Konorev Antiadrenergic Drugs Part 2 Flashcards

1
Q

what are direct acting antiadrenergic α adrenoceptor antagonists?

A
  • Non selective α1 and α2
    • phentolamine
    • phenoxybenzamine
  • α1 selective
    • prazosin
    • Tamsulosin
    • Doxazosin
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2
Q

What are the direct acting antiadrenergic drugs in the mixed blocker class?

A
  • Labetalol
  • Carvedilol
  • both are B and α1 antagonists
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3
Q

What are the direct acting antiadrenergic drugs that fall into the Beta adrenoceptor blockers?

A
  • B1 and B2 blockers
    • propanolol
    • pindolol
    • Nadolol
  • B1 Selective
    • Metoprolol
    • Betaxolol
    • Acebutolol
    • Atenolol
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4
Q

What are the indirect acting antiadrenergic drugs that fall under the NE release inhibiitor class?

A

Guanethidine

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5
Q

What are the indirect acting antiadrenergic drugs that fall under inhibition of tyrosine hydroxylase?

A

Metyrosine

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6
Q

Pharmacokinetics of Phentolamine?

A
  • reversible competitive α antagonist
  • Non covalent binding
  • Short acting
  • antagonized by high concentrations of agonist
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7
Q

Phenoxybenzamine pharmacokinetics?

A
  • non competitive irreversibole α antagonist
  • covalent binding
  • longer acting than phentolamine
  • Effect is not antagonized by α agonist
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8
Q

Pharmacodynamics of α antagonists on the cardiovascular system?

A
  • Decreased peripheral vascular resistance and BP
  • Postural hypotension
  • reflex tachycardia
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9
Q

Pharmacodynamics of α antagonists on the GU system?

A
  • relaxation of smooth muscle in prostate
  • Decreased resistance to flow of urine
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10
Q

Pharmacodynamics of α antagonists on the eye?

A

Relaxation of pupillary dilator muscles- miosis

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11
Q

Pheochromocytoma is treated with what drugs?

A

α antagonists such as:

  • Phentolamine
    • a direct acting antiadrenergic non selective α1 and α2 receptor antagonist
  • Phenoxybenzamine
    • a non selective α1 and α2 receptor antagonist
  • Metyrosine
    • Indirect acting antiadrenergic drug inhibitor of tyrosine hydroxylase
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12
Q

What is chronic (essential) HTN treated with? What are the drug classes?

A
  • Prazosin
  • Doxazosin
  • Both are α1 selective direct acting antiadrenergic drugs
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13
Q

How is ED treated?

A

Combination of phentolamine and a non specific vasodilator papaverine

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14
Q

Chronic urinary obstruction secondary to BPH is treated with what drug? What receptor does it prefer?

A
  • Tamsulosin
  • impacts α1A more than α1B receptors
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15
Q

AE’s of alpha antagonists?

A
  • seen less with α1 selelctive antagonists
  • Postural hypotension- due to antagonism of α1 in venous smooth muscle
  • Nasal stuffiness
  • Tachycardia
  • Retention of fluid and salt
  • Imparied ejaculation
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16
Q

What are the Mixed Beta adrenoceptor antagonists?

A
  • Labetalol B and α1
  • Carvedilol B and α1
17
Q

What are the B1 and B2 adrenoreceptor blockers?

A
  • Propanolol
  • Pindolol (partial agonist)
  • Nadolol
18
Q

What are the B1 selective adrenoceptor antagonists?

A
  • Metoprolol (inverse agonist)
  • Betaxolol (inverse agonist)
  • Acebutolol (partial agonist)
  • Atenolol
19
Q

What are the pro’s to using a beta blocker with Intrinsic Sympathomimetic Activity, in other words the drug is a partial agonist at the beta adrenergic receptor?

A
  • They have less risk for bradycardia
  • Increase VLDL/HDL
  • They block sympathetic effects but have submaximal effects of their own
20
Q

Pharmacodynamics of beta blockers on the heart?

A
  • Negative inotropic effect
  • Negative chronotropic effect
  • Slow AV node conduction
21
Q

Pharmacodynamics of beta blockers on blood vessels?

A
  • Initially see a rise in peripheral vascular resistance but with chronic use it leads to a decrease in PVR (lowering BP)
22
Q

How do Beta blockers impact Renin angiotensin system?

A

Inhibit renin release

23
Q

How do Beta blockers impact respiratory system?

A

Increase airway resistance

24
Q

How do Beta blockers impact the eye?

A

Reduce production of aqueous humor decreasing intraocular pressure

25
Q

How do beta blockers impact metabolism?

A
  • inhibit lipolysis
  • Increase VLDL decrease HDL
  • Inhibit glycogenolysis and gluconeogenesis in the liver
26
Q

Long term use of what two drug after a MI increase the survival?

A
  • Propanolol
    • B1 and B2 blocker
  • Metoprolol
    • B1 selective
27
Q

How do Beta blockers reduce the frequency of anginal episodes?

A
  • Block cardiac beta receptors and decrease cardiac work reducing oxygen consumption
28
Q

How do Beta blockers impact glaucoma?

A
  • Reduction in production of aqueous humor by ciliary body reduces intraocular pressure
  • Use Betaxolol
29
Q

What beta blocker is used to help with hyperthyroidism effects on the heart?

A

Propranolol

30
Q

AE’s of Beta blockers on CNS

A
  • Sedation
  • Sleep disturbance
  • Depression
31
Q

AE’s of Beta blockers on the respiratory and CV system?

A
  • Increases airway resistance
  • Trigger bronchospasm and asthma attack in susceptible people
  • Depress heart rate, contractility, and excitability of heart
32
Q

What are the effects on lipid profiles when using beta blockers?

A
  • Chronic use increases VLDL and decreases HDL
33
Q

How do beta blockers impact hypoglycemic episodes?

A
  • May delay recovery from insulin induced hypoglycemia by inhibiting glucose output by liver
  • Blunt perception of hypoglycemia
  • Switch to a B1 selective
34
Q

Abrupt discontinuation of beta blocker therapy can lead to what cardiac issues?

A
  • enhanced cardiac stimulation and arrhythmias
  • Increased risk in patients with ischemic heart disease
  • Need to gradually taper dosing to prevent sympathetic hyperresponsiveness and toxicity
35
Q

Which of the following effects of epinephrine will be blocked by metoprolol?

  • Contraction of radial sm mm in iris
  • Constriction of cutaneous vessels
  • Relaxation of bronchial sm mm
  • Increased renin release
A

Increased renin release