Cardiovascular Pharmacology Summary Part 4 Flashcards
Which drug is an oral anticoagulant?
Warfarin
What are the pharmacokinetics of Warfarin?
High protein binding!
Metabolized in the liver
What is the mechanism of action of Warfarin (Cellular)?
Blocks the liver metabolism of factor II, IV, IX, X. Inhibits the activity of Vitamin K epoxide reductase which concerts Vitamin K to its active form. Also inhibits Protein C which increases risk of thrombosis early in treatment.
What is the mechanism of action of Warfarin (physiological)?
Onset of action is about three days. Depends on serum half life of clotting factors. Only liver production is impacted by warfarin. Many drug interactions - liver metabolism and high protein binding.
What should be used to monitor Warfarin therapy?
Monitor prothrombin time.
Also INR increased by double.
What are the therapeutic uses of Warfarin?
- Used for long term prophylaxis for DVT, atrial fibrillation, pulmonary embolism.
- May prevent CAD long term in conjunction with aspirin. - Also in patients with a history of DVT and traumatic DVT and immobilization.
What are the adverse effects and contraindications of Warfarin?
- Strictly C/I in pregnancy! High risk of fetal abnormalities.
- Bleeding is major side effect
- Dermatitis can occur
Which drugs are fibrinolytics?
Streptokinase
Tissue plasminogen activator (t-PA)
Alteplase
What is the mechanism of action of the fibrinolytics (cellular)?
Converts inactive plasminogen to plasmin which breaks down fibrin = fibrin degradation products.
What is the mechanism of action of the fibrinolytics (physiological)?
Only attacks established clots, and no effect on new clot formation.
How are the fibrinolytics administered?
Injected
What are the therapeutic uses of the fibrinolytics?
Used for the treatment of pulmonary embolism and STEMI.
What are the adverse effects and contraindications of the fibrinolytics?
- Bleeding, especially hemorrhagic stroke
- Streptokinase can induce antibodies, cause allergy and inactivate after initial use.
- Do not use in unstable angina, may convert non-STEMI to full infarction.
Which drug is a neurotransmitter releaser?
Amphetamine
What is the cellular effect (MOA) of amphetamine?
Increase release of neurotransmitters from synaptic vesicles. NA, DA serotonin all increased. Increase conduction through AV node and conduction in SA node. Increased contractility. Increased O2 demand by the heart.
What is the physiological effect (MOA) of amphetamine?
Mimics the effect of NA and Adr on beta-1 in heart, increases heart rate and arrhythmia.
Potent central effects increase performance motivation and power.
What are the amphetamines used for?
Drugs of abuse.
Highly addictive, amphetamine more powerful then ephedrine.
What are the adverse effects associated with amphetamine use?
Tremor, anxiety, arrhythmia, heart failure.
Which drugs are parasympatholytics?
Atropine
Hyoscine
What is the mechanism of action of the parasympatholytics (cellular)?
Blocks post-ganglionic muscarinic receptors.
Decreases IP3.
What is the mechanism of action of the parasympatholytics (physiological)?
Generally decrease salivation, mydriasis, decreases peristalsis, prevent bladder voiding, increase heart rate, bronchodilation, decreases salivary gland secretion, increase bladder sphincter tone
What are the therapeutic uses of the parasympatholytics?
Stop vagal induced effects and decrease salivation in surgery.
Hyoscine = IBS
Can also be used in some forms of AV nodal block.