Cholinomimetic alkaloids

CHOLINOMIMETIC ALKALOIDS

  • Cholinomimetic alkaloids  stimulate the muscarinic receptors of cells innervated by post ganglionic cholinergic nerves. They are also effective in chronically denervated tissue and are not dependent upon endogenous acetylcholine.
  • Pilocarpine, muscarine and arecoline are naturally occuring parasympathomimetic alkaloids with minimal nicotinic effects.

Pilocarpine

  • It is obtained from Pilocarpus jaborandi and Pilocarpus microphyllus.
  • It is a potent parasympathomimetic.
  • It produces all the muscarinic responses of acetylcholine.
      • Increases secretion of exocrine glands - salivary, sweat, mucous, gastric, pancreatic secretions.
      • Causes contraction of the gastrointestinal tract smooth muscles and increases peristalsis.
      • Pupillary constriction is the most important effect observed.

Arecoline

  • It is obtained from Areca catechu.
  • It has some nicotinic agonistic activity.
  • It has been used as an anthelmintic to paralyze tapeworms.
  • Acts on the muscarinic receptors of effector cells of glands, smooth muscle and myocardium. It is more potent than pilocarpine.
  • Depresses the heart rate and blood pressure and causes dyspnoea.
  •  Secretions of the glands of the digestive tract are increased and peristalsis is also increased

Muscarine

  • It is obtained from the mushroom Amanita muscaria.
  • It is a potent parasympathomimetic.
  • It is not used clinically. If taken accidentally, the toxic effects include severe colic, diarrhoea, exocrine secretions, miosis, dyspnoea, hypotension and bradycardia.
  • The antidote of choice is atropine.
  • Oxotremorine is a synthetic agent.
Last modified: Tuesday, 15 May 2012, 5:26 AM