Adrenergic Drugs

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.
.

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.

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) .

Adrenergic Drugs

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Adrenergic Drugs

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Adrenergic Drugs

Steps Involved in Adrenergic

In adrenal medulla cells

The Two Main Receptor types

1.Rank order of potency of

Adr NA > Iso

Iso> Adr > NA

cAMP , Ca+ channel

Relative potency of NA Adr

Areas containing Adrenergic receptors

Overall Adrenergic Responses

Classification of Adrenergic Drugs

Administration & Preparations

Some important Drugs

Some important Drugs

Some important Drugs

Adverse effects and contraindications

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