Adrenergic Agonists And Antagonists 2 Flashcards

1
Q

Low dose of epinephrine mainly causes ______

A

Vasodilation due to β2 activation;

High doses: both α1 and β2 activated but vasoconstriction due to α1 > β2

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2
Q

Changes in _______ will produce a secondary homeostatic response that tends to compensate for any changes

A

MAP

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3
Q

What are the 5 classes of drugs that are adrenergic agonists?

A
  • α antagonists: non selective and α1
  • β antagonists: non selective and β1
  • α1 and β antagonists
  • partial agonists
  • drugs that act presynaptically
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4
Q

Drugs that are non selective α adrenergic blockers

A
  • phenoxybenzamine

- phentolamine

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5
Q

Phenoxybenzamine and phentolamien are _________

A

NON selective α adrenergic blockers

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6
Q

MOA of phenoxybenzamine and what is it used for?

A

Irreversible antagonist and is unsuccessful for treating hypertension

USED IN PHEOCHROMOCYTOMA

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7
Q

What drug would you give to treat pheochromocytoma

A

Phenoxybenzamine; give it prior to surgical removal of the tumor or if the tumor is inoperable

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8
Q

Phentolamine ______________ blocks __________

A

Reversibly; α1 and α2 receptors

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9
Q

What are some uses for phentolamine?

A
  • control of HTN during preoperatirve preparing and surgical excision in pheochromocytoma
  • used to DIAGNOSE pheochromocytoma via the phentolamine blocking test
  • prevention of dermal necrosis due to NE
  • solve hypertensive crisis due to stimulant drug overdose
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10
Q

______________ ↓ in response to epinephrine that is given in the presence of phenoxybenzamine

A

Systemic BP because the α1 action is blocked but NOT the β2 action → vasodilation

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11
Q

What is the clinical implication of someone taking α blockers and then they have a allergic reaction?

A

Would have to administer epinephrine but instead of ↑ their BP it would ↓ their BP because the β2 would be more activated because all the α receptors are blocked

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12
Q

List the 4 α1 selective adrenergic blockers

A
  • prazosin
  • terazosin
  • doxazosin
  • tamsulosin
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13
Q

What is important about when giving someone α1 blockers for the first time?

A

The first dose produces an exaggerated hypotensive response so the first dose should be 1/3 or 1/4 of the normal dose

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14
Q

α1 blockers are the drugs of choice for ______

A

Symptom relief of benign prostatic hyperplasia : relaxes smooth muscle in genitourinary tract improving urinary flow

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15
Q

__________ and __________ of the α1 blockers have longer half life

A

Terazosin; doxazosin

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16
Q

__________ is the α receptor subtype that is found predominant in the GU smooth muscle and _______ is selective for them

A

α1A; tamulosin

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17
Q

What are the benefits of using tamulosin?

A

Treat BPH with less effect on BP and less chance to cause orthostatic HTN because it acts specifically on α1A receptor

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18
Q

What are the non selective β blockers?

A
  • propranolol
  • nadolol
  • Timolol
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19
Q

Non selective β blockers are contraindicated in _______

A

Patients with asthma

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20
Q

Metabolic effects of non selective β blockers:

A

↓ glycogenolysis

↓ glucagon secretion

21
Q

what are the β1 selective adrenergic antagonists

A
  • atenolol
  • metoprolol
  • esmolol
22
Q

What kind of drugs would you give hypertensive patients with impaired pulmonary function

A

Β1 selective antagonists such as: atenolol and metoprolol

23
Q

What would you give diabetic hypertensive patients who are using insulin to treat their hypertension

A

Β1 selective antagonists: atenolol and metoprolol

24
Q

Esmolol is a _______________ drug and is given via _________ for ___________

A

Β1 selective antagonist; IV; rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter

25
Q

What is esmolol given to treat?

A

Control ventricular rate in patients with atrial fibrillation / atrial flutter

26
Q

What drugs are the α1 and β blockers

A

Labetalol and carvedilol

27
Q

Labetalol is a more potent as a ___________ antagonist than a ________ antagonist

A

β; α

28
Q

What are some clinical uses of carvedilol

A
  • HTN
  • CHF

Has antioxidant properties

29
Q

What kind of drug is pindolol and to whom would you give it?

A

Partial β agonist; to people with diminished cardiac reserve or a propensity to bradycardia

30
Q

β blockers, particularly ________ are effective in diminishing intraocular pressure in treating glaucoma

A

Timolol

31
Q

Conditions that β blockers can be used to treat:

A
  • HTN
  • glaucoma
  • migraines (prophylaxis)
  • hyperthyroidism
  • angina pectoris: they ↓ O2 requirement of the heart muscle
  • atrial fibrillation: esmolol
  • MI: protects myocardium to ↓ cardiac remodeling
  • performance anxiety
  • essential tremor
32
Q

β blockers are useful ______ management of stable angina

A

Chronic

33
Q

________ blockers are used to treat essential tremors

A

Β

34
Q

What are some adverse effects of β blockers

A
  • bronchoconstrction
  • impairs recovering from hypoglycemia because of blocking the β2 receptors in the liver AND the tachycardia associated with hypoglycemia is masked
35
Q

What is the risk fo taking β blockers in someone who is diabetic?

A

The β blocker can mask the tachycardia that comes with hypoglycemia so they must monitor sugar levels closely

36
Q

Lipid levees are relatively unaffected by ______ and_______

A

Labetalol & pindolol

37
Q

In terms of lipid metabolism, both non selective and β1 selective blockers ↑ ______ and ↓ ______

A

TG; HDL

38
Q

β blockers should be gradually tapered off to avoid ______________ and these adverse effects are due to ______

A

Tachycardia, HTN, and/or ischemia;

Up regulation of β receptors so if you remove the β blockers immediately, they will have an exaggerated sympathetic response

39
Q

What kind of drug is α methyltyrosine (metyrosine)

A

Inhibitor of NE synthesis

40
Q

What is the MOA of metyrosine and what is it used for?

A

MOA: competitive inhibitor of tyrosine hydroxylase

- used for: management of malignant pheochromocytoma

41
Q

Metyrosine is a ____________ inhibitor of _________which converts _________ to ________

A

Competitive; tyrosine hydroxylase;

Dopamine → NE

42
Q

Resperine is a reversibly / irreversibly blocks ________ causing ________

A

Reversibly;
VMAT (vesicles cannot store NE or dopamine)
Depletion of NE because they are in the cytoplasm which is where MAO is too

43
Q

What is the drug that is a reversible inhibitor of VMAT?

A

Tetrabenazine

44
Q

What drug is given for the treatment of chorea associated with Huntington’s Disease

A

Tetrabenazine

45
Q

What receptor is associated with the ciliary epithelium and activation of it produces aqueous humour?

A

β2

46
Q

Where are M3 receptors found on in the eye?

A
  • pupillary constrictor muscle

- ciliary muscle (contract facilitates OUTFLOW of aqueous humor and thus ↓ intraocular pressure)

47
Q

___________ receptors on the ciliary epithelium inhibit/facilitate secretion of aqueous humor

A

β2; facilitate

48
Q

________ antagonist can be used to ↓ intraocular pressure by ↓ secretion of aqueous humor

A

β2 antagonist