Medications from Acute Pain Flashcards
Hydrocodone + Tylenol (3)
Norco, Lortab, Vicodin
Dolophine
Methadone
MsContin, Kadian, MSIR
morphine
Percocet
oxycodone + acetaminophen
Percodan
oxycodone + aspirin
Controlled-released oxycodone is called
oxycontin
3-Methoxymorphine is ____
codeine
derived from opium poppy
Codeine is metabolized (CYP450) into two things:
10% morphine (active)
the rest into inactive norcodeine
if children 12 years or younger receive this medication, they can experience side effects w/o analgesia dt immature enzymes in the liver
codeine
Dose: (adult)
30-60 mg q 4hrs, max 360 mg/day
Codeine
Pediatric dosing for codeine
0.5-1 mg/kg
max 60 mg/dose
What is the ceiling effect dose for codeine?
60 mg
Opioids, alcohol, and anticholinergics interact with ______
codeine
Contraindications for codeine (4)
- hypersensitivity
- acute/chronic ashtma
- respiratory depression
- paralytic ileus
codeine works on what receptors
mu, kappa, delta
side effects include: N/V, brady, hypotension, respiratory depression, urinary retention, constipation, dizziness, miosis
synthetic 4-phenylpiperidine analogue of morphine and codeine
Tramadol
Tramadol is a racemic mixture of two enantiomers + & -
+ enanatiomer is centrally acting opioid agonist with moderate affinity to ____ receptor, weak affinity to ____ & ___, and opposes _____ reuptake
strong affinity: mu
weak: kappa and delta
opposes serotonin reuptake
Tramadol is a racemic mixture of two enantiomers + & -
( — )enantiomer inhibits _____ reuptake and stimulates _____ receptors
inh. norepinephrine reuptake
and stimulates alpha 2 receptors
Tramadol is metabolized by CYP450 into ______
o-desmethyltramadol
o-desmethyltramadol 2-4x more potent or weaker than Tramadol?
Potent
What is Tramadol’s potency compared to morphine?
1/5- 1/10s the potent to morphine
Tramadol’s onset PO
1-2 hrs
Tramadol’s protein binding
20%
Tramadol is contraindicated in patients that have what?
seizure disorders
T/F:
tramadol causes respiratory depressioin
false: minimal
T/F:
Tramadol is not associated with dependence, tolerance, or addiction
True
T/F:
Tramadol causes constipation
F: minimal
T/F:
Tramadol does not cause N/V
F: high incidence of N/V
Oral dose of Morphine is about ___x higher than IM or IV
3
Morphine primarily acts on what receptors
Mu 1 and Mu 2
This drug’s primary pathway for metabolism is conjugation with glucuronic acid in hepatic and extrahepatic sites, especially the kidney
Morphine
Morphine gets metabolised into two substances
morphine-6-glucuronide
morphine-3-glucuronide
T/F:
morphine-3-glucuronide contributes to analgesia
F: morphine-3-glucuronide causes adverse effects such as neurotoxicity and hyperalgesia
morphine-6-glucuronide contributes to analgesia
Morphine’s absorption into the CNS is minimal dt 3 things:
1.poor lipid solubility (morphine hydrophilic)
- high protein binding (35%)
- high degree of ionization at physiologic pH
Morphine IM
onset: ____
peak: _____
onset: 15-30 mins
peak: 45-90 mins
Women vs men
who has a greater analgesic potency and slower speed of offset with morphine
women
Morphine is contraindicated in what patients and why?
renal impairment dt metabolite morphine-6-glucuronide causing respiratory depression
______ is a semisynthetic derivative of thebaine
oxycodone
oxycodone has recently replaced ____ as the most used opioid worldwide
morphine
oxycodone can be made alone or combined with 3 things and has many names
acetaminophen (Percocet), aspirin (Percodan), and ibuprofen (Combunox)
This drug is used to tx neuropathic pain syndrome and to treat acute/chronic pain
oxycodone
controlled release oxycodone is called?
Oxycotin
Oxycodone is mainly a prodrug and is metabolized into two forms ___ & ____
(active) Oxymorphone
(inactive) noroxycodone
What receptors do oxycodone work on
Mu and Kappa
How is oxycodone metabolized and excreted?
Cype 450 (2D6) and excreted in the urine
T/F:
Oxycodone has an extensive first pass effect
true
Oxycodone (PO)
onset:
duration: IR & CR
onset: < 1hr
duration: IR 3-4 hrs
duration: CR: 12 hrs
Oxycodone dose PO
10-15 mg of oxycodone is equal to 10 mg Morphine
Protein binding of oxycodone
45%
T/F
Oxycodone can only be given PO
F: can be giving both IV/ PO (PO most common)
T/F: oxycodone doesn’t cause histamine release
F: oxycodone causes histamine release
This drug is a synthetic broad-spectrum opioid that has become the maintenance drug for opioid addiction due to its oral bioavailability (60-95%) high potency, and long duration of action
Methadone
What receptors does methadone work on?
weak non-competitive NMDA antagonist, serotonin reuptake inhibitor, monoamine transmitter reuptake inhibitor, and affinity for the mu- receptor
How is methadone metabolized and does it have an active metabolites?
metabolized by the liver CYP450 and only has inactive metabolites
What effect does carbamazepine have on methadone’s metabolism?
carbamazepine (anticonvulsant/ (Tegretol®)* ) is a CYP450 inducer, so it lowers the concentration of the drug in the bloodstream
What effect do antiretroviral agents and grapefruit have on methadone’s metabolism?
inhibit CYP45, so metabolism is reduced so the concentration of the drug is higher in the bloodstream
Does hepatic and renal impairment influence the clearance of methadone significantly?
No
Steady-state of methadone may take up to ____ days, dt extensive redistribution of the drug
10
The morphine/methadone equianalgesic ratio appears to be curvilinear:
3:1 at morphine doses < ___ mg/day
20:1 at morphine doses > ___ mg/day
3:1 at morphine doses < 100 mg/day
20:1 at morphine doses > 1000 mg/day
Methadone dose: PO/IM/SC
2.5-10 mg q4-12 hrs
Methadone has a high variable half-life pt to pt so dosing guidelines are unachievable.
Half-life range: ___ - ____
8-80 hours
“ * one time dose of 10 mg, you can guess about 12-24 hours of pain relief”
ciprofloxacin, diazepam, and ethanol (acute use) have what effect of methadone?
increase concentration/effect
Amprenavir, phenobarbital, phenytoin, rifampin (abx), MAOIs have what effect of methadone?
decrease concentration/effect
MAOIs have an unpredictable reaction with MAOIs
Methadone S/E includes: 4
hypotension, respiratory depression, sedation, confusion
This medication rarely cause these side effects:
pause-dependent dysrhythmia associated with bradycardia *, QT prolongation *, and torsades
methadone
____ is a phenylpiperidine-derivative synthetic opioid agonist that is structurally related to meperidine (demeral)
Fentanyl
This drug has high potency, rapid onset of action and short duration of action
fentanyl
Extensively metabolized by N-demethylation and produces ____, ____, ____
norfentanyl
hydroxyproprionyl-fentanyl
hydroxyproprionyl-norfentanyl
____ is the principal metabolite of fentanyl and is excreted by the kidneys
Norfentanyl and is structurally similar to normeperidine
This drug’s elimination is slightly prolonged despite a short duration of action due to the _____ serving as a large inactive reservoir
Fentanyl
lungs: large inactive reservoir
Why does fentanyl have a greater potency and more rapid onset compared to morphine?
lipid solubility
Fentanyl is lipophilic while morphine is hydrophilic
Where does 75% of first-pass effect occur for fentanyl?
lungs
what is the % protein binding for fentanyl?
84%
____: is a semisynthetic drug and hydrogenated ketone of analogue of morphine and can be formed by N-demethylation of hydrocodone
Hydromorphone
this drug is an effective alternative to morphine for tx of moderate to severe pain. Available in PO, IV, and rectal
Hydromorphone
How much stronger is hydromorphone than morphine when administered orally?
3-5x stronger
How much stronger is hydromorphone than morphine when administered parenterally?
8.5x stronger
Hydromorphone is metabolized in the liver to ____
hydromorphone-3-glucuronide (active)
Does hydromorphone-3-glucuronide have analgesic effects?
No, it lacks analgesic effects but may be an active metabolite that potentiates neurotoxic effects: allodynia, myoclonus, and seizures
luckily production of this product is low unless pt has renal insufficiency
Hydromorphone:
Parenteral dose for postoperative pain ____ mg every ___ -___ mins, titrated to achieve a balance btw pain relief and respiratory depression
dose: 0.2 mg
Q 3-5 mins
Duration of action for hydromorphone
3-4 hours
(same of IR of oxycodone)
Oral dose of hydromorphone
2-8 mg
____ a semi-synthetic opioid which is a codeine derivative
hydrocodone
how much stronger is hydrocodone to codeine?
6-8x stronger
Hydrocodone is commonly paired with ______
acetaminophen
Norco concentration
Norco: 5mg hydrocodone w/ 325 mg tylenol
Vicodin concentration
Vicodin: 5mg hydrocodone w/ 500 mg tylenol
Lortab concentration
Lortab: 7.5mg hydrocodone w/ 325mg tylenol
This drug is the second most abused prescription behind oxycodone
hydrocodone
The liver metabolizes hydrocodone and produces 2 metabolites: ___ & ____
hydromorphone (active)
Norhydrocodone (inactive)
30 mg of hydrocodone = ___ mg of morphine
10 mg of morphine
dose range of hydrocodone:
___ -____ mg hydrocodone w/ ___-___ mg of acetaminophen q4-6 hrs
2.5-10 mg of hydrocodone w/
300-750 mg of acetaminophen
4g max tylenol in 24 hrs
These side effects are for what drug:
meiosis, histamine release, pruritus, decreased hypercapnia drive/ RR, airway reflexes, bradycardia, hypotension, NV
hydrocodone
____: a semi-synthetic agonist-antagonist opioid derived from the opium alkaloid thebaine
Buprenorphine
Buprenorphine
partial agonist @ __ receptor
antagonist @ ___ receptor
and a weak ___ receptor agonist
partial agonist @ mu receptor
antagonist @ kappa receptor
and a weak delta receptor agonist
T/F: Burprenorphine
has less respiratory depression, less immune suppression, no accumulation in patients with renal function
True
What is Subutex
buprenorphine
What is the metabolite of buprenorphine?
Norbuprenorphine
What receptors do norbuprenorphine act on?
full agonist at mu, delta, and ORL-1
partial agonist at Kappa
Does Buprenorphine’s metabolite have more or less effect on respiratory depression?
Norbuprenorphine has extremely little antinociceptive potency but markedly increased respiratory depression (10fold)
Buprenorphine
____ mg = 10 mg of morphine
0.3 mg
Oral administration of buprenorphine results in high first-pass metabolism and can be bypassed by sublingual
sublingual administration –> onset of _____ mins
duration of ___-___ hrs
sublingual
onset: 30 mins
duration 6-9 hrs
Does renal impairment affect the elimination of buprenorphine?
No mainly hepatic elimination so there is little risk of accumulation with renal impairment
This drug can be resistant to antagonism with naloxone
buprenorphine
other name for phenytoin
Dilantin
other name for carbamazepine
tegretol
other name for Topiramate
Topamax
other name for baclofen
lioresal
other name for carisoprodol
soma
other name for cyclobenzaprine
flexeril
other name for Methocarbamol
robaxin
other name for Tizanidine
Zanaflex
Opioid conversion: Morphine
parenteral: 10 mg
Oral:
Oral: 30 mg
Opioid conversion: Hydromorphone
parenteral: 1.5 mg
Oral:
Oral: 7.5 mg
Opioid conversion: Oxycodone
Oral:
Oral: 20-30 mg*
parenteral: —-
Opioid conversion: Codeine
parenteral: 130 mg
Oral:
Oral: 200 mg
Opioid conversion: Hydrocodone
parenteral: —–
Oral:
parenteral: —–
Oral: 30 mg
Opioid conversion: Methadone
parenteral: 1.5-2.5
Oral:
Oral: 3-5 mg
Opioid conversion: Fentanyl
parenteral:
oral: —-
parenteral: 0.1 mg
oral: —-
