Autonomic pharm II Flashcards
What are the receptors on the ciliary muscle of the eye? What happens when each is activated?
M3 = contraction (parasymp) B2 = Relaxation (symp)
What are the receptors on the ciliary body of the eye? What happens when they are activated?
B1, B2
Increased aqueous humor production
Stimulation of the M receptors on the sphincter muscle and ciliary muscle causes what?
Miosis and spasm of accomodation
Activation of what receptors on the pupillary radial muscle causes mydriasis?
A1
What are the receptors on blood vessels that cause vasorelaxation? MOA?
M3–ACh allows Ca to flow into cells, leading to NO production
What is the MOA of NO?
Stimulation of guanylyl cyclase to make cGMP, inhibiting enzymes
When the endothelium of a blood vessel is damaged what happens to lose its ability to relax?
Fails to produce NO
How does the neuromuscular plate function?
ACh depolarizes the muscle membrane, allowing Na to produce EPSP
What leads to the stopping of signal for the neuromuscular junction?
AChesterases
What happens to nicotinic receptors on excessive activation?
desensitization
True or false: all autonomic ganglia have nicotinic receptors?
True
If all autonomic ganglia have nicotinic receptors, how does the ANS produce para and symp results?
Depends on the balance between symp and para innervation at a given tissue
Blood vessels are solely innervated by which division of the ANS?
Symp (leads to vasoconstriction)
The GI tract is solely innervated by which division of the ANS?
Para
What is the type of nicotinic receptor on the adrenal medulla? What is the response it elicits?
Nn, secretion of E and NE
What is the type of nicotinic receptor on autonomic ganglia? What is the response it elicits?
Nn–stimulation
What is the type of nicotinic receptor on the neuromuscular junction? What is the response it elicits?
Nm
muscle action
What are cholinomimetic drugs?
Drugs that work on choline receptors
What are the direct acting cholinomimetic drugs?
Cholinoceptor agonists (activate Muscarinic or nicotinic receptors)
What are the indirect acting cholinomimetic drugs?
inhibit acetylcholine esterase
NO synthase produces NO from what chemical?
R
Increasing [Ca] in vascular smooth muscle results in what?
Constriction
M3 activation in sphincters results in what? What is the one exception to this?
Relaxation
Lower esophageal sphincter will constrict
M3 activation in glands results in what?
Secretion
M3 activation on the bladder results in what?
Relaxation
M3 activation on the bronchioles results in what?
Contraction/bronchospasm
M2 activation on the SA node results in what?
decreased HR
M2 activation on the AV node results in what?
Decreased conduction velocity
M3 activation in the stomach results in what?
motility/cramps
M3 activation in the intestines results in what?
Contraction= diarrhea
M3 activation on blood vessels results in what?
Vasodilation
Why must drugs that act on nicotinic receptors be used carefully?
Because every presynaptic nerve uses nicotinic receptors
What are the two types of direct acting cholinoceptor agonists?
Muscarinic
Nicotinic
What are the two types of indirect acting cholinoceptor stimulants?
Reversible
Irreversible
Muscarinic or nicotinic direct acting cholinoceptor stimulant: ACh?
Muscarinic
Muscarinic or nicotinic direct acting cholinoceptor stimulant: muscarinic?
Muscarinic
Muscarinic or nicotinic direct acting cholinoceptor stimulant: methacholine?
Muscarinic
Muscarinic or nicotinic direct acting cholinoceptor stimulant: nicotine?
Nicotinic
Muscarinic or nicotinic direct acting cholinoceptor stimulant: succinylcholine?
Nicotinic
Muscarinic or nicotinic direct acting cholinoceptor stimulant: bethanechol?
Muscarinic
Muscarinic or nicotinic direct acting cholinoceptor stimulant: carbachol?
Muscarinic
Reversible or irreversible indirect acting cholinoceptor: edrophonium
Reversible
Reversible or irreversible indirect acting cholinoceptor: neostigamine
reversible
Reversible or irreversible indirect acting cholinoceptor:physostigmine
Reversible
Reversible or irreversible indirect acting cholinoceptor: echothiophate
Irreversible
Reversible or irreversible indirect acting cholinoceptor: malathion
Irreversible
Reversible or irreversible indirect acting cholinoceptor: parathion
Irreversible
Reversible or irreversible indirect acting cholinoceptor: denepezil
Reversible
Reversible or irreversible indirect acting cholinoceptor: sarin
Irreversible
All of the choline esters are what type of molecule?
Cationic quaternary ammonium (insoluble in lipids)
Why are direct acting cholinoceptor agonists poorly absorbed in the GI tract and CNS?
insoluble in lipids
Addition of what functional group to methacholine and bethanechol increases their half life?
methyl
carbachol and bethanechol are not susceptible to which enzyme?
Cholinesterase
What are the two choline esters that are not susceptible to acetylcholine esterase?
Carbachol
Bethanechol
Methacholine has more muscarinic, or nicotinic action?
Muscarinic
Bethanechol has more muscarinic or nicotinic action?
muscarinic
What are the effects of choline esters on the cardiovascular system?
Hypotension
Bradycardia
What are the effects of choline esters on the GI system? (3)
- Increased tone and contractility of gut
- Increased acid secretion
- n/v/d
What are the effects of choline esters on the GU system?
Involuntary urination
What are the effects of choline esters on the eyes?
Miosis
Contraction of ciliary muscle for near vision
What are the effects of choline esters on the respiratory system?
bronchoconstriction
What are the effects of choline esters on glands?
Increased secretions
What are homeostatic reflexes?
reflexes that respond to a stimulus to maintain homeostasis
Why does ACh have limited clinical use?
Fast degradation
What are the nicotinic effects of ACh?
not commonly seen since does not penetrate fat
How does ACh cause vasodilation?
Acts on M3 receptors to produce NO
What is the clinical use of methacholine?
Diagnosis of bronchiolar hypersensitivity via M3 receptors
What is the use of carbachol? MOA?
Activates both nicotinic and muscarinic cholinoceptors,
Open canal of schlemm to decrease intraocular pressure
What is the effect of high doses of carbachol?
cardiac arrest
What are the clinical uses of Bethanechol? What receptor does it act on?
Acts on M3 to increase detrusor tone, and increase gastric motility
(gastric atony
Gastric emptying, urinary retention)
Muscarine is found in what?
Mushrooms
What is the MOA of muscarine?
Directly activates all Muscarininc, ACh receptors with x100 potency
What are the symptoms of muscarine ingestion?
Increase secretions
Abdominal pain, n/v/d
Cardiac arrest
What is the MOA of pilocarpine?
Direct agonist of M3
What is pilocarpine used for in the eye? MOA?
Contraction of the iris sphincter muscle and ciliary muscles
Relieves glaucoma
What is pilocarpine used for when not used in the eye?
Tests autonomic state
Why should you not use choline agonists when there are peptic ulcers, GI tract disorders, or asthma?
Causes increased HCl secretion, and bronchoconstriction
What are the three major drugs that have antimuscarinic properties?
Quinidine
Procainamide
TCA
What are the two direct acting nicotinic drugs?
Nicotine
Succinylcholine
Nicotine acts on what receptors? What does this cause?
Nm–skeletal muscle contractions
Nn–lots o stuff
What is the effect of nicotine when it activates Nn receptors on the: heart?
Increases HR
What is the effect of nicotine when it activates Nn receptors on the: vasculature?
Peripheral vasoconstriction
What is the effect of nicotine when it activates Nn receptors on the: GI tract?
Increased gut motility
What is the effect of nicotine when it activates Nn receptors on the: Carotid bodies?
Increased respiratory rate
What is the effect of nicotine when it activates Nn receptors on the: medullary emetic chemoreceptors?
N/v
What is the effect of nicotine on the hypothalamus?
Increases cortisol, causing pleasant feeling
What is the MOA of indirect acting cholinomimetics?
Inhibit AchE
Is edrophonium short or long lasting?
Short
What are the clinical use of edrophonium?
Dx myasthenia gravis by blocking AchE
What is the MOA of myasthenia gravis?
Autoimmune attack against the nicotinic receptor
What are the two drugs used to treat myasthenia gravis?
Neostigmine
Pyridostigmine
What is the antidote for atropine overdose?
Physostigmine
Neostigmine is contraindicated with what condition?
Bladder obstruction
How do anti-AchE drugs work to treat glaucoma?
open canal of schlemm
What are the two cholinesterase inhibitors used in treating alzheimer’s? MOA?
Tacrine
Dopenezil
What is the neurotransmitter that is decreased in alzheimer’s?
Dopamine
What are the symptoms of cholinesterase inhibitor intoxication?
DUMBBELSS
What are the components of the DUMBBELSS mnemonic for cholinesterase intoxication?
Diarrhea Uncontrolled urination Miosis of eye Bronchiolar constriction Bradycardia Excitation of nervous system Lacrimation Sweating Salivation
What is the drug used to treat cholinesterase intoxication? MOA?
Atropine
Muscarinic receptor antagonist
What is the MOA of pralidoxim (2-PAM)?
Dephosphorylates the AChE