ADRENERGIC AGONISTS AND
PHARMACOLOGY OF
ADRENALINE
Dr. S P SRINIVAS NAYAK,
Assistant Professor, SUCP, HYD.
Telangana, India.
Classification of
Sympathomimetics/
Adrenergic Agonists
Classification of On the basis of their
therapeutic use:
1. Nasal decongestants:
Phenylephrine, xylometazoline,
pseudoephedrine, oxymetazoline, naphazoline
2. For allergic reactions
(anaphylactic shock): Adrenaline
3. To raise the blood pressure in shock:
Dopamine, noradrenaline,
ephedrine, phenylephrine,
methoxamine, mephentermine
4. As bronchodilator:
Salbutamol,
terbutaline,
salmeterol,
formoterol
5. As cardiac stimulant:
• Adrenaline, isoprenaline, dobutamine.
6. As CNS stimulant:
Amphetamine,
dextroamphetamine.
7. For local vasoconstrictor effect:
Adrenaline.
Adrenaline is used as a local haemostatic to
control bleeding following tooth extraction and
during surgical procedures in nose, throat,
larynx, or in cuts, injuries etc. because of its
vasoconstrictor effect.
• As anorexiant:
Dextroamphetamine,
mazindol,
phentermine,
sibutramine
ADRENALINE (EPINEPHRINE)
It is a catecholamine, which is secreted mainly by adrenal
medulla. Adrenaline is a direct acting nonselective adrenergic
agonist
PHARMACOLOGICAL ACTIONS OF
ADRENALINE
• 1. Cardiovascular system(CVS)
a. Heart: Adrenaline is a powerful cardiac stimulant
i. Increase in heart rate (positive chronotropic effect).
ii. Increase in myocardial contractility (positive inotropic
effect).
iii. Increase in conduction velocity (positive dromotropic
effect
b. Blood vessels and BP:
Blood vessels of the skin and mucous membranes are
constricted by adrenaline. It also constricts renal, mesenteric,
pulmonary and splanchnic vessels, but dilates the blood
vessels of skeletal muscle and coronary vessels .
2. RESPIRATORY SYSTEM:
Adrenaline rapidly relaxes (beta.2) bronchial
smooth muscle. It is a potent bronchodilator
but has a short duration of action. It inhibits the
release of inflammatory mediators from mast
cells (beta.2).
It also reduces secretions and relieves mucosal
congestion by vasoconstrictor effect (alpha.1).
3. Gastro intestinal tract(GIT)
• It relaxes the smooth muscle of the gut.
• It reduces the intestinal tone and peristaltic
movements.
• Mostly it causes
Constipation
4. Bladder:
• It relaxes the detrusor muscle and contracts
the sphincter. As a result, it may cause
difficulty in urination.
5. CNS:
• In therapeutic doses, adrenaline does not
cross the BBB and hence CNS effects are very
minimal.
• But in high doses, it may cause headache,
restlessness and tremor.
6. METABOLIC EFFECTS:
• Adrenaline increases the blood glucose level
by:
i. Stimulating hepatic glycogenolysis (beta2),
which is the predominant effect.
ii. Reducing insulin secretion.
iii. Decreasing the uptake of glucose by
peripheral tissues.
7. Other effects on each cell
• It reduces plasma K+ levels by promoting the
uptake of K+ into the cells, particularly into
the skeletal muscle.
• It causes hypokalemia
PHARMACOKINETICS
Adrenaline is not suitable for oral administration
because of its rapid inactivation in the GI mucosa
and liver.
Adrenaline can be given subcutaneously (s.c.). In
anaphylactic shock, the absorption of s.c.
adrenaline is very poor, hence given
intramuscularly.
In cardiac arrest, it is given intravenously. It does
not cross the BBB; is rapidly metabolized by COMT
and MAO and the metabolites are excreted in urine.
ADVERSE EFFECTS
• They are tachycardia, palpitation, headache,
restlessness, tremor and rise in BP.
• The serious side effects are cerebral haemorrhage and
cardiac arrhythmias.
• In high concentration, adrenaline may cause acute
pulmonary oedema due to shift of blood from systemic
to pulmonary circulation.
• Adrenaline is contraindicated in most of the
cardiovascular diseases such as hypertension, angina,
cardiac arrhythmias, CCF, etc.
• It should also be avoided in patients on beta-blockers
because it may cause hypertensive crisis and cerebral
haemorrhage due to unopposed action on vascular
alpha 1-receptors.
USES OF ADRENALINE
• Anaphylactic shock
• bronchial asthma
• Cardiac resuscitation, hypotension
• Prolongs the Duration of local anaesthesia
• controls Epistaxis and other capillary oozing
THANK YOU

Adrenaline pharmacology

  • 1.
    ADRENERGIC AGONISTS AND PHARMACOLOGYOF ADRENALINE Dr. S P SRINIVAS NAYAK, Assistant Professor, SUCP, HYD. Telangana, India.
  • 2.
    Classification of Sympathomimetics/ Adrenergic Agonists Classificationof On the basis of their therapeutic use: 1. Nasal decongestants: Phenylephrine, xylometazoline, pseudoephedrine, oxymetazoline, naphazoline
  • 3.
    2. For allergicreactions (anaphylactic shock): Adrenaline
  • 4.
    3. To raisethe blood pressure in shock: Dopamine, noradrenaline, ephedrine, phenylephrine, methoxamine, mephentermine
  • 5.
  • 6.
    5. As cardiacstimulant: • Adrenaline, isoprenaline, dobutamine.
  • 7.
    6. As CNSstimulant: Amphetamine, dextroamphetamine.
  • 8.
    7. For localvasoconstrictor effect: Adrenaline. Adrenaline is used as a local haemostatic to control bleeding following tooth extraction and during surgical procedures in nose, throat, larynx, or in cuts, injuries etc. because of its vasoconstrictor effect.
  • 9.
  • 10.
    ADRENALINE (EPINEPHRINE) It isa catecholamine, which is secreted mainly by adrenal medulla. Adrenaline is a direct acting nonselective adrenergic agonist
  • 11.
    PHARMACOLOGICAL ACTIONS OF ADRENALINE •1. Cardiovascular system(CVS) a. Heart: Adrenaline is a powerful cardiac stimulant i. Increase in heart rate (positive chronotropic effect). ii. Increase in myocardial contractility (positive inotropic effect). iii. Increase in conduction velocity (positive dromotropic effect b. Blood vessels and BP: Blood vessels of the skin and mucous membranes are constricted by adrenaline. It also constricts renal, mesenteric, pulmonary and splanchnic vessels, but dilates the blood vessels of skeletal muscle and coronary vessels .
  • 13.
    2. RESPIRATORY SYSTEM: Adrenalinerapidly relaxes (beta.2) bronchial smooth muscle. It is a potent bronchodilator but has a short duration of action. It inhibits the release of inflammatory mediators from mast cells (beta.2). It also reduces secretions and relieves mucosal congestion by vasoconstrictor effect (alpha.1).
  • 14.
    3. Gastro intestinaltract(GIT) • It relaxes the smooth muscle of the gut. • It reduces the intestinal tone and peristaltic movements. • Mostly it causes Constipation
  • 15.
    4. Bladder: • Itrelaxes the detrusor muscle and contracts the sphincter. As a result, it may cause difficulty in urination.
  • 16.
    5. CNS: • Intherapeutic doses, adrenaline does not cross the BBB and hence CNS effects are very minimal. • But in high doses, it may cause headache, restlessness and tremor.
  • 17.
    6. METABOLIC EFFECTS: •Adrenaline increases the blood glucose level by: i. Stimulating hepatic glycogenolysis (beta2), which is the predominant effect. ii. Reducing insulin secretion. iii. Decreasing the uptake of glucose by peripheral tissues.
  • 18.
    7. Other effectson each cell • It reduces plasma K+ levels by promoting the uptake of K+ into the cells, particularly into the skeletal muscle. • It causes hypokalemia
  • 19.
    PHARMACOKINETICS Adrenaline is notsuitable for oral administration because of its rapid inactivation in the GI mucosa and liver. Adrenaline can be given subcutaneously (s.c.). In anaphylactic shock, the absorption of s.c. adrenaline is very poor, hence given intramuscularly. In cardiac arrest, it is given intravenously. It does not cross the BBB; is rapidly metabolized by COMT and MAO and the metabolites are excreted in urine.
  • 20.
    ADVERSE EFFECTS • Theyare tachycardia, palpitation, headache, restlessness, tremor and rise in BP. • The serious side effects are cerebral haemorrhage and cardiac arrhythmias. • In high concentration, adrenaline may cause acute pulmonary oedema due to shift of blood from systemic to pulmonary circulation. • Adrenaline is contraindicated in most of the cardiovascular diseases such as hypertension, angina, cardiac arrhythmias, CCF, etc. • It should also be avoided in patients on beta-blockers because it may cause hypertensive crisis and cerebral haemorrhage due to unopposed action on vascular alpha 1-receptors.
  • 21.
    USES OF ADRENALINE •Anaphylactic shock • bronchial asthma • Cardiac resuscitation, hypotension • Prolongs the Duration of local anaesthesia • controls Epistaxis and other capillary oozing
  • 22.