CLASS

CATECHOLAMINE?

DRUG

RECEPTOR(S)

ACTIONS

Epinephrine

a1,4a2,4B1,4B2

UNTOWARD4EFFECTS

OTHER

Increase4HR,4BP,4contractility,4CO;4
Wide4angle4glaucoma;4w/4local4anesthetics4to4prolong4
vasoconstriction;4vasodilation4in4skeletal4muscle;4
action;4anaphylactic4shock;4complete4heart4block4or4
increase4in4blood,4glucose,4&4lactic4acid;4slight4
cardiac4arrest;4bronchodilator4in4asthma
decrease4PVR4**no4activation4of4baroreceptors

Palpitation,4cardiac4arrhythmias,4cerebral4
hemorrhage,4headache,4tremor,4
restlessness

No4P.O.,4life4saving4in4
anaphylaxis4or4cardiac4arrest

a1,4a2,4B1

Increase4BP,44contraction;4indirect4decrease4in4
HR;4vasoconstriction;4increase4PVR4**activation4 Hypotension,4shock
of4baroreceptors

Same4as4epi4+4hypertension

Rarely4used,4not4absorbed4
orally

B1,4B24

Decrease4in4PVR;4increase4in4CO;4
tachyarrhythmias;4bronchodilator

a1

Vasoconstriction

Clonidine

a2

Decrease4sympathetic4outflow4from4brain4to4
peripheryYY>4decreased4PVR4&4BP;4decrease4in4
sympathetic4outflow;4decreased4production4of4
aqueous4humor

Dobutamine

B1

Increase4in4contractility,4HR,4AV4conduction4(no4
IV4only,4Use4with4caution4in4
Short4term4treatment4of4cardiac4decompensation4after4
effect4on4dopamine4receptors=4no4renal4
Increase4in4BP4and4HR;4cardiac4arrhythmias patients4with4hypertension4or4
surgery,4or4patients4with4congestive4heart4failures4or4MI
vasodilation)
cardiac4arrhythmias

B2

Relaxation4of4bronchiole4&4uterine4smooth4
muscle;4activation4of4other4B24receptors4after4
systemic4administration

CatecholaminesA(rapid4
onset,4brief4duration,4
no4P.O.,4doesn't4
Norepinephrine
penetrate4BBB)

Isoproterenol

ADRENORECEPTORAAGONISTS

DirectlyAActingA
(Responses4not4
reduced4by4prior4
treatment)

Methoxamine
NonCcatecholamineA
(longer4duration4of4
action,4P.O.4okay)

Catecholamine

Phenylephrine

Metaproterenol
Albuterol
Terbutaline
Ritodrine
Formoterol
Salmeterol

THERAPEUTIC4APPLICATIONS

Palpitations,4tachycardia,4headache,4
flushed4skin,4cardiac4ischemia4patients4with4 IV,4inhalation4in4asthma
coronary4diseases
Mephentermine4&4
Treatment4of4supraventricular4tachycardia;4
Hypertension;4reflex4bradycardia;4dry4
metaraminol4also4act4indirectly4
vasoconstrictor4to4treat4postural4hypotension4following4
mouth;4sedation;4rebound4hypertension4 to4release4NE;4Midodrine4is4a4
spinal4anesthesia4&4shock;4phenylephrine=4nasal4
upon4abrupt4withdrawal4
prodrug
decongestant
I.V.,4P.O.
Bronchodilator4for4asthma,4complete4heart4block4or4
cardiac4arrest;4shock

Adjunctive4therapy4in4shock;4hypertension;4reduce4
sympathetic4response4to4withdrawal4from4narcotics,4
alcohol,4tobacco;4glaucoma

Sedation

Bronchodilator4for4asthma4&4COPD4(short4acting)
Stop4premature4labor,4bronchodilator4(short4acting)

Skeletal4muscle4tremor,4tachycardia4&4
other4cardiac4effects

Long4acting4for4prophylaxisY4treatment4of4
bronchospasm

NonCcatecholamine
IndirectlyAactingA
(responses4abolished4
by4prior4treatment)

Catecholamine
MixedAacting4
(response4reduced4by4
prior4treatment)

Parental,4P.O.

CNSAstimulation;4increase4in4BP;4myocardial4
stimulation;4primary4actions4on4heart4(B1)4and4
blood4vessels4(a)

Restlessness,4tremor,4insomnia,4anxiety,4
Treatment4of4ADHD,4narcolepsy,4parkinsonism,4epilepsy tachycardia,4hypertension,4cardiac4
arrhythmias

Inhalation,4P.O.4S.C.,4I.V.4Use4
with4caution4in4patients4with4
cardiovascular4disease
Marked4tolerance4occurs,4
chronic4use4leads4to4
dependence,4can4result4in4
hemorrhagic4stroke4in4patients4
with4underlying4disease,4
Schedule4II4drugs,4long4term4
use4can4cause4paranoid4
schizophrenia

Amphetamine

a,4B1

Dopamine

a1,4a2,4B1,4
Vasodilation4(coronary,4renal4mesenteric4beds);4
Cardiogenic4shock,4congestive4heart4failure,4treatment4
DA2,4releases4 increase4glomerular4filtration4rate;4increase4HR4
High4doses4lead4to4vasoconstriction
of4acute4renal4failure
NE
&4contractility;4increase4in4systolic4BP

IV

Ephedrine

a1,4a2,4B1,4B3,4 Similar4to4epinephrine4but4longer4lasting,4CNS4
stimulation
releases4NE

All4routes,4not4commonly4used4
*Ma4Huang

Bronchodilator4for4asthma,4nasal4congestion,4
hypotension4&4shock

Restlessness,4tremor,4insomnia,4anxiety,4
tachycardia,4hypertension

DRUG

RECEPTOR

Phenoxybenzomine
a1,1a2

ADRENORECEPTOR@ANTAGONISTS

Alpha@Adrenoreceptor@
Agonists

MoA
ACTIONS
Covalently1binds1to1a@
receptor=insurmountable1
competitive1antagonist,1blocks1
presynaptic1a@receptor1
Decrease1in1PVR1&1BP;1
mediated1inhibition1of1NE1
venodilation1
release

Phentolamine

Short1duration

Prazosin

Blocks1postjunctional1a11
receptors@@dilates1arterioles1
and1veins

Terazosin
Doxazosin

a1
Preference1for1a1A1and1a1D1
receptors@@prominent1in1
bladder1neck1&1prostate1gland@
@good1for1BPH

Tamsulosin

Decrease1in1PVR1&1BP;1relax1
smooth1muscles1in1neck1of1
urinary1bladder1&1postate

THERAPEUTIC1APPLICATIONS

UNTOWARD1EFFECTS

OTHER

Catecholamine1excess1(ex:1
pheocromocytoma)

Postural1hypotension,1failure1of1
ejaculation;1reflex1tachycardia1(not1
used1too1much1clinically)

Cardiac1stimulation1due1to1initiation1of1reflexes1&1
due1to1enhanced1release1of1NE1via1a21receptor1
blockade

Postural1hypotension

Phenoxybenzamine1produces1long@lasting1a@
receptor1blockade1at1high1doses1can1block1
neuronal1&1extraneuronal1uptake1of1amines;1
Prazosin11&1related1are1slective1for1a1@receptors;1
Tamsulosin1exhibits1some1selevtively1for1a11
receptors

Primary1hypertension,1increase1
urine1flow1in1benign1prostatic1
hyperplasia

Nadalol
1st1gen1non@ Pindolol
selective
Propranolol
Timolol

Partial1agonist,1membrane1
stabilizing
Membrane1stabilizing

Bradycardia;1negative1inotropic1
effect;1decrease1in1CO;1
bradyarrhythmias;1reduction1in1AV1
conduction1;1bronchoconstriction;1
fatique;1sleep1disturbances1
(insomnia;1nightmares);1prolongation1
of1hypoglycemia;1sexual1dysfunction1
in1men;1NVDF@1nausea,1vomiting,1
diarrhea,1flatulence
Above1+1vasodilation1(3rd1generation1drugs1cause1
release1of1NO)

Initial1increase1in1BP,1eventual1
"False1neurotransmitter,"1
decrease1in1BP1due1to1venous1
blocks1NE1uptake1&1displaces1
pooling1and1reduced1venous1
NE;1inhibition1of1NE1release;1
return@1decreased1CO,1long1
depletes1NE1store
duration@1does1not1enter1CNS

Mild1to1moderate1hypertension;1
Used1with1a1diuretic1bc1it1reduces1
glomerular1filtration1rate1causing1
Na+1and1H2O1retention;1decreases1
intraocular1pressure1in1glaucoma

Orthostatic1hypotension,1
parasympathetic1predominance1
(severe1diarrhea);1inhibition1of1
ejaculation;1can1precipitate1
congestive1failure

Reserpine

Blocks1uptake1of1biogenic1
amines1(NE,1dopamine,1
serotonin,1etc.)1into1storage1
vesicles1within1neuron@@>1
interferes1with1
neurotransmission1&1causes1
depletion1of1transmitters

Drowsiness,1lethargy,1
Reserpine1+1thiazide1diuretics1used1 parasympathetic1predominance1
for1mild1hypertension
(diarrhea),1severe1depression1and1
Parkinsonism

Metatyrosine

Inhibits1tyrosine1hydroxylase1
inhibiting1synthesis1of1NE

Inoperative1pheochromocytoma

Drowsiness,1parasympathomimetic1
effects1(diarrhea),1anxiety,1
P.O.
crystalluria

Methyldopa

Prodrug@1transformed1to1
active1drug1that1acts1on1a21
adrenergic1receptors1to1
Large1doses1can1reach1CNS
decreases1centrally1mediated1
sympathetic1outflow

Essential1hypertension

Sedation,1lethargy,1GI1disturbances,1
parasympathetic1excess,1depressed1 P.O.
liver1function,1impotence

Celiprolol

B1

B1,1B2,1a1

B1,1a2

Guanadrel
Guanethidine

ADRENERGIC@NEURONAL@
BLOCKING@AGENTS

a2

Membrane1stabilizing
Partial1agonist,1membrane1
stabilizing
Partial1agonist=1intrinsic1
sympathometic1(usually1
agonist,1but1antagonists1in1the1
presence1of1an1agonist)

Lower1BP;1decrease1in1HR,1
contractility,1CO;1slowed1
conduction1in1atrial1&1AV1node;1
increased1refractory1period@1AV1
node;1bronchoconstriction;1
prolonged1hypoglycemia;1
decrease1in1plasma1FFAs;1
reduction1HDL1cholesteral;1
increase1LDL;1hypokalemia;1
vasodilation

Pharmacological1effects1depend1on1degree1of1
sympatho@adrenal1tone;1bronchoconstriction1is1
concern1in1asthmatics1&1COPD;1hypoglycemia1is1
concern1in1hypoglycemics1&1diabetics1*Use1
metoprolol1if1bronchoconstriction,1hypoglycemia,1
peripheral1vascular1disease1is1a1concern

Angina1Pectoris;1hypertension1
cardiac1arrhythmias;1congestive1
heart1failure;1pheochromocytoma;1
glaucoma1(Timolol);1hypertrophic@
obstructive1cardiomyopathy;1
hyperthyroidism;1migraine1
prophylaxis;1acute1panic1
symptoms;1substance1abuse1
withdrawal;1variceal1bleeding1in1
protal1hypertension

2nd1gen1
Metoprolol
selective
Beta@AdrenoF
receptor@
Carteolol
Antagonists 3rd1gen1non@ Carvedilol
selective
Labetalol

3rd1gen1
selective

B1,1B2

Peripherally1&1centrally

Guanadrel1has1higher1bioavailability,1can1
upregulate1receptors

P.O.