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Pre-pharmacology > Chapter 8 (analgesics) > Flashcards

Chapter 8 (analgesics) Flashcards

1
Q

categories of analgesics

A

centrally-acting opioid narcotic analgesics
peripherally-acting non-opioid analgesics
Others; used to treat very specific pain disorders

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2
Q

centrally-acting opioid narcotics

A

opioid rc agonists; produce analgesia by going to brain and binding to opioid receptors

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3
Q

opioid receptors

A

mu, delta, and kappa

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4
Q

peripherally-acting non-opioid analgesics

A

prostaglandin inhibitors:

OTC analgesics that are NSAIDs and Tylenol

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5
Q

a2 adrenergic antagonists

A

clonidine; treats long-term chornic pain by injection into spinal cord

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6
Q

B blockers

A

drugs like propranolol useful in some migraines

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7
Q

TCAs

A

tricyclic antidepressants; often have pain-relieving properties even greater than their anti-depressive effects

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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

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9
Q

must choose an analgesic according to pain of pt. and…

A

their ability to tolerate the side effects

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10
Q

narcotics

A

any schedule 1-5 controlled substance regulated by the CSA of 1973
Includes heroin, methamphetamine, LSD, and opiods

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11
Q

opiates definition

A

naturally occuring mu receptor ags derived from opium (morphine, opium, codeine)

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12
Q

opioids definition

A

mu receptor agonists (natural or synthetic)

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13
Q

endogenous opioids

A

our natural pain-killers; enkephalins, endorphins, and dynorphins

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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

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15
Q

constipation side effects of opioids

A

why codeine can be used to treat diarrhea; occurs especially if taken long term

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16
Q

euphoria effects of opioids

A

why heroin is abused so much

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17
Q

Demerol

A

meperidine; first synthesized opioid

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18
Q

hydrocodone

A

mixed with acetaminophen in Vicodin and Lortab; used commonly outside of hospital

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19
Q

OxyContin

A

oxycodone; twice as potent as hydrocodone

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20
Q

Sublimaze

A

fentanyl; 100x more potent than morphine, given by IV

Most popular synthetic potent opioid administered in clinics and hospitals

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21
Q

sufentanyl

A

10x more potent than fentanyl, so 1000x more potent than morphine

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22
Q

non-narcotic analgesics

A

act peripherally, unlike opiods

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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

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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

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25
Q

opioids and tylenol

A

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

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26
Q

cough syrups codeine dose

A

about 5 mg

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27
Q

tylenol 3

A

300 mg tylenol with 30 mg codeine

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28
Q

tylenol 4

A

300 mg tylenol with 60 mg codeine

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29
Q

NSAIDs

A

non-steroidal anti-inflammatory drugs

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30
Q

traditional NSAIDs

A

include over 30 Rx medications and ibuprofen, ketoprofen, and naproxen

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31
Q

NSAID mechanism of action

A

block locally-acting eicosanoids; specifically prostaglandins and thromboxanes

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32
Q

PG

A

prostaglandins

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33
Q

TXA

A

thromboxanes

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34
Q

LT

A

leukotrienes

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35
Q

formation of eicosanoids

A

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

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36
Q

eicosanoids

A

synthesized by cells locally and act locally; do not really circulate systemically
Some are very important in other body processes, such as breathing

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37
Q

All eicosanoids

A

PGs, TXAs, and LTs (prostaglandins, thromboxanes, and leukotrienes)

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38
Q

AA cascade

A

arachidonic acid cascade: tissue injury leads to phospholipid release that eventually yields AA

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39
Q

Fork in AA cascade

A

leads to either PG and TXA production (by COX1 and 2) or LT production (by lipoxegenase)

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40
Q

some eicosanoids sensitize nerve endings so we perceive pain, so to counteract this process…

A

inhibiting cycloxengase enzymes to stop the ones that do this, but also inhibit PGs and TXAs that regulate BP, renal function, lung function, etc.

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41
Q

COX1

A

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)

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42
Q

COX2

A

better enzyme to inhibit for NSAIDS b/c it has less side effects

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43
Q

drug properties of NSAIDs

A

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

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44
Q

anticoagulation effects of NSAIDs

A

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

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45
Q

most commonly used NSAIDs

A

ibuprofen (Advil, Motrin), ketoprofen (Orudis), naproxen (Aleve, Naprosyn), and ketorolac (Toradol)

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46
Q

Advil

A

ibuprofen OTC; common NSAID

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47
Q

Orudis

A

ketoprofen OTC; common NSAID

48
Q

Aleve

A

naproxen OTC; common NSAID.

49
Q

Toradol

A

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
Q

Salicylates

A

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
Q

ASA

A

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
Q

Ecotrin

A

Aspirin

53
Q

Doan’s Pills

A

magnesium salicylate

54
Q

Pepto-Bismol

A

sodium salicylate

55
Q

Aspirin anticoagulation

A

more potent inhibitor of platelet function than other NSAIDs (lasts 4-7 days)

56
Q

Aspirin stomach issues

A

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
Q

protective prostaglandin

A

PG E2

58
Q

High dose salicylates can cause…

A

ringing in the ears

59
Q

Salicylates, especially Aspirin, has one adverse effect that no other NSAIDs have

A

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
Q

COX2

A

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
Q

Vioxx and Bextra

A

COX2 inhibs that were withdrawn from market b/c of covered up CV issues that led to Merk getting in huge trouble

62
Q

Celebrex

A

celecoxib; COX2 inhib, only one left on market. Actually let doctors know the CV issues so they can weigh CV risks versus benefits.

63
Q

APAP (acetyl-para-aminophenol)

A

Tylenol; acetaminophen; peripherally acting drug, but not an NSAID
Treats pain and fever, but NOT inflammation
Lower doses are becoming more popular

64
Q

APAP mechanism of action

A

inhibits some aspects of COX2 but precise mechanism is unknown

65
Q

Alka-Seltzer

A

ASA and antacid

66
Q

buffered aspirin

A

ASA and antacid

67
Q

Excedrin

A

acetaminophen, aspirin, and caffeine

Very dangerous and abused heavily; very bad for kidneys to take these all at the same time

68
Q

Percodan

A

oxycodone and ASA; S2 drug

69
Q

Vicodin

A

actaminophen and hydrocodone; S2

70
Q

Lortab

A

acetaminophen and hydrocodone; S2

71
Q

Percocet

A

oxycodone and acetaminophen; S2

-cet for acet- in acetaminophen

72
Q

Vicoprofen

A

hydrocodone and ibuprofen; S2

not very much ibuprofen, only 200 mg Ibuprofen and 7.5 mg hydrocodone

73
Q

opioid combinations are not great in the long term

A

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
Q

narcotic and non-narcotic combinations

A

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
Q

accidental overdose of Tylenol

A

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
Q

analgesics outside of narcotics (opioids) and non-narcotics (PG inhibitors)

A

“others” some diseases with pain don’t respond well to narcotics or NSAIDS

77
Q

Migraine headaches

A

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
Q

migraine treatments

A

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
Q

CCB

A

calcium channel blockers

80
Q

cluster headaches

A

more common in men. Best treated by 5-HT 1B receptor agonist; triptan drugs;
prevent headache from progressing so great if taken early

81
Q

5-HT (5-hydroxytryptamine)

A

serotonin

82
Q

Imitrex

A

sumatriptan; first and prototype triptan drug

83
Q

Triptan drugs

A

5-HT 1B agonists that prevent headache from progressing; not addictive
Used so that opioids like Demerol don’t have to be taken

84
Q

triptan drug names

A

frovatriptan, rizatriptan, zolmitriptan, eletriptan, naratriptan, and sumatriptan (Imitrex)

85
Q

Imitrex SC delivery

A

sumatriptan; FDA approved nitrogen gas-powered needle-free device for delivering sumatriptan succinate to subcutaneous tissue

86
Q

chronic pain cause

A

most often a complex mixture of many different, sometimes unrelated factors (often psychosocial factors) so drugs are not always the best treatment

87
Q

neuropathies causing chronic pain must often be treated with alternative approaches (not narcotics or NSAIDs) like…

A

TCA (tricyclic anti-depressants)

88
Q

shingles

A

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
Q

post herpetic neuralgia

A

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
Q

Elavil

A

amitriptyline; TCA

91
Q

complex regional pain syndrome

A

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
Q

Chronic pain treatments

A

pain meds, physical manipulation, counseling, and brain surgery to remove pain causing area

93
Q

methadone

A

opioid used for chronic pain management and for detoxification from addiction to opioids

94
Q

Buprenex

A

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
Q

ketamine

A

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
Q

Ultram

A

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
Q

Alka Seltzer

A

ASA with sodium bicarbonate (an antacid used to protect and settle stomach) in an effervescent tablet

98
Q

effervescent tablet

A

carbon tablets are tablets which are designed to dissolve in water, and release carbon dioxide.

99
Q

Naprosyn

A

naproxen Rx; common NSAID

100
Q

Motrin

A

ibuprofen Rx, common NSAID

101
Q

caffeine

A

methylxanthine (found in chocolate) type drug with bronchodilator properties; can be used to treat tension and migraine headaches

102
Q

verapamil

A

CCB; useful for nontradtional pain relief

103
Q

Ergot alkaloids

A

ergotamine; potent vasoconstrictor used for non-trad pain relief of migraines

104
Q

SSRI and SNRI antidepressants

A

can treat migraines

105
Q

Prozac

A

fluoxetine; SSRI can be used to treat migraines

106
Q

Cymbalta

A

duloxetine; SSNRI selective serotonin and norepinephrine reuptake inhibitor; can be used to treat migraines

107
Q

anticonvulsants

A

used to treat fibromyalgia

108
Q

Lyrica

A

pregabalin

109
Q

corticosteroids

A

decrease inflammation and can help with pain

110
Q

prednisone

A

corticosteroid; used to treat pain

111
Q

Lidoderm patch

A

lidocaine; local anesthetic

112
Q

capsaicin

A

compound found in chili peppers used in topical creams to deplete pain chemicals at site of injury

113
Q

Laudanum

A

tincture of opium

114
Q

first NSAID Rx to go OTC then another that followed

A

ibuprofen, then naproxen went from Rx Naprosyn to OTC aleve

115
Q

PGs derived from

A

AA; arachidonic acid

116
Q

Suboxone

A

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
Q

alternating NSAIDs and Tylenol

A

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

Pre-pharmacology (27 decks)

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