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Related Concept Videos

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

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: Pharmacokinetics01:31

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: Pharmacological Actions00:59

Direct-Acting Cholinergic Agonists: Pharmacological Actions

Direct-acting cholinergic agonists exert their pharmacological actions by mimicking the effects of acetylcholine on postsynaptic muscarinic receptors to generate parasympathetic responses. These agents elicit a range of physiological responses, including cardiovascular effects. For example, activation of muscarinic receptors induces bradycardia, decreased cardiac output, reduced peripheral resistance, and consequent hypotension. In the eye, stimulation of M3 receptors leads to smooth muscle...
Direct-Acting Cholinergic Agonists: Therapeutic Uses01:11

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 syndrome.
Indirect-Acting Cholinergic Agonists: Pharmacological Actions01:30

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...
Cholinergic Antagonists: Pharmacological Actions01:28

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...

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Related Experiment Video

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A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development
07:02

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Cholinergic drug interactions and heat tolerance

C B Matthew1, J F Glenn, W D Bowers

  • 1US Army Research Institute of Environmental Medicine, Natick, MA 01760.

Life Sciences
|January 1, 1994
PubMed
Summary

Subchronic administration of pyridostigmine bromide (PY) enhances heat tolerance in rats by improving thermoregulation through increased evaporative cooling. This effect, seen with PY and atropine (AT), mimics heat acclimation.

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A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development
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Area of Science:

  • Environmental Physiology
  • Pharmacology
  • Toxicology

Background:

  • Cholinergic compounds can have varied effects based on exposure duration.
  • Pyridostigmine bromide (PY) is used for organophosphorus poisoning prophylaxis, with atropine (AT) administration influencing its efficacy.
  • Atropine (AT) increases core body temperature in heat-exposed subjects.

Purpose of the Study:

  • To investigate if atropine's (AT) anticholinergic potency is modified after pyridostigmine bromide (PY) administration.
  • To assess the effects of acute versus subchronic PY administration on AT's thermoregulatory effects in heat-stressed rats.

Main Methods:

  • Rats received acute or subchronic (2 weeks) intravenous or osmotic pump administration of saline (SAL) or PY.
  • Following PY or SAL, rats were treated with SAL or AT (200 ug/kg).
  • Rats were then exposed to 41.5°C until core temperature reached 42.6°C, with heat tolerance and weight loss measured.

Main Results:

  • Subchronic PY administration significantly improved heat tolerance compared to acute PY.
  • Subchronic PY + AT treatment also resulted in greater heat tolerance than acute PY + AT.
  • % weight loss, indicating evaporative cooling, was higher in subchronically treated rats.

Conclusions:

  • Subchronic administration of anticholinesterase agents like PY can enhance thermoregulation and heat tolerance.
  • The observed improvements in heat tolerance resemble physiological changes associated with heat acclimation.
  • This suggests potential for subchronic PY to mitigate heat stress effects.