HEMATOLOGIC DRUGS

• Anti-thrombotics

• Thrombotics

• Prothrombotics

Hematologic drugs involve:

• Antiplatelets

• Anticoagulants

Anti-thrombotics is composed of two classes

1st event

Anti-platelets target what event?

2nd event

Anti-coagulants target what event?

Fibrinolytics

Thrombolytics is also known as?

Plasmin pathway

Thrombolytics is related to what pathway?

Anti-platelets

are also known as anti aggregants but the term commonly used is?

• Direct thrombin inhibitors

• Indirect thrombin inhibitors

Anti coagulants are classified into two classes:

• Parenteral

• Oral

Direct Thrombin Inhibitors are classified into two routes:

• Hirudin

• Lepirudin

• Bivalirudin

• Argatroban

DTI: Parenteral enumerate

• Ximelagratan

• Dabigratan

DTI: Oral

Hirudin

Parenteral DTI from leech saliva

Hirudu medicinalis

Which leech species does Hirudin originate from?

Hirudin

Parenteral DTI that has a high risk of hypersensitivity

Lepirudin

Parenteral DTI that is a recobinant form of hirudin

Lepirudin

Parenteral DTI: 1st line for the management of HIT (Heparin Induced Thrombocytopenia)

Bivalirudin

Parenteral DTI: used for Post PTCA (Percutaneous Transluminal Coronary Angioplasty)

Argatroban

Parenteral DTI: Alternative for HIT

Ximelagatran

Oral DTI: that has been withdrawn from the market

Dabigatran

The only oral DTI available in the market

Pradaxa

Dabigratan is marketed under what brand name?

Dabigratan

Oral DTI: Alternative for Warfarin, Stroke prophylaxis, management for thrombo embolic disorders, and deep vein thrombosis

• No significant food-drug interaction

• No PT-INR monitoring

Advantages of Dabigratan vs Warfarin

• Alternative to warfarin

• Stroke prophylaxis

• Management for thromboembolic disorders

• Deep vein thrombosis

Clinical uses of Dabigratan:

Lepirudin

Therapeutic use: Used in patients with Thrombosis related to heparin-induced thrombocytopenia

Bivalirudin

Therapeutic use: FDA-approved for use in post PTCA

Agatroban

Therapeutic use: FDA-approved for use in patients with HIT with or without thrombosis and coronary angioplasty in patients with HIT

Dabigatran

Therapeutic use: Approved for use in europe for prevention of venous thromboembolism in patients who have undergone hip or knee replacement surgery

• Parenteral

• Oral

Indirect thrombin inhibitrs are classified into two routes

Heparin

Parenteral ITI enumerate:

Warfarin

Oral ITI enumerate:

• Apixaban

• Rivaroxaban

New ITI enumerate:

• Apixaban

• Rivaroxaban

They are classified as oral CF Xa inhibitors

No monitoring required

Xabans are safer because?

Heparin

Parenteral ITI: A heterogenous mixture of sulfated mucopolysaccharides.

Sulfated mucopolysaccharides

Heparin is a heterogenous mixture of what?

• Regular heparin/HMW heparin/ Unfractionated heparin

• LMW heparins

Heparin are classified based on size:

• Enoxaparin

• Dalteparin

• Fondaparinux

• Fraxiparin

• Danaproid

Enumerate the LMW heparins

5k-30K

Molecular weight of HMW heparin?

Binds to antithrombin III which speeds its bleeding to 1000x fold

MOA of heparin

• Regular Heparin

• LMW (more selective to Xa)

Difference between the two forms of heparin?

6 hrs

Bleeding effect of heparin will occur within?

LMW heparin

Used for the management of acute coronary syndrome

LMW heparin

which forms of heparin is safe for pregnant women

LMW heparin

It is used for the treatment of APAS (Anti-phospholipid anti-body syndrome)

SQ

Route for HMW heparin for prophylaxis?

IV

Route for HMW heparin for treatment?

SQ

Route for LMW heparin for prophylaxis?

SQ

Route for LMW heparin for treatment?

aPTT (Activated partial thromboplastin time)

Monitoring for HMW heparin?

LMW heparin

In pregnancy, which forms of heparin is allowed to be given?

60-85 seconds delay

Goal of aPTT monitoring?

Underdosed (clot formation)

aPTT: less than 35 seconds is categorized as?

Overdose (bleeding)

aPTT: greater than 100 seconds is categorized as?

Protamine sulfate

Antidote for Heparin induced bleeding?

• 100 units of heparin

• 1 mg of protamine sulfate (IV)

Ratio of Protamine sulfate to heparin?

Mineralocorticoid deficiency

Long term use of Heparin is associated with?

• Bleeding

• Hair loss and reversible alopecia

• Osteoporosis

• Decreased in TAGs

• HIT

• Mineralocorticoid deficiency

Enumerate the toxicity of Heparin:

Heparin induced thrombocytopenia

it is a rare, immune-mediated thrombosis?

Low platelet levels

HIT is characterized by?

nice

Just understand the concept of why heparin is clotting and bleeding at the same time

Hapten

exogenous substances that is of carbohydrate moiety is classified as?

Contraindications of Heparin

• Brain

• Spinal cord

• Eye

• Patients undergoing

  • Lumbar puncture

  • Regional anesthetic block

Heparin should be avoided in patients who recently had a surgery of:

Hemoptysis

Spitting of blood by patient which is apparent with chronic tubercolosis

Ionized form of heparin (Excretable form)

Heparin + Protamine =