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M4: Pharmacology-Pharmacokinetics > Hematolytic Drugs > Flashcards

Hematolytic Drugs Flashcards

1
Q

Bleeding=
Clotting=

A

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

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2
Q

Platelet Migration and Aggregation

(3)

A
  1. Pro-Aggregants: CLOT
    • TXA2, ADP, 5HT [Platelet derived]
  2. Anti-Aggregants: BLEED
    • PGI2, PGE1, cAMP
      [Endothelial cell derived]
  3. Glycoproteins (GPs): CLOT
    • Receptors in the platelet
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3
Q

What are the type of Glycoprotein Receptors are the ff:

  1. binding of Platelet to COLLAGEN
  2. binding to Von Willebrand Factor (VWF)
  3. for interplatelet binding through FIBRINOGEN bridge
A
  1. GPIa
  2. GPIb
  3. GPIIb/GPIIa
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4
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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5
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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6
Q

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

A
  1. Extrinsic (Factor IIIa, VIIa)
  2. Intrinsic (Factors VIII, IX, XI,XII)
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7
Q

What is the end product of Blood Coagulation Cascade

A

2° Hemostasis/Red Thrombus

-stable clot

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8
Q

Which is for BLEEDING & CLOTTING

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

A

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

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9
Q

What drug prevents clot formation?

A

Antithrombotics

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10
Q

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

A

Anticoagulants=Bleeding

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11
Q

2 classes of anticoagulants

A
  1. Direct Acting Anticoagulants/Direct Thrombin Inhibitors
  2. Indirect Acting Anticoagulants/Indrect Thrombin Inhibitors
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12
Q

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

A

Direct Acting Anticoagulants/Direct Thrombin Inhibitors

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13
Q

Direct Acting Anticoagulants/Direct Thrombin Inhibitors

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

A

Hirudin (Parenteral)

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14
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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15
Q

Direct Acting Anticoagulants/Direct Thrombin Inhibitors

▪️Tx. of Acute Thrombosis Post-angioplasty

A

Bivalirudin (Parenteral)

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16
Q

Direct Acting Anticoagulants/Direct Thrombin Inhibitors

▪️Use as alternative to Lepirudin for HIT

A

Argatroban (Parenteral)

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17
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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18
Q

Advantages of Dabigatran to Warfarin

A
  1. No PT-INR monitoring
  2. No significant drug-food interaction

= safer

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19
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

20
Q

What Class of Anticoagulants is,

MOA: destroys clotting factors which activate prothrombin

A

Indirect Acting Anticoagulants/Indirect Thrombin Inhibitors

21
Q

2 Forms/Size of Heparin

A
  1. High MW Heparin (HMWH) / Unfractionated Heparin (UFH)
  2. Low MW Heparin (LMWH)
22
Q

ROA of Heparin?

A

Parenteral (IV)

23
Q

What Forms of Heparin is stated below?

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

A

LMWHeparin

24
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

25
Q

Is this HMWH or LMWH?

▪️Enoxaparin
▪️Dalteparin
▪️Tinzaparin
▪️Fondaparinux
▪️Danaproid

A

LMWH

26
Q

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

A

Heparin

27
Q

Indirect Acting Anticoagulants/Indirect Thrombin Inhibitors

▪️Xa inhibitors
- ex. (-xaban)

A

Apixaban
Rivaroxaban

  • no monitoring is required=safer
28
Q

Indirect Acting Anticoagulants/Indrect Thrombin Inhibitors

▪️Coumarin Derivatives
-only clinically useful: (?)

A

Warfarin

29
Q

Indirect Acting Anticoagulants/Indirect Thrombin Inhibitors

MOA: inhibits hepatic synthesis of vitamin K dependent clotting factor

Synthesis: Enzyme: VKERC- Vitamin K Epoxide Reductase Complex

A

Warfarin

30
Q

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

Mnemonics: 1972

A

X, IX VII, II

31
Q

Result if:

↑ PT-INR =
↓ PT-INR =

A

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

32
Q

What drug is under TXA2 Synthesis Inhibitor?

A

Aspirin

33
Q

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)

A

Aspirin

34
Q

What drug is under ADP Inhibitors?

A

Thienopyridines: (Irreversible)
▪️Ticlopidine
▪️Clopidogrel

Non-thienopyridines (Reversible)
▪️Ticagrelor

35
Q

What drug is stated below:

Use: alternative to ASA in stroke
prophylaxis

  • Full effect is seen in 11 days
A

250mg Ticlopidine

36
Q

What drugs is stated below:

USES:
▪️alternative to ASA in stroke
prophylaxis
▪️metabolized by CYP2C19 to its
active form
▪️replaced Ticlopidine

A

75mg Clopidogrel

37
Q

What drug is stated below?
under Phosphodiester inhibitors

USES:
▪️for pharmacologic stress
▪️antiplatelet but have to be combined with other antiplatelets (eg Aspirin)

A

Dipyridamole

38
Q

What drug is stated below?
under Phosphodiester inhibitors

USES:
▪️management of intermittent claudication
▪️antiplatelet but have to be combined with other antiplatelets (eg Aspirin)

A

Cilostazol

39
Q

What type of drug is stated below?

▪️aka: Thrombolytics
▪️accelerate activation of plasminogen to plasmin

A

Fibrinolytics

40
Q

What drug stated below?

Recombinant tPA
- Plasminogen-[tPA]>Plasmin

Drugs:
▪️? = natural
▪️? = recombinant

A

▪️Alteplase = natural
▪️Reteplase = recombinant

41
Q

What are the Prothrombotic Agents (3)

A
  1. Vitamin K (Drug: Vit K1-K3)
  2. Epsilon aminocaproic Acid (Drug: Tranexamic Acid (Hemostan))
  3. Serine Protease Inhibitor (Drug: Aprotinin)
42
Q

Prothrombotics

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

A

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

43
Q

Use of the ff:

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

A

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

44
Q

What drug is stated below?

Epsilon-aminocaproic Acid

Use: prevention & treatment of post-procedural bleeding (post-op dental surgery, hemoptysis)

A

Tranexamic Acid (Hemostan)

45
Q

Antidote in Warfarin

A

Vit. K1

46
Q

What Drug is stated below?

Serine Protease Inhibitor

Use: management or to minimize
bleeding in px undergoing CABG (Coronary Artery Bypass Graft)

A

Aprotinin

47
Q

What drug stated below

The lower the dose the greater the effect (↓dose=↑effect)

A

Antiplatelet
- Aspirin (325mg/day)

M4: Pharmacology-Pharmacokinetics (50 decks)

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