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Pharmacology > Adrenergic 1 > Flashcards

Adrenergic 1 Flashcards

1
Q

MIXED-ACTING ADRENERGIC AGONISTS?

A

EPHEDRINE
PSEUDOEPHEDRINE
• Induce release of norepinephrine
• Activate adrenergic receptors.

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2
Q

Ephedrine structure, pk, and uses

A

• Not a catecholamine: poor substrate for COMT
and MAO. Long duration of action.
• Excellent absorption orally and penetrates the
CNS.

EPHEDRINE: USES
• Used as a pressor agent, particularly during
spinal anesthesia.
• Used in myasthenia gravis.

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3
Q

PSEUDOEPHEDRINE uses?

A

• One of four ephedrine enantiomers.
• Available over the counter as a component of
many decongestant mixtures.

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4
Q

UPTAKE INHIBITORS?

A

COCAINE
ATOMOXETINE
MODAFINIL

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5
Q

MODAFINIL use?

A 
• Psychostimulant.
• MOA not fully known.
• Inhibits norepinephrine and dopamine
transporters.
• Increases synaptic concentrations of
norepinephrine, dopamine, serotonin and
glutamate, and decreases GABA levels.
• Used for the treatment of narcolepsy.
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6
Q

ATOMOXETINE use?

A

• Selective inhibitor of the norepinephrine
reuptake transporter.
• Indicated for the treatment of ADHD.

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7
Q

Cocaine use?

A

• Blocks monoamine reuptake.
• Monoamines accumulate in synaptic space.
• This results in potentiation and prolongation of
their central and peripheral actions.

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8
Q

RELEASING AGENTS?

A

AMPHETAMINE
METHYLPHENYDATE
TYRAMINE
• Cause norepinephrine release from presynaptic
terminals.
• Potentiate effects of norepinephrine produced
endogenously.

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9
Q

AMPHETAMINE use?

A

• Has central stimulatory action.
• Can increase blood pressure by alpha-agonist action
on vasculature as well as beta-stimulatory effects
on heart.
USES
• ADHD
• Narcolepsy

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10
Q

METHYLPHENIDATE use?

A
  • Structural analogue of amphetamine.

* Used to treat ADHD in children.

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11
Q

Tyramine consequence?

A 
• Found in fermented foods
such as ripe cheese and
Chianti wine.
• Normally oxidized by MAO.
• If the patient is taking MAO
inhibitors, it can precipitate
serious vasopressor
episodes.
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12
Q

BRIMONIDINE use?

A 
• Highly selective alpha-2 agonist.
• Given ocularly to lower intraocular pressure in
glaucoma.
• Reduces aqueous humor production and
increases outflow.
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13
Q

Methyldopa use and moa?

A

• Taken up by noradrenergic neurons.
• Converted to alpha-methylnorepinephrine which
activates central alpha2-adrenoceptors.
• This decreases blood pressure.
• Drug of choice for treatment of hypertension
during pregnancy.
• Adverse effects: sedation, impaired mental
concentration, xerostomia.

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14
Q

Clonidine use?

A

• Partial alpha2 agonist.
• Centrally acting antihypertensive.
• Activates central presynaptic alpha2-adrenoceptors.
• Reduces sympathetic outflow. This reduces
blood pressure.
• Adverse effects: lethargy, sedation, xerostomia.

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15
Q

PHENYLEPHRINE actions?

A

alpha 1-SELECTIVE ADRENERGIC AGONISTS
• Vasoconstriction: alpha 1 effect.
• Nasal decongestant . Given orally or topically.
• Mydriatic.
• Used to increase blood pressure in hypotension resulting from vasodilation in septic shock or
anesthesia.
• Used to increase blood pressure and terminate episodes of supraventricular tachycardia.

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16
Q

Beta2-ADRENERGIC AGONISTS

A
  • Evoke bronchodilation (beta2 effect)

* Used in asthma.

17
Q

Albuterol use?

A

SHORT-ACTING

• For management of acute asthma symptoms.

18
Q

Salmeterol & formoterol

A

LONG-ACTING
• Prolonged duration of action: 12 hours.
• Slow onset of action: not for prompt relief of acute
symptoms.

19
Q

DOBUTAMINE action and uses?

A

beta 1-SELECTIVE ADRENERGIC AGONISTS
• Predominantly a beta1 agonist.
• Potent inotrope, with comparatively mild chronotropic effects.
• Produces less increase in HR and less decrease in PVR than isoproterenol.
• Causes mild vasodilation.
• Increases myocardial O2 consumption. This is the basis of the dobutamine stress echocardiogram.

DOBUTAMINE: USES
• Management of acute heart failure.
• Management of cardiogenic shock.

20
Q

Isoproterenol uses, moa, effects?

A

• Activates beta 1 and beta 2 adrenergic receptors
• Increases heart rate, force of contraction, and
cardiac output (beta 1 effect).
• Dilates arterioles of skeletal muscle (beta 2 effect),
resulting in a decrease in peripheral vascular
resistance.
• Diastolic pressure falls. Systolic blood pressure
may remain unchanged or rise.
• Mean arterial pressure typically falls.
• Causes bronchodilation (beta 2 effect).

Isoproterenol use
• Isoproterenol may be used in emergencies to
stimulate heart rate in patients with bradycardia
or heart block

21
Q

Dopamine, what receptors does it act?

A

• Can activate dopamine, beta and alpha receptors.
• D1 > beta 1 > alpha 1
• The cardiovascular response to dopamine
depends on the dose infused.

22
Q

Low rates of dopamine infusion?

A 
• Dopamine activates D1 receptors, in renal and
other vascular beds, leading to:
• Vasodilation
• Increase in GFR
• Increase in renal blood flow
• Increase in sodium excretion
23
Q

Intermediate rates of dopamine infusion?

A

• Dopamine activates β1 receptors in the heart,
increasing cardiac output.
• There is negligible activation of β2 receptors.
• Dopamine causes release of NE from nerve
terminals, which contributes to its cardiac effects.
• Dopamine increases SBP.
• DBP is usually not changed significantly.
• MAP is increased.
• PVR is unchanged.

24
Q

High rates of dopamine infusion?

A

• Dopamine activates vascular alpha 1 receptors,
leading to vasoconstriction and a rise in
blood pressure.
• Total peripheral resistance may be increased

25
Q

Dopamine uses?

A

• Used in the treatment of severe CHF.
• Used in the treatment of cardiogenic and septic
shock.
• For management of shock intermediate to
high rates of infusion are used.

26
Q

Norepinephrine uses receptors act?

A
  • Agonist at alpha 1, alpha 2, and beta 1 receptors

* Little action on beta 2 receptors

27
Q

Norepinephrine effects? uses?

A

• Causes peripheral vasoconstriction (alpha 1 effect).
• Increases cardiac contractility (β1 effect).
• Increases peripheral vascular resistance, systolic
blood pressure and diastolic blood pressure.
• Cardiac output is unchanged or decreased.
• The increase in blood pressure triggers a
baroreceptor reflex resulting in bradycardia.

Norepinephrine uses?
• To treat shock because it increases vascular
resistance and therefore increases blood
pressure.

28
Q

EPINEPHRINE: USES?

A

• Anaphylactic Shock: drug of choice.
• Acute asthmatic attacks.
• Cardiac arrest
• In Local Anesthetics: Epinephrine increases
duration of local anesthesia by producing
vasoconstriction at the site of injection.

29
Q

When a low dose is given IV epinephrine actions?

A

• Peripheral resistance decreases, because beta 2
receptors are more sensitive to epinephrine
than alpha 1 receptors. Diastolic pressure falls.
• Systolic pressure increases due to increased
cardiac contractile force (beta 1 effect).
• Heart rate increases (beta 1 effect).
• There is no increase in mean blood pressure,
so the baroreceptor reflex does not kick in.
• Therefore, the effects of epinephrine depend on
the dose and the resultant ratio of the alpha 1 to beta 2
responses in the various vascular beds.

30
Q

When a large dose is given IV epinephrine actions?

A

• There is increase in blood pressure. Due to:
1. Increased ventricular contraction (beta 1 effect).
2. Increased heart rate (beta 1 effect) This may be
opposed by the baroreceptor reflex.
3. Vasoconstriction (alpha 1 effect).

31
Q

Describe epinephrine?

A

• Epinephrine acts as a hormone: after release
from the adrenal medulla into the blood it acts
on distant cells.
• Epinephrine is an agonist at both alpha and beta
adrenoceptors.
• At low concentrations epinephrine activates
mainly beta 1 and beta 2 receptors.
• At higher concentrations 1 effects become
more pronounced.

32
Q

Epinephrine effects?

A

• Increases heart rate and contractile force (beta 1 effect).
• Cardiac output increases: oxygen demand of the
myocardium increases.
• Increases renin release (beta 1 effect).
• Constricts arterioles in skin and viscera (alpha 1 effect).
• Dilates blood vessels of skeletal muscle (beta 2 effect).
• Relaxes bronchial smooth muscle (beta 2 effect).
• Increases liver glycogenolysis (beta 2 effect).
• Increases glucagon release (beta 2 effect).
• Increases lipolysis (beta 1 and beta 2 effect).

Pharmacology (49 decks)

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