Cholinergic Neurotransmitters

• Cholinergic Neurotransmitters
• Acetylcholine
• Cholinergic receptors

Parasympathomimetic agents

• Parasympathomimetic Agents
• Classification of Parasympathomimetic Agents

Various Direct-Acting Parasympathomimetic Agents

• Acetylcholine
• Carbachol*
• Bethanechol
• Methacholine
• Pilocarpine

Various Indirect-Acting Agents (Cholinesterase Inhibitors)

• Physostigmine
• Neostigmine*
• Pyridostigmine
• Edrophonium Chloride
• Tacrine Hydrochloride
• Ambenonium Chloride
• Isofluorphate (DFP – Diisopropyl fluorophosphate)
• Echothiophate Iodide
• Parathion
• Malathion

Cholinesterase Reactivator

• Pralidoxime Chloride (2-PAM)

Cholinergic Blocking agents

• Cholinergic Blocking Agents (Cholinolytics/Anticholinergics)

Solanaceous Alkaloids AND Analogues

• Atropine Sulfate
• Hyoscyamine Sulfate
• Scopolamine Hydrobromide
• Homatropine Hydrobromide
• Ipratropium Bromide*

Various Synthetic Cholinergic Blocking Agents

• Tropicamide
• Cyclopentolate Hydrochloride
• Clidinium Bromide
• Dicyclomine Hydrochloride*
• Glycopyrrolate
• Methantheline Bromide
• Propantheline Bromide
• Benztropine Mesylate
• Orphenadrine Citrate
• Biperiden Hydrochloride
• Procyclidine Hydrochloride*
• Tridihexethyl Chloride
• Isopropamide Iodide
• Ethopropazine Hydrochloride

Other Units of Medicinal Chemistry I

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Medicinal Chemistry I

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Other Subjects of B Pharmacy 4th Semester

Cholinergic Neurotransmitters and Agents – Summary

Unit III explores the pharmacology of cholinergic neurotransmitters and their corresponding agents that act on the parasympathetic nervous system. It begins with the biosynthesis and catabolism of acetylcholine, a key neurotransmitter responsible for transmitting nerve impulses in cholinergic neurons.

The unit explains the cholinergic receptors, divided into muscarinic and nicotinic types, and their distribution in various organs. It then focuses on parasympathomimetic agents, both direct-acting (e.g., acetylcholine, methacholine, carbachol, bethanechol, pilocarpine) and their structure-activity relationships (SAR).

Further, it details indirect-acting cholinergic agents, specifically cholinesterase inhibitors. These are classified into reversible (e.g., neostigmine, physostigmine, edrophonium) and irreversible inhibitors (e.g., isofluorophate, echothiophate, parathion, malathion). These drugs prevent the breakdown of acetylcholine, enhancing its action at synapses. Additionally, pralidoxime chloride is covered as a cholinesterase reactivator, used in poisoning cases.

The unit also includes cholinergic blocking agents, highlighting SAR of cholinolytics. These include natural alkaloids like atropine and scopolamine, as well as synthetic analogues like ipratropium, dicyclomine, glycopyrrolate, and benztropine. These agents block acetylcholine at muscarinic receptors, useful in treating conditions like asthma, peptic ulcers, and Parkinson’s disease.

Overall, this unit gives a thorough understanding of cholinergic pharmacology and its clinical applications.

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