlafaxine (Effexor®)
• May increase blood pressure

 Duloxetine (Cymbalta®)
• May cause hepatotoxicity
• May cause bilateral acute angle-closure glaucoma
(ACG)

22
Q

Monoamine Oxidase Inhibitors (MAOIs)

A

Irreversibly inhibit MAOs which metabolize NE, DA and 5-HT

Phenelzine (Nardil®)
Selegiline (Deprenyl®)

23
Q

Phenelzine (Nardil®)

A

Inhibits both MAO-A and MAO-B

  • Increases NE and 5-HT (and DA)
  • Actions persist longer than serum levels
  • Also a substrate for MAOs
  • Depression that hasn’t responded to other drugs
  • Drug of last choice - serious side effects
24
Q

Selegiline (Deprenyl®)

A

Selectively inhibits MAO-B

  • Increases DA
  • Fewer side effects
  • Also used in Parkinson’s
25
Q

MAOIs - Uses

A

Used for depression which doesn’t respond to other drugs

26
Q

MAOIs - Pharmacokinetics

A

Long half life; Effects persist after discontinuing drug

27
Q

MAOIs - Side Effects

A

• Hypertensive crisis (phenelzine) – MAO-A is inhibited
in GI tract; tyramine causes release of amines and,
with limited metabolism by MAO-A, can lead to severe
hypertension. Avoid foods with tyramine-red wine,
beer, aged cheese etc…
• Tremors, sedation or excitation and insomnia
• Orthostatic hypotension
• Weight gain - very common
• Anticholinergic effects -blurred vision, dry mouth, etc

28
Q

MAOI Drug Interactions

A

OTC cold and cough medications containing
sympathomimetic amines such as phenylephrine,
ephedrine, or amphetamines –can lead to severe
hypertension.
 Serotonin Syndrome - Meperidine,
dextromethorphan, TCAs, SSRIs – can lead to
hyperpyrexia.
 MAOIs can also inhibit CYP450 enzymes (2D6) –
affects metabolism of SSRIs, Ca++channel blockers,
etc…
 MAOI metabolism is affected by drugs that induce or
inhibit CYP450s

29
Q

Bupropion (Wellbutrin®) - MoA

A

 Inhibits DA, and to a minimal extent, NE and 5HT re-
uptake
 May work where others haven’t; Sometimes
combined with SSRIs

30
Q

Bupropion (Wellbutrin®) - Uses

A

ADHD, alcoholism (decreases craving)

Extended release for quitting smoking (Zyban®)

31
Q

Bupropion (Wellbutrin®) - Pharmacokinetics

A

extensive first-pass metabolism and high protein binding; active metabolites

32
Q

Bupropion (Wellbutrin®) - Side Effects

A

• Seizures - Contraindicated in patients with history of
seizures
• CNS effects - anxiety, insomnia, restlessness, tremor,
psychosis
• Cardiac - Tachycardia
• Sexual dysfunction side effects are rare

33
Q

Mirtazapine (Remeron®) - MoA

A

 Blocks presynaptic alpha2 receptors, which inhibit
release of NE and 5-HT.
 Increases release of NE and 5-HT
 Blocks 5-HT2A and 5-HT3 receptors

34
Q

Mirtazapine (Remeron®) - Uses

A

 Eliminates side effects associated with SSRIs (anxiety,

insomnia, nausea, sexual dysfunction).

35
Q

Mirtazapine (Remeron®) - Pharmacokinetics

A

Half-life 20-40 hrs; metabolized by multiple CYP450s

36
Q

Mirtazapine (Remeron®) - Side Effects

A

 Blocks histamine receptors, causing
drowsiness as a predominant side effect
- This may be an advantage in depressed
patients with insomnia and anxiety

37
Q

Atomoxetine (Strattera®)

A

 Selective inhibitor of norepinephrine reuptake.
 First non-stimulant for treatment of ADHD
 Does not cause euphoria; good choice for addicts
 May increase memory and attention
 Side effects - most common are GI distress and
insomnia
 Liver damage is possible but rare

38
Q

Trazodone (Desyrel®)

A

 5-HT2A receptor antagonist. Short half life; high first
pass metabolism
 Sedating, not good antidepressant, more often used
as a sleep aid
 Also used for pain management
 Side effects - include sedation, dizziness,
hypotension, nausea and priapism (rare but serious),
which limits use in males

39
Q

St John’s Wort (hypericin®)

A

 May be effective in mild depression
 Mechanism uncertain - May block reuptake or inhibit
MAO
 Causes photosensitivity
 DO NOT combine with other antidepressants - can
cause serotonin syndrome
 May prolong effects of general anesthetics
 Efficacy of oral contraceptives, digoxin, protease
inhibitors and warfarin reduced due to increased
metabolism

Pharmacology III (10 decks)

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