Drugs Heme Onc Flashcards
Direct thrombin inhibitors
Agatroban, bivalirubin, dagatran
How do you reverse warfarin
vit K, fresh frozen plasma
How do you reverse heparin
protamine sulfate (if HMW heparin, acute duration so can just discontinue) for LMWH and fondaparinaux
Thrombolytics
”-plase” Alteplase (tPa) Reteplase (rPa) Streptokinase tenecteplase (TNK-tPA)
Aspirin
irreversible COX1 COX2 inhibitor
ADP receptor inhibitors
Clopidogrel, prasugrel, ticagrelor (reversible), ticlopidine
Inhibits ADP receptors and thus blocks appearance of GpIIb/IIIa on cell surface
Cilostazol, dipyridamole
phosphodiesterase III inhibitor, increase cAMP and inhibits platelet aggregation; vasodilator
GpIIb/IIIa inhibitors
Abciximab, eptifibatide, tirofiban Prevents platelet aggregation
Abciximab made from monoclonal Fab fragments
Clinical use direct Xa inhibitors
DVT PE prophylaxis (rivaroxaban)
Stroke prophylaxis in patients with afib
Toxicity of direct Xa inhibitors
bleeding (nor reversal agent)
Use of direct thrombin inhibitors
Alternative to heparin for patients with HIT
Use of thrombolytics
Early MI, early ischemic stroke, direct thrombolysis in massive PE
Toxicity of thrombolytics
bleeding
contradidicated in patients with active bleeds, history of intracranial bleeding, recent surgery, known bleeding diathesis, or severe HT
Treat toxicity with aminocaproic acid
Toxicity of aspirin
Gastric ulcers, tinnitus,
chronic uses can lead to acute renal failure, interstitial nephritis, and upper GI bleeds
Reyes syndrome in children with flu
Overdose causes hyperventilation and resp alk –> mixed metabolic acidosis resp alk
Uses of ADP receptor blockers
Acute coronary syndrome, coronary stenting , decreases incidence or recurrance of thrombolytic stroke
Uses for phosphodiesterase inhibitors
intermittent claudication, cornonary vasodilation, prevent of stroke or TIA (combined with aspiring), angina prophylaxis
Phosphodiesterase inhibitor toxicity
nausea, headache, facial flushing, hypotension, abdominal pain
GP IIb/IIIa inhibitors toxicity
bleeding, thrombocytopenia
Methotrexate (MTX)
Folic acid analog that competitively inhibits dihydrofolate reductase (DHF –> THF)
THF needs to be methylated to donate to convert dUMP to dTMP
Clinical uses for MTX
ALL, lymphomas, choriocarcinoma, sarcoma
Ectopic pregnancy, medical abortion, rheumatoid arthritis, psoriasis, IBD, vasculitis
Toxicity for MTX
Myelosuppression reversible with leucovorin rescue
Hepatoxicity
Mucositis (mouth ulcers)
Pumonary fibrosis
5-flurouracil
pyrimadine analog that is bioactivated to 5F-dUMP which complexes with folic acid and as a complex inhibits thymidylate synthase which converts dUMP to dTMP
5-FU clinical uses
colon cancer, pancreatic cancer, carcinoma (topical)
Toxicity of 5-FU
myelosuppression not reversible with luecovorin (folinic acid)
What is the action of prednisone, prednisolone?
glucocorticoid that binds to an intracytosolic receptor and increases transcription of a variety of factors
What is prednisone used in?
Most common glucocorticoid used in cancer treatment
CLL, non hodgkins lymphoma
Autoimmune diseases
What is prednisone’s toxicity?
Cushing like symptoms, weight gain, cattaracts, acne, osteoporosis, HT, muscle breakdown, peptic ulcers, hyperglycemia, psychosis
Story; “Man complains of 15 lb weight gain and facial acne, has a BP of 142/90 and his glucose is 220”
What are the first line drugs for treatment of lead poisoning?
Dimercaprol and EDTA
Succimer for children
Which ADP receptor blocker is reversible?
Ticagrelor
All the rest are irreversible
ADP receptor inhibitor tox
Neutropenia (ticlopidine), TTP
