Chapter 7: Adrenergic Antagonists

Drug

Actions

Recepto
r

Therapeutic
Uses

Pharmacokinet
ics

Adverse Effects

Phenoxybenza -irreversibly and noncompetitively binds to

mine

Nonselect
ive blocker

-single
administration
can last for 24
hours
-after
administration it
takes a few hours
before actions
develop

-postural
hypotension
-nasal stuffiness
-nausea
-vomiting
-inhibit ejaculation
-induce reflex
tachycardia

-administration of
EPINEHPRINE in the
presence of this drug
causes decrease in
systemic BP
-actions of NE, are
diminished, not
reversed
-has to effect of
ISOPROTERENOL
-contraindicated in
patients with
decreased coronary
perfusion

Phentolamine

-competitive blocker
-EPINEPHRINE reversal

Nonselect
ive blocker

-Chronic
management of
pheochromocyto
ma
-Pre-surgical
administration
for
pheochromocyto
ma to avoid
hypertensive
crisis
-Raynauds
disease
-Autonomic
hyperreflexia
-Short
management of
pheochromocyto
ma

-single
administration
can last for 4
hours

-contraindicated in
patients with
decreased coronary
perfusion

-competitive blockers
- Tamsulosin: acts on 1A
receptors on SM of
prostate
-decrease the peripheral
vascular resistance and
lower arterial BP
-First-pass

Selective
1
blockers

-Prazosin,
Terazosin,
Doxazosin:
treatment of
HTN
-Tamsulosin,
Alfuzosin:
treatment of

-Doxazosin
excreted in feces,
and is the longest
acting of all these
drugs
-Rest of the drugs
are excreted in
urine

-Postural
hypotension
-Reflex cardiac
stimulation and
tachycardia
-Arrhythmias
-Anginal pain
-Dizziness
-Lack of energy
-Nasal congestion
-Headache
-Drowsiness
-Orthostatic
hypotension
-Inhibition of

the postsynaptic
receptors
-prevents
vasoconstriction of
peripheral BV, causing
reflex tachycardia
-blockade of presynaptic
inhibitory 2 receptors
can cause increased
cardiac output
-reverse the -agonist
actions of EPINEPHRINE

Prazosin
Terazosin
Doxazosin
Alfuzosin
Tamsulosin

Sweta Patel

Page 1

Others

-minimal changes in
CO, RBF, GFR
-Tamsulosin has least
effect on BP
-if used as
monotherapy in HTN,
they can cause CHF
-Prazosin can be used

Chapter 7: Adrenergic Antagonists

Yohimbine

Propranolol

Sweta Patel

(exaggerated
orthostatic hTN,
resulting in syncope)
effect occurs with 1st
administration of the
drugs, therefore should
be given at bedtime
-competitive
-works at the level of
the CNS to increase
sympathetic outflow to
the periphery
-diminishes CO due to
negative chronotropic
and inotropic effect
-decreased BP leads to
reflex peripheral
vasoconstriction
-reduced BP causes
decreased renal
perfusion, leading to
sodium retention
-depresses SA and AV
activity, resulting in
bradycardia
-causes
bronchoconstriction
-decreased
glycogenolysis and
glucagon secretion
-blocks the action of
ISOPROTERENOL on CVS
Page 2

BPH

Selective
2
blocker

-Sexual
stimulant
-Raynauds
disease

Nonselect
ive antagonis
t

-Chronic
management of
angina
-Attenuating
supraventricular
cardiac
arrhythmias
-HTN (Decreased
CO, inhibition of
renin release,
decreased
sympathetic
outflow from
CNS)
-Chronic tx of
glaucoma
(decreased
secretion of
aqueous humor
by ciliary body)

ejaculation and
retrograde
ejaculation

with a diuretic for

antihypertensive
effect

-contraindicated in
CNS and CV
conditions

-CIMETIDINE,
FLUOXETINE,
PAROXETINE,
RITONAVIR
interfere with
metabolism of the
drug
-BARBITURATES,
PHENYTOIN,
RIFAMPIN
stimulate its
metabolism

Bronchoconstrictio
n (causes death in
asthmatics)
-Arrhythmias
-impaired sexual
activity in some
-Fasting
hypoglycaemia

-contraindicated in
patients with COPD
or asthma
-often combined with
a diuretic to prevent
Na+ retention
-pronounced
hypoglycaemia may
occur after insulin
injection in a Type I
diabetic
-in the presence of
these drugs,
EPINEPHRINE doesnt
lower diastolic
pressure or stimulate
the heart
-Protective effect on
the myocardium

Chapter 7: Adrenergic Antagonists

Timolol
Nadolol

-Timolol: reduces
production of aqueous
humor in the eye

Nonselect
ive antagonis
t

Acebutolol
Atenolol
Metoprolol
Esmolol

-antagonize 1
receptors at doses 50to 100- fold less than
those required to block
2 receptors

Selective
1
antagonis
ts

Pindolol
Acebutolol

-Intrinsic
sympathetomimetic
activity
-Stimulate the
receptor to which they
are bound, but block
stimulation of the

Partial
agonists
(weak
stimulatio
n of 1
and 2)

Sweta Patel

Page 3

-Prophylactic for
migraine
-Acute
hyperthyroidism
-Given after MI,
it reduces infarct
size
-Timolol: chronic
open-angle
glaucoma
-Timolol:
systemic tx of
HTN
-Lower BP in
HTN
-Increase
exercise
tolerance in
angina
-Useful in
diabetic HTN pts
receiving insulin
or oral
hypoglycaemic
agents
-HTN in pts with
moderate
bradycardia
-Valuable in the
treatment of
diabetics

-Nadolol: very
long duration of
action

-more potent than

PROPRANOLOL

-Esmolol: short
lifetime, therefore
IV during surgery
or diagnostic
procedure

-cardioselectivity
pronounced at low
doses, lost at high
doses
-may be used in
asthmatics with
careful monitoring

-minimize the
disturbances of lipid
and carbohydrate
metabolism seen
with other -blockers

Chapter 7: Adrenergic Antagonists

Labetalol
Carvedilol

Reserpine

Guanethidine

Sweta Patel

receptor by
EPINEPHRINE and NE
-Produces peripheral
vasodilation, thereby
reducing BP
-Carvedilol: decreases
lipid peroxidation and
vascular wall thickening

-Blocks the Mg2+/ATPdependent transport of

NE, DA, serotonin from
the cytoplasm into
storage vesicles
-Sympathetic function is
impaired
-Blocks the release of
stored NE and displaces
NE from storage
vesicles

Page 4

and
antagonis
ts

-Useful in
treating HTN pts
for whom
increased
peripheral
vascular
resistance is
undesirable
(elderly, black
ppl)
-Labetalol:
pregnancyinduced HTN,
hypertensive
emergencies
-CHF

-Labetalol may be
administetered
through IV and
can rapidly lower
BP

-Orthostatic hTN
-Dizziness

-Slow onset
-Long duration of
action
-Effects that
persist for many
days after
discontinuation
-Orthostatic
hypotension
-Interferes w/ male
sexual function
-Hypertensive crisis
in pts with
pheochromocytom

Chapter 7: Adrenergic Antagonists

a

Sweta Patel

Page 5