Pharmacology IV Flashcards
T/F
The anticipation of pain will cause a greater perception of pain.
NSAID
True
Non-Steroidal Anti Inflammatory Drug
An unpleasant sensory or emotional experience associated with actual or potential tissue damage, or described in terms of such damage
Pain
Absence of pain in response to a stimulus that is normally painful
Analgesia
Absence of all sensory modalities
Anesthesia
What are endogenous morphines called?
Endorphins
*CNS - analgesia, euphoria
What was the first endorphin to be purified and acts as a delta receptor?
Enkephalins
“in the head” - greek
What endorphin has a high affinity for kappa-opioid receptor?
Dynorphins
Describe the 2 types of pain and what drugs alleviate these.
Dull, aching, inflammatory - NSAIDS
Sharp, piercing, lancinations - Narcotics
T/F
Narcotics are anti-inflammatory
False
NOT anti-inflammatory
What 2 types of drugs are best for Mild to Moderate pain?
Severe?
Salicylates, NSAIDS
Opiates
What type of analgesics act primarily at peripheral nerve endings, have antipyretic effects (mediated centrally) and inhibit prostaglandin synthesis?
Non-opioid Analgesics
What type of analgesic act primarily within the CNS and have depressive effects that reduce the response to pain?
Opioid Analgesics
T/F
Analgesia and anti-inflammatory effects in the periphery are obtained using Salicylates and NSAIDS.
True
CNS analgesia, anti-inflammtory effects, and antipyretic effect can be achieved using what 3 drugs?
NSAIDS
Acetaminophen (Tylenol)
Opiates (have more side effects)
***not Salicylates
______ are True Analgesics, while ______ only acts as analgesics.
NSAIDS
Opiates
______ inhibit prostaglandin synthesis by inhibiting COX.
NSAIDS
What 2 types of Prostaglandins do NSAIDS inhibit?
Cytoprotective
Inflammatory
______ is a “miscellaneous” analgesic and NOT an NSAID and works on COX 3 in the CNS
*it is not anti-inflammatory
Acetaminophen (Tylenol)
By what pathway do COX affecting drugs inhibit prostaglandins?
Cyclooxygenase > Endoperoxides > Prostaglandins (protective/inflammatory)
COX 1 controls what?
COX 2 controls what?
Cytoprotective/homeostatic Prostaglandins
Inflammatory Prostaglandins
Name 3 classes of Cytoprotective prostaglandins controlled by COX1.
Prostacyclin - stomach, endothelium
Prostaglandin E2 - kidneys
Thromboxane A2 - platelets
What type of Cyclooxegenase controls/maintains Renal blood flow, Body temp, BP, Heart rate, stomach acid, and Reproduction?
COX1
What explains ulceration/bleeding in GI tract due to taking NSAIDS?
COX1 inhibited
*protective mucous lining decreased
What drug blocks COX2 only?
Celebrex
What drug blocks COX 3?
Acetaminophen
- CNS suppression of prostaglandin synth
- NON anti-inflammatory
Non-selective NSAIDS block _______.
Selective NSAIDS block ______.
______ blocks COX 3 and is not categorized as an NSAID.
COX 1 and COX 2
COX 2 only (Celebrex - celecoxib)
Tylenol
T/F
Acetylsalicylic Acid reduces pain by inhibiting prostaglandin synth and works on COX 1 and 2.
True
Aspirin produces a peak effect on an empty stomach in _______.
30 minutes
Aspirin is widely distributed and ____ to plasma proteins
Poorly bound
Aspirin displays ______ kinetics, so its half-life is dose-dependent.
Zero-order kinetics
*constant amount, rather than constant %, is eliminated
Aspirin is a ____ and a ______ and a ______.
Analgesic
Antipyretic
Anti-inflammatory
What is the anti-inflammatory dose of Aspirin?
What will this dose do if chronically taken?
3500 mg/day
GI ulceration/bleeding
A dose of aspirin greater than _____/day is considered _______.
What was this dose once used to treat?
What is used to treat gout now?
3 g Uricosuric (excrete uric acid)
Gout
Probenecid (Benemid)
Low doses of aspirin can have the opposite effect of high doses in what way?
Hx of what makes aspirin no longer a choice?
Uric acid retention
Gout
How long does the anti-platelet effect of Aspirin last?
7-10 days
*Irreversible effect (lasts for life of platelet)
Aside from Aspirin’s anti-platelet effect, what is another way it reduces blood clots?
COX inhibitor shuts down Thromboxane A2
*Thromboxane A2 causes vasoconstriction and platelet aggregation
What is the low dose of Aspirin used to prevent stroke/heart attack?
81 mg
GI pain through direct irritation, inhibition of protective prostaglandins, and the exacerbation of pre-existing ulcers, gastritis, hiatal hernia, or reflux disease is caused by what drug?
*also bleeding due to irreversible effects on platelets
Aspirin
What is contraindicated in children with viral infections?
What is this called?
How does it manifest?
Aspirin
Reye’s Syndrome
Diarrhea/vomiting concentrated aspirin in blood.
Hepatotoxicity.
Fluid on brain (encephalitis)
At high doses, aspirin can cause tinnitus, confusion, dizziness, etc, along with Acidosis. This leads to ______.
_______ ensues.
Hyperventilation
Respiratory/Metabolic Acidosis
*death from OD on aspirin usually acidosis/electrolyte imbalance from 6-10 grams
T/F
Aspirin allergy is less than 1%, but many report allergy (usually stomach problems).
True
If allergic to Aspirin, what is a cross-sensitivity?
other NSAIDS
*avoid aspirin, all NSAIDS
What is the Aspirin hypersensitivity triad?
Aspirin hypersensitivity
Asthma
Nasal polyps
Describe the mechanism of the Aspirin allergy:
COX cascade inhibits PGE2 (bronchodilator)
Forms leukotrienes (bronchoconstrictors)
*looks like asthma attack
Due to the mechanism of Aspirin allergy, what is contraindicated for use?
Asthma
What are the 5 Contraindications for Aspirin?
Allergy
Chronic gastritis
Gout
Anticoagulants (warfarin/coumadin)
3rd Trimester (bleeding, decreases prostaglandins responsible for uterine contraction)
***low-dose aspirin in pregnancy has many benefits and is not teratogenic
Full strength dose aspirin:
prevention dose aspirin:
325 mg
81 mg
How can a person taking Aspirin (damaged platelets) still clot?
Fibrin
Thromboxane A2 still made by endothelial cells
What compound does COX mediate that affects formation of prostaglandin precursors and thromboxanes?
Arachidonic Acid
How are NSAIDS and Aspirins effects different on platelets?
NSAIDS reversible on blood platelets
Ibuprofen has a half life of _____
Naproxen has a half life of _____
1 day
4 days
*this might be 4-5 half lives - time to be off drug before procedure
What prophylactic can ibuprofen interfere with?
Low dose aspirin - 81 mg
*interferes with anti-platelet effect
In order to not interfere with Aspirin’s effects, ibuprofen should be given _____ after aspirin is ingested or _______ before aspirin ingestion.
40 minutes after
8 hrs before
What are 5 adverse side effects of NSAIDS?
Cardiovascular - MI, stroke, hypertension
Renal - function, nephrotoxicity
GI - bleeding in elderly, more than 3 drinks/day
CNS - dizziness, tinnitus, sedation
Skin rxns
______ is worse for kidneys and ____ is worse for liver, however both with damage both.
Ibuprofen
Tylenol
What syndrome sloughs skin from palms/feet and is associated with hypersensitivity to NSAIDS?
Steven-Johnson syndrome
How do NSAIDS damage the kidney (lead to necrosis in some cases)?
Prostaglandin inhibition shuts down renal blood flow
*5 days high dose dangerous for kidney
ibuprofen OTC dose
Rx dose:
onset:
duration:
1/2 life:
200 mg
400-800 mg
30-60 min
4-6 hrs
2-4 hrs
ibuprofen Dental dosing children:
adults:
max adult daily dose:
4-10 mg/kg (every 6-8 hrs)
200-400 mg (every 4-6 hrs)
1200 mg
ibuprofen 400-600 mg every ___ hrs for 24 hrs before dental procedure decreases post-op _____ and hastens healing time
6
edema
What is the “ceiling” for dental pain in an ibuprofen dose?
400 mg
*chronic inflammatory pain pts take more - but days/weeks to reach effects
**beyond 400 little analgesic effect gained
3 names for naproxen:
Aleve
Anaprox
Naprosyn
Naproxen analgesic onset:
half life:
duration:
dental dose:
max/day:
1 hr
12-17 hrs
analgesic less than 7 hrs, anti-inflammatory less than 12 hrs
500 mg initial, 250 every 6-8 hrs
1250 mg/day
Name 4 important NSAIDS used in dentistry (in other category):
piroxicam (Feldene) - longest lasting nsaid (45-50 hr 1/2 life)
flurbiprofen (ANSAID)
ketorolac (Toradol) - injection, opioid level relief
diflunisal (Dolobid)
T/F
Prescription drugs, expensive drugs, colored pills all give more pain relief (placebo effect)
True
T/F
Celebrex (celecoxib) is the only COX 2 selective inhibitor and was originally approved for arthritis pain.
COX 2 isn’t expressed in GI, platelets, or kidneys
True
True
What drug reduces risk for adenocarcinoma of the colon, improves lung cancer, and delays onset/degree of Alzheimer’s?
Celebrex (celecoxib)
T/F
Celebrex (celecoxib) is contraindicated with low-dose Aspirin use.
False
*perfectly ok to use with
T/F
Celebrex (celecoxib) is contraindicated with Aspirin/NSAID allergy?
True
What is the main side effect of Celebrex (celecoxib)?
What atom does Celebrex (celecoxib) contain that may cause allergy?
Unanticipated bleeding
Sulfa
T/F
Celebrex (celecoxib) in contraindicated with Hx of gastritis/gastric ulcer/GI bleeding AND pregnancy
True
*unanticipated bleeding side effect
What drug, used for autoimmune diseases and cancer, does ibuprofen interfere with?
How does ibuprofen interfere?
Methotrexate
Metabolic breakdown - causes toxicity
What 2 drugs interfere with Methotrexate?
How?
Ibuprofen - metabolic breakdown (toxicity)
Aspirin - displaces and interferes with clearance (toxicity)
Lithium excretion is blocked by what?
NSAIDS
How can Aspirin and NSAIDS be taken together?
Separate dosing intervals
Taking several NSAIDS together can have an additive toxic effect.
Alcohol increases GI bleeding associated with NSAIDS
True
True
_______ and ________ can decrease the effectiveness of many common antihypertensive medications.
(diuretics, beta blockers, ACE inhibitors)
Aspirin
NSAIDS
7 contraindications/cautions with NSAIDS
Asthma
CV
Renal
Coagulopathies
Ulcers (stomach, colitis)
Allergy to Aspirin/other NSAIDS
Geriatrics
Acetaminophen acts on COX 3 in CNS (more than peripheral) and doesn’t do what 3 things?
Inhibit platelet aggregation
Irritate GI tract
Cause bronchoconstriction
Acetaminophen is hepatotoxic and excreted by what?
Kidneys
Why shouldn’t you take Tylenol for arthritis?
NOT anti-inflammatory
Tylenol is equally potent to ______
No ____ irritation
Aspirin
Gastric
What is the max dose acetaminophen/day?
4000 mg (4 grams)
*although Tylenol brand now limits to 3 grams/day
Acetaminophen and Aspirin are equally _____ and equally ______, but ______ is less useful clinically.
Efficacious
Potent
Acetaminophen (b/c NOT anti-inflammatory)
Three characteristics absent Acetaminophen:
2 characteristics it has:
No anti-inflammatory effect, no effect on uric acid, no anti-coagulant effects
Analgesic and Antipyretic
Acetaminophen dental dosing Children:
Adults:
Max adults:
Max in pts regularly consume alcohol:
10-15 mg/kg (every 4-6 hrs)
325-650 mg (every 4-6 hrs)
4 grams/day
2 grams/day
2 situations to avoid using Acetaminophen:
Liver disease
Alcoholism
- more than 3 drinks/day increases risk liver damage
- *alcohol stimulates (enzymes that lead to) acetaminophens toxic metabolite
Acetaminophen combined with _______ leads to an increased bleeding risk.
Warfarin (coumadin)
- enhanced anticoagulation
- **increases 10-fold according to one study
T/F
Aspirin is more effective if given prior to initiation of pain
True
T/F
Aspirin and NSAIDS are Analgesics, Antipyretics, and Anti-inflammatory
Tylenol is an Analgesic and Antipyretic
True
Describe the GI side effects of Aspirin:
Dyspepsia, nausea, vomiting, gastric bleeding
- direct irritation/inhibition cytoprotective prostaglandins
- stimulated trigger zone in CNS for nausea/vomiting
- exacerbates ulcers, etc (acid)
NSAID analgesia occurs at what dose?
NSAID anti-inflammatory effects occur at what dose?
up to 400
over 400 (400-800 4x/day)
Prescription for ibuprofen for Dental Pain:
Rx:
Disp:
take:
Do not exceed:
Rx: ibuprofen 400 mg tablets
Disp: 16 tablets
Take 1-2 tablets by mouth 3-4 timer per day as needed for pain. Do not exceed 8 tablets within 24 hours.
What is the longest lasting NSAID?
dose?
half life?
piroxicam (Feldene)
10 mg 2x/day
45-50 hrs
flurbiprofen (ANSAID) dose:
onset:
1/2 life:
100 mg every 12 hrs
1-2 hrs
5.7 hrs