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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
Q

o benztropine/trihexyphenidyl

A

anticholinergic– lipid soluble (CNS entry) at M2; treat Parkinsons, and EPS symptoms due to antipsychotics  park your benz

20
Q

antihypertension drugs are…. they increase —-and cause —–

A

cholinergic cGMP, vasodilation

21
Q

2 phases of tobacco smoke

A

gas (CO) and particulate (nicotine)

21
Q

green tobacco sickness

A

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
Q

inactive processed form of nicotine?

A

cotinine

23
Q

two belladonna alkyloids that are toxic and found in plants?

A

atropine and scopolamine

24
Q

anticholinergics cause

A

decreased secretions(sweat, saliva, exocrine), mydriasis (pupilary dilation) and cycloplegia (no accomodation), tachycardia, decreased smooth m contraction, cns excitation and delirium

26
Q

pilocarpine

A

pilocholpine, plant alkaloid cystic fibrosis sweat test treat glaucoma (decreases intraocular pressure)

26
Q

dopamine reward pathway

A

• 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
Q

muscarine

A

from mushroom not used clinically

28
Q

what to treat xerostomia (issue w secretions)?

A

a cholinergic agonist! pilocarpine

30
Q

Use of ACh as cholinergic agonist

A

not effective since it is hydrolyzed too quickly by aacetylcholinesterase

32
Q

anticholinergic safe for asthma and copd

A

ipratropium (ipray tropium) doesnt affect bronchioles

34
Q

mechanism of muscle relaxation caused by muscarinic rceptors

A

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
Q

what is secondary messenger for cholinergic paths?

A

cGMP

36
Q

anticholinesterase for glaucoma?

A

ecothiophate (ecoth eye ophate)

37
Q

cholinergic (parasym) uses what pre and post synaptically?

A

ACh

38
Q

neuronal nicotinic receptor partial agonist?

A

varenicline a4B2 selective

39
Q

7 effects of M3 stimulation

A

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
Q

nicotine symptoms

A

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
Q

atropine

A

anticholinergic– cause mydriasis w cyclopegia (loss of accommodation), treat ‘anti-AChE poisoning’

42
Q

antagonists at cholinergic muscarinic receptors?

A

anti cholinergics if you wanna be anti-CHOLd, go to the TROPics (many of these drugs have trop in name)

44
Q

anticholinesterase used to diagnose myasthenia gravis?

A

edrophonium

46
Q

two anticholinergic drugs for asthma and copd?

A

ipratropium and tiotropium **tiotropium is better - longer duration

47
Q

cholinergic ester agonists cant cross BBB, why?

A

they have a charged ammonium group

49
Q

cholinergics depolarize what two regions?

A

cranial and sacral

50
Q

when does sympathetic use ach?

A

presynaptically

51
Q

what drug preferentially blocks neuronal nicotinic receptors?

A

hexamethonium C6

52
Q

cholinergic for GI issues? eye issues?

A

bethanachol pilocarpine

54
Q

anticholinergic symptoms (ex from atropine) treatment?

A

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
Q

complex response to nicotine dosing

A

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
Q

tertiary vs quaternary amine anticholinergics

A

3- can enter CNS (the rest) 4-cannot enter CNS(ipratropium, tiotropium)

57
Q

three chemoreceptors stimulates by nicotine?

A

 Aortic arch, carotid body – respiratory stimulus  Emetic trigger zone (usually don’t smoke) – nausea  Hypothalamus – stimulation of vasopressin (ADH) secretion

58
Q

three treatments for nicotine dependence

A

• 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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