Pharmaceutical and Medicinal Organic Chemistry - Adrenergic and Cholinergic Drugs

These flashcards cover key concepts related to adrenergic and cholinergic drugs, including mechanisms of action, drug classifications, and structure-activity relationships.

What are adrenergic agonists and how do they function?

Adrenergic agonists mimic norepinephrine and epinephrine effects, activating adrenergic receptors to produce a 'fight or flight' response.

What is the role of adrenergic antagonists?

Adrenergic antagonists block the effects of norepinephrine and epinephrine by binding to adrenergic receptors without activating them.

What are catecholamines and give examples?

Catecholamines are neurotransmitters that include norepinephrine (NE), epinephrine (E), and dopamine (DA).

How does the structure of phenylethylamine influence adrenergic activity?

Substituents on the phenylethylamine structure determine receptor selectivity and activity levels at alpha and beta adrenergic receptors.

What is the function of monoamine oxidase (MAO) in the context of catecholamines?

MAO metabolizes catecholamines like NE and E, leading to their rapid inactivation.

What are beta-blockers used for?

Beta-blockers are used to treat hypertension, angina, and arrhythmias by blocking beta-adrenergic receptors.

What are the effects of substituents on the aromatic ring in adrenergic drugs?

Hydroxyl groups at the 3' & 4' positions enhance adrenergic receptor activity for alpha and beta receptors.

What is the significance of selectivity in beta 2 agonists?

Beta 2 agonists, such as formoterol, are selective and not metabolized by COMT or MAO, leading to oral activity and long duration of action.

What are cholinergic agents and their main function?

Cholinergic agents stimulate the parasympathetic nervous system and mimic acetylcholine action.

What differentiates muscarinic receptors from nicotinic receptors?

Muscarinic receptors stimulate smooth muscle and slow heart rate, while nicotinic receptors affect skeletal muscle.

What is the IUPAC name of Epinephrine?

4-[(1R)-1-hydroxy-2-(methylamino)ethyl]benzene-1,2-diol.

What is the function of reversible acetylcholinesterase inhibitors?

They prevent the breakdown of acetylcholine, enhancing its activity at cholinergic receptors.

Name a specific non-selective beta-blocker.

Propranolol.

What modification enhances selectivity towards muscarinic receptors?

Introducing a methyl group at the alpha position of the ethylene bridge in cholinergic agents increases selectivity.

What is the role of atropine?

Atropine is a cholinergic antagonist that blocks the action of acetylcholine at muscarinic receptors.

How does drug structure impact pharmacokinetics and pharmacodynamics in adrenergic drugs?

The chemical structure influences absorption, metabolism, and overall activity of adrenergic drugs.