most cholinergic receptors are? exceptions?
muscarinic M1,M2, M3 but nicotinic at NMJ and autonomic ganglia
tertiary amine used as antagonist at ganglionic nicotinic receptors reduction in BP during surgery and emergencies
prevent degradation of ACh = enhances parasympathetic = cholinergic 7 (edrophonium, neostigmine, pyridostigmine, physostigmine, ecothiophate, donepezil, tacrine)
what to treat atropine overdose with?
physostigmine (fixostigmine), does cross BBB
two drugs to treat alzheimers
donepezil/tacrine anticholinesterases lipophilic, crosses BBB
2 anticholinergics for urinary incontinence?
oxybutinin tolterodine (tertiary amines - can enter BBB)
what drug preferentially blocks NMJ nicotinic receptors?
cholinergic drug that induces bronchospasm(M3), used for asthma challenge test
selective: M1 antagonist? M3 antagonist?
1- pirenzepine 3- tiotropium
what are neostigmine and pyridostigmine used for?
treat myasthenia gravis, urinary retention, and reerse NMJ block
nicotine stimulates increased ____firing and ______ released in ________
cortical neurons dopamine nucleus accumbens
treatment for acute nicotine poisoning?
hexamethonium (C6) and tetraethylammonium
quaternary amines used as ganglionic blockers (antagonist at ganglionic nicotinic receptors) -used to treat hypertension but no longer used due to extreme side effects
treat motion sickness and for CNS sedation
M1? M2? M3?
CNS/ens(enteric NS) heart exocrine glands/smooth m/blood vessels
what happens at very high doses of nicotine?
better for eyes than atropine
what drug to treat cystitis and reduce bladder spasms?
chronic nicotine toxicity
o Tar risk for cancer, emphysema, and bronchial disease o CO risk of CV diseases o Pregnant smokers risk of miscarriage or low birth weight o ADDICTION
to reduce acid secretions in peptic ulcer?
pirenzepine M1 selective
tricyclic antidepressant, decreases stomach acid
specificity of anticholinergics
none are very specific antagonize all muscarinic receptors; competitive antagonism
muscarinic agonist drug for post-op urinary retention and abdominal distension, slowly hydrolyzed
anticholinergic– lipid soluble (CNS entry) at M2; treat Parkinsons, and EPS symptoms due to antipsychotics park your benz
antihypertension drugs are.... they increase ----and cause -----
cholinergic cGMP, vasodilation
2 phases of tobacco smoke
gas (CO) and particulate (nicotine)
green tobacco sickness
acute nicotine poisoning o Ingested as insecticide, spray, tobacco; solution on skin is absorbed percutaneously easily o Symptoms: rapid onset of nausea, salivation, abdominal pain, diarrhea, cold sweat, confusion, dizziness, hearing and vision, weakness ***prostration, lower BP, difficult breathing ***weak, rapid pulse, convulsions, death o Treat: induce vomiting (after ingestions), artificial respiration, treat muscarinic toxicity (secretions) with atropine
inactive processed form of nicotine?
two belladonna alkyloids that are toxic and found in plants?
atropine and scopolamine