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Pharmacology II > Lect 6 adrenergic stimulants > Flashcards

Lect 6 adrenergic stimulants Flashcards

1
Q

What is Phenylephrine (Neofrin; Neo-Synephrine)? what does it cause?

A

α1 selective agonist

  1. vasoconstriction: increases peripheral vascular resistance -> BP increases -> reflex slowing of HR
    • use for hypotensive emergency
  2. vasoconstriction in nasal mucosa makes it an effective decongestant
    • ​​rebound effect possible
  3. mydriasis and may be used topically to dilate the eye for examination, without affecting accommodation
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2
Q

Pseudoephedrine (Sudafed)

A

alpha agonist

  • decongestant
  • *use caution in patients with hypertension, as may increase blood pressure
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3
Q

What are Xylometazoline (Otrivin) and Oxymetazoline (Afrin)? Function?

A
  • direct acting alpha agonists
  • topical nasal spray: decrease congestion
    • rebound effect occurs if used chronically, as receptors will down-regulate
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4
Q

What are Tetrahydrozoline (Visine) and Naphazoline (Clear Eyes)

A

direct acting alpha agonist

  • decrease redness by causing vasoconstriction
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5
Q

topical alpha agonists are contraindicated in what conditions

A
  • narrow angle glaucoma
  • HTN
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6
Q

MOA of Clonidine (Catapres)?

A

selective α2 agonist, which acts in the brain

  • stimulation of α2 receptors on presynaptic terminals in the CNS decreases the release of NE, and other transmitters, reducing overall sympathetic output to the periphery, and producing CNS depression
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7
Q

What is Clonidine (Catapres) used for clinically? Route of administration?

A
  • oral; transdermal patch
  • reduced sympathetic tone leads to a decrease in blood pressure: treat HTN
  • decreases craving for addicts in recovery
  • may decrease hot flashes
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8
Q

Clonidine (Catapres) side effects

A
  • dry mouth, sedation, sexual dysfunction
  • hypertension may occur if the drug is withdrawn abruptly
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9
Q

What drug class are Methyldopa (Aldomet), Guanabenz (Wytensin) and Guanfacine (Tenex)? Main clinical use?

A
  • alpha 2 agonists
  • HTN
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10
Q

What drug class are Apraclonidine (Iopidine) and Brimonidine (Alphagan) in? Main clinical use?

A
  • alpha 2 agonist
  • used in the eye to decrease intraocular pressure and treat glaucoma
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11
Q

What drug class is Tizanidine (Zanaflex) in? Main clinical function?

A
  • α2 agonist
  • muscle relaxant; reducing muscle spasticity
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12
Q

describe that effect that alpha 2 agonists have on the eye

A
  • decrease cAMP in ciliary body -> decrease production of aqueous humor
  • vasoconstriction in eye -> increases outflow of aqueous humor
  • prolonged alpha stimulation increases prostaglandins -> increasing outflow of aqueous humor
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13
Q

What drug class is Isoproterenol (Isuprel) in? Clinical use?

A
  • selective β1 and β2 agonist
  • B1: Inc rate and contractility of heart
  • B2: vasodilation of skeletal muscle and renal vascular bed
    • systolic pressure may rise initially due to increased cardiac output, but dilation of skeletal blood vessels will lead to a decrease in blood pressure, with a reflex increase in heart rate
  • used in emergency treatment for cardiac arrest and complete heart block
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14
Q

large doses of Isoproterenol (Isuprel) can cause

A
  • palpitations
  • sinus tachycardia
  • arrhythmia
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15
Q

What drug class is Dobutamine in? What is it used for clinically?

A
  • selective beta 1 agonist
  • positive inotrope: increase contractility
  1. cardiac stress test
  2. increases cardiac output in shock and congestive heart failure
  • in hypertensive patients, BP may increase if given too quickly
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16
Q

What drug class is albuterol in? main clinical use?

A
  • beta 2 agonist
  • inhaled for treatment of asthma
17
Q

Side effects of albuterol

A
  • tremor, tachycardia, palpitations
  • HA common with systemic administration
18
Q

What drug class is Mirabegron (Myrbetriq) in? Clinical use?

A
  • beta 3 agonist
  • treatment of patients with overactive bladder (OAB)
19
Q

adverse effects of Mirabegron (Myrbetriq)

A
  • HTN
  • sinus tachycardia
20
Q

Low doses of Dopamine (Intropin) cause? High doses cause?

A
  • low doses : activate D1 receptors in renal vascular beds, causing vasodilation and increasing renal blood flow, increases GFR
  • High doses: similar to epinephrine:
    • stimulates β1 receptors in the heart, producing a positive inotropic and chronotropic effect (inc HR)
    • cause release of norepinephrine and stimulate α1 receptors, causing vasoconstriction and increasing blood pressure
21
Q

clinical use of Dopamine (Intropin)

A
  • sometimes given intravenously to treat cardiac shock, as it will increase cardiac output without causing vasoconstriction
22
Q

what drug class is Fenoldopam (Corlopam) in? clinical use?

A
  • more selective D1 agonist
  • causes dilation of vascular beds, decreasing blood pressure
  • main use is to produce rapid decrease of blood pressure in severe hypertension
23
Q

MOA of amphetamine

A
  • indirect-acting drug that increases release of NE from neurons, especially in the CNS (brain)
24
Q

What effect does amphetamine have on CNS?

A
  • CNS stimulant
    • alertness, euphoria, insomnia, decreased appetite, increased motor activity
    • possible psychosis
25
Q

What effect does amphetamine have on peripheral system

A
  • tachycardia
  • hypertension
26
Q

side effects of amphetamine

A
  • HA, dizziness, palpitations, agitation, confusion, delirium
  • cerebral hemorrhage, convulsions and coma may occur at high doses
27
Q

What drug class is methylphenidate (Ritalin) in? clinical use?

A
  • Indirect-acting Sympathomimetics
  • decreases hyperactivity in attention deficit hyperactivity disorder
28
Q

MOA of cocaine

A
  • Indirect-acting Sympathomimetics
  • inhibits re-uptake of DA and NE into nerve terminals
  • effect is similar to that of amphetamine, but shorter acting and more intense
29
Q

adverse effects of cocaine

A
  • severe hypertension and stroke in otherwise healthy young adults
  • often causes tachycardia, may cause arrhythmias and myocardial infarction
  • long-term use may cause psychosis
30
Q

clinical use for cocaine

A
  • cocaine is a powerful vasoconstrictor, and is sometimes used for nasopharyngeal surgery to decrease blood flow and produce local anesthesia
31
Q

MOA of Tyramine

A
  • Indirect-acting Sympathomimetics
  • increases NE release from nerve terminals
    • displaces NE from vesicle, forms false transmitter- octopamine
32
Q

repeated application of Tyramine causes

A
  • Tachyplyaxis: rapidly diminishing response to successive doses of a drug, rendering it less effective.
33
Q

Metabolism of Tyramine

A

monoamine oxidase (MAO)

34
Q

Tyramine use should be limited in patients on what drug

A
  • in patients treated for depression with monoamine oxidase inhibitors, ingestion of large amounts of tyramine may cause a severe hypertensive crisis!

Pharmacology II (9 decks)

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