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
ketorolac (Torodol) use up to ___ days.
Primarily given by _____.
Causes _____ damage.
5
injection
Renal
diflunisal (Dolobid), aka?
onset:
duration:
1/2 life:
Super Aspirin (but just like aspirin)
1 hr
8-12 hrs
8-12 hrs
Presciption for diflunisal (Dolobid) Rx:
Disp:
Sig:
Rx: Dolobid 500 mg tablets
Disp: 16 tablets
Sig: Take 2 tablets initially, then 1 tablet every 8-12 hours as needed for pain
T/F
Cox 2 inhibitors are contraindicated with pregnancy
True
*no ibuprofen if prego
For high risk surgeries, Aspirin use must be discontinued _______ prior to surgery.
1-2 weeks
- platelets must regenerate
- *don’t take off if known risk factors for Heart Disease
NSAIDS should be discontinued by counting 4-5 half lives prior to surgery to prevent what?
Bleeding
*platelet effects reversible
What increases the Excretion of Aspirin?
Alkalinization by sodium bicarb (aspirin more ionized and excreted more)
T/F
Aspirin inhibits prostaglandin synth in the hypothalamus
(which prevents the induction of peripheral vasodilation/sweating)
True
High dose aspirin, above ____ mg, is used for arthritis management.
True
*chronic use leads to GI probs
T/F
Opiates are indicated to manage Moderate to Severe dental pain if the patient either cannot take NSAIDS or have some Contraindication for NSAIDS
True
Narcotics = Opiates = Opioids
What is found in Opium?
Opioids latest/correct term
Alkaloids found in Opium
T/F
Opioid receptors are the site of opioid action
True
*mediate specific pharmacologic effects
Where is the Analgesic Effect of Opiates produced in the brain?
Midbrain pain-modulating circuit
medulla/spinal cord/dorsal horn
Where are high concentrations of Endogenous Opioid peptides found?
Where does Systemic Administration of Opiods produce its analgesic effect?
Descending Pain Modulating Circuit
CNS - widely distributed in spinal cord and brain
The Pain Suppressor System (descending) involves ________ and _______ neurotransmitters.
Serotonin
Enkephalin-mediated (endogenous)
What are the 3 major components that mediate the Descending Analgesia System?
*opioids put directly into these 3 areas will have profound effects
Periaquaductal Grey Matter (midbrain)
Nucleus Raphe Magnus (medulla)
Inhibitory Neurons (dorsal horns)
Projections from the Periaqueductal Gray Matter (midbrain) are _____ and highly sensitive to morphine.
Projections from the dorsolateral pons are ______.
Serotonergic
Noradrenergic
T/F
Endogenous Opioids act as neurotransmitters, and are implicated in the mechanisms for the Placebo effect.
True
*brain actually releases endogenous opioids.
Name 3 groups of Endogenous Opioids.
Endorphins
Enkephalins
Dynorphins
Endogenous Opioids (endorphins, enkephalins, dynorphins) act through what 3 different G protein coupled receptors?
mu
delta
kappa
T/F
Endorphin can refer to all endogenous opioid peptides or a single specific opioid called Beta-endorphin.
True
What 2 sites produce Endogenous Opioids?
Pituitary Gland
Hypothalamus
Beta-Endorphin acts via _____ and influences ______ and ______.
Enkephalin is widely distributed and acts via ____ and _____.
Dynorphin is found in the spinal cord, brain, hypothalamus and acts via _____.
mu, appetite, sex
mu, delta
kappa
What endogenous endorphin acts via mu?
via mu and delta?
via kappa?
Beta-endorphin
Enkephalin
Dynorphin
Endorphins are comprised of ____ families of enkephalin-sequenced peptides.
3
*Proenkephalin A and B, and Pro-opiomelanocortin are the precursor molecules
Name 4 places Endorphins are found:
Pancreatic Islet Cells
Sympathetic Nervous System
Adrenal Medullary Chromaffin Cells
CNS
B-endorphin is distributed all over the brain, is involved in BP, temperature, food intake, and acts via ____ receptor.
Mu
Why do opioids cause constipation?
Mu receptors in GI tract
What class of endogenous opioids act as weak analgesics that mimic opiate activity?
What class are responsible for producing analgesia in placebo responders in acupuncture?
Enkephalins
Enkephalins
What accounts for the side effects (resp. depression, pupil constriction, decrease in body temp, and decrease in gut motility) of opioids?
Opiate receptors found in tissues NOT involved in Analgesia.
T/F
The recognition site (receptor site) is highly specific for Opioids
True
Name 5 Opioid receptor subtypes:
*which has best analgesic effect and is most addictive?
Mu (best analgesic/most addictive)
Delta
Kappa
Epsilon
Sigma (no longer opioid receptor)
What are the 2 subclassifications of Mu and what are their effects (3/1)?
Mu1 - Supraspinal analgesia, euphoria, physical dependence
Mu2 - Respiratory Depression
*Mu1 causes addiction
A drug must bind to ____ to be physically addicting
Mu
Drugs that bind to Mu have the best _____.
____ is the downside.
Analgesic properties
Addiction
What opioid receptor causes Spinal analgesia, miosis (pinpoint pupils), and sedation?
Kappa
What opioid receptor causes Analgesia, Emotion, and Seizures?
Delta
*rec use effect
What opioid receptor causes Analgesia (only listed effect)?
Epsilon
What opioid receptor causes Autonomic stimulation, Dysphoria, Hallucinations, nightmares, respiratory stimulation, tachycardia, and anxiety?
Sigma
What is determined by the strength of attachment of an opioid to its binding site?
Potency
Opioids cause _______ of nerve cells, ______ of nerve firing and _______ of transmitter release.
Hyperpolarization (potassium efflux)
Inhibition
Presynaptic inhibition
*the hyperpolarization makes less likely to respond to pain stimuli (inhibits Ca++ influx also) - this all decreases neurotransmitter release.
The hyperpolarization makes less likely to respond to pain stimuli (inhibits Ca++ influx also) - this all decreases neurotransmitter release.
True
Name 2 Opium Alkaloids
Morphine
Codeine
Name 4 Semi-synthetic opioids
Heroin
Oxycodone
Hydrocodone
Hydromorphone
Meperidine, methadone, fentanyl, pentazocine, buprenophine, tramadol, etc are all _______.
Fully synthetic opioids
Agonists elicit a ______, and Antagonists block agonists by ______.
Receptor response
Binding receptor
Morphine is a ______ Agonist
It has _____ Analgesia
It is ____ and ____ activated
Pure
Unlimited
Mu, Kappa
T/F
Tolerance happens with all opioids and Cross-tolerance also occurs
True
What drug acts as a Mu and Kappa Antagonist and is given for any OD.
- no analgesia
- *will reverse respiratory depression (all opioid depression)
naloxone (Narcan)
Opioid Distribution:
Metabolism:
Duration of Action:
Excretion:
1st pass, goes to fetus
Glucuronic acid conjugation in Liver
4-6 hrs orally
Metabolites exit in urine
4 Clinical uses of Opioid Drugs:
Analgesia
Sedation/euphoria
Cough suppression
GI (diarrhea)
Physical addiction, Respiratory depression, Constipation, Emesis (nausea), Miosis, Urinary retention, CNS stimulation, CV, Biliary tract constriction, Histamine release are all adverse effects of Opioids
True
What would indicate an allergy to an Opioid?
GI cramping and diarrhea
Most hypersensitivity rxns to Opioids are _____
Dermatologic
In dentistry, what are the 2 clinical indications for Opioid use?
(there are more in medicine)
Analgesia
Sedation
Opium is the dried juice obtained from the unripe seed capsules of the poppy plant _______.
Paparer somniferum
*25% dried juice alkaloids (morphine, codeine, etc)
**when smoke opium, mostly morphine and codeine
Name six Pure Agonists opioids like morphine:
heroin is also a pure agonist
oxycodone (Percodan, Percocet)
hydrocodone (Vicodin, Lorcet)
codeine
dihydrocodeine (Synalgos D-C)
meperidine (Demerol)
fentanyl
What mixed agonist/antagonist is equally potent as morphine and has superior oral efficacy?
What is it used for (2 things)?
Methadone (C-II)
Detox, chronic pain therapy
What antidote for an Opioid OD is given orally or IM?
What antidote is given IV to reverse OD of fentanyl and meperidine?
naltrexone (Depade, ReVia, Vivitrol)
naloxone (Narcan)
What “new” antagonist acts as a partial agonist (partial Mu agonist/weak Kappa antagonist)?
buprenorphine and naloxone (Bunavail)
*naloxone is the pure antagonist
Morphine is the Prototype Pure Agonist that acts like internal _____/______.
Enkephalins/Endorphins
How is morphine generally administered?
IM
- oral poorly absorbed
- *not used in dentistry
What is the most widely abused drug by hospital personnel (b/c no miosis)?
meperidine (Demerol)
What are the primary side effects to the synthetic drug meperidine (Demerol)?
*not as much sedation and euphoria as morphine/heroin
Nausea
Respiratory Depression (risk of death in addicts)
How is meperidine (Demerol) used in dentistry?
What are the advantages to using this instead of fentanyl?
(remember, this is the most abused drug by hospital personnel)
IV sedation (conscious)
Respiratory depression risk lower - wider margin of safety
What opioid, with many GI side effects, is one of the most frequently prescribed in dentistry?
Why is it given instead of morphine?
codeine *Tylenol III
can give orally
What is the optimum dose of codeine?
What is the potency compared to morphine?
60 mg
1/6 (10 mg morphine = 60 mg codeine)
What is the drug of choice for cough suppression?
codeine
codeine is indicated for moderate to moderately severe pain - what should you prescribe for severe pain?
oxycodone
Name 5 adverse rxns to codeine:
Nausea
Dizziness
Excitability
Constipation
Allergy - skin or asthma-like
What is the proper codeine dosing?
What system reflects mg concentration of codeine?
15-60 mg every 4-6 hrs
1 = 8 mg; 2 = 15 mg; 3 = 30 mg; 4 = 60 mg
Tylenol #3 has 300 mg acetminophen and ____mg codeine.
30
*Tylenol 1 (8 mg) sold OTC in Canada
Fiorinal with codeine (1,2,3) is a combo of _____, aspirin, and ______.
Barbituate
caffeine
hydrocodone (Vicodin) has acetaminophen that works ________ (as a pain reliever - fever lowering property works centrally) and opioid that works _______.
peripherally
centrally
hydrocodone (_______) is ____ times more potent than ____.
Vicodin
3
codeine
Name 2 hydrocodone/acetaminophen drugs that have 300 mg acetaminophen:
1 with 325 acetaminophen:
Vicodin, Xodol
Norco
hydrocodone also comes with ibuprofen (200 mg, low dose) and has 4 brand names:
Ibudone
Reprexain
Vicoprofen
Xylon
What drug with the same efficacy and potency of codeine, is no more effective than Tylenol III?
dihydrocodeine (Syngalos DC)
What Schedule II drug is highly addictive, as potent as morphine, and is used in dentistry in combo products for severe pain?
oxycodone
Name 4 examples of Oxycodone drugs:
Percocet
Percodan
Roxicet (doesn’t separate drug - drug seekers know)
Combunox
What drug, 100x more potent that morphine, is used in dentistry?
What is it used for?
3 ways administered?
fentanyl
conscious sedation only
IV, transdermal, lollipop
Active-Tramadol, EnovaRX-Tramadol, Ultram, Ultram ER, and 3 others (____,_____,____) are the tramadols
ConZip
Synapryn
FusePaq
What duration should tramadol be used for dental pain?
less than or equal to 5 days
What drug binds to Mu and inhibits the reuptake of norepinephrine and serotonin?
tramadol
Tramadol is associated with ______, and has a rare complication of anaphylaxis.
Seizures
Acetaminophen and tramadol is known as ______.
Ultracet
What NSAID provides analgesia at the Opioid level and in indicated for moderate to severe dental pain?
How long should this drug be used?
ketorolac (Toradol)
5 days
Because ketorolac (Toradol) is an NSAID, what complications must we watch for?
Bleeding/GI
Ketorolac (Toradol) dental dosing for Adults IM:
IV:
Oral:
60 mg single dose; 30 mg every 6 hrs; max 120mg/day
30 mg single dose; 30 mg every 6 hrs; max 120mg/day
20 mg single dose; 10 mg every 4-6 hrs; max 40 mg/day
T/F
Most pts are better managed with NSAIDS
True
If a patient demands more drugs, what should you do?
Refer to pain clinic
What is the most widely used opiate agent used for the management of dental pain?
What is the most widely used codeine preparation?
hydrocodone (Vicodin or Lorcet)
Tylenol III
What drug is prescribed if the pt has a history of codeine allergy?
meperidine (Demerol)
T/F
morphine and hydromorphone (Dilaudid) are used in Dentistry to manage severe pain
False
*these are NEVER used in dentistry
Caution/side effects for Elderly Patients, NSAIDS might ______
Aspirin
Opiates
GI bleeding
hemorrhage
constipation
From highest to lowest, rank Opiates by Potency:
fentanyl
morphine = oxycodone
meperidine
hydrocodone (3x codeine)
codeine (1/6 morphine) = dihydrocodeine
Opioid medications should only be used for…
The number of dispensed should be no more than…
treatment of acute pain
number doses needed
T/F
Sharing meds with others is illegal and driving should be avoided
True
T/F
Dentists use only short-acting opioids, and Long-acting opioids shouldn’t be used for treatment of acute pain
True
T/F
If pain persists beyond the anticipated treatment duration, the patient should be carefully reevaluated
True
What database must be checked before prescribing opioids (and periodically when renewing)?
Arizona Controlled Substances Prescription Drug Monitoring Program
What is one or more prolonged episodes of depression measured in weeks called?
Unipolar depression
What are 2 subtypes of Unipolar Depression?
Primary (endogenous - “chemical imbalance”)
Secondary (exogenous)
*secondary often develops with preexisting nonaffective disorder (trauma, chronic pain, etc)
Bipolar (manic depressive) is usually treated with what?
Lithium
T/F
Depression is the 3rd leading cause of death among 10-24 year olds, depression manifests in high risk behaviors, and introverts tend to seek stimulants.
True
T/F
Women are 2x as likely to experience depression as men
True
What is the comorbidity between Depression and Anxiety disorders?
50%
Primary (endogenous) Unipolar Depression is a chemical imbalance of what neurotransmitter in particular?
Serotonin
What are 3 functions of Serotonin
Mood elevator
Sleep
Satiety
Affective disorders are associated with what 2 neurotransmitter types in the brain?
noradrenergic
serotonergic
*circuitry between the 2 is closely linked
Decreased levels of Norepinepherine and/or Serotonin leads to…
Increased levels of these lead to…
Depression
Mania
*receptors equally important
What are the 2 proposed mechanisms for Antidepressants?
Increase extracellular levels of neurotransmitter
Improve Receptor Function
*therapeutic effects are only seen after several weeks of taking drugs
Why do women have greater incidence of depression?
Estrogen linked to serotonin levels
What 2 ways do Antidepressant Drugs increase neurotransmitter in synaptic cleft?
Inhibit reuptake
Degrade enzymes (that degrade neurotransmitter)
What Antidepressant increases synaptic serotonin and norepinephrine?
Increases synaptic norepinephrine?
Blocks the degradation of norepinephrine, dopamine, and serotonin?
Increases synaptic serotonin?
Tricyclics
Tetracyclics
MAO’Is
SSRI’s
What drug acts as a dopamine/norepinephrine/serotonin Reuptake Inhibitor, has Increased Risk for Seizures, and risk for emergent hypertension with concurrent nicotine patch use?
bupropion (Wellbutrin, Zyban)
*b/c of hypertension risk, take BP on pts using this drug
MAO is an enzyme responsible for the degradation of what?
MAOI, think ______, _______
norepinephrine, serotonin, and dopamine
Old drug, Old people
With MAOI’s, take ___ prior to administering local anesthesia, and use caution with ______.
BP
Epinephrine
4 MAOI’s
isocarboxazid (Marplan)
phenelzine (Nardil)
selegiline (Atapryl, Eldepryl, Selpak)
tranylcypromine (Parnate)
How do MAOI’s lead to a hyperadrenergic crisis?
what is released in the bloodstream?
What foods to avoid?
shuts off enzyme degradation in intestine/liver and vasoactive amines aren’t catabolized -
releases endogenous catecholamines
tyramine (hard cheese, red wine)
Name 3 popular SSRI’s
*which is only approved drug for children with OCD?
fluoxetine (Prozac, Sarafem)
paroxetine (Paxil)
*sertraline (Zoloft)
T/F
Antidepressants increase the risk of suicidal thinking with Major Depressive Disorder
True
Excitalopram (antidepressant) is not approved for use in ________.
children
What are the side effects of SSRI’s?
Agitation, anxiety, aggression, suicidal ideation (within 6 weeks)
T/F
Serotonin syndrome includes tremor, increased bowel sounds, tachycardia, agitation, autonomic instability
True
Name 4 Serotonin/Norepinephrine reuptake inhibitors
(these are different from Tricyclics - are “selective”)
*which treats fibromyalgia?
desvenlafaxine (Pristiq)
duloxetine (Cymbalta)
*milnacipran (Savella) - fibromyalgia
venlafaxine (Effexor XR)
Selective serotonin/norepinephrine reuptake inhibitors - should be used cautiously with what?
epinephrine
*could lead to too much
Effexor XR, generic name:
Therapeutic category:
Oral complications:
venlafaxine
selective serotonin/norepinephrine reuptake inhibitor (NOT Tricyclic)
xerostomia, stomatitis, taste, tongue discoloration
Name 1 Tetracyclic:
Mechanism?
treats?
maprotiline (Ludiomil)
norepinephrine reuptake inhibitor
anxiety with depression
Tricyclics block reuptake of _____ and ______ , and have an additional use because it exhibits _______ properties
norepinephrine
serotonin
analgesic
With Tricyclics, take ____ before local anesthesia, caution with ______
BP
epinephrine
Tricyclics have ______ effects causing blurred vision and xerostomia, ______ effects causing dizziness and reflex tachicardia, and __________, causing sedation.
Anticholinergic
Sympatholytic
Histamine antagonism
2 Tricyclics that block norepinephrine and serotonin?
2 Tricyclics that are selective norepinephrine reuptake blockers?
amitryptyline (Elavil) *granddaddy
imipramine (Tofranil)
desipramine (Norpramin)
nortripyline (Pamelor)
The weed, ______ has many DDI’s and what 4 antidepressive constituents?
St. John’s Wort
hyperforin
hypericin
flavonoids
tannins
T/F
St. John’s Wort is more efficacious than placebo for the treatment of mild to moderately severe depressive disorders
*Chochrane review concluded similarly effective to standard antidepressants
True
Hypericin in St. John’s Wort does what 2 things?
cyto P450 inducer in liver
reduced anticoagulant effect of warfarin (increases clotting)
Because St. John’s Wort is fairly powerful and has many DDI’s, (including rendering contraceptives ineffective in some users), the recommendation is to discontinue all herbs ____ days before surgery
14
T/F
The potency and efficacy of all antidepressants are similar
max blood conc 2-4 hrs, one dose/day
True
Antidepressants can have a side effect of orthostatic hypotension, so watch for ____ in older adults
Falling
Lithium, used for bipolar disorder, has what 2 brand names?
Eskalith
Lithobid
T/F
Lithium prevents the release of neurotransmitters and decreases the rate of serotonin synth
True
Lithium takes how long before improvements are seen?
Also, Lithium has a _____ therapeutic window
weeks
very low
T/F
Side effects of Lithium include nausea, vomiting, diarrhea, weakness, tremors, renal damage, hypothyroidism, thinning hair, sexual dysfunction
True
Diuretics, Anticonvulsants, Antihypertensives, and what other class of drug increase lithium levels in the blood and thus its toxicity?
NSAIDS
*contraindicated - use acetaminophen instead
