398 - 401 - Heme pharm Flashcards
What are two drugs that are derived from hirudin?
Argatroban
Bivalirudin
What is the mechanism of action of hirudin and its derivatives?
inhibits thrombin directly
When would you use a hirudin derivative?
instead of heparin for anticoagulating patients with HIT
What are two direct factor Xa inhibitors?
Apaxiban
Rivaroxaban
What are the applications of rivaroxaban?
- DVT
- PE
- Stroke prophylaxis in patients with a. fib
Do Xa factor inhibitors require coagulation monitoring?
Oral agents do not usually require monitoring
What is the reversal agent for Xa inhibitors?
no specific reversal agents are available
Name 3 thrombolytics
- alteplase (tPA)
- reteplase (rPA)
- tenecteplase (TNK-tPA)
What is the mechanism of thrombolytics?
Directly or indirectly aid conversion of
plasminogen → plasmin → cleaves thrombin and fibrin clots
What effect do thrombolytics have on PT, PTT, and platelet count?
↑PT
↑↑PTT
no change in platelet count
How do you treat toxicity of thrombolytics?
- amniocaproic acid (an inhibitor of fibrinolysis)
- fresh frozen plasma (replete factors)
- cryoprecipitate (replete factors)
Describe the effect of Asprin on:
- Bleeding time
- TXA2
- Prostaglandins
- PT
- PTT
- Bleeding time ↑
- TXA2 ↓
- Prostaglandins ↓
- PT - no change
- PTT - no change
What are the toxicities of asprin?
- Gastric ulceration
- tinnitus (CN VIII)
3 Acute renal failure - Interstitial nephritis
- Upper GI bleeding
- Reye syndrome in child w/ viral infection
What happens to the blood acid/base levels with asprin overdose?
Initially respiratory alkalosis, then superimposed by metabolic acidosis
What are 4 ADP receptor inhibitors?
- Clopidogrel
- Ticlopidine
- Prasugrel
- Ticagrelor
What are the clinical uses of ADP receptor inhibitors?
- Acute coronary syndrome
2. Coronary stenting
What are 2 toxicities of ADP receptor inhibitors?
- Neutropenia (ticlopidine)
2. TTP/HUS
What are two phosphodiesterase III inhibitors used as antiplatelet aggregation agents?
- Cilostazol
2. Dipyridamole
How do cilostazol and dipyridamole twerk?
Inhibit phospodiesterase III → ↑ cAMP in platelets → inhibit platelet aggregation, vasodilation
What are the clinical uses for cilostazol and dipyridamole?
- Intermittent claudication
- Coronary vasodilation
- Prevention of stroke or TIAs (combined w/ asprin)
- Angina prophylaxis
Toxicities of cilostazol and dipyridamole?
- Nausea
- Headache
- Facial flushing
- Hypotension
- Abdominal pain
What are 3 GP IIb/IIIa inhibitors?
- Abciximab
- Eptifibatide
- Tirofiban
What is abciximab made from?
monoclonal antibody Fab fragments
What are the uses for Gp IIb/IIIa inhibitors?
- Unstable angina
2. percutaneous transluminal coronary angioplasty
Toxicities of Gp IIb/IIIa inhibitors?
- bleeding
2. thrombocytopenia
