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270 S1 > 5.2 > Flashcards

5.2 Flashcards

1
Q

What are the side affects f muscarinic agonists?

A 
Diaphoresis
N/V/D
Tightness in bladder
Difficulty in visual accommodation
Hypotension
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2
Q

What do magic mushrooms effect?

A

Muscarinic receptors!

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3
Q

What is pilocarpine used for?

A

Extracted from a South American shrubs – 1875
Genus Pilocarpus
Natives chew leaves to stimulate salivation
Action – partial agonist at muscarinic receptors (primarily)
Sweat glands are very sensitive to pilocarpine

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4
Q

What is Salagen used for?

A

Xerostomia (dry mouth)–Sjogren syndrome or head neck radiation ease swallowing

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5
Q

What is isopto carbine used for?

A

Glaucoma
Miotic agent mydriasis reversal
(muscarinic agonist)

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6
Q

What is Cevimeline (Evoxac®) used for?

A

Indications: enhances lacrimal secretions in Sjogren’s syndrome
Muscarinic agonist – high affinity for M3
Lacrimal and salivary glands
Long lasting sialogogic action
Fewer SE than pilocarpine

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7
Q

What is arecoline?

A 
From Areca or Betel nuts
Consumed as a euphoretic
No therapeutic use
Edible lime + betel nut + piper betel leaves
Muscarinic agonist
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8
Q

How can nicotine be used clinically?

A

Smoking cessation; direct-activing on nicotinic receptors

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9
Q

What is lobeline?

A

Plant derivative – “Indian tobacco”
Smoking cessation
Mixed agonist-antagonist at Nicotinic receptor

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10
Q

What is the difference in pharmacokinetics between tertiary and quaternary amines?

A

Tertiary can cross the blood-brain barrier

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11
Q

What are the major systems impacted by muscarinic agonists?

A

CV- decrease HR, pumping power
GI- increase motility
Bladder- void
Eye- constrict

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12
Q

What happens with prolonged cholinomimetic agonist stimulation?

A

Post-ganglionic neurons stop firing –> muscle relaxation

Prevents electrical recovery = “depolarizing blockade”

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13
Q

What is an indirect-acting cholinomimetic?

A

AChE inhibitors

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14
Q

What are the types of AChE inhibitors??

A 
Carbamic acid esters + quaternary/tertiary ammonium group
Reversible inhibition
Simple alcohol + quaternary ammonium
Reversible inhibition
Organic derivatives of phosphoric acid
May be irreversible
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15
Q

What are Donepizil and galantamine?

A

Reversible AchE inhibitor- Do not act on receptor, but block breakdown of Ach, letting more Ach carry out its actions

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16
Q

What is neostigmine? Function?

A

AChE Inhibitor
Bloxiverz – reversal of non-depolarizing neuromuscular blocking agents (reversal of drug induced muscle paralysis – i.e. Atracurium (Tracrium®), Rocuronium (Zemuron®), Vecuronium (Norcuron®)…)
Urinary retention treatment and prophylaxis
Myasthenia gravis
Some direct nicotinic and muscarinic agonist effect

17
Q

What is pheostigmine? Function?

A

AChE inhibitor
reversal of non-depolarizing neuromuscular blocking agents (unapproved)
Treat Anticholinergic toxicity

18
Q

How does a depolarizing paralytic work?

A

Sux- Imitates Ach; binds to receptors causes depolarization = Na+ in, muscles fire, then muscle becomes refractory to stimulus
NMJ- depolarized, stays refractory

19
Q

How does a non-depolarizing paralytic work?

A

Binds to receptor, and blocks entrance of Na+ into cells, this prevents depolarization, cell membrane stays at resting voltage
=Competitive inhibition

20
Q

What is the mechanism of organophosphates?

A

AChE Inhibitors

21
Q

How are organophosphates absorbed and distributed in the body?

A

Well absorbed from skin, lung, gut, and conjunctiva (except echothiophate)
Widely distributed in body – CNS

22
Q

What are the CNS effects of organophosphates at low/high concentrations?

A

Low- alerting response

High- convulsions, coma, death

23
Q

What are the smooth muscle effects of organophosphates?

A

Contraction

24
Q

What are the effects of organophosphates at low/high concentrations on skeletal muscles?

A

Low: Inhibit AchE –> increase ACh –> increase strength of contraction
High: fibrillation and fasciculation

25
Q

How to remember the toxicity of organophosphates?

A 
SLUDGEM
Salivation
Lacrimation
Urination
Deification
Gastric hyper motility
Emesis
Miosis
26
Q

Tx for organophosphates? Rationale?

A

Atropine.

= too much PNS, need some SNS action

27
Q

What is Pralidoxime (2-PAM)?

A

AChE reactivator
Binds to the receptor organophosphate got expelled from its binding site  regenerate functional receptor
Used for nerve attacks. Not effective against neostigmine, physostigmine, or carbaryl

270 S1 (19 decks)

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