Pharmacology Class 2020 :Cholinergics Flashcards
What are the two components of the Peripheral nervous system?
Central which includes brain and brainstem
Peripheral which includes Autonomic and Somatic
The autonomic nervous system is split into two parts
Sympathetic
Parasympathetic
Almost all efferent fibers leaving the CNS are cholinergic
True or False
True
What neurotransmitter do all preganglionic neurons release?
ACH
Which part of the nervous system has the most cholinergic fibers?
Parasympathetic
Where are nicotinic acetylcholine receptors located?
skeletal muscles or somatic
Where are muscarinic ACH receptors found?
Cardiac
Smooth muscle
Neuron endings
Sweat glands
What two neurons are required within the autonomic nervous system reach a target organ?
preganglionic
postganglionic
What do cholinergics drugs do?
Mimic or block the actions of chemical transmitters
Are parasympathetic nerve fibers long or short?
short
All receptors at the neuromuscular junction have what type of receptors?
nicotinic
All target organs of the parasympathetics have what type of receptor?
Muscarinic
All autonomic ganglia have nicotinic receptors
True or False
True
What major neurotransmitter is stored in vesicles?
ACH
What enzyme synthesizes ACH?
ACH is derived from Actyl coenzyme A by Choline or CHAT acetyltransferase preganglionic nerve terminal
What releases ACH?
Calcium dependent exocytosis
Where does ACH bind?
Nicotinic receptors on postganglionic cells
Which enzyme hydrolyzes ACH?
Acetylcholinesterase
Where is acetylcholinesterase found?
neuronal membranes
What blocks the calcium dependent exocytosis of ACH?
Botullinum toxin
Where is ACH degraded?
By acetylcholinesterase in the post synaptic cell
What are cholinergic receptors?
ACH receptors
What is the location and function of the M1 receptor?
Location:
CNS neurons, sympathetic
postganglionic neurons
Function:
Increased intracellular Ca
What is the location and function of M2 receptor?
Location:
Myocardium, smooth muscle, CNS
neurons
Function:
Opening of K channels, inhibition of
adenylyl cyclase
What is the location and function of M3?
Location:
Exocrine glands, vessels, CNS neurons
Function: Increase intracellular calcium
What is the location and function of M4?
Location:
CNS neurons
Functions:
opening of potassium channels
Inhibition of adenyl cyclase
What is the location and function of M5?
Location:
Vascular endothelium
Function:
Increased intracellular calcium
What effects does cholinergics have upon the eyes?
Miosis or contraction of the pupil for accomodation
What is the affect of a cholinergic on the heart?
Decrease HR and BP
What is the affect of a cholinergic on respiratory?
Bronchial constrictions
Increased secretions
What is the affect of a cholinergic upon the GI?
Increased motility
Relax sphincters
Stimulates secretions
What is the affect of cholinergics on GU?
Relaxes sphincters
Bladder wall contraction
What is the affect of cholinergics on sweat glands?
Increase secretions such as tears, sweats, salivary
What are the two types of cholinergic drugs?
Direct Acting which directly act on ACH receptors
Indirect Acting which increases ACH through inhibition of acetylchoinesterase which allows more ACH to float around longer
What are the two types of direct cholinergic agonist?
Esters and Alkaloids
What are the ester form agonist?
Bethanechol
Carbechol
Methacholine
What are the alkaloid form of agonist?
Pilocarpine
Muscarine
What are the indirect and reversible cholinergic agonist?
Edrophonium Neostigmine Pyridostigmine Physostigmine Galantamine Donepezil Rivastigmine
What are the indirect and irreversible cholinergic agonist?
Malathion
Parathion
Sarin
Saron
The reversible indirect agonist are lipid soluble
True or False
False
Water Soluble
The irreversible indirect agonist are water soluble
True or False
False
Lipid Soluble
What are the characteristics of the reversible cholinergic indirect agonist?
Alcohols and carbamates
Shorter duration of action
minutes to hours
What are the characteristics of the irreversible cholinergic agonist?
Nerve gases and insecticides
Long duration of action due to covalent bonds between phosphorous enzyme complex
Some compounds last more than 100 hours
Cross BBB due to lipophilicity
What are the reversible agents of indirect irreversible cholenergic?
Atropine which blocks ACH binding to the receptor
What cholinergic agents are used to treat open angle acute glaucoma?
Pilocarpine by causing contraction of the iris and ciliay muscle which leads to aqueous humor outflow and decreases intraocular pressure
What can be used in the place of pilocarpine if the cholinergic is not effective in treating glaucoma?
Carbachol
What is the effect of cholinergics on the cardiovascular system?
Reduces peripheral vascular resistance and slows HR
Cholinergic Agents are not usually used to treat heart problems due to adverse effects of decreased inotrophy, decreased chronotropy and decreased vascular resistance
What affects do cholinergic have on respiratory?
contraction of the bronchial smooth muscle and stimulates secretion
What agent is used to help diagnose asthma?
Methacholine
Cholinergics should be avoided when treating asthma
True or False
True
What affect does cholinergics have on GI?
Increased motility, secretion and relaxes sphincters
What cholinergic drugs treat postoperative ileus?
Neostigmine and bethanecol
What cholinergic drugs treat dry mouth?
Pilocarpine
Cevimeline
What cholinergic drugs treat genitourinary?
Neostigmine by releasing post operative bladder retention through bladder contraction
Bethanechol which relieves urinary retention and neurogenic bladder by making bladder lose its tone
What is the medical condition myasthenia gravis?
Edrophonium is used as a diagnostic agent but not available in the US
What is the agent used to treat myasthenia gravis?
Pyridostigmine and neostigmine
What cholinergic drugs are used in the reversal of NMB?
pyridostigmine and neostigmine
Physostigmine
Inhibits the enzyme acetylcholinesterase and has a tertiary amine that allows it to cross the BBB in the unionized form.
What is the antidote to reverse toxic effects caused by pure anticholinergics?
Atropine Benztropine Scopolamine Atropa Belladonna
What is the adverse effects of physostigmine?
Seizures
Hallucinations
Arrythmia
What cholinergic agents treat alzheimer disease?
Donepezil
Galantamine
Rivastigmine
These drugs inhibit acetylcholinesterase which increases ACH in the CNS for synaptic transmission