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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
What enzyme is lost in alzhiemers disease?
Choline Acetyltransferase (makes ach)
26
What are the two forms of acetylcholinesterases?
AChE (CNS) and BuChE (plasma)
27
What kind of drug is Donepezil (Aricept)
Reversible and noncompetitive inhibitor of AChE (less adverse effects due to high selectivity) Alzheimers
28
How is Aricept metabolized?
Liver and kidney
29
What kind of drug is Rivastigmine (Exelon)
Carbamate Acetylcholinesterase Inhibitor Active at both AChE and BuChE Alzheimers
30
What kind of drug is galantamine (razadyne)
Competitive and reversible AChE inhibitor Allosterically modulates nAChR Alzheimers long term
31
What is the main problem with taking Alzheimers drugs long term?
May exacerbate behavioral problems with long term use
32
What is the mechanism for organophosphate inhibition of AChE
Form a covalent bond between the phosphate and hydroxyl group of the active site serine
33
What is isoflurophate?
DFP Dyflos Long acting anticholinesterase (organophosphate) Sarin
34
What is echothiophate?
Phospholine Used as eye drops for glaucoma Organophosphate has a quat amine
35
What are the signs and symptoms of organophosphate exposure/ due to the muscarinic receptors?
Vomiting Bronchospasm Hypotension Bradycardia SLUD Overstimulation of the muscarinic acetylcholine receptors in the parasympathetic system
36
What are the signs and symptoms of organophosphate exposure due to overstimulation of muscle nicotinic receptors at the NMJ?
Muscle weakness Fasciculations Paralysis
37
What are the signs and symptoms of organophosphate exposure due to overstimulation of nicotinic and muscarinic receptors in the CNS?
Confusion Agitation respiratory failure Coma
38
What kind of drugs can reverse overstimulation of the Parasympathetic system?
Oximes 2Pam Obidoxime HI6
39
What is the primary cause of death with AChEIs?
Failure of the muscles of respiration
40
Why is the treatment of organophosphates long term?
They are lipophilic in nature
41
What is glaucoma associated with?
Ocular hypertension
42
What can untreated glaucoma lead to?
permanent damage of the optic nerve and resultant visual field loss and blindness
43
What is the primary strategy in glaucoma?
To reduce the production of aqueous humor and then to increase the outflow of aqueous humor Opens the trabecular meshwork
44
What antimuscarinic drugs are selective for muscarinic receptors over nicotinic receptors?
Tertiary amines and alkaloids
45
What kind of drug is atropine?
Anticholinergic Dilates the pupils
46
What saying can be used to recognize the antimuscarinic overdose?
Dry as a bone Blind as a bat Red as a beet Hot as a hare Mad as a hatter
47
Why do antimuscarinics cause dryness?
Blocks sweating and salivation
48
What do antimuscarinics cause blindness?
Dilates pupils and causes blurred vision Blocks ciliary muscle contraction and loss of accommodation
49
Why do antimuscarinics cause redness?
Causes flushing of the skin and an atropine rash
50
Why do antimuscarinics cause hotness?
Marked rise in body temperature due to decreased sweating
51
What do antimuscarinics cause anger?
Delirium and toxic psychosis
52
How is scopolamine unlike atropine if they are both antimuscarinics?
It crosses the bbb more readily so it can be used for motion sickness and can cause CNS effects at lower doses
53
What is dicyclomine (bentyl) used for?
IBS
54
What is tropicamide used for?
Mydriatic agent
55
What is cyclopentolate used for?
mydriatic agent
56
What does flavoxate HCl do?
Urispas Oral urinary antispasmodic Relaxes spasms and increases the capacity of the bladder
57
What does oxybutinin HCl do?
Ditropan Decreases hyperreflexively of bladder and urge to void Can be sold OTC
58
What does tolterodine do?
Detrol Used for urinary incontinence, frequency and urgency/bed wetting Causes detrusor muscle relaxation
59
What does darifenacin do?
Enablex Has M3 selectivity (antispasmodic)
60
What does solifenacin do?
Vesicare M3 selectivity for antispasmodic urinary incontinence
61
What is significant about trospium?
Sanctura Only quaternary amine for urinary incontinence
62
What is fesoterodine?
Toviaz Newest oral antispasmodic for over active bladder Non selective muscarinic receptor antagonist
63
What kind of antispasmodics have fewer side effects?
Extended release forms
64
What is myrbetriq?
Mirabegron Beta 3 adrenergic receptor agonist Treats over active bladder Relaxes detrusor muscle
65
What are the uses of Quaternary amines?
GI hypermotility Peptic ulcers Presurgical adjuncts COPD
66
What kind of antimuscarinic drugs have higher affinity for nicotinic receptors?
Quaternary amines
67
What is methscopolamine Br (Pamine) used for?
Reducing stomach acid secretion through M1 receptors (peptic ulcers) Quaternary amines
68
What is Tussigon used for?
Homatropine methylbromide Used with hydrocodone as an antitussive to discourage abuse
69
What is glycopyrrolate used for?
Robinul Peptic ulcer disease or before surgery Quaternary amine Long acting one is used for COPD
70
How do anticholinergics help COPD?
Block parasympathetic cholinergic induced bronchoconstriction and mucus hypersecretion
71
What is ipratropium used for?
Atrovent Used for bronchospasms/ limits secretions Muscarinic antagonist Quaternary amine - short acting but cheaper
72
What is tiotropium used for?
Spiriva Longer duration than ipotropium Has selectivity for M1 and M3 receptors Decrease secretions and bronchospasms
73
What is Aclidinium Br used for?
Tudorza Pressair Long acting quat amine muscarinic antagonist use for COPD Hydrolyzed in the plasma
74
What is Umeclidinium used for?
Incruse Elipta COPD Quat amine antimuscarinic that blocks ACh in the M3 receptors which causes relaxation of smooth muscle Extended duration of action
75
What is glycopyrronium Br used for?
Seebri COPD Highly selective for M3 over M2 so more focused on secretions and brochodilations
76
What is beztropine used for?
Cogentin Parkinsons disease used for the tremors (tertiary)
77
What is trihexyphenidyl (artane) used for?
Parkinsons disease
78
What are the side effects of anticholinergics?
Anti Slud
79
What is the antidote for anticholinesterase poisoning?
Atropine
80
What are the treatments for antimuscarine toxicity?
Physostigmine IV (to overcome muscarine block) Diazepam IV for cns effect
81
What diagnoses should you not use antimuscarinics for?
BPH Glaucoma Tachycardia MI CHF GI or Gu obstructions
82
What OTC medication should be avoided when taking antimuscarinics?
Antihistamines
83
What kind of channels are nicotinic receptors?
Ligand gated inotropic channels that mediate fast ach neurotransmission
84
What are the two families of nicotinic receptors?
Neuronal nicotinic (CNS and ganglia) Muscle nicotinic (neuromuscular junction)
85
When does nicotine act as a ganglionic blocker?
Following chronic exposure Sustained depolarization of postganglionic membranes inducing a depolarization block
86
Why is nicotine addictive?
It stimulates nicotinic receptors on dopaminergic neurons which causes a dopamine reward pathway
87
What are the first line therapies for smoking cessation?
Nicotine replacement therapies Psychotropics (buproprion) Partial nicotinic receptor agonist (varenicline)
88
How does varenicline chantix work?
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
Why is the chantix dose gradually increased over time?
Minimize treatment related nausea and insomnia
90
Why have ganglionic blocking agents been largely abandoned?
They lack selectivity so they block all autonomic responses (cause tachycardia)
91
What are the side effects of neuromuscular junction blockers?
Histamine release (bronchial secretions, hypotension, bronchospasm)
92
What are the indications for NMJ blockers?
Partial or full muscle paralysis
93
What is d-Tubocurarine?
It is a nondepolarizing (competitive inhibitor) of the Neuromuscular junction
94
What kind of NMJ blocker is vecuronium?
Ammonio steroids (act as a spacer for quaternary centers) Little to no effect on blood pressure and fewer side effects
95
What type of drugs are rocuronium, vecuronium and pancuronium?
Ammonio steroids Nondepolarizing competitive inhibitors
96
What is significant about atracurium and cisatracurium?
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
What is the antidote for rocuronium and vecuronium?
Sugammadex (bridion)
98
What is succinylcholine?
Non competitive / depolarizing inhibitor of the NMJ
99
What is phase 1 block?
has to do with succinylcholine Depolarizes the end plate and induces neuromuscular blockade (muscle relaxation after faciculations)
100
How is succinylcholine a noncompetitive inhibitor?
It is not antagonized by achei
101
What is phase 2 block?
With continued presence of succinylcholine, desensitizes nicotinic receptors
102
What are the side effects of succinylcholine?
Hyperthermia Metabolic acidosis Tachycardia
103
What is the treatment for succinylcholine?
Admin of dantrolene IV Blocks the release of Calcium from SR at the ryanodine receptor
104
What is tizanidine?
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
What is baclofen?
Lioresal GABA b receptor agonist Gi-coupled metabotropic gaba receptor linked to channels Hyperpolarization of muscles (reduce Ca influx)
106
What is dantrolene?
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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