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CP-1 > Pharmacology DSA > Flashcards

Pharmacology DSA Flashcards

1
Q

What does VMAT-2 do?

A

transports NE, epi, DA, and serotonin into vesicles –> release upon AP and Ca2+ influx

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2
Q

What does reserpine do?

A

blocks VMAT-2 so NE, Epi, DA, and serotonin are not put into vesicles

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3
Q

What does hemicholinium do?

A

blocks choline’s transport into a cell for synthesis

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4
Q

What parts of epinephrine synthesis occur in the nerve cytoplasm?

A

Tyrosine –> dopa –> dopamine

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5
Q

What parts of epinephrine synthesis occur in the vesicle?

What part is mainly in the adrenal medulla?

A

Dopamine –> norepinephrine –> epinephrine

norepi –> epi is in adrenal medulla

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6
Q

What is the effect of alpha2 receptor stimulation?

A

decreased insulin secretion
aggregation
decreased release of NE
vascular SM contraction

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7
Q

What is the effect of beta2 receptor stimulation?

A

smooth muscle relaxation

glycogenolysis, uptake of K+

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8
Q

What transports tyrosine into a nerve terminal?

A

Na+ - dependent tyrosine transporter

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9
Q

Where are M1 receptors located and what is their effect?

A

CNS, ganglia

Gq = activation of PLC, IP3, DAG cascade

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10
Q

Where are beta3 receptors found?

what is their effect?

A

adipose tissue

lypolysis

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11
Q

What does dopamine act on?

A

CNS and renal vascular smooth muscle

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12
Q

What are the 2 major enzymes that metabolize catecholamines?

what is their final product that can exit the cell?

A

monoamine oxidase (MAO) and COMT

final product = VMA

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13
Q

What does NET do?

A

imports NE into nerve terminal (reuptake)

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14
Q

How does beta1 respond to epi and NE preferentially?

Where is it located?

A

epi = NE
juxtaglomerular cells
heart

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15
Q

Where are nAChRs located?

A

CNS
autonomic ganglia
adrenal medulla

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16
Q

What would low blood pressure do to a baroreceptor?

A

decrease baroreceptor stim –> decrease parasympathetic and increase sympathetic

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17
Q

How does beta2 respond to epi and NE preferentially?

Where is it located?

A

epi&raquo_space;Ne
smooth muscle (vascular, bronchial, GI, GU)
skeletal muscle

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18
Q

What NT is used for sweat gland stimulation?

A

ACh

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19
Q

What type of gpcr is beta1?

A

Gs –> increases adenylyl cyclase, cAMP, L-type Ca2+ channel openings

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20
Q

Where are M4 receptors located and what is their effect?

A

CNS

Gi = inhibit AC, decrease cAMP, activate K+ channels

21
Q

What are the main parts of the body with parasympathetic innervation?

A

cardiac and smooth muscle
gland cells
nerve terminals

22
Q

Where are muscarinic AChRs located?

A

CNS
autonomic ganglia
effector organs
sweat glands

23
Q

What is the major mechanism of terminating actions of catecholamines?

A

reuptake into nerve terminals

24
Q

What is acetylcholine mainly used in?

A

all preganglionic autonomic fibers
all pre and post ganglionic parasympathetic fibers
few postganglionic sympathetic (sweat glands)

25
Q

Where are M2 receptors located and what is their effect?

A

heart, nerves, smooth muscle

Gi = inhibit AC, decrease cAMP production, activate K+ channels

26
Q

How does alpha1 respond to epi and NE preferentially?

Where is alpha1 located?

A 
epi greater than or equal to NE
in vascular, GU SM
liver
intestinal smooth muscle
heart
27
Q

What is norepinephrine used in?

A

postganglionic sympathetic fibers

28
Q

What is the effect of alpha1 receptor stimulation?

A

contraction
glycogenolysis, gluconeogenesis
hyperpolarization and relaxation
increased contractile force, arrhythmias

29
Q

How is the adrenal gland stimulated to release epi and NE?

A

sympathetic ACh –> NAChrs –> 80% epi and 20% NE

30
Q

What is the effect of Beta1 receptor stimulation?

A

increased renin secretion

increased force and rate of contraction and AV nodal conduction velocity

31
Q

What are sympathomimetic agents?

A

drugs that mimic or enhance alpha and beta receptor stimulation

32
Q

What type of gpcr is alpha1?

A

Gq

33
Q

What type of gpcr is beta2?

A

Gs –> increases adenylyl cyclase

34
Q

Where are M3 receptors located and what is their effect?

A

glands, smooth muscle, endothelium

Gq = activation of PLC, IP3, DAG cascade

35
Q

How does alpha2 respond to epi and NE preferentially?

where is it located?

A 
epi >/= NE
pancreatic islets
platelets
nerve terminals
vascular smooth muscle
36
Q

What would high blood pressure do to a baroreceptor?

A

increase baroreceptor stimulation –> increase parasympathetic NS and decrease sympathetic

37
Q

What is the sequence of events of epinephrine synthesis?

A

Tyrosine –> dopa –> dopamine –> norepinephrine –> epinephrine

38
Q

Where does epinephrine synthesis occur?

A

adrenal medulla

in a few epinephrine-containing pathways in the brain

39
Q

What are the main parts of the body with sympathetic innervation?

A

sweat glands
cardiac and smooth muscle, certain gland cells
renal vascular smooth muscle

40
Q

Which muscarinic receptors are Gi?

A

M2, M4

41
Q

Which muscarinic receptors are Gq?

A

M1, M3, M5

42
Q

What is the function of nAChRs?

A

excitatory

release of catecholamines (in sympathetic ns?)

43
Q

What is the function of muscarinic AChRs?

A

excitatory and inhibitory

sweat secretion

44
Q

What type of gpcr is alpha2?

A

Gi

45
Q

What does cocaine do?

A

inhibits NET so there is more NE hanging out in the synapse

46
Q

What does DAT do?

A

reuptakes DA into nerve terminal

47
Q

How does the parasympathetic NS achieve vasodilation?

A

no innervation of SM

ACh –> mAChRs on endothelial cells –> NO released –> vasodilation

48
Q

Where are M5 receptors located and what is their effect?

A

CNS

Gq = activate PLC cascade, etc

49
Q

What type of gpcr is the beta3 receptor?

How does it preferentially respond to epi and NE?

A

Gs

NE > Epi

CP-1 (32 decks)

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