Term
| Describe the Arachadonic Acid Cascade in brief |
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Definition
Cell membranes have phospholipides removed by Phospholipase A2, creating arachidonic acid.
Can form either leukotries via Lipoxygenases or Thrombaxanes and Prostaglandins via Cycloxygenasases (COX-1 & COX-2) |
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Term
| What are some substances that cause pain? |
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Definition
| Potassium, Serotonin, Bradykinin, Histamine, Prostaglandins, Leuoktrienes and Substance P |
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Term
| Which Prostaglandins mediate inflammation/fever? |
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Definition
PGE2 and PGI2
Cause Erythema, Edema and increase local blood flow.
Fever is a result of increase PGE2 in the hypothalamus. |
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Term
| Describe how Prostaglandins affect Renal Function |
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Definition
Increase renal blood flow
Increase glomerular filtration rate
Cause renal vasodilation
Increased excretion of Na+, K+ and H2O |
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Term
| How do Prostaglandins affect GI function? |
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Definition
Promote secretion of mucus
Inhibit the acid secretion |
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Term
| Hematological function of Prostaglandins? |
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Definition
PGI2 inhibites cell aggregation (antithrombogenic)
TXA2 induces platelet aggregation (thrombogenic)
TXA2 also most potent vasoconstrictor known. |
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Term
| Can NSAIDS cause both thrombogenic and antithrombogenic effects? |
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Definition
Yes, it is dose dependent.
Low Dose = antithrombotic via TXA2 synthesis inhibition
High Dose = thrombotic via prostacyclin synthesis inhibition |
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Term
| What are some of the Anti-inflammatory/Analgesic Agents |
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Definition
Salicylates
Para-aminophenol derivitives
Proprionic Acid derivitives
heteroaryl acetic acids
enolic acids
indole and indene acetic acids
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Term
| What are the general characteristics of most NSAIDS? |
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Definition
Inhibit Cyclooxygenase
Analgesis, Anti-inflammatory, Antipyretic, Antiplatelet (4A's)
absorbed via stomach & small intestine
highly plasma bound
metabolized by liver and excreted via kidney |
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Term
| What are the contraindications for most NSAIDS? |
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Definition
Asparin Hypersensativity
Liver or kidney dysfunction
alcoholism, smoking (contribute to ulcers)
caution during pregnancy and breast feeding |
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Term
What drugs fall into the Salicylate family?
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Definition
Salicylic acid
Asparin (acetyl salicylic acid)
Difunisal |
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Term
Aspirin
Actions, MOA, Dangers |
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Definition
Action = all 4 A's
Stimulates respiration via uncoupling oxidative respiration, causes stmulation of medullary repsiratory center
Leads to alteration of acid-base equilibrium
MOA: irreversible inhibition of cyclooxygenase |
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Term
| Indications for aspirin use |
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Definition
| Pain, Fever (both pyrogen induced and CNS response), inflammation and cardiac conditions to reduce blood clotting |
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Term
|
Definition
CNS: tinnitus, vertigo, confusion/delirium
GI: nausea & emesis, ulceration w/bleeding
Hepatotoxicity: comes with prolonged high doses or viral infection |
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Term
| Contraindications for Aspirin |
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Definition
Hypersensativity, chronic liver diseas, gout, peptic ulcer
hemophilia or vitamin K deficiency
diabetes, chickinpox or influenze in children (Reyes Syndrome) |
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Term
| What as aspirin OD called? What are signs of mild toxicity and major toxicity? |
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Definition
OD called Salicysm
Minor: headache, dizziness, tinnitus, confusion, drowsiness, sweating, thirst, hyperventilation, nausea, emesis, diarrhea
Major: generalized convulsions, skin eruptions, alterations in acid-base balance, fever and dehydration, hyperpyrexia, sweating, vomiting and lost of water vapor due to hyperventilation |
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Term
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Definition
| Induce emesis, gastric lavage, activated charcoal, hydrate and attempt to correct acid-base balance |
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Term
| Difunisal (DOLOBID) actions |
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Definition
anti-inflammatory (more potent than aspirin)
analgesis
NO Antipyretic effects - (poor CNS penetration)
little to no antiplatelet activity and little to no blood loss compared to aspirin |
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Term
| Clinical use of difunisal? |
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Definition
Pain management
Osteoarthritis
Rheumatoid Arthritis |
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Term
| Diflunisal MOA, metabolism and Drug interactions? |
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Definition
MOA:competitive inhibition of cyclooxygenase
Metabolism: 99% bound to plasma albumin
Drug Interactions: competes witih oral hypoglycemics and anticoagulants |
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Term
| Diflunisal Side Effects and Contraindications |
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Definition
Dizziness
Nephritis
Gastric Ulceration
No Tinnitus
Astma is the only major contraindication |
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Term
| What are the Para-Aminophenol Derivatives? What are their effects? |
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Definition
Acetaminophen (TYLENOL)
Effect: Analgesis, Antipyretic and weak anti-inflammatory effect |
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Term
| Conditions and Indications for Acetaminophen use |
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Definition
Use where aspirin or other NSAIDS are contraindicated
Clinically can be used to treat gout when combined with probenecid |
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Term
|
Definition
Antipyretic by blockign cyclooxygenase in hypothalamus
Analgesis method unknown. |
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Term
| Acetomeniphen Side Effects |
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Definition
Hepatotoxicity
NO GI effects
No prolonged bleeding time
No effect on renal function or acid-base eq. |
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Term
|
Definition
2 stages, 12 and 48 hours
12 hours: nausea, vomiting, lethargy
48 hours: potentially fatal hepatic necrosis
Also see renal tubular necrosis and hypoglycemic coma |
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Term
| Contraindications for Acetomeniphen use? |
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Definition
Not for inflammatory conditions
analgesia adjunct with other antiinflammatory agents
caution needed with patients with liver disease. |
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Term
| What are the Proprionic Acid Derivatives and their MOA? |
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Definition
Ibuprofen (MOTRIN & RUFEN) and Naproxen (NAPROSYN & ANAPROX)
Competively inhibit cyclooxygenase
99% bound to plasma proteins
No interactions with oral hypoglycemics or oral anti-coagulants |
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Term
| Class and action of Ibuprofen |
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Definition
Proprianic Acid Derivative
Analgesic
Antiinflammatory
Antipyretic
Antiplatelets (reversible)
Same uses as aspirin, but reversible binding of platelets |
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Term
|
Definition
GI
epigastric pain, nausea, heartburn, sensation of "fullness"
gastric, duodenal, intestinal erosions (less than aspirin)
occult blood loss uncommon
occular disturbances, skin rashes, headache |
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Term
| Naproxen Class, MOA, Actions and Use |
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Definition
Class: Proprionic Acid Derivitives
MOA: Comeptitively inhibit Cyclooxygenase
Actions: Analgesic
Antiinflammatory
Antipyretic
Antiplatelet (reversible)
Use: Same as Aspirin |
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Term
|
Definition
1.competitive inhibitor of cyclooxygenase
2. inhibits hydrolytic enzymes of lysosomal system
3. inhibits migration of PMN leukocytes |
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Term
| What are the Heteroaryl Acetic Acids? |
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Definition
Ketorolac (TORADOL)
Tolmentin (Tolectin)
Diclofenac (VOLTAREN) |
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Term
| Ketolerac Actions, Use and MOA |
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Definition
MOA: completely absorbed after IM injection, very potent inhibitor of cyclooxygenase
Use: short term management of pain
Actions: analgesic, antiinflammatory, antipyretic and prolongs bleeding (reversible after 24-48 hours) |
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Term
Ketorolac Class, Side Effects and Contraindications
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Definition
Class: Heteroaryl Acetic Acids
SE: nausea, dyspepsia, GI Pain and drowsiness
Contra's: additive side-effects with other NSAIDS
partial or complete syndrome of nasal polyps, angioedema and bronchospams
previously demonstrated hypersensativity to ketorolac |
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Term
| Tometin Class, Actions, MOA and Use |
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Definition
Class: Heteroaeryl Acetic Acid
Actions: analgesis, antiinflammatory, antipyretic, prolonged bleeding time
less occult blood loss than aspirin
Use: Rheumatoid Arthritis and Osteoarthritis
MOA: competitive inhibitor of cyclooxygenase |
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Term
|
Definition
SE experienced by 25-40%
5-10% of patients will discontinue use
GI and duodenal ulcerations
CNS effects (tinnitus, nervousness, anxiety and drowsiness) |
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Term
| Diclofenac Class, Actions, MOA and Use |
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Definition
Class: Heteroaeryl Acetic Acid
Actions (3): analgesic, antiinflammatory, antipyretic
MOA: competitive inhibitor of COX and reduces intracellular concentrations of free arachidonate in leukocytes
Use: long term treatment of RA, OA and ankylosing spondylitis |
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Term
|
Definition
99% plasma protein bound
minimally competes with warfarin, but no affect on oral hypoglycemics
has a 50% first pass effect |
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Term
| What are the Enolic Acids? |
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Definition
Piroxicam (Feldene)
Phenylbutazone (BUTAZOLIDIN) |
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Term
| Piroxicam Class, Actions, Use and MOA |
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Definition
Class: Enolic Acids
Actions: Analgesic, Antiinflammatory, Antipyretic, Prolongs bleeding time
(equivalent to aspirin, indomethacin or naproxen, but much better tolerated)
Use: Osteoarthritis, rheumatoid arthritis and acute gout
MOA: potent inhibitor of COX, and inhibits activation of neutrophils and hemostasis |
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Term
| Phenylbutazone Class, Actions, Use and MOA |
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Definition
Class: Enolic Acid
Actions:
analgesic (inferior to aspirin for non-rheumatic pain)
antiinflammatory
antipyretic
very toxic - uricosuric similar to asprin
Use: acute gout and rheumatoid arthritis
MOA: inhibitor of COX |
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Term
| Phenylbutazone Metabolism and Side Effects |
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Definition
98% plasma protein bound
(competes with NSAIDS, warfarin, oral hypoglycemics and sulfonamides
Epigastric pain, nausea, emesis, skin rashes
GI ulceration
CNS: vertigo, insomnia, euphoria, nervousness
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Term
| Contraindications for Phenylbutazone |
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Definition
Cardiac, hepatic or renal dysfunction
Blood dyscrasias
promotes retention of Na+ and Cl- with water leading to cardiac compensation and pulmonary edema in some patients |
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Term
| What are the Indole and Indene Acetic Acids? |
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Definition
Indomethacin (INDOCIN)
Sulindac (CLINORIL) |
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Term
| Indomethacin & Sulindac Class, Action, Use, MOA |
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Definition
Class: Indole/Indene Acetic Acid
Action: Analgesic, Antiinflammatory, Antipyretic
Significant occult blood loss
Use: Rheumatoid arthritis, ankylosing spondylitis, acute gout
neonates, will close patent ductus arteriosus
MOA: Potent inhibitor of COX and inhibits mobility of PMN Leukocytes |
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Term
| Indomethacin and Sulindac Metabolism & Side effects |
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Definition
Metabolsim: oral absorbtion and IV injection
90% plasma bound, but also binds to tissues
Side Effects: 30-35% experience SE, 20% discontinue use
abdominal pain, nausea, anorexia
gastric ulceration w/ signifacant occult blood loss
CNS: sever frontal headache, vertigo, mental clouding, depression and psychosis
Skin rashers, allergic reactions, nephritis, aplastic anemai and thrombocytopenia |
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Term
| Contraindications for Indomethacin and Sulindac |
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Definition
Cannot be administered with warfarin b/c of increased risk of GI bleading
Interacts with diuretics
antihypertensives of thiazide diuretic class
Beta-Blockers and ACE inhibitors |
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Term
| What are the selective COX2 inhibitors? MOA? |
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Definition
Celecoxib (CELEBREX)
Rofecoxib (Vioxx)
Inhibit only COX2 and not COX1 (at therapeutic levels) |
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Term
| Class and Action of Celecoxib |
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Definition
Actions: Anti-inflammatory, analgesic, antipyretic
Class: COX2 inhibitors
Side Effects: GI Ulceration, bleeding, perforation (lower incidence than other NSAIDS)
may cause premature closure of ductus arteriousus |
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Term
Agent used to minimize side effects of NSAIDs? MOA? Contraindications?
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Definition
Misoprostol (CYTOTEC)
PGE1 analog
used to suppress gastric ulcerations
Use: patients with chronic NSAID treatments
Contraindicated in pregnancies due to abortive properties |
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Term
| Which Anti-microbials block cell wall synthesis, specifics not classes? |
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Definition
| Penicillin, Methicillin, Ampicillin, Pipercillin, Cephalosporins, Aztreonam, Imipenem |
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Term
| What Anti-microbials block peptidoglycan synthesis? |
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Definition
| Bacitracin and Vancomyocin |
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Term
| What Anti-microbials block nucelotide synthesis? |
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Definition
| Sulfonamides and Trimethoprim |
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