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MWU Pharmacology I > Cholinergics / Anticholinergics > Flashcards

Cholinergics / Anticholinergics Flashcards

1
Q

Name 4 Muscarinic agonists

A

1) Acetylcholine (Miochol-E)

2) Bethanechol

3) Pilocarpine
- Systemic: Salagen
- Opthalmic: Isopto Carpine

4) Cevemiline

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2
Q

Name 4 reversible Cholinesterase inhibitors

A

1) Physostigmine
2) Neostigmine (Bloxiverz)
3) Pyridostigmine (Mestinon, Regonol)
4) Donepezil (Aricept)

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3
Q

Name 3 kinds of Irreversible Cholinesterase Inhibitors

Name two compounds in two of these categories

A

1) Echothiophate ( Phospholine Iodide)

2) Organophosphate insecticides
- Malathion
- Parathion

3) Nerve Agents
- Sarin
- VX

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4
Q

Name a cholinesterase reactivator

A

Pralidoxime ( Protopam Chloride)

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5
Q

Name a drug that blocks acetylcholine release

A

**Botulinum toxin ** (BOTOX)

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6
Q

Name 6 Muscarinic Antagonists

A

1) Atropine
- systemic: AtroPen
- opthalamic: IsoptoAtropine)

2) Scopolamine

3) Dicyclomine

4) Ipratropium

5) Tolterodine

6 ) Tropicamide

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7
Q

Name 4 Direct Acting Muscarinic Agonists

A

1) Acetylcholine
2) Bethanechol**
3) Pilocarpine** (systemic: Salagen , Opthalmic: IsoptoCarpine)
4) Cevimeline ** (Evoxac)

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8
Q

Name some physiological effects of direct acting muscarinic agonists

GI, Heart Rate, Blood Pressure, bladder, ocular, secretions

A
  • Increased GI motility
  • Decreased HR
  • Decreased Blood Pressure
  • decreased cardiac output
  • direct vasodilation
  • Contraction of bladder and relaxation of urinary sphincters
  • Miosis and decreased intraocular pressure
  • Stimulation of secretions
  • salivation, lacrimation, GI secretions, sweating, etc.
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9
Q

Therapeutic uses of direct acting muscarinic agonists on Urinary and GI systems and some example medications

A

GI and Urinary applications (bethanechol)

  • Stimulation of peristalsis and increased GI motility
  • Formerly used to treat postoperative abdominal distention, gastric atony, adynamic ileus and GERD
  • More efficacious therapies are now available

Treatment of urinary retention and inadequate emptying of the bladder
* Postoperative urinary retention
* Diabetic autonomic retinopathy
* Chronic hypotonic, myogenic or neurogenic bladder

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10
Q

Name some ocular therapeutic applications of direct acting Muscarinic Agonists

A
  • Treatment of Glaucoma (carbachol and pilocarpine)
  • Opthalmic surgery (induction of miosis)(acetylcholine, carbachol, pilocarpine)
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11
Q

Name some therapeutic uses of direct acting muscarinic agonists for salivary gland dysfunctions and some example medications

A

Pilocarpine and cevimeline
Xerostomia (dry mouth) due to:
- Head and neck radiation
- Sjorgen syndrome (autoimmune disorder where salivary and lacrimal secretions are compromised)

  • They enhance salivary secretion and ease of swallowing
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12
Q

Name 8 adverse effects of direct acting Muscarinic Agonists

BP / HR / Lungs / GI / Urinary / Glandular / Salivary

A

Mainly the result of unwanted or excessive muscarinic stimulation

  1. Hypotension
  2. Bradycardia
  3. Bronchoconstriction
  4. Diarrhea
  5. Cramping
  6. Urinary incontinence
  7. Excessive sweating
  8. Salivation
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13
Q

Name contraindications of direct acting muscarinic agonists

Breathing / Cardiovascular / Stomach / bladder

A
  1. Asthma
  2. Cardiovascular
    * Bradycardia
    * Hypotension
    * Vasomotor instability
    * Coronary artery disease
  3. Peptic ulcer disease
  4. Weakened smooth muscle of the bladder or GI tract (such as after bladder surgery or intestinal anastomosis)
  5. Urinary or intestinal obstruction
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14
Q

Acetylcholine: What is it used for, rate of metabolism?

A

Muscarinic Agonist
* Limited use to ophthalmic surgery where rapid miosis is necessary
* When it is administered systemically, it is very rapidly hydrolyzed by “pseudocholinesterase” in the plasma

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15
Q

Bethanechol: Structure, effect on nicotinic receptors and use?

A

Muscarinic Agonist
* Analog of acetylcholine that is resistant to rapid hydrolysis
* Direct muscarinic agonist with little effect at nicotinic receptors
* Used to stimulate GI motility and treat urinary retention

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16
Q

Pilocarpine: Uses

A

Muscarinic Agonist
* Used in the treatment of glaucoma and xerostomia due to poor salivary
secretion

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17
Q

Cevimeline: Therapeutic Uses

A

Muscarinic Agonist
* Used in the treatment of xerostomia due to poor salivary secretion

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18
Q

How do cholinesterase inhibitors work, and name 7 physiological effects

GI / Bladder / HR / BP / Secretions / Eye / Skeletal Muscle / Bronchial

A

The cholinesterase inhibitors act by preventing the breakdown
of acetylcholine in the synapse

Increased GI motility and secretion
Contraction of bladder and relaxation of sphincters
Bradycardia and hypotension
Increased secretions (salivation, lacrimation, sweating, etc…)
Decreased intraocular pressure
Stimulation of skeletal muscle (therapeutic doses) / paralysis of
skeletal muscle (toxic doses)
Bronchoconstriction

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19
Q

Cholinesterase Inhibitors: Therapeutic uses

Bladder / Neurodegenerative diseases

A

Treatment of paralytic ileus and atony of the bladder (neostigmine)
- Abdominal distention and acute colonic pseudo-obstruction from a
variety of medical and surgical causes
- Atony (lack of physiological tone) of the bladder detrusor muscle of the urinary bladder

Treatment of Alzheimer disease (donepezil)
- AD patients have reduced cerebral content of choline acetyltransferase (leads to decrease in acetylcholine synthesis and impaired cortical cholinergic function)
- Cholinesterase inhibitors increase cholinergic transmission by
inhibiting cholinesterase at the synaptic cleft and provide modest
symptomatic benefit in patients with AD

20
Q

Cholinesterase Inhibitors Therapeutic Uses

neuromuscular

A

Treatment of myasthenia gravis (pyridostigmine) (neostigmine is
less commonly used)

Myasthenia gravis is an autoimmune neuromuscular disorder characterized by fluctuating motor weakness involving ocular, bulbar, limb, and/or respiratory muscles

21
Q

What causes muscle weakness in Myasthenia gravis, and how do cholinesterase inhibitors help?

A

The weakness is due to an antibody-mediated, immunologic attack
directed at proteins in the postsynaptic membrane of the
neuromuscular junction (acetylcholine receptors or receptor-associated proteins)

Acetylcholinesterase inhibitors retard the degradation of ACh that
occurs by enzymatic hydrolysis in the neuromuscular junction, resulting in a prolonged effect of ACh
- Variable improvement in strength in patients with MG
- Pyridostigmine provides marke improvement in some patients and little or none in others

22
Q

Name 2 drugs that can help treat glaucoma, and how they help. Why are they rarely used today?

1 Cholinergic agonist and 1 Cholinesterase Inhibitor

A

Pilocarpine: Cholinergic agonist
Echothiophate: Cholinesterase inhibitor

Work by contracting the ciliary muscle, these drugs put tension on the trabecular meshwork and increase the outflow of aqueous
humor through the canal of Schlemm

Rarely used today because:
- Ocular side effects such as fixed, small pupils, myopia, and increased subjective visual disturbance related to coexistent cataract

23
Q

What are some drugs that can protect against poisoning?

A

Treatment of poisoning with atropine or other antimuscarinic
drugs (physostigmine)

Pyridostigmine is used by the military to protect personnel
against nerve agents used in chemical warfare

24
Q

What are some adverse effects of Cholinesterase inhibitors

A

Toxic effects may be severe (cholinergic crisis) especially in
overdose situations (organophosphate insecticide poisoning or
nerve-gas poisoning)

 SLUDGE (salivation, lacrimation, urination, defecation, GI
distress, emesis)
 Skeletal muscle fasciculation followed by paralysis
 Bradycardia, hypotension, shock
 Severe miosis
 CNS stimulation and seizures followed by coma

25
Q

Cholinesterase Inhibitor Contraindications

A

Asthma
 Cardiovascular
 Bradycardia, hypotension, coronary artery disease
 Peptic ulcer disease
 Urinary or intestinal obstruction

26
Q

How do you treat acute cholinesterase inhibitor poisoning?

A

Administer high doses of atropine (2-4 mg IV initially) followed by 2 mg IM every 10 minutes until symptoms disappear to block muscarinic receptors

 Administer pralidoxime to reactivate enzyme (effective only with organophosphates)

 Provide additional symptomatic treatment as needed.

 Diazepam is useful for controlling seizures

27
Q

Neostigmine and Pyridostigmine

Function / CNS / Uses

A

 Reversible cholinesterase inhibitors
 Quaternary ammonium compounds that don’t enter the CNS

 Uses:
 Treatment of myasthenia gravis (both are longer acting)
 Neostigmine is used to treat paralytic ileus and atony of the bladder
 Pyridostigmine is also used by the military to protect troops against nerve agents
used in chemical warfare

28
Q

Donepezil

type / CNS / uses

A

Reversible cholinesterase inhibitor
 Nonquaternary, so it can get into the CNS
 Used in the treatment of mild to moderate Alzheimer disease

29
Q

Physostigmine

A

Reversible cholinesterase inhibitor
 Nonquaternary, so it can get into the CNS
 Used in treating poisoning with atropine or other antimuscarinic agents

30
Q

What is sarin / VX gas. Signs and symptoms, and how to treat?

A

 Nerve Gases (sarin, VX)
 Very potent and toxic, irreversible cholinesterase inhibitors
 Just a few droplets of sarin can kill an adult
 Signs and symptoms are typical for cholinesterase inhibitors
 Treat poisoning with atropine and pralidoxime

31
Q

What is pralidoxime?

Type / mechanism of action / uses

A

 Cholinesterase reactivator
 It chemically binds to the phosphate group that inhibits the enzyme and thereby regenerates the enzyme
 Antidote for organophosphate poisoning
 It must be used within 2 hours following exposure because the
phosphorylated enzyme changes to a form that can not be
regenerated

32
Q

What is Botulinum Toxin

Type / Mechanism of Action / Toxicity and Treatment

A

Toxin produced by Clostridium botulinium
 Humans usually are exposed by ingesting canned foods that were not processed properly

 Toxin prevents the release of acetylcholine from nerve endings
 It affects both the autonomic nerve endings (classic anticholinergic effects) and the neuromuscular junction (paralysis)

 Treatment involves aggressive symptomatic support (especially of respiratory function) plus administration of antibodies to the toxin

33
Q

Clinical Uses of Botulinum Toxin

A

Clinical uses as a locally injected neuromuscular blocker (sold under the brand name Botox)
 Reduce the appearance of facial wrinkles
 Excessive sweating (hyperhidrosis)
 Overactive bladder
 Lazy eye (an imbalance in the muscles responsible for positioning the eye)
 Eye twitching
 Prevention of chronic migraines

34
Q

Name some physiologic effects of Muscarinic Antagonists

secretions, GI, bladder, lungs, pupils, HR, CNS

A

 Drying of secretions (lacrimal, salivary, respiratory, GI, sweat, etc.)
 Decrease tone and motility of GI tract
 Relaxation of the bladder and urine retention
 Bronchodilation
 Mydriasis (dilation of pupil) with cycloplegia (loss of
accommodation) and pronounced increase in intraocular pressure
 Increased heart rate

 CNS
-Sedation and amnesia at low doses
- Excitation and seizures at toxic doses
- Some of the agents are quaternary salts that do not produce these CNS effects

35
Q

Muscarinic Antagonists Therapeutic Uses

GI, Urology, Eyes, Poisoning, Cardiac

A

 Treatment of GI disorders
 Cramping, diarrhea, irritable bowel syndrome

 Urology
 Treatment of urinary incontinence

 Ophthalmologic use as mydriatic agents
 Do not use in patients with glaucoma

 Antidote for poisoning with cholinesterase inhibitors or
muscarinic agonists (e.g. some types of mushroom poisoning)

 Prevention of motion sickness (scopolamine)

 Cardiac stimulation in emergency situations (atropine)

36
Q

Name 6 adverse effects of muscarinic antagonists

A

 Dry mouth
 Dry, hot skin
 Constipation
 Urine retention
 Visual disturbances, blurred vision, photophobia
 CNS effects
 Sedation, confusion, amnesia (especially in elderly patients)

37
Q

Muscarinic Antagonist Contraindications

A

 Glaucoma
 Prostatic hypertrophy
 Cardiovascular instability
 Severe ulcerative colitis

38
Q

Muscarinic Antagonist Contraindications

A

 Glaucoma
 Prostatic hypertrophy
 Cardiovascular instability
 Severe ulcerative colitis

39
Q

Symptoms of Muscarinic antagonist Acute Poisoning

A

Anticholinergic syndrome

Symptoms include:
Dry, hot skin and hyperthermia
Severe mydriasis, blurring of vision, photophobia

CNS stimulation
 Agitation, hallucinations, seizures progressing to coma and death

Cessation of GI motility (no bowel sounds)

 Cardiovascular
 Weak, rapid pulse, tachycardia and arrhythmias

40
Q

Treatment for Muscarinic Acute Poisoning

A

Treatment:
 Administration of physostigmine or other cholinesterase inhibitors
 Benzodiazepines for the treatment of seizures
 Ice baths to reduce hyperthermia
 Keep patient in a dark, quiet area to prevent photophobia and
excitement

41
Q

Atropine

type / clinical uses

A

Prototypical antimuscarinic agent

A naturally-occurring belladonna alkaloid found in the plant Deadly
Nightshade (Atropa belladonna) and Jimson weed

 Clinical uses:
 Bradycardia
 Inhibition of salivation and secretions (preanesthesia)
 Organophosphate or nerve agent poisoning

42
Q

Scopolamine

type / structure / clinical use

A

Muscarinic Antagonist
A natural product found in the plant Hyoscyamus niger (Henbane)
 Chemically similar to atropine

Clinical use:

 Transdermal patch (Transderm Scop) is used for the prevention of motion- sickness and vertigo

43
Q

Dicyclomine

clinical uses

A

Muscarinic Antagonist
Nonquaternary - enters CNS
 Widely used as an intestinal antispasmodic for the treatment of
irritable bowel syndrome

44
Q

Ipratropium

clinical use

A

 Quaternary salt
 Administered by inhalation for the treatment of asthma and COPD
 Fewer systemic effects

45
Q

Tolterodine

clinical use

A

Used to treat urinary incontinence

46
Q

Tropicamide

A

Widely used to dilate the pupil for ophthalmologic examination

MWU Pharmacology I (9 decks)

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