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41 Cards in this Set

  • Front
  • Back

Which clotting factors need vit K?

II, VII, IX and X. + Protein C and protein S

Name some coumarins

Warfarin, dicumarol

Mechanism of action of coumarins?

They inhibit vitamin K epoxide and vitamin K reductase, decreasing the amount of usable vit K since these enzymes recycle it.




The synthesis of clotting factors II, VII, IX and X + protein C and S decreases

How fast is the action of coumarins?

They are slow because their effect is functioning clotting factors needs to be eliminated. Takes 4 days.

When are coumarins indicated?

- Atrial fibrillation


- Artificial heart valve


- DVT prophylaxis

Pharmacokinetics of coumarins?

They have good oral absorption, strong plasma protein binding (97%) and are inactivated by CYP450 in the liver.

Why must the effect of coumarins be monitored, and how?

People respond differently to the same dose, so it is important to start with a low dose. INR of patient should be measured often and should be between 2 and 3.

When are coumarins contraindicated?

In pregnancy (teratogenic), liver and kidney failure.

Which drugs can decrease effect of coumarins?

Vitamin K and drugs that induce CYP450

Mechanism of action of unfractionated heparin?

It increases the effect of Antithrombin III, which is an endogenous molecule that inactivates factors XIIa, XIa, IXa, Xa and IIa.

How is heparin administered?

The size is large, so it is given IV or subcutaneously.




Immediate onset with IV, and 60 mins subcutaneous.

Indications of heparin?

Same as coumarins but when the effect is needed acutely.

What should be measured when giving a patient heparin, and what should be the target value?

Activated partial thromboplastin time (APTT). The target value should be 2 - 3 x a healthy control.

Is heparin safe during pregnancy?

Yes

What is the antidote for heparin?

Protamine sulphate

Side effects of heparin?

Heparin-induced thrombocytopaenia and thrombosis. Occurs if IgG and IgM antibodies against heparin and platelet factor 4 are produced.

What are low molecular weight heparins?

Fragments of regular, unfragmented heparin which are more predictable than regular heparin.

Name low molecular weight heparins

Enoxaparin, dalteparin and fondaparinux.

Why are low molecular weight heparins preferred over unfractionated heparin?

LMWH have longer half-time and they do not require routine blood tests every day or being administrated more often than 1-2 times a day so patients can inject themselves.

Which coagulation factors do the low molecular weight heparins inhibit?

Only Xa.

Pharmacokinetics for low molecular weight heparins?

Renal excretion, so should not be given to someone with renal failure.

What are direct acting oral anticoagulants?

Recent anticoagulants, which do not need monitoring. They directly inhibit clotting factors

Name a direct acting oral anticoagulant which inhibits IIa (thrombin)?

Dabigatran

Name some direct-acting oral anticoagulants which inhibit factor Xa?

Rivaroxaban, apixaxaban, edoxaban.

Mechanism of action of aspirin (acetylsalicylic acid)?

Inhibits cyclooxygenase 1 enzyme, which produces thromboxanes. By reducing the amount of thromboxane A2 in thrombocytes, aspirin interferes with platelet activation and aggregation.

When is aspirin indicated?

AMI


Ischaemic stroke


Angina pectoris


After coronary intervention


Prevention of cardiovascular disease


Prevention of colorectal cancer


Peripheral artery disease

Side effects of aspirin?

- Reye syndrome, encephalopathy, in children when taken during viral infection




- Peptic ulcer




- Aspirin asthma

Mechanism of action of P2Y12 blockers?

Inhibit P2Y12 receptor, found on platelets. This prevents platelet aggregation because the receptor binds usually to ADP from other activated platelets.

Mechanism of action of glycoprotein IIb/IIIa inhibitors

Bind to and inhibit receptor glycoprotein IIB/IIIA, preventing platelets to bind to each other and aggregate.

Name Glycoprotein IIb/IIIa inhibitors

Abciximab, eptifibatide, tirofiban

What are anticoagulants used for mostly?

Prevention of DVT and other venous thrombosis (due to stasis)

What are anti-platelet drugs mostly used for?

Acute treatment for coronary syndromes like NSTEMI, STEMI, unstable angina, phrophylaxis of acute coronary syndromes and cerebral stroke and in patients with stents.

What is the treatment for heparin induced thrombocytopaenia?

HIT is treated by taking the patient off heparins and giving another anticoagulant instead (not warfarin).

What are the advantages of LMWH compared to unfractionated heparin?

- No monitoring necessary




- Patients can be taught to inject themselves subcutaneously




- Lower risk of bleeding and HIT

What are the disadvantages of LMWH compared to unfractionated heparin?

LMWH are excreted renally so they can't be used in renal failure.

What are the advantages of DOACs compared to other anticoagulants?

- Don't require regular monitoring




- Can be taken orally

What are the disadvantages of DOACs compared to other anticoagulants?

- Antidotes are expensive and not readily available




- Should be used with care in people with liver or kidney failure

Name some P2Y12 receptor antagonists

Clopidogrel, prasugrel, ticagrelor

What are the indications for Glycoprotein IIb/IIIa inhibitors?

High-risk patients before and during coronary intervention

What is the antidote of dabigatran?

Idarucizumab

What is the antidote of apixaban and rivaroxaban?

Andexanet