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Flashcards in Pharmacology IV Deck (239)
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1
Q

T/F
The anticipation of pain will cause a greater perception of pain.

NSAID

A

True

Non-Steroidal Anti Inflammatory Drug

2
Q

An unpleasant sensory or emotional experience associated with actual or potential tissue damage, or described in terms of such damage

A

Pain

3
Q

Absence of pain in response to a stimulus that is normally painful

A

Analgesia

4
Q

Absence of all sensory modalities

A

Anesthesia

5
Q

What are endogenous morphines called?

A

Endorphins

*CNS - analgesia, euphoria

6
Q

What was the first endorphin to be purified and acts as a delta receptor?

A

Enkephalins

“in the head” - greek

7
Q

What endorphin has a high affinity for kappa-opioid receptor?

A

Dynorphins

8
Q

Describe the 2 types of pain and what drugs alleviate these.

A

Dull, aching, inflammatory - NSAIDS

Sharp, piercing, lancinations - Narcotics

9
Q

T/F

Narcotics are anti-inflammatory

A

False

NOT anti-inflammatory

10
Q

What 2 types of drugs are best for Mild to Moderate pain?

Severe?

A

Salicylates, NSAIDS

Opiates

11
Q

What type of analgesics act primarily at peripheral nerve endings, have antipyretic effects (mediated centrally) and inhibit prostaglandin synthesis?

A

Non-opioid Analgesics

12
Q

What type of analgesic act primarily within the CNS and have depressive effects that reduce the response to pain?

A

Opioid Analgesics

13
Q

T/F

Analgesia and anti-inflammatory effects in the periphery are obtained using Salicylates and NSAIDS.

A

True

14
Q

CNS analgesia, anti-inflammtory effects, and antipyretic effect can be achieved using what 3 drugs?

A

NSAIDS

Acetaminophen (Tylenol)

Opiates (have more side effects)

***not Salicylates

15
Q

______ are True Analgesics, while ______ only acts as analgesics.

A

NSAIDS

Opiates

16
Q

______ inhibit prostaglandin synthesis by inhibiting COX.

A

NSAIDS

17
Q

What 2 types of Prostaglandins do NSAIDS inhibit?

A

Cytoprotective

Inflammatory

18
Q

______ is a “miscellaneous” analgesic and NOT an NSAID and works on COX 3 in the CNS

*it is not anti-inflammatory

A

Acetaminophen (Tylenol)

19
Q

By what pathway do COX affecting drugs inhibit prostaglandins?

A

Cyclooxygenase > Endoperoxides > Prostaglandins (protective/inflammatory)

20
Q

COX 1 controls what?

COX 2 controls what?

A

Cytoprotective/homeostatic Prostaglandins

Inflammatory Prostaglandins

21
Q

Name 3 classes of Cytoprotective prostaglandins controlled by COX1.

A

Prostacyclin - stomach, endothelium

Prostaglandin E2 - kidneys

Thromboxane A2 - platelets

22
Q

What type of Cyclooxegenase controls/maintains Renal blood flow, Body temp, BP, Heart rate, stomach acid, and Reproduction?

A

COX1

23
Q

What explains ulceration/bleeding in GI tract due to taking NSAIDS?

A

COX1 inhibited

*protective mucous lining decreased

24
Q

What drug blocks COX2 only?

A

Celebrex

25
Q

What drug blocks COX 3?

A

Acetaminophen

  • CNS suppression of prostaglandin synth
  • NON anti-inflammatory
26
Q

Non-selective NSAIDS block _______.

Selective NSAIDS block ______.

______ blocks COX 3 and is not categorized as an NSAID.

A

COX 1 and COX 2

COX 2 only (Celebrex - celecoxib)

Tylenol

27
Q

T/F

Acetylsalicylic Acid reduces pain by inhibiting prostaglandin synth and works on COX 1 and 2.

A

True

28
Q

Aspirin produces a peak effect on an empty stomach in _______.

A

30 minutes

29
Q

Aspirin is widely distributed and ____ to plasma proteins

A

Poorly bound

30
Q

Aspirin displays ______ kinetics, so its half-life is dose-dependent.

A

Zero-order kinetics

*constant amount, rather than constant %, is eliminated

31
Q

Aspirin is a ____ and a ______ and a ______.

A

Analgesic

Antipyretic

Anti-inflammatory

32
Q

What is the anti-inflammatory dose of Aspirin?

What will this dose do if chronically taken?

A

3500 mg/day

GI ulceration/bleeding

33
Q

A dose of aspirin greater than _____/day is considered _______.

What was this dose once used to treat?

What is used to treat gout now?

A

3 g Uricosuric (excrete uric acid)

Gout

Probenecid (Benemid)

34
Q

Low doses of aspirin can have the opposite effect of high doses in what way?

Hx of what makes aspirin no longer a choice?

A

Uric acid retention

Gout

35
Q

How long does the anti-platelet effect of Aspirin last?

A

7-10 days

*Irreversible effect (lasts for life of platelet)

36
Q

Aside from Aspirin’s anti-platelet effect, what is another way it reduces blood clots?

A

COX inhibitor shuts down Thromboxane A2

*Thromboxane A2 causes vasoconstriction and platelet aggregation

37
Q

What is the low dose of Aspirin used to prevent stroke/heart attack?

A

81 mg

38
Q

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

A

Aspirin

39
Q

What is contraindicated in children with viral infections?

What is this called?

How does it manifest?

A

Aspirin

Reye’s Syndrome

Diarrhea/vomiting concentrated aspirin in blood.
Hepatotoxicity.
Fluid on brain (encephalitis)

40
Q

At high doses, aspirin can cause tinnitus, confusion, dizziness, etc, along with Acidosis. This leads to ______.

_______ ensues.

A

Hyperventilation

Respiratory/Metabolic Acidosis

*death from OD on aspirin usually acidosis/electrolyte imbalance from 6-10 grams

41
Q

T/F

Aspirin allergy is less than 1%, but many report allergy (usually stomach problems).

A

True

42
Q

If allergic to Aspirin, what is a cross-sensitivity?

A

other NSAIDS

*avoid aspirin, all NSAIDS

43
Q

What is the Aspirin hypersensitivity triad?

A

Aspirin hypersensitivity

Asthma

Nasal polyps

44
Q

Describe the mechanism of the Aspirin allergy:

A

COX cascade inhibits PGE2 (bronchodilator)

Forms leukotrienes (bronchoconstrictors)

*looks like asthma attack

45
Q

Due to the mechanism of Aspirin allergy, what is contraindicated for use?

A

Asthma

46
Q

What are the 5 Contraindications for Aspirin?

A

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

47
Q

Full strength dose aspirin:

prevention dose aspirin:

A

325 mg

81 mg

48
Q

How can a person taking Aspirin (damaged platelets) still clot?

A

Fibrin

Thromboxane A2 still made by endothelial cells

49
Q

What compound does COX mediate that affects formation of prostaglandin precursors and thromboxanes?

A

Arachidonic Acid

50
Q

How are NSAIDS and Aspirins effects different on platelets?

A

NSAIDS reversible on blood platelets

51
Q

Ibuprofen has a half life of _____

Naproxen has a half life of _____

A

1 day

4 days

*this might be 4-5 half lives - time to be off drug before procedure

52
Q

What prophylactic can ibuprofen interfere with?

A

Low dose aspirin - 81 mg

*interferes with anti-platelet effect

53
Q

In order to not interfere with Aspirin’s effects, ibuprofen should be given _____ after aspirin is ingested or _______ before aspirin ingestion.

A

40 minutes after

8 hrs before

54
Q

What are 5 adverse side effects of NSAIDS?

A

Cardiovascular - MI, stroke, hypertension

Renal - function, nephrotoxicity

GI - bleeding in elderly, more than 3 drinks/day

CNS - dizziness, tinnitus, sedation

Skin rxns

55
Q

______ is worse for kidneys and ____ is worse for liver, however both with damage both.

A

Ibuprofen

Tylenol

56
Q

What syndrome sloughs skin from palms/feet and is associated with hypersensitivity to NSAIDS?

A

Steven-Johnson syndrome

57
Q

How do NSAIDS damage the kidney (lead to necrosis in some cases)?

A

Prostaglandin inhibition shuts down renal blood flow

*5 days high dose dangerous for kidney

58
Q

ibuprofen OTC dose

Rx dose:

onset:

duration:

1/2 life:

A

200 mg

400-800 mg

30-60 min

4-6 hrs

2-4 hrs

59
Q

ibuprofen Dental dosing children:

adults:

max adult daily dose:

A

4-10 mg/kg (every 6-8 hrs)

200-400 mg (every 4-6 hrs)

1200 mg

60
Q

ibuprofen 400-600 mg every ___ hrs for 24 hrs before dental procedure decreases post-op _____ and hastens healing time

A

6

edema

61
Q

What is the “ceiling” for dental pain in an ibuprofen dose?

A

400 mg

*chronic inflammatory pain pts take more - but days/weeks to reach effects

**beyond 400 little analgesic effect gained

62
Q

3 names for naproxen:

A

Aleve

Anaprox

Naprosyn

63
Q

Naproxen analgesic onset:

half life:

duration:

dental dose:

max/day:

A

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

64
Q

Name 4 important NSAIDS used in dentistry (in other category):

A

piroxicam (Feldene) - longest lasting nsaid (45-50 hr 1/2 life)

flurbiprofen (ANSAID)

ketorolac (Toradol) - injection, opioid level relief

diflunisal (Dolobid)

65
Q

T/F

Prescription drugs, expensive drugs, colored pills all give more pain relief (placebo effect)

A

True

66
Q

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

A

True

True

67
Q

What drug reduces risk for adenocarcinoma of the colon, improves lung cancer, and delays onset/degree of Alzheimer’s?

A

Celebrex (celecoxib)

68
Q

T/F

Celebrex (celecoxib) is contraindicated with low-dose Aspirin use.

A

False

*perfectly ok to use with

69
Q

T/F

Celebrex (celecoxib) is contraindicated with Aspirin/NSAID allergy?

A

True

70
Q

What is the main side effect of Celebrex (celecoxib)?

What atom does Celebrex (celecoxib) contain that may cause allergy?

A

Unanticipated bleeding

Sulfa

71
Q

T/F

Celebrex (celecoxib) in contraindicated with Hx of gastritis/gastric ulcer/GI bleeding AND pregnancy

A

True

*unanticipated bleeding side effect

72
Q

What drug, used for autoimmune diseases and cancer, does ibuprofen interfere with?

How does ibuprofen interfere?

A

Methotrexate

Metabolic breakdown - causes toxicity

73
Q

What 2 drugs interfere with Methotrexate?

How?

A

Ibuprofen - metabolic breakdown (toxicity)

Aspirin - displaces and interferes with clearance (toxicity)

74
Q

Lithium excretion is blocked by what?

A

NSAIDS

75
Q

How can Aspirin and NSAIDS be taken together?

A

Separate dosing intervals

76
Q

Taking several NSAIDS together can have an additive toxic effect.

Alcohol increases GI bleeding associated with NSAIDS

A

True

True

77
Q

_______ and ________ can decrease the effectiveness of many common antihypertensive medications.

(diuretics, beta blockers, ACE inhibitors)

A

Aspirin

NSAIDS

78
Q

7 contraindications/cautions with NSAIDS

A

Asthma

CV

Renal

Coagulopathies

Ulcers (stomach, colitis)

Allergy to Aspirin/other NSAIDS

Geriatrics

79
Q

Acetaminophen acts on COX 3 in CNS (more than peripheral) and doesn’t do what 3 things?

A

Inhibit platelet aggregation

Irritate GI tract

Cause bronchoconstriction

80
Q

Acetaminophen is hepatotoxic and excreted by what?

A

Kidneys

81
Q

Why shouldn’t you take Tylenol for arthritis?

A

NOT anti-inflammatory

82
Q

Tylenol is equally potent to ______

No ____ irritation

A

Aspirin

Gastric

83
Q

What is the max dose acetaminophen/day?

A

4000 mg (4 grams)

*although Tylenol brand now limits to 3 grams/day

84
Q

Acetaminophen and Aspirin are equally _____ and equally ______, but ______ is less useful clinically.

A

Efficacious

Potent

Acetaminophen (b/c NOT anti-inflammatory)

85
Q

Three characteristics absent Acetaminophen:

2 characteristics it has:

A

No anti-inflammatory effect, no effect on uric acid, no anti-coagulant effects

Analgesic and Antipyretic

86
Q

Acetaminophen dental dosing Children:

Adults:

Max adults:

Max in pts regularly consume alcohol:

A

10-15 mg/kg (every 4-6 hrs)

325-650 mg (every 4-6 hrs)

4 grams/day

2 grams/day

87
Q

2 situations to avoid using Acetaminophen:

A

Liver disease

Alcoholism

  • more than 3 drinks/day increases risk liver damage
  • *alcohol stimulates (enzymes that lead to) acetaminophens toxic metabolite
88
Q

Acetaminophen combined with _______ leads to an increased bleeding risk.

A

Warfarin (coumadin)

  • enhanced anticoagulation
  • **increases 10-fold according to one study
89
Q

T/F

Aspirin is more effective if given prior to initiation of pain

A

True

90
Q

T/F
Aspirin and NSAIDS are Analgesics, Antipyretics, and Anti-inflammatory

Tylenol is an Analgesic and Antipyretic

A

True

91
Q

Describe the GI side effects of Aspirin:

A

Dyspepsia, nausea, vomiting, gastric bleeding

  • direct irritation/inhibition cytoprotective prostaglandins
  • stimulated trigger zone in CNS for nausea/vomiting
  • exacerbates ulcers, etc (acid)
92
Q

NSAID analgesia occurs at what dose?

NSAID anti-inflammatory effects occur at what dose?

A

up to 400

over 400 (400-800 4x/day)

93
Q

Prescription for ibuprofen for Dental Pain:
Rx:

Disp:

take:

Do not exceed:

A

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.

94
Q

What is the longest lasting NSAID?

dose?

half life?

A

piroxicam (Feldene)

10 mg 2x/day

45-50 hrs

95
Q

flurbiprofen (ANSAID) dose:

onset:

1/2 life:

A

100 mg every 12 hrs

1-2 hrs

5.7 hrs

96
Q

ketorolac (Torodol) use up to ___ days.

Primarily given by _____.

Causes _____ damage.

A

5

injection

Renal

97
Q

diflunisal (Dolobid), aka?

onset:

duration:

1/2 life:

A

Super Aspirin (but just like aspirin)

1 hr

8-12 hrs

8-12 hrs

98
Q

Presciption for diflunisal (Dolobid) Rx:

Disp:

Sig:

A

Rx: Dolobid 500 mg tablets

Disp: 16 tablets

Sig: Take 2 tablets initially, then 1 tablet every 8-12 hours as needed for pain

99
Q

T/F

Cox 2 inhibitors are contraindicated with pregnancy

A

True

*no ibuprofen if prego

100
Q

For high risk surgeries, Aspirin use must be discontinued _______ prior to surgery.

A

1-2 weeks

  • platelets must regenerate
  • *don’t take off if known risk factors for Heart Disease
101
Q

NSAIDS should be discontinued by counting 4-5 half lives prior to surgery to prevent what?

A

Bleeding

*platelet effects reversible

102
Q

What increases the Excretion of Aspirin?

A

Alkalinization by sodium bicarb (aspirin more ionized and excreted more)

103
Q

T/F
Aspirin inhibits prostaglandin synth in the hypothalamus

(which prevents the induction of peripheral vasodilation/sweating)

A

True

104
Q

High dose aspirin, above ____ mg, is used for arthritis management.

A

True

*chronic use leads to GI probs

105
Q

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

A

True

106
Q

Narcotics = Opiates = Opioids

What is found in Opium?

A

Opioids latest/correct term

Alkaloids found in Opium

107
Q

T/F

Opioid receptors are the site of opioid action

A

True

*mediate specific pharmacologic effects

108
Q

Where is the Analgesic Effect of Opiates produced in the brain?

A

Midbrain pain-modulating circuit

medulla/spinal cord/dorsal horn

109
Q

Where are high concentrations of Endogenous Opioid peptides found?

Where does Systemic Administration of Opiods produce its analgesic effect?

A

Descending Pain Modulating Circuit

CNS - widely distributed in spinal cord and brain

110
Q

The Pain Suppressor System (descending) involves ________ and _______ neurotransmitters.

A

Serotonin

Enkephalin-mediated (endogenous)

111
Q

What are the 3 major components that mediate the Descending Analgesia System?

*opioids put directly into these 3 areas will have profound effects

A

Periaquaductal Grey Matter (midbrain)

Nucleus Raphe Magnus (medulla)

Inhibitory Neurons (dorsal horns)

112
Q

Projections from the Periaqueductal Gray Matter (midbrain) are _____ and highly sensitive to morphine.

Projections from the dorsolateral pons are ______.

A

Serotonergic

Noradrenergic

113
Q

T/F

Endogenous Opioids act as neurotransmitters, and are implicated in the mechanisms for the Placebo effect.

A

True

*brain actually releases endogenous opioids.

114
Q

Name 3 groups of Endogenous Opioids.

A

Endorphins

Enkephalins

Dynorphins

115
Q

Endogenous Opioids (endorphins, enkephalins, dynorphins) act through what 3 different G protein coupled receptors?

A

mu

delta

kappa

116
Q

T/F

Endorphin can refer to all endogenous opioid peptides or a single specific opioid called Beta-endorphin.

A

True

117
Q

What 2 sites produce Endogenous Opioids?

A

Pituitary Gland

Hypothalamus

118
Q

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 _____.

A

mu, appetite, sex

mu, delta

kappa

119
Q

What endogenous endorphin acts via mu?

via mu and delta?

via kappa?

A

Beta-endorphin

Enkephalin

Dynorphin

120
Q

Endorphins are comprised of ____ families of enkephalin-sequenced peptides.

A

3

*Proenkephalin A and B, and Pro-opiomelanocortin are the precursor molecules

121
Q

Name 4 places Endorphins are found:

A

Pancreatic Islet Cells

Sympathetic Nervous System

Adrenal Medullary Chromaffin Cells

CNS

122
Q

B-endorphin is distributed all over the brain, is involved in BP, temperature, food intake, and acts via ____ receptor.

A

Mu

123
Q

Why do opioids cause constipation?

A

Mu receptors in GI tract

124
Q

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?

A

Enkephalins

Enkephalins

125
Q

What accounts for the side effects (resp. depression, pupil constriction, decrease in body temp, and decrease in gut motility) of opioids?

A

Opiate receptors found in tissues NOT involved in Analgesia.

126
Q

T/F

The recognition site (receptor site) is highly specific for Opioids

A

True

127
Q

Name 5 Opioid receptor subtypes:

*which has best analgesic effect and is most addictive?

A

Mu (best analgesic/most addictive)

Delta

Kappa

Epsilon

Sigma (no longer opioid receptor)

128
Q

What are the 2 subclassifications of Mu and what are their effects (3/1)?

A

Mu1 - Supraspinal analgesia, euphoria, physical dependence

Mu2 - Respiratory Depression

*Mu1 causes addiction

129
Q

A drug must bind to ____ to be physically addicting

A

Mu

130
Q

Drugs that bind to Mu have the best _____.

____ is the downside.

A

Analgesic properties

Addiction

131
Q

What opioid receptor causes Spinal analgesia, miosis (pinpoint pupils), and sedation?

A

Kappa

132
Q

What opioid receptor causes Analgesia, Emotion, and Seizures?

A

Delta

*rec use effect

133
Q

What opioid receptor causes Analgesia (only listed effect)?

A

Epsilon

134
Q

What opioid receptor causes Autonomic stimulation, Dysphoria, Hallucinations, nightmares, respiratory stimulation, tachycardia, and anxiety?

A

Sigma

135
Q

What is determined by the strength of attachment of an opioid to its binding site?

A

Potency

136
Q

Opioids cause _______ of nerve cells, ______ of nerve firing and _______ of transmitter release.

A

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.

137
Q

The hyperpolarization makes less likely to respond to pain stimuli (inhibits Ca++ influx also) - this all decreases neurotransmitter release.

A

True

138
Q

Name 2 Opium Alkaloids

A

Morphine

Codeine

139
Q

Name 4 Semi-synthetic opioids

A

Heroin

Oxycodone

Hydrocodone

Hydromorphone

140
Q

Meperidine, methadone, fentanyl, pentazocine, buprenophine, tramadol, etc are all _______.

A

Fully synthetic opioids

141
Q

Agonists elicit a ______, and Antagonists block agonists by ______.

A

Receptor response

Binding receptor

142
Q

Morphine is a ______ Agonist

It has _____ Analgesia

It is ____ and ____ activated

A

Pure

Unlimited

Mu, Kappa

143
Q

T/F

Tolerance happens with all opioids and Cross-tolerance also occurs

A

True

144
Q

What drug acts as a Mu and Kappa Antagonist and is given for any OD.

  • no analgesia
  • *will reverse respiratory depression (all opioid depression)
A

naloxone (Narcan)

145
Q

Opioid Distribution:

Metabolism:

Duration of Action:

Excretion:

A

1st pass, goes to fetus

Glucuronic acid conjugation in Liver

4-6 hrs orally

Metabolites exit in urine

146
Q

4 Clinical uses of Opioid Drugs:

A

Analgesia

Sedation/euphoria

Cough suppression

GI (diarrhea)

147
Q

Physical addiction, Respiratory depression, Constipation, Emesis (nausea), Miosis, Urinary retention, CNS stimulation, CV, Biliary tract constriction, Histamine release are all adverse effects of Opioids

A

True

148
Q

What would indicate an allergy to an Opioid?

A

GI cramping and diarrhea

149
Q

Most hypersensitivity rxns to Opioids are _____

A

Dermatologic

150
Q

In dentistry, what are the 2 clinical indications for Opioid use?

(there are more in medicine)

A

Analgesia

Sedation

151
Q

Opium is the dried juice obtained from the unripe seed capsules of the poppy plant _______.

A

Paparer somniferum

*25% dried juice alkaloids (morphine, codeine, etc)

**when smoke opium, mostly morphine and codeine

152
Q

Name six Pure Agonists opioids like morphine:

heroin is also a pure agonist

A

oxycodone (Percodan, Percocet)

hydrocodone (Vicodin, Lorcet)

codeine

dihydrocodeine (Synalgos D-C)

meperidine (Demerol)

fentanyl

153
Q

What mixed agonist/antagonist is equally potent as morphine and has superior oral efficacy?

What is it used for (2 things)?

A

Methadone (C-II)

Detox, chronic pain therapy

154
Q

What antidote for an Opioid OD is given orally or IM?

What antidote is given IV to reverse OD of fentanyl and meperidine?

A

naltrexone (Depade, ReVia, Vivitrol)

naloxone (Narcan)

155
Q

What “new” antagonist acts as a partial agonist (partial Mu agonist/weak Kappa antagonist)?

A

buprenorphine and naloxone (Bunavail)

*naloxone is the pure antagonist

156
Q

Morphine is the Prototype Pure Agonist that acts like internal _____/______.

A

Enkephalins/Endorphins

157
Q

How is morphine generally administered?

A

IM

  • oral poorly absorbed
  • *not used in dentistry
158
Q

What is the most widely abused drug by hospital personnel (b/c no miosis)?

A

meperidine (Demerol)

159
Q

What are the primary side effects to the synthetic drug meperidine (Demerol)?

*not as much sedation and euphoria as morphine/heroin

A

Nausea

Respiratory Depression (risk of death in addicts)

160
Q

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)

A

IV sedation (conscious)

Respiratory depression risk lower - wider margin of safety

161
Q

What opioid, with many GI side effects, is one of the most frequently prescribed in dentistry?

Why is it given instead of morphine?

A

codeine *Tylenol III

can give orally

162
Q

What is the optimum dose of codeine?

What is the potency compared to morphine?

A

60 mg

1/6 (10 mg morphine = 60 mg codeine)

163
Q

What is the drug of choice for cough suppression?

A

codeine

164
Q

codeine is indicated for moderate to moderately severe pain - what should you prescribe for severe pain?

A

oxycodone

165
Q

Name 5 adverse rxns to codeine:

A

Nausea

Dizziness

Excitability

Constipation

Allergy - skin or asthma-like

166
Q

What is the proper codeine dosing?

What system reflects mg concentration of codeine?

A

15-60 mg every 4-6 hrs

1 = 8 mg; 2 = 15 mg; 3 = 30 mg; 4 = 60 mg

167
Q

Tylenol #3 has 300 mg acetminophen and ____mg codeine.

A

30

*Tylenol 1 (8 mg) sold OTC in Canada

168
Q

Fiorinal with codeine (1,2,3) is a combo of _____, aspirin, and ______.

A

Barbituate

caffeine

169
Q

hydrocodone (Vicodin) has acetaminophen that works ________ (as a pain reliever - fever lowering property works centrally) and opioid that works _______.

A

peripherally

centrally

170
Q

hydrocodone (_______) is ____ times more potent than ____.

A

Vicodin

3

codeine

171
Q

Name 2 hydrocodone/acetaminophen drugs that have 300 mg acetaminophen:

1 with 325 acetaminophen:

A

Vicodin, Xodol

Norco

172
Q

hydrocodone also comes with ibuprofen (200 mg, low dose) and has 4 brand names:

A

Ibudone

Reprexain

Vicoprofen

Xylon

173
Q

What drug with the same efficacy and potency of codeine, is no more effective than Tylenol III?

A

dihydrocodeine (Syngalos DC)

174
Q

What Schedule II drug is highly addictive, as potent as morphine, and is used in dentistry in combo products for severe pain?

A

oxycodone

175
Q

Name 4 examples of Oxycodone drugs:

A

Percocet

Percodan

Roxicet (doesn’t separate drug - drug seekers know)

Combunox

176
Q

What drug, 100x more potent that morphine, is used in dentistry?

What is it used for?

3 ways administered?

A

fentanyl

conscious sedation only

IV, transdermal, lollipop

177
Q

Active-Tramadol, EnovaRX-Tramadol, Ultram, Ultram ER, and 3 others (____,_____,____) are the tramadols

A

ConZip

Synapryn

FusePaq

178
Q

What duration should tramadol be used for dental pain?

A

less than or equal to 5 days

179
Q

What drug binds to Mu and inhibits the reuptake of norepinephrine and serotonin?

A

tramadol

180
Q

Tramadol is associated with ______, and has a rare complication of anaphylaxis.

A

Seizures

181
Q

Acetaminophen and tramadol is known as ______.

A

Ultracet

182
Q

What NSAID provides analgesia at the Opioid level and in indicated for moderate to severe dental pain?

How long should this drug be used?

A

ketorolac (Toradol)

5 days

183
Q

Because ketorolac (Toradol) is an NSAID, what complications must we watch for?

A

Bleeding/GI

184
Q

Ketorolac (Toradol) dental dosing for Adults IM:

IV:

Oral:

A

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

185
Q

T/F

Most pts are better managed with NSAIDS

A

True

186
Q

If a patient demands more drugs, what should you do?

A

Refer to pain clinic

187
Q

What is the most widely used opiate agent used for the management of dental pain?

What is the most widely used codeine preparation?

A

hydrocodone (Vicodin or Lorcet)

Tylenol III

188
Q

What drug is prescribed if the pt has a history of codeine allergy?

A

meperidine (Demerol)

189
Q

T/F

morphine and hydromorphone (Dilaudid) are used in Dentistry to manage severe pain

A

False

*these are NEVER used in dentistry

190
Q

Caution/side effects for Elderly Patients, NSAIDS might ______

Aspirin

Opiates

A

GI bleeding

hemorrhage

constipation

191
Q

From highest to lowest, rank Opiates by Potency:

A

fentanyl

morphine = oxycodone

meperidine

hydrocodone (3x codeine)

codeine (1/6 morphine) = dihydrocodeine

192
Q

Opioid medications should only be used for…

The number of dispensed should be no more than…

A

treatment of acute pain

number doses needed

193
Q

T/F

Sharing meds with others is illegal and driving should be avoided

A

True

194
Q

T/F

Dentists use only short-acting opioids, and Long-acting opioids shouldn’t be used for treatment of acute pain

A

True

195
Q

T/F

If pain persists beyond the anticipated treatment duration, the patient should be carefully reevaluated

A

True

196
Q

What database must be checked before prescribing opioids (and periodically when renewing)?

A

Arizona Controlled Substances Prescription Drug Monitoring Program

197
Q

What is one or more prolonged episodes of depression measured in weeks called?

A

Unipolar depression

198
Q

What are 2 subtypes of Unipolar Depression?

A

Primary (endogenous - “chemical imbalance”)

Secondary (exogenous)

*secondary often develops with preexisting nonaffective disorder (trauma, chronic pain, etc)

199
Q

Bipolar (manic depressive) is usually treated with what?

A

Lithium

200
Q

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.

A

True

201
Q

T/F

Women are 2x as likely to experience depression as men

A

True

202
Q

What is the comorbidity between Depression and Anxiety disorders?

A

50%

203
Q

Primary (endogenous) Unipolar Depression is a chemical imbalance of what neurotransmitter in particular?

A

Serotonin

204
Q

What are 3 functions of Serotonin

A

Mood elevator

Sleep

Satiety

205
Q

Affective disorders are associated with what 2 neurotransmitter types in the brain?

A

noradrenergic

serotonergic

*circuitry between the 2 is closely linked

206
Q

Decreased levels of Norepinepherine and/or Serotonin leads to…

Increased levels of these lead to…

A

Depression

Mania

*receptors equally important

207
Q

What are the 2 proposed mechanisms for Antidepressants?

A

Increase extracellular levels of neurotransmitter

Improve Receptor Function

*therapeutic effects are only seen after several weeks of taking drugs

208
Q

Why do women have greater incidence of depression?

A

Estrogen linked to serotonin levels

209
Q

What 2 ways do Antidepressant Drugs increase neurotransmitter in synaptic cleft?

A

Inhibit reuptake

Degrade enzymes (that degrade neurotransmitter)

210
Q

What Antidepressant increases synaptic serotonin and norepinephrine?

Increases synaptic norepinephrine?

Blocks the degradation of norepinephrine, dopamine, and serotonin?

Increases synaptic serotonin?

A

Tricyclics

Tetracyclics

MAO’Is

SSRI’s

211
Q

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?

A

bupropion (Wellbutrin, Zyban)

*b/c of hypertension risk, take BP on pts using this drug

212
Q

MAO is an enzyme responsible for the degradation of what?

MAOI, think ______, _______

A

norepinephrine, serotonin, and dopamine

Old drug, Old people

213
Q

With MAOI’s, take ___ prior to administering local anesthesia, and use caution with ______.

A

BP

Epinephrine

214
Q

4 MAOI’s

A

isocarboxazid (Marplan)

phenelzine (Nardil)

selegiline (Atapryl, Eldepryl, Selpak)

tranylcypromine (Parnate)

215
Q

How do MAOI’s lead to a hyperadrenergic crisis?

what is released in the bloodstream?

What foods to avoid?

A

shuts off enzyme degradation in intestine/liver and vasoactive amines aren’t catabolized -

releases endogenous catecholamines

tyramine (hard cheese, red wine)

216
Q

Name 3 popular SSRI’s

*which is only approved drug for children with OCD?

A

fluoxetine (Prozac, Sarafem)

paroxetine (Paxil)

*sertraline (Zoloft)

217
Q

T/F

Antidepressants increase the risk of suicidal thinking with Major Depressive Disorder

A

True

218
Q

Excitalopram (antidepressant) is not approved for use in ________.

A

children

219
Q

What are the side effects of SSRI’s?

A

Agitation, anxiety, aggression, suicidal ideation (within 6 weeks)

220
Q

T/F

Serotonin syndrome includes tremor, increased bowel sounds, tachycardia, agitation, autonomic instability

A

True

221
Q

Name 4 Serotonin/Norepinephrine reuptake inhibitors
(these are different from Tricyclics - are “selective”)

*which treats fibromyalgia?

A

desvenlafaxine (Pristiq)

duloxetine (Cymbalta)

*milnacipran (Savella) - fibromyalgia

venlafaxine (Effexor XR)

222
Q

Selective serotonin/norepinephrine reuptake inhibitors - should be used cautiously with what?

A

epinephrine

*could lead to too much

223
Q

Effexor XR, generic name:

Therapeutic category:

Oral complications:

A

venlafaxine

selective serotonin/norepinephrine reuptake inhibitor (NOT Tricyclic)

xerostomia, stomatitis, taste, tongue discoloration

224
Q

Name 1 Tetracyclic:

Mechanism?

treats?

A

maprotiline (Ludiomil)

norepinephrine reuptake inhibitor

anxiety with depression

225
Q

Tricyclics block reuptake of _____ and ______ , and have an additional use because it exhibits _______ properties

A

norepinephrine

serotonin

analgesic

226
Q

With Tricyclics, take ____ before local anesthesia, caution with ______

A

BP

epinephrine

227
Q

Tricyclics have ______ effects causing blurred vision and xerostomia, ______ effects causing dizziness and reflex tachicardia, and __________, causing sedation.

A

Anticholinergic

Sympatholytic

Histamine antagonism

228
Q

2 Tricyclics that block norepinephrine and serotonin?

2 Tricyclics that are selective norepinephrine reuptake blockers?

A

amitryptyline (Elavil) *granddaddy

imipramine (Tofranil)

desipramine (Norpramin)

nortripyline (Pamelor)

229
Q

The weed, ______ has many DDI’s and what 4 antidepressive constituents?

A

St. John’s Wort

hyperforin

hypericin

flavonoids

tannins

230
Q

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

A

True

231
Q

Hypericin in St. John’s Wort does what 2 things?

A

cyto P450 inducer in liver

reduced anticoagulant effect of warfarin (increases clotting)

232
Q

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

A

14

233
Q

T/F
The potency and efficacy of all antidepressants are similar

max blood conc 2-4 hrs, one dose/day

A

True

234
Q

Antidepressants can have a side effect of orthostatic hypotension, so watch for ____ in older adults

A

Falling

235
Q

Lithium, used for bipolar disorder, has what 2 brand names?

A

Eskalith

Lithobid

236
Q

T/F

Lithium prevents the release of neurotransmitters and decreases the rate of serotonin synth

A

True

237
Q

Lithium takes how long before improvements are seen?

Also, Lithium has a _____ therapeutic window

A

weeks

very low

238
Q

T/F
Side effects of Lithium include nausea, vomiting, diarrhea, weakness, tremors, renal damage, hypothyroidism, thinning hair, sexual dysfunction

A

True

239
Q

Diuretics, Anticonvulsants, Antihypertensives, and what other class of drug increase lithium levels in the blood and thus its toxicity?

A

NSAIDS

*contraindicated - use acetaminophen instead

Decks in Tim's Cards Class (140):