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38 Cards in this Set
- Front
- Back
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Clopidigrel |
P2Y12 Receptor antagonist PRODRUG (extensive acitvation by CYP450) Irreversible binding Direct Binding |
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Prasugrel |
P2Y12 Receptor Antagonist Prodrug (moderate activation by CYP450) Irreversible, direct binding |
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Ticagrelor |
P2Y12 Receptor Antagonist NON PRODRUG Reversible Indirect binding = ADRs ADRs: SOB, Brady, arrythmia |
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Vorapaxar |
PAR1 Antagonist Prevents amino tail from associating w/ receptor PAR1 receptor is like Gq and Gi (increases Ca decreases cAMP) |
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Abiximab (Reopro) |
GPIIb/IIIa Antagonist Irreversible Vitronectin Antagonists (pro-coag) Pre/Intra angioplasty and stent placement |
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Tirofiban (Aggrastat) |
GPIIb/IIIa Antagonist Reversible Peptide, given IV |
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Eptifibatide (integrilin) |
GPIIb/IIIa Antagonist Reversible Small Molecule |
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TxA2 Receptor and effect |
Receptor: TPalpha and TPbeta Both- gq = increased Ca2+ Ligand: ? |
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ADP Receptor and effect |
P2Y1: Gq = Increased Ca2+ P2Y12: Gi = Decreased cAMP Activation of both exposes GpIIb/IIIa Receptors Ligand: ? |
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Thrombin Receptor and effect |
PAR1: Protease Activated Receptor 1 LIGAND binds extracellular portion, cleaves amino tail= folding upon itself = activated receptor => increased Ca2+ and decreased cAMP Ligand: ? |
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Fibrinogen/Fibrin Receptor and effect |
GpIIb/IIIa: Exposed when P2Y1 and P2Y12 bound and levels of Ca increase and cAMP decrease. LIGAND binds receptors on multiple platelets creating crosslinks between platelets. LIGAND: ? |
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PDE-3 Location, effect, use as drug target |
Phosphodiesterase found in platelets and cardiac myocytes.
Degrades cAMP = pro aggretory Inhibition = Increased cAMP= anti-agg and vasodilation also increased Ca in myocytes = risk of arrhythmias |
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Dipyridamole MOA (2), Indications |
MOA: PDE-3 inhibition = anti agg, anti-arryth. Adenosine transport inhibitor= increased ADP =increased A2 binding = vasodilation Indications: TIA/CVA prevention, MI prevent |
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Cilostazol MOA, Indications, Contra |
MOA: PDE-3 inhibitor Indications: PVD (intermittent claudication) CONTRA: HF and arrhythmia |
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Pentoxyifylline MOA, Indication |
MOA: Rheulogic modifier, makes RBCs more flexible - less aggregation Indication: PVD (intermitten cladication) |
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Anagrelide MOA, indication, ADR |
MOA: Inhibition of Phospholipase A2 in liver = decreased conversion of megakaryocytes to platelets
Indication: Polycythemia ADRs: Neutropenia |
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Unfractionated Heparin MOA (2), Indications, Dosing, ADRs |
MOA: Binds Anti-Thrombin III and Thrombin, catalyzes breakdown of thrombin (x10), inhibits factor Xa = decreased conversion of prothrombin to thrombin
Indications: Post-opp immob, bridge therapy Dosing: Dosed to increase PTT by 2x the unhepranized ADRS: Bleeding, HIT |
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Low Molecular Weight Heparins Members (3), MOA, Indications, Dosing, ROA |
Enoxaparin, Fragmin, Innohep MOA: Binds ATIII and inhibits Xa (no effect on thrombin degredation) Indications: Post Op immob, PREGNANCY Dosing: Based on pts weight, no monitoring ROA: SQ, outpatient |
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Protamine
MOA, Dosing, ADR |
Heparin Antidote
MOA: Binds neutralizes heparin Dosing: Based of plasma hep levels and pTT ADR: Anti-coag effect at high plasma lev, interfers w/ fibrinogen |
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Pentosan
MOA, Indication |
MOA: Binds ATIII decreases factor Xa Indication: Interstitial nephritis ADR: HIT |
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Fondaparinox MOA |
MOA: Binds ATIII and decreases Xa Indirect Xa inhibitor Low chance of HIt |
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Rivaroxiban (Xarelto), Apixiban (Eliquis) MOA, How supplied |
MOA: Direct Xa inhbitiors (decreased prothrombin activation) Oral Tabs No monitoring |
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Direct Thrombin Inhibitors MOA, Indications, Inj (4) and Oral(1) versions |
MOA: Inhibit thrombin from converting Fibrinogen to Fibrin Indications: Anti-HIT therapy, anti-coag therapy in pts w/ hitsory of HIT Inj: Desirudin,Lepirudin, bivalirudin, Agatroban Oral: Pradaxa |
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Coumarins MOA, Dosing, Genomics, Interax, |
MOA: Inhibition of VKORC1 = decreased synthesis of factors II, VII, IX and X Dosing: Initial 5-10mg, base off INR 3-5 later, INR goal of 2-3, DELAYED ONSET Pharmacogenomics: VKORC1 and CYP 2C9 Interactions: Vit K, Cephalosporins, PPB binders, CYP inducers or inhibitors |
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Coumarin Antidote? MOA, Admin, onset |
Phytonadione (Vit K) MOA: Provide more endogenous Vit K for Factor synthesis by VKORC1 Admin: Oral, but availible IV SLOW ONSET due to synthesis of factors Immediate antidote=packed platelets |
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Plasminogen Activation and effect |
Plasminogen activated to Plasmin by the action of tPA secreted by endothelial cells. Plasmin degrades fibrin leading to clot degredation |
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Streptokinase and Urokinase MOA, Indications, ADRS |
MOA: Enzymes produces from strep. bact. or enzyme from neonatal kidney cells that activate plasminogen Indications: Post MI/CVA, thromboembolisms (ASAP) ADRS: Hypersensitivity, Hypotension, Bleeding |
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rTPAs; Alteplase, Retaplase, Tenecteplase MOA, Indications, ADRs |
MOA: Analogues of endogeous tPA, at low levels= selectivity for fibrin in clot but given at high dose Indications: Post MI/CVA, Thromboembolism (ASAP) ADRs: Bleeding (No hypersensitivity or HYPOtension) |
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Tranexamic Acid MOA, Indications |
MOA: Inhibits activation of plasminogen = promotes clotting Indications: Heavy menstraution (taken PO PRN 5d during period |
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Aminocaproic Acid MOA, ROA/indications |
MOA: Inhibits BINDING of plasmin to Fibrin = Pro aggretory
ROA: Topical Soln: Used during surgery to prevent blood loss Oral Soln: Prior to dental work, prevent bleeding |
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Effects of PGE2 (5) |
Smooth Muscle Dilation (vasodilation) Stomach: Increased Mucus Production Nocioreceptors: Sensitization CNS: Sensitization to pain, increased body temp Inflammation: Used as a WBC chemokine (vasodilatory + attractant) |
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COX Isozymes: Where are they found COX-1, Cox-2, COX-3 |
COX-1: Ubiquitous COX-2: Brain, Kidney, Upregulated in inflammation COX-3: CNS (Animal studies) |
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Reyes Syndrome From, symptoms |
Rare Rxn to ASA in: Children <16yo who recently had flu Presentation: Acid/base disturbance, Glucose disturbances, ICP, Seizures, Coma, Convulsions, Liver damage Avoid ASA in <16YO |
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Cystienyl Leukotrienes (4) Members (4) Production Receptor Effect |
Includes LTC4, D4 and E4 AA converted by 5-lipoxygenase to LTA4 LTA4 converted by LTC4 sythase to C4 Non-enzymatic conversion to D4 and E4 Bind CysLT1 receptor = broncho constriction, dilation of nasal capilaries |
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Leukotriene B4 Biosynthesis Receptor Effect |
LTA4 converted by Epoxidehydroxylase to LTB4 LTB4 binds BLT Receptors = neutrophil attractant, and mucus production |
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Zileuton (Zyflo CR) MOA Indication Monitoring |
MOA: Inhibtion of 5-Lipoxygenase, which converts AA => LTA4 Indications: Asthma (not 1st line) Monitoring: LFTs, Pharmacogenomics: SNP of 5 lipoxygenase of LTC4 synthase alters efficacy |
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Montelukast, Pranlukast, Zafirlukast MOA, Indication, admin, adrs |
MOA: CysLT1 Receptor Antagonists Indication: Asthma, seasonal allergies Admin: PO QD ADRs: Upper resp. infection |
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Colchicine MOA, Indication, Dose, ADRs |
MOA: Suppresses activity of WBCs |
