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Pharm- Antipsychotics > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

Etiology of MDD

A

Changes in?
norepinephrine (NE)
serotonin (5-HT)
dopamine (DA)

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2
Q

Treatment Goals of MDD

A

Reduce symptoms of acute depression
Facilitate patient’s return to pre-morbid functioning
Prevent further episodes of depression
Hospitalization

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3
Q

Hospitalization should be based on what 4 factors?

A

Suicide risk
Physical state of health
Support system
Presence of psychotic features

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4
Q

Acute Phase of treatment for MDD

A

Lasting from 6-8 weeks

Goal: Remission of symptoms

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5
Q

Continuation phase of treatment for MDD

A

Lasting from 4-9 months(in addition to acute phase)

Goal: Eliminate residual symptoms and prevent relapse

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6
Q

Maintenance Phase of treatment for MDD

A

Lasting at least 12-36 months

Goal: Prevent recurrence

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7
Q

Choice of Agent is based on what for antidepressants?

A 
Patient’s history of response
Pharmacogenetics (hx of familial response)
Subtype of depression
Concurrent medical history
Potential for drug-drug interactions
Adverse events profile
Drug cost
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8
Q

What is the response to antidepressants?

A

Approx. 65-70% of patients with varying types of depression improve with drug therapy
Well-documented placebo effect
Adverse effects may occur immediately
Resolution of symptoms may take 2-4 weeks (or longer!)
Adherence is essential to a successful outcome

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9
Q

What are the 5 classes of antidepressants

A 
Tricyclic Antidepressants (TCAs)
Monoamine oxidase inhibitors (MAOIs)
Selective serotonin reuptake inhibitors (SSRIs)
Mixed 5-HT and NE reuptake inhibitors
Miscellaneous
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10
Q

What is the black box warning found on all antidepressants?

A

regarding ↑’d risk of suicidality in young adults

(18-24 years), during initial stages of treatment

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11
Q

TCA MOA

A 
Block muscarinic (M1), adrenergic (α1), histamine (H1) receptors
All potentiate activity of NE and 5-HT via reuptake blockade
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12
Q

TCA Pharmacokinetics

A

Well-absorbed; low bioavailability due to high 1st –pass metabolism in liver
T ½ about 24 hours (allows for QD dosing)
Highly lipophilic–> wide distribution throughout the body
Highly protein bound
hepatically metabolized

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13
Q

TCA Adverse Effects

A 
Tachycardia
Orthostatic hypotension
Cardiac rhythm changes (i.e., QRS prolongation, ST depression, flattened or inverted T waves)
Weight gain 
Sedation
decrease seizure threshold
sexual dysfunction****
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14
Q

What is really important to know about TCA’s?

A

narrow theraputic index

Fatal in overdose  cardiac conduction abnormalities (i.e., torsades de pointes)

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15
Q

Tertiary amine TCAs

A

More pronounced anticholinergic, antihistaminergic, and hypotensive effects
Avoid in elderly due to postural hypotension  risk of fall and other cardiovascular effects

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16
Q

TCA Contraindications? (6)

A

Patients with benign prostate hyperplasia
Patients with closed-angle glaucoma
Patients with cardiac disease
Baseline ECG (require for all)
Patients with hepatic impairment
Elderly patients
Particularly sensitive to antiACh effects
At ’d risk of TCA-induced cognitive toxicity (mild confusion to delirium)

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17
Q

TCA Drug interactions

A

Avoid use with other drugs that affect CYP450 system
May increase vasopressor response to direct-acting sympathomimetics (i.e., phenylephrine, epinephrine, NE)
Additive adverse effects with other agents with serotonergic, antiACh, sedative, or hypotensive properties

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18
Q

3 MAO-I medications

A

Phenelzine (Nardil®) (nonselective)
Tranylcypromine (Parnate®)
Selegiline transdermal patch (Emsam®)

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19
Q

Tranylcypromine (Parnate®)

A

Non-selective inhibition of MAO-A and MAO-B

Rare to see due to ADE

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20
Q

Selegiline transdermal patch (Emsam®)

A

Selective MAO-B inhibitor at 6 mg/24 hr patch (approx. 10 mg PO)
Non-selective inhibition at 9 mg- and 12 mg-per 24 hr patch

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21
Q

MAO-I MOA

A

Block metabolism of NE, 5-HT, and DA via inhibition of MAO enzyme
NE and 5-HT: metabolized by MAO-A
DA and Tyramine: metabolized by MAO-A and MAO-B

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22
Q

MAO-I pharmokinetics

A

Rapidly absorbed
Maximum MAO inhibition at 14 days
T ½ of 1-4 hrs
Clinical effects seen for up to 14 days after discontinuation

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23
Q

MAO-I Adverse Effects

A 
Orthostatic hypotension		-  Dizziness
Mydriasis				-  Edema
Piloerection				-  Insomnia
Tremor					-  Anorgasmia
Excessive daytime sleepiness
Weight gain
hepatic dysfunction
hypertensive crisis
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24
Q

Hypertensive Crisis that is an ADR in MAO-I

A

Occurs after ingestion of tyramine containing foods or drugs  dietary restriction
Tyramine = pressure amine; metabolized in gut by MAO enzymes
Causes release of NE from presynaptic sites
Signs and symptoms: hypertension, occipital headache, neck stiffness, diaphoresis, heart palpitations, nausea, vomiting
Medical emergency

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25
Q

MAO-I drug interactions

A

Washout period of 14 days necessary when switching from an MAOI to another antidepressant or from another antidepressant to an MAOI (5 week washout when switching from fluoxetine to an MAOI)
Serotonin syndrome with other antidepressants

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26
Q

What are 6 SSRI medications used?

A 
Fluoxetine (Prozac®)
Sertraline (Zoloft®)
Paroxetine (Paxil®)
Citalopram (Celexa®)
Escitalopram (Lexapro®)
Fluvoxamine (Luvox®) – FDA approved 					  for only OCD
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27
Q

SSRI’s

A

1st line therapy for MDD
Favorable safety profile
No evidence to suggest one SSRI more efficacious than another
Indicated for other psychiatric comorbidities
Anxiety disorders (i.e., OCD, PTSD, general anxiety

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28
Q

MOA of SSRI’s

A

Inhibit reuptake of 5-HT   5-HT activity in neuronal synapse
Low affinity for histaminergic, cholinergic, and α-adrenergic receptors

29
Q

Pharmacokinetics of SSRI’s

A

T ½ = approx. 24 hrs for sertraline, paroxetine, citalopram, and escitalopram
T ½ = 7+ days for fluoxetine (and active metabolite norfluoxetine) 4-5wks to get to steady state
Hepatic impairment significantly interferes with metabolism
Measurement of serum concentrations does not correlate with clinical outcome

30
Q

SSRI’s adverse effects

A

Nausea - Headache
Sleep disturbances - Agitation/anxiety
Sexual dysfunction - Tremor
Less sedating and cause less weight gain than TCAs or MAOIs
Serotonin syndrome with other serotonergic agents

31
Q

Discontinuations Syndrome of SSRI’s

A

Potential for withdrawal symptoms with abrupt discontinuation of short-acting SSRIs
Symptoms: vivid dreams, nightmares, tremor, dizziness, crying spells, nausea, poor concentration
Occurs as early a 1-4 days or up to 25 days after discontinuation
Taper dose slowly over a period of 7-10 days

32
Q

Fluoxetine Drug interactions

A

5-week washout after discontinuation before starting an MAOI (2-week washout for all other SSRIs)

33
Q

Sertraline Drug interactions

A

Weak inhibitor of CYP2D6 at low doses; becomes more potent at higher doses (still weaker than fluoxetine and paroxetine)
No known clinically significant drug interactions

34
Q

Citalopram and escitalopram Drug interactions

A

Possible dose dependent inhibition of CYP2D6

No known clinically significant drug interactions

35
Q

Fluvoxamine Drug interactions

A

Potent inhibitor of CYP1A2

Weak inhibitor at CYP2C9

36
Q

3 Mixed 5-HT/NE Reuptake Inhibitors

A

Venlafaxine (Effexor®)
Duloxetine (Cymbalta®)
Desvenlafaxine (Pristiq®) active metabolite of effexor

37
Q

Venlafaxine

A

Extended-release (XR) formulation considered a 1st line agent for MDD
No significant adverse affects or cardiac affects
3 divided doses

38
Q

Venlafaxine MOA

A

Potent 5-HT/NE reuptake inhibitor
5-HT reuptake inhibition 3-5 fold higher than NE reuptake inhibition at doses < 200 mg/day
Weak DA reuptake inhibitor

39
Q

Venlafaxine Pharmacokinetics

A

Well-absorbed
Minimal plasma protein binding
T ½ = 5-11 hrs (longer with XR formulation)
Substantial 1st pass metabolism via CYP2D6

40
Q

Venlafaxine Adverse effects

A

Side effect profile similar to SSRIs
Common side effects
Nausea, constipation, sedation, dry mouth, insomnia, dizziness, sweating, sexual dysfunction
Discontinuation syndrome
not for someone with uncontrolled HTN

41
Q

Drug interactions for Venlafaxine

A

Weak inhibitor of CYP2D6
Little or no inhibition of other CYP enzymes
Can potentially accumulate when combined with CYP2D6 inhibitors; use cautiously
Serotonin syndrome

42
Q

Duloxetine (5)

A

Balanced reuptake inhibitor if 5-HT and NE
FDA indicated for MDD, diabetic neuropathy and fibromyalgia
Adverse effect profile similar to venlafaxine (but no dose related  in BP)
Metabolized at CYP2D6 and CYP1A2
T ½ = 12 hrs

43
Q

Desvenlafaxine

A

Studies show no additional benefit above 50 mg/day with an increase in adverse effects at higher doses
Adverse effect profile similar to venlafaxine
No comparison studies with any other antidepressants

44
Q

Buproprion/Wellbutrin

A

Most potent neurochemical action is DA reuptake inhibition (increase DA activity)
Very low reuptake inhibition of NE
No appreciable effect of reuptake of 5-HT

45
Q

Buproprion/Wellbutrin indications

A

Depression: Wellbutrin® (immediate-release, SR, XL)

Smoking cessation: Zyban® (bupropion SR)

46
Q

Buproprion/Wellbutrin Adverse effects

A

Use with caution with drugs known to  seizure threshold
Use with an MAOI contraindicated
Very low inhibition of CYP 2D6
Use with agents metabolized via CYP2D6 should be used with caution

47
Q

Nefazodone MOA

A

Both a 5-HT2 antagonist and 5-HT reuptake inhibitor

Negligible affinity for cholinergic, histaminergic, dopaminergic receptors

48
Q

Nefazodone Adverse effects and black box warning

A

Black box warning related to cases of life-threatening hepatic failure
Common adverse events: light-headedness, dizziness, dry mouth, nausea, asthenia, orthostatic hypotension, sedation
Potent CYP3A4 inhibitor
Not a 1st line agent

49
Q

Trazodone immediate release

A

Use as antidepressant has decreased due to adverse effects (i.e., orthostatic hypotension, dizziness, sedation)
Usual dosage range: 150-300 mg/day
Commonly used as a sedative at does of 50-100 mg HS
Rare cases of priapism, QTc prolongation

50
Q

Trazodone extended release

A

Oleptro®
Starting dose: 150 mg once daily at bedtime
Increase by 75 mg/day every 3 days to a maximum of 375 mg/day.
Side-effect profile similar to immediate- release trazodone

51
Q

Mirtazapine

A

Remeron®
Selective, presynaptic α2-receptor antagonist
Enhancement of NE transmission by α2-autoreceptor blockade  stimulation of α2-adrenoreceptors  ’d 5-HT firing
T ½ = 20-40 hrs

52
Q

Mirtazapine adverse effect and drug interactions

A 
Adverse Effects
Sedation
Dry mouth
Constipation
Increased appetite
Weight gain

Drug interactions
Other sedating agents
MAOIs

53
Q

Vilazodone

A

Viibryd®- dual 5-HT activity

maintenance dose of 40 mg once daily with food

54
Q

Vilazodone Adverse effects

A

Adverse Effects:
Common: diarrhea, nausea, dizziness, dry mouth, insomnia, vomiting, and decreased libido, dry mouth
Rare: May cause new or worsening cataracts with long-term use

55
Q

Levomilnacipran

A

Fetzima® - SNRI
Twofold greater potency for norepinephrine relative to serotonin reuptake inhibition
Higher selectivity for norepinephrine reuptake inhibition compared with venlafaxine and duloxetine

56
Q

Levomilnacipran side effects

A

Side effects in clinical trials include nausea, constipation, and sweating
Primarily excreted by the kidneys
Role in treatment of depression unknown –only studied versus placebo

57
Q

Vortioxetine

A

Brintellix® - Serotonin re-uptake inhibitor and agonist

Most common adverse reactions: nausea, constipation and vomiting

58
Q

Vortioxetine drug interactions

A

Strong inhibitors of CYP2D6: Reduce dose by half
Strong CYP Inducers: Consider increasing dose
Role in treatment of depression unknown

59
Q

St. John’s wort

A

Herbal product – not regulated by the FDA
Found to be safe and effective for treatment of mild-to-moderate depression
significant drug interactions
Potent CYP3A4 inducer

60
Q

What is Electroconvulsive Therapy (ECT)

A

Small current used to induce a seizure
30 to 60 seconds in duration
Patients are sedated and neuromuscular blocking agents used to prevent muscle contractions
Course: 6-12 treatments (2-3 times/week)

61
Q

ECT indications?

A

high suicide risk
rapid physical decline
drug non-response or intolerability
history of prior response to ECT

62
Q

Contraindications and limitations of ECT

A

Contraindications: no absolute contraindications
Limitations/AEs: high relapse rate, impairments in memory and neurocognitive function, treatment- emergent mania, headache, nausea, muscle aches

63
Q

Elderly Populations

A

Depression often mistaken for another disorder (i.e., dementia)
Depressed mood may be less prominent than other symptoms (i.e., loss of appetite, cognitive impairment, sleeplessness, anergia, anhedonia)
Somatic complaints frequent
Increased suicide attempts
SSRIs 1st line
Start LOW and go SLOW

64
Q

Pregnancy Population

A

Risks and benefits must always be carefully weighed
New evidence for potential respiratory distress and withdrawal syndrome in neonates whose mothers took SSRIs during pregnancy
Risks of untreated depression?
ECT can be used safely during pregnancy
Sertraline and paroxetine appear in low concentrations in breast milk

65
Q

3 ways to evaluate the response of treatment

A

Target signs and symptoms
Quality-of-life issues
Tolerability of the agent

66
Q

Evaluation of target signs and symptoms (4)

A

Non-response: 50% ↓ in baseline symptoms

Remission: return to baseline functioning

67
Q

Antidepressants: General Dosing Information (4)

A

Lag time before start of therapy and onset of clinical response  can lead to noncompliance
Onset of activity usually takes 1-2 weeks
Improvement in energy, appetite, sleep disturbances
3-4 weeks usually required before mood- elevating response seen
Adequate trial: 6-8 weeks at a maximum dosage

68
Q

Treatment Resistant Depression

A

Definition = remission not achieved after 2 optimal antidepressant trials (6-8 weeks)

69
Q

2 approaches used for treatment of resistant depression

A

Switching

Augmentation with another antidepressant, lithium, T3 (triiodothyronine), atypical antipsychotic, ECT, psychotherapy

Pharm- Antipsychotics (2 decks)

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