Cholinergic Pharmacology I Flashcards

0
Q

Symptoms of intoxication of muscarine mimic what branch of the ANS?

A

PNS

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1
Q

What was the first identified agonist of muscarinic receptors?

A

Muscarine (compound found in certain mushrooms)

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2
Q

SLUD refers to the rapid classic spectrum of generalized muscarinic receptor activation. What does SLUD stand for?

A

Salivation, lacrimation, urination, defecation

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3
Q

What is the effect of a muscarine receptor agonist on the skin?

A

Vasodilation

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4
Q

Why does ACh have virtually no therapeutic applications?

A

It’s actions are diffuse, rapid hydrolysis via AChe and BChe

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5
Q

What muscarinic agonist can be taken orally for post operative abdominal distinction and has the effects of increasing the contractile force of smooth muscle throughout the gastrointestinal tract?

A

Bethanecol

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6
Q

What are 3 examples of muscarinic agonists?

A

Bethanecol, methacholine, pilocarpine

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7
Q

What muscarinic agonist taken orally is used in gastric atony and increases the force of gastric contractions?

A

Bethanechol

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8
Q

What muscarinic agonist taken subcutaneously is used for non obstructive urinary retention and increases smooth muscle contractions of the bladder body?

A

Bethanechol

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9
Q

What muscarinic agonist is used in the diagnoses of asthma by causing Bronchoconstriction and broncho secretion that could trigger an asthmatic event in a patient with asthma also has slight susceptibility to ChE?

A

Methacholine

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10
Q

What muscarinic agonist can be taken orally for xerostomia (dry eye/mouth) and facilitates lacrimal and salivary secretions?

A

Pilocarpine

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11
Q

What muscarinic agonist instilled into the eye is used to treat glaucoma by increased drainage of aqueous humor and relieves intraocular pressure

A

Pilocarpine

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12
Q

Glaucoma is characterized by too much pressure buildup in what part of the eye causing the lens to be pushed back into the retina?

A

Anterior chamber

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13
Q

Where does the aqueous humor drain?

A

Canal of schlemm

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14
Q

What are the two mechanisms behind glaucoma?

A

Too much production

Not enough drainage

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15
Q

What is characterized by an increase in intraocular pressure, leads to damage of ocular disk and irreversible blindness, leading cause of blindness in African Americans and third leading cause in Caucasians?

A

Glaucoma

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16
Q

What are the two types of glaucoma?

A
Narrow angle (acute congestive)
Wide angle (chronic simple)
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17
Q

What type of glaucoma requires drug treatment for management of an acute attack?

A

Narrow angle (acute congestive)

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18
Q

What type of glaucoma has a gradual insidious onset and requires chronic drug therapy?

A

Wide angle (chronic simple)

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19
Q

How do muscarinic agonsts (pilocarpine) lead to increased drainage of the aqueous humor by widening the canal of schlemm and decreasing ocular pressure?

A

Mimics PNS by causing ciliary muscle to contract/accomodation (when ciliary muscle contracts it opens canal of schlemm wider)

20
Q

Why are bethanechol and pilocarpine therapeutically useful muscarinic agonists?

A

Resistant to ChE
Limited or no nicotinic activity
Retain activity at relevant organ systems

21
Q

What muscarinic agonist has miotic action useful in reversing a narrow angle glaucoma attack, reversing mydriasis produced by atropine and some usefulness in wide angle glaucoma?

A

Pilocarpine

22
Q

What are some contraindications of muscarinic agonist use?

A

Asthma - increase bronchial secretion and smooth muscle contraction precipitating asthma attack
Peptic ulcer disease - increase acid secretion
Sweating, abdominal cramps, difficulty in visual accommodation, salvation

23
Q

Atropine is a plant alkaloid and potent selective muscarinic receptor antagonist from what plant?

A

Atropa Belladonna

24
Q

What blocks M3 muscarinic receptors in the eye, which blocks ACh action on circular fibers causing circular fibers to relax and pupil diameter to increase?

A

Atropine

25
Q

Muscarinic receptor antagonists inhibit what branch of the ANS?

A

PNS

26
Q

Why is there slight cardiac slowing with small doses of atropine?

A

Regulatory muscarinic receptors that regulate PNS if these are blocked PNS works better

27
Q

The effects of atropine are consistent with what?

A

PNS inhibition

28
Q

What are 4 muscarinic receptor antagonists?

A

Atropine, scopolamine, ipratropium, pirenzipine

29
Q

What muscarinic receptor antagonist has some selectivity for M1 receptors over M2 or M3?

A

Pirenzipine

30
Q

How does one overcome the lack of selectivity for the muscarinic receptor antagonists?

A

Local administration (ex: pulmonary inhalation, installation into the eyes)

31
Q

What was historically used for the treatment of peptic ulcers, has some selectivity for M1 now largely replaced by H. Pylori therapy, H2 antagonists, and proton pump inhibitors?

A

Pirenzipine

32
Q

What muscarinic antagonist is used to treat irritable bowel syndrome, can reduce tone and motility throughout gut tract, limited usefulness in many cases?

A

Atropine

33
Q

What muscarinic receptor antagonist is used to treat urinary disorders?

A

Oxybutynin ( glycopyrrolate, methscopolamine)

34
Q

What muscarinic antagonist is used to treat mild cystitis? ( anti microbial therapy essential in bacterial cystitis)

A

Oxybutynin ( glycopyrrolate, methscopolamine)

35
Q

What muscarinic receptor antagonist can be taken orally or via catheter to treat bladder spasm, post surgical prostatectomy and neurologic disease?

A

Oxybutynin ( glycopyrrolate, methscopolamine)

36
Q

What muscarinic receptor antagonist is used in chronic obstructive pulmonary disease COPD and asthma, blocks all muscarinic receptor subtypes, has minimal inhibitory effect on mucocilliary clearance relative to atropine?

A

Ipratropium

37
Q

What muscarinic antagonist has parenteral administration, tachycardia, bronchodilation, and inhibition of secretion?

A

Ipratropium

38
Q

What muscarinic antagonist when inhaled actions confined almost exclusively to mouth and airways, 90% of inhaled drug is swallowed, has very inefficient absorption from GI tract and has the common side effect of dry mouth?

A

Ipratropium

39
Q

What muscarinic antagonist has some utility in asthma but limited can provide virtually complete protection against Bronchoconstriction produced by subsequent inhalation of substances such as cigarette smoke, not as effective against stimuli such as histamine, bradykinin or prostaglandin

A

Ipratropium

40
Q

What muscarinic receptor antagonist is used in ophthalmology to induce mydriasis (pupil dilation- often required for thorough examination of retina and optic disc) and cyclogia (paralysis of ciliary muscle)?

A

Atropine

41
Q

What muscarinic receptor antagonist is used to treat motion sickness, the patch (TRANSDERM SCOP) delivers 0.5mg of this drug over 72 hours

A

Scopolamine

42
Q

What muscarinic receptor antagonist is used to treat poisoning by muscarine containing mushrooms?

A

Atropine

43
Q

What stimulation can result in complex and often unpredictable series of effects, wide range of systems affected: skeletal NMJ, autonomic ganglia, CNS, stimulation can desensitize receptors leading to excitation at low doses and block at high doses?

A

Nicotine

44
Q

Low doses stimulate, larger doses result in initial stimulation followed by very quick longer lasting blockade of transmission also increased heart rate, blood pressure, increase in GI motility describes what?

A

Nicotine effect on ANS

45
Q

Similar to ANS, stimulant phase usually obscured by rapidly developing paralysis describes what?

A

Nicotine effect on NMJ

46
Q

Effective stimulant, high dose stimulation followed by depression-central paralysis, chemoreceptor trigger zone stimulation- vomiting

A

Nicotine effect on CNS

47
Q

What amount of acute nicotine is fatal in adults?

A

60mg

48
Q

What are 4 things to treat nicotine toxicity?

A

Induce vomiting
Gastric lavage (stomach pump)
Respiratory assistance
Treatment of shock