Pharmacology of the Autonomic Drugs Flashcards
Which division of ANS has long preganglionic neurons?
Psymp
Preganglionic symp nt?
ACh
Preganglionic psymp nt?
ACh
Postganglionic symp nt?
NE
Postganglionic psymp nt?
ACh
Symp effects on eye
- Far focus
- Contraction of radial m→mydriasis (dilation)
Psymp effects on eye
- Contraction of circ. sphincter m→miosis (constriction)
- Contraction of ciliary m→ short focus
- More tear production
Symp effects on Digestive system
- Less secretion and motility
- More sphincter tone
Psymp effects on digestive system
- More secretion and motility
- Less sphincter tone
Symp effects on heart
- Increase HR
- Increase contraction force
Psymp effects on heart
- Decrease HR
- Decrease force
Symp effects on blood vessels
- Muscle vessels relax
- Skin and gut vessels constrict
Psymp effects on blood vessels
- Relaxes most
Symp effects on lungs
Relaxes bronchial smooth m
Psymp effects on lungs
Constricts bronchial smooth m
Symp effects on reproductive organs
- Relaxes blader
- Ejaculation (symp=shoot)
Psymp effects on reproductive organs
- Contracts bladder
- Erection (Psymp=point)
Symp effects on metabolism
Increase in blood glucose
Psymp effects on metabolism
Decrease in blood glucose
ACh removal
AChE
NE removal
- Reuptake
- COMT (catecholomethyltransferase)
- MAO (monoamine oxidase)
Subtypes of cholinergic receptors and what they alter
Nicotinic receptor: Alterted ion channel (ionotropic)
Muscarinic receptor: altered metabolism (metabotropic)
What branch of the ANS do cholinergic agents affect and what are their effects??
Primarily Psymp
Miosis
Increased in tear, sweat, and saliva
Decrease in bronchiole smooth m and HR
Muscarine
Direct muscarinic agonist
Pilocarpine
Direct muscarinic agonist
Bethanechol
Direct muscarinic agonist
Nicotine
Direct nicotinic agonist
Varenicline
Direct partial nicotinic agonist
Binds to receptor but does not fully activate it. Thus prevents others from binding.
Anti-smoking drug b/c binds but does not have effects of nicotine
What are the two agonists that act on nicotinic and muscarinic receptors?
ACh
Carbachol
How do indirect acting cholinergic agonists work and what are their effects?
Inhibit AChE
Similar to direct cholinergic agonists:
Miosis
Increased in tear, sweat, and saliva
Decrease in bronchiole smooth m and HR
But also affect muscle
Physostigmine
Indirect cholinergic agonist
Lasts for several hours
Inhibit AChE
Neostigmine
Indirect cholinergic agonist
Lasts for several hours
Inhibit AChE
Demecarium
Indirect cholinergic agonist
Lasts for several hours
Inhibit AChE
Echothiophate
Indirect cholinergic agonist
Lasts for 100s hours
Phosphorylates AChE
Edrophonium
Indirect cholinergic agonist
Doesn’t last very long
Inhibit AChE
What are indirect cholinergic agents used to treat?
Glaucoma
Myasthenia Gravis
Sjrogens Syndrome
Alzheimers (not very effective)
Donepezil
Indirect cholinergic agonist
Alzheimer’s tx
Tacrine
Indirect cholinergic agonist
Alzheimer’s tx
Pralidoxime
If given early can reduce any perm. damage caused by organophosphate AChE inhibitors
Malathion
Insecticide-cholinergic agonist
Irreversible AChE inhibitors
Sarin
Nerve gas-direct cholinergic agonist
Irreversible AChE inhibitors
Toxicities of cholinergic agonist
Diarrhea
Urination
Miosis
Bradycardia
Bronchoconstriction
Excitation of CNS*
Lacrimation
Salivation
*Paralysis, seizures, atoxia, amnesia
Atropine
Antimuscarinic agent
Blocks muscarinic receptor
Lasts 7-10 days
Scopolamine
Antimuscarinic agent
Blocks muscarinic receptor
Lasts 3-7 days
Homatropine
Antimuscarinic agent
Blocks muscarinic receptor
Used to dilate pupils
Cyclopentolate
Antimuscarinic agent
Blocks muscarinic receptor
Used to dilate pupils
Tropicamide
Antimuscarinic agent
Blocks muscarinic receptor
Used to dilate pupils
Ipratropium
Antimuscarinic agent
Blocks muscarinic receptor
Side effects of antimuscarinic agents
Mydriasis
Inhibits ciliary m→loss of accomodation→virtually blind
Less tear production
Bronchodilation
Dry mouth
Less gastric motility and secretion (constipation)
Urinary retention
Less sweating
Higher HR
Psychosis
“Mad, blind, dry, red, hot”
Succinylcholine
Direct nicotinic agonist
Antinicotinic agent-Depolarizing neuromuscular blocker
Long duration of action compared to acetylcholine
Initially activates receptor, eventually muscle hyperpolarization then paralysis
Non-depolarizing neuromuscular blockers that are antinicotinic agents are derived from?
curare
Pancuronium
Antinicotinic agent
non-depolarizing neuromuscular blockers
atracurium
Antinicotinic agent
non-depolarizing neuromuscular blockers
Rocuronium
Antinicotinic agent
non-depolarizing neuromuscular blockers
Most common one
Sugammadex
Reverses block by rocuronium by binding directly
Botulinum toxin type A
Inhibitor of ACh release
Cosmetically now
Originally for muscle spasms:
- Tics
- Strabismus
- Nystagmus
Sympathetic adrenoceptor subtypes
alpha 1: contract vascular smooth m–increase HR
alpha 2: activate presynaptic nerve terminals in CNS
Beta 1: increase HR and contraction force
Beta 2: relaxation of resp. vascular smooth m.
Epinephrine
Works on all adrenergic receptors
Causes increased HR, etc. etc.
Phenylephrine
Adrenergic agonist
Activates alpha1 receptors
Tx: congestion
Taken intranasally
Tetrahydrozoline (Visine)
Adrenergic agonist
Activates alpha1 receptors
Tx: congestion
Taken intranasally
Naphazoline
Adrenergic agonist
Activates alpha1 receptors
Tx: congestion
Taken intranasally
Clonidine
Adrenergic agonist
Activates alpha2 receptors
Decrease symp outflow from CNS
Tx: hypertension
Other analogs used for glaucoma (Decrease pressure)
alpha-methyl NE
Adrenergic agonist
Activates alpha2 receptors
Decrease symp outflow from CNS
Tx: hypertension
Other analogs used for glaucoma (Decrease pressure)
Agents that activate beta1 receptors
NE
Dobutamine
Agents that activate B2 receptors
“Nols and rols”
Metaproterenol
Terbutaline
Fenoterol
Albuterol
Tx: asthma
Causes bronchodilation
What induces the release of NE from nerve terminals?
Indirect acting amines:
Amphetamine, methamphetamine
Tyramine
Phenylpropanolamine
Pseudoephedrine
Prazosin
Adrenergic antagonist
alpha1 receptor blocker
Tx: hypertension
Alpha 1 receptor blockers are used to treat?
Hypertension
Benign prostatic hypertrophy
Specific B1 receptor blockers
“olol”s
Metoprolol
Acebutolol
Nebivolol
Atenolol
Esmolol
Alprenolol
These decrease HR
Non specific B1 and B2 blockers
Propanolol
Timolol
Levobunolol
Certeolol
Metipranolol
Phenoxybenzamine
Adrenergic antagonist
alpha1 receptor blocker
Tx: hypertension