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1
Q

What is the mechanism of action Cimetidine (ranitidine, famotidine, nizatidine)?

A

Reversible H2 blockade

- decreased secretion of H+ by parietal cells

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2
Q

Which H2 blocker is a CYP inhibitor?

A

Cimetidine

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3
Q

Which H2 blocker has anti-androgenic effects?

A

Cimetidine

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4
Q

What are the anti-androgenic effects seen with Cimetidine?

A

Prolactin release
Gynecomastia
Impotence

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5
Q

Which H2 blockers decrease renal excretion of creatinine?

A

Cimetidine and ranitidone

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6
Q

What class of drug is Omeprazole (lanzoprazole, esomeprazole, pantoprazole, dexlansoprozole)?

A

PPI, used in peptic ulcer, gastritis, GERD, and Z-E syndrome

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7
Q

What is the mechanism of action of Omeprazole?

A

Irreversibly inhibits Na/K ATPase in Parietal Cells of stomach

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8
Q

What class of drug is Cimetidine?

A

Inhibits acid secretion in peptic ulcer disease, gastritis, GERD

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9
Q

What drug is used in Zollinger-Ellison Syndrome?

A

Omeprazole

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10
Q

What GI drug/class of acid inhibitors increased risk of C. diff?

A

PPIs

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11
Q

What GI drug/class of acid inhibitors causes increased risk of hip fractures?

A

PPIs

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12
Q

What is the mechanism of action of bismuth and sucralfate?

A

Bind to the base of the ulcer

Provide physical protection so HCO3- can re-establish mucosa pH

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13
Q

What is the mechanism of action of Misprostol (GI) ?

A

PGE1 analog

Increased production, secretion of gastric mucosal barrier
Less acid production

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14
Q

What is the mechanism of action of Octreotide?

A

SST analog

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15
Q

What are the indications for Octreotide?

A

Acute variceal bleeds
VIPoma
Carcinoid tumors

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16
Q

What is a common side effect of all antacids?

A

Hypokalemia

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17
Q

What antacid causes constipation?

A

Aluminum hydroxide

Aluminimum amount of feces

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18
Q

What antacid causes hypophosphatemia?

A

Aluminum hydroxide

Aluminimum amount of phosphate

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19
Q

What antacid causes hypercalcemia?

A

Calcium carbonate

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20
Q

How does calcium carbonate decrease the effectiveness of other drugs?

A

Calcium carbonate chelates

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21
Q

What antacid causes diarrhea?

A

Magnesium hydroxide

Mg = Must go…to the bathroom

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22
Q

What antacid can cause seizure?

A

Aluminum hydroxide

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23
Q

What antacid can cause cardiac arrest?

A

Magnesium hydroxide

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24
Q

What are the osmotic laxatives (3)?

A

Magnesium hydroxide
Magnesium citrate
Polyethylene glycol
Lactulose

Ma(y) Po(op) a Lact

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25
What osmotic laxative is also used to treat hepatic encephalopathy?
Lactulose - Gut flora degrade into metabolites (lactic acid and acetic acid) that promote nitrogen excretion as NH4+
26
What does Infliximab target?
TNF-a
27
What does Infliximab treat?
Crohn's, UC, RA, Ankylosing spondylitis, psoriasis
28
What two functions does sulfasalazine bring together?
Anti-bacterial and anti-inflammatory
29
What does sulfasalazine treat?
UC and Crohn's (mild-moderate)
30
What is a 5HT3 antag used for anti-emesis?
Ondansetron
31
What is a D2 receptor antag used to create GI motility?
Metoclopramide
32
In what diseases in Metoclopramide contraindicated?
Parkinson's | Obstructed small bowel
33
What are some purine synthesis inhibitors used to treat IBD?
Azathioprine and Mercaptopurine | - Cause immunosuppression
34
What is a dihydrofolate reductase inhibitor used to treat IBD?
MTX - Blocks THF synthesis from folic acid - Causes immunosuppression
35
What is the function of LTB4, produced in the LOX pathway?
Neutrophil chemotactic agent Neutrophils arrive B4 others
36
What are the functions of LTC4, D4, E4, produced in the LOX pathway?
Bronchoconstriction (mainly) Vasoconstriction Contraction of smooth muscle Increased vascular permeability
37
What is the function of PGI1, produced on the COX pathway?
Platelet-Gathering-Inhibitor ``` Inhibits platelet aggregation Promotes vasodilation (decreased vascular tone) ``` (Also decreased bronchial tone, uterine tone)
38
What is the action of corticosteroids in the arachidonic acid pathway?
Phospholipase A2 inhibition | Also inhibitors of protein synth in the COX pathway
39
What drug is a LOX pathway inhibitor?
Zileuton is a lipoxygenase inhibitor
40
What drugs are the COX pathway inhibitors?
NSAIDs, aspirin, and acetaminophen are COX-2 inhibitors
41
What drugs are Leukotriene inhibitors (and which ones are inhibited)?
Zafirlukast, Montelukast Inhibit LTC4, D4, E4
42
What is the mechanism of Aspirin?
Irreversible inhibitor of COX-1 and COX-2 by covalent acetylation This decreases synthesis of TXA2 and prostaglandins
43
How does aspirin affect bleeding time, PT, PTT?
Increased bleeding time until new platelets are produced (7 days) No change in PT, PTT
44
What are the different functions of aspiring at low, medium, and high doses?
Low: decreased platelet aggregation Medium: antipyretic and analgesic High: anti-inflammatory
45
What is the effect of aspirin in treating children with viral illness?
Reye's Syndrome! Contraindication!
46
How does aspirin affect the respiratory centers?
Hyperventilation > Respiratory Alkalsosis
47
What are GI side effects of aspirin?
Gastric ulceration Acute renal failure Interstitial nephritis Upper GI bleed (with chronic use)
48
What is a neuro side effect of aspirin?
Tinnitus (CN VIII)
49
What is the function of PGE2 and PGF2, produced in the COX pathay?
Increase uterine tone | Decrease bronchial tone
50
What is the function of TXA2, produced int he COX pathway?
Increased platelet aggregation Increased vascular tone Increased bronchial tone
51
What products of the arachidonic acid pathway increase bronchial tone?
LTC4, LTD4, LTE4 & TXA2
52
What products of the arachidonic acid pathway decrease bronchial tone?
PGI2, PGE2, PGF2
53
What drugs (besides aspirin) are classified as NSAIDs?
Be KIIND to your body with NSAIDs Ketorolac, Indomethacin, Ibuprofen, Naprozen, Diclofenac
54
What is the mechanism of action of NSAIDs?
REVERSIBLY inhibit COX-1 and COX-2, block PG synth | contrast Aspirin, IRREVERSIBLE
55
... is an NSAID used to close a PDA.
Indomethacin
56
What is the effect of prostaglandins on the renal arterioles?
PGs vasodilate afferent arteriole
57
What drug is a selective COX-2 inhibitor?
Celecoxib
58
What is the action of a COX-2 inhibitor as compared to COX-1 and 2?
COX-2 works against inflammation and pain Spares COX-1 - Maintains gastric mucosa--no corrosive effects - Spares platelet function, as TXA2 depends on COX-1
59
What are the clinical indications of Celecoxib?
RA, osteoarthritis; patients with gastritis or ulcers
60
What are the adverse effects of Celecoxib?
Increased risk of thrombosis | Sulfa allergy
61
What is the difference between the use cases of Acetaminophen and Aspirin/NSAIDs?
Acetaminophen is not anti-inflammatory Is still antipyretic and analgesic
62
What is the mechanism of aciton of Acetaminophen?
Reversible COX inhibitor, mostly in the CNS
63
What is the main toxicity of Acetaminophen?
Hepatic necrosis NAPQI depletes glutathione and forms toxic tissue adducts in liver
64
What is the antidote to Acetaminophen hepatotox?
N-acetylcysteine Regenerates glutathione
65
Name a bisphosphonate.
Alendronate (all are -dronates)
66
What is the mechanism of action of a bisphosphonate?
Pyrophosphate analog that binds hydroxyapatite in bone Inhibits osteoclasts
67
What are the clinical indications for bisphosphonates?
Osteoporosis Hypercalcemia Paget disease of bone
68
Why are patients advised to take bisphosphonates with water and remain upright for 30 mins?
Corrosive esophagitis & osteonecrosis of jaw are potential adverse effects
69
What is the MOA of Allopurinol?
Inhibits Xanthine Oxidase, which ends up making less uric acid
70
How does Allopurinol affect concentrations of Azathioprine and 6-MP?
Increases concentrations, because both are metabolized by XO
71
What are the indications of Allopurinol?
Preventative for Gout | Also used in lymphoma and leukemia to prevent tumor lysis associated urate nephropathy
72
What is the MOA of Febuxostat?
Inhibits XO
73
What are the indications of Febuxostat?
Preventative for Gout
74
What is the MOA of Probenecid?
Uricosuric Inhibits reabsorption of uric acid in the PCT Also inhibits secretion of penicilin
75
What are the indications of Probenecid?
Preventative for Gout
76
What types of drugs work during acute gout?
NSAIDs Glucocorticoids Colchicine TNF-a inhibitors
77
What NSAIDs are used in acute gout?
Naproxen, Indomethacin
78
How does Indomethacin affect T and B cells?
Actually increases T and B cells!
79
What is the MOA of Colchicine?
Binds and stabilizes tubulin This inhibits microtubule polymerization Impairs leukocyte chemotaxis and degranulation
80
What are the indications of Colchicine?
Acute and Preventative for gout
81
What are the side effects of Colchicine?
GI side effects
82
What must be tested for before administering a TNF-a inhibitor?
TB, because TNF blockage prevents activation of macrophages
83
Name 3 TNF-a inhibitors.
Etanercept Infliximab Adalimumab
84
What is a fusion protein receptor for TNF-a, IgG, and Fc?
Etanercept EtanerCEPT is a TNF decoy reCEPTor Basically mops up these substances
85
What are the indications of Etanercept
RA, Psoriasis, Ankylosing Spondylitis
86
What is the MOA of Infliximab (and adalimumab)?
anti-TNF-a monoclonal antibody
87
What are the indications for infliximab (and adalimumab)?
IBD, RA, Psoriasis, Ankylosing Spondylitis
88
What is a recombinant uricase used in refractory gout?
Pegloticase
89
What is the MOA of insulin on the liver?
Increases uptake of glucose to be stored as glycogen
90
What is the MOA of insulin on muscle?
Increases glycogen and protein synthesis | Also K+ uptake
91
What is the MOA of insulin on fat?
Increases TG storage
92
What type of receptor does insulin bind/use to mediate its effects?
TK
93
What are the rapid acting insulins?
Lispro Aspart Glulisine no LAG
94
What are the indications for rapid acting insulin?
Postprandial glucose control in - DM 1 - DM 2 - GDM
95
What is a short acting insulin?
Regular insulin
96
What are the indications for regular insulin?
- DM 1 - DM2 - GDM - DKA (IV) - Hyperkalemia (+ glucose) - Stress hyperglycemia
97
What is intermediate acting insulin?
NPH
98
What are the indications for NPH insulin?
- DM 1 - DM2 - GDM
99
What are the long acting insulins?
Glargine Detemir GlaDe: long-lasting scent
100
What are the indications for long acting insulin?
Basal glucose control - DM1 - DM2 - GDM
101
What is the main adverse reaction of all the exogenous insulins?
Hypoglycemia
102
... is a Biguanide that is the 1st line therapy in DM 2.
Metformin
103
What is the MOA of Metformin?
Mainly decreases gluconeogenesis Increases glycolysis Increases peripheral glucose uptake (insulin sensitivity) - No risk of hypoglycemia b/c it's only using the insulin that is there endogenously
104
What are the indications for Metformin?
First line therapy in DM 2 Also used in: - Patients without islet function - PCOS
105
What is the most serious side effect of Metformin?
Lactic acidosis (thus contraindicated in renal failure)
106
What is the MOA of sulfonylureas?
Close K+ channel in beta-cell membrane, so cell depolarizes > Ca influx > release of endogenous insulin
107
What are the indications for sulfyonylureas?
DM 2 Require some islet fx, so useless in DM 1
108
What are the first generation sulfonylureas?
Tolbutamine Chlorpropamide (DM 2)
109
What are the second generation sulfonylureas?
Glyburide Glimepiride Glipizide (DM 2)
110
What are the adverse effects of first generation sulfonylureas, used in diabetes treatment?
Disulfiram-like effects
111
What are the adverse effects of second generation sulfonylureas, used in diabetes treatment?
Hypoglycemia
112
What is an adverse effect of all sulfonylureas, used in diabetes treatment?
Risk of hypoglycemia increases with renal failure
113
What is the mechanism of action of Thiazolidinediones in treating diabetes?
Increase insulin sensitivity in peripheral tissue Bind PPAR-g nuclear transcription regulator
114
What is the role of PPAR-g in glucose control?
Genes activated by PPAR-g regulate fatty acid storage and glucose metabolism. Activation of PPAR-g increases insulin sensitivity and levels of adiponectin
115
What are the two main Thiazolidinediones?
Pioglitazone Rosiglitazone "Zone P(par) is where you want to be"
116
What are the indications for Pioglitazone and Rosiglitazone in treating diabetes?
Monotherapy in DM 2 or combined with other agents
117
What are the adverse effects for Pioglitazone and Rosiglitazone in treating diabetes?
Weight gain, edema, hepatotox, heart failure
118
What is the MOA of a-glucosidase inhibitors in treating diabetes?
Inhibit intestinal brush border a-glucosidases - Delayed sugar hydrolysis and glucose absorption - Decreased postprandial hyperglycemia
119
What are the two main a-glucosidase inhibitors?
Acarbose Miglitol bAM! inhibitors (brush border, Acarbose, Miglitol)
120
What are the indications for Miglitol and Acarbose in treating diabetes?
Monotherapy in DM 2 or combined with other agents
121
What are the side effects of the a-glucosidase inhibitors in treating diabetes?
GI: flatulence! Cannot treat hypoglycemia with disaccharides, must use dextrose
122
...is an amylin analog that decreases gastric emptying and decreases glucagon.
Pramlintide
123
What are the indications for Pramlintide in treating diabetes?
DM 1 | DM 2
124
What are the adverse effects of Pramlintide in treating diabetes?
Hypoglycemia Nausea Diarrhea
125
GLP-1 analogs like... and...prime insulin release, so you can respond immediately to food.
Exenatide | Liraglutide
126
What is the MOA of Exenatide and Liraglutide in diabetes treatment?
Increase insulin, decrease glucagon release Cause weight loss and appetite suppression
127
What are the indications of Exenatide and Liraglutide in treating diabetes?
DM 2
128
What are the side effects of Exenatide and Liraglutide in treating diabetes?
N/V, pancreatitis
129
What are the DPP-4 inhibitors of diabetes management?
Linagliptin Saxagliptin Sitagliptin
130
What is the MOA of the DPP-4 inhibitors (-gliptins) in diabetes management?
Increased insulin, decreased glucagon release through increasing GLP, GIP
131
What are the indications for DPP-4 inhibitors (-gliptins) in diabetes management?
DM 2
132
What are the side effects of the DPP-4 inhibitors (-gliptins) in diabetes management?
Mild UTI or RTI
133
What are the SGLT 2 inhibitors used in diabetes management?
Canagliflozin | Dapagliflozin
134
What is the MOA of the -gliflozins used in diabetes management?
Block SGLT 2 so glucose cannot be reabsorbed from the kidney > glucosuria
135
What are the indications for the -gliflozins used in diabetes management?
DM 2
136
What are the side effects of -gliflozins used in diabetes management?
UTI Mycotic infections Increased urination Increased creatinine
137
... and ... are two drugs that block the oxidation and organification of iodine to inhibit thyroid hormone synthesis.
Propylthiouracil (PTU) and Methimazole
138
What specific hormone do both PTU and Methimazole block to inhibit iodine oxidation and organification?
Thyroid peroxidase
139
What additional action toes PTU have in inhibiting the action of thyroid hormone?
Also blocks 5' deiodinase, which decreases peripheral conversion of T4 to T3
140
What are the indications of PTU and Methimazole?
Hyperthyroidism
141
Which drug used to treat hyperthyroidism can be used in pregnancy?
PTU PTU: Peripheral and Pregnancy
142
What drug used in hyperthyroidism blocks T4 release from the thyroid?
Potassium iodide
143
What drug used in hyperthyroidism blocks iodide uptake into the thyroid?
Perchlorate
144
What are two drug replacements for thyroxine?
Levothyroxine | Triiodothyronine
145
What are the adverse effects of both PTU and Methimazole in treating hyperthyroidism?
Agranulocytosis (rare) Aplastic Anemia Skin Rash
146
What is an adverse effect of PTU in treating hyperthyroidism?
Hepatotox
147
What is an adverse effect of Methimazole in treating hyperthyroidism?
Teratogen, can cause aplasia cutis
148
What are the indications for Levothyroxine and T3?
Hypothyroidism | Myxedema
149
What are the adverse effects of Levothyroxine and T3?
Tachycardia Heat intolerance Tremors Arrhythmia (basically effects of overactive hormone)
150
What are the clinical indications for Growth Hormone?
GH deficiency Turner's Syndrome wasting in HIV/AIDs Short bowel syndrome
151
What is the MOA of Octreotide?
SST analog
152
What are the indications for Octreotide?
``` Acromegaly Carcinoid Gastrinoma Glucagonoma Esophageal varices ```
153
What are the indications for Oxytocin?
Stimulate labor, uterine contractions Milk let-down Control uterine hemorrhage
154
What are the indications for ADH (DDAVP, Desmopressin)?
Central DI (not nephrogenic)
155
What is the MOA of Demeclocycline?
ADH antagonist
156
What are the indications for Demeclocycline?
SIADH
157
What are the adverse effects of Demecloclycine?
Nephrogenic DI Photosensitivity Abnormalities of bone and teeth
158
What are two dopamine agonists used to treat prolactinomas?
Bromocriptine | Cabergaline
159
What are the adverse effects of DA agonists use to treat prolactinomas?
N/V, headache, orthostatic hypotension, psych sx | Valvular heart disease (Cabergaline only)
160
What is the mechanism of action of glucocorticoids?
Metabolic, catabolic, anti-inflammatory, and immunosuppressive effects mediated by interactions with glucocorticoid response elements and inhibition of transcription factors like NF-kB
161
What are the indications for glucocorticoids?
Many, but mainly: - Addison's disease (chronic primary adrenal insufficiency) - Inflammation - Immune suppression - Asthma
162
What are some signs of glucocorticoid toxicity?
Cushing's Syndrome: buffalo hump, moon facies, truncal obesity, muscle wasting, thin skin, easy brusing, osteoporosis, adrenocortical atrophy, peptic ulcer, diabetes
163
What can occur if glutocorticoids are stopped abruptly after chronic use?
Adrenal insufficiency
164
... is a steroid that works 1:1 at glucocorticoid and mineralocorticoid receptors.
Hydrocortisone
165
... is a steroid that works at glucocorticoid > mineralocorticoid receptors.
Prednisone | - Stronger at gluco receptors than hydrocortisone
166
... is a steroid that works at glucocorticoid >>> mineralocorticoid receptors, a pure glucocorticoid agonist.
Dexamethasone

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