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MBChB 3 Drug Database > Haematological Drugs > Flashcards

Haematological Drugs Flashcards

1
Q

What is an example of an anti-platelet drug?

A
  • Acetylsalicylic Acid (Aspirin)

* Clopidogrel

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2
Q

What is the mechanism of action for aspirin?

A
  • irreversible inactivation of cyclooxygenase (COX) enzyme
  • this reduces platelet thromboxane (TXA2) production and endothelial prostaglandin (PGI2) production.
  • reduced platelet thromboxane production reduces platelet aggregation and thrombus formation
  • reduced prostaglandin synthesis decreases nociceptive sensitisation and inflammation.
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3
Q

What is the main indication (use) of aspirin?

A
  • secondary prevention of thrombotic events

* pain relief

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4
Q

List some side effects of aspirin

A
  • bleeding
  • peptic ulceration
  • angioedema
  • bronchospasm
  • Reye’s syndrome (rare)
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5
Q

What information should you tell the patient before starting Aspirin?

A
  • avoid over the counter preparations that contain aspirin

* some patients advised to take a PPI alongside long-term aspirin

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6
Q

What drug class is clopidogrel?

A

an anti-platelet drug

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7
Q

What is the mechanism of action for Clopidogrel?

A
  • irreversibly blocks the ADP-receptor on platelet cell membranes
  • consequently inhibits formation of GPIIb/IIIa complex, required for platelet aggregation
  • decreased thrombus formation
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8
Q

What is the main indication of clopidogrel?

A

secondary prevention of thrombotic events

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9
Q

What are the side effects of clopidogrel?

A
  • bleeding

* abdominal pain/diarrhoea

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10
Q

What is important clinically regarding Pharmacokinetics/dynamics for clopidogrel?

A

Avoid in liver failure

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11
Q

What information should you tell the patient before starting Clopidogrel?

A
  • advise to stop before surgical procedures

* patients shouldn’t stop it without consulting doctor if they have an arterial stent in-situ

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12
Q

What class of drugs are Tenecteplase and Alteplase?

A

Recombinant Tissue Plasminogen Activator (rtPA)

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13
Q

What is the mechanism of action of rtPAs?

A
  • recombinant form of tissue plasminogen activator
  • catalyses conversion of plasminogen to plasmin
  • promotes fibrin clot lysis
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14
Q

What are the indications of Recombinant Tissue Plasminogen Activators?

A
  • acute ischaemic stroke within 4.5hrs of onset
  • MI within 12hrs of onset
  • massive PE
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15
Q

List the side effects of Tenecteplase and Alteplase

A
  • bleeding

* allergic reaction/angioedema

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16
Q

What are important pharmacokinetic/dynamic features to note clinically regarding rtPAs?

A
  • bolus-infusion regimen is used for Alteplase
  • Tenecteplase is given as a single bolus
  • PD interactions with other blood thinners
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17
Q

What info should you tell the patient before starting Tenecteplase or Alteplase?

A

When using thrombolytic drugs, patients should be aware of risk:benefit ratio, which should include reference to rate of bleeding complications

18
Q

What is are examples of a Heparin drug?

A

Unfractionated Heparin;

LMW Heparin

19
Q

What is the mechanism of action of heparins?

A
  • enhances activity of antithrombin III
  • antithrombin III inhibits thrombin
  • heparins also inhibits multiple other factors of the coagulation cascade
  • this produces its anticoagulant effect
20
Q

What are the indications of heparins?

A
  • treatment and prophylaxis of thromboembolic diseases, including induction of vitamin K antagonists.
  • renal dialysis
  • acute coronary syndrome treatment
21
Q

what are the side effects of heparin?

A
  • bleeding (major haemorrhage risk can be as 3.5%
  • heparin-induced thrombocytopenia
  • osteoporosis

(LMW heparins have less risk)

22
Q

what are important pharmacokinetic/dynamic features to note clinically regarding unfractionated heparins?

A
  • administered by continuous IV infusion or subcut injection
  • complex kinetics - non-linear relationship between dose/ 1/2 life and effect - needs TDM
  • effect monitored using activated PTT
  • anticoagulant effect reversed by protamine
  • unfractionated heparin has a shorter duration than LMW Heparin
  • used in preference to LMW heparin, in selected patients, due to the shorter duration of action and reversability with protamine
23
Q

What information should be given to patients before starting heparin?

A
  • risk of bleeding
  • regular blood monitoring required
  • (for LMW heparin) - will need blood testing prolonged therapy
24
Q

what are important pharmacokinetic/dynamic features to note clinically regarding LMW heparins?

A
  • subcut injection
  • more predictable dose-response relationship than unfractionated
  • 2-4 times longer plasma half-life than unfractionated
  • clearance is mostly renal, therefore longer 1/2 life if have renal failure
  • less readily reversed with protamine than unfractionated heparin
25
Q

What type of drug is warfarin?

A

a vitamin K antagonist

26
Q

what is the mechanism of action of warfarin?

A
  • inhibits vitamin K epoxide reductase
  • prevents recycling of vitamin K to reduced form after carboxylation of coagulation factors II, VII, IX and X.
  • prevents thrombus formation
27
Q

What are the indications of warfarin?

A
  • treatment of venous thromboembolism

* thromboprophylaxis in: AF / metallic heart valves / cardiomyopathy

28
Q

List the side effects of warfarin

A
  • bleeding
  • warfarin necrosis
  • osteoporosis
29
Q

What are important pharmacokinetic/dynamic features to note clinically regarding warfarin?

A
  • numerous drug interactions / food interactions
  • reversal by giving vitamin K
  • polymorphisms in key metabolising enzymes
  • needs therapeutic drug monitoring and monitored loading regimen
  • monitored with INR and dose adjusted according to indication
30
Q

What information should be given to patients before starting warfarin?

A
  • need for compliance / attendance at visits for monitoring
  • are needed with alcohol
  • must inform doctor before starting new drugs - avoid over counter aspiring preparations
31
Q

What is an example of a direct thrombin inhibitor?

A

Dabigatran (a DOAC/NOAC)

32
Q

What is the mechanism of action for dabigatran?

A
  • direct thrombin inhibitor, prevents conversion of fibrinogen to fibrin
  • this prevents thrombus formation
33
Q

What are the indications for dabigatran?

A
  • prophylaxis of venous thromboembolism

* thromboprophylaxis in non-valvular AF

34
Q

List some side effects of direct thrombin inhibitors

A
  • bleeding

* dyspepsia

35
Q

What are important pharmacokinetic/dynamic features to note clinically regarding direct thrombin inhibitors?

A
  • rapid onset of action
  • no available antidote currently
  • no food/few drug interactions
36
Q

What info should be given to a patient before starting a direct thrombin inhibitor?

A

• risk of bleeding

37
Q

Give some examples of Factor Xa Antagonists

A

rivaroxaban,

apixaban (a DOAC)

38
Q

what is the mechanism of action for Factor Xa Antagonists?

A
  • inhibits conversion of prothrombin → thrombin, reducing conc. of thrombin in blood
  • this inhibits formation of fibrin clots
39
Q

What are the indications of Factor Xa Antagonists?

A
  • prophylaxis of venous thromboembolism
  • thromboprophylaxis in non-valvular AF
  • Tx of venous thromboembolism
40
Q

What are some side effects of Factor Xa Antagonists?

A

bleeding and nausea

41
Q

What are important pharmacokinetics/dynamics features to note regarding Factor Xa Antagonists?

A
  • predictable drug interactions
  • no need for therapeutic monitoring
  • currently no antidote
  • for Apixaban - 75% metabolised by liver, rest is renally excreted
42
Q

What info should be given to a patient before starting a Factor Xa Antagonist?

A

risk of bleeding

MBChB 3 Drug Database (10 decks)

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