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63 Cards in this Set

  • Front
  • Back
Transferrin
Plasma protein that binds to Iron and transports to tissue
Ferrous sulfate
Oral treatment for hypochromic microcytic anemia, 20% Fe
Ferrous fumarate
Oral treatment for hypochromic microcytic anemia, 33% Fe
Ferrous gluconate
Oral treatment for hypochromic microcytic anemia, 12% Fe
Iron Dextran
IM/IV treatment for hypochromic microcytic anemia
Deferoxamine/deferasirox
parental/oral treatments for hematochromatosis/chronic overdose toxicity of iron
Hypochromic microcytic anemia
Iron deficiency
Pernicious Anemia
Lack of Gastric Intrinsic Factor (GIF)
Macrocytic anemia
VB12 or Folate deficiency
Methylfolate Trap
Increased accumulation of methylfolate and serum methylmalonic acid, decreased VB 12 in plasma
Cyanocobalamin injection
For pernicious anemia, 100-200 ug/day IM for 1-2 wks, maintenance: 1 mg once/month for life
Hydroxocobalamin
For pernicious anemia, IM injection only
Vitamin B12
For pernicious anemia, 2g daily, converted to coenzyme forms: methycobalamin, 5-deoxyadenosylcobalamin

binds to GIF, interacts with receptor on mucosal cells and is transported to the blood
Transcobalamin II
plasma b-globin that binds to VB 12 and transports to tissues and liver for activation/storage
Erythropoeitin
Hemolytic Growth Factor

Binds specific receptor and increases Ca and PG's

Stimulates proliferation and differentiation of committed erythroid precursor cells in bone marrow --> increases red cell production

T1/2 = 9 hours
Darbepoetin
Long-acting erythropoietin, given once weekly IV or SC

T1/2 = 25 hrs
Filgrastim
Granulocyte CSF

Stimulates neutrophils

T1/2 = 2-7 hrs
Sargramostim
Granulocyte/Macrophage CSF

Stimulates neutrophils, monocytes, macrophages

T1/2 = 2-7 hrs
Pegfilgrastim
Conjugation product of filgrastim and polyethylene glycol

Has much longer serum half life and can be given once every few weeks compared to Filgrastim
Oprelvekin
Megakaryocyte growth factor

Acts thru a specific cell surface cytokine receptor to stimulate the growth of lymphoid and myeloid cells, and the megakaryocyte progenators, and increase the number of peripheral platelets and neutrophils

T1/2 = 7-8 hrs
Heparin
Anticoagulant - binds antithrombin and increases rate of inhibition of CF by 1000X (esp. IIa and Xa)

Parenterally, IV or SC

T1/2 = 2 hr

Increase aPPT by 2-2.5X
Unfractionated Heparin (UFH)
Anticoagulant - mixture of highly electronegative acidic mucopolysaccharides consisting of repeating disaccharide units composed of glucosamine and either L-iduronic acid or D-glucuronic acid

MW - 5,000-30,000

Occurs naturally in granules of circulating basophils and tissue mast cells
Enoxaprin
Anticoagulant - Inhibits activated factor Xa, but has less effect on thrombin and on coagulation than heparin

LMW heparin - 3,000-8,000

T1/2 = 4 hr
Fondapariux
Anticoagulant - synthetic analog of heparin, increases factor Xa inhibition w/out neutralizing thrombin

T1/2 = 15 hrs
Protamine Sulfate
Overdose treatment for Heparin

Low MW strong basic protein which binds and neutralizes heparin - IV infusion
Lepirudin
Direct Thrombin Inhibitor - recombinant derivative of hirudin, an anticoagulant produced by leaches
Argatroban
Direct Thrombin inhibitor - small molecule synthetic derivative of L-arginine
Bivalirudin
Direct Thrombin Inhibitor - synthetic 20-AA analog of Lepirudin
Warfarin
Oral anticoagulant - inhibits synthesis of Vit-K depent CFs (II,VII,IX,X)

Antimetabolite of Vit-K - involves gamma carboxylation of glutamic acid residues of precursor and results in formation of Ca2+ binding sites

Prevents conversion of inactive Vit K epoxide to its active form

T1/2 = 36 hrs
Cimetidine
Antagonist of Warfarin

Increases catabolism by enzyme induction
Vitamin K (effect on Warfarin)
Antagonist

Increases CF synthesis
Cimetidine
Enhancer of Warfarin

Decreases catabolism by enzyme inhibition
Sulfonamides (effect on Warfarin)
Displace protein binding sites
Aspirin
Anti platelet drug

Irreversible acetylation of cyclooxygenase - inhibits synthesis of thromboxane A2 (platelet aggregator and vasoconstrictor)
Clopidogrel bisulfate
Anti platelet drug

Inhibits ADP binding to R and platelet aggregation
Abciximab
Blocks Platelet GP IIb/IIIa Receptors - humanized monoclonal Antibody directed against the GP IIb/IIIa complex
Eptifibatide
Blocks Platelet GP IIb/IIIa Receptors - analog that contains the arginine-glycine-aspartic acid sequence of fibrinogen
Streptokinase
Thrombolytic Drug - activates plaminogen --> lysis of formed clots

Commercial formulation of a naturally occuring thrombolytic enzyme by recombinant DNA techniques
Alteplase
Thrombolytic Drug - tissue-type plasminogen activator

A recombinant protein derivative of tissue plasminogen activator --> approved for thrombolysis in patients with acute MI
Vitamin K1
Hemostatic agent

required for postribosomal modification of clotting factors II, VII, IX and X in the liver
Aminocaproic Acid
Thrombolysis inhibitor

Chemically similar to lysine
--> it competitively inhibits plasminogen activation and this prevents fibrinolysis
Zidovudine
HIV reverse transcriptase inhibitor
Stavudizine
Nucleoside Reverse Transcriptase Inhibitor

Substitute for zidovudine

Thymine analog, high bioavailability

Painful peripheral neuropathy– reversible
Dose-Limiting (15%) --> Paresthesis, Numbness, M. Pain; M. Weakness,
Elevation in serum transaminases --> PANCREATITIS (rare)
Lamivudine
Nucleoside Reverse Transcriptase Inhibitor

Also for chronic hepatitis B

Cytosine analog
Emtricitabine
Nucleoside Reverse Transcriptase Inhibitor

Like lamivudine, but longer half life
Didanosine
Nucleoside Reverse Transcriptase Inhibitor

Mainly used in combination

Analog of deoxyadenosine

SEs - Painful peripheral neuropathy, acute pancreatitis
Acid labile
Abacavir
Nucleoside Reverse Transcriptase Inhibitor

Combination therapy

Guanosine analog

SEs - hypersensitivity rxns
Combivir
Zidovudine + lamivudine
Trizidivir
Zidovudine + lamivudine + abacavir
Epzicom
Abacavir + lamivudine
Truvada
Tenovir + emtricitabine
Tenovir
Nucleotide Reverse Transcriptase Inhibitor

competitive inhibitor of HIV RT

Combination therapy in patients who failed nucleoside RT inhibition

acyclic nucleotide analog of adenosine

SEs - renal impairment, fanconi's syndrome
Nevirapine
Non-nucleoside Reverse Transcriptase Inhibitor

SEs - rash --> Stevens-Johnson syndrome

Induces CYP3A4
Efavirenz
Non-nucleoside Reverse Transcriptase Inhibitor

Very long half life

SEs - vivid dreams

Induces CYP3A4

Avoid in pregnancy - teratogenic
Saquinavir
HIV protease inhibitor

Very poor oral bioavailability - 4% (soft-gel may help), least potent

Resistance may develop
Ritonavir
HIV protease inhibitor

Combination therapy

Good oral bioavailability

Potent inhibitor of CYP 3A4
Kaletra
Lopinavir + Ritonavir

Ritonavir inhibits CYP3A4 --> increases [Lopinavir]
Atazanavir
HIV protease inhibitor

Inhibitor of CYP3A4

SEs - hyperbilirubinemia/jaundice - competitively inhibits UDP-glucuronosyl transferase, which catalyzes bilirubin conjugation
Also prolongs PR interval
Darunavir
HIV protease inhibitor - very potent, works against strains resistant to other PIs

Taken orally with Ritonavir

SEs - increased plasma lipids
Fosamprenavir
Potent HIV protease inhibitor - prodrug, lowers pill burden

long half life

SEs - rash, Stevens-Johnson syndrome
Maraviroc
HIV-1 CCR5 inhibitor - Mphages

Combo therapy, only effective in 50%

SEs - cough, rash, upper RTA
Enfuvirtidae
HIV Fusion inhbitor - binds gp41 subunit

Combination therapy

SEs - Injection site rxn, nodules/cysts, eosinophilia, bacterial pneumonia
Raltegravir
HIV Integrase strand transfers inhibitor

Combination therapy

SEs - myopathy, rhabdomyolysis

metabolized by UDP-glucuronosyltransferase