Adrenergic Drugs

-Roshan

Sub-Topics

Introduction
Adrenergic Transmission
Adrenergic Receptors
Classification of Adrenergic drugs
Administration & preparations
Some Important Drugs
Therapeutic Uses
Adverse effects and contraindications

Introduction
The sympathetic nervous system is an important regulator of
the activities of organs such as the heart and peripheral
vasculature, especially in responses to stress.
The ultimate effects of sympathetic stimulation are mediated
by release from nerve terminals of norepinephrine that serves
to activate the adrenoceptors on postsynaptic sites.
Also, in response to a variety of stimuli such as stress, the
adrenal medulla releases epinephrine, which is transported in
the blood to target tissues
Drugs that mimic the actions of epinephrine or
norepinephrine are called sympathomimetic drugs

Steps Involved in Adrenergic

Transmission
1.
2.
3.
4.
5.
6.

Synthesis of CAs
Storage of CAs
Release of CAs
Binding to receptor
Uptake of CAs
Metabolism of CAs

Synthesis of CAs
Phenylalanine

In liver
Tyrosine

In adrenergic
neuronal
cytoplasm

DOPA

Dopamine

Inside vesicles
Noradrenaline

In adrenal medulla cells

Adrenaline

Adrenergic transmission

Adrenergic Receptors
Membrane bound G-coupled Receptors
Functions by or the intracellular
production of second messengers(cAMP or
IP3/DAG)
Ahlquist(1948) classified the Adrenergic
receptors to and types.

The Two Main Receptor types

Criteria

1.Rank order of potency of

agonist

Adr NA > Iso

Iso> Adr > NA

2. Antagonist(Important)

Phenoxybenzamine

Propranolol

3.Effector Pathway

IP3/DAG,cAMP , K+
channel

cAMP , Ca+ channel

4. Subtypes

12

123

-Receptors
Criteria

Location

Postjunctional on effector
organs

Prejunctional on nerve
ending, Brain, Pancreas(
cells),blood vessels

Function subserved

GU Smooth muscle-contraction
Vasoconstriction
Gland-secretion
Gut-relaxation
Liver-glycogenolysis
Heart-arrhythmia

Inhibition of Transmitter
release
Vasoconstriction
Decreased central
sympathetic flow
Decreased insulin release
Platelet aggregation

Selective Agonist

Phenylephrine,
Methoxamine

Clonidine

-Receptors
1

Location

Heart , JG cells in
Kidney

Eye,Bronchi,GIT,
Adipose
Liver,blood vessels,
urinary tract, uterus

Selective Agonist

Dobutamol

Salbutamol,
Terbutalin

BRL 37344

NA<< Adr

NA>Adr

Relative potency of NA Adr

NA and Adr

3(Atypical)

Areas containing Adrenergic receptors

Overall Adrenergic Responses

Classification of Adrenergic Drugs

Adrenergic Drugs
Pressor
Agents:

CNS
Stimulants:

Nasal
decongesants:

Broncho
dilators:

Cardiac
stimulants:

1.Dexampheta
mine

1.Phenylephrine

1.Formeterol

1.Adrenaline

1.Phenylepherine

2.Pseudoephedrine

2.Isoprenaline

2.Isoprenaline

2.Ephedrine

2.Amphetamin
e

3.Phenyl
propanolamine

3.Salbutamol

3.Dobutamine

3.Noradrenaline

Isoxsuprine

4.Terbutalin

4.Naphazoline

4.Dopamine

Salbutamol

5.Salmetrol

5.Oxymetazoline

5.Methoxamine

Terbutaline

6.Bambuterol

3.Methampheta
mine

6.Xylometazoline

2.Dexfenfluramine

Uterine
relaxants
&Vasodilators
:

3.Sibutramine

Ritodrine

Anorectics:
1.Fenfluramine

6.Mephentermine

Administration & Preparations

CAs are absorbed from the intestine but are rapidly degraded
by MAO and COMT present in the intestinal wall and liver.
Hence orally inactive.
1. Adrenaline: For systemic action0.2-0.5mg s.c.,i.m.
As local vasoconstrictor 1 in 200,000 to 1 in
100,000 added to lidocaine
2. Noradrenaline: 2-4g/min i.v infusion.
Rarely used as a pressor agent.
3. Isoprenaline(Isoproterenol): 20mg sublingual,
1-2 mg i.m,
5-10g/min i.v infusion

Some important Drugs

Dopamine(DA):
Normal dose: CO & Systolic BP
Moderately high dose:
.
Positive ionotropic effect
Large Dose: Vasoconstriction
.
Ephedrine:
Alkaloid from Ephedra vulgaris
100 times less potent than Adr
Crosses into the brain.
.

Some important Drugs

Amphetamines:
Orally active synthetic compound
.
Have pharmacological profile as that of Ephedrine
Exert potent CNS stimulation and weaker
.
cardiovascular actions.
Stimulate respiratory centre
.
(especially when depressed)
Hunger is supressed by action on feeding centre in
hypothalamus.

Some important Drugs

Phenylepherine:
Selective 1 agonist.
Causes raise in BP .
Used as Nasal decongestant
.
Used to reduce IOP(Glaucoma) .
Used to produce mydriasis when .
cycloplegia is not required

Therapeutic uses
1.
2.
3.
4.
5.
6.
7.

Allergic disorders
Bronchial asthma and COPD
Cardiac Uses
Vascular uses
Glaucoma
Uterine relaxant
Insulin hypoglycemia

Adverse effects and contraindications

Transient restlessness, palpitation, anxiety,tremor, pallor may
occur after s.c./i.m. injection of Adr.
Marked rise in BP leading to cerebral haemorrhage ,
ventricular tachycardia/ fibrillation, angina, myocardial
infarction are the hazards of large doses or inadvertant i.v.
injection of Adr.
Adr is contraindicated in hypertensive, hyperthyroid and
angina patients.
Adr should not be given during anesthesia with halothane
(risk of arrhythmias) and to patients receiving blockers
(marked rise in BP can occur due to unopposed action) .