Pharm Flashcards
(38 cards)
Heparin MOA
Activates antithrombin, which decreases action of IIa (thrombin) and factor Xa
LMWH acts predonminantly on factor Xa
Fondaparinux acts only on factor Xa
Acts in blood
Which anticoagulant does not cross the placenta?
Heparin
Which are the direct thrombin inhibitiors?
Bivalirudin
Argatroban
Dabigatran
Warfarin MOA
Interferes with gamma-carboxylation of vitamin-K dependent clotting facotrs II, VII, IX, and X, and protein C and S
Affects on extrinsic pathway (increases PT)
Acts @ liver
Which are the direct factor Xa inhibitors?
Apixaban
Rivoroxaban
How do thrombolytics work?
Directly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots
Increases PT
Increases PTT
No change in platelet count
Which are the ADP receptor inhibitors?
clopidogrel
prasugrel
ticagrelor (reversible)
ticlopidine
How do ADP receptor inhibitors work?
Inhibit platelet aggregation by irreversibly blocking ADP (P2Y12) receptor
Prevent expression of glycoproteins IIb/IIIa on platelet surface
Which are the glycoprotein IIb/IIIa inhibitors?
Abciximab - made from monoclonal antibody Fab fragments
Eptifibatide
Tirofiban
(prevent platelet agg)
Azathioprine MOA and use
Purine (thiol) analog
Leads to decreased purine synthesis
Metabolized into 6-MP
Used to prevent organ rejection, RA, IBD, SLE
With which medications should azathioprine NOT be used?
Azathioprine and 6-MP are metabolized by xanthine oxidase; therefore, both have increased toxicity when used with allopurinol or febuxostat
Cladribine MOA, use, and adverse effects
Purine analog with multiple mechs (inhibition of DNA polymerase, DNA strand breaks)
Used in hair cell leukemia
SEs: myelosuppression, nephrotoxicity, neurotoxicity
Cytarabine MOA, use, and adverse effects
Pyrimidine analog that results in DNA chain termination. At higher doses, also inhibits DNA pol
Used for leukemias and lymphomas
SEs: myelosuppression with megaloblastic anemia (“CYTarabine with panCYTopenia”)
5FU MOA, use, and adverse effects
Pyrimidine analog bioactivated to 5-FdUMP, which complexes with thymidylate synthase and folic acid
Complex inhibits thymidylate synthase, leading to decreased dTMP and decreased DNA synthesis
Used in colon cancer, pancreatic cancer, actinic keratosis, basal cell carcinoma
SEs: myelosuppression, palmar-plantar erythrodysesthesia (hand-foot syndrome)
Methotrexate MOA, use, and adverse effects
Folic acid analog that competitively inhibits dihydrofolate reductase, leading to decreased dTMP and decreased DNA synthesis
Used in lymphomas, leukemias, choriocarcinoma, sarcomas. Non-neoplastic: can also be used in ectopic pregnancy, medical abortion (with misoprostol), RA, PsC, IBD, vasculitis
SEs: myelosuppression, hepatotoxicity, mucositis, pulmonary fibrosis, folate deficiency, rare nephrotoxicity
Bleomycin MOA, use, and adverse effects
Antitumor antibiotic
Induces free radical formation, leading to breaks in DNA strands
Used in testicular cancer and Hodgkin’s lymphoma
SEs: Pulmonary fibrosis, skin hyperpigmentation
Dactinomycin MOA, use, and adverse effects
Antitumor antibiotic
Intercalates into DNA, preventing RNA synthesis
Used in Wilms tumor, Ewing sarcoma, rhabdomyosarcoma; also used for childhood tumors
SEs: myelosuppresion
Doxorubicin MOA, use, and adverse effects
Antitumor antibiotic
Generates free radicals. Intercalates DNA leading to breaks in DNA and decreased replication. Interferes with topoisomerase II enzyme
Used in solid tumors, leukemias, lymphomas
SEs: cardiotoxicity (dilated cardiomyopathy), myelosuppression, alopecia
Dexrazoxane can be used to prevent cardiotoxicyt
Busulfan MOA, use, and adverse effects
Alkylating agent
Cross-links DNA
Used to ablate patient’s bone marrow before bone marrow transplantation
SEs: severe myelosuppression (in almost all cases), pulmonary fibrosis, hyperpigmentation
Cyclophosphamide and/or ifosfamide MOA, use, and adverse effects
Alkylating agent
Cross-link DNA at guanine
Requires bioactivation by liver
Used in solid tumors, leukemia, lymphomas
SEs: myelosuppression, SIADH, hemorrhagic cystitis
- NOTE: hem cystitis is prevented with mesna and/or adequate hydration
Nitrosoureas MOA, use, and adverse effects
Alkylating agent
Requires bioactivation. Cross blood-brain barrier. Cross-links DNA.
Used for brain tumors (including GBM)
SEs: CNS toxicity (convulsions, dizziness, ataxia)
Procarbazine MOA, use, and adverse effects
Alkylating agent
Cell cycle phase: nonspecific alkylating agent (mech not yet defined)
Used for Hodgkin lymphoma, brain tumors
SEs: bone marrow suppression, pulmonary toxicity, leukemia
Taxanes (aka paclitaxel) MOA, use, and adverse effects
Microtubule inhibitor
Hyperstabilizes polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur)
Used for ovarian and breast carcinomas
SEs: myelosuppression, neuropathy, hypersensitivity
Vincristine, vinblastine MOA, use, and adverse effects
Microtubule inhibitor
Vinca alkaloids that bind beta-tubulin and inhibit its polymerization into microtubules leading to prevention of mitotic spindle formation (M-phase arrest)
Used for solid tumors, leukemias, Hodgkin’s (vinblastine) and Non-Hodgkin’s (vincristine) lymphomas
SEs: Vincristine: neurotoxicity (areflexia, peripheral neuritis), constipation (including paralytic ileus)
Vinblastine: bone marrow suppression - “blasts the bone marrow”
