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FA - Neurology > Neuro - Pharmacology (Epilepsy & Psychoactive drugs) > Flashcards

Neuro - Pharmacology (Epilepsy & Psychoactive drugs) Flashcards

Pg. 492-493 in First Aid 2014 Sections include: -Epilepsy drugs -Barbiturates -Benzodiazepines -Nonbenzodiazepine hypnotics

1
Q

Name 12 epilepsy drugs.

A

(1) Ethosuximide (2) Benzodiazepines (diazepam, lorazepam) (3) Phenytoin (4) Carbamazepine (5) Valproic acid (6) Gabpentin (7) Phenobarbital (8) Topiramate (9) Lamotrigine (10) Levetiracetam (11) Tiagabine (12) Vigabatrin

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2
Q

Name 10 epilepsy drugs used for simple partial seizures. For what other type of seizures can all 10 of these drugs be used?

A

(1) Phenytoin (2) Carbamazepine (3) Valproic Acid (4) Gabapentin (5) Phenobarbital (6) Topiramate (7) Lamotrigine (8) Levetiracetam (9) Tiagabine (10) Vigabatrin; Also used in partial complex seizures

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3
Q

Name 8 epilepsy drugs used for tonic-clonic generalized seizures.

A

(1) Phenytoin (2) Carbamezepine (3) Valproic acid (4) Gabapentin (5) Phenobarbital (6) Topiramate (7) Lamotrigine (8) Levetiracetam

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4
Q

Name 3 epilepsy drugs used for absence generalized seizures.

A

(1) Ethosuximide (2) Valproic acid (4) Lamotrigine

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5
Q

Name 2 epilepsy drugs used for status epilepticus generalized seizures.

A

(1) Benzodiazepines (diazepam, lorazepam) (2) Phenytoin

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6
Q

What is the first line epilepsy drug for simple partial seizures? For what other type of seizures is this the only first line epilepsy drug? For what type of seizures is this one of the several first line epilepsy drugs?

A

Carabamazepine; Complex partial seizures; Tonic-Clonic generalized seizures

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7
Q

What are 3 first line epileptic drugs for tonic-clonic generalized seizures?

A

(1) Phenytoin (2) Carbamazepine (3) Valproic acid

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8
Q

What is the first line epileptic drug for absence generalized seizures?

A

Ethosuximide; Think: “ethoSUXimide = SUCKS to have Silent (absence) Seizures”

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9
Q

What is the first line epileptic drug for acute status epilepticus generalized seizures? What is the first line epileptic drug for prophylaxis against status epilepticus generalized seizures?

A

Benzodiazepines (diazepam, lorazepam); Phenytoin

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10
Q

What is the mechanism of Ethosuximide?

A

Blocks thalamic T-type Ca2+ channels

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11
Q

For what type of seizure is Ethosuximide the first line epileptic drug?

A

Absence generalized seizures; Think: “ethoSUXimide = SUCKS to have Silent (absence) Seizures”

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12
Q

What are 5 side effects of ethosuximide?

A

(1) GI (2) Fatigue (3) Headache (4) Urticaria (5) Steven-Johnson syndrome; Think: “EFGHIJ - Ethosuximide causes Fatigue, GI distress, Headache, Itching, and Stevens-Johnson syndrome”

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13
Q

What is the mechanism of Benzodiazepines?

A

Increase GABAa action

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14
Q

What are 4 side effects of Benzodiazepines?

A

(1) Sedation (2) Tolerance (3) Dependence (4) Respiratory depression

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15
Q

For what type of seizures are Benzodiazepines used as first line epileptic drugs, and in what context?

A

Status epilepticus generalized seizures; First line for acute

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16
Q

For what other type of seizures (other than status epilepticus) are Benzodiazepines used? What is the first line drug used in this type of seizures?

A

Also for eclampsia seizures (1st line is MgSO4)

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17
Q

What are 2 examples of Benzodiazepines that can be used in status epilepticus?

A

Diazepam, Lorazepam

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18
Q

What is the mechanism of Phenytoin? What kind of kinetics does it have?

A

Increase Na+ channel inactivation; Zero-order kinetics

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19
Q

What are 13 side effects of phenytoin?

A

(1) Nystagmus (2) Diplopia (3) Ataxia (4) Sedation (5) Gingivial hyperplasia (6) Hirsuitism (7) Peripheral neuropathy (8) Megaloblastic anemia (9) Teratogenesis (fetal hydantoin syndrome) (10) SLE-like syndrome (11) Induction of cytochrome P-450 (12) Lymphadenopathy (13) Stevens-Johnson syndrome (14) Osteopenia

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20
Q

What type of phenytoin is used parenterally?

A

Fosphenytoin for parenteral use

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21
Q

In what type of seizures is phenytoin used as a first line epileptic drug for prophylaxis? In what other type of seizures is phenytoin used as a first line epileptic drug?

A

Status epilepticus generalized seizures (prophylaxis); Tonic-clonic generalized seizures

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22
Q

What is the mechanism of Carbamazepine?

A

Increase Na+ channel inactivation

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23
Q

What are 8 side effects of Carbamazepine?

A

(1) Diplopia (2) Ataxia (3) Blood dyscrasias (agranulocytosis, aplastic anemia) (4) Liver toxicity (5) Teratogenesis (6) Induction of cytochrome P-450 (7) SIADH (8) Stevens-Johnson syndrome

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24
Q

What epileptic drug is the first line for trigeminal neuralgia? For what types of seizures is this epileptic drug also used as a first line?

A

Carbamazepine; Simple partial seizures, Complex partial seizures, and Tonic-clonic generalized seizures

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25
Q

What is the mechanism of Valproic acid?

A

Increase Na+ channel inactivation, Increase GABA concentration by inhibiting GABA transaminase

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26
Q

What are 6 toxicities associated with Valproic acid?

A

(1) GI (2) Distress (3) Rare but fatal hepatotoxicity (measure LFT’s) (4) Neural tube defects in fetus (spina bifida) (5) Tremor (6) Weight gain

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27
Q

For what condition is Valproic acid contraindicated?

A

Contraindicated in pregnancy

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28
Q

Besides its use is simple/complex partial and/or tonic-clonic/absence generalized seizures, what are 2 other clinical uses for Valproic acid?

A

Also used for myoclonic seizures, bipolar disorder

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29
Q

What is the mechanism of Gabapentin? How is it designed?

A

Primarily inhibits high-voltage-activated Ca2+ channels; Designed as GABA analog

30
Q

What are 2 toxicities associated with Gabapentin?

A

(1) Sedation (2) Ataxia

31
Q

Other than seizures, what are 4 clinical uses for Gabapentin?

A

Also used for (1) peripheral neuropathy, (2) postherpetic neuralgia, (3) migraine prophylaxis, (4) bipolar disorder

32
Q

What is the mechanism of phenobarbital?

A

Increase GABAa action

33
Q

What are 5 toxicities associated with phenobarbital?

A

(1) Sedation (2) Tolerance (3) Dependence (4) Induction of cytochrome P-450 (5) Cardiorespiratory depression

34
Q

Which epilepsy drug is first line in neonates?

A

Phenobarbital

35
Q

What is the mechanism of topiramate?

A

Blocks Na+ channels, increase GABA action

36
Q

What are 4 toxicities to associate with topiramate?

A

(1) Sedation (2) Mental dulling (3) Kidney stones (4) Weight loss

37
Q

Besides seizures, what is another clinical use for topiramate?

A

Also used for migraine prevention

38
Q

What is the mechanism of Lamotrigine?

A

Blocks voltage-gated Na+ channels

39
Q

What is a toxicity of Lamotrigine? How is the risk of this toxicity reduced?

A

Stevens-Johnson syndrome (must be titrated slowly)

40
Q

What is the mechanism for Levetiracetam?

A

Unknown; May modulate GABA and glutamate release

41
Q

What is the mechanism for Tiagabine?

A

Increase GABA by inhibiting re-uptake

42
Q

What is the mechanism for Vigabatrin?

A

Increase GABA by irreversibly inhibiting GABA transaminase

43
Q

What characterizes Stevens-Johnson syndrome at initial onset? To what symptoms/signs does it progress?

A

Prodome of malaise and fever followed by rapid onset of erythematous/purpuric macules (oral, ocular, genital). Skin lesions progress to epidermal necrosis and sloughing.

44
Q

What are 4 examples of Barbiturates?

A

(1) Phenobarbital (2) Pentobarbital (3) Thiopental (4) Secobarbital

45
Q

What is the mechanism of Barbiturates?

A

Facilitate GABAa action by increasing duration of Cl- channel opening, thus decrease neuron firing; Think: “BarbiDURAtes increase DURAtion”

46
Q

In what condition are Barbiturates contraindicated?

A

Contraindicated in porphyria

47
Q

What are 4 clinical uses for Barbiturates?

A

Sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental)

48
Q

Which Barbiturate is used as induction of anesthesia?

A

Thiopental

49
Q

What are 2 potentially fatal toxicities of Barbiturates?

A

Respiratory and cardiovascular depression (can be fatal)

50
Q

Which toxicity of Barbiturates can be exacerbated by EtOH use?

A

CNS depression (can be exacerbated by EtOH use)

51
Q

What are 5 toxicities of Barbiturates?

A

(1) Respiratory and (2) Cardiovascular depression (can be fatal); (3) CNS depression (can be exacerbated by EtOH use); (4) Dependence; (5) Drug interactions (induces cytochrome P-450)

52
Q

What is the treatment of Barbiturates overdose?

A

Overdose treatment is supportive (assist respiration and maintain BP)

53
Q

Name 8 Benzodiazepines.

A

(1) Diazepam (2) Lorazepam (3) Triazolam (4) Temazepam (5) Oxazepam (6) Midazolam (7) Chlordiazepoxide (8) Alprazolam

54
Q

What is the mechanism of Benzodiazepines?

A

Facilitate GABAa action by increasing frequency of Cl- channel opening; Think: “FREnzodiazepines increase FREquency”

55
Q

What effect do Benzodiazepines have on the sleep cycle?

A

Decrease REM sleep

56
Q

What kind of half-lives and metabolites do most benzodiazepines have? What are the exceptions to this rule, and why?

A

Most have long half-lives and active metabolites (exceptions: triazolam, oxazepam, and midazolam are short acting –> higher addictive potential)

57
Q

What are 8 clinic uses for benzodiazepines?

A

(1) Anxiety (2) Spasticity (3) Status elipeticus (lorazepam and diazepam) (4) Detoxicification (especially alcohol withdraw-DTs) (5) Night terrors (6) Sleepwalking (7) General anesthetic (amnesia, muscle relaxation) (8) Hypnotic (insomnia)

58
Q

Which 2 benzodiazepines are used for status epilepticus?

A

Status epilepticus (lorazepam and diazepam)

59
Q

What are 2 toxicities associated with benzodiazepines? Give specific context where/if needed.

A

(1) Dependence (2) Additive CNS depression effects with alcohol

60
Q

What is an advantage of benzodiazepines over barbiturates?

A

Less risk of respiratory depression and coma than with barbiturates

61
Q

What is the treatment for benzodiazepine overdose?

A

Treat overdose with flumazenil (competitive antagonist at GABA benzodiazepine receptor)

62
Q

What is GABAa receptor? Name 3 substances that bind GABAa receptor.

A

Benzos, barbs, and EtOH all bind GABAa receptor, which is a ligand-gated Cl- channel

63
Q

What are 3 examples of Nonbenzodiazepine hypnotics?

A

(1) Zolpidem (Ambien) (2) Zaleplon (3) esZopiclone; Think: “All ZZZs put you to sleep”

64
Q

What is the mechanism of nonbenzodiazepine hypnotics?

A

Act via the BZ1 subtype of the GABA receptor

65
Q

What reverses the effects of nonbenzodiazepine hypnotics?

A

Effects reversed by flumzenil.

66
Q

What is the clinical use for nonbenzodiazepine hypnotics?

A

Insomnia

67
Q

What are 3 main toxicities associated with nonbenzodiazepine hypnotics?

A

(1) Ataxia (2) Headaches (3) Confusion

68
Q

What kind of duration do nonbenzodiazepine hypnotics have, and why?

A

Short duration because of rapid metabolism by liver enzymes

69
Q

How do nonbenzodiazepine hypnotics differ from older sedative-hypnotics?

A

Unlike older sedative-hypnotics, cause only modest day-after psychomotor depression and few amnestic effects

70
Q

How do nonbenzodiazepine hypnotics compare to benzodiazepines in terms of dependence risk?

A

Lower dependence risk than benzodiazepines

FA - Neurology (30 decks)

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