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3rd Quarter > Pharm Quiz #8 > Flashcards

Pharm Quiz #8 Flashcards

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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?

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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?

Study These Flashcards
A

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

25
What characteristics to Beta 1 receptors?
Selected agonist actions: increased myocardial contractility Mechanism: Gs, increased cAMP Agonists: isoproterenol, dobutamine, epi, NE Antagonists: Metoprolol, atenolol
26
What are characteristics to Beta 2 receptors?
Selected agonist actions: smooth muscle relaxation Mechanism: Gs, cAMP increased Agonists: Albuterol, terbutaline, isoproterenol Antagonists: Propranolol
27
What are characteristics to Beta 3 receptors?
Selected agonist actions: lipolysis Mechanism: Gs, cAMP increased Agonists: None in current use Antagonists: double cheeseburgers
28
How are catecholamines metabolized?
By monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT)
29
What are metabolites to catecholamines?
Pharmacologically inactive and include 3-methoxy-4-hydroxymandelic acid, metanephrine, and nor-metanephrine
30
Inhibition of reuptake produces greater ___ that inhibition of enzymes.
potentiation
31
Synthetic non-catecolamines not affected by COMT and thus depend on ___
MAO
32
Inhibition of catecholamine uptake by drugs such as ___ and ___ produce sympathomimetic effects
cocaine | tricyclic antidepressants
33
Synthetic non-catecholamines activate adrenergic receptors by evoking release of ___ from post ganglionic sympathetic nerve endings
NE
34
Indirect acting drugs
Mephentermine Metaraminol Ephedrine Cocaine -blocks the re-uptake of monoamines Amphetamine - promotes NE release from nerve endings and blocks NE re-uptake Methylphenidate
35
Indirect acting sympathomimetics require endogenous catecholamines to produce effects, little activity if catecholamines are ___
depleted
36
What are uses of indirect acting adrenergics?
Cocaine is used as a local anesthetic with vasoconstriction Appetite suppression ADD, ADHD, narcolepsy Abuse
37
Direct acting adrenergics do not require endogenous catecholamines to produce effects - active even if catecholamines are ___
depleted
38
Two structural classes of alpha 1 agonists
phenethylamines - related in structure to epi | imidazolines - related in structure to Afrin
39
List uses for alpha 1 agonists
Hypotension Ophthalmic preparations to induce mydrasis Cough and cold preparations - induces constriction of nasal mucosa, decreases resistance to air flow
40
Alpha 2 agonists, name one
Dexmedetomidine Effects: sedation, analgesia, sympatholysis, anxiolysis
41
What is the infusion rate of dexmedetomidine?
1 mic/kg loading dose, administered over 10 min, followed by maintenance infusion of 0.2-1 mic/kg/hour
42
Beta 1 adrenergic agonists, list direct acting agonists
Dopamine Dobutamine Epinephrine Isoproterenol
43
What are beta 1 agonists used for?
CHF Cardiogenic shock Increase myocardial contractility and CO
44
Stimulation of beta 1 receptors induces positive ___, ___, and ___ effects
Chronotropic Dromotropic Inotropic
45
Stimulation of renal beta 1 receptors causes ___ release, mediating extracellular volume and regulating mean arterial pressure
renin
46
Stimulation of beta 2 receptors induces smooth muscle ___, induces tremor in skeletal muscle, and ___ glycogenolysis in the liver and skeletal muscle
relaxation | increases
47
Stimulation of beta 3 receptors induces ___
lipolysis
48
Describe where the three types of beta receptors work?
B1 - heart and kidney B2 - lungs, GI tract, liver, uterus, vascular smooth muscle, skeletal muscle B3 - fat cells
49
List the effects of epinephrine
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
Epinephrine is a ___ agonist of adrenergic receptors
Non-selective
51
What amino acids make epinephrine?
Phenylalanine and tyrosine
52
List the steps for the production of Epi in the body
Tyrosine - DOPA - dopamine - NE - epinephrine
53
What nerve from the SNS stimulates the release of epinephrine?
Splanchnic nerves to the adrenal medulla
54
___ triggers exocytosis of chromaffin granules and release of epinephrine and NE into the bloodstream
Calcium
55
Explain the varying doses in epinephrine
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
What routes can epi be given?
IV, SQ, ETT, aerosol, topical

3rd Quarter (22 decks)

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