Term
|
Definition
Cofactor for ATIII. Reduces thrombin and Xa.
Immediate anticoagulation. OK during pregnancy. Monitor with aPTT.
Bleeding, HIT, osteoporosis, drug-drug interactions. Protamine sulfate for antidote. |
|
|
Term
|
Definition
| Low molecular weight heparin. Acts more on Xa, better bioavailability, 2-4 longer half-life. Less HIT risk. No laboratory monitoring needed. No antidote. |
|
|
Term
|
Definition
Hirudin derivative, directly inhibits thrombin.
Alternative to hepain, use in patients with HIT. |
|
|
Term
|
Definition
Hirudin derivative, directly inhibits thrombin.
Alternative to hepain, use in patients with HIT. |
|
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Term
|
Definition
Interferes with gamma-carboxylation of II, VII, IX, X, C, S (vitamin K dependent factors). Long half-life, P450 metabolized, plasma protein binding. Monitor with PT.
Use for chronic anticoagulation, NOT in pregnant women (crosses placenta).
Bleeding, teratogen, skin/tissue necrosis, DDIs. Vitamin K for OD, FFP for rapid reversal. |
|
|
Term
|
Definition
Thrombolytic; aids conversion of plasminogen to plasmin, which cleaves thrombin and fibrin.
Early MI, stroke.
Bleeding - intracranial, recent surg, severe HTN. Give aminocaproic acid or tranexamic acid: inhibits plasminogen activation. |
|
|
Term
|
Definition
Thrombolytic; aids conversion of plasminogen to plasmin, which cleaves thrombin and fibrin.
Early MI, stroke.
Bleeding - intracranial, recent surg, severe HTN. Give aminocaproic acid or tranexamic acid: inhibits plasminogen activation. |
|
|
Term
tPA (alteplase)
mech
use
tox |
|
Definition
Thrombolytic; aids conversion of plasminogen to plasmin, which cleaves thrombin and fibrin.
Early MI, stroke.
Bleeding - intracranial, recent surg, severe HTN. Give aminocaproic acid or tranexamic acid: inhibits plasminogen activation. |
|
|
Term
| APSAC (anistreplase) mech use tox |
|
Definition
= plasminogen + streptokinase
Anisoylated Plasminogen Streptokinase Activator Complex
Thrombolytic; aids conversion of plasminogen to plasmin, which cleaves thrombin and fibrin.
Early MI, stroke.
Bleeding - intracranial, recent surg, severe HTN.
Give aminocaproic acid or tranexamic acid: inhibits plasminogen activation. |
|
|
Term
|
Definition
inhibits plasminogen activation
use for reversal of thrombolytics (streptokinase, tPA, urokinase, APSAC) |
|
|
Term
|
Definition
inhibits plasminogen activation
use for reversal of thrombolytics (streptokinase, tPA, urokinase, APSAC) |
|
|
Term
|
Definition
Irreversibly block ADP receptor on platelets, prevent GpIIb/IIIa expression, less fibrinogen binding.
*P450 activated.
Acute coronary syndrome; coronary stenting. Decreases incidence of thrombotic stoke. Neutropenia, TTP, hemorrhage. |
|
|
Term
|
Definition
Irreversibly block ADP receptor on platelets, prevent GpIIb/IIIa expression, less fibrinogen binding.
Acute coronary syndrome; coronary stenting. Decreases incidence of thrombotic stoke.
Neutropenia, TTP, hemorrhage. |
|
|
Term
|
Definition
Antibody to GpIIb/IIIa. Prevents aggregation.
Acute coronary syndrome, percutaneous interventions.
Bleeding, thrombocytopenia. |
|
|
Term
|
Definition
Folic acid analog, inhibits DHFR.
Leukemias, lymphomas, choriocarcinoma, sarcomas. Abortion, ectopic pregnancy, rheumatoid arthritis, psoriasis.
Myelosuppresion (leucovorin rescue). Macrovesicular liver steatosis. Mucositis. Teratogenic. |
|
|
Term
5-fluorouracil (5-FU)
mech
use
tox |
|
Definition
Pyrimidine analog. Metabolized to 5F-dUMP. Covalently complexes with folic acid, inhibits thymidylate synthase.
Colon cancer, other solid tumors, topical for basal cell carcinoma. Synergy with methotrexate.
Myelosuppresion (no leucovorin rescue! Rescue with thymidine). Photosensitivity. |
|
|
Term
6-mercaptopurine (6-MP)
mech
use
tox |
|
Definition
Purine (thiol) analog, inhibit purine synthesis.
Activated by HGPRT.
Leukemias, lymphomas.
Bone marrow, GI, liver toxicity. Metabolized by xanthine oxidase, increased toxicity with allopurinol. |
|
|
Term
6-thioguanine (6-TG)
mech
use
tox |
|
Definition
Purine analog, inhibit purine synthesis. Activated by HGPRT.
ALL
Myelosuppression, liver toxicity. Metabolized by xanthine oxidase, toxicity with allopurinol. |
|
|
Term
Cytarabine (ara-C)
mech
use
tox |
|
Definition
Pyrimidine analog (cytosine arabinoside). Inhibits DNA polymerase.
AML, ALL, NHL.
Leukopenia, thrombocytopenia, megaloblastic anemia. |
|
|
Term
|
Definition
Intercalates in DNA, generates free radicals.
Wilms tumor, Ewings sarcoma, rhabdomyosarcoma. CHILDHOOD TUMORS.
Myelosuppression. |
|
|
Term
Doxorubicin (Adriamycin)
mech
use
tox |
|
Definition
Generates free radicals. Intercalates DNA. Inhibits topoisomerase II.
Hodgkins lymphoma, myelomas, sarcomas, solid tumors.
Dilated cardiomyopathy, myelosuppression, alopecia. Extravasation hazard. |
|
|
Term
|
Definition
Free radical formation.
Testicular cancer, Hodgkin's lymphoma.
Pulmonary fibrosis, skin changes. *minimal myelosuppression. |
|
|
Term
|
Definition
Inhibits topoisomerase II.
SCLC, prostate, testicular cancer.
Myelosuppression, GI irritation, alopecia. |
|
|
Term
|
Definition
Inhibits topoisomerase I
Chemotherapy |
|
|
Term
|
Definition
Inhibits topoisomerase I
chemotherapy |
|
|
Term
Cyclophosphamide
mech
use
tox |
|
Definition
Alkylating agent. Covalent interstrand DNA crosslink. Requires liver bioactivation.
NHL, breast, ovary. Immunosuppression.
Myelosuppression. Hemorrhagic cystitis, give with MESNA tp prevent. |
|
|
Term
|
Definition
Alkylating agent. Covalent interstrand DNA crosslink. Requires liver bioactivation.
NHL, breast, ovary. Immunosuppression.
Myelosuppression. |
|
|
Term
|
Definition
Nitrosurea: DNA interstrand crosslinking.
Requires activation; enters CNS.
Brain tumors.
Dizziness, ataxia. |
|
|
Term
|
Definition
Nitrosurea: DNA interstrand crosslinking.
Requires activation; enters CNS.
Brain tumors.
Dizziness, ataxia. |
|
|
Term
|
Definition
Nitrosurea: DNA interstrand crosslinking.
Requires activation; enters CNS.
Brain tumors.
Dizziness, ataxia. |
|
|
Term
|
Definition
Nitrosurea: DNA interstrand crosslinking.
Requires activation; enters CNS.
Brain tumors.
Dizziness, ataxia. |
|
|
Term
|
Definition
Alkylates DNA
CML. Pre-BMT ablation.
Pulmonary fibrosis, hyperpigmentation. |
|
|
Term
|
Definition
Microtubule inhibitor. Binds tubulin, M phase cannot continue.
Hodgkins, Wilms, choriocarcinoma.
*Peripheral neurotoxicity (areflexia, peripheral neuritis, paralytic ileus). |
|
|
Term
|
Definition
Microtubule inhibitor. Binds tubulin, M phase cannot continue.
Hodgkins, Wilms, choriocarcinoma.
*Bone marrow suppression. |
|
|
Term
| Paclitaxel and other -taxols |
|
Definition
STABILIZE microtubules, block M-phase.
Ovary, breast.
Myelosuppression, hypersensitivity. |
|
|
Term
|
Definition
Cross-link DNA (C for crosslink)
Test, bladder, ovary, lung
Nephrotoxicity, acoustic nerve damage (can't pee, can't hear a high C)
Use Amifostine to protect from nephrotoxicity, (thiol-based free-radical scavenger), or chloride diuresis (IV saline). |
|
|
Term
|
Definition
Cross-link DNA (C for crosslink)
Test, bladder, ovary, lung
Nephrotoxicity, acoustic nerve damage (can't pee, can't hear a high C)
Use Amifostine to protect from nephrotoxicity, (thiol-based free-radical scavenger), or chloride diuresis (IV normal saline). |
|
|
Term
|
Definition
Inhibit ribonucleotide reductase, inhibit DNA synth
melanoma, CML, sickle cell disease (increases HbF)
Myelosuppression, GI upset |
|
|
Term
|
Definition
Selective Estrogen Receptor Modifier - antagonist in breast, agonist in bone.
Breast cancer, osteoporosis.
May increase endometrial carcinoma risk via partial agonist effects. Hot flashes. |
|
|
Term
|
Definition
Selective Estrogen Receptor Modifier - antagonist in breast, agonist in bone.
Breast cancer, osteoporosis.
Endometrial antagonist, no endometrial carcinoma risk (vs. Tamoxifen) |
|
|
Term
|
Definition
aka Herceptin
Antibody to HER-2 receptor (erb-B2 gene).
BrCa with HER-2 expression.
Cardiotoxic. |
|
|
Term
|
Definition
aka Gleevec
Inhibits bcr-abl (philadelphia chromosome tyr kinase receptor)
CML, GI stromal tumors
Fluid retention |
|
|
Term
|
Definition
aka Gleevec
Inhibits bcr-abl (philadelphia chromosome tyr kinase receptor)
CML, GI stromal tumors
Fluid retention |
|
|
Term
|
Definition
Antibody to CD20
NHL, rheumatoid arthritis (with methotrexate) |
|
|
Term
|
Definition
Selective COX-2 inhibitor
Avoids normal NSAID adverse effects of GI ulceration, and inhibited platelet aggregation - purely anti-inflammatory.
However, long-term use linked to increased thrombotic risk, which may be due to decrease production of prostacyclin. |
|
|
Term
|
Definition
Block calcium-dependent potassium channels (Gardos) on RBCs. Prevent cellular dehydration, heme polymerization.
For sickle cell anemia. |
|
|
Term
|
Definition
| Traditional NSAID; reversible non-selective COX inhibitor. |
|
|
Term
|
Definition
| Tradiational NSAID; reversibly inhibits COX, non-selective |
|
|
Term
|
Definition
| Tradiational NSAID; non-selective, reversible COX inhibition |
|
|
Term
|
Definition
AKA leucovorin
readily converted to THF
For methotrexate rescue |
|
|
Term
|
Definition
Prodrug; converted to 5-FU in tumor.
CRC, breast
Cardiotoxic, dermatitis, GI, myelosuppression, thrombocytopenia |
|
|
Term
|
Definition
deoxycytidine analog; causes DNA synthesis stop
lung, pancreas, bladder, breast
Fever, fatigue, N/V, rash, hair loss, sores |
|
|
Term
|
Definition
Purine analog
Effective for CLL
Lymphopenia, anemia, thrombocytopenia |
|
|
Term
|
Definition
Purine analog (adenosine); adenosine deaminase resistant.
Hairy cell leukemia
Fever; otherwise well tolerated |
|
|
Term
|
Definition
Methylating agent; requires hepatic activation.
Melanoma, lymphomas, sarcoma.
N/V, myelosupression, sterility |
|
|
Term
|
Definition
Directly inhibits thrombin
Alternative to heparin, use in patients with HIT |
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|
