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Flashcards in Neuro Drugs Deck (101)
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1
Q

Epinephrine is an...

A

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

2
Q

Side effects of Epinephrine

A

mydriasis (do NOT use in closed-angle glaucoma)

3
Q

Brimonidine is an...

A

alpha2-agonist that decreased aquous humor synthesis (glaucoma)

4
Q

Brimonidine side effects

A

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

5
Q

Timolol, betaxolol and carteolol are...

A

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

6
Q

Acetazolamide is a...

A

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

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)

8
Q

Side effects of Pilocarpine and Carbachol

A

miosis and cyclospasm (contraction of ciliary muscle)

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.

10
Q

Latanoprost is a...

A

PGF2alpha agonist that increases outflow of aqueous humor.

11
Q

Latanoprost side effect

A

darkens color of iris

12
Q

Opioid analgesics (8)

A

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

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

14
Q

opiod receptors

A

mu = morphine delta = enkephalin kappa = dynorphin

15
Q

Clinical use of opioids (5)

A

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

16
Q

Toxciity of opioids

A

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

17
Q

Butorphanol MOA

A

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

18
Q

Use of Butorphanol

A

-severe pain

19
Q

Butorphanol can cause opioid withdrawal symptoms if...

A

pt is also taking full opioid agonist.

20
Q

Tramadol MOA

A

weak opioid agonist; also inhibits serotonin and NE reuptake

21
Q

Use of Tramadol

A

chronic pain

22
Q

Toxicity of Tramadol

A

-similar to opioids -decreases seizure threshold -serotonin syndrome

23
Q

Ethosuximide use

A

absence seizures (first line)

24
Q

MOA of Ethosuximide

A

blocks thalamic T-Type Calcium channels

25
Q

Side effects of Ethosuxamide

A

EFGHIJ -fatigue -GI distress -Headache -Itching -stevens-Johnson syndrome

26
Q

Benzodiazepines (2)

A

1. Diazepam 2. Lorazepam

27
Q

Use of Diazepam and Lorazepam

A

status epilepticus

28
Q

MOA of Benzodiazepines

A

increase GABAa action (can also be used for eclampsia seizures)

29
Q

SE of Benzodiazepines

A

sedation, tolerance, dependence, respiratory depression

30
Q

Phenytoin Use

A

Simple partial seizures complex partial seizures tonic-clonic seizures status epilepticus

31
Q

Phenytoin MOA

A

increase Na+ channel inactivation; zero-order kinetics

32
Q

Phenytoin side effects

A

-nystagmus -diplopia -ataxia -sedation -gingival hyperplasia -hirsutism -neuropathy -megaloblastic anemia -teratogenesis -SLE-like syndrome -induces CYP450s -Stevens Johnson -osteopenia

33
Q

Carbamazepine use

A

simple and complex partial seizures tonic-clonic seizures (1st line use for trigeminal neuralgia)

34
Q

Carbamazepine MOA

A

increased Na+ channel inactivation

35
Q

Side effects of Carbamazepine

A

-diplopia -ataxia -blood dyscrasias -liver toxicity -teratogenesis -induces CYP450s -Stevens Johnson -SIADH

36
Q

Valproic Acid uses

A

simple and complex partial seizures tonic-clonic seizures absence seizures (also for myoclonic seizures and bipolar disorder)

37
Q

Valproic Acid MOA

A

-increased Na+ channel inactivation -increased GABA concentration by inhibiting GABA trasmaminase

38
Q

Valproic Acid Side Effects

A

-rare but fatal hepatotoxicity (need to meausre LFTs) -neural tube defects (spina bifida) -tremor -weight gain

39
Q

Gabapentin uses

A

-partial and complex partial seizures -tonic-clonic seizures (also for peripheral neuropathy, postherheptic neuralgia, migraine prophylaxis and bipolar disorder)

40
Q

Gabapentin MOA

A

primarily inhibits high-voltage-activated Ca2+ channels; designed as GABA analog

41
Q

Gabapentin SE

A

-sedation -ataxia

42
Q

Phenobarbital uses

A

-simplex and complex partial seizures -tonic-clonic seizures (1st line in neonates)

43
Q

Phenobarbital mechanism

A

increased GABAa action

44
Q

Phenobarbital side effects

A

-sedation -tolerance -dependence -CYP450 induction -cardiorespiratory depression

45
Q

Topiramate uses

A

-simple and complex seizures -tonic-clonic seizures (also for migraine prophylaxis)

46
Q

Topirimate MOA

A

blocks Na+ channels and increases GABA action

47
Q

Topirimate SE

A

-sedation -mental dulling -kidney stones -weight loss

48
Q

Lamotrigine uses

A

-simple and complex partial seizures -tonic clonic seizures -absences seizures

49
Q

Lamotrigine MOA

A

-blocks voltage-gated Na+ channels

50
Q

Lamotrigine SE

A

Stevens-Johnson

51
Q

Levetiracetam uses

A

-simple and complex seizures -tonic-clonic seizures

52
Q

Levetiracetam MOA

A

unknown; may modulate GABA and glutamate release

53
Q

Tiagabine uses

A

simple and complex partial seizures

54
Q

Tiagabine MOA

A

increase GABA by inhibiting re-uptake by GAT-1

55
Q

Vigabatrin uses

A

simplex and complex partial seizures

56
Q

Vigabatrin MOA

A

Increases GABA by irreversibly inhibiting GABA tramsaminase

57
Q

Stevens-Johnson syndrome is...

A

a prodrome of malaise and fever followed by rapid onset of erythematous/purpuric macules. Skin lesions progress to epidermal necrosis and sloughing.

58
Q

Barbituates (4)

A

1. Phenobarbital 2. Pentobarbital 3. Thiopental 4. Secobarbital

59
Q

Barbituates MOA

A

facilitate GABAa action by increasing the duration of Cl- channel opening, thus decreasing neuron firing

60
Q

Barbiturates are contraindicated in...

A

porphyria

61
Q

Use of Barbituates

A

-sedative for anxiety -seizures -insomnia -induction of anesthesia (thiopental)

62
Q

Barbituate toxicity

A

-respiratory and CV depression -CNS depression -dependence -drug interactions

63
Q

OD of barbituates treatment is...

A

supportive (assist respiration and maintain BP).

64
Q

Benzodiazepines (8)

A

1. Dizaepam 2. Lorazepam 3. Triazolam 4. Temazepam 5. Oxazepam 6. Midazolam 7. Chlordiazepoxide 8. Alprazolam

65
Q

Benzodiazpeines MOA

A

facilitate GABAa action by increasing frequency of Cl- channel opening; decrease REM

66
Q

Most BDZs have long half-lives and active metabolites except...

A

triazolam, oxazepam and midazolam which are short acting and have higher abuse potential.

67
Q

Use of BDZs

A

-anxiety -spasticity -status epilepticus -night terrors -detoxification -sleepwalking -general anesthetic -insomnia

68
Q

Toxicity of BDZs

A

-dependence -additive CNS depression w/ alcohol (less risk of respiratory depression than barbituates)

69
Q

Treatment of BDZ overdose

A

Flumazenil (competitive antagonist at GABA benzodiazepine receptor)

70
Q

Nonbenzodiazepine Hypnotics (3)

A

1. Zolpidem 2. Zaleplon 3. esZopiclone

71
Q

MOA of Zolpidem, Zaleplon, and Eszopiclone

A

act via the BZ1 subtype of GABA receptor

72
Q

use of zolpidem, zaleplon, and eszopiclone

A

insomnia

73
Q

Drugs with decreased solubility in the blood have...

A

rapid induction and recovery times.

74
Q

Drugs with increased solubility in lipids have...

A

increased potency = 1/MAC. (MAC = minimal alveolar concentration required to prevent 50% of subjects from responding to noxious stimuli)

75
Q

Neuromuscular blocking drugs are used for...

A

muscle paralysis in surgery/mechanical ventilation. Selective for motor nicotinic receptor.

76
Q

Succinylcholine is a strong...

A

ACh receptor agonist that produces sustained depolarization and prevents muscle contraction.

77
Q

Phase II of the succinylcholine blockade can be reversed by...

A

cholinesterase inhibitors (these potentiate the block in phase I).

78
Q

Complications of Succinylcholine include...

A

hypercalcemia, hyperkalemia and malignant hyperthermia.

79
Q

Tubocurarine, Atracurium, Mivacurium, Pancuronium, Vecuronium and Rocuronium are...

A

competitive antagonists for the ACh receptor.

80
Q

Reversal of nondepolarizing blockade of ACh receptors is with...

A

neostigmine (give w/ atropine to prevent bradycardia), edrophonium.

81
Q

Dantrolene MOA

A

prevents release of Ca2+ from the SR of skeletal muscle

82
Q

Dantrolene use

A

malignant hyperthermia and neuroleptic malignant syndrome

83
Q

Parkinsonism is due to...

A

loss of dopaminergic neurons and excess cholinergic actiivty.

84
Q

Dopamine agonists (3)

A

Bromocriptine Pramipexole Ropinerole (for Parkinsonism)

85
Q

Parkinson drugs that increase dopamine

A

Amantadine (also used as an antiviral for influenza A and rubella) L-dopa/carbidopa

86
Q

Parkinson drugs that prevent the breakdown of dopamine

A

Selegiline (selective MAO-B inhibitor) Entacapone/Tolcapone (COMT inhibitors)

87
Q

Parkinson drugs that curb excess cholinergic activity

A

-Benztropine (antimuscarinic; improves rigidity and tremor but not bradykinesia)

88
Q

Levodopa Mechanism

A

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
Q

Carbidopa is a...

A

peripheral decarboyxlase inhibitor given with L-dopa to increase the availability of L-dopa in the brain and decrease peripheral side effects

90
Q

Toxicity of L-dopa

A

arrhythmias from increased peripheral formation of catecholamines; alternating dyskinesia and akinesia

91
Q

Selegine MOA

A

selectively inhibits MAO-B which metabolizes dopamine

92
Q

Alzhemier drugs (4)

A

Memantine Donepezil, Galantamine, Rivastigmine

93
Q

Memantine MOA

A

NMDA receptor antagonist; helps prevent excitotoxicity

94
Q

Donepezil, galantamine, rivastigmine MOA

A

AChE inhibitors

95
Q

Toxicity of Memantine

A

dizziness, confusion, hallucinations

96
Q

Toxicity of donepezil, galantamine, rivastigmine

A

nausea, dizziness, insomnia

97
Q

Huntington drugs (3)

A

Tetrabenazine, reserpine Haloperidol

98
Q

Tetrabenazine and Reserpine

A

inhibit vesicular monoamine transporter (VMAT); limits dopamine vesicle packaging and release

99
Q

Haloperidol is a...

A

dopamine receptor antagonist

100
Q

Sumatriptan MOA

A

5-HT1b/1d agonist that inhibits trigeminal nerve activation; prevents vasoactive peptide release; induces vasoconstriction

101
Q

Toxicity of sumatriptan

A

coronary vasospasm (contraindicated in pts with CAD or Prinzmetal angina)