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2nd Year - Pharmacology > 2. Cholinergic Drugs > Flashcards

2. Cholinergic Drugs Flashcards

1
Q

Location of M1 receptors

A

Gastric parietal cells
CNS neurons
Sympathetic postganglionic neurons

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2
Q

Location of M2 receptors

A

Myocardium

Smooth muscles

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3
Q

Location of M3 receptors

A

Glandular tissue

Vessels (smooth muscles and endothelium)

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4
Q

Location of nicotinic receptors

A

Skeletal NMJ
Adrenal medulla
Autonomic ganglia

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5
Q

Properties fo direct acting cholinergics

A

Binds and directly activates receptors
Have affinity and intrinsic activity
Independent of Ach release
Effects similar to endogenous Ach

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6
Q

Difference of metacholine from acetylcholine

A

Methyl substitution on the beta carbon side chain

The methyl group improved selectivity towards muscarinic receptors, and resistance to acetylcholinesterase

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7
Q

Difference of carbamic acid esters from acetic acid esterss

A

Presence of amino group causes resistant to acetylcholinesterase and increased duration of action

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8
Q

Properties of carbachol

A

Non-selective (binds to both muscarinic and nicotinic receptors)

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9
Q

Properties of bethanecol

A

More selective towards muscarinic receptors

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10
Q

Enumerate carbamic acid esters

A

Carbachol

Bethanechol

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11
Q

Pilocarpine: state selectivity, type of amine, and other important properties

A

Selective to muscarinic receptors, antagonized by atropine
Tertiary amine
Only cholinomimetic alkaloid with therapeutic use
Can penetrate the CNS at therapeutic doses

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12
Q

Used in the treatment of glaucoma

A

Carbachol (may also stimulate nicotinic receptors)

Pilocarpine

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13
Q

Muscarine: state selectivity, type of amine, and other important properties

A

Selective to muscarinic receptors, antagonized by atropine
Toxic when ingested and potentially fatal
No therapeutic use
Quaternary amine

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14
Q

Heart: state receptors involved and effects of cholinergic drugs

A

M2 receptors
Decreased HR, rate of conduction, force of contraction of the atrium
Decrease in cardiac output–> decrease in blood pressure

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15
Q

Blood vessels: state receptors involved and effects of cholinergic drugs

A

M3 receptors

Production of NO–> generalized vasodilation

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16
Q

GIT smooth muscles: state receptors involved and effects of cholinergic drugs

A

M3 receptors
increase tone and motility
increase in propulsive movement (ADR: cramps, colicky pain, spasm, nausea, vomiting, diarrhea)
increased intestinal gastric acid secretion

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17
Q

Urinary smooth muscles: state receptors involved and effects of cholinergic drugs

A

M3 receptors
Detrusor muscle contracts, sphincter muscles relax
increased urination

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18
Q

Used for GIT atony and urinary retention

A

Bethanechol

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19
Q

Respiratory smooth muscles: state receptors involved and effects of cholinergic drugs

A

M3 receptors
Bronchospasm
Increased bronchial secretions

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20
Q

Eye smooth muscles: state receptors involved and effects of cholinergic drugs

A

M3 receptors
Contraction of pupillary constrictor muscle and ciliary muscle –> miosis and cyclospasm
Lower IOP in glaucoma

21
Q

Used in the treatment of glaucoma as a miotic agent over carbachol

A

Pilocarpine; can cross the conjunctival membrane

22
Q

Glandular smooth muscles: state receptors involved and effects of cholinergic drugs

A

M3 receptors

Outpouring of secretions

23
Q

CNS: state receptors involved and effects of cholinergic drugs

A

M1 receptor

increase in locomotor activity and improved cognition

24
Q

Taclifenasine properties and indication

A

M1 selective agonist used in dementia

25
Q

Used for glaucoma

A

Pilocarpine and carbachol

26
Q

Used for GI disorders (postoperative abdominal distention, gastric atony, adynamic ileus)

A

Bethanechol

Neostigmine

27
Q

Used for xerostomia

A

Pilocarpine

28
Q

Used for dementia

A

Taclifenasine (muscarinic agonist)

Xanomeline

29
Q

Contraindications to the use of direct acting cholinomimetics

A 
Asthma
Hyperthyroidism
Coronary insufficiency
Acid peptic disease
GIT obstruction
30
Q

ADRs of direct acting cholinomimetics

A 
Flushing
Sweating
Salivation
Belching
Abdominal cramps
Urinary bladder tightness
Cyclospasm
Bronchospasm
Hypotension
Bradycardia
31
Q

Noncovalent acetylcholinesterase inhibitors

A

Edrophonium

Tacril and Donepezil

32
Q

Edrophonium properties: type of amine, binding, solubility, affinity, indications

A

Quaternary amine - non-lipid soluble
Reversible binding
Moderate affinity for AchE, to the anionic site, no covalent bond
Only used for diagnosis of myasthenia gravis and Tensilon test

33
Q

Tacrine and Donepezol properties

A

Inhibits AchE in the CNS, higher affinity
Lipid soluble, readily cross the BBB
Longer duration of action
Treatment of senile dementia of the Alzheimer type

34
Q

Carbamate inhibitors

A

Site of action: both active sites of AchE, covalent bond
Physostigmine (tertiary amine, lipid soluble)
Pyridostigmine
Neostigmine
Rivastigmine
Prpoxur

35
Q

Pyridostigmine indication

A

Chronic management of myasthenia gravis

36
Q

Neostigmine indication and properties

A

Stimulation of the bladder and GIT
Antidote to tubocurarine
Symptomatic treatment of MG

37
Q

Rivastigmine indication

A

Treatment of senile dementia of Alzheimer type

38
Q

Used for senile dementia of Alzheimer type

A

Rivastigmine
Donepezil
Tacrine
Galantamine

39
Q

used as a miotic agent in highly resistance case of glaucoma

A

Echothiophate

40
Q

Two active sites for AchE

A 
Anionic site (glutamate residue, basic moiety of Ach)
Esteratic site (histidine and serine residue)
41
Q

Site of action of organophosphates

A

Esteratic site

42
Q

Given for organophosphate poisoning before aging

A

Pralidoxime (PAM)

43
Q

Treatment for carbamate posoning

A

Atropine

44
Q

Used in acute angle closure glaucoma

A

Physostigmine and Pilocarpine

45
Q

Treatment of myasthenia gravis

A

Pyridostigmine
Abbenomium
Neostigmine

46
Q

Difference of myasthenic and cholinergic crisis

A

Myathenic crisis: due to undermedication; little to no Ach on NMJ
Chlonergic crisis: due to overmedication; too much Ach causing neuromuscular block

47
Q

After surgery, in reversing the neuromuscular block, what is administered?

A

Neostigmine or edrophonium PLUS atropine

To reverse the neuromuscular block without the muscarinic effect

48
Q

Acetic acid esters are abundant in __

A

NMJ
RBC in placent
Vascular tissues

2nd Year - Pharmacology (18 decks)

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