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MOD 2 > Paraympathetic pharmacology > Flashcards

Paraympathetic pharmacology Flashcards

1
Q

Pupil dilation is caused by?

A

Sympathetic

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2
Q

Bronchoconstriction is caused by?

A

Parasympathetic

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3
Q

Urination is caused by?

A

Parasympathetic

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4
Q

Dilation of blood vessels in skeletal muscle?

A

Sympathetic

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5
Q

Constipation is caused by?

A

Sympathetic

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6
Q

What brings choline into the presynaptic cleft?

A

cholinetransferase (with Na)

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7
Q

Choline acetyltransferase?

A

acetyl CoA and choline catalyzed to form acetylcholine

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8
Q

Block cholinetransferase?

A

Hemicholiniums

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9
Q

Vesamicol?

A

blocks Vesicular acetylcholine transporter, which brings Ach into vesicle

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10
Q

Acetylcholinesterase?

A

is bound and free floating, binds to Ach, breaks it down

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11
Q

Acteylcholine autoreceptor?

A

Ach binds to the receptor, stop the release

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12
Q

Heteroreceptors?

A

presynaptic receptor, different things bind to it, depending on location

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13
Q

Muscarinic receptors?

A

CNS, heart, smooth muscle, nerves, and endothelium
M1-M5 (M1-M3 functionally characterized)
Directly, Indirectly

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14
Q

Directly Muscarinic receptors?

A

binds directly to the receptor or Ach released from parasympathetic nerves
Activates muscarinic receptors on effector cells, alters organ function directly

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15
Q

Indirectly Muscarinic receptors?

A

interacts with muscarinic receptors on pre-synaptic nerve terminals to INHIBIT the release of NT
-alters organ function indirectly

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16
Q

Nicotinic receptors?

A

located on nerves and muscles
ligand gated ion channel
bind of 2 Ach molecules elicit a conformational change that allows Na to enter
-Ach initially stimulated and then blocks the receptor

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17
Q

MOA Nicotinic receptors?

A

channel opening allow Na and K ions to diffuse rapidly, cell depolarization

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18
Q

Depolarizing blockade?

A

presistent agonist occupancy at receptor, postganglionic neuron stops firing, skeletal muscle cell relaxes

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19
Q

Activate muscarinic receptors?

A

Eye, Secretory, GI, Genitourinary, respiratory, CV

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20
Q

Activated nicotinic receptors?

A

CNS, PNS, NM junction

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21
Q

Direct acting cholinomimetics?

A

Choline esters

Alkaloids

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22
Q

Choline esters?

A 
hydrophilic
hydrolyzed by actylcholinesterase in GI tract at various rates
Acetylcholine
Bethanechol
Carbachol
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23
Q

Alkaloids?

A

well absorbed from most sites of administration
acidification of urine accelerates clearance of pilocarpine and nicotine
Pilocarpine

24
Q

Indirect acting drugs?

A

Acetylcholinesterase (AChase)
terminate actions of ACh
act as inhibitors at the active site of the enzyme, increase endogenous ACh, (inhibit AChase, decrease breakdown of ACh)
Butyrylcholinesterase also inhibited

25
Q

Chemistry of indirect acting cholinomimetics?

A

Lipid soluble, inhibitors characterized by chemical groups

-Edrophonium, Neostigmine/Physostigmine, Organophosphates, Thiophosphates

26
Q

Absorption fo indirect acting cholinomimetics?

A

Poor absorption from conjunctiva, skin and lungs
Physostigmine is well absorbed from all sites and sued topically in the eye

organophosphate cholinesterase inhibitors are well absorbed skin, lung, gut and conjunctiva

thiophosphate insecticides are lipid soluble and rapidly absorbed, must be activated in the body

27
Q

AChases inhibitors reversible?

A

Edrophonium, Physostigmine, neostigmine, pyridostigmine

echothiphate (essentially irreversible)

28
Q

Physostigmine?

A

forms a stable intermediate with the AChases
wide range at muscarinic receptors
duration 2-4 hours, can enter and stim cholinergic sites in the CNS

29
Q

Physostigmine therapeutic use?

A

increase intenstinal and bladder motility
miosis and spasm of accomodation and lowers intra-ocular pressure topically in the eye

treat anticholinergic (atropine) drug overdoses

30
Q

Physostigmine adverse effects?

A

in CNS, may lead to convulsions
bradycardia and a fall in CO
accumulation of ACh– paralysis of skeletal m at the nm junction

31
Q

Neostigmine?

A

not enter CNS, greater effect on skeletal m, stim contaction before paralysis
30 min- 2hr

stimulate the bladder and GI tract
symptomatic treatment of myasthenia gravis

32
Q

Echothiophate?

A

generalized cholinergic stimulation
paralysis of motor function
convulsions
intense miosis

chronic treatment of open-angle glaucoma, may cause cataracts

33
Q

Urinary tract and GI Cholinomimetics?

A

can treat decreased smooth m activity associated with (post-operative ileus, congenital megacolon, neurogenic bladder)

can increase tone of lower esophageal sphincter (reflux esophogitis)

most widely used drugs:

  • choline esters: bethanechol
  • AChase inhibitors: neostigmine
34
Q

Myasthenia gravis?

A

Edrophonium used as a diagnositic test
Pydriostigmine (AChase inhibitors, DOC)
may cause excess stimulation of muscarinic receptors

35
Q

Alzheimer disease?

A

AChase inhibitors (Tacrine, donepezil, rivastigmine, galantamine)
delay the progression
tacrine was initial drug developed, but induces severe hepatotoxicity
GI distress is primary adverse effect

36
Q

Mucarinic excess?

A

due to pilocarpine and choline esters

  • adverse reactions: DUMBBELSS
  • treatment: atropine
37
Q

Acute nicotine treatment is symptomatic?

A

muscarinic stimulation- atropine

central stimuliation- diazepam/anticonvulsants

38
Q

Chronic nicotine toxicity (smoking)?

A

replacement therapy: Gum, transdermal patch, nasal spray, inhaler

Varenicline- partial nicotinic receptor agonist and antagonist, Chantix

39
Q

Major source of toxicity is?

A

pesticide use in agriculture and the home

  • muscarinic excess-initial effects
  • treatment includes atropine and pralidoxime (2-PAM)
40
Q

Anticholinesterase inhibitors (irrversible), organophosphates?

A

covalently binds via its phosphate group to the serine- OH group at the active site of the enzyme

permanently inactivates enzyme, only way to restore is to synthesize new enzyme molecules

41
Q

Aging?

A

slow release of an ethyl group makes it impossible for chemical reactivators to break the bond between drug and enzyme

42
Q

Pralidoxime (2-PAM)?

A

can reactivate inhibited acetylcholinesterase
displaces the phosphate group of the organophosphate and regenerates the enzyme, if given before aging, can reverse the effects of echothiophate and other agents

43
Q

DUMBBELSS?

A 
Diarrhea
Urination
Miosis
Bronchoconstriction
Bradycardia
Emesis/ Excite muscles
Lacrimation
Salivation
Sweating
44
Q

Antimuscarinic drugs?

A

prototype: atropine

45
Q

Antinicotinic drugs?

A

ganglionic blockers and NMJ blockers

46
Q

Pharmcokinetics/dynamics of antimuscarinic?

A

well absorbed from gut and conjunctival membranes
significant levels achieved in CNS within 30-60 min
Elimination can last -15 hours (atropine)
MOA: reversible blockade

47
Q

Effects of antimuscarinic agents?

A

CNS, eye, CV, respiratory, GI tract, genitourinary tract, sweat glands

48
Q

Pilocarpine on the eye?

A

miosis

49
Q

Atropine on the eye?

A

mydriasis

50
Q

Atropine?

A

binds competitively to receptor preventing ACh binding
acts both centrally and peripherally
duration- 4 hours

51
Q

Clinical uses atropine?

A

treats bradycardia
combined with opioid antidiarrheals

treatment of overdoses of AChase inhibitor insecticides and some mushroom poisonings: blocks the effects of excess ACh from acetylchonesterase inhibitors

52
Q

Scopolamine?

A

greater CNS action compared to atropine

actions
-effective anti-motion sickness, blocks short term memory, produces sedation

53
Q

Ipratropium?

A

synthetic analog to atropine
causes bronchodilation
treating asthma and chonic obstructive pulmonary disease (COPD)
Tiotrpoium similar action but longer bronchodilation effect

54
Q

Urinary incontinence clinical pharmacology?

A

Oxybutynin
Solifenacin
Tolterodine

55
Q

Uses for antimuscarinic?

A

cholinergic poisoning

atropine overdose

56
Q

contraindications antimuscarinics?

A

glaucoma

BPH

57
Q

AntiDUMBBELSS?

A 
Constipation
No urination
Mydriasis
Bronchodilation
Tachycardia
no emesis
no tearing
dry mouth
no sweat
Hot as a hare
blind as a bat
dry as a bone
red as a beet
mad as a hatter
bloated as a bladder

MOD 2 (6 decks)

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