Pharm Flashcards
Heparin
M: Activates antithrombin (decreases thrombin and factor Xa) – Unfractionated binds antithrombin and thrombin — LMWH (enoxaprin, dalteparin, fondaparinux) act more on factor Xa
C: Immediate for PE, acute coronary syndrome, MI, DVR – okay in pregnancy
T: HIT, osteoporosis – reversal with protamine sulfate
Heparin induced thrombocytopenia
IgG antibodies against heparin-bound platelet factor 4 –> activates platelets –> thrombosis and thrombocytopenia (Tx: Argatroban/Bivalirudin - direct thrombin inhibitors)
Argatroban, bivalirudin, dabigatrin
Inhibits thrombin directly – can be used instead of heparin if suffering from HIT
Warfarin
M: Blocks y-carboxylation of vitamin K factors – affected by mutations in VKORC1 gene
C: Chronic anticoagulation – NOT IN PREGNANCY
T: Bleeding, skin/tissue necrosis, early transient hypercoagulability (start with heparin)
Antidote: Reverse with vitamin K, rapid reversal with fresh frozen plasma
Heparin vs. Warfarin differences
H is parenteral, W is oral — H works in blood, W works in liver — H is acute, W is chronic — H is water soluble, W is lipid soluble (reason to use H in pregnancy)
Direct factor Xa inhibitors
Apixaban, rivaroxaban
C: Treatment/prophylaxis for DVT and PE
Thrombolytics
tPA, rPA, streptokinase, tenecteplase
M: Plasminogen to plasmin, cleaves thrombin and fibrin clots, increases PT/PTT
C: Early MI (within 6 hours), early ischemic stroke, severe PE
T: NO in active bleeding, recent surgery, or severe HTN – Tx toxicity with aminocaproic aicd
Aspirin
M: IRREVERSIBLY inhibits COX1 and COX2 via acetylation – effect lasts 120 days (until new platelets are produced)
C: Antipyretic, analgesic, anti-inflammatory, antiplatelet
T: Gastric ulcers, tinnitus, renal failure, interstitial nephritis, Reye syndrome (microvesicular fatty necrosis in liver of children with virus)
OVERDOSE: Initial respiratory alkalosis then mixed metabolic acidosis-respiratory alkalosis
ADP receptor inhibitors
Clopidogrel, prasugrel, ticagrelor, ticlopidine
M: Inhibit platelet aggregation by irreversibly blocking ADP receptors – prevent IIb/IIIa platelet surface
C: Acute coronary syndrome, coronary stenting
T: Neutropenia
Cilostazol, dipyridamole
M: Phosphodiesterase III inhibitors, increase cAMP in platelets, resulting in platelet aggregation (vasodilators)
C: Intermittent claudication, coronary vasodilation, prevention of stroke or TIAs
Abciximab, eptifibatide, tirofiban
M: GPIIb/IIIA inhibitors - prevent platelet aggregation
C: Unstable angina
Azathioprine, 6-mercaptopurine, 6-thioguanine
M: Purine analogs (decrease de novo purine synthesis) - activated by HGPRT
T: Myelosuppression
Cladribine (2-CDA)
M: Purine analog, high intracellular concentrations due to adenosine deaminase resistance
T: Myelosuppression, nephrotoxicity, neurotoxicity
Cytarabine (Ara-C)
M: Pyrimidine analog
T: Pancytopenia
5-fluorouracil
M: Binds to folic acid and inhibits thymidylate synthase
T: Myelosuppression (not reversible)
Methotrexate
M: Folic acid analog that inhibits dihydrofolate reductase
T: Myelosuppresion (reversible with leucovorin), hepatotoxicity, pulmonary fibrosis
Bleomycin
M: Inhibits free radical formation and breaks DNA strands
T: Pulmonary fibrosis
Dactinomycin
M: Intercalates in DNA
C: CHILDHOOD TUMORS
T: Myelosuppression
Doxorubicin, daunorubicin
M: Generates free radicals and decreases DNA replication
C: KIDS CANCER
T: Dilated cardiomyopathy, alopecia, myelosuppression
Busulfan
M: Cross links DNA
T: Pulmonary fibrosis
Cyclophosphamide, ifosfamide
M: Cross link DNA at guanine N-7
T: Hemorrhagic cystitis (prevent with mesna)
Nitrosoureas
M: Crosses blood-brain barrier, cross-link DNA
C: BRAIN TUMORS
T: CNS toxicity
Paclitaxel
M: Stabilize microtubules so mitotic spindles can’t break down
T: Myelosuppression
Vincristine, vinblastine
M: Bind B-tubulin and inhibit polymerization into microtubules
T: Peripheral neuropathy
