Antidepressant Pharmacology Flashcards

1
Q

Antidepressant Classes

A
SSRIs
SNRIs
TCA
MAOIs
Others: mirtazapine, bupropion, trazodone
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2
Q

What is the first line treatment of depressive disorders?

A

SSRIs

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3
Q

Examples of SSRIs

A
Fluoxetine (Prozac)
Sertraline (Zoloft)
Paroxetine (Paxil)
Citalopram (Celexa)
Fluvoxamine (Luvox)
Escitalopram (Lexapro)
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4
Q

Psychiatric Conditions that SSRIs Treat

A
Depression
Panic disorder
OCD
GAD
Social anxiety disorder
PTSD
Body dysmorphic disorder
Bulimia nervosa
Binge eating disorder
Premenstrual dysphoric disorder
Somatoform disorders
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5
Q

MOA for SSRIs

A

Block the presynaptic serotonin re-uptake pump

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6
Q

Pharmacokinetics of SSRIs

A

Absorbed in GI tract
Bind to proteins
Metabolism & elimination occur in the liver

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7
Q

Which SSRIs inhibit liver enzymes less than other SSRIs?

A

Citalopram

Escitalopram

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8
Q

Why is inhibition of liver enzymes important?

A

Less drug interactions

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9
Q

What should you be caution with prescribing with SSRIs?

A

Azole antifungals
Macrolide antibiotics
Omeprazole
Hepatic impairment

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10
Q

What SSRIs are contraindicated with tamoxifen?

A

Paroxetine

Fluoxetine

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11
Q

SSRI SE

A
Sexual dysfunction
Drowsiness
Weight gain
Dizziness
Insomnia
Anxiety
Diaphoresis
Diarrhea
Hyperprolactinemia
Headache
Dry mouth
Blurred vision
Nausea
Rash or pruritis
Tremor
Constipation
SIADH
Hyponatremia
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12
Q

Withdrawal Symptoms of SSRIs

A
Dysphoria
Dizziness
GI distress
Fatigue
Chills
Myalgias
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13
Q

How long do SSRIs take to take effect?

A

Some few weeks

Others 4-6 weeks

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14
Q

Most Common SE of SSRIs Initially

A

Headache
Dizziness
Nausea
Diarrhea

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15
Q

What drug is good to use when concerned about drug interactions?

A

Citalopram (Celexa)

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16
Q

What risk is important in citalopram (Celexa)?

A

QT prolongation

Arrhythmia + hepatic impairment OR age >60 years OR on other CYP219 inhibitors

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17
Q

What is an isomer & similar to citalopram?

A

Escitalopram (Lexapro)

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18
Q

Which SSRI is more likely to cause activation and have the least problems with weight gain?

A

Fluoxetine (Prozac)

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19
Q

What is the most common SE of fluvoxamine (Luvox)?

A

Weight gain (2.6%)
Nausea
Sedation

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20
Q

Which SSRI is contraindicated with Tamoxifen & has a significant withdrawal symptoms?

A

Paroxetine (Paxil)

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21
Q

Which SSRI is more likely to cause diarrhea?

A

Sertraline (Zoloft)

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22
Q

More Intense SE of SSRIs

A

Increase risk of suicide as the patient recovers
Increase risk of abnormal bleeding
Possible increase in bone fractures
May affect male fertility

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23
Q

Examples of SNRIs

A

Venlafaxine (Effexor)
Duloxetine (Cymbalta)
Desvenlafaxine (Pristiq)

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24
Q

What do SNRI’s act on?

A

Serotonin

Norepinephrine

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25
Q

Uses for SNRIs

A
Depression
Panic disorder
GAD
Social anxiety disorder
OCD
PTSD
Body dysmorphic disorder
Diabetic peripheral neuropathy
Fibromyalgia
Menopausal hot flashes
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26
Q

MOA of SNRIs

A

Inhibit the re-uptake of serotonin & norepinephrine

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27
Q

Pharmacokinetics of SNRIs

A

Food can decrease the rate of absorption but not the degree of absorption
Can eat with food if severe SE post dose

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28
Q

SNRI SE

A
Nausea
Dizziness
Diaphoresis
Sexual dysfunction
Sedation
Agitation
Fatigue
Diarrhea
Constipation
Anorexia
Insomnia
Dry mouth
Orthostatic hypotension
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29
Q

What are the most common SE of SNRIs?

A

Nausea
Dizziness
Diaphoresis

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30
Q

What needs to be monitored with the use of SNRIs?

A

Blood pressure

31
Q

What is the most common SE of desvenlafaxine (Pristiq)

A

Nausea

32
Q

Contraindications for Duloxetine (Cymbalta)

A

Uncontrolled angle closure glaucoma
Severe renal impairment (relative)
Severe liver impairment (relative)

33
Q

What else is duloxetine (Cymbalta) used for?

A

Diabetic neuropathy

Fibromyalgia

34
Q

Venlafaxine (Effexor)

A
Increase BP
Upper GI bleed
Adjust dose in hepatic & liver impairment
Slow taper to avoid withdrawal symptoms
QT prolongation
35
Q

Examples of Tertiary Amines

A
Amitriptyline
Clomipramine
Doxepin
Imipramine
Trimipramine
36
Q

What are tertiary amines more potent at blocking the uptake of neurotransmitter?

A

Serotonin

37
Q

Examples of Secondary Amines

A

Desipramine
Nortriptyline
Protriptyline

38
Q

What are secondary amines more potent at blocking the uptake of neurotransmitter?

A

Norepinephrine

39
Q

TCA Uses

A

Insomnia
Neuropathic pain
Fibromyalgia

40
Q

When are TCAs usually avoided?

A

Treatment of depression due to anticholinergic SE

41
Q

MOA of TCAs

A

Inhibit re-uptake of serotonin & norepinephrine

Block muscarinic, histamine & alpha-adrenergic receptors

42
Q

Pharmacokinetics of TCAs

A

Rapid/near complete absorption
First pass metabolism
Binds to proteins
Active metabolites

43
Q

Cardiac SE of TCAs

A

Heart block
Ventricular arrhythmias
Sudden death

44
Q

TCAs

A
Lower seizure threshold
Increase bone fractures
Block histamine receptors
Block acetylcholine receptors
Dangerous in overdose
45
Q

What does blocking histamine receptors with TCAs cause?

A

Sedation
Increased appetite
Confusion
Delirium

46
Q

What does blocking acetylcholine receptors with TCAs cause?

A

Blurred vision
Constipation
Dry mouth
Urinary retention

47
Q

Why are TCAs not well tolerated in the elderly?

A

Orthostatic hypotension
Anticholinergic SE
Heavily sedating
Cardiac SE

48
Q

Examples of MAOIs

A

Phenelzine (Nardil)

Tranylcypromaine (Parnate)

49
Q

What can MAOI drug-drug interactions cause?

A

Serotonin syndrome

HTN crisis

50
Q

What dietary restrictions are necessary with MAOIs?

A

No tyramine containing foods

51
Q

Why are MAOIs poorly tolerated?

A

Side effects

52
Q

Other Antidepressant Medications

A
Trazodone (Desyrel)
Bupropion (Wellbutrin)
Mirtazapine (Remeron)
Vilazodone (Viibryd)
Vortioxetine (Brintellix)
53
Q

MOA of Trazodone (Desyrel)

A

Serotonin antagonists & re-uptake inhibitors

54
Q

What is trazodone (Desyrel) usually used for?

A

Sleep

55
Q

SE to watch for with trazodone (Desyrel)

A

Sedation
Orthostasis
Priapism

56
Q

Uses for Bupropion (Wellbutrin)

A

Major depressive disorder
ADHD
Smoking cessation

57
Q

MOA of Bupropion (Wellbutrin)

A

Inhibits the re-uptake of dopamine

58
Q

Effects of Bupropion

A

Anxiety
Lowers seizure threshold
Avoid in bulimia due to possible electrolyte disturbances

59
Q

Who is Bupropion good for?

A

Patients with fatigue, hypersomnia, or poor concentration

60
Q

What can Bupropion be added on to for the treatment of sexual SE?

A

SSRIs

61
Q

Bupropion Considerations

A
No sexual SE
Smoking cessation
Co-morbid ADHD
Often used with SSRIs
Consider with sleepy, slowed down patients
Preg. Cat. C
62
Q

MOA of Mirtazapine (Remeron)

A

Blocks adrenergic receptors leading to an increased release of norepinephrine & serotonin
Blocks sertonergic receptors & increases serotonin mediated neurotransmission

63
Q

SE of Mirtazepine (Remeron)

A

Sedation
Weight gain
Less sexual SE
Good for patients with nausea

64
Q

2 New Antidepressant Drugs

A

Vilazodone (Viibryd)

Vortioxetine (Brintellix)

65
Q

Serotonin Syndrome

A

Simultaneous administration of two serotonergic agent

Sometimes after invitation of a single sertonergic drug or increasing the dose

66
Q

Drugs that can cause serotonin syndrome

A

Psych: SSRIs, SNRIs, TCA, MAOI, nefazadone, trazadone, bupropion, buspirone, lithium
Pain: pentaxocine (Talwin), meperidine (Demerol), tramadol, fentanyl, cyclobenzaprine (Flexeril)
Migraine: triptans, ergots
Neuro: levodopa, carbidopa-levodopa, valproate, carbamezepine
OTC: dextromethorphan (Robitussin), St. John’s wort
Antiemetics: odansetron (Zofran), ganisetron (Kytril)
Street drugs: cocaine, meth, MDMA (ecstasy), LSD
ADHD: amphetamine derivatives, dextroamphetamine
Weight loss drugs
Metaclopramide (Reglan)

67
Q

Serotonin Syndrome PE

A
Hyperthermia
Agitation
Ocular clonus
Tremor
Akathisia
Deep tendon hyperreflexia
Clonus, muscle rigidity
Dilated pupils
Dry mucus membranes
Increased bowel sounds
Flushed skin
Diaphoresis
68
Q

HARM from Serotonin Syndrome

A

H: hyperthermia
A: autonomic instability
R: rigidity
M: myclonus

69
Q

Signs/Symptoms of Serotonin Syndrome

A

Anxiety
Agitated delirium
Restlessness
Disorientation

70
Q

Autonomic Manifestations of Serotonin Syndrome

A
Diaphoresis
Tachycardia
Hyperthermia
HTN
Vomiting
Diarrhea
71
Q

Types of Neuromuscular Hyperactivity

A
Tremor
Muscle rigidity
Myclonus
Hyperreflexia
Bilateral Babinski sign
72
Q

Hunter Criteria for Serotonin Syndrome

A

Serotoniergic agent PLUS spontaneous clonus OR inducible clonus & agitation or diaphroesis OR ocular clonus & agitation or diaphoresis OR tremor & hyperreflexia OR hypertonia & temp >38C & ocular clonus or inducible clonus

73
Q

Treatment for Serotonin Syndrome

A
DC sertonergic agents
Sedate using lorazepam
Supplemental O2
IV fluids
Cardiac monitor
Benzo's don't work, use cyproheptadine
Temp >41.1C (106F), immediate intubation & sedation
Avoid acetaminophen
74
Q

Which drugs carry the greatest risk for serotonin syndrome?

A

MAOIs