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Final Test: Dynamics II > Sympathomimetics II: Examples of Synthetic Agonists > Flashcards

Sympathomimetics II: Examples of Synthetic Agonists Flashcards

1
Q

What is oxmetazoline

A

its a sympathomimetic– a non selective alpha agonist and a synthetic

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2
Q

What are some other names for oxymetazoline?

A

generic, afrin, neo-synephrine 12 hour and many other over the counter nasal soultions

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3
Q

Whay is oxymetazolined used for?

A

its used for the short term treatment of nasal decongestion

relief of redness of the eyes from cold swimming and contacts

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4
Q

What are the formulations of oxymetazoline and what is important about these routes?

A

nasal: spray or drops
ophthalmic: drops

both route can lead to systemic absorption

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5
Q

What is the mechanism of action of oxymetazoline for nasal administration?

A

is the direct administration of alpha-receptors in the nasal mucosa-vasoconstriction; results in decreased blood flow and decreases congestion

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6
Q

What is the mechanism of action for ophthalmic administration?

A

the activation of alpha receptors- vasoconstriction in the arterioles of the conjunctiva; it result in decreased conjunctival congestion

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7
Q

What are the side effects of oxymetazoline?

A

headaches

nervousness

trouble sleepting

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8
Q

What side effects can nasal administration of oxymetazoline have on the body?

A

results in rebound congestion, buring of the nasal mucosa and sneezing

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9
Q

What effects does opthalmic administration of oxymetazoline have on the body?

A

results in rebound irritation, conjunctivitis with long term use

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10
Q

What are the drug interactions of oxymetazoline?

A

TCA- significant systemic absorption of oxymetazoline could lead to tachycarida and arrhythmias

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11
Q

What conditions are oxymetazoline contraindicated with?

A

heart disease, hypertension, and diabetes

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12
Q

What is phenylephrine?

A

its an alpha agonist; synthetic; sympathomimetic

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13
Q

What is are the other names for phenylephrine used to treat nasal congestion?

A

sinex, neo-synephrine- treatment of nasal congestion

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14
Q

What are neo-synephrine and neo-synephrine, relief?

A

neo-synephrine, relief: is used as a mydriatic (diagnostic) and conjuctival decongestant

neo-synephrine- usedd for acute hypotension and as an adjunt to local anesthesia

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15
Q

What are the nasal forms of phenylephrine and what is their duration of action?

A

spray or drops

duration of action is 30 min to 4 hours

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16
Q

How is opthalmic of phenylephrine administered and how long do its effects last ?

A

solution, effects occur within 30 min; last up to 3 hours

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17
Q

Where can phenylephrine be given or how is it dosed?

A

can be given IV, SC, and IM

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18
Q

What is the onset of action of IM and SC phenylephrine?

A

its 10-15 min

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19
Q

What is the onset of action of IV phenylephrine?

A

its immediate

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20
Q

How is phenylephrine metabolized?

A

its not broken down by COMT (because it has only one hydroxyls)—longer duration of action

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21
Q

What happens to the application of nasal and opthalmic routes when using phenylephrine?

A

can lead to systemic absorption

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22
Q

What is the mechanism of action of phenylephrine on nasal stuructures?

A

activation of alpha-1 results in vasoconstriction of the arterioles of the nasal mucosa

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23
Q

What is the mechanism of action of phenylephrine on the ophthalmics?

A

stimulation of alpha-1 receptors contracts the dilatory muscle of the pupil producing mydriasis. the alpha receptor activation constricts the arterioles of the conjuctiva to decreas congestion

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24
Q

What is the mechanism of action of systemic phenylephrine?

A

vasopressor-activates alpha-1 receptors to produce vasocontriction; an increase in total peripheral resistance occurs with an elevation in both systolic and diastolic blood pressure; the pressor effect leads to pronounced bradycardia via the vagus

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25
Q

What is the mechanism of action of phenylephrine with anesthetic adjunct?

A

constricts the vessels in the skin, mucous membranes and viscera (GI) via—alpha-1 receptor activation;

this decreases the rate of vascular absorption of the local anesthetics thereby prolonging their duration of action and decreasing the risk of to toxicity

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26
Q

What are the side effects of phenylephrine on the nasal structure?

A

its the same as oxymetazoline

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27
Q

What are the side effects of phenylephrine on opthalmics?

A

tachycardia, vomitting, tingling in the hands and feet and headache

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28
Q

What are the side effects of alpha-agonist on the CNS?

A

dizzinines

nervousness

restlessness

trembling

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29
Q

What

A
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30
Q

What is the inhalation anesthetics and phenylephrine?

A

increased risk of arrhythmias and senstization of the myocardium to sympathomimetics

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31
Q

What are the drug interactions beteween local anesthetics and phenylephrine?

A

may cut off blood flow to fingers and toes

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32
Q

What is the drug interaction between TCA and Cocaine + phenylephrine?

A

potentiation of the cardiovascular effects of these drugs manily tachycardia and arrhythmias

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33
Q

What is the drug interaction between phenylephrine and beta blockers?

A

unopposed alpha-receptor activity resulting in hypertension; inhibition of therapeutic effects

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34
Q

What is the drug interaction between digitalis and phenylephrine?

A

increased risk of arrythmias

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35
Q

What is the drug conbination between ergot dervatives and phenylephrine?

A

potentiated vascoconstriction, hypertension

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36
Q

What is the drug interaction between MAO inhibitors or phenylephrine?

A

potentiates and prolongs effects of phenylephrine; increased risk of hypertension and arrhythmias

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37
Q

What is clonidine?

A

its a selective alpha-2 agonist

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38
Q

What are some more commerical names for clonidine?

A

Oral; Catapres

generic, Transdermal; Catapres TTS

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39
Q

What is clonidine used for?

A

used for the treatment of hypertension, usually a step II addition or substitution

and treatment of hypertensive emergencies

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40
Q

What are the non-label uses of clonidine?

A

non-label uses include amelioration of nicotine and opiate withdrawal symptoms which are CNS mediated

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41
Q

How does the oral dose interact with the body?

A

the oral dose is well-absorbed duration of antihypertensive action is about 8 hours

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42
Q

Where is the clonidine transdermal patch located and what is its druation of action?

A

it is placed on the chest or upper arm–the drug is absorbed at a constant rate and the duration of action is between 7 dyas when the patch is presnent and for 8 hours folloing removal

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43
Q

What are characteristics of clonidine?

A

its lipophilic and crosses the BBB

44
Q

What is the mechanism of action of clonidine?

A

it is an anti-hypertensive- agonist at alpha 2 receptors; activation of alpha 2 receptors in the central nervous systerm decreases sympathetic outflow (decreased NE release) to the heart, kidneys and preipheral vasculature; results in a decrease in total peripheral resistance, diastolic and systolic blood pressure and heart rate

45
Q

What are some withdrawl symptoms of clonidine?

A

a reduction in sympathetic outflow and inhibition of the locus ceruleus in the brain (an NE containing nucleus)

46
Q

What are the side effects of clonidine?

A

itching and redness with the use of the patch

drug mouth with oral use

drowsiness

dizziness

rebound hypertension in 5-20% of patients especially following abrupt cessation of use

47
Q

What are the drug interactions of clonidine with TCAs and appetite suppressants?

A

may decrease the anti-hypertensives effects

48
Q

What are the drug interactions of beta blockers with clonidine?

A

discontinuation of both beta-blocker and clonidine simultantaneouly can increase risk of rebound hypertension

49
Q

How should the patient be taken of beta blocker while on clonidine?

A

discontinue the beta blocker first several days before ending the clonidine

50
Q

What is important for clonidine to work properly?

A

compliance is essential for clonidine to work properly

51
Q

What isoproteranol?

A

its a non-selective beta agonist

52
Q

What are the commerical names of isoperoteranol?

A

Aerolene

Isuprel

Medi-Haler

Vaps-Iso

53
Q

What is isoproteranol used for?

A

its used as a bronchodilator for the treatment of:

asthma

bronchitis

emphysema

bronchospasm

obstructive pulmonary disease

its not the first choice ofor prophylaxis of this disease

54
Q

What else can isoproteranol used for?

A

its a cardiac stimulate for treatment of cardiac arrest and standstill, Adam-Stokes syndrome and AV block (both are forms of syncope which is altered consciousness due to reduced blood flow to the brain, fainting), carotoid sinus hypersensitivity and ventricular tachycardia and arrhythmia, bradycardia and hypo-perfusion syndrome (shock)

55
Q

What are the forms of isoproteranol that lead to rapid absorption?

A

inhalation and parenteral administration

56
Q

What are the forms of administration of isoproteranol that lead to variable absorption?

A

sublingual and rectal administration

57
Q

Where can isoproteranol enter?

A

it can enter the breast milk

58
Q

What contraindications of dobutamine?

A

hypovolemia

myocardial infarction

idiopathic hypertrophic subaortic stenosis

59
Q

What is the mechanism of action for the brochioles for isoproteranol?

A

agonist at beta-2 receptors in the lungs; this results in the dilation of bronchial smooth muscle, leading to reduced airway reistance and increasing lung capacity; activation of the beta-2 receptors increase cAMP production which relaxes the smooth muscle and also inhibits the release of mediators (such as histamine) of hypersensitivity from mast cells

60
Q

What is the mechanism of action of isoproteranol on cardiac stimulation?

A

an agonist of beta-1 receptors on the heart; this produces an increase in heart rate (positive chronotropic) via the sino-atrial node; an increase in the force of contraction (positive inotropic) in the myocardium; increase in the conduction velocity-shortening the refractory period of AV node

61
Q

What is the mechanism of action of isoproteranol and peripheral vasculature?

A

produces dilation of the smooth muscle surrounding the vasculature of the skeletal muscle va the beta-2 receptor; this relieves the intensive vasoconstriction that occurs after hypovolemic shock.

62
Q

What are the side effects of isoproteranol?

A

dry mouth and throat

nervousness and restlessness

trouble sleeping

pinkish saliva

63
Q

At what point which taking isoproteranol should a doctor be seen?

A

a doctor should be seen with persistent: chest pain, dizziness, severe headache, large increase in blood pressure, irregular or fast heart beat, severe weakness, and nausea and vomitting.

64
Q

What is the drug interaction of isoproteranol with inhalation anesthetics?

A

increased risk of arrhythmias and sensitization of the myocardium to sympathomimetics

65
Q

What are the drug interactions of isoproteranol and TCA and Cocaine?

A

potentiation of the cardiovascular effects of these drugs mainly tachycardia and arrhythmias

66
Q

What is the drug interaction between beta blockers and isoproteranol?

A

unopposed alpha-receptor activity resulting in hypertension; inhibition of therapeutic effects

67
Q

What is the drug interaction between digitalis and isoproteranol?

A

increased risk of arrhythmias

68
Q

When is isoproteranol contraindicated?

A

in most forms of heart disease

69
Q

What is dobutamine?

A

its a beta-1 selective agonist

70
Q

When is dobutamine used?

A

injection: dobutrex

71
Q

What is dobutamine used to treat?

A

used for treatment of cardiac decompensation (inablility to maintain adequate circulation) secondary to depressed contractility (as opposed to vascular damage) resulting from CHF and cardiac surgery

72
Q

How is dobutamine administered and what is its duration of action?

A

its give IV- onset of action is immediate; its duration of action is minutes

73
Q

What is the mechanism of action of dobutamine?

A

a direct acting inotropic agent, it stimulates beta-1 receptor on the heart to increase myocardial contractility and stroke volume; results in an increase in cardiac output

74
Q

What does dobutamine do to blood flow?

A

it increase the coronary blood flow and oxygen consumption

the systemic vascular resistance is decreased (afterload reduction) however systolic blood pressure and pulse pressure remain unchanged due to increased cardiac output

75
Q

What does dobutamine do to AV node conduction?

A

facilitates AV node conduction; renal blood flow and urine output is increased due to the increase in cardiac output

76
Q

What are the side effects of dobutamine?

A

an increase in systolic blood pressure of 10 to 20 mmHg in most patients but some patients can have an increase of over 50 mmHg

increase in heart rate of 30 or more BPM

premature ventricular beats

no major drug interactions

77
Q
A
78
Q

What is terbutaline?

A

a selective beta 2 agonist

79
Q

What are commerical names terbutaline?

A

inhalation; brethaire, oral;

brethine

bricanyl

80
Q

What is terbutaline used for?

A

as a bronchodilator for the same indications as isoproteranol as for the prophylaxis of asthma and bronchospasm

81
Q

What are some other uses of terbutaline?

A

its used for the treatment of prophylaxis premature labor

82
Q

What is the onset of action terbutaline?

A

60-120 min; while for inhalation its 5-30 min; it has a slow onset compared to other anti-asthmatics

83
Q

What is the mechanism of action for terbutaline?

A

selective agonist for beta-2 receptors which causes the relaxation of smooth muscle in the bronchi and uterus

84
Q

What are the side effects of terbutaline?

A

restlessness and nervousness

trembling

trouble sleeping

doctor should be seen with persistent: chest pain, dizziness, severe headache, large increase in blood pressure, irregular or fast heart beat, severe weakness, nausea and vomitting

85
Q

What are the drug interaction of terbutaline with inhalation anesthetics?

A

increased risk of arrhythmias and sensitixation of the myocardium to sympathomimetics

86
Q

What are the drug interactions of terbutaline with TCA and cocaine?

A

potentiate cardiovascular effects of these drugs mainly tachycardia and arrhythmias

87
Q

What are the drug interactions of terbutaline with beta blockers?

A

unopposed alpha receptors activity resulting in hypertension; inhibition of therapeutic effects

88
Q

What does drug interactions of terbutaline and digitalis have?

A

increased arrhythmias

89
Q

what is the drug interaction between MAO inhibitors and terbutaline?

A

potentiated effects on vasculature

90
Q

What is albuterol?

A

its a beta two selective agonist

91
Q

What is commerical name for albuterol?

A

ventolin, proventil

92
Q

What are the pharmacological properties and therapeutic indication of albuterol?

A

they are similare to terbutaline–considered more bronchoselective in effects

93
Q

How is albuterol administered?

A
94
Q

What is ritodrine?

A

its is a beta-2 selective agonist

95
Q

What is its use and what are its pharmacological properties?

A

is used specifically for the use of uterine relaxant

the pharmacological properties resembles those of other agents

96
Q

How is ritodrine administered?

A

it can be administered intravenously to selected patients to arrest premature labor; can prolong pregnancy

97
Q

How is ritodrine’s pharmacokinetic properties?

A

are complex and incompletely defined, especially in pregnant women

98
Q

What are salmeterol?

A

Its a long acting beta-2 selective agonist

99
Q

What is another commerical name for salmeterol?

A

serevent

100
Q

What is formoterol?

A

its a long acting beta selective agonist

101
Q

What is a commerical name for formoterol?

A

its foradil

102
Q

What is salmeterol and formoterol

and how do they achieve their effect ?

A

they are a new generation of long acting (12 hour or more) beta-2 selective agents.

they acchieve their effect due to their high lipid solubility; agents dissolve in the smooth muscle membrane in high concentrations (one other postulated mechanism is that they attach to mooring proteins close to beta-receptors)

this allows slow constant release over a long period of time; agents are not recommended for asthma monotherapy

103
Q

What are the long action beta-2 selective agonist agents used for?

A

salmeterol and formoterol are agents of choice for treating nocturnal asthma despite anti-inflammatory management of the use of other agents

104
Q

What is the benefit of combining salmeterol and formoterol with corticosteroids?

A

they are highly efficacious when combined with corticosteroids

105
Q

What can salmeterol and formoterol not be used for?

A

not relief of acute asthma attacks- not a rescue inhaler

106
Q

How should long acting beta-2 selective agonist be taken with?

A

give with anti-inflammatory agents ; it is recommended patients are optimized on these agents before long acting beta-2 agonist given

107
Q

what is so dangerous about long acting beta-2 selective agonist?

A

it has been shown that monotherapy may increase death

Final Test: Dynamics II (11 decks)

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