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3rd Quarter > Pharm Quiz #8 > Flashcards

Pharm Quiz #8 Flashcards

1
Q

List naturally occurring catecholamines

A

Epinephrine
Norephinephrine
Dopamine

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2
Q

List synthetic catecholamines

A

Isoproterenol

Dobutamine

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3
Q

List synthetic non-catecholamines

A 
Ephedrine
Amphetamines
Phenylepherine
Methoxamine
Mephentermine
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4
Q

List pharmacologic effects of adrenergic agonists

A 
Vasoconstriction (arterioles, capacitance vessels)
Vasodilation (skeletal muscle)
Bronchodilation
Cardiac stimulation
Lipolysis, glycogenolysis
CNS stimulation
Modulation of insulin
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5
Q

What is the structure of adrenergic drugs?

A

Adrenergic agonists derived from beta-phenyl-ethylamine
Hydroxyl groups on the 3 and 4 carbon positions of the benzene ring designate catechol status
Non-catecholamines are deficient at the 3 and 4 carbon substitution

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6
Q

List the six steps of adrenergic transmission

A 
Synthesis
Storage
Release via Ca++ mediated exocytosis
Binding
Degradation
Recycling
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7
Q

Epi and NE binding to receptors alter the ___ conformation - three dimensional shape of the receptor

A

chemical

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8
Q

A1 couples to Gq which results in increased intracellular ___

A

Calcium

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9
Q

A2 couples to Gi causing a decrease of ___ activity

A

cAMP

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10
Q

B receptors couple to Gs and increase intracellular ___ activity

A

cAMP

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11
Q

Sympathomimetic drugs have their effect on adrenergic receptors located in the ___ and ___

A

CNS and ANS

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12
Q

In the adrenergic system (SNS), what is the post-gangionic neurotransmitter? Pre-ganglionic?

A

Post - Epi or NE

Pre - Ach

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13
Q

In the PNS, what is the post-ganglionic neurotransmitter? Pre-ganglionic?

A

Ach for both

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14
Q

Where are A1 receptors found and what do they do?

A

Post synaptic sites

Vasoconstriction, mydriasis, relaxation of GI, contraction of GI sphincters, contraction of bladder sphincters

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15
Q

Where are A2 receptors found and what do they do?

A

Pre-synaptic sites

Inhibition of NE (post-synaptic), platelet aggregation, hyperpolarization of cells in the CNS, sedation

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16
Q

What happens when adrenergic receptors are activated?

A

Heart rate increases, pupils dilate, energy is mobilized, and blood flow diverted from non-essential organs to skeletal muscle

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17
Q

What are the subtypes of beta receptors?

A

B1, B2, and B3

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18
Q

Phenylephrine is an agonist of what receptors?

A

alpha only

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19
Q

All adrenergic receptors are linked to Gs proteins, which are linked to ___. Agonist binding causes a rise in the second messenger ___.

A

Adenylate cyclase

cAMP

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20
Q

Downstream effectors of cAMP include ___ which mediates intracellular events following homrone binding.

A

protein kinase (PKA)

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21
Q

What are the mechanism, agonist, and antagonist of alpha 1 receptors?

A

Selected agonist actions: smooth muscle contraction
Mechanism: Gq
Agonist: NE, phenylephrine, methoxamine
Antagonists: phenoxybenzamine,, phentolamine

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22
Q

What are the characteristics of alpha 2 receptors?

A

Agonist potency: NE > epinephrine > isoproterenol
Selected agonist actions: smooth muscle contraction, neurotransmitter inhibition
Mechanism: Gi
Agonists: dexamedetomidine, clonidine
Antagonists: yohimbine

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23
Q

Where are alpha 2 receptors found?

A

In the peripheral and central nervous systems, platelets, and a variety of organs, including the liver, pancreas, kidney, and eye

24
Q

Alpha 2 G proteins - modulate cellular activity by… what?

A

Activated G proteins modulate cellular activity by signaling a second messenger system or by modulating ion channel activity

25
Q

What characteristics to Beta 1 receptors?

A

Selected agonist actions: increased myocardial contractility
Mechanism: Gs, increased cAMP
Agonists: isoproterenol, dobutamine, epi, NE
Antagonists: Metoprolol, atenolol

26
Q

What are characteristics to Beta 2 receptors?

A

Selected agonist actions: smooth muscle relaxation
Mechanism: Gs, cAMP increased
Agonists: Albuterol, terbutaline, isoproterenol
Antagonists: Propranolol

27
Q

What are characteristics to Beta 3 receptors?

A

Selected agonist actions: lipolysis
Mechanism: Gs, cAMP increased
Agonists: None in current use
Antagonists: double cheeseburgers

28
Q

How are catecholamines metabolized?

A

By monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT)

29
Q

What are metabolites to catecholamines?

A

Pharmacologically inactive and include 3-methoxy-4-hydroxymandelic acid, metanephrine, and nor-metanephrine

30
Q

Inhibition of reuptake produces greater ___ that inhibition of enzymes.

A

potentiation

31
Q

Synthetic non-catecolamines not affected by COMT and thus depend on ___

A

MAO

32
Q

Inhibition of catecholamine uptake by drugs such as ___ and ___ produce sympathomimetic effects

A

cocaine

tricyclic antidepressants

33
Q

Synthetic non-catecholamines activate adrenergic receptors by evoking release of ___ from post ganglionic sympathetic nerve endings

A

NE

34
Q

Indirect acting drugs

A

Mephentermine
Metaraminol
Ephedrine
Cocaine -blocks the re-uptake of monoamines
Amphetamine - promotes NE release from nerve endings and blocks NE re-uptake
Methylphenidate

35
Q

Indirect acting sympathomimetics require endogenous catecholamines to produce effects, little activity if catecholamines are ___

A

depleted

36
Q

What are uses of indirect acting adrenergics?

A

Cocaine is used as a local anesthetic with vasoconstriction
Appetite suppression
ADD, ADHD, narcolepsy
Abuse

37
Q

Direct acting adrenergics do not require endogenous catecholamines to produce effects - active even if catecholamines are ___

A

depleted

38
Q

Two structural classes of alpha 1 agonists

A

phenethylamines - related in structure to epi

imidazolines - related in structure to Afrin

39
Q

List uses for alpha 1 agonists

A

Hypotension
Ophthalmic preparations to induce mydrasis
Cough and cold preparations - induces constriction of nasal mucosa, decreases resistance to air flow

40
Q

Alpha 2 agonists, name one

A

Dexmedetomidine
Effects:
sedation, analgesia, sympatholysis, anxiolysis

41
Q

What is the infusion rate of dexmedetomidine?

A

1 mic/kg loading dose, administered over 10 min, followed by maintenance infusion of 0.2-1 mic/kg/hour

42
Q

Beta 1 adrenergic agonists, list direct acting agonists

A

Dopamine
Dobutamine
Epinephrine
Isoproterenol

43
Q

What are beta 1 agonists used for?

A

CHF
Cardiogenic shock
Increase myocardial contractility and CO

44
Q

Stimulation of beta 1 receptors induces positive ___, ___, and ___ effects

A

Chronotropic
Dromotropic
Inotropic

45
Q

Stimulation of renal beta 1 receptors causes ___ release, mediating extracellular volume and regulating mean arterial pressure

A

renin

46
Q

Stimulation of beta 2 receptors induces smooth muscle ___, induces tremor in skeletal muscle, and ___ glycogenolysis in the liver and skeletal muscle

A

relaxation

increases

47
Q

Stimulation of beta 3 receptors induces ___

A

lipolysis

48
Q

Describe where the three types of beta receptors work?

A

B1 - heart and kidney
B2 - lungs, GI tract, liver, uterus, vascular smooth muscle, skeletal muscle
B3 - fat cells

49
Q

List the effects of epinephrine

A

Increases HR and SV
Dilates the pupils
constricts arterioles in the skin and GI tract
Dilates arterioles in skeletal muscles
Elevates blood sugar by catabolism of glycogen to glucose in the liver
Begins the breakdown of lipids in fat cells
Suppresses the immune system

50
Q

Epinephrine is a ___ agonist of adrenergic receptors

A

Non-selective

51
Q

What amino acids make epinephrine?

A

Phenylalanine and tyrosine

52
Q

List the steps for the production of Epi in the body

A

Tyrosine - DOPA - dopamine - NE - epinephrine

53
Q

What nerve from the SNS stimulates the release of epinephrine?

A

Splanchnic nerves to the adrenal medulla

54
Q

___ triggers exocytosis of chromaffin granules and release of epinephrine and NE into the bloodstream

A

Calcium

55
Q

Explain the varying doses in epinephrine

A

Doses of 1-2 mcg/min stimulate beta 2 in peripheral vasculature
Doses of 4 mcg/min stimulate beta 1 in heart
Doses of 10-20 mcg/min stimulate both beta1 and beta2 with alpha predominating in vascular beds

56
Q

What routes can epi be given?

A

IV, SQ, ETT, aerosol, topical

3rd Quarter (22 decks)

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