Pharm Quiz #8 Flashcards Preview

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Flashcards in Pharm Quiz #8 Deck (56):
1

List naturally occurring catecholamines

Epinephrine
Norephinephrine
Dopamine

2

List synthetic catecholamines

Isoproterenol
Dobutamine

3

List synthetic non-catecholamines

Ephedrine
Amphetamines
Phenylepherine
Methoxamine
Mephentermine

4

List pharmacologic effects of adrenergic agonists

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

5

What is the structure of adrenergic drugs?

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

6

List the six steps of adrenergic transmission

Synthesis
Storage
Release via Ca++ mediated exocytosis
Binding
Degradation
Recycling

7

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

chemical

8

A1 couples to Gq which results in increased intracellular ___

Calcium

9

A2 couples to Gi causing a decrease of ___ activity

cAMP

10

B receptors couple to Gs and increase intracellular ___ activity

cAMP

11

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

CNS and ANS

12

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

Post - Epi or NE
Pre - Ach

13

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

Ach for both

14

Where are A1 receptors found and what do they do?

Post synaptic sites

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

15

Where are A2 receptors found and what do they do?

Pre-synaptic sites

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

16

What happens when adrenergic receptors are activated?

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

17

What are the subtypes of beta receptors?

B1, B2, and B3

18

Phenylephrine is an agonist of what receptors?

alpha only

19

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

Adenylate cyclase
cAMP

20

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

protein kinase (PKA)

21

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

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

22

What are the characteristics of alpha 2 receptors?

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

23

Where are alpha 2 receptors found?

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

24

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

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