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Haematology Pharmacology and More > Pharmacology: Drugs used to treat and prevent thrombotic events > Flashcards

Pharmacology: Drugs used to treat and prevent thrombotic events Flashcards

1
Q

Fibrinolytic Agents

Describe the mechanism of action, and Pharmacokinetics of Fibrinolytic Agents

A

They dissolve exising clots. Activates plasminogen to Plasmin, which will then dissolve clot(lyse fibrin).

Onset of action (20minutes to 2 hours)
Parenteral Administration

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2
Q

Fibrinolytic Agents

Discuss the Indications for Fibrinolytic Agents.

A
  1. Myocardial Infarction
  2. Ischaemic Stroke
  3. Pulmonary Thromboembolism
  4. Arterial Thrombosis
  5. Thromboembolism
  6. Deep Vein Thrombosis
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3
Q

Fibrinolytic Agents

Discuss the Available Agents for Fibrinolytic Agents

A

Streptokinase
Alteplase (tPA=tissie Plasminogen Activator)
Tenecteplase (MI only)

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4
Q

Fibrinolytic agents

Discuss the adverse reactions and Contraindications of Fibrinolytic Agents.

A

Adverse Effects
Bleeding
Increased risk of Haemorragic, Embolic or Thrombotic Stroke
Lysis of Clothing Factors (VIII and V)
Lysis of Physiological ‘normal’ clots (recent trauma, surgery)

Contraindications
Cerebro-vascular accident

Reversal of Fibronolytic agents if with TRANEXAMIC ACID

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4
Q

Fibrinolytic Agents

Discuss the adverse reactions and Contraindications of Fibrinolytic Agents.

A

Adverse Effects
Bleeding
Increased risk of Haemorragic, Embolic or Thrombotic Stroke
Lysis of Clothing Factors (VIII and V)
Lysis of Physiological ‘normal’ clots (recent trauma, surgery)

Contraindications
Cerebro-vascular accident

Reversal of Fibronolytic agents if with TRANEXAMIC ACID

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5
Q

Fibrinolytic Agents

Desribe the indications for Streptokinase and name its alternative.

A

Indications

With streptokinase, there is Antibody formation which limits use. It is not supposed to be reused between 5 days to 2 years after the first use

  1. Acute Pulmonary Embolism
  2. Acute Myocardial Ischaemia
  3. Acute Arterial Thrombosis, Thromboembolism
  4. Deep Vein Thrombosis
  5. Ischaemic Stroke (only soon after onset)

Alternative
ALTEPLASE- it has no antibody formation but there is RISK OF** INTRACRANIAL BLEEDING**

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6
Q

Heparin

Describe the MOA of Heparin

A

Heparin increases binding of anti-thrombin to thrombin and factor Xa

Heparin inhibits factor 7a, 9a, 11a and 10a

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7
Q

Heparin

Describe the adverse effects and mode of administration of Heparin

A

Side Effects
Haemorrage
allergy- hypersensitivity reactions
Long term use- Osteoporosis
Reversible Alopecia (baldness)

Administration- ONLY IV

**Continuous Therapeutic drug monitoring is required

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8
Q

Heparin

Name the LMWH, describe thier MOA and USES.

A

Names
Dalteparin, Enoxaparin and Nadroparin

Uses
DVT
Acute VTED
Acute MI
Trauma Patients

it has improved bioavailability than heparin

**TDM is not required

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9
Q

Heparin

Describe the containdications of HEPARIN/LMWH

A

Hypersensitivity
Active Bleeding
Thrombocytopenia
Intracranial Haemorrhage
Infective Endocarditis
Active TB, Ulceration of GIT
Surgery of brain, SPinal Cord, EYE
Lumbar Puncture, Spinal Block Anaesthesia

THE HI TAPS

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10
Q

Warfin

Describe the Clinical USe and MOA of warfin

A

Clinical Use
Chronic Anticoagulation
Therapeutic Drug Monitoring is essential
MOA
It is a Vitamin K antagonist (know the vitamin K dependent clotting factors)

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11
Q

Describe Warfin Adverse Drug Reactions

A

Haemorrage
Intracerebral/ Subdural Haematoma
Increased risk of feta brain haemorrhage in Third and Second Trimester
induce clot formation via protein C/S effect leaving to thrombosis microvasculature

DO NOT GIVE WARFIN INHEPARIN INDUCED THROMBOCYTOPENIA

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12
Q

WARFIN

Describe the drug interactions of Warfin

A
  1. Drugs that bind with warfin in the GIT- eg, Cholestyramine (chole-sty-ramine)
  2. Substances altering protein binding0 eg, sodium Valproate
  3. Drugs with anticoagulant/antipaltelet effect, eg, NSAIDS
  4. Drug Metabolism
    (a)Increased metabolism- CYP2C9 inducers, eg, Carbamazepine, Rifampicin
    (b) Decreased metabolism by CYP2C( inhibitors),eg, Azole antifungals, antidepressants, Itraconazole, fluconazolr, fluoxethine antiplatelet drug, clopidrogel
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13
Q

Warfin

So what if we adminster Warfin, and there’s major bleeding. What do you do?

A

Stop Warfin, slow IV Vitamin K, Factor IX complec or Fresh Frozen Plasma
closely monitor

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14
Q

Describe the Rivaroxaban & Apixaban

A
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15
Q

Describe the Indications(treatment+prophylaxis), MOA and Contraindications for Rivaroxaban and Apixaban.

A

Prophylaxis
1. Venous thromboembolism
2. Knee and hip replacement surgery
3. Stroke Prevention

Treatment
1. DVT
2. Pulmonary 🫁 Embolism

MOA
Inhibits Factor Xa

Contraindications
Active bleeding
Recent Brain-, spinal cord-, ophthalmic surgery.

16
Q

Describe the MOA, Indications, Cautions, Drug Reversal for Dabigatran Etixilate

[DABI-GA-TRAN ETIXI-LATE]

A

MOA
1. Binds to thrombin active site and blocks it.

INDICATIONS
1. Same as for Rivaroxaban

CAUTION
1.DI with Amiodarone and Verapamil
2. CI spinal anesthesia
In long tern treatment, in elderly, monitor renal function and reduce dose if impaired.

Reversal Drug in Emergency: Idarucizumab.

17
Q

[Antiplatelet Agents]
Describe the MOA, Indications, DI and dose of Aspirin

A

MOA
irreversible inhibition of platelet cyclooxygenase
Decrease thromboxane A2 synthesis and Decrease/inhibit platelet activation.

Drug Interactions
With Warfin and causes bleeding.

Indications:
Prevention of Ischaemic Heart Disease, TIA
Stroke Prevention

Dose: 75-150 mg

18
Q

Clopidogrel and Prasugrel are an alternative to Aspirin.

Describe their Indications, CI. Di and dose.

A

Indications:
1. MI
2. Stoke Thromboembolic Stroke and TIA,
3. Acute Coronary Syndrome

CI
1. Active Bleeding,
2. ADR
3. Thrombocytopenia

Dose: 75 mg daily and 300g in Acute Coronary Syndrome.

19
Q

Describe Use, ADR and Drug Interactions of Tigagrelor

A

Use: Acute Coronary Syndrome

*ADR**
Bleeding- stop 5 days before surgery
GIT- Abdominal pain, dyspepsia, diarrhea, Nausea
CNS- Skin Rash, Dyspnoea, Epistaxis, Hyperuricaemia

Drug Interactions
1.CYP3A4 Inhibitors (Eg) Itraconazole–> causing Bleeding.
2. CYP3A4 Inducers (Eg) Rifampicin, Carbamazepine–> Decrease Efficacy.
3. Oral Anticoagulants–> Bleeding
4. NSAIDS–> Occult GIT bleeding
5. Simvastatin–> Increase AUC and Cmax of Simvastatin.

20
Q

Describe the MOA, Use and Pharmacokinetics of Tirofiban.

A

● Antagonist to Glycoprotein IIb/IIIa
● Restricted to high risk patients
●Given IV only
● Use] Prevents Early MI in unstable angina,
● Adjunct to Heparin and Aspirin in high risk patients

21
Q

Describe the Indications, ADR of Eptifibatide and Abciximab

A

ADR: Bleeding and Thrombocytopenia

INDICATION: Unstable angina, Percutaneous Coronary Interventions

Abciximab effect lasts longer than epfibatide

Eptifibatide: Longer plasma T1/2 than abciximab.

Haematology Pharmacology and More (17 decks)

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