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Hematology pharmacology - Coggle Diagram
Hematology pharmacology
heparin
can use during pregnancy
adverse: bleedig, thrombocytopenia, osteoporosis
immediate anticoagulation for PE, ACS, MI, DVT
subcutaeously, without monitorig, not easily reversible
activate antithrombin→↓ action of factor 2a and 10a, short half time
heparin-induced thrombocytopenia: antibody-heparin-PF4 complex activate platelets
direct thrombin inhibitors
for venous thromboembolism, AF
inhibit activity of free and clot-associated thrombin
warfarin
have effect on extrinsic pathway and ↑PT, long half life
for chronic anticoagulation, not used in pregnant women
interfere with γ-carboxylation of vitaminK-dependent clotting factors 2,7,9,10 and protein C and S
adverse: bleeding, teratogenic, skin/tissue necrosis, hypercoagulation (protein C deplete before factor 2 and 10 deplete
for reversal of warfarin, give vitamin K, FFP or PCC(rapid)
initial heparin therapy reduces risk of recurrent venous thromboembolism and skin/tissue necrosis
direct factor 10a inhibitor
for treatment and prophylaxis of DVT and PE, prophylaxis of stroke
directly inhibit factor 10a
thrombolytics
aid conversion of plasminogen to plasmin→cleaves thrombin and fibrin clot, ↑PT, PTT
for early MI, early ischemic stroke, severe PE
tPA, rPA, etc
bleeding, contraindicated in active bleeding, history of intracranial bleeding, recent surgery, severe hypertension
ADP receptor inhibitor
for ACS
inhibit platelet aggregation by irreversible blocking ADP receptor, prevent expression of Gp2b/3a
cilostazol, dipyridamole
for intermittent claudication(間欠性跛行), coronary vasodilation, prevention of stroke or TIA
phosphodiesterase inhibitor, ↑cAMP, inhibition of platelet aggregation, vasodilator
Gp2b/3a inhibitor
for unstable angina, percutaneous coronary intervention
bind to Gp2b/3a on activated platelet, preventing aggregation
cancer drug
antimetabolites
prevent DNA synthesis
azathioprine, 6-mercaptopurine
for preventing organ rejection, rheumatoid arthritis, IBD, SLE
adverse: myelosupression, GI, liver toxicity
azathioprine is metabolized into 6-MP, ↓de nove purine synthesis
cladribine
adverse: myelosuppression, nephrotoxicity, neurotoxicity
for hairy cell leukemia
purine analog
cytarabine
AML, lymphoma
myelosuppression, megaloblastic anemia
pyrimidine analog, DNA chain termination
5-fluorouracil
colon cancer, pancreatic cancer, actinic keratosis, basal cell carcinoma
myelosuppression, palmer planter syndrome
pyrimidine analog bioactivated to 5-FdUMP, complex with thymidine synthase and folic acid, complex inhibit dihydrofolate reductase→↓dTMP→↓DNA synthesis
methotrexate
ALL, lymphomas, choriocarcinoma, sarcoma, ectopic pregnancy, medical abortion, rheumatoid arthritis, psoriasis(乾癬), IBD, vasculitis
adverse: myelosuppressio, hepatotoxicity, mucositis, pulmonary fibrosis, etc
folic acid analog inhibit dihydrofolate reductase→↓dTMP→↓DNA synthesis
antitumor antibiotics
dactinomycin
prevent RNA synthesis
for Wilms tumor, Ewing sarcoma, rhabdomyosarcoma(横紋筋肉腫)
adverse: myelosuppression
doxorubicin, daunorubicin
generate free radical, breaks in DNA, interfere with topoisomerase 2 enzyme
for solid tumor, leukemia, lymphoma
adverse: cardiotoxicity, myelosuppression, alopecia
bleomycin
for testicular cancer, Hodgkin lymphoma
free radical formation→breaks in DNA strands
alkylating agent
cyclophosphamide, ifosfamide
for solid tumor, leukemia, lymphoma
adverse: myelosuppression, SIADH, hemorrhagic cystitis
closs link DNA at guanine
nitrosoureas
require bioactivation, closs BBB, cross link DNA
for brain tumor
busulfan
cross-link DNA
ablate bone marrow
adverse: myelosuppression, pulmonary fibrosis, hyperpigmentation
procarbezine
Hodgkin lymphoma, brain tumors
mechanism not yet defined
microtubule inhibitor
paclitaxel, other taxanes
for ovarian and breast carcinoma
mitotic spindle cannot break down
vincristine, vinblastine
for solid tumor, leukemia, Hodgkin and non-Hodglin lymphoma
bind β-tubulin, prevent mitoic spindle formation
other drug
etoposide, teniposide
inhibit topoisomerase2→↑DNA degradiation
for solid tumor, leukemia, lymphoma
imatinib
tyrosine kinase inhibitor of BCR-ABL and c-kit
for CML, GI stromal tumor
cisplatin, carboplatin
cross-link DNA
for testicular, bladder, ovary, and lung carcinoma
adverse: nephrotoxicity, peripheral neuropathy, ototoxicity
irinotecan, topotecan
inhibit topoisomerase 1 and prevent DNA unwinding and replication
for colon cancer, ovarian and small cell lung cancer
hydroxyurea
inhibit ribonucleotide reductase→↓DNA synthesis
for myeloproliferative disorders, sickle cell
severe myelosuppression
bevacizumab
monoclonal antibody against VEGF, inhibit angiogenesis
for solid tumor, wet age-related macular degeneration
erlotinib
EGFR thyrosine kinase inhibitor
non-small cell lung carcinoma
cetuximab
monoclonal antibody against EGFR
colorectal cancer, head and neck cancer
rituximab
monoclonal antibody against CD20 (on most Bcell neoplasm)
for non Hodgkin lymphoma, CLL, ITP, rheumatoid arthritis
bortezomib, carfilzomib
proteasome inhibitor, induce arrest at G2-M phase and apoptosis
for multiple myeloma, mantle cell lymphoma
tamoxifen, raloxifene
selective estrogen receptor modulator
for breast cancer
trastuzumab
monoclonal antibody against HER-2, a thyrosine kinase receptor
for breast cancer, gastric cancer
adverse: cardiotoxicity
vemurafenib
small molecule inhibitor of BRAF oncogene melanoma
for metastatic melanoma
resburicase
recombinant uricase that catalyzes metabolism of uric acid to allantoin
for tumor lysis syndrome