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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
Rasagiline
- 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
26
Entacapone
- 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
27
Tolcapone
- 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!!!)
28
Benztropine
- 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
29
Diphenhydramine
- 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
30
Trihexyphenidyl
- 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
31
Isradipine
- 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
32
Fluoxetine
- for Huntington's - sympomatic tx only - an SSRI for tx of depression sx
33
Carbamezapine
- for Huntington's - symptomatic tx only - a voltage gated Na channel blocker for treatment of depression
34
Reserpine
- for Huntington's - symptomatic tx only - for Chorea - VMAT inhibitor that causes depletion of DA
35
Tetrabenazine
- for Huntington's - symptomatic tx only - for Chorea - VMAT inhibitor that causes depletion of DA
36
Chlorpromazine
- for Huntington's - symptomatic tx only - D2 antagonist for tx of chorea sx - can cause increase in indirect pathway (Parkinson's)
37
Haloperidol
- for Huntington's - symptomatic tx only - D2 antagonist for tx of chorea sx - can cause an increase in indirect pathway (Parkinson's)
38
Ketamine
- analgesic - NMDA receptor blocker that prevents surgery induced wind up - SE: hallucinations, amnesia, HTN, inc. ICP
39
Dextromethorphan
- analgesic used as a cough suppressant - NMDA receptor blocker that prevents surgery induced wind up - SE: dizziness, confusion, fatigue
40
Carbamezapine
- voltage gated Na channel blocker used to treat neuropathic pain
41
Naloxone
- opiate antag - cause withdrawal sx, but used to antagonize opiate AE's - t1/2 30 min - parenteral only
42
Naltrexone
- 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
Nalmefine
- opiate antag - cause withdrawal sx, but used to antagonize opiate AE's - 11 hr t1/2 - parenteral only
44
mu
- aka OP3 receptor - endorphins - cortical and spinal analgesia, sedation, dec respiration, dec GI transit, altered hormone and NT release
45
delta
- aka OP1 receptor - enkephalins - cortical and spinal analgesia, altered hormone and NT release
46
kappa
- aka OP2 receptor - dynorphins - cortical and spinal analgesia, psychomimetic, GI transit
47
most well absorbed mechanism of opiate delivery
SC/IM
48
Distribution of opiate drugs
distributes to organs with highest blood flow first: aka muscle (when it gets to adipose, it stays there a while)
49
AE's of opiate drugs
- restlessness/ hyperactivity/convulsions - respiratory depression - N/V - inc ICP - OHTN - constip, urin ret - pruritis, urticaria, bradycardia, mitosis
50
which opiates cause histamine release? don't?
morphine does | fentanyl doesn't
51
Opiate OD triad*****
``` Coma (from dec. cortical stimulation) Respiratory Acidosis (dec. resp drive) Pinpoint pupils (modulation at Edinger Westphal nucleus) ```
52
Opiate drug interactions
sedatives antipsychotics MAOIs
53
what do you have to worry about with codeine?
variability in CYPs | it crosses breast milk
54
which opiates are not contraindicated with renal failure?
hydromorphine | fentanyl
55
morphine
mu > kappa | low oral bioavailability
56
hydromorphone
mu low oral availability ok for renal failure
57
methadone
``` 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
meperidine
mu medium oral availability 1 metabolite is CNS toxic also anticholinergic
59
fentanyl
``` mu low oral availability transdermal patch, lozenge heat makes patch drug depot faster suicidal ideation ok for renal failure ```
60
remifentanil
mu | IV only
61
codeine
mu high oral availability converted to morphine by CYP2D6
62
hydrocodone
mu | medium oral availability
63
oxycodone
mu | medium oral availability
64
pentazocine
mu, kappa | medium oral availabilty
65
nalbuphine
partial mu, kappa | IV only
66
buprenorphine
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
butorphanol
mu, kappa | IV only
68
tramadol
opiate
69
propoxyphene
old opiate that was withdrawal b/c of long QT arrhythmias
70
treatment for opiate withdrawl
inpatient: methadone outpatient: clonidine
71
Why are opiate associated with addiction?
Addiction is associated with inc DA. | Opiates disinhibit DA signaling, so inhibit GABA from blocking DA.
72
dependence vs addiction
dependence requires chronic use (it is physical) and addiction does not (it is psychological)
73
morphine: codeine > 2:1
pt is taking heroine
74
morphine: codeine <2:1
pt is taking codeine
75
toxic screen morphine:codeine significance
- synthetic opiates are negative | - fluoroqinolones can be false positive
76
Loperamide
- opiate for nonanalgesia - for diarrhea, dec GI transit - OTC - doesn't cross BBB
77
Diphenoxylate
- opiate for nonanalgesia - formulated with atropine to dec abuse - for diarrhea, dec GI transit
78
Gabapentin and Pregalabin
- non narcotic pain drug - blocks alpha2delta subunit of Ca channel - inhibits neuronal hyperexcitability - doesn't affect GABA
79
Lamotrigine and Carbamezapine
- non narcotic pain drug - voltage gated Na channel blocker - dec neuronal conduction - dose adjust in hepatic failure - BBW: SJS, vision, carbamez causes agranulocytosis
80
TCAs
- 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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