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

Non-Opiate Analgesics Flashcards

(72 cards)

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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
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

Pharmacology - Test #4 (9 decks)

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