Antidepressant Pharmacology Flashcards Preview

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Flashcards in Antidepressant Pharmacology Deck (74):
1

Antidepressant Classes

SSRIs
SNRIs
TCA
MAOIs
Others: mirtazapine, bupropion, trazodone

2

What is the first line treatment of depressive disorders?

SSRIs

3

Examples of SSRIs

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

4

Psychiatric Conditions that SSRIs Treat

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

5

MOA for SSRIs

Block the presynaptic serotonin re-uptake pump

6

Pharmacokinetics of SSRIs

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

7

Which SSRIs inhibit liver enzymes less than other SSRIs?

Citalopram
Escitalopram

8

Why is inhibition of liver enzymes important?

Less drug interactions

9

What should you be caution with prescribing with SSRIs?

Azole antifungals
Macrolide antibiotics
Omeprazole
Hepatic impairment

10

What SSRIs are contraindicated with tamoxifen?

Paroxetine
Fluoxetine

11

SSRI SE

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

12

Withdrawal Symptoms of SSRIs

Dysphoria
Dizziness
GI distress
Fatigue
Chills
Myalgias

13

How long do SSRIs take to take effect?

Some few weeks
Others 4-6 weeks

14

Most Common SE of SSRIs Initially

Headache
Dizziness
Nausea
Diarrhea

15

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

Citalopram (Celexa)

16

What risk is important in citalopram (Celexa)?

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

17

What is an isomer & similar to citalopram?

Escitalopram (Lexapro)

18

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

Fluoxetine (Prozac)

19

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

Weight gain (2.6%)
Nausea
Sedation

20

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

Paroxetine (Paxil)

21

Which SSRI is more likely to cause diarrhea?

Sertraline (Zoloft)

22

More Intense SE of SSRIs

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

23

Examples of SNRIs

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

24

What do SNRI's act on?

Serotonin
Norepinephrine

25

Uses for SNRIs

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

26

MOA of SNRIs

Inhibit the re-uptake of serotonin & norepinephrine

27

Pharmacokinetics of SNRIs

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

28

SNRI SE

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

29

What are the most common SE of SNRIs?

Nausea
Dizziness
Diaphoresis

30

What needs to be monitored with the use of SNRIs?

Blood pressure

31

What is the most common SE of desvenlafaxine (Pristiq)

Nausea

32

Contraindications for Duloxetine (Cymbalta)

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

33

What else is duloxetine (Cymbalta) used for?

Diabetic neuropathy
Fibromyalgia

34

Venlafaxine (Effexor)

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

35

Examples of Tertiary Amines

Amitriptyline
Clomipramine
Doxepin
Imipramine
Trimipramine

36

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

Serotonin

37

Examples of Secondary Amines

Desipramine
Nortriptyline
Protriptyline

38

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

Norepinephrine

39

TCA Uses

Insomnia
Neuropathic pain
Fibromyalgia

40

When are TCAs usually avoided?

Treatment of depression due to anticholinergic SE

41

MOA of TCAs

Inhibit re-uptake of serotonin & norepinephrine
Block muscarinic, histamine & alpha-adrenergic receptors

42

Pharmacokinetics of TCAs

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

43

Cardiac SE of TCAs

Heart block
Ventricular arrhythmias
Sudden death

44

TCAs

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

45

What does blocking histamine receptors with TCAs cause?

Sedation
Increased appetite
Confusion
Delirium

46

What does blocking acetylcholine receptors with TCAs cause?

Blurred vision
Constipation
Dry mouth
Urinary retention

47

Why are TCAs not well tolerated in the elderly?

Orthostatic hypotension
Anticholinergic SE
Heavily sedating
Cardiac SE

48

Examples of MAOIs

Phenelzine (Nardil)
Tranylcypromaine (Parnate)

49

What can MAOI drug-drug interactions cause?

Serotonin syndrome
HTN crisis

50

What dietary restrictions are necessary with MAOIs?

No tyramine containing foods

51

Why are MAOIs poorly tolerated?

Side effects

52

Other Antidepressant Medications

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

53

MOA of Trazodone (Desyrel)

Serotonin antagonists & re-uptake inhibitors

54

What is trazodone (Desyrel) usually used for?

Sleep

55

SE to watch for with trazodone (Desyrel)

Sedation
Orthostasis
Priapism

56

Uses for Bupropion (Wellbutrin)

Major depressive disorder
ADHD
Smoking cessation

57

MOA of Bupropion (Wellbutrin)

Inhibits the re-uptake of dopamine

58

Effects of Bupropion

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

59

Who is Bupropion good for?

Patients with fatigue, hypersomnia, or poor concentration

60

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

SSRIs

61

Bupropion Considerations

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

62

MOA of Mirtazapine (Remeron)

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

63

SE of Mirtazepine (Remeron)

Sedation
Weight gain
Less sexual SE
Good for patients with nausea

64

2 New Antidepressant Drugs

Vilazodone (Viibryd)
Vortioxetine (Brintellix)

65

Serotonin Syndrome

Simultaneous administration of two serotonergic agent
Sometimes after invitation of a single sertonergic drug or increasing the dose

66

Drugs that can cause serotonin syndrome

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

Serotonin Syndrome PE

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

68

HARM from Serotonin Syndrome

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

69

Signs/Symptoms of Serotonin Syndrome

Anxiety
Agitated delirium
Restlessness
Disorientation

70

Autonomic Manifestations of Serotonin Syndrome

Diaphoresis
Tachycardia
Hyperthermia
HTN
Vomiting
Diarrhea

71

Types of Neuromuscular Hyperactivity

Tremor
Muscle rigidity
Myclonus
Hyperreflexia
Bilateral Babinski sign

72

Hunter Criteria for Serotonin Syndrome

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

Treatment for Serotonin Syndrome

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

Which drugs carry the greatest risk for serotonin syndrome?

MAOIs