Week 6- Bleedy meds Flashcards
what drug class is nitroglycerine?
nitrate
what drug class is isosorbide dinitrate?
nitrate
what is the mechanism of action of nitroglycerin and isosorbide dinitrate?
Provides nitric oxide to vascular endothelium
Decrease preload and afterload
Increase cGMP = decrease platelet aggregation
what drugs are in the nitrate class?
nitroglycerine and isosorbide dinitrate
common uses of nitroglycerine
Angina
Dilates coronaries to bring more blood flow (less so with atherosclerosis)
Short acting
HF (not 1st line)
which is a short acting nitrate?
nitroglycerine
best route of nitrates and why
sublingual d/t significant first pass effect
which is long-acting nitrate?
isosorbide ninitrate- better sustained nitrate activity and better anginal propy
AKA long acting
side effects of nitrates
headache, N/V, orthostatic hypotension
major adverse effects/warnings with nitrates
Vasodilation increases ICP:
Do not use in head trauma or cerebral hemorrhage
Postural hypotension + syncope
Not used in pregnancy
medication instructions with nitrates
Tabs lose potency with air heat and moisture
also tolerance can occur so start low and go slow
drug interactions w/ nitrates
anti-HTNs. Etoh, CCBs. haldol (anything that decreases BP)
Sildenafil/ Viagra: Profound Hypotension ***
what drugs are reductase inhibitors?
atorvastatin and rosuvastatin
what drugs are bile acid sequestrants?
cholestyramine
what drug class is atorvastatin
reductase inhibitor
what drug class is rosuvastatin
reductase inhibitor
what drug class is cholestyramine
bile acid sequestarant
how do reductase inhibitors work?
Block synthesis of cholesterol in the liver by competitively inhibiting HMG-CoA reductase activity.
Increase catabolism of LDL and increase in liver’s extraction of LDL reductase.
Also has anti-inflammatory properties (moreso for CV rather than cholesterol)
how does cholestyramine work?
Exchange chloride ions for negatively charged bile acids by the liver. Increases uptake of LDL from plasma results in the upregulation of high-infinity of LDL receptors on cell membranes
what are common uses of atorvastatin and rosuvastatin?
Reduce LDL
First-line in monotherapy and in combos
which reductase inhibitor is most potent
rosuvastatin
which statin is most readily absorbed?
atorvastatin
common side effects of reductase inhibitors
headache and myalgias
black box warning of reductase inhibitors (statins)
possible BG increases along with concentration and memory issues
contraindications and major adverse reactions of statins
acute liver disease, intracerebral hemorrhage
*check LFTs prior to starting
what drugs increase risk of rhabdomylosis
if reductase inhibitors and bile sequestrants are taken together it increases the risk!
med instructions of reductase inhibitors
usually taken in PM
how do bile acid sequestrants/cholestyramine work?
Exchange chloride ions for negatively charged bile acids by the liver. Increases uptake of LDL from plasma results in the upregulation of high-infinity of LDL receptors on cell membranes.
LDL reduced by 10-35%
common uses of cholestyramine
reduce LDL- best for patients with low CV risk and cant reduce LDL by diet
pharmacokinetics of cholestyramine
not absorbed- works in GI tract by binding bile acids
side effects of cholestyramine
constipation– use of laxative
N/V
ADRs of cholestyramine
can reduce folate levels
what drug is a fibric acid derivatives
gemfibrozil
what class is gemfibrozil
fibric acid derivative
how does gemfibrozil work?
Increase lipolysis of triglycerides via lipoprotein lipase (decrease in 50+% of triglyceride levels)
Also decrease in LDL
HLD increased by 15%-25%
First line for elevated triglycerides in women?
use of gemfibrozil
reduce VLDL, best at increasing HDL
major ADRs of gemfibrozil
may increase cholesterol excretion into the bile, D/C if gallstones found.. may also cause anemia
med instructions for gemfibrozil
must be taken before meals
how does ezetimibe work?
Blocks absorption of cholesterol across intestinal border (LDL reduction) Binds with cholesterol in intestine
what is ezetimibe used for
first line for kids with familial hypercholesteremia
how does evolocumab work?
Monocolonal antibody PCSK9 inhibitor. Alter protein activity that transport LDL into the liver
important things to know about evolocumab
super expensive- used with other statins when desired outcome isn’t met
which drugs are anticoagulants
warfarin, heparin, enoxaparin, apixaban, dabigatran
what class is warfarin
anticoagulant
how does warfarin work
Inhibit hepatic synthesis of clotting factors including factor X
what is warfarin used for
Mechanical valve
AFIB
(second line for VTE/PE)
common side effects of warfarin
bleeding, hemorrhagic necrosis of skin, ** hard to DOSE!!!
black box warning of warfarin
do not give to pregnant people, also can cause hyper coagulable state
DDI of warfarin
Do not give with NSAIDs
MANY drug interactions with CYP2C9 inhibitors.. Specifically Amiodarone and Metronidazole
what is antidote of warfarin
vitamin K
what is an important diet teaching of warfarin
watch leafy greens
what drug class is heparin
anticoagulant
how does heparin work
accelerate antithrombin 3 activity
what is heparin used for
DVT, PE, STEMI, NSTEMI, ischemic CVA and DIC
common side effects of heparin
can cause hyperkalemia, caution w/ renal insufficiency or DM
major ADRs/ CI of heparin
Contraindicated in hepatic and renal diseases (advanced)
can cause HITT
antidote of heparin
protamine sulfate
DDI of heparin
PCN IV and cephalosporins increase bleeding risk
what is enoxaparin
low molecular weight heparin (anticoag)
how does enoxaparin work
accelerate antithrombin 3 activity
what is lovenox used for
DVT prophy and/or PE, post-op thromboembolism preention
how is heparin and lovenox given
SC/IV
side effects of lovenox
Bleeding (higher risk for renal patients)… also given SC
ADRs of lovenox
CrCl cut off for lovenox use
what does lovenox interact with
Interacts w/ salicylates, NSAIDs, dipyridamole, sulfinpyrazone, ticlopidine
notable differences between lovenox and heparin
heparin requires more frequent lab monitoring!!!!!!!
what drug class is apixaban?
eliquis- direct factor Xa inhibitor
what is apixaban used for
a.fib
side effects of apixaban
bleeding
BBW of apixaban
increased risk of thrombolytic events upon discontinuation & transitioning to warfarin from direct Xa inhibitor increases the risk of CVA
drug interactions of apixaban
can give without regard to food
watch for ketoconazole, ritonavir and st john’s wort
how is apixaban metabolized
CYP3A4 metabolism :(
what drug class is dabigatran?
anti-coag
how does dabigatran work
direct thrombin inhibitor
what is dabigatran used for
Prevention and treatment of thromboembolism (DVT), stroke/embolism prevention in a fib peeps
pharmacokinetic considerations of dabigatran
absorbed in GI tract, avoid high fat foods, eliminated in urine
side effects of dabigatran
bleeding, GI side effects, angioedma and thrombocytopenia
black box warning of dabigatran and apixaban
BBW: Increased risk of thrombotic events upon discontinuation
DDI of dabigatran
Rifampin, ketoconzaole, verapamil (CCB), plavix, amiodarone, all bleed-y meds
CI of all anticoagulants
Contraindications: Hypersensitivity, active bleeding, hemophilia, thrombocytopenia, severe HTN, intracranial hemorrhage, infective endocarditis, active TB, ulcerative lesions of GI tract
which drugs are antiplatelets
ASA and clopidogrel
what class is aspirin
antiplatelet
what class is clopidogrel (plavix)
antiplatelet
how does aspirin work
Blocks an enzyme called cyclooxygenase, interferes w/ platelet aggregation AKA ~antiplatelet~
impact prostaglandin metabolism
how does clopidogrel work
Reduces platelet aggregation by inhibiting the pathway of platelets
what is aspirin used for
MI and stroke prevention, antithrombotic therapy for ischemic stroke
what is clopidogrel used for
Prevention of new ischemic event (CVS or MI), ACS
pharmacokinetics about clopidogrel
PRODRUG babyyyyyy, converted in the liver to a metabolite that works
side effects of clopidogrel
bleeding (bleeding precautions in place)
side effects of ASA
Normalish ones: GI upset, unusual bleeding (bleeding precautions)
Scary ones:REYE SYNDROME, upper GI bleeding, tinnitis
signs of ASA toxicity
HA, hyperventilation, agitation, confusion, lethargy, diarrhea, sweating
do ASA and clopidogrel require routine labs
no
when is ASA sensitivity higher
in people with asthma
when is clopidogrel contraindicated
hepatic disease, patient should NOT have GI ulcers
DDI of clopidogrel
Other bleed-y meds (anti-coags), PPIs, antiacids, digoxin, theophylline, phenytoin ~drugs that inhibit CYP2C19~, caution w/ natural supplements
DDI with aspirin
Hypersensitivity and cross-sensitivity with NSAIDs, increase bleeding risk w/ anticoagu/antiplatelets, etc
how does oral iron work
supplement- iron makes up hemoglobin
when is oral iron used
Blood loss iron deficiency anemia
(BUT balanced diet is best way to prevent iron deficiency)
side effects of PO iron
GI symptoms better to give with food even through it decreases absorption, can cause dark stool and teeth staining
when is PO iron c/i
Contraindicated in hemochromatosis and hemolytic anemia
DDI of PO iron supplement
Chelation with levodopa penicillamine and quinolones, competitive absorption with antacids, cimetidine, tetracyclines
folic acid mechanism
a supplement- Deficiency related to poor diet, ileal disease or phenytoin use
Increased demand in pregnancy
who is deficiency of folic acid common in
pregnant peeps, alcoholics, liver disease
pharmacokinetics of folate
Folate= nucleoprotein synthesis and erythropoiesis
Produces WBC platelets
side effects of folate
GI side effects
when is folic acid contraindicated
when B12 is low– fix low B12 first
common DDI of folic acid
Sulfonamides, methotrexate and triamterene interfere ith activation
what is vitamin b 12
Necessary for fatty acid synthesis
Necessary for folate synthesis
when is b12 commonly used
malabsorption
Pregnancy
side effects of b12
GI side effects
c/i of b12
hypersensitivity to cobalt
