Mechanisms of action Flashcards
irreversibly (covalent), non-selectively inhibits COX, reducing PG and TXA2 synthesis
Aspirin (ASA)
inhibits COX and PG synthase
Acetaminophen
enhances 5-HT release (which attenuates pain mediator generation) and regulates body temperature by acting centrally
Acetaminophen
A_____ acts centrally whereas A______ acts peripherally in pain relief
Acetaminophen, Aspirin
Selectively, reversibly (non-covalent) inhibits COX-2 and reduces PG synthesis
Celecoxib
which two opium alkaloids are synthetic?
Hydrocodone and Heroin
which two opium alkaloids are naturally occurring?
Morphine and Codeine
Act through G-protein coupled Mu, Delta, Kappa opioid receptors, stimulate prolactin and growth hormone release
Hydrocodone/Acetaminophen
Hyperpolarization with Hydrocodone/Acetaminphen is caused by outflow/decrease in _____ and increase/influx of _____
Potassium (K+); Chloride (Cl-)
central acting synthetic opioid
Tramadol
agonist selective for mu receptors and weak inhibitor of NE/5-HT reuptake
Tramadol
unilateral, pulsating, lasting 2-72 hours
Migraine
behind or around one eye, excruciating, sharp pain, lasting 15-90 minutes
Cluster headaches
bilateral around head, dull/persistent, driven by stress, up to 7 days per episode
Tension headaches
prophylactic migraine therapy
Topiramate
acute migraine attack therapy
Triptans (e.g. sumatriptan), Ergotamines
B-blockers cause ______ of blood vessels and trycyclin antidepressants cause an ____ in serotonin levels for prophylaxis migraine therapy
vasoconstriction; increase
selectively activates vascular serotonin 5 HT-1 receptors
Sumatriptan
stimulates neuronal serotonin receptors, decreasing the release of peptides substance P and CGRP
Sumatriptan
which migraine drug is structurally similar to biogenic amines?
Ergotamine
which migraine drug inhibits CN-V pain transmission?
Ergotamine
which migraine drugs stimulate serotonin receptors producing intracranial vasoconstriction?
Sumatriptan, Ergotamine
drug that blocks voltage-gated sodium channels, inhibits carbonic anhydrase, and antagonizes glutamate receptors
Topiramate
augments GABA activity and stimulates Cl- channel and which causes hyperpolarization
Topiramate
in coagulation, the ____ pathway affects the ____ of vit K dependent coagulation factors
extrinsic; synthesis
in coagulation, the ____ pathway affects the _____ of coagulation factors
intrinsic; activation
the ____ pathway is more important to the coagulation process and the ____ pathway is more important to the inflammation pathway
extrinsic; intrinsic
factor __ is common to both extrinsic and intrinsic coagulation pathways
X
factor X cause conversion of ____ to _____
prothrombin to thrombin
thrombin causes conversion of _____ to ______
fibrinogen to fibrin
which drug inhibits ____ of oxidized vitamin K which prevents activation of factors __, __, __, ___ which are in intrinsic, extrinsic, and common pathways?
reduction; II, VII, IX, X; coumadin
fractionated low molecular weight heparin in ____ binds to antithrombin which causes _____ inactivation of clotting factor __a and __a and ____ inhibits coagulation
Enoxoparin; irreversible; Xa; IIa (thrombin); indirectly
which is predictable and safer- enoxoparin or heparin?
Enoxoparin- it has a longer half life, less bleeding, and can be done outpatient
which anti-hemolytic has NO antidote?
Rivaroxaban
binds to the active site of factor Xa which inhibits coagulation
Rivaroxaban
The 5 platelet stimulating agents that activate GP IIa/IIIb receptors for thrombus formation are?
TXA2, ADP, thrombin, serotonin, collagen
ADP receptor blocker that IRREVERSIBLY blocks ___ dependent activation of GP receptor is what drug?
calcium; Clopidogrel
