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Indirect-Acting Cholinergic Agonists: Pharmacological Actions

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

Indirect-acting cholinergic agonists, also known as anticholinesterases, exert their pharmacological effects by enhancing cholinergic transmission in various body parts, including the neuromuscular junction, autonomic cholinergic synapses, and the brain.
At the neuromuscular junction, these agents work by inhibiting the breakdown of acetylcholine, allowing it to remain bound to the receptor and bind to nearby receptors. This process leads to repetitive firing of the endplate, causing muscle...

Direct-Acting Cholinergic Agonists: Pharmacokinetics

Direct-Acting Cholinergic Agonists: Pharmacokinetics

Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...

Direct-Acting Cholinergic Agonists: Therapeutic Uses

Direct-Acting Cholinergic Agonists: Therapeutic Uses

Direct-acting cholinergic agonists have many therapeutic uses in various medical fields. Choline esters, including acetylcholine, have limited clinical utility due to their non-selectivity and short duration of action. Still, acetylcholine and carbachol are applied topically during ophthalmologic surgery to induce miosis. Pilocarpine, a muscarinic and ganglionic stimulator, effectively treats open-angle glaucoma and alleviates xerostomia and dry mouth caused by radiotherapy or Sjögren...

Cholinergic Antagonists: Pharmacological Actions

Cholinergic Antagonists: Pharmacological Actions

Antimuscarinic drugs block muscarinic receptors in multiple systems, including the gut, eye, smooth muscles, respiratory tract, cardiovascular, and central nervous systems. They produce similar effects with varying selectivity depending on the specific agent and tissue. Here are the key pharmacological actions of antimuscarinics:
Gastrointestinal Effects: Antimuscarinics reduce gut contractions, increase gastric emptying, and slow intestinal transit. They partly inhibit gastric acid secretion...

Cholinergic Receptors: Muscarinic

Cholinergic Receptors: Muscarinic

The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine.
The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+....

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Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice

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Cholinergic Capsules and Academic Admonitions.

Palmer Taylor¹

¹Department of Pharmacology, Skaggs School of Pharmacy and Pharmaceutical Sciences, and School of Medicine, University of California, San Diego, La Jolla, California 92093, USA;

Annual Review of Pharmacology and Toxicology

|January 7, 2021

Summary

This narrative details a 60-year academic career in health sciences, focusing on leadership roles in establishing pharmacology departments and pharmacy schools. It offers insights for navigating academic and industry career paths.

Keywords:

academic coordination in pharmacy and medicine acetylcholinesterase autobiography neurotransmission nicotinic acetylcholine receptors pharmacology teaching

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Area of Science:

Academic Health Sciences
Pharmacology
Pharmacy Education

Background:

A 60-year career in academic health sciences is presented, spanning graduate training to leadership positions.
The evolution of the Department of Pharmacology at the University of California, San Diego (UCSD) from a division to a standalone department is highlighted.
The establishment of the Skaggs School of Pharmacy and Pharmaceutical Sciences at UCSD is described.

Purpose of the Study:

To share experiences and insights from a career in academic health sciences.
To provide guidance for individuals considering opportunities in academic health sciences, the pharmaceutical industry, or government agencies.
To reflect on the challenges and successes in establishing new academic programs and departments.

Main Methods:

Retrospective narrative of a career spanning six decades.
Personal account of leadership roles in academic administration and program development.
Case study of departmental and school establishment within a medical university.

Main Results:

Successfully transitioned from a family pharmacy to leadership roles in medical and pharmacy schools.
Played a key role in the formation of the Department of Pharmacology and the Skaggs School of Pharmacy at UCSD.
Navigated significant academic, curricular, and accreditation challenges through collaborative efforts.

Conclusions:

Career progression in academic health sciences involves strategic decision-making and overcoming challenges.
Leadership in establishing new academic entities requires collaboration and creative problem-solving.
Personal experiences can serve as a valuable resource for aspiring professionals in related fields.