Learning Objectives Focused Flashcards
1
Q
What is the MOA of the Vitamin K Antagonist Coumadin [Warfarin]?
A
Inhibits Vitamin K dependent coagulation factor synthesis
2
Q
What is the MOA of the Coagulation Factor Antagonist Enoxaparin [Lovenox]?
A
Irreversibly inactivates clotting factor-Xa much more-so than Factor-IIa (thrombin)
It is LMW heparin extract making it more predictable than normal heparin
3
Q
What is the MOA of the Coagulation Factor Antagonist Rivaroxaban [Xarelto]?
A
Factor-Xa inhibitor (converts prothrombin to thrombin
Selectively blocks the active site of Factor-Xa, inhibiting blood coagulation.
4
Q
What is the MOA of the Platelet Inhibitor Clopidogrel [Plavix]?
A
Irreversible inhibition of platelet ADP receptors which normally trigger platelet activation and aggregation via downstream activation of GIIIb/IIa
5
Q
What is the MOA of the GPIIIa/IIb receptor antagonist Abciximab [ReoPro]?
A
Fab fragment binds to GPIIIb/IIa receptor of human platelets and inhibits platelet aggregation
Binds to vitronectin receptor on platelets and vessels wall endothelial and smooth muscle cells
6
Q
Specify normal/abnormal total cholesterol.
A
Desirable - 200
7
Q
Specify normal/abnormal LDL cholesterol.
A
Desirable - 130
8
Q
Specify normal/abnormal HDL cholesterol.
A
Desirable - >60
9
Q
Which two statins produce the greatest serum LDL cholesterol reduction?
A
Atorvastin and Rosuvastatin (50%)
10
Q
Which statin produces the greatest triacylglycerol reduction?
A
Atorvastatin (29%)
11
Q
Which two statins produce the greatest HDL cholesterol increase?
A
Pravastatin and Simvastatin (12%)
12
Q
Which two statins have the ability to penetrate the CNS?
A
Lovastatin and Simvastatin
13
Q
What is the MOA of the HMG-CoA Reductase Inhibitor Atorvstastin [Lipitor]?
A
Competitively inhibits HMG-CoA Reductase which is responsible for an early, rate limiting step in cholesterol biosynthesis
Increases hepatic LDL receptors, enhancing catabolism
14
Q
What are the common adverse effects of Atorvstastin?
A
nasopharyngitis, myalgia, myopathy impaired function associated w/ elevated serum transaminase levels (jaundice), amnesia
15
Q
What are the ocular adverse effects of Atorvstastin?
A
Diplopia, ptosis, pseudo-CME & blurred vision, elevated IOP, intraocular hemorrhage, cataracts
16
Q
What happens when you take cyclosporine, erythromycin or azalea antifungals with Atorvastatin? (unique)
A
Myopathy exacerbation (a common adverse effect of Atorvastatin)
17
Q
What is the contraindication of Atorvastatin?
A
Azole Antifungals
18
Q
When is Fenofibrate commonly prescribed?
A
In conjunction with statins or in statin resistant patients
19
Q
What is the MOA of the Fibrate Fenofibrate [TriCor]?
A
Stimulates nuclear receptor PPAR which modulates transcription of insulin (get’s energy into our cells) sensitive genes in live, muscle and adipose tissue (release of lipids into the bloodstream)
Enhances HDL production; inhibits triglyceride synthesis and stimulates catabolism of triglyceride-rich lipoproteins
Greatest effect on cells that reproduce the fastest
20
Q
What are the common adverse effects of Fenofibrate?
A
headache, rhinitis, flu syndrome
21
Q
What are the serious adverse effects of Fenofibrate?
A
SJS, TEN (toxic epidermal necrolysis), hepatitis, cirrhosis, thromboembolism, myositis, myopathy, rhabdomyolysis
22
Q
What are the drug interactions of Fenofibrate?
A
Acyclovir, aminoglycoside, cyclosporine, gancyclovir - impaired renal elimination
Impaired metabolism of Sulfonylureas (Diabetes med)
23
Q
What is Niacin commonly known as?
A
OTC Vitamin B3
24
Q
What is the MOA of Niacin?
A
Inhibits lipolysis in adipose tissue, resulting in reduced hepatic VLDL synthesis and production of LDLs in plasma
25
What are the common adverse effects of Niacin?
headache, pseudo CME (goes away if you stop taking), flushing, pruritus, hyper pigmentation, jaundice, xeroderma, orthostatic hypotension
26
What is the unique ocular adverse effect of Niacin?
Toxic Amblyopia (the only one that does this)
27
What are the serious adverse effects of Niacin?
Hepatotoxicity, arrythmias
28
What are the drug interactions of Niacin?
Alpha and Beta Blockers - additive effect
29
What are the cautions to consider when thinking of using Niacin?
Diabetes (elevated blood sugar), sugar (anti-platelet effect)
30
What is the MOA of the Cholesterol Absorption Inhibitor Ezetimibe [Zetia]?
Inhibits dietary and biliary cholesterol absorption at small intestinal brush border
Used in conjunction with statins (inhibit cholesterol function, while these inhibit absorption)
31
What are the common adverse effects of Ezetimibe?
sinusitis, influenza, diarrhea
32
What are the serious adverse effects of Ezetimibe?
angioedema, anaphylaxis, hepatitis (need a healthy liver to lower lipid levels), thrombocytopenia
33
What is the effect of taking Cyclosporine and Ezetimibe?
May increase levels of both drugs as they are both processed through the liver
34
What are the cautions when taking Ezetimibe?
Hepatic Impairment
35
By what factor can you multiply A1C by to get your eAG?
Between 21 and 24
Ex. 6 * 21 = 126
Ex. 10 * 24 = 240
These values correspond to the table provided
36
Why is Metformin the first line drug for DM-2 treatment?
High efficacy, low hypoglycemia risk, has neutral/loss of weight, low cost
37
What are the main second line DM-2 drugs and why?
DPP-4 Inhibitors and GLP-1 Receptor Agonists
| Because they have similar effects (most importantly weight effects) to Metformin although they are more expensive
38
For DM-2 when do we decide to use Insulin?
When Metformin does not work by itself, in a 2 drug combo or a 3 drug combo. This is the most complex of insulin strategies.
39
What is the average age of onset/diagnosis for DM-1?
Childhood or puberty
40
What is the average age of onset/diagnosis for LADA?
Adults
41
What is the average age of onset/diagnosis for DM-2?
Commonly >35 years of age
42
What is the average age of onset/diagnosis for MODY?
20 - 60 years of age
43
What is the MOA of the Biguanide Metformin [Glucophage]?
Biguanide based; activates AMP-activated protein kinase (AMPK) which in turn suppresses hepatic gluconeogenesis & intestinal glucose absorption; increases insulin sensitivity
Essentially is helps cells respond better to insulin
44
What are the common adverse effects of Metformin?
Headache, metallic taste, rash
45
What are the serious adverse effects of Metformin?
Lactic Acidosis (CO in bloodstream = toxic), Megaloblastic anemia (reduced oxygen transport to eye)
46
What are the main drug interactions of all Diabetes drugs?
Fish Oils, Decongestants, Steroids - antagonistic (increase blood sugar)
Flaxseed Oil - Additive
Beta-Blockers - Mask Hypoglycemia
NSAIDs - prolonged effect
47
Which drugs when taken with Metformin cause induced lactic acidosis?
Aminoglycosides, amphotericin, ganciclovir, acyclovir due to nephrotoxicity
48
What is the MOA of the Sulfonylurea Glipizide [Glucotrol]?
It is a Sulfonylurea which stimulates pancreatic islet beta cell insulin release through a Ca++ dependent pathway
49
What are the common adverse effects of Glipizide?
headache, photosensitivity, hypoglycemia
50
What are the serious adverse effects of Glipizide?
Death due to cardiovascular complications
51
What is the MOA of Thiazolidinedione/TZD/Glitazone Pioglitazone [Actos]?
Insulin sensitizer selectivity stimulates nuclear receptor PPAR which increases insulin sensitivity in the liver, skeletal muscle and adipose tissue
52
What are some additional effects that can happen when messing with the PPAR pathway?
Increasing sensitization of insulin, creation of ROS, and creation of substances integral in inflammation
53
What are the common adverse effects of Pioglitazones?
Fluid retention, weight gain (due to pulling lipids out of the bloodstream), headache, sinusitis, pharyngitis, dyspnea
54
What are the serious adverse effects of Pioglitazone?
Diabetic macular edema (due to fluid retention), bladder cancer (lawsuits)
55
What is the MOA of the DDP-4 Inhibitor Sitagliptin [Januvia]?
Inhibits DDP-4, slowing incretin (GI hormone secreted while eating) breakdown, insulin synthesis/release, decreasing glucagon levels
56
What are the common and adverse effects of Sitagliptin?
Common - headache
| Serious - renal failure, SJS
57
What is the MOA of the SGLT-2 Inhibitor/Gliflozin Canaglifozin [Invokana]?
Inhibits sodium-glucose cotransporter 2, reducing glucose reabsorption & increasing urinary glucose secretion
The kidney eliminates sugar from the bloodstream resulting in more urination, thirst and dehydration
58
What are the common adverse effects of Canaglifozin?
Increased urination, thirst and dehydration
59
What are the serious adverse effects of Canaglifozin?
Orthostatic hypotension, fractures, bone density loss (loss of electrolytes like Ca due to increased urination)
60
What additive effect can Ophthalmic Beta Blockers have when taken with Canaglifozin?
Additive risk of hypotension
61
What is the MOA of the GLP-1 Agonist Dulaglutide [Trulicity]?
Activates glucagon-like-peptide-1 receptor on beta cells, increasing insulin secretion, decreasing glucagon secretion and delaying gastric emptying (incretin mimetic)
62
What are the common and serious adverse effects of Dulaglutide?
Common - tachycardia
| Serious - hypersensitivity, thyroid carcinoma
63
What is the MOA of Insulin Glargine [Lantus, Youjeo]?
Slow release, micro-crystalized rDNA insulin analog for stable day long blood sugar regulation to be used in post-prandial combination with fast acting insulin
Insulin stimulates peripheral glucose uptake and inhibits gluconeogenesis, lipolysis and proteolysis
64
What are the common adverse effects of Insulin Glargine?
Hypoglycemia, local lipodystrophy, pruritus (due to crystals?), weight gain, edema
65
Should insulin be taken after its expiration?
No, it is one of the few drugs that is not recommended to be taken after its expiration date
66
What is the biggest caution to consider when taking Insulin Glargine?
Infection b/c it causes your body to go into fight or flight which dumps glucose into the bloodstream. If the pt has poor glucose regulation, they will have an augmented reaction to any infection
67
When Beta 2 is stimulated how does it affect the liver and kidneys?
Hepatic - causes glycogenolysis and gluconeogenesis
| Pancreatic - causes increased insulin released
68
When Alpha 2 is stimulated how does it affect the kidneys?
Decreased insulin release
69
What is the MOA of the Proton Pump Inhibitor Esomeprazole [Nexium]?
Irreversibly inhibits gastric parietal cell H+-K+-ATPase inhibiting gastric acid secretion
Histamine, ACh, PG's and gastrin all cause activation of the the proton pump, esomeprazole blocks all of these
70
What are the common adverse effects of Esomemeprazole?
Headache, constipation or diarrhea, xerostomia, flatulence
71
What at the serious adverse effects of Esomeprazole?
SJS, TEN
72
What are the drug interactions to consider when prescribing Esomeprazole?
Impaired absorption of Azole Antifungals and Certain Antiviral Agents (take with acidic drink to enhance absorption)
Azole Antifungals - impaired metabolism
CAIs: exacerbation of hypomagnesemia
73
What is the MOA of the H2 Receptor Blocker Cimetidine [Tagamet]?
Selective antagonism of gastric parietal cell H2 receptors
74
What was the first H2 receptor blocker found?
Cimetidine
75
What are the common adverse effects of Cimetidine?
Headache, dizziness
76
What are the serious adverse effects of Cimetidine?
Food and drug allergies (GI not used to undigested food, similar to trying to breath water), blood dycrasias, psychosis, depression, reversible impotence, gynecomastia
77
What are the drug interactions to consider when prescribing Cimetidine?
Impaired absorption of azalea antifungals/certain antivirals
Impaired metabolism of caffeine (NSAID + Caffeine)
Impaired metabolism of cyclosporine
78
What are the common causes of Gatric/Peptic Ulcers?
Excessive hydrochloric acid secretion
Helicobacter pylori infection
NSAID toxicity
Inadequate mucosal defense against gastric acid
79
What is the cause of Gastric-Esophageal Reflux Disease (GERD)?
Excessive hydrochloric acid secretion
80
What is the MOA of the thyroid therapy Levothyroxine Sodium?
Synthetic T4 (tetra-iodothryonine)
81
What are the common adverse effects of Levothyroxine Sodium?
Basically it would induce hyperthyroidism
Weight loss, diaphoresis, headache, alopecia, hypertension, pseudo tumor cerebra in children (swelling of the optic nerve due to ICP), hallucination
82
What are the ocular adverse effects of Levothyroxine Sodium?
Myasthenia graves like symptoms - diplopia, ptosis, EOM paresis
83
What are the drug interactions to consider when prescribing Levothyroxine?
Sympathomimetics (phenylephrine) - additive
| Sympatholytics - antagonistic
84
What is the MOA of the Menopausal Therapy Estrone [Menest]?
Binds to estrogen receptors, developing and maintaining female sex characteristics and reproductive systems
85
What are the common adverse effects of Estrone?
Headache, migraine, elevated BP, weight changes, fluid retention, contact lens intolerance (eyes to dry), vision changes.
86
What are the Black Box Warnings for Estrone?
Endometrial cancer, stroke, DVT, MI and Invasive Breast Cancer
87
What are the drug interactions to consider when prescribing Estrone?
Azole Antigungals - impaired metabolism
Adverse effects of steroids may be increased
Anti-hyperlipidemic effects of Omega-3FA's may be antagonized
88
What are the contraindications of Estrone and Yaz?
Hypertension, Smoking, Migraine (with aura > without aura)
89
What is the MOA of the contraceptive drug Drospirenon/Ethinyl Estradiol [Yaz]?
Suppresses LH & FSH, inhibiting ovulation; alters cervical mucous and endometrium
90
What is the dosing schedule of Yaz?
It is monophasic meaning you take it as one constant dose throughout the entire cycle
91
What are the common adverse effects of Yaz?
Headache, weight changes, BP elevated, increased cholesterol, contact lens intolerance
92
What are the severe adverse effects of Yaz?
MI, stroke, ocular lesions
93
What are the Black Box warnings associated with Yaz?
Smoking and CV events
94
What are the drug interactions associated with Yaz?
Impaired metabolism of Cyclosporine
NSAIDs - additive hyperkalemia
Tetracyclines, penicillins, cephalosporins, macrolides, quinolones - decreased efficacy
Ascorbic acid - decreased metabolism
95
What are the MOA of the Selective Estrogen Receptor Modulator (SERM) Tamoxifen [Soltamox]?
Binds to estrogen receptors, producing estrogenic and anti-estrogeni effects
96
What are the common adverse effects of Tamoxifen?
Dizziness, headache, VA changes
97
What are the severe adverse effects of Tamoxifen?
Thromboembolism, stroke, pancytopenia, retinopathy, cataracts
98
What are the drug interactions to consider when prescribing Tamoxifen?
May increase cyclosporine, systemic steroid, oxycodone levels
Chlorpheniramine, macrolides - inhibit hepatic production of active metabolites
99
What is the dosing for each indication for the osteoporosis drug Alendronate [Fosamax]?
Osteoporosis - 35 - 70mg awk
| Paget's Bone Disease - 40 mg qd x 6 months
100
What are the adverse effects of Alendronate?
Common - photosensitivity
| Serious - angioedema, uveitis (risk in new users/women), scleritis
101
What are the drug interactions to consider when prescribing Alendronate?
NSAIDs - additive GI irritation
102
Describe the pathology and relative incidence of Osteoporosis.
Characterized by a reduction in bone density and structure, increasing the risk of fracture.
Commonly seen in post-menopausal women vs age-related senile causes; both effect females 2X more than males
Iatrogenic causes include steroids, some anti-epileptic agents, anticoagulants, PPI's, thiazolidinediones and lithium
103
What are the most common cancers responsible for cancer-related deaths?
Males - 28% lung and bronchus, 10% prostate
| Females - 26% lung and bronchus, 14% breast
104
What are the most common causes of newly diagnosed cancer cases?
Men - 28% prostate, 14% lung and bronchus
| Female - 29% breast, 14% lung and bronchus
105
What are the indications of Methotrexate [Trexall]?
Rheumatoid arthritis, psoriasis, choriocarcinoma
106
What is the dosing schedule for Methotrexate?
RA, Psoriasis - 7.5 - 25mg PO qwk
| Choriocarcinoma - 15 - 30 mg PO qd x 5d
107
What is the MOA of Methotrexate?
Acts on folic acid analogue, inhibits DHFR, thus preventing formation of FH4 (sulfas & trimethoprim follow this pathway)
Inhibits lymphocyte proliferation
Anti-inflammatory effects mediated by adenosine pathways
108
What are the common and severe adverse effects of Methotrexate?
Common - photosensitivity, pruritus, anemia, dizziness
| Serious - nephrotoxicity
109
What are the Black Box warnings associated with Methotrexate?
Deaths reported; monitor bone marrow (reduction of immune cells opening up to infection), liver, lung & kidneys; opportunistic infections, potentially fatal myelosuppression w/ NSAIDs (two drugs put together put too much stress on the kidneys)
110
What are the drug interactions to consider when prescribing Methotrexate?
NSAIDs, Sulfa, Cipro, Penicillins - reduced renal elimination
Tetracyclines - elevated levels
Cyclosporine - reduced hepatic metabolism
Ganciclovir - additive myelosuppression
Systemic Corticosteroids - additive immunosuppression
111
Describe the underlying pathological process responsible for Emesis.
A protective mechanism that eliminates harmful substances from the GIT.
There are two brainstem sites: the chemoreceptor trigger zone (outside BBB), the emetic center (protected by BBB)
112
What kind of drugs will be anti-emetics?
Drugs that induce fight or flight like steroids, anticholinergics, antihistamines.
Benzodiazepines stimulate GABA creating an overall inhibitory effect making it a low anti-emetic
113
What is the emetic potential of Methotrexate?
Low
114
Why is Promethazine prescribed?
It is an antihistamine by design, used as an antipsychotic previously
Since antihistamines have anticholinergic effects it is an effective anti-emetic
115
Why is Ondanestrone prescribed?
Made specifically for X-ray & chemotherapy related N & V making it the most likely anti-emetic patients on chemo will be on
116
What is the MOA of the H1 Antagonist Promethazine [Phernergan]?
Non selective central and peripheral H1 antagonist
| Some D2 antagonism exists
117
What is the MOA of the D2 Antagonist Chlorpromazine [Thorazine]?
Selective D2 Antagonist
118
What is the MOA of the 5-HT3 Antagonist Ondanestron [Zofran, Zuplenz]?
Selectively antagonizes 5-HT3 receptors
119
What are the common adverse effects of Promethazine?
Drowsiness, blurred vision, confusion, dermatitis, photosensitivity
120
What are the serious adverse effects of Promethazine?
Thrombocytopenia, agranulocytosis
121
What are the Black Box Warnings associated with Promethazine?
Respiratory depression, severe tissue injury (gangrene)
122
What are the drug interactions commonly associated with Promethazine and Chlorpromazine?
Macrolide's, Azoles, CAIs - prolonged Qt segment
Pilocarpine - antagonistic
Impaired metabolism of Beta-Blocker (liver)
Anticholinergics, sedating antihistaminic, olopatadine nasal - additive
Seizure risk w/ Omega-6FA (no explanation) > only for Promethazine
123
What does dosing look like for Chlorpromazine?
Takes 10 - 20 times more to treat psychosis which is why they look like zombies
124
What are the common adverse effects of Chlorpromazine?
Drowsiness, blurred vision, ocular pigmentation, photosensitivity
125
What other drugs do you see ocular pigmentation as a side effect in?
Prostaglandin Analogs
| Phenylephrine (adenochrome deposits from phenylephrine)
126
What are the serious adverse effects of Chlorpromazine?
Blood dycrasias
127
What are the common adverse effects of Ondanestrone?
Headache, urinary retention, constipation
128
What are the serious adverse effects of Ondanestrone?
SJS, TEN, Serotonin Syndrome
129
What are the very unique ocular adverse effects of Ondanestrone?
Transient Blindness, Oculogyric Crisis (bilateral upward deviation)
130
What are the drug interactions considered when prescribing Ondanestrone?
Macrolide's, steroids, opioids, fluoroquinolone - prolonged QT
