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Neuro 1 > Pharm > Flashcards

Pharm Flashcards

1
Q

DA receptor agonist

A

activate D2 receptor: reduce activation of indirect pathway

Tx: (early) Parkinson’s, advanced PD in combo with L-DOPA to reduce “on-off”

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2
Q

MAO-B inhibitor

A

prevents DA metabolism (may prevent free radicals)
Tx: Parkinson’s
DI (do not take with): meperidine, TCAs, SSRIs
AE: potentate AE of L-DOPA

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3
Q

COMT inhibitor

A
  1. prevents DA metabolism: prolong action of L-DOPA
  2. increases L-DOPA bioavailability
  3. reduces 3OMD production that may compete with L-DOPA for GI and BBB transport
    Tx: Parkinson’s with L-DOPA to reduce fluctuations
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4
Q

antimuscarinics

A

block cholinergic activation in striatum
Tx: Parkinson’s (early or adjunct to L-DOPA)
AE: drowsiness, confusion, delusion, hallucination, mood change
other AE: dry mouth, blurred vision, mydriasis, urinary retention, constipation, tachycardia, palpitations, arrhythmia, increased intraocular pressure
CI: BPH, glaucoma, OBD
DI: TCA, antihistamines

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5
Q

VMAT inhibitor

A 
deplete DA (inhibit packaging into vesicles)
Tx: Huntington's
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6
Q

D2 receptor antagonist

A

Tx: Huntington’s

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7
Q

L-DOPA

A

DA replacement: crosses BBB unlike DA
converted to DA by L-AAD
Tx: Parkinson’s (late only :due to tolerance: Tavalin; early and late: Dr. J)
AE (L-DOPA alone): GI (anorexia, N/V), arrhythmia, orthostatic hypotension
DI: Vit. B6 increases metabolism
CI: MAO-A inhibitors (hypertensive crisis), psychotic patient, glaucoma (close), cardiac disease, peptic ulcer, melanoma
give BEFORE meal (L-AA and L-DOPA compete for GI transporters)
give with CARBIDOPA

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8
Q

carbidopa

A

L-aromatic amino acid decarboxylase (L-AAD) inhibitor: does not cross BBB
reduces peripheral L-DOPA conversion to DA
reduces amount needed and AE of L-DOPA
AE (in combo with L-DOPA): behavioral, dyskinesia
give with L-DOPA

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9
Q

bromocriptine

A

DA receptor agonist: D2 agonist/ D1 partial agonist

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10
Q

pramipexole

A

DA receptor agonist: D2 selective agonist

free radical scavenger

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11
Q

ropinirole

A

DA receptor agonist: D2 selective agonist

metabolized by CYP1A2

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12
Q

apomorphine

A

DA receptor agonist: D1/D2 agonist

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13
Q

amantadine

A

antiviral
enhance DA release (possibly enhance synthesis, inhibit DA uptake, interaction with NMDA receptors)
Tx: Parkinson’s (modest and short lived effects)
AE: depression, agitation, irritability, insomnia, excitement, hallucinations, confusion, restless
overdoes: psychosis
CI: seizures, HF

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14
Q

selegiline

A

MAO-B inhibitor
metabolites: meth/amphetamine: increase DA release
Tx: patients whose responsiveness to L-DOPA has declined (not useful alone)

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15
Q

rasagiline

A

MAO-B inhibitor: more potent

Tx: late Parkinson’s with L-DOPA, early Parkinson’s alone

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16
Q

entacapone

A

COMT inhibitor: PERIPHERAL only

PREFERRED over tolcapone

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17
Q

tolcapone

A

COMT inhibitor: PERIPHERAL and CENTRAL

AE: hepatic (why entacapone is preferred)

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18
Q

benztropine

A

antimuscarinic

Tx: Parkinson’s

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19
Q

diphenhydramine

A

antimuscarinic

Tx: Parkinson’s

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20
Q

trihexyphenidyl

A

antimuscarinic

Tx: Parkinson’s

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21
Q

reserpine

A

VMAT inhibitor

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22
Q

tetrabenazine

A

VMAT inhibitor

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23
Q

chlorpromazine

A

D2 receptor antagonist

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24
Q

haloperidol

A

D2 receptor antagonist

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25
Q

Idiopathic Parkinson’s vs. Parkinsonism

A

Idiopathic: unknown origin, genetic component

Parkinsonism: associated with infection (encephalitis), stroke, trauma, antipsychotics, MPTP; Tx RESISTANT

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26
Q

Advantages of DA agonist Tx in Parkinson’s

A
  1. no activation needed
  2. no toxic metabolites
  3. no competition for GI absorption or across BBB
  4. more selective: fewer AE
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27
Q

L-type Ca channel antagonist

A

future Parkinson’s Tx

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28
Q

fluoxetine

A

Tx: Huntington’s associated depression

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29
Q

opiate agonist

A

mu receptor agonist
SPINAL CORD and BRAIN
pre-synaptic: inhibit Ca entry
post-synaptic: activate K channels (hyper polarize cell)
Tx: pain
AE: SEDATION, N/V, pruritus, RESPIRATORY DEPRESSION, immunosuppression, increase intracranial pressure, orthostatic hypotension, CONSTIPATION, urinary retention, SOMNOLENCE

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30
Q

opiate partial agonist/antagonist

A

mu receptor partial agonist
can precipitate WITHDRAWAL in addicts and patients on full agonist chronically
decreased: analgesia and respiratory depression compared to morphine

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31
Q

opiate antagonist

A

mu, delta and kappa receptor antagonist

precipitate withdrawal in dependent patients

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32
Q

NMDA receptor antagonist

A 
non-narcotic
NMDA activation leads to Ca entry and central sensitization
Tx: pain 
NO resp. depression
AE: PSYCHOMIMETIC
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33
Q

TCAs

A

non-narcotic
CYP2D6
NE, 5-HT reuptake blocker (act on ascending corticospinal monoamine pathways)
Tx: pain
AE: dizzy, headache, fatigue, drowsiness, lethargy, hypersomnia, difficulty concentrating, memory impairment

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34
Q

anticonvulsants

A

non-narcotic
Ca or Na channel block
AE: SUICIDAL IDEATION
Tx: pain

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35
Q

alfentanil

A

opiate agonist

use: anesthesia

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36
Q

codeine

A 
opiate agonist
use: in combo with NSAIDs, COUGH suppression (not better than placebo in UR disorder or COPD)
orally available  
converted to MORPHINE
CI: accumulate in renal insufficiency
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37
Q

fentanyl

A

opiate agonist
use: anesthesia
can accumulate in adipose
can give in renal insufficiency

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38
Q

hydrocodone

A

opiate agonist

commonly abused

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39
Q

hydromorphone

A

opiate agonist
commonly abused
can give in renal insufficiency

40
Q

methadone

A

opiate agonist
block NMDA receptors, additive respiratory depression with heroin
Tx: inpatient opiate withdrawal
LONG ACTING; opioid dependence; Tx of choice for OPIOID DEPENDENT PREGNANT woman
req. SPECIAL PHYSICIAN LICENSE
AE: prolonged QT, ARRHYHMIA, constipation, reduced libido, sweating, drowsy

41
Q

meperidine

A

opiate agonist

antimuscarinic: tachycardia, no mitosis or GI spasms
metabolite: normeperidine: CYP, SSRI, can cause seizures; CNS stimulant toxicity in renal dysfunction

42
Q

oxycodone

A

opiate agonist
commonly abused
orally available

43
Q

oxymorphone

A

opiate agonist

commonly abused

44
Q

sufentanil

A

opiate agonist
MOST POTENT analgesic
use: anesthesia

45
Q

remifentanil

A

opiate agonist

use: anesthesia

46
Q

tramadol

A

WEAK opiate agonist
NE, 5-HT reupatake inhibitor
AE: seizures, blood sugar regulation
CI: accumulate in renal insufficiency

47
Q

butorphanol

A 
IV/SL; poor oral
opiate partial agonist
kappa agonist: DYSPHORIA
more sedation that nalbuphine
use: acute pain (post-op), nasal form for migraine;
CEILING effect: low overdose risk 
AE: WITHDRAWAL
48
Q

buprenorphine

A 
opiate partial agonist
delta and kappa antagonist
opioid dependence: TIGHT BINDING (displaces other opioids) with slow release (long duration of action)
CAD patient: increase cardiac problems
combine with NALOXONE to prevent abuse
does NOT req. a special license
49
Q

nalbuphine

A

opiate partial agonist
kappa agonist: DYSPHORIA
CAD patients: NO increase in cardiac problems

50
Q

pentazocine

A

opiate partial agonist
kappa agonist: DYSPHORIA
CAD patient: increase cardiac problems

51
Q

naloxone

A 
IV
NO ORAL BIOAVAILABILITY
opiate antagonist
Tx: opioid overdose, decrease opiate AE
can be formulated with opiate agonist to prevent drug abuse (not effective orally, antagonist if injection of crushed pill)
cross BBB
52
Q

naltrexone

A

ORAL
opiate antagonist: decrease baseline B-endorphin release (blocks DA elevation)
use: maintenance program for addicts (decrease alcohol craving); opioid dependence (poor adherence)
cross BBB

53
Q

methylnaltrexone

A

opiate antagonist

does NOT pass BBB: decreases AE of opioids without impacting central analgesia

54
Q

ketamine

A

NMDA antagonist

Tx: acute severe pain

55
Q

dextromethorphan

A

low affinity NMDA antagonist and antitussive
Tx: chronic, post-op pain; COUGH (mu and non-opiate receptors)
AE: hallucination, habit forming

56
Q

amitriptyline

A

TCA

57
Q

nortriptyline

A

TCA

58
Q

imipramine

A

TCA

59
Q

desipramine

A

TCA

60
Q

gabapentin

A

anticonvulsant
MoA: inhibition of voltage-gated Ca channels via alpha-2-delta subunit
AE: SEDATION, peripheral edema, GI
decrease dose in renal insufficiency

61
Q

lamotrigene

A 
anticonvulsant
Na channel blocker
use: neuropathy, stroke, MS, phantom limb
AE: blurred vision, hematologic
BBW: RASH (Steven-Johnson)
Tx: ancillary pain management
62
Q

carbamazepine

A 
anticonvulsant
Na channel blocker
CYP interactions
AE: dizzy, drowsy, agranulocytosis
Tx: ancillary pain management, Huntington's depression
63
Q

pregabalin

A

anticonvulsant
MoA: inhibition of voltage-gated Ca channels via alpha-2-delta subunit
AE: SEDATION, peripheral edema, GI
decrease dose in renal insufficiency

64
Q

Pain NT

A
  1. glutamate
  2. substance P
  3. CGRP (calcitonin gene-related peptide)
65
Q

mu opioid receptor (OP-3)

A 
highest affinity: ENDORPHINS
activation decreases pre-synaptic Ca influx and increases post-synaptic K efflux to reduce pain
1. supra spinal and spinal analgesia
2. RESIPIRATORY DEPRESSION
3. DECREASE GI TRANSIT
4. modulation of hormone and NT release
66
Q

delta opioid receptor (OP-1)

A

highest affinity: ENKEPHALINS

  1. supra spinal and spinal analgesia
  2. modulation of hormone and NT release
67
Q

kappa opioid receptor (OP-2)

A

highest affinity: DYNORPHINS

  1. supra spinal and spinal analgesia
  2. PSYCHOTOMIMETIC
  3. DECREASE GI TRANSIT
68
Q

alpha 2 agonist

A

SPINAL
pre-synaptic reduction in sympathetic outflow
Tx: pain
AE: sedation, hypotension, bradycardia

69
Q

clonidine

A

alpha 2 agonist
Tx: outpatient opiate withdrawal
not effective for: insomnia, muscle cramps, GI
AE: sedation, dry mouth, constipation at high dose

70
Q

dexmedetomidine

A

alpha 2 agonist

71
Q

What drugs that treat pain act

  1. peripherally
  2. in spinal cord
  3. centrally
  4. on initial signal transduction
A
  1. Na channel blockers
  2. opioids, anticonvulsants, antidepressants, alpha 2 agonist, NSAIDs
  3. opioids
  4. NSAIDs
72
Q

What are the most potent opioids?

A

fentanyl series

73
Q

morphine

A 
opiate agonist
kappa agonist
use: pulmonary edema, diarrhea
POOR ORAL BIOAVAILABILITY 
CI: renal failure
74
Q

Which opioid can be given transdermally?
When would you use it?
Considerations?

A

fentanyl
use in dysphagia, constipation, poor GI absorption (outpatient)
considerations: time to accumulate, have to take off to prevent OD, less constipation

75
Q

Which opioids can be given rectally?

A
  1. morphine
  2. hydromorphone
  3. oxymorphone
76
Q

Which opioids would you combine with an NSAID?

A

hydrocodone, oxycodone

77
Q

Where can opioids accumulate?

A

main reservoir: skeletal muscle

can accumulate in adipose with continued delivery: storage allows slow drug release

78
Q

opiate overdose signs

A
  1. coma
  2. pinpoint pupils
  3. respiratory depression
    altered mental status, severe perspiration, shock, pulmonary edema, unresponsive
79
Q

Drugs that worsen opioid CNS depression

A
  1. sedative hypnotics
    2 antipsychotic tranquilizers
  2. MAOI
80
Q

What AE of opioids do patients not develop tolerance to?

A
  1. mitosis
  2. constipation
  3. convulsions
    moderate tolerance: bradycardia
81
Q

What effects of opioids do patients develop tolerance to?

A
  1. analgesia
  2. euphoria, dysphoria
  3. mental clouding
  4. sedation
  5. respiratory depression
  6. anti-diuresis
  7. N/V
  8. cough suppression
82
Q

How does tolerance develop in opioid use?
1. classical view
2. other view
Why does this not occur with endogenous opioids?

A
  1. receptor phosphorylation by GRK increases affinity for beta-arrestin leading to internalization with degradation or recycling back to membrane after resensitization
  2. desensitization does not require endocytosis of receptor
    morphine: more degradation than with endogenous enkephalin
83
Q

How can you manage opioid AE?

  1. constipation
  2. somnolence
  3. N/V
  4. respiratory depression
  5. pruritus
A
  1. laxative, opioid antagonist in refractory
  2. remove additive CNS acting drugs, opiate rotation, Tx of Sx: methylphenidate, modafinil, dextroamphetamine
  3. titrate up dose, change route of delivery
  4. withhold dose, opioid antagonist: naloxone
  5. antihistamine
84
Q

Signs of opiate withdrawal

A
  1. agitation
  2. diaphoresis
  3. lacrimation, rhinorrhea
  4. piloerection
  5. dilated pupils
    also: anxiety, fear, sleep disturbance, nausea, diarrhea, pain
85
Q

How can you confirm suspected opiate intoxication?

What is the draw back?

A

Ab based enzymatic immunoassay (EIA)
ID’s: morphine, heroin, hydrocodone, codeine

FALSE NEG with synthetic opioids (fentanyl, meperidine, methadone)
can’t get precise concentration
FALSE POS.: fluoroquinolones (-floxacin)
sporadic pos. with semi-synteitc: oxycodone, hydromorphone

86
Q

How can you get the precise concentration of opiate metabolites in an opiate intoxicated patient?

A

GC-Mass Spec

87
Q

voltage gated Ca channel blocker

A

GABA
MoA: prevent trafficking of channel to surface (up regulation of channel occurs in hyper sensitization)
AE: dizzy, drowsy
Tx: ancillary pain med

88
Q

What do anticonvulsants carry an increased risk of

A

suicidal ideation

89
Q

What controls cough?

A

nucleus of solitary tract

90
Q

loperamide

A

antidiarrheal opioid: inhibit cholinergic nerves in enteric nervous system
no BBB access: no analgesia

91
Q

diphenoxylate

A

need prescription
antidiarrheal opioid: inhibit cholinergic nerves in enteric nervous system
no analgesia at recommended dose
ATROPINE added to discourage abuse

92
Q

complimentary and alternative medicine (CAM) pain Tx reasoning

A

opioids have AE and are addictive
some seem to reduce pain; herbals lack research (can have AE and interactions too)
1. spinal manipulation
2. massage
3. acupuncture
4. transcutaneous electric nerve stimulation

CAM could causes AE

93
Q

What opioids can be prescribed in renal failure?

A

hydromorphone

oxycodone

94
Q

What opioid can be used in alcohol dependence and craving?

A

naltrexone

95
Q

What opioid antagonist can be used for opiate addiction?

A

naloxone

96
Q
  1. Only partial opioid agonist with out dysphoria/ kappa agonism?
  2. Which ones do have Kappa affects?
A
  1. buprenorphine (use with naloxone)

2. nalbuphine, pentazocine, butorphanol, morphine (full agonist)

Neuro 1 (10 decks)

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