Antiseizure Drugs

Epilepsy
• Epilepsy is -------------------------------.

• Seizures are -------------------------------.

• The causes of seizure are many and include -------- ---------------, ---------,
------------, ------------ and ----------------.

• Seizures are classified into two major types :- ------------- and -----------.
These two classes of seizures are subclassified into other types of
seizures as shown in the table below.
 CLASSIFICATION OF SEIZURES
• Partial focal seizures
- --------------- seizures
- --------------- seizures
- ------------------------

Generalised seizures
- ---------------- seizures
- --------------------) seizures
- ---------
- ----------------------
- ------------------------
- --------------------
 Drugs used in partial seizures and
generalised tonic-clonic seizures
• The major drugs used in partial and generalised seizures are --------- (and
related compounds), ---------, ----------, and the -------------. The availability of
newer drugs- --------, ----------, -------------, -----------, ----------, --------------, --------
--, -------------, ------------and ----------- is altering clinical practice in some
countries where this drugs are available.
• The table below summarises the drugs used in various seizures and their
side effects.

Subclass, Drugs Mechanism of action Pharmacokinetics, Clinical

application
CYCLIC UREIDES Block ------------- through Absorption is --------- dependent.
------------ action on ---------. Decrease Highly -----------------. No -----------.
------------ ------------------. ------- dependent elimination. T1/2
=-----------.
Fosphenytoin is for ------, ------
routes. -------- seizures, -------------
seizures
 Antiseizure drugs
Subclass, Drug Mechanism of action Pharmacokinetics, Clinical
CYCLIC application
UREIDES
------------- Similar to phenytoin, but Well absorbed -------. --------- bound to
converted to ---------- plasma proteins. Peak concentration in
--------. T1/2 is --------h.. Two active
metabolites (---------- and ----------).
Generalised -------- seizures, ---------
seizures

--------------- Enhances -----------. Nearly complete ---------. --------- bound

Reduces -------------- to plasma proteins. Peak concentration
in ---------- h. No active --------. T1/2
varies from -------------.
Generalised -------- seizures, ---------
seizures, ----------- seizures, --------
seizures, status ----------
 Antiseizure drugs
Subclass, Drug Mechanism of action
CYCLIC UREIDES
---------- Reduces low-threshold
Ca2+ currents (----- -type)
Pharmacokinetics,
Clinical application
Well absorbed -------, Peak
level in ---------. -------
protein bound. Completely
metabolised -----------. T1/2
typically ------------.
---------seizure
 Antiseizure Drugs

Subclass, Drug Mechanism of action Pharmacokinetics,

------------
Carbamazepine Blocks --------- through
action on ---------.
Decreases ------------
Clinical application
Well absorbed --------. Peak
level in ----------. No
significant ------------------
Metabolised in part to -------.
1/2 of parent drug ranges
from ----------.
Generalised --------
seizures, --------- seizures

Other drugs in this subclass are ---------, and ---------------

 Antiseizure Drugs
Subclass, Drug Mechanism of action Pharmacokinetics,
Clinical application
Benzodiazepines
----------- Potentiates -------- Well absorbed -----. --------
responses administration gives peak
concentration in 1h with -----
-% bioavailability. Can be
given IV for --------. ------
protein bound. Extensively
metabolised to ----------. T1/2
is -------
Status ---------, seizure -------
----

----------- As for diazepam Over ----% bioavailability.

Extensively metabolised but
--------. T1/2 is -------------.
Others include -------------
and ------------
 Antiseizure Drugs

Subclass, Drug Mechanism of action Pharmacokinetics,

----------- Clinical application
DERIVATIVES
Gabapentin Decreases ------- by acting on -- Bioavailabity ----%
------------ decreasing with ------
doses. -------- bound to
plasma proteins. Not --------
. T1/2 -------.Generalised ----
---seizures, ----- seizures, --
------ seizurre

---------- As for gabapectin Well absorbed -------, -----

bound to --------, not --------.
T1/2 ------. ---------- seizures

----------- ---------- inhibits GABA- --------- --------% bioavailability

orally, ------ bound to
plasma proteins,not -------.
-------- seizures
 Antiseizure Drugs
Subclass, Drug Mechanism of action Pharmacokinetics,
Clinical application
GABA
DERIVATIVES
Vigabatrin Irreversibly inhibits GABA- 70% bioavailability orally,
transaminase Not bound to plasma
proteins,not metabolised.
T1/2 6-8hr (not relevant
because of irreversible
action)
Partial seizures, infantile
spasm.
 Antiseizure Drugs
Drug Toxicities, side effects

Phenytoin -----------------------------------------

Primidone ------------------------------------

Phenobarbital ----------------------------

Ethosuximide --------------------------------
 Antiseizure Drugs
Drug Toxicities, side effects

Carbamazepine ----------------------

Diazepam -----------------

Clonazepam ----------------

Gabapentin ---------------
 Antiseizure Drugs
• Other drugs include ---------, ------------, ------------, ------------, ----------- ---------
------