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Everything basic about cholinergic drugs
Cholnergic Drugs intro
Activity |
at Cholinergic synapsis- that use Ach as neurotransmitter |
Cholinergic Receptors |
Previous cheat sheet |
Cholnergic Stimulants |
Increase activity at ACh line synapses. |
Direct acting Cholinergic Stimulants |
Bind directly with the Cholinergic receptor |
Indirect acting Cholinergic stimulants |
increase synaptic activity by inhibiting the ACh linesterase enzyme located at Cholinergic synapse |
Direct Acting Cholinergic Stimulants
Cholinergic Agonists |
Function: similar to Ach Molecule |
Ach |
Is DIRECT ACTING Cholinergic stimulant |
Muscurininc Cholinegic Stimulants |
More beneficial , primarily AFFECT the peripheral tissues while exerting a minimal effect on the cholinergic receptors located in the autonomic ganglia and the neuromuscular junction. |
Clinical use |
only few are useful |
Follow The Table |
Every durg |
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Indirect-acting Cholinergic Stimulants
Function |
increase activity at cholinergic synapses by inhibiting the Achsterase enzyme that is responsible for destroying Ach after this neurotransmitter is released from the presynaptic terminal.So it allows more Ach to remain in the Synapse. FINALLY: It increases in cholinergic synaptic transmission. |
Also known as |
Cholinesterase inhibitors / antichlinesterase agents |
What it does finally |
Exert a stimulatory effect on the peripheral muscuranic cholinergic synapses and on the cholinergic synapses found at the autonomic ganglia, at the skeletal neuromuscular junction, and within certain aspects of the CNS. |
Adverse effects
p. 293 |
Problems and adverse effects |
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Clinical Applications
Mainly: Both |
decrease in smooth muscle tone tha toccur in GI trct and bladder following abdominal surgery or trauma. |
Indirectly |
glaucoma, myasthenia gravis, alzheimer disease and to reverse the effects from an overdose of other drugs such as neuromuscular blocking agents and anticholinestergics. |
Alzheimer disease |
p. 292 |
Glaucoma |
Myasthenia Gravis |
Reversal of Neuromuscular blockage |
Reversal of Ach-Induced CNS toxicity |
Antecholinergic Drugs
Function |
Competitive antagonists of the postsynaptic Cholinergic receptors: So they bind reversibly to the cholinergic receptor but do NOT activate it. |
Binding... |
BLOCKS the receptor from teh efects of endogenously released Ach ---> diminishing the cellular response to Cholinergic stimulation. |
Other names |
Antinuscurinic/antinicotinic DRUGS |
AntiNicotinic Nn-Antagonists |
USED for Extreme High BP and Hypertensive emergencies |
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To produce Surgery by blocking the Skeletal NMJ |
Antimuscarinic AntiCholinergic Drugs
Atropine |
Prototype Drug |
Obtained from: |
Extract of plants such as belladonna and jimsonweed |
Action |
BLOCK Postsynaptic Cholinergic Muscarinic Receptor |
Five subtypes M1-M5 |
Antagonize cholinergic receptors on number of tissues which leads to side effects (see above Cheat sheet) |
Clinical Application |
GI, Parkinson, and treat clinical disorder (table 19-2, p. 295) |
Parkinsons |
Deficiency of the dopamine in the basal ganglia. --> leads to overactivity of central cholinergic synapse |
CVS |
Atropine- primarirly use to block vagus nerve on myocardium. Slows heart rate, conduction of the cardiac action postential thorughout the myoardium. |
Motion sickness |
antimuscarinics - Scopolamine |
poisoning |
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