Parenteral anticoagulation (I/V) Amboss Flashcards
Unfractionated heparin (UFH). What drug?
Heparin
What is heparin administration for prophylaxis?
subcutaneous
What is heparin administration for therapeutic?
continuous intravenous infusion (therapeutic administration requires infusion pump)
Heparin monitoring?
aPTT and platelet count
including PLT baseline before treatment is started
Heparin clearance?
Clearance: hepatic (preferred agent for patients with renal insufficiency)
Heparin’s antidote?
Protamine sulfate
Charge of heparin?
negative
protamine sulfate charge?
positive
Why protamine sulfate binds heparin?
positively-charged protein that can neutralize negatively-charged heparin by forming inactive complexes
What drug is preferred for renal insufficiency?
Heparin - because its clearance is hepatic, not renal
What to monitor when use heparin in order to detect HIT?
platelets must be continuously monitored during heparin therapy and a baseline should be established before commencing treatment
Low molecular weight heparin (LMWH) drugs?
enoxaparin, dalteparin, tinzaparin, nadroparin, certoparin
LMWH. Administration?
Subcutaneous
LMWH. Monitoring?
Anti-factor Xa activity can be assessed in specific cases; not generally recommended –>
Only necessary in specific cases, e.g., patients with renal failure, underweight/overweight, as there is a risk of accumulation or underdosing. Anti-factor Xa activity needs to be checked 4 hours after administration (follow-up necessary as drug level is only consistent after several administrations)
LMWH. Clearance?
renal
Why LMWH not suitable in renal insufficiency?
Clearance: renal (contraindicated for patients with renal insufficiency)
LMWH antidote? What scope of reversal?
protamine sulfate (partial reversal –> Protamine antagonizes 50% of the effect of LMWH)
Synthetic heparin. What drug?
fondaparinux
Fondaparinux. Administration?
subcutaneous
Fondaparinux. Monitoring?
Same as heparin:
Not generally recommended;
Anti-factor Xa activity can be assessed in specific cases (Such cases include conditions with increased coagulability (e.g., chronic kidney disease, anemia, thrombocytopenia).
Fondaparinux. Antidote?
Possibly activated prothrombin complex concentrates (aPCC)
Heparinoid (glycosaminoglycan). What drug?
danaparoid
Heparinoid (glycosaminoglycan). All other same with administration and monitoring and antidote as in heparin/fondaparinux.
.
Direct thrombin inhibitors. Drugs?
I/v argatroban, bivalirudin, desirudin
p/o dabigatranas
Direct thrombin inhibitors. Monitoring?
not recommended
Direct thrombin inhibitors. Antidote?
Possibly aPCC and/or antifibrinolytics (e.g., tranexamic acid) - if no reversal agent available
Dabigatran: idarucizumab (monoclonal antibody)
Heparin mechanism?
Enhances the activity of antithrombin –> and it leads to decreased action of IIa and Xa. (IT’S INDIRECT INHIBITION!!!!! NES DIRECTLY AFFECT ANTITHROMBIN, NOT IIa and Xa).
Heparin mechanism. Xa inhibition?
antithrombin III potentiation → inhibition of factor Xa → decreased activation of prothrombin → ↓ thrombin→ ↓ fibrinogen activation → ↓ fibrin
Heparin mechanism. IIa inhibition?
Thrombin (factor IIa): UFH binds antithrombin III and thrombin simultaneously at two distinct binding sites → antithrombin III and thrombin held by heparin in close proximity (complex formation) → ↑ thrombin inhibition → ↓ fibrinogen activation → ↓ fibrin
Heparin half life?
SHORT - therefore anticoagulant effect quickly ceases once administration is stopped