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

Non-Opiate Analgesics Flashcards

1
Q

Examples of amine autocoids

A

Histamine, Serotonin

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2
Q

Examples of lipid derived autocoids

A

PGs and Leukotrienes

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3
Q

Peptide hormone autocoids

A

Bradykinin, Angiotensin

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4
Q

Four Classes of NSAIDs

A 
Salicylates (Aspirin)
Arylpropionic Acids (Ibuprofen, Naproxen)
Arylacetic acids (Indomethacin, diclofenac, ketorolac)
Enolic acids (Piroxicam, Meloxicam)
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5
Q

Most important p-Aminophenol class drug

A

Acetaminophen

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6
Q

Three therapeutic applications of NSAIDs

A

Analgesic
Antipyretic (acetaminophen)
Anti-inflammatory

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7
Q

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

A 
Headache
Chronic Postsurgical (Tyl + Opioid Mixes)
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8
Q

Effects of COX-1 inhibition

A

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.

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9
Q

Effect of PGE2 and PGI2 in the stomach

A

Inhibit acid secretion
Promote Mucus Secretion
Inhibition leading to stomach ulcers

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10
Q

Effects of PGI2 (outside of stomach)

A

Vasodilation, Reduced Platelet aggregation

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11
Q

COX2 inhibition will serve an important role in

A

inhibition of inflammation induced by cytokines/inflamm. mediators

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12
Q

How does Aspirin work?

A

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

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13
Q

Important details about Salicylate absorption

A

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

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14
Q

Important details of Salicylate distribution

A

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

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15
Q

Salicylate half life

A

12 hours because its extensively conjugated

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16
Q

How do you increase excretion of Salicylates in urine?

A

Increase urinary pH

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17
Q

Ways that non-salicylates are metabolized

A

Oxidation
Demethylation
Conjugation

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18
Q

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

A

Children – Reye’s Syndrome (Liver failure, deepening coma, seizures, etc.)

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19
Q

Common name for Ibuprofen? Naproxen?

A

Ibuprofen – Advil

Naproxen – Aleve

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20
Q

Difference between Ibuprofen and Naproxen?

A

Half Lives
Ibuprofen – 2 hrs
Naproxen – 14 hours

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21
Q

Important acetic acid derivative pain meds (and basic information)

A

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

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22
Q

Risks of diclofenac/voltaren

A

Increased risk of peptic ulcer and renal dysfxn

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23
Q

Risks of long term indomethacin

A

Acute gouty arthritis
Ankylosing spondylitis
Pericarditis

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24
Q

Use of enolic acids?

A

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

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25
Q

Examples of enolic acids

A

Meloxicam (20 hrs)

Piroxicam (57 hrs)

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26
Q

Advantages of acetaminophen over other NSAIDs

A

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

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27
Q

Disadvantages of acetaminophen over other NSAIDs

A

Little clinically useful antiinflammatory activity

acute overdose may lead to fatal hepatic necrosis

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28
Q

Adverse effects of salicylate overdose

A

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

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29
Q

Tretment of salicylate poisoning

A

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

30
Q

Risks of non-salicylate NSAIDs

A

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

31
Q

Adverse effects of Acetaminophen overuse

A

Renal toxicity, Papillary necrosis

Dose Dependent Hepatic Necrosis (esp. w/ OH)

32
Q

Name a selective Cox2 inhibitor. Why use one?

A

Rofecoxib (Vioxx)

Reduce ulcers and GI Bleeds

33
Q

Why was Vioxx taken off the market?

A

High chance of blood clots, strokes, and MI

34
Q

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

A

Celebrex

35
Q

Who shouldn’t use NSAIDs

A

CKD, Peptic Ulcer Disease, GI bleeders

In high doses, inhibits bone healing

36
Q

What are DMARDs

A

Disease Modifying Anti-Rheumatic Drugs

37
Q

Three main classes of DMARDs

A

Antiproliferative agents
IL-1 Blockers
TNF-alpha blcokers

38
Q

Examples of anti-proliferative DMARDs

A

Methotrexate, Cyclophosphamide, Azathioprine

Leflunomide

39
Q

What are anti-proliferative DMARDs stopping from proliferating

A

B and T cell proliferation

40
Q

Name the IL-1 Blocking DMARD

A

Anakinra (kineret)

41
Q

Absolute contraindications for anakinra?

A

Pre-existing malignancy

Neutropenia

42
Q

Three main TNF-alpha blockers

A

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

43
Q

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

A

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

44
Q

Downside of using a TNF-alpha blcoker

A

Immunosuppressants – especially contra. for patients with previous TB

45
Q

Fatal toxicities associated with all DMARDs

A 
Hepatotoxicity
Hematotoxicitiy
Teratogenicity
Nephrotoxocity
CV tox
46
Q

Main drugs to give for acute gout

A

Colchicine + NSAIDs (indomethacin)

47
Q

How does Colchicine work?

A

Bind to tubulin, which interferes with mitotic spindle fxn

Depolymerized microtubules stop granulocyte migration, phagocytic activity, and inhibits lactate and cytokine release.

48
Q

Adverse effects of Colchicine

A

Toxic to rapidly proliferating intestinal epithelial cells

Nausea, vomiting, diarrhea, cramps

49
Q

Main drugs for chronic gout

A

Allopurinol
Febuxostat
Probenecid

50
Q

How does allopurinol work?

A

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

51
Q

How does febuxostat (Adenuric) work?

A

Its a new non-purine inhibitor of xanthine oxidase

More effective at lowering serum uric acid than tophus area than allopurinol.

52
Q

How does Probenecid work?

A

Competes for renal tubular anion transporter

Blocks the reabsorption of urate in prox. tubules

53
Q

What type of Gout should not be treated with probenecid

A

Overproducers

54
Q

What is psuedogout?

A

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

55
Q

Which ion channels are associated pain

A

TRP, Nav, Cav

56
Q

How does blocking sodium channels prevent pain

A

Prevents hypopolarization/depolarization

Blocks action potentials

57
Q

Mutations of Nav 1.7 cause what

A

Gain of fxn – Severe Pain

Loss of Fxn – diminished patients

58
Q

Topical anesthetics that influence the activity of sodium channels

A

Lidocaine
Benzocaine
Oxybuprocaine (in optho)

59
Q

Important details about Lidocaine

A 
Local analgesia (dentistry), itching, burning
15 minute local onset, lasts 30-120 minutes
60
Q

Important details for Bupivicaine

A

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

61
Q

Important details for Benzocaine

A

OTC, oral ulcers, ear pain

Lower allergy risk

62
Q

Name important Sodium channel blockers

A

Lamotrigine
Amitryptiline
Carbamezipine

63
Q

Important details for Lamotrigine

A

Off label use for peripheral neuropathy, migraine

Risk of developing Stevens Johnsons

64
Q

Important details for amitryptiline?

A

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

65
Q

Important details for carbamezipine

A

Used for trigeminal neuralgia, Bipolar, and Seizures

Can be Teratogenic

66
Q

Sodium channel blockers with SNRI’s Functionality

A

Duloxetine (Cymbalta)

Venlafaxine (Effexor)

67
Q

What do you use Duloxetine (Cymbalta) for?

A

Diabetic Pain, Fibromyalgia, Peripheral Neuropathy

68
Q

Details on Venlafaxine

A

Used off label for diabetic neuropathic pain

SNRI – anti-depresant/anxyiolytic

69
Q

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

A

Milnacipran (Fibromyalgia, SNRI)

Tapentadol (Diabetic Neuropathic Pain, NRI)

70
Q

SSRIs used for pain assocaited depression

A

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

Escitalopram, Citalopram

71
Q

Pharmacokinetics of TCA/SNRIs

A

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

72
Q

Calcium channel blockers that have an influence on pain

Diabetic Neuralgia, Fibromyalgia, Neuropathic Pain

A

Gabapentin (Neurontin)
Pregabalin (Lyrica)
Ziconotide
Levetiracetam

Pharmacology - Test #4 (9 decks)

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