A: 16-19 Flashcards
3 types of anti-PLT therapy
COX inhibitiors: Aspirin
Glycoprotein IIb/IIIa receptor inhibitor: Abciximab
ADP-R antagonists: Clopidogrel, Prasugrel, Ticagrelor
ADP זה כמו שהקלידו סתם במקלדת
כמו גרל
Clap your hand and pres on the tica
What is the result of blocking COX in PLT?
Decrease TXA2 –> Decrease stimulatory effect of PLT aggregation
Other name for Aspirin
Acetylsalicylic acid
Aspirin dosage amount: Anti-PLT vs. Anti-inflammatory
Anti-PLT(anti-thrombotic) requires lower dose than anti-inflammatory dose
Aspirin indications
Prevention and treatment of arterial thrombosis
Prevents MI, TIA, Ischemic stroke
Prophylaxis in arrhythmias
Aspirin side effects
GI toxicity
Nephrotoxicity Apirinnn=neprho
hypersensitivity rxn due to increased Leukotrienea
Hyperventilation metabolic acidosis A=A
Hyperthermia
Coma (overdose)
HSN
Tinnitus
Glycoprotein IIb/IIIa receptor inhibitor=
Abciximab
Abciximab
How to give and what is the molecule?
Parenteral
IgG Ab
Abciximab indications
Acute coronary syndrome (short period) - eg. unstable angina, MI
Used during PCI to prevent re-stenosis
Post angioplasty to prevent stenosis
Abciximab side effects
Bleeding
Thrombocytopenia with prolonged use
ADP-R antagonists
Clopidogrel
Prasugrel
Ticagrelor
Clopidogrel
Prasugrel
What are they as molecules?
Do they require activation?
Prodrugs
Activated by CYP450
Oral
What can block the activation of Clopidogrel, Prasugrel?
Omeprazole
Which ADP-R antagonists does not require activation?
Ticagrelor
יש לו שם קצת שונה אז בטח הוא תרופה חדשה
Clopidogrel
Prasugrel
Ticagrelor
Indications
- Acute coronary syndrome
- prevention of restenosis after PCI
- prevention and treatment of arterial thrombosis
Post angioplasty to prevent stenosis
Prophylaxis in arrhythmias
- from book table
Clopidogrel
Prasugrel
Ticagrelor
Side effects
- Bleeding
- GI disturbances
- Neutropenia (hematologic abnormality) - clopidogrel less hematotoxic!
-TTP: disseminated formation of small thrombi, PLT consumption and
thrombocytopenia (very rare, by toclopidine)
Heparin inactivates
- complexes with anti-thrombin-3
- irreversibly inactivates : Thrombin and factor Xa
VII
IX
XI
XII
Heparin drugs
Unfractionated Heparin
Low Molecular Weight Heparin: Dalteparin, enoxaparin)
Fondaparinux (fond of the parinux) - similar to LMWH
Dalte is like smaller than alpha
Unfractionated Heparin
What is it
How to give it
How to monitor?
Acidic polysaccharide polymer
IV, SC. ( we dont use I.M because can cause hematoma!)
aPTT : activated partial thromboplastin time
Low Molecular Weight Heparin
Name of the drug
Dalteparin
enoxaparin
Low Molecular Weight Heparin
How is it different than Unfractionated Heparin?
Selective for Xa
Higher bioavailability
Longer duration of action
Renal metabolism
- note: protamine sulfate reversal in only “partially effective “ with LMWH
Synthestic Heparin=
Fondaparinux
Fondaparinux target
More selective for Xa
Fondaparinux
How to give?
SC
Heparin indicactions
Acute and rapid anticoagulation
DIC
Which anticoagulation will we give during pregnancy?
LMWH
Heparin side effects
Bleeding (monitor with aPTT)
HIT “heparin induced thrombocytopenia”
Osteoporosis (chronic use)
heppaa
לחשוב על בהד 10 ועל הבחורה ששברה את הגב שזה מתקשר לאוסטאופורוסיס
Warfarin is a type of ______ anticoagulants
Coumarin
Warfarin MOA
Inhibit Vitamin K epoxidase reductase (VKOR)
Prevents post-trans. gamma carboxylation of factors II, VII, IX, X
Vit. K is important for which factors?
II VII IX X Protein C, S
Complete theraputic effect with Warfarin is achieved after
2-3 days
Warfarin drug info
Lipid soluble
Oral
Highly bound to plasma proteins (albumin; NSAID can displace it )
Warfarin metabolism
CYP450
CYP450 inducers
- reduce the anticoagulant, increase warfarin clearance
- barbiturates
- carbamazepine
- phenytoin
- rifampin,
Cytochrome P450 inhibitors (cg,
- amiodarone
-selective serotonin reuptake inhibitors,
- cimetidine
reduce warfarin’ s clearance and increase the anticoagulant
How should we monitor Warfarin use?
PT (INR)
INR theraputic range using Warfarin
2-3
Warfarin indications
Chronic anticoagulation
Warfarin contraindication
Pregnancy
Warfarin side effects
- Skin vascular necrosis (thrombosis early in therapy due to defiency of Protein C)
- Bleeding (monitor vitk1 & PT)
- Teratogenic
- Drug interactions
note: protein C= endogenous vit-k-dep anticogulant with short T1/2
Direct acting Thrombin inhibitors
Bivalirudin
Dabigatran
ביווה ודבי חברות ממש טובות ושתיהן יחד מעקבות את טרומבין
Bivalirudin
Dabigatran
How are they given?
Bivalirudin: Parenteral
Dabigatran: Oral
דבי היא זו שמדברת מלא
ביווה שקטה יותר
Which Direct acting Thrombin inhibitors does not require monitoring by PT/PTT?
Dabigatran
כי היא מדברת כל כך הרבה ואף אחד לא רוצה להתקרב
Bivalirudin indications
- Anticoag. in patients with HIT
- In combination with Aspirin during PCI
Dabigatran indications
- prevention of stoke and systemic emboli in A. Fib (chronic therapy as an alternative therapy for Warfarin )
- prophylaxis of venous thromboemboli (VTE) following hip/knee surgery
- reduction of risk of recurrent VTE
Which drug class are considered to be Noval Oral Anticoagulants?
Direct acting factor Xa inhibitors
Direct acting factor Xa inhibitors:
Rivaroxaban
(apixaban, edoxaban)
לחשוב על הנהר בציור של סקצי
rivaroxxxxaban factor x
Rivaroxanban indications
Prevention of :
- venous thromboembolism after knee/hip surgery
- pulmonary emboli
- embolic stroke in A. Fib patients
tPA drugs
Alteplase
Reteplase
אל תתקרב ראה- תה! פלס
What is the difference btw. Alteplase and Reteplase?
Alteplase: Rebcombinant tPA
Reteplase: Modified Rebcombinant tPA
Which has faster and longer duration of action?
Alteplase
Reteplase
Reteplase
rete is more rapid
Alteplase
Reteplase
Indications
Short term management of thrombotic events (MI, PE…)
- coronary a. thrombosis
- Ischemic stroke
- pulmonary embolism
Alteplase
Reteplase
Side effects
Bleeding
Cerebral hemorrhage
Alteplase
Reteplase
What is the drug group?
tPA (thrombolytics)
Direct conversion of plasminogen into Plasmin which degrades thrombi
Thrombolytic therapy contraindications
Active internal bleeding Suspected aortic dissection Recent head trauma Previous hemorrhagic stroke Trauma or surgery in the past 2 weeks Previous ischemic stroke within the last 1 year
Fibrin foam=
A spongy substance prepared from fibrinogen and thrombin from human blood plasma and
used especially after saturation with thrombin as an absorbable clotting agent in surgical wounds
Vit. K indications
Vit. K deficiency
Reversal of excessive Warfarin anticlotting activity
Who will likely have a Vit. K def.?
Patients with fat malabsorption
New borns
Vit. K side effects
severe Infusion reaction when given IV or IM
**Can also be given orally
Antiplasmin drugs
Aminocaproic acid ( competitively inhibit plasminogen activation)
tran-examic acid : analogue of aminocaproic a
Aminocaproic acid
How to give?
Oral
Parenteral
Aminocaproic acid indications
- Management of acute beeding in patients with hemophilia or other bleeding disorders
- Reverse the activity of fibrinolytic agents (excessive fibrinolysis)
Aminocaproic acid side effects
Thrombosis
Hypotension
Myopathy
Diarrhea
Aminocaproic acid
Contraindications
DIC
Bleeding of the upper urinary tract
Iron drugs I should know for the test
Iron-hydroxide-polymaltose Complex
Iron-hydroxide-polymaltose Complex
How is it given?
Oral
Iron deficiency manifests as which anemia?
Hypochromic microcytic anemia
Acute iron overdose
Shock Necrotizing gastroenteritis Abdominal pain Bloody diarrhea Lethargy Dysnea
Chronic iron overdose
Hemochromatosis (Heart, liver, pancreas damage)
Antitode for acute iron poisoning
Deferoxamine
Vit. B12 preparations (2)
Methyl-cobalamin: Natural
Hydroxo-cobalamin: Synthetic
Vit. B12 manifests as which anemia?
Megaloblastic anemia
Which drug is used as Cyanide antidote?
Hydroxocobalamin
Folic acid is given how?
Oral
Folic acid indications
Folic acid deficiency
Prevention of congenital neural tube defects
Erythropoiesis stimulating agent=
Epoetin alfa
Epoetin alfa indications
Anemia of chronic renal disease, AIDS and cancer
Pre-operative
Epoetin alfa side effects
HTN
Thrombotic complications
RBC aplasia
In which case will we give Epoetin alfa?
Very severe anemias
How and when to give Epoetin alfa?
IV or SC
1-3 times/week
Myeloid growth factor=
Filgastrin
Filgastrin MOA
Stimulates G-CSF receptors expressed on mature neutrphils and their progenitors
G-CSF=
Granulocytes Colony Stimulating Factor
How is Filgastrim given?
SC daily
Filgastrin indications
Neutropenia assosiated with congenital neutropenia
Cyclic neutropenia
Myelodysplasia
Aplastic anemia
Mobilization of peripheral blood cells in preparation for stem cell transplantation
Filgastrin side effects
Bone pain
Splenic rupture
