5 Catecholamines & Sympathomimetic Drugs

Front 1

What are the endogenous catecholamines?
Which receptors do they act on?
Effects?
General therapeutic uses?

Back 1

-Norepinephrine (NE) = noradrenalin
-Epinephrine (EPI) = adrenalin
-Dopamine (DA) = dopamine

-They are mixed alpha & beta adrenergic receptor agonists
-Dopamine activates D receptors

-Effects of activation of sympathetic NS
-Autonomic NS effects

Front 2

EPINEPHRINE

Receptors?
General physilogical Effects?

Back 2

-beta 1 & 2, alpha 1 & 2
-Depends on dosage
-low dose: beta effects predominate
-high dose: alpha effects

Front 3

EPINEPHRINE

Effects on the heart?
Effects on the vasculature?
Effects on Respration?
Effects on Genitourinary?
Effects on the eye?

Back 3

-Increase HR & strength of ventricular contraction
-Low doses: decreased TPR & diastolic pressure, High dose: increased TPR & BP
-Relaxes SM of airways: bronchodialation, inhibits inflammatory mediator release from mast cells, decreases vascular permeability in lung, decrease plasma protein extravasation, Increases cilia beat freq (beta receptors)
-Relaxes detrussor muscle in bladder & relaxes uterus
-Dilates pupil by relaxing ciliary muscle, increases aqueous humor outflow & decreases production

Front 4

EPINEPHRINE

Therapeutic uses?

Back 4

-Bronchospasm: Activates beta 2 to relax SM
-Anaphylaxis: Epi pen's for shock, beta 2 bronchodialation, alpha 1 vasoconstriction, beta 1 increase cardiac output
-Local hemostasis: prolong actions of local anesthetics by decreasing blood flow to area (alpha 1)

Front 5

EPINEPHRINE

Adverse effects on:

Heart?
Vasculature?
Respiratory?

Back 5

Too much leads to:
-Cardiac: Palpitations, arrhythmias, angina (beta 1)
-Vascular: Pallor, stroke (alpha 1)
-Respiratory: distress/pulmonary edema (alpha 1 causes resistance)

Front 6

EPINEPHRINE

Contraindications/Precautions

Back 6

-Patients on beta receptor antagonists (beta blockers)=>Leads to massive a-1 response
-cardiovascular disease (increased cardiac workload w/ EPI)
-diabetes(beta 2 & increase in gluconeogenesis)
-hyperthyroidism (elevated heart rate)
-taking MAOI's or tricyclics(block NE transporters so don't clear it)
-pregnant (alpha 1 loss of blood to fetus)

Front 7

NOREPINEPHRINE

Receptors?
Physilogical effects?

Back 7

-Both alpha & beta w/ greater beta 1
-Vasculature: increased vasoconstriction => Increased TPR
-Cardiac: depends on patient status

Front 8

NOREPINEPHRINE

Therapeutic uses?

Back 8

-Blood pressure control in acute hypotensive states: alpha 1
-Cardiac arrest & profound hypotension: beta 1
-beta 1 in heart & alpha 1 in vasculature

Front 9

NOREPINEPHRINE

Adverse effects?
Contraindications?

Back 9

-Cardiac: Bradycardia, arrhythmias
-Vascular: decreased blood flow to vital organs, extravasation necrosis @ IV site
-Respiratory: distress, edema

-Mesenteric or peripheral vascular thrombosis
-Precaution: extravasation @ IV site
-MAOI's or tricyclics

Front 10

NOREPINEPHRINE

Contraindications?

Back 10

-Pheochromocytomas: tumors producing NE & EPI
-Uncorrected tachyarrhythmias or ventricular fibrillation
-Occlusive vascular disease
-MAOI's

Front 11

DOPAMINE

Receptors?
Physiological Effects?

Heart?
Vasculature?
Kidney?

Back 11

-Depends on dose: D>beta>alpha
-D1 >> D2
-Cardiac: increased HR & output (B-1)
-Vascular: High dose = increased BP (a-1)
-Renal: Increased glomerular filtration, blood flow, natriuresis/diuresis(treat hypertension)
-D1 = Na+ & H2O out

Front 12

DOPAMINE

Therapeutic uses?
Adverse effects?

Back 12

-Shock/hemodynamic imbalance
-Heart failure

-Cardiac: tachycardia
-Vascular: hypertension, local ischemic necrosis

Front 13

ALPHA 1 AGONISTS

List the drugs

Back 13

PHENYLEPHRINE
MIDODRINE
OXYMETAZOLINE

Front 14

ALPHA 1 AGONISTS

Physiological effects?

Back 14

Vascular: increased MAP
Cardiac: decreased HR
Ocular: mydriasis (pupil dilation)
Genitourinary: urinary retention

Front 15

ALPHA 1 AGONISTS

Therapeutic uses?

Back 15

-Treat hypotension/shock
-Nasal decongestion (alpha 1 to mucosa vasculature)
-Mydriasis (pupil dilation)

Front 16

ALPHA 1 AGONISTS

Adverse effects?
Contraindications?

Back 16

-Cardiovascular: Hypertension/stroke/MI;bradycardia
-Urinary retention

-Severe hypertension or ventricular tachycardia
-MAOI's or tricyclics

Front 17

ALPHA 2 AGONISTS

List the drugs
Treats what main disease?

Back 17

BRIMONIDINE
apraclonidine

THINK GLAUCOMA

Front 18

ALPHA 2 AGONISTS

Physiological effect?
Therapeutic Uses?

Back 18

-Decreases production of aqueous humor & increases uveoscleral outflow
-Treats open-angle glaucoma

Front 19

ALPHA 2 AGONISTS

Adverse effects?
Contraindications/Precaution?

Back 19

-Eye redness or stinging
-Allergic reactions
-bradycardia

-MAOI's(contraindication) & tricyclics(precaution)

Front 20

Beta Agonists

Non-Selective drugs?
Beta-2 selective drugs?

Back 20

-ISOPROTERENOL

-ALBUTEROL
-LEVALBUTEROL
-TERBUTALINE
-FORMOTEROL

Front 21

ISOPROTERENOL

Back 21

Non-selective beta agonist
Limited in use

Front 22

ALBUTEROL

Mode of administration?
Therapeutic use?

Back 22

Beta-2 selective
Oral or inhalation
Given in ER nebulized for acute exacerbations of asthma

Front 23

LEVALBUTEROL

-Mode of administration?
-Therapeutic use?

Back 23

-R-isomer of albuterol
-Inhalation
-Used in relief & prevention of bronchospasm

Front 24

TERBUTALINE

-Mode of administration?
-Therapeutic use?

Back 24

-Oral, injection
-ONLY beta-2 bronchodilator, used as IV admin in ER treatment of status asthmaticus

Front 25

FORMOTEROL

Unique characteristic?
Contraindications?

Back 25

-2X the potency, more lipophilic = Longer duration
-BLACK BOX WARNING: may increase risk of ashtma-related death

Front 26

BETA AGONISTS

Physiological effects?

Back 26

-Bronchodilation
-Enhanced mucociliary clearance
-Inhibits mast cell release of inflammatory mediators
-Decreased TPR
-Increased cardiac output

Front 27

BETA AGONISTS

Therapeutic uses?

Back 27

-Bronchospasm: beta-2 agonists are the DRUGS OF CHOICE for sympathomimetic in treating ASTHMA
-Cardiovascular (Isoproterenol only)
-Heart block
-Cardiac arrest
-Hypovolemic states/shock

Front 28

BETA AGONISTS

Adverse effects?
How do you limit these effects?

Back 28

**All side effets are less likely w/ administration by inhalation**
-Cardiac: palpitations, tachycardia
-Skeletal muscle tremor: develop tolerance

Front 29

BETA AGONISTS

Contraindications/Precautions?

Back 29

-tachyarrhythmias, vetricular arrhythmias, angina, heart block caused by digitalis(isoproterenol)
-cardiovascular disorders(precaution for B-2's)
-Diabetes(precaution)

Front 30

MIXED AGONISTS

List drugs

Back 30

DOBUTAMINE
EPHEDRINE
PSEUDOEPHEDRINE

Front 31

DOBUTAMINE

Physiological effect?
Therapeutic uses?

Back 31

-Binds BOTH alpha & beta with predominant B-1 effects on heart
-More potent inotropic effects
-Peripheral resistance unchanged

-Cardiac decompensation due to organic heart disease or cardiac surgery

Front 32

DOBUTAMINE

Adverse effects?
Contraindications/Precautions?

Back 32

-Cardiac: Increase HR
-Vascular: Increase BP
-Tachyphylaxis(avoid w/continuous low dose infusion)

-Idiopathic hypertrophic subaortic stenosis(obstruction to cardiac flow)

Front 33

EPHEDRINE & PSEUDOEPHEDRINE

-Receptors?
Physiological effets?

Back 33

**Pseudoephedrine is less potent**

-Act on both alpha & beta receptors indirectly by releasing NE

-Cardiac: Increased HR & contractility
-Vascular: variable change in TPR
-Respiratory: Bronchodilation
-CNS: Penetrates BBB, CNS stimulation

Front 34

EPHEDRINE & PSEUDOEPHEDRINE

Therapeutic uses?

Back 34

Hypotension: a1
Nasal decongetion: a1
OTC asthma: b-2 bronchodilation

Front 35

EPHEDRINE & PSEUDOEPHEDRINE

Adverse effects?
Contraindications/Precautions?

Back 35

-Cardiac: palpitaiton, arrhythmias, tachycardia or bradycardia
-Vascular: hypertension
-Genitourinary: urinary obstruction w/ benign prostatic hypertrophy
-CNS: nervousness, restlessness, psychological disturbances

-MAOI's
-Cardovascular disease, hyperthyroidism, diabetes, prostatic hypertrophy

Front 36

DOPAMINE RECEPTOR AGONISTS

List the drugs

Back 36

FENOLDOPAM

Front 37

FENOLDOPAM

Receptors?
Physiological effects?

Back 37

D1 receptor activation
-Vascular: hypotension & renal vasodilation
-Renal: Natriuresis & diuresis

Front 38

FENOLDOPAM

Therapeutic use?
Adverse effects?
Contraindications/Precautions?

Back 38

-Hypertension: given IV

-Headach most common, hypotension, tachycardia
-Glaucoma

Front 39

INDIRECT AGONISTS/SYMPATHOMIMETICS

List drugs

Back 39

COCAINE
METHYLPHENIDATE
TYRAMINE
dextroamphetamine/amphetamine

Front 40

COCAINE

Pharmacology?
Therapeutic uses?

Back 40

-Blocks re-uptake of catecholamines =>Increases dopamine & NE
-Hemostasis: Used in ENT surgery
-Local anesthesia

Front 41

METHYLPHENIDATE

Pharmacology?

Back 41

-Blocks reuptake of catecholamines

Front 42

TYRAMINE

Pharmacology?
Clearance by which enzyme?
Contraindications?
Adverse effects?

Back 42

-by-product of tyrosine metabolism
-metabolized by MAO (MAOI's contraindicated)
-Can produce hypertensive crisis due to excessive NE release