Pharmacology final - ALL Flashcards
Parasympathetic receptors and NT?
Nicotinic - Muscarinic
Ach - Ach
Sympathetic receptors and NT
Nicotinic - Adrenergic
Ach - NE/Epi
Ach synthesized from?
Enzyme?
Coline + Acetyl-CoA
Choline-Acetyl transferase
Choline uptake into presynaptic cell inhibitor?
Hemicholinum
Inhibitor of Ach exocytosis in presynaptic nerve ending?
Botulinum toxin
Major termination of synaptic Ach?
Acetylcholine esterase enzyme breaks it down
Reversible indirect acting cholinomimetic drugs?
Edrophonium
Physostigmine
Neostigmine
Irreversible indirect acting cholinomimetic drugs?
Malathion
Parathone
Function of indirect acting cholinomimetic drugs?
Inhibit Ach esterase causing no breakdown of Ach in synapse
Result of:
- Presynaptic cholinomimetic stimulation
- Direct cholinomimetic stimulation
- Indirect cholinomimetic stimulation
- Increase Ach
- Direct receptor binding increasing effect
- Prolonging synaptic Ach by inhibiting break down
Presynaptic increase of Ach ?
4-aminopyridin - increase Choline uptake
Increased EC calcium
Alpha-Latrotoxin stimulates Ach release in absence of Ca (Widow spider venom)
Difference between Ach and Carbachols?
Carbachols have a NH3 instead of a CH3 group
Carbachol T 1/2 and choline esterase resistance?
very resistant
long acting
Neostigmine administration?
No GI absorption must be given IV
Inhibitor of Ach storage?
Vesamicol
Negativ feedback of Ach release?
Alpha-2 receptor binding of Ach or NE
Dopamin-2 receptor binding dopamin
Block AP in NMJ by Procaine so no release
AB that may inhibit Ach release?
Tetracyclines
Aminoglycosides
Especially in Myasthenia gravis
Myasthenia Gravis?
Ab against nicotinic receptors in the NMJ causing no activation
Treatment og Myasthenia Gravis?
The -stigmines causing increase Ach in synapse
Neostigmin
Pyridostigmine
physostigmine
Drug used in diagnosis of Myasthenia Gravis?
Edrophonium since it is very short acting and can test if the patient has relife when administered
(t1/2 is 15 min)
Anti-Ach esterase that can pass the BBB?
Physostigmine
Drug used in Atropin overdose?
Physostigmine
SE of Ach-esterase inhibitors?
Just lis what would happen if we have an overstimulation of Ach (parasympathetic) DUMBELL Diarrhea Urination Miosis Bradycardia Bronchospasms Lacrimation Salivation
Why can increased Ach lead to flaccid paralysis?
Nicotinic overactivation leads to inhibition (Cholinergic toxicity) like insecticide poisoning