Autonomic Drugs Flashcards
Primary neurotransmitter in sympathetic NS and acts on ____
Norepinephrine (noradrenaline)
Alpha and beta adrenergic receptors
Sweat glands use ____ receptors
muscarinic acetylcholine
Even though its in sympathetic NS
Primary neurotransmitter in parasympathetic NS and acts on ____
Acetylcholine
muscarinic ACh receptors
Epinephrine produced in ___.
Activates most ____ receptors.
Synthesis requires ____
Adrenal medulla
Adrenergic
phenoethanolamine N-methyltransferase
Catecholamine synthesized from ___.
Rate limiting step:
Tyrosine
Tyrosine –> L-Dopa by tyrosine hydroxylase
Catecholamines (3)
Dopamine
Norepinephrine
Epineprine
Endogenous agonist for muscarinic and nicotinic receptors
Acetylcholine
Muscarinic receptors found on ___.
Mediates: (3)
targets of parasympathetic innervation
- Slowing cardiovascular function
- Increasing secretion
- Stimulating intestinal peristalsis
Subtypes of muscarinic receptors:
M1-M5
M1: neural M2: cardiac M3: glandular/smooth muscle (bladder) M4: CNS M5: unclear role
Odd numbered muscarinic receptors act via ___
Mediate:
Inositol triphosphase pathway
Parasympathetic vasodilation
Bronchoconstriction
Increased GI tract motility
Increased salivation, sweating and voiding, defecation
Even numbered muscarinic receptors act via ___
Found in:
Mediate:
inhibiting adenylyl cycase and reduce cyclic AMP
Heart
slowing heart rate, decreasing contractility
2 Main types of nicotinic receptors
- Skeletal muscle: mediates contraction
2. Neuronal: found in autonomic ganglia, brain, adrenal medulla
Metabolite of nicotine
cotinine
Varenicline =
Use:
Partial agonist of neuronal nicotinic receptor that mediates reward effect of nicotine
Treat nicotine dependence
Mivacurium, pancuronium, vecuronium =
Uses:
Nicotinic ACh receptor antagonist
Nueromuscular blocker: paralyze muscle in Sx
Clinical uses of AChe Inhibitors
Myasthenia gravis: Symptomatic treatment to try to get a lot of ACh in junction to overcome loss of receptor
Alzheimer’s disease: Penetrate CNS to overcome deficiency of cholinergic signaling
Donepezil
Rivastigmine
Galantamine
AChE inhibitors used in Alzheimer’s Disease
Pyridostigmine
Long acting AChE inhibitor used for Myasthenia gravis
Organophosphate AChE inhibitors cause
IRREVSERSIBLE inhibition of AChE
AChE inhibitor poisoning causes:
Symptoms:
activation of both muscarinic and nicotinic receptors
“DUMBLESS”: diarrhea, urination, miosis, bronchoconstriction, excitation (mm. and CNS), lacrimation, salivation, sweating
Treatment of AChE poisoning (2)
Atropine: blocks overstimulation of muscarinic receptors
Pralidoxime: prevents irreversible inhibition of AChE by organophosphate compound
Bethanechol, carbachol, pilocarpine =
Use:
Muscarinic acetylcholine receptor agonist
Topical treatment of glaucoma
Bethanechol =
Use:
Muscarinic acetylcholine receptor agonist
Urinary retention
Atropine =
Uses:
Muscarinic acetylcholine receptor antagonist
Penetrates CNS, BBB
Severe bradycardia
AChE poisoning
Tropicamide =
Uses:
Muscarinic acetylcholine receptor antagonist
Pupil dilation of ophthalmology
Scopolamine =
Uses:
Muscarinic acetylcholine receptor antagonist
Motion sickness
Glycopyrrolate =
Uses:
Muscarinic acetylcholine receptor antagonist
Dry secretions
Benztropine, diphenhydramine =
Uses:
Muscarinic acetylcholine receptor antagonists
Parkinsonism
Ipratropium, tiotropium =
Uses:
Muscarinic acetylcholine receptor antagonist
Asthma
Chronic obstructive pulmonary disease