3 - Muscarinic Agonists Flashcards

1
Q

Diabetic autonomic neuropathy may _______

and affect _____

A

precede other complications

affect one or more organs

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2
Q

Mechanisms of neuropathy

A

Metabolic nerve damage
neurovascular insufficiency
AI damage
Neurohormonal growth factor deficiency

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3
Q

Clinically, the most important form of autonomic neuropathy

A

Caradiovascuar

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4
Q

Common in patients with liver disease

A

Autonomic (mainly VAGAL) dysfunction

Exaggerated by alcohol abuse

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5
Q

Advanced chronic liver disease is characterized by…

A

Peripheral arterial vasodilation

Increased plasma catecholamine concentrataions

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6
Q

Botulism toxin MOA

A

cleaves SNAP-25 in the SNARE complex

Inhibiting release of Ach in vesicles

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7
Q

Hyperthyroidism mimics ___________

A

hyperadrenergic state

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8
Q

Hyperthyroidism heart rate is __ and ___

A

irregular and fast

Treat with Beta blockers

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9
Q

Hyperthyroidism-related tachycardia is a contraindication for ____________

A

Muscarinic agonists (even though they decrease CO)

Can induce atrial fibrillation

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10
Q

Graves disease etiology

A

AI disease against TSH receptor –> activation

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11
Q

Crosstalk between Thyroid and Adrenal

A

Adrenal gland activation produces GC’s

GCs inhibit enzyme that converts T4 into active T3

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12
Q

Effect of reduced body weight

A

Lower T3 and Sy ANS

Heightened PSy

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13
Q

Hyperthyroidism causes _________ of adrenergic receptors

A

Desensitization

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14
Q

Hypothyroidism causes _________ of adrenergic receptors

A

Sensitization

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15
Q

Undiagnosed Hypothyroidism most common in women

A

iodine deficiency

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16
Q

Hashimotos thyroiditis symptoms

A

Cold, dry skin, hair loss, slowed heart rate

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17
Q

Cholinergic stimulation can reduce…

A

symptoms of neuropathic ANS disorders

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18
Q

Effects of cholinergic stimulation

A
Increase of ureteral peristalsis
BP increase
Increased GI tone
Bronchoconstriction + mucus secretion
Increase glandular activity
Miosis, drainage of anterior chamber
19
Q

Types of drugs that increase cholinergic stimulation

A

AchEI’s

Muscarinic agents

20
Q

Muscarine was the first _______

Problem/sides?

A

parasympathomimetic

Can cross BBB and cause convulsions

21
Q

Direct acting Cholinergic recepor agonists are ______

A

Esters

22
Q

Examples of direct cholinergic agonists

A

Ach
Bethanechol
Carbachol
Methacholine

23
Q

What causes the polarity of direct receptor agonists?

Due to the polarity of direct agonists, they have…

A

The quaternary ammonium

limited CNS distribution and GI absorption

24
Q

Carbachol acts on which receptors

A

mAchR + nAchR

25
Q

Methacholine acts on which receptors

A

All, but mostly mAchR

“M”uscarinic for “M”ethacholine

26
Q

Risk with nAchR activity

A

Systemic fatal OD

–> nicotinic receptors son diaphragm and IC’s

(still low risk d/t polarity)

27
Q

Ocular use for muscarinic agents

A

Treatment for glaucoma

reduces intra-ocular pressure

28
Q

Mechanisms for glaucoma

A

Overproduction of humor

Drainage canal blockage

29
Q

Which type of glaucoma is the emergency?

A

Closed angle

canal of schlemm occluded between iris and corneal/scleral layer

30
Q

Endothelial cells with ____ secete aq. humor

A

B2-AR

31
Q

____ blocks B2AR in the endothelial cells of the eye

A

Timolol

blocks without miosis or loss of accommodation

32
Q

Muscarinic agonsts for the treatment of glaucoma

A

Carbachol

Pilocarpine

33
Q

Carbachol is a ____

PK?

A

Full agonist, longer acting

2-5 minute onset, can last 24h if intra-ocuar

34
Q

Pilocarpiine is a ____

MOA?

A
Partial agonist (less headache)
relieves Canal of Schlemm blockage
35
Q

Sides for pilocarpine

A

Sweating, salivation, diarrhea, mucus secretion

Miosis (blurred vision, impaired night vision)

Reduced BBB function (can enter CNS and cause epilepsy at higher doses!)

36
Q

Bethanecatechol use

A

Urinary retention

Post-op ileus (GI atony)

37
Q

Avoid bethanecatechol use in

A

bladder outlet obstruction (stones, BPH, tumor)

38
Q

Bethanecatechol MOA

A

muscarinic selective, doesnt bind to nicotinic

resistant to AchE

39
Q

Cevimelie and pilocarpine uses

A

Xerostomia
After head/neck radiation
Sjogrens

40
Q

Nicotinic agonists for cessation

A

Nicotine (full agonist, protonated at acidic pH)

Varenicline (partial agonist of a4B2 nicotonic receptor, blocks nicotine from binding at the same time)

41
Q

Sides for Nicotine

A

Irritation at site, tachycaridia/arrhythmia, dyspnea

42
Q

Sides for Varenicline

A

GiT related

Dream stuff

43
Q

Varenicline reduces ________

A

effects of withdrawal