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CPR 1st half > Cholinergics/anticholinergics > Flashcards

Cholinergics/anticholinergics Flashcards

1
Q

most cholinergic receptors are? exceptions?

A

muscarinic M1,M2, M3 but nicotinic at NMJ and autonomic ganglia

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1
Q

trimethaphan

A

tertiary amine used as antagonist at ganglionic nicotinic receptors reduction in BP during surgery and emergencies

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2
Q

anticholinesterases

A

prevent degradation of ACh = enhances parasympathetic = cholinergic 7 (edrophonium, neostigmine, pyridostigmine, physostigmine, ecothiophate, donepezil, tacrine)

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2
Q

what to treat atropine overdose with?

A

physostigmine (fixostigmine), does cross BBB

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2
Q

two drugs to treat alzheimers

A

donepezil/tacrine anticholinesterases lipophilic, crosses BBB

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2
Q

2 anticholinergics for urinary incontinence?

A

oxybutinin tolterodine (tertiary amines - can enter BBB)

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3
Q

what drug preferentially blocks NMJ nicotinic receptors?

A

tubocurarine

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4
Q

methacholine

A

cholinergic drug that induces bronchospasm(M3), used for asthma challenge test

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5
Q

selective: M1 antagonist? M3 antagonist?

A

1- pirenzepine 3- tiotropium

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6
Q

what are neostigmine and pyridostigmine used for?

A

treat myasthenia gravis, urinary retention, and reerse NMJ block

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6
Q

nicotine stimulates increased ____firing and ______ released in ________

A

cortical neurons dopamine nucleus accumbens

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6
Q

treatment for acute nicotine poisoning?

A

atropine

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6
Q

hexamethonium (C6) and tetraethylammonium

A

quaternary amines used as ganglionic blockers (antagonist at ganglionic nicotinic receptors) -used to treat hypertension but no longer used due to extreme side effects

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8
Q

treat motion sickness and for CNS sedation

A

scopolamine

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9
Q

M1? M2? M3?

A

CNS/ens(enteric NS) heart exocrine glands/smooth m/blood vessels

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10
Q

what happens at very high doses of nicotine?

A

ganglionic blockade

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11
Q

homatropine

A

better for eyes than atropine

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11
Q

what drug to treat cystitis and reduce bladder spasms?

A

anticholinergic oxybutinin

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11
Q

chronic nicotine toxicity

A

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

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12
Q

to reduce acid secretions in peptic ulcer?

A

pirenzepine M1 selective

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13
Q

pirenzepine

A

tricyclic antidepressant, decreases stomach acid

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14
Q

specificity of anticholinergics

A

none are very specific  antagonize all muscarinic receptors; competitive antagonism

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16
Q

cholinergics broncho_____

A

constrict

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17
Q

bethanachol

A

muscarinic agonist drug for post-op urinary retention and abdominal distension, slowly hydrolyzed

18
o benztropine/trihexyphenidyl
anticholinergic– lipid soluble (CNS entry) at M2; treat Parkinsons, and EPS symptoms due to antipsychotics  park your benz
20
antihypertension drugs are.... they increase ----and cause -----
cholinergic cGMP, vasodilation
21
2 phases of tobacco smoke
gas (CO) and particulate (nicotine)
21
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
22
inactive processed form of nicotine?
cotinine
23
two belladonna alkyloids that are toxic and found in plants?
atropine and scopolamine
24
anticholinergics cause
decreased secretions(sweat, saliva, exocrine), mydriasis (pupilary dilation) and cycloplegia (no accomodation), tachycardia, decreased smooth m contraction, cns excitation and delirium
26
pilocarpine
pilocholpine, plant alkaloid cystic fibrosis sweat test treat glaucoma (decreases intraocular pressure)
26
dopamine reward pathway
• Nicotine enters brain  stimulates nicotine receptors  dopamine release --\> nucleus accumbens and prefrontal cortex • Nicotine activates VTA(ventral tegmental area) dopamine neurons directly via stimulation of nicotinic cholinergic receptors and indirectly via stimulation of receptors on glutamatergic nerve terminals that innervate the dopamine cells
27
muscarine
from mushroom not used clinically
28
what to treat xerostomia (issue w secretions)?
a cholinergic agonist! pilocarpine
30
Use of ACh as cholinergic agonist
not effective since it is hydrolyzed too quickly by aacetylcholinesterase
32
anticholinergic safe for asthma and copd
ipratropium (ipray tropium) doesnt affect bronchioles
34
mechanism of muscle relaxation caused by muscarinic rceptors
in arterioles and small vessels ACh --\> M3 of endothelial cells --\> activates Gq protein --\> increase IP3--\> increases intracellular Ca2+ --\> activates NOS (NO synthase) --\> generates NO NO --\> diffuses to smooth muscle cell --\> activates guanyl cyclase --\> cGMP causes relaxation decreased TPR and BP
35
what is secondary messenger for cholinergic paths?
cGMP
36
anticholinesterase for glaucoma?
ecothiophate (ecoth eye ophate)
37
cholinergic (parasym) uses what pre and post synaptically?
ACh
38
neuronal nicotinic receptor partial agonist?
varenicline a4B2 selective
39
7 effects of M3 stimulation
increase exocrine secreton, increase gut motility, miosis with pupillary sphincter contraction, accomodation via ciliary contraction, bronchoconstriction, bladder constriction, decrease arterial tone M3 makes you pee
40
nicotine symptoms
affects both S and PS – they oppose and you will see mixture of symptoms but sympathetic part is stronger for CV and parasympathetic is stronger for GI o Sympathomimetic = vasoconstriction, tachycardia, increased BP (all three due to NE), adrenal medullary stimulation (EPI), mydriasis, bronchodilation, sweating o Parasympathomimetic = bradycardia, increased motility and secretion in GI, bladder contraction (go pee), miosis
41
atropine
anticholinergic– cause mydriasis w cyclopegia (loss of accommodation), treat ‘anti-AChE poisoning’
42
antagonists at cholinergic muscarinic receptors?
anti cholinergics if you wanna be anti-CHOLd, go to the TROPics (many of these drugs have trop in name)
44
anticholinesterase used to diagnose myasthenia gravis?
edrophonium
46
two anticholinergic drugs for asthma and copd?
ipratropium and tiotropium \*\*tiotropium is better - longer duration
47
cholinergic ester agonists cant cross BBB, why?
they have a charged ammonium group
49
cholinergics depolarize what two regions?
cranial and sacral
50
when does sympathetic use ach?
presynaptically
51
what drug preferentially blocks neuronal nicotinic receptors?
hexamethonium C6
52
cholinergic for GI issues? eye issues?
bethanachol pilocarpine
54
anticholinergic symptoms (ex from atropine) treatment?
Hot as a hare, dry as a bone, red as a beet, bind as a bat, mad as a hatter tx: anticholinesterase to increase ACh levels
55
complex response to nicotine dosing
o Low [] are ganglionic stimulants o moderate [] produces a depolarizing block of ganglionic transmission  if you constantly hit the receptors with Ach/nicotine  they will no longer respond (no electrical recover) o Both sympathetic and parasympathetic ganglia are affected
56
tertiary vs quaternary amine anticholinergics
3- can enter CNS (the rest) 4-cannot enter CNS(ipratropium, tiotropium)
57
three chemoreceptors stimulates by nicotine?
 Aortic arch, carotid body – respiratory stimulus  Emetic trigger zone (usually don’t smoke) – nausea  Hypothalamus – stimulation of vasopressin (ADH) secretion
58
three treatments for nicotine dependence
• Replacement therapy – OTC chewing gum, patches, nasal spray/inhaler (too addictive?) • Varenicline (Chantix)– nicotine receptor alpha4beta2 partial agonist o Activates receptor less than nicotine and blocks nicotine from acting o Well tolerated with some stimulation S/PS effects • Antidepressants – Bupropion

CPR 1st half (11 decks)

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