Coagulation Pharmacology/Basic pharm across lifespan
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enoxaparin (lovenox)-LMWH(10x less thrombocytopenia) SQonly.
- Therapeutic class: Anticoagulant
- Preg. C: C
- MOA: Combines with Antithrombin III to Inactivate clotting factors IX,X,XI,XII. Inhibit conversion of prothrombin to thrombin. May be given IV infusion or SQ only. Low molecular weight heparin is SQ and always given in abdomen*safer.
- Indications: Acute thromboembolic disorders, DVT, Pulmonary embolism, Unstable angina, Evolving MI, Prophylaxis
- Contraindications: Severe HTN, Severe thrombocytopenia (low platelets in blood), serious renal or hepatic impairment.
- Adverse effects: Abnormal bleeding, Heparin induced thrombocytopenia.
- Interactions: Potentiation with other anticoagulant, inhibited anticoagulation with nicotine, digoxin, tetracyclines, antihistamines. Ginger, garlic, green tea, and ginkho.
- Precaution: dosage in units, double check dose. Read lab values before giving. Monitor aPTT (activated partial thromboplastin time)- Goal 1.5 to 2.5 times control value. Control 25-35 seconds which is normal. Over 100 seconds too high.
- Antidote: plasma-protamine sulfate given IV, 1mg for every 100 units of heparin
Warfarin (coumadin) Most widely used drug
- Therapeutic Class: Anticoagulant
- Pharm Class: Vitamin K Antagonist
- Preg Cat: X
- MOA: inhibits two enzymes involved in formation of activated vitamin K-takes 2-7 days to reach therapeutic effect. Acts in liver to prevent synthesis of factors II, VII, IX, X-(highly protein bound) Therapeutic value-2.0-3.0INR, PO only due to CYP450 enzymes.
- Indications: A-Fib, DVT, pulmonary embolism
- Contraindications: recent trauma, active internal bleeding, serious bleeding disorers, intracranial hemorrhage, severe HTN, bacterial endocarditis, renal/liver impairment.
- Adverse effects: abnormal bleeding drug may remain in body for up to 10 days.
- Interactions: Many interactions (check pt. current medications to insure safe administration) Aspirin can potentiate warfrain. Avoid-excessive alcohol and vitamin K rich foods.
- Antidote: Vitamin K
Aspirin (ASA-Acetylsalicylic acid)
- Therapeutic class: antiplatelet
- Preg. Cat: D
- MOA: inhibits formation of Thromboxane A2, a powerful inducer of platelet aggregation. Single dose may persist for one week.
- Indications: cx pain,prevention of strokes and MI. 81mg/day prophylaxis for MI, Medium dose of 162-325mg for acute MI.
- Contraindications:Hypersensitivity to drug.
- Adverse effects: GI bleeding, GI upset, nausea, vommiting, headache, dizziness, allergic reactions.
- Interactions: potentiation with warfrain.
Adenosine diaphosphate receptor Blocker-Clopidogrel (plavix)
- Therapeutic Class: Antiplatelet
- Pharm Class: ADP Blocker
- Preg. Cat: B
- MOA: alter the plasma membrane of platelets so they cannot aggregate.
- Indications: Prevention of thromboembolic events, PVD, A-fib to prevent Stroke or PE. prevent DVT. Given PO once daily.
- Contraindications: Pt. with active bleeding or thrombocytopenia, Hepatic failure/impariment.
- Black box warning: Effectiveness dependent on CYP 450 enzymes, poor metabolizers will exhibit less therapeutic effect and more adverse cardio events.
- Adverse effects: flu like syndrome, headache, bruising, rash/allergic reaction, pruritis(severe itching). abnormal bleeding. URTI.
- Interactions: other anticoagulants, thrombolytic agents, NSAID, barbituates.
Glycoprotein receptor antagonist
unneeded for exam friday.
- Therapetuic Class: antiplatelet
- Pharm: Glycoprotein receptor antagonist
- Preg cat: B
- MOA: block attachment of glycoprotein enzyme to platelet; necessary for platelet aggregation
- Indications: same as other platelets
Alteplase (activase) TPA-Tissue plasminogen activator
- Therapeutic class: antithrombi
- Pharm class: thrombolytic
- Preg cat: C
- MOA: Produced through recombinat DNA technology, Identical to human tPA, Activates fibrinolytic agents which digest fibrin and dissolves the clot.
- Indications: preferred drug for treatment of Stroke due to thrombus.
- Contraindications: Recent GI bleed, surgery or trauma, bacterial endocarditis, uncontrolled HTN.
- Adverse effects: Life threatening intracerebral hemorrhage, atrial or ventricular dysrhythmias.
- Interactions: Concurrent use with anticoagulants, antiplatelets or nsaids including aspirin may increase the risk of bleeding.
What Lab tests for Heparin?
- Collect blood 30 mins prior to administering drug, have protamine sulfate avail- 1mg for every 100 units heparin.
- Monitored by-
- aPTT: (activated partial thromboplastin time)
- Goal: 1.5 to 2.5 times control value
- Control: (normal)-25 to 35 seconds
- Over: 100 seconds too high.
Which Lab tests for Warfrain (coumadin)
- Monitor PT and INR
- Regulated by INR
- Therapeutic value: 2.0-3.0
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