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Neuro Drugs Flashcards

1
Q

Epinephrine is an…

A

alpha-agonist that decreases aqueous humor synthesis via vasoconstriction. (use for open-angle glaucoma)

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2
Q

Side effects of Epinephrine

A

mydriasis (do NOT use in closed-angle glaucoma)

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3
Q

Brimonidine is an…

A

alpha2-agonist that decreased aquous humor synthesis (glaucoma)

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4
Q

Brimonidine side effects

A

-blurry vision -ocular hyperemia -foregin body sensation -ocular allergic rxn and pruritis

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5
Q

Timolol, betaxolol and carteolol are…

A

beta-blockers that decrease aqueous humor synthesis. (glaucoma)

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6
Q

Acetazolamide is a…

A

diuretic that decreases aqeous humor synthesis via inhibition of carbonic anhydrase.

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7
Q

Pilocarpine and Carbachol are…

A

direct cholinomimetics that increase outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular meshwork. (glaucoma)

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8
Q

Side effects of Pilocarpine and Carbachol

A

miosis and cyclospasm (contraction of ciliary muscle)

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9
Q

Physostigimine and Echothiophate are..

A

indirect cholinomimetics that can be used in emergencies and are very effective at opening meshwork into the canal of Schlemm.

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10
Q

Latanoprost is a…

A

PGF2alpha agonist that increases outflow of aqueous humor.

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11
Q

Latanoprost side effect

A

darkens color of iris

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12
Q

Opioid analgesics (8)

A
  1. morphine 2. fentanyl 3. codeine 4. loperamide 5. methadone 6.meperidine 7. dextromethorphan 8. diphenoxylate
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13
Q

Opioids mechanism

A

act as agonists at opioid receptors to modulate synaptic transmission (open K+ channels and close Ca2+ leading to decreased synaptic transmission); this inhibits release of ACh, NE, 5-HT, glutamate and substance P

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14
Q

opiod receptors

A

mu = morphine delta = enkephalin kappa = dynorphin

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15
Q

Clinical use of opioids (5)

A

pain cough suppression diarrhea (loperamide and diphenoxylate) acute pulmonary edema maintenance for heroin addicts (methadone)

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16
Q

Toxciity of opioids

A

-addiction -respiratory depression -constipation -miosis -additive CNS depression

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17
Q

Butorphanol MOA

A

mu-opioid partial agonist and kappa-opioid agonist; produces analgesia

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18
Q

Use of Butorphanol

A

-severe pain

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19
Q

Butorphanol can cause opioid withdrawal symptoms if…

A

pt is also taking full opioid agonist.

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20
Q

Tramadol MOA

A

weak opioid agonist; also inhibits serotonin and NE reuptake

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21
Q

Use of Tramadol

A

chronic pain

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22
Q

Toxicity of Tramadol

A

-similar to opioids -decreases seizure threshold -serotonin syndrome

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23
Q

Ethosuximide use

A

absence seizures (first line)

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24
Q

MOA of Ethosuximide

A

blocks thalamic T-Type Calcium channels

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25
Side effects of Ethosuxamide
EFGHIJ -fatigue -GI distress -Headache -Itching -stevens-Johnson syndrome
26
Benzodiazepines (2)
1. Diazepam 2. Lorazepam
27
Use of Diazepam and Lorazepam
status epilepticus
28
MOA of Benzodiazepines
increase GABAa action (can also be used for eclampsia seizures)
29
SE of Benzodiazepines
sedation, tolerance, dependence, respiratory depression
30
Phenytoin Use
Simple partial seizures complex partial seizures tonic-clonic seizures status epilepticus
31
Phenytoin MOA
increase Na+ channel inactivation; zero-order kinetics
32
Phenytoin side effects
-nystagmus -diplopia -ataxia -sedation -gingival hyperplasia -hirsutism -neuropathy -megaloblastic anemia -teratogenesis -SLE-like syndrome -induces CYP450s -Stevens Johnson -osteopenia
33
Carbamazepine use
simple and complex partial seizures tonic-clonic seizures (1st line use for trigeminal neuralgia)
34
Carbamazepine MOA
increased Na+ channel inactivation
35
Side effects of Carbamazepine
-diplopia -ataxia -blood dyscrasias -liver toxicity -teratogenesis -induces CYP450s -Stevens Johnson -SIADH
36
Valproic Acid uses
simple and complex partial seizures tonic-clonic seizures absence seizures (also for myoclonic seizures and bipolar disorder)
37
Valproic Acid MOA
-increased Na+ channel inactivation -increased GABA concentration by inhibiting GABA trasmaminase
38
Valproic Acid Side Effects
-rare but fatal hepatotoxicity (need to meausre LFTs) -neural tube defects (spina bifida) -tremor -weight gain
39
Gabapentin uses
-partial and complex partial seizures -tonic-clonic seizures (also for peripheral neuropathy, postherheptic neuralgia, migraine prophylaxis and bipolar disorder)
40
Gabapentin MOA
primarily inhibits high-voltage-activated Ca2+ channels; designed as GABA analog
41
Gabapentin SE
-sedation -ataxia
42
Phenobarbital uses
-simplex and complex partial seizures -tonic-clonic seizures (1st line in neonates)
43
Phenobarbital mechanism
increased GABAa action
44
Phenobarbital side effects
-sedation -tolerance -dependence -CYP450 induction -cardiorespiratory depression
45
Topiramate uses
-simple and complex seizures -tonic-clonic seizures (also for migraine prophylaxis)
46
Topirimate MOA
blocks Na+ channels and increases GABA action
47
Topirimate SE
-sedation -mental dulling -kidney stones -weight loss
48
Lamotrigine uses
-simple and complex partial seizures -tonic clonic seizures -absences seizures
49
Lamotrigine MOA
-blocks voltage-gated Na+ channels
50
Lamotrigine SE
Stevens-Johnson
51
Levetiracetam uses
-simple and complex seizures -tonic-clonic seizures
52
Levetiracetam MOA
unknown; may modulate GABA and glutamate release
53
Tiagabine uses
simple and complex partial seizures
54
Tiagabine MOA
increase GABA by inhibiting re-uptake by GAT-1
55
Vigabatrin uses
simplex and complex partial seizures
56
Vigabatrin MOA
Increases GABA by irreversibly inhibiting GABA tramsaminase
57
Stevens-Johnson syndrome is...
a prodrome of malaise and fever followed by rapid onset of erythematous/purpuric macules. Skin lesions progress to epidermal necrosis and sloughing.
58
Barbituates (4)
1. Phenobarbital 2. Pentobarbital 3. Thiopental 4. Secobarbital
59
Barbituates MOA
facilitate GABAa action by increasing the duration of Cl- channel opening, thus decreasing neuron firing
60
Barbiturates are contraindicated in...
porphyria
61
Use of Barbituates
-sedative for anxiety -seizures -insomnia -induction of anesthesia (thiopental)
62
Barbituate toxicity
-respiratory and CV depression -CNS depression -dependence -drug interactions
63
OD of barbituates treatment is...
supportive (assist respiration and maintain BP).
64
Benzodiazepines (8)
1. Dizaepam 2. Lorazepam 3. Triazolam 4. Temazepam 5. Oxazepam 6. Midazolam 7. Chlordiazepoxide 8. Alprazolam
65
Benzodiazpeines MOA
facilitate GABAa action by increasing frequency of Cl- channel opening; decrease REM
66
Most BDZs have long half-lives and active metabolites except...
triazolam, oxazepam and midazolam which are short acting and have higher abuse potential.
67
Use of BDZs
-anxiety -spasticity -status epilepticus -night terrors -detoxification -sleepwalking -general anesthetic -insomnia
68
Toxicity of BDZs
-dependence -additive CNS depression w/ alcohol (less risk of respiratory depression than barbituates)
69
Treatment of BDZ overdose
Flumazenil (competitive antagonist at GABA benzodiazepine receptor)
70
Nonbenzodiazepine Hypnotics (3)
1. Zolpidem 2. Zaleplon 3. esZopiclone
71
MOA of Zolpidem, Zaleplon, and Eszopiclone
act via the BZ1 subtype of GABA receptor
72
use of zolpidem, zaleplon, and eszopiclone
insomnia
73
Drugs with decreased solubility in the blood have...
rapid induction and recovery times.
74
Drugs with increased solubility in lipids have...
increased potency = 1/MAC. (MAC = minimal alveolar concentration required to prevent 50% of subjects from responding to noxious stimuli)
75
Neuromuscular blocking drugs are used for...
muscle paralysis in surgery/mechanical ventilation. Selective for motor nicotinic receptor.
76
Succinylcholine is a strong...
ACh receptor agonist that produces sustained depolarization and prevents muscle contraction.
77
Phase II of the succinylcholine blockade can be reversed by...
cholinesterase inhibitors (these potentiate the block in phase I).
78
Complications of Succinylcholine include...
hypercalcemia, hyperkalemia and malignant hyperthermia.
79
Tubocurarine, Atracurium, Mivacurium, Pancuronium, Vecuronium and Rocuronium are...
competitive antagonists for the ACh receptor.
80
Reversal of nondepolarizing blockade of ACh receptors is with...
neostigmine (give w/ atropine to prevent bradycardia), edrophonium.
81
Dantrolene MOA
prevents release of Ca2+ from the SR of skeletal muscle
82
Dantrolene use
malignant hyperthermia and neuroleptic malignant syndrome
83
Parkinsonism is due to...
loss of dopaminergic neurons and excess cholinergic actiivty.
84
Dopamine agonists (3)
Bromocriptine Pramipexole Ropinerole (for Parkinsonism)
85
Parkinson drugs that increase dopamine
Amantadine (also used as an antiviral for influenza A and rubella) L-dopa/carbidopa
86
Parkinson drugs that prevent the breakdown of dopamine
Selegiline (selective MAO-B inhibitor) Entacapone/Tolcapone (COMT inhibitors)
87
Parkinson drugs that curb excess cholinergic activity
-Benztropine (antimuscarinic; improves rigidity and tremor but not bradykinesia)
88
Levodopa Mechanism
increases the level of dopamine in the brain because it can cross the BBB (unlike dopamine) and is then convernted to DA by dopa decarboxylase; used for Parkinson
89
Carbidopa is a...
peripheral decarboyxlase inhibitor given with L-dopa to increase the availability of L-dopa in the brain and decrease peripheral side effects
90
Toxicity of L-dopa
arrhythmias from increased peripheral formation of catecholamines; alternating dyskinesia and akinesia
91
Selegine MOA
selectively inhibits MAO-B which metabolizes dopamine
92
Alzhemier drugs (4)
Memantine Donepezil, Galantamine, Rivastigmine
93
Memantine MOA
NMDA receptor antagonist; helps prevent excitotoxicity
94
Donepezil, galantamine, rivastigmine MOA
AChE inhibitors
95
Toxicity of Memantine
dizziness, confusion, hallucinations
96
Toxicity of donepezil, galantamine, rivastigmine
nausea, dizziness, insomnia
97
Huntington drugs (3)
Tetrabenazine, reserpine Haloperidol
98
Tetrabenazine and Reserpine
inhibit vesicular monoamine transporter (VMAT); limits dopamine vesicle packaging and release
99
Haloperidol is a...
dopamine receptor antagonist
100
Sumatriptan MOA
5-HT1b/1d agonist that inhibits trigeminal nerve activation; prevents vasoactive peptide release; induces vasoconstriction
101
Toxicity of sumatriptan
coronary vasospasm (contraindicated in pts with CAD or Prinzmetal angina)

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