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34 Cards in this Set

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Epoetin alfa
Indication: anemia with chronic kidney disease, surgery, AIDS, cancer chemotherapy, chronic inflammation

MOA: bind to receptors on committed erythroid progenitors in bone marrow, promote survival, proliferation, maturation

Paenterally

Metabolism: T1/2= 4-8 hrs

Adverse effects: thromboembolic effects (migratory thrombophlebitis, microvascular thrombosis, PE), risk with high Hgb, Fe deficiency can develop

check once or twice a week until stabilized

Recombinant
darbapoetin alfa
Indication: anemia with chronic kidney disease, surgery, AIDS, cancer chemotherapy, chronic inflammation

MOA: bind to receptors on committed erythroid progenitors in bone marrow, promote survival, proliferation, maturation

Paenterally

Metabolism: T1/2= 4-8 hrs

Adverse effects: thromboembolic effects (migratory thrombophlebitis, microvascular thrombosis, PE), risk with high Hgb, Fe deficiency can develop

check once or twice a week until stabilized

novel
sargramostim
GM-CSF

Indication: autologous bone marrow transplant to shorten neutropenia, intensive chemotherapy,myelodyslpasia, aplastic anemia, AIDS

MOA: synergistic with growth factors to increase neutrophil, monocyte production, increase migration, phagocytosis, superoxide production, Ab cell toxicity of neutrophils/macrophages/ esinophils

Metabolsim: T1/2 = 2-3 hrs, leukocyte increase over 7-10 days, baseline 2-10 days after stop

Side Effects: bone pain, malaise, flu-like symptoms, supraventricular tachycardia

1st dose effect: flushing, hypotension, nausea, vomit, dyspnea--> granulocyte sequestration in pulm circulation
filgrastim
G-CSF

Indication: severe neutropenia after stem cell transplant/ chemo

MOA: stimulation of CFU-G to increase neutrophil production, enhance phagocytic, cytotoic fxn of neutrophils

Metabolism: t1/2: 3.5 hrs, subq injection

Side Effects: bone pain, local skin reaction
pegfilgrastim
G-CSF

Indication: severe neutropenia after stem cell transplant/ chemo

MOA: stimulation of CFU-G to increase neutrophil production, enhance phagocytic, cytotoic fxn of neutrophils

Metabolism: t1/2: 3.5 hrs, subq injection

not cleared by kidney, by neutrophil mediated

Side Effects: bone pain, local skin reaction
Oprelvekin
Indication: patients undergoing chemotherapy when severe thrombocyopenia has occured with prior cycles

MOA: recomb form of IL-11 which enhances megakaroyoctye maturation--> increase blood platelet counts

Side Effects: fluid retnetion, tachycardia, palpitations, edema, shortness of breath

clinical use: drug discontinued when platelets above 100 k
Thrombopoietin
recombo human megakaryocyte growth and development factor/ human thrombopoietin

Indications: chemo therapy and radiation induced myelosuppression with subsequent thrombocytopenia

MOA: stem cell differentiation into megakaryocyte progenitors and stimulates megakaryocytopoiesis to increase platelet production

Side Effects: anti- recombinant Ab cross reactive with native = thrombocytopenia
Ferrous sulfate
Indication: oral iron in ppl with Fe deficiency and can absorb

MOA: restore Fe stores = marrow can produce normal RBC

Side Effects: upper GI discomfort, heartburn, nausea, hemochromatosis/ Fe overload

Clinical use: rise in retic count takes 4-7 days so effectiveness cannot determine until 3-4 weeks
Ferrous gluconate
Indication: oral iron in ppl with Fe deficiency and can absorb

MOA: restore Fe stores = marrow can produce normal RBC

Side Effects: upper GI discomfort, heartburn, nausea, hemochromatosis/ Fe overload

Clinical use: rise in retic count takes 4-7 days so effectiveness cannot determine until 3-4 weeks
polysaccharide-Fe complex
Indication: oral iron in ppl with Fe deficiency and can absorb

MOA: restore Fe stores = marrow can produce normal RBC

Side Effects: upper GI discomfort, heartburn, nausea, hemochromatosis/ Fe overload

Clinical use: rise in retic count takes 4-7 days so effectiveness cannot determine until 3-4 weeks
Sodium Ferric gluconate complex in sucrose
Indication: Fe deficiency where Iron administration = ineffective, malabsorption states, oral Fe intolerant

Absorption: <500 mg = t 1/2--> 6 hrs, 1 g = 1-2 weeks through reticuloendothelial cells

Side effects: malaise, rare anaphylactic reaction, lower than in iron dextran, headache, fever, arthralgias, urticaria
Iron Sucrose
Indication: Fe deficiency where Iron administration = ineffective, malabsorption states, oral Fe intolerant

Absorption: <500 mg = t 1/2--> 6 hrs, 1 g = 1-2 weeks through reticuloendothelial cells

Side effects: malaise, rare anaphylactic reaction, headache, fever, arthralgias, urticaria
Iron dextran
Indication: Fe deficiency where Iron administration = ineffective, malabsorption states, oral Fe intolerant

Absorption: <500 mg = t 1/2--> 6 hrs, 1 g = 1-2 weeks through reticuloendothelial cells

Side effects: malaise, rare anaphylactic reaction, headache, fever, arthralgias, urticaria
Cyanocobalamin
Indication: treatment of anemia due to B12 deficiency

Absorption: No intrinsic factor or with ileal disease = no absorption, large dose does not equate with greater retention

Side effects: anaphylaxis with IV injection, paraenterally = IM

Clinical use: only for vitamin defeciency, maintain for life for those who can't absorb
Folic acid
Indication: Megaloblastic anemia due to folate deficiency, pregnancy, disease state with high cell turnover, treat high homocysteine

MOA: essential step in purine synthesis, deficiency --> megaloblastic anemia but no neuro defects, in pregnancy--> neural tube defects

Absorption: proximal portion of small intestine and need proteins on mucosal cell membrane, enterohepatic circulation

Side Effects: rare reports of reaction to paraenteral injection, large amounts counteract anti-epileptic effect of phenobarbitol, phenytoin, primidone

Clinical use: improve megaloblastic anemia of B12 deficiency, but not neuro, need to make sure its folate or B12 deficiency
Heparin
Indication: initial treatment of venous thrombosis, PE, acute coronary syndrome, acute MI, coronary surgical procedures, DIC, low dose to prevent venous thromboembolism

MOA: catalyzing antithrombin to inhibit of coagulation, antithrombin acts on thrombin, factor Xa (LW), factor IX

IV or subq

Metabolism: immediate onset IV, 1-2 hrs subq, 100 u/ kg = t1/2- 1 hr, 800 u/kg = t1/2 5 hrs--> degrade by reticuloendothelial system

Side Effects: bleeding, hepatic function, osteoporosis, hyperkalemia- inhibit aldo

Unique: Heparin induced Thrombocytopenia, less with LW, caused by IgG Ab vs. heparin + platelet factor 4 = activates platelets and thrombin generated
Enoxaparin
Indication: initial treatment of venous thrombosis, PE, acute coronary syndrome, acute MI, coronary surgical procedures, DIC, low dose to prevent venous thromboembolism

MOA: catalyzing antithrombin to inhibit of coagulation, acts mostly on factor Xa

IV or subq

Metabolism: immediate onset IV, 1-2 hrs subq, 100 u/ kg = t1/2- 1 hr, 800 u/kg = t1/2 5 hrs--> degrade by reticuloendothelial system

Side Effects: bleeding, hepatic function, osteoporosis, hyperkalemia- inhibit aldo

contraindicated in renal failure
dalteparin
Indication: initial treatment of venous thrombosis, PE, acute coronary syndrome, acute MI, coronary surgical procedures, DIC, low dose to prevent venous thromboembolism

MOA: catalyzing antithrombin to inhibit of coagulation, acts mostly on factor Xa

IV or subq

Metabolism: immediate onset IV, 1-2 hrs subq, 100 u/ kg = t1/2- 1 hr, 800 u/kg = t1/2 5 hrs--> degrade by reticuloendothelial system

Side Effects: bleeding, hepatic function, osteoporosis, hyperkalemia- inhibit aldo

contraindicated in renal failure
ardeparin
Indication: initial treatment of venous thrombosis, PE, acute coronary syndrome, acute MI, coronary surgical procedures, DIC, low dose to prevent venous thromboembolism

MOA: catalyzing antithrombin to inhibit of coagulation, acts mostly on factor Xa

IV or subq

Metabolism: immediate onset IV, 1-2 hrs subq, 100 u/ kg = t1/2- 1 hr, 800 u/kg = t1/2 5 hrs--> degrade by reticuloendothelial system

Side Effects: bleeding, hepatic function, osteoporosis, hyperkalemia- inhibit aldo

contraindicated in renal failure
nadroparin
Indication: initial treatment of venous thrombosis, PE, acute coronary syndrome, acute MI, coronary surgical procedures, DIC, low dose to prevent venous thromboembolism

MOA: catalyzing antithrombin to inhibit of coagulation, acts mostly on factor Xa

IV or subq

Metabolism: immediate onset IV, 1-2 hrs subq, 100 u/ kg = t1/2- 1 hr, 800 u/kg = t1/2 5 hrs--> degrade by reticuloendothelial system

Side Effects: bleeding, hepatic function, osteoporosis, hyperkalemia- inhibit aldo

contraindicated in renal failure
raviparin
Indication: initial treatment of venous thrombosis, PE, acute coronary syndrome, acute MI, coronary surgical procedures, DIC, low dose to prevent venous thromboembolism

MOA: catalyzing antithrombin to inhibit of coagulation, acts mostly on factor Xa

IV or subq

Metabolism: immediate onset IV, 1-2 hrs subq, 100 u/ kg = t1/2- 1 hr, 800 u/kg = t1/2 5 hrs--> degrade by reticuloendothelial system

Side Effects: bleeding, hepatic function, osteoporosis, hyperkalemia- inhibit aldo

contraindicated in renal failure
Fondaparinux
Indication: initial treatment of venous thrombosis, PE, acute coronary syndrome, acute MI, coronary surgical procedures, DIC, low dose to prevent venous thromboembolism

MOA: pentasaccharide that is a factor Xa inhibitor

subq

Metabolism: immediate onset, T1/2 = 17-21 hrs, degrade by reticuloendothelial system

contraindicated in renal failure

Side Effects: bleeding, hepatic function, osteoporosis, hyperkalemia- inhibit aldo
Protamine Sulfate
Indication: too much heparin

MOA: binds tightly to heparain and neutralizes its anticoagulant effect

Side Effects: anaphylactic with diabetes mellitus who have protamine- containing insulin
Lepirudin
Recombo hirudin- leech saliva

Indication: treatment of heperain induced thrombocytopenia

Metabolism: IV, excrete by kidney, T1/2 = 1.3 hrs,

Side effects: may develop antihirudin Ab

MOA: direct thrombin inhibitor
Bivalirudin
Synthetic

Indication: alternative to heperin in angioplasty

MOA: directly inhibits thrombin

T1/2 = 25 min, cleared by renal, IV
Argatroban
Synthetic based on L-arginine

Indication: alternative to lepirudin for prophylaxis of patients with HIT

T1/2 = 40-50 min, excrete in bile

MOA: binds reversible to catalytic site of thrombin
Danaparoid
Indication: prophylaxis for deep vein thrombosis, HIT

MOA: inhibits factor Xa by antithrombin

Subq

T1/2= 1 day, renal clearence
Drotrecogin alfa
recombo form of human activated protein C

MOA: inhibits coagulation by inactivation of factors Va and VIIIa

help with severe sepsis
Warfarin
indications: oral anticoagulant to prevent/ recurrance of DVT, PE, systemic embolization from prosthetic valve, atrial fib

MOA: antagonist of vitakmin K, decrease 30-50% vit K dependent coagulation factor made by liver, factors made less active

Absorption: complete absorbed, 99% plasma bound, does achieve effect on circulationg coagulation factors have been cleared, 3-5 days later/ duration 2-5 days after cessation

Side Effects: bleeding, birth defects, skin necrosis, purple toe syndrome, alopecia, urticaria, dermatitis, fever, venous limb gangrene, mulitcentric skin lesions

drug interactions: alter uptake/ metabolism of oral anticaogulant, vitamin K 2) alteration of synthesis , function, clearence of hemostatic factors
Streptokinase
from B hemolytic streptococci

Indication: acute treatment of MI, non-hemorrhagic stroke, dissolve pathogenic thrombi - occlude arteries, PE, prosthetic heart valves

MOA: actives plasminogen to plasmin by binding to plasminogen and form complex which activates plasminogen to plasmin- no intrinsic enzymatic activity, plasmin then lyses fibrin

Side effects: bleeding 1) lysis of fibrin at site of injury 2) systemic lytic state breaking down clotting factors

Contraindications: recent major surgery, serious recent bleeding, uncontrolled HTN, CVA, Intracranial disease, aortic dissection, acute pericarditis
Alteplase
Indication: acute treatment of MI, non-hemorrhagic stroke, dissolve pathogenic thrombi - occlude arteries, PE, prosthetic heart valves

MOA: directly activates plasminogen, more specific to activating plasminogen attached to fibrin = more clot specific

T1/2 = 5-10 min, IV

Side effects: bleeding 1) lysis of fibrin at site of injury 2) systemic lytic state breaking down clotting factors

Contraindications: recent major surgery, serious recent bleeding, uncontrolled HTN, CVA, Intracranial disease, aortic dissection, acute pericarditis
Reteplase
Indication: acute treatment of MI, non-hemorrhagic stroke, dissolve pathogenic thrombi - occlude arteries, PE, prosthetic heart valves

MOA: directly activates plasminogen, more specific to activating plasminogen attached to fibrin = more clot specific

T1/2 = 5-10 min, IV

Side effects: bleeding 1) lysis of fibrin at site of injury 2) systemic lytic state breaking down clotting factors

Contraindications: recent major surgery, serious recent bleeding, uncontrolled HTN, CVA, Intracranial disease, aortic dissection, acute pericarditis



Side effects: bleeding 1) lysis of fibrin at site of injury 2) systemic lytic state breaking down clotting factors

Contraindications: recent major surgery, serious recent bleeding, uncontrolled HTN, CVA, Intracranial disease, aortic dissection, acute pericarditis
tenecteplase
Indication: acute treatment of MI, non-hemorrhagic stroke, dissolve pathogenic thrombi - occlude arteries, PE, prosthetic heart valves

MOA: directly activates plasminogen, more specific to activating plasminogen attached to fibrin = more clot specific

T1/2 = 5-10 min, IV

Side effects: bleeding 1) lysis of fibrin at site of injury 2) systemic lytic state breaking down clotting factors

Contraindications: recent major surgery, serious recent bleeding, uncontrolled HTN, CVA, Intracranial disease, aortic dissection, acute pericarditis
Aminocaproic acid
Indication: reduce bleeding after surgery (prostate, tooth extraction)

MOA: competes for lysine binding sites on plasminogen and plasmin, blocks the interaction of plasmin with fibrin, reverse excessive fibrinolysis

oral/ IV
absorbed rapidly, excrete unchanged

Side Effects: excessive thrombosis, myopathy, muscle necrosis