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Test 4 - mild and strong analgesics
N/A
174
Pharmacology
Graduate
03/30/2010

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Term
Somatic pain
Definition
A well-localized constant, achy area in skin and subcutaneous tissues and less well-localized in bone, connective tissues, blood vessels, and muscles
Term
Incisional pain, bone fractures, bony metastasis, osteoarthritis and rheumatoid arthritis, peripheral vascular disease:

These cause what kind of pain?
Definition
somatic pain
Term
Visceral pain
Definition
Poorly localized, crampy, diffuse, and deep sensation originating from an internal organ or a cavity lining.
Term
Bladder distention and spasms, intestinal distention, inflammatory bowel disease, hiatal hernia, organ metastasis, and pericarditis:

These cause what kind of pain?
Definition
visceral pain
Term
Neuropathic pain
Definition
A poorly localized, electric-shock-like, lancinating, shooting sensation originating from injury to a peripheral nerve, the spinal cord, or the brain
Term
Diabetic neuropathy, radiculopathy, postherpetic neuralgia, phantom limb pain, and tumor-related nerve compression:

These cause what kind of pain?
Definition
Neuropathic pain
Term
Characterize pain interms of the following: (7)
Definition
1) Location
2) Mode and time of onset
3) Associated features, e.g., nausea, muscle spasm
4) Quality and time-intensity attributes
5) Duration
6) Severity (scale of 0-10)
7) Provoking and relieving factors
Term
What pain stimuli are specific to skin?
Definition
pricking, cutting, crushing, burning, and freezing
Term
What pain stimuli are specific to viscera?
Definition
Inflamed mucosa, distention or spasm of smooth muscle, and traction on the mesenteric attachment.

(Insensitive to pricking, cutting, crushing, burning, and freezing)
Term
What pain stimuli are specific to skeletal and cardiac muscle?
Definition
ischemia (intermittent claudication/ angina), necrosis, hemorrhage, and injection of irritating solutions as well as by injuries of connective tissue sheaths.
Term
What pain stimuli are specific to joints?
Definition
Synovial membrane inflammation, exposure to hypertonic saline.

(Insensitive to pricking, cutting, and cautery.)
Term
What pain stimuli are specific to ligaments?
Definition
Stretching and tearing.
Term
What pain stimuli are specific to periosteum?
Definition
Injury, inflammation.
Term
What pain stimuli are specific to blood vessels?
Definition
Piercing by a needle, inflammation, distension, traction
Term
What pain stimuli are specific to nerves?
Definition
Inflammation, compression of roots and sensory ganglia.
Term
3 types of sensory receptors:
Definition
1) neuroepithelial
2) epithelial
3) neuronal
Term
Example of neuro-epithelial sensory receptor?
Definition
olfactory epithelium neurons

(the neuron itself replaces the epithelial tissue as a sensor)
Term
Examples of epithelial sensory receptors:

(4)
Definition
1) Epidermal Merkel cells (sustained pressure mechanosensors)
2) taste buds
3) auditory receptors
4) retinal photoreceptors
Term
examples of neuronal sensory receptors: (2)
Definition
1) cutaneous sensors (except Merkel)
2) proprioceptors
Term
Nociceptors or pain sensors are _________ sensory receptors
Definition
neuronal
Term
What neuron type is associated with nociception?
Definition
unipolar neuron
Term
Local anesthetics block nerve conduction at the _____________ ____________ .
Definition
peripheral nerve
Term
Fibers responsible for pain, temperature and touch?
Definition
A-delta fibers
Term
Fibers responsible for pain, temperature and some mechanoreception ?
Definition
C fibers
Term
A-delta fibers synapse in?
Definition
Rexed's lamina I of the dorsal horn.
Term
C fibers synapse in the ?
Definition
substantia gelatinosa of the dorsal horn
Term
Pain comes in 2 forms: acute/sharp/highly localized and then chronic/slow/dull/aching. What determines this?
Definition
The conduction of the acute pain is on the A-δ fibers. In contrast the C fibers are slower, 2 m/s conduction. That is the neurological basis for different types of pain.
Term
The Neospinothalamic tract is for fast acute, pain and synapses where?
Definition
in the thalamus (it has one synapse)
Term
the Paleospinothalamic is for slow, chronic pain and synapses where?
Definition
Reticular nuclei of brainstem then thalamus (according to transcript)
Term
The periaqueductal grey is very important for the ___________________.
Definition
endogenous analgesic system
Term
T/F: pain can be generated in the absence of any stimulus
Definition
T (he referenced empathetic pain when parent watches child in pain)
Term
______ _________ affect synaptic transmission in CNS structures.
Definition
strong analgesics
Term
________ __________ affects signal generation at the synapse.
Definition
mild analgesics
Term
Morphine and meperidine are ___________ __________.
Definition
strong analgesics
Term
aspirin is a _________ __________
Definition
mild analgesic
Term
site of action of morphine and meperidine?
Definition
CNS
Term
site of action of aspirin?
Definition
CNS and PNS
Term
codeine can be used for a pain level of ____
Definition
5
Term
morphine and meperidine may be used for a pain level of ____
Definition
10
Term
aspirin may be used for a pain level of _____
Definition
0-3
Term
inflammation activates _______________ to release arachidonic acid from membrane phospholipids.
Definition
phospholipase A2
Term
PGH synthase is a ______________ enzyme
Definition
bifunctional
Term
2 functions of PGH synhase:
Definition
1) COX
2) hydroperoxidase
Term
what is the difference b/w COX I and II?
Definition
I: endogenous/constitutive in most cells
II: inducible isoform (induced by inflammation)
Term
hydroperoxidases do what?
Definition
degrade hydrogen peroxide to PGH2
Term
5 bioactive prostaglandins from PGH2:
Definition
1) TXA2 (platelets, lungs)
2) PGE2 (renal collecting tubule)
3) PGI2 (endothelial cells)
4) PGJ2 (brain)
5) PGF2-alpha (uterus, kinda like oxytocin)
Term
arachidonic acid is transformed to HETEs and leukotrienes by __________________.
Definition
lipoxygenase
Term
_________ ___________ is mediated by HETEs.
Definition
leukocyte infiltration
Term
leukocyte infiltration will not be blocked by ___________.
Definition
NSAIDs (obvious i know, but he said it was an important exam pt, that this is a totally diff enzyme than the COX enzymes which may be blocked by NSAIDs)
Term
montelukast/singulair directly blocks the production of ______________
Definition
leukotrienes (not on test, but he said was very important to know)
Term
2 bronchoconstrictors:
Definition
1) thromboxane (TXA2)
2) leukotrienes
Term
PGE2 cause what for signs of inflammation:
Definition
1) redness
2) heat
3) pain
4) swelling
Term
____________ potentiate the effects of bradykinin and histamine on pain and fever
Definition
prostaglandins
Term
_________________ (PGE2 analog) used to treat drug-induced ulcers in elderly
Definition
misoprostol
Term
actions of PGE2 concerning GIT: (3)
Definition
1)inhibit acid secretion
2)increase mucous secretion
3)cytoprotective and prevents ulceration
Term
Actions of PGF concerning GIT (2):
Definition
1) inhibit acid secretion
2) increase mucous secretion
Term
_______ & _________ cause contraction in uterine smooth muscle.
Definition
PGE2 and PGF2-alpha
Term
_____________(PGE2 analog) contracts uterus and expels fetus
Definition
misoprostol
Term
Misoprostol + progesterone receptor blocker (mifepristone) is known as
Definition
RU-486 (ends pregnancy)
Term
furosemide upregulates COX2 activity which increases ___________
Definition
PGE2
Term
PGE2 can block __________ reabsorption
Definition
NaCl
Term
4 positive effects of NSAIDs:
Definition
1)anti-inflammatory
2)analgesic
3)antipyretic
4)antiaggregation
Term
tinnitus, dizziness and headache may be an adverse side effect of _____________.
Definition
NSAIDs
Term
adverse effects of NSAIDs in CNS: (3)
Definition
1)tinnitus
2)headaches
3)dizziness
Term
adverse effects of NSAIDs in CVS: (3)
Definition
1)edema
2)hypertension
3)congestive heart failure
Term
adverse effects of NSAIDs in GI: (3)
Definition
1)nausea
2)ulcers
3)bleeding
Term
adverse effects of NSAIDs in blood: (3)
Definition
1)neutropenia
2)thrombocytopenia
3)anemia
Term
adverse effect of NSAIDs on liver:
Definition
hepatic failure
Term
adverse effect of NSAIDs on lungs:
Definition
asthma
Term
3 adverse effects of NSAIDs on kidneys:
Definition
1)hyperkalemia
2)renal insufficiency
3)proteinuria
Term
which NSAID is safe for people with ulcers?
Definition
Naproxen
Term
Which drug is the only parenteral analgesic in the NSAID class?
Definition
ketorolac
Term
List of ten NSAIDs (mild analgesics) non-selective COX-inhibitors:

(al-medhi suggested good idea to know all)
Definition
1)aspirin
2)diclofenac
3)etodolac
4)ibuprofen
5)indomethacin
6)ketoprofen
7)ketorolac
8)naproxen
9)piroxicam
10)sulindac
Term
Name 1 drawback to acetaminophen:
Definition
It has no anti-inflammatory effect. It treats fever and pain but do not use for inflammation!
Term
Celecoxib and meloxicam are _____________ inhibitors.
Definition
COX-2 selective
Term
2 pros to using a COX-2 selective inhibitor as opposed to non-selective COX inhibitor:
Definition
1)No antiaggregation effects
2)less GI bleeding
Term
2 examples of COX-2 selective inhibtors:
Definition
1)celecoxib
2)Meloxicam
Term
COX-2 is the isoform of ____________ _________that resides in macrophages and in joint cells, the “synovialcytes.”
Definition
prostaglandin synthase
Term
2 side effects of COX-2 specific inhibitors:
Definition
1) higher thrombotic events
2) nephrotoxicity
Term
salicylic acid can be used as a ____________.
Definition
keratolytic
Term
Name 4 things salicylic acid may be used for:
Definition
1)warts
2)corns
3)fungus
4)eczema
Term
A wart can be lysed with ____________ _______.
Definition
salicylic acid
Term
oil of wintergreen contains ___________ _________.

( i have no idea if this is relevant or not, al-medhi put lots of rando stuff on the slides)
Definition
methyl salicylate
Term
prostaglandins lower the required levels of _____________ to elicit a pain response. This is the mechanism of _______________.
Definition
substance P; hyperalgesia
Term
pyrogens, agents such as LPS of bacteria, viruses, and others, induce fever via _______________.
Definition
prostaglandins
Term
How does aspirin (acetylsalicylic acid) prevent binding of arachidonic acid to PGH synthase?
Definition
by acetylating the PGH synthase
Term
____________ prevents sensitization of receptors by prostaglandins, and thus hyperalgesia
Definition
aspirin (acetylsalicylic acid)
Term
____________ Inhibits pyrogen-induced prostaglandin synthesis and resets hypothalamic thermostat
Definition
aspirin (acetylsalicylic acid)
Term
aspirin induces antipyresis by: (2)
Definition
1)inhibiting pyrogen-induced prostagladin synthesis
2)vasodilation of skin vessels to dissipate more heat
Term
leukocyte infiltration cannot be blocked by NSAIDS or aspirin. It can only be blocked by ___________ ____________.
Definition
lipoxygenase inhibitors
Term
Aspirin (acetylsalicylic acid) is antithrombotic b/c: (2)
Definition
1) anucleate platelets are unable to synthesize new PGH (8-10 days to replace platelets)
2)loss of thromboxane inhibits platelet aggregation and increases bleeding time


*PGH synthase is replaced w/in 12 hrs in other tissues
Term
_____________ has a muco-protective effect
Definition
PGE2
Term
Aspirin may cause gastric ulceration & bleeding due to inhibition of ______ synthesis locally
Definition
PGE2
Term
chronic toxicity by aspirin is otherwise known as ?
Definition
salicylism
Term
Salicylism may cause: (3)
Definition
1)tinnitus
2)decreased hearing
3)vertigo
Term
10-30 g single dose of aspirin may cause:
Definition
acute salicylate toxicity
Term
This diuretic can enhance the toxic effects of aspirin.
Definition
acetazolamide
Term
_________ has a direct effect on the respiratory center to increase rate and depth of breathing
Definition
aspirin
Term
___________ increases GI bleeding induced by salicylates
Definition
alcohol
Term
Treat overdose of acetominophen (tylenol) with __________________.
Definition
N–ACETYLCYSTEIN (MUCOMYST)
Term
Tylenol does not have an ____________ effect.
Definition
anti-inflammatory
Term
Why is acetaminophen (tylenol) not anti-inflammatory ?
Definition
There is a high concentration of peroxides in inflamed tissue blocking the action.
Term
toxic effect of tylenol?
Definition
hepatic necrosis
Term
Papaverine is a _________ _________ relaxant.
Definition
smooth muscle
Term
3 medically relevant alkaloids: (3)
Definition
1)morphine
2)codeine
3)papaverine
Term
_________ are narcotic analgesics like morphine that produce analgesia without loss of consciousness.
Definition
opioid (opium-like)
Term
Drugs derived from opium are known as _______.
Definition
opiates
Term
Opioid drugs act mostly via the ________ _________.
Definition
MOP (µ) receptor
Term
pinpoint pupil is a sign of _______ toxicity
Definition
opioid
Term
opioid receptors located in the ____________ effect neuroendocrine function.
Definition
hypothalamus
Term
Opioid receptors located in the __________________ effect coughing, respiration, vomiting, & miosis.
Definition
ventral brain stem
Term
opioid receptors located in ___________________ effect mood & behavior.
Definition
limbic structures
Term
opioid receptors located in ____________, __________ & _____________ regulate pain sensation.
Definition
dorsal horn, periaqueductal grey & thalamus
Term
Respiratory depression is caused only by the _________ opioid receptor.
Definition
Mu
Term
Do not give opioids to pulmonary disease pts due to ________________
Definition
respiratory depression
Term
Drug historically used to treat diarrhea:
Definition
Morphine
Term
Dyspnea and pain are greatly relieved by _________ in an MI pt.
Definition
morphine
Term
What kind of receptor are opioid receptors?
Definition
G-protein coupled receptors (Gi)
Term
activation of opioid GPCR does what 2 things to hyperpolarize the cell?
Definition
1)open K channels (efflux of Ca)
2)close Ca channles (blocking Ca influx)

*hyperpolarization--this causes a blockade of Neurotransmitter Release
and Pain Transmission
Term
If you use morphine chronically,binding of _________ leads to internalization of morphine receptors
Definition
B-arrestins
Term
acute tolerance of morphine is caused by _____________ activation
Definition
B-arrestin
Term
B-arrestins cause internalization of ________________
Definition
morphine receptors
Term
T/F: all effects of morphine are subject to mechanism of tolerance
Definition
F
Term
3 effects of morphine that are not affected by the mechanism of tolerance:
Definition
1)miosis
2)constipation
3)convulsion
Term
High tolerance to ____________ can develop with long term morphine use.
Definition
analgesia (there is a long list of others but they are considered side-effects)
Term
Naloxone is a ______________________
Definition
morphine antagonist
Term
T/F: humans have endogenous morphine-like substances
Definition
T
Term
name 3 families of endogenous opioid peptides:
Definition
1)endorphins
2)enkephalins
3)dynorphins
Term
_____________ is the smallest endogenous opioid peptide that is synthesized by the body
Definition
enkephalin
Term
___________ is the precursor for B-endorphins
Definition
Pro-opiomelanocortin (POMC)
Term
2 forms of enkephalins:
Definition
Met & leu
Term
6 possible products of Pro-opiomelanocortin (POMC):
Definition
1)MSH (alpha, gamma and beta)
2)ACTH
3)lipotropin (beta and gamma)
4)CLIP
5)B-endorphin
6)met-enkephalin
Term
enkephalin neurons of periaqueductal grey project into ___________________________.
Definition
raphe magnus nucleus
Term
enkephail receptor activation blocks the release of ____________ or _______________
Definition
substance P; glutamate
Term
How does activation of enkephalin neuron cause analgesia?
Definition
by preventing the release of substance from primary nociceptor neuron in the dorsal horn. Therefore, it cannot depolarize the dorsal horn 2nd order neuron
Term
Which mu-receptor agonist is short acting and good for small procedures?
Definition
meperidine
Term
Fentanyl may be used as a patch and is _______________ times more potent than morphine
Definition
1,000
Term
_______________ is 4 times more potent than morphine
Definition
hydromorphone
Term
When you switch in a post-operative patient from IM form to a tablet form, you ____________ the dose of morphine
Definition
increase
Term
4 partial agonists of mu opioid receptors
Definition
1)codeine
2)oxycodone
3)hydrocodone
4)propoxyphene
Term
How does the potency of codeine compare to that of morphine?
Definition
it is not as potent (partial agonist).
Requires dosage of 130 mg vs. 30 mg of morphine
Term
How is codeine usually administered?
Definition
orally
Term
Buprenorphine is a ________________ that acts on more than one opioid receptor.
Definition
mixed agonist
Term
Mixed agonists of opioid receptors are sometimes used to treat opioid dependence. Why?
Definition
b/c the may act as antagonists or agonists on varying opioid receptors. This may help with treating withdrawal effects without completely removing the opioid ligand
Term
Name the most potent opioid receptor mixed agonist.
Definition
buprenorphin
Term
Name 4 opioid receptor mixed agonists:
Definition
1)buprenorphin
2)butorphanol
3)nalbuphine
4)pentazocine
Term
Why are opioids and NSAIDs synergistic?
Definition
NSAIDs block COX which increases the availability of arachidonic acid to be acted on by lipoxygenase.

*lipoxygenase products facilitate opening of K+-channels by opioids.
Term
Due to ______________, morphine is 2 to 6-fold less potent orally than parenterally
Definition
first pass metabolism
Term
Methadone is used in place of morphine when?
Definition
(long acting drugs) when less frequent dosing required
Term
remifentanil is used in place of morphine when?
Definition
For short, painful procedures – quick acting, fast-dissipating drugs
Term
7 additional routes of administration of opioid analgesics:
Definition
1)rectal transmucosal
2)epidural
3)subarachnoid
4)oral transmucosal
5)transdermal patch
6)iontophoresis
7)inhalation
Term
subarachnoid administration of opioid analgesics allows direct access to ____________ & ____________.
Definition
1)dorsal horn neurons
2)brain structures

*allows these drugs to act much longer than they do upon alternate administration routes
Term
3 drugs which may be administered through the subarachnoid: (opioid analgesics)
Definition
1)morphine
2)meperidine
3)fentanyl
Term
opioid analgesics administered as an epidural are usually introduced as an ______________.
Definition
infusion
Term
____________ uses an electrical current to push the medicine through the skin
Definition
iontophoresis
Term
In _____________________, Patient has limited control of dosing from infusion pump within tightly mandated parameters
Definition
PCA, patient controlled analgesia
Term
In ______________________, a catheter connected to a computer can monitor the opioid levels in the blood and can then maintain therapeutic levels of opioids in the blood.
Definition
Computer-Assisted Continuous Infusion (CACI)

*only used for patients emerging from unconsciousness in the ICU
Term
Why is morphine helpful in treating dyspnea? (2)
Definition
1)decreased peripheral resistance
2)increased capacity of peripheral vascular compartments
Term
Morphine is contraindicated in _____________________.
Definition
pulmonary edema due to respiratory disease
Term
2 opioids used to suppress cough reflex:
Definition
1)codeine
2)dextromethorphan (isomer of codeine analog methorphan; no analgesic or addictive properties)
Term
opioids directly inhibit __________ in the rhythm-generating respiratory center neurons in the Pre-Boetzinger complex
Definition
5HT4 receptors (serotonin receptors)
Term
In respiratory depression caused by opioids, what happens to the body's sensitivity to O2?
Definition
its unaltered, this may cause apnea
Term
BIM U8 + fentanyl =
Definition
analgesia without apnea
Term
10 adverse affects of opioids
Definition
1)sedation
2)depression of cough reflex
3)miosis
4)truncal rigidity (think highly lipid suloble opioids like fentanyl)
5)nausea & vomiting
6)euphoria
7)convulsion (due to inhibition of GABA release)
8)endocrine changes
9)constipation
10)reduced O2 consumption of myocardium
Term
3 drugs in coma cocktail:
Definition
1)Naloxone
2)thiamine
3)dextrose
Term
Naltrexone is an _______________
Definition
opioid antagonist
Term
what drugs work against neuropathic pain?
Definition
antidepressants
Term
5 examples of neuropathic pain:
Definition
1)Polyneuropathy
2)Postherpetic neuralgia
3)Trigeminal neuralgia (Tic doloreaux)
4)Glossopharyngeal neuralgia
5)Myelitis
Term
these drugs block serotonin reuptake and facilitate the action of the endogenous opioid analgesic system.
Definition
tricyclic antidepressants
Term
Name 3 tricyclic antidepressants:
Definition
1)IMIPRAMINE
2)AMITRIPTYLINE
3)DOXEPIN
Term
Name 4 anticonvulsants:
Definition
1)PHENYTOIN
2)CARBAMAZEPINE
3)GABAPENTIN
4)LEVETIRACETAM
Term
These drugs block Na-channel and prevent neuronal firing
Definition
anticonvulsants
Term
family of drugs that are 5HT 1D/1B agonists
Definition
triptans
Term
3 drug groups used to treat migraines
Definition
1)triptans (5HT agonists)
2)ergot alkaloids
3)NSAIDs or combo NSAIDs + opioids
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