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Pharm 2015 > Drugs of the Cholinergic System > Flashcards

Drugs of the Cholinergic System Flashcards

1
Q

Bethanechol

A

Cholinomimetic

Choline Ester:
_Direct Acting
_Selective
_Agonist

@ GI and Bladder Smooth Muscle
(Relatively Selective)

Use:

1) Constipation due to Lack of Tone
2) Urinary Retention

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2
Q

Methacholine

A

Cholinomimetic

Choline Ester:
_Direct Acting
_Selective
_Agonist

@ Heart
Predominantly Muscarinic

Use:
1) Bronchial Inhalation Challenge Test
(Triggers Bronchoconstriction)

2) Slows Heart Rate

Adverse Effects:
Arrhythmias
Heart Blocks

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3
Q

Pilocarpine

A

Alkaloid

Tertiary Amine
Lipid-Soluble

@ Sweat and Salivary Glands
Muscarinic Mostly

Uses:

1) Xerostomia (oral)
2) Glaucoma (eye drops) (not first line)

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4
Q

Muscarine

A

Alkaloid.
Mushroom.

Muscarinic

Poisoning is treated with Atropine

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5
Q

Nicotinic

A

Alkaloid.
Tobacco.

Nicotinic

Ganglion Stimulant

Highly Toxic

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6
Q

Edrophonium

A

Truly Reversible, Truly Competitive Anticholinesterase

Diagnostic for Myasthenia Gravis

Short-acting

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7
Q

Physostigmine

A

Reversible Anticholinesterase

Tertiary Amine
Lipid-Soluble
Enters CNS

False Substrate; Hydrolyzed by Enzyme

Use:
1) Antimuscarinic Toxicity

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8
Q

Neostigmine

A

Reversible Anticholinesterase

Quaternary Amine
Ionized
No CNS

False Substrates
Hydrolyzed by Enzyme

Uses:

1) Antimuscarinic Toxicity
2) Atony in Post-operative Ileus

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9
Q

Donepezil

A

Centrally Acting Reversible Anticholinesterase

-Used to Treat Alzheimer’s
-Lipid-Soluble; Enter CNS.
(Not quaternary)
-Patch administration.
*Donepezil,
*Rivastigmine,
*Galantamine
*Tacrine

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10
Q

Rivastigmine

A

Centrally Acting Reversible Anticholinesterase

-Used to Treat Alzheimer’s
-Lipid-Soluble; Enter CNS.
(Not quaternary)
-Patch administration.
*Donepezil,
*Rivastigmine,
*Galantamine
*Tacrine

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11
Q

Galantamine

A

Centrally Acting Reversible Anticholinesterase

-Used to Treat Alzheimer’s
-Lipid-Soluble; Enter CNS.
(Not quaternary)
-Patch administration.
*Donepezil,
*Rivastigmine,
*Galantamine
*Tacrine

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12
Q

Tacrine

A

Centrally Acting Reversible Anticholinesterase

-Used to Treat Alzheimer’s
-Lipid-Soluble; Enter CNS.
(Not quaternary)
-Patch administration.
*Donepezil,
*Rivastigmine,
*Galantamine
*Tacrine

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13
Q

Pyridostigmine

A

Reversible Anticholinesterase

@ Peripheral Nervous System
(Doesn’t readily enter CNS)

Was used to treat Organophosphate Poisoning

Adverse Effects:
Gulf War Syndrome with Repeated Doses:
Muscle Aches and Weakness, Diarrhea, Fatigue, Cognitive Problems.

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14
Q

Echothiophate

A

Irreversible Anticholinesterase

Organophosphate

Long-Acting

Causes Miosis

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15
Q

Malathion

A

Irreversible Anticholinesterase

Organophosphate

Insecticide

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16
Q

Sarin

A

Irreversible Anticholinesterase

Organophosphate

Nerve Gas

17
Q

Atropine

A

Anti-Muscarinic

Tertiary Alkaloid
Lipid-Soluble
Cross BBB
Enter CNS

Found in
_Belladonna (Deadly Nightshade)
_Datura Stramonium (stinkweed)

Uses:
_Bradycardia or Heart Block due to Excess Vagal Tone
_Cholinergic Poisoning by Muscarine and/or Anticholinesterase Organophosphates
_Excessive Salivation (Hyperhidrosis)

Effects Vary with Dose:

1) *Small Doses:
* Decreased Salivation and
* Decreased Sweating

2) Larger Doses:
Dilated Pupils,
Blurring of Near Vision,
Tachycardia (Palpitations)

3) Even Larger Doses: 
Difficulty Speaking and Swallowing, 
Restlessness and Fatigue, 
Headache, 
Hot Dry skin, 
Difficulty Urinating, 
Reduced GI Motility

**At Low Therapeutic doses, Atropine has almost no detectable CNS effects.
CNS Stimulation is prominent with *Toxic doses:
_Restlessness,
_Irritability,
_Disorientation, _Hallucinations.

(Secretions are very, very sensitive to small doses of Atropine.)

Atropine Poisoning Symptoms:
_Dry Mouth, Thirst
_Blurred Vision (Cycloplegia), Photophobia (Mydriasis)
_Hot, Dry, Flushed Skin
_Increased Body Temperature
_Palpitations
_Restlessness, Excitement, Hallucinations

Red as a Beet
Hot as a Hare
Dry as a Bone
Blind as a Bat
Mad as a Hatter

Atropine is Contra-indicated in Narrow Angle Glaucoma (Angle Closure Glaucoma).
_B/c this occurs when the iris blocks the outflow canal of aqueous humor from the eye.
(Atropine would cause the Ciliary muscle to block the flow.)

Contraindicated in Prostatic Hypertrophy.

Atropine causes Urinary Retention, especially in Elderly Males
_B/c of Enlarged Prostate

Lomotil (used to treat Diarrhea)
_Contains Atropine
_May be source of Atropine poisoning, especially in Children

18
Q

Scopolamine

A

Anti-Muscarinic

Tertiary Alkaloid
Lipid-Soluble
Cross BBB
Enter CNS

CNS Depressant in Clinical Dosage

  • -Drowsiness
  • -Amnesia

Use: Anti-Emetic
(Motion Sickness)

In people with Severe Pain:
_Causes CNS Excitation and Hallucinations

19
Q

Dicyclomine

A

Anti-Muscarinic

Tertiary Synthetic
Lipid-Soluble
Cross BBB
Enter CNS

Use: Bowel Spasms
(Gastric disorder; GI Tract)

20
Q

Tropicamide

A

Anti-Muscarinic

Tertiary Synthetic
Lipid-Soluble
Cross BBB
Enter CNS

Use: Mydriasis and Cycloplegia for Eye Exams
(Cycloplegia = paralysis of Ciliary muscle)

21
Q

Benztropin

A

Anti-Muscarinic

Tertiary Synthetic
Lipid-Soluble
Cross BBB
Enter CNS

Use: Parkinson’s

22
Q

Trihexyphenidyl

A

Anti-Muscarinic

Tertiary Synthetic
Lipid-Soluble
Cross BBB
Enter CNS

Use: Parkinson’s

23
Q

Ipratropium

A

Anti-Muscarinic

Quaternary
Ionized
Can’t cross BBB

Use: COPD

24
Q

Tiotropium

A

Anti-Muscarinic

Quaternary
Ionized
Can’t cross BBB

Use: COPD

25
Q

Oxybutynin

A

Antimuscarinic

Some M3 Selectivity

Use: Urinary Frequency

26
Q

Solifenacin

A

Antimuscarinic

Better M3 Selectivity (than Oxybutynin)

Use: Urinary Frequency

27
Q

Darifenacin

A

Antimuscarinic

Better M3 Selectivity (than Oxybutynin)

Use: Urinary Frequency

28
Q

Tolteridine

A

M3 Selective Antimuscarinic

Use: Urinary Frequency

29
Q

Trospium

A

Non-Selective Antimuscarinic

Use: Urinary Frequency

30
Q

Curare

A

Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker

1) Quaternary Alkaloid
2) No CNS effects @ Therapeutic doses

3) Not well Absorbed after Oral administration
(which is why they were able to eat the meat of the animals they had killed with Curare)

South American Arrow Poison

Active Compound is D-Tubocurarine

31
Q

D-Tubocurarine

A

Prototype Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker

Active compound in Curare

1) Quaternary Alkaloid
2) Not well absorbed with Oral administration
3) No CNS effects @ Therapeutic doses

4) Weak Ganglionic Blocker
=> Hypotension

5) Liberates Histamine
=> Hypotension
=> Bronchospasm
(These adverse effects are why we no longer use this)

32
Q

Atracurium

A

Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker

**Broken Down by Hoffman Elimination!
=> **Temperature and pH Dependent
_Not Enzymatic breakdown
(Not patient dependent)

**Does NOT Depend on Hepatic or Renal Function for its breakdown.
_Thus, will last just as long in elderly and healthy younger person.

Also Broken Down by Ester Hydrolysis

33
Q

Cisatracurium

A

Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker

Stereoisomer of Atracurium

Produces Less Histamine than Atracurium

(Now widely used)

34
Q

Rocuronium

A

Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker

Has Steroid structure.

Rapid Onset

Intermediate Duration

May be used to Facilitate Intubation.
(Like, need the patient to be paralyzed briefly for just a brief procedure, like intubation)

35
Q

Gantacurium

A

Non-Depolarizing (Competitive Antagonist) Neuromuscular (Nicotinic) Blocker

Investigational

New class (chemical structure)

Ultra-Short-Acting

–May be an Alternative to Succinylcholine (which is a Depolarizing blocker and the only other ultra-short-acting blocker available)

36
Q

Succinylcholine

A

Prototype Depolarizing (Partial Agonist) Neuromuscular Blockers

1) Very Brief Duration of Action (5-10 min)
2) Hydrolyzed by Plasma Pseudocholinesterase

_____________
May Get Prolonged Action:

1) Severe Malnutrition
(Not synthesizing enough Pseudocholinesterase)

2) Hepatic Disease
(Not synthesizing enough Pseudocholinesterase)

3) Drug Interactions:
_Neostigmine and other Anticholinesterases
_Ester Local Anesthetics

(Esters are Broken down by Pseudocholinesterase; thus, compete with succinylcholine for enzymatic breakdown)

4) Organophosphate Exposure
(Chronic, Sub-Clinical):
e.g. Field workers and Avid Gardeners with Chronic, Low-dose use of Insecticides

5) Succinylcholine Apnea:
Genetic difference in type of Pseudocholinesterase (less effective form)

\_\_\_\_\_\_\_\_\_\_
Diazepam:
_Increases Duration of Non-Depolarizing Blockers 
_Decreases Duration of Succinylcholine
(Depolarizing Blocker)

____________
Adverse Effects:

1) Malignant Hyperthermia:
Treat with Dantrolene*

2) Hyperkalemia
=> Results in Cardiac Depression

(More common in Burn, Trauma patients; Dangerous if on Digoxin)

3) Histamine Release

4) Ganglionic Block:
=> Hypotension!

5) Bradycardia: (Muscarinic)
_Cardiac Arrest may result

6) Increased Bronchial Secretions (Muscarinic)

(Both Succinylcholine and Acetylcholine are derived from Choline. So, may act @ Muscarinic receptors too.)

7) Fasciculations of Abdominal Muscles:
Causing Increased IntraGastric Pressure:
=> Increased Risk for Reflux

(Most likely in patients with Delayed Gastric Emptying, e.g. Diabetics, Morbid Obesity

8) Increased IntraOcular Pressure:
- -Transient (Peaks @ 2-4 min)

9) Post-Operative Muscle Pain

__________________
HOW TO REVERSE EFFECTS:
_Give Plasma!!
Need Normal Pseudocholinesterase!!!
_Cannot give Neostigmine b/c will only exacerbate.
_Don’t give Atropine because Atropine is a Muscarinic Blocker.

37
Q

Trimethaphan

A

Ganglion Blockers

No longer available in USA

Uses:
_Anti-Hypertensive (Short-term, for Hypertensive Crisis)

Adverse Effects:
_Many; Depend on the predominant tone at the time of the block
_Usually see Decreased Muscarinic Effects:

1) Mydriasis (Dilated Pupils) (Iris)
2) Cycloplegia, Blurred Vision (Ciliary muscle) (Accommodation)
3) Dry Mouth (Xerostomia),

4) Anhidrosis (Sweat Glands)
(Sympathetic)

5) Tachycardia
6) Constipation
7) Urinary Retention

Note:
1) Predominant Tone in Vasculature is Sympathetic.
_Ganglionic Block results in Vasodilation, Hypotension.
(Sweat Glands Sympathetic too)

2) Predominant Tone everywhere else is Parasympathetic.
_Ganglionic Block results in Anti-Muscarinic effects.

38
Q

Mecamylamine

A

Ganglion Blockers

No longer available in USA

Uses:
_Anti-Hypertensive (Short-term, for Hypertensive Crisis)

Adverse Effects:
_Many; Depend on the predominant tone at the time of the block
_Usually see Decreased Muscarinic Effects:

1) Mydriasis (Dilated Pupils) (Iris)
2) Cycloplegia, Blurred Vision (Ciliary muscle) (Accommodation)
3) Dry Mouth (Xerostomia),

4) Anhidrosis (Sweat Glands)
(Sympathetic)

5) Tachycardia
6) Constipation
7) Urinary Retention

Note:
1) Predominant Tone in Vasculature is Sympathetic.
Ganglionic Block results in Vasodilation, Hypotension.
(Sweat Glands Sympathetic too)

2) Predominant Tone everywhere else is Parasympathetic.
Ganglionic Block results in Anti-Muscarinic effects.

39
Q

Botulinum Toxin

A

Inhibits Release of Acetylcholine

  • Uses (Diluted form):
    1) Local Muscle Spasms

2) Excessive Sweating
3) Cosmetic (Reduce Wrinkles)
4) Migraines

Extremely Toxic! High Mortality.
Recovery: Weeks to Months

Food Poisoning
=> Progressive Parasympathetic Block
=> Motor Paralysis

1) Dry Mouth,
2) Blurred Vision
3) Difficulty Swallowing
4) Progressive Respiratory Paralysis => Death!

Anti-toxin is used to treat the poison.

Pharm 2015 (22 decks)

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