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Pharmacology Exam 2 > Sympath- Adrenergic Agonists- Endogenous Catecholamines > Flashcards

Sympath- Adrenergic Agonists- Endogenous Catecholamines Flashcards

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1
Q

What are the three types of Adrenergic Agonists?

A

1) Direct Acting ( selective and non selective)
2) Mixed acting
3) Indirect Acting

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2
Q

What is the Mixed Acting Adrenergic agonist?

A

Ephedrine

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3
Q

What are the 4 indirect acting Adrenergic agents?

A

Releasing Agents (amphetamine, tyramine)

Uptake inhibitors (cocaine)

MAOI Inhibitors (selegiline)

COMT Inhibitors (entacapone)

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4
Q

What are the Direct acting adrenergic Agonist groups?

A 
Endogenous catecholamines
Beta Agonists (nonselective)
Beta 2-selective agonists
(Short-acting) 
( Long acting) 
(Very Long acting) 
Beta 3-selective agonists 
Alpha 1-selective agonists
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5
Q

What are the important direct acting Endogenous catecholamines?

A

Epinephrine

Norepinephrine

Dopamine

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6
Q

What are the important direct acting beta agonists?

A

Isoproterenol
Dobutamine

( non selective)

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7
Q

What are the beta 2 selective agonists that are short acting?

A

Albuterol

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8
Q

What are the beta 2 selective agonists that are long acting?

A

Sametrol

Formoterol

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9
Q

What are the Beta 2 selective agonists that are very long acting?

A

Inadacterol
Vilanterol
Olodaterol

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10
Q

What are Beta 3 selective agonists?

A

Mirabegron

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11
Q

What is an Alpha 1 selective agonist?

A

Phenylephrine

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12
Q

What is a mixed acting Andrenergic Agonist?

A

Pseudoephedrine

Ephedrine

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13
Q

What are indirect acting Adrenergic Agonists

A

Amphetamine

Dextroamphetamine

Methylphenidate

*cocaine and methamphetamine

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14
Q

Go over mean arterial pressure, cardiac output, and baroceptor reflex.

A

MAP
CO
Baroceptor Reflex

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15
Q

How do Adrenergic receptors affect the vasculature?

A

Activation of Alpha 1 =vasoconstriction

Skin,splanchnic, nasal mucosa, skeletal muscle

Activation of Alpha 2
=minor vasoconstriction

Activation of Beta 2
=vasodilation in skeletal muscle

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16
Q

How do adrenergic receptors affect the heart?

A

Beta Receptors: Beta 1 Primary
Beta 2 important in heart failure

activation leads to: increased pacemaker/ heart rate, conduction velocity, contractility. Increased cardiac output.

Alpha receptors: myocardium functionally important in heart failure.

Minor increase in contractility

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17
Q

Go over localization of adrenergic receptors.

A

Slide 12

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18
Q

Describe the mechanism of action of Epinephrine.

A

Epinephrine is an adrenergic agonist and stimulates both alpha and beta receptors.

It is a potent vasoconstrictor

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19
Q

What are the cardiovascular effects of Epinephrine?

A

Blood Pressure: increased systolic pressure/ Decreased diastolic pressure

Heart: Increased heart rate, contractile force, cardiac output.

Vasculature: construction of most vascular beds

Dilation of skeletal muscle blood vessels

See tables on slide 14/15

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20
Q

What are the effects of Epinephrine on the respiratory system?

A

Bronchodilation

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21
Q

What are the metabolic effects of Epinephrine

A

Hyperglycemia
- stimulates gluconeogenesis

Lypolysis- increased free fatty acids

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22
Q

What are the adverse effects of Epinephrine?

A

Cerebral hemorrhage because increase in BP.

Cardiac arrhythmia

Angina- in patients with coronary artery disease.

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23
Q

What are the contraindications of Epinephrine?

A

Do not give to patients on non-selective beta blockers.

Results in unopposed activation of vascular a1 receptors.

Leading to severe hypertension and cerebral hemorrhage.

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24
Q

What are the therapeutic uses for Epinephrine?

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A

Hypersensitive reactions due to allergy. Epi Pen

Co-administration with local anesthetics
Increases duration of action by increasing local blood flow. ( tooth)

Bradyarrhythmias - restore rhythm in patients with cardiac arrest.

Ophthalmic uses
Mydriatic agent for ocular surgery
Glaucoma

25
What is the mechanism of action in Norepinephrine?
Similar to Epinephrine | Little to no action on beta 2 receptors
26
What are the cardiovascular Effects of Norepinephrine?
Blood pressure: increased systolic and diastolic pressure. Heart: decreased heart rate Increased contractile force CARDIAC OUTPUT IS UNCHANGED Vasculature: construction of vascular beds Increased peripheral vascular resistance. Alpha1)
27
What are the adverse effects of Norepinephrine?
Bradycardia Cardiac Arrhythmias Severe hypertension Necrosis at injection site ( imparted circulation) Peripheral vascular insufficiency - Reduced blood flow to organs
28
What are the therapeutic uses for Norepinephrine?
Vasoconstrictor in intensive care situations to raise or support blue pressure Neurological injury and spinal anesthesia to raise or support blood pressure.
29
What is dopamine?
A Metabolic Precursor of NE and Epinephrine An Neurotransmitter in the CNS -Important in the regulation of movement.
30
What is the Mechanism of Action for Dopamine?
In low concentrations it’s an Agonist of D1 receptors In high concentrations Agonist of beta 1 and alpha 1 receptors
31
What are the cardiovascular effects of Dopamine?
Low dose: vasodilation of kidney, mesenteric, and coronary vasculature D1 Intermediate dose: beta 1 Increased heart rate and contractility Increased systolic pressure High dose: alpha 1 Vasoconstriction and increased peripheral vascular resistance
32
What are the therapeutic uses of Dopamine:
1) Severe decompensated heart failure 2) cardiogenic shock 3) septic shock
33
What is the mechanism of action for isoproterenol?
Potent, non selective beta agonist Very low affinity for alpha receptors
34
What are the cardiovascular effects of isoproterenol?
Blood pressure: Increase the diastolic pressure MAP will decrease Heart: increase heart rate, contractile force, cardiac output Vasculature: Decrease peripheral resistance Primary in skeletal muscle and vasculature Respiratory: Bronchodilation
35
What are the adverse effects of Isoproterenol?
Palpitations Tachycardia Headache Flushing Cardiac ischemia and arrhythmias more common in patients with underlying coronary artery disease
36
What are the therapeutic uses for isoproterenol?
Emergency stimulation of heart rate | Patients with bradycardia or heart block.
37
What is the mechanism of action of Dobutamine?
-isomer is an alpha1 agonist +isomer is an alpha 1 antagonist Both are agonists of beta receptors with the positive isomer being 10xs more effective A race mic mixture is beta agonist
38
Cardiovascular effects dobutamine
Blood pressure: minor effect Heart: increased cardiac output and contractility Vasculature: Minimal effect on peripheral resistance
39
What are the adverse effects of dobutamine?
Blood pressure and heart rate may increase significantly. Patients with Afibrillation are at risk for ventricular response.
40
What are the therapeutic uses for Dobutamine?
Short-term management of patients with cardiac decompensation after heart surgery, congestive heart failure, acute myocardial infarction.
41
What are the mechanism of action for Beta 2 selective Adrenergic receptor agonists?
Selective agonist of beta 2 receptors ( selectivity is lost at high concentrations) Treat asthma and COPD Administered by inhalation. Pulmonary effects: Bronchodilation Reduced airway inflammation
42
What are the adverse effects for Beta 2 selective Adrenergic receptor agonists?
Tremor Anxiety Tachycardia Arrhythmia *maoi increases this Note: likelihood of adverse effects is reduced by inhalation administration.
43
Name and Describe a short-acting beta 2 selective agonist.
Albuterol Duration of action 3-6 hours Onset of action: Bronchodilation within 15 min Therapeutic use: Asthma
44
Name and describe long acting Beta2 selective agonist?
Salmetrol and Formoterol Duration of actions 12+ hours after inhaled Onset of action Salmeterol: slow Formoterol: Bronchodilation in minutes Therapeutic uses: COPD Asthma
45
Name and describe a beta 3 selective agonist?
Expressed in brown fat GI and bladder. Mechanism of action: relaxation of the detrusor muscle. ( increased bladder capacity ) Adverse effects: hypertension, UTI, headache Therapeutic use: urinary incontinence
46
What are **Phenylephrine and Midodrine?
Alpha 1 selective agonist: Mechanism of action: potent, direct-acting alpha 1 Adrenergic agonist Cardiovascular effects: increased blood pressure Decreased heart rate Vasoconstriction and decreased blood flow
47
What are the therapeutic uses of phenylephrine?
Hypotension Nasal decongestant Ophthalmic - Mydriatic agent
48
Know slide 44
Read slide 44
49
What is Ephedrine
Both a direct and indirect sympathomimetic: Alpha and beta adrenergic receptor agonist Enhances release of NE from sympathetic neurons
50
What are the effects of Ephedrine?
``` Increases blood pressured Stimulates heart rate and cardiac output Increases peripheral resistance Increase resistance to outflow of urine (alpha receptors in the base of the bladder) Bronchodilation Potent CNS stimulant ```
51
What are the adverse effects of ephedrine?
Hypertension Insomnia Serious adverse cardiovascular effects for this with diseases or predisposed heart conditions
52
What is pseudoephedrine?
A mixed acting sympathomimetic like ephedrine. It is a direct Alpha 1 agonist. Therapeutic use: nasal decongestant Precursor to methamphetamine
53
What are indirect acting sympathomimetics?
Cocaine : Schedule 2 Amphetamine: CNS Stimulant
54
Describe Cocaine:
Mechanism of action: inhibits reuptake of biogenetic amines from the synaptic cleft. Increases Blood pressure Increases heart rate Adverse effects: cardiac arrhythmia, myocarditis, aortic dissection, cerebral vasoconstriction Therapeutic use: topical anesthesia of the upper respiratory tract.
55
What is Amphetamine and what is the mechanism of action?
Powerful CNS stimulant with peripheral sympathomimetic actions. Mechanism of action: release biogenic amines from storage vesicles in CNS and peripheral sympathetic nerve terminals. Inhibits vesicular monoamine transporter VMAT
56
What are the cardiovascular effects of amphetamine:
Increased systolic and diastolic pressure. Slow heart rate Other smooth muscles: Contraction of urinary sphincter Unpredictable GI effects
57
What is the therapeutic use of Amphetamines:
treatment of narcolepsy and ADHD
58
What are similar drugs to methamphetamine?
Methamphetamine Methylphenidate All are schedule 2 Narcolepsy and ADHD

Pharmacology Exam 2 (7 decks)

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