Cardiovascular Pharmacology Summary Part 4 Flashcards

1
Q

Which drug is an oral anticoagulant?

A

Warfarin

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2
Q

What are the pharmacokinetics of Warfarin?

A

High protein binding!

Metabolized in the liver

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3
Q

What is the mechanism of action of Warfarin (Cellular)?

A

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.

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4
Q

What is the mechanism of action of Warfarin (physiological)?

A

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.

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5
Q

What should be used to monitor Warfarin therapy?

A

Monitor prothrombin time.

Also INR increased by double.

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6
Q

What are the therapeutic uses of Warfarin?

A
  1. Used for long term prophylaxis for DVT, atrial fibrillation, pulmonary embolism.
    - May prevent CAD long term in conjunction with aspirin.
  2. Also in patients with a history of DVT and traumatic DVT and immobilization.
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7
Q

What are the adverse effects and contraindications of Warfarin?

A
  1. Strictly C/I in pregnancy! High risk of fetal abnormalities.
  2. Bleeding is major side effect
  3. Dermatitis can occur
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8
Q

Which drugs are fibrinolytics?

A

Streptokinase
Tissue plasminogen activator (t-PA)
Alteplase

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9
Q

What is the mechanism of action of the fibrinolytics (cellular)?

A

Converts inactive plasminogen to plasmin which breaks down fibrin = fibrin degradation products.

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10
Q

What is the mechanism of action of the fibrinolytics (physiological)?

A

Only attacks established clots, and no effect on new clot formation.

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11
Q

How are the fibrinolytics administered?

A

Injected

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12
Q

What are the therapeutic uses of the fibrinolytics?

A

Used for the treatment of pulmonary embolism and STEMI.

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13
Q

What are the adverse effects and contraindications of the fibrinolytics?

A
  1. Bleeding, especially hemorrhagic stroke
  2. Streptokinase can induce antibodies, cause allergy and inactivate after initial use.
  3. Do not use in unstable angina, may convert non-STEMI to full infarction.
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14
Q

Which drug is a neurotransmitter releaser?

A

Amphetamine

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15
Q

What is the cellular effect (MOA) of amphetamine?

A

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.

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16
Q

What is the physiological effect (MOA) of amphetamine?

A

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.

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17
Q

What are the amphetamines used for?

A

Drugs of abuse.

Highly addictive, amphetamine more powerful then ephedrine.

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18
Q

What are the adverse effects associated with amphetamine use?

A

Tremor, anxiety, arrhythmia, heart failure.

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19
Q

Which drugs are parasympatholytics?

A

Atropine

Hyoscine

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20
Q

What is the mechanism of action of the parasympatholytics (cellular)?

A

Blocks post-ganglionic muscarinic receptors.

Decreases IP3.

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21
Q

What is the mechanism of action of the parasympatholytics (physiological)?

A

Generally decrease salivation, mydriasis, decreases peristalsis, prevent bladder voiding, increase heart rate, bronchodilation, decreases salivary gland secretion, increase bladder sphincter tone

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22
Q

What are the therapeutic uses of the parasympatholytics?

A

Stop vagal induced effects and decrease salivation in surgery.
Hyoscine = IBS
Can also be used in some forms of AV nodal block.

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23
Q

What are the adverse effects / contraindications of the parasympatholytics?

A
  1. Dry mouth
  2. Tachycardia
  3. Constipation
  4. Urine retention
  5. Blurred vision & mydriasis
  6. Glaucoma
24
Q

Which drug is a neurotransmitter re-uptake inhibitor?

A

Cocaine

25
Q

What is the cellular effect (MOA) of cocaine?

A

Increases release of neurotransmitters from synaptic vesicles. NA, DA, serotonin all increased. Increased conduction through AV node and conduction in SA node. Increases contractility. Increases oxygen demand by the heart.

26
Q

What is the physiological effect (MOA) of cocaine?

A

Mimics the effect of NA and Adr on beta-1 in the heart. Increase heart rate and arrhythmia. Potent central effects increase performance, motivation and power.

27
Q

What is cocaine used for?

A

Drug of abuse, highly addictive.

Occasionally used as a local anesthetic but a highly addictive substance.

28
Q

What are the adverse effects associated with cocaine use?

A

Tremor, anxiety, arrhythmia, heart failure.

29
Q

Which drug is an alpha-1 agonist?

A

Phenylephrine

30
Q

How is phenylephrine given?

A

Topical or oral

31
Q

What is the mechanism of action of phenylephrine (chemical)?

A

Direct alpha-1 effects stimulate receptors leading to increase in vascular smooth muscle activity.

32
Q

What is the mechanism of action of phenylephrine (physiological)?

A

Mimics the effect of NA and Adrenaline on arterioles. Constricts arteries that perfuse nasal mucosa causing decongestion and relief of allergic symptoms.

33
Q

What is phenylephrine used for?

A

Used for the symptomatic control of symptoms of the common cold and allergies.

34
Q

What are the adverse effects and contraindications of phenylephrine?

A
  1. Increases TPR = C/I in hypertension

2. Topical application may cause rebound increase in symptoms and watery discharge.

35
Q

Which drug is an indirect alpha-1 agonist and amine releaser?

A

Pseudoephedrine / ephedrine

36
Q

What is the mechanism of action of pseudoephedrine / ephedrine (cellular)?

A

Increases release of NA (mainly) but also DA. Indirect release of NA stimulates alpha 1 receptors leading to increase in vascular smooth muscle activity.

37
Q

What is the mechanism of action of pseudoephedrine / ephedrine (physiological)?

A

Mimics the effect of NA and Adrenaline on arterioles. Constricts arteries that perfuse nasal mucosa causing decongestion and relief of allergic symptoms.

38
Q

What is pseudoephedrine / ephedrine used for?

A

Used for the symptomatic control of symptoms of the common cold and allergies.

39
Q

What are the adverse effects / contraindications of pseudoephedrine / ephedrine?

A
  1. Increases TPR = C/I in hypertension

2. Central effects like tremor, anxiety, tachycardia and palpitations.

40
Q

Which drug is an alpha 1, beta 1 and beta 2 agonist?

A

Adrenaline

41
Q

How is adrenaline administered?

A

Only used IV

42
Q

What is the mechanism of action of adrenaline (cellular)?

A

Increases conduction through AV node and conduction in SA node. Increases contractility. Increase oxygen demand by the heart. Direct alpha 1 effects stimulate beta 2 receptors.

43
Q

What is the mechanism of action of adrenaline (physiological)?

A

Mimics the effect of NA and Adrenaline on beta-1 cells in the heart and JG cells

44
Q

What are the therapeutic uses of adrenaline?

A
  1. Increases cardiac output and HR
    = used in anaphylaxis and cardiogenic shock
  2. Also used as local vasoconstrictor for prolonging the action of local amide anesthetics
45
Q

What are the adverse effects and contraindications of adrenaline?

A

Tremor, anxiety, arrhythmia, heart failure

46
Q

Which drug is a beta 2 agonist?

A

Salbutamol

47
Q

How is Salbutamol administered?

A

MDI, tabs, syrup, IV

48
Q

What is the mechanism of action of Salbutamol (cellular)?

A

Stimulate beta 2 receptors in the bronchioles. Increase cAMP.

49
Q

What is the mechanism of action of Salbutamol (physiological)?

A

Mimics the effect of adrenaline on beta 2 receptors in the lungs, skeletal muscle and liver. Also inhibits uterine contractions.

50
Q

What are the therapeutic uses of Salbutamol?

A
  1. Increase airway diameter, used in asthma and COPD

2. Also prevents premature labor in pre-term women

51
Q

What are the adverse effects / contraindications of salbutamol?

A

Tremor, anxiety, tachycardia

= mainly at high doses through beta-1 cardiac effects

52
Q

Which drug is a beta 1 receptor agonist?

A

Dobutamine

53
Q

How is dobutamine administered?

A

Only given IV

54
Q

What is the mechanism of action of dobutamine (cellular)?

A

Increase conduction through AV node and conduction tin SA node. Increase contractility. Increase oxygen demand by the heart.

55
Q

What is the mechanism of action of dobutamine (physiological)?

A

Mimics the effect of NA and Adr on beta-1 in heart and JG cells.

56
Q

What are the therapeutic uses of dobutamine?

A

Increases CO and HR
= Both uses in cardiogenic shock
Increases CO and renal perfusion

57
Q

What are the adverse effects / contraindications of dobutamine?

A

Tremor, anxiety, arrhythmia, heart failure