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pharmacology > lecture 6 > Flashcards

lecture 6 Flashcards

1
Q

Autonomic Nervous System

A

involuntary: sympathetic/thoracolumbar outflow and parasympathetic/craniosacral outflow

two neuron pathway?

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2
Q

acetylcholine works on ________ receptors while norepinephrine mainly on ______

A

nicotinic; adrenergic

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3
Q

sympathetic releases _______. para releases _______

A

norepinephrine; acetylcholine

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4
Q

muscarinic receptors in the heart

A

M2 - coupled to G alpha i (inhibits adenylyl cyclase and decreases cAMP)

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5
Q

muscarinic receptors in the lungs

A

M3 - coupled to Gq (activates phospholipase C - calcium release thus contraction)

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6
Q

muscarinic stimulation of the parasympathetic nervous system in the lungs promotes _________

A

bronchoconstriction

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7
Q

muscarinic receptors (M1-M5) and what they do

A

GPCRs, M1, M3, and M5 all activate PLC (contraction of smooth muscle), M2 (ACh) is in the heart and slows conduction, decreasing contraction force of the heart

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8
Q

four adrenergic receptors

A

alpha1 (blood vessels), beta 1 (in heart), beta 2(in lungs, one in each), alpha 2 are presynaptic

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9
Q

cocaine and ecstasy will increase levels of norepinephrine how?

A

blocking the transporters, so it builds up in the vesicle

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10
Q

amphetamine-adderall for ADHD, or methyphenidate (ritalin) mechanism

A

tyramine displaces NE.

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11
Q

monoamine oxidase (MOAs) break down ________ and examples

A

tyramine, NE and dopamine
MAO A - phenelzine
MAO B - selegiline for parkinson’s

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12
Q

too much tyramine can cause

(wine and cheese effect)

A

hypertension

if you dont have enough MAOs to break it down you can die

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13
Q

actions of cocaine and amphetamines

A

c- blocks the DA (dopa) transporter, so DA that has been released stays out a lot longer

amph- reverses the DA transporter, so more DA is released and stays out longer, also blocks degradation of DA

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14
Q

amphetamines mechanism of action

A

normal dopaminergic synapse. amphetamine enters via DAT as a substrate. enters vesicles via VMAT1 to displace DA and inhibits MAO. DA concentration rises in the cytosol. DA is expelled into synapse via reverse transport.

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15
Q

“pleasure center” is the ____ in the brain

A

VTA (ventral tegmental area)

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16
Q

reward and mesolimbic dopamine

A

activation of reward pathway leads to increased dopamine in Nucleus Accumbens

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17
Q

DA usually released in a ______ way, and acts on __ receptors. Increasing activity (something important or a drug like coke), would release DA in a _____ way, and activates __ receptors.

A

tonic, D2; phasic, D1

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18
Q

all autonomic receptors are coupled to _____________

A

GTP binding proteins

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19
Q

alpha 1 (G-alpha-q)

A

smooth muscle contraction. activate phospholipase C –> intracellular calcium

cocaine eyes

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20
Q

alpha 2

A

brain.
inhibit adenylyl cyclase

21
Q

beta 1 (NE) (G alpha s)

A

increase heart rate, conduction velocity, and contractility.
SA, AV node and HIS-purkinje cells.
stimulate adenylyl cyclase

also found in the kidney for renin.

22
Q

beta 2 (G alpha s)

A

lung relaxation.
stimulate adenylyl cyclase.
cAMP –> PKA –> inactivates MLCK and decreases affinity for calcium/CaM

23
Q

alpha 1 receptors could increase blood pressure. why?

A

they release calcium, causing contraction and thus constriction of blood vessels

24
Q

presynaptic alpha2 receptors decrease release of ________

A

norepinephrine, bc the beta gamma subunit binds to the calcium channel inhibiting it

25
Q

clonidine

A

produces bradycardia and hypotension to decrease BP

26
Q

miosis (para)

A

pupillary constricion

27
Q

mydriasis (sympathetic)

A

pupil dilation

28
Q

sympathomimetics and examples

A

imitate the effects of the sympathetic nervous system, activating alpha or beta receptors or both

(alpha-1) decongestants like phenylephrine (Sudafed) induce vasoconstriction of blood vessels in the nose

(alpha-1) local anesthetics contain epinephrine to increase duration by causing vasoconstriction at site of injection

(beta-2) bronchospasm and cardiac arrest- epinephrine

(beta 2 and alpha 1) anaphylaxis - epinephrine relaxes bronchioles, increases BP

cardiovascular collapse (alpha 1 and beta 1) - norepinephrine

29
Q

anti asthmatic drugs include (broad)

A

bronchodilators, anti-inflammatory agents, leukotriene modifiers

e.g. Spiriva

30
Q

lipocortin-1

A
31
Q

LTC4, LTD4, LTE4 constitute

A

slow reaching substance of anaphylaxis

32
Q

leukotrine antagonist drugs

A
33
Q

corticosteroids

A

help decrease inflammation by decreasing transcription of cytokines and increase lipocortin which inhibits PLA2 and thus the downstream production of inflammatory stuff

34
Q

adrenergic agonists for asthma

A

albuterol! beta 2 receptors
bronchodilator
long acting salmeterol

35
Q

advair

A

fluticasone and salmeterol
steroid + b2 agonist
longer acting

36
Q

atrovent

A

ipatropium bromide
inhibit muscarnic receptors
anti-cholinergic

37
Q

beta blockers

A

block beta-1 receptors to decrease the rate at which the heart works

antihypertensive
ischemic heart disease (chronic angina, reduces cardiac workload)
arrythmias (vfib)

e.g. metoprolol, atenolol

38
Q

beta blocker side effects

A

bad dreams, cold exremities, decreased exercise tolerance, fatigue depression and impotence, heart failure

39
Q

alpha sympatholytics (alpha blockers)

A

bind to alpha receptors to block the effects of endogenous agonists

e.g. prazosin (minipress) for hypertension

40
Q

targets of drugs with muscarinic action

A

exocrine glands, smooth muscles, cardiac tissue

41
Q

cholinomimetics

A

mimic ACh receptor agonists

direct acting: choline esters, alkaloids-plants; complex structure
e.g. bethanechol (choline esters), pilocarpine (alkaloid)

indirect acting: cholinesterase inhibitors, carbamates, phosphates

42
Q

natural alkaloids

A

muscarine:
poision in some mushrooms that causes hypotension, sweating, emesis, bradycardia, miosis, etc.

pilocarpine (salagen):
pure mucarinic agent in low doses used for dryness of mouth and constriction of pupils
for glaucoma

43
Q

clinical use of direct acting muscarinic agonists

A

glaucoma and gastric atony/urinary retention

44
Q

indirect acting parasympathomimetics (acetylcholinesterase inhibitors)

A
45
Q

toxic reactions

A
46
Q

treatment of toxicity

A
47
Q

anticholinergics/parasympatholytics

A

atropine

48
Q

atropine actions

A

depresses salivation and bronchial secretions, bronchodilation, relax GI,

49
Q

neuromuscular blocking drugs

A

non-depol: tubocurarine blocks NMJ
depol: succinylcholine
activate nicotinic acetylcholine receptors
for muscle relaxtion

pharmacology (10 decks)

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