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Pharmacology Test #3 > Alpha and Beta Adrenergics > Flashcards

Alpha and Beta Adrenergics Flashcards

1
Q

Direct acting adrenergic receptor agonists

A

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

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2
Q

alpha 2 receptors mainly mediate

A

cardio control center in the CNS (brain stem)

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3
Q

Beta 1 receptors mainly deal with what

A

heart (cardiac muscle), control renin release in the kidney

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4
Q

Beta 2 receptors mainly deal with what

A

smooth muscle vasculature, skeletal muscle blood vessels, bronchiole smooth muscle and uterine smooth muscle

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5
Q

direct acting alpha1 receptor agonists mediate

A

vasoconstriction and can also mediate pupil dilation (radial muscle under alpha1 control)

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6
Q

alpha 1 receptor agonists

A

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

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7
Q

alpha 2 receptor agonists

A 
Clonidine (Catapres)
Methyldopa (Aldomet)
Guanabenz (Wytensin)
Guanfacine (Texex)
Tizanidine (Zanaflex)
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8
Q

Non-selective beta receptor agonist

A

Isoproterenol (Isuprel)

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9
Q

Beta1-selective receptor agonists

A

Dobutamine (Dobutrex)

Dopamine (Inotropin)

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10
Q

Beta2-selective receptor agonists

A 
Terbutaline (Brethine, Bricanyl)
Metaproterenol (Metaprel, Alupent)
Albuterol (Proventil, Ventolin)
Salmeterol (Serevent)
Ritodrine (Yutopar)
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11
Q

What is the EC50?

A

drug concentration at which 50% of the receptors are activated

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12
Q

cardiovascular effects of alpha1 agonists

A

vasoconstriction, which increases blood pressure

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13
Q

cardiovascular effects of beta1 agonists

A

expect increased heart rate, but baroreceptors increase vagal tone, which slows heart rate

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14
Q

cardiovascular effects of beta2 agonists

A

vasodilation, which decreases the blood pressure (drop in bp may also trigger baroreceptor reflex to increase heart rate)

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15
Q

effects of norepinephrine on heart rate

A

net effect = decreased heart rate
alpha1 agonist increases blood pressure but increases heart rate from beta1 agonist increases vagal tone, which decreases heart rate

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16
Q

effects of epinephrine on heart rate

A

observe expected increase in heart rate with beta1

alpha1 and beta2 essentially cancel out effects on blood pressure ( no change in BP)

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17
Q

effects of isoproterenol on heart rate

A

increase in heart rate
beta2 - decrease in blood pressure, increase heart rate
beta1 - increase in heart rate

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18
Q

What type of agonist is l-Norephinephrine (Levophed)

A

potent alpha and beta1 receptor agonist

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19
Q

What is l-Norephinephrine used for?

A

used as a pressor, drives blood pressure up, stimulates heart (slow/no change in heart rate)

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20
Q

What type of agonist is Ephinephrine (Adrenalin)?

A

potent alpha, beta1, and beta2 receptor agonist

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21
Q

What is Ephinephrine (Adrenalin) used for?

A

anaphylaxis, glaucoma, in combination with local anesthetics (vasoconstriction to keep anesthetic in area longer)

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22
Q

What type of agonist is Phenylephrine (Neo-Synephrine)?

A

potent alpha1 receptor agonist

very effective orally (not a substrate for COMT)

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23
Q

What is Phenylephrine used for?

A

nasal decongestant, mydriasis without cycloplegia (paralysis of ciliary muscle in eye), glaucoma, pressor (raises BP)

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24
Q

What type of agonist is Naphazoline (Privine)

A

partial agonist at alpha receptors

25
Q

What type of agonist is Tetrahydrozoline (Visine)

A

partial agonist at alpha receptors

26
Q

What type of agonist is Oxymetazoline (Afrin, Visine)

A

partial agonist at alpha receptors

27
Q

alpha1 agonist side effects

A

changes in blood pressure (increase)

CNS stimulation at increased doses

28
Q

What are Nephazoline, Tetrahydrozoline, and Oxymetazoline used for?

A

nasal and ophthalmic decongestants

OTC in nasal sprays

29
Q

What is the concern with Nephazoline, Tetrahydrozoline, and Oxymetazoline?

A

Tachyphylaxis/Desensitization: causes alpha1 receptors to not respond as well long-term, can cause rebound congestion

30
Q

What type of agonist is Clonidine (Catapres)?

A

selective alpha2 receptor agonist

31
Q

Clinical effects of Clonidine

A

clinical effect linked to activation of alpha2 receptors in the nucleus of the solitary tract (cardiovascular center)

32
Q

Uses of Clonidine

A

very effective anti-hypertensive agent, opiate withdrawal

33
Q

How do alpha2 adrenergic agonists reduce blood pressure

A

by reducing sympathetic output from the brain

34
Q

cardiovascular effects from the decreased sympathetic tone caused by alpha-adrenergic agonists

A

decreased heart rate, decreased contractility, decreased renin release, decreased vasoconstriction

35
Q

Guanabenz (Wytensin) and Guanfacine (Tenex, Intuiv)

A

variants of Clonidine, used in hypertension and ADHD (guanfacine)

36
Q

What is Methyldopa (Aldomet)?

A

a prodrug metabolized to active alpha2 receptor agonist, (1R, 2S)-alpha-methylnorepinephrine

37
Q

Where does Methyldopa act?

A

acts at CNS alpha2 receptors to decrease sympathetic outflow

38
Q

What is Methyldopa used for?

A

hypertension

39
Q

Apraclonidine (Iopidine)

A

alpha2 receptor agonist

used in glaucoma

40
Q

Tizanidine (Zanaflex)

A

alpha2 receptor agonist

used for muscle spasticity (alpha2 receptors in the spinal cord activate the reflex arc)

41
Q

Adverse effects of alpha2-adrenergic receptor agonists

A

sedation, sodium and water retention, dry mouth, withdrawal symptoms

42
Q

What kind of agonist is Isoproterenol (Isuprel)?

A

non-selective beta receptor agonist

43
Q

What is isoproterenol used for?

A

asthma, chronic obstructive pulmonary disease, cardiostimulant

44
Q

What type of agonists are Metaproterenol and Terbutaline?

A

selective beta2 receptor agonists

resorcinol derivatives

45
Q

What are Metaproterenol and Terbutaline used for?

A

asthma, COPD; Terbutaline used as tocolytic (prevents premature labor)

46
Q

What kind of effect can you observe only at high doses of Metaproterenol and Terbutaline?

A

cardiac effects

47
Q

What type of agonist is Albuterol (Ventolin, Proventil) and Levalbuterol (Xopenex)?

A

selective beta2 receptor agonists

48
Q

What is Albuterol/Levalbuterol used for?

A

short acting bronchodilation; asthma and COPD

49
Q

What type of agonist is Salmeterol and Formoterol?

A

selective beta2 receptor agonist

50
Q

How is Salmeterol/Formoterol different from albuterol?

A

Salmeterol/Formoterol are a long acting agents (not recommended for acute treatment of asthma symptoms)

51
Q

How is Salmeterol/Formoterol used?

A

long acting bronchodilation; asthma and COPD

52
Q

Different between Salmeterol and Formoterol?

A

onset of action:
Salmeterol - 10-20 min
Formoterol -

53
Q

What is the net effect of Dobutamine (Dobutrex)?

A

positive inotropic effect on heart with little chronotropic effect (increases force of contraction with little increase in heart rate)

54
Q

What is Dobutamine used for?

A

acute heart failure, shock

55
Q

Where do indirect-acting sympathomimetrics act?

A

act at a target other than the receptor - causes a buildup of neurotransmitter

56
Q

Name some indirect-acting sympathomimetics

A

amphetamine, pseudoephedrine, ephedrine, phenylpropanolamine, tyramine

57
Q

How do indirect-acting sympathomimetics work?

A

promote release of NE via reverse action of plasma membrane transporter

58
Q

Clinical uses of indirect acting sympathomimetics

A

amphetamines: ADHD, narcolepsy, anorexiant
others: nasal decongestants

Pharmacology Test #3 (13 decks)

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