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What are the two types of Cholinesterases and where are they located?
- 1. Acetyl Cholinesterase--- Neuromuscular Junction
- 2. Butyryl Cholinesterase--- Plasma and liver
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What are the two types of Nicotinic recepters and where are they located?
- 1. Nicotinic Nerve--- Adrenal Medulla, Autonomic ganglia
- 2. Nicotinic Muscle--- Neuromuscular junction.
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For muscarinic recepters M1,M2,and M3. Where are they located?
What is there mechanism of action?
- M1---CNS, Ganglia and GI--- PLC/IP3--- increase in Ca
- M2--- Heart--- inhibits Adenyl Cyclase--- K leaving cell
- M3--- Smoooth Muscle, BV, Eye, Sweat and lacrimal glands--- PLC/IP3--- increase in Ca
note: respiratory, GI and bladder are M1/3
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Name the Cholinergic agonists. (MCBCP)
Which are Susceptable to Cholinesterase?
- Methacholine---Slight
- Carbachol-------Negligible
- Bethanechol----Negligible
- Cevimeline
- Pilocarpine
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What is the Function of AntiCholinesterases?
what are the two types?
They inhibit the enzyme Acetylcholinesterase, thus decreasing the breakdown of ACh, prolonging its existance.
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Name the irreversible Anti-ChE agents.
What is the group called?
Parathion, Malathion, Diazinon
Called Organophospherous compounds
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Name the Reversible Anti-ChE.
Which are short acting and which are Medium acting?
- Edrophonium--- Short (5-10 mins)
- Neostigmine
- Physostimine
- Pyridostigmine
- Tacrine
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What are some nerve gas poisons? (SST)
Soman, Sarin, Tabun
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What is the Problem in Myasthenia Gravis?
What drugs are used in Myasthenia Gravis?
It is an autoimmune disorder, in which weakness is caused by circulating antibodies that block acetylcholine receptors at the post-synaptic neuromuscular junction,inhibiting the stimulative effect of the neurotransmitter acetylcholine.
Edrophonium, Neostigmine, Ambenonium, Pyridostigmine
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When trying to determine if a patient is having either a Myasthenia crisis or an overdose on the Anti-ChE medication, what should be given?
- Edrophonium- because it is short acting. If it helps= Myasthenic crisis
- if not= due to overdose.
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What are the major differences between Neostigmine and Physostigmine?
Neostigmine: CNS action absent (water soluble), used in MyG,Ileus, and urinary retention. By itself can cause muscle contraction.
Physostigmine: CNS action present (crosses BBB), used in glaucoma and is the antidote for Atropine poisoning.
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What is a Cholinesterase activator?
Name one.
What are its limitations?
When would you used it?
It frees the enzyme from the Anti-AchE
- PAM (Pralidoxime)
- Ineffective in the case of Physostigmine poisoning (anionic site not available)
effective treatment for: Nerve agents and Organophospherous compounds poisoning.
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Treat Glaucoma (wide angle)
Pilocarpine
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treat atony of the Bladder and GIT
Bethanechol
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treat Bronchial Hyperreactivity
Methacholine
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used after competative blockade of nicotinic receptor of skeletal muscle fibers.
Neostigmine
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Treat Myasthenia Gravis
Neostigmine
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Treat Alzheimers disease
- Donepezil
- Galantamine
- Rivastigmine
- Tacrine
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What are the naturally occuring AntiCh drugs?
what is the difference between the two?
Atropine-- CNS stimulate
Scopolamine-- CNS depressant
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What are the Synthetic AntiCh drugs? (ICTTTDDPGBHO)
Ipratropium, Cyclopentolate, Tropicamide, Darifenacin, Pirenzepine, Glycopyrrolate, Tolterodine, Flavoxate, Trihexyphenidyl, Benztropine, Homatropine, Oxybutynin, Dicyclomine
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What does Atropine do?
It blocks the Muscarinic recepters (M1,2,3)
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Preanesthetic Medication
Glycopyrrolate
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Antispasmodic in IBS
Dicyclomine
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Bronchial asthma and COPD
Ipratropium
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Treat Mydriatic and Cycloplegia
Cyclopentolate and Tropicamide
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Anti-Parkinsonism
- Trihexyphenidyl
- Benztropine
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Overactive bladder
- Oxybutynin
- Tolterodine
- Darifenacin
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Motion sickness
Scopolamine
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What are the Therapeutic uses of Botulinum Toxin type A?
- 1. Migraine Headaches
- 2. Winkles
- 3. Axillary Hyperhydrosis
- 4. Blepharospasm, Torticollis
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