Analgesic Drugs Flashcards

1
Q

Acetaminophen chemical name

A

N-acetyl-para-aminophenol

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2
Q

Acetaminophen INN

A

Paracetamol

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3
Q

Paracetamol USAN

A

Acetaminophen

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4
Q

Phenacetin can cause various toxic effects:

A

▪ Hemolytic anemia
▪ Cancer
▪ Kidney failure
▪ Methemoglobinemia

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5
Q

One of the most common drugs that is involved in suicide attempts and accidental poisoning.

A

Acetaminophen

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6
Q

Uses of acetaminophen

A

Analgesic & Antipyretic

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7
Q

T/F: Acetaminophen is an NSAID

A

FALSE

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8
Q

It is a weak COX-1 and COX-2 inhibitor

A

Acetaminophen

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9
Q

Active toxic metabolite of acetaminophen

A

N-acetyl-p-benzoquinone imine (NAPQI) or NAPBQI

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10
Q

Major metabolism pathway of acetaminophen

A

Glucuronidation

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11
Q

Fatal dose of acetaminophen

A

15 g (30 tablets)

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12
Q

Acetaminophen overdose during pregnancy has been associated with

A

fetal death and spontaneous abortion

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13
Q

Acetaminophen acute ingestion of __________ in children is potentially hepatotoxic.

A

more than 140 mg/kg

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14
Q

Acetaminophen acute ingestion of __________ in adults is potentially hepatotoxic.

A

6 g

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15
Q

Children < 10-12 yrs. old are ______ susceptible due to smaller contribution of cytochromeP-450 to acetaminophen metabolism.

A

LESS

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16
Q

Ingestion of 15 g of acetaminophen may be fatal, death being caused by

A

severe hepatotoxicity with centrilobular necrosis

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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

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18
Q

Early after acute acetaminophen overdose

A

Anorexia, Nausea/Vomiting

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19
Q

After 24-28 hours of acetaminophen overdose

A

• Prothrombin time and transaminase levels rise
• Hepatic necrosis is evident

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20
Q

acute hepatic failure, encephalopathy, and death is collectively known as

A

Fulminant hepatic failure

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21
Q

Falsely elevated acetaminophen levels may occur in the presence of _______________

A

high levels of salicylate

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22
Q

Spontaneous vomiting due to acetaminophen overdose may delay the administration of antidote and charcoal and should be treated with ___________

A

Metoclopramide

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23
Q

may be necessary for massive hepatic failure

A

Liver transplant

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24
Q

Antidote for acetaminophen overdose

A

N-acetylcysteine, 140 mg/kg orally

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25
Q

Brand names of NAC available as IV

A

Acetadote

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26
Q

Brand names of NAC available as oral

A

Mucomyst

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27
Q

Acetaminophen will be metabolized by the enzyme CYP450, specifically ______

A

2E1

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28
Q

removes acetaminophen from blood effectively

A

Hemoperfusion

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29
Q

uses cartridge containing activated charcoal

A

Hemoperfusion

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30
Q

These are chemically diverse group of agents that share similar pharmacologic properties and are widely used for control of pain and inflammation.

A

NSAIDs

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31
Q

Overdose by most of the agents (NSAIDs) in this group usually produces only ________

A

mild gastrointestinal upset

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32
Q

Pepto-Bismol (bismuth subsalicylate) is used for

A

Ulcer

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33
Q

Before the introduction of child-resistant containers, _____________ was one of the leading causes of accidental death in children

A

salicylate overdose

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34
Q

Dose of aspirin used as analgesic and antipyretic

A

650 mg - 4 g

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35
Q

Dose of aspirin used as anti-inflammatory

A

4-8 g

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36
Q

Dose of aspirin used as antiplatelet

A

75-81 mg

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37
Q

________________ leading to respiratory alkalosis, metabolic acidosis contributing to dehydration

A

Hyperventilation

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38
Q

Characterized by low level of carbon dioxide in the blood. Happens only during hyperventilation

A

Respiratory alkalosis

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39
Q

Blood test that measures how long it takes for a person’s blood to clot.

A

Prothrombin time (PTT)

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40
Q

Average therapeutic single dose of aspirin

A

10 mg/kg

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41
Q

Usual daily therapeutic dose of aspirin

A

40-60 mg/kg/d

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42
Q

Aspirin acute ingestion of ________ will produce mild intoxication

A

150-200 mg/kg

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43
Q

Aspirin acute ingestion of ________ will produce severe intoxication

A

300-500 mg/kg

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44
Q

Chronic intoxication of aspirin may occur with ingestion of

A

more than 100 mg/kg/d for 2 or more days

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45
Q

Plasma concentration of aspirin that may cause tinnitus

A

50 mg/dL

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46
Q

Plasma concentration of aspirin that may cause anti-inflammatory uricosuric

A

20 mg/dL

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47
Q

Severe intoxication of salicylates causes

A

Coma, seizures, hypoglycemia, hyperthermia, and pulmonary edema

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48
Q

Salicylate overdose caused death by

A

CNS failure and cardiovascular collapse

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49
Q

Salicylism effects

A

vomiting, tinnitus, decreased hearing, and vertigo

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50
Q

more common with acute intoxication of salicylates

A

Cerebral and pulmonary edema

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51
Q

increases brain salicylate concentration and worsening toxicity

A

Systemic acidemia

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52
Q

Chronic therapeutic concentrations in arthritis patients range from

A

100 to 300 mg/L (10-30 mg/dL)

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53
Q

A level greater than 600 mg/L (60 mg/dL) accompanied by ________

A

acidosis and altered mental status

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54
Q

Treat metabolic acidosis with

A

intravenous sodium bicarbonate

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55
Q

Replace fluid and electrolyte deficits caused by vomiting and hyperventilation with

A

intravenous crystalloid solutions

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56
Q

Monitor asymptomatic patients for a minimum of ______

A

6 hours

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57
Q

frequently given both to prevent acidemia and to promote salicylate elimination by the kidneys

A

Sodium bicarbonate

58
Q

Effective in enhancing urinary excretion of salicylate

A

Urinary alkalinization

59
Q

Very effective in rapidly removing salicylate and correcting acid-base and fluid abnormalities.

A

Hemodialysis

60
Q

With COX and LOX inhibitory effects

A

Indomethacin (Indocin) & Diclofenac (Voltaren, Cataflam)

61
Q

described as a persistent opening between 2 major blood vessels leading to the heart

A

Patent ductus arteriosus

62
Q

Maximum daily dose of indomethacin

A

200 mg/day

63
Q

introduced in 1963, is an indole derivative

A

Indomethacin

64
Q

Used for PDA

A

Indomethacin, Ibuprofen

65
Q

Sulindac (Clinoril) adult dose

A

150-200 mg twice daily or 300-400 mg once daily

66
Q

Maximum Daily Dose of Sulindac

A

400 mg

67
Q

Should be administered with food or milk

A

Sulindac

68
Q

Common adr of sulindac

A

● Stevens Johnson Syndrome
● Thrombocytopenia
● Agranulocytosis
● Nephrotic syndrome

69
Q

Short half-life. Should be given frequently

A

Tolmetin (Tolectin)

70
Q

ineffective in the treatment of gout

A

Tolmetin

71
Q

Indole acetic acid

A

Indomethacin, Sulindac, Tolmetin

72
Q

Pyrazoles

A

Phenylbutazone, Oxyphenbutazone

73
Q

Salicylates

A

ASA, Difflunisal, Methylsalicylate

74
Q

Propionic Acid

A

Ibuprofen, Naproxen, Ketoprofen

75
Q

Fenamates

A

Mefenamic acid, Meclofenamic acid

76
Q

Adr of tolmetin

A

Thrombocytopenic purpura

77
Q

Rare blood disorder, characterized by clotting in small blood vessels of the body, which result in low platelet count.

A

Thrombocytopenic purpura

78
Q

Maximum Daily Dose of Tolmetin

A

1800 mg/day

79
Q

Originally made available for use in humans for the treatment of rheumatoid arthritis and gout in 1949.

A

Phenylbutazone (Butazolidine)

80
Q

No longer approved, and therefore not marketed, for any human use in the US

A

Phenylbutazone (Butazolidine)

81
Q

Phenylbutazone adr

A

Aplastic anemia & Agranulocytosis

82
Q

Maximum Daily Dose of Phenylbutazone

A

800 mg/day

83
Q

Salicylic acid derivative that has analgesic & anti-inflammatory activity

A

Diflunisal (Dolobid)

84
Q

Used for cancer pain with bone metastases

A

Diflunisal

85
Q

Can also be used as pain control for dental surgery

A

Diflunisal

86
Q

Maximum Daily Dose of Diflunisal

A

1500 mg/day

87
Q

maximum duration of treatment for Ketorolac (Toralol)

A

5 days

88
Q

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

A

Ketorolac

89
Q

If used with Opioid, it may decrease the opioid treatment by 25-50%

A

Ketorolac

90
Q

Successfully replaced morphine in mild to moderate post-surgical pain.

A

Ketorolac

91
Q

Adr of Ketorolac after 5 days of use

A

Nephrotoxicity

92
Q

Maximum daily dose of parenteral (IM, IV) Ketorolac

A

120 mg

93
Q

Maximum daily dose of oral Ketorolac

A

40 mg

94
Q

the only non-acid NSAID

A

Nabumetone (Relafen)

95
Q

Given as ketone prodrug that resembles Naproxen in structure.

A

Nabumetone

96
Q

Converted to active acetic acid derivative in the body

A

Nabumetone

97
Q

Maximum Daily Dose of Nabumetone

A

2000 mg

98
Q

Common adr of Nabumetone

A

Pseudoporphyria & Photosensitivity

99
Q

phenyl propionic acid derivative

A

Ibuprofen (Motrin, Advil)

100
Q

Caution: Px with liver impairment. This can cause liver damage.

A

Ibuprofen (Motrin, Advil)

101
Q

known to cause less fluid retention

A

Ibuprofen (Motrin, Advil)

102
Q

Common Hematologic effects of Ibuprofen

A

Agranulocytosis & Aplastic anemia

103
Q

NSAIDs that can cause agranulocytosis & aplastic anemia

A

Phenylbutazone & Ibuprofen

104
Q

Maximum Daily Dose of Ibuprofen

A

3200 mg/day

105
Q

Dose of Ibuprofen for inflammatory disease

A

400-800 mg/dose 3-4 times/day

106
Q

Dose of Ibuprofen for analgesic/pain/fever/dysmenorrhea

A

200-400 mg/dose every 4-6 hours

107
Q

Maximum Daily Dose of Ibuprofen for analgesic/pain/fever/dysmenorrhea

A

1.2 g

108
Q

propionic acid derivative

A

Flurbiprofen (Ansaid)

109
Q

Its (S)(-) enantiomer inhibits COX nonselectively.

A

Flurbiprofen

110
Q

Dose of Flurbiprofen for inflammatory disease

A

50-100 mg/dose 3-4 times/day

111
Q

Maximum Daily Dose of Flurbiprofen

A

400 mg/day

112
Q

Flurbiprofen is associated with (CATM)

A

● Cogwheel Rigidity
● Ataxia
● Tremor
● Myoclonus

113
Q

napthylpropionic acid derivative

A

Naproxen (Naprosyn)

114
Q

only NSAID presently marketed as single enantiomer

A

Naproxen

115
Q

Dose of Naproxen intended for rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis:

A

250-500 mg orally twice daily

116
Q

Naproxen dose may be increased to

A

1.5 g/d

117
Q

Maximum Daily Dose of Naproxen

A

1375 mg/day

118
Q

Intermediate risk caused by naproxen

A

Stomach ulcer

119
Q

To reduce the stomach ulceration

A

Combine with PPI

120
Q

Dosing adjustment is advised to px with hepatic impairment

A

Piroxicam (Feldene)

121
Q

Increase incident of peptic ulcer and bleeding (doses >20mg/day)

A

Piroxicam

122
Q

High risk of peptic ulcer (9.5x higher than other NSAIDs)

A

Piroxicam

123
Q

Adult dose of Piroxicam

A

10-20 mg/day once daily

124
Q

Maximum Daily Dose of Piroxicam

A

20 mg

125
Q

It is not widely used in humans as it has a high rate (30-60%) rate of GI side effects.

A

Meclofenamate (Meclomen)

126
Q

Before, it is used in joint, muscular pain, arthritis, and dysmenorrhea

A

Meclofenamate

127
Q

Inhibits both COX & Phospholipase A2

A

Mefenamic acid (Ponstan)

128
Q

Maximum daily dose of Mefenamic acid

A

4000 mg/day

129
Q

Adr of Mefenamic acid

A

Diarrhea & Abdominal pain

130
Q

At what dose does Diclofenac appear to impair renal blood flow and Glomerular Filtration rate?

A

250 mg/day

131
Q

Maximum daily doses of Diclofenac

A

225 mg
XR: 200 mg

132
Q

Diclofenac dose for RA

A

150-200 mg/day orally

133
Q

Diclofenac dose for OA

A

100-150 mg/day orally

134
Q

active metabolite of phenylbutazone

A

Oxyphenbutazone

135
Q

Toxicity effects of NSAIDs may be attributed to

A

inhibition of cyclooxygenase

136
Q

Acute or chronic intoxication of NSAIDs may affect gastric mucosa and renal blood flow due to a __________________

A

decrease in prostaglandins

137
Q

T/F: NSAID intoxication occurs after ingestion of more than 5-10 times the usual therapeutic dose

A

TRUE

138
Q

_____________ overdose produces same toxicity as with salicylate poisoning.

A

Diflunisal

139
Q

solutions of sterile water with added electrolytes to approximate demineral content of human plasma

A

Intravenous crystalloid solutions

140
Q

used for patients with prothrombin time (PT) delay caused by hypoprothrombinemia

A

Vitamin K (phytonadione)