Unit 2-ANS, Anticoagulants, Hemoglobin, Antimalarials, Histamine Flashcards

1
Q

Common side effects of cholinomimetics

A

SLUDGE:

  • Salivation
  • Lacrimation
  • Urination
  • Diaphoresis
  • GI Upset (diarrhea)
  • Emesis (vomiting)
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2
Q

Bethanecol

Drug Class

A

Direct acting carbamic acid ester

(cholinomimetic)

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3
Q

Bethanecol

Mechanism

A

Direct-acting muscarinic cholinomimetic

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4
Q

Bethanecol

Uses

A
  • Post-operative and neurogenic ileus;
  • urinary retention (bowel and bladder smooth muscle ACh-innervated)
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5
Q

Bethanecol

Side effects

A

SLUDGE

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6
Q

Muscarine

Drug Class

A

Direct acting non-ester alkaloid

(cholinomimetic)

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7
Q

Muscarine

Mechanism

A

Direct-acting muscarinic cholinomimetic

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8
Q

Muscarine

Side Effects

A

SLUDGE

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9
Q

Pilocarpine

Drug Class

A

Direct acting non-ester alkaloid

(cholinomimetic)

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10
Q

Pilocarpine

Mechanism

A

Direct-acting muscarinic cholinomimetic

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11
Q

Pilocarpine

Uses

A

Glaucoma (ACh activates sphincter and ciliary muscles of eye)

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12
Q

Pilocarpine

Side effects

A

SLUDGE

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13
Q

Cevimeline

Drug Class

A

Direct acting non-ester alkaloid

(cholinomimetic)

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14
Q

Cevimeline

Mechanism

A

Direct-acting muscarinic cholinomimetic

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15
Q

Cevimeline

Uses

A

Dry mouth (in, e.g., Sjogren’s, post-radiation therapy; via increased salivation)

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16
Q

Cevimeline

Side effects

A

SLUDGE

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17
Q

Nicotine

Drug class

A

Direct acting non-ester alkaloid

(cholinomimetic)

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18
Q

Nicotine

Mechanism

A

Direct-acting nicotinic cholinomimetic

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19
Q

Nicotine

Uses

A

Smoking cessation (reduces cravings)

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20
Q

Neostigmine

Drug class

A

Indirect acting carbamate

(cholinomimetic)

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21
Q

Neostigmine

Mechanism

A

AChE inhibitor (short acting)

Lasts 0.5-2 hours

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22
Q

Neostigmine

Uses

A
  • Post-operative and neurogenic ileus;
  • urinary retention;
  • myasthenia gravis;
  • reversal of neuromuscular blockade
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23
Q

Neostigmine

Side effects

A
  • SLUDGE + general increase in cholinergic neurotransmission;
  • paralysis
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24
Q

Physostigmine

Drug class

A

Indirect acting carbamate

(cholinomimetic)

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25
Q

Physostigmine

Mechanism

A

AChE inhibitor (short acting)

Lasts 0.5-2 hours

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26
Q

Physostigmine

Uses

A

Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)

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27
Q

Physostigmine

Side effects

A

SLUDGE + general increase in cholinergic neurotransmission; paralysis

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28
Q

Donepezil

Drug Class

A

Indirect acting non-ester

(cholinomimetic)

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29
Q

Donepezil

Mechanism

A

AChE inhibitor

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30
Q

Donepezil

Uses

A

Alzheimer’s (amplifies endogenous ACh in brain)

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31
Q

Donepezil

Side effects

A

SLUDGE + general increase in cholinergic neurotransmission; paralysis

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32
Q

Edrophonium

Drug class

A

Indirect acting non-ester

(cholinomimetic)

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33
Q

Edrophonium

Mechanism

A

AChE inhibitor (v. short acting)

Lasts 5-15 minutes

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34
Q

Edrophonium

Uses

A
  • Myasthenia gravis (differentiating deficiency versus ACh crisis);
  • ileus
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35
Q

Edrophonium

Side effects

A

SLUDGE + general increase in cholinergic neurotransmission; paralysis

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36
Q

Ectothiophate

Drug Class

A

Indirect acting organophosphate

(cholinomimetic)

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37
Q

Ectothiophate

Mechanism

A

AChE inhibitor (long acting)

Lasts >100 hours

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38
Q

Ectothiophate

Uses

A

Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)

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39
Q

Ectothiophate

Side effects

A

SLUDGE + general increase in cholinergic neurotransmission; paralysis

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40
Q

Pralidoxime

Drug class

A

Strong nucleophile

(cholinomimetic)

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41
Q

Pralidoxime

Mechanism

A

Regenerates phosphorylated AChE

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42
Q

Pralidoxime

Uses

A

Poisoning by nerve gas, insecticide

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43
Q

Sarin

Drug class

A

Very potent indirect acting organophosphate

(cholinomimetic)

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44
Q

Sarin

Mechanism

A

AChE inhibitor

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45
Q

Sarin

Uses

A

Volatile nerve gas

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46
Q

Sarin

Side effects

A
  • SLUDGE + general increase in cholinergic neurotransmission; paralysis
  • Death
  • Treat with pralidoxime and atropine before aging
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47
Q

Parathion

Drug class

A

Very potent indirect acting organophosphate

(cholinomimetic)

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48
Q

Parathion

Mechanism

A

AChE inhibitor

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49
Q

Parathion

Uses

A

Insecticide

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50
Q

Parathion

Side effects

A
  • SLUDGE + general increase in cholinergic neurotransmission; paralysis
  • Death
  • Treat with pralidoxime and atropine before aging
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51
Q

Atropine

Drug Class

A

Tertiary amine antimuscarinic

(Cholinergic Receptor-Inhibitors)

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52
Q

Atropine

Mechanism

A

Blocks muscarinic receptors

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53
Q

Atropine

Uses

A

Mydriasis; cycloplegia

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54
Q

Atropine

Side effects

A

General block of muscarinic functions

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55
Q

Scopalamine

Drug class

A

Tertiary amine antimuscarinic

(Cholinergic Receptor-Inhibitors)

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56
Q

Scopalamine

Mechanism

A

Blocks muscarinic receptors

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57
Q

Scopalamine

Uses

A

Prevent or reduce motion sickness

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58
Q

Scopalamine

Side effects

A

General block of muscarinic functions

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59
Q

Dicyclomine

Drug class

A

Tertiary amine antimuscarinic

(Cholinergic Receptor-Inhibitors)

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60
Q

Dicyclomine

Mechanism

A

Blocks muscarinic receptors

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61
Q

Dicyclomine

Uses

A

Reduce transient hypermotility

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62
Q

Dicyclomine

Side effects

A

General block of muscarinic functions

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63
Q

Tropicamide

Drug class

A

Tertiary amine antimuscarinic

(Cholinergic Receptor-Inhibitors)

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64
Q

Tropicamide

Uses

A

Mydriasis; cycloplegia

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65
Q

Tropicamide

Side effects

A

General block of muscarinic functions

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66
Q

Tropicamide

Mechanism

A

Blocks muscarinic receptors

Very rapidly metabolized

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67
Q

Tolterodine

Drug class

A

Tertiary amine antimuscarinic

(Cholinergic Receptor-Inhibitors)

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68
Q

Tolterodine

Mechanism

A

Blocks muscarinic receptors

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69
Q

Tolterodine

Uses

A

Treat transient cystitis; postoperative bladder spasms; incontinence

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70
Q

Tolterodine

Side effects

A

General block of muscarinic functions

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71
Q

Benztropine

Drug Class

A

Tertiary amine antimuscarinic

(Cholinergic Receptor-Inhibitors)

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72
Q

Benztropine

Mechanism

A

Blocks muscarinic receptors

*crosses BBB*

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73
Q

Benztropine

Uses

A

Treat manifestations of Parkinson’s disease

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74
Q

Benztropine

Side effects

A

General block of muscarinic functions

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75
Q

Glycopyrrolate

Drug class

A

Quaternary amine antimuscarinic

(Cholinergic Receptor-Inhibitors)

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76
Q

Glycopyrrolate

Mechanism

A

Blocks muscarinic receptors

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77
Q

Glycopyrrolate

Uses

A

Reduce transient hypermotility

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78
Q

Glycopyrrolate

Side effects

A

General block of muscarinic functions

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79
Q

Tertiary vs Quaternary amine antimuscarinics

A

Tertiary: uncharged, crosses BBB

Quaternary: +charged; does not cross BBB

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80
Q

Ipatroprium

Drug class

A

Quarternary amine antimuscarinic

(Cholinergic Receptor-Inhibitors)

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81
Q

Ipatroprium

Mechanism

A

Blocks muscarinic receptors

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82
Q

Ipatroprium

Uses

A

Bronchodilation in asthma or COPD

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83
Q

Ipatroprium

Side effects

A

General block of muscarinic functions

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84
Q

Tiotroprium

Drug class

A

Quarternary amine antimuscarinic

(Cholinergic Receptor-Inhibitors)

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85
Q

Tiotroprium

Mechanism

A

Blocks muscarinic receptors

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86
Q

Tiotroprium

Uses

A

Bronchodilation in asthma or COPD

(Longer acting than ipratropium)

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87
Q

Tiotroprium

Side effects

A

General block of muscarinic functions

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88
Q

Hexamethonium

Drug Class

A

Ganglionic blocker

(Cholinergic Receptor-Inhibitors)

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89
Q

Hexamethonium

Mechanism

A

Blocks ganglionic (Nn) receptor and sympathetic tone

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90
Q

Hexamethonium

Uses

A

Hypertensive crisis; “Bloodless” field surgery

(rarely used now)

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91
Q

Mecamylamine

Drug Class

A

Ganglionic blocker

(Cholinergic Receptor-Inhibitors)

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92
Q

Mecamylamine

Mechanism

A

Blocks ganglionic (Nn) receptor and sympathetic tone

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93
Q

Mecamylamine

Uses

A

Hypertensive crisis; “Bloodless” field surgery

(rarely used now)

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94
Q

Succinylcholine

Drug class

A

Depolarizing blocker

(Cholinergic Receptor-Inhibitors)

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95
Q

Succinylcholine

Mechanism

A

Overstimulation of nicotinic receptor, leading to desensitization of muscle unit to further ACh stimulation

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96
Q

Succinylcholine

Uses

A
  • Brief procedures (e.g., tracheal intubation, reset dislocated joints)
  • Produces flaccid paralysis within 1 minute
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97
Q

Succinylcholine

Side effects

A
  • Respiratory paralysis;
  • disturbance of autonomic function
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98
Q

Tubocurarine

Drug class

A

Nondepolarizing blocker

(Cholinergic Receptor-Inhibitors)

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99
Q

Tubocurarine

Mechanism

A
  • Blocks nicotinic (Nm) receptor
  • Lasts 30-60 minutes
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100
Q

Tubocurarine

Uses

A

Muscle relaxant for surgery w/o deep anesthesia

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101
Q

Tubocurarine

Side effects

A

Respiratory paralysis; disturbance of autonomic function

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102
Q

Mivacurium

Drug Class

A

Nondepolarizing blocker

(Cholinergic Receptor-Inhibitors)

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103
Q

Mivacurium

Mechanism

A
  • Blocks nicotinic (Nm) receptor
  • Rapidly hydrolyzed, short acting
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104
Q

Mivacurium

Uses

A

Muscle relaxant for surgery w/o deep anesthesia

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105
Q

Mivacurium

Side effects

A

Respiratory paralysis; disturbance of autonomic function

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106
Q

Botulinum toxin

Drug class

A

Local paralytic

(Cholinergic Receptor-Inhibitors)

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107
Q

Botulinum toxin

Mechanism

A

Blocks vesicle fusion and ACh release on presynaptic terminal by degrading SNAP-25

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108
Q

Botulinum toxin

Uses

A

Reduce frown lines and wrinkles; achalasia; strabismus; oromandibular dystonia

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109
Q

Norepinephrine

Drug class

A

Non-selective agonist

(Adrenergic receptor agonist)

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110
Q

Norepinephrine

Mechanism

A

Agonist: α1, α2, β1

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111
Q

Norepinephrine

Uses

A

Acute Hypotension

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112
Q

Norepinephrine

Side effects

A

Hypertension; arrythmias; headache

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113
Q

Epinephrine

Drug class

A

Non-selective agonist

(adrenergic receptor agonist)

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114
Q

Epinephrine

Mechanism

A

Agonist: α1, (α2), β1, β2

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115
Q

Epinephrine

Uses

A
  • Anaphylactic shock;
  • combined with local anesthetics;
  • glaucoma
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116
Q

Epinephrine

Side effects

A

Palpitation; arrhythmias; headache

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117
Q

Amphetamine

Drug class

A

Indirect acting

(Adrenergic receptor agonist)

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118
Q

Amphetamine

Mechanism

A

Increases release of NE

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119
Q

Amphetamine

Uses

A

ADHD, narcolepsy, recreation

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120
Q

Amphetamine

Side effects

A

Hypertension, insomnia, anxiety, arrhythmias

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121
Q

Isoproterenol

Drug class

A

Non-selective β agonist

(adrenergic receptor agonist)

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122
Q

Isoproterenol

Mechanism

A

Agonist: β1, β2

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123
Q

Isoproterenol

Uses

A

shock; heart block

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124
Q

Isoproterenol

Side effects

A

Palpitation; tachyarrhythmia; headache

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125
Q

Dobutamine

Drug class

A

β1-selective β agonist

(adrenergic receptor agonist)

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126
Q

Dobutamine

Mechanism

A

Agonist: β1

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127
Q

Dobutamine

Uses

A

Cardiac decompensation; shock; heart block

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128
Q

Dobutamine

Side effects

A

Tachyarrythmias; hypertension

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129
Q

Albuterol

Drug class

A

β2-selective β agonist

(adrenergic receptor agonist)

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130
Q

Albuterol

Mechanism

A
  • Agonist: β2
  • 10-15 minutes to take action, 6-12 hours (max) of duration; nebulizer delivers more, but greater side effects; oral is least effective (requires more dose –> side effects); can be used night symptoms, but not ideal
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131
Q

Albuterol

Uses

A

Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD

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132
Q

Albuterol

Side effects

A
  • Can mask progressively severe inflammation
  • Tachycardia, muscle tremor
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133
Q

Terbutaline

Drug class

A

β2-selective β agonist

(adrenergic receptor agonist)

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134
Q

Terbutaline

mechanism

A
  • Agonist: β2
  • 10-15 minutes to take action, 6-12 hours (max) of duration; nebulizer delivers more, but greater side effects; oral is least effective (requires more dose –> side effects); can be used night symptoms, but not ideal
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135
Q

Terbutaline

Uses

A
  • Prevent or reverse exercise-induced bronchospasm
  • mild asthma
  • COPD
  • early labor
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136
Q

Terbutaline

Side effects

A
  • Can mask progressively severe inflammation
  • Tachycardia, muscle tremor
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137
Q

Phenylephrine

Drug Class

A

α1-selective α agonist

(adrenergic receptor agonist)

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138
Q

Phenylephrine

Mechanism

A

Agonist: α1

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139
Q

Phenylephrine

Uses

A

Nasal congestion; postural Hypotension

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140
Q

Phenylephrine

Side effects

A

Hypertension; reflex bradycardia

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141
Q

Clonidine

Drug class

A

α2-selective α agonist

(cholinergic receptor agonist)

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142
Q

Clonidine

Uses

A

Hypertension; shock; withdrawal from drug dependence

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143
Q

Clonidine

Side effects

A

Sedation

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144
Q

α-methyldopa

Drug class

A

α2-selective α agonist

(cholinergic receptor agonist)

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145
Q

α-methyldopa

Mechanism

A

Metabolite (a-methylnorepinephrine) activates CNS a2 receptors

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146
Q

α-methyldopa

Uses

A

Hypertension

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147
Q

α-methyldopa

Side effects

A

Sedation

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148
Q

Fenoldopam

Drug class

A

Selective dopamine agonist

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149
Q

Fenoldopam

Mechanism

A

Agonist: D1 only

~10 minute half-life

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150
Q

Fenoldopam

Uses

A

Increase blood flow at renal, mesenteric, and cerebral arteries

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151
Q

Dopamine

Drug class

A

Mixed acting (direct/indirect)

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152
Q

Dopamine

Mechanism

A

Agonist: D1, α1, β1

Low dose = Direct @ D1 Receptors
Medium dose = Direct @ Beta 1, some Indirect
High dose = Direct @ Alpha 1, some Indirect

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153
Q

Dopamine

Uses

A

Shock, renal failure, hypotension

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154
Q

Dopamine

Side effects

A

Vasoconstriction (@ high doses)

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155
Q

Phentolamine

Drug class

A

Non-selective α-antagonist

(adrenergic receptor antagonist)

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156
Q

Phentolamine

Mechanism

A

Antagonist: α1, α2

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157
Q

Phentolamine

Uses

A

Pheochromocytoma, Raynaud’s, frostbite

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158
Q

Phentolamine

Side effects

A

Postural hypotension; inhibit ejaculation

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159
Q

Phenoxybenzamine

Drug class

A

Non-selective α-antagonist

(cholinergic receptor antagonist)

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160
Q

Phenoxybenzamine

Mechanism

A

Antagonist: α1, α2; non-competitive blocker (covalent bond to receptor)

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161
Q

Phenoxybenzamine

Uses

A

Pheochromocytoma, Raynaud’s, frostbite

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162
Q

Phenoxybenzamine

Side effects

A

Postural hypotension; inhibit ejaculation

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163
Q

Prazosin

Drug class

A

α1-selective antagonist

(adrenergic receptor antagonist)

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164
Q

Prazosin

Mechanism

A

Antagonist: α1

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165
Q

Prazosin

Uses

A

Primary HTN, BPH

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166
Q

Prazosin

Side effects

A

Postural hypotension (usually 1st dose)

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167
Q

Terazosin

Drug Class

A

α1-selective antagonist

(cholinergic receptor antagonist)

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168
Q

Terazosin

Mechanism

A

Antagonist: α1

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169
Q

Terazosin

Uses

A

Primary HTN, BPH

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170
Q

Terazosin

Side effects

A

Postural hypotension (usually 1st dose)

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171
Q

Propranolol

Drug Class

A

Non-selective β-antagonist (1st generation)

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172
Q

Propranolol

Mechanism

A

Antagonist: β1, β2

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173
Q

Propranolol

Uses

A

Angina, Hypertension, Arrythmias

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174
Q

Propranolol

Side effects

A

Bradycardia, Bronchoconstriction, Sexual Dysfunction

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175
Q

Timolol

Drug class

A

Non-selective β-antagonist (1st generation)

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176
Q

Timolol

Mechanism

A

Antagonist: β1, β2

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177
Q

Timolol

Uses

A

Glaucoma

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178
Q

Timolol

Side effects

A

Bradycardia, Bronchoconstriction, Sexual Dysfunction

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179
Q

Metoprolol

Drug Class

A

β1-selective antagonist (2nd generation)

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180
Q

Metoprolol

Mechanism

A

Antagonist: β1

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181
Q

Metoprolol

Uses

A

HTN, Angina, Arrythmias, CHF

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182
Q

Metoprolol

Side effects

A

Bradycardia, Sexual Dysfunction

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183
Q

Atenolol

Drug Class

A

β1-selective antagonist (2nd generation)

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184
Q

Atenolol

Mechanism

A

Antagonist: β1

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185
Q

Atenolol

Uses

A

HTN, Angina, Arrythmias, CHF

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186
Q

Atenolol

Side effects

A

Bradycardia, Sexual Dysfunction

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187
Q

Bisoprolol

Drug class

A

β1-selective antagonist (2nd generation)

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188
Q

Bisoprolol

Mechanism

A

Antagonist: β1

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189
Q

Bisoprolol

Uses

A

HTN, Angina, Arrythmias, CHF

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190
Q

Bisoprolol

Side effects

A

Bradycardia, Sexual Dysfunction

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191
Q

Carvedilol

Drug class

A

Non-selective β-antagonist (3rd generation “A”)

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192
Q

Carvedilol

Mechanism

A

Antagonist: β1, β2

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193
Q

Carvedilol

Uses

A

CHF, HTN

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194
Q

Carvedilol

Side effects

A

Bradycardia, Fatigue

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195
Q

Labetalol

Drug class

A

Non-selective β-antagonist (3rd generation “A”)

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196
Q

Labetalol

Mechanism

A

Antagonist: β1, β2

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197
Q

Labetalol

Uses

A

CHF, HTN

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198
Q

Labetalol

Side effects

A

Bradycardia, Fatigue

199
Q

Betaxolol

Drug class

A

β1-selective antagonist (3rd generation “B”)

200
Q

Betaxolol

Mechanism

A

Antagonist: β1

201
Q

Betaxolol

Uses

A

CHF, HTN

202
Q

Betaxolol

Side effects

A

Bradycardia

203
Q

Tyramine

Drug Class

A

Indirect acting agonist

(adrenergic)

204
Q

Tyramine

Mechanism

A

Increases cytoplasmic NE release

Tyramine is involved with an exchange transporter: tyramine goes in, NE comes out

205
Q

Cocaine

Mechanism

A

Prevents NE reuptake

206
Q

Cocaine

Therapeutics

A

Local anesthetic, vasoconstrictor

207
Q

Cocaine

Side effects

A

Insomnia, anxiety, arrhythmias

208
Q

Guanethidine

Drug class

A

Nerve ending blocker

209
Q

Guanethidine

Mechanism

A

False neurotransmitter (vesicles become full of guanethidine rather than NE)

(Doesn’t cross BBB)

210
Q

Guanethidine

Uses

A

Antihypertensive

211
Q

Guanethidine

Side effects

A

Many and serious

Not used much in US

212
Q

Reserpine

Drug class

A

Nerve ending blocker

213
Q

Reserpine

Mechanism

A

Release of empty vesicles (NE is not taken into vesicles b/c it binds uptake transporter and stops it)

214
Q

Reserpine

Uses

A

Older antihypertensive

Cheap! (used abroad, not here)

215
Q

Reserpine

Side effects

A

Many and serious (depression and suicide are major ones)

216
Q

α-me-tyrosine

Drug class

A

Nerve ending blocker

217
Q

α-me-tyrosine

Mechanism

A

Inhibit tyrosine hydroxylase (decreases NE synthesis)

218
Q

α-me-tyrosine

Uses

A

Pheochromocytoma

219
Q

α-me-tyrosine

Side effects

A

Many and serious

220
Q

Ephedrine

Drug class

A

Mixed, direct (β2)/indirect agonist

221
Q

Ephedrine

Uses

A

Nasal decongestion, anorexic

222
Q

Hyperbaric oxygen

Uses

A

Prevents lipid peroxidation (?) and delayed neurologic sequelae in CO poisoning

223
Q

Nitrites

Mechanism

A
  • Turns RBC hemoglobin to methemoglobin; CN moves from Fe(3+) on cytochromes to those in RBCs creating cyanomethemoglobin
  • Dangerous in concurrent CO poisoning
224
Q

Sodium thiosulfate

Mechanism

A

Enhances normal metabolism of cyanide via rhodanase

225
Q

Hydroxycobalamin

Mechanism

A

Binds with cyanide –> cyanocobalamin (B12)

226
Q

Hydroxycobalamin

Uses

A
  • Smoke inhalation victims not improving with supportive care, cyanide exposure, nitroprusside at risk patients
  • Give concurrently with sodium thiosulfate
227
Q

Methylene Blue

Mechanism

A

Cofactor of NADPH reductase; gains electron, donates directly to reduce methemoglobin

228
Q

Methylene Blue

Uses

A

Methemoglobinemia >20-30%, or with symptoms

229
Q

Methylene Blue

Side effects

A
  • Hemolytic anemia (weak oxidizing capability)
  • Painful at injection site, dyspnea, restlessness, tremor, precordial pain, and apprehension
230
Q

Quinine

Drug Class

A

Quinolone derivitive

231
Q

Quinine

Mechanism

A

Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases

232
Q

Quinine

Uses

A

Prophylaxis, treatment of acute malarial attacks

(Also called quinidine (used in anti-arrhythmias))

233
Q

Quinine

Side effects

A

Cinchonism, hypotension, hypoglycemia, abortion, arrhythmias

234
Q

Chloroquine

Drug class

A

Quinolone derivitive

235
Q

Chloroquine

Mechanism

A

Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases

236
Q

Chloroquine

Uses

A

Prophylaxis, treatment of acute malarial attacks

237
Q

Chloroquine

Side effects

A

Itching (Africans), retinitis (rare)

238
Q

Hydroxychloroquine

Drug class

A

Quinolone derivitive

239
Q

Hydroxychloroquine

Mechanism

A

Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases

240
Q

Hydroxychloroquine

Uses

A

Prophylaxis, treatment of acute malarial attacks

241
Q

Mefloquine

Drug class

A

Quinolone derivitive

242
Q

Mefloquine

Mechanism

A

Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases

243
Q

Mefloquine

Uses

A

Prophylaxis, treatment of acute malarial attacks

244
Q

Primaquine

Drug class

A

Quinolone derivitive

245
Q

Primaquine

Mechanism

A

Forms quinolone-quinone intermediates that oxidize schizont membranes

(Only drug that inhibits exoerythrocytic schyzogony)

246
Q

Primaquine

Uses

A

Prophylaxis, treatment of acute malarial attacks

247
Q

Primaquine

Side effects

A

Hemolysis (G6PD), methemoglobinemia

Fever, nausea, vomiting

248
Q

Amantadine

Mechanism

A

Positive charge helps chloroquine overcome chloroquine-resistant malaria vacuoles; point mutations against amantadine return bacteria to chloroquine-sensitivity

249
Q

Artesunate

Drug class

A

Artemisinin compound

250
Q

Artesunate

Mechanism

A

Specifically and selectively inhibit SERCA of P. falciparum

251
Q

Artesunate

Side effects

A

Neurotoxicity, prolongation of QT interval

252
Q

Artemether

Drug class

A

Artemisinin compound

253
Q

Artemether

Mechanism

A

Specifically and selectively inhibit SERCA of P. falciparum

254
Q

Lumefantrine

Drug class

A

Aminoalcohol

255
Q

Lumefantrine

Uses

A

Used in combination w/artemether (called Coartem)

256
Q

Atovoquone

Drug class

A

Napthalene

257
Q

Atovoquone

Mechanism

A

Depolarizes parasitic mitochondria and inhibits their electron transport

258
Q

Atovoquone

Uses

A

Used in combination w/proguanil

259
Q

Chloroguanide aka proguanil

Drug class

A

Antifolates

260
Q

Chloroguanide

Mechanism

A

Dihydrofolate reductase inhibitors (human and parasite pathway)

261
Q

Tetracycline

Drug class

A

Antibiotic

262
Q

Tetracycline

Uses

A

Severe malaria & chloroquine-resistant uncomplicated malaria

263
Q

Clindamycin

Drug class

A

Antibiotic

264
Q

Clindamycin

Uses

A

Severe malaria & chloroquine-resistant uncomplicated malaria

265
Q

Doxycycline

Drug class

A

Antibiotic

266
Q

Doxycycline

Uses

A

Severe malaria & chloroquine-resistant uncomplicated malaria

267
Q

Doxycycline

Side effects

A

Photosensitivity

268
Q

Aspirin

Drug class

A

Salicylate

269
Q

Aspirin

Mechanism

A

Acetyl-salicylic acid irreversibly acetylates COX-1 and -2; metabolite (salicylic acid) reversibly inhibits COX-1 and -2

270
Q

Aspirin

Uses

A

Antiplatelet, analgesic and antipyretic, and anti-inflammatory (in ascending order of amount taken); often taken as a “baby aspirin” to prevent MI, CVA

271
Q

Aspirin

Side effects

A

GI irritation, bleeding and anemia, hepatotoxicity, and salicylate toxicity

Nephrotoxicity in elderly or hypovolemic patients; rare hypersensitivity reaction

272
Q

Diflunisal

Drug class

A

Salicylate

273
Q

Diflunisal

Mechanism

A

Difluorophenyl derivitive of salicylic acid, which reversibly inhibits COX-1 and -2

274
Q

Diflunisal

Uses

A

Osteoarthritis, musculoskeletal strains/sprains, pain after dental extraction, and postepisiotomy pain

275
Q

Diflunisal

Side effects

A

Fewer GI side effects and less effect on platelets than aspirin

276
Q

Acetaminophen

Drug class

A

Para-amino phenol

277
Q

Acetaminophen

Mechanism

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

Poor function in presence of peroxides (as found in sites of inflammation); mostly metabolized via conjugation, but minor pathway via P450 enzymes may lead to toxic intermediate (N-acetyl-benzoquinoneimine)

278
Q

Acetaminophen

Uses

A

Analgesic and antipyretic effect similar to aspirin, but weak anti-inflammatory effects

279
Q

Acetaminophen

Side effects

A

Renal tubular necrosis if chronically abused with other NSAIDs; hepatic necrosis with overdose

GI irritation (less than aspirin)

280
Q

Indomethacin

Drug class

A

Indole

281
Q

Indomethacin

Mechanism

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

282
Q

Indomethacin

Uses

A

Rhematoid arthritis (10X as potent as aspirin), ankylosing spondylitis, osteoarthritis, acute gout

283
Q

Indomethacin

Side effects

A

At times, thrombocytopenia, aplastic anemia, and severe frontal headaches

Nephrotoxicity in elderly or hypovolemic patients

284
Q

Sulindac

Drug class

A

Indole

285
Q

Sulindac

Mechanism

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

286
Q

Sulindac

Uses

A

Rhematoid arthritis, ankylosing spondylitis, osteoarthritis, acute gout

Half as potent as indomethacin; side effects less frequent

287
Q

Sulindac

Side effects

A

At times, thrombocytopenia, aplastic anemia, and severe frontal headaches

Nephrotoxicity in elderly or hypovolemic patients

288
Q

Ibuprofen

Drug class

A

Proprionic acid derivative

289
Q

Ibuprofen

Mechanism

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

290
Q

Ibuprofen

Uses

A

Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

291
Q

Ibuprofen

Side effects

A

GI irritation; hepatotoxicity (less frequent than aspirin)

292
Q

Flurbiprofen

Drug class

A

Proprionic acid dervitive

293
Q

Flurbiprofen

Mechanism

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

294
Q

Flurbiprofen

Uses

A

Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

Can be used topically (obtains high synovial concentration)

295
Q

Flurbiprofen

Side effects

A

GI irritation; hepatotoxicity (less frequent than aspirin)

296
Q

Naproxen

Drug class

A

Propionic acid derivative

297
Q

Naproxen

Mechanism

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

Longer half-life than most proprionic acid derivitives (13 hours vs. 1-2 hours)

298
Q

Naproxen

Uses

A

Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

299
Q

Naproxen

Side effects

A

GI irritation; hepatotoxicity (less frequent than aspirin)

300
Q

Oxaprozin

Drug class

A

Proprionic acid derivative

301
Q

Oxaprozin

Mechanism

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

Much longer half-life than most proprionic acid derivitives (50 hours vs. 1-2 hours)

302
Q

Oxaprozin

Uses

A

Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

303
Q

Piroxicam

Drug class

A

Enolic acid

304
Q

Piroxicam

Mechanism

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

Very long half-life (45 hours) permits single daily dose

305
Q

Piroxicam

Uses

A

Long-term treatment of rheumatoid arthritis or osteoarthritis; also, ankylosing spondylitis, acute musculoskeletal disorders, acute gout

306
Q

Piroxicam

Side effects

A

Same as aspirin:

GI irritation, bleeding and anemia, hepatotoxicity, and salicylate toxicity

Nephrotoxicity in elderly or hypovolemic patients; rare hypersensitivity reaction

307
Q

Ketorolac

Drug action

A

Heteroaryl acetic acids

308
Q

Keterolac

Mechanism

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

Injectable (one of few NSAIDs available for this)

309
Q

Keterolac

Uses

A

Post-operative pain; inflammatory eye conditions

310
Q

Keterolac

Side effects

A

Same as aspirin; relatively nonirritating

311
Q

Diclofenac

Drug class

A

Heteroaryl acetic acids

312
Q

Diclofenac

Mechanism

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

313
Q

Diclofenac

Uses

A

Long-term treatment of rheumatoid arthritis or osteoarthritis; also, ankylosing spondylitis, migraines

also topically as ophthalmic solution for post-tx of eye surgery (like diclofenac)

314
Q

Diclofenac

Side effects

A

G. I. irritation

315
Q

Celocoxib

Drug class

A

COX-2 inhibitor

316
Q

Celocoxib

Mechanism

A

Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site)

317
Q

Celocoxib

Uses

A

Same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs

318
Q

Celocoxib

Side effects

A

Less GI toxicity than traditional NSAIDs

Contraindicated in patients with heart problems/pregnancy

319
Q

Etoricoxib

Drug class

A

COX-2 inhibitor

320
Q

Etoricoxib

Mechanism

A

Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site)

321
Q

Etoricoxib

Uses

A

Same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs

322
Q

Etoricoxib

Side effects

A

Less GI toxicity than traditional NSAIDs

Contraindicated in patients with heart problems/pregnancy

323
Q

Hydrocortisone

Drug class

A

Steroid

324
Q

Hydrocortisone

Uses

A

Dermatitis, psoriasis

325
Q

Hydrocortisone

Side effects

A

Atrophy/thinning of skin (collagen), stretch marks, talangiectasias, acne, cataract or glaucoma if applied near eye

Systemically, affects hypothalamic-pituitary-adrenal axis –> growth retardation

326
Q

Cyclosporine

Drug class

A

Immunosuppressant

327
Q

Cyclosporine

Uses

A

Inflammatory conditions (psoriasis)

328
Q

Cyclosporine

Side effects

A

Raise blood pressure, damage kidneys if used long-term

329
Q

Methotrexate

Drug class

A

Folate analog

330
Q

Methotrexate

Mechanism

A

Inhibits DHFR

331
Q

Methotrexate

Uses

A

Inflammatory conditions (psoriasis), conditions needing immunosuppression

332
Q

Methotrexate

Side effects

A
  • Hepatotoxicity (develops slowly, can give up to 4.5 g over life); pulmonary toxicity (develops quickly); leukopenia; rarely, renal toxicity
  • Nausea, vomiting
  • PO, IM (1/week); any drug increasing unbound protein may cause methotrexate toxicity (sulfa, salicylates, TCN, phenytoin)
333
Q

Biologics

Mechanism

A

Block TNF-a

334
Q

Biologics

Uses

A

Inflammatory conditions, arthritis

335
Q

Biologics

Side effects

A
  • Few (may unmask neurologic disease, latent infections (must do PPDs), malignancies)
  • costly
336
Q

UV light therapy

Class

A

UVA, UVB, UVC

337
Q

UV Light Therapy

Mechanism

A
  • Immunosuppression of T-cells via type I or type II reactions –> mono- or bifunctional adducts in DNA
338
Q

UV Light Therapy

Uses

A
  • Inflammatory conditions: atopic dermatitis, CTCL, lichen planus, psoriasis (not useful for non-inflammatory conditions)
  • Usually used with psoralens (photosensitizing agents that increase efficacy); phenothiazines, thiazides, sulfonamides, NSAIDs, tetracycline, benzodiazapenes also sensitize skin to light therapy
339
Q

UV Light Therapy

Side effects

A

Skin cancer, thinning/leathering of skin

340
Q

Isotretinoin

Class

A

Retinoid

341
Q

Isotretinoin

Mechanism

A

Stimulate epithelial cell turnover; also anti-inflammatory

342
Q

Isotretinoin

Uses

A
  • Acne
  • Good as adjunct to other therapies
343
Q

Isotretinoin

Side effects

A

Teratogenic effects (washes out in three weeks)

344
Q

Acitretin

Class

A

Retinoid

345
Q

Acitretin

Mechanism

A

Stimulate epithelial cell turnover; also anti-inflammatory

346
Q

Acitretin

Uses

A
  • Psoriasis
  • Good as adjunct to other therapies
347
Q

Acitretin

Side effects

A

Teratogenic effects (stays in fat stores for three years)

348
Q

H1 receptor antagonist

Mechanism

A
  • H1 receptor antagonist; rapidly absorbed orally, widely distributed, rapidly metabolized via liver microsomes
  • Older agents cross CNS to cause central effects
349
Q

H1 receptor antagonist

Uses

A

Allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids

350
Q

H1 receptor antagonist

Side effects

A

Sedation, anti-muscarinic action, poisoning (especially children) with convulsions, allergy, local anesthesia

351
Q

Diphenhydramine (Benadryl)

Drug Class

A

Ether/ethanolamine derivitive

352
Q

Diphenhydramine (Benadryl)

Uses

A

Allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids

353
Q

H1 receptor antagonist

Side effects

A

Anti-muscarinic, sedating

354
Q

Tripenelennamine
Drug class

A

Ethylenediamine derivitive

355
Q

Tripelennamine

Mechanism

A

H1 receptor antagonist

356
Q

Tripelennamine

Uses

A

OTC sleep aid

357
Q

Meclizine

Drug class

A

Piperazine derivative

358
Q

Meclizine

Mechanism

A

H1 receptor antagonist

359
Q

Meclizine

Uses

A

Motion sickness

360
Q

Promethazine

Mechanism

A

H1 receptor antagonist

361
Q

Promethazine

Uses

A

Antiemetic

362
Q

Promethazine

Side effects

A

Anti-muscarinic, sedating

363
Q

Chlorpheniramine

Mechanism

A

H1 receptor antagonist

364
Q

Chlorpheniramine

Uses

A

Component of “cold” medications

365
Q

Chlorpheniramine

Side effects

A

Less sedating

366
Q

Loratadine

Mechanism

A

2nd generation H1 receptor antagonist

367
Q

Loratadine

Uses

A

Allergic rhinitis

368
Q

Loratadine

Side effects

A
  • No sedation
  • Cardiovascular effects (rare, with high doses)
  • Poorly crosses BBB, so fewer central and side effects
369
Q

Fexofenadine

Mechanism

A

2nd generation H1 receptor antagonist

370
Q

Fexofenadine

Uses

A

Allergic rhinitis

371
Q

Fexofenadine

Side effects

A
  • No sedation
  • Cardiovascular effects (rare, with high doses)
  • Poorly crosses BBB, so fewer central and side effects
372
Q

Azelastine

Mechanism

A

2nd generation H1 receptor antagonist

373
Q

Azelastine

Uses

A

Allergic rhinitis (intranasal spray), allergic conjunctivitis (ophthalmic solution)

374
Q

Azelastine

Side effects

A
  • No sedation
  • Poorly crosses BBB, so fewer central and side effects
375
Q

Cetirazine

Mechanism

A

2nd generation H1 receptor antagonist

376
Q

Cetirazine

Uses

A

Allergic rhinitis

377
Q

Cetirazine

Side effects

A
  • No sedation
  • Poorly crosses BBB, so fewer central and side effects
378
Q

Cimetidine

Mechanism

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)

379
Q

Cimetidine

Uses

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

380
Q

Cimetidine

Side effects

A

Antiandrogen (causing impotence and gynecomastia), inhibition of P450 enzymes

CNS dysfunction possible

Most side effects of H2-blocker class

381
Q

Ranitidine

Mechanism

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)

382
Q

Ranitidine

Uses

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

383
Q

Ranitidine

Side effects

A

Liver toxicity

CNS dysfunction possible

384
Q

Famotidine

Mechanism

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)

385
Q

Famotidine

Uses

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

386
Q

Famotidine

Side effects

A

CNS dysfunction possible

387
Q

Nizatidine

Mechanism

A

H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)

388
Q

Nizatidine

Uses

A

Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions

389
Q

Nizatidine

Side effects

A

CNS dysfunction possible

Least side effects of H2-blocker class

390
Q

Cyproheptidine

Mechanism

A

Antihistaminic and antiserotinergic

391
Q

Cyproheptidine

Uses

A

Skin allergies (urticaria, anti-H1), diarrhea of carcinoid syndrome (anti-5HT2)

392
Q

Cyproheptidine

Side effects

A

Sedation, antimuscarinic

393
Q

Ketanserin

Mechanism

A

Selective 5HT2A,2C receptor antagonist, as well as α1 and H1 receptor antagonist

394
Q

Ketanserin

Uses

A

Antihypertensive (relaxes vascular and tracheal smooth muscle), antiplatelet aggregation

395
Q

Odansetron

Mechanism

A

5HT3 receptor antagonist

396
Q

Odansetron

Side effects

A

Nausea and vomiting in chemotherapy

397
Q

Ergot alkaloids

Mechanism

A

Agonist and antagonist actions at 5HT and α-adrenergic receptors

398
Q

Ergot alkaloids

Side effects

A

Powerful hallucinations, smooth muscle contraction (vascular and uterine)

399
Q

Ergotamine

Class

A

Ergot alkaloid

400
Q

Ergotamine

Mechanism

A

Nonspecific partial agonist at all 5HT1,2 receptors; partial agonist at α-adrenergic receptors

401
Q

Ergotamine

Uses

A

Prodrome of migraines

402
Q

Ergotamine

Side effects

A

N/V, cumulative and prolonged vasoconstriction

403
Q

Methyseride

Class

A

Ergot alkaloid

404
Q

Methyseride

Mechanism

A

Partial agonist at all 5HT1 receptors, antagonist at 5HT2

405
Q

Methyseride

Uses

A

Prophylaxis of migraines

406
Q

Methyseride

Side effects

A

GI disturbances, inflammatory fibrosis (chronic use), hallucinations

Withdrawn from U.S. market

407
Q

Ergonovine

Class

A

Ergot alkaloid

408
Q

Ergonovine

Uses

A

Postpartum hemorrhage (Oxytocic)

409
Q

Bromocriptine

Class

A

Ergot alkaloid

410
Q

Bromocriptine

Mechanism

A

Dopamine agonist

411
Q

Bromocriptine

Uses

A

Hyperprolactinemia

412
Q

Triptan

Class

A

Non-ergot serotonin analogs

413
Q

Triptan

Mechanism

A

5HT1B,D receptor agonist

414
Q

Triptan

Side effects

A

Effective (70%) migraine treatment

415
Q

Unfractionated heparin

Drug class

A

Indirect thrombin inhibitors

416
Q

Unfractionated heparin

Mechanism

A

Bind antithrombin, potentiating formation of antithrombin-coagulation factor complex (Xa, IIa)

417
Q

Unfractionated heparin

Uses

A
  • Prevention and treatment of venous thromboembolism
  • Given parenterally; monitored via PTT (want 2-2.5X normal value); reversed by protamine
418
Q

Unfractionated heparin

Side effects

A

HIT, bleeding

Osteoporosis

419
Q

Dalteparin

Drug class

A

Indirect thrombin inhibitors

420
Q

Dalteparin

Mechanism

A

LMWH that inhibits thrombin less effectively than Xa

421
Q

Dalteparin

Uses

A
  • Prevent thrombosis and embolism from clots
  • Monitored by heparin assay (anti-factor Xa); longer half-life than heparin (1-2/day); reversed by protamine
422
Q

Dalteparin

Side effects

A

Bleeding

423
Q

Enoxaparin

Drug class

A

Indirect thrombin inhibitors

424
Q

Enoxaparin

Mechanism

A

LMWH that inhibits thrombin less effectively than Xa

425
Q

Enoxaparin

Uses

A
  • Drug of choice in pregnancy; prevention and treatment of venous thromboembolism
  • Can be monitored by heparin assay (anti-factor Xa); longer half-life than heparin (1-2/day); reversed by protamine
426
Q

Enoxaparin

Side effects

A

HIT; bleeding;

osteoporosis and thrombocytopenia uncommon

427
Q

Fondaparinux

Drug class

A

Indirect thrombin inhibitors

428
Q

Fondaparinux

Mechanism

A

Synthetic polysaccharide that binds active site of antithrombin; inhibits Xa

Activates antithrombin, inhibits Xa

429
Q

Fondaparinux

Uses

A

Given for HIT

430
Q

Fondaparinux

Side effects

A

Bleeding

No antidote

431
Q

Warfarin

Drug class

A

Vitamin K antagonist

432
Q

Warfarin

Mechanism

A

Blocks vitamin K-dependent gamma-carboxylation of factors II, VII, IX, X, Protein C and S (does not affect already synthesized factors)

Metabolism enhanced by drugs that induce P450 activity (e.g., barbiturates); monitored by PT/INR; reversed by vitamin K and factor concentrates;

433
Q

Warfarin

Uses

A

Long term anticoagulation

434
Q

Warfarin

Side effects

A

Thrombosis (protein C depression)

Bleeding

contraindicated in pregnancy (teratogen)

435
Q

Bivalirudin

Drug class

A

Direct thrombin inhibitor

436
Q

Bivalirudin

Mechanism

A

Inactivate fibrinogen-bound AND unbound thrombin; irreversible

Administered parenterally; monitored by PTT

437
Q

Bivalirudin

Uses

A

Percutaneous coronary intervention (PCI)

438
Q

Bivalirudin

Side effects

A

Bleeding

No antidote

439
Q

Argatroban

Drug class

A

Direct thrombin inhibitor

440
Q

Argatroban

Mechanism

A

Inactivate fibrinogen-bound AND unbound thrombin

441
Q

Argatroban

Uses

A

Percutaneous coronary intervention (PCI); HIT

Administered parenterally; monitored by PTT;

442
Q

Argatroban

Side effects

A

Bleeding

No antidote

443
Q

Dabigatran

Drug class

A

Direct thrombin inhibitor

444
Q

Dabigatran

Mechanism

A

Inactivate fibrinogen-bound AND unbound thrombin; competitive (reversible)

Oral

Renal fixed dose clearance

445
Q

Dabigatran

Uses

A

DVT / PE; AFib

446
Q

Dabigatran

Side effects

A

Bleeding

No antidote

447
Q

Rivaroxaban

Drug class

A

Direct Xa inhibitor

448
Q

Rivaroxaban

Mechanism

A

Reversible bind active site of Xa

Oral

Fixed renal clearance

449
Q

Rivaroxaban

Uses

A

DVT / PE prophylaxis

450
Q

Rivaroxaban

Side effects

A

Bleeding

No antidote

451
Q

Apixaban

Drug class

A

Direct Xa inhibitor

452
Q

Apixaban

Mechanism

A

Reversible bind active site of Xa

Oral

Fixed renal dose clearance

453
Q

Apixaban

Uses

A

DVT / PE prophylaxis

454
Q

Apixaban

Side effects

A

Bleeding

No antidote

455
Q

Alteplase

Drug class

A

Fibrinolytic

456
Q

Alteplase

Mechanism

A

Lyse already formed clots by activating plasminogen

457
Q

Alteplase

Uses

A

STEMI; acute stroke; PE

458
Q

Reteplase

Drug class

A

Fibrinolytic

459
Q

Reteplase

Mechanism

A

Lyse already formed clots; less clot specific, more systemic activation

Short half life

460
Q

Reteplase

Uses

A

STEMI

461
Q

Reteplase

Side effects

A

Bleeding

Arrhythmia

462
Q

Tenecteplase

Drug class

A

Fibrinolytic

463
Q

Tenecteplase

Mechanism

A

Lyse already formed clots; more clot specific, less systemic activation

464
Q

Tenecteplase

Uses

A

STEMI

465
Q

Aspirin

Drug class (in clotting)

A

Antiplatelet

466
Q

Aspirin

Mechanism (in clotting)

A

Irreversibly inhibits platelets, preventing thromboxane A2 formation

467
Q

Aspirin

Uses (in clotting)

A

Often as “baby aspirin” to prevent and treat MI and stroke

468
Q

Dipyridamole

Drug class

A

Antiplatelet

469
Q

Dipyridamole

Mechanism

A

PDE inhibitor –> increase in platelet cAMP–> decrease aggregation

470
Q

Dipyridamole

Uses

A

Weak antiplatelet effect

Given parenterally

471
Q

Cilostazol

Drug class

A

Antiplatelet

472
Q

Cilostazol

Mechanism

A

PDE inhibitor –> increase in platelet cAMP–> decrease aggregation

473
Q

Cilostazol

Uses

A

Weak antiplatelet effect

474
Q

Clopidogrel

Drug class

A

Antiplatelet

475
Q

Clopidogrel

Mechanism

A

Inhibits platelet ADP receptors (P2Y12)

476
Q

Clopidogrel

Uses

A

Prevent & treat ACS, stroke, peripheral vascular disease, angina, stent

477
Q

Clopidogrel

Side effects

A

Bleeding; TTP (rare)

Reversed by platelet transfusion

478
Q

Prasugrel

Drug class

A

Antiplatelet

479
Q

Prasugrel

Mechanism

A

Inhibits platelet ADP receptors (P2Y12)

480
Q

Prasugrel

Uses

A

Prevent & treat ACS, stroke, peripheral vascular disease, angina, stent

Can be used in patients with clopidogrel resistance

481
Q

Prasugrel

Side effects

A

More bleeding and more potent than clopidogrel

482
Q

Ticagrelor

Drug class

A

Antiplatelet

483
Q

Ticagrelor

Mechanism

A

Allosteric reversible inhibitor of ADP Receptor (P2Y12)

484
Q

Ticagrelor

Uses

A

ACS, PCI

485
Q

Abciximab

Drug class

A

Antiplatelet

486
Q

Abciximab

Mechanism

A

Monoclonal antibody against GP IIb/IIIa

Given parenterally

487
Q

Abciximab

Side effects

A

May elicit immune response

488
Q

Eptifibatide

Drug class

A

Antiplatelet

489
Q

Eptifibatide

Mechanism

A

Fibrinogen analog which competes with endogenous fibrinogen for IIb/IIIa

Given parenterally

490
Q

Eptifibatide

Side effects

A

Bleeding; ACS; PCI

Thrombocytopenia

491
Q

Tirofiban

Drug class

A

antiplatelet

492
Q

Tirofiban

Mechanism

A

Fibrinogen analog which competes with endogenous fibrinogen and vWF for IIb/IIIa

Given parenterally; immediate effect

493
Q

Tirofiban

Side effects

A

Bleeding; NSTE-ACS