Adrenergic release inhibitor

A class of drugs that inhibit the release of adrenergic neurotransmitters

Adrenergic release inhibitors are a class of drugs that prevent the release of norepinephrine and other catecholamines from the sympathetic nervous system. These drugs are primarily used in the treatment of hypertension and certain types of cardiac arrhythmias.

Mechanism of Action

Adrenergic release inhibitors work by interfering with the normal process of neurotransmitter release from adrenergic neurons. This can be achieved through various mechanisms, such as blocking the vesicular monoamine transporter (VMAT), inhibiting the fusion of synaptic vesicles with the presynaptic membrane, or depleting the stores of neurotransmitters within the neuron.

Examples

One of the most well-known adrenergic release inhibitors is guanethidine, which is used to manage hypertension. Guanethidine works by entering adrenergic neurons and preventing the release of norepinephrine, leading to decreased sympathetic activity and lowered blood pressure.

Clinical Uses

Adrenergic release inhibitors are primarily used in the management of hypertension. By reducing the release of norepinephrine, these drugs decrease peripheral vascular resistance and lower blood pressure. They may also be used in the treatment of certain types of cardiac arrhythmias, where excessive sympathetic activity is a contributing factor.

Side Effects

The use of adrenergic release inhibitors can lead to several side effects due to their action on the sympathetic nervous system. Common side effects include orthostatic hypotension, bradycardia, and fatigue. Patients may also experience nasal congestion and gastrointestinal disturbances.

Related pages

• Adrenergic receptor
• Sympathetic nervous system
• Hypertension
• Cardiac arrhythmia

Gallery

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  Structure of Guanethidine