Systems Drugs Flashcards
1
Q
Mech of cyclosporine
A
Binds Cyclophilin –> Complex inhibits calcineurin –> prevents IL-2 transcription
2
Q
Uses of cyclosporine
A
Transplant rejection prophylaxis
Psoriasis
Rheumatoid arthritis
3
Q
Cyclosporine toxicity
A
Nephrotoxicity HTN, Hyperlipidemia Neurotoxicity Gingival hyperplasia Hirsutism
4
Q
Mech of Tacrolimus
A
Binds FK506BP –> complex inhibits calcineurin –> Prevents IL-2 transcription
5
Q
uses of Tacrolimus
A
Transplant rejection prophylaxis.
6
Q
Tacrolimus toxicity
A
Similar to cyclosporine
Increased risk of diabetes and neurotoxicity
No gingival hyperplasia or hirsutism.
7
Q
Sirolimus mechanism
A
Binds FKBP-12 –> complex inhibits mTOR –> prevents T-cell response to IL-2
8
Q
Sirolimus uses
A
Kidney transplant rejection prophylaxis.
9
Q
Sirolimus toxicity
A
Anemia thrombocytopenia leukopenia insulin resistance hyperlipidemia
non-nephrotoxic.
10
Q
Daclizumab / Basiliximab mechanism
A
Monoclonal antibody; blocks IL-2R.
11
Q
Daclizumab / Basiliximab uses
A
Kidney transplant rejection prophylaxis.
12
Q
Daclizumab / Basiliximab toxicity
A
Edema, hypertension, tremor.
13
Q
Azothioprine mechanism
A
Antimetabolite precursor of 6-mercaptopurine.
Inhibits lymphocyte proliferation by blocking nucleotide synthesis.
14
Q
Azothioprine uses
A
Transplant rejection prophylaxis rheumatoid arthritis Crohn disease glomerulonephritis other autoimmune conditions.
15
Q
Azothioprine toxicity
A
Leukopenia, anemia, thrombocytopenia.
Degraded by Xanthine Oxidase - don’t give with allopurinol
16
Q
Mycophenolate mechanism
A
Inhibits IMP dehydrogenase - decreased synthesis of guanine
Inhibits rapid proliferation of B and T cells
17
Q
Mycophenolate toxicity
A
Hyperglycemia
hyperlipidemia
Increased risk of lymphoma and infections
18
Q
Thalidomide mechanims
A
Suppresses TNF alpha production
Increases NK cells and IL-2
19
Q
Thalidomide uses
A
Erythema nodosum leprosum (Hansen Disease)
Multiple myeloma
20
Q
Thalidomide toxicity
A
Terratogen
21
Q
Aldesleukin (IL-2) use
A
Renal cell carcinoma
Metastatic melanoma
22
Q
Epoetin alfa (erythropoietin) use
A
Anemias (especially in renal failure)
23
Q
Thrombopoietin
A
Thrombocytopenia
24
Q
Oprelvekin (interleukin-11)
A
Thrombocytopenia
25
Filgrastim (G-CSF)
Recovery of bone marrow
26
Sargramostim (GM-CSF)
Recovery of bone marrow
27
INF-Alpha use
Chronic Hep B and C
Kaposi Sarcoma
Malignant melanoma
Hairy cell leukemia
28
IFN beta use
Multiple sclerosis
29
IFN gamma use
Chronic granulomatous disease
30
Romiplostim, eltrombopag use
Thrombocytopenia
31
Alemtuzumab target and use
CD52 --> CLL
32
Bevacizumab target and use
VEGF --> Colorectal cancer, renal carcinoma
33
Cetuximab target and use
EGFR --> Stage 4 colorectal cancer / head and neck cancer
34
Rituximab target and use
CD 20
B-cell non-hodgkin lymphoma
CLL
Rheumatoid arthritis
Immune thrombocytopenic purpura
35
Trastuzumab target and use
HER2/neu --> Breast cancer
36
Adalimumab / infliximab target and use
Soluble TNF alpha receptor
IBD
rheumatoid arthritis
ankylosing spondylitis
psoriasis
37
Eculizumab target and use
complement protein C5
Paroxysmal nocturnal hemoglobinuria
38
Natalizumab target and use
alpha4-integrin
Multiple sclerosis
Crohn disease
39
Abciximab target and use
platelet glycoproteins IIb/IIIa
prevention of ischemic complications in patients undergoing PCI
40
Denosumab target and use
RANKL
Osteoporosis
Inhibits osteoclast maturation
41
Digoxin immune Fab target and use
Antidote for digoxin toxicitiy
42
Omalizumab target and use
IgE
allergic asthma; prevents IgE binding to FceR1
43
Palivizumab target and use
RSV F-protein
RSV prophylaxis for high risk infants
44
Ranibizumab, bevacizumab target and use
VEGF
Neovascular age-related macular degernation
45
HMG-CoA reductase inhibitor mechanism
Inhibits HMG-CoA --> mevalonate
Decreases mortality in CAD patients
46
HMG-CoA reductase uses
Lower LDL a lot
| Increased HDL
47
HMG-CoA reductase toxicities
Hepatotoxicity (Increased LFT)
| Myopathy (esp when used with fibrates or niacin)
48
Cholestyramine, Colestipol, Colesevelam mechanism
Prevents intestinal reabsorption of bile acids
49
Cholestyramine, Colestipol, Colesevelam use
Lower LDL
50
Cholestyramine, Colestipol, Colesevelam tox
GI upset
| Decreased absorption of other drugs and ADEK
51
Ezetimibe mechanism
Decreases cholesterol absorption at brush border
52
Ezetimibe uses
Lower LDL
53
Ezetimibe tox
Diarrhea
| Rare LFT rise
54
Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate mechanism
Upregulates LPL to increase TG clearance
Activated PPAR alpha to induce HDL synth
55
Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate uses
Lower TAGs
56
Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate toxicity
myopathy (increased with statin use)
| cholesterol gallstones
57
Niacin mechanism
Inhibits lipolysis
| reduces VLDL synthesis
58
Niacin uses
lower LDL
| Higher HDL
59
Niacin toxicity
Red, flushing of face (prevent with NSAID)
Hyperglycemia
Hyperuricemia
60
Opioid (Morphine, fentanyl, loperamide, methadone, meperidine, dextromethorphan, diphenoxylate, pentazocine) mechanism
Agonist at mu receptor - opens K+ channel, closes Ca2+ channel
Inhibits release of Ach, NE, 5-HT, glutamate, substance P
61
Dextromethorphan use
cough suppression
62
Loperamide, diphenoxylate use
Diarrhea
63
Maintenance for heroin addiction
Methadone
Buprenorphine + naloxone
64
Toxicity of opioids
```
Addiction
Respiratory depression
miosis (cannot build tolerance)
constipation (cannot build tolerance)
CNS depression
```
65
Pentazocine mechanism
(Opioid) partial agonist at mu receptor + weak antagonist at mu receptor
Opioid designed to minimize addictive capacity
Can precipitate withdrawl symptoms in addicts
66
Halothane, isoflurane, sevoflurane, N2O mechanism
unknown
67
Halothane, isoflurane, sevoflurane, N2O effects
Myocardial depression
Resp depression
Nausea/emesis
Increased cerebral blood flow (decreased metabolic demand)
68
Halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, N2O toxicity
Hepatotoxicity (Halothane)
nephrotoxicity (methoxyflurane)
Pro-convulsant (Enflurane)
Expansion of trapped gas in body cavity (N2O)
Malignant hyperthermia (all but N2O)
69
Barbiturates mechanism
Increases duration of Cl- channel opening in GABA neurons
70
Barbiturate uses
Induction of anesthesia and short surgical procedures
Sedative for anxiety
seizures
insomnia
71
How is barbiturate effect terminated?
Rapid redistribution into tissue (skel muscle and fat)
72
Benzodiazapine mechanism
Increases the frequency of Cl- channel opening in GABA neurons
73
Short acting benzos
Diazepam
Lorazepam
Alprozolam
Midazolam
74
Long acting benzos
Timazepan
| Chlordiazepoxide (alcohol withdrawl)
75
Benzodiazapine toxicity
```
severe post op resp depression
Decreased BP (treat with flumazenil)
anterograde amnesia
Dependence
CNS depression
```
76
Ketamine mechanism
PCP analog --> Blocks NMDA receptors
77
Ketamine toxicity
Disorientation
hallucination
bad dreams
Increased cerebral blood flow
78
Propofol mechanism
Potentiates GABA
79
Propofol use
IV induction agent
sedation in ICU
rapid anesthesia induction
Short procedures
80
How are the effects of propofol terminated?
Rapid redistribution to the rest of the body (15 min)
metabolized by liver
81
Tramadol use
non-addictive analgesic
| Chronic pain
82
Barbiturate toxicity
Resp and cardio depression (fatal)
CNS depression
dependence
CYP450 inducer
83
Benzodiazapine use
```
Anxiety
spasticity
status epilepticus (lorazepam diazepam)
Delirium tremens (EtOH withdrawl)
night terrors / sleep walking
general anesthetic
```
84
Zolpidem, Zaleplon, Eszopiclone mechanism
Non-benzo hypnotics
Act via BZ1 subtype of GABA receptor (binds GABA but not where benzo's attach)
Short duration because of rapid metabolism by liver enzymes
85
Zolpidem, Zaleplon, Eszopiclone use
Insomnia
86
Zolpidem, Zaleplon, Eszopiclone toxicity
```
Ataia
headache
confusion
Modest day after psychomotor depression
slight amnesia
```
87
Memantine mechanism
NMDA receptor antagonist - prevents excitotoxicity
88
Memantine use
Alzheimer's Dementia
89
Memantine side effects
Dizziness, confusion, hallucination
90
Butorphanol mechanism
kappa opioid agonist and mu opioid partial agonist
analgesia
91
Butorphanol uses
Severe pain (migrane / labor)
92
Butorphanol toxicity
Opioid withdrawl symptoms if patient is also taking full opioid agonist
OD not easily reversed with naloxone.
Less respiratory depression than full opioid
93
Tramadol mechanism
Weak opioid agonist
| Inhibits 5-HT and NE reuptake
94
Tramadol toxicity
Similar to opioids
Decreases seizure threshold
Serotonin syndrome
95
Ethosuximide mech
blocks thalamic T-type Ca channels
96
Ethosuximide uses
Absence seizures
97
Ethosuximide toxicity
GI, fatigue, headache, urticaria, Steven-Johnson syndrome.
EFGHIJ—Ethosuximide causes Fatigue, GI distress, Headache, Itching, and Stevens-Johnson syndrome
98
Phenytoin mech
Increases Na+ channel inactivation; zero-order kinetics
99
Phenytoin uses
Simple seizures
Complex seizures
Tonic-clonic seizures
Status epilepticus
100
Phenytoin toxicity
```
Nystagmus
diplopia
ataxia
sedation
gingival hyperplasia
hirsutism
peripheral neuropathy
megaloblastic anemia
teratogenesis (fetal hydantoin syndrome)
SLE-like syndrome
induction of cytochrome P-450
lymphadenopathy
Stevens- Johnson syndrome
osteopenia
```
101
Carbamazepine mech
Increase Na+ channel inactivation
102
Carbamazepine use
Simple
Complex
Tonic-clonic
103
Carbamazepine toxicity
Diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenesis, induction of cytochrome P-450, SIADH, Stevens-Johnson syndrome
104
Valproic acid mech
Na+ channel inactivation, GABA concentration by inhibiting GABA transaminase
105
Valproic acid use
Simple
Complex
Tonic-clonic*
Absence seizures
106
Valproic acid toxicity
GI, distress, rare but fatal hepatotoxicity (measure LFTs), neural tube defects in fetus (spina bifida), tremor, weight gain, contraindicated in pregnancy
107
Gabapentin mech
Primarily inhibits high- voltage-activated Ca2+ channels; designed as GABA analog
108
Gabapentin use
Simple
Complex
Tonic-clonic
109
Gabapentin toxicity
Sedation, ataxia
110
Topiramate mech
Blocks Na+ channels, Increases GABA action
111
Topiramate use
Simple
Complex
Tonic-clonic
112
Topiramate toxicity
Sedation, mental dulling, kidney stones, weight loss
113
Lamotrigine mech
Blocks voltage-gated Na+ channels
114
Lamotrigine use
Simple
Complex
Tonic-clonic
Absence seizure
115
Lamotrigine toxicity
Stevens-Johnson syndrome (must be titrated slowly)
116
Levetiracetam mech
Unknown; may modulate GABA and glutamate release
117
Levetiracetam use
Simple
Complex
Tonic-clonic
118
Tiagabine mech
Increase GABA by inhibiting re-uptake
119
Tiagabine use
Simple and complex seizures
120
Vigabatrin mech
Increase GABA by irreversibly inhibiting GABA transaminase
121
Vigabatrin use
Simple and complex seizures
122
What are the local anesthetics?
Esters - Procaine, cocaine, tetracaine
Amides - Lidocaine, mepivicaine, bupivicaine
123
Local anesthetic mech
Block Na+ channels by binding to specific receptors on inner portion of channel.
Preferentially bind to activated Na+ channels, so most effective in rapidly firing neurons
124
Order of nerve blockade with local anesthetics
Small-diameter fibers > large diameter.
Myelinated fibers > unmyelinated fibers.
Overall, size factor predominates over myelination such that:
Small myelinated fibers > small unmyelinated fibers > large myelinated fibers > large unmyelinated fibers.
125
Bupivicaine toxicity
severe cardiovascular toxicity
126
Local anesthetic toxicity
CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, hypotension, and arrhythmias (cocaine).
127
Succinylcholine mech
Depolarizing NMJ blocker
Strong ACh receptor agonist; produces sustained depolarization and prevents muscle contraction.
128
Succinylcholine toxicity
Hypercalcemia, hyperkalemia, and malignant hyperthermia.
129
Tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium mechanism
Non-depolarizing NMJ blocker
Competitive antagonists—compete with ACh for receptors.
130
Dantrolene mechanism
Prevents the release of Ca2+ from the sarcoplasmic reticulum of skeletal muscle.
131
Baclofen mech
inhibits GABA(B) receptors at spinal cord level inducing skeletal muscle relaxation
132
Baclofen use
muscle spams (acute low back pain)
133
Cyclobenzaprine mech
Centrally acting skeletal muscle relaxant. Structurally related to TCA's and similar anti-cholinergic side effects
134
Cyclobenzaprine use
muscle spasm
135
Bromocriptine mech
Ergot - Dopamine agonist (peripheral vasoconstrictor)
136
Bromocriptine use
Parkinsons
137
Pramipexol and ropinerole mech
Non-ergot Dopamine agonist
138
Pramipexol and ropinerole use
Parkinsons
139
Amantadine mech
Increase dopamine release
140
Amantadine use
Parkinsons
141
Levodopa + carbidopa mech
Levodopa - just L-DOPA the precursor to dopamine
Carbidopa - inhibits DOPA decarboxylase therby inhibiting peripheral conversion of L-DOPA to dopamine (L-Dopa better crosses BBB)
142
Entacapone and Tolcapone mech
prevents peripheral L-DOPA degradation by inhibiting COMT
143
Selegiline mech
blocks conversion of dopamine into 3-MT by selectively inhibiting MAO-B
144
Selegiline toxicity
enhances adverse effects of L-dopa
145
Levodopa/carbidopa toxicity
Arrhythmias from increased peripheral formation of catecholamines
Long-term use = Dyskinesia following administration, akinesia between doses
("on-off phenomenon")
146
Tetrabenazine and Reserpine mech
inhibit vesicular monoamine transporter limiting dopamine vesicle packaging and release
147
Tetrabenazine and Reserpine use
Huntington Disease
148
Haloperidol mech
D2 receptor antagnoist
149
Haloperidol use
Huntingtons Disease
150
Sumatriptan mech
5-HT1B/1D agonist.
Inhibits trigeminal nerve activation
prevents vasoactive peptide release
induces vasoconstriction
Half-life
151
Sumatriptan use
acute migrane, cluster headache attacks
152
Sumatriptan toxicity
Coronary vasospasm (contraindicated in patients with CAD or Prinzmetal angina), mild tingling.
153
Drugs safe to use in pregnancy
"Hypertensive Moms Love Nifedipine"
Hydralazine
Methyldopa
Labetolol
Nifidepine
154
Penicillin Mech
Binds Penicillin binding protein (transpeptidases)
Block transpeptidase (cross-linking of peptidoglycan cell wall)
Activate autolytic enzymes
155
Penicillin use
Mostly for Gram pos (S. pneumoniae, S. pyogenes, Actinomyces)
N. meningitidis and T. pallidum
Bactericidal for gram-positive cocci, gram-positive rods, gram-negative cocci, and spirochetes.
156
Penicillin toxicity
Hypersensitivity reaction
Hemolytic anemia
157
Penicillin resistance mech
penicillinase in bacteria cleaves B-lactam ring
158
Ampicillin, amoxicillin (aminopenicillins) mech
Binds Penicillin binding protein (transpeptidases)
Block transpeptidase (cross-linking of peptidoglycan cell wall)
Wider spectrum
159
Name the B-lactamase inhibitors
Clavulanic acid
Sulbactam
Tazobactam
160
Which aminopenicillin has great oral bioavailability?
Amoxicillin > Ampicillin
161
Ampicillin, amoxicillin (aminopenicillins) use
HELPSS
```
Haemophilus influenzae
E. coli
Listeria monocytogenes
Proteus mirabilis
Salmonella
Shigella
enterococci
```
Often used in UTI's (not first line)
Neonatal infections --> E. Coli / Listeria
162
Ampicillin, amoxicillin (aminopenicillins) toxicity
Hypersensitivity
Rash --> when given for empiric treatment of EBV mono
Pseudomembranous collitis
163
Dicloxacillin, nafcillin, oxacillin mech
Same as penicillin (narrow spectrum)
Penicillin resistant because of bulky R group
164
Dicloxacillin, nafcillin, oxacillin use
S. Aureus (except for MRSA)
165
Dicloxacillin, nafcillin, oxacillin tox
Hypersensitivity reaction
| Interstitial nephritis
166
Piperacillin, ticaracillin mech
Same as penicillin
Anti-pseudomonals
Psedomonas
Gram negative rods
Give with B-lactamase inhibitors
167
Cephalosporin mech
B-lactam drugs that inhibit cell wall synthesis
Binds PBP's
Inhibits peptidoglycan synthesis
Less susceptible to penicillinases
Bactericidal
168
Which organisms are generally not covered by cephalosporins?
LAME
Listeria
Atypicals (Chlamydia, Mycoplasma)
MRSA
Enterococci
169
1st generation cephalosporins and uses
Cefazolin
Cephalexin
Gram positive cocci
PEcK
Proteus mirabilis
E. Coli
Klebsiella
170
Cefazolin use
1st generation cephalosporin
| Prior to surgery to prevent S. Aureus wound infections
171
2nd generation cephalosporins and uses
Cefoxitin
Cefaclor
Cefuroxime
Gram positive cocci
HENS PEcK
H. Influenzae
Enterobacte aerogenes
Neisseria spp.
Serratia marcescens
Proteus Mirabilis
E. Coli
Klebsiella
172
3rd generation cephalosporins and uses
Ceftriaxone --> meningitis, gonorrhea, Lyme
Cefotaxime
Ceftazidime --> Pseudomonas
Cefdinir --> resistant otitis media
Serious gram negative infections resistant to other B-lactams
Still covers S. Pneumo but has lost most other gram + coverage
173
4th generation cephalosporin and uses
Cefepime
Big gun broad spectrum
Gram - organisms
Gram + organisms
Increased activity against Pseudomonas
174
5th generation cephalosporin and uses
Broad spectrum gram + and gram - organisms
Covers MRSA
Does not cover pseudomonas
175
Cephalosporin toxicity
Hypersensitivity reactions
autoimmune hemolytic anemia
Disulfram-like reaction with EtOH
vitamin K deficiency
Cross reactivity with penicillin
176
What happens when you give a cephalosporin with an aminoglycoside?
Ceph increases the nephrotoxicity of aminoglycoside
177
Mech of resistance against cephalosporins
Structural changes to the penicillin binding proteins (transpeptidase)
178
Carbepenems names and mech
Imipenem, meropenem, Ertapenem, Doripenem
Broad spectrum, B-lactamase resistant, cell wall inhibitor
179
What is a carbepenem always administered with and why?
Cilastin because it inhibits renal inactivation of drug in the renal tubules
Renal dihydropeptidase I
180
Carbepenem use
Empiric treatment of life threatening disease
Gram + cocci
Gram - rods
anaerobes
181
Carbepenem tox
GI distress
skin rash
CNS tox (seizures) at high levels
182
Meropenem has which added advantage against other carbepenems?
Less seizure risk
| stable against dehydropeptidase I in kidneys
183
Aztreonam mech
Prevents peptidoglycan cross-linking by binding PBP3 (Penicillin binding protein 3)
Synergistic with aminoglycosides
184
Can you use aztreonam in a patient allergic to penicillin?
yes - no cross reactivity
185
Aztreonam use
Gram - rods only
For those who cannot tolerate aminoglycosides because of renal insufficiency
186
Aztreonam toxicities
usually nontoxic
| some GI upset
187
Vanco mechanism
Binds D-ala D-ala portion of cell wall precursor
Bactericidal
188
Vanco use
```
Gram + bugs only -->serious MDR organisms
MRSA
S. Epidermidis
Enterococcus spp.
C. Diff (oral dose)
```
189
Vanco tox
NOT trouble free
Nephrotoxicity
Ototoxicity
Thrombophlebitis
Red man syndrome --> diffuse flushing
190
What do you do if a patient gets red man syndrome from vanco use?
Withdraw drug
pre-treat with anti-histamines
slow the infusion rate
191
Mech of resistance against vanco
Amino acid modification D-ala D-ala changed to D-ala D-lac
192
What drug classes are used to treat primary (essential) HTN?
Thiazide
ACE I
ARBs
Dihydropyridine CCB
193
What drug classes are used to treat HTN with heart failure
Diuretics
ACEI / ARB
B-blockers in compensated HF
Aldosterone antagonists
194
What drug classes are used to treat HTN with diabetes mellitus
ACEI / ARB (protective against diabetic nephropathy)
CCB
Thiazides
B-blockers
195
CCB names and uses
Amlodipine, clevidipine, nicardipine, nifedipine, nimodipine
Diltiazem, verapamil (non-dihydropyridines)
Blocks v-dependent L-type calcium channels of cardiac and smooth muscle to decrease contractility
196
Dihydropyridine use
```
HTN
Angina (including prinzmetal)
Raynauds phenomenon
Esophageal spasm
Migrane prophylaxis
```
197
Nimodipine use
SAH (prevents cerebral vasospasm)
198
Clevidipine use
HTN urgency or emergency
199
Non-dihydropyridine use
HTN
Angina
A Fib / A flutter
200
Non-dihydropyridine toxicity
Cardiac depression
| AV block
201
Dihydropyridine tox
```
Peripheral edema
flushing
dizziness
hyperprolactinemia (verapamil)
Constipation
Gingival hyperplasia
Reflex tachycardia
```
202
Hydralazine mech
Increases cGMP --> smooth muscle relaxation
Relaxes arterioles > veins (Afterload reduction)
203
Hydralazine use
```
Severe HTN
Heart failure (with organic nitrate)
```
Safe to use during pregnancy
Frequently given with B-blocker for reflex tachy
204
Hydralazine tox
Compensatory tachycardia (contraindicated in angina/CAD)
fluid retention
headache
angina
SLE like syndrome
205
Nitroprusside mech
short acting increase in cGMP via direct release of NO
206
Nitroprusside use
Hypertensive emergency
207
Nitroprusside tox
Cyanide toxicity (releases cyanide)
208
Fenoldopam mech
D1 receptor agonist --> Coronary, peripheral, renal, and splanchnic vasodilation
Decreases BP and Increases natriuresis
209
Minoxidil mech
opens K+ channels in smooth muscles leading to relaxation
210
Minoxidil use
Severe HTN
211
Minoxidil tox
Hypertrichosis
Hypotension
reflex tachy
fluid retention / edema
212
Nitrate names and mech
Nitroglycerin, isosorbide dinitrate, isosorbide mononitrate
Increase cGMP (smooth muscle relaxation)
dilates veins >> arteries (preload reduction)
213
Nitrate use
angina
acute coronary syndrome
pulmonary edema
214
Nitrate tox
Reflex tachycardia (treat with β-blockers)
hypotension
flushing
headache
215
Describe industrial exposure of nitrates
Development of tolerance for vasodilating action during work week and loss of tolerance over the weekend
Results in tachycardia, dizziness, and headache upon re-exposure
216
Which B-blockers are contraindicated in angina?
Pindolol
Acebutolol
Partial B-agonists
217
Digoxin mech
Inhibits Na/K ATPase creating a smaller gradient for NCX to pump calcium out (positive inotrope)
Stimulates vagus nerve to decrease HR
218
Digoxin use
Heart failure (increase contractility)
A Fib (decrease conduction at AV node and depression of SA node)
219
Digoxin tox
Cholinergic — nausea, vomiting, diarrhea, blurry yellow vision (think Van Gogh).
```
ECG:
Increased PR
Decreased QT
ST scooping
T-wave inversion
arrhythmia
AV block.
```
Hyperkalemia
220
What factors predispose you to digoxin toxicity
renal failure (?excretion)
hypokalemia (permissive for digoxin
binding at K+-binding site on Na+/K+ ATPase)
verapamil, amiodarone, quinidine (Decreases digoxin clearance; displaces digoxin from tissue-binding sites)
221
Digoxin antidote
slowly normalize K+
Cardiac pacer
Mg 2+
Anti-digoxin Fab fragments
222
Class I anti-arrhythmics mech
Na channel blockers
Slow or block (decrease) conduction (especially in depolarized cells)
Decreases slope of phase 0 depolarization
State dependent (depress tissue that is frequently depolarized)
223
Class IA anti-arrhythmics names and mech
Quinidine, Procainamide, Disopyramide
Increase AP duration
Increase ERP in ventricular action potential
Increase QT interval
224
Class IA anti-arrhythmics use
Both atrial and ventricular arrhythmias
Re-entrant SVT
Ectopic SVT
V-Tach
225
Class IA anti-arrhythmics tox
Cinchonism (headache, tinnitus with quinidine)
reversible SLE-like syndrome (procainamide), heart failure (disopyramide)
thrombocytopenia
torsades de pointes due to increased QT interval.
226
Class IB anti-arrhythmics names and mech
Lidocaine, Mexiletine, Tocainide
Decrease AP duration
Slows recovery of v-gated Na channels
Preferentially affects ischemic or depolarized purkinje and ventricular tissue
Phenytoin can also fit in here
227
Class IB anti-arrhythmics use
Acute ventricular arrhythmia (especially post MI)
Digitalis induced arrhythmia
228
Class IB anti-arrhythmics to
CNS stimulation/depression
Cardiovascular depression
Hyperkalemia increases the toxicity of IB drugs
229
Class IC anti-arrhythmics names and mech
Flecainide, Propafenone
Significantly prolongs ERP in AV node and accessory bypass tracts (strong Phase 0 block)
No effect on ERP in purkinje and ventricular tissues
Minimal effect on AP duration
230
Class IC anti-arrhythmics use
SVT including A Fib
Last resort in refractory V-tach
231
Class IC anti-arrhythmics tox
Pro-arrhythmic especially post MI
232
Class II anti-arrhythmics names and mech
Metoprolol, propranolol, esmolol, atenolol, timolol, carvedilol
Decrease SA and AV nodal activity by decrease cAMP
Decreased Ca current
Suppress abnormal pacemakers by decreasing slope of phase 4 (slows funny current channel opening)
233
Class II anti-arrhythmics use
SVT
ventricular rate control for A Fib
Atrial flutter
234
Class II anti-arrhythmics tox
Impotence
exacerbation of COPD and asthma
cardiovascular effects (bradycardia, AV block, CHF)
CNS effects (sedation, sleep alterations).
May mask the signs of hypoglycemia.
Metoprolol - dylipidemia
Propranolol - exacerbate vasospasm in prinzmetal
235
B-blocker overdose treatment
Saline
atropine
glucagon
236
Class III anti-arrhythmics names and mech
Amiodarone, Ibutilide, Dofetilide, Sotalol
Increases AP duration
Increases ERP
Increases QT interval (slows phase 3 repol)
237
Class III anti-arrhythmics use
A fib
a flutter
v-tach (amiodarone, sotalol)
238
Class III anti-arrhythmics tox
Sotalol - Torsades / excessive B blockade
Ibutilide - torsades
```
Amiodarone:
Pulm fibrosis
hepatotoxicity
hypothyroidism / hyperthyroidism
act as haptens (corneal deposits, blue/gray skin deposits resulting in photodermatitis)
neurologic effects
constipation
bradycardia / heart block / HF
```
239
Class IV anti-arrhythmics names and mech
Verapamil, diltiazem
Decreased conduction velocity
Increased ERP
Increased PR interval
Decreased slope of phase 0 in pacemakers
240
Class IV anti-arrhythmics use
Prevention of nodal arrythmias (SVT)
| rate control in a fib
241
Class IV anti-arrhythmics tox
```
Constipation
flushing
edema
Heart failure
AV block
sinus node depression
Torsades
```
242
Adenosine mech
Increases K+ out of cells --> hyperpolarizing the cell and decreases intracellular Ca
short acting ~15 seconds
Effects blunted by theophylline and caffeine (both are adenosine receptor antagonists)
243
Adenosine use
Drug of choice in diagnosing / abolishing supraventricular tachycardia
244
Adenosine tox
flushing, hypotension, chest pain, sense of impending doom, bronchospasm
245
Mg2+ use
Effective in torsades and digoxin toxicity
246
H2 blockers names and mech
Cimetidine, ranitidine, famotidine, nizatidine
Reversible block of histamine H2-receptors
247
H2 blockers use
Peptic ulcer, gastritis, mild esophageal reflux.
248
Cimetidine tox
potent CYP inhibitor
antiandrogenic effects (prolactin release, gynecomastia, impotence, decreased libido in males)
Can cross BBB and placenta
Both cimetidine and ranitidine can decrease renal excretion of creatinine
249
PPI names and mech
Omeprazole, lansoprazole, esomeprazole, pantoprazole, dexlansoprazole
Irreversibly inhibits H/K ATPase on parietal cells
250
PPI uses
Peptic ulcer, gastritis, esophageal reflux, Zollinger-Ellison syndrome
251
PPI tox
Increased risk of C. difficile infection
pneumonia
Hip fractures
Decreased serum Mg2+ with long-term use.
252
Bismuth / sucralfate mech
Bind to ulcer base, providing physical protection and allowing HCO3– secretion to reestablish pH gradient in the mucous layer.
253
Bismuth / sucralfate use
Increased ulcer healing
| Traveler's diarrhea
254
Misoprostol mech
A PGE1 analog
Increased production and secretion of gastric mucous barrier
Decreased acid production.
255
Misoprostol use
Prevention of NSAID induced peptic ulcers
maintain PDA
induction of labor (off-label) ripens cervix
256
Misoprostol
Diarrhea
Contraindicated in women of childbearing potential (abortifacient) --> stimulant effect on uterus
257
Octreotide mech
Long acting somatostatin analog
Inhibits actions of many splanchnic vasoconstriction hormones
258
Octreotide
Acute variceal bleeds
Acromegaly
VIPoma
Carcinoid tumors
259
Octreotide
Nausea, cramps, steatorrhea
260
Antacid side effects
can affect absorption, bioavailability, or urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying
261
Aluminum hydroxide tox
```
Constipation
Hypophosphatemia
proximal muscle weakness
osteodystrophy
seizures
```
262
Calcium carbonate tox
Hypercalcemia (stimulates gastrin release)
| rebound increase in acid
263
Magnesium hydroxide tox
Diarrhea
hyporeflexia
hypotension
cardiac arrest
264
Osmotic laxative names and mech
Magnesium hydroxide, magnesium citrate, polyethylene glycol, lactulose
Osmotic load to draw water into GI lumen
265
Osmotic laxative use
Constipation
Lactulose - treats hepatic encephalopathy --> gut flora degrades it into lactic acid and acetic acid --> promotes ntirogen excretion as NH4+
266
Osmotic laxative tox
Diarrhea
dehydration
may be abused by bullimics
267
Sulfasalazine mech
Combination of sulfapyridine (antibacterial) and 5-aminosalicylic acid (anti-inflamm)
Activated by colonic bacteria
268
Sulfasalazine use
UC
| CD
269
Sulfasalzine tox
Malaise
nausea
sulfonamide toxicity
reversible oligospermia
270
Ondansetron mech
5-HT3 antagonist
Decreased vagal stimulation
Powerful central-acting antiemetic.
271
Ondansetron use
Control vomiting postoperatively and in patients undergoing cancer chemotherapy
272
Ondansetron tox
Headache
constipation
QT interval prolongation
273
Metoclopramide mech
```
D2 receptor antagonist
Increased resting tone of gut
Increased contractility of gut
Increased LES tone
Increased gut motility
```
Does not influence colon transport time
274
Metoclopramide use
diabetic and post-OP gastroparesis
| anti-emetic
275
Metoclopramide tox
Increased parkinsonian effects
Tardive dyskinesia
Restlessness, drowsiness, fatigue, depression, nausea, diarrhea.
Drug interaction with digoxin and diabetic agents
Contraindicated in patients with small bowel obstruction or Parkinson disease (D1 receptor blockade)
276
Orlistat mech
Inhibits gastric and pancreatic lipase
| Decreases breakdown and absorption of dietary fats
277
Orlistat use
Weight loss
278
Orlistat tox
Steatorrhea
| Decreased absorption of ADEK
