Hematolytic Drugs Flashcards
Bleeding=
Clotting=
Bleeding= Hemorrhage (labnaw)
Clotting=Thrombosis (lapot)
Platelet Migration and Aggregation
(3)
- Pro-Aggregants: CLOT
- TXA2, ADP, 5HT [Platelet derived]
- Anti-Aggregants: BLEED
- PGI2, PGE1, cAMP
[Endothelial cell derived]
- PGI2, PGE1, cAMP
- Glycoproteins (GPs): CLOT
- Receptors in the platelet
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
- GPIa
- GPIb
- GPIIb/GPIIa
What is the end product of platelet migration and aggregation
1° Hemostasis (aka: White Thrombus/Platelet Drug)
-clot is unstable (weak bridge)
What is the Goal of “Activation of blood coagulation cascade”?
GOAL:
▪️To strengthen the weak bridge
▪️ To activate Fibrinogen to Fibrin
2 Pathways involve in activation of blood coagulation cascade (clotting factors)
- Extrinsic (Factor IIIa, VIIa)
- Intrinsic (Factors VIII, IX, XI,XII)
What is the end product of Blood Coagulation Cascade
2° Hemostasis/Red Thrombus
-stable clot
Which is for BLEEDING & CLOTTING
▪️Antithrombotics: (?)
▪️Fibrinolytics: (?)
▪️Prothrombotics: (?)
▪️Antithrombotics: BLEEDING
▪️Fibrinolytics: BLEEDING
▪️Prothrombotics: CLOTTING
What drug prevents clot formation?
Antithrombotics
What type of drug interfere the coagulation cascade by acting on different clotting factors
Anticoagulants=Bleeding
2 classes of anticoagulants
- Direct Acting Anticoagulants/Direct Thrombin Inhibitors
- Indirect Acting Anticoagulants/Indrect Thrombin Inhibitors
MOA: Direct IIa Inhibition
Ex: ROA (Parenteral, Oral)
Direct Acting Anticoagulants/Direct Thrombin Inhibitors
Direct Acting Anticoagulants/Direct Thrombin Inhibitors
▪️Natural from Hirudo Medicinals (medicinal leech)
▪️↑risk: hypersensitivity
Hirudin (Parenteral)
Direct Acting Anticoagulants/Direct Thrombin Inhibitors
▪️ Recombinant form of Hirudin
▪️ Less associated with hypersensitivity reaction
▪️1st Line for HIT (Heparin-Induced Thrombocytopenia)
Lepirudin (Parenteral)
Direct Acting Anticoagulants/Direct Thrombin Inhibitors
▪️Tx. of Acute Thrombosis Post-angioplasty
Bivalirudin (Parenteral)
Direct Acting Anticoagulants/Direct Thrombin Inhibitors
▪️Use as alternative to Lepirudin for HIT
Argatroban (Parenteral)
Direct Acting Anticoagulants/Direct Thrombin Inhibitors
▪️Alternative to Warfarin in the ff. conditions;
- stroke prophylaxis
- vascular thromboembolic D/O
- deep vein thrombosis
Dabigatran (Oral)
Advantages of Dabigatran to Warfarin
- No PT-INR monitoring
- No significant drug-food interaction
= safer
What are the drugs under Direct Acting Anticoagulants/Direct Thrombin Inhibitors (Parenteral & Oral)
Mnemonics: LHBA-D
Parenteral (IV)
1. Lepirudin
2. Hirudin
3. Bivalirudin
4. Argatroban
Oral (PO)
1. Dabigatran
What Class of Anticoagulants is,
MOA: destroys clotting factors which activate prothrombin
Indirect Acting Anticoagulants/Indirect Thrombin Inhibitors
2 Forms/Size of Heparin
- High MW Heparin (HMWH) / Unfractionated Heparin (UFH)
- Low MW Heparin (LMWH)
ROA of Heparin?
Parenteral (IV)
What Forms of Heparin is stated below?
▪️MOA: Inhibts Xa only
▪️ROA: SQ
▪️Monitoring: No Mandatory Monitoring=safer
▪️✅️ Pregnancy
LMWHeparin
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
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)
- Vitamin K (Drug: Vit K1-K3)
- Epsilon aminocaproic Acid (Drug: Tranexamic Acid (Hemostan))
- 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)
