A31. Drugs used in coagulation disorders III: Fibrinolytic drugs. Drugs used in bleeding disorders

Question 1

List the drugs used in bleeding disorders.

Answer 1

1. Local antihemorrhagic
2. Systemic
3. Vitamin K
4. Fibrinolytic inhibitors: omega aminocaproic acid derivatives (EACA), aprotinin
5. Plasma Fractions
6. Desmopressin

Question 2

What is the MOA of desmopressin?

Answer 2

Desmopressin increases activity of factor VIII.

Question 3

What are the indications for fibrinolytic drug use?

Answer 3

1. Multiple PE
2. Central DVT
3. AMI

Question 4

What are the indications of Desmopressin?

Answer 4

Can be used in pts with mild hemophilia A or vWF disease.

Question 5

What are the indications of Vitamin K therapy?

Answer 5

Used for reversal of anticoag effect.

Question 6

List the local antihemorrhagics.

Answer 6

1. Vasoconstrictors: Epinephrine, NE
2. Protein denaturing compounds: close small capillaries.
3. Potassium aluminum sulfate: old aftershave.
4. Large molecules with large surface: collagen, gelatin, fibrin, activate intrinsic pathway

Question 7

What are the adverse effects of EACA?

Answer 7

1. Intravascular Thrombi
2. Hypotension
3. Myopathy
4. GI symptoms: Abdominal discomfort, Diarrhea.
5. Nasal stuffiness

Question 8

What are the adverse effects of taking Fibrinolytics?

Answer 8

1. Bleeding: (incidence 15%, lethal 0.5%) short therapy → less bleeding complications
2. Hypersensitivity rxn: in streptokinase, anistreplase, staphylokinase.

Question 9

What are the Contraindications of taking fibrinolytics?

Answer 9

1. Active bleeding
2. Serious GI or cerebral bleeding w/in 3 months
3. Surgery (incl biopsy), severe trauma w/in 10 days
4. Severe hypertension
5. Aortic dissection
6. Acute pericarditis

Question 10

What are the adverse effects of Aprotinin?

Answer 10

1. Anaphylactic rxn
2. Reversible transaminase and serum creatinine level ↑

Question 11

What are the indications of Plasma fractions?

Answer 11

Plasma fractions are cryopreciptates from whole blood. It is given for deficiencies in plasma coag factors.

Question 12

What is the route of administration and DOA of Vitamin K?

Answer 12

Vitamin K can be given orally or IV (IV can be problematic, can cause dyspnea, chest and back pain, possibly death). The onset of effect delayed by at least 6 hours, complete effect is not seen until 1 day has passed. Routine admin for all newborns, esp. premature.

Question 13

What are the indications of EACA?

Answer 13

1. Bleeding from fibrinolytics
2. Post-surgical bleeding
3. Adjunct therapy in hemophilia
4. Prophylaxis for rebleeding from intracranial aneurysms

Question 14

What is the MOA of omega aminocaproic acid derivatives (EACA)?

Answer 14

EACA are Competitive antagonist at lysin binding sites of plasminogen. Structurally EACA are similar to lysin.

Question 15

What is the MOA of Aprotinin?

Answer 15

Aprotinin is a serine protease inhibitor, isolated from cattle lung. It inhibits not only plasmin, but tryspin, kallikrein, chymotrypsin. No absorption from oral admin. parenteral use only.

Question 16

What are the indications of Aprotinin?

Answer 16

1. Bleeding due to thrombolytic treatment.
2. Extracorporeal circulation for cardiac surgery, CABG
3. Liver transplant

Question 17

List the plasminogen activators.

Answer 17

1. tPA (Tissue plasminogen activator)
2. Urokinase
3. Streptokinase
4. Staphylokinase