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DIRECT ADRENOMIMETICS

3.2.1.Mixed action Adrenomimetics

List of drugs

Epinephrine hydrochloride

Dopamine hydrochloride

Mechanism of action of epinephrine: direct stimulation of α1, α2, β1, β2- adrenoreceptors.

Pharmacological effects of epinephrine:

Type of receptors Organ Effect
Stimulation of α1- adrenoreceptors Eye Dilation of pupil (midriasis)
Blood vessels Constriction (due to contraction of smooth muscles of blood vessels)
Stimulation of α2- adrenoreceptors Blood vessels Constriction (due to contraction of smooth muscles of blood vessels)
Stimulation of β1- adrenoreceptors Heart Increasing of heart rate, heart contractility, heart conductance and heart excitability
Stimulation of β2- adrenoreceptors Bronchi Dilation (due to relaxation of smooth muscles of bronchi)
Uterus Relaxation (due to relaxation of smooth muscles of uterus)
Mast cells Inhibition of degranulation (i.e. inhibition of releasing of histamine from mast cells)

Indications for epinephrine:

1. Bronchospasm (relieving).

Epinephrine → stimulation of β2- adrenoreceptors → dilation of bronchi → relieving of bronchospasm

2. Hypoglycemic coma

Epinephrine → α1, α2, β1, β2- adrenoreceptors → increasing of the glucose level in the blood (due to disruption of glycogen in the liver etc.) → relieving of hypoglycemic coma.

3. Anaphylactic (allergic) shock

Epinephrine → stimulation of β2- adrenoreceptors → inhibition of degranulation of mast cells → relieving of anaphylactic (allergic) shock.

Side effects:

Epinephrine can produce cardiac arrhythmias.

Mechanism of action of dopamine: mostly direct stimulation of D1-receptors (dopamine receptor type 1) and α1- adrenoreceptors.

Pharmacological effects of dopamine: iincreasing of heart contractility + dilation of blood vessels.

Indications for dopamine:

1. Shocks of different aetiology (e.g. cardiogenic shock etc.)

 

3.2.2. Alfa-adrenomimetics

List of drugs

α1, α2- adrenomimetics: Norepinephrine bitartrate

α1- adrenomimetics: phenylephrine hydrochloride

α2- adrenomimetics: naphazoline hydrochloride

Mechanism of action

Phenylephrine produces direct stimulation of α1-adrenoreceptors.

Naphazoline produces direct stimulation of α2-adrenoreceptors

Pharmacological effects:

 

for phenylephrine:

 

Type of receptors Organ Effect
Stimulation of α1- adrenoreceptors Eye Dilation of pupil (midriasis)
Blood vessels Constriction (due to contraction of smooth muscles of blood vessels)

 

for naphazoline:

 

Type of receptors Organ Effect
Stimulation of α2- adrenoreceptors Blood vessels Constriction (due to contraction of smooth muscles of blood vessels)

 



Indications

1. Acute hypotension (circulatory collapse) – relieving

Phenylephrine → stimulation of α1-adrenoreceptors → constriction of blood vessels → increasing of arterial pressure

2. Rhinitis

Naphazoline → stimulation of α2-adrenoreceptors → constriction of blood vessels → decreasing of running nose

 

 

3.2.3. Beta-adrenomimetics

List of drugs

β1, β2- adrenomimetics: isoprenaline sulfate

β1- adrenomimetics: dobutamine hydrochloride

β2- adrenomimetics: fenoterol, salbutamol

Mechanism of action

Isoprenaline sulfate produces direct stimulation of β1, β2- adrenoreceptors.

Dobutamine produces direct stimulation of β1- adrenoreceptors.

Fenoterol, salbutamol produce direct stimulation of β2- adrenoreceptors

Pharmacological effects:

 

for isopreneline:

 

Type of receptors Organ Effect
Stimulation of β1- adrenoreceptors Heart Increasing of heart rate, heart contractility, heart conductance and heart excitability
Stimulation of β2- adrenoreceptors Bronchi Dilation (due to relaxation of smooth muscles of bronchi)
Uterus Relaxation (due to relaxation of smooth muscles of uterus)
Mast cells Inhibition of degranulation (i.e. inhibition of releasing of histamine from mast cells)

 

for dobutamine:

 

Type of receptors Organ Effect
Stimulation of β1- adrenoreceptors Heart Increasing of heart rate, heart contractility, heart conductance and heart excitability

 

for fenoterol, salbutamol:

 

Type of receptors Organ Effect
Stimulation of β2- adrenoreceptors Bronchi Dilation (due to relaxation of smooth muscles of bronchi)
Uterus Relaxation (due to relaxation of smooth muscles of uterus)
Mast cells Inhibition of degranulation (i.e. inhibition of releasing of histamine from mast cells)

 

Indications

 

  1. Acute heart failure

Dobutamine → stimulation of β1- adrenoreceptors → increasing of heart rate, heart contractility, heart conductance and heart excitability → relieving of acute heart failure

  1. Bronchospasm (prophylaxy and relieving)

Isopreneline, Fenoterol, Salbutamol → stimulation of β2- adrenoreceptors → dilation of bronchi → prophylaxy and relieving of bronchospasm

  1. Relaxation of uterus to prevent preterm labor (delivery) of child.

Isopreneline, Fenoterol, Salbutamol → stimulation of β2- adrenoreceptors → relaxation of uterus → prevention of preterm labor (delivery) of child.

 

 


Date: 2015-12-18; view: 848


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