Non-Opiate Analgesics Flashcards Preview

Pharmacology - Test #4 > Non-Opiate Analgesics > Flashcards

Flashcards in Non-Opiate Analgesics Deck (72):
1

Examples of amine autocoids

Histamine, Serotonin

2

Examples of lipid derived autocoids

PGs and Leukotrienes

3

Peptide hormone autocoids

Bradykinin, Angiotensin

4

Four Classes of NSAIDs

Salicylates (Aspirin)
Arylpropionic Acids (Ibuprofen, Naproxen)
Arylacetic acids (Indomethacin, diclofenac, ketorolac)
Enolic acids (Piroxicam, Meloxicam)

5

Most important p-Aminophenol class drug

Acetaminophen

6

Three therapeutic applications of NSAIDs

Analgesic
Antipyretic (acetaminophen)
Anti-inflammatory

7

In which cases would you relieve pain with tylenol rather than ibuprofen

Headache
Chronic Postsurgical (Tyl + Opioid Mixes)

8

Effects of COX-1 inhibition

Reduction of thromboxanes, causing reduced platelet aggregation. This helps platelets act as a blood thinner. Can inhibit PGE and PGI that are protective in stomach.

9

Effect of PGE2 and PGI2 in the stomach

Inhibit acid secretion
Promote Mucus Secretion
Inhibition leading to stomach ulcers

10

Effects of PGI2 (outside of stomach)

Vasodilation, Reduced Platelet aggregation

11

COX2 inhibition will serve an important role in

inhibition of inflammation induced by cytokines/inflamm. mediators

12

How does Aspirin work?

It irreversibly inhibits cyclooxygenase 1/2 by acetylation of COX. Duration effect corresponds to time required for new protein synthesis.

13

Important details about Salicylate absorption

Rapidly absorbed from stomach and jejunum (asp mostly in jej)
Passive diffusion of free acid
Delayed by presence of food

14

Important details of Salicylate distribution

Throughout most tissues and fluids
Readily crosses placenta
Competes with many drugs for binding sites

15

Salicylate half life

12 hours because its extensively conjugated

16

How do you increase excretion of Salicylates in urine?

Increase urinary pH

17

Ways that non-salicylates are metabolized

Oxidation
Demethylation
Conjugation

18

What patient population do you need to worry about giving aspirin to?

Children -- Reye's Syndrome (Liver failure, deepening coma, seizures, etc.)

19

Common name for Ibuprofen? Naproxen?

Ibuprofen -- Advil
Naproxen -- Aleve

20

Difference between Ibuprofen and Naproxen?

Half Lives
Ibuprofen -- 2 hrs
Naproxen -- 14 hours

21

Important acetic acid derivative pain meds (and basic information)

Diclofenac/Voltaren (Gel for arthritic pain)
Indomethacin (Reversible inhibitor of PG synth)
Ketorolac/Toradol

22

Risks of diclofenac/voltaren

Increased risk of peptic ulcer and renal dysfxn

23

Risks of long term indomethacin

Acute gouty arthritis
Ankylosing spondylitis
Pericarditis

24

Use of enolic acids?

Used to treat arthritis because of great joint penetration
Few GI side effects
Long half life

25

Examples of enolic acids

Meloxicam (20 hrs)
Piroxicam (57 hrs)

26

Advantages of acetaminophen over other NSAIDs

no GI toxicity
No effect on platelet aggregation
No Reyes
In low doses, OK for liver patients

27

Disadvantages of acetaminophen over other NSAIDs

Little clinically useful antiinflammatory activity
acute overdose may lead to fatal hepatic necrosis

28

Adverse effects of salicylate overdose

Metabolic Acidosis
Vertigo/Tinnitus/hearing probs
N/V, Delirium, Psychosis --> Coma

29

Tretment of salicylate poisoning

Reduce salicylate load (urination, dialysis)
Charcoal
Correct Metabolic Imbalance

30

Risks of non-salicylate NSAIDs

GI ulceration
Inhibition of Renal Fxn
Inhibition of Platelet Aggregation
Inhibition of uterine motility

31

Adverse effects of Acetaminophen overuse

Renal toxicity, Papillary necrosis
Dose Dependent Hepatic Necrosis (esp. w/ OH)

32

Name a selective Cox2 inhibitor. Why use one?

Rofecoxib (Vioxx)
Reduce ulcers and GI Bleeds

33

Why was Vioxx taken off the market?

High chance of blood clots, strokes, and MI

34

What is the only Cox2 selective inhibitor left on the market?

Celebrex

35

Who shouldn't use NSAIDs

CKD, Peptic Ulcer Disease, GI bleeders
In high doses, inhibits bone healing

36

What are DMARDs

Disease Modifying Anti-Rheumatic Drugs

37

Three main classes of DMARDs

Antiproliferative agents
IL-1 Blockers
TNF-alpha blcokers

38

Examples of anti-proliferative DMARDs

Methotrexate, Cyclophosphamide, Azathioprine
Leflunomide

39

What are anti-proliferative DMARDs stopping from proliferating

B and T cell proliferation

40

Name the IL-1 Blocking DMARD

Anakinra (kineret)

41

Absolute contraindications for anakinra?

Pre-existing malignancy
Neutropenia

42

Three main TNF-alpha blockers

Etanercept (Enbrel)
Infliximab (Remicade)
Adalimumab (Humira)

43

TNF alpha blockers. How do they work and what are they used to treat

They bock the interaction between macrophages and T cell receptors, downregulating both in the process. Used to treat RA , Crohns, and Ulcerative Colitis

44

Downside of using a TNF-alpha blcoker

Immunosuppressants -- especially contra. for patients with previous TB

45

Fatal toxicities associated with all DMARDs

Hepatotoxicity
Hematotoxicitiy
Teratogenicity
Nephrotoxocity
CV tox

46

Main drugs to give for acute gout

Colchicine + NSAIDs (indomethacin)

47

How does Colchicine work?

Bind to tubulin, which interferes with mitotic spindle fxn
Depolymerized microtubules stop granulocyte migration, phagocytic activity, and inhibits lactate and cytokine release.

48

Adverse effects of Colchicine

Toxic to rapidly proliferating intestinal epithelial cells
Nausea, vomiting, diarrhea, cramps

49

Main drugs for chronic gout

Allopurinol
Febuxostat
Probenecid

50

How does allopurinol work?

Inhibitor of xanthine oxidase
Increased half-life of prebenecid
contra-indicated in acute gout

51

How does febuxostat (Adenuric) work?

Its a new non-purine inhibitor of xanthine oxidase
More effective at lowering serum uric acid than tophus area than allopurinol.

52

How does Probenecid work?

Competes for renal tubular anion transporter
Blocks the reabsorption of urate in prox. tubules

53

What type of Gout should not be treated with probenecid

Overproducers

54

What is psuedogout?

Calcium pyrophosphate dihydrate crystal deposition disease
Leave behing positively birefringent crystals
Chondrocalcinosis on radiographs

55

Which ion channels are associated pain

TRP, Nav, Cav

56

How does blocking sodium channels prevent pain

Prevents hypopolarization/depolarization
Blocks action potentials

57

Mutations of Nav 1.7 cause what

Gain of fxn -- Severe Pain
Loss of Fxn -- diminished patients

58

Topical anesthetics that influence the activity of sodium channels

Lidocaine
Benzocaine
Oxybuprocaine (in optho)

59

Important details about Lidocaine

Local analgesia (dentistry), itching, burning
15 minute local onset, lasts 30-120 minutes

60

Important details for Bupivicaine

Longer lasting than Lidocaine (3.5 hrs), used in epidural anesthesia

61

Important details for Benzocaine

OTC, oral ulcers, ear pain
Lower allergy risk

62

Name important Sodium channel blockers

Lamotrigine
Amitryptiline
Carbamezipine

63

Important details for Lamotrigine

Off label use for peripheral neuropathy, migraine
Risk of developing Stevens Johnsons

64

Important details for amitryptiline?

Post-herpetic neuralgia, Polyneuropathy, Fibro, Visceral Pain
Overdose toxicity

65

Important details for carbamezipine

Used for trigeminal neuralgia, Bipolar, and Seizures
Can be Teratogenic

66

Sodium channel blockers with SNRI's Functionality

Duloxetine (Cymbalta)
Venlafaxine (Effexor)

67

What do you use Duloxetine (Cymbalta) for?

Diabetic Pain, Fibromyalgia, Peripheral Neuropathy

68

Details on Venlafaxine

Used off label for diabetic neuropathic pain
SNRI -- anti-depresant/anxyiolytic

69

List SNRIs that don't have an effect on sodium channel effect and what you use them for

Milnacipran (Fibromyalgia, SNRI)
Tapentadol (Diabetic Neuropathic Pain, NRI)

70

SSRIs used for pain assocaited depression

Fluoxetine (Prozac), Paroxetine (Paxil), Setraline (Zoloft)
Escitalopram, Citalopram

71

Pharmacokinetics of TCA/SNRIs

Rapid Oral Absorption
90% protein bound
Hepatic Metabolism (2D6)
Renal Excretion

72

Calcium channel blockers that have an influence on pain
Diabetic Neuralgia, Fibromyalgia, Neuropathic Pain

Gabapentin (Neurontin)
Pregabalin (Lyrica)
Ziconotide
Levetiracetam