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Pharmacology I > Lecture 14/15 - Adrenergic Stimulants > Flashcards

Lecture 14/15 - Adrenergic Stimulants Flashcards

1
Q

What are the catecholamines? (three)

A

Epinepherine
Norepinephrine
Isoproterenol

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2
Q

What is the beta1 agonist?

A

Dobutamine

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3
Q

What is the beta2 agonist?

A

Albuterol

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4
Q

What is the alpha agonist?

A

Phenylphrine

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5
Q

What are the alpha2 agonists? (four)

A

Xylazine
Detomidine
Medetomidine
Dexmedetomidine

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6
Q

What are three other adrenergic stimulants that aren’t really receptor related?

A

Amphetamine
Cocaine
Tyramine

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7
Q

Where is NE released from?

A

Nerves + Adrenal medulla

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8
Q

What does NE stimulate?

A

Alpha + B1

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9
Q

Where is EPI released from?

A

Adrenal medulla

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10
Q

What does EPI stimulate?

A

Alpha + Beta

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11
Q

What inhibits tyrosine hydroxylase?

A

Metyrosine

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12
Q

What is the basic progression of Tyrosine to Epi?

A

Tyrosine - L-DOPA - Dopamine - NE - EPI

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13
Q

What are the two way that NE/EPI/ISO are metabolized?

A

MAO - in nerve

COMT - in circulation

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14
Q

What two drugs stimulate NE release?

A

Amphetamines + Tyramine

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15
Q

What does cocaine do in the adrenergic terminal?

A

Inhibit NE reuptake

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16
Q

What compound would you test to test NE levels in the body?

A

VMA levels in urine

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17
Q

What does SNS stimulation of Alpha1 do?

A

Vasoconstriction

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18
Q

What does SNS stimulation of Beta1 do?

A

Increase heart rate + contractility

Renin secretion

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19
Q

What does SNS stimulation of Beta2 do?

A

Vasodilation of skeletal muscle BV

Glycogenolysis

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20
Q

What does SNS stimulation of Beta3 do?

A

Lipolysis

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21
Q

What does SNS stimulation of Alpha2 do?

A

Inhibit NE release (or any NT)

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22
Q

What occurs with indirect acting drug when denervation happens?

A

No longer work

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23
Q

What occurs with direct acting drugs when denervation occurs?

A

Increase activity possible

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24
Q

What makes up NE?

A

Dopamine + hydroxyl group

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25
Q

What does NE stimulate?

A

Alpha + B1

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26
Q

What makes up EPI?

A

NE + Methyl group

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27
Q

What does EPI stimulate?

A

Alpha + Beta

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28
Q

What makes up Isoproterenol?

A

EPI + 2 methyl groups

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29
Q

What does isoproterenol stimulate?

A

Betas

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30
Q

Where is isoproterenol found in the body?

A

Not, synthetically made drug

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31
Q

What is the ranking of sensitivity to alpha receptors?

A

EPI > or = NE&raquo_space;»»> ISO

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32
Q

What is the most basic characteristic of alpha1?

A

Excitatory

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33
Q

What stimulates alpha1?

A

Phenylephrine

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34
Q

What is the activity of alpha2?

A

Inhibitory, pre-synaptically

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35
Q

What activates alpha2?

A

Clonidine

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36
Q

What are the results of Phenylephrine administration?

A

Vasoconstriction = Increased resistance
Mydrasis
Prostate + bladder base + urtheral spincter = contract
Pilomotor SM stimulation

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37
Q

What are the results of Xylazine administration?

A

Decreased NE release = Decreased BP
Inhibit ACh release = Decreased secretions
CNS depression

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38
Q

What happens with general alpha agonists in the cardiovascular system?

A

Increased arterial resistance (Diastolic)

Increased BP = Baroreceptors = Decreased HR

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39
Q

What happens with general alpha agonists in the eye?

A

Mydriasis (no effect of accommodation)
Decreased production of Aqueous humor
Increased outflow of aqueous humor

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40
Q

What happens with respiration in the presence of alpha agonists?

A

Constrict nasal + upper airway BV

41
Q

What happens in the genitourinary tract in the presence of an alpha agonist?

A

Increase continence

Ejaculation

42
Q

What is the compound preference in Beta1?

A

ISO> EPI = NE

43
Q

What is the compound preference in Beta2?

A

ISO>EPI»NE

44
Q

What is the compound preference in Beta 3?

A

Iso = NE > EPI

45
Q

What type of receptors are betas?

46
Q

What is the effect of Dobutamine adminstration?

A

Increased HR + Force
Increase automaticity
Increased Renin secretion

47
Q

What is the effect of Albuterol adminstration?

A

Bronchodilation = relax bronchial SM
BV to skeletal muscles dilate
Glucogenolysis + Gluconeogenesis
K+ uptake into muscle

48
Q

What is the general affects of beta receptor activation in the cardiovascular system?

A 
Increased HR + Force 
Ca+ influx
AV/SA node conduction increases = automaticity 
Ventricular conduction increase 
Increased O2 consumption 
Increased CO = Increased systolic
49
Q

What is the general effects of beta receptor activation in the eye?

A

increase aqueous humor production
increase ocular pressure
Slight relaxation of ciliary muscle

50
Q

What occurs in the respiratory system with beta receptor activation?

A

Bronchial SM relaxation

51
Q

What does beta receptor activation do in the gentiourinary system?

A

Decrease contractions of uterus

Relax bladder wall

52
Q

What does beta receptor activation do in regards to metabolism?

A

Increase Renin secretion (1)
Glycogenolysis + K+ uptake into cells + Inc. insulin (2)
Lipolysis (3)

53
Q

What happens with NE administration with BP and HR?

A

HR increases, with decrease from baroreceptor reflex

D/S Pressure increase

54
Q

What happens with phenylephrine administration with BP and HR?

A

Vasoconstriction = Increased BP

Baroreceptor reflex = decreased HR

55
Q

What is phenylephrine used for/

A

Hypotensive emergencies

56
Q

Whats the upside to using phenylephrine in a clincal emergency situation?

A

Can increase BP without affecting HR

57
Q

What is an important thing you must watch out for with stopping phenylephrine termination?

A

Rebound effect

58
Q

What fungus produces ergot alkaloids?

A

Claviceps purpurea

59
Q

What are the symptoms or ergotism?

A

dementia + hallucinations + stimulation of uterine SM

Vasoconstriction = gangrene

60
Q

What receptors does ergotamine activate?

A

Partial agonist for Alpha + Serotonin

61
Q

What does medetomidine activate?

62
Q

What occurs with medetomidine activation?

A

Inhibit NE release in brain = Sedation + Analgesia
Decrease SNS output
Decrease BP + HR + RR

63
Q

What is the general characteristic of Detomidine?

A

Long duration of action

64
Q

What is the general characteristic of Romifidine?

A

less ataxia than others

65
Q

What is the general characteristic of Xylazine?

A

Increased risk of vomiting

66
Q

What is clonidine used for?

A

Decrease BP in humans

67
Q

What are the peripheral side effects of alpha2 agonist administration?

A

Vomiting in small animals
Decreased GI motility + acid
Hypertension followed by Hypo + Brady
Reduced RR

68
Q

What is important to know about sheep and goats in regards to alpha 2 agonists?

A

increase resipratory rate + airway pressure

69
Q

What does isoproterenol stimulate?

70
Q

What are the effects of isoproterenol on BP and HR?

A

Increase rate + force of heart
Vasodilation (B2) = decreased BP (Diastolic + MAP)
Baroreceptor reflex further increases HR

71
Q

What is isoproterenol used for?

A

Cardiac arrest + Heart block

72
Q

What can an overdose of isoproterenol cause?

A

palpitations + sinus tachycardia + arrhythmia

73
Q

What does dobutamine activate?

74
Q

What happens with dobutamine administration?

A

Increase force and rate of heart

Short duration

75
Q

What are the uses for dobutamine?

A

Increase CO in shock or CHF

76
Q

What is terbutaline used for?

A

Oral treatment of bronchospasms

RAO/heaves in horses

77
Q

What are the side effects of terbutaline?

A

Tremors + Tachycardia + Headache

78
Q

What is albuterol used for?

A

Rapid bronchodilation

79
Q

What is clenbuterol used for?

A

RAO in horses

Uterine relaxation in cattle

80
Q

What are the affects of NE administration on the cardiovascular system?

A

Increase BP (PP unchanged)
Decreased BF to kidneys + spleen + liver
HR increases but then decreases
Increased peripheral resistance

81
Q

When is NE used clinically?

A

Hypotensive crisis

82
Q

What happens if NE + atropine given together?

A

Vagal reflex blocked = Increased HR

83
Q

What is a really bad side effect of NE adminstration?

A

Necrosis if gets into area with poor circulation

84
Q

What happens with a low dose of EPI?

A

B2 mostly stimulated
Vasodilation = Decrease Diastolic
MAP same

85
Q

What happens with high dose of EPI?

A

Alpha activated as well
Vasocontriction
BP increases

86
Q

What are the four big reasons for epinephrine use?

A

Vasoconstriction
Anaphylactic shock
Cardiac arrest + complete heart block
Bronchodilation

87
Q

What are the side effects of EPI administration?

A

Throbbing headache
Palpitations + angina
Restlessness + tremors

88
Q

What is dopamine used for clinically?

A

Treat cardiogenic shock

Increase BF + CO w/o vasoconstriction

89
Q

Why does a High dose of Dopamine increase heart rate?

A

NE is made from this

90
Q

What occurs with amphetamine administration?

A

NE + DA release

DA = indirect

91
Q

What symptoms are seen with amphetamine adminstration?

A

Tremor + Tachycardia + Hypertension

Agitation + Insomina + increase motor activity

92
Q

What is horner’s syndrome?

A

SNS denervation to one eye

93
Q

What occurs with Horner’s syndrome?

94
Q

With Horner’s syndrome what is the response to a indirect agonist?

95
Q

With Horner’s syndrome what is the response to a direct agonist?

A

Increased response

96
Q

How does Tyramine work, in a general sense?

A

Indirectly

97
Q

What does tyramine do?

A

Gets into vesicles and displaces NE

98
Q

What is a major symptom with tyramine?

A

Tachyphylaxis w/ repeated application

Severe hypertension

99
Q

When does someone come into contact with tyramine?

A

Found in food

Normally broken down by MAO’s in GI, unless patient is on MAO inhibitor

Pharmacology I (21 decks)

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