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

Sympath- Adrenergic Agonists- Endogenous Catecholamines Flashcards

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?

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
Q

What is the mechanism of action in Norepinephrine?

A

Similar to Epinephrine

Little to no action on beta 2 receptors

26
Q

What are the cardiovascular Effects of Norepinephrine?

A

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
Q

What are the adverse effects of Norepinephrine?

A

Bradycardia

Cardiac Arrhythmias

Severe hypertension

Necrosis at injection site ( imparted circulation)

Peripheral vascular insufficiency
- Reduced blood flow to organs

28
Q

What are the therapeutic uses for Norepinephrine?

A

Vasoconstrictor in intensive care situations to raise or support blue pressure

Neurological injury and spinal anesthesia to raise or support blood pressure.

29
Q

What is dopamine?

A

A Metabolic Precursor of NE and Epinephrine
An Neurotransmitter in the CNS

-Important in the regulation of movement.

30
Q

What is the Mechanism of Action for Dopamine?

A

In low concentrations it’s an Agonist of D1 receptors

In high concentrations
Agonist of beta 1 and alpha 1 receptors

31
Q

What are the cardiovascular effects of Dopamine?

A

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
Q

What are the therapeutic uses of Dopamine:

A

1) Severe decompensated heart failure
2) cardiogenic shock
3) septic shock

33
Q

What is the mechanism of action for isoproterenol?

A

Potent, non selective beta agonist

Very low affinity for alpha receptors

34
Q

What are the cardiovascular effects of isoproterenol?

A

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
Q

What are the adverse effects of Isoproterenol?

A

Palpitations
Tachycardia
Headache
Flushing

Cardiac ischemia and arrhythmias more common in patients with underlying coronary artery disease

36
Q

What are the therapeutic uses for isoproterenol?

A

Emergency stimulation of heart rate

Patients with bradycardia or heart block.

37
Q

What is the mechanism of action of Dobutamine?

A

-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
Q

Cardiovascular effects dobutamine

A

Blood pressure: minor effect

Heart: increased cardiac output and contractility

Vasculature: Minimal effect on peripheral resistance

39
Q

What are the adverse effects of dobutamine?

A

Blood pressure and heart rate may increase significantly.

Patients with Afibrillation are at risk for ventricular response.

40
Q

What are the therapeutic uses for Dobutamine?

A

Short-term management of patients with cardiac decompensation after heart surgery, congestive heart failure, acute myocardial infarction.

41
Q

What are the mechanism of action for Beta 2 selective Adrenergic receptor agonists?

A

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
Q

What are the adverse effects for Beta 2 selective Adrenergic receptor agonists?

A

Tremor
Anxiety
Tachycardia
Arrhythmia *maoi increases this

Note: likelihood of adverse effects is reduced by inhalation administration.

43
Q

Name and Describe a short-acting beta 2 selective agonist.

A

Albuterol

Duration of action 3-6 hours

Onset of action: Bronchodilation within 15 min

Therapeutic use: Asthma

44
Q

Name and describe long acting Beta2 selective agonist?

A

Salmetrol and Formoterol

Duration of actions 12+ hours after inhaled

Onset of action Salmeterol: slow
Formoterol: Bronchodilation in minutes

Therapeutic uses: COPD Asthma

45
Q

Name and describe a beta 3 selective agonist?

A

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
Q

What are **Phenylephrine and Midodrine?

A

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
Q

What are the therapeutic uses of phenylephrine?

A

Hypotension
Nasal decongestant
Ophthalmic - Mydriatic agent

48
Q

Know slide 44

A

Read slide 44

49
Q

What is Ephedrine

A

Both a direct and indirect sympathomimetic:
Alpha and beta adrenergic receptor agonist

Enhances release of NE from sympathetic neurons

50
Q

What are the effects of Ephedrine?

A 
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
Q

What are the adverse effects of ephedrine?

A

Hypertension

Insomnia

Serious adverse cardiovascular effects for this with diseases or predisposed heart conditions

52
Q

What is pseudoephedrine?

A

A mixed acting sympathomimetic like ephedrine.
It is a direct Alpha 1 agonist.

Therapeutic use: nasal decongestant
Precursor to methamphetamine

53
Q

What are indirect acting sympathomimetics?

A

Cocaine : Schedule 2

Amphetamine: CNS Stimulant

54
Q

Describe Cocaine:

A

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
Q

What is Amphetamine and what is the mechanism of action?

A

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
Q

What are the cardiovascular effects of amphetamine:

A

Increased systolic and diastolic pressure.
Slow heart rate
Other smooth muscles: Contraction of urinary sphincter
Unpredictable GI effects

57
Q

What is the therapeutic use of Amphetamines:

A

treatment of narcolepsy and ADHD

58
Q

What are similar drugs to methamphetamine?

A

Methamphetamine
Methylphenidate

All are schedule 2
Narcolepsy and ADHD

Pharmacology Exam 2 (7 decks)

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