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Pharmac Gpp > Muscarinic And Nicotinic Blockers > Flashcards

Muscarinic And Nicotinic Blockers Flashcards

1
Q

Functions of nervous system

A

1) sensation
2) integration
3) response

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2
Q

What does somatic and ANS innervate

A

Somatic nervous system innervates skeletal muscles
ANS innervates Cardiac, smooth muscles and glandular epithelium

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3
Q

ACH is a neurotransmitter in

A

All motor fibers leaving CNS
Autonomic ganglia
Postganglionic parasympathetic fibers
Postganglionic sympathetic fibers in M, sweat glands
Adrenal medulla
Motor neurons running to striated muscles

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4
Q

Examples of Nicotinic receptor agonists

A

Nicotine, acetylcholine, choline, epibartidine, lobeline, varenicline and cytisine

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5
Q

Dominant receptor in ganglion is _______
List other receptors that can be found

A

Nicotinic NN receptors are the dominant
Others: M1,M2, adrenergic, dopaminergic, aminergic, peptidergic receptors

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6
Q

Selective Nicotinic agonist (Natural)

A

Nicotine( small doses)
Lobeline

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7
Q

Selective Nicotinic agonist (Synthetic)

A

DMPP Dimethyl phenyl piperazinium
TMA tetramethyl ammonium

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8
Q

Non selective muscarinic agonists

A

Acetylcholine, pilocarpine, Carbachol, anti cholinesterase

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9
Q

Excessive amounts of selective Nicotinic agonists leads to

A

Sustained depolarization and ganglion block

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10
Q

Clinical use of nicotine

A

Nicotine can be used as transdermal patches to treat nicotine dependence and can also aid smoking cessation

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11
Q

Clinical use of varenicline

A

As a partial agonist it can reduce both the craving and pleasurable effect of cigarettes and other tobacco products
Through this mechanism it helps some patients quit smoking

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12
Q

Cholinergic blocking drugs

A

Muscarinic antagonists, parasympatholytics, anticholinergics

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13
Q

Muscarinic receptor sites

A

Heart
Smooth muscles of GIT
Salivary glands
Genitourinary tract
Urinary bladder

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14
Q

List the cholinergic antagonists

A

Vesamicol
Hemicholinium
Botulinum toxins
Non depolarizing blocking agent e.g tubocurarine
Depolarizing blocking agents e.g suxamethonium

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15
Q

What does vesamicol inhibit

A

It inhibits VAT vesicular acetycholine transporter so acetylcholine won’t be transported into vescicles for storage

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16
Q

What does Hemicholinium inhibit

A

Inhibits choline transporter so choline can’t enter the neuron

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17
Q

Botulinum what does it do

A

It cleaves snare proteins and without snare proteins vescicles cannot fuse with membrane and then released

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18
Q

Example of non depolarizing blocking agent and function

A

Tubocurarine
Prevents acetylcholine from binding to post synaptic receptor

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19
Q

Example of depolarizing blocking agents and function

A

Suxamethonium
Blocks action of acetylcholine on post synaptic cleft and causes continuous depolarization until there is sensitivity of receptor

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20
Q

Where is M1 located

A

Primarily CNS ( cortex, hippocampus, corpus striatum), stomach

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21
Q

Function of M1 receptors on CNS

A

Improves learning , memory and motor function

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22
Q

Clinically selective anti cholinergic drugs on M1 receptors

A

Pirenzepine, telenzepine, dicyclomine, trihexyphenidyl

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23
Q

Clinical effects of M1 receptors

A

Hydrogen ion secretion

24
Q

Clinical correlates of m2 receptors on CNS

A

Tremor, analgesia

25
Q

Function of M2 receptors at presynaptic terminals/ cholinergic nerve endings of peripheral and central neurons

A

Reduces acetylcholine release

26
Q

Clinically selective anti cholinergic drugs on M2 receptors

A

Tripitamine, methoctramine

27
Q

Effect of M3 on vascular smooth muscle

A

It’s activity is mediated through the release of NO to produce vasodilation

28
Q

Clinically selective M3 anticholinergics

A

Darifenacin, solifenacin, oxybutynin, tolterodine

29
Q

Antagonist of M4 receptor

A

Himbacine

30
Q

Function of M4 receptors

A

They function as inhibitory auto receptors for acetylcholine
When activated m4 receptors inhibit ACH release in striatum

31
Q

List the anti muscarinic drugs
Natural

A

Atropine (DL hyoscyamine)
Scopolamine ( L hyoscine)

32
Q

List the anti muscarinic drugs
Synthetic tertiary structural analogue of atropine

A

Homatropine

33
Q

List the anti muscarinic drugs
Synthetic quaternary structural analogue of atropine

A

1) Atropine methyl nitrate
2) homatropine methyl bromide
3) methscopolamine bromide
4) Ipratropium
5) Tiotropium

34
Q

List the anti muscarinic drugs
Synthetic tertiary structurally non related to atropine

A

Pirenzepine
Dicyclomine
Cyclopentolate
Oxyphenycyclimine
Tropicamide

35
Q

List the anti muscarinic drugs
Synthetic quaternary structurally non related to atropine

A

Methantheline
Propantheline
Isopropamide
Glycopyrrolate

36
Q

Natural alkaloids from antimuscarinic drugs

A

Atropine
Hyoscine (scopolamine)

37
Q

Myadriatics semi synthetic derivatives

A

Homatropine

38
Q

Antiasthmatics semi synthetic derivatives

A

Ipratropium
Tiotropium bromide

39
Q

GI spasmolytics semi synthetic derivatives

A

Hyoscine butyl bromide

40
Q

Myadriatics synthetic compounds

A

Tropicamide, cyclopentolate

41
Q

Myadriatics synthetic compounds

A

Tropicamide, cyclopentolate

42
Q

Myadriatics synthetic compounds

A

Tropicamide, cyclopentolate

43
Q

Myadriatics synthetic compounds

A

Tropicamide, cyclopentolate

44
Q

In the CNS atropine produces mainly _______ effects , low doses cause _________ higher doses cause __________ and ___________

A

Excitatory effects
mild restlessness
Agitation and disorientation

45
Q

The central effects of atropine on CNS could be opposed by

A

Anticholinesterases e.g phsyostigmine (an effective antidote to atropine poisoning)

46
Q

Hyoscine in low dose causes ______

A

Marked sedation similar to atropine at high doses

47
Q

Atropine like drugs affect _______ reducing ________ and _________ in _______ disease

A

Extrapyramidal system
Involuntary movements and
Rigidity
In parkinston’s disease

48
Q

Atropine produces a mild anaesthetic action on the _____

A

Cornea

49
Q

How is atropine eliminated

A

50% metabolized in the liver and the remaining excreted unchanged in urine

50
Q

Half life of atropine

A

Approx 4 hrs

51
Q

Anti cholinergic toxicity mnemonics

A

Hot as a hare ( hyperthermia)
Dry as a bone (dry skin)
Red as a beet (flushed)
Blind as a bat (mydriasis)
Mad as a hatter (delirium)

52
Q

Anticholinergic toxicity

A

1) altered level of consciousness (hallucinations, delirium, coma, slurred speech)
2) seizures
3) sinus tarchychardia
4) hypertension
5) Mydriasis
6) Dry eyes
7) Dry mouth
8) reduced bowel sounds
9) constipation
10) urinary retention
11) hyperthermia

53
Q

Management of toxicity

A

1) control hyperthermia using cold sponging or ice bags
2) agitation might require physical constraints or chemical constraints ( benzodiazepines)
3) if ingested gastric labake
4) Antidote: physiostigmine 1-3 mg SC or IV for both central and pheripheral effects
Neostigmine ineffective for central effects

54
Q

Management of anticholinergic toxicity is contraindicated in patients with

A

Bradychardia, intraventricular conduction delay, AV nodal block ,asthma,seizures and wheezing

55
Q

Atropine delays gastric ________ and delays __________ of other drugs

A

Emptying
Absorption

56
Q

Antacids interfere with absorption of _________

A

Anticholinergics

Pharmac Gpp (5 decks)

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