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Analgesics and Anti-inflammatory
UMKC SOM Pharmacology
25
Medical
Graduate
11/25/2013

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Cards

Term
NSAIDs
MOA
PK
AE
DI
Definition
Ibuprofen, Naproxen, Indomethacin and Sulindac
Inhibit conversion of arachadonic acid, irreversibly inhibiting the enzyme cyclooxygenase
Analgesia (ceiling effect), anti inflame action (epigastric distress), platelet function
Inhibit production of the mucous layer
Use PPI to precent NSAID gastric ulcer
Nephrotox, increased Na and H2O retention
NSAIDs block ACE inhibitors, B Blockers,
Increase Warfarin anticoag
Term
Aspirin
MOA
PK
AE
DI
Definition
COX 1 inhibitor (a little COX 2 also)
Pain and platelet blocking
CNS- tinnitus, HSN, Uric acid excretion, Resp depression, *Reye syndrome (not for use in kids), GI symptoms
Term
Acetaminophen
MOA
PK
AE
DI
Definition
MOA unkown. No effects on platelets or bleeding time
Hepatic metabolism, conjugated with glucuronic acid and sulfuric acid
Both conjugates are excreted by the kidneys
N-acetylcysteine is an antidote for acetaminophen
No GI problems or DIs
Term
Naloxone
MOA
PK
AE
DI
Definition
Antidote for opioid poisoning. Short DOA
Get increase of NE release centrally with opioid WD
Term
MorphineMOA
PK
AE
DI
Definition
Analgesic gold standard
Hepatic metabolism with glucuronic acid conjugation
M6G is more potent than parent compound and undergoes enter-hepatic recycling. Half life is 2-3 hrs
Mets can accum in renal dx
H release: urticaria, pruritis, rare asthma exacerbation
Term
Heroin
MOA
PK
AE
DI
Definition
Morphine prodrug, crosses the BBB faster, lipid soluble
Rapidly met to MAM
Can cause euphoria by altering DA in the ventral segmental pathway
Anticholinergics can inc risk of constipation
Term
Pure Opiods
Definition
Morphine, heroin, codeine, meperidine, Methadone, oxycodone, fentanyl
Term
Codeine
MOA
PK
AE
DI
Definition
Low potency, used for antitussive uses
CYP 2D6 inhib can abolish the effects of codeine
High PO/IV ratio
Used for visceral pain, cough with pain
Term
Merperidine
MOA
PK
AE
DI
Definition
Not used much due to seizures and renal acc
Term
Methadone
MOA
PK
AE
DI
Definition
NMDA antagonist
High PO/IV ratio
Term
Oxycodone
MOA
PK
AE
DI
Definition
High ratio also
Term
Fentanyl
MOA
PK
AE
DI
Definition
Used as patch, or lollipop
Potency is 60 times more than morphine
DOA is 20-30 min
Resp ceiling at high doses
Term
Mixed Acting Opiods
Definition
Butorphanol, Tramadol,
Term
Butorphanol
MOA
PK
AE
DI
Definition
CNS actions include analgesia and sedation
Parenteral, nasal spray for migraines
Term
Tramadol
MOA
PK
AE
DI
Definition
Stim opiod Rs, block reuptake of 5HT3 and NE
Impaired renal funct results in decreased excretion of tramadol and its active met, M1. Dose Adj < 30 CrCL
Seizures in renal impaired
Term
Muscle Relaxants
MOA
PK
AE
DI
Definition
Cyclobenzaprine (TCAs, lots SEs)
Baclofen (GABA inhibit NT, spasticity from MS)
Diazepam (BZ blocks spinal polysynaptic pathways)
Dantrolene (direct acting skeletal muscle relax, blocks ca release from SR) - to tx MH
Term
Ergotamines
MOA
PK
AE
DI
Definition
inhibit the trigeminal nerve pathway
Serotonin 1B, 1D, 1F Rs
Not for pregnancy, lactation, ischemic disorders, CA vasospasm, uncontrolled HTN, liver kidney dx
Term
Triptans
MOA
PK
AE
DI
Definition
Agonist at the 5HT 1B/1D R
Burning at site, flushing, drowsiness, fatigue
CI'd with CAD, HTN
Term
MOA of Migraine tx
Definition
Vasoconstriction
Block release of vasoactive neuropeptides
Interrupt pain signal tm
Term
Migraine Prevention Meds
Definition
TCAs, B Blockers, Ca Ch blockers, anti-epileptic drugs
Term
Receptor subtypes
Definition
Mu1- supraspinal analgesia
Mu2- resp depression, CV, GI, spinal analgesia, miosis, phys dependence
Delta- spinal and supraspinal
Kappa- spinal, sedation, dysmorphic effects, mitosis, resp depression
Term
Kappa
Definition
morphine
Term
Delta
Definition
Meperidine, methadone, morphine, fentanyl
Term
Mu2
Definition
morphine, meperidine, fentanyl, methodone, buprenorphine
Term
Mu1
Definition
Morphine, meperidine, fentanyl, methadone, Buprenorphine
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