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Pharmacology -- Test #3 > Adrenergic Agents - Day 1 > Flashcards

Adrenergic Agents - Day 1 Flashcards

1
Q

List three direct acting adrenergic receptor agonists

A

Dopamine (Intropin)
Norepinephrine (Levophed)
Epinephrine (Adrenalin)

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2
Q

Dopamine is an activator of ______ receptors.

Where in the body is dopamine especially important?

A

Beta adrenergic

Kidney

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3
Q

Dopamine is converted to NE by…

A

beta-hydroxylase

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4
Q

NE is an activator of _____ receptors.

A

alpha adrenergic receptors

also its okay at B1, but not so much B2

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5
Q

alpha1 receptors are especially important at what location?

A

Vascular System

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6
Q

alpha2 receptors are especially important at what location?

A

Presynaptic feedback

CV control in the brainstem

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7
Q

beta1 receptors are especially important at what location?

A

Heart

Kidney (For Renin Release)

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8
Q

beta2 receptors are especially important at what location?

A

Smooth muscle in BV of skeletal muscles

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9
Q

Direct agonists for alpha1 receptors (3)?

A

Phenylephrine (Neosynephrine)
Methoxamine (Vasoxyl)
Oxymetazoline (Visine)

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10
Q

Alpha1 receptors work by…

A

activation will trigger Gq to turn on PIP2. Leads to IP3 (which ups Ca) and DAG (which activated PKC)

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11
Q

Alpha2 receptors are directly activated by (5)…

A 
Clonidine (Catapres)
Methyldopa (Aldomet)
Guanabenz (Wytensin)
Guanfacine (Tenex)
Tizanidine (Zanaflex)
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12
Q

How do alpha2 receptors work?

A

Turn on Gi, which inhibits Adenylate Cyclase (stopping cAMP signalling) and opens K channels to make cells more negative (and harder for nerves to fire)

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13
Q

Example of a non-selective beta receptor agonist?

A

Isoproterenol (Isuprel)

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14
Q

List two beta-1 adrenergic receptor agonists.

A

Dobutamine (Dobutrex)

Dopamine (Intropin)

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15
Q

List 5 beta2 adrenergic receptor agonists.

A 
Metaproterenol (Metaprel, Alupent)
Albuterol (Proventil, Ventolin)
Salmeterol (Serevent)
Terbutaline (Brethine, Bricanyl)
Ritodrine (Yutopar)
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16
Q

How do beta adrenergic receptors work

A

Turn up Gs proteins, more AC, more cAMP

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17
Q

Alpha1 Adrenergic activation. Rank Phenylephrine, Epinephrine, Norepinephrine, and Isoproterenol from most potent to least potent.

A

PENI

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18
Q

Beta1 and Beta2 Adrenergic activation. Rank Phenylephrine, Epinephrine, Norepinephrine, and Isoproterenol from most potent to least potent.

A

IENP

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19
Q

Out of Phenylephrine, Epinephrine, Norepinephrine, and Isoproterenol, whose potency changes the most from beta 1 to beta 2.

A

Norepinephrine is much less potent in beta2

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20
Q

Cardiovascular effects of Norepinephrine. Tell me all about them.

A

NE is an alpha1 agonist, so it will trigger constriction of the vessels, increasing the BP. The increase in BP triggers the Vagus nerve to drop the pulse rate.

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21
Q

Cardiovascular effects of Epinephrine. Tell me about them.

A

E activates alpha1, beta1 and 2. Beta 1 stimulates the heart rate while causing a minor dilation of the vessels in the skeletal muscle. Beta2 and alpha 1 cancel out. Overall there is minimal BP change.

22
Q

Cardiovascular effects of Isoproterenol. Tell me about them.

A

Beta1 will increase heart rate while beta2 will decrease peripheral resistance. This results in a drop in BP.

23
Q

What is l-NE (Levophed)? What is it a substrate for? How is it dosed? What is it used for?

A

alpha and beta1 agonist.
Substrate for MAO and COMT.
Dosed Parenterally.
Used as a pressor.

24
Q

What is Epinephrine (adrenaline)? What is it a substrate for? How is it dosed? What is it used for?

A

alpha, beta1, and beta2 agonist.
Substrate for MAO and COMT.
Dosed Parenterally.
Anaphylaxis, glaucoma, with local anasthetics.

25
Q

Why use Epinephrine with anesthetics?

A

To diminish blood flow and keep the anasthetic at the site.

26
Q

What is added to preparations of NE and E to prevent oxidation?

A

Sodium Bisulfite.

27
Q

Phenylephrine activates what receptors?

A

alpha1

28
Q

Phenylephrine is a substrate for…

A

MAO

Not COMT, so orally useable

29
Q

Phenylephrine MO Administration?

A

Parenteral, Oral, Local

Basically – whatever the fuck you want.

30
Q

Phenylephrine uses?

A

Mydriasis without cycloplegia
Glaucoma
Pressor
NASAL DECONGESTANT

31
Q

The 2-aralkylimidazolines include which drugs?

A

Naphazoline
Tetrahydrozoline
Oxymetazoline

32
Q

2-aralkylimidazolines activate which receptors?

A

alpha

33
Q

2-aralkylimidazolines are administered how? why?

A

Locally/Topically

To promote vasoconstriction

34
Q

Concerns with overuse of 2-aralkylimidazolines in a patient?

A

Tachyphylaxis (desensitization of receptors)

35
Q

Uses for 2-aralkylimidazolines?

A

Nasal and ophthalmic decongestants

36
Q

Clonidine is an activator of which receptors?

A

Alpha2

37
Q

Significance of Clonidine’s dichlorophenyl ring?

A

Decreases the pKA from 13.6 to 8.0

Prevents charge, helps Clonidine get to target.

38
Q

How is Clonidine administered?

A

Oral, parenteral, transdermal

39
Q

Uses for Clonidine?

A

Hypertension, Opiate Withdrawl

40
Q

How does Clonidine (or alpha2 adrenergic agonists in general) actually lower BP?

A

Clonidine turns off SNS –> decreased heart rate, decreased heart contractility, decreased renin release, and vasodilation.

41
Q

What do Guanabenz and Guanfacine have in common?

A

They are open ring imidazolidines.

42
Q

Guanabenz and Guanfacine act on which receptors?

A

alpha2

43
Q

Guanabenz and Guanfacine. Whats important and unique about each.

A

Guanafacine – Can treat ADHD

Guanabenz – Short half life of 6 hours (half of the others)

44
Q

Guanabenz and Guanfacine are typically prescribed to treat…

A

Hypertension

45
Q

Methyldopa acts on which receptor type?

A

alpha2

46
Q

What is Methyldopa?

A

A prodrug metabolized into its active form (1r,2s)-alpha-methylnorepinephrine

47
Q

What does Methyldopa do for patients physiologically?

A

Acts on CNS alpha2s to decrease sympathetic outflow.

48
Q

Why prescribe Methyldopa?

A

Hypertension

49
Q

Non BP related use of apraclonidine?

A

Glaucoma (but not really anymore…the world is going in a more beta-blocker-y direction these days)

50
Q

Non-BP related use of Tizanidine?

A

Muscle spasticity.
For example messed up reflex arcs of cerebral palsy. By increasing the activity of the alpha2 receptors in the spinal cord that control these arcs, spasticity goes down.

Pharmacology -- Test #3 (13 decks)

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