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SRNAPharmacology I > EXAM 4-Antidepressant Agents > Flashcards

EXAM 4-Antidepressant Agents Flashcards

1
Q

Antidepressant target

A

Targeting neurons in the NS< and specific neurotransmitter altered (NE or 5-HT pathways)

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2
Q

Antidepressants lacks

A

dopamine 2 receptor antagonists

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3
Q

High incidence of adverse effects

A

CV, CNS and anticholinergic toxicities

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4
Q

Clinical uses of TCAs

A

Depression
Migraine
Anxiety
Enuresis

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5
Q

Classification of TCAs

A

Tertiary amine

Secondary amine

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6
Q

• TCAs block the reuptake of both NE and 5-HT into the presynaptic nerve
terminal via inhibiting NET and SERT and thus enhance noradrenergic and
serotonergic transmission

A
  • TCA’s ALSO block/antagonize other types of receptors to varying degrees which contributes to the different adverse effect profile of the individiual agent
  • α1-adrenergic antagonism
  • H1 antagonism – antihistamine effects
  • Muscarinic antagonism – anticholinergic effects
  • Block Na+ channels – leads to cardiac conduction abnormalities
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7
Q

Pharmcokinetics of TCA

A

Highly protein bound >90% extensive liver metabolism

high Vd

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8
Q

Quinidin like effect

A

because block fast na channel

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9
Q

TCA and cardiac effects

A

Cardiac conduction abnormalities occur primarily in overdose situations

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10
Q

TCA and seizures

A

Decrease seizure threshold.

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11
Q

What can cause Withdrawal symptoms

A

Abrupt cessation of treatment may produce withdrawal symptoms

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12
Q

• Tertiary amines are metabolized into

A

active secondary amines

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13
Q

Short half life predict withdrawal

A

Pharmacokinetics : half life

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14
Q

TCA drug to drug, never give which drug?

A

MAOIs – NEVER GIVE AT THE SAME TIME!!!

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15
Q

*****TCA can do what to sympathomimetic agents?

A

Potentiate/decreases

Interaction is COMPLEX AND PREDICTABLE

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16
Q

Recently started on TCA,

A

an exaggerated pressor response should be anticipated from direct or indirect acting sympathomimetics.. MORE PRONOUNCED such as EPHEDRINE (primarily indirect)

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17
Q

Induction of anesthesia may be associated with an increase risk
of cardiac arrhythmias in patient’s treated with TCAs
• The dose of exogenous epinephrine necessary to produce
cardiac dysrhythmias during anesthesia with a volatile
anesthetic is decreased by TCAs

A

Normal dose of epinephrine, may be associated with higher risk

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18
Q

A potential for an increase in cardiac arrhythmias may be observed in patients treated with ______ _____ and _____

A

Halothane, pancuronium and TCAs

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19
Q

• Because the anticholinergic (antimuscarinic) effects of drugs are additive, the use of centrally acting anticholinergic (antimuscarinic) agents for preoperative medication of patients treated with TCAs. Exception is this medication ______

A

may be associated with increased risk of postoperative delirium and confusion; Glycopyrrolate

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20
Q

Glycopyrrolate

A

is less likely to have this drug interaction in patients being treated with

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21
Q

Centrally acting , name 2 medications

A

Scopalamine

Glycopyrrolate

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22
Q

TCA can cause_____and using _________can increase the risk

A

HYPOTENSION

Alpha 1 antagonists.

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23
Q

TCA overdose can be

A

life threatening
CNS and cardiotoxicity
Severe hypotension and cardiac depressant “quinidine -effect)
CNS depression, respiratory depression, coma, seizures

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24
Q

GI decomtamination

A

Large volume gastric lavage

EMESIS is contraindicated

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25
TCA overdose management
- ECG and monitoring - Airway, IV - GI decomtaminiation - Hyperventilation or serum alkalinization with IV sodium
26
TCA, those antiarrhythmics contraindicated
1A and 1 C
27
SSRI clinical use
do not need to know
28
SSRI MOA
Selectively inhibit the re-uptake into the pre-synaptic nerve terminal by inhibiting SERT
29
SSRI do not block those 2 receptors
do not block histamine or alpha adrenergic receptors.
30
SSRI most common to remember
NAUSEA
31
Less common of SSRI
Increase risk of bleeding post op (because of serotonin on platelet)
32
Withdrawal: Least common with Fluoxetine due to
long-half life of both fluoxetine and its active metabolite, norfluoxetine.
33
Drugs to drug interaction with SSRIs
CYP 450 enzymes | SSRIs are inhibitors of many CYP450 Enzyme systems
34
What is the most potent CYP450 inhibitor of all SSRIs?
Fluoxetine
35
MOAI
do not use any SSRI within 14 days of stopping an MAOIs | MUST WAIT AT LEAST 5 weeks after stopping fluoxetine before starting any MAOI
36
Zyvox (Linezolid)
non-selevitve MAOI propertises | Combined use of risk SEROTONIN SYNDROME
37
Serotonin Syndrome
rare but severe, potentially life threatening condition that can occur with the use of SSRI.
38
Symptoms of serotonin syndrome
AMS: Agitation, hallucinations, coma Tachycardia, hyperthermia, hypertension in more severe: resemble NMS which include hyperthermia, muscle rigidity, myoclonus and coma.
39
MEMORIZE Differential diagnosis of serotonin sydrndome KNOW chart table43-5
SS : serotonin agonists | NMS
40
Longest half life of all SSRI
Fluoxetine
41
Pharmacokinetics of fluoxetine
prolonged half life | highly protein bound
42
SSNIs
Serotonin NE uptake inhibitors.
43
SSNIs MOA
primarily block reuptake and NE and dopamine in pre-synaptic terminal
44
Adverse effects of SSNI
Nausea, nausea, nausea, HTN Increased bleeding post op
45
MOAIs
monoamine oxidase inhibitors
46
MOAis MOA
Nonselective IRREVERSIBLE of MOA-A and MOA-B both peripheral and Central actions
47
MOA inhibit what ?
inhibit enzyme responsible for the breakdown of NE, 5-HT, Dopamine, Epi, and EXOGENOUS MONOAMINES( Tyramine)
48
Since MAOis are IRREVERSIBLE
it takes up to 2 weeks for MAO activity to recover
49
MAOis major adverse effects
ORTHOSTATIC HYPOTENSION
50
Must maintain a _______ on MAOIs
Strict diet
51
Foods that contain tyramine and beta-phenylethanolamine
should avoided in patient with MAOis due to increased risk of developing hyptertensive crisis (hypertension and Hyperpyrexia)
52
MAO-A in the intestinal wall and MAO-A and MOA-B in the liver normally degrade dietary tyramine?
Mao inhibition leads to the accumulation of tyramine in adrenergic nerve terminals and neurotransmitter vesicles and induces NE release and this increase release of NE stimulates post-synaptic receptors in the periphery increasing blood pressure to dangerous levels.
53
Esmolol and MAOIs consideration?
Use in caution because ESMOLOL is cardio-selective for beta 1 and may leave alpha 1 unblock, and MAOIs release NE which will bind to alpha 1 receptor. Give labetalol, or other drugs.
54
Prohibited food in MAO-A
``` Pork Liver, fava beans Avocados, cheese alcohol wines ```
55
Sympathomimetic such as ephedrine and phenylephinre
reduce the dose to 1/3
56
Do not give any with MAOs
in-direct symptomimetics (ephedrine)
57
Do not give with MAOs ( 2 )
induce skeletal muscle rigidity | SERTONIN SYNDROME
58
Post op shivering harder to manage because what is contraindicated with MAOIs?
CANNOT give meperidine or meperidine derivatives
59
Do not use these class of meds within 14 days of
TCAs SSRIs SNRIs
60
Use caution with _____ and_____why>
cocaine and local anesthetics; potentiation effects.
61
Anesthetics requirements for volatile anesthetics with MAOis
increased
62
General anesthesia and spinal anesthesia with the MAOIs
HYPOTENSION may be exaggerated.
63
Are responses to Nondepolarizing NMB altered by MAOIs
NO
64
For MAOIs recovery of normal enzyme function is dependent of what?
- Synthesis and transport of new MAO enzyme to monoaminergic nerve terminals.
65
MAOIs are the
3rd line or last line agents | Limited use for patient resistant to other forms of therapy because on toxicities risk of drugs and food interactions.
66
Trazodone act as a _____ | what receptors does it block?
Acts as a potent antagonist at 5-HT2 receptors and to a lesser degree also selectively inhibits neuronal reuptake of 5-HT • It also significantly blocks alpha1 adrenergic (postural hypotension) and histamine (H1) receptors
67
Cases of life-threatening hepatic failure have been reported in patients treated with
Nefazodone!!!
68
Weight loss managmenet smoking cessation ANti-depressant
Bupropion
69
Buproprion
causing seizures.
70
Combining anesthetics that causes seizure with Buproprion
would increase seizure threshold
71
Serotonin Reuptake inhibitor.
Vilazodone
72
Vortioxetine (BRintellix)
Complex medication SSRI and also antagonist at multiple receptors DOES MANY THINGS Antagonist, partial agonist, agonist
73
Sent apart Brintellix
TERMINAL HALF LIFE 66 Hours
74
Buspirinone Used for ______ does it interact with GABA? lack?
Anti -anxiety ( not related to any other class) Mimi the anti anxiety proper of benzo BUT DOES NOT interact with GABA receptors and lack prominent sedative, anticonvulsant and skeletal muscle relaxants
75
Lithium
Acute and maintenance therapy for Bipolar disorder | Lithium is the gold standard in bipolar treatment.
76
Lithium indications
Bipolar disorder | Depression (manic)
77
Exact mechanism of lithium
NO ONE KNOWS
78
Lithium is route _____, bioavailability is _____
PO ; 100
79
Lithium half life is a _____and excreted via______
24 hours; Kidney
80
Lithium competes with
Na for reabsorption in the proximal renal tubule, therefore , lithium retention can be increased by Na+ loss
81
NA depletion
dehydration will increase lithium reabsorption by the proximal tubule.
82
General range for most indications
0.6- 1.2 mmol/L
83
Drugs to Drug Lithium (increase reabsorption)
Thiazide ---> Increase LoOP--->Increase NSAIDS-->Increase (this is KETOROLAC, Ibuprofen) ACEi and ARBs
84
Drugs to Drug Lithium (increase reabsorption)
Neuromuscular Carbamazepine Antipsychotics
85
Neuromusclular blockade
Lithium prolonged effects of non-depolarizing and depolarizing NMB CCB --> Increase CNS toxicity
86
Lithium may potentiate ________or increase the risk for
EPS, NMS
87
Haldol with lithium
encephalopathic syndrome with | irreversible brain syndrome
88
Renal adverse effects
polyuria polydipsia VERY COMMON | 2L /day
89
Lithium induced nephrogenic DI
Amiloride can be given to treat
90
Lithium with any sedatives
InCREASE RISK OF SEDATION
91
Lithium
EKG changes - T wave flattening and inversion (U waves | QRS complex prolongation, sinus Brasdy, AV blocs when level are >2.5 mol/L
92
Lithium toxicity
>2 toxic
93
Lithium less than 1.5 mol/L
Fine hand tremor, nausea, vomiting, diarrhea, skeletal muscle weakness, mild polyuria and polydipsia
94
Lithium 1.5 -2.5
Muscle twitching, nygstamus
95
Lithium Over 2.5
BRAIN (seizure, coma) and CARDIAC symptoms
96
Name anesthesia implications & Lithium
NMB MAY BE prolonged | Lithium associated sedation suggests anesthetic requirements for injected and inhaled anesthetics could be DECREASED
97
CNS and lithiums
HIGH PLASMA concentration may delay recovery from the CNS depressant effects of barbiturates.

SRNAPharmacology I (29 decks)

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