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PHRM 825 > PHRM 825: Adrenergic Drugs > Flashcards

PHRM 825: Adrenergic Drugs Flashcards

1
Q

Norepinephrine

A
  • alpha 1 and beta 1 receptor agonist
  • Substrate for MAO and COMT
  • Administration: parenteral
  • Used as a pressor
  • Sodium bisulfate used in preparations to prevent oxidation
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2
Q

Epinephrine

A
  • Potent alpha, beta 1, and beta 2 receptor agonist
  • Substrate for MAO and COMT
  • Administration: Parenteral
  • Sodium bisulfate 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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3
Q

Isoproterenol

A

Beta 1 and beta 2 receptor agonist

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4
Q

Phenylephrine

A
  • Potent alpha 1 receptor agonist
  • Substrate for MAO
  • Administration: parenteral, oral, local
  • Uses: Mydriasis without cycloplegia, glaucoma, pressor, nasal decongestant
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5
Q

Naphazoline

A
  • Partial agonists at alpha 1 receptors
  • Administrated 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
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6
Q

Tetrahydrozoline

A
  • Partial agonists at alpha 1 receptors
  • Administrated 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
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7
Q

Oxymetazoline

A
  • Partial agonists at alpha 1 receptors
  • Administrated 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
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8
Q

Clonidine

A
  • Selective alpha 2 receptor agonist
  • (Phenylimino)imidazolidine
  • The basicity fo the guanidine group is decreased because of the attachment to the dichlorophenyl ring
  • Clinical effect linked to activation of alpha 2 receptors in the nucleus of the solitary tract (cardiovascular center)
  • Administration: Oral, parenteral, transdermal
  • Uses: Hypertension, opiate withdrawal
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9
Q

How do alpha 2 adrenergic agonists reduce BP?

A

By reducing sympathetic output from the brain

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10
Q

Guanabenz

A
  • Half life: ~6 hours
  • “Open-ring” imidazolidines
  • Two atom bridge to the guanidine group decreases the pKa so that the drug is mostly non-ionized at physiological pH
  • Administration: Oral
  • Uses: Hypertension
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11
Q

Guanfacine

A
  • Half life: ~12-16 hours
  • “Open-ring” imidazolidines
  • Two atom bridge to the guanidine group decreases the pKa so that the drug is mostly non-ionized at physiological pH
  • Administration: Oral
  • Uses: Hypertension, ADHD
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12
Q

Methyldopa

A
  • Prodrug metabolized to active alpha 2 receptor agonist, (1R,2S)-alpha-methylnorepinephrine
  • Act as CNS alpha 2 receptors to decrease sympathetic outflow
  • Water soluble, ester hydrochloride salt Methyldopate is used for parenteral solutions
  • Administration: Oral (methyldopa); Parenteral (methyldopate)
  • Uses: Hypertension
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13
Q

Adverse effects of alpha 2 adrenergic receptor agonists

A
  • Sedation
  • Sodium and water retention
  • Dry mouth
  • Withdrawal syndrome
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14
Q

Apraclonidine

A
  • alpha 2 receptor agonist

- Uses: Glaucoma

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15
Q

Tizanidine

A
  • alpha 2 receptor agonist

- Uses: Muscle spasticity

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16
Q

Isoproterenol

A
  • Non-selective beta 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, COPD, cardiostimulant
17
Q

Metaproterenol

A
  • Selective beta 2 receptor agonist
  • Resorcinol derivatives
  • 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
18
Q

Terbutaline

A
  • Selective beta 2 receptor agonist
  • Resorcinol derivatives
  • 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, tocolytic (prevents premature labor)
19
Q

Albuterol

A
  • Selective beta 2 receptor agonist
  • Meta hydroxymethyl derivatives
  • 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
20
Q

Salmeterol

A
  • Selective beta 2 receptor agonist
  • Meta hydroxymethyl derivatives
  • Bronchodilation
  • Onset of action: 10-20 mins
  • Cardiac effects observed only at high doses
  • Not metabolized by MAO or COMT
  • Longer duration of action than isoproterenol
  • Administration: Inhaled (metered dose inhaler and powder)
  • Uses: Long-term asthma, COPD
  • Not recommended for acute treatment of asthma sympmtoms
21
Q

Formoterol

A
  • Selective beta 2 receptor agonists
  • Bronchodilation
  • Not metabolized by MAO or COMT
  • Onset of action: <5 mins
  • Longer duration of action
  • Administration: inhaled (metered dose inhaler and powder)
  • Uses: long-term asthma, COPD
  • Not recommended for acute treatment of asthma symptoms
22
Q

Dobutamine

A
  • Dopamine derivative
  • Available as a racemic mixture
  • (+)-enantiomer: potent beta 1 receptor agonist; alpha 1 receptor antagonist
  • (-)-enantiomer: potent alpha 1 receptor agonist, potency for beta 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 minutes)
  • Administration: Parenteral
  • Use: Acute heart failure, shock
23
Q

What are examples of indirect-acting sympathomimetics?

A
  • Amphetamine
  • Pseudoephedrine
  • Ephedrine
  • Phenylpropanolamine
  • Tyramine
24
Q

How do indirect-acting sympathomimetics work?

A

Promote release of NE via reverse action plasma membrnae transporter

25
Q

Clinical uses of indirect-acting sympathomimetics

A
  • Amphetamines: ADHD, narcolepsy, anorexiant

- Others: nasal decongestants

PHRM 825 (36 decks)

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