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firstaid - pharm(2) Flashcards

1
Q

Cyclosporine

A

Inhibits calcineurin –> blocks differentiation/activation of T cells –> NO IL-2 (or its receptor) is made

for organ transplant patients

adv rxn: 
nephrotoxicity
gingival hyperplasia
HYPERlipidemia/HYPERglycemia
hirsutism
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2
Q

Tacrolimus

A

Similar to cyclosporine
Inhibits calcineurin –> no IL-2 secretion

Immunosuppresive in organ transplant pts.

adv rxn: everything similar to cyclosporine EXCEPT NO gingival hyperplasia & hirsutism

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3
Q

Sirolimus (Rapamycin)

A

Inhibits mTOR
Inhibits T cell proliferation in response to IL-2

Kidney transplant pts. – use in combo w/ cyclosporine & corticosteroids

adv. rxns:
Hyperlipidemia
Thrombocytopenia
Leukopenia

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4
Q

Azathioprine

A

antimetabolite precursor of 6-mercaptopurine

interferes w/ metabolism/synthesis of nucleic acids; toxic to lymphocytes

Kidney transplants
Autoimmune disorders (glomerulonephritis & hemolytic anemia)

Bone marrow suppression; toxic effects may be increased w/ allupurinol (since mercaptopurine is metabolized by xanthine oxidase)

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5
Q

Muromonab-CD3 (OKT3)

A

Binds CD3 (epsilon chain) on T cells – blocks CD3 interaction w/ T-cell signal transduction

Prevent acute rejection after KIDNEY transplant

adv rxns: cytokine release, hypersensitivity reaction

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6
Q

Aldesleukin (IL-2)

A

Renal cell carcinoma

Metastatic melanoma

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7
Q

Epoetin alfa

A

Anemias (esp in renal failure)

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8
Q

Filgrastim

A

GCSF –> recovery of bone marrow

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9
Q

Sargramostim

A

GMCSF –> recovery of bone marrow

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10
Q

a-interferon

A

Hep B&C
Kaposi’s sarcoma
Leukemia
Malignant melanoma

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11
Q

b-interferon

A

Multiple sclerosis

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12
Q

y-interferon

A

Chronic granulomatous disease

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13
Q

Oprelvekin (IL-11)

A

Thrombocytopenia

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14
Q

Thrombopoietin

A

Thrombocytopenia

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15
Q

Digoxin Immune Fab

A

target = digoxin

andtidote for digoxin toxicity

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16
Q

Infliximab

A

target = TNF-a

Crohn’s, RA, psoriatic arthritis, anklyosing spondylitis

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17
Q

Adalimumab

A

target = TNF-a

Crohn’s, RA, psoriatic arthritis

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18
Q

Abciximab

A

target = glycoprotein IIb/IIIa

prevent cardiac ischemia in unstable angina & pts. treated w/ percutaneous coronary intervention

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19
Q

Trastuzumab

A

Herceptin
target = HER2

HER2-overexpressing breast cancer

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20
Q

Rituximab

A

target = CD20

B-cell non-Hodgkin’s lymphoma

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21
Q

Omalizumab

A

target = IgE

severe asthma

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22
Q

When must B-blockers be used w/ caution in treating HTN?

A

Pts. w/ decompensated CHF (contraindicated in cardiogenic shock - LOW cardiac output)

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23
Q

ACE inhibitor relationship w/ diabetes mellitus

A

Protective against diabetic nephropathy

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24
Q

Antihypertensives for pts. w/ deiabetes mellitus

A

ACE inhibitors/ARBs
Ca2+ channel blockers
a-blockers
b-blockers

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25
DHP Ca2+ channel blockers
Nifedipine Amlodipine works on SMOOTH MUSCLE --> decrease BP (vessels relax)
26
non-DHP Ca2+ channel blockers
Verapamil Diltiazem HEART specific --> decrease contractility
27
Ad. Side effect of verapamil
AV block ``` slows down AV node decrease contractility (due to decrease Ca2+) --> weaken heart (BAD for CHF pts.) ```
28
Ca2+ channel indications
``` HTN Angina Arrhythmias (not nifedipine*) Prinzmetal's angina Raynaud's ```
29
Ca2+ channel adv. rxns
``` Cardiac depression AV block (Verapamil) Edema Flushing Dizziness (low CO) ```
30
Hydralazine
Increase cGMP --> smooth muscle relaxation VASODILATE arterioles>> veins AFTERLOAD reduced
31
Hydralazine: indications
Severe HTN CHF (problem w/ afterload) FIRST LINE therapy for HTN in pregnancy (with methyldopa)
32
What is hydralazine normally co-administered w/ to prevent one of its side effects? What additional side effects are present?
B-blocker co-administration w/ hydralazine to PREVENT reflex tachycardia Compensatory reflex tachycardia makes drug CONTRAindicated in angina/CAD Lupus-like syndrome
33
Rx for malignant HTN
``` Nitroprusside Labetalol Fenoldopam Nicardipine Clevidipine ```
34
Nitroprusside
Increase cGMP via release of NO Cause CN toxicity (releases CN) Short acting
35
Fenoldopam
Dopamine D1 receptor agonist ``` Vasodilation of: Coronary Peripheral Renal Splanchnic ``` Decrease BP and increase natriuresis
36
Nitroglycerin
Vasodilate by releasing NO in smooth muscle Increase cGMP Dilates VEINS>>arteries (contrast w/ hydralazine) ``` Decrease PRELOAD (less blood volume returning to heart from systemic system) ```
37
Isosorbide dinitrate
Same fxn. as nitroglycerin
38
Anti-anginal therapy (goal is to decrease myocardial O2 consumption - MVO2)
1. Nitrates (preload) Dilates veins: --decrease EDV (amount of venous return to heart) --decrease BP --decrease ejection time --decrease MVO2 -- increase contractility&HR (reflex response) 2. B-blockers (afterload) - -Increase EDV - -increase ejection time - - decrease contractility&HR (antiarrhythmic to counter nitrates effects) 3. Nitrates + b-blockers - -decrease BP - -decrease HR - -GREAT decrease in MVO2
39
Examples of anti-anginal drugs
Ca2+ channel blockers: Nifedipine ~ Nitrates Verapamil ~ B-blockers
40
What b-blockers should NEVER be used in treatment of angina?
Pindolol Acebutolol Partial B-agonists -- CONTRAINDICATED in angina
41
HMG-CoA reductase inhibitors: examples
"-statin" ``` Lovastatin Pravastatin Simvastatin Atorvastatin Rosuvastatin ```
42
Mechanism of HMG-CoA reductase inhibitors
Lowers LDL Inhibit HMG-CoA --> mevalonate conversion
43
Toxicities of HMG-CoA reductase inhibitors
``` Hepatotoxic Rhabdomyolysis (breakdown of muscle fibers) ```
44
Niacin effect on lipids
Decrease LDL | Increase HDL
45
Niacin (vitamin B3): MOA
inhibits lipolysis in adipose reduces hepatic VLDL secretion into circulation
46
Niacin toxicities
Red, flushed face (give ASA to decrease symptom) Hyperglycemia (acanthosis nigricans) Hyperuricemia (MAKES GOUT WORSE)
47
What lipid lowering drug should be avoided in treating gout patients?
Niacin --> causes hyperuricemia --> exacerbates gout
48
Bile acid resins: examples
Cholestyramine Colestipol Colesevelam
49
Bile acid resins: MOA
Prevent intestinal reabsorption of bile acids --> liver uses cholesterol in body to make more bile acids DECREASES LDL
50
Side effects of bile acid resins
Bad taste GI discomfort Decrease absorption of fat-soluble vitamins Cholesterol GALLSTONES
51
Cholesterol absorption blockers: example
Ezetimibe
52
Cholesterol absorption blockers: MOA
Decrease LDL Prevent cholesterol reabsorption at small intestine brush border
53
Side effect of Ezetimibe
Diarrhea
54
Fibrates: examples
Gemfibrozil Clofibrate Bezafibrate Fenofibrate
55
Fibrates: MOA
Upregulate lipoprotein lipase (LPL) --> increase TG clearance Decrease TGs!
56
Toxicities of Fibrates
Myositis Hepatotoxic Cholesterol GALLSTONES
57
Concommitent use of fibrates + statins leads to what toxicity?
Rhabdomyolysis
58
Cardiac glycoside: example
Digoxin
59
Digoxin: MOA
Inhibits Na+/K+ ATPase --> inhibit Na+/Ca2+ antiport --> INCREASE intracellular Ca2+ --> positive inotropy Increase contractility Stimulates vagus nerve --> DECREASE HR
60
Digoxin: indications
CHF (increase contractility) a. fib (decrease conduction at AV node & depression of SA node)
61
Digoxin toxicities
Blurry yellow vision T wave inversion, AV block Increase PR, decrease QT
62
Poor prognostic indicator while on digoxin treatment
Hyperkalemia
63
Factors predisposing pt. to digoxin toxicity
Renal failure Hypokalemia Quinidine (decrease digoxin clearance)
64
Antidote for digoxin toxicity (4)
Normalize K+ (slowly!) Lidocaine Anti-digoxin Fab fragments Mg2+
65
``` Antiarrhythmics: Na+ channel blockers (class IA) ```
Quinidine Procainamide Disopyramide Increase AP duration Increase effective refractory period (ERP)* Increase QT interval For use in ventricular tachycardia, reentrant & ectopic supraventricular tachycardia
66
What phase of the ventricular action potential curve is affected by Class I antiarrythmics?
Phase 0
67
Toxicities: Quinidine
Cinchonism - headache, tinnitus
68
Toxicities: Procainamide
Reversible SLE-like syndrome
69
Toxicities: Disopyramide
Heart failure
70
Toxicities for all class IA antiarrhythmics
Thrombocytopenia Torsades de pointes (due to increase QT interval)
71
``` Antiarrythmics: Na+ channel blockers (class IB) ```
Lidocaine Mexiletine Tocainide Decrease AP duration Acute ventricular arrhythmias -- preferred for post-MI patients* Digitalis-induced arhythmias*
72
What class of antiarrhythmics does phenytoin fall into?
Class IB
73
``` Antiarrhythmics: Na+ channel blockers (class IC) ```
Flecainide Propafenone Use for V. tach that progress to V. fib or intractable SVT LAST RESORT - for pts. with no structural abnormalities
74
When is use of class IC antiarrhythmics contraindicated?
Post-MI patients Pts. with no structural abnormalities Significantly prolong refractory period in AV node
75
``` Antiarrhythmics: B-blockers (class II) ```
Metoprolol Propanolol Esmolol Timolol Decrease SA and AV node activity via decrease cAMP and decrease Ca2+ currents AV node most sensitive* Increase PR interval Use for V. tach, SVT Slows ventricular rate during a. fib & a. flutter*
76
What phase of the ventricular action potential curve is affected by Class II antiarrhythmics?
Phase 4
77
Toxicities of class II antiarrhythmics
Impotence Asthma exacerbation CNS sedation cardiovascular (bradycardia, AV block, CHF) MASK signs of HYPOGLYCEMIA Treat toxicity w/ glucagon
78
Toxicity specific to metoprolol
Dyslipidemia
79
Toxicity specific to propranolol
Exacerbate vasospasm in Prinzmetal's angina
80
``` Antiarrhythmics: K+ channel blockers (class III) ```
``` "AIDS": Amiodarone Ibutilide Dofetilide Sotalol ``` Used when other antiarrythmics fail
81
Why are class III antiarrhythmics only used after other Rx have failed?
Prolonged QT interval --> could lead to torsades de pointes
82
Toxicity: Sotalol
Torsades de pointes | Excessive B block
83
Toxicity: Ibutilide
Torsades de pointes
84
Amiodarone toxicity
``` Pulmonary fibrosis Hepatotoxicity Hypothyroidism/hyperthyroidism (due to drug composition containing 40% Iodine) Corneal deposits Skin deposits (blue/gray) Photodermatitis ```
85
Tests to monitor what systems while patient is on Amiodarone?
Lungs Liver Thyroid
86
Why is Amiodarone a special antiarrhythmic?
Has class I, II, III, IV effects bc it alters lipid membrane
87
Arrhythmics: Ca2+ channel blockers (class IV)
Verapamil Diltiazem Decrease conduction velocity Increase ERP Increase PR interval
88
Class IV antiarrhythmics used to prevent?
nodal arrhythmias (SVT)
89
Adenosine indication
Increase K+ out of cells --> HYPERPOLARIZE cell and DECREASE influx of Ca into cell Use to diagnose/abolish SVT SHORT acting (~15 secs)
90
What can block effects of adenosine on cardiac conduction?
Theophylline | Caffeine
91
Mg2+ indication (what type of cardiac conditions?)
Torsades de pointes | Digoxin toxicity
92
Management of Type 1 diabetes
low sugar diet | insulin replacement
93
Management of Type 2 diabetes
dietary modification & exercise --> weight loss oral hypoglycemics insulin replacement (due to eventual loss of Islet cells producing adequate amount of insulin & increased insulin resistance as disease progresses)
94
Rapid-acting insulin
Lispro Aspart Glulisine
95
Short-acting insulin
Regular insulin
96
Intermediate acting insulin
NPH
97
Long-acting insulin
Glargine | Detemir
98
Insulin: MOA | liver, muscle, fat
Bind insulin receptor (tyrosine kinase activity) Liver: increase glucose storage as glycogen Muscle: increase glycogen & protein synthesis, K+ uptake Fat: helps TG storage
99
Insulin indications
Type 1 & 2 DM, gestational diabetes Life-threatening hyperkalemia* Stress-induced hyperglycemia
100
Insulin toxicity
Hypoglycemia
101
Metformin: MOA
Decrease gluconeogenesis Increase glycolysis (breaks down glucose --> makes ATP) Increase peripheral glucose uptake (INCREASE insulin sensitivity)
102
Metformin: indications
1st line for Type 2 DIABETES
103
Metformin: toxicity
Lactic acidosis
104
When is metformin use contraindicated?
Pts. with RENAL FAILURE (due to lactic acidosis side effect)
105
Sulfonylurea: 1st gen (2)
Tolbutamide | Chlorpropamide
106
Sulfonylurea: 2nd gen (3)
Glyburide Glimepiride Glipizide
107
Sulfonylurea: MOA
Close K+ channel in B-cell membrane --> cell depolarize --> Ca2+ influx --> insulin release
108
Sulfonylurea: indications
Stimulate release of ENDOGENOUS INSULIN in Type 2 diabetes Requires islet function (NOT effective in type 1 diabetes!)
109
Sulfonylurea: toxicity (1st gen vs. 2nd gen)
1st gen: disulfiram-like effects (Disulfiram is Antabuse -- used for long term treatment of alcoholics) 2nd gen: hypoglycemia
110
Glitazones/thiazolidinediones
Pioglitazone | Rosiglitazone
111
Pioglitazone & Rosiglitazon: MOA
Increase insulin sensitivity Binds PPAR-y nuclear transcription regulator
112
PPAR-y nuclear transcription regulator
Transcription regulator responsible for increasing insulin sensitivity & increase levels of adiponectin--fatty acid storage
113
Pioglitazone & Rosiglitazon: indications
Type 2 diabetes
114
Pioglitazone & Rosiglitazon: toxicity
Weight gain Edema Hepatotoxicity Heart failure (CHF exacerbation, MI)
115
a-glucosidase inhibitors (2)
Acarbose | Miglitol
116
a-glucosidase inhibitors: MOA
Inhibit intestinal brush border a-glucosidases DELAYS sugar hydrolysis & glucose absorption --> DECREASES availability of sugars --> DECREASE postprandial hyperglycemia
117
a-glucosidase inhibitors: indications
Type 2 diabetes
118
a-glucosidase inhibitors: toxicity
Gi disturbances (b/c they act at intestinal brush border) don’t use these drugs much anymore
119
Amylin analogs (1)
Pramlintide
120
Pramlintide: MOA, indications, toxicity
MOA: decrease glucagon (decrease sugars) Indication: type 1&2 diabetes Toxicity: Hypogylcemia
121
GLP-1 analogs (2)
Glucagon-like peptide (**opposite of normal glucagon which is anti-insulin; GLP is pro-insulin!**) Exenatide Liraglutide
122
GLP-1 analogs: MOA
Increase insulin | Decrease glucagon release
123
GLP-1 analogs: indications
Type 2 diabetes
124
GLP-1 analogs: toxicity
Pancreatitis
125
DPP-4 inhibitors (3)
Linagliptin Saxagliptin Sitagliptin
126
Relationship btwn DPP-4 and GLP-1
DPP-4 metabolizes GLP-1 Inhibit DPP-4 to keep GLP-1 in circulation
127
DPP-4 inhibitors: MOA, indications, toxicity
MOA & indications (same as GLP-1): Increase insulin Decrease glucagon Type 2 diabetes Toxicity: mild urinary/respiratory tract infections
128
Propylthiouracil Methimazole (MOA); what extra function does propylthiouracil have?
Blocks peroxidase --> inhibit organification of iodide --> inhibit coupling of thyroid hormone synthesis (can't make T3 or T4) Propylthiouracil also blocks 5'-deiodinase (decrease peripheral converion of T4 to T3); Active form T3 isn't made
129
Propylthiouracil Methimazole (Indications)
Hyperthyroidism
130
Propylthiouracil Methimazole (Toxicity)
Skin rash Aplastic anemia* Agranulocytosis (rare) Hepatotoxicity (Propylthiouracil) Teratogen (Methimazole)
131
Levothyroxine Triiodothyronine (MOA)
Thyroxine replacement
132
Levothyroxine Triiodothyronine (Indications)
Hypothyroidism | Myxedema
133
Levothyroxine Triiodothyronine (Toxicity)
Tachycardia Heat intolerance Tremors Arrhythmias
134
Hypothalamic/pituitary drugs (4)
1) GH 2) Somatostatin (Octreotide) 3) Oxytocin 4) ADH (Desmopressin)
135
1) GH 2) Somatostatin (Octreotide) 3) Oxytocin 4) ADH (Desmopressin) Indications for drugs?
GH: GH deficiency, Turner syndrome Octreotide/Somatostatin: Acromegaly, Carcinoid, Gastrinoma, Glucagonoma, Esophageal varices Oxytocin: Stimulates labor, uterine contractions, MILK LET-DOWN, controls uterine hemorrhage (contraction of uterus to stop bleeding) ADH (desmopressin): Pituitary Diabetes Insipidus
136
Demeclocycline: MOA
ADH antagonist (member of tetracyclin family)
137
Demeclocycline: Indications
SIADH
138
Demeclocycline: Toxicity
Nephrogenic Diabetes Insipidus Photosensitivity Abnormalities in bone & teeth (b/c Demeclocycline is a tetracycline)
139
Glucocorticoids (5)
``` Hydrocortisone Prednisone Triamcinolone Dexamethasone Beclomethasone ```
140
Glucocorticoids: MOA
Decrease production of leukotrienes & prostaglandins via: 1) inhibition of phopholipase A2 2) inhibition of COX-2 expression
141
Glucocorticoids: Indications
Addison's diesease (primary adrenal insufficiency -- CAN'T make any cortisol) Inflammation Immune suppression Asthma
142
Glucocorticoids: Toxicity
Iatrogenic Cushing's syndrome: buffalo hump, moon facies, truncal obesity, muscle wasting, thin skin, easy bruising, osteoporosis, adrenocortical atrophy, peptic ulcers, diabetes (if chronic) Adrenal insufficiency (when drug stopped abruptly) -- adrenal atrophy after prolonged glucocorticoid use (due to negative feedback)
143
H2 blockers (4)
Cimetidine Ranitidine Famotidine Nizatidine
144
H2 blockers: MOA
Blocks histamine H2-receptors (reversible) --> DECREASE H+ secreteion from parietal cells
145
H2 blockers: Indications
Peptic ulcer, gastritis, mild esophageal reflux
146
H2 blockers: toxicity
Cimetidine: a) Cytochrome P450 inhibitor b) Antiandrogenic effects* -- prolactin release, gynecomastia, impotence, decrease libido c) can cross blood-brain barrier (confusion, dizziness); cross placenta Cimetidine + Ranitidine: DECREASE renal excretion of creatinine
147
Proton pump inhibitors (5)
``` Omeprazole Lansoprazole Esomeprazole Pantoprazole Dexlansoprazole ```
148
Proton pump inhibitors: MOA
Inhibit H+/K+ ATPase in stomach parietal cells (irreversible)
149
Proton pump inhibitors: Indications
Peptic ulcer, gastritis, esophageal reflux Zollinger-Ellison syndrome*
150
Proton pump inhibitors: toxicity*
C. difficile infection Pneumonia Hip fractures Decrease serum Mg2+ after chronic use
151
Bismuth Sucralfate (MOA)
Binds to ulcer base - physical protection while HCO3- secretion reestablishes pH graident in mucous layer
152
Bismuth Sucralfate (Indications)
Increase ulcer healing | Traveler's diarrhea
153
Misoprostol: MOA
PGE1 analog Increase production and secretion of gatric mucous barrier Decrease acid production
154
Misoprostol: Indications
Prevent NSAID-induced peptic ulcers Maintenance of patent ductus arteriosus Induce labor (ripens cervix)
155
Maintenance of patnet ductus arteriosus Induce labor Prevent NSAID-induced peptic ulcers
Misoprostol
156
Misoprostol: Toxicity & contraindication
Diarrhea Contraindicated in women with childbearing potential (abortifacient)
157
Octreotide: MOA
Long-acting somatostatin analog
158
Octreotide: Indications
Acute variceal bleeds, acromegaly, carcinoid syndrome VIPOMA: produce vasoactive intestinal peptide -- secretes a lot of H2O and electrolytes --> diarrhea, hypokalemia, achlorhydria, dehydration
159
Octreotide: Toxicity
Steatorrhea | Nausea, cramps
160
Antacids (3)
Aluminum hydroxide Magnesium hydroxide Calcium carbonate
161
Antacid use: common side effect
Hypokalemia
162
Aluminum hydroxide: side effects
``` Constipation Hypophosphatemia Proximal muscle weakness Osteodystrophy Seizures ```
163
Magnesium hydroxide: side effects
Diarrhea Hyporeflexia Hypotension Cardiac arrest (Mg2+ relaxes smooth muscles -- hence side effects of Mg(OH)2
164
Calcium carbonate: side effects; specifically -- what drug interactions occur?
Hypercalcemia Rebound INCREASE in acid (due to excess Ca2+ which causes increase gastrin production --> increase stomach acid) Can chelate and decrease effectiveness of other drugs (tetracycline)
165
Osmotic laxative (4)
Magnesium hydroxide Magnesium citrate Polyethylene glycol Lactulose
166
Osmotic laxative: MOA
Provide osmotic load --> draws water out
167
Lactulose: special MOA other than just providing osmotic load (for treatment of constipation)
Treats hepatic encephalopathy (gut flora degrade toxic substances normally removed by liver into metabolites = lactic acid & acetic acid) --> promote nitrogen excretion as NH4+ Hepatic encephalopathy = confusion, altered level of consciousness, coma due to accumulation of toxic substances normally removed by the liver
168
Osmotic laxative: Indications
Constipation
169
Osmotic laxative: Toxicity
Diarrhea Dehydration (Abused by bulimics)
170
Infliximab: MOA
Monoclonal antibody to TNF-alpha
171
Infliximab: Indications
Crohn's disease UC Rheumatoid arthritis
172
Infliximab: Toxicity
Infection (reactivation of latent TB) Fever Hypotension
173
Sulfasalazine: MOA
Combination of: sulfapyridine (antibacterial) & 5-aminosalicyclic acid (anti-inflammatory) Has to be activated by colonic bacteria
174
Sulfasalazine: Indications
UC | Crohn's disease
175
Sulfasalazine: Toxicity
Sulfonamide toxicity | Oligospermia
176
Ondansetron: MOA
5-HT3 antagonist Central-acting antiemetic
177
Ondansetron: Indications
Controls vomiting postoperatively Vomiting in pts. undergoing chemotherapy
178
Ondansetron: Toxicity
Constipation | contrast this w/ carcinoid syndrome when an excess of serotonin --> diarrhea
179
Metoclopramide: MOA
D2 receptor antagonist Increase resting tone, contractility, LES tone, motility
180
Metoclopramide: Indications
Diabetic & post-surgery gastroparesis Anti-emetic
181
Metoclopramide: Toxicity
Increase Parkinsonian effects (tremor, rigidity, slowness of movement) Contraindicated in pts. w/ small bowel obstruction or Parkinson's disease
182
What drug interactions occur w/ Metoclopramide?
Interacts w/ digoxin & diabetic agents
183
Pro-kinetic Rx to get things moving in gut:
Increase Ach Increase serotonin Decrease dopamine
184
Mannitol: MOA
Osmotic diuretic Increase tubular fluid osmolarity --> increase urine flow (more H2O in urine) Decrease intracranial/intraocular pressure
185
Mannitol: Indications
Drug overdose Elevated intracranial/intraocular pressure (neuro procedures)
186
Mannitol: Toxicity & contraindications
Pulmonary edema Contraindicated in anuria (absolutely no urine production), CHF
187
Acetazoladmide: MOA
Carbonic anhydrase inhibitor Osmotic diuretic NaHCO3 diuresis (since NaHCO3 can't be broken down to CO2 + H2O to be reabsorbed from tubule lumen) --> reduction in HCO3- stores
188
Acetazoladmide: Indications
a) Glacucoma (need to decrease pressure) b) Urinary alkalinization (need to prevent kidney stone formation) c) Metabolic alkalosis d) Altitude sickness (respiratory alkalosis, appropriate metabolic acidosis compensation)
189
Acetazoladmide: Toxicity
Hyperchloremic metabolic acidosis (Excess H+ and Cl-) Paresthesias NH3 toxicity Sulfa allergy
190
Furosemide: MOA
Loop diuretic Inhibits cotransport of Na+ K+ and 2Cl- Renal medulla loses hypertonicity; urine is no longer concentrated
191
Relationship of furosemide to PGE release
Increase PGE release --> vasodilation of afferent arteriole | can be inhibited by ASA
192
Relationship of furosemide to Ca2+
Increase Ca2+ excretion
193
Furosemide: Indications
``` a) Edematous states: CHF cirrhosis nephrotic syndrome pulmonary edema ``` b) Hypertension c) Hypercalemia (b/c furosemide Loop diuretic Loses Ca2+)
194
Furosemide: Toxicity
``` Ototoxicity Hypokalemia Dehydration Allergy (sulfa) Nephritis (interstitial) Gout ``` "OH DANG"
195
Ethacrynic acid: MOA
Phenoxyacetic acid Loop diuretic that is NOT a sulfonamide (for pts. w/ sulfa allergy) Inhibits cotransport of Na+ K+ and 2Cl- (same as furosemide)
196
Ethacynic acid: Indications
Diuresis in pts. w/ sulfa allergy
197
Ethacrynic acid: toxicity
Hyperuricemia ``` All others similar to furosemide: "OH DaNG" Ototoxicity Hypokalemia Dehydration no sulfa Allergy!* Nephritis (interstitial) Gout ```
198
When is ethacrynic acid absolutely contraindicated?
Pts. w/ GOUT
199
Hydrochlorothiazide (HCTZ): MOA
Inhibits NaCl reabsorption in PCT - reduce diluting capacity of nephron Acts on DCT
200
HCTZ relationship to Ca2+
Decrease Ca2+ excretion (keeps Ca2+)
201
HCTZ: indications
HTN, CHF Idiopathic hypercalciuria Nephrogenic diabetes insipidus* (doesn't respond to ADH)
202
HCTZ: toxicity
Hypokalemic metabolic alkalosis Hyponatremia ``` Hyper"GLUC": HyperGlycemia HyperLipidemia HyperUricemia HyperCalcemia ``` Sulfa allergy
203
Loop diuretic to give patient w/ sulfa allergy
Ethacrynic acid
204
Renal Rx to avoid in patients w/ gout
Loop diuretic
205
K+ sparing diuretics (4)
Spironolactone, Eplerenone | Triamterene, Amiloride
206
K+ sparing diuretics: MOA
Spironolactone & Eplerenone: competitive aldosterone receptor antagonist Triamterene & Amiloride: blocks Na+ channels (same channels aldosterone acts on)
207
K+ sparing diuretics: indications
Hyperaldosteronism K+ depletion CHF
208
K+ sparing diuretics: toxicity
Hyperkalemia --> arrhythmias Spironolactone --> gyncomastia, antiandrogen effects
209
Diuretics: changes in urine NaCl
all diuretics INCREASE urine NaCl
210
Diuretics: changes in urine K+
All increase K+ excretion in urine --> toxicity potential: hypokalemia (except for K+ sparing diuretics)
211
Diuretics: changes in blood pH (ACIDEMIA)
Carbonic anhydrase inhibitors (decrease HCO3- reabsorption) K+ sparing (aldosterone prevents K+ and H+ secretion into urine); also hyperkalemia --> K+ enters cells, H+ exits cells into blood --> acidemia
212
Diuretics: changes in blood pH (ALKALEMIA)
Loop diuretics Thiazides Volume contraction --> increase ATII --> increase Na+/H+ exchange --> increase HCO3- reabsorption (contraction alkalosis) Low K+ states… H+ is exchanged for Na+ in cortical collecting tubule --> alkalosis & "paradoxical aciduria"
213
Diuretics: changes in urine Ca2+
Lose Ca2+ w/ loop diuretics | Keep Ca2+ w/ thiazides (HCTZ)
214
ACE inhibitors (3)
Captopril Enalapril Lisinopril
215
ACE inhibitors: MOA
Decrease ATII Prevent constriction of EFFERENT arterioles --> DECREASE GFR Increase bradykinin (vasodilator)
216
ACE inhibitors: Indications
HTN, CHF (prevent unfavorable heart remodeling due to HTN) Proteinuria (decrease GFR) Diabetic renal disease
217
ACE inhibitors: Toxicity
Increase bradykinin --> increase cough (kallekrein) Angioedema Teratogen* (fetal renal malformation) Creatinine (increase due to decrease GFR) Hyperkalemia (due to less GFR) Hypotension
218
Advantage of using ATII receptor blockers (-sartans) over ACE inhibitors
ARBs similar actions as ACE inhibitors but: ARBs have REDUCED angioedema & cough
219
When is use of ACE inhibitors contraindicated?
Pts. with bilateral renal artery stenosis (since ACE inhibitors further DECREASE GFR --> renal failure)
220
Leuprolide: MOA
GnRH analog agonist: pulsatile use antagonist: continuous use
221
Leuprolide: indications
Pulsatile: Infertility Continuous: Prostate cancer Uterine fibrinoids Precocious puberty
222
Leuprolide: toxicity
Antiandrogen
223
What other drug is used w/ leuprolide to treat prostate cancer?
Flutamide
224
Testosterone, methyltestosterone: MOA
agonist at androgen receptors
225
Testosterone, methyltestosterone: Indications
Hypogonadism --> develops secondary sex characteristics Stimulates anabolism --> recovery after burn/injury
226
Testosterone, methyltestosterone: Toxicity
Masculinization in females Reduce intratesticular testosterone in males (inhibits release of LH via negative feedback) --> testicular atrophy
227
Testosterone, methyltestosterone: association w/ lipoproteins
``` Increase LDL (bad!!) Decrease HDL (also bad!!) ```
228
Testosterone, methyltestosterone: association w/ growth in children
Premature closure of epiphyseal plate (pediatrics have early growth spurt but end up being shorter than their potential height bc of premature closure of growth plates)
229
Antiandrogens (4)
Finasteride Flutamide Ketoconazole Spironolactone
230
Finasteride: MOA
Inhibits 5a-reductase Testosterone CANNOT be converted to DHT
231
Finasteride: Indication
Benign prostatic hypertrophy
232
Alternative use for Finasteride
Male pattern baldness --> generates new hair growth
233
Flutamide: MOA
Competitive inhibitor of androgens at TESTOSTERONE RECEPTOR
234
Ketoconazole: MOA
Inhibits steroid synthesis (inhibits 17,20-Desmolase)
235
Spironolactone: MOA
Inhibits steroid BINDING
236
Rx for polycystic ovarian syndrome to prevent hirsutism
Ketoconazole & Spironolactone
237
Side effects of Ketoconazole & Spironolactone
Gynecomastia | Amenorrhea
238
Estrogens (3)
Ethinyl estradiol DES Mestranol
239
When is ethinyl estradiol, DES, mestranol absolutely contraindicated?
ER positive breast cancer History of DVTs (due to increased risk of thrombi)
240
Ethinyl estradiol DES Mestranol (MOA)
Bind estrogen receptors
241
Ethinyl estradiol DES Mestranol (Indications)
Hypogonadism Ovarian failure Menstrual abnormalities Hormone replacement therapy (HRT) in postmenopausal Men: androgen dependent prostate cancer
242
Ethinyl estradiol DES Mestranol (Toxicity)
Increase risk of endometrial cancer Bleeding (post menopausal women) Clear cell adenocarcinoma of vagina (females exposed to DES in utero)* Increase thrombi risk
243
Selective estrogen receptor modulators -SERMs (3)
Clomiphene Tamoxifen Raloxifene
244
Clomiphene: MOA
Partial agonist at ER in hypothalamus Prevents negative feedback --> increase release of LH and FSH --> ovulation
245
Clomiphene: Indications
Infertility Polycystic ovarian syndrome
246
Clomiphene: toxicity
Hot flashes Ovarian enlargement Multiple, simultaneous pregnancies Visual disturbances
247
Tamoxifen
Antagonist at breast tissue Treat/prevent ER positive breast cancer
248
Raloxifene
Agonist on bone - reduces resorption of bone Treats osteoporosis
249
Hormone replacement therapy (for postmenopausal)
Relief/prevention of menopausal symptoms (hot flashes, vaginal atrophy) Osteoporosis (increase estrogen, decrease osteoclast activity)
250
Complications of HRT
unopposed estrogen replacement increase ENDOMETRIAL cancer --> need to add progesterone possible increase in CV risk
251
Anastrozole | Exemestane: MOA
Aromatase inhibitors Inhibits conversion of testosterone to estradiol
252
Anastrozole | Exemestane: Indications
Use in postmenopausal women w/ breast cancer
253
Progestins: MOA
Bind progesterone receptors Reduce growth & vascularization of endometrium
254
Progestins: Indications
Oral contraceptives ``` Endometrial cancer (from unopposed estrogen) ``` Abnormal uterine bleeding
255
Mifepristone (RU-486): MOA
Competitive inhibitor of progestins at progesterone receptors
256
Mifepristone (RU-486): Indications
Termination of pregnancy No more progesterone --> endometrium sheds (similar to end of menses cycle)
257
What other Rx is usually administered w/ Mifepristone? What does this Rx do?
Misoprostol (PGE1) Uterine contractions (labor induction)
258
Mifepristone (RU-486): Toxicity
Heavy bleeding
259
Oral contraception (synthetic progestins, estrogen): MOA on hypothalamus
Inhibit LH/FSH --> no estrogen surge --> no LH surge --> no ovulation
260
Oral contraception: progestin specific effects
Progestins --> thickening of cervical mucus --> limit access of sperm to uterus Inhibit endometrial proliferation --> endometrium less suitable for implantation of embryo
261
When is oral contraception contraindicated?
Smokers > 35yrs of age (increase risk of cardiovascular events) Pts. w/ history of: a) thromboembolism & stroke b) estrogen-dependent tumor
262
Terbutaline
b2 agonist - relax uterus causes PREMATURE uterine contractions
263
Tamsulosin
a1 antagonist - inhibit smooth muscle contraction treats BPH: selective for a1A,D receptors (found on prostate); does NOT affect vascular a1B receptors
264
Sildenafil Vardenafil (MOA)
Inhibit phosphodiesterase --> increase cGMP Smooth muscle relaxes --> increase blood flow --> penile erection
265
Sildenafil Vardenafil (toxicity)
Blue-green color vision Hypotension (life threatening) if pt. is also on Nitrates Headache Dyspepsia
266
Danazol: MOA
Partial agonist at androgen receptors
267
Danazol: Indications
Endometriosis Hereditary angioedema
268
Danazol: toxicity
Masculinization (acne, hirsutism) Decrease HDL levels Hepatotoxic Edema Weight gain
269
H1 blockers: MOA
Reversible inhibitors of H1 histamine receptors
270
H1 blockers - 1st gen (3)
Diphenhydramine Dimenhydrinate Chlorpheniramine
271
H1 blockers - 1st gen (Indications)
Motion sickness* Sleep aid* Allergy
272
H1 blockers - 1st gen (Toxicity)
Sedation Antimuscarinic Anti-a-adrenergic (hypotension, dizziness)
273
H1 blockers - 2nd gen (3)
Loratidine Fexofenadine Desloratadine
274
H1 blockers - 2nd gen (Indication)
Allergy
275
H1 blockers - 2nd gen (Toxicity)
DECREASED entry into CNS (far less sedating) preferred antihistamine due to less drowsiness
276
Asthma drug targets (2 processes that mediate bronchoconstriction)
1) inflammation | 2) parasympathetic tone
277
Short acting b2 agonist (acute exacerbation)
Albuterol - relaxes smooth muscle
278
Long acting b2 agonist (prophylaxis of asthma)
Salmeterol | Formoterol
279
Side effects of Salmeterol & Formoterol
Tremor | Arrhythmia
280
Theophylline | Methylxanthines
Inhibit phosphodiesterase --> decrease cAMP hydrolysis --> increase overall cAMP concentration --> bronchodilation
281
Toxicities of Theophylline
Narrow TI (cardiotoxic, neurotoxic) Metabolized by P450
282
Relationship of theophylline & adenosine
Theophylline blocks action of adenosine
283
Asthma drug (muscarinic antagonist)
Ipratropium Blocks muscarinic receptor --> prevent bronchoconstriction
284
Muscarinic antagonist: indications
Tiotropium: COPD -- long acting anti-muscarinic Ipratropium: asthma (blocks bronchoconstriction)
285
Increase Ach Increase Adenosine; relationship to asthma?
Both increase in Ach and increase in adenosine --> bronchoconstriction muscarinic antagonists & theophylline used to inhibit Ach and adenosine, respectively
286
Corticosteroids (2)
Beclomethasone | Fluticasone
287
1st line therapy for chronic asthma
Corticosteroids
288
Corticosteroids: MOA
Inhibit cytokine synthesis by inhibiting NF-kB No NF-kB --> no TNF-a
289
Antileukotrienes (3)
Montelukast Zafirlukast Zileuton
290
Montelukast, Zafirlukast: MOA
Block leukotriene receptors Esp. good for ASA-induced asthma
291
Zileuton: MOA
Inhibit 5-lipoxygenase pathway Blocks conversion of arachidonic acid to leukotrienes
292
Omalizumab
anti-IgE antibody used in allergic asthma (that is resistant to inhaled steroids and long acting b2 agonists)
293
Guaifenesin
thins respiratory secretions; does NOT suppress cough reflex
294
N-acetylcysteine
mucolytic - loosen mucus plugs in CF patients also antidote for acetaminophen toxicity
295
Bosentan
antagonizes endothelin-1 receptors (decrease pulmonary vascular resistance) Rx for pulmonary HTN 
296
Dextromethorphan; MOA, indications; what is it an analog of?
Antitussive Antagonize NMDA glutamate receptors
297
What is dextromethorphan an analog of?
Analog of codeine; mild opioid effect in excess Give NALOXONE for overdose mild abuse potential
298
Pseudoephedrine Phenylephrine (MOA)
Sympathomimetic a-agonistic nasal decongestant
299
Pseudoephedrine Phenylephrine (Indications)
Reduce hyperemia, edema, nasal congestion Open obstructed Eustachian tubes Pseudoephedrine also used as stimulant
300
Pseudoephedrine Phenylephrine (Toxicity)
HTN (a-agoonist activity) CNS stimulation & anxiety (pseudoephedrine)
301
Methacholine
muscarinic receptor agonist used in asthma challenge testing
302
LTB4
Neutrophil chemotactic
303
LTC4 LTD4 LTE4
Bronchoconstriction Vasoconstriction Contraction of smooth muscle Increase vascular permeability
304
PGE2
increase uterine tone decrease vascular tone, bronchial tone
305
TXA2
increase platelet aggregation increase vascular tone increase bronchial tone
306
PGI2
PGI2 = Prostacyclin inhibits platelet aggregation promotes vasodilation
307
Aspirin (ASA): MOA
Irreversibly inhibit COX-1 and COX-2 via acetylation Decrease TXA2 and prostaglandins Increase bleeding time, no effect on PT or PTT
308
ASA: Indication
Low dose: decrease platelet aggregation Intermediate: Antipyretic/analgesic High dose: Anti-inflammatory
309
ASA: Toxicity
Gastric ulceration Tinnitus (CNVIII) Chronic use: Renal failure, interstitial nephritis Upper GI bleeding
310
ASA relationship w/ respiratory system
ASA stimulates respiratory centers --> hyperventilation --> respiratory alkalosis
311
ASA: use in children
Reye's syndrome in children given ASA for viral infection Exception: can give children ASA for Kawasaki's disease
312
NSAIDs (5)
``` Ibuprofen Naproxen Indomethacin Ketorolac Diclofenac ```
313
NSAIDs: MOA
Reversible inhibition of COX Blocks prostaglandin synthesis --> vasoconstriction occurs
314
NSAIDs: Indications
Antipyretic Analgesic Anti-inflammatory Indomethacin: closes PDA
315
NSAIDs: Toxicity
Interstitial nephritis Gastric ulcer: prostaglandins protect gastric mucosa Renal ischemia: prostaglandins vasodilate afferent arteriole
316
COX-2 inhibitor (1)
Celecoxib
317
Celecoxib: MOA
Reversible inhibition of COX-2 --> decrease inflammation & pain
318
Why is COX-2 inhibitor preferred over non-selective NSAIDs?
Spares TXA2 production --> platelet function remains Spares gastric mucosa --> no gastric bleeding
319
Celecoxib: Indications
Rheumatoid arthritis Osteoarthritis Pts. w/ gastritis or uclers
320
Celecoxib: Toxicity
Increase thrombosis | Sulfa allergy
321
Acetaminophen: MOA
Inhibits COX in CNS
322
Acetaminophen: Indications
Antipyretic Analgesic Give to children w/ upper respiratory illness
323
Acetaminophen: Toxicity
Hepatic necrosis
324
Acetaminophen metabolites: how does it cause liver toxicity?
Metabolites deplete glutathione --> toxic tissue adducts in liver N-acetylcysteine --> regenerates glutathione
325
Bisphosphonates
Alendronate | and other "-dronates"
326
Alendronate: MOA
Pyrophosphate analog Binds hydroxyapatite in bone Inhibit osteoclast activity
327
Alendronate: Indications
Osteoporosis Hypercalcemia Paget's disease of the bone Pts. on corticosteroids: need prophylactic bisphosphonates
328
Alendronate: Toxicity
Corrosive esophagitis (pt. needs to remain upright for 30mins after taking medication) Osteonecrosis of the jaw
329
Gout: chronic (4)
Allopurinol Febuxostat Probenecid Colchicine
330
Allopurinol
Inhibits xanthine oxidase (no conversion of hypoxanthine --> xanthine; xanthine --> uric acid) DECREASED uric acid production
331
Allopurinol: Indication
Chronic gout Lymphoma & Leukemia: prevent tumor lysis-associated urate nephropathy Increase concentrations of azathioprine (drug given for prevention of organ rejection in pts. w/ kidney transplant) & 6-MP
332
Febuxostat
Inhibit xanthine oxidase
333
Probenecid
Inhibit reabsorption of uric acid in PCT
334
Relationship of Probenecid & Penicillin
Probenecid inhibits secretion of penicillin
335
Colchicine
Binds/stabilizes tubulin --> inhibit polymerizations --> inhibit leukocyte chemotaxis and degranulation
336
Gout: acute (2)
NSAIDs | Glucocorticoids
337
ASA administration to pts. w/ gout
DO NOT give salicylates --> decrease uric acid clearance in urine --> increased likelihood of gout!
338
TNF-alpha inhibitors (2)
Etanercept | Infliximab, Adalimumab
339
Use of TNF-alpha inhibitors predispose to what condition?
Reactivation of latent TB TNF blockage --> no activation of macrophages --> no destruction of phagocytosed microbes
340
Etanercept: MOA
Fusion protein serves as receptor for TNF-a + IgG Fc Produced by recombinant DNA Etanercept is TNF decoy receptor (binds up all TNF-a in body)
341
Etanercept: Indications
Rheumatoid arthritis Psoriasis Ankylosing spondylitis
342
Infliximab Adalimumab (MOA)
Anti-TNF-a monoclonal antibody
343
Infliximab Adalimumab (Indications)
Crohn's disease Rheumatoid arthritis Ankylosing spondylitis Psoriasis

STEP1 - TLe (8 decks)

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