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CV Module > CV Pharm-Anti Hypertensives > Flashcards

CV Pharm-Anti Hypertensives Flashcards

1
Q

What are the effects of the sympathetic nervous system in HTN?

A
  1. Via Barometric reflex
    - increases HR
    - Vasoconstriction
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2
Q

Where does AT act to produce hypervolemia via retention of Na and H2O?

A

Proximal tubule

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3
Q

What is the neurotransmitter of the sympathetic nervous system?

A

Norepi

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4
Q

Which receptors does Norepinephrine act on?

A

Alpha adrenergic & Beta Adrenergic

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5
Q

What type of receptors are the Angiotensin receptors and Alpha adrenergic receptors?

A

These are GQ coupled receptors, whose activation results in the release of Phospholipase C which acts on PIP2 to create DAG & IP3 which results in release of Calcium from the SR

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6
Q

Where are the Alpha Adrenergic and ATII receptors primarily?

A

In Smooth muscle (VSM) cells

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7
Q

What kind of receptors are in the heart cells?

A

Beta Adrenergic receptors

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8
Q

What are the Beta Adrenergic receptors coupled to?

A

GS coupled

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9
Q

What does activation of the Beta Adrenergic receptors result in?

A

Activation of Adenylate cyclase which converts ATP to cAMP which the activates the L-Type Calcium channels via PK-A

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10
Q

Where is Epinephrine made?

A

Adrenal Medulla

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11
Q

What are the predominant receptors in the heart and Lung?

A

B1 in the Heart

B2 in the Lung

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12
Q

What are the effects of NorEpi after binding with Beta1 receptors in the heart?

A
  1. Increase of force of myocardial contraction
  2. Increase in HR
  3. Increase in the rate of myocardial relaxation
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13
Q

What is the major receptor upon which norepi acts in peripheral blood vessels?

A

Alpha 1 receptors (including in the kidney)

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14
Q

What is the effect of norepi action on PBV?

A

Increase in systolic and diastolic Pressures

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15
Q

Which causes the greater vasoconstriction Norepi or Epi and why?

A

Norepinephrine because it does not induce compensatory vasodilation via Beta2 receptors on blood vessels supplying skeletal muscle

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16
Q

What are the peripheral vessels most acted on by the sympathetic nervous system?

A
  1. Precapillary arterioles

2. Venules

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17
Q

What is the function of the Alpha2 receptors in the presynaptic cleft?

A

To feedback inhibit the release of norepi

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18
Q

How is adrenergic receptor signalling terminated?

A

By Uptake 1 of the transmitter usually by the presynaptic neuron

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19
Q

How does Reserpine work?

A

Inhibits (uptake 2) VMAT the transporter of Dopamine and Norepi into transmitter vesicles of adrenergic nerves

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20
Q

What is the effect of reserpine?

A

TPR is reduced due to the highly reduced amount of norepi to act on Alpha receptors

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21
Q

How is reserpine administered?

A

.5mg Orally

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22
Q

What are the side effects of Reserpine?

A

Sedation and mental depression

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23
Q

When is reserpine contraindicated?

A
  1. In patients with a history of mental depression (increases suicidal tendencies)
  2. In patients with a history of Duodenal ulcers
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24
Q

What is the mechanism of action of the alpha 1 selective blockers (osin)

A

Block the peripheral alpha 1 receptors (mostly on arterioles and venules)

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25
Q

What is the effect of Alpha 1 blockers?

A

1.Reduced Total peripheral resistance and reduced BP

26
Q

What is another use of the Alpha 1 blockers?

A

BPH by relaxing the muscles of the bladder and prostate

27
Q

What are some benefits of Alpha 1 blockers?

A

Increase HDL lower LDL

Beneficial effect on insulin resistance

28
Q

What is the preferred patient population for the Alpha1 blockers (osin)?

A

Healthy Older men with hypertension and BPH

29
Q

What are the side effects of The selective Alpha1 blockers?

A

Orthostatic hypertension, first dose should be taken before bed
Sometimes dizziness and vertigo drowsiness and palpitations

30
Q

When would you use The nonselective alpha blockers Phentolamine and Phenoxybenzamine?

A

Preoperative to prevent hypertensive crisis in patients undergoing surgery for pheochromocytoma

31
Q

What is Intristic sympathomimetic activity?

A

Partial agonist action by adrenoreceptor blockers

32
Q

What Beta Blockers are known to have ISA activity?

A

Pindolol and Acebutolol

33
Q

What is meant by the “Membrane Stabilizing effect?”

A

The ability of certain Beta Blockers to have a local anesthetic action

34
Q

Which beta blockers have no membrane-stabilizing activity?

A
  1. Timolol

2. Atenolol

35
Q

Which of the Beta Blockers are Non B1 selective?

A

Those beginning with letters from N-Z i.e Propranolol, Timolol Pindolol

36
Q

Which of the Beta Blockers has the Lowest and Highest lipid solubility?

A
  1. Highest = Propranolol

2. Lowest = Atenolol

37
Q

What are the effects of Beta 1 selective beta blockers in normal individuals?

A

Blocking of myocardial Beta 1 adrenergic receptors results in decreased HR, decreased contractility, thus decreased cardiac output.

38
Q

What is the effect of Beta Blockers in the kidney?

A

They Block the Beta1 receptors in the kidney and inhibit the release of Renin

39
Q

Which Beta Blocker has no effect on Renin release

A

Pindolol

40
Q

What would be the effect of Beta Blockers on Peripheral NE?

A

Decrease the release of peripheral NE by inhibiting presynaptic B adrenergic receptors

41
Q

When are Beta Blockers most effective?

A

In cases of high Renin hypertension like is most common in Young and caucasians.

42
Q

What is the therapy of choice for hypertensive patients who have also had MI, ischemic heart disease or CHF?

A

Beta Blockers

43
Q

What are some conditions that are compelling for Beta Blockers?

A

1,Hyperthyroidism

2.Migranes

44
Q

What drugs can be used to reduce the risk of a second heart attack?

A

Beta Blocker i.e Carvedilol, Metoprolol-XL and Bisoprolol

45
Q

Those Beta Blockers with membrane stabilizing activity can also be used as?

A

Antiarrhythmic drugs

46
Q

In what chronic condition is propranolol and all nonselective Beta Blockers contraindicated?

A

Asthma as they can induce Bronchospasms

47
Q

How must Beta Blocker Therapy be terminated?

A

Gradually due to that fact that receptors are upregulated during therapy

48
Q

Which Long Acting Beta Blocker is considered to be the “Best”

A

Bisoprolol

49
Q

If during surgery one discovers and arrhythmia (possibly due to halothane anesthetic) what should be IV administered to the patient?

A

Esmolol (Brevibloc)

50
Q

What are the side effects of Beta Blockers?

A
  1. Cold extremeties from unopposed alpha adrenergic action which constricts blood vessels
  2. Bradycardia
  3. Bronchospasm
  4. CNS side effects Bad dreams etc
51
Q

Which calcium channel Blockers are contraindicated with Beta Blockers and why?

A

Verapamil and Diltiazem for dangerous Bradycardia

52
Q

What are the metabolic side effects of Beta Blockers?

A
  1. Block Glycogenolysis and delay recovery from Hypoglycemia in type 1 diabetes
  2. Can Block Hormone sensitive Lipase and increase LDL and decrease HDL and increase triglycerides
53
Q

What is Labetalol?

A

IV Beta Blocker for treatment of Hypertensive emergencies, Is a non-selective with Alpha-1 receptor antagonism

54
Q

What is Carvedilol?

A

3rd Gen Beta Blocker with Alpha-1 antagonist activity, is also an antioxidant that scavenges ROS.

55
Q

When is Carvedilol used?

A

Primarily for CHF and HTN

56
Q

Where is Carvedilol etabolized?

A

Hepatic (2D6) metabolism

57
Q

With what drugs should Carvedilol be avoided?

A

With CYP2D inhibitors like Cimetidine, fluoxetine, quinidine

58
Q

What is Celiprolol?

A

Cardio selective + Beta-2 agonism

59
Q

What is unique about Celiprolol?

A

Directly vasodilates Blood vessels due to its partial Agonist activity

60
Q

When is Celiprolol used?

A

Treatment of HTN and Angina

61
Q

What is the drug of choice in HTN with Metabolic syndrome?

A

Nebivolol

CV Module (24 decks)

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