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Pharmacology Final > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

1
Q

Autonomic Nervous System

A
  • The SNS is the counterpart of the parasympathetic nervous system
  • Together they make up the ANS
  • They provide a checks-and-balances system for maintaining the normal homeostasis of the autonomic functions of the human body
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2
Q

Adrenergic Drugs

A
  • Drugs that stimulate the sympathetic nervous system (SNS)
    • Adrenergic agonists
    • Sympathomimetics
  • Mimic the effects of SNS neurotransmitters (catecholamines)
    • Norepinephrine (NE)
    • Epinephrine EPI)
    • Dopamine
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3
Q

Catecholamines

A
  • substances that can produce a sympathomimetic response
  • Metabolized by two enzymes:
    • Monoamine oxidase=MAO
    • Catechol ortho-methyltransferase=COMT
  • Endogenous
    - epinephrine, norepi, dopamine
  • Synthetic
    - Dobutamine, phenylephrine
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4
Q

MOA for Adrenergic Drugs

A
  • Direct-acting sympathomimetic
    • Binds directly to the receptor and causes a physiologic response
  • Indirect-acting sympathomimetic
    - causes release of catecholamine from storage sites (vesicles) in nerve ending
    - catecholamine then binds to receptors and causes a physiologic response
  • Mixed -acting sympathomimetic
    • Directly stimulates the receptor by binding to it
    • Indirectly stimulates the receptor by causing the release of stored neurotransmitters from vesicles in the nerve endings
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5
Q

Alpha-Adrenergic Receptors

A
  • Divided into alpha1 and alpha2 receptors
  • differentiated by their location on nerves
  • Alpha1-adrenergic receptors
  • Alpha2-adrenergic receptors
    • control the release of neurotransmitters
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6
Q

Drug effects of Alpha-Adrenergic Receptors

A
  • stimulation of alpha-adrenergic receptors on smooth muscles results in:
    • vasoconstriction of GI smooth muscles
    • Relaxation of GI smooth muscles (decreased motility)
    • Constriction of bladder sphincter
    • Contraction of uterus
    • Male ejaculation
    • Contraction of pupillary muscles of the eye (dilated pupils)
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7
Q

Beta-Adrenergic Receptors

A
  • All are located on postsynaptic effector cells
    • Beta1-adrenergic receptors-located primarily in the heart
    • Beta2-adrenergic receptors-located in smooth muscle of the bronchioles, arterioles, and visceral organs
  • Responses
    • Bronchial, GI, and urterine smooth muscle relaxation
      - Glycogenolysis
      - Cardiac stimulation
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8
Q

Drug effects of Beta-adrenergic receptors

A
  • stimulation of beta1-adrenergic receptors on the myocardium, artrioventricular (AV) node, and sinoatrial (SA) node results in cardiac stimulation
    • increased force of contraction (POSITIVE INOTROPIC EFFECT)
    • Increased heart rate (POSITIVE CHRONOTROPIC EFFECT)
    • increased conduction through AV node (POSITIVE DROMOTROPIC EFFECT)
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9
Q

Drug effects of Beta-adrenergic receptors

A
  • Stimulation of beta2-adrenergic receptors on the airways results in
    • Bronchodilation (relaxation of the bronchi)
  • Other effects:
    • Uterine relaxation
    • Glycogenolysis in the liver
    • Increased renin secretion in the kidneys
    • Relaxation of GI smooth muscles (decreased motility)
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10
Q

Dopaminergic Receptors

A
  • an additional adrenergic receptor
  • stimulated by dopamine
  • caused dilation of the following blood vessels, resulting in increased blood flow
    • renal
    • mesenteric
    • coronary
    • cerebral
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11
Q

Cardiovascular effects for Blood Vessels

A

receptors Alpha1 and beta2 causing VASOCONSTRICTION, VASODILATION

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12
Q

cardiovascular effects for cardiac muscle

A

Beta1 Increased contractility

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13
Q

Cardiovascular effects for AV node

A

Beta1 increased heart rate

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14
Q

Cardiovascular effects for SA node

A

Beta1 increased heart rate

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15
Q

Genitourinary effect on bladder sphincter

A

Alpha1 constriction

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16
Q

Genitourinary effect on Penis

A

Alpha1 ejaculation

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17
Q

Genitourinary effect on Uterus

A

Alpha1 and beta2 contraction and relaxation

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18
Q

Gastrointestinal effect on muscle

A

Beta2 and alpha decreased motility

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19
Q

Gastrointestinal effect on sphincters

A

Alpha1 constriction

20
Q

Respiratory effect on bronchial muscles

A

Beta2 dilation

21
Q

Endocrine effect on Liver

A

Alpha1 and Beta2 glycogenolysis

22
Q

Ocular effect on Pupils

A

Alpha1 dilation (mydriasis)

23
Q

Bronchodilators

A

drugs that stimulate beta2-adrenergic receptors of bronchial smooth muscles, causing relaxation, resulting in bronchodilation

24
Q

Examples of bronchodilators

A

albuterol, ephedrine, epinephrine, formterol, levalbuterol, metaproterenol, pirbuterol, and salmeterol

25
Q

Treatment of nasal congestion

A
  • Intranasal (topical) application causes contrction of dilated arterioles and reduction of nasal blood flow, thus decreasing congestion
  • Alpha1-adrenergic receptors
26
Q

Examples of nasal congestion

A

-ephedrine, naphazoline, oxymetazoline, phenylephrine, and tetrahydrozoline

27
Q

Temporary relief of conjunctival congestion

A
  • alpha-adrenergic receptors

- examples: epinephrine, naphazoline, phenylephrine, tretrahydrozoline

28
Q

Reduction of intraocular pressure and dilation of pupils: treatment of open-angle glaucoma

A
  • Alpha-adrenergic receptors

- Examples: epinephrine and dipivefrin

29
Q

Overactive Bladder Indications

A
  • relaxes the detrusor muscle during the storage phase of the bladder fill cycle
  • increases bladder storage capacity
  • Mirabegron (Myrbetriaq)
30
Q

Cardioselective sympathomimetics

A
  • used to support the heart during cardiac failure or shock; various alpha and beta receptors affected
  • Rhythm makers
  • Examples: Dobutamine, ephedrine, fenoldooam, midodrine, dopamine, epinephrine, phenylephrine, norepinephrine
31
Q

Adverse Effects of Alpha-adrenergic

A
  • headache, restlessness, excitement, insomnia, euphoria
  • chest pain, vasoconstriction, reflexive bradycardia, palpitations, dysrhythmias
  • Anorexia, dry mouth, nausea, vomiting, taste changness
32
Q

Adverse Effects of Beta-adrenergic drugs

A
  • mild tremors, headache, nervousness, dizziness
  • increased heart rate, palpitations, fluctuations of blood pressure
  • sweating, nausea, vomiting, muscle cramps
33
Q

Toxicity and Management of Overdose

A
  • From excessive CNS stimulation
    • seizures
    • Intracranial bleeding due to extreme elevation of blood pressure
  • Short half-lives, thus effects are short-lived
  • Symptom management and support the respiratory and cardiac system
34
Q

Vasoactive Adrenergics: Dobutamine

A
  • Beta1-selective vasoactive adrenergic drug that is structurally similar to the naturally ocurring catecholamine dopamine
  • Stimulates beta1 receptors on heart muscle; increases cardiac output by increasing contractility, which increases the stroke volume, especially in patients with heart failure
  • IV drug; given by continuous infusion
35
Q

Dopamine

A
  • naturally occurring catecholamine neurotransmitter
  • potent dopaminergic as well as beta1-and alpha1 adrenergic receptor activity
  • Low dosages: can dilate blood vessels in the brain, heart, kidneys, and mesentery, which increases blood flow to these areas
  • Higher infusion rates: improve cardiac contractility and output
  • Highest doses: vasoconstriction (alpha1-adrenergic receptor activity)
36
Q

Epinephrine

A
  • Endogenous vasoactive catecholamine
  • acts directly on both the alpha-and beta-adrenergic receptors of tissue innervated by the SNS
  • prototypical nonselective adrenergic agonist
  • Adninstered in emergency situations
  • One of the primary vasoactive drugs used in many advanced cardiac life support protocols
37
Q

Fenoldopam (Corlopam)

A
  • periperal dopamine-1 agonists
  • used to lower blood pressure by inducing arteriolar vasodilation through stimulation of D1 receptors
  • short-term treatment of severe hypertension
  • increases renal blood flow
  • given parenterally
38
Q

Midodrine (Proamatine)

A
  • Prodrug that is converted in liver to its active form: desglymidodrine
  • Alpha1-adrenergic receptors stimulator
  • used for symptomatic orthostatic hypotension
  • oral dosing
  • should not be given within 4 hours of bedtime
39
Q

Mirabegron (Myrbetriq)

A
  • Beta3 agonist
  • relaxes detrusor muscle leading to increased bladder capacity
  • used for treatment of overactive bladder
  • Adverse effects: hypertension, UTI, Headache, Nasopharyngitits, nausea, dizziness
40
Q

Nrepinephrine (Levophed)

A
  • stimulates alpha-adrenergic receptors
  • causes vasoconstriction
  • direct-stimulating beta-adrenergic effects on the heart
  • no stimulation to beta2-adrenergic receptors of the lung
  • treatment of hypotension and shock
  • administered by continuous infusion
41
Q

Phenylephrine (Neo-Synephrine)

A
  • works almost exclusively on the alpha-adrenergic receptors
  • used primarily for short-term treatment to raise blood pressure in patients in shock
  • control of supraventricular tachycardias
  • vasoconstriction in regional anesthesia
  • Topical ophthalmic drug
  • nasal decongestant
42
Q

Chronic Lung disease education

A
  • avoid factors to exacerbate their condition
  • encourage fluid intake if permitted
  • educate patients about proper dosing, use of equipment and equipment care
  • educate on appropriate use of inhalers
43
Q

What may happen if you over use a nasal decongestant?

A

may cause rebound nasal congestion or ulcerations

44
Q

What happens if you administer two adrenergic drugs together?

A

may precipitate severe cardiovascular effects such as tachycardia or hypertension

45
Q

Can adrenergic drugs be given orally?

A

no, digestive enzymes will destroy

Pharmacology Final (7 decks)

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