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Analgesic drugs
Pharmacology Module 3
147
Medical
07/14/2009

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Term
What is the most common type of pain?
Definition
nociceptive pain
Term
What type of pain involves conscious experience of noxious stimulus (mechanical, thermal, chemical) that has damaged nml tissue?
Definition
nociceptive pain
Term
Which stage of nociceptive pain involves tissue damage releasing sensitizing substances sucha s prostaglandins, bradykinin, substance p, and histamin, w/nn ending depolarization sending action potential to spinal cord?
Definition
transduction
Term
Which stage of nociceptive pain involves impulse to brainstem, then cortex via neurotransmitters such as substance p and glutamate?
Definition
transmission
Term
Which stage of nociceptive pain involves protective measures?
Definition
perception
Term
Which stage of nociceptive pain involves pain impulses charged or inhibited by release of endogenous opioids, serotonin, norepinephrine, and gaba?
Definition
modulation
Term
What is one of the most difficult pains to tx?
Definition
neuropathic pain
Term
What type of pain involves healing process- adaptive mechanism to prevent contact w/, or movmt of, injured area until healing complete? This involves chemical substances produced, such as prostaglandin 32 that sensitize nociceptive nn ending and make it hypersensitive to stimuli.
Definition
inflammatory pain
Term
What type of pain is caused by damage to the ns resulting in disturbance of function?
Definition
neuropathic pain
Term
Is neuropathic pain peripheral or central?
Definition
either, depending on lesion
Term
diabetes, hiv, trigeminal neuralgia, and phantom limb pain can cause what type of pain?
Definition
neuropathic pain
Term
What is a catch all term for pain where no neurologic or peripheral pathology is detected?
Definition
functional pain
Term
What type of pain is due to abnml responsiveness of ns?
Definition
functional pain
Term
Fibromyalgia, ibs, noncardiac chest pain cause what type of pain?
Definition
functional pain
Term
What are 3 types of non-opiopds?
Definition
acetaminophen, salicylates, nsaids (nonslecetive cox inhibitiors, cox-2 selective inhibitors)
Term
What are 3 categories of opiods?
Definition
agonists, partial agonists, antagonists
Term
What are 3 adjuvant agents for analgesia?
Definition
antidepressants, anticonvulsants, local anesthetics
Term
What are 2 alt names for acetominophen?
Definition
tylenol, paracetamol (europe)
Term
What is the moa of acetaminophen?
Definition
exact moa unknown.
Term
What is a weak inhibitor of cox enzymes 1 and 2 in peripheray and cox-3 in brain?
Definition
acetaminohpen
Term
what is an enzyme necessary for prostaglandin synthesis?
Definition
cox
Term
What are adrs of acetaminophen?
Definition
nmly safe in tx doses. no effect on bleeding time gi tract. potential for tubular necrosis w/chronic dosing
Term
When can tx doses cause acetaminophen toxicity?
Definition
tx dosing w/risk factors such as etoh- abuse, pre-existing liver disease, and other hepatotoxic drugs
Term
What is teh major pathway for acetaminophen toxicity?
Definition
conjugation w/metabolites and excreted in urine
Term
What is the minor pathway for acetaminophen?
Definition
p450 oxidation producing *toxic intermediate* which is detoxified by conjugation w/*gluthione*
Term
When does xs dose of acetaminophen cause toxicity?
Definition
conjugation of pathways saturated. gluthione stores in liver depleted. xs toxic metabolite binds to hepatocytes resulting in hepatic necrosis
Term
What is the antidote for actetaminophen od?
Definition
n-acetylcysteine (mucomyst) restores glutathione levels- best if given w/in 8 hrs of ingestion. give 140 mg/kg loading dose po diluted in juice followed by 70 mg/kg every 4 hrs x 17 doses
Term
What are dosage forms of acetaminophen?
Definition
capusles, tablets, suppositories, solns, drops. 80 mg, 160 mg, 325 mg, 500 mg (extra strength), 650 (arthritis strength)
Term
Why should parents be careful when administering acetaminophen to children?
Definition
drops versus liquid- different amts
Term
With what can acetaminophen be combined for perscriptions?
Definition
oxycodone (percocet, tylox), hydrocodone (vicodin) and codeine (tylenol #3)
Term
What doses should not be exceeded in adults, elderly, peds?
Definition
4 gm/day. 3 gm/day. 10-15 mg/kg q 4-6 hrs
Term
What term comes from the gk: 'juice', and refers to morphine-like drugs, natural or synthetic, agonist or antagonis that is used interchangeably w/the term narcotic?
Definition
opiods
Term
There are 20 different alkaloids, 10% morphine of what drug?
Definition
opiods
Term
What are endogenous peptides that modulate pain perception, including enkephalins and endorphins?
Definition
opiod receptors
Term
what are 4 types of opiod receptors?
Definition
kappa, mu, sigma, delta
Term
What is the range of differences w/opiod agonist's *pharmacodynamic activities*?
Definition
all have simialr pharmacodynamic activities. all stimulate mu (endorphin) receptor for analgesia. also cause respiratory depression, euphoria, constipation, and dependence.
Term
How are apparent differences in potency of opioid agonists explained?
Definition
by physiochemical and pharmacokinetic differences
Term
How can all opiods be made equianalgesic?
Definition
correcting for dose and route of administration (equianalgesic- change doses so effect is equal between 2 drugs)
Term
Are conversion factors for opiod agonists definitive rules or just guidelines?
Definition
just guidelines
Term
How does individual variation occur w/opiod agonist bioavailability?
Definition
individual variation in first pass metabolism and cross tolerance
Term
To what class of opioid agonist does morphine belong?
Definition
strong opioid agonists
Term
To what class of opioid agonist does oxycodone belong?
Definition
opioid agonists
Term
To what class of opioid agonist does oxymorphone belong?
Definition
strong opioid agonists
Term
To what class of opioid agonist does hydromorphone belong?
Definition
strong opioid agonist
Term
To what class of opioid agonist does meperidine (demerol) belong?
Definition
strong opioid agonist
Term
To what class of opioid agonist does fentanyl (duragesic) belong?
Definition
strong opioid agonist
Term
To what class of opioid agonist does methadone belong?
Definition
strong opioid agonist
Term
To what class of opioid agonist does codeine belong?
Definition
moderate to weak opioid agonist
Term
To what class of opioid agonist does propoxyphene (darvon) belong?
Definition
moderate to weak opioid agonists
Term
To what class of opioid agonist does tramadol (ultram) belong?
Definition
moderate to weak opioid agonists
Term
What opioid agonists are used for moderate to severe pain?
Definition
strong opioid agonists
Term
What opioid agonists are used for mild to moderate pain, heigher doses for severe pain will cause xs adverse effects?
Definition
moderate to weak opioid agonists
Term
What drug is the std that all opioids are compared to?
Definition
morphine
Term
What opiate involves 1st pass metabolism to water soluble active metabolites that are renally excreted?
Definition
morphine
Term
What is the parental: oral dose ratio for morphine for chronic v. acute pain?
Definition
1:3 for chronic pain. 1:6 for acute pain
Term
By what % is it necessary to reduce morphine dose in elderly or renal failure? Why?
Definition
25% due to accumulation of metabolites
Term
What opiate involves the greates variety of dosage forms?
Definition
morphine
Term
How can morphine be administered?
Definition
injection, immediate release (q4hrs)- tablets, capsules, soln, rectal suppositories, extended release
Term
What are the dose-lmting side effects of oxycodone?
Definition
no dose lmting side effects
Term
What is the potency of oxycodone relative to morphine?
Definition
equipotent
Term
How is oxycodone administered?
Definition
oral dosage form. immediate release, extended release (oxycontin), combined w/tylenol (percocet)
Term
When might dosage of oxycodone need to be reduced?
Definition
if CrCl<60 mL/min
Term
What are the problems with oxycodone?
Definition
cost, abuse of oxycontin
Term
Comparing hydromorphnoe (dilaudid) and morphine, which is shorter acting? which is more potent? how is hydromorphone administered?
Definition
hydromorphone shorter acting and more potent than morphine. poor oral potency.
Term
What is useful if pt is morphine tolerant? how is hydromorphone administered?
Definition
hydromorphone- dilaudid-hp, 10mg/ml injection. poor oral potency- available as rectal suppository. can be given subq
Term
What schedule is oxycodone?
Definition
C-II
Term
What is a synthetic opioid w/low oral bioavailability that is not useful as an oral agent?
Definition
meperidine (demerol)
Term
Does meperidien (demerol) have a long or short half-life?
Definition
short (3hrs)
Term
What is the bioequivalence of meperidine (demerol)?
Definition
morphine 10 mg iv = demerol 75 mg iv = demerol 300mg po
Term
What are the adverse rxns of meperidine (demerol)? Why?
Definition
toxic metabolite (normeperidine) renaly excreted. half life 16-30 hrs.. accumulation w/oral dose, renal dysfunction. can cause neurtoxicity, seizures.
Term
What is the t1/2 of normeperidine?
Definition
toxic metabolite of meperidine. t1/2=16-30 hrs
Term
With what type of drugs can meperidine (demerol) have drug interactions?
Definition
meperidine (demerol)
Term
What drug was approved by the fda in an oral dose in 2006?
Definition
oxymorphone (opana)
Term
What recently approved opiate has a black box warning?
Definition
oxymorphone (opana)
Term
To what other opioid is oxymorphone (opana) structurally related?
Definition
hydromorphone
Term
What percent bioavailability is involved w/oxymorphone (opana)?
Definition
10%
Term
What is the bioequivalence between oxymorphone (opana) and morphine?
Definition
10 mg = 30 mg morphine
Term
How is oxymorphone (opana) administered?
Definition
available as ir tablets 5 and 10 mg and er 1 12 hrs
Term
What drug has the following potential danges: currently heavily marketed and very expensive. if crushed and give iv may get equivalent of 100 mg morphine iv -> od. food increases peak plasma concentration by 50% and etoh- by 200%!`
Definition
oxymorphone (opana)
Term
What drug is 50-100x as potent as morphine?
Definition
fentanyl (sublimaze)
Term
How is fentanyl (sublimaze) available for anesthesi?
Definition
short acting injectable
Term
How can fentanyl (sublimaze) be administered oral transmucosally?
Definition
lozenge on a stick (actiq) for breakthrough cancer pain only
Term
What is available as an oral effervescent buccal tablet?
Definition
fentora also for breakthrough cancer pain
Term
What opiate involves 16 hrs for initial effect, lasts 2-3 days. calculate 24 hr morphine equivalent requirement. 60 mg/day im ms = 100 mcg/hr fentanyl. durageic-50 = $95/15 day. disposal problems?
Definition
transdermal (duragesic) for chronic pain- fentanyl
Term
What is the t1/2 of methadone?
Definition
synthetic opioid w/long t1/2 of up to 5 days
Term
What opioid is used in detox and maintentance programs- less acute withdroaw sx?
Definition
methadone
Term
What opioid has an analgesic duration only 8 hrs that accumulates w/repetitive dosing leading ot delayed side effects w/good oral potency?
Definition
methadone
Term
What is a methyl derivative of morphine?
Definition
codeine
Term
What opioid is usually combined w/non-opioid?
Definition
60 mg codeine=650 mg tylenol in analgesia. tylenol#3=30 mg codeine+300 mg tylenol
Term
What is the most common opiate rx right now?
Definition
hydrocodone
Term
Why is codeine dosing lmtd?
Definition
due to adr. n/v adn *constapation*. should not exceed 400 mg/day po
Term
What is the equivalence btwn codeine and morphine?
Definition
10 mg morphine 1v = 130 mg codeine iv = 200 mg codeine po
Term
What opioid also has antitussive action?
Definition
codeine
Term
What drug is similar to codeine but only available orally?
Definition
hydrocodone.
Term
What is the equivalence btwn hydrocodone and codeine?
Definition
hydrocodone 5 mg = codeine 30 mg
Term
Which has a higher abuse potential: hydrocodone or codeine?
Definition
hydrocodone
Term
With what drug is hydrocodone often combined?
Definition
combined w/acetaminophen. max acetaminophen (T) intake should be 4000 mg/day. vicodin, lortab. 500-750 mg T.
Term
What class are cough preparations of hydrocodone?
Definition
c-III
Term
What opioid is structurally related to methadone?
Definition
propoxyphene (darvon)
Term
What should be avoided w/chronic dosing of propoxyphene (darvon)?
Definition
accumulation of metabolite w/chronic dosing. t1/2=12 hrs, norproxyphene=24-36 hrs. norproxyphene is cardiotoxic. use caution in renal failure, elderly. dose ceiling due to adverse effects.
Term
To what opioid is propoxyphene (darvon) structurally related?
Definition
methadone
Term
What is darvocet-n100?
Definition
100mg PN + 650mg T
Term
How strong of an analgesic is propoxyphene (darvon)?
Definition
mild analgesic (65mg less than or equal to 650 mg T)
Term
To what is propoxyphene hcl 65mg equivalent?
Definition
propoxyphene napsylate 100 mg
Term
What is the statistical difference in pain intensity btwn T and T/propoxyphene combinatin?
Definition
no difference
Term
What is a synthetic analog of codeine?
Definition
tramadol (ultram)
Term
What is the unique analgesic activity of tramadol (ultram)?
Definition
binds weakly to mu-receptor, plus, inhibits serotonin and norepinephrine reuptake
Term
What are common adr of tramadol (ultram)?
Definition
common: nausea, dizziness, *cns excitation*/rather than sedation. increased *risk of seizure* at high doses or in pts w/head injury or takng drugs that lower seizure threshold
Term
What are some drug interactions of tramadol (ultram)?
Definition
met by cyp2d6 to active metabolite (prodrug). inhibitors of cyp 2d6 can lower analgesic effect. increased risk of serotonin sx (chest pain, tachycardia, htn, agitation) when combined w/ssri antidepressants or triptan drugs for migraine
Term
What is the depenence potential for tramadol?
Definition
potential for dependence but no dea restrictions for now
Term
What is the t1/2 of tramadol (ultram)?
Definition
5-9 hrs
Term
Which is more effective for acute pain: tramadol (ultram) or vicodin?
Definition
vicodin
Term
With what drug is tramadol available in combination?
Definition
tramadol (ultram)
Term
What opioid is a partial agonist-antagonist similar to pentazocine (talwin)? how is it delivered? for what is it indicated? How many doses per prescription?
Definition
butorphanol (stadol nasal spray) Partial agonist-antagonist
Similar to pentazocine (Talwin)
Transnasal delivery with onset and duration similar to IM
Indicated for migraine and postoperative pain
15 doses per spray pump
Term
What drug involves *immediate reversal of opioid effect*?
Definition
naloxone (narcan)
Term
What drug can ppt severe withdrawal sx if opioid dependent?
Definition
naloxone (narcan)
Term
What is a pure opioid antagonists displacing opioid from receptor site?
what is its t1/2? How is it administered?
Definition
naloxone. Long acting pure opioid antagonist
Approved for treatment of alcohol dependence
Duration of action = 24 hrs
Must be opioid free
12 week course lowers alcohol craving
Term
What is a long acting pure opioid antagonist approved for tx of etoh- dependence? What is the duration of action? How must it be formulated? What is the course and effect?
Definition
naltrexone. Long acting pure opioid antagonist
Approved for treatment of alcohol dependence
Duration of action = 24 hrs
Must be opioid free
12 week course lowers alcohol craving
Term
What is the most toxic effect of opioids?
Definition
respiratory depression. dose dependent, tolerance develops w/in 507 days of atc dosing
Term
what adverse effect of opioids precedes respiratory depression?
Definition
sedation
Term
What are 6 adrs of opioids?
Definition
Respiratory depression – most toxic effect
Dose dependent
Tolerance develops within 5-7 days of ATC dosing
Sedation
precedes respiratory depression
Constipation (can increase N&V)
Nausea and vomiting (vestibular)
Itching (histamine release)
Urinary retention
Term
What is the aim of opioid titration?
Definition
aim is to obtain and maintain opioid level which lies inside the tx window
Term
When opioid levels rise above upper parameter, how do pts feel? how do they feel when opioids drop below lower parameter?
Definition
hung-over. breakthrough pain.
Term
Which consequences of long term opioid tx requires increased dose for same analgesic effect- develops slowly w/chornic use?
Definition
tolerance and cross tolerance
Term
What consequence of long term opioid x involves natrual process that develops w/chronic use and time course function of opioid t1/2?
Definition
physical dependence and withdrawl
Term
What consequence of long term opioid tx involves dysfunctional pattern of use for purposes other than alleviation of pain, w/tolerance and dependence not necesarily present?
Definition
addiction
Term
What consequence of long term opioid tx involves pts w/severe unrelenting pain preoccupied w/obtaining opioids?
Definition
pseudoaddiction
Term
What are 8 sx of opioid physical dependence and withdraw?
Definition
Begins within 6 hrs and peaks in 36-48 hrs
Rhinorrhea – runny nose
Lacrimation – tearing
Hyperthermia, chills
Myalgia – muscle aches
Emesis, diarrhea, GI cramping
Anxiety, agitation, hostility
Sleeplessness
Term
What is a preprogrammed basal iv dose, self-bolus dose, and lock-out period?
Definition
pt controlled analgesia (pca)
Term
What alt opioid delivery technique usually involves fentanyl + analgesic?
Definition
epidural
Term
What alt opioid delivery technique is for labor?
Definition
pt controlled epidural analgesia
Term
Mrs. Jones has been receiving hydromorphone via PCA pump at a dose of 0.5 mg/hr after surgery to correct spinal stenosis. Her pain has been well controlled on this dose and her attending physician wants to discharge her on controlled-release morphine (MS Contin). What would be an appropriate dose?
Definition
HM 0.5 mg/hr IV = HM 12 mg/24 hrs IV
HM 12 mg/24 hrs IV = MS 80 mg/24 hrs IV
MS 80 mg/24 hrs IV = MS 240 mg/24 hrs PO
Recommend MS Contin 120 mg q12 hrs
Term
What schedule are heroin and lsd?
Definition
schedule I
Term
On what are schedules of controlled substances based?
Definition
based on potential for abuse and depenence
Term
Which schedule of controlled substances involves morphine, codeine, oxycodone, and amphetamines?
Definition
schedule II
Term
Which schedule of controlled substances involved Tw/codeine or hydrocodone?
Definition
schedule III
Term
Which schedule of controlled substances involves benzodiazepines, phenobarbital, chloral hydrate, and propoxyphene?
Definition
shedule IV
Term
What schedule of controlled substances involves narcotic cough/antidiarrheal meds?
Definition
schedule v
Term
What schedule of controlled substances involves all other rx drugs?
Definition
schedule vi
Term
Which schedule involves the following: DEA number required.
Written prescription required, except in emergency.
Emergency prescription:
Amount to last through emergency.
Written prescription mailed to dispenser within 7 days. Otherwise DEA notified by pharmacy.
“Authorized for emergency dispensing” must be written on prescription.
No refills. Not valid after 6 months.
Definition
schedule ii
Term
Which schedule involves the following: Refills allowed. Up to 5 refills or 6 months (whichever comes first) for schedule III-V.
DEA # required.
May be “called in” to pharmacy.
Definition
schedule iii-V
Term
What are agents that are indicated for conditions other than pain, but have analgesic properties for some painful conditions?
Definition
adjuvant
Term
What agents are: Primarily for neuropathic pain
MOA: block Na+ and Ca+ ion channels, enhance GABA, and block NMDA receptors
Gabapentin (Neurontin)
Somnolence, dizziness, and fatigue
900-1800 mg/day?
Definition
antiepileptic agents
Term
Which class of drugs involve amitryptyline (elavil)?
Definition
tricyclic antidepressants (TCA's). also ssri's
Term
What type of drugs are the following: Injectable glucocorticoids
Topical anesthetics
Lidocaine patch (Lidoderm)
Capsaicin
Definition
adjuvant analgesic agents
Term
What is used as an analgesic for mild to moderate pain, antipyretic, however has no anti-inflammatory activity (not an nsaid)?
Definition
T
Term
i
Definition