Cathecolamine,

sympathomimetic
drugs & adrenergic
receptor antagonist
By : dr. Nur Hesti Kusumasari
Bagian Farmakologi
FK Univ. Malahayati

Cathecolamine,
sympathomimetic drugs
Cathecolamines released by the sympathetic
nervous system and adrenal medulla
Norepinephrine is the major neurotransmitter in
the peripheral sympathetic nervous system
Epinephrine is the primary hormone secreted by
the adrenal medulla
The sympathomimetics are divided into subgroup
on the basis of their spectrum (, , or dopamine
receptor affinity) or mode of action (direct or
indirect)

Cathecolamine,
sympathomimetic drugs
Action of cathecolamine & sympathomimetic
drugs :
1) Peripheral excitatory action (smooth muscle :
blood vessels supplying skin, mucous
membranes, salivary&sweat glands)
2) Peripheral inhibitory action (smooth muscle :
wall of the gut, bronchus, blood supplying
skeletal muscle)
3) Cardiac excitatory action
HR & force of contraction

Cathecolamine,
sympathomimetic drugs
4) Metabolic action
glicogenolysis in liver & muscle
5) Endocrine action
seretion of insulin, renin & pituitary
hormones
6) CNS action
Respiratory stimulation, psychomotor
activity, reduction in appetite

Cathecolamine,
sympathomimetic drugs
7) Presynaptic action
Inhibition or facilitation of the release
neurotransmitters (epinephrine &
acetylcholine)

Cathecolamine,
sympathomimetic drugs
Organ System Effect :
CNS
Have a spectrum of stimulant effect (eg, amphetamine) :
anorexia, euphoria, and insomnia
Eye
dilator pupillary (mydriasis), IOP by non selective
agonist
Bronchi
relaxing bronchial muscle by 2 agonist
Gastrointestinal Tract
activation of and receptor leads to relaxation

Cathecolamine,
sympathomimetic drugs
Genitourinary Tract
increase sphincter tone (). Uterine relaxation
in pregnant women near term (2 agonist)
Vascular system
depend on their dominant receptor
1 agonists (eg, phenylephrine) constrict skin
& splanchnic blood vessel and peripheral
vasc resistane & venous return

Cathecolamine,
sympathomimetic drugs
2 agonist (eg, clonidine) vasoconstriction (iv or
topically), accumulate in the CNS and
sympathetic outflow and blood pressure
(orally)
agonist (2 agonist eg, terbutaline) arterial
tone in the skeletal muscle vasc bed &
peripheral vasc resistane and arterial blood
pressure. 1 have a little effect on vessels
Dopamine vasodilation in the splanchnic and
renal vasc bed

Cathecolamine,
sympathomimetic drugs
Heart
rate of cardiac pacemaker (normal and
abnormal), AV node conduction, ardia
force(1 and 2)
Cardiovacular actions
cause a reflex increase in vagal outflow ( and
1)
Metabolic and hormonal effect
renin secretion (1), insulin secretion (2)
and glycogenolysis in the liver, stimulate
lipolysis

Cathecolamine,
sympathomimetic drugs
Clinical Uses
Anaphylaxis
Epinephrine is the DOC for the treatment of
anaphylactic shock
CNS
Amphetamine is widely used and abused for their
CNS effects. Indications : narcolepsy, attention
deficit disorder, weight reduction.
Abused: deferring sleep, mood-elevating,
euphoria.

Cathecolamine,
sympathomimetic drugs
Eye
agonist (eg, phenylephrine) used to produce
mydriasis without cycloplegia), reduce
conjunctival itching and congestion e.c irritation or
allergy (Topically). Epinephrine used for glaucoma
Bonchi
2-selective agonists are DOC in the treatment of
acute asthmatic bronchoconstriction. Short ating
(eg, terbutaline, albuterol, metaproterenol) for
acute episodes, and long acting (eg, salmeterol)
for prophylaxis

Cathecolamine,
sympathomimetic drugs
Cardiovascular Applications
Acute heart failure and shock (1 agonists
increase in blood fllow)
Genitourinary Tract
2-agonists (ritodrine, terbutaline) are used to
suppress premature labor, but the cardiac
stimulation may be hazardous to mother and
fetus.
Ephedrine are used to improve urinary
continence in children and the elderly with
enuresis

Adrenergic Receptor
antagonists (Adrenoceptor
Blockers)
Separately into : Alpha-blockers and
Beta-blockers

Alpha-blockers
Classification :
1) Irreversible, long acting
eg, phenoxibenzamine is 1 selective
2) Reversible, short acting
eg, phentolamine is a competitive, reversible
blocking agent, nonselective
3) Alpha1 selective
eg, Prazosin, terazosin, doxazosin are selective,
reversible 1 blockers
4) Alpha2 selective
eg, Yohimbine, rauwolscine are 2 selective
competitive antagonists

Alpha-blockers
Pharmacokinetics
These drugs are all active by the oral as
well as parenteral route
Duration of action :
Phenoxybenzamine (48h)
Phentolamine (2-4 h)
Alpha1 selective blockers (8-24 h)

Alpha-blockers
Pharmacological Effect
Nonselective blockers : reduction in
vascular tone with a reduction of both
arterial and venous pressure
Selective blockers: reducing blood
pressure

Alpha-blockers
Clinical Uses
Nonselective blockers:
Phenoxybenzamine used in the presurgical
management of phaechromocytoma (to reduce
hypertension)
Penile erection in men with erectile dysfunction
(phentolamine or yohimbine)
Selective blockers:
used in hypertension (prazosisn, terazosin,
doxazosin)
prevention in urinary retention in men with BPH

Beta Blockers
Classified into subgroup on the basis of
1 selectivity, partial agonis activity, local
anesthetic action and lipid solubility.
1 receptor selectivity (1 blocks > 2
blocks) eg, acebutolol, atenolol, esmolol,
metaprolol is advantage when treating in
patient with asthma