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Flashcards in anti-depressants and mood stabilizers Deck (83):
1

what is the biogenic amine hypothesis for depression?

a functional deficit of monoamines (mostly NE & 5-HT) is thought to be involved in the pathophys. of depression

2

which population of pts needs to be warned about which BBW of antidepressants, especially during the initial weeks of treatment?

children and adolescents with thoughts of suicide

3

antidepressant drugs that are substrates for ___________ (MDR1; P-gp) which exists at the BBB limits the ability of drugs to accumulate in the brain

ABCB1

4

name the 4 antidepressants that are substrates for MDR1

citalopram
venlafaxine
paroxetine
amitriptyline
"can't volley proper antidepressants"

5

name the two antidepressants that are not substrates for MDR1

mirtazapine
fluoxetine

6

what are some of the indications for TCA therapy?

major depression, pain/anxiety disorders (OCD, phobias, panic), ADHD, nocturnal enuresis (imipramine), depression assoc. w/ schizophrenia

7

what is the MOA of TCAs?

inhibits the reuptake of 5-HT & NE into presynaptic terminals--> potentiate and prolong the actions of these neurotransmitters--> receptors and transporter regulation w/ repeated treatment
-also block mACh, 5-HT, & histamine receptors

8

orthostatic hypotension is an AE of TCAs due to antagonism of what receptor?

antagonism of alpha-ARs

9

blurred vision, worsening of narrow-angle glaucoma, dry mouth, constipation, urinary retention, tachycardia are all AEs of TCAs due to antagonism of what receptor?

antagonism of mAChR

10

what are some metabolic/endocrine related AEs of TCAs?

weight gain
sexual disturbances

11

what happens in TCA overdose?

has low therapeutic index
CV effects including: arrhythmias, direct myocardial depression, worsening of CHF
-also: acidosis, delirium seizures

"3 C's: convulsions, coma, cardiotoxicity"

12

describe some of the PKs of TCAs?

high first pass metabolism
high lipid solubility (allows distribution to brain & fat)
highly protein bound (high Vd), which limits excretion (leading to long half-life)

13

tertiary amines (TCAs) are metabolized to active secondary amines by what?

demethylation (imipramine, amitriptyline--> nortriptyline)

14

the tricylclic ring is subject to oxidation by what cyp enzyme and also can be conjugated?

subject to CYP2D6 oxidation & conjugation

15

name the atypical antidepressant drug: moderate inhibition of serotonin reuptake but primarily acts s a 5-HT2a antagonist & 5-HT1a partial agonist (SARI) useful in the treatment of depression characterized by anxiety and sleep disturbances

trazodone

16

trazodone inhibits which CYP enzyme?

CYP3A4

17

name the drug: analog of mianserin

mirtazepine

18

name the drug: enhances release of serotonin & NE by antagonizing presynaptic alpha-2ARs. Antagonizes 5-HT2 receptors.

mirtazepine

19

what are the AEs of mirtazepine?

potent antihistaminic--> sedating
increased weight gain
(tetracyclic antidepressant)

20

name the drug: weak blocker of DAT, SERT, & NET. active metabolite is a NE reuptake blocker

buproprion (also used in smoking cessation)

21

what are the AEs of buproprion?

agitation, anxiety, restlessness
risk of seizure, (no sexual AEs)

22

name the antidepressant drug: inhibits serotonin & NE reuptake (SNRI). Lacks antihistaminergic, anticholinergic, and antiadrenergic properties--> does not have TCA-like side effects

venlafaxine

23

what are the AEs of venlafaxine?

produces a small, sustained HTN, sweating dizzyness, nausea, anxiety

24

what is the most potent SNRI available?

duloxetine (100x more potent than venlafaxine)

25

describe the bioavailability and protein binding of duloxetine

50% bioavailability
highly bound to plasma proteins (95%)

26

duloxetine is metabolized by what two CYP enzyme?

CYP2D6 & CYP1A2

27

name the drug: recently approved serotonin modulator and stimulator. potent blocker of SERT & high efficacy partial agonist at 5-HT1a receptors. Partial agonist (5-HT-1b) and antagonist at 5-HT1d 3a, & 7 receptors?

vortioxetine

28

name the 5 SSRIs

Fluoxetine + Fluvoxamine
Paroxetine
Sertraline
Citalopram

"Flashbacks paralyze senior citizens"

29

what is the first line therapy in pts diagnosed with major depression?

SSRIs (also used to treat panic, OCD, social-anxiety disorder, ADHD, and some eating disorders)

30

describe the general behavior/clinical effects of SSRIs-acute

CNS stim.
anxiety
agitation

31

describe the general behavior/clinical effects of SSRIs-chronic

2-6 wks
improvement of most or all clinical symptoms, CNS activation remains

32

what are the AEs of SSRIs?

Nausea
decreased libido
sexual dysfunction
low incidence CV & anticholinergic
note: higher therapeutic index

33

what is the active metabolite of fluoxetine?

norfluoxetine-has half life of 7-9 days

34

most of the SSRIs are metabolized by what CYP enzymes?

CYP2D6 (strong inhib.)
CYP2C19 (strong inhib.)
CYP3A4

35

what drug class is contraindicated with SSRIs?

MAOIs (taking them together can cause serotonin syndrome)

36

serotonin syndrome is due largely to overstimulation of what receptors in the central grey (midbrain) and medulla?

5-HT1A

37

what is the clinical presentation of serotonin syndrome?

hyperpyrexia
hyperreflexia
tremor
shivering
myoclonus
agitation
seizures
confusion
delirium
CV collapse
coma

38

other than MAOis what other drugs can trigger serotonin syndrome?

can also be triggered by increased 5-HT release (amphetamines, MDMA) or via 5-HT agonists (LSD, buspirone, L-Tryptophan)

39

name the 4 MAOIs

tranylcypromine (not on drug list)
phenelzine
isocarboxazid (not on drug list)
Selegiline (MAO-B inhibitor)


"MAO Takes Pride in Shanghai"

40

what are the indications for MAOis?

typically used in pts who are unresponsive to treatment with other antidepressants and for whom ECT is not suitable.
-also used for panic disorder, agoraphobia

41

MOA of the monoamine oxidase inhibitors?

blocks oxidative metabolism of monoamines by IRREVERSIBLE inhibition of MAO-A & MAO-B in nerve terminals (MAO-A metabolizes primarily NE, 5-HT, tyramine; MAO-B mostly DA selective)

42

describe the general behavior/clinical effects of MAOIs-acute

CNS stim.
agitation
possibly euphoria

43

describe the general behavior/clinical effects of MAOIs-chronic

2-6 wks: improvement of most or all symptoms, CNS activation remains

44

what are the AEs of MAOIs?

sleep disturbances (increased arousal)
orthostatic hypotension
weight gain
some sexual dysfunction
hypertensive crisis ( with ingestion of tyramine)

45

MAOIs are inactivated by what process?

acetylation (phamacogenomic differences)

46

what are some of the drug interactions for MAOis?

foods containing high amounts of tyramine (cheese)

47

what can happen when taking MAOIs & sympathomimetic drugs?

acute hypertensive reaction

48

what can happen taking MAOis with meperidine, or dextromethorpham?

hyperpyrexia
delirium
convulsions
coma
death

49

name the 3 drugs used as mood-stabilizers

lithium
valproate
carbamazepine

"moody lions value carbs"

50

what are the indications for the mood stabilizers?

maintenance of manic depression (bipolar affective disorder)

51

MOA of lithium?

most favored hypothesis is Li inhibition of inositol phosphate signaling. also inhibits neurotransmitter-stim. adenylyl cyclase activity. Effective in ~60% of pts

52

what are the adverse effects for lithium?

very narrow therapeutic window
-neurologic/psychiatric: tremor, ataxia, hyperactivity, aphasia, sedation fatigue
-Glandular: edema, mild hypothyroidism
-renal: polydipsia, polyuria (nephrogenic diabetes insipidus)
-cardiac: bradycardia-tachycardia (sick sinus)
other: acne, folliculitis and exacerbates psoriasis

53

which drug can cause polyuria (nephrogenic diabetes insipidus?

lithium

54

which drug can cause bradycardia-tachycardia (sick-sinus)?

lithium

55

which drug can exacerbate psoriasis?

lithium

56

what are the drug interactions with lithium?

sensitive to diuretics & NSAIDs

57

name the two anticonvulsants that are now frequently used in the management of bipolar disorder

valproate & carbamazepine

58

what are the advantages of valproate and carbamazepine over Lithium?

increase dose faster, quicker response, better therapeutic index

59

what are the disadvantages valproate and carbamazepine compared to lithium?

less experience, efficacy questionable in severe disease

60

which drug is first line for bipolar disorder?

lithium (however milder forms of bipolar disorder may be treated with anticonvulsants)

61

what is the drug of choice when absence seizures are also accompanied with tonic-clonic seizures?

valproic acid

62

what is the MOA of valproic acid?

inhibits voltage-gated Na+ channels by stabilizing the inactivated state of the channel. Block of channel activity is use-dependent.
-Also blocks Ca2+ channels (T-type) to a lesser extent
-can also stim. GABA synthesis & inhibit GABA degradation
-at high doses may increase resting K+ conductances

63

valproate inhibits its own metabolism and the metabolism of other drugs via which CYP enzyme?

CYP2C

64

what are the AEs of valproate?

nausea, abd. pain, heartburn, sedation may be a problem, hepatotoxicity can be common (recomend liver function test)

65

what is the drug of choice for partial seizures, also may be used for generalized tonic-clonic seizures, also effective for trigeminal neuralgia?

carbamazepine

66

MOA for carbamazepine?

inhibition of Na channels (prolongs recovery time from inactivation)

67

which drug is metabolized primarily by CYP3A4 to an active metabolite 10,11-epoxide?

carbamazepine

68

name the two SNRIs

venlafaxine
duloxetine

69

name the TCAs (8)

Amitriptyline
nortriptyline
imipramine
desipramine
protriptyline

(all TCAs end in iptyline or ipramine except doxepin and amoxapine)

70

what are the drug interactions for carbamazepine?

carbamazepine is a broad spectrum inducer of CYP2C & 3A families & in addition to induction of UGTs

71

what are the AEs of carbamazepine?

diplopia & ataxia are common
mild GI upset
at high doses drowsiness
rash common idiosyncratic reaction
some occurences of aplastic anemia

72

name the drug that matches the pt with most benefit: elderly pt; a pt with agitated depression or pt w/ GI distress

citalopram

73

name the drug that matches the pt with most benefit: noncompliant or forgetful pt; excessive fatigue

fluoxetine

74

name the drug that matches the pt with most benefit: less likely to produce initial anxiety &/or insomnia

paroxetine

75

name the drug that matches the pt with most benefit: the medical/surgical pt on one or more drugs. initial activation and increased alertness desired

sertraline

76

name the drug that matches the pt with most benefit: pts with menopausal symptoms or failing an SSRI trial. At higher doses pts with chronic pain

venlafaxine

77

name the drug that matches the pt with most benefit: pt with depression and chronic pain (effects on pain are dose-dependent) pt failing an SSRI trial

duloxetine

78

name the drug that matches the pt with most benefit: the medically ill pt with weight loss, insomnia and nausea

mirtazapine

79

name the drug that matches the pt with most benefit: the now depressed or potentially bipolar pt. The apathetic, low energy pt. Pts motivated to stop smoking. Helpful for ADHD

buproprion

80

which antidepressant is "unlikely" to cause sexual dysfunction?

mirtazapine

81

which antidepressant "rarely" causes sexual dysfunction?

buproprion

82

name the drug that matches the pt with the least benefit: pts who are agitated, very anxious &/or panicky. Pts at risk for seizures &/or w/ hx of head trauma, substance abuse, eating disorder or electrolyte disturbance

buproprion

83

name the drug that matches the pt with the least benefit: pts who are agitated, very anxious &/or panicky. Pts at risk for seizures &/or w/ hx of head trauma, substance abuse, eating disorder or electrolyte disturbance

buproprion