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Pharmacology > Cholinergic > Flashcards

Cholinergic Flashcards

0
Q

Physostigmine

A

Carbamate (reversible competitive inhibitor of AChE)- used to treat wide angle glaucoma, can facilitate development of cataracts, enter CNS and reverse the effects of atropine and other antimuscarinics

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1
Q

Edrophonium

A

Simple competitive reversible inhibitor of AChE- used to test of myasthenia gravis

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2
Q

Neostigmine

A

Carbamate- treatment for myasthenia gravis and loss of tone in GI tract and bladder

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3
Q

Pyridostigmine

A

Carbamate- used in myasthenia gravis and prophylactic to nerve gas exposure

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4
Q

Organophosphates (‘irreversible’ inhibitors of AChE)

A

Ecothiophate- only clinically useful one, used to treat glaucoma

Malathion/parathion- farm insectacides

Sarin/soman- nerve gas

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5
Q

Donepezil/rivastigmine

Galamantine

A

Orally active cholinesterase inhibitors used in the treatment of Alzheimer’s

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6
Q

Atropine

A

Muscarinic antagonist. Long-lasting mydriasis which is used for opthalmoscopic examination (now other agents are preferred). It is also used as a “pharmacological patch” to treat amblyopia.
Cycloplegia – used in children to permit accurate determination of refractive errors.
Sinus bradycardia and atrioventricular block
Reduction of salivary and respiratory secretions, thereby preventing airway obstruction in
patients receiving general anesthesia (now other agents are preferred)
Intestinal spasms and pain. Reduction of gastric acid secretion (now other agents such as proton pump inhibitor and histamine receptors blockers are preferred)
Reversal of muscarinic or acetylcholinesterase inhibitor poisoning.
Prevention of muscarinic side effects in patient receiving cholinesterase inhibitors for Myasthenia gravis.
Prevention of muscarinic side effects in patient receiving neostigmine to reverse
neuromuscular block (glycopyrrolate preferred)
Mixed with diphenoxylate (a mild opioid agonist). This combination known as Lomotil is used as an antidiarrheal.

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7
Q

Scopolamine

A

Muscarinic antagonist. Motion sickness; the major side effect is drowsiness. Administered as a patch.

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8
Q

Tropicamide, Cyclopentolate, Homatropine

A

Muscarinic antagonist. Fast but short acting mydriatic agents. (May be used in combination with an alpha adrenergic agonist)

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9
Q

Ipratropium

A 
Muscarinic antagonist. Quaternary amine that administered by inhalation 
Ipratropium is used as a bronchodilator. Particularly effective for use in chronic obstructive 
pulmonary disease (COPD).   
Tiotropium  - similar to ipratropium, but longer acting
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11
Q

Tolterodine

A

Muscarinic antagonist (Bladder). Management of overactive bladder with symptoms of increased urinary frequency, urgency, nocturia, and incontinence.
Thought to have fewer adverse effects such dry mouth and blurred vision.
Contraindicated for individuals with narrow-angle glaucoma

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12
Q

Dicyclomine

A

Muscarinic antagonist (GI). Relaxes intestinal smooth muscle. Used to for irritable bowl symptoms.

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12
Q

Benztropine

A

Used to relieve extrapyramidal symptoms in Parkinson’s patients or in patients taking
antipsychotics

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13
Q

Glycopyrrolate

A

Muscarinic antagonist. Low doses preferentially inhibit secretion, so the drug is used preoperatively to inhibit secretions.
Prevention of excessive generalized sweating
Prevention of muscarinic side effects in patient receiving neostigmine to reverse
neuromuscular block.

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14
Q

ADVERSE ACTIONS OF ANTI-MUSCARINICS

A

Dry mouth (xerostomia)
Blurred vision (mydriasis and cycloplegia)
Hot, flushed skin (anhidrosis and cutaneous vasodilitation)
Constipation
Difficulty in urinating
Tachycardia
CNS effects: confusion, sedation, delirium
(“Dry as a bone; red as a beet; hot as a hare; blind as a bat; mad as a hatter”)

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15
Q

CLASSES OF OTHER DRUGS IN WHICH SOME MEMBERS HAVE ANTI-MUSCARINIC ACTIVITY (THIS IS IMPORTANT)

A 
Antihistamines (eg. diphenhydramine) 
Antidepressants  -  tricyclics  (eg. amitriptyline)  [unfortunately, attempted overdoses with tricyclic antidepressants are still very common] 
Phenothiazine antipsychotics (eg. chlorpromazine)
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17
Q

Hexamethonium

A

nACHR antagonist (ganglionic) first effective anti-hypertensive (not used anymore). Problems of poor absorption and autonomic side effects led to discontinuation of its use.

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17
Q

Bethanechol

A 
Muscarinic agonist (GI). Postop/ Postpartum
for bladder  Promote salivation
18
Q

Acetylcholine

A

It has limited clinical use but can be used intraocularly to produce miosis after the extraction of the lens. Also, it may be used during diagnostic coronary angiography where intracoronary injection causes vasodilation. Can be used to diagnose vasospastic angina where intracoronary injection of the acetylcholine has a direct on smooth muscle causing contraction.

19
Q

Methacholine

A

may be used for diagnosis of bronchial hyperreactivity and asthmatic conditions, very carefully.

20
Q

Carbachol

A

used for wide-angle glaucoma, only when other cholinomimetics are no longer effective.

21
Q

Bethanechol

A

used postoperatively after abdominal surgery and postpartum to reduce bladder distention; alternative to pilocarpine for promotion of salivation under conditions of xerostomia

22
Q

SIDE EFFECT OF CHOLINE ESTERS

A

sweating, cramps and diarrhea, excess salivation, decreased

pulse, etc. (DUMBELS)

23
Q

CONTRAINDICATIONS FOR USE OF CHOLINE ESTERS

A

Asthma; may precipitate an asthmatic attack due to muscarinic-mediated bronchial contraction
Urinary obstruction
Acid-peptic disease; may induce gastric acid secretion

24
Q

Pilocarpine

A

activates primarily muscarinic receptors. It may be used as miotic agent (eye drops; last about 1 day), particularly for wide-angle glaucoma. Narrow-angle glaucoma is a medical emergency, usually requiring surgery. Pilocarpine plus physostigmine (anti-cholinesterase) are often used initially, for immediate control of intraocular pressure, before surgery.

25
Q

ATROPINE

A

1) Ocular effects of atropine –
A. Mydriasis - Relaxes the iris sphincter, which allows sympathetic tone to predominate on the radial muscle.
B. Blocks accommodation – Relaxes/paralyzes the ciliary muscle, which increases tension on the ligaments, thereby flattening the lens.
C. Inhibits lacrimation
2) Cardiac effects of atropine –
A. Standard doses may increase heart rate and atrioventricular conduction by blocking vagal input.
B. Very low doses may initial decrease heart rate by first blocking presynaptic receptors.
3) Respiratory effects of atropine –
A. Bronchial smooth muscle relaxation and dilation
B. Inhibit secretions
4) Gastrointestinal and urinary tract effects –
A. Reduces lower esophageal muscle tone
B. Relaxes gastrointestinal tone, (not the sphincters) prolonging intestinal transit time
C. Inhibits gastric acid secretion
D. Relaxes detrusor muscle of the bladder causing urinary retention
5) Central nervous system effects of atropine
A. Atropine and scopolamine are tertiary amines, therefore, they can be distributed to the CNS.
B. Scopolamine is generally more sedating than atropine
C. Atropine first causes stimulation, followed by a sedating effect.
D. High doses can cause confusion and/or hallucinations.
6) Other effects of atropine –
A. Inhibits sweating, possibly leading to hyperthermia which then causes cutaneous vasodilation.

26
Q

Atropine uses

A

Long-lasting mydriasis which is used for opthalmoscopic examination (now other agents are
preferred). It is also used as a “pharmacological patch” to treat amblyopia.
Cycloplegia – used in children to permit accurate determination of refractive errors.
Sinus bradycardia and atrioventricular block
Reduction of salivary and respiratory secretions, thereby preventing airway obstruction in patients receiving general anesthesia (now other agents are preferred)
Intestinal spasms and pain.
Reduction of gastric acid secretion (now other agents such as proton pump inhibitor and histamine receptors blockers are preferred)
Reversal of muscarinic or acetylcholinesterase inhibitor poisoning.
Prevention of muscarinic side effects in patient receiving cholinesterase inhibitors for Myasthenia gravis.
Prevention of muscarinic side effects in patient receiving neostigmine to reverse neuromuscular block (glycopyrrolate preferred)
Mixed with diphenoxylate (a mild opioid agonist). This combination known as Lomotil is used as an antidiarrheal.

27
Q

Scopolamine

A

Motion sickness; the major side effect is drowsiness. Administered as a patch.

28
Q

Tropicamide, Cyclopentolate, Homatropine

A

Fast but short acting mydriatic agents. (May be used in combination with an alpha adrenergic agonist)

29
Q

Ipratropium

A

Quaternary amine that administered by inhalation
Ipratropium is used as a bronchodilator. Particularly effective for use in chronic obstructive pulmonary disease (COPD).
Tiotropium - similar to ipratropium, but longer acting.

30
Q

Tolterodine

A

Management of overactive bladder with symptoms of increased urinary frequency, urgency, nocturia, and incontinence. Thought to have fewer adverse effects such dry mouth and blurred vision.
Contraindicated for individuals with narrow-angle glaucoma

31
Q

DICYCLOMINE

A

Relaxes intestinal smooth muscle. Used to for irritable bowl symptoms.

32
Q

Glycopyrrolate

A

Low doses preferentially inhibit secretion, so the drug is used preoperatively to inhibit secretions.
Prevention of excessive generalized sweating
Prevention of muscarinic side effects in patient receiving neostigmine to reverse neuromuscular block

33
Q

Benztropine

A

Used to relieve extrapyramidal symptoms in Parkinson’s patients or in patients taking antipsychotics

34
Q

ADVERSE ACTIONS OF ANTI-MUSCARINICS

A

Dry mouth (xerostomia)
Blurred vision (mydriasis and cycloplegia)
Hot, flushed skin (anhidrosis and cutaneous vasodilitation)
Constipation
Difficulty in urinating
Tachycardia
CNS effects: confusion, sedation, delirium
(“Dry as a bone; red as a beet; hot as a hare; blind as a bat; mad as a hatter”)

35
Q

CLASSES OF OTHER DRUGS IN WHICH SOME MEMBERS HAVE ANTI-MUSCARINIC ACTIVITY

A

Antihistamines (eg. diphenhydramine)
Antidepressants - tricyclics (eg. amitriptyline) [unfortunately, attempted overdoses with
tricyclic antidepressants are still very common]
Phenothiazine antipsychotics (eg. chlorpromazine)

36
Q

Action of Nicotine

A

Stimulation of autonomic ganglia followed by ganglionic blockade (dose-dependent)
Stimulation of adrenal medulla (possible significant secretion of epinephrine)
Stimulation of CNS: alerting response; change in respiration

37
Q

nicotine toxicity

A

Gastrointestinal – nausea, vomiting, salivation, diarrhea
Cardiovascular – tachycardia/bradycardia, hypertension/hypotension, arrhythmia
CNS – lethargy, confusion, seizures, coma
Peripheral nervous system – diaphoresis,
Muscles - tremors, fasiculations, weakness, paralysis
Endocrine – increased epinephrine release

38
Q

MECAMYLAMINE

A

Antagonist at nAChR at ganglion. Improve GI absorption,

Tourette’s syndrome

39
Q

HEXAMETHONIUM

A

Antagonist at nAChR at ganglion. Prevents baroreceptor reflex

40
Q

Mecamylamine

A

nAchR antagonist (ganglionic)l. Can be used to improve gastrointestinal absorption. Recent interest in its use for Tourette Syndrome.

41
Q

Methacholine

A

Muscarinic agonist. Test for bronchial hyperreactivity (carefully; dangerous drug)

42
Q

Carbachol

A

AchR agonist. Wide angle glaucoma (second-or third-line)

43
Q

Pilocarpine

A

Partial muscarinic agonist. Miotic agent for wide-
angle glaucoma; also used with acetylcholinesterase inhibitor for emergency treatment of narrow-angle glaucoma; Promote salivation

Pharmacology (28 decks)

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