Unit 2-ANS, Anticoagulants, Hemoglobin, Antimalarials, Histamine Flashcards
(493 cards)
1
Q
Common side effects of cholinomimetics
A
SLUDGE:
- Salivation
- Lacrimation
- Urination
- Diaphoresis
- GI Upset (diarrhea)
- Emesis (vomiting)
2
Q
Bethanecol
Drug Class
A
Direct acting carbamic acid ester
(cholinomimetic)
3
Q
Bethanecol
Mechanism
A
Direct-acting muscarinic cholinomimetic
4
Q
Bethanecol
Uses
A
- Post-operative and neurogenic ileus;
- urinary retention (bowel and bladder smooth muscle ACh-innervated)
5
Q
Bethanecol
Side effects
A
SLUDGE
6
Q
Muscarine
Drug Class
A
Direct acting non-ester alkaloid
(cholinomimetic)
7
Q
Muscarine
Mechanism
A
Direct-acting muscarinic cholinomimetic
8
Q
Muscarine
Side Effects
A
SLUDGE
9
Q
Pilocarpine
Drug Class
A
Direct acting non-ester alkaloid
(cholinomimetic)
10
Q
Pilocarpine
Mechanism
A
Direct-acting muscarinic cholinomimetic
11
Q
Pilocarpine
Uses
A
Glaucoma (ACh activates sphincter and ciliary muscles of eye)
12
Q
Pilocarpine
Side effects
A
SLUDGE
13
Q
Cevimeline
Drug Class
A
Direct acting non-ester alkaloid
(cholinomimetic)
14
Q
Cevimeline
Mechanism
A
Direct-acting muscarinic cholinomimetic
15
Q
Cevimeline
Uses
A
Dry mouth (in, e.g., Sjogren’s, post-radiation therapy; via increased salivation)
16
Q
Cevimeline
Side effects
A
SLUDGE
17
Q
Nicotine
Drug class
A
Direct acting non-ester alkaloid
(cholinomimetic)
18
Q
Nicotine
Mechanism
A
Direct-acting nicotinic cholinomimetic
19
Q
Nicotine
Uses
A
Smoking cessation (reduces cravings)
20
Q
Neostigmine
Drug class
A
Indirect acting carbamate
(cholinomimetic)
21
Q
Neostigmine
Mechanism
A
AChE inhibitor (short acting)
Lasts 0.5-2 hours
22
Q
Neostigmine
Uses
A
- Post-operative and neurogenic ileus;
- urinary retention;
- myasthenia gravis;
- reversal of neuromuscular blockade
23
Q
Neostigmine
Side effects
A
- SLUDGE + general increase in cholinergic neurotransmission;
- paralysis
24
Q
Physostigmine
Drug class
A
Indirect acting carbamate
(cholinomimetic)
25
Physostigmine
Mechanism
AChE inhibitor (short acting)
Lasts 0.5-2 hours
26
Physostigmine
Uses
Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
27
Physostigmine
Side effects
SLUDGE + general increase in cholinergic neurotransmission; paralysis
28
Donepezil
Drug Class
Indirect acting non-ester
| (cholinomimetic)
29
Donepezil
Mechanism
AChE inhibitor
30
Donepezil
Uses
Alzheimer's (amplifies endogenous ACh in brain)
31
Donepezil
Side effects
SLUDGE + general increase in cholinergic neurotransmission; paralysis
32
Edrophonium
Drug class
Indirect acting non-ester
| (cholinomimetic)
33
Edrophonium
Mechanism
AChE inhibitor (v. short acting)
Lasts 5-15 minutes
34
Edrophonium
Uses
* Myasthenia gravis (differentiating deficiency versus ACh crisis);
* ileus
35
Edrophonium
Side effects
SLUDGE + general increase in cholinergic neurotransmission; paralysis
36
Ectothiophate
Drug Class
Indirect acting organophosphate
| (cholinomimetic)
37
Ectothiophate
Mechanism
AChE inhibitor (long acting)
Lasts \>100 hours
38
Ectothiophate
Uses
Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
39
Ectothiophate
Side effects
SLUDGE + general increase in cholinergic neurotransmission; paralysis
40
Pralidoxime
Drug class
Strong nucleophile
| (cholinomimetic)
41
Pralidoxime
Mechanism
Regenerates phosphorylated AChE
42
Pralidoxime
Uses
Poisoning by nerve gas, insecticide
43
Sarin
Drug class
Very potent indirect acting organophosphate
(cholinomimetic)
44
Sarin
Mechanism
AChE inhibitor
45
Sarin
Uses
Volatile nerve gas
46
Sarin
Side effects
* SLUDGE + general increase in cholinergic neurotransmission; paralysis
* Death
* Treat with pralidoxime and atropine before aging
47
Parathion
Drug class
Very potent indirect acting organophosphate
(cholinomimetic)
48
Parathion
Mechanism
AChE inhibitor
49
Parathion
Uses
Insecticide
50
Parathion
Side effects
* SLUDGE + general increase in cholinergic neurotransmission; paralysis
* Death
* Treat with pralidoxime and atropine before aging
51
Atropine
Drug Class
Tertiary amine antimuscarinic
| (Cholinergic Receptor-Inhibitors)
52
Atropine
Mechanism
Blocks muscarinic receptors
53
Atropine
Uses
Mydriasis; cycloplegia
54
Atropine
Side effects
General block of muscarinic functions
55
Scopalamine
Drug class
Tertiary amine antimuscarinic
| (Cholinergic Receptor-Inhibitors)
56
Scopalamine
Mechanism
Blocks muscarinic receptors
57
Scopalamine
Uses
Prevent or reduce motion sickness
58
Scopalamine
Side effects
General block of muscarinic functions
59
Dicyclomine
Drug class
Tertiary amine antimuscarinic
| (Cholinergic Receptor-Inhibitors)
60
Dicyclomine
Mechanism
Blocks muscarinic receptors
61
Dicyclomine
Uses
Reduce transient hypermotility
62
Dicyclomine
Side effects
General block of muscarinic functions
63
Tropicamide
Drug class
Tertiary amine antimuscarinic
| (Cholinergic Receptor-Inhibitors)
64
Tropicamide
Uses
Mydriasis; cycloplegia
65
Tropicamide
Side effects
General block of muscarinic functions
66
Tropicamide
Mechanism
Blocks muscarinic receptors
Very rapidly metabolized
67
Tolterodine
Drug class
Tertiary amine antimuscarinic
| (Cholinergic Receptor-Inhibitors)
68
Tolterodine
Mechanism
Blocks muscarinic receptors
69
Tolterodine
Uses
Treat transient cystitis; postoperative bladder spasms; incontinence
70
Tolterodine
Side effects
General block of muscarinic functions
71
Benztropine
Drug Class
Tertiary amine antimuscarinic
| (Cholinergic Receptor-Inhibitors)
72
Benztropine
Mechanism
Blocks muscarinic receptors
\*crosses BBB\*
73
Benztropine
Uses
Treat manifestations of Parkinson's disease
74
Benztropine
Side effects
General block of muscarinic functions
75
Glycopyrrolate
Drug class
Quaternary amine antimuscarinic
| (Cholinergic Receptor-Inhibitors)
76
Glycopyrrolate
Mechanism
Blocks muscarinic receptors
77
Glycopyrrolate
Uses
Reduce transient hypermotility
78
Glycopyrrolate
Side effects
General block of muscarinic functions
79
Tertiary vs Quaternary amine antimuscarinics
Tertiary: uncharged, crosses BBB
Quaternary: +charged; does not cross BBB
80
Ipatroprium
Drug class
Quarternary amine antimuscarinic
| (Cholinergic Receptor-Inhibitors)
81
Ipatroprium
Mechanism
Blocks muscarinic receptors
82
Ipatroprium
Uses
Bronchodilation in asthma or COPD
83
Ipatroprium
Side effects
General block of muscarinic functions
84
Tiotroprium
Drug class
Quarternary amine antimuscarinic
| (Cholinergic Receptor-Inhibitors)
85
Tiotroprium
Mechanism
Blocks muscarinic receptors
86
Tiotroprium
Uses
Bronchodilation in asthma or COPD
| (Longer acting than ipratropium)
87
Tiotroprium
Side effects
General block of muscarinic functions
88
Hexamethonium
Drug Class
Ganglionic blocker
| (Cholinergic Receptor-Inhibitors)
89
Hexamethonium
Mechanism
Blocks ganglionic (Nn) receptor and sympathetic tone
90
Hexamethonium
Uses
Hypertensive crisis; "Bloodless" field surgery
(rarely used now)
91
Mecamylamine
Drug Class
Ganglionic blocker
| (Cholinergic Receptor-Inhibitors)
92
Mecamylamine
Mechanism
Blocks ganglionic (Nn) receptor and sympathetic tone
93
Mecamylamine
Uses
Hypertensive crisis; "Bloodless" field surgery
(rarely used now)
94
Succinylcholine
Drug class
Depolarizing blocker
| (Cholinergic Receptor-Inhibitors)
95
Succinylcholine
Mechanism
Overstimulation of nicotinic receptor, leading to desensitization of muscle unit to further ACh stimulation
96
Succinylcholine
Uses
* Brief procedures (e.g., tracheal intubation, reset dislocated joints)
* Produces flaccid paralysis within 1 minute
97
Succinylcholine
Side effects
* Respiratory paralysis;
* disturbance of autonomic function
98
Tubocurarine
Drug class
Nondepolarizing blocker
| (Cholinergic Receptor-Inhibitors)
99
Tubocurarine
Mechanism
* Blocks nicotinic (Nm) receptor
* Lasts 30-60 minutes
100
Tubocurarine
Uses
Muscle relaxant for surgery w/o deep anesthesia
101
Tubocurarine
Side effects
Respiratory paralysis; disturbance of autonomic function
102
Mivacurium
Drug Class
Nondepolarizing blocker
| (Cholinergic Receptor-Inhibitors)
103
Mivacurium
Mechanism
* Blocks nicotinic (Nm) receptor
* Rapidly hydrolyzed, short acting
104
Mivacurium
Uses
Muscle relaxant for surgery w/o deep anesthesia
105
Mivacurium
Side effects
Respiratory paralysis; disturbance of autonomic function
106
Botulinum toxin
Drug class
Local paralytic
| (Cholinergic Receptor-Inhibitors)
107
Botulinum toxin
Mechanism
Blocks vesicle fusion and ACh release on presynaptic terminal by degrading SNAP-25
108
Botulinum toxin
Uses
Reduce frown lines and wrinkles; achalasia; strabismus; oromandibular dystonia
109
Norepinephrine
Drug class
Non-selective agonist
| (Adrenergic receptor agonist)
110
Norepinephrine
Mechanism
Agonist: α1, α2, β1
111
Norepinephrine
Uses
Acute Hypotension
112
Norepinephrine
Side effects
Hypertension; arrythmias; headache
113
Epinephrine
Drug class
Non-selective agonist
| (adrenergic receptor agonist)
114
Epinephrine
Mechanism
Agonist: α1, (α2), β1, β2
115
Epinephrine
Uses
* Anaphylactic shock;
* combined with local anesthetics;
* glaucoma
116
Epinephrine
Side effects
Palpitation; arrhythmias; headache
117
Amphetamine
Drug class
Indirect acting
| (Adrenergic receptor agonist)
118
Amphetamine
Mechanism
Increases release of NE
119
Amphetamine
Uses
ADHD, narcolepsy, recreation
120
Amphetamine
Side effects
Hypertension, insomnia, anxiety, arrhythmias
121
Isoproterenol
Drug class
Non-selective β agonist
| (adrenergic receptor agonist)
122
Isoproterenol
Mechanism
Agonist: β1, β2
123
Isoproterenol
Uses
shock; heart block
124
Isoproterenol
Side effects
Palpitation; tachyarrhythmia; headache
125
Dobutamine
Drug class
β1-selective β agonist
| (adrenergic receptor agonist)
126
Dobutamine
Mechanism
Agonist: β1
127
Dobutamine
Uses
Cardiac decompensation; shock; heart block
128
Dobutamine
Side effects
Tachyarrythmias; hypertension
129
Albuterol
Drug class
β2-selective β agonist
| (adrenergic receptor agonist)
130
Albuterol
Mechanism
* 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
131
Albuterol
Uses
Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD
132
Albuterol
Side effects
* Can mask progressively severe inflammation
* Tachycardia, muscle tremor
133
Terbutaline
Drug class
β2-selective β agonist
| (adrenergic receptor agonist)
134
Terbutaline
mechanism
* 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
135
Terbutaline
Uses
* Prevent or reverse exercise-induced bronchospasm
* mild asthma
* COPD
* early labor
136
Terbutaline
Side effects
* Can mask progressively severe inflammation
* Tachycardia, muscle tremor
137
Phenylephrine
Drug Class
α1-selective α agonist
| (adrenergic receptor agonist)
138
Phenylephrine
Mechanism
Agonist: α1
139
Phenylephrine
Uses
Nasal congestion; postural Hypotension
140
Phenylephrine
Side effects
Hypertension; reflex bradycardia
141
Clonidine
Drug class
α2-selective α agonist
| (cholinergic receptor agonist)
142
Clonidine
Uses
Hypertension; shock; withdrawal from drug dependence
143
Clonidine
Side effects
Sedation
144
α-methyldopa
Drug class
α2-selective α agonist
| (cholinergic receptor agonist)
145
α-methyldopa
Mechanism
Metabolite (a-methylnorepinephrine) activates CNS a2 receptors
146
α-methyldopa
Uses
Hypertension
147
α-methyldopa
Side effects
Sedation
148
Fenoldopam
Drug class
Selective dopamine agonist
149
Fenoldopam
Mechanism
Agonist: D1 only
~10 minute half-life
150
Fenoldopam
Uses
Increase blood flow at renal, mesenteric, and cerebral arteries
151
Dopamine
Drug class
Mixed acting (direct/indirect)
152
Dopamine
Mechanism
Agonist: D1, α1, β1
Low dose = Direct @ D1 Receptors
Medium dose = Direct @ Beta 1, some Indirect
High dose = Direct @ Alpha 1, some Indirect
153
Dopamine
Uses
Shock, renal failure, hypotension
154
Dopamine
Side effects
Vasoconstriction (@ high doses)
155
Phentolamine
Drug class
Non-selective α-antagonist
| (adrenergic receptor antagonist)
156
Phentolamine
Mechanism
Antagonist: α1, α2
157
Phentolamine
Uses
Pheochromocytoma, Raynaud's, frostbite
158
Phentolamine
Side effects
Postural hypotension; inhibit ejaculation
159
Phenoxybenzamine
Drug class
Non-selective α-antagonist
| (cholinergic receptor antagonist)
160
Phenoxybenzamine
Mechanism
Antagonist: α1, α2; non-competitive blocker (covalent bond to receptor)
161
Phenoxybenzamine
Uses
Pheochromocytoma, Raynaud's, frostbite
162
Phenoxybenzamine
Side effects
Postural hypotension; inhibit ejaculation
163
Prazosin
Drug class
α1-selective antagonist
| (adrenergic receptor antagonist)
164
Prazosin
Mechanism
Antagonist: α1
165
Prazosin
Uses
Primary HTN, BPH
166
Prazosin
Side effects
Postural hypotension (usually 1st dose)
167
Terazosin
Drug Class
α1-selective antagonist
| (cholinergic receptor antagonist)
168
Terazosin
Mechanism
Antagonist: α1
169
Terazosin
Uses
Primary HTN, BPH
170
Terazosin
Side effects
Postural hypotension (usually 1st dose)
171
Propranolol
Drug Class
Non-selective β-antagonist (1st generation)
172
Propranolol
Mechanism
Antagonist: β1, β2
173
Propranolol
Uses
Angina, Hypertension, Arrythmias
174
Propranolol
Side effects
Bradycardia, Bronchoconstriction, Sexual Dysfunction
175
Timolol
Drug class
Non-selective β-antagonist (1st generation)
176
Timolol
Mechanism
Antagonist: β1, β2
177
Timolol
Uses
Glaucoma
178
Timolol
Side effects
Bradycardia, Bronchoconstriction, Sexual Dysfunction
179
Metoprolol
Drug Class
β1-selective antagonist (2nd generation)
180
Metoprolol
Mechanism
Antagonist: β1
181
Metoprolol
Uses
HTN, Angina, Arrythmias, CHF
182
Metoprolol
Side effects
Bradycardia, Sexual Dysfunction
183
Atenolol
Drug Class
β1-selective antagonist (2nd generation)
184
Atenolol
Mechanism
Antagonist: β1
185
Atenolol
Uses
HTN, Angina, Arrythmias, CHF
186
Atenolol
Side effects
Bradycardia, Sexual Dysfunction
187
Bisoprolol
Drug class
β1-selective antagonist (2nd generation)
188
Bisoprolol
Mechanism
Antagonist: β1
189
Bisoprolol
Uses
HTN, Angina, Arrythmias, CHF
190
Bisoprolol
Side effects
Bradycardia, Sexual Dysfunction
191
Carvedilol
Drug class
Non-selective β-antagonist (3rd generation "A")
192
Carvedilol
Mechanism
Antagonist: β1, β2
193
Carvedilol
Uses
CHF, HTN
194
Carvedilol
Side effects
Bradycardia, Fatigue
195
Labetalol
Drug class
Non-selective β-antagonist (3rd generation "A")
196
Labetalol
Mechanism
Antagonist: β1, β2
197
Labetalol
Uses
CHF, HTN
198
Labetalol
Side effects
Bradycardia, Fatigue
199
Betaxolol
Drug class
β1-selective antagonist (3rd generation "B")
200
Betaxolol
Mechanism
Antagonist: β1
201
Betaxolol
Uses
CHF, HTN
202
Betaxolol
Side effects
Bradycardia
203
Tyramine
Drug Class
Indirect acting agonist
| (adrenergic)
204
Tyramine
Mechanism
Increases cytoplasmic NE release
Tyramine is involved with an exchange transporter: tyramine goes in, NE comes out
205
Cocaine
Mechanism
Prevents NE reuptake
206
Cocaine
Therapeutics
Local anesthetic, vasoconstrictor
207
Cocaine
Side effects
Insomnia, anxiety, arrhythmias
208
Guanethidine
Drug class
Nerve ending blocker
209
Guanethidine
Mechanism
False neurotransmitter (vesicles become full of guanethidine rather than NE)
(Doesn't cross BBB)
210
Guanethidine
Uses
Antihypertensive
211
Guanethidine
Side effects
Many and serious
Not used much in US
212
Reserpine
Drug class
Nerve ending blocker
213
Reserpine
Mechanism
Release of empty vesicles (NE is not taken into vesicles b/c it binds uptake transporter and stops it)
214
Reserpine
Uses
Older antihypertensive
Cheap! (used abroad, not here)
215
Reserpine
Side effects
Many and serious (depression and suicide are major ones)
216
α-me-tyrosine
Drug class
Nerve ending blocker
217
α-me-tyrosine
Mechanism
Inhibit tyrosine hydroxylase (decreases NE synthesis)
218
α-me-tyrosine
Uses
Pheochromocytoma
219
α-me-tyrosine
Side effects
Many and serious
220
Ephedrine
Drug class
Mixed, direct (β2)/indirect agonist
221
Ephedrine
Uses
Nasal decongestion, anorexic
222
Hyperbaric oxygen
Uses
Prevents lipid peroxidation (?) and delayed neurologic sequelae in CO poisoning
223
Nitrites
Mechanism
* Turns RBC hemoglobin to methemoglobin; CN moves from Fe(3+) on cytochromes to those in RBCs creating cyanomethemoglobin
* Dangerous in concurrent CO poisoning
224
Sodium thiosulfate
Mechanism
Enhances normal metabolism of cyanide via rhodanase
225
Hydroxycobalamin
Mechanism
Binds with cyanide --\> cyanocobalamin (B12)
226
Hydroxycobalamin
Uses
* Smoke inhalation victims not improving with supportive care, cyanide exposure, nitroprusside at risk patients
* Give concurrently with sodium thiosulfate
227
Methylene Blue
Mechanism
Cofactor of NADPH reductase; gains electron, donates directly to reduce methemoglobin
228
Methylene Blue
Uses
Methemoglobinemia \>20-30%, or with symptoms
229
Methylene Blue
Side effects
* Hemolytic anemia (weak oxidizing capability)
* Painful at injection site, dyspnea, restlessness, tremor, precordial pain, and apprehension
230
Quinine
Drug Class
Quinolone derivitive
231
Quinine
Mechanism
Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases
232
Quinine
Uses
Prophylaxis, treatment of acute malarial attacks
(Also called quinidine (used in anti-arrhythmias))
233
Quinine
Side effects
Cinchonism, hypotension, hypoglycemia, abortion, arrhythmias
234
Chloroquine
Drug class
Quinolone derivitive
235
Chloroquine
Mechanism
Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases
236
Chloroquine
Uses
Prophylaxis, treatment of acute malarial attacks
237
Chloroquine
Side effects
Itching (Africans), retinitis (rare)
238
Hydroxychloroquine
Drug class
Quinolone derivitive
239
Hydroxychloroquine
Mechanism
Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases
240
Hydroxychloroquine
Uses
Prophylaxis, treatment of acute malarial attacks
241
Mefloquine
Drug class
Quinolone derivitive
242
Mefloquine
Mechanism
Accumulate in parasite’s food vacuole, disrupt heme polymerization to hemozoin, yielding oxidative damage to membranes and digestive proteases
243
Mefloquine
Uses
Prophylaxis, treatment of acute malarial attacks
244
Primaquine
Drug class
Quinolone derivitive
245
Primaquine
Mechanism
Forms quinolone-quinone intermediates that oxidize schizont membranes
(Only drug that inhibits exoerythrocytic schyzogony)
246
Primaquine
Uses
Prophylaxis, treatment of acute malarial attacks
247
Primaquine
Side effects
Hemolysis (G6PD), methemoglobinemia
Fever, nausea, vomiting
248
Amantadine
Mechanism
Positive charge helps chloroquine overcome chloroquine-resistant malaria vacuoles; point mutations against amantadine return bacteria to chloroquine-sensitivity
249
Artesunate
Drug class
Artemisinin compound
250
Artesunate
Mechanism
Specifically and selectively inhibit SERCA of P. falciparum
251
Artesunate
Side effects
Neurotoxicity, prolongation of QT interval
252
Artemether
Drug class
Artemisinin compound
253
Artemether
Mechanism
Specifically and selectively inhibit SERCA of P. falciparum
254
Lumefantrine
Drug class
Aminoalcohol
255
Lumefantrine
Uses
Used in combination w/artemether (called Coartem)
256
Atovoquone
Drug class
Napthalene
257
Atovoquone
Mechanism
Depolarizes parasitic mitochondria and inhibits their electron transport
258
Atovoquone
Uses
Used in combination w/proguanil
259
Chloroguanide aka proguanil
Drug class
Antifolates
260
Chloroguanide
Mechanism
Dihydrofolate reductase inhibitors (human and parasite pathway)
261
Tetracycline
Drug class
Antibiotic
262
Tetracycline
Uses
Severe malaria & chloroquine-resistant uncomplicated malaria
263
Clindamycin
Drug class
Antibiotic
264
Clindamycin
Uses
Severe malaria & chloroquine-resistant uncomplicated malaria
265
Doxycycline
Drug class
Antibiotic
266
Doxycycline
Uses
Severe malaria & chloroquine-resistant uncomplicated malaria
267
Doxycycline
Side effects
Photosensitivity
268
Aspirin
Drug class
Salicylate
269
Aspirin
Mechanism
Acetyl-salicylic acid irreversibly acetylates COX-1 and -2; metabolite (salicylic acid) reversibly inhibits COX-1 and -2
270
Aspirin
Uses
Antiplatelet, analgesic and antipyretic, and anti-inflammatory (in ascending order of amount taken); often taken as a "baby aspirin" to prevent MI, CVA
271
Aspirin
Side effects
GI irritation, bleeding and anemia, hepatotoxicity, and salicylate toxicity
Nephrotoxicity in elderly or hypovolemic patients; rare hypersensitivity reaction
272
Diflunisal
Drug class
Salicylate
273
Diflunisal
Mechanism
Difluorophenyl derivitive of salicylic acid, which reversibly inhibits COX-1 and -2
274
Diflunisal
Uses
Osteoarthritis, musculoskeletal strains/sprains, pain after dental extraction, and postepisiotomy pain
275
Diflunisal
Side effects
Fewer GI side effects and less effect on platelets than aspirin
276
Acetaminophen
Drug class
Para-amino phenol
277
Acetaminophen
Mechanism
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
Acetaminophen
Uses
Analgesic and antipyretic effect similar to aspirin, but weak anti-inflammatory effects
279
Acetaminophen
Side effects
Renal tubular necrosis if chronically abused with other NSAIDs; hepatic necrosis with overdose
GI irritation (less than aspirin)
280
Indomethacin
Drug class
Indole
281
Indomethacin
Mechanism
Reversibly inhibits COX-1 and -2 (favors COX-1)
282
Indomethacin
Uses
Rhematoid arthritis (10X as potent as aspirin), ankylosing spondylitis, osteoarthritis, acute gout
283
Indomethacin
Side effects
At times, thrombocytopenia, aplastic anemia, and severe frontal headaches
Nephrotoxicity in elderly or hypovolemic patients
284
Sulindac
Drug class
Indole
285
Sulindac
Mechanism
Reversibly inhibits COX-1 and -2 (favors COX-1)
286
Sulindac
Uses
Rhematoid arthritis, ankylosing spondylitis, osteoarthritis, acute gout
Half as potent as indomethacin; side effects less frequent
287
Sulindac
Side effects
At times, thrombocytopenia, aplastic anemia, and severe frontal headaches
Nephrotoxicity in elderly or hypovolemic patients
288
Ibuprofen
Drug class
Proprionic acid derivative
289
Ibuprofen
Mechanism
Reversibly inhibits COX-1 and -2 (favors COX-1)
290
Ibuprofen
Uses
Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries
291
Ibuprofen
Side effects
GI irritation; hepatotoxicity (less frequent than aspirin)
292
Flurbiprofen
Drug class
Proprionic acid dervitive
293
Flurbiprofen
Mechanism
Reversibly inhibits COX-1 and -2 (favors COX-1)
294
Flurbiprofen
Uses
Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries
Can be used topically (obtains high synovial concentration)
295
Flurbiprofen
Side effects
GI irritation; hepatotoxicity (less frequent than aspirin)
296
Naproxen
Drug class
Propionic acid derivative
297
Naproxen
Mechanism
Reversibly inhibits COX-1 and -2 (favors COX-1)
Longer half-life than most proprionic acid derivitives (13 hours vs. 1-2 hours)
298
Naproxen
Uses
Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries
299
Naproxen
Side effects
GI irritation; hepatotoxicity (less frequent than aspirin)
300
Oxaprozin
Drug class
Proprionic acid derivative
301
Oxaprozin
Mechanism
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
Oxaprozin
Uses
Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries
303
Piroxicam
Drug class
Enolic acid
304
Piroxicam
Mechanism
Reversibly inhibits COX-1 and -2 (favors COX-1)
Very long half-life (45 hours) permits single daily dose
305
Piroxicam
Uses
Long-term treatment of rheumatoid arthritis or osteoarthritis; also, ankylosing spondylitis, acute musculoskeletal disorders, acute gout
306
Piroxicam
Side effects
Same as aspirin:
GI irritation, bleeding and anemia, hepatotoxicity, and salicylate toxicity
Nephrotoxicity in elderly or hypovolemic patients; rare hypersensitivity reaction
307
Ketorolac
Drug action
Heteroaryl acetic acids
308
Keterolac
Mechanism
Reversibly inhibits COX-1 and -2 (favors COX-1)
Injectable (one of few NSAIDs available for this)
309
Keterolac
Uses
Post-operative pain; inflammatory eye conditions
310
Keterolac
Side effects
Same as aspirin; relatively nonirritating
311
Diclofenac
Drug class
Heteroaryl acetic acids
312
Diclofenac
Mechanism
Reversibly inhibits COX-1 and -2 (favors COX-1)
313
Diclofenac
Uses
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
Diclofenac
Side effects
G. I. irritation
315
Celocoxib
Drug class
COX-2 inhibitor
316
Celocoxib
Mechanism
Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site)
317
Celocoxib
Uses
Same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs
318
Celocoxib
Side effects
Less GI toxicity than traditional NSAIDs
Contraindicated in patients with heart problems/pregnancy
319
Etoricoxib
Drug class
COX-2 inhibitor
320
Etoricoxib
Mechanism
Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site)
321
Etoricoxib
Uses
Same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs
322
Etoricoxib
Side effects
Less GI toxicity than traditional NSAIDs
Contraindicated in patients with heart problems/pregnancy
323
Hydrocortisone
Drug class
Steroid
324
Hydrocortisone
Uses
Dermatitis, psoriasis
325
Hydrocortisone
Side effects
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
Cyclosporine
Drug class
Immunosuppressant
327
Cyclosporine
Uses
Inflammatory conditions (psoriasis)
328
Cyclosporine
Side effects
Raise blood pressure, damage kidneys if used long-term
329
Methotrexate
Drug class
Folate analog
330
Methotrexate
Mechanism
Inhibits DHFR
331
Methotrexate
Uses
Inflammatory conditions (psoriasis), conditions needing immunosuppression
332
Methotrexate
Side effects
* 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
Biologics
Mechanism
Block TNF-a
334
Biologics
Uses
Inflammatory conditions, arthritis
335
Biologics
Side effects
* Few (may unmask neurologic disease, latent infections (must do PPDs), malignancies)
* costly
336
UV light therapy
Class
UVA, UVB, UVC
337
UV Light Therapy
Mechanism
* Immunosuppression of T-cells via type I or type II reactions --\> mono- or bifunctional adducts in DNA
338
UV Light Therapy
Uses
* 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
UV Light Therapy
Side effects
Skin cancer, thinning/leathering of skin
340
Isotretinoin
Class
Retinoid
341
Isotretinoin
Mechanism
Stimulate epithelial cell turnover; also anti-inflammatory
342
Isotretinoin
Uses
* Acne
* Good as adjunct to other therapies
343
Isotretinoin
Side effects
Teratogenic effects (washes out in three weeks)
344
Acitretin
Class
Retinoid
345
Acitretin
Mechanism
Stimulate epithelial cell turnover; also anti-inflammatory
346
Acitretin
Uses
* Psoriasis
* Good as adjunct to other therapies
347
Acitretin
Side effects
Teratogenic effects (stays in fat stores for three years)
348
H1 receptor antagonist
Mechanism
* H1 receptor antagonist; rapidly absorbed orally, widely distributed, rapidly metabolized via liver microsomes
* Older agents cross CNS to cause central effects
349
H1 receptor antagonist
Uses
Allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids
350
H1 receptor antagonist
Side effects
Sedation, anti-muscarinic action, poisoning (especially children) with convulsions, allergy, local anesthesia
351
Diphenhydramine (Benadryl)
Drug Class
Ether/ethanolamine derivitive
352
Diphenhydramine (Benadryl)
Uses
Allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids
353
H1 receptor antagonist
Side effects
Anti-muscarinic, sedating
354
Tripenelennamine
Drug class
Ethylenediamine derivitive
355
Tripelennamine
Mechanism
H1 receptor antagonist
356
Tripelennamine
Uses
OTC sleep aid
357
Meclizine
Drug class
Piperazine derivative
358
Meclizine
Mechanism
H1 receptor antagonist
359
Meclizine
Uses
Motion sickness
360
Promethazine
Mechanism
H1 receptor antagonist
361
Promethazine
Uses
Antiemetic
362
Promethazine
Side effects
Anti-muscarinic, sedating
363
Chlorpheniramine
Mechanism
H1 receptor antagonist
364
Chlorpheniramine
Uses
Component of "cold" medications
365
Chlorpheniramine
Side effects
Less sedating
366
Loratadine
Mechanism
2nd generation H1 receptor antagonist
367
Loratadine
Uses
Allergic rhinitis
368
Loratadine
Side effects
* No sedation
* Cardiovascular effects (rare, with high doses)
* Poorly crosses BBB, so fewer central and side effects
369
Fexofenadine
Mechanism
2nd generation H1 receptor antagonist
370
Fexofenadine
Uses
Allergic rhinitis
371
Fexofenadine
Side effects
* No sedation
* Cardiovascular effects (rare, with high doses)
* Poorly crosses BBB, so fewer central and side effects
372
Azelastine
Mechanism
2nd generation H1 receptor antagonist
373
Azelastine
Uses
Allergic rhinitis (intranasal spray), allergic conjunctivitis (ophthalmic solution)
374
Azelastine
Side effects
* No sedation
* Poorly crosses BBB, so fewer central and side effects
375
Cetirazine
Mechanism
2nd generation H1 receptor antagonist
376
Cetirazine
Uses
Allergic rhinitis
377
Cetirazine
Side effects
* No sedation
* Poorly crosses BBB, so fewer central and side effects
378
Cimetidine
Mechanism
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
379
Cimetidine
Uses
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
380
Cimetidine
Side effects
Antiandrogen (causing impotence and gynecomastia), inhibition of P450 enzymes
CNS dysfunction possible
Most side effects of H2-blocker class
381
Ranitidine
Mechanism
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
382
Ranitidine
Uses
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
383
Ranitidine
Side effects
Liver toxicity
CNS dysfunction possible
384
Famotidine
Mechanism
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
385
Famotidine
Uses
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
386
Famotidine
Side effects
CNS dysfunction possible
387
Nizatidine
Mechanism
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
388
Nizatidine
Uses
Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
389
Nizatidine
Side effects
CNS dysfunction possible
Least side effects of H2-blocker class
390
Cyproheptidine
Mechanism
Antihistaminic and antiserotinergic
391
Cyproheptidine
Uses
Skin allergies (urticaria, anti-H1), diarrhea of carcinoid syndrome (anti-5HT2)
392
Cyproheptidine
Side effects
Sedation, antimuscarinic
393
Ketanserin
Mechanism
Selective 5HT2A,2C receptor antagonist, as well as α1 and H1 receptor antagonist
394
Ketanserin
Uses
Antihypertensive (relaxes vascular and tracheal smooth muscle), antiplatelet aggregation
395
Odansetron
Mechanism
5HT3 receptor antagonist
396
Odansetron
Side effects
Nausea and vomiting in chemotherapy
397
Ergot alkaloids
Mechanism
Agonist and antagonist actions at 5HT and α-adrenergic receptors
398
Ergot alkaloids
Side effects
Powerful hallucinations, smooth muscle contraction (vascular and uterine)
399
Ergotamine
Class
Ergot alkaloid
400
Ergotamine
Mechanism
Nonspecific partial agonist at all 5HT1,2 receptors; partial agonist at α-adrenergic receptors
401
Ergotamine
Uses
Prodrome of migraines
402
Ergotamine
Side effects
N/V, cumulative and prolonged vasoconstriction
403
Methyseride
Class
Ergot alkaloid
404
Methyseride
Mechanism
Partial agonist at all 5HT1 receptors, antagonist at 5HT2
405
Methyseride
Uses
Prophylaxis of migraines
406
Methyseride
Side effects
GI disturbances, inflammatory fibrosis (chronic use), hallucinations
Withdrawn from U.S. market
407
Ergonovine
Class
Ergot alkaloid
408
Ergonovine
Uses
Postpartum hemorrhage (Oxytocic)
409
Bromocriptine
Class
Ergot alkaloid
410
Bromocriptine
Mechanism
Dopamine agonist
411
Bromocriptine
Uses
Hyperprolactinemia
412
Triptan
Class
Non-ergot serotonin analogs
413
Triptan
Mechanism
5HT1B,D receptor agonist
414
Triptan
Side effects
Effective (70%) migraine treatment
415
Unfractionated heparin
Drug class
Indirect thrombin inhibitors
416
Unfractionated heparin
Mechanism
Bind antithrombin, potentiating formation of antithrombin-coagulation factor complex (Xa, IIa)
417
Unfractionated heparin
Uses
* Prevention and treatment of venous thromboembolism
* Given parenterally; monitored via PTT (want 2-2.5X normal value); reversed by protamine
418
Unfractionated heparin
Side effects
HIT, bleeding
Osteoporosis
419
Dalteparin
Drug class
Indirect thrombin inhibitors
420
Dalteparin
Mechanism
LMWH that inhibits thrombin less effectively than Xa
421
Dalteparin
Uses
* 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
Dalteparin
Side effects
Bleeding
423
Enoxaparin
Drug class
Indirect thrombin inhibitors
424
Enoxaparin
Mechanism
LMWH that inhibits thrombin less effectively than Xa
425
Enoxaparin
Uses
* 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
Enoxaparin
Side effects
HIT; bleeding;
osteoporosis and thrombocytopenia uncommon
427
Fondaparinux
Drug class
Indirect thrombin inhibitors
428
Fondaparinux
Mechanism
Synthetic polysaccharide that binds active site of antithrombin; inhibits Xa
Activates antithrombin, inhibits Xa
429
Fondaparinux
Uses
Given for HIT
430
Fondaparinux
Side effects
Bleeding
No antidote
431
Warfarin
Drug class
Vitamin K antagonist
432
Warfarin
Mechanism
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
Warfarin
Uses
Long term anticoagulation
434
Warfarin
Side effects
Thrombosis (protein C depression)
Bleeding
contraindicated in pregnancy (teratogen)
435
Bivalirudin
Drug class
Direct thrombin inhibitor
436
Bivalirudin
Mechanism
Inactivate fibrinogen-bound AND unbound thrombin; irreversible
Administered parenterally; monitored by PTT
437
Bivalirudin
Uses
Percutaneous coronary intervention (PCI)
438
Bivalirudin
Side effects
Bleeding
No antidote
439
Argatroban
Drug class
Direct thrombin inhibitor
440
Argatroban
Mechanism
Inactivate fibrinogen-bound AND unbound thrombin
441
Argatroban
Uses
Percutaneous coronary intervention (PCI); HIT
Administered parenterally; monitored by PTT;
442
Argatroban
Side effects
Bleeding
No antidote
443
Dabigatran
Drug class
Direct thrombin inhibitor
444
Dabigatran
Mechanism
Inactivate fibrinogen-bound AND unbound thrombin; competitive (reversible)
Oral
Renal fixed dose clearance
445
Dabigatran
Uses
DVT / PE; AFib
446
Dabigatran
Side effects
Bleeding
No antidote
447
Rivaroxaban
Drug class
Direct Xa inhibitor
448
Rivaroxaban
Mechanism
Reversible bind active site of Xa
Oral
Fixed renal clearance
449
Rivaroxaban
Uses
DVT / PE prophylaxis
450
Rivaroxaban
Side effects
Bleeding
No antidote
451
Apixaban
Drug class
Direct Xa inhibitor
452
Apixaban
Mechanism
Reversible bind active site of Xa
Oral
Fixed renal dose clearance
453
Apixaban
Uses
DVT / PE prophylaxis
454
Apixaban
Side effects
Bleeding
No antidote
455
Alteplase
Drug class
Fibrinolytic
456
Alteplase
Mechanism
Lyse already formed clots by activating plasminogen
457
Alteplase
Uses
STEMI; acute stroke; PE
458
Reteplase
Drug class
Fibrinolytic
459
Reteplase
Mechanism
Lyse already formed clots; less clot specific, more systemic activation
Short half life
460
Reteplase
Uses
STEMI
461
Reteplase
Side effects
Bleeding
Arrhythmia
462
Tenecteplase
Drug class
Fibrinolytic
463
Tenecteplase
Mechanism
Lyse already formed clots; more clot specific, less systemic activation
464
Tenecteplase
Uses
STEMI
465
Aspirin
Drug class (in clotting)
Antiplatelet
466
Aspirin
Mechanism (in clotting)
Irreversibly inhibits platelets, preventing thromboxane A2 formation
467
Aspirin
Uses (in clotting)
Often as "baby aspirin" to prevent and treat MI and stroke
468
Dipyridamole
Drug class
Antiplatelet
469
Dipyridamole
Mechanism
PDE inhibitor --\> increase in platelet cAMP--\> decrease aggregation
470
Dipyridamole
Uses
Weak antiplatelet effect
Given parenterally
471
Cilostazol
Drug class
Antiplatelet
472
Cilostazol
Mechanism
PDE inhibitor --\> increase in platelet cAMP--\> decrease aggregation
473
Cilostazol
Uses
Weak antiplatelet effect
474
Clopidogrel
Drug class
Antiplatelet
475
Clopidogrel
Mechanism
Inhibits platelet ADP receptors (P2Y12)
476
Clopidogrel
Uses
Prevent & treat ACS, stroke, peripheral vascular disease, angina, stent
477
Clopidogrel
Side effects
Bleeding; TTP (rare)
Reversed by platelet transfusion
478
Prasugrel
Drug class
Antiplatelet
479
Prasugrel
Mechanism
Inhibits platelet ADP receptors (P2Y12)
480
Prasugrel
Uses
Prevent & treat ACS, stroke, peripheral vascular disease, angina, stent
Can be used in patients with clopidogrel resistance
481
Prasugrel
Side effects
More bleeding and more potent than clopidogrel
482
Ticagrelor
Drug class
Antiplatelet
483
Ticagrelor
Mechanism
Allosteric reversible inhibitor of ADP Receptor (P2Y12)
484
Ticagrelor
Uses
ACS, PCI
485
Abciximab
Drug class
Antiplatelet
486
Abciximab
Mechanism
Monoclonal antibody against GP IIb/IIIa
Given parenterally
487
Abciximab
Side effects
May elicit immune response
488
Eptifibatide
Drug class
Antiplatelet
489
Eptifibatide
Mechanism
Fibrinogen analog which competes with endogenous fibrinogen for IIb/IIIa
Given parenterally
490
Eptifibatide
Side effects
Bleeding; ACS; PCI
Thrombocytopenia
491
Tirofiban
Drug class
antiplatelet
492
Tirofiban
Mechanism
Fibrinogen analog which competes with endogenous fibrinogen and vWF for IIb/IIIa
Given parenterally; immediate effect
493
Tirofiban
Side effects
Bleeding; NSTE-ACS
