Pain Management Part 1

Front 1

Pathophysiology of Pain- Pain is categorized as either ____ or _____.

Back 1

Acute or chronic

Front 2

Pathophysiology of Pain- What leads to the sensation of pain?

Back 2

The Stimulation of free nerve endings

Front 3

Pathophysiology of Pain- What does the Noxious stimuli pass through?

Back 3

the spinal cord to the thalmus

Front 4

Pathophysiology of Pain- When Noxious stimuli passes through the spinal cord to thalmus what happens?

Back 4

usually endogenous opioids bind to receptors and inhibit the transmission of pain impulses

Front 5

Pathophysiology of Pain- What happens if the pain is too great?

Back 5

then the body is not able to produce enough endogenous opioids to bind to the receptors causing pain

Front 6

Pathophysiology of Pain- These pain Receptors are activated by? (3)

Back 6

mechanical, thermal and chemical impulses

Front 7

Pathophysiology of Pain- The Release of these may activate pain receptors? (5)

Back 7

bradykinins, prostaglandins, histamine, leukotrienes, serotonin

Front 8

Pathophysiology of Pain- The MOA of some of these agents may prevent what?

Back 8

The release of some of these chemical impulses within these receptors.

Front 9

Pathophysiology of Pain- Another subtype of chronic pain is?

Back 9

Neuropathic (chronic) pain

Front 10

Pathophysiology of Pain- With Neuropathic (chronic) pain there is an Abnormal processing of what?

Back 10

sensory input by the peripheral or CNS.

Front 11

Pathophysiology of Pain- In Neuropathic (chronic) pain
Nerve damage may cause what?

Back 11

spontaneous nerve stimulation

Front 12

Pathophysiology of Pain- When Neuropathic (chronic) pain Nerve damage causes spontaneous nerve stimulation, what can happen?

Back 12

The autonomic neuronal pain stimulation and progressive increase in discharge of neurons causes the chronic nueropathic pain syndrome.

Front 13

Pathophysiology of Pain- Some conditions where neuropathic pain is more common include: (6)

Back 13

LBP (low back pain- particularly pain where the discs are encroaching on the nerve endings), diabetic neuropathy, postherpetic neuralgia, autonomic neuronal pain stimulation, cancer related pain, and spinal cord injury

Front 14

Pathophysiology of Pain- For patients who have LBP (low back pain- particularly pain where the discs are encroaching on the nerve endings), diabetic neuropathy, postherpetic neuralgia, autonomic neuronal pain stimulation, cancer related pain, and spinal cord injury these 3 types of drugs may not be as effective, so other avenues must be looked at:

Back 14

Opioid analgesics, NSAIDS, and acetominophen

Front 15

Non-opioid Analgesics include: (2)

Back 15

Tylenol & NSAIDs

Front 16

Non-opioid Analgesics
Acetaminophen (Tylenol®) is found?

Back 16

OTC

Front 17

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Most pt's already start taking this if they have?

Back 17

Any chronic pain or any acute pain syndrome.

Front 18

Non-opioid Analgesics
Acetaminophen (Tylenol®)
What is the MOA?

Back 18

Analgesic and antipyretic activity through inhibition of prostaglandin synthesis.

Front 19

Non-opioid Analgesics
Acetaminophen (Tylenol®)
The Antipyretic activity is due to what?

Back 19

to direct action on hypothalmic heat-regulating center of the brain

Front 20

Non-opioid Analgesics
Acetaminophen (Tylenol®) The Antipyretic activity also Increases dissipation of body heat through what?

Back 20

vasodilation and sweating

Front 21

Non-opioid Analgesics
Acetaminophen (Tylenol®)
inhibits cyclooxygenase enzymes where? (which is (2)?)

Back 21

centrally (COX 1 and Cox 2)

Front 22

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Does not inhibit what?

Back 22

peripheral cyclooxygenase unlike aspirin

Front 23

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Does not inhibit peripheral cyclooxygenase-therefore it limits what, in comparison to what?

Back 23

limiting its anti-inflammatory and antiplatelet effects; Aspirin

Front 24

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Pharmacokinetics
It is Rapidly absorbed from?

Back 24

the GI tract after oral ingestion

Front 25

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Pharmacokinetics
Which form is absorbed faster?

Back 25

Liquid absorbed faster than tablets

Front 26

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Pharmacokinetics
What about protein binding?

Back 26

Has Minimal protein binding at therapeutic doses

Front 27

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Pharmacokinetics
It is extensively metabolized in the liver by? and to a lesser extent by?

Back 27

Extensively metabolized in the liver by CYP 1A2 and to a lesser extent by CYP 2E1

Front 28

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Pharmacokinetics
It is Extensively metabolized in the liver by CYP 1A2 and 2E1 into (3)?

Back 28

inactive conjugates of glucuronic acids
and sulfuric acids
and to a hepatotoxic intermediate.

Front 29

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Pharmacokinetics
The hepatotoxic intermediate is detoxified by?

Back 29

glutathione which is produced w/in the body.

Front 30

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Pharmacokinetics
The hepatotoxic intermediate is detoxified by glutathione. This detoxification process is saturated at?

Back 30

supratherapeutic doses.

Front 31

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Pharmacokinetics
If glutathione stores are depleted in the body by either of these, then what happens?

Back 31

by long-term or toxic doses then hepatic toxicity can occur

Front 32

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Pharmacokinetics
What is the mechanism behind hepatotoxicity with tylenol?

Back 32

The hepatotoxic intermediate is detoxified by glutathione. This detoxification process is saturated at supratherapeutic doses.
If glutathione stores are depleted by long-term or toxic doses than hepatic toxicity can occur

Front 33

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Pharmacokinetics
Maximum adult daily dose is?

Back 33

4g/day

Front 34

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Clinical Uses
Treatment of mild to moderate pain associated with conditions such as (4)

Back 34

arthritis (first-line agent), gouty arthritis, the flu, other viral or bacterial infections

Front 35

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Clinical Uses
Fever?

Back 35

Fever reduction

Front 36

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Clinical Uses
Useful in patients with

Back 36

aspirin allergy, bleeding disorders (i.e. hemophilia), upper GI disease (ulcer, gastritis, hiatal hernia), or those who are receiving anticoagulant therapy (NSAIDs or ASA would be contraindicated here)

Front 37

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Clinical Uses
Drug of choice in elderly due to?

Back 37

less GI and renal effects

Front 38

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Clinical Uses
Can be used in children (dose and time frame)

Back 38

(dose 10-15mg/kg Q4-6 hours)

Front 39

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Clinical Uses

Back 39

Treatment of mild to moderate pain associated with conditions such as arthritis (first-line agent), gout, the flu, other viral or bacterial infections

Fever reduction

Useful in patients with aspirin allergy, bleeding disorders (i.e. hemophilia), upper GI disease (ulcer, gastritis, hiatal hernia), or those who are receiving anticoagulant therapy

Drug of choice in elderly due to less GI and renal effects

Can be used in children (dose 10-15mg/kg Q4-6 hours)

Front 40

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Adverse Effects are generally?

Back 40

very rare

Front 41

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Adverse Effects
when used in recommended doses?

Back 41

Generally well-tolerated

Front 42

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Adverse Effects
Hypersensitivity reactions can occur- 3

Back 42

Skin eruptions, urticaria, fever

Front 43

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Rare Adverse Effects 3

Back 43

hemolytic anemia, leukopenia, neutropenia

Front 44

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Adverse Effects
with doses of 5-8g/day for several weeks (maximum dose is 4g/day) what can occur?

Back 44

Toxic hepatitis has been seen

Front 45

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Adverse Effects
in acute overdose situations these 2 can occur:

Back 45

Fatal hepatic necrosis and renal tubular necrosis

Front 46

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Adverse Effects
Toxicity: first 24 hours you will see: 5

Back 46

nausea, vomiting, drowsiness, lethargy, confusion

Front 47

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Adverse Effects
Toxicity 24-72 hrs

Back 47

liver toxicity (AST/ALT elevation)

Front 48

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Adverse Effects
Toxicity Recovery can last up to

Back 48

to 2 weeks; pt's will recover from an O/D if treated quickly

Front 49

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Drug Interactions are limited, but if used with these (Concommitant use), it
may increase risk of hepatotoxicity: 5

Back 49

barbiturates, carbamazepine, phenytoin, rifampin, ETOH

Front 50

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Drug Interactions safer than ASA/NSAIDS with what drug?

Back 50

warfarin

Front 51

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Drug Interactions
Although safer than ASA/NSAIDS with warfarin, what can be seen with prolonged use of APAP and warfarin?

Back 51

increased INR can be seen

Front 52

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Precautions/Contraindications
Caution in patients with these 2 things?

Back 52

if they have hepatic disease or are chronic alcoholics

Front 53

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Precautions/Contraindications
Caution in patients with hepatic disease-chronic alcoholics should not exceed

Back 53

2g/day

Front 54

Non-opioid Analgesics
Acetaminophen (Tylenol®)
Precautions/Contraindications
Pregnancy category

Back 54

Pregnancy category B-used in all stages of pregnancy and during breast-feeding

Front 55

3 categories of Nonsteroidal Anti-inflammatory Drugs (NSAIDs)

Back 55

Salicylates

“Traditional” non-selective NSAIDS (inhibit both COX-1 and COX-2)

COX-2 Inhibitors

Front 56

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
2 subcategories of Salicylates

Back 56

ASA

meds that contain components of ASA

Front 57

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
Medications in COX-2 Inhibitors (newer class)

Back 57

Celebrex

Vyox used to be in this category before being removed from the market.

Front 58

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)What are the non-combination Acetasalicylic acid, Aspirin, ASA (all OTC)? 4

Back 58

Low dose (baby aspirin) 81 mg
Enteric-coated aspirin
Effervescent tablets (Alka Seltzer)
Regular strength 325 mg

Front 59

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)What are the Nonacetylated salicylates?
4

Back 59

Salsalate (RX, Argesic-SA)
Diflunisal (RX, Dolobid)
Choline magnesium salicylate (RX, Trilcosal)
Magnesium salicylate (OTC, Doan’s)

Front 60

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)Combination Products that are Acetasalicylic acid, Aspirin, ASA
2

Back 60

Aspirin, acetaminophen, caffeine (OTC, Excedrin, Goody’s)

Aspirin, butalbital, caffeine (RX, controlled-Fiorinal)-comes with or without Codeine

Front 61

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)Combination Products that are Nonacetylated salicylates
1

Back 61

Aspirin, caffeine (OTC, Anacin)

Front 62

What is the most common RX product that is a salicylate?

Back 62

Fiorinal

Front 63

What is the most common RX product that is a salicylate can come with or without?

Back 63

codeine

Front 64

What is the most common RX product that is a salicylate can come with or without codeine, and both are what?

Back 64

controlled and cannot be prescribed solely by a NP in FL

Front 65

Fiorinal is a combo of 3 and with or without?

Back 65

Aspirin, butalbital, caffeine

codeine

Front 66

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
4 categories of “Traditional” NSAIDS (inhibit COX-1 and COX-2)

Back 66

Propionic acid derivatives

Nonacidic Compounds

Oxicam derivatives

Acetic acid derivatives

Front 67

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
“Traditional” NSAIDS (inhibit COX-1 and COX-2)
What are the Propionic acid derivatives? 6

Back 67

1) Ibuprofen (RX and OTC strengths available Motrin, Nuprin, Advil)
2) Fenoprofen (Nalfon)
3) Naproxen (Naprosyn), Naproxen sodium (RX-Anaprox, OTC-Aleve)
4) Ketoprofen (RX,generic, OTC-Orudis-KT)
5) Oxaprozin (Daypro)
6) Flurbiprofen (generic)

Front 68

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
“Traditional” NSAIDS (inhibit COX-1 and COX-2)
What are the Nonacidic Compounds? 1

Back 68

Nabumetone (Relafen-generic only)

Front 69

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
“Traditional” NSAIDS (inhibit COX-1 and COX-2)
What are the Oxicam derivatives?

Back 69

1) Piroxicam (Feldene)
2) Meloxicam (Mobic)-more selective

Front 70

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
“Traditional” NSAIDS (inhibit COX-1 and COX-2)
What are the Acetic acid derivatives?

Back 70

1) Indomethacin (IV, PO, Indocin)
2) Etodolac (Lodine)
3) Diclofenac potassium immediate release (Cataflam)
4) Diclofenac & Misoprostil (Arthrotec)
5) Ketorolac (IV, IM, PO, Toradol)
6) Sulindac (Clinoril)
7) Diclofenac potassium delayed release (Voltaren, 1.5% topical gel Pennsaid®)

Front 71

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
“Traditional” NSAIDS they all inhibit COX-1 and COX-2 with the exception of which one? What is important about this?

Back 71

Meloxicam (Mobic)- lesser of adverse effect profile.

Front 72

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
“Traditional” NSAIDS they all inhibit COX-1 and COX-2
Which Acetic acid derivative is solely used in the tx of gout?

Back 72

Indomethacin (IV, PO, Indocin)

Front 73

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
“Traditional” NSAIDS they all inhibit COX-1 and COX-2
Which Acetic acid derivative is specific for renal calculi or kidney stones?

Back 73

Ketorolac (IV, IM, PO, Toradol)

Front 74

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
“Traditional” NSAIDS they all inhibit COX-1 and COX-2
Keorolac or Toradol, which is specific for renal calculi or kidney stones is used in the outpatient settings how?

Back 74

for max of 5 days for renal stones due to potential for AE and toxicity.

Front 75

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
“Traditional” NSAIDS they all inhibit COX-1 and COX-2
Which Acetic acid derivative (topical) has been used with success to treat arthritis?

Back 75

1.5% topical gel Pennsaid (Diclofenac potassium delayed release)

Front 76

Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
“Traditional” NSAIDS they all inhibit COX-1 and COX-2
Which Acetic acid derivative combo helps prevent some of the gastric irritation that can occur with NSAIDs?

Back 76

Diclofenac & Misoprostil (Arthrotec)
It's the misoprostil portion that has this effect!!!!

Front 77

Salicylates & "Traditional” NSAIDS MOA?

Back 77

Nonselective inhibitors of the cyclooxygenase enzyme (COX-1 and COX-2)-which in turn inhibits production of prostaglandins

Front 78

Salicylates & "Traditional” NSAIDS MOA works where?

Back 78

Act on periphery as well as CNS, which is different from Tylenol bc Tylenol only works on the CNS, not PNS.

Front 79

Salicylates & "Traditional” NSAIDS MOA analgesic effects?

Back 79

Inhibition of prostaglandin synthesis that causes a relief of pain.

Front 80

Salicylates & "Traditional” NSAIDS MOA analgesic effects- What do prostaglandins do?

Back 80

Prostaglandins sensitize nerve endings to the action of bradykinin, histamine, and other chemical mediators released during inflammation.

Front 81

Salicylates & "Traditional” NSAIDS MOA analgesic effects- So, if prostaglandins are inhibited, what happens?

Back 81

The nerve endings become desensitized to the pain.

Front 82

Salicylates & "Traditional” NSAIDS MOA Antipyretic
effects-

Back 82

Decreased activity of PGE2
(bc of inhibition of prostaglandins as well- PGE2)

Front 83

Salicylates & "Traditional” NSAIDS MOA Antipyretic
effects- PGE2 acts on the?

Back 83

PGE2 acts on the thermoregulatory center in the hypothalamus to elevate body temperature. 

Front 84

Salicylates & "Traditional” NSAIDS MOA Antipyretic
effects- If PGE2 which acts on the thermoregulatory center in the hypothalamus to elevate body temperature is blocked, what happens? 

Back 84

Body temp cannot rise...

Front 85

Salicylates & "Traditional” NSAIDS What are the 2 MOA that these have that Acetaminophen does not have?

Back 85

Anti-inflammatory
& Anti-platelet effects

Front 86

Salicylates & "Traditional” NSAIDS MOA Anti-inflammatory effects?

Back 86

This is due to the inhibition of prostaglandin synthesis in inflamed tissue, inhibition of other inflammatory mediators, and inhibition of leukocyte migration.

Front 87

Salicylates & "Traditional” NSAIDS MOA Anti-inflammatory effects this activity is through the inhibition of?

Back 87

This activity is through inhibition of peripheral cyclooxygenase, unlike Acetaminophen which is only in the CNS.

Front 88

Salicylates & "Traditional” NSAIDS MOA Anti-platelet effects are caused by?

Back 88

Decreased production of thromboxane (a key mediator of platelet function which influences platelets to change shape, release granules and aggregate)

Front 89

Salicylates & "Traditional” NSAIDS MOA Anti-platelet effects, so if there is a Decreased production of thromboxane, what happens?

Back 89

platelets can't change shape and aggregate

Front 90

Salicylates & "Traditional” NSAIDS MOA Anti-platelet effects activity is through inhibition of?

Back 90

peripheral cyclooxygenase.

Front 91

Salicylates & "Traditional” NSAIDS Pharmacokinetics
They are both absorbed how?

Back 91

Rapidly absorbed in the GI tract

Front 92

Salicylates & "Traditional” NSAIDS Pharmacokinetics
Uniquely to ASA Bioavailability of ASA depends on

Back 92

formulation (enteric-coated or not, if there is gastric contents (food in tummy) and if gastric pH is decreased (acidic), then bioavailability is decreased. Antacids increase gastric pH (alkalinity) in stomach and bioavailability increases.

Front 93

Salicylates & "Traditional” NSAIDS Pharmacokinetics, what about protein and these agents?

Back 93

Highly protein bound with ASA being somewhat less than < NSAIDS

Front 94

Salicylates & "Traditional” NSAIDS Pharmacokinetics
Onset of action/half life depends on what?

Back 94

the formulation (which can vary depending on the agent used)

Front 95

Salicylates & "Traditional” NSAIDS Pharmacokinetics
Metabolized by the ____ & excreted _____

Back 95

liver (hepatic metabolism) & renally excreted

Front 96

Salicylates & "Traditional” NSAIDS Pharmacokinetics
Which of these agents are particularly metabolized by CYP2C9? (3)

Back 96

1) Piroxicam (Feldene)

2) Meloxicam (Mobic)
Both of the above are
“Traditional” NSAIDS Oxicam derivatives

3) Ketorolac (Toradol)- which is an Acetic acid derivative traditional NSAID

Front 97

Salicylates & "Traditional” NSAIDS Clinical Uses: Treatment of mild to moderate pain in conditions such as (5)

Back 97

rheumatoid and osteoarthritis, gouty arthritis, dysmenorrhea, post-operative pain

Front 98

Salicylates & "Traditional” NSAIDS Clinical Uses: These sx's associated with the flu

Back 98

Fever reduction and pain relief associated with the flu and other viral infections (ibuprofen safe for use in children, 6-10mg/kg Q6-8 hrs)

Front 99

Salicylates & "Traditional” NSAIDS Clinical Uses: ibuprofen safe for use in children (dose and frequency)

Back 99

(ibuprofen safe for use in children, 6-10mg/kg Q6-8 hrs)

Front 100

Salicylates & "Traditional” NSAIDS Clinical Uses: Indomethacin

Back 100

Indomethacin-only used in the treatment of acute gouty arthritis

Front 101

Salicylates & "Traditional” NSAIDS Clinical Uses: baby aspirin

Back 101

Prevention of MI

Front 102

Salicylates & "Traditional” NSAIDS Clinical Uses: aspirin (3)

Back 102

Stroke prophylaxis (aspirin)
Adjunct in acute MI and stroke (aspirin)

Front 103

Salicylates & "Traditional” NSAIDS most common Adverse Effects:

Back 103

GI

Front 104

Salicylates & "Traditional” NSAIDS Adverse Effects: GI

Back 104

GI distress (~20%), gastric erosion*, peptic ulcer formation and perforation, and inflammation of duodenum and large intestine

Hepatic problems

Front 105

Salicylates & "Traditional” NSAIDS Adverse Effects: GI, Hepatic problems are most frequently associated with the use of (2)

Back 105

the propionic acid and acetic acid classes

Front 106

Salicylates & "Traditional” NSAIDS Adverse Effects: Renal (3)

Back 106

1) Related to inhibition of prostaglandins which maintain renal perfusion*-so if the prostaglandins are inhibited, then renal perfusion is decreased, and this causes #2:

2) Can produce renal failure in patients with preexisting reduced blood flow*

3) Not to be given when dehydration is a concern (pt is dehydrated)-may result in renal failure

Front 107

Salicylates & "Traditional” NSAIDS Adverse Effects: 2 CV

Back 107

fluid retention*, edema*

Front 108

Salicylates & "Traditional” NSAIDS Adverse Effects: 2 Hypersensitivity reactions

Back 108

rash, anaphylactic reactions

Front 109

Salicylates & "Traditional” NSAIDS Adverse Effects: 3 Heme

Back 109

anemia, thrombocytopenia*, neutropenia (since non-salicylate NSAIDS are reversible inhibitors of cylcooxygenase, effect on platelets is less)

Front 110

Salicylates & "Traditional” NSAIDS Adverse Effects: CNS (less common)

Back 110

aseptic meningitis, cognitive dysfunction in elderly patients, indomethacin may aggravate depression or other psychiatric disorders

Front 111

Adverse Effects of Salicylates (in addition to the ones that are common with the traditional NSAIDs: Salicylism which includes: 3

Back 111

tinnitus, hearing loss, vertigo (all reversible when meds are discontinued)

Front 112

Adverse Effects of Salicylates (in addition to the ones that are common with the traditional NSAIDs: Large doses can produce

Back 112

Large doses can produce liver injury. Not recommended for patients with chronic liver disease.

Front 113

Salicylates (in addition to the ones that are common with the traditional NSAIDs: Acute overdose of Salicylates you will see: 6

Back 113

may be fatal. Metabolic acidosis, nausea, vomiting, stupor, coma, hyperthermia

Front 114

Salicylates and traditional NSAIDs
Drug Interactions: The NSAIDs and to a lesser extent salicylates May reduce the antihypertensive effects of (3)

Back 114

diuretics, beta blockers, and ACE inhibitors.

Front 115

Salicylates and traditional NSAIDs
Drug Interactions: anticoagulant effects?

Back 115

Large doses may increase anticoagulant effects

Front 116

Salicylates and traditional NSAIDs
Drug Interactions: Why is aspirin more likely to increase risk of bleeding with anticoagulants?

Back 116

due to more profound anti-platelet effects

Front 117

Salicylates and traditional NSAIDs
Drug Interactions: What happens to the clearance of lithium with these drugs and why?

Back 117

May decrease clearance of lithium, bc lithium is renally excreted, and these drugs decrease renal perfusion increasing the chance of lithium toxicity.

Front 118

Salicylates and traditional NSAIDs
Drug Interactions: Effects of Alcohol on these drugs?

Back 118

Alcohol may increase risk of GI toxicity

Front 119

Salicylates and traditional NSAIDs
Drug Interactions: Effects of cyclosporine (immunosuppressant drug used to prevent rejection in transplants) with these drugs?

Back 119

Increased risk of renal dysfunction with cyclosporine

Front 120

Salicylates and traditional NSAIDs
Drug Interactions: Effects of methotrexate with these drugs?

Back 120

Decreased clearance of methotrexate

Front 121

Salicylates and traditional NSAIDs
Drug Interactions: What is methotrexate used for?

Back 121

Tx of RA and is a chomotherapy agent.

Front 122

Salicylates and traditional NSAIDs
Precautions/Contraindications
Contraindicated in patients with: (4)

Back 122

syndrome of nasal polyps, angioedema,
asthma,
& to any bronchospastic reactivity to aspirin or other NSAIDS

Front 123

Salicylates and traditional NSAIDs
Precautions/Contraindications
Use with caution in patients with pre-existing (5) or risk factors for (1)

Back 123

renal disease,
CHF,
cirrhosis,
ulcer
or GI bleeding

peptic ulcer disease (alcohol, smoking)

Front 124

Salicylates and traditional NSAIDs
Precautions/Contraindications
May combine NSAIDS with _________ with GI distress

Back 124

misoprostol 200mcg QID

Front 125

Salicylates and traditional NSAIDs
Precautions/Contraindications
NSAIDS have black box warning regarding: (3) and risk increased with

Back 125

possible CV thrombotic events, MI and stroke

risk increases with duration of use and pt already has CV disease or risk factors associated with CV dse.

Front 126

Salicylates and traditional NSAIDs
Precautions/Contraindications
Aspirin is contraindicated in pt's younger than what age and why? Mortality rate?

Back 126

Aspirin associated with the occurrence of Reye's syndrome when given to children with varicella (i.e., chickenpox) or influenza

Very rare condition, but mortality rate is 20-30% if a pt contracts this.

Front 127

Salicylates and traditional NSAIDs
Precautions/Contraindications
What agents are Pregnancy category B in 1st, 2nd trimester (5)? All others are?

Back 127

ibuprofen, ketoprophen, naproxen, flurbiprofen, diclofenac

all others category C

Front 128

Salicylates and traditional NSAIDs
Precautions/Contraindications
What is used with recurrent miscarriages to help prevent future miscarriages?

Back 128

ASA may be used with recurrent miscarriages

Front 129

Salicylates and traditional NSAIDs
Precautions/Contraindications
All agents are category D during 3rd trimester due to risk of what?

Back 129

premature closure of the ductus arteriosis in the fetus

Front 130

COX-2 Inhibitors (2)

Back 130

Celecoxib (Celebrex)

Vyox was in this category but was taken off the market.

Front 131

COX-2 Inhibitors
Mechanism of Action
More selective inhibition of?

Back 131

COX-2-an enzyme that plays a role in pain and inflammation

Front 132

COX-2 Inhibitors
Mechanism of Action
Do not inhibit

Back 132

COX-1 enzyme which helps maintain gastric mucosal protection (all other NSAIDS & ASA inhibit COX-1 which doesn't maintain gastric mucosal protectio). So, with this drug you get less gastric AEs!

Front 133

COX-2 Inhibitors
Mechanism of Action
COX-2 inhibitors have less

Back 133

anti-platelet effects

Front 134

COX-2 Inhibitors
Clinical Uses:
Mild to moderate pain in conditions such as: (3)

Back 134

osteoarthritis, rheumatoid arthritis, and to a lesser extent dysmenorrhea

Front 135

COX-2 Inhibitors
Clinical Uses:
Expensive, reserved for those

Back 135

at increased risk for GI adverse effects that can't tolerate NSAIDs and ASA due to increased GI adverse effects.

Front 136

COX-2 Inhibitors
Pharmacokinetics absorbed?

Back 136

Well-absorbed from the GI tract

Front 137

COX-2 Inhibitors
Pharmacokinetics What happens with protein?

Back 137

Highly protein bound

Front 138

COX-2 Inhibitors
Pharmacokinetics: How are they metabolized?

Back 138

Hepatic metabolism: Celecoxib (> 97%) via CYP 2C9

Front 139

COX-2 Inhibitors
Pharmacokinetics: How are they eliminated?

Back 139

Renally eliminated

Front 140

COX-2 Inhibitors
Drug Interactions
Similar interactions to?

Back 140

See drug interactions for NSAIDS
Similar interactions

Front 141

COX-2 Inhibitors
Drug Interactions
Other meds that are involved with ______ may affect levels of Cox 2 inhibitors

Back 141

CYP2C9;

Inducers can decrease therapeutic effects

Inhibitors can lead to toxicity

Front 142

COX-2 Inhibitors
Drug Interactions with Warfarin?

Back 142

Warfarin-may increase risk of bleeding, however to a lesser extent than traditional NSAIDs and salicylates.

Front 143

COX-2 Inhibitors
Adverse Effects, these Claim to have less ___ effects, although this could still happen. What are they? 5

Back 143

GI; Dyspepsia*, diarrhea, abdominal pain (risk of GI ulcers less than with traditional NSAIDs but cases have still been reported), hepatitis (rare)

Front 144

COX-2 Inhibitors
Derm Adverse Effects? 2

Back 144

rash, urticaria

Front 145

COX-2 Inhibitors
Renal adverse effects-similar to other _______, however, these 2 conditions can occur as well.

Back 145

NSAIDS*;
Renal insufficiency, acute renal failure

Front 146

COX-2 Inhibitors
CV Adverse Effects 2

Back 146

Edema*, hypertension*

Front 147

COX-2 Inhibitors-Celecoxib (Celebrex)
Precautions/Contraindications
BC the MOA is somewhat similar to traditional NSAIDs, the most important precautions and contraindications include pt's with a Hx of?

Back 147

CV dse or CV risk factors & in pt's who have renal insufficiency, it's important to monitor for usage of this med and any AEs.

Front 148

COX-2 Inhibitors-Celecoxib (Celebrex) Precautions/Contraindications
Similar to?

Back 148

Traditional NSAIDs

Front 149

COX-2 Inhibitors-Celecoxib (Celebrex) Precautions/Contraindications
Celecoxib contraindicated in patients with?

Back 149

hypersensitivity to sulfonamides, sulfa

Front 150

COX-2 Inhibitors-Celecoxib (Celebrex) Precautions/Contraindications
Pregnancy category?

Back 150

Pregnancy category C; considered category D in third trimester due to risk of premature closure of the ductus arteriosis

Front 151

COX-2 Inhibitors-Celecoxib (Celebrex) Precautions/Contraindications
Not often used in pregnancy unless?

Back 151

benefits outweigh the risks

Front 152

Opioid Analgesics and Opioid-Like Analgesics:
Test questions on this section will not be asking how you will start pt's on these meds (scheduled), they will be asking?

Back 152

What to monitor for when they are on these agents, AEs, MOAs and such, bc NPs cannot prescribe these without the physician approval in FL.

Front 153

3 Agonists Related to Morphine

Back 153

Morphine (IV, PO-immediate release)Schedule II

PO-sustained release=MS Contin, Oramorph, Kadian) Schedule II

Hydromorphone (IV, PO, Dilaudid)-Schedule II

Front 154

Agonists Related to Morphine PO-immediate release is and what schedule is it?

Back 154

Morphine; Schedule II

Front 155

Agonists Related to Morphine PO-sustained release is and what schedule is it? 3 names...

Back 155

MS Contin, Oramorph, Kadian) Schedule II

Front 156

Agonists Related to Morphine: Hydromorphone AKA what schedule is it?

Back 156

Dilaudid; Schedule II

Front 157

3 Agonists Related to Codeine

Back 157

Codeine (PO, available as codeine or in many combination products) Schedule II, combination products Schedule III

Oxycodone (PO, immediate release as oxycodone or in many combination products, sustained release-Oxycontin) Schedule II

Hydrocodone [available as hydrocodone-Hycodan or in combination products) Schedule III

Front 158

Agonists Related to Codeine
immediate release oxycodone name?

Back 158

oxycodone

Front 159

Agonists Related to Codeine
sustained release oxycodone name?

Back 159

Oxycontin

Front 160

Agonists Related to Codeine
Hydrocodone [available as?

Back 160

hydrocodone-Hycodan

Front 161

Agonists Related to Codeine - Most of these are schedule II drugs except for?

Back 161

The combo drugs

Front 162

6 Synthetic Opioid Agonists

Back 162

Meperidine
Methadone
Propoxyphene
Levorphanol
Fentanyl
Tramadol

Front 163

The 2 most commonly used Synthetic Opioid Agonists

Back 163

Meperidine & Fentanyl

Front 164

Which Synthetic Opioid Agonist is used for pain management and also for pt's who are in recovery for drug addiction?

Back 164

Methadone

Front 165

Which Synthetic Opioid Agonist was very recently taken off the market, when and why?

Back 165

Propoxyphene, Nov. 2010, due to cardiotoxic effects

Front 166

Which Synthetic Opioid Agonist can a NP prescribe and why?

Back 166

Tramadol bc it is a partial agonist and not controlled...

Front 167

Synthetic Opioid Agonists AKA?
Meperidine

Back 167

Demerol

Front 168

Synthetic Opioid Agonists AKA?
Methadone

Back 168

Dolophine

Front 169

Synthetic Opioid Agonists AKA?
Propoxyphene

Back 169

Darvon

Front 170

Synthetic Opioid Agonists AKA?
Levorphanol

Back 170

Levo-Dromoran

Front 171

Synthetic Opioid Agonists AKA?
Fentanyl

Back 171

Duragesic

Front 172

Synthetic Opioid Partial Agonists AKA?
Tramadol

Back 172

Ultram

Front 173

Synthetic Opioid Partial Agonists Tramadol/Ultram comes in a combo product w/ what med and also what formulation?

Back 173

Acetaminophen, ER

Front 174

Combination Products
What is this drug made up of?
Rubitussin-AC

Back 174

Codeine, guaifenesin

Front 175

Combination Products
What is this drug made up of?
Tylenol #2, Tylenol #3, Tylenol #4

Back 175

Codeine, acetaminophen
Schedule III

Front 176

Combination Products
What is this drug made up of?
Vicodin,Vicodin ES, Lortab

Back 176

Hydrocodone, acetaminophen Schedule III

Front 177

Combination Products
What is this drug made up of?
Percodan

Back 177

Oxycodone, aspirin

Front 178

Combination Products
What is this drug made up of?
Percocet, Tylox

Back 178

Oxycodone, acetaminophen
Schedule III

Front 179

Combination Products
What is this drug made up of?
Robitussin-DAC

Back 179

Codeine, guaifenesin, pseudoephedrine

Front 180

Combination Products
What is this drug made up of?
Phenergan with codeine

Back 180

Codeine, promethazine

Front 181

Combination Products
What is this drug made up of?
Darvocet

Back 181

Propoxyphene, acetaminophen
****recent propoxyphene removal from market due to cardiotoxic effects
Schedule IV

Front 182

Combination Products
What is this drug made up of?
Darvon

Back 182

Propoxyphene, aspirin
****recent propoxyphene removal from market due to cardiotoxic effects
Schedule IV

Front 183

Combination Products
What is this drug made up of?
Ultracet

Back 183

Tramadol, acetaminophen
not scheduled

Front 184

What are the 3 types of receptors these stimulate Opioid Analgesics and Opioid-Like Analgesics?

Which ones do you see stimulated the most?

Back 184

Stimulation of µ (mu) receptors

Stimulation of k (kappa) receptors

Stimulation of the (little triangle shape for Delta)(Delta) receptors

The mu and kappa receptors are stimulated the most. The delta receptors are stimulated to a lesser degree and they have antagonistic activity.

Front 185

Opioid Analgesics and Opioid-Like Analgesics Mechanism of Action of Stimulation of µ (mu) receptors? 6

Back 185

Analgesia, euphoria, respiratory depression, miosis (excessive smallness or contraction of the pupil of the eye), decreased gastrointestinal motility, and physical dependence.

Front 186

Opioid Analgesics and Opioid-Like Analgesics Mechanism of Action of Stimulation of µ (mu) receptors analgesic effect is through?

Back 186

alteration of pain perception and emotional response to pain.

Front 187

Opioid Analgesics and Opioid-Like Analgesics
Mechanism of Action of Stimulation of k (kappa) receptors causes?
5

Back 187

Analgesia, respiratory depression, sedation as well as, dysphoria and some psychomimetic effects (i.e., disorientation and/or depersonalization).

Front 188

Opioid Analgesics and Opioid-Like Analgesics
Mechanism of Action of Stimulation of Stimulation of (symbol is a triangle) (Delta) receptors causes?
7

Back 188

Mediates antagonist activity-analgesia, tachycardia, tachypnea, dysphoria, hallucinations, mydriasis (pupil constriction), hypertonia

Front 189

Opioid Analgesics and Opioid-Like Analgesics
What do the mu receptor agonists do (2) and where are they located (2)?

Back 189

1) Mediate analgesia
2) Can cause opioid induced constipation

Located in GI tract and CNS

Front 190

Opioid Analgesics and Opioid-Like Analgesics
What do the mu receptor non-selective antagonists do? 3

Back 190

1) Can reverse the effects of the mu-opioid agonists
2) Can reverse analgesia
3) Can cause central opioid W/D symptoms in pt's who are physically dependant on opioids

Front 191

Opioid Analgesics and Opioid-Like Analgesics
Mechanism of Action
Some of these agents also have Antitussive effects, how does this occur?

Back 191

through direct action on receptors in the cough center of the medulla

Front 192

Opioid Analgesics and Opioid-Like Analgesics
Mechanism of Action
Cough suppression can be achieved how?

Back 192

at lower doses than those required to produce analgesia.

Front 193

Opioid Analgesics and Opioid-Like Analgesics
Mechanism of Action
With these agents Hypotension is possibly due to?

Back 193

an increase in histamine release and/or depression of the vasomotor center in the medulla.

Front 194

Opioid Analgesics and Opioid-Like Analgesics
Mechanism of Action
Often you will see these 2 things with the ingestion of these agents?

Back 194

Peripheral vasodilation, decreased PVR

Front 195

Opioid Analgesics and Opioid-Like Analgesics
Mechanism of Action
Induction of nausea and vomiting with these agents possibly occurs from?

Back 195

direct stimulation of the vestibular system and/or the chemoreceptor trigger zone in the CNS

Front 196

Opioid Analgesics and Opioid-Like Analgesics
Mechanism of Action
Opiate agonists increase smooth muscle tone in these places? 4

Back 196

antral portion of the stomach, the small intestine (especially the duodenum), the large intestine, and the sphincters.

Front 197

Opioid Analgesics and Opioid-Like Analgesics
Mechanism of Action
Opiate agonists also decrease secretions from these? 3

Back 197

the stomach, pancreas, and biliary tract.

Front 198

Opioid Analgesics and Opioid-Like Analgesics
Mechanism of Action
The combination of effects of opiate agonists on the GI tract results in?

Back 198

constipation and delayed digestion.

Front 199

Opioid Analgesics and Opioid-Like Analgesics
Mechanism of Action
What happens with Urinary smooth muscle tone with these agents?

Back 199

Urinary smooth muscle tone is also increased and urinary retention can be seen

Front 200

Tramadol (Ultram)
MOA- not a controlled substance or an _____, but acts as a?

Back 200

opioid, acts as a weak agonist at mu opiate receptor

Front 201

Tramadol (Ultram)
MOA- similar to __________, but also?

Back 201

opiate receptor agonists, but also produces analgesia through inhibiting monoamine reuptake

Front 202

Tramadol (Ultram)
MOA- despite it being a non-controlled substance, this can occur bc of the MOA above?

Back 202

Physical and psychological dependence has been seen

Front 203

Opioid Analgesics and Opioid-Like Analgesics
Pharmacokinetics- how are these absorbed?

Back 203

Rapidly absorbed from GI tract

Front 204

Opioid Analgesics and Opioid-Like Analgesics
Pharmacokinetics- What is the difference btwn PO Morphine and IV Morphine?

Back 204

PO morphine has 1/3 to 1/6 the potency has IV morphine due to significant first-pass metabolism of morphine

Front 205

Opioid Analgesics and Opioid-Like Analgesics
Pharmacokinetics- How are these agents metabolized?

Back 205

Metabolized in the liver (primarily non-oxidative metabolism but some metabolism via CYP2D6)

Front 206

Opioid Analgesics and Opioid-Like Analgesics
Pharmacokinetics- How are these agents excreted?

Back 206

Excreted in the urine

Front 207

Opioid Analgesics and Opioid-Like Analgesics
Pharmacokinetics- How is Tramadol primarily metabolized ?

Back 207

by CYP2D6

Front 208

Opioid Analgesics and Opioid-Like Analgesics
Pharmacokinetics- What is the difference btwn PO and IV Meperidine?

Back 208

Meperidine is about ½ effective orally as compared to IV-oral administration NOT recommended

Front 209

Opioid Analgesics and Opioid-Like AnalgesicsPharmacokinetics- Meperidine is metabolized by?

Back 209

hyrdrolysis, glucuronidation, and demethylation

Front 210

Opioid Analgesics and Opioid-Like AnalgesicsPharmacokinetics- normeperidine is what and is excreted how?

Back 210

normeperidine is active metabolite that is renally eliminated

Front 211

Opioid Analgesics and Opioid-Like Analgesics
Pharmacokinetics- Controlled release formulations of oxycodone and morphine allow for what?

Back 211

less frequent administration and also limits the potential for abuse.

Front 212

Opioid Analgesics and Opioid-Like Analgesics:
Clinical Uses (2)

Back 212

1) Treatment of moderate to severe acute and chronic pain
2) Opiate agonist withdrawal (methadone)

Front 213

Opioid Analgesics and Opioid-Like Analgesics:
Clinical Uses Pregnancy cat?

Back 213

Pregnancy category C; pregnancy category D when used for prolonged periods or at high doses close to term

Front 214

Opioid Analgesics and Opioid-Like Analgesics:
Adverse Effects: CNS 7

Back 214

Sedation*, dizziness*, respiratory depression*, seizures (tramadol, meperidine), euphoria, dysphoria, hallucinations

Front 215

Opioid Analgesics and Opioid-Like Analgesics:
Adverse Effects:
GI/GU: 6

Back 215

nausea*, vomiting*, sweating, constipation*, dry mouth, urinary retention

Front 216

Opioid Analgesics and Opioid-Like Analgesics:
Adverse Effects:
CV 1

Back 216

hypotension*

Front 217

Opioid Analgesics and Opioid-Like Analgesics:
Adverse Effects:
Derm: 2

Back 217

rash, itching due to stimulation of histamine release

Front 218

Opioid Analgesics and Opioid-Like Analgesics:
Adverse Effects:
Signs of intoxication**: 5

Back 218

miosis, drowsiness, decreased rate and depth of respiration, bradycardia, hypotension

Front 219

Opioid Analgesics and Opioid-Like Analgesics
Drug Interactions
Concurrent use with antidiarrheals may cause

Back 219

severe constipation

Front 220

Opioid Analgesics and Opioid-Like Analgesics
Drug Interactions
Concurrent use with other CNS depressants may cause (biggest complication)

Back 220

additive CNS effects and respiratory depression bc they already cause this!

Front 221

Opioid Analgesics and Opioid-Like Analgesics
Drug Interactions
In comparison to the opioids, Tramadol does have more adverse effects. Tramadol levels may be increased by? 5

Back 221

agents that inhibit CYP2D6 (fluoxetine, paroxetine, ritonavir, cimetidine, amiodarone)

Front 222

Opioid Analgesics and Opioid-Like Analgesics
Drug Interactions
In comparison to the opioids, Tramadol does have more adverse effects. These drugs cause an increased risk of seizures with Tramadol? 3

Back 222

SSRIs, TCAs, & phenothiazines

Front 223

Opioid Analgesics and Opioid-Like Analgesics
Drug Interactions
In comparison to the opioids, Tramadol does have more adverse effects. Why does Tramadol increases risk of serotonin syndrome?

Back 223

It has some effects on seratonin, and if you give with other seratonergic agents, you have an increased risk of seratonin syndrome.

Front 224

Opioid Analgesics and Opioid-Like Analgesics
Drug Interactions
Efficacy of tramadol may be decreased by ? 5

Back 224

carbamazepine, barbiturates, phenytoin, fosphenytoin, and rifampin

Front 225

Opioid Analgesics and Opioid-Like Analgesics
Contraindications/Precautions
Avoid abrupt discontinuation of these agents why?

Back 225

withdrawal can be seen

Front 226

Opioid Analgesics and Opioid-Like Analgesics
Contraindications/Precautions
ETOH?

Back 226

Contraindicated with ETOH intoxication

Front 227

Opioid Analgesics and Opioid-Like Analgesics
Contraindications/Precautions
cardiac arrhythmias

Back 227

Contraindicated with cardiac arrhythmias

Front 228

Opioid Analgesics and Opioid-Like Analgesics
Contraindications/Precautions
Extreme caution with head injury and increased ICP why?

Back 228

sx's may be masked by use of opioids

Front 229

Opioid Analgesics and Opioid-Like Analgesics
Contraindications/Precautions
Extreme caution with decreased respiratory reserve (i.e. COPD), why?

Back 229

May worsen ability to breathe bc of resp. depression.

Front 230

Opioid Analgesics and Opioid-Like Analgesics
Contraindications/Precautions
Contraindicated with cardiac arrhythmias such as?

Back 230

SVT

Front 231

Opioid Analgesics and Opioid-Like Analgesics
Contraindications/Precautions
Extreme caution with prostatic hypertrophy or urethral stricture why?

Back 231

Due to the AE of urinary retention

Front 232

Opioid Analgesics and Opioid Analgesics and Opioid-Like Analgesics
Contraindications/Precautions
Extreme caution with elderly or debilitated patients why?

Back 232

AEs are much more pronounced in the elderly

Front 233

Opioid Analgesics and Opioid-Like Analgesics
Contraindications/Precautions
Extreme caution with acute abdominal pain why?

Back 233

Can mask sx's of pain

Front 234

Opioid Analgesics and Opioid Analgesics and Opioid-Like Analgesics
Contraindications/Precautions
Caution with renal and/or hepatic dysfunction why?

Back 234

Toxicity may occur.

Front 235

Opiod Mixed agonist/antagonists and Partial agonist 4

Back 235

Buprenorphine
Nalbuphine
Butorphanol
Pentazocine

Front 236

Opiod Mixed agonist/antagonists and Partial agonist Buprenorphine IV form?

Back 236

IV-Buprenex

Front 237

Opiod Mixed agonist/antagonists and Partial agonist Buprenorphine SL form?

Back 237

sublinqual-Suboxone

Front 238

Opiod Mixed agonist/antagonists and Partial agonist Buprenorphine transdermal form?

Back 238

Butrans**** recently released

Front 239

Opiod Mixed agonist/antagonists and Partial agonist
Nalbuphine IV form

Back 239

Nubain

Front 240

Opiod Mixed agonist/antagonists and Partial agonist
Butorphanol IV form

Back 240

Stadol

Front 241

Opiod Mixed agonist/antagonists and Partial agonist
Butorphanol Nasal Spray form and used for?

Back 241

Stadol NS, migraine HAs

Front 242

Opiod Mixed agonist/antagonists and Partial agonist Pentazocine PO form

Back 242

Talwin- rarely used

Front 243

Opiod Mixed agonist/antagonists and Partial agonist
Most common ones used?

Back 243

Nubain and Stadol NS

Front 244

Mixed agonist/antagonists and Partial agonist
MOA- Bind to what and have low affinity for?

Back 244

kappa receptors but have low affinity for mu receptors

Front 245

Mixed agonist/antagonists and Partial agonist
MOA- Can antagonize the effects of mu-opioid agonists, so consequently?

Back 245

sedation and euphoria not usually noted. Less potential for abuse.

Front 246

Mixed agonist/antagonists and Partial agonist
MOA- As analgesics?

Back 246

are slightly less efficacious in treatment of severe pain and may create some W/D symptoms in pt's taking opioid analgesics that are opioid agonists.

Front 247

Opioid Antagonists 3

Back 247

Naloxone (Narcan)
Nalmephene (Revex)
Naltrexone (ReVia)

Front 248

Opioid Antagonists: Naloxone AKA?

Back 248

Narcan

Front 249

Opioid Antagonists: Nalmephene AKA?

Back 249

Revex

Front 250

Opioid Antagonists: Naltrexone AKA?

Back 250

ReVia

Front 251

Opioid Antagonists
Which is the most common one?

Back 251

Naloxone
or Narcan

Front 252

Opioid Antagonists
Naloxone- Used to? Has a high affinity for?

Back 252

Used to reverse the effects of opiod agonists (so it is an opioid antagonist) so it blocks the mu receptors to reverse the effects of the ingestion of opioids. Has high affinity for mu receptors.

Front 253

Opioid Antagonists
Naloxone- If used to reverse the effects of mixed-acting opioids, must?

Back 253

give higher doses.

Front 254

Opioid Antagonists
Naltrexone is what?

Back 254

A Naloxone analog that has a longer duration of action.

Front 255

Opioid Antagonists
Naltrexone Approved for use in treatment of ?

Back 255

alcohol dependence as well as opioid dependence

Front 256

Similarly to the Mixed agonist/antagonists and Partial agonist All drugs in this class (Opioid Antagonists) can precipitate?

Back 256

a withdrawal syndrome in people physically dependent on an opioid.

Front 257

Agents to Treat Neuropathic Pain- def of NP?

Back 257

chronic pain condition

Front 258

Neuropathic Pain is a chronic pain condition that can be seen in what 3 conditions?

Back 258

diabetes
post-herpatic neuralgia
fibromyalgia

Front 259

Agents to Treat Neuropathic Pain- some agents that are approved for chronic neuropathic pain are?

Back 259

Tricyclic antidepressants*
Some SSRIs*
Cymbalta*- which is an SNRI similar to Effexor
Neurontin*
Lyrica

Front 260

Agents to Treat Neuropathic Pain- only agent we will look at is?

Back 260

Pregabalin (Lyrica®) fairly new came out 4-5 yrs ago

Front 261

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Structurally related to?

Back 261

gabapentin (Neurontin) but greater potency in treating pain and seizures

Front 262

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
MOA- Seizure action

Back 262

unknown

Front 263

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
MOA on pain?

Back 263

Pain-increases GABA at the neuron site
GABA is an inhibitory NT that helps to decrease pain stimulation at the neuron.

Front 264

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
MOA- Produces increases in?

Back 264

glutamic acid decarboxylase activity

Front 265

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
MOA- Reduces what?

Back 265

Reduces neuronal calcium currents which is thought to be the action on treating pain

Front 266

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Pharmacokinetics-
absorbed?

Back 266

Rapidly absorbed in the GI tract

Front 267

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Pharmacokinetics-
bioavailability?

Back 267

90%

Front 268

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Pharmacokinetics-
protein?

Back 268

Not protein bound

Front 269

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Pharmacokinetics- metabolism?

Back 269

No metabolism via liver-no CYP involvement and this is helpful when identifying drugs that don't have drug-drug interactions.

Front 270

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Pharmacokinetics- Excreted

Back 270

Excreted in urine

Front 271

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Pharmacokinetics- Half life

Back 271

Half life 6 hours
so usually dosed 2-3 times per day

Front 272

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)Clinical Uses: 1 for 3 conditions

Back 272

Neuropathic pain
in conditions such as diabetes, post-herpetic neuralgia, and fibromyalgia

Front 273

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Adverse effects
CNS- 8

Back 273

CNS-dizziness*, drowsiness*, ataxia, abnormal gait, confusion, difficulty concentrating, memory impairment
& sometimes pt's will c/o feeling like they are in a fog

Front 274

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Adverse effects
GI-

Back 274

GI-dry mouth*, constipation*, weight gain*

Front 275

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Adverse effects
CV

Back 275

Peripheral edema*

Front 276

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Adverse effects
Hypersensitivity reaction (rare)-

Back 276

angioedema

Front 277

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Adverse effects
With abrupt discontinuation, what happens?

Back 277

insomnia*, N/V, headache which is why it is important to tell pt's they will need to be weaned off of this med.

Front 278

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Drug interactions
very limited, but Increased incidence of peripheral edema and weight gain with?

Back 278

thiazolidinediones (glitazones) for diabetes

Front 279

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Drug interactions
Increased risk of angioedema with concurrent use with?

Back 279

ACE inhibitors, but it is rare.

Front 280

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Drug interactions
Further CNS depression with?

Back 280

with other agents that cause CNS depression and/or alcohol.

Front 281

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Contraindications/precautions
Pregnancy Category?

Back 281

Pregnancy Category C
though not typically used in pregnancy

Front 282

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Contraindications/precautions
Not used in?

Back 282

children < 18 -years old

Front 283

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Contraindications/precautions
In pt's with renal impairment

Back 283

Lower dose in those with renal impairment bc the drug is renally excreted, drug is also cleared via dialysis

Front 284

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Contraindications/precautions
Caution in those with history of?

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Caution in those with history of angioedema type reactions
as this may increase the risk of this type of reaction

Front 285

Agents to Treat Neuropathic Pain- Pregabalin (Lyrica®)
Contraindications/precautions
Caution in patients with CHF
bc of?

Back 285

potential for peripheral edema