Term
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Definition
Rickettsia, Orientia, Coxiella, Ehrlichia
MOA: prevent tRNA binding to 30S
MOR: influx/efflux, binding site mutation, inactivation
SE: GI, photosenitivity, brown teeth for fetus/young children, nephrotoxicity (not in doxycycline b/c not secreted by kidney) |
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Term
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Definition
2nd choice for Orientia; pregnant women instead of tetracyclines (or rifampin)
MOA: binds 50S peptidyltransferase near site of macrolide action (inhibit one another)
MOR: plasmid encoded acetyltransferase, decreased permeability, binding site mutation
SE: inhibits synthesis of IMM proteins, anemia/leukopenia/thrombocytopenia, aplastic crisis/fatal pancytopenia (<1%) |
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Term
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Definition
Antimalarial for P. vivax, P. ovale; treat hepatic and gametocytic forms
MOA: ROS that inhibit ETC
SE: GI, mild anemia, cyanosis, acute hemolytic anemia in people w/ G6PD deficiency
Given orally->IV = hypotension |
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Term
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Definition
Antimalarial for P. falciparum, P. malariae, P. vivax, P. ovale (prophylaxis and treatment); RBC form; very long 1/2 life
MOA: accumulates in food vacuole, inhibits hemozoin formation from heme released by Hb degradation-> ROS
MOR: decreased accumulation-> choloroquine resistance transport gene (CRT)
SE: usu only if given rapidly IV; CV |
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Term
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Definition
Antimalarial for P. falciparum prophylaxis/treatment; RBC form
MOA: accumulates in food vacuole, inhibits hemozoin formation from heme released by Hb degradation-> ROS
MOR: decreased accumulation
SE: dizziness, headaches, A/V disturbances, nightmares |
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Term
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Definition
Antimalarial for P. falciparum treatment; RBC and gametocytic forms
MOA: heme Fe cleavage of endoperoxide-> ROS; ATPase damage via alkylation
No resistance
SE: induces cytP450s, including a self metabolizer (affects dosage), teratogenic, neurotoxic
Recrudescence decreased w/ mefloquine combo |
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Term
| Pyrimethamine-sulfadoxine |
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Definition
Antimalarial for P. falciparum treatment; RBC form
MOA: inhibits DHFR/TS and PABA utilization
MOR: DHFR/TS mutation
SE: skin rash, folate deficiency, renal toxicity |
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Term
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Definition
Antimalarial for P. falciparum treatment; primary hepatic and RBC stages
MOA: metabolized to an active cyclogaunil; inhibits DHFR/TS
MOR: DHFR/TS mutation
SE: GI, blood in stool |
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Term
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Definition
P. falciparum, Babesia
MOA: accumulates in food vacuole, inhibits hemozoin formation from heme released by Hb degradation-> ROS
MOR: decreased accumulation (PF multidrug resistant gene)
SE: CV (worse in quinidine), hypotension, hypoglycemia, cinchonism (A/V disturbances) |
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Term
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Definition
Babesia
MOA: binds 50S peptidyltransferase to block translocation; also work on apicoplast ribosome
SE: diarrhea, pseudomembranous colitis (kills GI bacteria except C. dificile)-> can be fatal |
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Term
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Definition
Bartonella, Babesia
MOA: binds 50S peptidyltransferase to block translocation
Decreased drug interactions b/o cytP450 inhibition
Large tissue distribution, high cellular concentration |
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Term
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Definition
ALL, Hodgkin's Disease, NHL, MM
IV
MOA: binds beta-tubulin to prevent cell division
MOR: efflux pump
SE: neurological (peripheral neuropathy), limited myelosuppresion, alopecia |
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Term
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Definition
ALL, Hodkin's Disease, NHL, MM
Adrenocorticosteroid
MOA: Lympholytic by inducing apoptosis
SE: glucose intolerance, immunosuppresion, osteoporosis, psychosis |
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Term
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Definition
ALL
MOA: purine analog, activated by HGPRT
MOR: decreased HGPRT, increased efflux, increased repair
SE: bone marrow suppression, anorexia, nausea, teratogenic |
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Term
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Definition
ALL
Parenteral
MOA: converts asparagine to aspartate in lymphoblastic leukemia cells
SE: hypersensitivity, hyperglycemia, clotting abnormalities, decreased albumin production |
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Term
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Definition
APL
MOA: RA acid binding to RAR induces cellular differentiation; t(15;17) causes decreased RAR; ATRA overrides aberrant RAR to promote differentiation into neutrophils
SE: teratogenic, not 100% remission |
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Term
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Definition
AML
MOA: 2'-OH inhibits DNA chain elongation via steric hindrance
MOR: cytidine deaminase, dCMP deaminase, decreased deoxycytidine kinase (so no phosphorylation for DNA polymerase addition)
SE: severe immunosuppression, GI, increased hepatic enzyme production, pulmonary edema, dermatitis |
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Term
| Daunorubicin, Idarubicin, Doxorubicin |
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Definition
ALL, Hodkin's Disease & NHL & MM (doxorubicin)
IV
MOA: intercalates, inhibits topoisomerase II, ROS
SE: cardiotoxicity, bone marrow suppression, alopecia, GI, red urine (doxorubicin, daunorubicin) |
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Term
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Definition
ALL, CLL, NHL, MM
MOA: alkylation
MOR: decreased influx, increased DNA repair, increased metabolism
SE: acrolein made as a breakdown product, toxic to bladder-> neutralize w/ MESNA |
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Term
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Definition
AML
MOA: conjugated monoclonal Ab allowing direct delivery to cancer cells; cytotoxic Ab against CD33 on leukemic myeloblasts
SE: minimal infusion related toxicity (less w/ glucocorticoids), BM suppression, hepatic toxicity |
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Term
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Definition
CLL
MOA: interalates DNA, inhibits topoisomerase II, cannot produce ROS b/c lacks 4th ring
SE: less cardiotoxicity compared to daunorubicin, doxorubicin, idarubicin |
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Term
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Definition
CLL, Hairy Cell Leukemia, NHL
MOA: purine analogs; inhibits DNA polymerase, incorporated into DNA and RNA, promotes apoptosis; resistant to deamination
MOR: decreased deoxycytidine kinase
SE: myelosuppression, GI, chills, fever |
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Term
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Definition
CLL, B cell-NHL
MOA: naked monoclonal chimeric Ab; ADCC and CDC; mouse Fab w/ human Fc; against CD20 (B cells)-> induces autophosphorylation and activation of tyrosine kinases that induce c-myc and MHC formation; sensitizes tumor cells for apoptosis by chemotherapy
SE: infusion reaction |
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Term
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Definition
CLL, B-CLL
MOA: naked monoclonal humanized Ab; ADCC and CDC; Fab amino acids from mouse, rest human; against CD52 (B/T cells)
SE: less than rituximab b/c more human like; acute infusion reaction, depressed hematopoietic and T cell production |
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Term
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Definition
CLL, NHL
Oral
MOA: activated to a nitrogen mustard by cytP450; alkylating agent
SE: lacks normal alkylation SEs |
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Term
| Gleevec (imatinib mesylate) |
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Definition
CML
MOA: BCR-ABL kinase inhibitor, binds to ATP binding site
MOR: ATP site mutation
SE: GI, edema, muscle cramps |
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Term
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Definition
CML
Oral along with IFN-alpha
MOA: alkylation
SE: pancytopenia, teratogenic |
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Term
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Definition
CML
MOA: inhibits ribonucleoside diphosphate reductase to block conversion of ribonucleotide to deoxyribonucleotide
SE: GI, myelosuppression, teratogenic
Also used to decrease vaso-crisis in SC disease |
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Term
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Definition
Hairy Cell Leukemia
MOA: adenosine deaminase inhibitor; leads to build up of adenosine and deoxyadenosine which blocks DNA synthesis by feedback inhibiting ribonucleotide reductase, so no deoxynucleotides
SE: long lasting immunosuppression, fatal pulmonary toxicity if given w/ fludarabine, GI, skin rash |
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Term
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Definition
Hodgkin's Disease
MOA: direct alkylating agent
SE: vomiting, lacrimation, bone marrow suppression |
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Term
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Definition
Hodkin's Disease
MOA: alkyation
MOR: increased repair
SE: sedation, carcinogenic, teratogenic, mutagenic, infertility |
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Term
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Definition
MM
MOA: activated into metabolites; disruption of Bcl-2, block NF-kB, inhibit IL-6 production-> growth arrest/apoptosis; cell adhesion inhibition to BM stromal cells via decreased IL-6; decreased angiogenesis; enhanced IFN-gamma and IL-2 production-> increased NK function
SE: teratogenic (stumpy limbs), sedation, constipation, peripheral sensory neuropathy
SE less in lanalidomide |
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Term
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Definition
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Term
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Definition
HL, NHL, MM
MOA: spontaneous cleavage of nitrosurea group into alkylating agent and isocyanite which causes delayed and prolonged platelet and granulocyte suppression
SE: veno-occlusion disease, pulmonary fibrosis, renal failure, secondary leukemia, can cross BBB |
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Term
| Ferrous sulfate; Ferrous gluconate |
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Definition
Oral iron salts to treat iron deficiency
Regulated by intestinal mucosa; no need to monitor levels
Continued 3-6 months after correction
SE: GI but are dose related |
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Term
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Definition
IV/IM for those who cannot absorb iron, have chronic blood loss, chronic kidney disease
Requires monitoring of iron storage levels
SE: headache, light-headed, fever, nausea, vomiting, rarely anaphylaxis w/ HMW dextran |
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Term
| Iron sucrose complex, Iron sodium complex |
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Definition
IV for iron deficiency
Less likely to induce hypersensitvity |
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Term
| Vitamin B12 aka extrinsic factor |
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Definition
Needed for methyl transfer to form THF and for homocysteine->methionine; cofactor for methylmalonyl-CoA synthase (forms succinyl-CoA)
Dietary source: microbe produced; requires intrinsic factor for absorption via ileum; transported in blood w/ transcobalamin II
B12 vs folate deficiency-> Schilling test
Deficiency: megaloblastic macrocytic anemia, hypercellular bone marrow, neurological symptoms |
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Term
| Cyanocobalamin, Hydroxocobalamin |
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Definition
IM treatment for B12 deficiency
Converted to active forms-> deoxyadensylcobalamin, methylcobalamin
Hydroxocobalamin preferred b/c more highly protein bound and remains in circulation longer |
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Term
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Definition
Dietary form = polyglutamate N5-methylTHF; hydrolyzed to monoglutamate for absorption in jejunum
Oral supplement absorbed well always
Deficiency: macrocytic anemia, lacks neurological symptoms
Deficiency can be caused by methotrexate, trimethoprim, pyrimethamine-> DHFR inhibitors |
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Term
| Erythropoietin (epoietin alpha) |
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Definition
Endogenous from kidney; used to treat anemia, especially of chronic renal failure
MOA: stimulates ertyroid proliferation and differentiation via JAK/STAT activation
Patients w/ EPO <100 U/L respond best
SE: hypertension and thrombotic complications due to rapid increase in Hct/Hb |
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Term
| Darbepoietin alpha (NESP) |
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Definition
Glycosylated EPO w/ longer 1/2 life; used to treat anemia, especially of chronic renal failure
Given IV or SC
MOA: stimulates ertyroid proliferation and differentiation via JAK/STAT activation
SE: hypertension, thrombotic complications |
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Term
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Definition
Treatment of thrombocytopenia secondary to chemotherapy of non-myeloid cancers
MOA: stimulates lymphoid and myeloid cell growth via cytokines; increases platelet and neutrophil numbers
SE: fatigue, headache, dizziness, anemia, dyspnea, atrial arrhythmia |
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Term
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Definition
Treatment of chemotherapy induced and HSC transplantation thrombocytopenia
MOA: stimulates growth of megakaryocytes |
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Term
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Definition
HMW parenteral anticoagulant-> effective against venous thrombosis, pulmonary embolism, angina, myocardial infarction
Continuous IV infusion
MOA: indirect thrombin inhibition by inducing antithrombin III-> inhibits thrombin, IXa, Xa
Is not consumed during reaction-> higher the dose, higher the 1/2 life
Cannot cross placenta; must watch PTT-> a double the normal PTT = therapeutic
SE: HIT, bleeding
Contraindications: HIT, hemophilia, hypersensitvity, hemorrhage, sever hypertension, recent surgery of eye, brain, spinal cord |
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Term
| Enoxaprin, Dalteparin, Tinzaparin |
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Definition
LMW parenteral anticoagulant-> effective for venous thrombosis, pulmonary embolism, angina
IV or SC-> IV effect immediate, SC effect 1-2 hours
MOA: inducing antithrombin III to inhibit Xa
Is not consumed during reaction-> higher the dose, higher the 1/2 life
Cannot cross placenta
Increased bioavailability, less frequent dosing, and monitoring not necessary compared to HMW heparin
SE: less chance of HIT compared to HMW heparin, bleeding, decreased clearance in renal disease
Contraindications: HIT, hemophilia, hypersensitvity, hemorrhage, sever hypertension, recent surgery of eye, brain, spinal cord |
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Term
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Definition
Parenteral anticoagulant; synthetic derivative-> effective against venous thrombosis, pulmonary embolism, angina, myocardial infarction
IV or SC-> IV effect immediate, SC effect 1-2 hours
MOA: inducing antithrombin III to inhibit Xa
Is not consumed during reaction-> higher the dose, higher the 1/2 life
Cannot cross placenta
Increase bioavailability, less frequent dosing, and monitoring not necessary compared to HMW heparin
SE: least likely to trigger HIT, bleeding
Contraindications: HIT, hemophilia, hypersensitvity, hemorrhage, sever hypertension, recent surgery of eye, brain, spinal cord |
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Term
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Definition
Used in heparin overdose
IV
MOA: very basic peptide that binds heparin
Does not work for fondaparinux |
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Term
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Definition
Anticoagulant in leech saliva
MOA: irreversibly binds thrombin |
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Term
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Definition
Parenteral anticoagulant; recombinant hirudin
MOA: directly inhibits thrombin by binding to catalytic site
Used in patients w/ HIT; caution in those w/ renal insufficiency b/o clearance |
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Term
|
Definition
Parenteral anticoagulant
MOA: directly inhibits thrombin
Used in patients undergoing coronary angioplasty |
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Term
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Definition
Parenteral anticoagulant
MOA: reversibly binds thrombin catalytic site
Metabolized by P450s, so caution in those w/ hepatic insufficiency |
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Term
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Definition
Parenteral anticoagulant; mix of non-heparin GAGs
Prophylaxis for deep venous thrombosis; used in patients w/ HIT
MOA: promotes inhibition of Xa by antithrombin III |
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Term
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Definition
Oral anticoagulant
MOA: blocks gamma-carboxylation of glutamate residues in prothrombin, VII, IX, X by preventing vitamin K reduction
8 hour delay for effect; long 1/2 life
SE: crosses the placenta-> hemorrhagic disease, bone deformities; bleeding
Drug Interactions: pharmacodynamic-> barbituates induce cytP450s; pharmacokinetic-> vitamin K reduces the effect by increasing clotting factors
Excess bleeding can be stopped by vitamin K or recombinant factor VIIa |
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Term
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Definition
Fibrinolytic; not an enzyme itself
MOA: forms complex w/ plasminogen that catalyzes conversion to plasmin
Indications: peripheral arterial and venous thrombi |
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Term
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Definition
Fibrinolytic; human enzyme produced by kidney
MOA: directly converts plasminogen to plasmin |
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Term
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Definition
Fibrinolytic
MOA: purified human plasminogen + streptokinase
More selective for clot plasminogen when given via continuous IV |
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Term
| Tissue plasminogen activator (t-PA) |
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Definition
Fibrinolytic
MOA: preferentially activates plasminogen bound to fibrin-> confines fibrinolysis to thrombus, but can lyse all thrombi
Approved for use in acute ischemic stoke w/in 3 hours of onset |
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Term
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Definition
Fibrinolytic; recombinant human t-PA
MOA: activates plasminogen, but lacks the fibrin binding domain, so less fibrin specific than t-PA |
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Term
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Definition
Fibrinolytic; mutant t-PA
MOA: activates plasminogen and is more fibrin specific than t-PA
Long 1/2 life; given as IV bolus |
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Term
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Definition
Antiplatelet
MOA: irreversibly acetylates and inactives COX1, reducing TXA2 synthesis (TXA2 = vasconstriction, pro-clotting; so is serotonin)
Low dose therapy for primary prophylaxis of myocardial infarction |
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Term
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Definition
Antiplatelet
MOA: inhibits ADP pathway activation of platelets by blocking ADP receptors on platelets
Prevent thrombosis during coronary stent placement
SE: few |
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Term
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Definition
Antiplatelet
MOA: inhibits ADP pathway activation of platelets by blocking ADP receptors on platelets
Prevent thrombosis during coronary stent placement
SE: nausea, dyspnea, diarrhea, hemorrhage, leukopenia, TTP |
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Term
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Definition
Fibrinolytic; parenteral
MOA: monoclonal antibody directed against IIb-IIIa receptor complex, blocking interaction b/w platelet and fibrinogen, vitronectin, fibronectin
Use in percutaneous coronary intervention and in acute coronary syndrom |
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Term
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Definition
Fibrinolytic; parenteral
MOA: analog of the carboxy terminal sequence of the delta chain of fibrinogen, preventing fibrinogen binding to IIb-IIIa via competitive inhibition |
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Term
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Definition
Bleeding disorder prevention; K1 given to newborns
K1- found in food; clinically in oral and parenteral forms
K2- found in human tissues; made by bacteria
MOA: helps in synthesis of thrombin, VII, IX, X, protein C, protein S by aiding in gamma-carboxylation of glutamate residues
SE: rapid infusion of K1-> dyspnea, chest and back pain, death |
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Term
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Definition
Treat bleeding disorders via plasma fractions
MOA: increases factor VIII activity in those w/ mild hemophilia A or von Willebrand disease |
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Term
| Autoplex, FEIBA (factor eight inhibitor bypassing activity) |
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Definition
Treat bleeding disorders via plasma fractions
MOA: factor IX concentrates that contain activated clotting factors; treat patients w/ inhibitors or Abs to factor VIII or IX
SE: might increase qualitative abnormalities of fibrinogen |
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Term
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Definition
Treat bleeding disorders; plasma protein fraction from whole blood
MOA: treat deficiencies or qualitative abnormalities of fibrinogen or in patients w/ factor VIII deficiency or vWF disease |
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Term
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Definition
Treat bleeding disorders; synthetic inhibitor of fibrinolysis
MOA: competitively inhibits plasminogen activation
Adjunct therapy for hemophilia, therapy for bleeding from fibrinolytic therapy, prophylaxis from intracranial aneurysms
SE: intravascular thrombosis, hypotension, GI discomfort |
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Term
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Definition
Treat bleeding disorders
MOA: serine protease inhibitor; inhibits plasmin
Use in patients undergoing coronary bypass grafting-> reduces blood loss
SE: anaphylaxis |
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Term
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Definition
Platelet antagonist
Lowers peripheral, pulmonary, and coronary resistance |
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Term
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Definition
Antiplatelet
MOA: vasodilation; inhibits platelet activity by inhibiting adenosine uptake and cGMP phosphodiesterase
Used in combination w/ aspirin |
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Term
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Definition
Antidote for acute arsenic poisoning or for acute lead poisoning (in combo w/ EDTA)
MOA: chelation via -SH
Given IM as 10% solution in peanut oil
Excreted by kidney w/in 48 hours
SE: HTN, tachycardia, nausea, vomiting, lacrimation, salivation, fever in children, may redistribute the the CNS |
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Term
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Definition
Antidote for acute arsenic poisoning or in conjunction w/ dimercaprol for lead poisoning in children
Oral, water soluble analog of dimercaprol
MOA: chelation via disulfide moieties
SE: GI, rash |
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Term
| Edetate calcium disodium (EDTA) |
|
Definition
Lead chelator; also used for zinc, magnesium, and radionuclide poisoning
MOA: chelation via O and N extracellularly (too polar to enter cells)
Administered IV as calcium disodium salt or risk depletion of calcium stores; poor oral absorption which may increase lead absorption
Excreted by kidneys; contraindicated in renal insufficiency
SE: nephrotoxicity |
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Term
|
Definition
Chelation of arsenic and lead; water soluble analog of dimercaprol
Alternative to IM dimercaprol/oral succimer for acute arsenic poisoning and oral succimer for lead poisoning
MOA: chelation
Oral or IV
SE: vasodilation and hypotension if IV infused too quickly |
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Term
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Definition
Chelation of copper or lead; oral
Rapidly enters CNS to decrease copper levels in Wilson's disease
MOA: chelation -NH2 and -SH
SE: hypersensitivity, nephrotoxicity, pancytopenia |
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Term
|
Definition
Iron chelation
Poor oral absorption-> IV or IM slow to prevent hypotension
MOA: chelation of non-biologically chelated iron
SE: flushing, fever, GI discomfort, rash, pulmonary complications, neurotoxicity, increased risk of infection |
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Term
|
Definition
Historic antimicrobial which contained arsenic
SE: cancers |
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Term
|
Definition
Prevention of hemolytic disease of the newborn
Given to Rho(D)- mother after birth, miscarriage, or abortion of Rho(D)+ baby
MOA: plasma derived IgG that clears infants RBCs from maternal circulation before memory B cell generation
SE: rare; injection site discomfort, slight fever, risk of infectious disease transmission b/c plasma derived |
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Term
| Intravenous immunoglobulin (IVIG) |
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Definition
Non-specific polyclonal IgG prepared from donor pools
Treatment of Ig deficiency, autoimmune disorders, HIV, BM transplants, Lupus
MOA: reduction in T-helper cells, increases T cell suppressors, blocking Fc receptor |
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Term
|
Definition
IVIG preparation from donors immunized against specific toxins or viruses-> VZV, rabies, tetanus, hepatitis B
MOA: passive transfer of high titer antibodies to reduce risk/severity of infection
SE: risk of infusion acquired disease |
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