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?

A

Tyramine

25
Q

Does tyramine have a central or peripheral effect?

A

peripheral

26
Q

What does it mean if a drug has a peripheral effect? Central effect?

A

peripheral: does not cross BBB
central: crosses BBB

27
Q

What is Tyramine’s mechanism of action as a sympathomimetic?

A

induce catecholamine release

28
Q

What is Cocaine’s mechanism of action as a sympathomimetic?

A

inhibit NA and DA reuptake

29
Q

TRUE or FASLE: of the indirectly acting sympathomimetics, Tyramine is also a local anaesthetic.

A

FALSE –> COCAINE is a local anasethetic

30
Q

Does cocaine mainly exhibit a peripheral or central effect?

A

mainly central effect

31
Q

Elevation of which catecholamine causes euphoria?

A

dopamine

32
Q

What are the therapeutic uses of -caines?

A
  • local anesthetic for ear, nose, throat surgery
  • hemostatic (limits its own absorption into systemic circulation and prevents bleeding)
33
Q

Name 3 amphetamines.

A
  • methylphenidate (Ritalin)
  • adderall (mix of amphetamine and dextroamphetamine)
  • “ecstasy” (MDMA)
34
Q

Do CNS or PNS effects dominate when using amphetamines?

A

CNS effects

35
Q

What are the CNS effects of amphetamines?

A

mild alerting, improved attention, elevation of mood, insomnia, euphoria, anorexia

36
Q

What are the CNS effects of cocaine?

A

alerting, elevation of mood, insomnia, euphoria

37
Q

What is the danger of using Tyramine?

A

severe hypertension and cardiac dysrhythmias

38
Q

What could be a reason for why amphetamines are no longer used as diet pills?

A

they can cause anorexia

39
Q

What are some therapeutic uses of amphetamines?

A
  • treat attention-deficit hyperkinetic syndrome
  • treat narcolepsy
40
Q

What are amphetamines’ mechanism of action?

A

increase NA and DA release from terminal via REVERSE UPTAKE SYSTEM (i.e. reversely pumped out of the uptake transporter)

41
Q

Does amphetamines’ mechanism of action occur during ongoing nerve activity or in the absence of ongoing nerve activity?

A

absence of ongoing nerve activity

42
Q

Name 4 receptor-selective sympathomimetics.

A
  • isoproterenol (isoprenaline, INA)
  • dobutamine
  • salbutamol
  • phenylephrine