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Pharm III > Exam 1 Anticonvulsants, Sedative-hypnotics > Flashcards

Exam 1 Anticonvulsants, Sedative-hypnotics Flashcards

1
Q

Anticonvulsants that induce CYP450

A

Phenytoin, Carbamazepine, Phenobarbital induce CYP450

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2
Q

Anticonvulsants that inhibit Na Channels

A 
Phenytoin (Dilantin) 
Carbamazepine (Tegretol)
Lamotrigine, 
Valproate, 
Topiramate
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3
Q

Drugs that can cause SJS

A 
Phenytoin
Carbamazepine
Phenobarbital
Lamotrigine
Valproate
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4
Q

Drugs that inhibit T type Ca channels

A

Ethosuximide

Valproate

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5
Q

What drugs work by enhancing GABA inhibitory activity

A

Valproate
BZs: Diazepam (Valium), Lorazepam (Ativan)
Barbiturates: Phenobarbital, Gabapentin

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6
Q

What drugs work by decreasing excitatory glutamate activity

A

*those that inhibit Na and T type Ca channels, help block NMDA glutamate receptor

Na channel inhibition: carbamazepine, phenytoin, lamotrigine, topiramate, valproate

Ca channel inhibition: ethosuximide, valproate

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7
Q

DOC partial seizures

A

Carbamazepine (Tegretol)

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8
Q

What types of seizures are there?

A

Partial:

  • simple
  • complex
  • partial with secondary generalized

Generalized

  • tonic/clonic
  • myoclonic
  • absence
  • atonic
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9
Q

what happens with activation of NMDA glutamate receptors

A

activation of glutamate receptors results in seizures

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10
Q

What does blockade of GABA receptors cause and what drug can do this

A

Flumazinel blocks GABA receptors

*blocking GABA R causes SEIZURES

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11
Q

GABA anticonvulsant MOA involves what

A

enhancing GABA inhibitory activity

  • inhibit GABA metab
  • stimulate GABA receptors
  • meds that work through GABA MOA: Phenobarbital, gabapentin, valproic acid, BZ (Diazepam/Valium, Lorazepam/Ativan)
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12
Q

Describe and classify and absence seizure

A

absence is a generalized seizure (petit mal)

  • sudden onset; brief 10-30 sec
  • loss of awareness, NOT LOC
  • may be some mild clonic mvmt
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13
Q

what causes generalized seizures

A

reciprocal firing of thalamus and cortex

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14
Q

describe tonic clonic (grand mal) seizures. What class do they belong to

A

Tonic clonic = generalized seizure

  • initial tonic rigidity (15-30s)
  • subsequent tremor
  • eventually clonic jerking 1-2 min
  • LOC
  • pt stuporous and confused
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15
Q

describe partial seizures

A

begin in focused area in cortex then spread

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16
Q

describe and classify simple seizures

A

SImple seizures are Partial
focal, brief 20-90 sec
*grimacing, focal clonic jerking of an extremity
*no LOC

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17
Q

Describe and classify complex seizures

A

Complex seizures are partial

  • longer than simple (<2 min)
  • altered or LOC, Hallucinations
  • temporal lobe; auto mvmt
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18
Q

Describe and classify Partial with secondary generalized tonic-clonic

A

LOC

Muscle contractions alt with relaxation

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19
Q

GABA NT and enhancement of GABA inhibitory activity is protective against

A

both generalized and partial seizures

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20
Q

What channels are over-active in absence seizures

A

T type Ca channels

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21
Q

Anticonvulsant Drugs that are known to cause SJS include

A

Phenytoin, Carbamazepine, Phenobarbital, Lamotrigine, Valproic acid

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22
Q

Phenytoin Uses

A

partial, generalized tonic clonic seizures

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23
Q

Phenytoin (dilantin) PK

A

not water soluble so not injectable (fosphenytoin is injectable form)

  • first order elimination at low dose
  • zero order at therapeutic and higher doses
  • small change in dose/elimination can cause big changes in plasma levels
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24
Q

what drug interactions does phenytoin (dilantin) have

A

interacts with drugs that alter CYP450 is phenobarbital and carbamazepine (both induce)
*Phenytoin is metab by and induces CYP450

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25
Q

use and SE of phenytoin (Dilantin) include

A

*used for partial and tonic-clonic seizures
*Nystagmus, diplopia, ataxia, sedation,
GINGIVAL HYPERPLASIA
*long term:
coarsening of facial features, mild peripheral neuropathy, abnormal vit D metab, SJS, PregCatD

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26
Q

Use Carbamazepine (Tegretol)

A

DOC partial seizures

  • gen tonic clonic
  • bipolar
  • TRIGEMINAL NEURALGIA
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27
Q

MOA and PK of Carbamazepine (Tegretol)

A

MOA: blocks Na channels, inhibits NE release and reuptake

PK: induces and is metab by CYP450
*lots of drug interactions

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28
Q

Drug interaction of Carbamazepine (Tegretol)

A

bc it is metab by and induces CYP450…

  • increases metab of: pheny, ethosuximide, valproic acid, haloperidol, oral contraceptives
  • metab ^ by: Phenobarb, phenytoin, valproic acid
  • metab inhibited by: cimetidin, fluoxetine
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29
Q

Side Effects of Carbamazepine (Tegretol)

A

Diplopia, ataxia, GI upset, drowsiness

  • aplastic anemia and agranulocytosis
  • SJS
  • preg cat D
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30
Q

MOA of Phenobarbital (Luminal)

A

Prolongs opening of Cl channel at GABA R

alters Na and Ca conductance at high conc.

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31
Q

Primary use of Phenobarbital (luminal)

A

partial seizures, Gen tonic clonic (like Phenytoin)

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32
Q

How is Phenobarbital (Luminal) metabolized?

A

good oral absorption
Crosses BBB
Liver metab
Induces CYP450 with chronic use - increases metab of phenytoin and carbamazepine

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33
Q

Is there a withdrawal/dependence component to Phenobarbital (Luminal)

A

Yes
withdrawal: can be severe - restless, anxiety, weakness, orthostatic hypoTN, hyperactive reflexes and seizures

*severe physio and psych dependence

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34
Q

What are potential SE of Phenobarbital (luminal)

A 
CNS depression (can last 10-22 hr)
Paradoxical excitement
Vertigo, N/V, allergic rxn
May depress vasomotor and resp centers
*severe physio and psych dependence
35
Q

what are contraindications to barbiturate

A
  • Enhances porphyrin synthesis (CI in porphyria)
  • pulmonary insufficiency: may cause resp depress
  • SUPRA-ADDITIVE effects: when combined with other CNS depressants (alcohol) the effects are more than what is expected
  • withdrawal can be severe: restlessness, anxiety, weakness, orthostatic hypoTN, hyperactive reflexes and seizures
36
Q

what are the OD and toxicity components of Barbiturates

A

Low MOS, no ceiling effect (bc Barb work independently of GABA)
effects supra-additive esp with EtOH

OD sx: coma, resp depression, hypoTN

37
Q

How do you treat Barbiturate OD and toxicity

A

Tx is supportive
May be cleared with diuresis and alkalinization of the urine

Do not treat with stimulants bc stimulants increase mortality rate

38
Q

What are the effects of BZ?

A
  • most commonly used group of anxiolytics and sedative hypnotics
  • cause CNS depression: decrease in anxiety often with drowsiness
  • hypnosis with high doses
39
Q

Why are BZ the most commonly used group of anxiolytics and sedative hypnotics

A

By of the PK and duration of action in BZ

*conversion to metabolites increase half life, increasing duration of action

40
Q

How are BZ metabolized/absorbed/administered

A

Oral absorption
may be given IV in emerg or for pre-anesthesia
Elderly do not metab BZ as quickly
CYP3A4 metab in liver, converted to active metab

41
Q

describe the metabolism of diazepam, including half life information (*diazepam is BZ)

A

Diazepam (43hr) –> desmethyldiazepam (24hr) –> oxazepam (8hr)

Total half life ~ 75 hr; Diazepam is LONG acting

42
Q

Action and half life of Flurazepam (a BZ)

A

Flurazepam 74 hr half life, long acting

*cyp3A4 metab

43
Q

What are the intermediate BZ and their half life

A

Alprazolam (Xanax): <6hr, converted to short acting metabolites

Oxazepam/Lorazepam (6-24 hr) converted to inactive metabolites

44
Q

What BZ is short acting and what is it used for

A

Midazolam (Versed) <2 hr, used as pre anesthestic

45
Q

What MOA do BZ use

A

bind to specific sites on GABAa receptor

  • effect DEPENDENT on GABA (unlike barbs)
  • increases affinity of receptor to GABA prolonging its action
  • ceiling effect
46
Q

What anxiety disorders are benzodiazepines not used in

A

OCD: SSRI
Phobia/Panic: SSRI
PTSD: antidepressants
anxiety in children & adolescents: antidepressants

47
Q

What is used to treat insomnia? SE?

A

Flurazepam (Dalmane) and temazepam (restoril) used as hypnotics (fly to sleep.. flurazepam, temazepam, insomnia)

*minor depression of REM sleep, may cause hangover effect *flurazepam is long acting

48
Q

What is used to treat insomnia that is due to difficulty falling but not staying asleep?

A

Shorter acting drugs

?Midazolem (Versed) is short, Alprazolam and Lorazepam are intermediate?

49
Q

What is used to treat status epilepticus

A

Diazepam and Lorazepam

*Lora has Daily seizures (lorazepam, Diazepam, epilepsy)

50
Q

Diazepam and Lorazepam are used to treat what seizure condition

A

status epilepticus

51
Q

?? is used in prep for anesthesia for short surgical procedures? How is it administered? SE?

A

Midazolam (Versed) - a short acting BZ
given IV
*anterograde amnesia

52
Q

What BZ is sometimes used for acute muscle spasm and pain due to injury

A

Diazepam (Valium)

*im dying from the muscle spasms

53
Q

Because long term use of alcohol or barbiturates can produce physical dependence and result in severe withdrawal, what is used to taper withdrawal?

A

Longer acting BZ are used to provide a more tapered withdrawal

Chlordiazepoxide, Diazepam, Lorazepam

54
Q

What are SE of BZ

A

CNS depression
Less common blurred vision, hallucination
Paradoxical excitement (due to dis-inhibition of suppressed behavior) - more common in elderly
Supra-additive (BZ+Barb+EtOH)
Sleep-related behaviors (sleep driving, eating, walking)

*effect most common in first few weeks, decrease as tolerance develops

55
Q

Is tolerance common in BZ use? what about physical dependence?

A

Tolerance common, but generally don’t increase dose

  • physical dependence may occur, abuse potential (though schedule IV)
  • taper slowly following chronic use
56
Q

BZ withdrawal effects include

A
  • rebound anxiety and insomnia
    • makes sense bc BZ are used to treat anxiety and insomnia
  • Muscle weakness, tremor, hyperalgesia, N/V, wt loss, convulsions
  • taper BZ slowly following chronic use
57
Q

What is the OD risk with BZ?

A

relatively safe, but OD generally results in long deep sleep (1-2d), schedule IV drug

*fatalities may occur in people with respiratory difficulties, in children, and when combined with alcohol

58
Q

Fatalities due to BZ use may occur in

A

people with respiratory difficulties, children, and when combined with alcohol

59
Q

What is Flumazenil (Mazicon)

A

BZ antagonist, used to reverse the effects of BZ by competing for GABA receptor

ex: used to reverse Midazolam (Versed) which sometimes causes respiratory depression

60
Q

Besides reversing the effect of BZ, Flumazenil (Mazicon)…?

A

reverses the effects of other drugs ie “z drugs” (zolpidem, Zaleplon, Eszopiclone

61
Q

How long is Flumazenil’s (the BZ antagonist) duration of action? What is the main adverse effect? and who should not be given Flumazenil

A

Duration: 30 min
Major adverse effect: triggers withdrawal and seizures in pt who are physically dependent on BZ

*Do not use in pt with hx of seizures

62
Q

Besides barbs and BZ, what other group of sedative hypnotics are there

A

the z drugs:

Zolpidem (Ambien), Zaleplon (sonata), & Eszopiclone (Lunesta)

63
Q

How do the z drugs (zolpidem, zaleplon, eszopiclone) work? and what properties do they have

A

Bind to BZ1 subtype of GABA receptor to increase GABA mediated inhibition –> sedation zZZzzZz

*Z drugs has very strong and rapid SEDATIVE effects, but no anxiolytic/anticonvulsant/muscle relaxant properties

64
Q

PK of the z drugs?

A

Good oral absorption
Peak levels 30-60 min, short DOA thus morning drowsiness is unlikely (but eszopiclone is longer)
Metab in Liver (CYP3A4); thus half life may be prolonged in severe hepatic disease

65
Q

What are the side effects of the z drugs?
Zolpidem (Ambien)
Zaleplon (Sonata)
Eszopiclone (Lunesta)

A
  • generally very high MOS
  • Gi: diarrhea, nausea
  • CNS: drowsy, dizzy
  • Sleep related behaviors (like BZ)
  • Amnesia occurs with higher than recommended doses; confusion/memory loss/psychosis in elderly
  • may increase depressant effects of other sedative drugs SUPRAadditive
  • low tolerance/dependence
  • rebound insomnia after rapid dc
  • withdrawaL CNS stim, anxiety, seizures with abrupt cessation after long term use of eszopiclone
66
Q

Withdrawal occurs with what z drug and what are the sx

A

withdrawal with eszopiclone (bc longer half life)

sx: CNS stim, anxiety, seizures with abrupt cessation after long term use

67
Q

What is Ramelteon (Rozerem) and how does it work

A

Ramelteon (Rozerem) = Melatonin analogue; resets sleep-wake cycle; promotes sleepiness with no GABA effect

68
Q

Does Ramelteon (Rozerem) rely on GABA to promote sleepiness

*resets sleep/wake cycle

A

No, Ramelteon (Rozerem) is a melatonin analogue

69
Q

Pk of Ramelteon (Rozerem)?

A

Oral absorption, CYP450 metab (3A4, 2C9) in liver; extensive first pass metabolism

*additive sedation with alcohol and other sedative hypnotics

70
Q

What are side effects of Ramelteon (Rozerem), the melatonin analogue

A

very few

drowsiness, dizziness, nausea

71
Q

What is Diphenhydramine (Benadryl)

A

Not classical sedative, but older antihistamine with sedative properties
*active ingredient in majority of OTC preparations for insomnia

72
Q

What is Diphenydramine (Benadryl) and other older antihistamines with sedative properties useful for

A

occasional insomnia

*especially useful for insomniac who has been addicted to BZ or alcohol

73
Q

How does Chloral Hydrate (Noctec) work

A

converted to trichloroethanol which causes sedation; acts similarly to Barbiturates on GABAa receptor

74
Q

Is Chloral Hydrate (Noctec) safe? can if cause any harmful SE?

A

Chloral Hydrate has low MOS

  • high doses induce RESP and VASOMOTOR dep
  • causes gastric irritation, N/V, allergic rxn, and potentially cardiac arrhythmia

*long term use may cause liver damage and fatal intoxication

75
Q

Long term use of Chloral Hydrate (Noctec) may cause

A

liver damage and fatal intoxication

76
Q

What is chloral hydrate (noctec) used for

A

note: cheap
* used in children for sedation during pediatric dental procedures
* used in nursing homes and chronic care instit.

  • use as sedative hypnotic NOT RECOMMENDED
77
Q

What is Buspirone (BuSpar) and how does it work

A

Buspirone relieves anxiety w/o causing sedation

  • partial agonist at POSTsynaptic 5-HT1A (serotonin) receptor to inhibit cell signaling
  • Full agonist for PREsynaptic 5-HT1A receptors to decrease release of 5-HT
  • takes 2 wk for effect, no muscle relaxant or anticonvulsant properties
78
Q

What is Buspirone (BuSpar) used for

A

relieves anxiety without producing sedation (2 wk for effect) specifically:

  1. gen anxiety and anxiety w/ depression
  2. ADHD and autistic pt with anxiety
  3. PMS
  • no muscle relaxant or anticonvulsant properties
  • does not potentiate CNS depression with EtOH or BZ
79
Q

Does Buspirone (BuSpar), and anxiolytic, have an addiction potential? What is it not good for treating?

A

Buspirone (BuSpar) has very low addiction potential thus is an excellent choice of anxiety in recovering alcoholics/addicts
*not good for severe anxiety and/or panic disorder

80
Q

What drugs are good for Insomnia/sedation and anxiety in recovering alcoholics or addicts

A

for Insomnia and sedation: Diphenydramine (benadryl)

For anxiety: Buspirone (BuSpar)

81
Q

What is the PK of Buspirone (BuSpar) and anxiolytic

A

good oral absorption
high 1st pass (like Ramelteon, melatonin analogue)
CYP 3A4 liver metab

82
Q

What is the safety of Buspirone (BuSpar)? What SE might it have?

A

fairly safe even in high doses

*may cause light-headedness, restlessness, HA, drowsiness, N/V

83
Q

DOC for enuresis (bed wetting)

A

tricyclic antidepressants

Pharm III (9 decks)

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