VIII - CNS Flashcards
1
Q
bind GABA-A receptor subunits to increase frequency of chloride channel opening which causes membrane hyperpolarization
A
benzodiazepines (TOPNOTCH)
2
Q
SE: anterograde amnesia, decreased psychomotor skills, unwanted daytime sedation, tolerance, dependence liability and rebound insomnia or anxiety
A
benzodiazepines (TOPNOTCH)
3
Q
BZD that can be used for seizure disorders, Bipolar disorder and infantile spasm
A
Clonazepam (TOPNOTCH)
4
Q
Why is Lorazepam preferred over Diazepam in status epilepticus
A
due to its long distribution halflife (TOPNOTCH)
5
Q
date-rape drug
A
Flunitrazepam (TOPNOTCH)
6
Q
BZD used for alcohol withdrawal
A
Diazepam and Chlordiazepoxide (TOPNOTCH)
7
Q
antagonist at benzodiazepine sites on GABA-A receptor
A
Flumazenil (TOPNOTCH)
8
Q
bind to GABA-A receptor sites to increase duration of chloride channel opening, block glutamic acid neurotransmission
A
barbiturates (TOPNOTCH)
9
Q
which has greater dependence liability: barbiturates or benzodiazepine
A
barbiturates (TOPNOTCH)
10
Q
Barbiturate with the highest lipid solubility
A
Thiopental (TOPNOTCH)
11
Q
barbiturate for status epilepticus
A
Phenobarbital (TOPNOTCH)
12
Q
SE: acute intermittent porphyria
A
barbiturates (TOPNOTCH)
13
Q
High dose BZD and Barbs may suppress seizure but at the expenses of marked sedation EXCEPT for
A
Clonazepam and Phenobarbital (TOPNOTCH)
14
Q
only interact with GABA-A receptors with alpha-1 subunit; For insomnia and sleep disorder esp when sleep onset is delayed
A
Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)
15
Q
dependence liability and withdrawal symptoms is less than that of benzodiazepines
A
Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)
16
Q
lack anti-convulsant, anti-anxiety and muscle relaxant effects, effects are reversed with Flumazenil, very rapid onset of action, may dec REM sleep
A
Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)
17
Q
increasing use due to rapid onset with minimal effects on the sleep pattern and cause less daytime cognitive impairment as compared to BZD
A
Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)
18
Q
partial agonist at 5-HT1A receptors and possibly D2 receptors, used For generalized anxiety disorders
A
Buspirone (TOPNOTCH)
19
Q
slow onset of action (more than 1week), metabolized by CYP3A4, safe for pregnant patients
A
Buspirone (TOPNOTCH)
20
Q
activates melatonin receptors (MT1 and MT2 receptors) in the suprachiasmatic nuclei in the CNS leading to dec latency of sleep onset
A
Ramelteon (TOPNOTCH)
21
Q
block voltage-gated Na channel; DOC for generalized tonic-clonic seizures, DOC for partial seizures, can be used for migraine
A
Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin (TOPNOTCH)
22
Q
SE: nystagmus, diplopia, sedation, gingival hyperplasia, hirsutism, anemias, peripheral neuropathy (absent DTRs), osteoporosis, fetal hydantoin syndrome, abnormalities in Vit D metabolism
A
Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin (TOPNOTCH)
23
Q
preferred in prolonged therapy for status epilepticus because it is less sedating
A
phenytoin (TOPNOTCH)
24
Q
block voltage-gated Na channels and decreases glutamate release; DOC for trigeminal neuralgia, DOC for generalized tonic-clonic seizures, DOC for partial seizures, for bipolar disorders
A
Carbamazepine, Oxcarbazepine (TOPNOTCH)
25
SE: diplopia, cognitive dysfunction, drowsiness, ataxia, blood dyscrasias, Stevens-Johnson syndrome, erythematous rash, teratogen (spina bifida and craniofacial anomalies), hyponatremia
Carbamazepine, Oxcarbazepine (hyponatremia) (TOPNOTCH)
26
may be used for acute manic phase and as prophylaxis in the depressive phase
Carbamazepine, Oxcarbazepine (TOPNOTCH)
27
blocks high-frequency firing of neurons which modifies amino acid metabolism; DOC for bipolar disorder (acute mania), DOC for generalized tonic-clonic seizures and absence seizure, partial seizures, myoclonic seizures, also used for Bipolar disorders
Valproic acid (TOPNOTCH)
28
anti-manic that is CYP450 inhibitor
Valproic acid (TOPNOTCH)
29
for status epilepticus in children ; primary anticonvulsant in infants, children and pregnant patients
Phenobarbital (TOPNOTCH)
30
inhibit low threshold (T-type) Ca currents esp in thalamic neurons ; DOC for absence seizure
Ethosuximide, Phensuximide, Methsuximide (TOPNOTCH)
31
blocks Ca channels, increases GABA release ; For neuropathic pain such as postherpetic neuralgia, partial seizures, migraine
Gabapentin, Pregabalin (TOPNOTCH)
32
structural analogues of GABA but does not activate GABA receptor directly ; also have the same effect on Ca currents like Ethosuximide
Gabapentin, Pregabalin (TOPNOTCH)
33
blocks Na and Ca channels and decreases glutamate, used for acute manic phase and as prophylaxis in the depressive phase
Lamotrigine (TOPNOTCH)
34
primarily undergoes glucuronidation reaction ; SE: dizziness, ataxia, nausea, rash, SJS / TEN
Lamotrigine (TOPNOTCH)
35
Bind synaptic protein selectively inhibiting hypersynchronization of epileptiform burst firing ; For generalized tonic-clonic seizures, partial seizures
Levetiracetam (TOPNOTCH)
36
not metabolized by CYP450 enzymes, eliminated in the kidneys in their unchanged form
Levetiracetam (TOPNOTCH)
37
multiple actions on synaptic function, probably via actions on phosphorylation (Na, Ca, GABA, AMPA-glutamate, carbonic anhydrase)
Topiramate, Felbamate (TOPNOTCH)
38
also facilitate the inhibitory actions of GABA but its exact MOA is still unknown
Felbamate (TOPNOTCH)
39
Antiseizure drugs with the most number of MOA, undergo both hepatic and renal metabolism
Topiramate, Felbamate (TOPNOTCH)
40
Irreversibly inactivates GABA aminotransaminase (GABA-T) which terminates the action of GABA ; For GTC seizure
Vigabatrin (TOPNOTCH)
41
Inhibits GABA transporter (GAT-1) in neurons and glia thus inhibiting its reuptake, leading to prolongation of GABA effects ; For partial seizures
Tiagabine (TOPNOTCH)
42
SE: visual field defects
Vigabatrin (TOPNOTCH)
43
Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N receptors
Inhalational anesthetics (TOPNOTCH)
44
SE: megaloblastic anemia on prolonged exposure; Euphoria (laughing gas), bronchodilation
Nitrous Oxide (TOPNOTCH)
45
Lowest Potency (highest MAC) and least cardiotoxic
Nitrous Oxide (TOPNOTCH)
46
all inhaled anesthetcis cause bronchodilation except
Desflurane (TOPNOTCH)
47
SE: catecholamine-induced arrhythmias, peripheral vasodilation, bronchodilation
Isoflurane (TOPNOTCH)
48
SE: spike-and-wave activity in EEG, muscle twitching, breath-holding, myocardial depression, renal insufficiency (due to Flourine release), dec cardiac output, bronchodilation
Enflurane (TOPNOTCH)
49
has pungent odor which limits its use
Enflurane (TOPNOTCH)
50
SE: catecholamine-induced arrhythmias, myocardial depression, post-operative hepatitis, dec cardiac output, bronchodilation
Halothane (TOPNOTCH)
51
Highest potency and lowest MAC (very slow onset and recovery)
Methoxyflurane (TOPNOTCH)
52
a usual adjunct with inhalational anesthetics and IV opioids, has a slow onset but longer DOA
Midazolam (TOPNOTCH)
53
Blocks excitation by glutamate at NMDA receptors; For dissociative anesthesia (analgesia, amnesia and catatonia but with retained consciousness)
Ketamine (TOPNOTCH)
54
congener of Phencyclidine / angel dust
Ketamine (TOPNOTCH)
55
For general anesthesia to patients with limited cardiac or respiratory reserve
Etomidate (TOPNOTCH)
56
Interacts with mu, sigma, kappa receptors for endogenous opioid peptides ; For high risk patients who might not survive general anesthesia
Opioid analgesics: Fentanyl, morphine, alfentanil, remifentanil (TOPNOTCH)
57
SE: respiratory depression, chest wall rigidity (which may cause impaired ventilation) and constipation
Opioid analgesics: Fentanyl, morphine, alfentanil, remifentanil (TOPNOTCH)
58
Antidote is Naloxone / Naltrexone
Opioid toxicity (TOPNOTCH)
59
milk of anesthesia
Propofol, Fospropofol (TOPNOTCH)
60
Potentiates GABA-A receptors, blocks Na channels; For prolonged sedation esp in ICU patients and also in OPD surgeries
Propofol, Fospropofol (TOPNOTCH)
61
Blockade of Na channels slows which prevents axon potential propagation
Local Anesthetics (TOPNOTCH)
62
Shortest half-life among local anesthetics
Procaine (TOPNOTCH)
63
For local anesthesia, topical anesthesia
Benzocaine, Cocaine, Tetracaine (TOPNOTCH)
64
Use cautiously in sunburns, Topical only
Benzocaine (TOPNOTCH)
65
with intrinsic sympathomimetic activity so it does not need an alpha agonist (like epinephrine) to limit its systemic absorption
Cocaine (TOPNOTCH)
66
All local anesthetics are vasodilators EXCEPT
Cocaine (TOPNOTCH)
67
SE: light-headedness, sedation, restlessness, nystagmus, seizures, respiratory, CV depression, abuse liability, severe hypertension, cerebral hemorrhage, cardiac arrhythmia, MI
Cocaine (TOPNOTCH)
68
For local anesthesia, spinal anesthesia, epidural anesthesia, topical ophthalmic anesthesia
Tetracaine (TOPNOTCH)
69
Blockade of Na channels slows which prevents axon potential propagation; For local anesthesia, antiarrythmia (group 1B activity), used for post-MI and for digitalis toxicity
Lidocaine (TOPNOTCH)
70
For local anesthesia, dental anesthesia
Prilocaine (TOPNOTCH)
71
local anesthetic that can cause methemoglobinemia
Prilocaine (TOPNOTCH)
72
For local anesthesia, epidural anesthesia, intrathecal anesthesia
Bupivacaine (TOPNOTCH)
73
Use with caution in pregnant women and patients with cardiac disease (may cause heartblock, arrhyhtmia and hypotension)
Bupivacaine (TOPNOTCH)
74
Longest half-life among local anesthesia
Ropivacaine (TOPNOTCH)
75
Depolarizing Neuromuscular Blocker
Succinylcholine (TOPNOTCH)
76
Agonist at Ach-N receptors causing initial twitch then persistent depolarization
Succinylcholine (TOPNOTCH)
77
SE: muscle pain, hyperkalemia, increased intragastric pressure leading to regurgitation (aspiration), increased intraocular pressure, malignant hyperthermia
Succinylcholine (TOPNOTCH)
78
Metabolized by pseudocholinesterase ; may cause malignant hyperthermia if given together with inhaled anesthetics
Succinylcholine (TOPNOTCH)
79
a common SE for this group is Histamine release
Non-Depolarizing Neuromuscular Blocker (TOPNOTCH)
80
Undergoes Hoffman elimination (rapid spontaneous breakdown)
Atracurium (TOPNOTCH)
81
converted to Laudanosine which can cause seizures
Atracurium (TOPNOTCH)
82
short-acting Non-Depolarizing Neuromuscular Blocker
Mivacurium (TOPNOTCH)
83
intermediate-acting Non-Depolarizing Neuromuscular Blocker ; Undergoes elimination in bile
Vecuronium (TOPNOTCH)
84
Suggamadex is a novel reversal agent for
Rocuronium (TOPNOTCH)
85
Competitive antagonists at skeletal muscle nicotinic acetylcholine receptors; For skeletal muscle relaxation during intubation and general anesthesia
Non-Depolarizing Neuromuscular Blocker (TOPNOTCH)
86
long-acting Non-Depolarizing Neuromuscular Blocker; may cause heart block
Pancuronium (TOPNOTCH)
87
Relatively contraindicated in myocardial ischemia; reverse effects with neostigmine
Tubocurarine (TOPNOTCH)
88
a dopamine precursor
Levodopa (TOPNOTCH)
89
inhibits peripheral metabolism via dopa decarboxylase
carbidopa (TOPNOTCH)
90
SE: GI upset (emesis), dyskinesia (choreoathetosis), behavioural changes (anxiety, agitation, confusion, delusion), on-off phenomena, wearing-off phenomena, postural hypotension, tachycardia
Levodopa-carbidopa (TOPNOTCH)
91
Partial agonist at dopamine D2 receptors in brain
Bromocriptine, Pergolide (TOPNOTCH)
92
For Parkinson's disease which is levodopa intolerance, hyperprolactinemia
Bromocriptine, Pergolide (TOPNOTCH)
93
SE: anorexia, n/v, dyskinesia, postural hypotension, behavioural changes, erythromelalgia, pulmonary infiltrate
Bromocriptine (TOPNOTCH)
94
Partial agonist at dopamine D3 receptors in brain
Pramipexole (TOPNOTCH)
95
SE: Contraindicated for patients with active peptic ulcer disease, psychotic illnesss or recent MI
Pramipexole, Ropinirole (TOPNOTCH)
96
Partial agonist at dopamine D3 receptors, antagonist at 5-HT and alpha adrenoceptors
Apomorphine (TOPNOTCH)
97
For off-periods of Parkinson's disease, alcoholism, opiate addiction, erectile dysfunction, alzheimer's disease
Apomorphine (TOPNOTCH)
98
Selective inhibitors of MAO type B leading to decreased degradation of dopamine, increases response to levodopa/carbidopa
Selegiline, Rasagiline (TOPNOTCH)
99
Block L-dopa metabolism by inhibiting catechol-O-methyltransferase in periphery and CNS, prolongs response to levodopa
Entacapone, Tolcapone (TOPNOTCH)
100
T or F: Entacapone only acts in the periphery while Tolcapone acts both in the periphery and CNS
TRUE (TOPNOTCH)
101
enhances dopaminergic transmission by unknown mechanism, maybe by influencing the synthesis, release or reuptake of dopamine
Amantadine (TOPNOTCH)
102
SE: behavioral changes (restlessness, agitation, insomnia, hallucination, psychosis), livedo reticularis, GI disturbances, urinary retention, postural hypotension, peripheral edema
Amantadine (TOPNOTCH)
103
Decrease the excitatory actions of cholinergic neurons on cells in the striatum by blocking muscarinic receptors
Benztropine, Biperiden, Trihexyphenidyl, Orphenadrine (TOPNOTCH)
104
as adjunct for parkinson's disease and extrapyramidal symptoms caused by antipsychotics
Benztropine, Biperiden, Trihexyphenidyl, Orphenadrine (TOPNOTCH)
105
Blocks D2 receptos more than 5-HT2 receptors
Typical Antipsyhotics (TOPNOTCH)
106
Typical Antipsychotic, SE: retinal deposits and arryhthmias
Thioridazine (TOPNOTCH)
107
has the Strongest autonomic effects; only antipsychotic with fatal overdose
Thioridazine (TOPNOTCH)
108
For schizophrenia and other psychotic disorders, huntington's disease and tourette's syndrome
Haloperidol, Droperidol (TOPNOTCH)
109
SE: extrapyramidal dysfunction, tardive dyskinesia, hyperprolactinemia, neuroleptic malignant syndrome
Haloperidol, Droperidol (TOPNOTCH)
110
Only antipsychotic that reduces the risk of suicide
Clozapine (TOPNOTCH)
111
For schizophrenia (refractory, suicidal) and other psychotic disorders
Clozapine (TOPNOTCH)
112
Blocks 5-HT2 receptors more than D2 receptors
Atypical Antipsychotics (TOPNOTCH)
113
SE: Extrapyramidal dysfunction (less), hyperprolactinemia (less), postural hypotension, weight gain, hyperglycemia, hyperlipidemia, myocarditis, agranulocytosis, seizures, ileus, hypersalivation (sialotthea)
Clozapine (TOPNOTCH)
114
weight gain and hyperglycemia is prominent, safe in pregnancy
Olanzapine (TOPNOTCH)
115
SE: Extrapyramidal dysfunction (less), hyperprolactinemia (less), postural hypotension, weight gain, somnolence, fatigue, sleep paralysis, hypnagogic hallucinations, cataracts, priapism, QT prolongation (TDP) ; safe in pregnancy
Quetiapine (TOPNOTCH)
116
Only antipsychotic approved for schizophrenia in the youth
Risperidone (TOPNOTCH)
117
Increased mortality in elderly patients with dementia-related psychosis ; can cause TDP
Ziprasidone (TOPNOTCH)
118
Least sedating atypical antipsychotics
Aripiprazole (TOPNOTCH)
119
Uncertain MOA but the proposed MOA is by inhibiting the enzyme involved in the recycling of neuronal membrane phosphoinositides which causes depletion of phosphatidylinositol bisphosphate, thus consequently decreasing IP3 and DAG leading to decreased neurotransmission
Lithium (TOPNOTCH)
120
SE: Tremor, sedation, ataxia, aphasia, thyroid enlargement, hypothyroidism, reversible nephrogenic diabetes insipidus, edema, acneiform skin eruption, leukocytosis, teratogen (ebstein's anomaly), bradycardia
Lithium (TOPNOTCH)
121
Block NE and 5-HT transporters leading to potentiation of NT action at postsynaptic receptors
Tricyclic Antidepressants (TOPNOTCH)
122
Tricyclic Antidepressants
Imipramine, Clomipramine, Desipramine, Amitryptyline, Nortryptiline (TOPNOTCH)
123
For MDD (most effective), bipolar disorder, acute panic attacks, ADHD, chronic pain states, as sleeping aid, OCD ; this group is very useful for patients with psychomotor retardation, sleep disturbance, poor appetite and weight loss
Imipramine, Clomipramine, Desipramine, Amitryptyline, Nortryptiline (TOPNOTCH)
124
3Cs of TCA overdose
Coma, Cardiotoxicity, Convulsions (TOPNOTCH)
125
longterm use may lead to down-regulation of Beta receptors leading to a decrease in BP and depression of cardiac conduction
Tricyclic Antidepressants (TOPNOTCH)
126
Inhibits neuronal reuptake of serotonin by inhibiting Serotonin Transporter (SERT)
SSRI (TOPNOTCH)
127
SSRIs
Fluoxetine, Paroxetine, Citalopram, Escitalopram, Sertraline, Fluvoxamine (TOPNOTCH)
128
DOC for OCD, for MDD, anxiety, panic attacks, phobias, PTSD, GAD, bulimia, premenstrual dysphoric disorder, alcohol dependence
Fluoxetine, Paroxetine, Citalopram, Escitalopram, Sertraline, Fluvoxamine (TOPNOTCH)
129
This antidepressant group can decrease appetite leading to weight loss
SSRI (TOPNOTCH)
130
Inhibits neuronal reuptake of serotonin and norepinephrine by binding to transporters for both 5HT and NE
SNRI (TOPNOTCH)
131
SNRIs
Venlafaxine, Duloxetine, Desvenlafaxine (TOPNOTCH)
132
differ from TCA in lacking blockade of H1, M and alpha receptors ; Increased risk for suicide in children and adolescents
SNRIs (TOPNOTCH)
133
Blocks 5-HT2A receptors, weak inhibitor of NE and 5HT transporters
Serotonin antagonist (TOPNOTCH)
134
Antidepressant Serotonin antagonist
Trazodone, Nefazodone (TOPNOTCH)
135
Strong norepinephrine reuptake inhibitor and weak serotonin reuptake inhibitor, blocks dopamine D2 receptors
Tetracyclics: Amoxapine (TOPNOTCH)
136
Increases amine release from nerve endings by antagonism of presynaptic a2 adrenoceptors, also blocks serotonin 5-HT2A receptors
Tetracyclics: Mirtazapine (TOPNOTCH)
137
Inhibits neuronal reuptake of dopamine and norepinephrine, increase dopamine and norepinephrine activity
Tetracyclics: Bupropion (TOPNOTCH)
138
Inhibits MAO type A and type B, increases CNS levels of NE and serotonin
Phenelzine, tranylcypromine (TOPNOTCH)
139
MAO-B selective inhibitor
Selegiline (TOPNOTCH)
140
Triad of opioid overdose
miosis, coma, respiratory depression (TOPNOTCH)
141
Strong agonist at u receptors; For severe pain, pain associated with acute MI, for pulmonary edema
Morphine (TOPNOTCH)
142
morphine is metabolized in the body to _____ which has equal analgesic activity as morphine
morphine-6-glucuronide (TOPNOTCH)
143
Strong agonist at u receptors; For severe pain, adjunct in anesthesia, chronic pain and breakthrough cancer pain
Fentanyl (TOPNOTCH)
144
Strong agonist at u and k receptors, inhibits pain neurotransmission, muscarinic blocking actions; For moderate to severe pain, labor analgesia, spasmodic pain (biliary, renal), preoperative sedation
Meperidine (TOPNOTCH)
145
Only opioid that does not cause miosis and biliary contraction
Meperidine (TOPNOTCH)
146
opioid of choice for pain relief in pancreatitis
Meperidine (TOPNOTCH)
147
metabolized to normeperidine which can cause _____ therefore contraindicated in patients with ______
seizure, seizure disorder (TOPNOTCH)
148
full opioid agonist, Strong agonist at u receptors, inhibits pain neurotransmission, binds NMDA receptors and antagonizes the effects of glutamate; For moderate to severe pain, opioid dependence, opioid withdrawal
Methadone (TOPNOTCH)
149
used as maintenance therapy for opioid dependence
Methadone (TOPNOTCH)
150
Decreases sensitivity of cough receptors, depressing the medullary cough center through sigma receptors stimulation; For cough suppression
Dextrometorphan, codeine (TOPNOTCH)
151
codeine is metabolized by CYP2D6 to ______
morphine (TOPNOTCH)
152
SE: miosis, restlessness, respiratory depression, increased ICP, postural hypotension, urinary retention, pruritus, addiction liability
Opioid analgesics (TOPNOTCH)
153
Mixed Agonist-Antagonist: Strong agonist at k receptors, weak antagonist activity at u receptors
Nalbuphine, buprenorphine, butorphanol, pentazocine (TOPNOTCH)
154
Weak agonist at u receptors, inhibits pain neurotransmission; For mild to moderate pain, restless leg syndrome
Propoxyphene, levopropoxyphene, dextropropoxyphene (TOPNOTCH)
155
Competitively blocks u, sigma and k receptors, rapidly reverses effects of opioid agonists; For opioid overdose, opioid and alcohol dependence
Naloxone, naltrexone, nalmefene (TOPNOTCH)
156
Weak agonist at u receptors, inhibits neuronal reuptake of serotonin and norepinephrine; For moderate pain, chronic pain syndrome, neuropathic pain
Tramadol (TOPNOTCH)
