Adrenergic Pharm Flashcards by Brock Wiley

Where do adrenergic drugs take effect?

SNS

a and B receptors (NE) - cardiac muscle, smooth muscle, glands, nerve terminals
D1 receptors (dopamine) - renal vascular smooth muscle

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Where do cholenergic drugs take effect?

PNS

*MAChR (ACh) - cardiac muscle, smooth muscle, glands, nerve terminals, sweat glands

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Are sweat glands under sympathetic or parasympathetic control?

Sympathetic

but controlled by MAChR/ACh, and therefore affected by cholenergic drugs
cholinomimetics and AChE inhibitors can induce sweating, anticholinergics can inhibit sweating

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G protein and effects of

a1 receptors

Gq, increased IP3, DAG

*increased Ca actvates PKC

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G protein and effects of

a2 receptors

Gi, decreased cAMP

*decreased PKA activity

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G protein and effects of

B receptors

Gs, increase cAMP

*increased PKA activity

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G protein and effects of

D1 receptors

Gs, increase cAMP

*increased PKA activity

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G protein and effects of

D2 receptors

Gi, decrease cAMP

*decreased PKA activity

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Phenylephrine MOA

a1 agonist

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Clonidine MOA

a2 agonist

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Dobutamine MOA

B1 > B2 agonist

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Isoprotenol MOA

B1 = B2 agonist

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Albuterol MOA

B2 > B1 agonist

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Effects of a1 activation

*Phenylephrine, Norepinephrine

Vasoconstriction

*agonists can cause reflex bradycardia (phenylephrine, norepinephrine)

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Effects of a2 activation

*Clonidine

Sympatholytic, decreased BP and HR

*also cause platelet aggregation

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Effects of B1 activation

Increased HR and contractility, increased renin release

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Effects of B2 activation

Respiratory, uterine and vascular smooth muscle relaxation

K+ uptake in skeletal muscle
Gluconeogenesis and glycogenolysis in liver

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Effects of B3 activation

Relaxation of detrusor muscle

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Effects of D1 activation

Dilates renal vasculature

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Effects of D2 activation

modulates neurotransmitter release in brain

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Effects of epinephrine

Increased HR and contractility (B1)
Increases SBP, decreases bronchial secretions (a1)
Decreases DBP, relaxes bronchial SM, muscle tremor due to K+ uptake, liver glycogenolysis and gluconeogenesis (B2)

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Adrenergic receptors found in the skin and mucous membranes

mostly a1

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Adrenergic receptors found in the skeletal muscle

a1 and B2

Adrenergic receptors found in the kidneys and brain

D1 and a1

Effects of norepinephrine

- Potent vasoconstriction, increased BP (a1) - Decreased HR (reflex bradycardia) - Increased contractility (B1) *no B2 effects

Effects of nonselective B agonists (B1=B2) *Isoproterenol

- Increased HR and contractility (B1) - Vasodilation, decreased BP (B2) - Bronchodilation (B2)

In a patient in hypotensive emergency, what can be used to increase blood pressure?

a1 agonist effects: Norepinephrine, phenylephrine

In a patient with chronic hypotension, what can be used to increase blood pressure?

Ephedrine *indirect adrenomimetic, increases NE and dopamine release and is direct receptor agonist

What can be given to a patient in cardiogenic shock?

Dobutamine * B1 agonist * can also be used short term in acute HF

What adrenomimetic can be given to treat HTN?

Clonidine

Emergency therapy for complete AV block and cardiac arrest

Epi, isoproterenol

Adrenomimetics used to help treat depression

Phenelzine, Selegiline *MAO inhibitors

Adrenomimetics used for narcolepsy (sudden sleep attacks)

Amphetamines, methylphenidate *Methylphenidate also used for ADHD

Adrenomimetics used for appetite suppression in obesity

Ephedrine, amphetamines

Adrenomimetic used to treat asthma

Albuterol

Adrenomimetic used to treat nasal decongestion

Phenylephrine, ephedrine

Treatment for anaphylaxis

Epi

Cocaine MOA

NE and DA reuptake inhibitor

Amphetamines, methylphenidate, tyramine MOA

Increased NE and DA release, inhibited reuptake

Ephedrine MOA

Increased NE and DA release, and direct receptor agonist

Metyrosine MOA

indirect acting adrenergic antagonist *inhibits tyrosine hydroxylase

Guanethidine MOA

indirect acting adrenergic antagonist *depletes and prevents storageof NE

Phentolamine, Phenoxybenzamine MOA and difference

Non-selective a1/a2 receptor antagonists * Phentolamine non-covalent bonding and therefore shorter acting (reversible) * Phenoxybenzamine covalent bonding and therefore longer acting (irreversible) * treatment for catecholamine excess in pheochromocytoma * phentolamine can also be injected into the penis to treat ED

- osin drugs MOA | * Prazosin, Tamulosin, Doxazosin

Selective a1 receptor inhibitors

Alpha antagonists used for essential HTN treatment

Prazosin, Doxazosin *non-selective alpha blockers are NOT used for HTN (phentolamine, etc.)

Alpha antagonist used for chronic urinary obstruction in BPH

Tamulosin *greater selectivity for a1a receptors (vs a1b), which contributes most to prostate smooth muscle contraction

Labetalol, Carvedilol MOA

Mixed B and a1 antagonists

Propanolol, Pindolol, Nadolol MOA

Non-selective B1 and B2 antagonists

Acebutolol, Betaxolol, Atenolol, Metropolol MOA

Selective B1 antagonists

B blockers that are pure antagonists

- Atenolol - Nadolol - Propanolol *highest risk of bradycardia

B blockers that are partial agonists

- Acebutolol - Labetalol - Pindolol *lower risk of bradycardia

B blockers that are inverse agonists

- Betaxolol - Metropolol *lower risk of bradycardia

B blockers used in heart failure

Metoprolol, Carvedilol

Beta blocker used in glaucoma

Betaxolol

B blocker used in hyperthyroidism

Propanolol