Lecture 14/15 - Adrenergic Stimulants Flashcards
1
Q
What are the catecholamines? (three)
A
Epinepherine
Norepinephrine
Isoproterenol
2
Q
What is the beta1 agonist?
A
Dobutamine
3
Q
What is the beta2 agonist?
A
Albuterol
4
Q
What is the alpha agonist?
A
Phenylphrine
5
Q
What are the alpha2 agonists? (four)
A
Xylazine
Detomidine
Medetomidine
Dexmedetomidine
6
Q
What are three other adrenergic stimulants that aren’t really receptor related?
A
Amphetamine
Cocaine
Tyramine
7
Q
Where is NE released from?
A
Nerves + Adrenal medulla
8
Q
What does NE stimulate?
A
Alpha + B1
9
Q
Where is EPI released from?
A
Adrenal medulla
10
Q
What does EPI stimulate?
A
Alpha + Beta
11
Q
What inhibits tyrosine hydroxylase?
A
Metyrosine
12
Q
What is the basic progression of Tyrosine to Epi?
A
Tyrosine - L-DOPA - Dopamine - NE - EPI
13
Q
What are the two way that NE/EPI/ISO are metabolized?
A
MAO - in nerve
COMT - in circulation
14
Q
What two drugs stimulate NE release?
A
Amphetamines + Tyramine
15
Q
What does cocaine do in the adrenergic terminal?
A
Inhibit NE reuptake
16
Q
What compound would you test to test NE levels in the body?
A
VMA levels in urine
17
Q
What does SNS stimulation of Alpha1 do?
A
Vasoconstriction
18
Q
What does SNS stimulation of Beta1 do?
A
Increase heart rate + contractility
Renin secretion
19
Q
What does SNS stimulation of Beta2 do?
A
Vasodilation of skeletal muscle BV
Glycogenolysis
20
Q
What does SNS stimulation of Beta3 do?
A
Lipolysis
21
Q
What does SNS stimulation of Alpha2 do?
A
Inhibit NE release (or any NT)
22
Q
What occurs with indirect acting drug when denervation happens?
A
No longer work
23
Q
What occurs with direct acting drugs when denervation occurs?
A
Increase activity possible
24
Q
What makes up NE?
A
Dopamine + hydroxyl group
25
What does NE stimulate?
Alpha + B1
26
What makes up EPI?
NE + Methyl group
27
What does EPI stimulate?
Alpha + Beta
28
What makes up Isoproterenol?
EPI + 2 methyl groups
29
What does isoproterenol stimulate?
Betas
30
Where is isoproterenol found in the body?
Not, synthetically made drug
31
What is the ranking of sensitivity to alpha receptors?
EPI > or = NE >>>>>>> ISO
32
What is the most basic characteristic of alpha1?
Excitatory
33
What stimulates alpha1?
Phenylephrine
34
What is the activity of alpha2?
Inhibitory, pre-synaptically
35
What activates alpha2?
Clonidine
36
What are the results of Phenylephrine administration?
Vasoconstriction = Increased resistance
Mydrasis
Prostate + bladder base + urtheral spincter = contract
Pilomotor SM stimulation
37
What are the results of Xylazine administration?
Decreased NE release = Decreased BP
Inhibit ACh release = Decreased secretions
CNS depression
38
What happens with general alpha agonists in the cardiovascular system?
Increased arterial resistance (Diastolic)
| Increased BP = Baroreceptors = Decreased HR
39
What happens with general alpha agonists in the eye?
Mydriasis (no effect of accommodation)
Decreased production of Aqueous humor
Increased outflow of aqueous humor
40
What happens with respiration in the presence of alpha agonists?
Constrict nasal + upper airway BV
41
What happens in the genitourinary tract in the presence of an alpha agonist?
Increase continence
| Ejaculation
42
What is the compound preference in Beta1?
ISO> EPI = NE
43
What is the compound preference in Beta2?
ISO>EPI>>NE
44
What is the compound preference in Beta 3?
Iso = NE > EPI
45
What type of receptors are betas?
Gs
46
What is the effect of Dobutamine adminstration?
Increased HR + Force
Increase automaticity
Increased Renin secretion
47
What is the effect of Albuterol adminstration?
Bronchodilation = relax bronchial SM
BV to skeletal muscles dilate
Glucogenolysis + Gluconeogenesis
K+ uptake into muscle
48
What is the general affects of beta receptor activation in the cardiovascular system?
```
Increased HR + Force
Ca+ influx
AV/SA node conduction increases = automaticity
Ventricular conduction increase
Increased O2 consumption
Increased CO = Increased systolic
```
49
What is the general effects of beta receptor activation in the eye?
increase aqueous humor production
increase ocular pressure
Slight relaxation of ciliary muscle
50
What occurs in the respiratory system with beta receptor activation?
Bronchial SM relaxation
51
What does beta receptor activation do in the gentiourinary system?
Decrease contractions of uterus
| Relax bladder wall
52
What does beta receptor activation do in regards to metabolism?
Increase Renin secretion (1)
Glycogenolysis + K+ uptake into cells + Inc. insulin (2)
Lipolysis (3)
53
What happens with NE administration with BP and HR?
HR increases, with decrease from baroreceptor reflex
| D/S Pressure increase
54
What happens with phenylephrine administration with BP and HR?
Vasoconstriction = Increased BP
| Baroreceptor reflex = decreased HR
55
What is phenylephrine used for/
Hypotensive emergencies
56
Whats the upside to using phenylephrine in a clincal emergency situation?
Can increase BP without affecting HR
57
What is an important thing you must watch out for with stopping phenylephrine termination?
Rebound effect
58
What fungus produces ergot alkaloids?
Claviceps purpurea
59
What are the symptoms or ergotism?
dementia + hallucinations + stimulation of uterine SM
| Vasoconstriction = gangrene
60
What receptors does ergotamine activate?
Partial agonist for Alpha + Serotonin
61
What does medetomidine activate?
Alpha 2
62
What occurs with medetomidine activation?
Inhibit NE release in brain = Sedation + Analgesia
Decrease SNS output
Decrease BP + HR + RR
63
What is the general characteristic of Detomidine?
Long duration of action
64
What is the general characteristic of Romifidine?
less ataxia than others
65
What is the general characteristic of Xylazine?
Increased risk of vomiting
66
What is clonidine used for?
Decrease BP in humans
67
What are the peripheral side effects of alpha2 agonist administration?
Vomiting in small animals
Decreased GI motility + acid
Hypertension followed by Hypo + Brady
Reduced RR
68
What is important to know about sheep and goats in regards to alpha 2 agonists?
increase resipratory rate + airway pressure
69
What does isoproterenol stimulate?
B1 + 2
70
What are the effects of isoproterenol on BP and HR?
Increase rate + force of heart
Vasodilation (B2) = decreased BP (Diastolic + MAP)
Baroreceptor reflex further increases HR
71
What is isoproterenol used for?
Cardiac arrest + Heart block
72
What can an overdose of isoproterenol cause?
palpitations + sinus tachycardia + arrhythmia
73
What does dobutamine activate?
beta1
74
What happens with dobutamine administration?
Increase force and rate of heart
| Short duration
75
What are the uses for dobutamine?
Increase CO in shock or CHF
76
What is terbutaline used for?
Oral treatment of bronchospasms
| RAO/heaves in horses
77
What are the side effects of terbutaline?
Tremors + Tachycardia + Headache
78
What is albuterol used for?
Rapid bronchodilation
79
What is clenbuterol used for?
RAO in horses
| Uterine relaxation in cattle
80
What are the affects of NE administration on the cardiovascular system?
Increase BP (PP unchanged)
Decreased BF to kidneys + spleen + liver
HR increases but then decreases
Increased peripheral resistance
81
When is NE used clinically?
Hypotensive crisis
82
What happens if NE + atropine given together?
Vagal reflex blocked = Increased HR
83
What is a really bad side effect of NE adminstration?
Necrosis if gets into area with poor circulation
84
What happens with a low dose of EPI?
B2 mostly stimulated
Vasodilation = Decrease Diastolic
MAP same
85
What happens with high dose of EPI?
Alpha activated as well
Vasocontriction
BP increases
86
What are the four big reasons for epinephrine use?
Vasoconstriction
Anaphylactic shock
Cardiac arrest + complete heart block
Bronchodilation
87
What are the side effects of EPI administration?
Throbbing headache
Palpitations + angina
Restlessness + tremors
88
What is dopamine used for clinically?
Treat cardiogenic shock
| Increase BF + CO w/o vasoconstriction
89
Why does a High dose of Dopamine increase heart rate?
NE is made from this
90
What occurs with amphetamine administration?
NE + DA release
| DA = indirect
91
What symptoms are seen with amphetamine adminstration?
Tremor + Tachycardia + Hypertension
| Agitation + Insomina + increase motor activity
92
What is horner's syndrome?
SNS denervation to one eye
93
What occurs with Horner's syndrome?
Miosis
94
With Horner's syndrome what is the response to a indirect agonist?
No change
95
With Horner's syndrome what is the response to a direct agonist?
Increased response
96
How does Tyramine work, in a general sense?
Indirectly
97
What does tyramine do?
Gets into vesicles and displaces NE
98
What is a major symptom with tyramine?
Tachyphylaxis w/ repeated application
| Severe hypertension
99
When does someone come into contact with tyramine?
Found in food
| Normally broken down by MAO's in GI, unless patient is on MAO inhibitor
