?????????? ??????????????

1
?????????? ?????????????? ??????????????? ?
???????? ??????????? ???????

• ?????? ???????
• 30 ??. ?????? (2010)

2
?????????

• ?? ?????????????, ???????? ?????????? ?? ??????
  ? ???????? ?????????, ?????????? ?? ? ?????????
  ?? ????????, ????? ????? ?? ??????????? ??
  ????????? ?? ??????????.
• ?? ? ???? ?? ???-??????? ??????????? ?? ????????
  ??????? 4-10 ?? 1000 ???? ?????????
• ???????? ????????
• ???????????? ???????
• ????????????? ? ?????? ??????? - 50 ?? 10
  ??????? ???????, ? 70 ?? 20 ???.
• ??????? ?? ????????, ????????, ? ??????????????
  ??????? ?? ????????? ??????????, ?????? ??
  ???????, ???????? ??? ???????????? ???????.
• ????????????? ?? ??????? ????? ?? ????????
  ?????????? ????? (excitotoxicity).

3
?????????
4
?????????

• ????????????? ???????-???????? ???????? (grand
  mal) - ????? ???????? ??????????,
  ??????????????? ????????? ?? ??????????.
  ????????? ???? ??????, ?????? ? ??????? ?,
• ???? ???? ????????? ?????????? ????????? ? ???.
• ?????? (petit mal) - ?????????????? ?????????,
  ???????? ? ?????? ???????, ??? ????????, ??? ????
  ?????? ??????, ??????? ?? ????? ? ? ??????????? ?
  ????? ?? ?????????? ????????????..
• ??????????? (???????) ????????. ?? ?? ??????????
  ?? ???????????? ?????????, ???????? ???? ????
  ???? ?? ??????, ??? ?? ?? ???????????. ?
  ?????????? ?? ???? ??? ???? ?? ?????? ?
  ?????????, ?????????? ?? ????????. ???? ??
  ???-????? ????????? ???????? ??? ???????????
  ????????.

5
??????? ?? ??

• ?????? ????? ????????? ?????????? ?????????
  (EPSP) ? ??????????? ?????????????? ?????????
  (IPSP).
• ??? ?? ????????? ????????? ?? ??????????
  ???????????????? ? ????????????????? ??
  ????????????? ??????? ?? ??????????????? ??????.

• ?????????? ??????????????
• ??????????? Phenobarbital (1912)
• ?????????? Phenytoin (1938)
• ???????????????? Trimethadione
• ??????????? Ethosuximide
• ???????????? Carbamazepine, Oxcarbazepine
• ?????????????? Diazepam, Clonazepam,
  Clorazepate
• ????????? Valproic acid, Sodium valproate

• Vigabatrin
• Gabapentin
• Lamotrigine
• Felbamate
• Tiagabine
• Topiramate
• Levetiracetam

????
6
????????? ?? ????????

• ??????????? ?? GABA ??????
• - ????????????? ????
• - ?????????? ?? GABA ??????????????
• - ?????????? ????????
• ?????????? ?? Na ????? Phenytoin,
  Carbamazepine,Valproate,Lamotrigine
• ????????? ?? T-(???????????? ?????????) ? L-???
  ???????? ?????? Ethosuximide (T-???), Gabapentin
  (L-???)?
• ????????? ?? ??????????? ???????? NMDA (N
  -methyl-D-aspartate) ?????? (????
  ??????-??????????? ?????) felbamate, valproic
  acid ? AMPA/Kainate ?????? topiramate?
• ???? ????????? (levetiracetam, zonisamide),
  ???????? ?? ?????, ?????????? ?????????.
  ????????? ?? ?????????? ?? ???????????
  ??????????? ??????? 2A, ????? ??? ???? ?
  ??????-????????? ?????? ?? ????????????? ??
  ???????????????.

Barbiturates (Phenobarbital) Benzodiazepines
Vigabatrin Tiagabine Gabapentin
7
????????????? ?? ??????????? ???????????? ??
????????? ????? ? ????????? ?? ??????-??????????
?????????? ??????????.
????????? ?? ????????
?-???????? ?? ????????? ?? ??????????
??????????? ??????????? ? ????????????????? ???
? ?????????????? ?? ?????????.
8
??????????? ???????? ?? GABA-A ?????????
?????????????? (? ????? Cl-????? ? ???????),
??????????? (? ????????? ?? ???????? ?? ??????),
Ganaloxone????????? ?? ???????? ??????
Tiagabine?????????? ?? GABA ?????????????
Vigabatrine?????????? ?? ???????????????????????
Gabapentin, Valproate????????????? Progabide
????????? ?? ????????
GABA-A-?????????? ?????? ????????? ????????
??????? ???????? ?? (Cl-) ? ???? ??
???????????????.
9
A????????????????????? ????????
???????-???????? ???????(grand mal) carbamazepine, oxcarbazepine, phenytoin, valproate, vigabatrin, lamotrigin, gabapentin, topiramate
??????? (petit mal) ethosuximide, valproate, lamotrigine, clonazepam
??????? ?? ???????????? ?? carbamazepine, oxcarbazepine, valproate clonazepam, topiramate, phenytoin, lamotrigine
?? ?????? diazepam i.v. per rectum, diazepam, clonazepam i.v.
???????????? ????? carbamazepine, gabapentin
????????????? ?? ???????????? carbamazepine, valproate, lamotrigine
10
????????? ???????? ??? ??? ?? ?????? ?? ???
Carbamazepine ??????, ?????????, ??????, ?????????????, ?????, ?????? ???????????, ????????? ??? ?????? ???????, ??????????, ????????
Ethosuximide ??????, ????????? ????????? ?? ????, ???????????, ??????????????
Felbamate ??????, ?????????, ?????????, ?????????? ????????, ?????????, ??????????, ???????
Gabapentin - ?????????, ???????????, ???????
Lamotrigine ?????????, ?????? ???????????, ??????????
Levetiracetam ???????? ?????, ?????????, ???????????, ?????????????
Oxcarbazepine ??????, ?????????, ???????????? ???????, ??????????, ?????????, ???????, ?????? ???????
Phenytoin ??????????? ?? ???????, ??????????, ??????, ?????????????? ????????, ??????? ?????, ?????? ???????, ???????, ??????????
Pregabalin ??????????? ???????????, ??????????, ???????
Primidone, phenobarbital ??????, ?????? ?????????? ?? ????, ???????, ????????, ???????????? ???????, ??????????????, ???????, ????????, ??????????
Tiagabine - ???????????, ????? ?? ???????, ?????????, ??????, ????????, ??????, ?????? ????????????, ??????? ?????
Topiramate ?????? ?? ?????, ???????? ??????, ?????????? Fatigue, nervousness, difficulty concentrating, confusion, depression, anorexia, language problems, anxiety, mood problems, tremor
Valproate ??????? ?? ?????, ??????, ?????????, ????????, ????????? ??? ??????????? ??????

11
PHENYTOIN
Antiepileptic Drugs Author Juan G Ochoa
CARBAMAZEPINE
LAMOTRIGINE
ETHOSUXIMIDE
DIAZEPAM
1. Katzung BG. Bacis and clinical pharmacology,
11th ed. 2009 2.Ochoa JG. Antiepileptic drugs.
Available from http//emedicine.medscape.com/arti
cle/1187334-overview 3.Tripathi KD. Essential of
medical Pharmacology, 5th ed. 2004 4.
???????????? ??? ?????????? ?? ??. ?????? ? ?.
?????????