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Other Nervous System Pharmacology Flashcards

(128 cards)

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1
Q

Nondepolarizing neuromuscluar blocking drugs

A

Used for muscle paralysis during mechanical ventilation or surgery.
Used for long term motor paralysis which may occur within 5 minutes and most agents are later excreted or metabolized by the liver

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2
Q

How do nondepolarizing neuromuscular blocking drugs work

A

Competitive antagonists with acetylcholine at the post junctional membrane nicotonic receptors of the neuromuscular junction leaving fewer bindin gsitres for ach

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3
Q

Are nondepolarizing neuromuscular blocking drugs reversible

A

Yup

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4
Q

How do you reverse nondepolarizing neuromuscular blocking drugs

A

Cholinesterase inhibitors

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5
Q

What can cholinesterase inhibitors be used to diagnose

A

Myasthenia gravis

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6
Q

Suffix of nondepolarizing neuromuscular blocking drugs

A

Rium besides tubocurarine

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7
Q

Examples of nondepolarizing neuromuscular blocking drugs

A

Tubocurarine, atracurium, mivacurium, pancuronim, vecuronium, rocuronium

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8
Q

Nondepolarizing neuromuscular blocking drugs are competitive antagonists

A

With acetylcholine at the post junctional membrane nicotonic receptors of the neuromuscular junction. Leave few binding sites

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9
Q

Nondepolarizing neuromuscular blocking drugs reversal

A

Cholinesterase inhibitors

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10
Q

Nondepolarizing neuromuscular blocking drugs. What cholinesterase inhibitors may be used to reverse

A

Neostigmine and edrophonium

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11
Q

Diagnosis and treatment of myasthenia gravis

A

Diagnose with neostigmine and edrophonium

Treat with neostigmine

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12
Q

Succinylcholine

A

Paralytic agent used for surgeries or short procedures such as intubation

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13
Q

How does succinylcholine work

A

Binding at motor nicotonic acetylcholine receptors and keeping myocytes in a depolarizes state
Prevents ach from binding to receptors and muscle contraction

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14
Q

What is the first phase of succinylcholine mechanism of action

A

Phase 1-administered agent is non-reversible. Myocytes still have succinylcholine actively bound to motor nicotonic receptors and there is constantt depolarizes state.
Patients often show fasciculations and held contractions

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15
Q

What is phase 2 of succinylcholine mechanism of action

A

Receptors become sensitized and repolarize. They can only be aroused for action potential with larger amounts of acetylcholine, which is why neostigmine can be used to help reverse paralysis in phase 2

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16
Q

How can we reverse phase II of succinylcholine

A

Neostigmine (an acetylcholinesterase inhibitor )

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17
Q

Major side effect of succinylcholine

A

Malignant hyperthermia

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18
Q

Who should we not give succinylcholine to

A

Patients in a hyperkalamic state

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19
Q

Indications for succinylcholine

A

In surgery or short procedures can be used for patients in trauma care to help withintubation or those undergoing electroconvulsive therapy

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20
Q

How does succinylcholine cause neuromuscular block

A

Binds to the nicotonic acetylcholine receptor and keeps the muscular action potential stuck in a depolarizes state

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21
Q

What receptor does succinylcholine bind to

A

Motor nicotinic receptor , which normally binds ach

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22
Q

Succinylcholine is an ach receptor ___

A

Agonist

Opens sodium channels and causes membrane depolarization

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23
Q

Why does succinylcholine prevent muscular contraction

A

Cells cant repolarize and contract again

Can be observed immediately after IV. Patients fasciculate and are unable to contract again even after electrical stimulation

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24
Q

Phase 1 succinylcholine

A

Maintaining the muscle cels membrane potential above threshold.
Cells kept in a depolarizes state as succinylcholine is bound to the receptor and succinylcholine isn’t broken down quickly .
This period of paralysis cant be overcome bc no where for ach to bind

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25
Phase 2 succinylcholine
Cells being repolarized but blocked . The myocytes become sensitive to ach; they are desensitized This phase is reversible but needs a larger ach stimulus to cause contraction
26
How can we reverse phase 2 of succinylcholine
Neostigmine which prevents breakdown of ach in the plasma which leads to an increase ach concentration.
27
Why would we want to reverse phase 2 of succinylcholine
To overcome desensitization experience by paralyzed patients in phase 2
28
What do parkinsons drugs do
Counter neurotransmitter pathologies experienced by patients
29
How do parkinsons drugs work
Increase dopamine bioavailability or antagonizing acetylcholine
30
Describe parkinsons
Cell death in midbrain, with degeneration of the substantia nigra, which serves to generate dopamine. This leads to a neurotransmitter imbalance with decreased dopamine and relatively increased ach(a balance of these neurotransmitters is necessary for coordinated motor movement)
31
What are the antiparkinson drugs
BALSA | Bromocriptine, amantadine, levodopa, selegiline, antimuscarinics
32
Bromocriptine
Potent dopaminergic agonist
33
Amantadine
Unknown mechanism | But can also be antiviral
34
Levodopa (L-Dopa)
Dopamine isomer which readily crosses the BBB
35
Selegiline
Inhibits MAO-B , an enzyme which acts to break down dopamine.
36
Anti muscarinic drugs, like benztropine
Block cholinergic neuronal activity and are more successful at treating tremor and rigidity than bradykinesia
37
Parkinson
Neurodegeneratice disorder caused by death of dopamine generating cells in the substantia nigra. It is due to this cellular death and decreased dopamine the motor symptoms arise
38
Why do parkinsons get increase in ach
Bc dopamine decreases and there is an imbalance of neurotransmitters required for motor control (not a gross excess of ach, just an imbalance leading to higher ach in comparison to dopamine)
39
Bromocriptine
Ergot alkaloid Dopamine agonist and increases its bioavailability Also effects serotonergic, alpha adrenergic and glutamate receptors
40
Amantadine
Antiparkinsons and antiviral Increases dopamine release by a poorly understood mechanism Also has anticholinergic action
41
Levodopa
Dopamine isomer commonly administered with carbidopa Protected from breakdown by carbidopa in the gut and periphery and readily passes through the blood brain barrier to increase central dopamine bioavailability
42
Selegiline
MAO-B -enzyme which metabolizes dopamine int he body Selegiline is an MAO-B inhibitor and prevents breakdown of dopamine, increasing its bioavailability
43
Antimuscarinic drugs, like benztropine
Block muscarinic receptors to curb cholinergic neuron activity. Works to alleviate tremor and rigidity associated with parkinsons but does not work well for treating bradykinesia
44
Levodopa/carbidopa
Levocarb Treat parkinsons Increases dopamine delivery in the brain.
45
Does levodopa cross the BBB
Yup
46
What happens to levodopa once cross BBB
Converted to dopamine centrally
47
Why is levodopa given with carbidopa
Inhibits DOPA decarboxylase, and protects L dopa from being broken into dopamine peripherally and in the gut before it crosses the BBB
48
Side effect of levocarb
Arrhythmia/tachyarrhythmia | Dyskinesia
49
Why does levocarb cause arrhythmia
Peripheral conversion of the drug into catecholamine But usually mitigated by carbidopa
50
Why does levocarb cause dyskinesia
Distortion or difficulty with voluntary movement may occur with long term use
51
Carbamazepine (tegretol)
Anticonvulsant medication that decreases seizure activity caused by high frequency neuronal discharge
52
Indication for carbamazepine (tegretol)
Seizures Trigeminal neuralgia Symptoms associated with bipolar disorder
53
Side effects of carbamazepine (tegretol)
``` Blurred vision, vertigo, and headache are common Steven-johnson syndrome (SJS) Toxic epidermal necrolysis (TEN) Hepatotoxicity Blood dyscrasias (aplastic anemia) ```
54
Why not give carbamazepine (tegretol) to pregnant women
Teratogen
55
What do when give patient carbamazepine
Monitor for signs of water retention
56
Why not give someone on carbamazepine (tegretol) grapefruit juice
Increases serum carbamazepine
57
How does carbamazepine work
Binds to sodium channels and prevents the normal action potential activity resulting in prolonged sodium channel inactivity and decreased neuronal excitability that leads to seizure activity
58
Indications for carbamazepine
Seizures Bipolar Trigeminal neuralgia
59
How does carbamazepine treat seizures
Prolongs inactivation of sodium channels and suppresses high frequency neuronal discharge that contribute to the development of partial seizures and tonic clones seizures. This drug does not help treat absence, myoclonic, or atomic seizures
60
How does carbamazepine treat bipolar
It is an antiepilectic drug used to suppress mania and stabilize mood. Continued use may prevent mania and depression
61
How does carbamazepine treat trigeminal neuralgia
Decreases neuropathic pain along the trigeminal nerve but is not indicated as an analgesic for other types of pain
62
Why might carbamazepine cause nystagmus, blurred vision, and diplopia
Idk but tolerance with continued use
63
Why does carbamazepine cause ataxia , vertigo, headache
In first weeks. | Minimize by starting on low dose with largest dose at bedtime
64
Whay does carbamazepine cause hepatotoxicity
Increases the number of drug metabolizing enzymes in the liver A dysfunctional liver may lead to liver damage and result in hepatotoxicity and hepatitis
65
How manage liver concern in patient on carbamazepine
Do liver tests | Inform patient to contact doctor if get symptoms of liver damage
66
What are symptoms of liver damage
Dark urine, clay colored stools, jaundice , rash
67
Why does carbamazepine cause blood dyscrasias (agranulocytosis and fatal aplastic anemia)
May cause bone marrow suppression
68
How manage blood dyscrasias in patient on carbamazepine
Obtain blood count before treatment Do not give to patients with pre existing hematologist abnormalities Notify physician if patient has symptoms of blood dyscrasias
69
What are symptoms of blood dyscrasias
Fever, pallor, weakness, easy bruising, petechiae
70
Why does carbamazepine cause water retention
Increases secretion of ADH and inhibits renal excretion of water. Leading to water retention and decreased blood osmolarity
71
Who may water retention be determinetal to
Patients with heart failure
72
How manage a patient on carbamazepine if concerned about water retention
Monitor sodium level in serum
73
How does carbamazepine cause SJS, rash, toxic epidermal necrolysis
Genetic variation primarily found in patients of Asian descent have an increased susceptibility of developing SJS or TEN on carbamazepine
74
What do if patient has rash? SJS or TEN?
Antihistamine | Stop the drug
75
Why avoid grapefruit juice on carbamazepine
Grapefruit juice prevents normal drug metabolism and increases serum levels Increases the amount of toxic carbamazepine to toxic plasma levels
76
Memantine
NMDA receptor antagonist which helps prevent excitotoxicity in patients with Alzheimer’s disease It is a glutamergic antagonist at NMDA receptors
77
How does memantine work
Halting an influx of Ca preventing excitotoxicity to neurons, (neuronal excitotoxicity is mediated by Ca which activated intracellular enzymes leading to cell destruction ) this shows symptomatic improvement in patients
78
Side effects of memantine
Confusion and hallucinations
79
General purpose of memantine
NMDA receptor antagonist which helps prevent excitotoxicity in patients with Alzheimer’s disease
80
Memantine is a glutamatergic __ at NMDA receptors
Antagonist (impede an influx of Ca , halting excitotoxicity to neurons) this drug is low affinity and short acting with a modest effect
81
How does memantine prevent excitotoxicity
Antagonizing NMDA receptors | Preventing excitotoxicity
82
How does excitotoxicity happen
Ca which activates intracellular enzymes leading to cell destruction
83
Donepezil
Acetylcholinesterase inhibitor used to treat Alzheimer’s disease
84
What other drug can be used for Alzheimer’s
Rivastigmine
85
How does donepezil work
Inhibiting the actions of acetylcholinesterase which acts to break down the neurotransmitter acetylcholine Leading to an increase in circulating ach
86
Side effects of donepexzil
Related to excess cholinergic activity | Include dizziness, nausea, and vomiting, vivid dreams, and GI upset
87
Sumatriptan
Triptan family | For acute migraines and cluster headaches
88
Half life of sumatriptan
Short 2 hours
89
How does sumatriptan work
Agonist at 5HT 1B/1D autoreceptors and acts to inhibit the firing of serotonin neurons Causing a reduction in the synthesis and release of serotonin
90
What happens when sumatriptan binds to 5HT 1B/1D receptors
Adenylate cyclase is inhibited via regulatory G proteins, increasing intracellular Ca and affecting other intracellular events Eventually this results in inhibition of trigeminal nerve firing and vasoconstriction
91
Side effects of sumatriptan
Coronary vasospasm which may lead to MI
92
Who should we not give sumatriptan to
Prinzmetals angina or severe coronary artery disease
93
How do Tristan’s inhibit trigeminal nerve activation
Inhibit firing of trigeminal nerve
94
Why do Tristan’s cause vasoconstriction
Inhibit AC and intracellular Ca increases causing vasoconstriction and reduces vascular dilation
95
Why does sumatripatan cause coronary vasoaspam
Can cause MI
96
Why not give sumatriptan to people with prinzmetals angina or people with CAD
Due to vasospastic side effects
97
Butorphanol
For migraine headaches and severe pain (labor pains)
98
How does butorphanol work
Mixed actions at the receptor level and is an agonist for micro and kappa receptors while being a competitive antagonist at micro receptors
99
What is the significance of butorphanol being an agonist/antagonist at micro receptors
It causes less respiratory depression than full opioid agonist drugs
100
Side effects butorphanol
Withdrawal Usually happen when patient also treated with full opioid agonist -competing with the opioid at micro receptors competing with the adjunct opioid drug being taken leading to withdrawal
101
Indications for butorphanol
Migraine , severe pain, labor
102
How is butorphanol administered for migraine
Nasal spray
103
Is butorphanol more effective in women or men
Women labor
104
Micro receptors
Mu receptor
105
Withdrawal symptoms from butorphanol . How can we treat
Naloxone-but cant reverse overdose really
106
Gabapentin
To treat different seizure presentations, peripheral neuropathic pain and migraine prophylaxis Bipolar and post herpetic neuralgia-off label though
107
What was the original purpose of gabapentin
GABA analog but does not act on the same neuronal receptors
108
How does gabapentin works
A lot of gaps in knowledge | Inhibitshigh coltage gated Ca channels leading to decreased levels of mono amine neurotransmitters
109
Side effects of gabapentin
Sedation/sluggish | Ataxia
110
Indication for cabapentin (primary)
Seizure bc has anticonvulsant actions against smile and complex partial seizures as well as tonic clonic generalized seizures (grand mal)
111
Indication for gabapentin (secondary)
Peripheral Neuropathy (chronic neuropathic pain or fibromyalgia), postherpetic neuralgia (along dermatomic regions in response to varicella infections-but pregabalin is more commonly used), bipolar (combined with another mood stabilizer), migraine prophylaxis
112
Mechanism of action gabapentin
Inhibits voltage gated Ca channels inhibiting their action and decreasing monoamine neurotransmitters.
113
Pregabalin (Lyrica)
GABA analog that binds to the nerve terminals of the calcium channels and prevent calcium influx , which inhibits release of certain neurotransmitters
114
Indication for pregabalin
Seizures, neuropathic pain and fibromyalgia
115
Side effects of pregabalin
Dizziness, somnolence, weight gain, headache, angioedema
116
Patients on pregabalin have an increased risk of developing ___ or __ __
Rhabdomyolysis | Drug dependence
117
How does pregabalin work
Bind and inhibit Ca channels at nerve terminal and inhibits calcium influx. Decreases release of glutamate, norepinephrine, and substance P
118
How does decrease in neurotransmitters from pregabalin help control seizures
Control them and give relief to neuropathic pain
119
Pregabalin is a GABA analog, does it enhance GABA inhibitory actions?
Nope
120
How does pregabalin decrease seizure
Decreasing abnormal electrical activity int he brain
121
How does pregabalin help with neuropathic pain
Alters chemicals int he brain responsible for transmitting pain signals across the nervous system and decrease neuropathic pain
122
How can pregabalin help diabetics
Neuropathic pain associated with nerve damage
123
How can pregabalin help patients with spinal cord injury caused by herpes zoster
Receive pain
124
How can pregabalin help patients with fibromyalgia
They may have neuropathic pain relief
125
How does pregabalin help fibromyaligai
Decrease pain | But decrease pain relief after a few months
126
Side effects pregabalin
Headache, dizziness, somnolence, weight gain, angioedema (allergic type reaction), rhabdomyolysis
127
What is a problem with pregabalin
Dependence
128
Pregabalin is listed as what
Under schedule V of the drug enforcement agency’s controlled substances act

Pharmacology (52 decks)

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