11 Adrenergics II Flashcards

1
Q

11

Postsynaptic adrenergic receptors (alpha 1, beta 1, beta 2, and DA 1 are primarily located in 4 major areas which are?

A

1) Cardiac Muscle
2) Smooth Muscle
3) Glands
4) Renal vasculature

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2
Q

11

Drugs that stimulate adrenergic transmission are most commonly used for what?

A

Hypotensive therapies

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3
Q

11

Drugs that inhibit adrenergic transmission are most commonly used for what?

A

Hypertensive therapies.

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4
Q

11

Would you inhibit or stimulate adrenergic transmission to increase blood flow to the skin and splanchnic areas?

A

You would inhibit adrenergics.

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5
Q

11

post ganglionic nerve terminal receptors are alpha 2 and DA 2. Agonist of these receptors have what effects on the body?

A

They deplete NE agents decreasing the sympathetic response. (This is because they are neg. feedback looping)

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6
Q

11

T/F A post-junctional antagonist of adrenergic receptors has the same overall effect as an agonist of pre-junctional adrenergic receptors?

A

True

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7
Q

11

Clonidine, Guanabenz, and alpha methyldopa are examples of what type of drug?

A

alpha 2 receptor agonists.

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8
Q

11

An alpha 2 receptor agonist would cause decreased peripheral resistance, decrease heart rate, and decrease C.O. What effect does an alpha 2 receptor have on blood pressure?

A

Decreased blood pressure would be observed. However, alpha 2 agonists do not affect baroreceptor reflexes and rarely elicit orthostatic hypertension.

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9
Q

11

Alpha 2 agonist have side effects which include?

A

1) sedation
2) xerostomia
3) anorexia
4) fluid retention
5) Vivid dreams and CNS stimulation.

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10
Q

11

Bromocriptine is an example of what type of drug?

A

D2 receptor agonist.

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11
Q

11

Bromocriptine is primarily used as an anti parkinsons agent. What are some of its peripheral side effects?

A

1) postural hypotension

2) cardiac arrhythmia

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12
Q

11

T/F D2 receptors on post synaptic effector sites in the CNS are involved in negative feedback inhibition?

A

False. They are not, only in the periphery.

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13
Q

11

Reserpine is considered a NE depleting drug. How does it work? How long does it act.

A

1) It depletes stores of biogenic amines (Epi, norepi, DA, serotonin) in both the CNS and PNS by blocking transport into storage vesicles.
2) It has a long duration of action.

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14
Q

11

Reserpine has side effects which include?

A

1) sedation
2) depression
3) Parkinsonian symptoms
4) Increased GI motility leading to ulcers.

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15
Q

11

what function does Guanethidine have?

A

it prevents the release of NE (only) by stabilizing neuronal membranes and interfering with exocytosis.

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16
Q

11

How does guanethidine get into the nerve terminal?

A

through the amine 1 transporter

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17
Q

11

what effect does cocaine and tricyclic antidepressants (NET inhibitors) have on guanethidine activity?

A

They both block its activity because guanethidine has to first be taken up by amine 1 transporter to be effective. If this transporter is shut down, then guanethidine becomes ineffective.

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18
Q

11

Why would you give your patient guanethidine?

A

You would give it to them as an anti hypertensive.

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19
Q

11

Alpha methyldopa is a drug used for?

A

anti hypertension

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20
Q

11

how does alpha methyldopa work?

A

Alpha methyldopa replaces DOPA in the synthesis of NE. The result is that you no longer get pure NE but rather alpha methly NE which elicits a much weaker response than pure NE.

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21
Q

11

T/F Alpha methyl NE (MNE) is described as a False Neurotransmitter?

A

True. It takes the place of NE but does not do the same level of action.

22
Q

11

Is MNE (methyl NE) able to get into the CNS? What does it do?

A

Yes. This is how it acts as an anti hypertensive. It targets the brain stem affecting the vasomotor center.

23
Q

11

what are some of the chronic side effects of methyl NE?

A

hemolytic anemiahepatitisleukopenialupus like problems.

24
Q

11

an alpha 1 adrenergic blocker would have what effects?

A

inhibit constriction/contraction resulting in lower MAPRelieve inhibition on GI

25
Q

11

Which type of alpha 1 antagonists are reversible? Irreversible?

A

reversible=competitiveIrreversible=non competitive

26
Q

11

T/F Beta 1 blocker inhibit cardiac output?

A

true

27
Q

11

Phenoxybenzamine is an example of what type of drug?

A

alpha 1 adrenergic blocker.

28
Q

11

Is phenoxybenzamine competitive or non competitive? and how does it work?

A

1) Non competitive
2) It covalantly binds to the alpha 1 receptor blocking its activity. It also binds to amine I transport blocking its ability to reuptake NE.

29
Q

11

Phenoxybenzamine usually works for 24 hours as an alpha 1 adrenergic blocker decreasing the sympathetic response. What ill effects will this drug have on the body?

A

Postural hypotensiontachycardia

30
Q

11

T/F Phenoxybenzamine is used as treatment for pheochromocytomas?

A

true for the management of hypertension before surgery.

31
Q

11

What is prazosin? competitive or non competitive?

A

Its an alpha 1 antagonistcompetitive

32
Q

11

Prazosin can be used as an antihypertensive with little or no effect on tachycardia. Why would this be?

A

It is alpha 1 receptor selective. (No beta 1)

33
Q

11

what does the drug phentolamine do?

A

its a competitive antagonist for the alpha 1 receptor. (Note that this drug is considered a dirty drug in that it inhibits both alpha 1 and alpha 2 receptors and can even interact with muscarinic and histamine receptors)

34
Q

11

T/F The therapeutic use of phentolamine relates to its action on the B2 receptor?

A

False. Its action relates to the hypotensive effect is has by blocking alpha 1 receptors.

35
Q

11

It was mentioned earlier that the drug phenoxybenzamine can be used to manage a pheochromocytoma. Can the drug Phentolamine also be used for this?

A

Yes

36
Q

11

T/F most beta blockers are pure antagonists?

A

true. (This means that the agent binds the receptor but does not activate it)

37
Q

11

Beta receptor inhibitors are widely used for?

A

hypertension therapy. (they are usually used in conjunction with diuretics)

38
Q

11

why would you favor using a beta blocker over an alpha 1 blocker for treating a patient with asthma?

A

Because beta 1 receptor blockers are effective for treating hypertension, and less prone to induce bronchoconstriction because there is some beta 2 cross reactivity.

39
Q

11

Propranolol, pindolol, timolol, and Nadolol are all examples of what type of drug?

A

1)beta 1 and beta 2 blockers (antagonists)

40
Q

11

Why is Timolol widely used for glaucoma therapy?

A

it lowers the intraocular pressure

41
Q

11

T/F Propranolol a beta 1 and 2 antagonist is an effective prophylactic treatment to prevent recurrence of Myocardial infarction?

A

True Because the beta 2 activity allows for dilation of the arteries/veins in the heart.

42
Q

11

T/F Beta 2 antagonists should be given to those with hypertension and asthma?

A

False. Beta 2 antagonists can allow further bronchoconstriction because beta 2 usually relaxes smooth m. in the bronchioles.

43
Q

11

Betaxolol, atenolol, metoprolol, and esmolol are all examples of which type of drug?

A

Beta 1 antagonists (specific)

44
Q

11

T/F Metoprolol a beta 1 antagonist is an effective prophylactic agent to prevent recurrences of myocardial infarction?

A

True

45
Q

11

Beta 1 adrenergic blockers (antagonists) target what?

A

they have cardiac specificity

46
Q

11

what are some common side effects when using propranolol and metoprolol (beta 1 blockers)?

A

ataxiadizziness

47
Q

11

why do Nadolol and atenolol (beta 1 blockers) not cause as many side effects?

A

becuase they cannot cross the BBB

48
Q

11

What is the biggest concern when using beta blockers?

A

they must be used with caution on patients with cardiac insufficiency because you decrease the HR, contractility, and C.O.

49
Q

11

What are the 5 medical diseases listed that are usually treated with adrenergic antagonists?

A

1) pheochomocytoma (alpha 1 antagonist)
2) Hypertension (beta blockers main, alpha 1 can be used)
3) Ischemic heart disease (beta blockers)
4) Glaucoma (beta blockers)
5) urinary obstruction (alpha 1 treatment)

50
Q

11

why are beta blockers used for glaucoma?

A

they lower intraocular pressure by reducing production of aqueous humor.