Neuro-psych Drugs Flashcards

1
Q

Role of tertiary amines in TCAs

A

Have two methyl groups in side chain with dominant effect on serotonin reuptake

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2
Q

Role of secondary amines in TCAs

A

Single methyl group with dominant effect on norepinephrine reuptake

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3
Q

TCA pharmacokinetics

A

Good GI absorption but high first pass (50%)

Large Vd

Liver metabolism

Long half-life >24hrs

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4
Q

Adverse effects of TCAs

A

Dry mouth (xerostomia)
Urinary hesitancy
Decreased gastric motility
Blurred vision

Orthostatic hypotension

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5
Q

Cardiac effects of TCAs

A

Increased Arrhythmogenicity
-tachycardia/palpitations
-Prolonged QTc
-narrow therapeutic index should be considered in patients with suicidal ideation

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6
Q

Anesthesia Implications: TCAs

A

Exaggerated response to indirect Sympathomimetics- ephedrine

Prolonged use- adrenergic desensitization and catecholamine depletion=vasoplegia

Pro-arrhythmic effect with volatiles

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7
Q

SSRI mechanism

A

5-HTT inhibition and modulation of post synaptic 5-HT receptors

Also production of neuroprotective proteins along with anti-inflammatory effects

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8
Q

SSRI pharmacokinetics

A

Hepatic metabolism

Most have inactive metabolites

Half-life about a day- can take weeks for adverse reactions to resolve completely

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9
Q

SSRI adverse effects

A

Mostly well tolerated

Sexual dysfunction, weight changes, dizziness, sleep disturbances

Serotonin syndrome- agitation-increased sympathetic outflow, can mimic malignant hyperthermia, -usually occurs in combination with other drugs modulating serotonin activity

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10
Q

SSRI anesthetic considerations

A

Prolonged QTC

Inhibit platelet aggregation

Serotonin syndrome

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11
Q

MAOI mechanism

A

Irreversibly binds MAO, inhibits enzyme for up to two weeks

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12
Q

MAO-A

A

Metabolizes via deamination: serotonin, epinephrine, norepinephrine, melatonin, dopamine, tryptamine

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13
Q

MAO-B

A

Metabolizes via deamination: phenylethylamine, tyramine, dopamine, tryptamine,

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14
Q

Adverse effects of MAOIs

A

Avoid foods containing large amounts of tyramine

Orthostatic hypotension

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15
Q

MAOI drug interactions

A

Indirect acting Sympathomimetics may case hypertensive crisis
AVOID ephedrine
AVOID phenylpiperidine opioids, especially meperidine=life threatening hypertensive crisis

Morphine is opioid of choice

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16
Q

First generation antipsychotics

A

Blockade of D2 dopamine receptors

Compazine
Phenergan
Haldol
Reglan

Not commonly given due to high incidence of adverse effects

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17
Q

Extrapyramidal symptoms

A

Involuntary movement disorders

Dystonia-acute spasm/muscle contraction-give anti cholinergic to reverse- can occur after one dose

Akathesia- restlessness-same treatment

Pseudoparkinsonism- generally reversible- typically don’t give dopamine antagonists with Parkinson’s since it exacerbates symptoms

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18
Q

Tardive dyskinesia

A

Choreoathetoid movements (wormlike)
From Chronic therapy

Anticholinergic agents may worsen TD

Administration of D2 antagonist will exacerbate TD

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19
Q

Neuromalignant syndrome

A

Closely resembles malignant hyperthermia and serotonin syndrome

Mortality 50%, rare, rhabdo in severe cases

Treatment- dantrolene and supportive care- with addition of a dopamine agonist (bromocriptine)

20
Q

Clozapine (clozaril)

A

2nd Gen
Dopamine Antagonist (D4) and 5-HT 2c/2a serotonergic receptors

Schizophrenia

Adverse effects:
agranulocytosis-low wbcs
Myocarditis
Orthostatic hypotension, ketoacidosis

21
Q

Olanzapine (zyprexa)

A

2nd gen
Dopamine antagonist, 5-HT2a, & alpha1-adrenergic antagonism…. Also weak GABAa agonist

Bipolar

Adverse: POTENTIATION OF BENZOS
Weight gain, diabetogenesis
EPS

22
Q

Quetiapine (Seroquel)

A

2nd Gen
Less D2, high affinity for 5-HT2a and H1 histamine=sedation

Schizophrenia/ bipolar-polar

Adverse effects:
Sedation
Weight gain
Diabetogenesis

23
Q

Aripiprazole (abilify)

A

2nd gen

Schizophrenia/ bipolar

Partial antagonism/agonism of serotonin and dopamine systems

24
Q

Risperidone (Risperdal)

A

2nd Gen

High affinity for 5-HT2a

Schizophrenia/bipolar

Well tolerated generally

25
Q

Lithium

A

Narrow therapeutic index= increased toxicity

Thiazide diuretics/ACEI/ARA blockers/NSAIDS all increase blood levels

Prolongs NMBDs duration of action

26
Q

Valproate (depakote)

A

Anticonvulsant

Hepatitis/pancreatitis
Thrombocytopenia/platelet dysfunction

Increases metabolism of NMBDs

27
Q

Carbamazepine (Tegretol)

A

Anticonvulsant

Blood dyscrasias
SIADH

Increased metabolism of NMBDs as well as versed/fentanyl/tramadol

28
Q

Lamotrigine (lamictal)

A

Anticonvulsant
Severe derm reactions

Increased metabolism of NMBDs

29
Q

Amphetamine MOA

A

enhances dopaminergic/serotnergic and noradrenergic release

30
Q

Methylphenidate MOA

A

Norepi and dopamine reuptake inhibitor

ADHD/Narcolepsy/obesity

31
Q

Levodopa Mechanism

A

Converted to dopamine in CNS- normalizing dopamine levels in corpus striatum and binding pre/post dopamine receptors

32
Q

Why is levodopa administered with carbidopa?

A

Carbidopa is a AAAD (aromatic L-amino acid decarboxylase)

Prevents accumulation of dopamine in the periphery and increases cerebral bioavailability of levodopa

33
Q

Levodopa anesthetic considerations

A

Continue in perioperative period due to short half-life

Give just before surgery and just after- have patient bring it in

Consider NG for longer procedures for intraop admin

34
Q

Pramipexole

A

Adjunct with levodopa/carbidopa

No major anesthetic considerations

35
Q

Treating Myasthenia Gravis

A

In addition to immunomodulators, anticholinesterases are used to increase ACh at the NMJ

-primarily pyridostigmine

Interference with NMBDs and potential to prolong ester-local anesthetics and succinylcholine

36
Q

SSRI with active metabolite

A

Fluoxetine- extends typically SSRI half-life from 1 to 2-3 days

37
Q

Phenothiazine examples and class

A

First generation antipsychotics

Prochlorperazine (compazine)
promethazine (phenergan)
Chlorpromazine (Thorazine)

38
Q

Butyrophenones

A

First Gen antipsychotics

Haloperidol (haldol)
Droperidol (Inapsine)

39
Q

Benzamide class and example

A

Metoclopramide (reglan)

40
Q

Clozapine (clozaril) adverse effects

A

Agranulocytosis
Myocarditis/cardiomyopathy
Hyperglycemia/DKA

41
Q

2nd gen antipsychotic with benzo potentiation

A

Olanzapine (zyprexa)

Also weak gaba receptor agonist

42
Q

Reason for sedation with seroquel

A

Histamine 1 receptor affinity

43
Q

Interesting thing about aripiprazole (abilify) MOA

A

Partial AGONIST of D2 and 5HT, also strong antagonism of other Dopamine/serotonin receptors…

44
Q

Compared to clozapine, Risperidone (risperdal) has:

A

20-50 times higher affinity for 5HT and D2 receptors

Well tolerated/no QT prolongation

45
Q

Avoid chronic NSAIDs with this antipsychotic

A

Lithium

46
Q

QTC prolongers

A

SSRIs
TCAs

Ondansetron
Granosetron
Dolanosetron

Promethazine
Diphenhydramine
Dimenhydrinate

Droperidol
Haloperidol
Metoclopramide

NOT: palonosetron/aprepitant or scopolamine