Hematolytic Drugs Flashcards by Mark Agustin

Q

Bleeding=
Clotting=

A

Bleeding= Hemorrhage (labnaw)
Clotting=Thrombosis (lapot)

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Q

Platelet Migration and Aggregation

(3)

A

Pro-Aggregants: CLOT
- TXA2, ADP, 5HT [Platelet derived]
Anti-Aggregants: BLEED
- PGI2, PGE1, cAMP
  [Endothelial cell derived]
Glycoproteins (GPs): CLOT
- Receptors in the platelet

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Q

What are the type of Glycoprotein Receptors are the ff:

binding of Platelet to COLLAGEN
binding to Von Willebrand Factor (VWF)
for interplatelet binding through FIBRINOGEN bridge

A

GPIa
GPIb
GPIIb/GPIIa

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Q

What is the end product of platelet migration and aggregation

A

1° Hemostasis (aka: White Thrombus/Platelet Drug)

-clot is unstable (weak bridge)

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Q

What is the Goal of “Activation of blood coagulation cascade”?

A

GOAL:
▪️To strengthen the weak bridge
▪️ To activate Fibrinogen to Fibrin

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Q

2 Pathways involve in activation of blood coagulation cascade (clotting factors)

A

Extrinsic (Factor IIIa, VIIa)
Intrinsic (Factors VIII, IX, XI,XII)

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Q

What is the end product of Blood Coagulation Cascade

A

2° Hemostasis/Red Thrombus

-stable clot

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Q

Which is for BLEEDING & CLOTTING

▪️Antithrombotics: (?)
▪️Fibrinolytics: (?)
▪️Prothrombotics: (?)

A

▪️Antithrombotics: BLEEDING
▪️Fibrinolytics: BLEEDING
▪️Prothrombotics: CLOTTING

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Q

What drug prevents clot formation?

A

Antithrombotics

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Q

What type of drug interfere the coagulation cascade by acting on different clotting factors

A

Anticoagulants=Bleeding

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Q

2 classes of anticoagulants

A

Direct Acting Anticoagulants/Direct Thrombin Inhibitors
Indirect Acting Anticoagulants/Indrect Thrombin Inhibitors

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Q

MOA: Direct IIa Inhibition
Ex: ROA (Parenteral, Oral)

A

Direct Acting Anticoagulants/Direct Thrombin Inhibitors

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Q

Direct Acting Anticoagulants/Direct Thrombin Inhibitors

▪️Natural from Hirudo Medicinals (medicinal leech)
▪️↑risk: hypersensitivity

A

Hirudin (Parenteral)

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Q

Direct Acting Anticoagulants/Direct Thrombin Inhibitors

▪️ Recombinant form of Hirudin
▪️ Less associated with hypersensitivity reaction
▪️1st Line for HIT (Heparin-Induced Thrombocytopenia)

A

Lepirudin (Parenteral)

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Q

Direct Acting Anticoagulants/Direct Thrombin Inhibitors

▪️Tx. of Acute Thrombosis Post-angioplasty

A

Bivalirudin (Parenteral)

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Q

Direct Acting Anticoagulants/Direct Thrombin Inhibitors

▪️Use as alternative to Lepirudin for HIT

A

Argatroban (Parenteral)

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Q

Direct Acting Anticoagulants/Direct Thrombin Inhibitors

▪️Alternative to Warfarin in the ff. conditions;
- stroke prophylaxis
- vascular thromboembolic D/O
- deep vein thrombosis

A

Dabigatran (Oral)

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Q

Advantages of Dabigatran to Warfarin

A

No PT-INR monitoring
No significant drug-food interaction

= safer

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Q

What are the drugs under Direct Acting Anticoagulants/Direct Thrombin Inhibitors (Parenteral & Oral)

Mnemonics: LHBA-D

A

Parenteral (IV)
1. Lepirudin
2. Hirudin
3. Bivalirudin
4. Argatroban

Oral (PO)
1. Dabigatran

Q

What Class of Anticoagulants is,

MOA: destroys clotting factors which activate prothrombin

A

Indirect Acting Anticoagulants/Indirect Thrombin Inhibitors

Q

2 Forms/Size of Heparin

A

High MW Heparin (HMWH) / Unfractionated Heparin (UFH)
Low MW Heparin (LMWH)

Q

ROA of Heparin?

A

Parenteral (IV)

Q

What Forms of Heparin is stated below?

▪️MOA: Inhibts Xa only
▪️ROA: SQ
▪️Monitoring: No Mandatory Monitoring=safer
▪️✅️ Pregnancy

A

LMWHeparin

Q

What Forms of Heparin is stated below?

▪️MOA: Inactivation of IXa, Xa, XIa, XIIIa
▪️ROA: IV bolus or Infusion
▪️Monitoring: aPTTT: Activated Partial Thromboplastin Time
▪️ ❌️ Pregnancy

A

HMWH / UFH

Is this HMWH or LMWH? ▪️Enoxaparin ▪️Dalteparin ▪️Tinzaparin ▪️Fondaparinux ▪️Danaproid

LMWH

What Drug is stated below: USES ▪️ when initiating anticoagulant therapy ▪️ immediate bleeding ▪️for @ the beginning of Warfarin therapy ▪️Mgt. of DVT, venous thromboembolism, acute coronary syndrome, pulmonary embolism

Heparin

Indirect Acting Anticoagulants/Indirect Thrombin Inhibitors ▪️Xa inhibitors - ex. (-xaban)

Apixaban Rivaroxaban - no monitoring is required=safer

Indirect Acting Anticoagulants/Indrect Thrombin Inhibitors ▪️Coumarin Derivatives -only clinically useful: (?)

Warfarin

Indirect Acting Anticoagulants/Indirect Thrombin Inhibitors MOA: inhibits hepatic synthesis of vitamin K dependent clotting factor Synthesis: Enzyme: VKERC- Vitamin K Epoxide Reductase Complex

Warfarin

What are the Vit. K dependent clotting factors of Warfarin? Mnemonics: 1972

X, IX VII, II

Result if: ↑ PT-INR = ↓ PT-INR =

↑ PT-INR = Hemorrhage ↓ PT-INR = Thrombosis

What drug is under TXA2 Synthesis Inhibitor?

Aspirin

What drug is stated below: MOA: ▪️Irreversible acetylation of COX ▪️Low TXA2=inhibit platelet aggregation USES: ▪️1st line antiplatelet ▪️For primary & secondary prevention of thrombotic events (MI, stroke)

Aspirin

What drug is under ADP Inhibitors?

Thienopyridines: (Irreversible) ▪️Ticlopidine ▪️Clopidogrel Non-thienopyridines (Reversible) ▪️Ticagrelor

What drug is stated below: Use: alternative to ASA in stroke prophylaxis - Full effect is seen in 11 days

250mg Ticlopidine

What drugs is stated below: USES: ▪️alternative to ASA in stroke prophylaxis ▪️metabolized by CYP2C19 to its active form ▪️replaced Ticlopidine

75mg Clopidogrel

What drug is stated below? under Phosphodiester inhibitors USES: ▪️for pharmacologic stress ▪️antiplatelet but have to be combined with other antiplatelets (eg Aspirin)

Dipyridamole

What drug is stated below? under Phosphodiester inhibitors USES: ▪️management of intermittent claudication ▪️antiplatelet but have to be combined with other antiplatelets (eg Aspirin)

Cilostazol

What type of drug is stated below? ▪️aka: Thrombolytics ▪️accelerate activation of plasminogen to plasmin

Fibrinolytics

What drug stated below? Recombinant tPA - Plasminogen-[tPA]>Plasmin Drugs: ▪️? = natural ▪️? = recombinant

▪️Alteplase = natural ▪️Reteplase = recombinant

What are the Prothrombotic Agents (3)

1. Vitamin K (Drug: Vit K1-K3) 2. Epsilon aminocaproic Acid (Drug: Tranexamic Acid (Hemostan)) 3. Serine Protease Inhibitor (Drug: Aprotinin)

Prothrombotics Vit K1: aka ? Vit K2: aka ? Vit K3: aka ?

Vit K1: (Phytonadione) Vit K2: (Menaquinone) Vit K3: (Menadione)

Use of the ff: ▪️Vit K1: (Phytonadione) ▪️Vit K2: (Menaquinone) ▪️Vit K3: (Menadione)

▪️Vit K1: clinically useful (Prevention: Hemorrhagic D/O of newborns) ▪️Vit K2: synthesized by colonic bacteria flora ▪️Vit. K3: water soluble; used in assays

What drug is stated below? Epsilon-aminocaproic Acid Use: prevention & treatment of post-procedural bleeding (post-op dental surgery, hemoptysis)

Tranexamic Acid (Hemostan)

Antidote in Warfarin

Vit. K1

What Drug is stated below? Serine Protease Inhibitor Use: management or to minimize bleeding in px undergoing CABG (Coronary Artery Bypass Graft)

Aprotinin

What drug stated below The lower the dose the greater the effect (↓dose=↑effect)

Antiplatelet - Aspirin (325mg/day)