1. methoxamine 2. phenylephrine 3. pseudoephedrine

1. clonidine 2. alpha-methyldopa 3. Methylnorepinephrine

ANS part 2: adrenergic Flashcards by Suraya Dhalla

alpha 1 agonists

methoxamine
phenylephrine
pseudoephedrine

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alpha 2 agonists

clonidine
alpha-methyldopa
Methylnorepinephrine

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beta 1 agonists

dobutamine

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beta 2 agonist

salbutamol

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beta 3 agonist

brl37344

- mirabegron

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the sympathetic NS can have different types of receptors. what are they and what do they innervate?

adrenergic (for adrenal medulla)
noradrenergic (smooth m, heart, glands)
dopamine d1 (renal b.v)
acetalcholine muscarinic (sweat glands, b.v., skeletal muscles)

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adrenergic receptors are what type of receptor

GPCR

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alpha 1 agonist binds to what g protein/activation?

Gq (excitation)

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beta 1 and beta 2 agonist binds to what g protein/activation?

Gs (excitation)

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alpha 2 binds to what g protein/activation?

Gi (inhibition)

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alpha receptors have a high affinity for

E > NE&raquo_space; isoproterenol

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Non-specific antagonist for alpha receptors

phentolamine

Phenoxybenzamine

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alpha 1 and 2 receptors are found

on blood vessels

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binding to alpha 1 causes

vasoconstriction (and BP increases)

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binding to alpha 2 causes

vasodilation

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binding to alpha 1 causes excitation or inhibition of Gq?

excitation

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alpha 1 receptors are found pre or post synaptic?

POST

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Ag of alpha 1

methoxamine
phenylephrine
Pseudoephidrine

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Antag of alpha 1 and action

prazosin, vasodilation

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binding to alpha 2 causes excitation or inhibition?

inhibition of Gi

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where is alpha 2 receptor found (pre or post synaptic)

PRE AND POST

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Ag alpha 2 receptor and action

clonidine

Alpha methyldopa methylnorpinephrine, vasodilation

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Antag of alpha 2 receptor and action

yohimbine, vasocontriction

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affinity of beta receptors to agonists

isoproterenol&raquo_space; E > NE

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antagonist of beta receptors

propranolol

location of beta 1

heart

location of beta 2

respiratory system

location of beta 3

adipose tissue

antag beta 1

atenolol

effect of dobutamine

- increase HR | - increase chronotropy

effect of salbutamol

-bronchoDILATION

what is salbutamol used to treat

- asthma | - COPD

what does brl3744 do

- increase body temp | - decrease fat

what does atenolol do

- decrease HR | - decrease BP

what 2 agonists bind to both alpha and beta

-NE and E

NE has an affinity for which beta receptor

beta 1 (heart)

E has an affinity for which beta receptor

beta 1 and 2 (heart and resp. - use to treat asthma attack)

dopamine has a high affinity for which receptor

D1 and D2 (dopamine receptors)

isoproterenol has a high affinity for which receptor

beta 1 and 2

fenoldopam has a high affinity for which receptor

what are the 5 endogenous adrenergic agonists

catecholamines: 1. dopamine 2. NE/E 3. NA/A

agonist for beta 2

- albuterol - terbutaline - metaproternol - ritodrine

all CA's are synthesized from

tyrosine

order of CA molecules that are synthesized

tyrosine -> dopa -> dopamine -> norepi -> epi

dopamine is metabolised by what enzyme to form what

dopamine -> DOPAC (via MAO: monoamine oxidase)

DOPAC is metabolized by what enzyme to form what

COMT to form HVA

where is MAO found

mitochondrial surface

where is COMT found

cytoplasm

NA and A are metabolised by COMT and MAO to form what

VMA

Epi binding to alpha1 causes

vasoconstriction, increase BP, and reflex bradycardia

Epi binding to beta 1 causes

increase BP, inotropic and chronotropic

Epi binding to beta 2 causes

- bronchodilation | - coronary vasodilation (more blood to heart to help with increased BP)

what are the systemic therapeutic indications for Epi

1. cardiac arrest 2. hypotension/shock 3. bronchospasm 4. hypersensitivity reactions/anaphylactic shock

what are the topical therapeutic indications for Epi

1. prolongued action of local anesthetics | 2. topical hemostatic

is NE a potent agonist for alpha and beta?

only alpha and beta 1 | *weak beta 2 agonist

effect of NE

- B1: increase BP - inotropic and chronotropic - A1: vasoconstriction - mydriasis

what is NE used to treat

shock (with severe hypotension)

low doses of dopamine will cause

renal and splanchnic vasodilation

high doses of dopamine will cause

- vasodilation | - increased renal blood flow, diuresis, and natriuresis

why does dopamine have limited CNS access

- high polarity | - peripheral metabolism

what is dopamine used to treat

- severe hypertension | - shock (cardiogenic, renal failure)

methoxamine administered intravenously has ___(faster/slower) effects and activity compared to intramuscularly

faster and higher

what is methoxamine used to treat

- hypotensive states - maintain BP during surgery - paroxysmal atrial tachycardia

what effect does phenylephrine have

- lower HR | - increase stroke output

what is phenylephrine used to treat

-hypotensive state

what is pseudoephedrine used to treat

nasal decongestion

what is clonidine used to treat

hypertension

what are 3 adverse effects of clonidine

1. dry mouth 2. sedation 3. bradycardia

what is alpha-methyldopa used to treat

hypertension

how does alpha-methyldopa work

inhibits DOPA decarboxylase, so prevents the formation of CA's

what is dobutamine used to treat

congestive heart failure

what is salbutamol used to treat

- asthma - chronic bronchitis - pulmonary emphysema

what is mirabegron used to treat

overactive bladder

mechanism of action for amphetamine

- increase release of NE/DA - inhibit MAO - alpha agonist

CNS stimulation effects of amphetamine (D-amph)

- sleep and fatigue reversal - stim medullary respiratory center - suppress appetite - psychosis - potential for abuse and addiction

PNS stimulation effects of amphetamine (L-amph)

- increase cardiovascular | - GI (dry mouth, metallic taste, nausea, vomiting, diarrhea)

name 4 indirect adrenergic agonists

1. amphetamine 2. methylphenidate 3. moclobemide 4. phenelzine

methylphenidate is a mild CNS stimulator. what is it used to treat

- ADHD | - narcolepsy

MAO inhibitors work by

inhibiting MAO, so increase monoamines in CNS

what are MAO inhibitors used to treat

depression

name 2 indirect acting adrenergic antagonists and what they do

1. alpha-methyldopa (inhibits DOPA-decarboxylase) | 2. reserpine (inhibit vesicular transport)

give 2 examples of MAO inhibitors

- moclobemid (reversible) | - phenelzine (irreversible)