Cholinomimetics/ Lytics Flashcards
Neurotransmitter in parasympathetic system
ACh
Cholinoreceptors include
Muscarinic and nicotinic receptors
Location of nicotinic receptors
Skeletal muscle endplates adrenal medulla
Location of muscarinic receptors
M1 CNS
M2 heart
M3 smooth muscle and exocrine glands
Activation of cholinergic receptors causes?
Negative chronotropic, inotropic and dromotropic effects
Bronchoconstriction, increase bronchosecretions, vasodilation
Acid production
Examples of direct acting parasympathomimetics
Pilocarpine, bethanechol carbachol
Examples of indirect acting cholinergic drugs
Neostigmine, physiostigmine, endrophonium, demecarium
Mechanism of action of indirect acting cholinomimetics
Prevent the action of Acetylcholinesterase.
Mechanism of action of muscarinic cholinomimetics
-Activate muscarinic receptors
-Receptors activate inhibitory G Protein which stimulate phospholipase C.
-this leads to mobilization of intracellular calcium and influx of extracellular calcium
Mechanism of action of nicotinic cholinomimetics
-they act on nicotinic receptors which act as ligand gated ion channels.
- activation of which causes conformational changes leading to influx of sodium
Clinical uses of cholinomimetics and Ach
Treat myasthenia gravis
Postparative ileus
Urinary retention
Acute angle glaucoma
Mechanism of action of indirect acting cholinomimetics
Prevent the açtion of cholinesterases to increase concentration of ACh and it bioavailability at neuromuscular junction
Examples of cholinoreceptor antagonist
Atropine(prototype)
Scopolamine
Ipratropium bromide
Tiotropium
Clinical uses of cholinoreceptor antagonist
Benztropine: treat parkinson’s
Ipratropium bromide: can’t cross BBB treats COPD and asthma
Tertiary amines cross BBB can antagonist organophosphate compounds
Examples of tertiary amines
Atropine and scopolamine