736 Top Drugs 2023 copy.pdf

736 Top Drugs 2023...

736 Top Drugs 2023 1 of Brand Indication(s) Adjust Route Boxed warning Contraindications Side Effects Major DDI Other Comments Direct Thrombin Inhibitors: Directly inhibits thrombin (Factor IIa). Binds to the active thrombin site of free and clot-associated thrombin. DVT/PE Treatment and Prodrug Prevention, Nonvalvular A- Premature Discontinuation, Active Bleeding, Mechanical Bleeding risk Do not break, chew, or open capsule Dabigatran Pradaxa R PO Common: Dyspepsia, Gastritis-Like Symptoms, Bleeding Fib (Reduce Stroke Risk), Spinal/Epidural Hematoma Prosthetic Heart Valves PGP inx Take with a full glass of water Thromboprophylaxis Idarucizumab (Praxbind)=antidote Common: bleeding, anemia, hypotension, chest pain, HIT, PCI -thrombosis and Bleeding risk Argatroban H IV Active major bleed HA, N/V/D, dyspnea, backache, fever Increase in INR is seen independent of warfarin use with risk for HIT warfarin (increase INR) Serious: hemorrhage, cardiac arrest, sepsis Common: hypotension, HA Bivalirudin Angiomax PCI - thrombosis R IV Active major bleed Bleeding risk Safe to use in HIT. Serious: Vfib, retroperitoneal/intracranial bleeding Factor Xa Inhibitors: Reversible and selective active site inhibitor of Factor Xa, resulting in decreased thrombin generation and thrombus formation. If patient is 80 years or older and weighs 60 kg or less or DVT/PE Treatment and has a SCr of 1.5 or more, reduce the dose to 2.5mg BID Prevention in Nonvalvular A-Fib Apixaban Eliquis R PO Nonvalvular A-Fib (Reduce Avoid grapefruit juice Stroke Risk) Andexanet alfa (Andexxa), Prothrombin complex Bleeding risk concentrate (Kcentra)= antidotes Premature Discontinuation, Common: bleeding Active Bleeding CYP3A4 inx Spinal/Epidural Hematoma Serious: GI bleeding, hemorrhage, increased LFT's DVT/PE Treatment and PGP inx Prevention Administer 15 and 20mg tablets with food Nonvalvular A-Fib (Reduce Edoxaban is an alternative agent Rivaroxaban Xarelto R PO Stroke Risk) Andexanet alfa (Andexxa), Prothrombin complex Risk reduction of major CVD concentrate (Kcentra)=antidotes events in CAD/PAD Glycoprotein IIb/IIIa Inhibitor: inhibits platelet aggregation by specifically binding to GPIIb/IIIa and preventing fibrinogen CVA within 30 days, active Common: chest pain, hypotension, injection site abnormal bleeding, Percutaneous coronary reaction, hemorrhage, NV Eptifibatide Integrilin R IV surgery/trauma within 6 weeks, Bleeding risk Alternative IV agent: abciximab (no longer in market) intervention, adjunct Serious: thrombocytopenia, anaphylaxis, CVA, severe HTN (SBP >200 mm Hg or intercranial hemorrhage DBP>110mm Hg), renal dialysis Unfractioned Heparin: Binds to antithrombin (AT), which then inactivates thrombin (Factor IIa) and Factor Xa. Also prevents the conversion of fibrinogen to fibrin. ACS, VTE treatment, VTE Severe Thrombocytopenia, HIT Common: Thrombocytopenia, increased LFT's prophylaxis Fatal medication errors- check dosage Heparin N IV, injection History, Uncontrolled Active Serious: Bleeding, HIT, Bleeding risk Flush: maintain patency of Protamine=antidote Bleeding (Except for DIC) Hyperkalemia, Osteoporosis (Long Term Use) IV device Low Molecular Weight Heparin: Bind to AT and have greater affinity of inhibiting Factor Xa than Factor IIa. Active Major Bleed, Thrombocytopenia associated ACS, VTE treatment, VTE Subcut, Spinal/Epidural Hematomas: May with positive antiplatelet antibody Common: Anemia, Increased LFTs, Thrombocytopenia More predictable anticoagulant response than UFH, and Enoxaparin Lovenox R Bleeding risk prophylaxis injection result in long-term paralysis. in the presence of Enoxaparin, Serious: Bleeding, pneumonia, hyperkalemia does not usually require Anti-Factor Xa levels Hypersensitivity (Heparin, Pork, Benzyl Alcohol) Vitamin K Antagonist: Competitively inhibits vitamin K reductase (VKORC1), which reduces Vitamin K epoxide and causes depletion of Factors II, VII, IX, X, Proteins C and S. Pregnancy (except mechanical S-enantiomer being more potent. Common: Minor bleeding Bleeding risk heart valves at high Initial dose in healthy outpatients: 10mg daily X 2 days. Serious: Hemorrhage, skin necrosis, purple toe CYP2C9 inx thromboembolism risk) or pre- Start warfarin on the same day as the parenteral Coumadin Fatal bleeding (Vitamin K is the syndrome CYP1A2 inx Warfarin Anticoagulation N PO eclampsia, Hemorrhagic anticoagulant; continue both minimum of 5 days and INR Jantoven antidote) Tablet colors: Please Let George Bush Bring Peaches CYP3A4 inx Tendencies, Blood Dyscrasias, is 2 or greater for X 24 hours. To Your Wedding (1, 2, 2.5, 3, 4, 5, 6, 7.5, 10 mg: pink, Amiodarone; Bactrim; Metronidazole; Uncontrolled HTN, Antidotes: Phytonadione (Vitamin K), Prothrombin lavender, green, brown, blue, peach, teal, yellow, white) Most antibiotics; Vitamin K Noncompliance, Major surgery complex concentrate (Kcentra) NSAIDS: inhibition of platelet function by acetylation of the platelet cyclooxygenase (COX) resulting in the irreversible blockade of the formation of thromboxane A2 Children/teens for viral infection S/s of toxicity: tinnitus cardioprotection, pain, fever, Aspirin Bayer N PO, rectal Severe skin rash: stop Bleeding risk Food and water minimize ADRs. OA, RA immediately Dipyridamole/Aspirin- Aggrenox 736 Top Drugs 2023 2 of P2Y12 Inhibitors: Irreversibly inhibit P2Y12 (On ADP Receptors) on platelets, which results in inhibition of platelet activation and aggregation. ACS, Stroke, Established Prodrug, CYP2C19 poor Bleeding risk Stop 5 days before elective surgery Clopidogrel Plavix N PO Active bleeding PAD metabolizers CYP2C19 inx Avoid grapefruit juice Not recommended in patients 75 years and older unless ACS patients managed with Active bleeding, history stroke or Prasugrel Effient N PO Fatal bleeding Bleeding, Hematoma, Pruritus (Clopidogrel) Bleeding risk high risk PCI TIA Dyspnea, Increased SCr and Uric Acid (Ticagrelor) Stop 7 days before elective surgery Fatal bleeding, Aspirin doses Active bleeding, severe hepatic Bleeding risk Stop 5 days before elective surgery Ticagrelor Brilinta ACS N PO greater than 100 reduce impairment CYP3A4 inx Avoid grapefruit juice effectiveness Fibrinolytics: Breaks down clots by binding to fibrin in a thrombus and converting plasminogen to plasmin. 2nd Generation, due to clot-specific binding. Acute ischemic stoke, PE, Alteplase Activase N IV, injection Risk of bleeding Bleeding risk STEMI Serious: arrhythmias, intracranial hemorrhage, Tenecteplase TNKase STEMI N IV Risk of bleeding angioedema Bleeding risk Reteplase Retavase STEMI N IV Risk of bleeding Bleeding risk urine volume and increases osmolality. Can also cause smooth muscle contraction in the GI tract by V1 stimulus which releases prolactin and ACTH via V3 receptor. Common: Bradyarrhythmia, Tachyarrhythmia increases factor VIII levels and may be useful in Cardiogenic shock, septic Serious: Afib, MI, Hemorrhagic shock, Increase Bilirubin, Vasopressin Vasostrict N IV hemophiliacs shock Anaphylaxis, Limb Ischemia, Pulmonary edema, Water toxicity ADH Inhibitor: V2 receptor antagonist. Inhibits ADH medicated water reabsorption in the distal tubule Common: Increased ALT/SGPT levels, increases thirst, Autosomal dominant eGFR