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STEP 1 (5) > Pharm- Autonomic Drugs > Flashcards

Pharm- Autonomic Drugs Flashcards

1
Q

Describe nicotinic receptors

A

these ACh receptors are ligand-gated Na/K channels

Two types: NN found on autonomic ganglia and NM found on neuromuscular junctions

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2
Q

Describe muscarinic receptors

A

ACh receptors that are G protein-coupled receptors that usually act through 2nd messengers

5 subtypes: M1-M5

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3
Q

Describe the a1 receptor

A

Gq coupled to produced vascular smooth muscle contraction, increased pupillary dilator muscle contraction (mydriasis), and intestinal and bladder sphincter muscle contraction

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4
Q

Describe the a2 receptor

A

Gi coupled receptor to produce decreased sympathetic outflow, decreased insulin release, decreased lipolysis, decreased aqueous humor production, and increased platelet aggregation

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5
Q

Describe the B1 receptor

A

Gs coupled receptor to produce increased HR, contractility, increased renin release, and increased lipolysis

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6
Q

Describe the B2 receptor

A

Gs coupled receptor to produce vasodilation, bronchodilation, increased lipolysis, increased insulin release, decreased uterine tone (tocolysis), ciliary muscle relaxation, and increased aqeuous humor production

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7
Q

Describe the M1 receptor

A

Gq coupled receptor to modulate the CNS and enteric nervous system

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8
Q

Describe the M2 receptor

A

Gi coupled receptor to porduce decreased HR and atrial contractility

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9
Q

Describe the M3 receptor

A

Gq coupled receptor to produce:

increased exocrine gland secretions (e.g. lacrimal, salivary, gastric acid), increased gut peristalsis, increased bladder contraction, bronchoconstriction, increased papillary sphincter muscle contraction (miosis), ciliary muscle contraction (accommodation)

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10
Q

Describe the D1 receptor

A

Gs coupled receptor to relax renal vascular smooth muscle

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11
Q

Describe the D2 receptor

A

Gi coupled receptor to modulate NTM release in the brain

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12
Q

Describe the H1 receptor

A

Gq coupled receptor to produce nasal and bronchial mucus production, increased vascular permeability, pruritis, pain, and contraction of the bronchioles

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13
Q

Describe the H2 receptor

A

Gs coupled receptor to increased gastric acid secretion

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14
Q

Describe the V1 receptor

A

Gq coupled receptor to increased vascular smooth muscle cotnraction

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15
Q

Describe the V2 receptor

A

Gs coupled to increase H2O permeability and reabsorption in the collecting tubules of the kidney

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16
Q

What are the autonomic receptors coupled to Gq?

A

H1, a1, V1, M1

M3

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17
Q

What are the autonomic receptors coupled to Gs?

A

B1, B2, D1,

H2, V2

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18
Q

What are the autonomic receptors coupled to Gi?

A

M2, a2, D2

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19
Q

What are the main cholinergic agonists?

A

Bethanechol

Carbachol

Methacholine

Pilocarpine

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20
Q

What are the main uses of Bethanechol?

A

Postoperative ileus, neurogenic ileus and urinary retention that works by activating the bowel and bladder smooth muscle (resistant to AChE)

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21
Q

What are the main uses of Carbachol?

A

Constriction of the pupil and relieving intraocular pressure in glaucoma

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22
Q

What are the main uses of Methacholine?

A

challenge test for asthma that stimulates muscarinic receptors in airways when inhaled

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23
Q

What are the main uses of Pilocarpine?

A

Potent stimulator of sweat, tears, and saliver for open angle glaucoma

24
Q

What are the anti-AChEs (indirect cholinergic agonists)?

A

Donepeil, Rivastigmine, Galantamine

Edrophonium

Nesostigmine

Physostigmine

Pyridostigmine

25
Q

What are the main uses of Donepeil, Rivastigmine, Galantamine?

A

Alzheimer tx

26
Q

What are the main uses of Edrophonium?

A

Diagnosis of myasthenia gravia (Extremely short acting) but it is now more commonly diagnosed via anti-AChR Ab test

27
Q

How might cholinesterase inhibitor poisoning present (commonly due to organophosphates seen in insecticides- usually seen in farmers)?

A

DUMBBELSS

Diarrhea, Urination, Miosis, Bronchospasm

Bradycardia, Excitation of skeletal muscle and CNS

Lacrimation, Sweating, and Salivation

28
Q

What is the antidote for cholinesterase toxicity?

A

Atropine and Pralidoxime (regenerates AChE if given daily)

29
Q

What is a major use of Pyridogstigmine?

A

Increases ACh for tx of Myasthenia gravis

30
Q

What is a major use of physostigmine?

A

atropine overdose

31
Q

What are the major muscarinic antagonists?

A

Atrophin, homatropine, tropicamide (prouces mydriasis and cycloplegia)

Benztropine (Parkinson disease tx)

Glycopyrrolate (drooling, peptic ulcer)

Hyoscyamine, Dicyclomine (Antispasmodics for IBS)

Ipratropium, tiotropium (COPD, asthma)

Scopolamine (Motion sickness)

32
Q

What are oxybutynin, Solifenacin, and Tolerodine?

A

Muscarinic antagonists that reduce bladder spasms and urge urinary incontinence in tx of overactive bladder

33
Q

What are the main physiologic outcomes of atropine (muscarinic antagonist) use?

A

Pupil dilation and cycloplegia

decreased airway secretions

decreased stomach secretions

decreased gut motility

decreased urgency in cystitis

34
Q

What are the AEs of atropine?

A

elevated body temp due to decreased sweating

rapid pulse, dry mouth, dry skin

cycloplegia

constipation

can cause acute angle-closure glaucoma in elderly

disorientation

35
Q

What is Tetrodotoxin?

A

Highly potent toxin found in pufferfish that binds fast voltage-gated N+ channels in cardiac and nerve tissue preventing depolarization (blocks AP with changing resting potential), resulting in symptoms of nauseas, diarrhea, wekaness, dizziness, loss of reflexes, and paresthesias

Tx: supportive

36
Q

What is Ciguatoxin?

A

Toxin released during ingestion of reef rish (e.g. barracuda, snapper, moray ell) that causes ciuatera fish poisoning by opening Na+ channels causing depolarization

37
Q

How does ciguatoxin poisoning present?

A

Symptoms often confused with cholinergic poisoning and include:

Temp-related dysesthesia (e.g. cold feels hot, hot feels cold) is the classic finding

Tx is supportive

38
Q

What causes SCOMBROID poisoning?

A

Caused by consumption of dark-meat fish such as bonito, mahi-mahi, and tuna) that is improperly stored at warm temps

39
Q

How does c present?

A

Acute-onset of burning sensation of the mouth, flushing of the face, erythema, urticaria, pruritis, and HA

May cause anaphylaxis like presentation with bronchospasm, angioedema, and hypotension (frequently misdiagnpsed as fish allergy)

40
Q

What mediates scrombroid poisoning?

A

Bacterial histidine decarboxylase converts histidine to histamine which is not degraded by cooking (tx with antihistamines if needed)

41
Q

What receptors does albuterol and salmeterol act on?

A

B2 > B1

42
Q

What are the uses of albuterol and salmeterol?

A

albuterol for asthma

salmeterol for long-term asthma or COPD control

43
Q

What receptors does Dobutamine bind to?

A

B1 > B2,a for tx of heart failure (inotropic > chronotropic) and cardiac stress testing

44
Q

What receptors does Dopamine bind to?

A

D1=D2 > B > a for tx of unstable bradycardia, HF, shock (inotropic and chronotropic a effects predominate at high doses)

45
Q

What receptors does Epi bind to?

A

B > a for tx of anaphylaxis, asthma, open-angle glaucoma (a effects predominate at high doses)

Significantly stronger effect at B2 receptor than nor

46
Q

What receptors does Isoproterenol bind to?

A

B1 = B2 for tx of eelectrophysoiologic evaluation of tachyarrhyhtmias (can worsen ischemia)

47
Q

What receptors does Nor bind to?

A

a1 > a2 > B1 for tx of hypotension (but decreases renal perfusion)

48
Q

Note about the tx of cocaine overdose:

A

Never give BBs if suspected because it can lead to unopposed a1 activation and extreme HTN

49
Q

Note about Nor and Iso

A

Nor increases systolic and diastolic pressures as a result of a1-mediated vasoconstriction, which increases MAP and leads to reflex bradycardia

Iso has little a effect but causes B2-mediated vasodilation, resulting in decreased MAP and increased heart rate through B1 and reflex activity

50
Q

What are the uses of clonidine?

A

a2- agonist used for HTN crisis (does not decrease renal blood flow)

ADHD and Tourette Syndrome (only if they are both present)- if only ADHD- use a stimulant, and use an antipsychotic for Tourettes only

51
Q

What are some nonselective a-blockers and their applications?

A

Phenoxybenzamine for pheochromocytoma (preoperatively) to prevent catecholamine crisis

Phentolamine (reversible)- for tx of those on MAOIs who eat tyramine foods

52
Q

How would MAP change if you have epi followed by an a-blocker?

A
53
Q

How would MAP change if you have phenylephrine followed by an a-blocker?

A

MAP would increased after giving phenylephrine but only return to baseline after the a-blocker because phenylephrine has no B activity (pure a-agonist)

54
Q

What are the B1-selective BBs?

A

A to M

Acebutolol, atenolol, betaxolol, Esmolol, Metoprolol

55
Q

What are the nonselective BBs?

A

N to Z

Nadolol, Pindolol, Propranolol, Timolol

STEP 1 (5) (11 decks)

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