Autonomic Pharmacology 4 Flashcards

1
Q

In blood vessels, are alpha or beta adrenoreceptors associated with Gi?

A

alpha = Gi

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2
Q

In blood vessels, are alpha or beta adrenoreceptors associated with Gs?

A

beta = Gs

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3
Q

What is the effect of alpha2 receptor stimulation in blood vessels?

A

vasodilation –> decrease peripheral resistance –> reduce BP

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4
Q

Which adrenoreceptor(s) is/are associated with skin and spleen blood vessels and capacitance vessels? Does binding at this/these receptor(s) cause constriction or dilation?

A

skin and spleen blood vessels and capacitance vessels are associated with ALPHA1

alpha1 –> constriction

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5
Q

Which adrenoreceptor(s) is/are associated with muscle blood vessels? Does binding at this/these receptors cause constriction or dilation?

A

muscle blood vessels are associated with ALPHA1 and BETA2

alpha1 –> constriction
beta2 –> dilation

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6
Q

What effect does presynaptic alpha2 stimulation/binding have on NA release in blood vessels?

What effect does presynaptic beta receptor stimulation/binding have on NA release in blood vessels?

A

presynaptic alpha2 –> decrease NA

presynaptic beta –> increase NA

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7
Q

What is the main adrenoceptor found in the heart?

A

beta1 is the main adrenoreceptor in the heart

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8
Q

What is the effect of adrenoreceptor binding/stimulation in the heart?

A

increased Ca2+ influx –> increased force and rate of contraction –>. increased conduction of A-V node (palpitations)

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9
Q

Why do beta agonists pose a cardiac risk?

A

since beta adrenoreceptor binding stimulates the heart (e.g. palpitations), beta agonists can cause SEVERE CARDIA DYSRHYTHMIAS

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10
Q

Which adrenoreceptor(s) stimulate the radial pupil dilator muscle of the iris? What is the effect of stimulation?

A
  • alpha receptors
  • stimulation causes mydriasis/dilation
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11
Q

Which adrenoreceptor is found on bronchiole smooth muscle? What is the effect of stimulating this adrenoreceptor?

A
  • beta2
  • relax bronchiole smooth muscle
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12
Q

What adrenoreceptor is found in nasal blood vessels? What is the effect of stimulating this receptor? Would it be easier or harder to breathe if the receptor is stimulated? Why?

A
  • alpha receptor
  • stimulation causes vasoconstriction
  • stimulation makes it easier to breathe because vasoconstriction decreases blood flow, which decreases inflammation and opens up the nose
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13
Q

What is the effect of alpha agonists in the GI tract? What is the effect of beta agonists in the GI tract?

A

alpha and beta both cause relaxation in the GI tract

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14
Q

How do alpha2 agonists affect the GI tract?

A

indirect relaxation of GI tract via decreased release of ACh

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15
Q

Do alpha agonists promote or inhibit micturition? What is the mechanism?

A

inhibit micturition by constricting the bladder

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16
Q

What is the effect of an alpha2 agonist on insulin and renin release? what about a beta2 agonist?

A

alpha agonist –> inhibit insulin and renin release
beta agonist –> stimulate insulin and renin release

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17
Q

What is the effect of beta3 stimulation in fat cells?

A

promote lipolysis

18
Q

What is the effect of beta stimulation in liver?

A

promote glycogenolysis

19
Q

Name a non-selective sympathomimetic. (hint: it’s a catecholamine)

A

adrenaline (epinephrine)

20
Q

What is the effect of adrenaline binding to alpha receptors in skeletal muscle blood vessels?

A

vasoconstriction

21
Q

What is the effect of adrenaline binding to beta2 receptors in skeletal muscle blood vessels?

A

vasodilation

22
Q

What is the therapeutic effects of adrenaline as a vasoconstrictor?

A

-vasoconstrictor mixed with anaesthetics prolongs nerve block duration

-vasoconstriction prevents loss of anaesthetics into systemic circulation

-treat anaphylaxis

23
Q

Name 4 indirectly acting sympathomimetics.

A

Tyramine, Cocaine, Amphetamines, Tricyclic Antidepressants

24
Q

Which sympathomimetic exhibits the cheese effect?

25
Does tyramine have a central or peripheral effect?
peripheral
26
What does it mean if a drug has a peripheral effect? Central effect?
peripheral: does not cross BBB central: crosses BBB
27
What is Tyramine's mechanism of action as a sympathomimetic?
induce catecholamine release
28
What is Cocaine's mechanism of action as a sympathomimetic?
inhibit NA and DA reuptake
29
TRUE or FASLE: of the indirectly acting sympathomimetics, Tyramine is also a local anaesthetic.
FALSE --> COCAINE is a local anasethetic
30
Does cocaine mainly exhibit a peripheral or central effect?
mainly central effect
31
Elevation of which catecholamine causes euphoria?
dopamine
32
What are the therapeutic uses of -caines?
- local anesthetic for ear, nose, throat surgery - hemostatic (limits its own absorption into systemic circulation and prevents bleeding)
33
Name 3 amphetamines.
- methylphenidate (Ritalin) - adderall (mix of amphetamine and dextroamphetamine) - "ecstasy" (MDMA)
34
Do CNS or PNS effects dominate when using amphetamines?
CNS effects
35
What are the CNS effects of amphetamines?
mild alerting, improved attention, elevation of mood, insomnia, euphoria, anorexia
36
What are the CNS effects of cocaine?
alerting, elevation of mood, insomnia, euphoria
37
What is the danger of using Tyramine?
severe hypertension and cardiac dysrhythmias
38
What could be a reason for why amphetamines are no longer used as diet pills?
they can cause anorexia
39
What are some therapeutic uses of amphetamines?
- treat attention-deficit hyperkinetic syndrome - treat narcolepsy
40
What are amphetamines' mechanism of action?
increase NA and DA release from terminal via REVERSE UPTAKE SYSTEM (i.e. reversely pumped out of the uptake transporter)
41
Does amphetamines' mechanism of action occur during ongoing nerve activity or in the absence of ongoing nerve activity?
absence of ongoing nerve activity
42
Name 4 receptor-selective sympathomimetics.
- isoproterenol (isoprenaline, INA) - dobutamine - salbutamol - phenylephrine