FINALđ Flashcards
What does each stage of hemostasis target?
Primary
Secondary
Fibrinolysis
Primary = platelets Secondary = clotting factors Fibrinolysis = plasmin
What drugs are antiplatelets?
..there are 6
PAR1 blockers PDE inhibitors COX inhibitors P2Y12 inhibitors SSRIs GP2b3a inhibitors
What is the MOA of Vorapaxar?
AEs?
PAR-1 blocker: reversible inhibition of platelet thrombin Râs
AEs: rarely usedâŚ
What is the MOA, uses, and AEs of dipyridamole and cilostazol?
PDE inhibitors: raise cAMP, resulting in vasodilation, inhibition of platelet activation
Uses: tx thrombocytosis (leukemia)
AEs: inhibit megakaryocyte development + dec. platelet #
What is the MOA, AEs, and use of aspirin?
Irreversibly inhibits COX 1 + 2
AEs: inc. bleeding risk
Use: anti-thrombotic
Whatâs the MOA, AEs, use of nonselective NSAIDs?
Reversible inhibit COX 1 + 2
BLOCK ASA BINDING SITE
AE: inc bleeding risk; dec. efficacy of ASA
Use: NOT used as anti-thrombotic
Whatâs the MOA, AEs of selective NSAIDs?
Reversible inhibit COX2»_space; 1
AE: inc. clotting risk
What do P2Y12 inhibitors do?
Block ADP (for platelet activation)
What is another name for irreversible P2Y12 inhibitors?
Irreversible = thienopyridines
Whatâs the MOA/interactions for Clopidogrel?
Irreversible P2Y12 inhibitor
PRODRUG - 2 STEP PROCESS = SLOWEST ONSET
DDI: omeprazole
Whatâs MOA/interaction of prasugrel?
Irreversible P2Y12 inhibitor
PRODRUG - 1 STEP = FASTER ONSET
DDI: fewer
What are the MOA/limitations of Ticagrelor?
Reversible P2Y12 inhibitor - active drug/metabolite
Requires BID dosing
MAX 81mg ASA
What are the MOA/limitations of Cangrelor?
Reversible P2Y12 inhibitor - drug active
FASTEST on/off
Interferes w/ thienopyridines
IV ONLY
$$$
Whatâs the MOA/AE/use of SSRIs?
Inhibit platelet activation by serotonin
AE: inc. risk of bleeds
NOT used as anti-thrombotic
What does GP2b3a do?
Helps platelets bind vWF and fibrinogen to stick to each other or vessel wall
What are MOA/elimination/onset of Abciximab?
GP2b3a inhibitor: persistent binding to receptor (host ABâs may dec. efficacy)
Elimination: proteolytic
effect up to 7 DAYs
$$$
What are MOA/elimination/onset of Eptifibatide?
GP2b3a reversible inhibitor (not immunogenic)
Elimination: renal
Effect 4-8 hours
$$
What are MOA/elimination/onset of Tirofiban?
GP2b3a reversible inhibitor (not immunogenic)
Elimination: renal
Effect 4-8 hours
$
Whatâs the MOA/admin/elimination/titration of DABIGATRAN?
direct thrombin (CF II) inhibitors PO - BID Elimination: renal (t1/2: 12-17 hrs) NOT titration but may inc. PTT/INR NO effect on anti-Xa
What is the reversal agent for DABIGATRAN?
Idarucizumab
Whatâs the MOA/admin/elimination/titration of BIVALIRUDIN?
Direct thrombin (CF II) inhibitor IV - continuous Elimination: proteolytic (t1/2 = 25 min) Titration w/ PTT (may inc. INR) NO effect on anti-Xa
Whatâs the MOA/admin/elimination/titration of Argatroban?
Direct thrombin (CFII) inhibitor IV - continuous Elimination: hepatic (t1/2 = 40-50 min) Titrated w/ PTT (may inc. INR) NO effect on anti-Xa
What is the reversal agent for factor Xa inhibitors?
Andexanet alfa
Whatâs the MOA/admin/elimination/titration of Rivaroxaban?
Factor Xa inhibitor - PO/ qD or BID Elimination: hepatic (t1/2 = 5-9 hrs) NOT titrated (but may inc. PTT, INR, anti-Xa)
Whatâs the MOA/admin/elimination/titration of Apixaban?
Factor Xa inhibitor - PO/ BID Elimination: hepatic (t1/2 = 12 hrs) NOT titrated (may inc PTT, INR, anti-Xa)
Whatâs the MOA/admin/elimination/titration of EDOXABAN?
Factor Xa inhibitor - PO/ qD Elimination: renal + hepatic (t1/2 = 10-14 hrs) NOT titrated (may inc. PTT, INR, anti-Xa)
LESS EFFECTIVE IF CrCL > 95
What does Anti-thrombin (ATIII) do?
Made by liver, circulates in blood and inhibits CFs by binding in stable 1:1 complex
Inhibits Xa unbound to platelets and IIa unbound to fibrin
Whatâs the MOA/AE/elimination/admin of unfractionated heparin (UFH)?
Allosteric activation of ATIII - complex formed w/ thrombin + Xa
IV or SQ
Elimination: reticuloendothelial system (macs, ECs) = no renal adjustment
AEs: HIT; osteopenia (prolonged use)
What is the reversal agent for UFH?
Protamine
How is UFH monitored?
PTT
Whatâs the MOA/AE/elimination/admin of Enoxaparin, Dalteparin?
LMWH: more uniform mixture that binds Xa»_space; IIa
Elimination: renal
QD or BID
AE: lower HIT
Whatâs the reversal agent for LMWH?
Protamine
Whatâs the MOA/AE/elimination/admin of fondaparinux?
Stimulates ATIII to inhibit Xa only QD dosing (longest t1/2) SQ Elimination: renal AE: does NOT cause HIT
How is fondaparinux monitored?
Anti-Xa
Whatâs the MOA/AE of Warfarin?
inhibits VKOR: dec. vitamin K and prevents activation of CFs
AEs: skin necrosis âpurple toe syndromeâ
Teratogenic, genetic variability
Describe what happens in days 1 and beyond on warfarin
Day 1: liver makes fewer CFs, but those already in circulation unaffected
Day 2-4: INR beings inc. - if protein S/C depleted = hyperCOAGUABLE
Days >5: anticoagulation
What are the t1/2s of CF depletion under warfarin?
VII = 4-6 hrs greatest effect on INR
C = 8 hrs S = 30 hrs X = 48 hrs II = 72 hrs
What are DDIs associated with warfarin
CYP inducers = dec. INR = inc. clotting
(Carbamazepine, phenytoin, rifampin, phenobarbital, CHRONIC EtOH)
CYP inhibitors = inc. INR = inc. bleeding
(Amiodarone, fluconazole, acute EtOH)
Antiplatelets/anticoagulants = no change INR ; inc. bleeding
What are disease interactions with warfarin?
Sensitive: hyperthyroidism, decompensated HF, liver disease, malnourishment, low albumin, low body weight
Resistant: hypOthyroidism, high body weight
Whatâs the MOA and use of citrate?
Dec. Ca (required for CFs to localize to membrane)
Use: anticoagulation of stored blood/blood circuits
What is the MOA/use/half-life of alteplase?
Fibrinolytic: binds fibrin and converts plasminogen to plasmin in order to break up clot
Use: acute ischemic stroke
SHORT t1/2
What is the MOA/use/half-life of tenecteplase?
Fibrinolytic: more specific binding to fibrin and more resistant to plasminogen activator inhibitor (PAI-I)
Use: MI
Longer t1/2 = SINGLE BOLUS
Whatâs the MOA/use of desmopressin (DDAVP)?
Binds V2 Râs to trigger release of stored vWF in order to activate platelets
Use: tx bleeding
Distinguish b/w single vs. multiple vs. blood products for coagulopathy
Single factor products = hemophilias
Multiple = bleeding (warfarin)
Blood products = (liver failure) contain factors AND fibrinogen
What is the MOA/use of aminocaproic acid, tranexamic acid?
Anti-fibrinolytics: competitively inhibit plasmin/plasminogen
Use: control bleeding (surgical, dental, trauma)
What are the irreversible inhibitors (antiplatelets)?
Aspirin
Clopidogrel
Prasugrel
Abciximab
Describe acute management for ischemic stroke
THROMBOLYTICS (for re-perfusion)
Other:
+ secondary prophylaxis (anti-platelets, warfarin, direct oral anticoagulants- DOACs)
+ control BP (nicardipine, beta blockers, hydralazine, NTP)
+ avoid hypErglycemia
Whatâs the thrombolytic/fibrinolytic used for ischemic stroke?
Alteplase
For secondary prophylaxis, what can patients take if allergic to aspirin?
P2Y12 inhibitors
Whatâs the MOA/AE for nicardipine?
DHP-CCB prevents release of internal Ca stores so heart muscle doesnât respond to signal = vasodilation
IV 1st line for BP CONTROL IN STROKE
AE: headache, peripheral edema, hypOtension, tachycardia, N/V, flushing
Whats AE/DDI for beta blockers?
Angina, bronchospasm, insomnia/depression/fatigue/ dec. HDL and inc. TG
DDI: other AV blocking or anti-HTN agents
Differentiate MOA of Esmolol vs. Labetalol
(For stroke)
Esmolol: beta1 selective = dec. BP/HR
Labetalol: beta1/2, alpha1, partial beta2 agonist = dec. BP/HR and arterial vasodilation (alpha, beta2)
Whatâs the MOA/AEs for hydralazine?
Directly relaxes arteriolar smooth muscle; may dec. calcium to dec. contraction; vasodilation
AE: headache, hypotension, fluid retention, palpitations, tachycardia
DRUG-INDUCED LUPUS SYNDROME ..typically resolves w/ DC
Whatâs the MOA/AE/caution for nitroprusside (NTP)?
NO will activate guanylate cycylase to inc. cGMP in vascular smooth muscle = venous/arteriolar dilation = dec. AL/BP
AE: hypotension, CN toxicity, thiocyanite toxicity (tinnitus, tremor)
RISK WITH RENAL DISEASE
What products can be given for life threatening/serious bleeding?
Vitamin K
Prothrombin complex concentrates (PCC) = Kcentra
Fresh frozen plasma (FFP) blood group specific
Idarucizumab
What BBW is associated with vitamin K?
IV admin = risk of anaphylaxis
What AEs are associated with idarucizumab?
Hypokalemia, delirium, constipation, pyrexia hypersensitivity, thrombosis
What can be given for subarachnoid hemorrhage?
Aminocaproic acid
Nimodopine
What is the MOA/AE of aminocaproic acid?
Blocks plasmin:fibrin interaction to inhibit fibrinolysis
AE: hypOtension, bradycardia, myopathy
Whatâs the MOA/AE of nimodopine?
DHP-CCB = arterial vasodilation
AE: hypotension, headache, flushing, edema, nausea, sinus bradycardia
Which beta lactams are not renally eliminated and therefore do not need dose adjustments?
Nafcillin
Oxacillin
Ceftriaxone
What cephalosporins pass BBB and can be used to treat meningitis?
Cefuroxime
Ceftriaxone
Cefotaxime
Ceftazidine
What cephalosporins can be used to tx anaerobic (B. Fragilis) infections?
Cefoxitin
Cefotetan
What PCN is not impaired by food when administered?
Amoxicillin
What AEs associated with PCNs?
+Hypersensitivity: skin rash, fever, joint swelling, pruritis, leukopenia, anaphylaxis
+GI: D (killed flora)
What does Ceftaroline treat and not treat?
Only beta lactam to tx MRSA
Does NOT treat pseudomonas
What AEs are associated with CSNs?
Hypersensitivity, GI distress,
Intolerance to EtOH (Cefotetan inhibits ADH)
Potentially nephrotoxic (mainly 1st gen)
Which CSNs could be used for surgical prophylaxis?
1st gen = Cefazolin, cephalexin
How is aztreonam administered?
IV
Use if allergic to PCN or CSN
Which carbapenem is coadministered with cilastatin?
Imipenem
What AEs are associated with Carbapenems?
GI, hypersensitivity, CNS: seizures (imipenem)
What AEs are associated with vancomycin?
Hypersensitivity âRED MAN SYNDROMEâ - cx by histamine
Ototoxicity (mainly when combined w/ aminoglycosides)
What is daptomycin used to treat?
VRE, MRSA, VRSA
NOT used in pneumonia - inactivated by surfactant