Antidepressant Pharmacology Flashcards

(74 cards)

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
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
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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 ```
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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