Chapter 8 (analgesics) Flashcards
(117 cards)
1
Q
categories of analgesics
A
centrally-acting opioid narcotic analgesics
peripherally-acting non-opioid analgesics
Others; used to treat very specific pain disorders
2
Q
centrally-acting opioid narcotics
A
opioid rc agonists; produce analgesia by going to brain and binding to opioid receptors
3
Q
opioid receptors
A
mu, delta, and kappa
4
Q
peripherally-acting non-opioid analgesics
A
prostaglandin inhibitors:
OTC analgesics that are NSAIDs and Tylenol
5
Q
a2 adrenergic antagonists
A
clonidine; treats long-term chornic pain by injection into spinal cord
6
Q
B blockers
A
drugs like propranolol useful in some migraines
7
Q
TCAs
A
tricyclic antidepressants; often have pain-relieving properties even greater than their anti-depressive effects
8
Q
Na channel blocker
A
all local anesthetics; awesome locally but can’t be used for headaches, sprained ankle, etc. b/c they must be injected
9
Q
must choose an analgesic according to pain of pt. and…
A
their ability to tolerate the side effects
10
Q
narcotics
A
any schedule 1-5 controlled substance regulated by the CSA of 1973
Includes heroin, methamphetamine, LSD, and opiods
11
Q
opiates definition
A
naturally occuring mu receptor ags derived from opium (morphine, opium, codeine)
12
Q
opioids definition
A
mu receptor agonists (natural or synthetic)
13
Q
endogenous opioids
A
our natural pain-killers; enkephalins, endorphins, and dynorphins
14
Q
opioid effects
A
always produces analgesia and almost guarantee constipation
sometimes there is sedation (even to the point of respiratory depression), miosis (excessive pupil constriction) euphoria, nausea, or urinary retention
15
Q
constipation side effects of opioids
A
why codeine can be used to treat diarrhea; occurs especially if taken long term
16
Q
euphoria effects of opioids
A
why heroin is abused so much
17
Q
Demerol
A
meperidine; first synthesized opioid
18
Q
hydrocodone
A
mixed with acetaminophen in Vicodin and Lortab; used commonly outside of hospital
19
Q
OxyContin
A
oxycodone; twice as potent as hydrocodone
20
Q
Sublimaze
A
fentanyl; 100x more potent than morphine, given by IV
Most popular synthetic potent opioid administered in clinics and hospitals
21
Q
sufentanyl
A
10x more potent than fentanyl, so 1000x more potent than morphine
22
Q
non-narcotic analgesics
A
act peripherally, unlike opiods
23
Q
opioid scheduling
A
all controlled:
S1: heroin
S2: oxycodone (Percocet, OxyContin), codeine, hydrocodone, 1/2 as potent as oxycodone so requires higher doses-some states require triplicate paperwork for S2
S5: cough syrups with low doses of codeine
24
Q
opioid dosing
A
differs greatly between people b/c there is up to a 10 fold difference in how tow people respond to same drug and dose; unlike many other drugs like digoxin where everyone responds basically the same to a similar dose
25
opioids and tylenol
combined b/c of synergistic effect, but many people do not know they are getting acetaminophen and overdose on it from taking it on top of their combination
26
cough syrups codeine dose
about 5 mg
27
tylenol 3
300 mg tylenol with 30 mg codeine
28
tylenol 4
300 mg tylenol with 60 mg codeine
29
NSAIDs
non-steroidal anti-inflammatory drugs
30
traditional NSAIDs
include over 30 Rx medications and ibuprofen, ketoprofen, and naproxen
31
NSAID mechanism of action
block locally-acting eicosanoids; specifically prostaglandins and thromboxanes
32
PG
prostaglandins
33
TXA
thromboxanes
34
LT
leukotrienes
35
formation of eicosanoids
arachidonic acid (AA) cascade forms many PGs, TXAs, and LTs that control normal body processes, but some also contribute to pain, inflammation, fever, and cramps
36
eicosanoids
synthesized by cells locally and act locally; do not really circulate systemically
Some are very important in other body processes, such as breathing
37
All eicosanoids
PGs, TXAs, and LTs (prostaglandins, thromboxanes, and leukotrienes)
38
AA cascade
arachidonic acid cascade: tissue injury leads to phospholipid release that eventually yields AA
39
Fork in AA cascade
leads to either PG and TXA production (by COX1 and 2) or LT production (by lipoxegenase)
40
some eicosanoids sensitize nerve endings so we perceive pain, so to counteract this process...
inhibiting cycloxengase enzymes to stop the ones that do this, but also inhibit PGs and TXAs that regulate BP, renal function, lung function, etc.
41
COX1
inhibiting this (like by Aspirin) leads to the most side effects such as platelets to be less sticky or unregulated BP (normally would be fine, but in compromised patients-like elderly-it could be a big deal)
42
COX2
better enzyme to inhibit for NSAIDS b/c it has less side effects
43
drug properties of NSAIDs
analgesia peripherally by PG inhibition
anti-inflammation by PG inhibition
antipyresis (fever reduction) by hypothalamus action
anticoagulation; to a greater or lesser extent (with the exception of cox2 inhibits) by preventing them from sticking together
44
anticoagulation effects of NSAIDs
Cause bleeding risk or ulcers; differ based on the drug; aspirin effects can last for 4-7 days so must be avoided leading up to surgery, while advil effect is only 4-8 hours for anticoagulation
45
most commonly used NSAIDs
ibuprofen (Advil, Motrin), ketoprofen (Orudis), naproxen (Aleve, Naprosyn), and ketorolac (Toradol)
46
Advil
ibuprofen OTC; common NSAID
47
Orudis
ketoprofen OTC; common NSAID
48
Aleve
naproxen OTC; common NSAID.
49
Toradol
ketorolac; potent NSAID given IM commonly to send patients home after surgery and used widely in professional athletics
Very strong pain relief, similar to morphine, but not as addictive (but side e's of stomach pain/upset and ulcers)
50
Salicylates
subclass of traditional NSAIDs; includes Aspirin, Ecotrin, magnesium salicylate, magnesium salicylate (Doan's Pills), sodium salicylate (Pepto-Bismol), and ASA mixed with sodium bicarbonate (Alka Seltzer)
51
ASA
Aspirin; acetylsalicylic acid; COX1 and 2 inhibitor
Be careful about expiration date b/c it decomposes into vinegar and salicylic acid which eats through tissue (used to burn off warts)
52
Ecotrin
Aspirin
53
Doan's Pills
magnesium salicylate
54
Pepto-Bismol
sodium salicylate
55
Aspirin anticoagulation
more potent inhibitor of platelet function than other NSAIDs (lasts 4-7 days)
56
Aspirin stomach issues
it is an acid, and also b/c it inhibits protective prostaglandins (PG E2) which protect the stomach lining then peptic ulcer disease (PUD) and GI bleeding
57
protective prostaglandin
PG E2
58
High dose salicylates can cause...
ringing in the ears
59
Salicylates, especially Aspirin, has one adverse effect that no other NSAIDs have
Link to Reye's syndrome: a disorder of the liver and brain that occurs in higher rates with kids under 16 who are taking salicylates during colds, flu, and chicken pox
So don't give NSAIDs to kids with these viral infections
60
COX2
found only to be active in states of inflammation, not all the time like COX1; great b/c people who are old and can't risk side effects of COX1 inhibitors can still take, but have increased risk of heart attack and stroke
61
Vioxx and Bextra
COX2 inhibs that were withdrawn from market b/c of covered up CV issues that led to Merk getting in huge trouble
62
Celebrex
celecoxib; COX2 inhib, only one left on market. Actually let doctors know the CV issues so they can weigh CV risks versus benefits.
63
APAP (acetyl-para-aminophenol)
Tylenol; acetaminophen; peripherally acting drug, but not an NSAID
Treats pain and fever, but NOT inflammation
Lower doses are becoming more popular
64
APAP mechanism of action
inhibits some aspects of COX2 but precise mechanism is unknown
65
Alka-Seltzer
ASA and antacid
66
buffered aspirin
ASA and antacid
67
Excedrin
acetaminophen, aspirin, and caffeine
| Very dangerous and abused heavily; very bad for kidneys to take these all at the same time
68
Percodan
oxycodone and ASA; S2 drug
69
Vicodin
actaminophen and hydrocodone; S2
70
Lortab
acetaminophen and hydrocodone; S2
71
Percocet
oxycodone and acetaminophen; S2
| -cet for acet- in acetaminophen
72
Vicoprofen
hydrocodone and ibuprofen; S2
| not very much ibuprofen, only 200 mg Ibuprofen and 7.5 mg hydrocodone
73
opioid combinations are not great in the long term
patients would be better with 6-12 months transitioning off and losing bad side effects and having better personal lives
More than two weeks on a opioid is a bad sign
74
narcotic and non-narcotic combinations
have synergistic potentiating effect; especially when taking centrally acting drug and peripherally acting drug b/c analgesics work via two very different mechanisms
Pain relief is much greater
75
accidental overdose of Tylenol
most common cause of liver failure requiring a transplant is acetaminophen overdose and poisoning. Occurring more often than ever b/c of many Tylenol containing combination drugs and people don't realize it so they take even more Tylenol.
76
analgesics outside of narcotics (opioids) and non-narcotics (PG inhibitors)
"others" some diseases with pain don't respond well to narcotics or NSAIDS
77
Migraine headaches
8x more likely in women. Aura comes on before headache which are certain signs noted by pts.
Some respond to opioids but don't want people to rely on these drugs though so other treatments are used.
Before migraine, vasodilation occurs followed by vasoconstriction which causes migraine
78
migraine treatments
ergotamine used; a powerful vasoconstrictor used to prevent vasodilation that occurs before migraine so the dilation and constriction cannot occur to stop the migraine if drug works in time to stop it
B blockers and CCB
SSRI antidepressants
a few antiseizure and antipsychotic drugs
79
CCB
calcium channel blockers
80
cluster headaches
more common in men. Best treated by 5-HT 1B receptor agonist; triptan drugs;
prevent headache from progressing so great if taken early
81
5-HT (5-hydroxytryptamine)
serotonin
82
Imitrex
sumatriptan; first and prototype triptan drug
83
Triptan drugs
5-HT 1B agonists that prevent headache from progressing; not addictive
Used so that opioids like Demerol don't have to be taken
84
triptan drug names
frovatriptan, rizatriptan, zolmitriptan, eletriptan, naratriptan, and sumatriptan (Imitrex)
85
Imitrex SC delivery
sumatriptan; FDA approved nitrogen gas-powered needle-free device for delivering sumatriptan succinate to subcutaneous tissue
86
chronic pain cause
most often a complex mixture of many different, sometimes unrelated factors (often psychosocial factors) so drugs are not always the best treatment
87
neuropathies causing chronic pain must often be treated with alternative approaches (not narcotics or NSAIDs) like...
TCA (tricyclic anti-depressants)
88
shingles
painful skin eruption caused by same virus that causes chicken pox; people who had chicken pox earlier in life can have virus sequester into a nerve and reactive later in life and just effect that nerve
10% of people can get post herpetic neuralgia
89
post herpetic neuralgia
incapacitating nerve pain syndrome (chronic)
Opioids don't work well b/c it is neuropathic pain
TCA are often used in lower dose than for depression
90
Elavil
amitriptyline; TCA
91
complex regional pain syndrome
RSD; reflex sympathetic dystrophy
Unusual, but very dismal condition that can last for a lifetime; terrible pain called causalgia
It can happen to anyone with no warning
TCAs used and spinal stimulators
92
Chronic pain treatments
pain meds, physical manipulation, counseling, and brain surgery to remove pain causing area
93
methadone
opioid used for chronic pain management and for detoxification from addiction to opioids
94
Buprenex
buprenorphine; partial agonist/antagonist (mixed agonist/antagonist) at mu receptor used in withdrawals from narcotic addiction and for migraines
Also used for those who need opioid but Dr's are worried about addiction/full effect and can easily be taken as just a squirt up the nose
95
ketamine
kappa opioid rc agonist; strongest pain reliever we know of other than inducing unconsciousness by general anesthesia
Originally an animal tranquilizer used for anesthesia now but causes hallucinations so must be careful
96
Ultram
tramadol; unknown mechanism, but very popular alternative to strong opioids and only has very mild opioid effect
1/100 binding at mu receptor compared to morphine and works well if pt. can't take NSAID
97
Alka Seltzer
ASA with sodium bicarbonate (an antacid used to protect and settle stomach) in an effervescent tablet
98
effervescent tablet
carbon tablets are tablets which are designed to dissolve in water, and release carbon dioxide.
99
Naprosyn
naproxen Rx; common NSAID
100
Motrin
ibuprofen Rx, common NSAID
101
caffeine
methylxanthine (found in chocolate) type drug with bronchodilator properties; can be used to treat tension and migraine headaches
102
verapamil
CCB; useful for nontradtional pain relief
103
Ergot alkaloids
ergotamine; potent vasoconstrictor used for non-trad pain relief of migraines
104
SSRI and SNRI antidepressants
can treat migraines
105
Prozac
fluoxetine; SSRI can be used to treat migraines
106
Cymbalta
duloxetine; SSNRI selective serotonin and norepinephrine reuptake inhibitor; can be used to treat migraines
107
anticonvulsants
used to treat fibromyalgia
108
Lyrica
pregabalin
109
corticosteroids
decrease inflammation and can help with pain
110
prednisone
corticosteroid; used to treat pain
111
Lidoderm patch
lidocaine; local anesthetic
112
capsaicin
compound found in chili peppers used in topical creams to deplete pain chemicals at site of injury
113
Laudanum
tincture of opium
114
first NSAID Rx to go OTC then another that followed
ibuprofen, then naproxen went from Rx Naprosyn to OTC aleve
115
PGs derived from
AA; arachidonic acid
116
Suboxone
therapy to help people get off opioids; combo of partial mu agonist/antagonist buprenorphine and a mostly inconsequential dose of full mu antag naloxone (prevents addicts from abusing this drug that is meant to help them wean off opioids)
117
alternating NSAIDs and Tylenol
Synergistic in analgesic effect and toxicity; very hard on kidneys, only to be done in the very short term; mainly to bring down a high fever from anti-pyretic effects
