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Flashcards in Neuro Drugs Deck (101):
1

Epinephrine is an...

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

2

Side effects of Epinephrine

mydriasis (do NOT use in closed-angle glaucoma)

3

Brimonidine is an...

alpha2-agonist that decreased aquous humor synthesis (glaucoma)

4

Brimonidine side effects

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

5

Timolol, betaxolol and carteolol are...

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

6

Acetazolamide is a...

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

7

Pilocarpine and Carbachol are...

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

8

Side effects of Pilocarpine and Carbachol

miosis and cyclospasm (contraction of ciliary muscle)

9

Physostigimine and Echothiophate are..

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

10

Latanoprost is a...

PGF2alpha agonist that increases outflow of aqueous humor.

11

Latanoprost side effect

darkens color of iris

12

Opioid analgesics (8)

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

13

Opioids mechanism

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

opiod receptors

mu = morphine delta = enkephalin kappa = dynorphin

15

Clinical use of opioids (5)

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

16

Toxciity of opioids

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

17

Butorphanol MOA

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

18

Use of Butorphanol

-severe pain

19

Butorphanol can cause opioid withdrawal symptoms if...

pt is also taking full opioid agonist.

20

Tramadol MOA

weak opioid agonist; also inhibits serotonin and NE reuptake

21

Use of Tramadol

chronic pain

22

Toxicity of Tramadol

-similar to opioids -decreases seizure threshold -serotonin syndrome

23

Ethosuximide use

absence seizures (first line)

24

MOA of Ethosuximide

blocks thalamic T-Type Calcium channels

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)