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Pharm Flashcards

1
Q

easily pass through BBB

A

H20
gases (CO2, O2)
lipophilic/nonionized things

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2
Q

Duration of effect of lipophilic drug

A

crosses BBB easily, so in and out fast (short duration)

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3
Q

Elimination of lipophilic drug

A

goes to adipose tissue and stays there a while, so long elimination

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4
Q

P-gp transporter

A

= ABCB1 apical transporter

- antidepressants are a substrate

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5
Q

Depression and p-gp

A
  • stress makes it harder for corticosteroids to exhibit negative fb by getting through BBB because depression limits p-gp activity
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6
Q

Excitatory NTs

A

glutamate
aspartate
(acidic AA’s)

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7
Q

Inhibitory NTs

A

GABA
glycine
B alanine
taurine

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8
Q

Where are NEs highest in concentration?

A

Hypothalamus
Amygdala
Dentate Gyrus of Hippocampus
Locus Ceruleus of Pons

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9
Q

Adrenergic pathways are important in…

A

sleep and arousal regulation

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10
Q

PTSD may be due to

A

Beta activation in amygdala

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11
Q

What pathways are involved in wakefulness?

A

Ach and NE

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12
Q

What is special about antipsychotics?

A

They don’t possess uniform receptor activation. Can have SE’s by modulating adrenergic, cholinergic, histaminergic, serotinergic receptors

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13
Q

Antidepressants MOA

A

typically block reuptake of 5HT, NE, or Dopamine

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14
Q

What’s special about the amygdala?

A

every NT acts here

high alpha1, beta1

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15
Q

Tx for intrusion component of PTSD

A

Beta blockers

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16
Q

Tx for hyperarousal component of PTSD

A

alpha blockers

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17
Q

L-DOPA/Levodopa

A
  • for Parkinson’s
  • replenishes DA stores in SNc
  • orally, but inhibited by food
  • converted in periphery and brain to DOPA by L-AAD (so given with Carbidopa to inhibit peripheral conversion, b/c that Dopa can’t cross BBB)
  • AE alone: GI, CV (arrythmia’s, Orthosthypoten)
  • AE with Carbidopa: behavioral (give antipsychotics) dyskinesias (hyper)
  • single most effective treatment, BUT don’t use early b/c on-off phenom and gets exhausted in 3-5 yrs
  • contra: psychotic, glaucoma, CV, PUD, melanoma, DDI with VitB6
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18
Q

General tx strategies for Parkinson’s

A
  • replace Dopa
  • stimulate D2 receptor with Dopa agonist
  • inc. Dopa release
  • inhibit Dopa metab
  • alter DA/ACh balance
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19
Q

Apomorphine

A
  • Dopa agonist for Parkinson’s
  • good initial therapy
  • nonselective
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20
Q

Bromocriptine

A
  • Dopa agonist for Parkinson’s
  • good initial therapy
  • D2/D1 selectivity
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21
Q

Pramipexole

A
  • Dopa agonist for Parkinson’s
  • good initial therapy
  • D2 selective
  • free radical scavenger
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22
Q

Ropinirole

A
  • Dopa agonist for Parkinson’s
  • good initial therapy
  • D2 selective, CYP1A2 metab
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23
Q

Amantadine

A
  • for Parkinson’s
  • antiviral that inc. Dopa release
  • MOA unknown
  • AE: psychotic, psychosis with OD
  • contra: seizures and CHF
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24
Q

Selegiline

A
  • MAO-B inhibitor for Parkinson’s
  • very potent inhibitor of Dopa metab
  • used when L-dopa starts to be less effective
  • metabolized into amphetamine/methamphetamine
  • DDI with Meperidine, TCAs, SSRIs
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25
Q

Rasagiline

A
  • MAO-B inhibitor for Parkinson’s
  • very potent inhibitor of Dopa metal
  • used when L-dopa starts to be less effective
  • metabolized into amphetamine/methamphetamine
  • DDI with Meperidine, TCAs, SSRIs
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26
Q

Entacapone

A
  • DA metab inhibitor for Parkinson’s
  • COMT inhibitor that prolongs action of L-Dopa, inc its bioavailability, reduces ON/OFF
  • no AEs since it only inhibits COMT peripherally
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27
Q

Tolcapone

A
  • DA Metab inhibitor for Parkinson’s
  • COMT inhibitor that prolongs action of L-Dopa, inc its bioavailability, reduces ON/OFF
  • AE: Hepatic failure (pt has to sign a consent!!!)
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28
Q

Benztropine

A
  • alters DA/ACh balance for Parkinson’s tx
  • since ACh opposes DA action in striatum
  • it’s actually an anticholinergic
  • used BEFORE L-Dopa
  • CNS AE: sedation, confusion, hallucination, mood change
  • PNS AE: opposite of SLUDGEBBB
  • contra: BPH, OBD, glaucoma
  • DDI: anti H1’s, TCAs
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29
Q

Diphenhydramine

A
  • alters DA/ACh balance for Parkinson’s tx
  • since ACh opposes DA action in striatum
  • it’s actually an anticholinergic
  • used BEFORE L-Dopa
  • CNS AE: sedation, confusion, hallucination, mood change
  • PNS AE: opposite of SLUDGEBBB
  • contra: BPH, OBD, glaucoma
  • DDI: anti H1’s, TCAs
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30
Q

Trihexyphenidyl

A
  • alters DA/ACh balance for Parkinson’s tx
  • since ACh opposes DA action in striatum
  • it’s actually an anticholinergic
  • used BEFORE L-Dopa
  • CNS AE: sedation, confusion, hallucination, mood change
  • PNS AE: opposite of SLUDGEBBB
  • contra: BPH, OBD, glaucoma
  • DDI: anti H1’s, TCAs
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31
Q

Isradipine

A
  • future target for Parkinson’s tx
  • blocks L-type Ca channels in SNc, reverts pacemaking to HCN1 and Na channels (like juvenile neurons)
  • may prevent progression
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32
Q

Fluoxetine

A
  • for Huntington’s
  • sympomatic tx only
  • an SSRI for tx of depression sx
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33
Q

Carbamezapine

A
  • for Huntington’s
  • symptomatic tx only
  • a voltage gated Na channel blocker for treatment of depression
34
Q

Reserpine

A
  • for Huntington’s
  • symptomatic tx only
  • for Chorea
  • VMAT inhibitor that causes depletion of DA
35
Q

Tetrabenazine

A
  • for Huntington’s
  • symptomatic tx only
  • for Chorea
  • VMAT inhibitor that causes depletion of DA
36
Q

Chlorpromazine

A
  • for Huntington’s
  • symptomatic tx only
  • D2 antagonist for tx of chorea sx
  • can cause increase in indirect pathway (Parkinson’s)
37
Q

Haloperidol

A
  • for Huntington’s
  • symptomatic tx only
  • D2 antagonist for tx of chorea sx
  • can cause an increase in indirect pathway (Parkinson’s)
38
Q

Ketamine

A
  • analgesic
  • NMDA receptor blocker that prevents surgery induced wind up
  • SE: hallucinations, amnesia, HTN, inc. ICP
39
Q

Dextromethorphan

A
  • analgesic used as a cough suppressant
  • NMDA receptor blocker that prevents surgery induced wind up
  • SE: dizziness, confusion, fatigue
40
Q

Carbamezapine

A
  • voltage gated Na channel blocker used to treat neuropathic pain
41
Q

Naloxone

A
  • opiate antag
  • cause withdrawal sx, but used to antagonize opiate AE’s
  • t1/2 30 min
  • parenteral only
42
Q

Naltrexone

A
  • opiate antag
  • cause withdrawal sx, but used to antagonize opiate AE’s
  • 4hr t1/2, also IM
  • used for addiction programs
  • tightly binds and slowly releases from receptors
  • used for alcohol cravings (dec. beta endorphin release)
43
Q

Nalmefine

A
  • opiate antag
  • cause withdrawal sx, but used to antagonize opiate AE’s
  • 11 hr t1/2
  • parenteral only
44
Q

mu

A
  • aka OP3 receptor
  • endorphins
  • cortical and spinal analgesia, sedation, dec respiration, dec GI transit, altered hormone and NT release
45
Q

delta

A
  • aka OP1 receptor
  • enkephalins
  • cortical and spinal analgesia, altered hormone and NT release
46
Q

kappa

A
  • aka OP2 receptor
  • dynorphins
  • cortical and spinal analgesia, psychomimetic, GI transit
47
Q

most well absorbed mechanism of opiate delivery

A

SC/IM

48
Q

Distribution of opiate drugs

A

distributes to organs with highest blood flow first: aka muscle (when it gets to adipose, it stays there a while)

49
Q

AE’s of opiate drugs

A
  • restlessness/ hyperactivity/convulsions
  • respiratory depression
  • N/V
  • inc ICP
  • OHTN
  • constip, urin ret
  • pruritis, urticaria, bradycardia, mitosis
50
Q

which opiates cause histamine release? don’t?

A

morphine does

fentanyl doesn’t

51
Q

Opiate OD triad*****

A 
Coma (from dec. cortical stimulation)
Respiratory Acidosis (dec. resp drive)
Pinpoint pupils (modulation at Edinger Westphal nucleus)
52
Q

Opiate drug interactions

A

sedatives
antipsychotics
MAOIs

53
Q

what do you have to worry about with codeine?

A

variability in CYPs

it crosses breast milk

54
Q

which opiates are not contraindicated with renal failure?

A

hydromorphine

fentanyl

55
Q

morphine

A

mu > kappa

low oral bioavailability

56
Q

hydromorphone

A

mu
low oral availability
ok for renal failure

57
Q

methadone

A 
mu
high oral availability
t1/2 120 hours
used to manage opiate withdrawal
used for pregnant addicts
cause cause dec libido and QT arrhythmias
58
Q

meperidine

A

mu
medium oral availability
1 metabolite is CNS toxic
also anticholinergic

59
Q

fentanyl

A 
mu
low oral availability
transdermal patch, lozenge 
heat makes patch drug depot faster
suicidal ideation
ok for renal failure
60
Q

remifentanil

A

mu

IV only

61
Q

codeine

A

mu
high oral availability
converted to morphine by CYP2D6

62
Q

hydrocodone

A

mu

medium oral availability

63
Q

oxycodone

A

mu

medium oral availability

64
Q

pentazocine

A

mu, kappa

medium oral availabilty

65
Q

nalbuphine

A

partial mu, kappa

IV only

66
Q

buprenorphine

A

mu, partial delta, partial kappa
made with naloxone so it can’t be crushed and injected
used for dependence programs
low oral bioavailabilty
strong binding at receptor, low risk of OD

67
Q

butorphanol

A

mu, kappa

IV only

68
Q

tramadol

A

opiate

69
Q

propoxyphene

A

old opiate that was withdrawal b/c of long QT arrhythmias

70
Q

treatment for opiate withdrawl

A

inpatient: methadone
outpatient: clonidine

71
Q

Why are opiate associated with addiction?

A

Addiction is associated with inc DA.

Opiates disinhibit DA signaling, so inhibit GABA from blocking DA.

72
Q

dependence vs addiction

A

dependence requires chronic use (it is physical) and addiction does not (it is psychological)

73
Q

morphine: codeine > 2:1

A

pt is taking heroine

74
Q

morphine: codeine <2:1

A

pt is taking codeine

75
Q

toxic screen morphine:codeine significance

A
  • synthetic opiates are negative

- fluoroqinolones can be false positive

76
Q

Loperamide

A
  • opiate for nonanalgesia
  • for diarrhea, dec GI transit
  • OTC
  • doesn’t cross BBB
77
Q

Diphenoxylate

A
  • opiate for nonanalgesia
  • formulated with atropine to dec abuse
  • for diarrhea, dec GI transit
78
Q

Gabapentin and Pregalabin

A
  • non narcotic pain drug
  • blocks alpha2delta subunit of Ca channel
  • inhibits neuronal hyperexcitability
  • doesn’t affect GABA
79
Q

Lamotrigine and Carbamezapine

A
  • non narcotic pain drug
  • voltage gated Na channel blocker
  • dec neuronal conduction
  • dose adjust in hepatic failure
  • BBW: SJS, vision, carbamez causes agranulocytosis
80
Q

TCAs

A
  • non narcotic pain med
  • NE and 5HT reuptake inhibitor useful for pain (ascending MAO in pain)
  • CYP2D6 metab
  • AE: drowsy, fatigue, memory impairment

Neuro (5 decks)

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