FA General Pharmacology Flashcards
(188 cards)
1
Q
Cholinomimetic Agents
A
Direct: Bethanecol, Carbachol, Pilocarpine, Methacholine
Indirect: Neostigmine, Pyridostigmine, Physostigmine, Donepezil, Rivastigmine, Galantamine, Edrophonium
2
Q
Cholinomimetic Agent Toxicity
A
Watch for exacerbation of COPD, asthma, and peptic ulcers when given to susceptible patients
3
Q
Bethanecol Use
A
Postoperative ileus, neurogenic ileus, and urinary retention
4
Q
Bethanecol Mechanism
A
Activates bowel and bladder smooth muscle; resistant to AChE.
5
Q
Carbachol Use
A
Glaucoma, pupillary constriction, and relief of intraocular pressure
6
Q
Carbachol Mechanism
A
Carbon copy of acetylcholine
7
Q
Pilocarpine Use
A
Potent stimulator of sweat, tears, and saliva. Open-angle and closed-angle glaucoma.
8
Q
Pilocarpine Mechanism
A
Contracts ciliary muscle of eye (open-angle glaucoma), pupillary sphincter (closed-angle glaucoma); resistant to AChE.
9
Q
Methacholine Use
A
Challenge test for diagnosis of asthma
10
Q
Methacholine Mechanism
A
Stimulates muscarinic receptors in airway when
inhaled
11
Q
Neostigmine Use
A
Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative)
12
Q
Neostigmine Mechanism
A
↑ endogenous ACh.
Neo CNS = No CNS penetration.
13
Q
Pyridostigmine Use
A
Myasthenia gravis (long acting); does not penetrate CNS
14
Q
Pyridostigmine Mechanism
A
↑ endogenous ACh; ↑ strength. Pyridostigmine
gets rid of myasthenia gravis.
15
Q
Physostigmine Use
A
Anticholinergic toxicity (crosses blood-brain barrier → CNS)
16
Q
Physostigmine Mechanism
A
↑ endogenous ACh. Physostigmine “phyxes”
atropine overdose.
17
Q
Donepezil, Rivastigmine, Galantamine Use
A
Alzheimer disease
18
Q
Donepezil, Rivastigmine, Galantamine Mechanism
A
↑ endogenous ACh.
19
Q
Edrophonium Use
A
Historically, diagnosis of myasthenia gravis (extremely short acting). Myasthenia now diagnosed by anti-AChR Ab (antiacetylcholine receptor antibody) test.
20
Q
Edrophonium Mechanism
A
↑ endogenous ACh.
21
Q
Cholinesterase Inhibitor Poisoning
A
Often due to organophosphates, such as parathion, that irreversibly inhibit AChE.
Causes DUMBBELSS: Diarrhea, Urination, Miosis,
Bronchospasm, Bradycardia, Excitation
of skeletal muscle and CNS, Lacrimation,
Sweating, and Salivation.
Organophosphates are components of
insecticides; poisoning usually seen in farmers.
Antidote—atropine (competitive inhibitor) +
pralidoxime (regenerates AChE if given early).
22
Q
Muscarinic Antagonists
A
Atropine, Homatropine, Tropicamide, Benztropine, Scopolamine, Ipratropium, Tiotropium, Oxybutynin, Darifenacin, Solifenacin, Glycopyrrolate
23
Q
Eye Muscarinic Antagonists
A
Atropine, Homatropine, Tropicamide
24
Q
CNS Muscarinic Antagonists
A
Benztropine, Scopolamine
25
Respiratory Muscarinic Antagonists
Ipratropium, Tiotropium
26
Genitourinary Muscarinic Antagonists
Oxybutynin, Darifenacin, Solifenacin
27
Gastrointestinal/Respiratory Muscarinic Antagonist
Glycopyrrolate
28
Atropine, Homatropine, Tropicamide Use
Produce mydriasis and cycloplegia
29
Benztropine Use
Parkinson disease
30
Scopolamine Use
Motion sickness
31
Ipratropium, Tiotropium Use
COPD, asthma
32
Oxybutynin, Darifenacin, Solifenacin Use
Reduce urgency in mild cystitis and reduce bladder spasms. Other agents: tolterodine, fesoterodine, trospium.
33
Glycopyrrolate Use
Parenteral: preoperative use to reduce airway secretions.
Oral: drooling, peptic ulcer.
34
Atropine Mechanism
Muscarinic antagonist.
35
Atropine Use
Used to treat bradycardia and for ophthalmic applications. ↑ pupil dilation, cycloplegia, ↓ airway secretions, ↓ stomach acid secretion, ↓ gut motility, ↓ urinary urgency in cystitis
36
Atropine Toxicity
↑ body temperature (due to ↓ sweating); rapid pulse; dry mouth; dry, flushed skin; cycloplegia; constipation; disorientation Can cause acute angle-closure glaucoma in elderly (due to mydriasis), urinary retention in men with prostatic hyperplasia, and hyperthermia in infants
37
Sympathomimetics
Direct: Epinephrine, Norepinephrine, Isoproterenol, Dopamine, Dobutamine, Phenylephrine, Albuterol, Salmeterol, Terbutaline
Indirect: Amphetamine, Ephedrine, Cocaine
38
Epinephrine Mechanism
β > α
39
Epinephrine Use
Anaphylaxis, open angle glaucoma, asthma, hypotension; α effects predominate at high doses
40
Norepinephrine Mechanism
α1 > α2 > β1
Causes ↑ in systolic and diastolic pressures as a result of α1-mediated vasoconstriction → ↑ mean arterial pressure → bradycardia.
41
Norepinephrine Use
Hypotension (but ↓ renal perfusion)
42
Isoproterenol Mechanism
β1 = β2
Isoproterenol (no longer commonly used) has little a effect but causes β2-mediated vasodilation, resulting in ↓ mean arterial pressure and ↑ heart rate through β1 and reflex activity.
43
Isoproterenol Use
Electrophysiologic evaluation of tachyarrhythmias. Can worsen ischemia.
44
Dopamine Mechanism
D1 = D2 > β > α
45
Dopamine Use
Unstable bradycardia, heart failure, shock; inotropic and chronotropic α effects predominate at high doses
46
Dobutamine Mechanism
β1 > β2, α
47
Dobutamine Use
Heart failure (inotropic > chronotropic), cardiac stress testing
48
Phenylephrine Mechanism
α1 > α2
49
Phenylephrine Use
Hypotension (vasoconstrictor), ocular procedures (mydriatic), rhinitis (decongestant)
50
Albuterol, Salmeterol, Terbutaline Mechanism
β2 > β1
51
Albuterol, Salmeterol, Terbutaline Use
Albuterol for acute asthma; salmeterol for longterm asthma or COPD control; terbutaline to reduce premature uterine contractions
52
Amphetamine Mechanism
Indirect general agonist (sympathetic), reuptake inhibitor, also releases stored catecholamines
53
Amphetamine Use
Narcolepsy, obesity, attention deficit disorder
54
Ephedrine Mechanism
Indirect general agonist (sympathetics), releases stored catecholamines
55
Ephedrine Use
Nasal decongestion, urinary incontinence, hypotension
56
Cocaine Mechanism
Indirect general agonist (sympathetics), reuptake inhibitor
57
Cocaine Use
Causes vasoconstriction and local anesthesia;
never give β-blockers if cocaine intoxication is
suspected (can lead to unopposed α1 activation
and extreme hypertension)
58
Sympatholytics
Clonidine, α-methyldopa
59
Clonidine Use
```
Hypertensive urgency (limited situations); does not decrease renal blood flow.
ADHD, severe pain, and a variety of off-label indications (e.g. ethanol and opioid withdrawal)
```
60
Clonidine Toxicity
CNS depression, bradycardia, hypotension, respiratory depression, and small pupil size
61
α-methyldopa Use
Hypertension in pregnancy (safe in pregnancy)
62
α-methyldopa Toxicity
Direct Coombs positive hemolytic anemia, SLE-like syndrome
63
α-blockers
Non-selective: Phenoxybenzamine (irreversible), Phentolamine (reversible)
α1 selective: Prazosin, Terazosin, Doxazosin, Tamsulosin
α2 selective: Mirtazapine
64
Non-selective α-blockers
Phenoxybenzamine (irreversible), Phentolamine (reversible)
65
α1-blockers
Prazosin, Terazosin, Doxazosin, Tamsulosin
66
α2-blockers
Mirtazapine
67
Phenoxybenzamine Use
Pheochromocytoma (used preoperatively) to prevent catecholamine (hypertensive) crisis
68
Phenoxybenzamine Toxicity
Orthostatic hypotension, reflex tachycardia
69
Phentolamine Use
Give to patients on MAO inhibitors who eat tyramine-containing foods
70
α1-blocker Use
Urinary symptoms of BPH; PTSD (prazosin); hypertension (except tamsulosin)
71
α1-blocker Toxicity
1st-dose orthostatic hypotension, dizziness, headache
72
Mirtazapine Use
Depression
73
Mirtazapine Toxicity
Sedation, ↑ serum cholesterol, ↑ appetite
74
β-blockers
Metoprolol, acebutolol, betaxolol, carvedilol, esmolol, atenolol, nadolol, timolol, pindolol, labetalol
75
β-blocker Use
Angina Pectoris: ↓ heart rate and contractility, resulting in ↓ O2 consumption
MI: β-blockers (metoprolol, carvedilol, and bisoprolol) ↓ mortality
SVT (metoprolol, esmolol): ↓ AV conduction velocity (class II antiarrhythmic)
Hypertension: ↓ cardiac output, ↓ renin secretion (due to β1-receptor blockade on JGA cells)
CHF: Slows progression of chronic failure Glaucoma (timolol): ↓ secretion of aqueous humor
76
β-blocker Toxicity
Impotence, cardiovascular adverse effects (bradycardia, AV block, CHF), CNS adverse effects (seizures, sedation, sleep alterations), dyslipidemia (metoprolol), and asthmatics/ COPDers (may cause exacerbation).
Avoid in cocaine users due to risk of unopposed α-adrenergic receptor agonist activity.
Despite theoretical concern of masking hypoglycemia in diabetics, benefits likely outweigh risks; not contraindicated.
77
β1-selective antagonists (β1 > β2)
acebutolol (partial agonist), atenolol, betaxolol, esmolol, metoprolol
Selective antagonists mostly go from A to M (β1 with 1st half of alphabet)
78
Nonselective β-antagonists (β1 = β2)
nadolol, pindolol (partial agonist), propranolol, timolol
| Nonselective antagonists mostly go from N to Z (β2 with 2nd half of alphabet)
79
Nonselective α- and β-antagonists
carvedilol, labetalol
| Nonselective α- and β-antagonists have modified suffixes (instead of “-olol”)
80
Nebivolol Mechanism
Combines cardiac-selective
β1‑adrenergic blockade with stimulation
of β3‑receptors, which activate nitric oxide
synthase in the vasculature
81
Acetaminophen Antidote
N-acetylcysteine (replenishes glutathione)
82
AChE inhibitor, Organophosphate Antidote
Atropine followed by pralidoxime
83
Amphetamine (basic) Antidote
NH4Cl (acidify urine)
84
Antimuscarinic, Anticholinergic Antidote
Physostigmine salicylate, control hyperthermia
85
Benzodiazepine Antidote
Flumazenil
86
β-blocker Antidote
Glucagon
87
Carbon Monoxide Antidote
100% O2, hyperbaric O2
88
Copper, Arsenic, Gold Antidote
Penicillamine
89
Cyanide Antidote
Nitrite + thiosulfate, hydroxocobalamin
90
Digitalis Antidote
Anti-dig Fab fragments
91
Heparin Antidote
Protamine sulfate
92
Iron Antidote
Deferoxamine, deferasirox
93
Lead Antidote
EDTA, dimercaprol, succimer, penicillamine
94
Mercury, Arsenic, Gold Antidote
Dimercaprol (BAL), succimer
95
Methanol, Ethylene Glycol (Antifreeze) Antidote
Fomepizole > ethanol, dialysis
96
Methemoglobin Antidote
Methylene blue, vitamin C
97
Opioid Antidote
Naloxone
98
Salicylate Antidote
NaHCO3 (alkalinize urine), dialysis
99
TCA Antidote
NaHCO3 (plasma alkalinization)
100
tPA, streptokinase, urokinase Antidote
Aminocaproic acid
101
Warfarin Antidote
Vitamin K, plasma (if active bleeding)
102
Reaction Causes: Coronary Vasospasm
Cocain, Sumatriptan, Ergot Alkaloids
103
Reaction Causes: Cutaneous Flushing Cause
Vancomycin, Adenosine, Niacin, Ca2+ channel blockers
104
Reaction Causes: Dilated Cardiomyopathy Cause
Doxorubicin, Daunorubicin
105
Reaction Causes: Torsades de Pointes Causes
Class III (e.g., sotalol) and class IA (e.g., quinidine) antiarrhythmics, macrolide antibiotics, antipsychotics, TCAs
106
Reaction Causes: Adrenocortical Insufficiency
HPA suppression 2° to glucocorticoid withdrawal
107
Reaction Causes: Hot Flashes
Tamoxifen, clomiphene
108
Reaction Causes: Hyperglycemia
Tacrolimus, Protease inhibitors, Niacin, HCTZ, β-blockers, Corticosteroids
109
Reaction Causes: Hypothyroidism
Lithium, amiodarone, sulfonamides
110
Reaction Causes: Acute Cholestatic Hepatitis, Jaundice
Erythromycin
111
Reaction Causes: Diarrhea
Metformin, Erythromycin, Colchicine, Orlistat,
| Acarbose
112
Reaction Causes: Focal to Massive Hepatic Necrosis
Halothane, Amanita phalloides (death cap mushroom), Valproic acid, Acetaminophen
113
Reaction Causes: Hepatitis
INH
114
Reaction Causes: Pancreatitis
Didanosine, Corticosteroids, Alcohol, Valproic acid, Azathioprine, Diuretics (furosemide, HCTZ)
115
Reaction Causes: Pseudomembranous Colitis
Clindamycin, ampicillin, cephalosporins
| Antibiotics predispose to superinfection by resistant C. difficile
116
Reaction Causes: Agranulocytosis
Dapsone, Clozapine, Carbamazepine, Colchicine, Methimazole, Propylthiouracil
117
Reaction Causes: Aplastic Anemia
Carbamazepine, Methimazole, NSAIDs, Benzene, Chloramphenicol, Propylthiouracil
118
Reaction Causes: Direct Coombs-Positive Hemolytic Anemia
Methyldopa, penicillin
119
Reaction Causes: Gray Baby Syndrome
Chloramphenicol
120
Reaction Causes: Hemolysis in G6PD Deficiency
INH, Sulfonamides, Dapsone, Primaquine, Aspirin, Ibuprofen, Nitrofurantoin
121
Reaction Causes: Megaloblastic Anemia
Phenytoin, Methotrexate, Sulfa drugs
122
Reaction Causes: Thrombocytopenia
Heparin, cimetidine
123
Reaction Causes: Thrombotic Complications
OCPs (e.g., estrogens)
124
Reaction Causes: Fat redistribution
Protease inhibitors, Glucocorticoids
125
Reaction Causes: Gingival Hyperplasia
Phenytoin, verapamil, cyclosporine, nifedipine
126
Reaction Causes: Hyperuricemia (Gout)
Pyrazinamide, Thiazides, Furosemide, Niacin, Cyclosporine
127
Reaction Causes: Myopathy
Fibrates, niacin, colchicine, hydroxychloroquine, interferon-α, penicillamine, statins, glucocorticoids
128
Reaction Causes: Osteoporosis
Corticosteroids, heparin
129
Reaction Causes: Photosensitivity
Sulfonamides, Amiodarone, Tetracyclines, 5-FU
130
Reaction Causes: Rash (Stevens-Johnson Syndrome)
Anti-epileptic drugs (ethosuximide, carbamazepine, lamotrigine, phenytoin, phenobarbital), Allopurinol, Sulfa drugs, Penicillin
131
Reaction Causes: SLE-like Syndrome
Sulfa drugs, Hydralazine, INH, Procainamide, Phenytoin, Etanercept
132
Reaction Causes: Teeth Discoloration
Tetracyclines
133
Reaction Causes: Tendonitis, Tendon Rupture, and Cartilage Damage
Fluoroquinolones
134
Reaction Causes: Cinchonism
Quinidine, quinine
135
Reaction Causes: Parkinson-like Syndrome
Antipsychotics, Reserpine, Metoclopramide
136
Reaction Causes: Seizures
INH (vitamin B6 deficiency), Bupropion, Imipenem/cilastatin, Tramadol, Enflurane, Metoclopramide
137
Reaction Causes: Tardive Dyskinesia
Antipsychotics, metoclopramide
138
Reaction Causes: Diabetes Insipidus
Lithium, demeclocycline
139
Reaction Causes: Fanconi Syndrome
Expired tetracycline
140
Reaction Causes: Hemorrhagic Cystitis
Cyclophosphamide, ifosfamide
| Prevent by coadministering with mesna
141
Reaction Causes: Interstitial Nephritis
Methicillin, NSAIDs, furosemide
142
Reaction Causes: SIADH
Carbamazepine, Cyclophosphamide, SSRIs
143
Reaction Causes: Dry Cough
ACE inhibitors
144
Reaction Causes: Pulmonary Fibrosis
Bleomycin, Amiodarone, Busulfan, Methotrexate
145
Reaction Causes: Antimuscarinic
Atropine, TCAs, H1-blockers, antipsychotics
146
Reaction Causes: Disulfiram-like Reaction
Metronidazole, certain cephalosporins, griseofulvin, procarbazine, 1st-generation sulfonylureas
147
Reaction Causes: Nephrotoxicity/Ototoxicity
Aminoglycosides, vancomycin, loop diuretics, cisplatin
148
Cytochrome P-450 Inducers (+)
Chronic alcohol use, Modafinil, St. John’s wort, Phenytoin, Phenobarbital, Nevirapine, Rifampin, Griseofulvin, Carbamazepine
149
Cytochrome P-450 Substrates
Anti-epileptics, Antidepressants, Antipsychotics, Anesthetics, Theophylline, Warfarin, Statins, OCPs
150
Cytochrome P-450 Inhibitors (-)
Acute alcohol abuse, Gemfibrozil, Ciprofloxacin, Isoniazid, Grapefruit juice, Quinidine, Amiodarone, Ketoconazole, Macrolides, Sulfonamides, Cimetidine, Ritonavir
151
Sulfa Drugs
Probenecid, Furosemide, Acetazolamide, Celecoxib, Thiazides, Sulfonamide antibiotics, Sulfasalazine
Patients with sulfa allergies may develop fever, urinary tract infection, Stevens-Johnson syndrome, hemolytic anemia, thrombocytopenia, agranulocytosis, and urticaria (hives). Symptoms range from mild to life threatening.
152
Drug Names: -azole
Ergosterol synthesis inhibitor
| Ketoconazole
153
Drug Names: -bendazole
Antiparasitic/antihelmintic
| Mebendazole
154
Drug Names: -cillin
Peptidoglycan synthesis inhibitor
| Ampicillin
155
Drug Names: -cycline
Protein synthesis inhibitor
| Tetracycline
156
Drug Names: -ivir
Neuraminidase inhibitor
| Oseltamivir
157
Drug Names: -navir
Protease inhibitor
| Ritonavir
158
Drug Names: -ovir
DNA polymerase inhibitor
| Acyclovir
159
Drug Names: -thromycin
Macrolide antibiotic
| Azithromycin
160
Drug Names: -ane
Inhalational general anesthetic
| Halothane
161
Drug Names: -azine
Typical antipsychotic
| Thioridazine
162
Drug Names: -barbital
Barbiturate
| Phenobarbital
163
Drug Names: -caine
Local anesthetic
| Lidocaine
164
Drug Names: -etine
SSRI
| Fluoxetine
165
Drug Names: -ipramine
TCA
| Imipramine
166
Drug Names: -triptan
5-HT1B/1D agonists
| Sumatriptan
167
Drug Names: -triptyline
TCA
| Amitriptyline
168
Drug Names: -zepam
Benzodiazepine
| Diazepam
169
Drug Names: -zolam
Benzodiazepine
| Alprazolam
170
Drug Names: -chol
Cholinergic agonist
| Bethanechol/carbachol
171
Drug Names: -curium or -curonium
Non-depolarizing paralytic
| Atracurium or vecuronium
172
Drug Names: -olol
β-blocker
| Propranolol
173
Drug Names: -stigmine
AChE inhibitor
| Neostigmine
174
Drug Names: -terol
β2-agonist
| Albuterol
175
Drug Names: -zosin
α1-antagonist
| Prazosin
176
Drug Names: -afil
PDE-5 inhibitor
| Sildenafil
177
Drug Names: -dipine
Dihydropyridine CCB
| Amlodipine
178
Drug Names: -pril
ACE inhibitor
| Captopril
179
Drug Names: -sartan
Angiotensin-II receptor blocker
| Losartan
180
Drug Names: -statin
HMG-CoA reductase inhibitor
| Atorvastatin
181
Drug Names: -dronate
Bisphosphonate
| Alendronate
182
Drug Names: -glitazone
PPAR-γ activator
| Rosiglitazone
183
Drug Names: -prazole
Proton pump inhibitor
| Omeprazole
184
Drug Names: -prost
Prostaglandin analog
| Latanoprost
185
Drug Names: -tidine
H2-antagonist
| Cimetidine
186
Drug Names: -tropin
Pituitary hormone
| Somatotropin
187
Drug Names: -ximab
Chimeric monoclonal Ab
| Basiliximab
188
Drug Names: -zumab
Humanized monoclonal Ab
| Daclizumab
