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Pharmacology- Katzung (Spring 2019) > Pharmacology: Katzung symphathomimetics > Flashcards

Pharmacology: Katzung symphathomimetics Flashcards

1
Q

What are the two classes of symphathomimetics?

A

(1) direct acting

(2) indirect acting

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2
Q

What are the two classes of direct acting symphathomimetics?

A

(1) Alpha agonists

(2) Beta agonists

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3
Q

What are the two classes of indirect acting symphathomimetis?

A

(1) releasers

(2) re-uptake inhibitors

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4
Q

What are the three subclasses of direct acting sympathomimetics?

A

(1) catecholamines
(2) Non-catecholamines
(3) Non-catecholamine beta selective.

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5
Q

To what drug class do epinephrine, norepinephrine, Dopamine, isoproterenol, and dobutamine belong to?

A

They are catecholamines.

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6
Q

What is the mechanism of action for Epinephrine?

A

Epinephrine is an alpha 1 & 2, Beta 1,2, & 3 agonist.

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7
Q

What is the clinical use for epinephrine?

A

Epinephrine is used for anaphylaxis and hemostasis.

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8
Q

What are the major toxicities of epinephrine?

A

(1) hypertension
(2) arrythmia
(3) stroke
(4) MI
(5) pulmonary edema

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9
Q

What is the mechanism of action for Norepinephrine?

A

Alpha 1 & 2. Beta 1 agonist.

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10
Q

What are the clinical uses for Norepinephrine?

A

Neurogenic shock, last resort therapy in shock.

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11
Q

What are the adverse effects associated with norepinephrine?

A

(1) vasospasm
(2) tissue necrosis
(3) excessive blood pressure increase
(4) arrythmias
(5) infarction

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12
Q

What is the mechanism of action for dopamine?

A

D1, Alpha1, Alpha 2, beta 1, beta 2, beta 3 agonist

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13
Q

What are the clinical uses for dopamine?

A

(1) Shock
(2) renal shutdown
(3) occasionally heart failure

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14
Q

What are the adverse affects of dopamine?

A

(1) cardiovascular disturbances

(2) arrythmias

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15
Q

What is the mechanism of action for isoproterenol?

A

Isoproterenol is a Beta 1, 2, & 3 agonist

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16
Q

What is the clinical use for isoproterenol?

A

isoproterenol is used for acute asthma by nebulizer.

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17
Q

What is the mechanism of action for dobutamine?

A

Dobutamine is a beta 1 agonist

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18
Q

What is the primary clinical use for dobutamine?

A

Dobutamine is a beta 1 agonist used in acute heart failure to increase cardiac output.

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19
Q

What is the mechanism of action for phenylephrine?

A

Phenylephrine is an alpha 1 alpha 2 agonist

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20
Q

What is the primary clinical use for phenylephrine?

A

(1) decongestant
(2) Mydriatic
(3) neurogenic hyotension.

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21
Q

What are the adverse affects associated with phenylephrine?

A

(1) hypertension
(2) stroke
(3) MI

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22
Q

What is the mechanism of action for albuterol, metaproterenol, terbutaline, Salmeterol, and formoterol?

A

They are all Beta 2 agonists.

23
Q

What is the primary clinical use for albuterol, metaproterenol, and terbutaline?

A

They are used for prompt onset for acute bronchospasm.

24
Q

What are the adverse effects of the selective beta 2 agonists?

A

(1) tachycardia

(2) tremor.

25
Q

What are clinical uses for salmeterol, and formoterol?

A

Salmeterol, and formoterol are not useful in acute bronchospasm. They are used only with corticosteroids for prophylaxis. Slow onset, long action.

26
Q

What are the three classes of indirect acting symphathomimetics?

A

(1) Phenylisopropylamines
(2) cocaine
(3) Tyramine

27
Q

What class of drugs do amphetamine, methamphetamine, and ephedrine belong to and what is their mechanism of action?

A

They are phenylisopropylamines. The MOA is that they displace stored catecholamines.

28
Q

What are the clinical uses for Amphetamine and methamphetamine?

A

(1) narcolepsy
(2) anorexiant
(3) ADHD

29
Q

What are the adverse effects associated with Amphetamine and methamphetamine?

A

(1) High addiction liability
(2) Paranoia
(3) aggression
(4) insomnia
(5) Hypertension

30
Q

What are the clinical uses for ephedrine?

A

(1) narcolepsy
(2) idiopathic postural hypotension
(3) enuresis
Lower addiction liability than amphetamines

31
Q

What is the mechanism of action for Cocaine?

A

Cocaine blocks norepinephrine and dopamine re-uptake

32
Q

What are the clinical uses for cocaine?

A

(1) local anesthetic

(2) intrinsic hemostatic action

33
Q

What are the adverse effects associated with cocaine?

A

(1) very high addiction liability
(2) Hypertension
(3) arrythmias
(4) siezures. (common with overdose)

34
Q

What is the mechanism of action for tyramine?

A

Tyramine displaces stored catecholamines

35
Q

What are the clinical uses for tyramine?

A

No clinical uses but found in fermented foods

36
Q

How is tyramine metabolized?

A

Usually has a high first pass effect however in those taking MAO inhibitors it is absrobed.

37
Q

What are the adverse effects associated with tyramine?

A

(1) hypertension
(2) arrythmias
(3) stroke
(4) MI

38
Q

What effect can MAO and COMT inhibitors have on symphathomimetics?

A

They will increase the intracellular stores of catecholamines and may therefore potentiate the action of catecholamine releasers.

39
Q

Amphetamines have what unique pharmacokinetic property?

A

amphetamines are resistant to MAO.

40
Q

Where are alpha 1 receptors found?

A

(1) vascular smooth muscle (contraction)
(2) eye (contraction of pupillary dilator and pilomotor smooth muscle)
(3) Liver (stimulate glycogenolysis)

41
Q

Where are alpha 2 receptors found?

A

(1) Nerve terminals (inhibits transmitters)
(2) Platelets (stimulate aggregation)
(3) Some vascular smooth muscle (contraction)
(4) fat cells (inhibits lipolysis)
(5) pancreatic beta cells (inhibits insulin release)

42
Q

Where are Beta 1 receptors found?

A

(1) heart ( increases HR and contractility)

2) Juxtaglomerular cells (stimulates renin

43
Q

Where are beta 2 receptors found?

A

(1) Airway, uterine, and vascular smooth muscle (relaxes)
(2) Liver (stimulates glycogenolysis)
(3) pancreatic beta cells (stimulates insulin release
(4) somatic motor neuron terminals (causes tremor)
(5) Heart (stimulates rate and force)

44
Q

Where are beta 3 receptors found?

A

(1) fat cells (stimulates lipolysis)

45
Q

Where are D1 receptors found?

A

renal and splanchnic blood vessels (dilates)

46
Q

Where are D2 receptors found?

A

Nerve terminals (inhibits adenylyl cyclase.)

47
Q

What kind of drug is clonidine?

A

Clonidine is an alpha 2 agonist

48
Q

What are the effects of the alpha 2 agonists like clonidine?

A

(1) vasoconstriction when taken IV

(2) reduced sympathetic outflow and blood pressure when given orally.

49
Q

What are the effects of beta agonists on the heart?

A

They increase rate and contractility. The direct effect overcomes the baroreceptor reflex from the increased pressure.

50
Q

What are the effects on the heart of the pure alpha agonists?

A

They usually slow the heart rate because of the baroreceptor reflex.

51
Q

What class of drug is tetrahydrozoline?

A

Tetrahydrozoline is an alpha agonist use to produce mydriasis.

52
Q

What class of drugs do apraclonidine and brimonidine belong to?

A

They are alpha 2 agonists that are used for glaucoma

53
Q

What is midrodine?

A

Midrodine is an alpha 1 agonist that is used for orthostatic hypertension.

Pharmacology- Katzung (Spring 2019) (52 decks)

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