Exam 4: NSAIDs/Non-Opioids yo-Part 1 to Aspirin Flashcards by Austin Shackelford

Patients who ________ having pain or who have fear and anxiety will perceive more pain.

ANTICIPATE!!!

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_______: “an unpleasant sensory or emotional experience associated with actual or potential tissue damage, or described in terms of such damage”

Pain

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_______ = absence of pain in response to a stimulus that is normally painful

Analgesia

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________ = absence of all sensory modalities

Anesthesia

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2 Types of pain: _______ = non- steroidal anti-inflammatory analgesics (NSAIDS) are most effective…..AND…._________ = opiates (narcotics) are most effective

Dull, aching, inflammatory……AND……Sharp, piercing, lancinations

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Hey, I don’t think I saw this enough…Narcotics are NOT __________.

anti-inflammatory

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Degrees of Pain & what to use: _____ = Salicylates, NSAIDS most effective…._______ = Salicylates, NSAIDS most effective….________ = opiates are best

Mild…Moderate…Severe

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Locus of Action…haha that sounds cool: Non-opioid Analgesics- Act primarily at ________ nerve endings…._______ effect mediated centrally… Mechanism: inhibit _________ synthesis

peripheral….Antipyretic…prostaglandin

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Locus of Action…haha that sounds cool: Opioid Analgesics-Act primarily within ______…..Mechanism: _______ CNS which reduces response to pain (pain reaction)

CNS….depress

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Locus of Action...haha that sounds cool: \_\_\_\_\_\_\_\_ (local pain control) = analgesia, anti-inflammatory effects THEREFORE \_\_\_\_\_\_\_\_, \_\_\_\_\_\_\_ are used; few side effects....All non-opioid analgesics work on the \_\_\_\_\_\_\_\_
nervous system (as well as CNS)

Periphery…salicyclates and NSAIDs….PNS

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Locus of Action…haha that sounds cool: ________ = analgesia, anti- inflammatory effects, ANTIPYRETIC effect…..NSAIDS; acetaminophen (Tylenol)…..opiates = more side effects

CNS

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The WAR- NSAIDs VS Opioids- _______ = true analgesics; stop the pain from where it is occurring

NSAIDs

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The WAR- NSAIDs VS Opioids- ________ = diminish your awareness of pain, so act as analgesics (don’t feel pain)

Opiates

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The WAR- NSAIDs VS Opioids- NSAIDS inhibit _________ synthesis; they accomplish this by inhibiting the __________ enzyme.

prostaglandin…cyclooxygenase

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The WAR- NSAIDs VS Opioids- NSAIDs inhibit ________ PG as well as PG associated with _________.

cytoprotective…inflammation

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What is another name for salicyclics?

Aspirin

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How many drugs approved by the US are in the NSAIDs family? Whats one example?

22…ibuprofen

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acetaminophen (Tylenol) = classified as a “__________” analgesic (not NSAID), as it works on COX-___ in the CNS, and is NOT ________.

miscellanious…COX 3…anti-inflammatory

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What is the grandfather molecule of prostaglandin synthesis?

Arach-id-onic Acid

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What are the four steps to forming prostaglandins? Where do NSAIDs/Salicyclics intervene?

Arachidonic Acid–>Cyclooxygenase (Salicyclics/NSAIDs inhibit here)–>Endoperoxidases—>Prostaglandins

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Non-selective NSAIDs are COX-__ & ____ inhibitors.

COX-1 & 2

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COX-1 leads to ________ prostaglandins which promote _________. ERGO- blocking COX-1 will lead to side effects in the _____, ______, and ______ aggregation.

cytoProtective….homeostasis….stomach, kidneys, platelet

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What are the three end products of COX-1?

1.Prostacyclin-stomach endothelium 2.Prostaglandin E2-kidneys 3.Thromboxane A2-platelets

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COX-2 leads to the prostaglandins that are correlated with ________…which is our goal!

inflammation

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Salicyclates and NSAIDs block which COX(s)?

COX-1 AND COX-2 non selectively

COX-___ Regulates the amount of stomach acid produced

COX-1

Blocking COX-___ with aspirin or NSAIDS decreases production of protective _______ in the gastric lining = explains side effect of GU ulceration and bleeding

COX-1...mucous

COX-___ is the inducible form which is produced when you experience trauma and need inflammatory response for healing

COX-2

Drugs that block COX 2 are primarily used for ______.

arthritis

COX-___ have no effect on the stomach = leave cytoprotective prostaglandins intact.

COX-2

What is THE ONLY COX-2 selective inhibitor on the market?

Celebrex

COX-__: Recently discovered (2002), Works in the central nervous system, Suppresses prostaglandin synthesis, No anti-inflammatory effects, this is how acetaminophen (Tylenol) works (pain control but no anti-inflammatory effects)

COX-3

COX-3: Works in the ______.

CNS

COX-3: Suppresses _______ synthesis

prostaglandin

COX-3: NO _______ effects

anti-inflammatory

COX-3: This is how __________ (Tylenol) works (pain control but no anti-inflammatory effects)

acetaminophen

Non-selective NSAIDs = block both COX-__ and COX-__...MOST NSAIDs in use today (eg. ibuprofen)

COX-1 and COX-2

Selective NSAIDS = block COX-__ only....Only one available on U.S. market: _______ (_______) used primarily for arthritis pain.

cele-COX-ib (Celebrex)

Remember that acetaminophen (Tylenol) blocks COX-__ but it is NOT categorized as an _____.

COX-3...NSAID

What is the abbreviation of Aspirin? What is its pharmalogic class? Comes from extracts of _______.

ASA...salicylate...willow bark

What is the most useful salicyclate for analgesia?

Aspirin

What is the chemical structure of Aspirin?

AcetylSaliCyclic Acid

Most of aspirin’s effects are due to inhibition of __________.

prostaglandin synthesis

Prostaglandins are synthesized _______ by inflammatory stimuli.

locally...shop local broooo

Prostaglandins sensitize pain ________ to substances such as bradykinin, therefore reduction in _________ = reduction in pain.

receptors....prostaglandins

Aspirin is MORE effective if given ______ painful stimuli are experienced

BEFORE!!!!!

Aspirin is more effective against _______ pain (caused by inflammation) versus ______ pain (direct irritation of nerve endings)

throbbing...stabbing

Kinetics of ASA-Rapidly and completely absorbed from stomach and small intestine, producing peak effect on empty stomach in ___ minutes

30 minutes

Kinetics of ASA- Widely distributed; poorly bound to _______

plasma proteins

Kinetics of ASA- Hydrolyzed to ________ in GI tract and via _______ effect in liver

salicyclate...FIRST PASS

Kinetics of ASA- Conjugated with ______ and ________ acid by liver

glycine...glu-cur-onic acid

Kinetics of ASA- Half-life is ______-dependent, small doses = half life of __-__ hours...Higher dose = 15-30 hours

DOSE...small=2-3 hours...higher =15-30 hours

Kinetics of ASA- It follows ______ order kinetics.

Zero

Kinetics of ASA- May lead to ________ situation if take too much

poisoning

Kinetics of ASA- _______ increased by alkalinization with sodium bicarbonate which increases the proportion of the aspirin that is in the ______ form that is therefore excreted

Excretion...ionized

Effects of Aspirin-Analgesic:Relieves _____ to _____ pain, not potent enough for intense pain, use an opioid.

mild to moderate

Effects of Aspirin-Considered an antipyretic because it inhibits ________ synthesis in the _________....it also induces peripheral ________ and sweating.

prostaglandin synthesis....hypothalamus...dilation

Effects of Aspirin-Anti-inflammatory: Prostaglandins are potent vasodilating agents that also increase capillary permeability.....Inhibition causes decreased erythema and _______ of inflamed area

swelling

Effects of Aspirin-Anti-inflammatory: Important because almost all dental pain is __________ in nature....High dose aspirin is used to relieve pain and inflammation of ______ too!

inflammatory.....arthritis

Effects of Aspirin- the Analgesic dose = dosing used for pain control is NOT ENOUGH for ________ effects!

anti-inflammatory

HOW many mg of aspirin is needed for anti-inflammatory effect? What are the 2 side effects of this high of a dose?

3500 mg....stomach ulceration and bleeding

Effects of Aspirin-Large/high doses (greater than ___ g per day) – produces _______ effect = excretion of uric acid in urine...At one time, aspirin was used to treat ____ but, Aspirin is no longer used for this purpose

3 g...URICO-SURIC...gout!

What analgesic should a person with gout stay away from?

Aspirin...patient takes probenecid (Benemid) to excrete uric acid (stops absorption of uric acid back into bloodstream)...aspirin can ANTAGONIZE these effects

Effects of Aspirin:Anti-platelet effect = _________ effect that lasts for the life of the platelet (___-___ days)...Reduces platelet adhesiveness/aggregation by interfering with _________ (____) release = prolongs bleeding time

irreversible....7-10 days...adenosine diphosphate (ADP)

Effects of Aspirin: Aspirin inhibits cyclooxygenase which inhibits the formation of __________, which facilitates clotting, so by reducing this, aspirin reduces the risk for _______ and ______! AT about ____ mg/day

thromboxane A2...blood clots and stroke!...81 mg

Adverse effects of aspirin ________: dyspepsia, nausea, vomiting, gastric bleeding...WHY?

Gastointestinal..inhibits the COX-1 Cytoprotective enzymes!!

Adverse effects of aspirin-Stimulates chemoreceptor ______ zone in the CNS (nausea and vomiting)

trigger

Adverse effects of aspirin--Exacerbates ________ ulcers, gastritis, hiatal hernia, reflux disease

PRE-EXISTING

Adverse effects of aspirin- What is it called when aspirin inhibits the production of PROTHROMBIN?

Inhibits production of prothrombin = hypo-prothrombin-emia!!

Adverse effects of aspirin-the GI bleeding caused by aspirin is often ______!

painless

What is the name of this syndrome??? aspirin contraindicated in children/adolescents with viral infections (flu, chickenpox)

Reye's syndrome

Reye's Syndrome can manifest with fluid in _____ (encephalitis) and ________ = often fatal

brain...hepatotoxicity

What do we use instead of aspirin if a child is sick? (most of the time its viral origin!)

Acetaminophen (Tylenol)

What is a classic warning sign of Salicyism (toxicity of aspirin)?

Tinnitus

Aspirin toxicity- At high doses = _________ = produces _________; then compensatory renal loss of _______, Na and K = leads to respiratory AND _______ acidosis!!!

hyperventilation...respiratory alkalosis..bicarb...metabolic

Death from aspirin poisoning is usually ______ and ______ imbalance

acidosis and electrolyte

Aspirin toxicity-Usually occurs in overdose ranges from __-___ grams in adults

6-10 grams

Allergies to aspirin are pretty rare...Less than __% incidence

These are signs of a ________: rash, wheezing, urticaria (hives), angioneurotic edema, anaphylaxis

TRUE aspirin allergy

Allergy to aspirin CAN mean a person has __________ to other NSAIDs!

CROSS-sensativity

________ are more likely to have hypersensitivity reaction to aspirin (incidence ranges from 5- 15%)...STEEEEEVVVEEEE....THEREFORE ________ is a CONTRAINDICATION for aspirin use.

ASMATICS!!!....Asthma

What is the ASPIRIN hypersensitivity TRIAD??

1. Aspirin Hypersensativity 2.ASTHMA 3.Nasal Polyps

Mechanism of aspirin allergy...Shift in COX cascade to inhibit bronchodilating ______.....Shifts to favor unopposed lipoxygenase pathway and formation of ________ (bronchoconstrictors)

PGE2...LEUKOTRIENES

Allergic reactions look like _______ attacks = bronchial effects...in fact, in asthmatics, aspirin sensitivity develops over about ____ exposures

asthma...15

Cray cray patients- When aspirin is applied directly to oral mucosa, ester in water splits to ______ acid and salicylic acid and makes an "______"

acetic..."aspirin burn"

Oral ulcerations = chewing aspirin-containing ____.

gum...whaaaa they make that?!

Summary...time to use your memory tricks! What are the 4 contraindications to aspirin?

1.Allergy (bronchal rxn) 2.Chronic Gastritis 3.Gout 4.Anticoagulants

Aspirin displaces ______ from plasma proteins and therefore increases risk for a hemmorage.

warfarin

When is Aspirin contraindicated in pregnancy? What is the FDA category? BUT _______ aspirin has not been shown to be teratogenic.

The 3rd trimester!....C/D woah!..low dose

Aspirin and Prego-Can ______ labor (decreases prostaglandins responsible for uterine contractions)......Increases risk for _______ complications in mother....Risk of premature closing of the ________ in fetus, resulting in pulmonary vasculature abnormalities and pulmonary hypertension in newborn.

prolong (AINT NOBODY GOT TIME FOR THAT!)....BLEEDING....ductus arteriosus

Aspirin DOSING-___ mg for cardio-protective...____ mg for full strength dose (during a M.I.)

81 mg...325 mg

Aspirin Dosing- ____-____ mg every ___-___ hours UP TO ____ g per DAY!!!

325 - 650 mg...4-6 hours...up to 4 grams per day

Aspirin dosing: Children: ___-___ mg/kg/dose every 4-6 hours, up to a total of __ grams per day

10-15...4 g per day

Discontinue Aspirin? ______ aspirin therapy (81 mg daily) = NO need to discontinue

LOW DOSE

1 single dose of aspirin exerts an effect for a minimum of __ days

4 days

Discontinue Aspirin? For highly invasive surgeries, must weigh risk to patient versus bleeding risks...Eg: patients with cardiac stents are on aspirin and antiplatelet drug (Plavix) = discontinue _______ but not _______ before surgery

Plavix...aspirin

If patient is taking aspirin because of cardiac history, then __________ before advising the patient to discontinue the drug = benefit must outweigh risks to the patient

consult the patient’s physician!!!!

Potential for “________” risks (MI, stroke) if suddenly discontinue the use of aspirin!!

"catastophic"

What makes a person on aspirin clot why wouldn't they just bleed out??? _____ AND endothelial cells continue to make ___________.

FIBRIN...thromboxane A2

FUN FACTS! Methyl salicylate (oil of wintergreen) – Icy Hot, Ben Gay, Trolamine salicylate - Myoflex, Salicylic acid – Compound W, Magnesium salicylate – Doan’s pills ALL ARE SALICYCLATES used ________.

TOPICALLY