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UNIT 7 DRUGS STIMULATING ADRENERGIC NEUROTRANSMISSION Adrenergic agonists (adrenomimetics)

Note:

Drugs of this class mimic the effects of the sympathetic nervous system by activating adre-noceptors or inducing the release of endogenous norepinephrine.

1. TOPICS TO DISCUSS

1. Types and subtypes of adrenoceptors and their main localizations in organs and tissues. Effects of stimulation of adrenoceptors. Transduction pathways in cardiomyocytes and smooth muscle cells. Diagram of adrenergic synapse with localization of adrenoceptors (presynaptic, postsynaptic, and nonsynaptic).

2. Classification of adrenergic agonists.

3. Agonists of a1-adrenoceptors. Effects of a1-adrenomimetics on the tone of arterial vessels, arterial blood pressure, and heart rate. Therapeutic uses and main adverse effects of a1-adrenomimetics. Mechanism of reflex bradycardia caused by a1-adrenomimetics (diagram of baroreflex).

4. Agonists of a2-adrenoceptors used as nasal de-congestants. Pharmacological effects of cloni-dine (action on vascular tone, heart rate and contractility, arterial blood pressure). Mechanisms of its hypotensive action (using the diagrams of baroreflex and adrenergic synapses). Therapeutic uses and main adverse effects.

5. Pharmacological effects and therapeutic use of β1-adrenomimetics. Dobutamine and dopamine (action on contractility and heart rate). Dose-dependent action of dopamine on arterial vascular tone (renal and mesenteric vascular beds).

6. Selective β2-adrenomimetics. Their main pharmacological effects on bronchial tone, tone of the myometrium, tone of arterial vessels, and heart rate. Therapeutic uses and main adverse effects. The main difference between salbutamol, salmeterol and formoterol. β3-adrenomimetic mirabegron. The main pharmacological effects and therapeutic uses.

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