Adrenergic Agonists And Antagonists 2 Flashcards

(48 cards)

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
What is esmolol given to treat?
Control ventricular rate in patients with atrial fibrillation / atrial flutter
26
What drugs are the α1 and β blockers
Labetalol and carvedilol
27
Labetalol is a more potent as a ___________ antagonist than a ________ antagonist
β; α
28
What are some clinical uses of carvedilol
- HTN - CHF Has antioxidant properties
29
What kind of drug is pindolol and to whom would you give it?
Partial β agonist; to people with diminished cardiac reserve or a propensity to bradycardia
30
β blockers, particularly ________ are effective in diminishing intraocular pressure in treating glaucoma
Timolol
31
Conditions that β blockers can be used to treat:
- 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
β blockers are useful ______ management of stable angina
Chronic
33
________ blockers are used to treat essential tremors
Β
34
What are some adverse effects of β blockers
- bronchoconstrction - impairs recovering from hypoglycemia because of blocking the β2 receptors in the liver AND the tachycardia associated with hypoglycemia is masked
35
What is the risk fo taking β blockers in someone who is diabetic?
The β blocker can mask the tachycardia that comes with hypoglycemia so they must monitor sugar levels closely
36
Lipid levees are relatively unaffected by ______ and_______
Labetalol & pindolol
37
In terms of lipid metabolism, both non selective and β1 selective blockers ↑ ______ and ↓ ______
TG; HDL
38
β blockers should be gradually tapered off to avoid ______________ and these adverse effects are due to ______
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
What kind of drug is α methyltyrosine (metyrosine)
Inhibitor of NE synthesis
40
What is the MOA of metyrosine and what is it used for?
MOA: competitive inhibitor of tyrosine hydroxylase | - used for: management of malignant pheochromocytoma
41
Metyrosine is a ____________ inhibitor of _________which converts _________ to ________
Competitive; tyrosine hydroxylase; | Dopamine → NE
42
Resperine is a reversibly / irreversibly blocks ________ causing ________
Reversibly; VMAT (vesicles cannot store NE or dopamine) Depletion of NE because they are in the cytoplasm which is where MAO is too
43
What is the drug that is a reversible inhibitor of VMAT?
Tetrabenazine
44
What drug is given for the treatment of chorea associated with Huntington’s Disease
Tetrabenazine
45
What receptor is associated with the ciliary epithelium and activation of it produces aqueous humour?
β2
46
Where are M3 receptors found on in the eye?
- pupillary constrictor muscle | - ciliary muscle (contract facilitates OUTFLOW of aqueous humor and thus ↓ intraocular pressure)
47
___________ receptors on the ciliary epithelium inhibit/facilitate secretion of aqueous humor
β2; facilitate
48
________ antagonist can be used to ↓ intraocular pressure by ↓ secretion of aqueous humor
β2 antagonist