Test 1 Flashcards
1
Q
Drugs for mild pain
A
APAP, Aspirin, NSAIDs, Cox-2 inhibitors
2
Q
Drugs for moderate pain
A
NSAIDs, Opioid + APAP, Tramadol
3
Q
Drugs for severe pain
A
Opiods
4
Q
APAP MoA
A
- Inhibit the synthesis of prostaglandins in the CNS
- work peripherally to block pain impulse generation
5
Q
Dosing for APAP
A
325-650 mg q4h or 100 mg Q6h or
1000 mg Q6h
6
Q
Max dosing for liver patient on APAP
A
2 gram/day
7
Q
Max dosing for APAP
A
4 grams/day
8
Q
APAP routes
A
PO, PR. IV is very expensive
9
Q
APAP adverse effects
A
hepatotoxicity
10
Q
Function of cox-1
A
cytoprotective: protects GI, lungs, and kidneys; plays part in platelet aggregation and vasoconstriction
11
Q
Function of cox-2
A
Inflammatory: Inflammation, pain • Antiplatelet •Vasodilation
12
Q
Aspirin MoA
A
irreversibly binds to cox-1 and cox-2
13
Q
Aspirin properties
A
analgesia
anti-inflammatory
antipyretic
antiplatelet (irreversible)
14
Q
Aspirin antiplatelet MoA
A
prevents synthesis of thromboxane A (a vasoconstrictor and iducer of platelet aggregation)
15
Q
Aspirin onset
A
15-20 minutes
16
Q
Aspirin peak
A
1-3 hours
17
Q
Aspirin duration
A
3-6 hours
18
Q
Aspirin half-life
A
3 hours
19
Q
Aspirin elimination
A
urine and liver
20
Q
Aspirin adverse effects
A
GI bleeding, salycylism, reye’s syndrome, asthma patients: bronchospasm, uticaria, angiodema
21
Q
Salicylism
A
dizziness, deafness, tinnitus
22
Q
Important NSAIDs
A
Ibuprofen, Indomethacin, Ketoralac, Naproxen
23
Q
NSAIDs properties
A
analgesic, antinflammatory, antipyretic, antiplatelet (reversible)
24
Q
NSAID adverse effects
A
cardio: fluid retention, htn, edema GI: irritation, ulcers, bleeding, perforation Respiratory: bronchospasm Skin: rash Renal: insufficiency or liver failure
25
NSAID black box warning
serious CV event, GI bleed perforation
26
Which med is used for periop pain in CABG
NSAIDs
27
Ketorolac route
IV and IM
28
Ketorolac usage
short term mgmt of mod to sever pain (max 5 days)
29
Ketorolac adverse effects
severe post-op bleeding; renal failure
30
Advantages of cox-2 inhibitor
- decreased pain and inflammation with minimal GI side effects
- no effect on platelet aggregation/improved bleeding profile
31
Disadvantages of cox-2 inhibitor
- renal dysfunction
- avoid in pts who have sulfa allergy
- CV events (increased vasoconstriction)
32
Morphine routes
PO, PR, IV, IM, SubQ, epidural, intrathecal
33
Morphine doses*
PO: 15-30 q4h PRN
| IV_ 2-4 mg q4h PRN
34
Morphine elimination*
renally
35
Unique morphine properties
2 active metabolites; histamine release (hypotension and pruritis)
36
Hydromorphone trade name
dilaudid
37
Hydromorphone routes
PO, PR, IV, IM, SubQ, epidural
38
Hydromorphone dosing*
PO: 2-4 mg q4-6 h
IV: 0.2-1 mg q2-3h
39
Hydromorphone metabolism
half life: 2-3 hours
not renally cleared
no active metabolites
40
Methadone route
PO, IV, IM, SubQ
41
Methadone metabolism
- biphasic elimination: analgesic 1/2 life: 8-12 h; terminal 1/2 life: 24-36h
- renally cleared
42
Methadone adverse effects
QT prolongation*; serotenergic effects; lower seizure threshold
43
Meperidine route
PO, IV, IM, SubQ
44
Meperidine dosing
IV: 50-150 mg q4-6h
45
Meperedine metabolism (and active metabolite)
renally; normeperidine
46
Meperedine adverse effects
anxiety, tremors, serotolinergic effects
47
Drug used for post op shivering
Meperidine
48
Codeine dosing
15-60 mg q4h
49
Codeine usage
mild to moderate acute pain; antitussive
50
Codeine metabolism
major CYP 2D6 substrate--if pt lacks enzyme they won't experience benefits
51
Codeine route
PO only
52
Hydrocodone route
PO only
53
Hydrocodone dose
5-10 mg q4-6h
54
Hydrocodone usage
acute mod to severe pain in pts w/ limited opiod use
55
Hydrocodone combos (immediate release)
Vicodin (Hy+APAP)
| Vicoprofen (Hy+ibuprofen)
56
Hydrocodone combos (extended release)
Zohydro (ER 12hrs)
| Hysingla (ER 24 hrs)
57
Fentanyl routes
transdermal ,IV, lozenge, buccal, intranasal, sublingual, epidural
58
Fentanyl dose
IV: 25-50 mcg q2-3 h
59
Fentanyl metabolism
- metabolized by CYP3A4
- preferred agent in liver failure
- high potency and lipid solubility=rapid onset
60
Fentanyl adverse effects
bradycardia and chest wall rigidity
61
Partial agonist med
buprenorphine
62
Antagonist action
- Compete with endogenous and exogenous opiods at mu receptors
- prevent or reverse opioid-induced side effects
63
Naloxone usage
- to reverse toxic effects of agonists and agonist-antagonist
- may be used orally to prevent opioid-induced constipation
64
Naloxone disadvantages
- repeated dosing may be necessary based upon half-life of agonist
- Poor systemic bioavailability due to extensive first pass
65
Naltrexone route
IM depot and PO
66
Naltrexone usage
```
opioid dependence (if they slip up and take opioid it won't have intended effect)
NOT for acute reversal of toxic effects
```
67
Naltrexone adverse effects
Hepatotoxic
68
Methylnaltrexone route
SubQ only
69
Methylnaltrexone usage
to treat opioid induced constipation with chronic opioid use
| NOT for acute reversal of toxic effects
70
Methylnaltrexone metabolism
renally eliminated
| doesn't cross blood brain barrier (acts on peripheral mu receptors like GI tract)
71
Methylnaltrexone adverse effect
potential GI perforation
72
Morphine conversion
P 10: O 30
73
Hydromorphone conversion
P 1.5: O 7.5
74
Mepiridine conversion
P 100: O 300
75
Codeine conversion
P 100: O 200
76
Buprenorphine conversion
P 0.3: O 0.4 (sl)
77
Tramadol route
PO only
78
Tramadol MoA
- weak opiate mu receptor binding
| - inhibition of norepinephrine and serotonin reuptake
79
Tramadol dosing
25-100 mg q4-6h
80
Tramadol metabolism
- extensive CYP 2D6
| - renally and hepatically cleared
81
Tramadol adverse effects
- lower seizure threshold
- sedation
- less respiratory depression and GI motility; less euphoria
82
Class-wide opioid adverse effects
respiratory depression, sedation, constipation, fatigue, confusion, hallucinations/nightmares, GI, N/V, brady
83
Tolerance to resp depression
w/in 5-7 days
84
Tolerance to sedation
within days to weeks
85
Opioid effects that pt never gains tolerance to
miosis, constipation, seizures
86
High tolerance development to
```
Analgesia
Euphoria/dysphoria
Mental clouding
Sedation
Respiratory depression
Antidiuresis Nausea/vomiting
Cough suppression
```
87
Moderate tolerance development to
bradycardia
88
Meds to treat opioid addiction
methadone, buprenorphine, naloxone, naltrexone
89
Chronic pain regimen (opioid)
long acting with short acting for breakthrough pain
90
Calculation for breakthrough pain
10-15% of daily dose of reg sched opioid
91
Opiods with active metabolites
meperidine, morphine
92
Meds for neuropathic pain
SNRIs, TCA, Calcium channel a2-δ ligands; lidocaine patch (2nd line); opioids (3rd line)
93
SNRIs
duloxetine, venlafaxine
94
TCAs
nortirptyline, despiramine
95
First line meds for migraine
ASA, APAP, NSAIDs, triptans
96
APAP combos for migraine
Exedrin - w/ caffeine
Floricet - caffeine/butalbital
NSAIDs
97
Triptan MoA
Selective agonists of 5-HT1B and 5-HT1D receptors
• Normalizes dilated intracranial arteries through enhanced
vasoconstriction
• Peripheral neuronal inhibition
• Inhibition of transmission through second-order neurons of the trigeminocervical complex
98
Triptan effective up to ___ hours after onset
4
99
Triptan contraindications
• Heart disease
• Peripheral vascular disease • Cerebrovascular disease
-Severe hepatic impairment
• Uncontrolled hypertension
100
Triptan considerations
Use within 24 hours of ergotamine derivatives
Use within 2 weeks of therapy with monoamine
oxidase inhibitors (MAOI)
101
DMARD characteristics
Should initiate within first 3 months of symptom onset
Given to reduce mortality and prevent progression of RA
Onset: delayed weeks to months before benefit seen • No direct analgesic or anti-inflammatory effect
Narrow range of effectiveness
Unique adverse event profile: use often limited by
toxicities
Consists of nonbiologic and biologic agents
102
First line DMARD
Methotrexate
103
Methotrexate onset
2-3 weeks (max 4 -6)
104
Methotrexate route
oral or subq
105
Methotrexate MoA
• Folic acid antagonist, immunosuppressant
| Inhibits T-lymphocytes proliferation and cytokine production
106
Hydroxychloroquine route
PO only
107
Hydroxychloroquine adverse options
Relatively safe and well tolerated
• Lack myelosuppressive, renal, hepatic toxicities
• GI toxicity (nausea, vomiting, diarrhea); ocular toxicity (corneal deposits, irreversible retinopathy: baseline and q6 month eye exams)
• Rash, alopecia, skin pigmentation changes
108
Hydroxychloroquine route
PO only
109
Hydroxychloroquine MoA
Unknown but has some anti-inflammatory properties
| -Onset may be delayed up to 6 weeks
110
Adalimubab (Humira)
| dosage
subQ injections every other week
111
Adalimubab (Humira)
| metabolism
Onset: 1 – 4 weeks
| Half-life: about 10 – 20 days
112
Adalimubab (Humira) Role in therapy
monotherapy OR in combination with methotrexate
113
Adalimubab (Humira) adverse effects
local site injections
114
Tofacitinib (Xeljanz®) MoA
Janus Kinase (JAK) Inhibitor
Major 3A4 substrate
115
Tofacitinib (Xeljanz®) indications
* Moderate to severe RA
| * Adequate / Intolerant response to methotrexate
116
Tofacitinib (Xeljanz®) adverse effects
URIs, HA, diarrhea, increased LFTs, bone marrow suppression (lymphopenia, neutropenia, anemia), GI perforation, interstitial lung disease
117
TB Screening for Biologic Agents
Initially: TST (TB skin test) or IGRA (interferon-gamma- release assay)
• Negative: start biologic
• Positive: chest x-ray, sputum for AFB
Latent TB: treat at least one month then start biologic
Active TB: complete treatment for TB then start
biologic
If risk factors, screen annually
118
Goals for gylcemic control
* A1c < 6.5 – 7.0%
* Fasting glucose 80 – 130 mg/dL
* Peak postprandial glucose (1–2 hours after a meal) <180 mg/dL
119
Rapid acting insulin
```
Insulin lispro (Humalog)
Insulin aspart (NovoLog) Insulin glulisine (Aventis)
```
120
Rapid acting insulin onset
15-30 minutes
121
Short acting insulin
Regular Humulin R
122
Short acting insulin onset
30 minutes
123
Intermediate acting insulin
NPH Humulin N
| NPH Novolin N
124
Long acting insulin
```
Insulin glargine (Lantus) – 100 units/mL
Insulin glargine (Basaglar) – 100 units/mL
Insulin glargine (Toujeo) -- 300 units/mL
Insulin detemir (Levemir) Insulin degludec (Tresiba)
```
125
Glargine onset
4-5 hours
126
Glargine duration
22-24 hours
127
Detemir onset
2 hours
128
Detemir peak
3-9 hours
129
Detemir duration
14-24 hours
130
Initial type 2 insulin dosing
0.2 units/kg/day
131
1 unit of insulin will lower blood glucose by ____ mg/dL
50
132
Sulfonylureas MoA
increase secretion of insulin from beta cells, increase insulin sensitivity
133
Sulfonylureas metabolism
- hepatically metabolized
| - renal w/ glyburide
134
Sulfonylureas adverse effects
- hypoglycemia (most common)
- derm rash, sensitivities
- GI disturbances
- weight gain
135
Sulfonylureas
Glyburide, glipizide, glimepiride
136
Biguanides MoA
- lowers hepatic glucose output
| - increases peripheral glucose uptake and utilization
137
Biguanides contraindications
renal impairment def
possibly hepatic impairment and CHF
eGFR<30
138
When to hold biguanides for 48 hours?
eGFR 30-60 + contrast dye
139
When to re-evaluate biguanides dosing?
eGFR goes < 45
140
When to avoid starting biguanides?
eGFR 30-45
141
Incretins
GLP1 and DPP4 inhibitors
142
GLP1
glucagon like peptide
143
Biguanides adverse effects
N/V/D, metallic taste, rarely lactic acidosis
144
Biguanides advantages
- no hypoglycemia
- weight loss
- lowers triglycerides
145
GLP1 function
- stimulate insulin release
- delay gastric emptying
- suppress postprandial glucagon release
146
GLP-1 agonists
Exenatide
Liraglutide
Albiglutide
Dulaglutide
think glip tide
147
GLP-1 adverse effects
N/V - slow gastric emptying
HA
pacreatitis (rare)
148
GLP -1 administration
- pre-filled pens for subQ injections
| - admin once or twice daily to once weekly
149
DPP-4 inhibitors
gliptins
150
DPP-4 MoA
Inhibits DPP-4 enzyme that is responsible for the breakdown on incretin hormones GLP-1
151
DPP-4 advantages
demonstrates CV safety (but doesn't reduce risk)
152
SGLT inhibitors
glifozins
153
SGLT MoA
increase glucose in urine, and increase loss of glucose through the kidney (lowers blood sugar)/reduces reabsorption of glucose
154
SGLT advantages
weight loss
- low risk of hypoglycemia
- blood pressure lowering
- renal protection
- lowers CHF exacerbation
155
SGLT concerns
- limb amputation (rare)
- electrolyte distrubacnes
- UTI
- yeast infections
- malignancy
156
Thioureas
propylthiouracil
| methimazole
157
Thiourea MoA
shuts down production of thyroid hormones
158
Thioureas adverse effects
rash
fluid retention
leukopenia
159
Drug of choice for thyroid replacement
Levothyroxine
160
Levothyroxine MoA
produces physiologic levels of both T4 and T3
161
Levothyroxine onset
2-3 weeks
162
Levothyroxine adverse effects
heart failure
MI
Angina
Hyperthyroidism
163
Triptan names
Sumatriptan and Zolmitriptan
164
Hydromorphone trade name
Dilaudid
165
DM meds that can cause hypoglycemia
Insulin and sulfanylureas
166
Serotoninergic effects
Methadone
meperidine
tramadol
triptans
167
Cox-2 selective pros and cons
- increase CV events
| - decrease GI effects
168
Cox-1 selective pros and cons
- cardioprotective at low doses
| - increase risk for GI effects
