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Pharmacology > Cholinergics > Flashcards

Cholinergics Flashcards

1
Q

Nicotinic Antagonist
Competitive Nn blocker

Use - lowers blood pressure
This drug was introduced in the 50’s and there are way better anti-hypertensives

A

MECAMYLAMINE

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2
Q

TACRINE, DONEPZIL, RIVASTIGMINE, GALANTAMINE

A

Long acting AChE-inhibitors used to treat DEMENTIA

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3
Q

BETHANACHOL

A

Half-life - long, not a substrate for acetylcholinesterase

Use - Nonobstructive GI Disorders or URINARY RETENTION

Stimulate GI motility and bladder emptying

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4
Q

d-Tubocurarine

A

Muscle relaxant
Active component in curare, hypotension
Rarely used due to tendency to release histamine and cause bronchospasm
Some cross reactivity with Nn

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5
Q

CARBACHOL

A

Half-life - long, not a substrate for acetylcholinesterase

Pupillary constriction
Use - limited, because nicotinic activity stimulates all autonomic ganglia

Some application in treating glaucoma

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6
Q

More selective for M1, which lessens side effects
Less tendency for dry mouth/blurred vision
Peptic Ulcer Disease - suppresses acid secretion via action on parietal cells

A

PIRENZIPINE

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7
Q

TIOTROPIUM

A

Bronchodilation

Supposedly more bronchoselective than ipratropium
Has less affinity for M2 receptors (doesn’t cause cardiac side effects)
Increase exercise tolerance

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8
Q

Spasmolytic

Stimulates presynaptic GABA-B receptors, suppressing excitatory transmissions

A

BACLOFEN

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9
Q

Similar to neostigmine but with a longer duration

MYASTHENIA GRAVIS — primary drug

A

PYRIDOSTIMINE

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10
Q

Inhibits calcium release from sarcoplasmic reticulum

Treat malignant hypertherima

A

DANTROLENE

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11
Q

Muscle relaxant
Active component in curare, hypotension
Rarely used due to tendency to release histamine and cause bronchospasm
Some cross reactivity with Nn

A

d-Tubocurarine

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12
Q

Chronic Asthma/COPD - induces bronchodilation but does not inhibit ciliary motility
Note for acute asthma attacks (beta-2 agonists are much better)
Rhinorrhea — stops runny nose

A

IPRATROPIUM

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13
Q

MECAMYLAMINE

A

Nicotinic Antagonist
Competitive Nn blocker

Use - lowers blood pressure
This drug was introduced in the 50’s and there are way better anti-hypertensives

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14
Q

ATROPINE

A

M1, M2, and M3 receptors
Eyes - causes MYDRIASIS & CYCLOPLEGIA
Promotes BRONCHODILATION and reduces secretions

Initial bradycardia, but in general causes TACHYCARDIA
TREAT AV-blocks and post-MI bradycardia

GI - antispasmodic, can be used to treat IBS

Use for OVERACTIVE BLADDER

Anti-AchE poisoning

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15
Q

BACLOFEN

A

Spasmolytic

Stimulates presynaptic GABA-B receptors, suppressing excitatory transmissions

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16
Q

PYRIDOSTIMINE

A

Similar to neostigmine but with a longer duration

MYASTHENIA GRAVIS — primary drug

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17
Q

TOLTERODINE, OXYBUTYNIN, DARIFENACIN, SOLIFENACIN

A

Slightly more selective for the M3 receptors
Used to treat OVERACTIVE BLADDER and incontinence
Neurologic problems

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18
Q

SUCCINYLCHOLINE

A 
Depolarizing blocker
Hyperkalemia
Myalgia 
Ganglionic Stimulation
Malignant Hyperthermia
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19
Q

Eyes - causes MYDRIASIS & CYCLOPLEGIA
Promotes BRONCHODILATION and reduces secretions

Initial bradycardia, but in general causes TACHYCARDIA
TREAT AV-blocks and post-MI bradycardia

GI - antispasmodic, can be used to treat IBS

Use for OVERACTIVE BLADDER

Anti-AchE poisoning

A

ATROPINE

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20
Q

Prophylactic for MOTION SICKNESS

Can be used as a patch

A

SCOPOLAMINE

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21
Q 
Depolarizing blocker
Hyperkalemia
Myalgia 
Ganglionic Stimulation
Malignant Hyperthermia
A

SUCCINYLCHOLINE

22
Q

PIRENZIPINE

A

More selective for M1, which lessens side effects
Less tendency for dry mouth/blurred vision
Peptic Ulcer Disease - suppresses acid secretion via action on parietal cells

23
Q

Partial nicotinic agonist that reduces nicotine craving

Causes nightmares

A

VARENCICLINE

24
Q

Covalently bind and inactivate AChE, undergo aging (irreversible)

SLUDGEM symptoms - Bradycardic, Excessive Tearing, Can’t breathe

A

Parathion, Malathion, Echothiophate

25
Q 
Use — DIAGNOSIS of myasthenia gravis via injection
Cholinergic Crisis (Tensilon Test) - identify if they are OVER or UNDER treated
A

EDROPHONIUM

26
Q

IPRATROPIUM

A

Chronic Asthma/COPD - induces bronchodilation but does not inhibit ciliary motility
Note for acute asthma attacks (beta-2 agonists are much better)
Rhinorrhea — stops runny nose

27
Q

Anti-Cholinergic Toxicity

A

Hot dry skin, Dry mouth, Dry eyes
Mydriasis and Cyclopegia —> Blurred vision (Blind as a bat)

Narrowing of anterior chamber and diminished outflow of aqueous humor

Sedation, Agitation, Hallucination, Coma (Mad as a Hatter)

28
Q

PILOCARPINE

A

Half-life - long, not a substrate for acetylcholinesterase

Glaucoma - contracts ciliary muscle and increases outflow of aqueous humor

Xerostomia - stimulates salivary glands, useful in Sjorgen’s syndrome

Can cause Diaphoresis

29
Q

GI atony - used in cases of post-operative paralysis of the GI tract
GU atony - used in post-operative dysuria
Glaucoma - miosis, lowers IOP
Myasthenia Gravis - most common treatment in the US, increases Ach concentration @ NMJ
NM blockade reversal - reverses paralysis from competitive NM blockade agents (eg Curare and related drugs)

A

NEOSTIGMINE

30
Q

Act on GABA receptors in the CNS

A

DIAZEPAM

31
Q

Long acting AChE-inhibitors used to treat DEMENTIA

A

TACRINE, DONEPZIL, RIVASTIGMINE, GALANTAMINE

32
Q

Half-life - long, not a substrate for acetylcholinesterase

Use - Nonobstructive GI Disorders or URINARY RETENTION

Stimulate GI motility and bladder emptying

A

BETHANACHOL

33
Q

Slightly more selective for the M3 receptors
Used to treat OVERACTIVE BLADDER and incontinence
Neurologic problems

A

TOLTERODINE, OXYBUTYNIN, DARIFENACIN, SOLIFENACIN

34
Q

METHACHOLINE

A

No effect in normal patients, but will provoke airway constriction in asthmatics

Used to diagnose bronchial hyperreactivity (asthma) WHEEZING

35
Q

SCOPOLAMINE

A

Prophylactic for MOTION SICKNESS

Can be used as a patch

36
Q

No effect in normal patients, but will provoke airway constriction in asthmatics

Used to diagnose bronchial hyperreactivity (asthma) WHEEZING

A

METHACHOLINE

37
Q

EDROPHONIUM

A 
Use — DIAGNOSIS of myasthenia gravis via injection
Cholinergic Crisis (Tensilon Test) - identify if they are OVER or UNDER treated
38
Q

Parathion, Malathion, Echothiophate

A

Organophosphates
Covalently bind and inactivate AChE, undergo aging (irreversible)

SLUDGEM symptoms - Bradycardic, Excessive Tearing, Can’t breathe

Tx: Pralidoximine, Atropine

39
Q

Half-life - long, not a substrate for acetylcholinesterase

Glaucoma - contracts ciliary muscle and increases outflow of aqueous humor

Xerostomia - stimulates salivary glands, useful in Sjorgen’s syndrome

Can cause Diaphoresis

A

PILOCARPINE

40
Q

Bronchodilation

Has less affinity for M2 receptors (doesn’t cause cardiac side effects)
Increase exercise tolerance

A

TIOTROPIUM

41
Q

VARENCICLINE (“Chantix”)

A

Partial nicotinic agonist that reduces nicotine craving
Causes nightmares

1-800-VERY CLEAN

42
Q

Sometimes used in ophthalmic surgery to constrict pupil (Miochol)

A

Acetylcholine

43
Q

Acetylcholine

A

Half-life - very short, rapidly metabolized by acetylcholinesterase

Use - Limited clinical use due to potential side effects, sometimes used in ophthalmic surgery to constrict pupil (Miochol)

44
Q

NEOSTIGMINE

A

GI atony - used in cases of post-operative paralysis of the GI tract
GU atony - used in post-operative dysuria
Glaucoma - miosis, lowers IOP
Myasthenia Gravis - most common treatment in the US, increases Ach concentration @ NMJ
NM blockade reversal - reverses paralysis from competitive NM blockade agents (eg Curare and related drugs)

45
Q

DIAZEPAM

A

Spasmolytic

Benzodiazepines act on GABA receptors in the CNS

46
Q

Rocuronium

A

Muscle relaxant for surgery

Nm selective, no CV side effects

47
Q

Muscle relaxant for surgery

Nm selective, no CV side effects

A

Rocuronium

48
Q

DANTROLENE

A

Inhibits calcium release from sarcoplasmic reticulum

Treat malignant hyperthermia

49
Q

Half-life - long, not a substrate for acetylcholinesterase

Pupillary constriction
Use - limited, because nicotinic activity stimulates all autonomic ganglia

Some application in treating glaucoma

A

CARBACHOL

50
Q

Hot dry skin, Dry mouth, Dry eyes
Mydriasis and Cyclopegia —> Blurred vision (Blind as a bat)

Narrowing of anterior chamber and diminished outflow of aqueous humor

Sedation, Agitation, Hallucination, Coma (Mad as a Hatter)

A

Anti-Cholinergic Toxicity

Pharmacology (19 decks)

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