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Pharmacology > Direct Cholinomimetics and indirect cholinomimetics > Flashcards

Direct Cholinomimetics and indirect cholinomimetics Flashcards

1
Q

What are direct cholinomimetics

A

Agonists at muscarinic cholinoreceptors and increase parasympathetic activity

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2
Q

Direct cholinomimetics work at muscarinic cholinoreceptors and thus have similar effects as stimulation of the ___ division

A

Parasympathetic

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3
Q

Examples of direct cholinomimetics

A

Bethanechol
Methacholine
Pilocarpine
Carbachol

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4
Q

What is bethanechol

A

Direct cholinomimetic agent used to induce bladder and GI smooth muscle contraction (motility)

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5
Q

What is bethanechol structurally similar to

A

Acetylcholine

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6
Q

How does bethanechol prevent urine retention and ileus

A

Stimulating smooth muscle motor activity

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7
Q

What is methacholine

A

Direct cholinomimetic , parasympathomimetic drug, used in the bronchial challenge test to help diagnose asthma

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8
Q

How is methacholine used for diagnosis of asthma with bronchial hypersensitivity

A

If asthma is less clinically apparent they are more sensitive to methacholine challenge, compared to normal patients

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9
Q

What is pilocarpine

A

Potent stimulator of sweat, tears, and saliva used for both open and closed angle glaucoma

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10
Q

What does pilocarpine do

A

Contractsciliary muscles of the eye (treat open angled glaucoma) and causes pupillary sphincter contraction (closed angle glaucoma).

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11
Q

How is pilocarpine administered

A

Ocular insert or as eyedrops

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12
Q

MOA of pilocarpine

A

Contract the ciliary muscle of the eye for open angle glaucoma and the pupillary sphincter for closed angle glaucoma.

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13
Q

What is pilocarpine resistant to

A

Acetylcholinesterase

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14
Q

Patients show __ after administration of pilocarpine

A

Miosis

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15
Q

What is carbachol

A

Cholinomimetic agent similar to ach

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16
Q

What is carbachol used for

A

Open angle glaucoma

Rare-closed angle glaucoma

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17
Q

How does carbachol help with open angle glaucoma

A

Helps relieve intraocular pressure and can be used to cause pupillary constriction

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18
Q

What is an indirect cholinomimetic

A

Decrease the action of the acetylcholinesterase enzyme (which works to break down acetylcholine)

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19
Q

What are indirect cholinomimetics also called

A

Anticholinesterases

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20
Q

What does indirect cholinomimetics lead to

A

Increased duration and action of the neurotransmitter acetylcholine

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21
Q

What indirect cholinomimetics don’t cross the BBB

A

Edrophonium, neostigmine and pyridostigmine

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22
Q

What are indirect cholinomimetics that that don’t cross the BBB used to treat

A

Myasthenia gravis

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23
Q

What is neostigmine used to treat

A

Ileus

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24
Q

What are the indirect cholinomimetics examples

A 
Physostigmine
Donepezil
Ambenonium
Neostigmine
Pyridosstigmine
Edrophonium
Echothiophate
Tacrine
Rivastigmine
Galantamine
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25
Q

Indirect cholinomimetics that cross the BBB care __ acting

A

Centrally

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26
Q

What is physostigmine used for

A

Atropine overdose and dementia

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27
Q

What is donepezil used for

A

Alzheimer’s

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28
Q

Describe endrophonium

A

Reversible acetylcholinesterase inhibitor, which prevents the breakdown of acetylcholine

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29
Q

How does edrophonium work

A

Competitively inhibiting acetylcholinesterase at the neuromuscular junction

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30
Q

Edrophonium is used to diagnose __ __

A

Myasthenia gravis

31
Q

Describe the tensilon test

A

Myasthenia gravis can be diagnosed with edrophonium as patients immediately show decreased muscle weakness

32
Q

What are pyridostigmine and neostigmine

A

Cholinomimetics or parasympathomimetics, which work to reversible inhibit acetylcholinesterase and do not cross the BBB

33
Q

What do we use pyridostigmine and neostigmine treat

A

Myasthenia gravis

34
Q

Neostigmine in addition to treating myasthenia gravis, treats what

A

Reverse neuromuscular blocking agents in anesthesia

35
Q

Why are pyridostigmine and neostigmine used for long term treatment of myasthenia gravis

A

Improve muscle function by slowing the natural enzyme cholinesterase that degrades acetylcholine in the motor end plate; the neurotransmitter is therefore around longer to stimulate its receptor

36
Q

What else can neostigmine used to also treat

A

Post operative and neurogenic ileus as well as in treating urinary retention

37
Q

Physostigmine

A

More hydrophobic than other indirect cholinomimetics, and crosses the BBB

38
Q

What is physostigmine used to treat

A

Atropine and anticholinergic drug overdoses

39
Q

Physostigmine is helpful in inducing ___

A

Miosis

Leading to decreased intraocular pressure

40
Q

What is donepezil

A

Acetylcholinesterase inhibitor which is used for treating Alzheimer’s disease

41
Q

In Alzheimer’s ,patients have decreased ___ levels

A

Acetylcholine

42
Q

How does donepezil treat Alzheimer’s

A

Centrally acting acetylcholinesterase inhibitors help increase the available amount of relative acetylcholine

43
Q

What is pilocarpine (pilocar)

A

Direct cholinergic agonist that contracts the iris sphincter and ciliary muscle of the eyes

44
Q

What indicates pilocarpine

A

Glaucoma and xerostomia (dry mouth)

45
Q

Side effects of pilocarpine

A

Retinal detachment, decreased visual acuity and eye. Irritation, cholinergic side effects (bradycardia, bronchospasm, hypotension, and diarrhea)

46
Q

Who should we not give pilocarpine to

A

Asthma and bradycardia

Because causes systemic effects

47
Q

Pilocarpine is a direct acting cholinergic agonist that ___ aqueous blood flow

A

Increases

48
Q

Pilocarpine mimics the effects of ____ and serves as a messenger between nerve cells and various organs throughout the body

A

Acetylcholine

49
Q

What does pilocarpine , a parasympathomimetic agent stimulate

A

Cholinergic receptors and may lead to systemic effects such as bronchospasm or hypotension

50
Q

Pilocarpine treacle intraocular pressure in patients with angle closure glaucoma. How

A

Contracts the iris sphincter of the eyes and causes pupil constriction or miosis

51
Q

Pilocarpine contracts the ciliary muscle and focuses the lens for __ vision

A

Near

52
Q

Indications for pilocarpine

A

Xerostomia

Glaucoma

53
Q

How does pilocarpine treat xerostomia

A

Stimulates salivaryglands

54
Q

What causes xerostomia

A

Meds, chemotherapy, or Sjögren’s syndrome

55
Q

How does pilocarpine treat glaucoma (open angle)

A

Lowers IOP
Second line for open angle glaucoma
Contract ciliary muscles and widens to facilitate aqueous humor outflow

56
Q

How does pilocarpine treat patients with glaucoma (closed angle)

A

Contraction of the iris sphincter pulls the iris from impeding aqueous humor outflow
Can treat acute cases of primary closed angle glaucoma

57
Q

Side effects of pilocarpine

A

Detached retina
Decreased visual acuity
Eye irritation
Cholinergic effects

58
Q

Why does pilocarpine cause detracted retina

A

Lens and vitreous to move forward and may create a retinal tear. Sustained contraction of the ciliary muscle may lead to retinal detachment

59
Q

How does pilocarpine cause decreased visual acuity

A

Constricting pupils, may cause blurred vision and decreased visual acuity. Contraction of the ciliary muscle focuses the lens for near vision.

60
Q

Why does pilocarpine cause eye irritation

A

Administered topically to the lower conjunctiva as a solution or gel.

61
Q

What are the cholinergic effects of pilocarpine

A

Bradycardia, bronchospasm, hypotension, and hypersalivation , urinary urgency, diarrhea, and sweating.

62
Q

What can be administered to reverse systemic toxicity caused by pilocarpine

A

Atropine

63
Q

Who should you not give pilocarpine to

A

Asthma or bradycardia

Don’t want to worsen symptoms

64
Q

Acetylcholinerase inhibitor poisoning /organophosphate toxicity/cholinergic overdose. Who is it seen in

A

Farmers , as organophosphate are commonly found in insecticides

65
Q

What happens in acetylcholinesterase inhibitor poisoning

A

Irreversibly inhibit acetylcholinesterase

66
Q

Antidotes to acetylcholinesterase inhibitor poisoning

A

Atropine and pralidoxime

67
Q

Symptoms of acetylcholinesterase inhibitors

A

DUMBBELSS

Including excitation

68
Q

Why get DUMBBELSS symptoms with acetylcholinesterase inhibitor poisoning

A

Massive discharge of the parasympathetic nervous system

69
Q

Why get excitation with acetylcholinesterase inhibitor poisoning

A

CNS effects of cholinergic overdoes bc excitation of both CNS and muscle

70
Q

What are acetylcholinesterase inhibitors

A

Drugs that inhibit the enzyme which breaks down acetylcholine

71
Q

Antidotes to acetylcholinesterase inhibitor

A

Atropine and pralidoxime

72
Q

How does atropine stop acetylcholinesterase inhibitor

A

Competitive antagonist of muscarinic acetylcholine receptors, which is why it is a great antidote

73
Q

Why does pralidoxime antidote to acetylcholinesterase inhibitor

A

For organophosphate poisoning in conjunction with atropine
Binds to the site where an acetylcholinesterase inhibitor has attached, then regenerates the enzyme to allow it to function again and break down more acetylcholine at the synapse

Pharmacology (52 decks)

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