Drugs Flashcards
Heparin
Mechanism
Toxicity
Types
Mechanism
Binds antithrombin so it can inhibit II and X
Toxicity
Bleeding
Osteoporosis
Heparin Induced TCP (Ab binds heparin/PF4 complex) –> thrombosis.
Reverse with protamine sulfate
Types
Low molecular weight (mostly 10) - subQ and not easily reversible
Unfractionated (mostly 2) - IV and reversible
Argatrobran and Bivalirudin
Mechanism
Uses
Mechanism
Blocks Factor II (thrombin)
Uses
Heparin Induced TCP
Warfarin (Coumadin)
Mechanism
Uses
Toxicity
Mechanism
Inhibits Vitamin K Epoxide Reductase so Vitamin K cannot be regenerated to y carboxylate 2, 7, 9, 10 C and S. (Metabolized by p450).
Uses
Anticoagulation but not in pregnancy.
Toxicity
Bleeding
Teratogenic
Warfarin Induced Skin Necrosis (Protein C deficiency)
Reverse with fresh frozen plasma and Vitamin K
Apixaban and Rivaroxaban
Mechanism
Uses
Toxicity
Mechanism
Inhibit Factor X (like FondaparineuX)
Uses
Anticoagulation and does not require monitoring when taken orally.
Toxicity
Bleeding without a reversal agent.
Thrombolytics Name Mechanism Use Toxicity
Name
Alteplase, reteplase, teneteplase
Mechanism
TPA which convert plasminogen to plasmin
Use
To lyse clots in PE, MI, Stroke etc.
Toxicity
Bleeding (never in active bleeding, recent surgery or severe hypertension)
Reverse with aminocaproic acid (inhibits fibrinolysis) and administer cryoprecipitate.
Aspirin
Mechanism
Use
Toxicity
Mechanism Blocks COX (covalent acetylation) which prevents TXA2 and PGs from being released by platelets to promote 2nd wave of aggregation.
Use Antiplatelet Antipyretic Antiinflammatory Analgesic
Toxicity
1) Renal failure and necrosis
2) GI ulceration and bleeding
3) Reye syndrome in kids with viral syndrome
4) Respiratory and metabolic alkalosis
ADP receptor inhibitors Name Mechanism Use Toxicity
Name
Clopidogrel, Prasugrel, Ticagrelor, Ticlopidine
Mechanism
Blocks ADP receptor (PSY12) for platelets, which cross links fibrinogen.
Use
Anti-platelet.
MI , stents, strokes.
Toxicity
Ticlopidine - neutropenia.
TTP/HUS may be seen
Cilostazol and Dipyridamole
Mechanism
Use
Toxicity
Mechanism
PDEIII inhibitor. Prevent platelets from making cAMP and aggregating. Vasodilates.
Use
Claudication, TIA, angina, stroke prevention.
Toxicity
Facial flushing, hypotension.
GPIIbIIIa inhibitors Name Mechanism Use Toxicity
Name
Abciximab, eptifibatide, tirofiban
Mechanism
GPIIbIIIa inhibitors, prevent platelet aggregation.
Use
Unstable angina, PCI.
Toxicity
Bleeding, thrombocytopenia.
Cell cycle drugs
M - Vina alkaloids and taxols
S - Antimetabolites
S and G2 - Etoposide
G2 - Bleomycin
What drugs inhibit nucleotide synthesis?
5-FU and MTX
Inhibit thymidine
6-MCP
Inhibit Purine
What drugs inhibit DNA replication?
1) Cross link DNA
Alkylating agents and Cisplatin
2) DNA intercalators
Dactinomycin and doxorubicin
3) Inhibit topoisomerase
Etoposide
What drugs inhibit cell division?
1) Inhibit microtubule formation
Vinka alkaloids
2) Inhibit microtubule disassembly
Paclitaxel
Methotrexate
Mechanism
Use
Toxicity
Mechanism Inhibit DHFR (folate analogue) which inhibits dTMP synthesis
Use
Cancer, abortion, RA, psoriasis and IBD
Toxicity - 3Ms
1) Myelosuppression reversible with leucovorin rescue
2) Mucositis
3) Macrovesicular fatty change in liver
5FU
Mechanism
Use
Toxicity
Mechanism
Pyrimidine analogue which blocks thymidilate synthase and inhibits dTMP synthesis
Use
Cancer (colon, pancreas, basal cell)
Toxicity
Photosensitive (Fotosensitive FU)
Myelosuppression (can’t use leucovorin)
Overdose reversal: Uridine
Cytarabine (arabinofuranosyl cytidine)
Mechanism
Use
Toxicity
Mechanism
Pyrimidine analogue which inhibits DNA polymerase
Use
Leukemia and lymphoma
Toxicity
Pancytopenia (Cytapenia)
Azathioprine 6-MP 6-thioguanine Mechanism Use Toxicity
Mechanism
Purine analogues which block de novo purine synthesis (activated by HGPRT)
Use
Azathioprine (organ rejection, RA, SLE)
6-MP and 6-thioguanine (Leukemia, IBD)
Toxicity
Allopurinol increases toxicity (bc xanthine oxidase cannot break down Azathioprine
and 6-MP)
Also bone marrow, liver, GI tract.
Dactinomycin (actinomycin D)
Mechanism
Use
Toxicity
Mechanism
DNA intercalator
Use Childhood tumors (children ACT out) Wilm's, Ewing, Rhadbomyosarcoma
Toxicity
Myelosuppression