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SIMPLICIFIED VERSION

ADRENONEGATIVE DRUGS)

 

SYMPATHOLYTICS

List of drugs

Reserpine

Guanethidine

Mechanism of action

These drugs produce inhibition of releasing of norepinephrine from presynaps, As result, there will be the decreasing of norepinephrine concentration in the synaptic cleft and absence of stimulation of α1, α2, β1, β2- adrenoreceptors.

Pharmacological effects

Previous time you studied the pharmacological effects of Indirect adrenomimetics (see my previous material). For today topic «Sympatholytics» pharmacological effects will be strongly opposite (see table):

 

Type of receptors Organ Effect
Absence of stimulation of α1- adrenoreceptors Blood vessels Dilation (due to relaxation of smooth muscles of blood vessels)
Absence of stimulation of α2- adrenoreceptors Blood vessels Dilation (due to relaxation of smooth muscles of blood vessels)
Absence of stimulation of β1- adrenoreceptors Heart Decreasing of heart rate, heart contractility, heart conductance and heart excitability
Absence of stimulation of β2- adrenoreceptors Bronchi Constriction (due to contraction of smooth muscles of bronchi)

 

Indications

1. Hypertension (chronic treatment)

Reserpine, Guanethidine → absence of stimulation of α1, α2-adrenoreceptors → dilation of blood vessels + absence of stimulation of β1-adrenoreceptors → decreasing of heart rate and heart contractility = due to dilation of blood vessels and decreasing of heart rate and heart contractility there will be the decreasing of arterial pressure.

2. Tachyarrhythmia (tachycardia)

Reserpine, Guanethidine → absence of stimulation of β1-adrenoreceptors → decreasing of heart rate → inhibition of tachyarrhythmia (tachycardia).

 

ALFA-ADRENOBLOCKERS

List of drugs

α1, α2-adrenoblockers: phentolamine mesylate

α1- adrenoblockers: prazosin hydrochloride

Mechanism of action

Phentolamine produces direct blockage of α1, α2-adrenoreceptors.

Prazosin produces direct blockage of α1-adrenoreceptors

Pharmacological effects:

Previous time you studied the pharmacological effects of Alfa-adrenomimetics (see my previous material). For today topic «Alfa-adrenoblockers» pharmacological effects will be strongly opposite (see table):

 

for phentolamine:

 

Type of receptors Organ Effect
Blockage of α1- adrenoreceptors Blood vessels Dilation (due to relaxation of smooth muscles of blood vessels)
Blockage of α2- adrenoreceptors Blood vessels Dilation (due to relaxation of smooth muscles of blood vessels)

 

for prazosin:

 

Type of receptors Organ Effect
Blockage of α1- adrenoreceptors Blood vessels Dilation (due to relaxation of smooth muscles of blood vessels)

 



Indications

1. Relieving of hypertensive crises

Phentolamine → blockage of α1, α2-adrenoreceptors → dilation of blood vessels → decreasing of arterial pressure.

2. Hypertension (chronic treatment)

Prazosin → blockage of α1-adrenoreceptors → dilation of blood vessels → decreasing of arterial pressure.

 

 


Date: 2015-12-18; view: 649


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