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Therapeutics > Direct Acting Adrenergic Receptor Agonists > Flashcards

Direct Acting Adrenergic Receptor Agonists Flashcards

1
Q

Dopamine (Intropin)

A

Beta 1 adrenergic agonist

-will activate beta adrenergic receptors on it own

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2
Q

Norepinephrine (Levophed)

A

Adrenergic agonist

 a1- Vasoconstriction = Increase Blood Pressure
 b1- Expect ¬increase heart rate BUT Baroreceptors increase vagal tone (brake)
thus net effect = decrease Heart rate

	Potent a and b1 receptor  agonist
	Substrate for MAO and COMT
	Parenteral administration
	Used as a pressor
	Sodium bisulfite used in  preparations to prevent  oxidation
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3
Q

Epinephrine (Adrenalin)

A

Adrenergic agonist

 a1- Vasoconstriction = EXPECT increase Blood Pressure, BUT…
 b2- Vasodilation = a1 and b2 essentially cancel out effects on BP = no change in BP = No Baroreceptor Effect!!!!
 b1- Observe expected increase¬ in Heart rate (No Baroreceptor Reflex)

 Potent a, b1, and b2 receptor agonist
 Substrate for MAO and COMT
 Parenteral administration
 Sodium bisulfite used in preparations to prevent oxidation
 Available as many salts: hydrochloride, nitrate, bitartrate
 Uses: Anaphylaxis, glaucoma, in combination with local anesthetics

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4
Q

Phenylephrine (Neosynephrine)

A

A1 adrenergic agonist
(increase blood pressure - vasoconstriction, decrease heart rate - vagus nerve kicks in)

 Potent a1 receptor agonist
 Substrate for MAO
 Administration: Parenteral, oral, local
 Uses: Mydriasis without cycloplegia, glaucoma, pressor, nasal decongestant

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5
Q

Methoxamine (Vasoxyl)

A

A1 adrenergic agonist

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6
Q

Oxymetazoline (Visine)

A

A1 adrenergic agonist

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7
Q

Clonidine (Catapres)

A

A2 adrenergic receptor

 (Phenylimino)imidazolidine
 Selective a2 receptor agonist
 The basicity of the guanidine group (pKa = 13.6) is decreased (to pKa = 8.0) because of the attachment to the dichlorophenyl ring
 Clinical effect linked to activation of a2 receptors in the nucleus of the solitary tract (cardiovascular center)
 Administration: Oral, parenteral, transdermal
 Uses: Hypertension, opiate withdrawal

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8
Q

Methyldopa (Aldomet)

A

A2 adrenergic receptor

-Prodrug

 Methyldopa (Aldomet)
 A prodrug metabolized to active
a2 receptor agonist, (1R, 2S)-a- methylnorepinephrine
 Act at CNS a2 receptors to decrease sympathetic outflow
 Water soluble, ester hydrochloride salt Methyldopate is used for parenteral solutions
 Administration: Methyldopa, oral; Methyldopate; parenteral
 Uses: Hypertension

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9
Q

Guanabenz (Wytensin)

A

A2 adrenergic receptor

 “Open-ring” imidazolidines
 Two atom bridge to the guanidine group decreases the pKa so that the drug is mostly non-ionized at physiological pH
 Guanabenz has the shortest t-1/2 at ~ 6 hours. Half-life of clonidine and guanfacine is 12-16 hours
 Administration: oral
 Uses: Hypertension, ADHD (guanfacine)

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10
Q

Guanfacine (Tenex, Intuiv)

A

A2 receptor agonist

 “Open-ring” imidazolidines
 Two atom bridge to the guanidine group decreases the pKa so that the drug is mostly non-ionized at physiological pH
 Guanabenz has the shortest t-1/2 at ~ 6 hours. Half-life of clonidine and guanfacine is 12-16 hours
 Administration: oral
 Uses: Hypertension, ADHD (guanfacine)

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11
Q

Tizanidine (Zanaflex)

A

A2 adrenergic receptor

-muscle spasticity

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12
Q

Isoproterenol (Isuprel)

A

Non-selective B receptor

 b2- Vasodilation = Decrease Blood Pressure (Drop in BP may also trigger Baroreceptor reflex to increase¬ Heart rate)
 b1- Observe expected increase in Heart rate (Baroreceptor Reflex may also contribute to -increase Heart rate)

 Non-selective b receptor agonist
 Bronchodilation
 Increased cardiac output
 Metabolized by conjugation reactions (Phase II) and by COMT
 Not sensitive to MAO
 Administration: Oral, parenteral, local (inhaled)
 Uses: Asthma, Chronic Obstructive Pulmonary Disease
(COPD), Cardiostimulant

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13
Q

Dobutamine (Dobutrex)

A 
B1 adrenergic receptor
	Dopamine derivative
	***Available as a racemic mixture
	***(+)-enantiomer: potent b1  receptor agonist; a1 receptor
antagonist
	***(-)-enantiomer: potent a1  receptor agonist, potency for b receptors reduced 10X
	Net effect is positive inotropic  effect on heart with little  chronotropic effect
	Metabolized by COMT and
conjugation, not sensitive to  MAO
	Short half-life (~2 min)
	Administered: Parenteral
	***Use: Acute heart failure,  shock
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14
Q

Dopamine (Intropin)

A

B1 adrenergic receptor

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15
Q

Terbutaline (Brethine, Bricanyl)

A

B2 adrenergic receptor

 Resorcinol derivatives
 Selective b2 receptor agonists
 Bronchodilation
 Cardiac effects observed only at high doses
 Not metabolized by MAO or COMT
 Longer duration of action than isoproterenol
 Administration: Oral, parenteral, local (inhaled)
 Uses: Asthma, COPD; Terbutaline used as tocolytic (prevent premature labor)

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16
Q

Metaproterenol (Metaprel, Alupent)

A

B2 adrenergic receptor

 Resorcinol derivatives
 Selective b2 receptor agonists
 Bronchodilation
 Cardiac effects observed only at high doses
 Not metabolized by MAO or COMT
 Longer duration of action than isoproterenol
 Administration: Oral, parenteral, local (inhaled)
 Uses: Asthma, COPD; Terbutaline used as tocolytic (prevent premature labor)

17
Q

Albuterol (Proventil, Ventolin)

A

B2 adrenergic receptor

	Meta hydroxymethyl derivatives
	Selective b2 receptor agonists
	Bronchodilation
	Cardiac effects observed only at high doses
	Not metabolized by MAO or COMT
	Longer duration of action than
	isoproterenol
	Administration: Oral, local  (inhaled)
	Uses: Asthma, COPD
18
Q

Salmeterol (Serevent)

A

B2 adrenergic receptor

	Meta hydroxymethyl derivatives
	Selective b2 receptor agonists
	Bronchodilation
	Cardiac effects observed only at high doses
	Not metabolized by MAO or COMT
	Longer duration of action than
	isoproterenol
	Administration: Oral, local  (inhaled)
	Uses: Asthma, COPD
19
Q

Ritodrine (Yutopar)

A

B2 adrenergic receptor

20
Q

Naphazoline (Privine)

A1 receptor agonist

A

 Partial agonists at a receptors
 Administered locally/topically to promote vasoconstriction
 Basic nature of imidazoline ring causes compounds to exist in ionized form at physiologic pH
 Tachyphylaxis/Desensitization
 Uses: Nasal and ophthalmic decongestants

21
Q

Tetrahydrozoline (Visine)

A1 receptor agonist

A

 Partial agonists at a receptors
 Administered locally/topically to promote vasoconstriction
 Basic nature of imidazoline ring causes compounds to exist in ionized form at physiologic pH
 Tachyphylaxis/Desensitization
 Uses: Nasal and ophthalmic decongestants

22
Q

Oxymetazoline (Afrin, Visine)

A1 receptor agonist

A

 Partial agonists at a receptors
 Administered locally/topically to promote vasoconstriction
 Basic nature of imidazoline ring causes compounds to exist in ionized form at physiologic pH
 Tachyphylaxis/Desensitization
 Uses: Nasal and ophthalmic decongestants

23
Q

Apraclonidine (Iopidine)

A2 receptor agonist

A

 Glaucoma

24
Q

Formoterol (Foradil)

Beta receptor agonist

A 
	Selective b2 receptor agonists
	Bronchodilation
	Not metabolized by MAO or COMT
	Onset of action:
	 Salmeterol 10-20 min
	Formoterol < 5 min
	Longer duration of action
	Administration: inhaled (metered-  dose inhaler and powder)
	Uses: Long-term Asthma, COPD
	Not recommended for acute  treatment of asthma symptoms

Therapeutics (11 decks)

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