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test 2 Flashcards

1
Q

Where do direct acting agonist bind?

A

Directly to cholinergic receptors

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2
Q

What affects do direct acting agonists have on the heart?

A

Decrease conduction
Brady cardia

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3
Q

What affects do direct acting agonists have on visceral smooth muscle?

A

Increase motility in the Gi
Increase detrusor muscle tone
Decrease sphincter tone

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4
Q

What affect do direct acting agonist have on the eyes?

A

Contracts the sphincter of the iris, contraction of the ciliary muscle, decrease ocular pressure (allows for accomodation)

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5
Q

What affects do direct acting agonists have on exocrine glands?

A

Increase in SLUDD
Sweat
Lacrimation
Urination
Digestion
Diarrhea

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6
Q

What is acetylcholine used for?

A

It is a direct acting agonist used for ophthalmology

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7
Q

What is methacholine used for?

A

Test bronchial hyper reactivity (Bronchiolar constriction of direct acting agonist)
Has muscarinic selectivity

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8
Q

What is carbachol used for?

A

Direct acting agonist used for opthalmology
Has increased stability

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9
Q

What is bethanechol (urecholine) used for?

A

Bladder and GI Hypotonia
Direct acting agonist that is more stable and has muscarinic selectivity

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10
Q

What is pilocarpine used for?

A

Glaucoma and xerostomia it is a muscarinic selective direct acting agonist

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11
Q

What is cevimeline used for?

A

Xerostomia
Sojourn’s Syndrome
Selective on the M3 receptor direct acting agonist

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12
Q

What is the treatment for toxicity of cholinomimetic compounds?

A

Atropine (or other muscarinic receptor antagonist)

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13
Q

How do indirecting acting Cholinomimetics work?

A

They are cholinesterase inhibitors (increase amounts of ACH in the synaptic terminal)

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14
Q

What is the main difference in responses between direct acting and indirect acting cholinomimetics?

A

Indirect acting has the addition of nicotinic responses (muscle and CNS)

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15
Q

What are the main therapeutic targets of AChE inhibitors?

A

Skeletal muscle
Central nervous system for Alzheimers
Decrease intraocular pressure of the eye
SLUDD

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16
Q

What is the role of edrophonium?

A

To diagnose myasthenia gravis but it is a simple alcohol so too short acting so we do not use anymore

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17
Q

What are carbamate esters also called?

A

Medium acting anticholinesterases
Sometimes called suicide inhibitors (parent compounds are cleaved by enzyme)

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18
Q

What kind of AChEI is neostigmine?

A

Reversible medium acting anticholinesterase (carbamate ester)

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19
Q

What does neostigmine do?

A

Prostigmin or neostigmine is used to reverse competitive neuromuscular block that happens during myasthenia gravis

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20
Q

What is pyridostigmine used for?

A

Mestinon
Used for myasthenia gravis (better absorption and duration of action than neostigmine)

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21
Q

What is physostigmine used for?

A

Used in eye drops for treatment of glaucoma

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22
Q

What is the most common type of irreversible dementia?

A

Alzheimer’s disease

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23
Q

What is the most common type of reversible dementia?

A

Delirium

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24
Q

What is the most common drug associated with delirium that has anticholinergic activity?

A

Diphenhydramine

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25
Q

What enzyme is lost in alzhiemers disease?

A

Choline Acetyltransferase (makes ach)

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26
Q

What are the two forms of acetylcholinesterases?

A

AChE (CNS) and BuChE (plasma)

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27
Q

What kind of drug is Donepezil (Aricept)

A

Reversible and noncompetitive inhibitor of AChE
(less adverse effects due to high selectivity)
Alzheimers

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28
Q

How is Aricept metabolized?

A

Liver and kidney

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29
Q

What kind of drug is Rivastigmine (Exelon)

A

Carbamate Acetylcholinesterase Inhibitor
Active at both AChE and BuChE
Alzheimers

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30
Q

What kind of drug is galantamine (razadyne)

A

Competitive and reversible AChE inhibitor
Allosterically modulates nAChR
Alzheimers long term

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31
Q

What is the main problem with taking Alzheimers drugs long term?

A

May exacerbate behavioral problems with long term use

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32
Q

What is the mechanism for organophosphate inhibition of AChE

A

Form a covalent bond between the phosphate and hydroxyl group of the active site serine

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33
Q

What is isoflurophate?

A

DFP
Dyflos
Long acting anticholinesterase (organophosphate)
Sarin

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34
Q

What is echothiophate?

A

Phospholine
Used as eye drops for glaucoma
Organophosphate has a quat amine

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35
Q

What are the signs and symptoms of organophosphate exposure/ due to the muscarinic receptors?

A

Vomiting
Bronchospasm
Hypotension
Bradycardia
SLUD
Overstimulation of the muscarinic acetylcholine receptors in the parasympathetic system

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36
Q

What are the signs and symptoms of organophosphate exposure due to overstimulation of muscle nicotinic receptors at the NMJ?

A

Muscle weakness
Fasciculations
Paralysis

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37
Q

What are the signs and symptoms of organophosphate exposure due to overstimulation of nicotinic and muscarinic receptors in the CNS?

A

Confusion
Agitation
respiratory failure
Coma

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38
Q

What kind of drugs can reverse overstimulation of the Parasympathetic system?

A

Oximes
2Pam
Obidoxime
HI6

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39
Q

What is the primary cause of death with AChEIs?

A

Failure of the muscles of respiration

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40
Q

Why is the treatment of organophosphates long term?

A

They are lipophilic in nature

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41
Q

What is glaucoma associated with?

A

Ocular hypertension

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42
Q

What can untreated glaucoma lead to?

A

permanent damage of the optic nerve and resultant visual field loss and blindness

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43
Q

What is the primary strategy in glaucoma?

A

To reduce the production of aqueous humor and then to increase the outflow of aqueous humor
Opens the trabecular meshwork

44
Q

What antimuscarinic drugs are selective for muscarinic receptors over nicotinic receptors?

A

Tertiary amines and alkaloids

45
Q

What kind of drug is atropine?

A

Anticholinergic
Dilates the pupils

46
Q

What saying can be used to recognize the antimuscarinic overdose?

A

Dry as a bone
Blind as a bat
Red as a beet
Hot as a hare
Mad as a hatter

47
Q

Why do antimuscarinics cause dryness?

A

Blocks sweating and salivation

48
Q

What do antimuscarinics cause blindness?

A

Dilates pupils and causes blurred vision
Blocks ciliary muscle contraction and loss of accommodation

49
Q

Why do antimuscarinics cause redness?

A

Causes flushing of the skin and an atropine rash

50
Q

Why do antimuscarinics cause hotness?

A

Marked rise in body temperature due to decreased sweating

51
Q

What do antimuscarinics cause anger?

A

Delirium and toxic psychosis

52
Q

How is scopolamine unlike atropine if they are both antimuscarinics?

A

It crosses the bbb more readily so it can be used for motion sickness and can cause CNS effects at lower doses

53
Q

What is dicyclomine (bentyl) used for?

A

IBS

54
Q

What is tropicamide used for?

A

Mydriatic agent

55
Q

What is cyclopentolate used for?

A

mydriatic agent

56
Q

What does flavoxate HCl do?

A

Urispas
Oral urinary antispasmodic
Relaxes spasms and increases the capacity of the bladder

57
Q

What does oxybutinin HCl do?

A

Ditropan
Decreases hyperreflexively of bladder and urge to void
Can be sold OTC

58
Q

What does tolterodine do?

A

Detrol
Used for urinary incontinence, frequency and urgency/bed wetting
Causes detrusor muscle relaxation

59
Q

What does darifenacin do?

A

Enablex
Has M3 selectivity (antispasmodic)

60
Q

What does solifenacin do?

A

Vesicare
M3 selectivity for antispasmodic urinary incontinence

61
Q

What is significant about trospium?

A

Sanctura
Only quaternary amine for urinary incontinence

62
Q

What is fesoterodine?

A

Toviaz
Newest oral antispasmodic for over active bladder
Non selective muscarinic receptor antagonist

63
Q

What kind of antispasmodics have fewer side effects?

A

Extended release forms

64
Q

What is myrbetriq?

A

Mirabegron
Beta 3 adrenergic receptor agonist
Treats over active bladder
Relaxes detrusor muscle

65
Q

What are the uses of Quaternary amines?

A

GI hypermotility
Peptic ulcers
Presurgical adjuncts
COPD

66
Q

What kind of antimuscarinic drugs have higher affinity for nicotinic receptors?

A

Quaternary amines

67
Q

What is methscopolamine Br (Pamine) used for?

A

Reducing stomach acid secretion through M1 receptors (peptic ulcers)
Quaternary amines

68
Q

What is Tussigon used for?

A

Homatropine methylbromide
Used with hydrocodone as an antitussive to discourage abuse

69
Q

What is glycopyrrolate used for?

A

Robinul
Peptic ulcer disease or before surgery
Quaternary amine
Long acting one is used for COPD

70
Q

How do anticholinergics help COPD?

A

Block parasympathetic cholinergic induced bronchoconstriction and mucus hypersecretion

71
Q

What is ipratropium used for?

A

Atrovent
Used for bronchospasms/ limits secretions
Muscarinic antagonist
Quaternary amine - short acting but cheaper

72
Q

What is tiotropium used for?

A

Spiriva
Longer duration than ipotropium
Has selectivity for M1 and M3 receptors
Decrease secretions and bronchospasms

73
Q

What is Aclidinium Br used for?

A

Tudorza Pressair
Long acting quat amine muscarinic antagonist use for COPD
Hydrolyzed in the plasma

74
Q

What is Umeclidinium used for?

A

Incruse Elipta
COPD
Quat amine antimuscarinic that blocks ACh in the M3 receptors which causes relaxation of smooth muscle
Extended duration of action

75
Q

What is glycopyrronium Br used for?

A

Seebri
COPD
Highly selective for M3 over M2 so more focused on secretions and brochodilations

76
Q

What is beztropine used for?

A

Cogentin
Parkinsons disease used for the tremors (tertiary)

77
Q

What is trihexyphenidyl (artane) used for?

A

Parkinsons disease

78
Q

What are the side effects of anticholinergics?

A

Anti Slud

79
Q

What is the antidote for anticholinesterase poisoning?

A

Atropine

80
Q

What are the treatments for antimuscarine toxicity?

A

Physostigmine IV (to overcome muscarine block)
Diazepam IV for cns effect

81
Q

What diagnoses should you not use antimuscarinics for?

A

BPH
Glaucoma
Tachycardia
MI
CHF
GI or Gu obstructions

82
Q

What OTC medication should be avoided when taking antimuscarinics?

A

Antihistamines

83
Q

What kind of channels are nicotinic receptors?

A

Ligand gated inotropic channels that mediate fast ach neurotransmission

84
Q

What are the two families of nicotinic receptors?

A

Neuronal nicotinic (CNS and ganglia)
Muscle nicotinic (neuromuscular junction)

85
Q

When does nicotine act as a ganglionic blocker?

A

Following chronic exposure
Sustained depolarization of postganglionic membranes inducing a depolarization block

86
Q

Why is nicotine addictive?

A

It stimulates nicotinic receptors on dopaminergic neurons which causes a dopamine reward pathway

87
Q

What are the first line therapies for smoking cessation?

A

Nicotine replacement therapies
Psychotropics (buproprion)
Partial nicotinic receptor agonist (varenicline)

88
Q

How does varenicline chantix work?

A

It is a partial agonist that binds selectively with high affinity to the alpha 4 beta 2 neuronal nicotinic ach receptors in the cns
(competitively inhibits binding of nicotine so the reward does not occur)

89
Q

Why is the chantix dose gradually increased over time?

A

Minimize treatment related nausea and insomnia

90
Q

Why have ganglionic blocking agents been largely abandoned?

A

They lack selectivity so they block all autonomic responses (cause tachycardia)

91
Q

What are the side effects of neuromuscular junction blockers?

A

Histamine release (bronchial secretions, hypotension, bronchospasm)

92
Q

What are the indications for NMJ blockers?

A

Partial or full muscle paralysis

93
Q

What is d-Tubocurarine?

A

It is a nondepolarizing (competitive inhibitor) of the Neuromuscular junction

94
Q

What kind of NMJ blocker is vecuronium?

A

Ammonio steroids
(act as a spacer for quaternary centers)
Little to no effect on blood pressure and fewer side effects

95
Q

What type of drugs are rocuronium, vecuronium and pancuronium?

A

Ammonio steroids
Nondepolarizing competitive inhibitors

96
Q

What is significant about atracurium and cisatracurium?

A

They are nondepolarizing agents that are not cleared renally (cleared through hoffman elimination) so they can be give to those with impaired renal function

97
Q

What is the antidote for rocuronium and vecuronium?

A

Sugammadex (bridion)

98
Q

What is succinylcholine?

A

Non competitive / depolarizing inhibitor of the NMJ

99
Q

What is phase 1 block?

A

has to do with succinylcholine
Depolarizes the end plate and induces neuromuscular blockade (muscle relaxation after faciculations)

100
Q

How is succinylcholine a noncompetitive inhibitor?

A

It is not antagonized by achei

101
Q

What is phase 2 block?

A

With continued presence of succinylcholine, desensitizes nicotinic receptors

102
Q

What are the side effects of succinylcholine?

A

Hyperthermia
Metabolic acidosis
Tachycardia

103
Q

What is the treatment for succinylcholine?

A

Admin of dantrolene IV
Blocks the release of Calcium from SR at the ryanodine receptor

104
Q

What is tizanidine?

A

Zanaflex
Centrally acting alpha 2 agonist
Increases presynaptic inhibition of motor neurons and nociceptive transmission in the dorsal horn (relieve spasms )
Fewer side effects than clonidine

105
Q

What is baclofen?

A

Lioresal
GABA b receptor agonist
Gi-coupled metabotropic gaba receptor linked to channels
Hyperpolarization of muscles (reduce Ca influx)

106
Q

What is dantrolene?

A

Dantrium
Works directly on the skeletal muscle
Blocks release of Ca from SR by binding to the ryanodine receptor

MPT (5 decks)

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