Analgesics Flashcards
(103 cards)
1
Q
Prostaglandins mediate what?
A
Local inflammatory mediators
2
Q
PGE2 sensitizes what?
A
Nerve endings to the action of bradykinin, histamine, and other chemical mediators
3
Q
All NSIDs act how?
A
By inhibiting the synthesis of prostaglandins
4
Q
What are the two conventional NSAIDs?
A
Acetylsalicylic Acid
Celecoxib
5
Q
What is the “other” NSAID?
A
Acetaminophen
6
Q
What is the life cycle of platelets?
A
7-10 days
7
Q
Why is it best to discontinue NSAIDs for 2 weeks before surgery?
A
NSAIDs kill off platelets, so you need to allow them to regenerate before surgery
8
Q
What dose of ASA is needed for analgesia?
A
160-325mg
9
Q
What dose of ASA is needed for anti-pyretic?
A
160-325mg
10
Q
What dose of ASA is needed for anti-inflammatory?
A
325-650mg
11
Q
What dosing of ASA will kill platelets?
A
80-160mg
12
Q
How/why does ASA kill platelets?
A
Causes irreversible inhibition of COX-1(TXA2) for the life of the platelets
13
Q
What two benefits does Acetaminophen have over ASA?
A
No GI effects
Safe in pregnancy
14
Q
What two disadvantages does Acetaminophen have compared to ASA?
A
No inflammatory control
No platelet inhibition (may not be an advantage…)
15
Q
What is the MOA of Aspirin?
A
Irreversibly, non-selectively inhibits COX, reducing PG and TXA2 synthesis
16
Q
What are the two common adverse effects of Aspirin?
A
Bleeding time doubles
Headache
17
Q
What is the one hypersensitivity reaction to Aspirin?
A
Angioedema
18
Q
What conditions cause Reye’s Syndrome?
A
A child with a fever from an active viral infection taking Aspirin
19
Q
What three things occur in Reye’s Syndrome?
A
GI disturbances
Liver Degeneration
Encephalopathy
20
Q
What is the rate of mortality in Reye’s Syndrome?
A
35%
21
Q
Reye’s Syndrome can occur in kids up to about what age?
A
15
22
Q
Aspirin reacts with what three groups of drugs?
A
- Ophthalmic/oral NSAIDS and Omega-3s
- Aectaminophen and Cyclosporine
- Steroids
23
Q
What is the result of an Aspirin and NSAID/Omega-3 interaction?
A
Hemorrhage risk - additive
24
Q
What is the result of an Aspirin and Acetaminophen/cyclosporine interaction?
A
Nephrotoxicity - additive
25
What is the result of an Aspirin and Steroid interaction?
GI toxicity - additive
26
What are the 5 contraindications associated with Aspirin?
1. Hemorrhagic disorders
2. Pregnancy, esp. 3rd trimester
3. Corneal denervation/dry eye
4. NSAID/ASA induced asthma
5. Chronic GIT inflammation/active peptic ulcer
27
What are the two indications for Acetaminophen?
Mild pain
| Fever
28
What is the MOA of Acetaminophen for the analgesic effect?
Inhibits COX and enhances 5-HT release
29
What is the MOA of Acetaminophen for the antipyretic effect?
Acts centrally at the hypothalamus by inhibiting PG synthetase
30
Acetaminophen only inhibits inflammation where?
Centrally - not peripherally
31
What are the 3 common side effects of Acetaminophen?
Nausea
Rash
Headache
32
What are the 3 serious adverse effects of Acetaminophen?
Acute hepatotoxicity
Acute renal tubular necrosis
Chronic analgesic nephropathy
33
What are the three categories of drugs that interact with Acetaminophen?
Acetaminophen/antihitstaminic combos
ASA
Lidocaine Topical
34
What is the effect of the interaction of Acetaminophen with acetaminophen/antihistaminic combos?
Hepatotoxicity - additive
35
What is the effect of the interaction of Acetaminophen with ASA?
Nephropathy - additive
36
What is the effect of the interaction of acetaminophen with topical lidocaine?
Methemoglobinemia - additive
37
What are the 4 indications for Celecoxib?
Arthritis
Ankylosing Spondylitis
Dysmenorrhea
Acute pain
38
What is the MOA of Celecoxib?
Selectively inhibits COX-2 and reduces PG synthesis
39
What is the common adverse effect of Celecoxib?
Headache
40
What are the 3 cardiovascular black box warnings of Celecoxib?
Stroke
Myocardial infarction
Congestive heart failure
41
What are the 2 GI black box warnings for Celecoxib?
Bleed
| Ulceration/perforation
42
Celecoxib contains what moiety?
Sulfonamide
43
What are the two drug categories that interact with Celecoxib?
NSAIDS (esp Ketorolac)/Corticosteroids
| Azoles
44
What is the effect of the interaction of NSAIDs/Corticosteroids with Celecoxib?
Hemorrhage
45
What is the effect of the interaction of Celecoxib with Azoles?
Impaired metabolism (buildup of celecoxib)
46
What is the contraindication to Celecoxib?
Sulfonamide allergy
47
What does neurogenic pain respond best to?
Anticonvulsants or antidepressants
48
What type of drug is the drug of choice for severe chronic malignant/nonmalignant pain?
Opioids
49
What FDA class do narcotics belong to?
II
50
What is the MOA of Hydrocodone?
Inhibit adenylyl cyclase activity
Enhance K+ outflow to hyperpolarize nerves affecting neuronal excitability and muscle tone
Stimulates prolactin and growth hormone release
51
What receptors does Hydrocodone act through?
G-protein-coupled Mu, Kappa and delta "opioid" receptors
52
Where does hydrocodone act, centrally or peripherally?
Centrally
53
What are the 6 common adverse effects of Hydrocodone?
```
Lightheadedness
Dizziness
Sedation
Miosis
Puritis
Flushing
```
54
Why might Hydrocodone cause flushing?
Histamine release
55
What are the 3 cardiovascular adverse effects of Hydrocodone?
Bradycardia
Tachycardia
Orthostatic hypotension
56
What are the 3 CNS adverse effects of Hydrocodone?
Drowsiness
Mood changes
Elevated intracranial pressure
57
How long does it take for drowsiness to kick in with hydrocodone use?
About 1 week
58
With Hydrocodone use, are mood changes quick to occur, or slow to occur?
Quick tolerance
59
With Hydrocodone use, what causes pupillary miosis?
Excitatory action on the parasympathetic nerve to the iris sphincter
60
What are the 3 drugs that interact with Hydrocodone?
Anticholinergics
Classic Antihistamines
Carbonic Anhydrase Inhibitors
61
What occurs in the interaction of Hydrocodone and Anticholinergics?
Constipation/paralytic ileus - additive
62
What occurs in the interaction of Hydrocodone and Classic Antihistamines?
CNS depression - additive
63
What occurs in the interaction of Hydrocodone and CAIs?
CNS toxicity - additive
64
What is the contraindication for Hydrocodone?
Mydriatic procedures - antagonizes
65
What is the Non-Conventional opioid?
Tramadol
66
What is the indication for tramadol?
Moderate/severe pain
67
What is the MOA of Tramadol?
Mu receptor agonist - effect is greater with active metabolite
Weak inhibitor of Ne/5-HT reuptake
68
What does NE stand for?
Norepinephrine
69
What is 5-HT?
Serotonin
70
What are the 3 common adverse effects of Tramadol?
Headache
Puritis
Flushing
71
What is the CNS adverse effect of Tramadol?
Serotonin syndrome
72
What is the cardiovascular adverse effect of Tramadol?
Orthostatic hypotension
73
What are the 3 classes of drugs that interact with Tramadol?
Anticholinergics
Classic antihistaminics
Azoles
74
Tramadol antagonizes which ACh receptors?
Both muscarinic and nicotinic
75
Migraines are what kind of disorder?
Neurovascular
76
Up to 1/3 of patients with migraine experience what?
Visual aura
77
High levels of what are associated with migraines?
Serotonin
78
What signs are associated with the prodromal phase of a migraine?
Arterial vasoconstriction
| Release of serotonin
79
What signs are associated with the headache phase of migraines?
Cerebral vasodilation
| Lower than normal levels of serotonin
80
What is the top prophylactic migrane drug class?
Topiramate
81
What are the two classes of abortive drugs for migraines?
Triptans
| Ergotamines
82
What are the 2 indications for Sumatriptan?
Acute migraines
| Cluster headaches
83
What is the MOA of Sumatriptan?
Selectively activates vascular serotonin 5HT-1 receptors, causing intracranial vasoconstriction
Stimulates neuronal serotonin receptors, decreasing the release of peptides including Substance P and CGRP
84
What is the common adverse effect of Sumatriptan?
Dizziness
85
What is the 1 hypersensitivity to Sumatriptan?
Angioedema
86
What are the 2 ocular adverse effects of Sumatriptan?
Partial vision loss
| Transient/permanent blindness
87
What is the 1 caution for Sumatriptan?
Hypertension (it causes vasoconstriction)
88
What are the 2 indications for Ergotamine?
Migraine
| Cluster headache
89
Ergotamine is structurally similar to what?
Biogenic Amines
90
What is the MOA of Ergotamine?
Stimulates serotonin receptors producing intracranial vasoconstriction, and inhibition of CN-V pain transmission
91
What is the 1 adverse effect of Ergotamine?
Photosensitivity
92
What are the 4 drug types that inhibit ergotamine metabolism?
Macrolides
Azoles
Fluoroquinolones
Cyclosporine
93
What happens when tetracyclines interact with Ergotamine?
May increase risk of Ergot toxicity
94
What happens with Ergotamine interacts with Timolol?
Peripheral vasoconstriction is enhanced
95
What are the 2 indications for Topiramate?
Migraine prophylaxis
| Seizures
96
What requires a higher dose of Topiramate, migrain prophylaxis, or seizures?
Seizures
97
What is the MOA of Topiramate?
Blocks voltage-gated Na channels
Augments GABA activity
Antagonizes glutamate receptors
Inhibits CAI
98
What are the 5 common adverse effects of Topiramate?
Bleeding
Nystagmus
Diplopia
Visual disturbance
99
What are the 5 serious adverse effects of Topiramate?
```
Angle closure glaucoma
Myopia
Maculopathy
Hemorrhage
Anemia
```
100
What may occur when Topiramate interacts with CAIs or Steroids?
Hypokalemia - additive
101
What may occur when Topiramate interacts with Gluoroquinolones?
QT prolongation
102
What may occur when Topiramate interacts with Opioids or classic Antihistamines?
Increased risk of CNS depression
103
What is the 1 caution for Topiramate?
Hemorrhage
