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How does Warfarin work?
Interferes with the γ-carboxylation of Vitamin K dependent clotting factors 2,7,9, 10, Protein C and Protein S
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How is the therapeutic effect of warfarin monitored?
By measuring the Prothrombin time (PT) and International normalized ratio (INR)
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What is the target International normalized ratio (INR) for therapeutic warfarin coagulation?
- 2-3
- There is increased bleeding when INR is above 3.
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What can be used for the fastest reversal of warfarin's side effect?
Fresh frozen plasma
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What can be used for reversing warfarin-induced anticoagulation?
- Vitamin K
- Fresh frozen plasma- fastest reversal
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What is the use of Protamine sulfate? How does it work?
- Used for Heparin reversal
- It is a positively charged molecule that binds negatively charged heparin ⇨ chemically inactivating heparin
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Which drug is used in heparin reversal?
Protamine sulfate
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What is the use of Aminocaproic acid? How does it work?
- Used to treat toxicity with Thombolytics - alteplase (tPA), streptokinase, tenecteplase (TNK-tPA)
- Inhibits plasminogen activators thus preventing bleeding due to fibrinolysis.
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How do we treat toxicity with plasminogen activators (Plasminogen ⇨ Plasmin)?
Aminocaproic acid
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How do we treat Streptokinase toxicity?
- Streptokinase (plasminogen ⇨ plasmin ⇨ fibrinolysis). Can cause excessive bleeding
- Aminocaproic acid- inhibitor of fibrinolysis
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How do we treat Alteplase toxicity?
- Alteplase (plasminogen ⇨ plasmin ⇨ fibrinolysis). Can cause excessive bleeding
- Aminocaproic acid- inhibitor of fibrinolysis
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How do we treat Tenecteplase toxicity?
- Telecteplase (TNK-tPA) (plasminogen ⇨ plasmin ⇨ fibrinolysis). Can cause excessive bleeding
- Aminocaproic acid- inhibitor of fibrinolysis
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What does Cryoprecipitate contain?
- Factor 8
- Factor 13
- von Willebrand factor
- Fibrinogen
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How can we treat coagulation deficiencies involving factor 8?
Cryoprecipitate
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What is the function of fibrinogen? How can we treat its deficiency?
- Fibrinogen binds GpIIb/ IIIa receptors and links platelets.
- Cryoprecipitate.
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What is the mechanism and use of Bethanechol?
- MOA: muscarinic agonist/ cholinergic agonist
- Use: Activates bowel and bladder smooth muscle (esp. postop)
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What drug can be used to treat postoperatively urinary retention?
- Bethanechol- muscarinic agonist
- α1 blocker
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Which receptors play a role in urinary retention?
alpha 1 receptors ↑intestinal and bladder spincter muscle contraction
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Which receptors allows you to pee?
M3 makes you pee
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What is the MOA and use of Oxybutynin?
- MOA: muscarinic antagonist
- Use: Urinary incontinence/ overactive bladder (Oxybutynin causes you to retain your urine).
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What role does hydroxyurea play in the treatment of sickle cell anemia?
- Increases fetal hemoglobin (Hb F) synthesis by an unknown mechanism.
- Hydroxyurea is reserved for patients with frequent pain crises.
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What role does Gardos channel blockers play in the treatment of sickle cell disease?
They hinder the efflux of potassium and water from the cell, preventing dehydration of RBCs and polymerization of Hb S
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What can be used to treat sickle cell disease?
- Hydroxyurea (⇧fetal Hb F)
- Hydration
- Gardos channel blocker (prevents dehydration and polymerization)
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What is the MOA of hydroxyurea?
- Inhibits ribonucleotide reductase which converts UDP ⇨ dUDP (Pyrimidine base production)
- ⇩DNA synthesis (S-phase specific)
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This drug inhibits the conversion of UPD to dUDP in pyrimidine base production.
- HYDROXYUREA
- Inhibits ribonucleotide reductase which converts UDP ⇨ dUDP (Pyrimidine base production)
- ⇩DNA synthesis (S-phase specific)
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This drug inhibits ribonucleotide reductase.
Hydroxyurea
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How do we treat drug induced parkinsonism?
- Benztropine/ Trihexyphenidyl- antimuscarinic which improves tremor and rigidity
- Amantadine - ⇧dopamine release
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What causes drug induced parkinsonism?
- Antipsychotics
- Riserpine
- Metroclopramide (gastric motility agent, antiemetic)
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What is the MOA and use of Benztropine?
- MOA: muscarinic antagonist
- Use: Parkinsomism- improves tremor and rigidity but has little effects on bradykinesia
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This drug is used to improve tremor and rigidity in Parkinson disease.
Benztropine, Tihexyphenydyl
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What is the MOA and use of Nystatin?
“Swish and swallow” for oral candidiasis (thrush); topical for diaper rash or vaginal candidiasis.
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