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Pharmacology -- Test #3 > Introduction Into Autonomic Pharmacology > Flashcards

Introduction Into Autonomic Pharmacology Flashcards

1
Q

Compounds associated with the parasympathetic system?

A

Acetylcholine
Muscarine
Nicotine

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2
Q

Compounds associated with the sympathetic system?

A

Norepinephrine/Noradrenaline

Epinephrine (Adrenaline)

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3
Q

Cholinergic drugs influence….

Adrenergic drugs influence…

A

Parasympathetic

Sympathetic

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4
Q

The receptors of the PANS are named after exogenous agents. What are they

A

Muscarine and Nicotine

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5
Q

Sympathetic preganglionic fibers leave the CNS through which spinal nerves?

A

Thoracic and Lumbar

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6
Q

Parasympathetic preganglionic fibers leave the CNS through which spinal nerves?

A

Cranial Nerves

Sacral

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7
Q

All preganglionic nerves release _____ into post ganglioncic nerves expressing ____ receptors

A

Acetylcholine

Nicotinic Cholinergic Receptors

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8
Q

Somatic motor neurons release _____ directly onto _______ receptors

A

Acetylcholine

Nicotinic cholinergic receptors

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9
Q

Parasympathetic postganglionic nerves release _____ onto organs with _____ receptors

A

Acetylcholine

Muscarinic

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10
Q

Sympathetic postgangionic nerves primarily release _____ that can bind to _____ receptors

A

Norepinephrine

Adrenergic

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11
Q

Sympathetic postganglionic nerves acting on skin release ____ onto _____ receptors

A

Acetylcholine

Muscarinic Receptors of Thermoregulatory Sweat Glands

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12
Q

Sympathetic postganglionic nerves acting on the kidneys release ____ to bind ______ receptors

A

Dopamine

Dopamine D1 to cause vasodilation

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13
Q

Postganglionic sympathetics acting on the adrenals cause….

A

Epi and a little bit of NE release into the bloodstream

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14
Q

Which muscarinic receptors are found postsynaptically?

Presynaptically?

A

Post – 1, 3, 4, 5

Pre – 2, 4

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15
Q

Why have muscarinic receptors presynaptically?

A

Inhibitory autoreceptors

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16
Q

ACh in the synapse is quickly metabolized by ______ and ______

A

Acetylcholinesterase

Butylcholineesterase

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17
Q

ACh metabolism generates…

A

Acetate and Choline

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18
Q

What does ChAT do?

A

Choline AcetylTransferase transfers an acetyl to choline from AcCoA to remake ACh.

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19
Q

ACh is taken back into synaptic vesicles by…

A

Acetylcholine transporter (vAchT)

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20
Q

Sympathetic receptors found post synaptically?

Pre synaptically?

A

Post – alpha1, beta1, beta2

Pre – alpha2, beta2

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21
Q

How is NE made?

A

Tyrosine turned to DOPA by tyrosine hydroxylase
DOPA to Dopamine by Aromatic Acid Decarboxylase
Dopamine to NE by dopamine beta-hydroxylase

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22
Q

After release, NE is returned by ____

A

NET (NorEpinephrine Transporter)

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23
Q

What two fates may occur for NE after its reuptake?

A

MAOs could turn it into dihydroxyphenylglycol

Taken into vesicles by VMAT (vesicular monamine transporter)

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24
Q

Postsynaptically, NE is metabolized by ______ into ______

A

COMT (catechl-0-methyltransferase

Normetanephrine

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25
Q

How do Methylphenidate (Ritalin) and amphetamines (adderall) increase NE/DA release?

A

Blocking VMAT

Indirect activation of SANS

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26
Q

Classification of drugs that mimic acetylcholine? Block acetylcholine?

A

Parasympathomimetic

Parasympatholytic

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27
Q

Classification of drugs that mimic NE? Block NE?

A

Sympathetomimetic

Sympatholytic

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28
Q

Three sites you might look for Nicotinic Cholinergic receptors?

A

Ganglionic
Skeletal Muscle
Neronal

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29
Q

Nicotinic cholinergic receptors consist of ___ subunits

A

5

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30
Q

Nicotinic cholinergic receptors – why should be care about their subunits?

A

The arrangement decides on function and affinity

ex. the pentameric alpha7 homomeric Ach receptor can bind 5 ACh molecules

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31
Q

Gq coupled Muscarinic receptors include…

A

M1, M3, M5

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32
Q

Gi coupled Muscarinic receptors include…

A

M2, M4

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33
Q

In PANS, the most important presynaptic muscarinic receptor is _____ and the most important postsynaptic receptors is _____.

34
Q

M2 is primarily located where?

A

Heart and Bladder

Also, Certain brain regions

35
Q

Which muscarinic receptors are usually found in the brain?

A

M1, M4, M5

36
Q

Function of M5 receptors?

A

Vasodilation of cerebral blood vessels

37
Q

Describe the structure of muscarinic receptors?

A

GPCRS

7 transmembrane

38
Q

Effects of M3 activation?

A

Increases in calcium

Neuronal activation through a PLC mechanism

39
Q

Effects of M2 activation?

A

Inhibit NT release by activating GIRK and inhibiting VGCC via AC inhibition

40
Q

Adrenergic receptors are invited into ____ subtypes with three isoforms each

A

alpha1, alpha2, and beta

41
Q

G couplings for alpha1, alpha2, and beta subtypes

A

Alpha1 – Gq-coupled
Alpha2 – Gi-coupled
beta – Gs-coupled

42
Q

Which adrenergic receptors are primarily responsible for SANS responses?

A

alpha1 and beta

43
Q

Where are alpha2 receptors at?

A

Mostly CNS

also GI tract and pancreas

44
Q

The radial muscles of the iris contain ____ receptors

A

alpha1

aka. THE DILATOR

45
Q

The circular muscles of the iris contain _____ receptors

A

M3

Cause consriction, Miosis

46
Q

The ciliary muscles contain ___ receptors

47
Q

Why should we care about the M3R on ciliary muscles?

A

Contraction changes accommodation

Stretches trabecular meshwork, may reduce open angle glaucoma

48
Q

Beta receptors are also present on the ciliary endothelium. Why?

A

They increase the secretion of aqueous humor

Blockage for glaucoma treatment

49
Q

Blood Pressure is driven by what two factors

A

Flow (Q)

Resistance (R)

50
Q

Flow is driven by what two factors

A 
Stroke Volume (SV)
Heart Rate (HR)
51
Q

How can the autonomic nervous system control Bloodpressure?

A

Control R with Vasodilation/Vasoconstriction
Control SV by changing force of contraction
Control HR by changing frequency

52
Q

ANS triggered vasoconstriction uses ____ receptors in vascular smooth muscles

53
Q

Activation of Beta2 receptors in vessels cause…

A

Relaxation of the smooth muscle

Vasodilation

54
Q

What vessels are exposed to both alpha and beta stimulation, who wins?

55
Q

How are alpha1 and alpha2 receptors in vessel walls activated? What do they do?

A

Activated by Ep in the blood stream

Cause vasoconstriction

56
Q

What is the significance of non-innervated M3 receptors in the endothelial lining?

A

They respond to exogenous cholinergic drugs

57
Q

Activation of endothelial M3s causes….

A

Release of NO
Vasodilation by relaxation of the vascular smooth muscle
Trumps the vasoconstriction response of smooth muscle M3

58
Q

ANS responses in the heart are primarily mediated by ____ and ____

A

M2 and beta1

59
Q

The beta receptors in the heart cause…

A

Increase in HR and force of contraction

60
Q

M2 receptors in the heart cause…

A

Slowed HR and decreased force of contraction

61
Q

parasympathetic receptors in the lung are mostly ______. They are located on ______.

A

M3

Smooth muscle cells and mucosal glands

62
Q

Activation of M3 in the lungs causes…

A

Bronchoconstriction

Release of Mucous

63
Q

Sympathetic receptors in the lungs are primarily…. and located on…..

A

beta2

Smooth muscle cells

64
Q

Activation of beta2 in the lungs causes

A

Muscle relaxation and Bronchodilation

65
Q

Apocrine sweat glands (stress induced), Piloerection, and erector muscles use….

A

alpha 1 receptors

66
Q

Where are apocrine sweat glands usually found

A

Armpits, Genatalia, Palms

67
Q

What receptors are responsible for eccrine (thermoregulatory) sweating?

68
Q

Parasympathetic and Sympathetic receptor and response.

Salivary Glands.

A

Both increase secretion – alpha1, M3

69
Q

Parasympathetic and Sympathetic receptor and response.

Smooth Muscle Sphincters.

A 
S = Contraction (alpha1)
P = Relaxation (M2)
70
Q

Parasympathetic and Sympathetic receptor and response.

Smooth muscle walls

A 
S = Relaxation (alpha2, beta2)
P = Contraction (M3)
71
Q

Parasympathetic and Sympathetic receptor and response.

GI secretions.

A 
S = Inhibition (alpha2)
P = Increased (M1,M3)
72
Q

Parasympathetic and Sympathetic receptor and response. Bladder Wall.

A 
S = Relaxation (beta3)
P = Contraction (M3)
73
Q

Sympathetic receptor and response. Ureter and sphincter.

A

Contraction (alpha1)

74
Q

Sympathetic receptor and response. Uterus.

A

Relaxation (beta2)

Contraction (alpha1)

75
Q

Sympathetic receptor and response. Penis

A

Ejaculation (alpha1)

76
Q

Sympathetic receptor and response. Liver.

A

Gluconeogenesis, Glycogenolysis (alpha1, beta2)

77
Q

Sympathetic receptor and response. Fat cells.

A

Lipolysis (alpha1, beta1-3)

78
Q

Sympathetic receptor and response. Kidney.

A

Increased renin secretion (beta1)

79
Q

Sympathetic receptor and response. Pancreas.

A

Decreased Insulin release (alpha2)

80
Q

Activation of M3 receptor on the bladder causes…

A

Contraction of the bladder wall

urge to urinate

81
Q

Beta3 activition on the detrusor wall causes…

A

relaxation

82
Q

Activation of alpha1 on the urethra causes…

A

contraction

Pharmacology -- Test #3 (13 decks)

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