Pharm Flashcards
(96 cards)
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”
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
3
Q
COMT inhibitor
A
- prevents DA metabolism: prolong action of L-DOPA
- increases L-DOPA bioavailability
- reduces 3OMD production that may compete with L-DOPA for GI and BBB transport
Tx: Parkinson’s with L-DOPA to reduce fluctuations
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
5
Q
VMAT inhibitor
A
deplete DA (inhibit packaging into vesicles) Tx: Huntington's
6
Q
D2 receptor antagonist
A
Tx: Huntington’s
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
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
9
Q
bromocriptine
A
DA receptor agonist: D2 agonist/ D1 partial agonist
10
Q
pramipexole
A
DA receptor agonist: D2 selective agonist
free radical scavenger
11
Q
ropinirole
A
DA receptor agonist: D2 selective agonist
metabolized by CYP1A2
12
Q
apomorphine
A
DA receptor agonist: D1/D2 agonist
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
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)
15
Q
rasagiline
A
MAO-B inhibitor: more potent
Tx: late Parkinson’s with L-DOPA, early Parkinson’s alone
16
Q
entacapone
A
COMT inhibitor: PERIPHERAL only
PREFERRED over tolcapone
17
Q
tolcapone
A
COMT inhibitor: PERIPHERAL and CENTRAL
AE: hepatic (why entacapone is preferred)
18
Q
benztropine
A
antimuscarinic
Tx: Parkinson’s
19
Q
diphenhydramine
A
antimuscarinic
Tx: Parkinson’s
20
Q
trihexyphenidyl
A
antimuscarinic
Tx: Parkinson’s
21
Q
reserpine
A
VMAT inhibitor
22
Q
tetrabenazine
A
VMAT inhibitor
23
Q
chlorpromazine
A
D2 receptor antagonist
24
Q
haloperidol
A
D2 receptor antagonist
25
Idiopathic Parkinson's vs. Parkinsonism
Idiopathic: unknown origin, genetic component
Parkinsonism: associated with infection (encephalitis), stroke, trauma, antipsychotics, MPTP; Tx RESISTANT
26
Advantages of DA agonist Tx in Parkinson's
1. no activation needed
2. no toxic metabolites
3. no competition for GI absorption or across BBB
4. more selective: fewer AE
27
L-type Ca channel antagonist
future Parkinson's Tx
28
fluoxetine
Tx: Huntington's associated depression
29
opiate agonist
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
30
opiate partial agonist/antagonist
mu receptor partial agonist
can precipitate WITHDRAWAL in addicts and patients on full agonist chronically
decreased: analgesia and respiratory depression compared to morphine
31
opiate antagonist
mu, delta and kappa receptor antagonist
| precipitate withdrawal in dependent patients
32
NMDA receptor antagonist
```
non-narcotic
NMDA activation leads to Ca entry and central sensitization
Tx: pain
NO resp. depression
AE: PSYCHOMIMETIC
```
33
TCAs
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
34
anticonvulsants
non-narcotic
Ca or Na channel block
AE: SUICIDAL IDEATION
Tx: pain
35
alfentanil
opiate agonist
| use: anesthesia
36
codeine
```
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
```
37
fentanyl
opiate agonist
use: anesthesia
can accumulate in adipose
can give in renal insufficiency
38
hydrocodone
opiate agonist
| commonly abused
39
hydromorphone
opiate agonist
commonly abused
can give in renal insufficiency
40
methadone
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
meperidine
opiate agonist
antimuscarinic: tachycardia, no mitosis or GI spasms
metabolite: normeperidine: CYP, SSRI, can cause seizures; CNS stimulant toxicity in renal dysfunction
42
oxycodone
opiate agonist
commonly abused
orally available
43
oxymorphone
opiate agonist
| commonly abused
44
sufentanil
opiate agonist
MOST POTENT analgesic
use: anesthesia
45
remifentanil
opiate agonist
| use: anesthesia
46
tramadol
WEAK opiate agonist
NE, 5-HT reupatake inhibitor
AE: seizures, blood sugar regulation
CI: accumulate in renal insufficiency
47
butorphanol
```
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
buprenorphine
```
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
nalbuphine
opiate partial agonist
kappa agonist: DYSPHORIA
CAD patients: NO increase in cardiac problems
50
pentazocine
opiate partial agonist
kappa agonist: DYSPHORIA
CAD patient: increase cardiac problems
51
naloxone
```
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
naltrexone
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
methylnaltrexone
opiate antagonist
| does NOT pass BBB: decreases AE of opioids without impacting central analgesia
54
ketamine
NMDA antagonist
| Tx: acute severe pain
55
dextromethorphan
low affinity NMDA antagonist and antitussive
Tx: chronic, post-op pain; COUGH (mu and non-opiate receptors)
AE: hallucination, habit forming
56
amitriptyline
TCA
57
nortriptyline
TCA
58
imipramine
TCA
59
desipramine
TCA
60
gabapentin
anticonvulsant
MoA: inhibition of voltage-gated Ca channels via alpha-2-delta subunit
AE: SEDATION, peripheral edema, GI
decrease dose in renal insufficiency
61
lamotrigene
```
anticonvulsant
Na channel blocker
use: neuropathy, stroke, MS, phantom limb
AE: blurred vision, hematologic
BBW: RASH (Steven-Johnson)
Tx: ancillary pain management
```
62
carbamazepine
```
anticonvulsant
Na channel blocker
CYP interactions
AE: dizzy, drowsy, agranulocytosis
Tx: ancillary pain management, Huntington's depression
```
63
pregabalin
anticonvulsant
MoA: inhibition of voltage-gated Ca channels via alpha-2-delta subunit
AE: SEDATION, peripheral edema, GI
decrease dose in renal insufficiency
64
Pain NT
1. glutamate
2. substance P
3. CGRP (calcitonin gene-related peptide)
65
mu opioid receptor (OP-3)
```
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
delta opioid receptor (OP-1)
highest affinity: ENKEPHALINS
1. supra spinal and spinal analgesia
2. modulation of hormone and NT release
67
kappa opioid receptor (OP-2)
highest affinity: DYNORPHINS
1. supra spinal and spinal analgesia
2. PSYCHOTOMIMETIC
3. DECREASE GI TRANSIT
68
alpha 2 agonist
SPINAL
pre-synaptic reduction in sympathetic outflow
Tx: pain
AE: sedation, hypotension, bradycardia
69
clonidine
alpha 2 agonist
Tx: outpatient opiate withdrawal
not effective for: insomnia, muscle cramps, GI
AE: sedation, dry mouth, constipation at high dose
70
dexmedetomidine
alpha 2 agonist
71
What drugs that treat pain act
1. peripherally
2. in spinal cord
3. centrally
4. on initial signal transduction
1. Na channel blockers
2. opioids, anticonvulsants, antidepressants, alpha 2 agonist, NSAIDs
3. opioids
4. NSAIDs
72
What are the most potent opioids?
fentanyl series
73
morphine
```
opiate agonist
kappa agonist
use: pulmonary edema, diarrhea
POOR ORAL BIOAVAILABILITY
CI: renal failure
```
74
Which opioid can be given transdermally?
When would you use it?
Considerations?
fentanyl
use in dysphagia, constipation, poor GI absorption (outpatient)
considerations: time to accumulate, have to take off to prevent OD, less constipation
75
Which opioids can be given rectally?
1. morphine
2. hydromorphone
3. oxymorphone
76
Which opioids would you combine with an NSAID?
hydrocodone, oxycodone
77
Where can opioids accumulate?
main reservoir: skeletal muscle
| can accumulate in adipose with continued delivery: storage allows slow drug release
78
opiate overdose signs
1. coma
2. pinpoint pupils
3. respiratory depression
altered mental status, severe perspiration, shock, pulmonary edema, unresponsive
79
Drugs that worsen opioid CNS depression
1. sedative hypnotics
2 antipsychotic tranquilizers
3. MAOI
80
What AE of opioids do patients not develop tolerance to?
1. mitosis
2. constipation
3. convulsions
moderate tolerance: bradycardia
81
What effects of opioids do patients develop tolerance to?
1. analgesia
2. euphoria, dysphoria
3. mental clouding
4. sedation
5. respiratory depression
6. anti-diuresis
7. N/V
8. cough suppression
82
How does tolerance develop in opioid use?
1. classical view
2. other view
Why does this not occur with endogenous opioids?
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
How can you manage opioid AE?
1. constipation
2. somnolence
3. N/V
4. respiratory depression
5. pruritus
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
Signs of opiate withdrawal
1. agitation
2. diaphoresis
3. lacrimation, rhinorrhea
4. piloerection
4. dilated pupils
also: anxiety, fear, sleep disturbance, nausea, diarrhea, pain
85
How can you confirm suspected opiate intoxication?
What is the draw back?
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
How can you get the precise concentration of opiate metabolites in an opiate intoxicated patient?
GC-Mass Spec
87
voltage gated Ca channel blocker
GABA
MoA: prevent trafficking of channel to surface (up regulation of channel occurs in hyper sensitization)
AE: dizzy, drowsy
Tx: ancillary pain med
88
What do anticonvulsants carry an increased risk of
suicidal ideation
89
What controls cough?
nucleus of solitary tract
90
loperamide
antidiarrheal opioid: inhibit cholinergic nerves in enteric nervous system
no BBB access: no analgesia
91
diphenoxylate
need prescription
antidiarrheal opioid: inhibit cholinergic nerves in enteric nervous system
no analgesia at recommended dose
ATROPINE added to discourage abuse
92
complimentary and alternative medicine (CAM) pain Tx reasoning
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
What opioids can be prescribed in renal failure?
hydromorphone
| oxycodone
94
What opioid can be used in alcohol dependence and craving?
naltrexone
95
What opioid antagonist can be used for opiate addiction?
naloxone
96
1. Only partial opioid agonist with out dysphoria/ kappa agonism?
2. Which ones do have Kappa affects?
1. buprenorphine (use with naloxone)
| 2. nalbuphine, pentazocine, butorphanol, morphine (full agonist)
