Analgesic Drugs Flashcards
(140 cards)
1
Q
Acetaminophen chemical name
A
N-acetyl-para-aminophenol
2
Q
Acetaminophen INN
A
Paracetamol
3
Q
Paracetamol USAN
A
Acetaminophen
4
Q
Phenacetin can cause various toxic effects:
A
▪ Hemolytic anemia
▪ Cancer
▪ Kidney failure
▪ Methemoglobinemia
5
Q
One of the most common drugs that is involved in suicide attempts and accidental poisoning.
A
Acetaminophen
6
Q
Uses of acetaminophen
A
Analgesic & Antipyretic
7
Q
T/F: Acetaminophen is an NSAID
A
FALSE
8
Q
It is a weak COX-1 and COX-2 inhibitor
A
Acetaminophen
9
Q
Active toxic metabolite of acetaminophen
A
N-acetyl-p-benzoquinone imine (NAPQI) or NAPBQI
10
Q
Major metabolism pathway of acetaminophen
A
Glucuronidation
11
Q
Fatal dose of acetaminophen
A
15 g (30 tablets)
12
Q
Acetaminophen overdose during pregnancy has been associated with
A
fetal death and spontaneous abortion
13
Q
Acetaminophen acute ingestion of __________ in children is potentially hepatotoxic.
A
more than 140 mg/kg
14
Q
Acetaminophen acute ingestion of __________ in adults is potentially hepatotoxic.
A
6 g
15
Q
Children < 10-12 yrs. old are ______ susceptible due to smaller contribution of cytochromeP-450 to acetaminophen metabolism.
A
LESS
16
Q
Ingestion of 15 g of acetaminophen may be fatal, death being caused by
A
severe hepatotoxicity with centrilobular necrosis
17
Q
Ingestion of 15 g of acetaminophen may be fatal, death being caused by severe hepatotoxicity with centrilobular necrosis, sometimes associated with ____________________.
A
acute renal tubular necrosis
18
Q
Early after acute acetaminophen overdose
A
Anorexia, Nausea/Vomiting
19
Q
After 24-28 hours of acetaminophen overdose
A
• Prothrombin time and transaminase levels rise
• Hepatic necrosis is evident
20
Q
acute hepatic failure, encephalopathy, and death is collectively known as
A
Fulminant hepatic failure
21
Q
Falsely elevated acetaminophen levels may occur in the presence of _______________
A
high levels of salicylate
22
Q
Spontaneous vomiting due to acetaminophen overdose may delay the administration of antidote and charcoal and should be treated with ___________
A
Metoclopramide
23
Q
may be necessary for massive hepatic failure
A
Liver transplant
24
Q
Antidote for acetaminophen overdose
A
N-acetylcysteine, 140 mg/kg orally
25
Brand names of NAC available as IV
Acetadote
26
Brand names of NAC available as oral
Mucomyst
27
Acetaminophen will be metabolized by the enzyme CYP450, specifically ______
2E1
28
removes acetaminophen from blood effectively
Hemoperfusion
29
uses cartridge containing activated charcoal
Hemoperfusion
30
These are chemically diverse group of agents that share similar pharmacologic properties and are widely used for control of pain and inflammation.
NSAIDs
31
Overdose by most of the agents (NSAIDs) in this group usually produces only ________
mild gastrointestinal upset
32
Pepto-Bismol (bismuth subsalicylate) is used for
Ulcer
33
Before the introduction of child-resistant containers, _____________ was one of the leading causes of accidental death in children
salicylate overdose
34
Dose of aspirin used as analgesic and antipyretic
650 mg - 4 g
35
Dose of aspirin used as anti-inflammatory
4-8 g
36
Dose of aspirin used as antiplatelet
75-81 mg
37
________________ leading to respiratory alkalosis, metabolic acidosis contributing to dehydration
Hyperventilation
38
Characterized by low level of carbon dioxide in the blood. Happens only during hyperventilation
Respiratory alkalosis
39
Blood test that measures how long it takes for a person’s blood to clot.
Prothrombin time (PTT)
40
Average therapeutic single dose of aspirin
10 mg/kg
41
Usual daily therapeutic dose of aspirin
40-60 mg/kg/d
42
Aspirin acute ingestion of ________ will produce mild intoxication
150-200 mg/kg
43
Aspirin acute ingestion of ________ will produce severe intoxication
300-500 mg/kg
44
Chronic intoxication of aspirin may occur with ingestion of
more than 100 mg/kg/d for 2 or more days
45
Plasma concentration of aspirin that may cause tinnitus
50 mg/dL
46
Plasma concentration of aspirin that may cause anti-inflammatory uricosuric
20 mg/dL
47
Severe intoxication of salicylates causes
Coma, seizures, hypoglycemia, hyperthermia, and pulmonary edema
48
Salicylate overdose caused death by
CNS failure and cardiovascular collapse
49
Salicylism effects
vomiting, tinnitus, decreased hearing, and vertigo
50
more common with acute intoxication of salicylates
Cerebral and pulmonary edema
51
increases brain salicylate concentration and worsening toxicity
Systemic acidemia
52
Chronic therapeutic concentrations in arthritis patients range from
100 to 300 mg/L (10-30 mg/dL)
53
A level greater than 600 mg/L (60 mg/dL) accompanied by ________
acidosis and altered mental status
54
Treat metabolic acidosis with
intravenous sodium bicarbonate
55
Replace fluid and electrolyte deficits caused by vomiting and hyperventilation with
intravenous crystalloid solutions
56
Monitor asymptomatic patients for a minimum of ______
6 hours
57
frequently given both to prevent acidemia and to promote salicylate elimination by the kidneys
Sodium bicarbonate
58
Effective in enhancing urinary excretion of salicylate
Urinary alkalinization
59
Very effective in rapidly removing salicylate and correcting acid-base and fluid abnormalities.
Hemodialysis
60
With COX and LOX inhibitory effects
Indomethacin (Indocin) & Diclofenac (Voltaren, Cataflam)
61
described as a persistent opening between 2 major blood vessels leading to the heart
Patent ductus arteriosus
62
Maximum daily dose of indomethacin
200 mg/day
63
introduced in 1963, is an indole derivative
Indomethacin
64
Used for PDA
Indomethacin, Ibuprofen
65
Sulindac (Clinoril) adult dose
150-200 mg twice daily or 300-400 mg once daily
66
Maximum Daily Dose of Sulindac
400 mg
67
Should be administered with food or milk
Sulindac
68
Common adr of sulindac
● Stevens Johnson Syndrome
● Thrombocytopenia
● Agranulocytosis
● Nephrotic syndrome
69
Short half-life. Should be given frequently
Tolmetin (Tolectin)
70
ineffective in the treatment of gout
Tolmetin
71
Indole acetic acid
Indomethacin, Sulindac, Tolmetin
72
Pyrazoles
Phenylbutazone, Oxyphenbutazone
73
Salicylates
ASA, Difflunisal, Methylsalicylate
74
Propionic Acid
Ibuprofen, Naproxen, Ketoprofen
75
Fenamates
Mefenamic acid, Meclofenamic acid
76
Adr of tolmetin
Thrombocytopenic purpura
77
Rare blood disorder, characterized by clotting in small blood vessels of the body, which result in low platelet count.
Thrombocytopenic purpura
78
Maximum Daily Dose of Tolmetin
1800 mg/day
79
Originally made available for use in humans for the treatment of rheumatoid arthritis and gout in 1949.
Phenylbutazone (Butazolidine)
80
No longer approved, and therefore not marketed, for any human use in the US
Phenylbutazone (Butazolidine)
81
Phenylbutazone adr
Aplastic anemia & Agranulocytosis
82
Maximum Daily Dose of Phenylbutazone
800 mg/day
83
Salicylic acid derivative that has analgesic & anti-inflammatory activity
Diflunisal (Dolobid)
84
Used for cancer pain with bone metastases
Diflunisal
85
Can also be used as pain control for dental surgery
Diflunisal
86
Maximum Daily Dose of Diflunisal
1500 mg/day
87
maximum duration of treatment for Ketorolac (Toralol)
5 days
88
A heteroacyl acetic acid derivative with a very potent analgesic effect and moderate anti-inflammatory effect, given IV or IM for surgical procedures and post-surgical pain
Ketorolac
89
If used with Opioid, it may decrease the opioid treatment by 25-50%
Ketorolac
90
Successfully replaced morphine in mild to moderate post-surgical pain.
Ketorolac
91
Adr of Ketorolac after 5 days of use
Nephrotoxicity
92
Maximum daily dose of parenteral (IM, IV) Ketorolac
120 mg
93
Maximum daily dose of oral Ketorolac
40 mg
94
the only non-acid NSAID
Nabumetone (Relafen)
95
Given as ketone prodrug that resembles Naproxen in structure.
Nabumetone
96
Converted to active acetic acid derivative in the body
Nabumetone
97
Maximum Daily Dose of Nabumetone
2000 mg
98
Common adr of Nabumetone
Pseudoporphyria & Photosensitivity
99
phenyl propionic acid derivative
Ibuprofen (Motrin, Advil)
100
Caution: Px with liver impairment. This can cause liver damage.
Ibuprofen (Motrin, Advil)
101
known to cause less fluid retention
Ibuprofen (Motrin, Advil)
102
Common Hematologic effects of Ibuprofen
Agranulocytosis & Aplastic anemia
103
NSAIDs that can cause agranulocytosis & aplastic anemia
Phenylbutazone & Ibuprofen
104
Maximum Daily Dose of Ibuprofen
3200 mg/day
105
Dose of Ibuprofen for inflammatory disease
400-800 mg/dose 3-4 times/day
106
Dose of Ibuprofen for analgesic/pain/fever/dysmenorrhea
200-400 mg/dose every 4-6 hours
107
Maximum Daily Dose of Ibuprofen for analgesic/pain/fever/dysmenorrhea
1.2 g
108
propionic acid derivative
Flurbiprofen (Ansaid)
109
Its (S)(-) enantiomer inhibits COX nonselectively.
Flurbiprofen
110
Dose of Flurbiprofen for inflammatory disease
50-100 mg/dose 3-4 times/day
111
Maximum Daily Dose of Flurbiprofen
400 mg/day
112
Flurbiprofen is associated with (CATM)
● Cogwheel Rigidity
● Ataxia
● Tremor
● Myoclonus
113
napthylpropionic acid derivative
Naproxen (Naprosyn)
114
only NSAID presently marketed as single enantiomer
Naproxen
115
Dose of Naproxen intended for rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis:
250-500 mg orally twice daily
116
Naproxen dose may be increased to
1.5 g/d
117
Maximum Daily Dose of Naproxen
1375 mg/day
118
Intermediate risk caused by naproxen
Stomach ulcer
119
To reduce the stomach ulceration
Combine with PPI
120
Dosing adjustment is advised to px with hepatic impairment
Piroxicam (Feldene)
121
Increase incident of peptic ulcer and bleeding (doses >20mg/day)
Piroxicam
122
High risk of peptic ulcer (9.5x higher than other NSAIDs)
Piroxicam
123
Adult dose of Piroxicam
10-20 mg/day once daily
124
Maximum Daily Dose of Piroxicam
20 mg
125
It is not widely used in humans as it has a high rate (30-60%) rate of GI side effects.
Meclofenamate (Meclomen)
126
Before, it is used in joint, muscular pain, arthritis, and dysmenorrhea
Meclofenamate
127
Inhibits both COX & Phospholipase A2
Mefenamic acid (Ponstan)
128
Maximum daily dose of Mefenamic acid
4000 mg/day
129
Adr of Mefenamic acid
Diarrhea & Abdominal pain
130
At what dose does Diclofenac appear to impair renal blood flow and Glomerular Filtration rate?
250 mg/day
131
Maximum daily doses of Diclofenac
225 mg
XR: 200 mg
132
Diclofenac dose for RA
150-200 mg/day orally
133
Diclofenac dose for OA
100-150 mg/day orally
134
active metabolite of phenylbutazone
Oxyphenbutazone
135
Toxicity effects of NSAIDs may be attributed to
inhibition of cyclooxygenase
136
Acute or chronic intoxication of NSAIDs may affect gastric mucosa and renal blood flow due to a __________________
decrease in prostaglandins
137
T/F: NSAID intoxication occurs after ingestion of more than 5-10 times the usual therapeutic dose
TRUE
138
_____________ overdose produces same toxicity as with salicylate poisoning.
Diflunisal
139
solutions of sterile water with added electrolytes to approximate demineral content of human plasma
Intravenous crystalloid solutions
140
used for patients with prothrombin time (PT) delay caused by hypoprothrombinemia
Vitamin K (phytonadione)
