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SFM6 > Neuropharmacology > Flashcards

Neuropharmacology Flashcards

1
Q

diazepam

A

CNS spasmolytic
benzodiazepine
GABA-A-R allosteric AGonist

mx:

  • postsynaptic inhibitory effect
  • facilitates GABA binding/potentiates inhibitory actions
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2
Q

baclofen

A

CNS spasmolytic
GABA-B-R AGonist

mx:

  • pre and post synaptic inhibitory effect
  • direct potentiation of inhibitory actions of GABA-R
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3
Q

gabapentin

A

CNS spasmolytic
antiepileptic
GABA mimic

mx:

  • does NOT bind to GABA-R
  • mimics GABA actions
  • blocks voltage-sensitive Ca++ channels on presynaptic terminal

pk:

  • not metabolized
  • excreted in urine
  • no significant interactions
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4
Q

tizanidine

A

CNS spasmolytic
alpha-2 adrenergic R AGonist

mx:

  • presynaptic inhibitory effect
  • centrally acting

uses:

  • spasm
  • cramping
  • muscle tightness d/t MS
  • back pain
  • spinal injury
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5
Q

BoNT

A

PNS spasmolytic

mx:
- inhibits ACh release from presynaptic terminal

uses:

  • dystonia
  • strabismus
  • torticollis
  • generalized spastic disorders
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6
Q

dantrolene

A

PNS spasmolytic

mx:
- inhibits Ca++ release from SR

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7
Q

mx drug entry to brain

A

diffusion

  • free drug
  • lipid soluble
  • small molecule
  • YES: cortisol, dexamethosone, some statins
  • NO: cholesterol

diffusion w/ ion trapping

  • nonionized form of weak acids or bases crosses in
  • becomes ionized and can’t get out

facilitated transport

  • amino acid tansporters
  • Glut-1 transporter
  • vitamin transporters at choroid plexus

receptor mediated endocytosis
- transferrin (iron) insulin, leptin, peptides

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8
Q

P-gp efflux pump

A

P-glycoprotein
ATP-dependent

limits xenobiotics to brain

  • analgesics
  • antiepileptics
  • antidepressants
  • anti-HIV
  • anti-microbials
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9
Q

ceftriaxone

A

uses:

  • Neisseria meningitidis
  • most pneumococcus

mx:

  • 3rd gen ceph
  • direct TPA binding

dose:
- higher for CNS infections

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10
Q

vancomycin

A

uses:
- strep pneumonia (incl. meningitis)

mx:
- inhibition of peptidoglycan synthesis by binding peptide chain

dose:
- higher for CNS infections

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11
Q

ampicillin

A

uses:

  • listeria monocytogenes
  • part of empiric abx cocktail for meningitis in:
    • pregnant
    • neonates
    • i.c.

dose:
- higher for CNS infections

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12
Q

dexamethasone

A

uses (among others…)

  • part of empiric abx cocktail for meningitis
  • (when gram stain back) only continue if strep pneumoniae

rationale:

  • massive inflammatory response from abx killing bacteria can worsen CNS damage and possibly sepsis
  • only beneficial for strep pneumoniae (based on empiric data) but not harmful in other meningitises
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13
Q

ischemic stroke tx

A

IV thrombolytics:

  • alteplase (1st gen)
  • tenecteplase

+endovascular thrombectomy

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14
Q

hemorrhagic stroke tx

A
  • reversal agents for blood thinners
  • aggressive bp management
  • clotting factors
  • blood
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15
Q

levodopa

A

L-DOPA
DA precursor
effective for PD tx
but large doses required –> sfx and AEs w/ extended use

sfx/AEs:
early:
- n+v
- depression
- pychosis
- orthostatic hypOtension
late:
- fluctuating motor responses d/t end-of-dose periods
- on/off periods - sudden loss of sx control despite L-DOPA levels
* dyskinesias (after several years)
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16
Q

carbadopa

A

dopa decarboxylase inhibitor
administered w/ levodopa in PD to prevent side effects from peripheral conversion of levodopa to epinephrine
does not cross BBB

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17
Q

levodopa dyskinesias

A

50-90% of pts w/ long-term use (~60% 10 yr)
involuntary movements
- coreiform (dance-like)
- maybe: dystonia, myoclonus
- any part of body
- potential for respiratory muscle involvement

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18
Q

dopamine receptor agonists

A

directly activate post-synaptic DA receptors
tx PD

e. g.
- ropinirole
- pramipexole
- rotigotine

sfx/AEs

  • n+v
  • orthostatic hypOtension
  • dose-related psych fx e.g.
  • daytime sleepiness
  • impulse control disorder
  • mood instability/changes
  • vivid dreams
  • narcolepsy-like sleep attacks
  • less dyskinesia vs L-DOPA
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19
Q

ropinirole

A

dopamine receptor agonist
D2/D3
t1/2 ~6h

PD

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20
Q

pramipexole

A

dopamine receptor agonist
D2/D3
t1/2 8-12h

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21
Q

rotigotine

A

dopamine receptor agonist
non-selective
once-daily transdermal patch

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22
Q

apomorphine

A

short-acting non-ergot dopamine agonist
D1/D2
t1/2 ~40 min

“rescue” med/fast onset
- acute tx of hypOmobility, end-of-dose fx, on-off episodes

sfx:

  • n+v
  • orthostatic hypOtension
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23
Q

amantadine

A

DA releaser
- amphetamine like
DA reuptake inhibitor
NMDA receptor ANTagonist

uses

  • monotherapy in early PD
  • L-DOPA induced dyskinesias

not metabolized
safe in liver disease

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24
Q

MAO-B inhibitors

A

inhibit DA metabolism
PD

e. g.
- selegiline
- rasagiline
- safinamide

serious drug interactions (d/t also inhibiting NE, 5-HT metabolism)

  • SSRIs
  • TCAs
  • tyramine containing foods
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25
Q

selegiline

A

irreversible MAO-B inhibitor

PD

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26
Q

rasagiline

A

irreversible MAO-B inhibitor

PD

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27
Q

safinamide

A

reversible selective MAO=B inhibitor
inhibits glutamate release
helps with levodopa “off” episodes

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28
Q

muscarinic receptor antagonists in PD

A

e. g.
- trihexyphenidyl
- benzotropine

mainly tx tremor
weak efficacy
limited clinical utility

in PD:
- dopamine deficit –> excessive ACh activity

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29
Q

istradefylline

A

use:
- PD add-on (to levodopa/carb)

mx:

  • adenosine A2A receptor antagonist
  • A2A colocalize w/ D2 receptors, decreases D2 receptor affinity for DA
  • inhibitor –> increase D2 receptor activation (inhibitory dopamine receptor)
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30
Q

entacapone

A

peripheral COMT inhibitor

increases L-DOPA bioavailability for given dose

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31
Q

Sinemet

A

levodopa/carbidopa combo drug

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32
Q

opicapone

A

peripheral COMT inhibitor
increases L-DOPA bioavailability
>entacapone
once-daily

PD - add on to levodopa/carb especially if +motor fluctuations

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33
Q

tolcapone

A

peripheral and CNS COMT inhibitor

hepatotoxicity concerns

34
Q

mainline PD tx

A

1+ of (generally tried in this order):

L-DOPA + carbidopa (sinemet)
- most effective, but concern for long-term use

DA D2/3 receptor agonists e.g.:

  • ropinirole
  • pramipexole

MAO-B inhibitors e.g.:

  • rasagiline
  • selegiline
  • safinamide

individualize to pt needs
lowest dose singly or in combo for pt’s needs

35
Q

second line / adjuvant PD tx

A

anticholinergics for tremor e.g.

  • benztropine
  • trihexyphenidyl

DA releaser/reuptake inhibitor
- amantadine

COMT inhibitors e.g.

  • entacapone
  • opicapone
  • tolcapone

adenosine A2A receptor antagonist
- istradefylline

36
Q

when to initiate PD therapy

A

when sx interfere w/ fx or qol

tx is for sx only - no advantage to starting early, and increases sfx burden

37
Q

drug-induced parkinsonism

A

d/t:

  • antipsychotics - D2 antagonists
  • reserpine - depletes NE/5-HT/DA

reversible, but may require weeks to months after stopping med

38
Q

PET in PD

A

generally reserved for research or atypical cases

F-DOPA tracer
shows reduced DA uptake in putamen>caudate
typically progresses from unilateral to bilateral

39
Q

benzodiazapines mx

A

allosteric GABA-A-R binding
enhances GABA fx (inhibitory)
increase efficiency of GABA-ergic synaptic transmission
membrane hyperpolarization –> decrease firing rate of neurons

40
Q

benzos pharmacodynamics

A

well absorbed po
throughout body - very lipid soluble
primary hepatic clearance phase I and II

oxidation –> active metabolites in some cases

  • longer effected t1/2
  • drug accumulation w/ repeated administration
  • diazepam, chlordiazepoxide, clonazepam (valium, librium, klonapin)

oxazepam and lorazepam (serax, Ativan)

  • no active metabolites
  • minor accumulation
41
Q

ASM

A

anti-seizure med
preferred term (now)
more appropriate term than AED/antiepileptic, as drugs target seizures, not underlying causes of epilepsy

42
Q

when to initiate/dc ASMs

A

initiate after 2nd seizure
or 1st if EEG/MRI/CT abnormal
withdraw if seizure free >2 years and low risk

43
Q

drug resistant epilepsy

A

early in tx failure of 2 drugs

<5% b//c seizure free

44
Q

ASM CYP P450 inhibitor

A

valproic acid - 2C

45
Q

ASM CYP P450 inducers

A

carbamazepine - 3A4 and 2C
phenobarbital - 3A4 and 2C
phenytoin - 3A4 and 2C

46
Q

sodium channel blockers

A

first line ASMs

e. g.:
- lamotrigine - fewest sfx/AEs/fetus risk (t1/2 22h)
- carbamazepine - short-ish t1/2 (8h)
- phenytoin (t1/2 22h)

47
Q

GABA/chloride channel agonists

A

benzos - rapid onset; first-line for status epilepticus
valproate
phenobarbital - very high pregnancy risk; 80h t1/2, outdated but common in developing countries

48
Q

first line for status epilepticus

A

benzos
usually lorazepam d/t short on-slow off
effective ~1-3 min, 22h t1/2

49
Q

topiramate

A

broad spectrum ASM
useful for migraine prevention
t1/2 21 h

multiple mx

  • sodium channel
  • glutamate R
  • GABA-R

high preg risk
low rash risk
mixed hepatic and urinary

50
Q

gabapentin

A

action similar to GABA but mx unrelated
binds voltage-gated Ca++ channels
inhibit release of excitatory neurotransmitters

adjuvant for focal seizures

51
Q

levetiracetam

A

first-line ASM for all seizure types
SV2A inhibitor - synaptic vesicle protein - inhibition –> no pool of nt-containing vesicles
reduces excitatory nt release

renal clearance
low preg risk
low rash risk

sfx:
fatigue
irritability
HA
insomnia
52
Q

lacosamide

A

focal onset and primary generalized seizures
enhanced slow inactivation of voltage gated Na channels

t1/2 13h
preg risk
low rsh risk

53
Q

parampanel

A

broad spectrum ASM
selective non-competitive AMPA-R (glutamate) blocker

t1/2 105h
preg risk

54
Q

clobazam

A

adjuvant for LGS
GABA-A agonist

t1/2 36-42 h
preg risk
low rash risk

55
Q

absence-only seizure tx

A

ethosuximide
- t-type Ca++ channel blocker in thalamus; low potency but works well for absence seizures (not other types)
(or)
valproic acid

56
Q

CBD sz

A

both CBD and THC show anticonvulsant properties, CBD (–) psychotropic fx
multiple targets

add on to clobazam in LGS

57
Q

GCSE tx

A

generalized convulsive status epilepticus

first line tx:
IV lorazepam

if persistent
barbiturate (fosphenytoin, VPA, or phenobarbital)

refractory
midazolam or propofol

super refractory >24 h
high morbidity
tx pentobarbital coma (medically-induced coma)

58
Q

focal onset epilepsy

first line

A

levitiracetam
lamotrigine
carbamazepine

59
Q

primary generalized tonic clonic epilepsy

first line

A

levetiracetam
lamotrigine
valproic acid

60
Q

absence only epilepsy

first line

A

ethosuximide

valproic acid

61
Q

LGS

first line

A

valproic acid
levetiracetam
clobazam

more likely to need 2+ to achieve control

62
Q

lamotrigine

A

voltage gated Na+ blocker
rash risk
low preg risk
first line for focal onset and primary generalized tonic clonic

63
Q

nitrous oxide

A

inhibition at NMDA-R
blockade of glutamate release

non-volatile
inhalational
generalized anesthetic

fx:

  • amnesia (explicit emory)
  • deep sedation / unconsciousness
  • immobility to pain
  • autonomic reflex blunting and depression
    i. e. near “complete” anesthetic fx
respiratory volume --
rr --
minute vent --
apnea threshold increase
bronchodilator
airway irritability --
bp down
CV fx down
SVR up
HR down/neutral
coronary vasodilation --
no uterine relaxation (can be used for labor pain)

environmental: ozone depletion
114 yr atmospheric lifetime

64
Q

MAC

A

minimum alveolar concentration

“dosage” of inhaled anesthetic

65
Q

sevoflurane

A

inhalational generalized anesthetic

decrease respiratory volume
increased rr
decreased minute vent
increased apnea threshold
bronchodilator
airway irritability --
bp down
CV fx down
SVR down
HR --
coronary vasodilation
uterine relaxation - caution in c-section
66
Q

desflurane

A

inhalational generalized anesthetic

decrease respiratory volume
increased rr
decreased minute vent
increased apnea threshold
bronchodilator
very increased airway irritability
bp down
CV fx down
SVR down
HR up or --
coronary vasodilation
uterine relaxation - caution in c-section

environmental: ozone depletion
- 1 h at 1 MAC ~ carbon footprint of 200-400 mi in avg car

67
Q

isoflurane

A

inhalational generalized anesthetic

decreased respiratory volume
rr --
very decreased minute ventilation
increased apneic threshold
bronchodilation
airway irritability
bp down
CV fx down
SVR down
HR up
coronary vasodilation
uterine relaxation - caution in c-section
68
Q

propofol

A

IV anesthetic
induction and maintenance
most frequent

use:

  • short cases
  • outpt
  • neurosurg
  • optho
  • other cases, as long as normal myocardial fx

fx:

  • no analgesia
  • hypnosis (GABA-A mediated)
  • sedation
  • anti-emetic
  • dopaminergic - nucleus accumbens (abuse potential, euphoria)
  • decreases CBF in elevated ICP
  • respiratory depression
  • inhibits hypercapneic respiratory drive
  • low incidence of anaphylaxis
  • decreased bp, co, svr, rr; ?hr

sfx:

  • injection site pain
  • sepsis/infections
  • liver metabolism
69
Q

ketamine

A

IV or IM anesthetic
phencyclidine/PCP
glutamic acid inhibitor at NMDA-R

uses:

  • trauma + hypOvolemia/shock
  • peds, esp CV repair
  • asthmatics
  • adjuvant for chronic pain, others at sub anesthetic doses

fx:

  • analgesia
  • no injection site pain
  • sedation
  • dissociation
  • increased CBF and ICP
  • increased bp, hr, co, sir
  • rr –, bronchoconstriction

sfx:

  • psych rxn on awakening:
  • vivid dreams
  • extracorporeal experiences
  • illusions
  • excitement, confusion, euphoria and/or fear
  • possible benzo attenuation
70
Q

etomidate

A

IV anesthetic
GABA-A mediated

uses:

  • CV surg
  • any case involving compromised CV fx
  • neurosurg (second choice to propofol)

fx:

  • hypnosis / sedation
  • no analgesia
  • burst suppression on EEG / barbiturate-like effect
  • decreased CBF and ICP
  • neutral bp, hr, co, svr, rr

sfx:

  • increases EEG activity in epileptogenic foci
  • transient decrease in cortisol
  • injection site pain
  • n+v
  • myoclonus
  • hiccups
71
Q

dexmedtomidine

A

selective alpha-2 receptor agonist
IV anesthetic

uses:

  • intubated pts in ICU
  • pts w/ ventilation issues requiring sedation

fx:

  • sleep like hypnosis
  • no reliable amnesia
  • minimal respiratory fx
  • decreased hr, co, bp
72
Q

succinylcholine

A

depolarizing NMB
structurally similar to ACh
binds alpha subunit of Nic-R
continuous Na+ opening –> persistent depolarization / fasciculations –» flaccid paralysis

use:

  • rapid / brief paralysis
  • intubation
  • very short procedures e.g. laryngoscopy, biopsy

fx returns after 5-10 min
metabolism by plasma pseudocholinesterase

sfx:

  • myalgias
  • increased ICP, IOP, intragastric pressure
  • prolonged paralysis if atypical pseudocholinesterase
  • hypER-K esp if recent burns, certain neurologic/muscular disorders, renal failure
  • malignant hyperthermia in susceptible pts
73
Q

short acting NDMB

A

non-depolarizing muscle blocker

mivacurium 12-20 min

  • pseudocholinesterase metabolism
  • not available in US
74
Q

intermediate acting NDMB

A

rocuronium 35-75 min

  • appropriate for rapid intubation
  • most commonly used NDMB

atracurium/cisatracurium 40-75 min
- common in liver/kidney disease

vecuronium 45-90 min

75
Q

long acting NDMB

A

pancuronium 60-90 min

  • renal excretion
  • may increase hr by vagal antagonism
76
Q

NDMB c/i

A

anaphylaxis risk

- c/i in asthma, sepsis, other susceptible pts

77
Q

NDMB reversal

A

ACh-ase-I + antimuscarininc

  • usually neostigmine + glycopyrrolate (sometimes atropine)
  • antimuscarinic counteracts parasympathetic cholinergic sx
  • possible cholinergic crisis / SLUDGE

sugammedex

  • bind NDMB
  • works best w/ rocuronium
  • does not work w/ benzylisoquinolines i.e. cisatracurium
78
Q

atropine

A

anticholinergic
reversal of anesthesia
tx organophosphate poisoning (acute; definitive is pralidoxime)
anti-SLUDGE
fast onset, short duration
crosses bbb
also used to tx bradycardia (ACLS algorithm)

79
Q

glycopyrrolate

A 
anticholinergic
reversal of anesthesia
intermediate onset, longer duration
does not cross BBB
may also be used to t x bradycardia
80
Q

organophosphates

A

irreversible ACh-ase-I

in ophthalmology:

  • miosis (pupillary constriction)
  • reduce IOP
81
Q

pralidoxime

A

definitive tx for organophosphate poisoning

give ASAP b/f irreversible conjugate forms

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