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Pharmacology Final > Anticonvulsants > Flashcards

Anticonvulsants Flashcards

1
Q

What class is phenobarbital?

A

barbiturates

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2
Q

what is considered a first line agent for the control of seizures in neonates?

A

phenobarb

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3
Q

how effective is phenobarb?

A

it is frequently ineffective in achieving complete seizure control in neonates

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4
Q

what are indications for phenobarb use?

A

neonatal seizures, generalized tonic clonic seizures, partial seizures and prolonged febrile convulsions; can also be used in NAS and infants with cholestasis (enhances bile secretion)

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5
Q

why are newer agents not considered first line?

A

newer agents (ex: keppra) may develop a role in mgmt of neonatal sz as it becomes more frequently used- more clinical trials are needed

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6
Q

what are the advantages of phenobarb?

A

wide spectrum of phenobarb activity, wide therapeutic range, availability of parenteral and enteral dose forms, low cost and extensive experience of use in peds

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7
Q

what are the disadvantages of phenobarb?

A

resp depressions, sedation, physical dependence, negative cognitive effects, hyperactivity and potential adverse effects on developing neurons

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8
Q

what is the effect of age on vol of distribution?

A

as the infant’s gestation age increases, the vol of distribution decreases ( dec in total body H2O and concurrent increase in total body fat)

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9
Q

what is the mechanism of action for phenobarb?

A

potentiation of inhibitory neurotransmission by prolonging the open state of GABA- mediated sodium channels

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10
Q

the suppression of what may also contribute to the therapeutic effects of phenobarb?

A

the selective suppression of abnormal neurons

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11
Q

what is the vol of distribution of phenobarb?

A

it has a large vol of distribution, distributing into all tissue, 50% bound to plasma protein

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12
Q

what is the typical doseage of phenobarb?

A

loading dose: 20 mg/kg IV; additional doses: 5-10 mg/kg IV Q 30-60 min may be required if sz persist

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13
Q

what is the therapeutic level of phenobarb?

A

30-40 mcg/mL

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14
Q

at what rate should phenobarb be administered?

A

10-15 min

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15
Q

what side effects can be seen in serum concentrations of 40-50 mcg/mL of phenobarb?

A

resp depression &/or coma; bradycardia with levels >50 mcg/mL

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16
Q

what side effects can be seen in serum concentrations > 80 mcg/mL of phenobarb?

A

resp depression &/or death

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17
Q

what have current studies demonstrated with regards to phenobarb dosing?

A

infants may require up to 40mg/kg total loading dose and effective sz control has been r/t phenobarb dose with 70% control in doses of 40 mg/kg

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18
Q

what special considerations should be made for infants on ECMO?

A

require higher doses to achieve effective serum concentrations (r/t large vol of distribution of infant + circuit)

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19
Q

what is the half life of phenobarb?

A

long elimination time, avg 100-200 hours in neonates

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20
Q

how is phenobarb metabolized?

A

primarily in the liver and excreted in urine

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21
Q

what class of drug is lorazepam?

A

benzodiazepine; indicated as an anticonvulsant

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22
Q

what is the indication for lorazepam in neonates?

A

for the acute management of patients with sz refractory to conventional therapy

23
Q

CNS depression is dependent upon what with regards to lorazepam?

A

dose dependent

24
Q

what is the onset of action of lorazepam?

A

within 5 min

25
Q

when is peak conc achieved with lorazepam?

A

within 45 min

26
Q

what is the duration of action of lorazepam?

A

3-24 hours

27
Q

what is the mean half life of lorazepam?

A

40 hours

28
Q

what is the typical doseage of lorazepam?

A

0.05-0.1 mg/kg per dose IV slow push, repeat dosing may be required

29
Q

what should be monitored closely with regards to lorazepam administration?

A

IV site for signs of phlebitis &/or infiltration; needs close monitoring of renal fx (excreted by the kidneys)

30
Q

what are the adverse effects of lorazepam?

A

resp depression and some rhythmic myoclonic jerking has been noted in premature infants

31
Q

what class of drug is levetiracetam?

A

anticonvulsant

32
Q

what are the indications for levetiracetam administration?

A

2nd line of therapy for sz that are refractory to phenobarb and other anticonvulsants; recently has been used as an alternative to phenobarb in neonates

33
Q

what is the mechanism of action of levetiracetam?

A

inhibits burst firing without affecting neuronal excitability

34
Q

what is the typical dosing of levetiracetam?

A

10mg/kg IV Q24h; infuse over 15 min

35
Q

what is the onset of action of levetiracetam?

A

30 min

36
Q

when is peak conc achieved with levetiracetam?

A

within 2 hours

37
Q

what is the mean half life of levetiracetam?

A

6 hours

38
Q

what is the therapeutic serum levels of levetiracetam?

A

don’t routinely monitor drug levels but should be between 10-40 mcg/mL

39
Q

what are the adverse effects of levetiracetam?

A

overall very minimal; somnolence, fatigue, ataxia, headache and behavioral changes (agitation, hostility, aggression, irritability, depression, nervousness)- difficult to assess in neonates

40
Q

what class of drug is phenytoin?

A

anticonvulsant

41
Q

how frequently is pheytoin administered?

A

2nd most commonly administered nonbenzo

42
Q

what are the indications of phenytoin administration?

A

2nd line therapy for managing neonatal sz, status epilepticus, generalized tonic clonic sz and partial sz with or without secondary generalization

43
Q

what is the mechanism of action of phenytoin?

A

blockade of voltage-sensitive Na channels, thus inhibiting repetitive neuronal firing

44
Q

what are the additional actions of phenytoin?

A

alterations of Na, K and Ca conduction, membrane potentials and concentration of AA, norepi, acetylcholine and GABA

45
Q

why are small incremental doses of phenytoin recommended?

A

as serum phenytoin conc increases, the fraction of drug eliminated per unit of time decreases; small increases in dose can result in disproportionately large increases in the actual serum conc

46
Q

what is the route of metabolism of phenytoin?

A

hepatic

47
Q

what is the typical doseage of phenytoin?

A

loading dose: 15-20 mg/kg IV; maintenance dose: 3-5 mg/kg IV Q12h (doses are based on age and wt)

48
Q

why is the rate of infusion of phenytoin important?

A

slow infusion to prevent cardiac toxicity

49
Q

what is the max rate of phenytoin infusion?

A

0.5 mg/kg/min

50
Q

what is the only IVF compatiable with phenytoin?

A

NS; numerous clinically significant pharmacokinetic and pharmacodynamic drug interactions involving phenytoin have been noted

51
Q

what is the therapeutic range of phenytoin?

A

8-15 mcg/mL

52
Q

why is TDM recommended with phenytoin?

A

to maximize therapeutic effect and minimize toxicity

53
Q

what are the cardiac toxicity effects of phenytoin?

A

bradycardias and hypotension; a/w propolineglyco and ethanol consitutents of parenteral formulations

Pharmacology Final (5 decks)

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