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PHRM 825 > PHRM 825: Antiadrenergic Drugs > Flashcards

PHRM 825: Antiadrenergic Drugs Flashcards

1
Q

Phenoxybenzamine

A
  • Non-selective alpha receptor antagonist (a1 and a2)
  • Also blocks Ach, Histamine, and serotonin receptors
  • Irreversible antagonist resulting from covalent modification of receptor
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2
Q

Phentolamine

A
  • Non-selective alpha receptor antagonist (a1 and a2)
  • Competitive (reversible) blocker
  • Potent vasodilator, but induces pronounced reflex tachycardia
  • Blocks of presynaptic alpha 2 receptors may promote release of NE
  • Also blocks 5-HT receptors, and is a muscarinic and histamine receptor agonist
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3
Q

Prazosin

A
  • alpha 1 adrenergic receptor antagonist
  • Half-life: 3 hours
  • “Quinazoline”
  • Undergo extensive metabolism, excreted mainly in the bile
  • Vasodilators
  • Relaxation of smooth muscle in enlarged prostate and in bladder base
  • “First-dose” effect
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4
Q

Terazosin

A
  • alpha 1 adrenergic receptor antagonist
  • Half-life: 12 hours
  • “Quinazoline”
  • Undergo extensive metabolism, excreted mainly in the bile
  • Vasodilators
  • Relaxation of smooth muscle in enlarged prostate and in bladder base
  • “First-dose” effect
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5
Q

Doxazosin

A
  • alpha 1 adrenergic receptor antagonist
  • Half-life: 20 hours
  • “Quinazoline”
  • Undergo extensive metabolism, excreted mainly in the bile
  • Vasodilators
  • Relaxation of smooth muscle in enlarged prostate and in bladder base
  • “First-dose” effect
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6
Q

Yohimbine

A
  • alpha 2 adrenergic receptor antagonist
  • Indole alkaloid
  • Found in Rubaceae and related trees. Also in Rauwolfia Serpentina
  • Blockade of alpha 2 receptor increases sympathetic discharge
  • Folklore suggests use in the treatment of male impotence
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7
Q

Propranolol

A
  • Non-selective beta-adrenergic receptor antagonist
  • Lipophilic
  • Local anesthetic properties
  • Blockade is activity-dependent
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8
Q

Pharmacologic effects of all beta-adrenergic receptor antagonists

A
  • Decreased cardiac output
  • Reduced renin release
  • Increase VLDL, decrease HDL
  • Inhibit lipolysis
  • Inhibit compensatory glycogenolysis and glucose release in response to hypoglycemia
  • Increase bronchial airway resistance
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9
Q

What are therapeutic uses for beta-adrenergic receptor antagonists?

A
  • Hypertension
  • Angina
  • Cardiac arrhythmias
  • Migraine
  • Stage fright
  • Thyrotoxicosis
  • Glaucoma
  • Congestive heart failure (types II and III)
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10
Q

Nadolol

A
  • Non-selective beta-adrenergic receptor antagonists
  • Less lipophilic than propranolol
  • Long half-life: ~20 hours
  • Mostly excreted unchanged in urine (not metabolized)
  • Administration: Oral
  • Uses: Hypertension, angina, migraine
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11
Q

Timolol

A
  • Non-selective beta-adrenergic receptor antagonist
  • Thiadiazole nucleus with morpholine ring
  • Administration: Oral, ophthalmic
  • Uses: Hypertension, angina, migraine, glaucoma
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12
Q

How do beta blockers affect pupil size?

A

They don’t. There are no beta receptors in the eye

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13
Q

Pindolol

A
  • Non-selective beta-adrenergic receptor antagonist
  • Possesses “intrinsic sympathomimetic activity” (ISA)
  • Partial agonist
  • Less likely to cause bradycardia and lipid abnormalities
  • Administration: Oral
  • Uses: Hypertension, angina, migraine
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14
Q

Carteolol

A
  • Non-selective beta-adrenergic receptor antagonist
  • Possess “intrinsic sympathomimetic activity” (ISA)
  • Partial agonist
  • Less likely to cause bradycardia and lipid abnormalities
  • Administration: Oral, Ophthalmic
  • Uses: Hypertension, glaucoma
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15
Q

Metoprolol

A
  • Selective beta 1-adrenergic receptor antagonist
  • “Cardio-selective”
  • Less bronchoconstriction
  • Moderate lipophilicity
  • Half-life: 3-4 hours
  • Significant first-pass metabolism
  • Administration: Oral, parenteral
  • Uses: Hypertension, angina, antiarrhythmic, congestive heart failure
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16
Q

Atenolol

A
  • Selective beta 1-adrenergic receptor antagonist
  • “Cardio-selective”
  • Less bronchoconstriction
  • Low lipophilicity
  • Half-life 6-9 hours
  • Administration: Oral, parenteral
  • Uses: Hypertension, angina
17
Q

Bisopropolol

A
  • Selective beta 1-adrenergic receptor antagonist
  • “Cardio-selective”
  • Less bronchoconstriction
  • Moderate lipophilicity
  • Half-life: 3-4 hours
  • Significant first-pass metabolism
  • Administration: Oral, parenteral
  • Uses: Hypertension, angina, antiarrhythmic, congestive heart failure
18
Q

Esmolol

A
  • Selective beta 1-adrenergic receptor antagonist
  • Very short acting
  • Half-life: 9 minutes
  • Rapid hydrolysis by esterases found in RBCs
  • Administration: Parenteral
  • Incompatible with sodium bicarbonate
  • Uses: Supraventricular tachycardia, atrial fibrillation/flutter, perioperative hypertension
19
Q

Nebivolol

A
  • 3rd generation beta 1-adrenergic receptor antagonist
  • Low lipid solubility
  • Vasodilation due to nitric oxide production
  • Hypertension
20
Q

Labetolol

A
  • Non-selective beta receptor antagonist
  • Alpha 1 receptor antagonist
  • Two asymmetric carbons
  • (1R, 1’R)-isomer possessing beta blocking activity
  • (1S, 1’R)-isomer possessing alpha 1 receptor blocking activity
  • Beta blocking activity prevents reflex tachycardia normally associated with alpha 1 receptor antagonists
  • Administration: oral, parenteral
  • Uses: Hypertension, hypertensive crisis
21
Q

Carvedilol

A
  • Non-selective beta receptor antagonist
  • Alpha 1 receptor antagonist
  • Both enantiomers antagonize alpha 1 receptors
  • Only (S)-enantiomer possesses beta-blocking activity
  • Beta-blocking activity prevents reflex tachycardia normally associated with alpha receptor antagonists
  • Administration: Oral
  • Uses: Hypertension, congestive heart failure (types II and III)
22
Q

Side effects of beta-blocker:

A
  • Bradycardia
  • AV block
  • Sedation
  • Mask symptoms of hypoglycemia
  • Withdrawal synrome
23
Q

Contraindications of beta blockers

A
  • Asthma
  • COPD
  • Congestive heart failure (Type IV)
24
Q

Reserpine

A
  • Catecholamine depleter
  • Indole alkaloid obtained from the root of Rauwolfia serpentina
  • Block vesicular monamine transporters
  • Deplete vesicular pool of NE
  • Slow onset of action
  • Sustained effect (weeks)
  • Used in the treatment of hypertension
  • May precipitate depression
25
Q

Bretylium tosylate

A
  • Reduces storage or release of NE
  • Aromatic quaternary ammonium
  • Precise mechanism unknown
  • Displace and release NE and prevent further release (depletion)
  • Local anesthetic
  • Administered: Parenteral
  • Uses: Antiarrhythmic (ventricular fibrillation)

PHRM 825 (36 decks)

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