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SFM6 > Neuropharmacology > Flashcards

Neuropharmacology Flashcards

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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
selegiline
irreversible MAO-B inhibitor | PD
26
rasagiline
irreversible MAO-B inhibitor | PD
27
safinamide
reversible selective MAO=B inhibitor inhibits glutamate release helps with levodopa "off" episodes
28
muscarinic receptor antagonists in PD
e. g. - trihexyphenidyl - benzotropine mainly tx tremor weak efficacy limited clinical utility in PD: - dopamine deficit --> excessive ACh activity
29
istradefylline
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)
30
entacapone
peripheral COMT inhibitor | increases L-DOPA bioavailability for given dose
31
Sinemet
levodopa/carbidopa combo drug
32
opicapone
peripheral COMT inhibitor increases L-DOPA bioavailability >entacapone once-daily PD - add on to levodopa/carb especially if +motor fluctuations
33
tolcapone
peripheral and CNS COMT inhibitor | hepatotoxicity concerns
34
mainline PD tx
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
second line / adjuvant PD tx
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
when to initiate PD therapy
when sx interfere w/ fx or qol | tx is for sx only - no advantage to starting early, and increases sfx burden
37
drug-induced parkinsonism
d/t: - antipsychotics - D2 antagonists - reserpine - depletes NE/5-HT/DA reversible, but may require weeks to months after stopping med
38
PET in PD
generally reserved for research or atypical cases F-DOPA tracer shows reduced DA uptake in putamen>caudate typically progresses from unilateral to bilateral
39
benzodiazapines mx
allosteric GABA-A-R binding enhances GABA fx (inhibitory) increase efficiency of GABA-ergic synaptic transmission membrane hyperpolarization --> decrease firing rate of neurons
40
benzos pharmacodynamics
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
ASM
anti-seizure med preferred term (now) more appropriate term than AED/antiepileptic, as drugs target seizures, not underlying causes of epilepsy
42
when to initiate/dc ASMs
initiate after 2nd seizure or 1st if EEG/MRI/CT abnormal withdraw if seizure free >2 years and low risk
43
drug resistant epilepsy
early in tx failure of 2 drugs | <5% b//c seizure free
44
ASM CYP P450 inhibitor
valproic acid - 2C
45
ASM CYP P450 inducers
carbamazepine - 3A4 and 2C phenobarbital - 3A4 and 2C phenytoin - 3A4 and 2C
46
sodium channel blockers
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
GABA/chloride channel agonists
benzos - rapid onset; first-line for status epilepticus valproate phenobarbital - very high pregnancy risk; 80h t1/2, outdated but common in developing countries
48
first line for status epilepticus
benzos usually lorazepam d/t short on-slow off effective ~1-3 min, 22h t1/2
49
topiramate
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
gabapentin
action similar to GABA but mx unrelated binds voltage-gated Ca++ channels inhibit release of excitatory neurotransmitters adjuvant for focal seizures
51
levetiracetam
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
lacosamide
focal onset and primary generalized seizures enhanced slow inactivation of voltage gated Na channels t1/2 13h preg risk low rsh risk
53
parampanel
broad spectrum ASM selective non-competitive AMPA-R (glutamate) blocker t1/2 105h preg risk
54
clobazam
adjuvant for LGS GABA-A agonist t1/2 36-42 h preg risk low rash risk
55
absence-only seizure tx
ethosuximide - t-type Ca++ channel blocker in thalamus; low potency but works well for absence seizures (not other types) (or) valproic acid
56
CBD sz
both CBD and THC show anticonvulsant properties, CBD (–) psychotropic fx multiple targets add on to clobazam in LGS
57
GCSE tx
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
focal onset epilepsy | first line
levitiracetam lamotrigine carbamazepine
59
primary generalized tonic clonic epilepsy | first line
levetiracetam lamotrigine valproic acid
60
absence only epilepsy | first line
ethosuximide | valproic acid
61
LGS | first line
valproic acid levetiracetam clobazam more likely to need 2+ to achieve control
62
lamotrigine
voltage gated Na+ blocker rash risk low preg risk first line for focal onset and primary generalized tonic clonic
63
nitrous oxide
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
MAC
minimum alveolar concentration | "dosage" of inhaled anesthetic
65
sevoflurane
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
desflurane
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
isoflurane
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
propofol
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
ketamine
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
etomidate
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
dexmedtomidine
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
succinylcholine
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
short acting NDMB
non-depolarizing muscle blocker mivacurium 12-20 min - pseudocholinesterase metabolism - not available in US
74
intermediate acting NDMB
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
long acting NDMB
pancuronium 60-90 min - renal excretion - may increase hr by vagal antagonism
76
NDMB c/i
anaphylaxis risk | - c/i in asthma, sepsis, other susceptible pts
77
NDMB reversal
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
atropine
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
glycopyrrolate
``` anticholinergic reversal of anesthesia intermediate onset, longer duration does not cross BBB may also be used to t x bradycardia ```
80
organophosphates
irreversible ACh-ase-I in ophthalmology: - miosis (pupillary constriction) - reduce IOP
81
pralidoxime
definitive tx for organophosphate poisoning | give ASAP b/f irreversible conjugate forms

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