Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
66 Cards in this Set
- Front
- Back
Histimine causes what
|
dilation of blood vessels allowing phagocytes to migrate to area
|
|
Cause of pain?
|
1. Increased tissue pressure
2. Actions of inflammatory mediators |
|
How is phagocytosis initiated
|
Opsonins molecule adaptors
→Coat foreign surfaces and SIGNAL leukos that a particle should be attacked |
|
Phagocytic cell with opsonized particle leads to
|
engulfment and destruction of agent
|
|
The cyclooxygenase pathway leads to the formation of what
|
1.PGH2 – Used to synthesize prostaglandins (PGE2 and PFF2 alpha)
2.Prostacyclin 3.Thromboxanes (TxA2) |
|
Prostaglandins, PGE2, PGf2 acts where
|
smooth muscle,
|
|
PGE2?
|
inflammation and fever
|
|
what is Thromboxane (TxA2)
|
Chief eiconsanoid product of platelets
→POTENT VASOCONSTRICTOR and PROMOTER of PLATELET ADHESION and AGGREGATION |
|
Prostacyclin (PGI-2) acts where and does what?
|
Primary eiconsanoid product of vascular endothelium. Functions as a VASODILATOR, VENODILATOR, INHIBITOR OF PLATELET AGGREGATION
|
|
What is critical in regulation of systemic blood pressure and thrombogenesis
|
Local balance of TxA2 and PGI-2
|
|
Housekeeping actions of COX 1
|
1. Vascular homeostasis
2. Maintenance of Renal and GI blood flow 3. Renal Function 4. Intestinal Mucosal Proliferation 5. Platelet Function 6. Antithrombogenesis |
|
As needed functions of COX 2
|
Inflammation, Fever, Pain, Transduction of Painful Stimuli in Spinal Cord, Mitogenesis, Renal Adaptation to Stresses, Deposition of Trabecular bone, Ovulation, Placentation, Uterine Contractions of Labor
|
|
ACETAMINOPHEN MOA
|
Believed to inhibit synthesis of prostaglandins in CNS (COX-3?)
→Works peripherally to inhibit pain impulse generation |
|
ACETAMINOPHEN used to TX
|
Mild pain/febrile conditions
|
|
What does acetaminophen lack?
|
anti-inflammatory effects, antiplatelet effect and GI Toxicity
|
|
Majore acetaminophen SE? how do you avoid this?
|
HEPATOXICITY***** in overdosage
→Avoid or use lower daily dose in older adults and patients with risk for hepatoxicity such as: ALCOHOLICS & MALNOURISHED |
|
What does acetaminophen interact with?
|
INTERACTIONS WITH WARFARIN→Prolongs INR and CYP-450 inducing drugs
|
|
SALICYLATES (Aspirin: Bayer, Ecotrin) MOA
|
Irreversibly inhibits platelet function for the life of the platelet (7-10 days)
|
|
Salicylate effects
|
anti-inflammatory, analgesic, antipyretic, anti-platelet
|
|
Salicylates anti-inflammatory effects due to
|
reduced synthesis of eicosanoid mediators
|
|
Salicylates analgesic effects?
|
Peripherally and at site of inflammation and at Sub-cortical sites
|
|
Salicylates antipyretic effects?
|
1.Vasodilation (Heat dissipation)
2.Antagonizes pyrogen induced prostaglandin production 3.Blocks CNS response to Interleukin 1 (by macrophages) |
|
Salicylates anti-platelet effects?
|
inhibition of thromboxane synthesis
|
|
Uses of salicylates?
|
1.Relief mild to moderate pain
2.High Dose- Significant anti-inflammatory properties 3.RA 4.Inflammatory Joint Diseases 5.Antipyretic 6.Antiplatelet: • Decrease TIAs • Unstable Angina • Reduce CABG thrombosis • Reduce Coronary artery thrombosis |
|
***BEST DRUG FOR* REDUCING FEVER!!!****
|
salicylates
|
|
Salicylates CNS SE?
|
1. Tinnitus
2. Decreased Hearing 3. Vertigo 4. Hyperpnea (Inc. RR) |
|
AT low levels, what metabolic SE does salicylates have
|
Respiratory Alkalosis secondary to increased ventilation
|
|
Accumulation of salicyclic acid can cause what
|
met. acidosis
|
|
GI effects of salicylates?
|
1.Gastric mucosal irritation (Undissolved tab)
2.GI bleeding associated with erosive gastritis due to inhibited prostaglandins |
|
Concurrent use of what meds lead to inc. Salicylate SE
|
glucocorticoids, anticoagulants
|
|
REnal Salicylate SE? why does this occur
|
Reversible decrease in GFR (secondary to arteriolar vasoconstriction)
|
|
Why may hypersensitivity reactions occur with salicylates
|
Aspirin induced asthma (Due to leukotriene synthesis)
|
|
When may Reye syndrome occur?
|
aspirin Use in children during/following viral infection can cause Reye Syndrome
|
|
What are PROPIONIC ACID DERIVATIVES
|
Ibuprofen
Naproxenn (Naprosyn, Aleve), Ketoprofen (Orudis, Oruvail), Flurbiprofen (Ansaid) |
|
what are propionic acid derivatives used for
|
Potent analgesic used in:
1. RA 2. OA 3. Ankylosin Sponylitis 4. Gout 5. Primary Dysmenorrhea |
|
Compare propionic acid derivatives compared to aspirin?
|
→Less frequent GI irritation/Bleed than aspirin
→Platelet effects are REVERSIBLE for all non selective NSAID’s except Aspirin |
|
Propionic acid derivatives CI
|
1. Nasal Polyps
2. Angioedema 3. Aspirin Sensitivity |
|
How can propionic acid derivatives Can alter cardioprotective effect of low dose aspirin
|
competing for binding sites
|
|
Naproxenn (Naprosyn, Aleve) features
|
Longer Half Life, 20 Times more potent than aspirin, Less Severe GI effects than aspirin
|
|
Ketoprofen (Orudis, Oruvail) features
|
25 mg dose comparable to 400 mg of ibuprofen
|
|
Flurbiprofen (Ansaid) featues
|
Can be used as a topical ophthalmic for inhibition of intra-operative miosis
|
|
ACETIC ACID DERIVATIVES MOA
|
Besides inhibiting cyclo-oxygenase, many AAD’s promote unesterified AA into triglyceride reducing substrate for Cyclooxygenase and lipoxygenase
|
|
types of ACETIC ACID DERIVATIVES?
|
Indomethacin (Indocin), Sulindac (Clinoril), Etodolac (Lodine), Diclofenac (Voltaren), Ketorlac (Toradol)
|
|
Indomethacin (Indocin) MOA and use
|
Direct inhibitor of neutrophil motility
→Specific use in promoting closure of PDA in newborns by inhibiting vasodilatory eicosanoids PGE2 and PGI-2 |
|
Indomethacin (Indocin) SE
|
GI and CNS adverse effect more severe than other NSAIDs
|
|
Sulindac (Clinoril
|
More frequently implicated in HEPATOXICITY than other NSAIDs
|
|
Etodolac (Lodine)
|
200 mg dose comparable to effect of 400mg ibuprofen
|
|
Diclofenac (Voltaren)
|
More potent anti-inflammatory than indomethacin and naproxen, Used widely in treatment of pain associated with RENAL STONES
|
|
How is Diclofenac available
|
topical patch for pain due to trauma and gel for painful joints
|
|
Ketorlac (Toradol) use and forms available
|
Strong analgesic properties particular for post-surgical patients, AVAILABLE AS IV FORMUALTION
|
|
Ketorlac (Toradol) SE
|
RENAL TOXICITY- Limit use to 3-5 days
|
|
Examples of OXICAM DERIVATIVES
|
Piroxicam (Feldene), Meloxicam (Mobic)
|
|
Piroxicam (Feldene) MOA
|
As effective as other NSAIDs but may be better tolerated
→Modulates neutrophil function by inhibiting collagenase proteoglycanase and oxidative burst |
|
Piroxicam (Feldene) pharmokinetics
|
Long half life, may be administered once daily
|
|
Meloxicam (Mobic) MOA and AE
|
Reported to be more COX-2 selective at low dose, Overall adverse effects similar to other NSAIDs
|
|
KETONE NSAIDs: Nabutemone (Relafen) MOA
|
Prodrug
Reported to be comparatively COX-2 selective at low dose |
|
KETONE NSAIDs: Nabutemone (Relafen) AE and pharmkinetics
|
Overall Adverse effects when dosed in the usual range are similar to NSAIDs
May give once or twice daily |
|
What are the COX-2 SELECTIVE INHIBITORS
|
Celecoxib (Celebrex)
Refecoxib (Vioxx) (withdrawn) Valdecoxib (Bextra) (withdrawn) Celecoxib (Celebrex |
|
COX-2 effects? what do they NOT effect?
|
100 x greater COX-2 selectivity
1.Anti-inflammatory 2.Antipyretic 3.Analgesic NO anti-platelet effect |
|
COX 2 AE
|
Increased THROMBOGENICITY (Prolonged inhibition of vascular COX-2 with endothelial cells→PGI-2)
|
|
COX 2 NSAIDS has reduced what
|
GI tox
|
|
Refecoxib was withdrawn in 2004 due to what
|
increased thrombogenicity with prolonged use→ MI & STROKE
|
|
What is celecoxib used for
|
Approved for OA, RA and juvenile RA (OVER 2 Y/O)
Ankylosing Spondylitis, Acute pain in adults, primary dysmenorrhea Reduction of adenomatous colorectal polyps in FAP. |
|
What is celecoxib an option for
|
patient requiring chronic NSAID use with risk of gastropathy
|
|
increased risk of what with celecoxib?
|
fatal and dose dependent C/V thrombotic events (STROKE) as well as
1.Hypertension 2.Edema 3.Heart Failure |
|
Celecoxib is CI in what
|
Treatment of pain with CABG
|