ANTICONVULSANTS

Anticonvulsants
 Drugs used for epileptic seizures
 Suppress the abnormal electric impulses
from the seizure focus to other cortical areas
 Prevents the seizure but not eliminating the cause
of the seizure
 Classified as Central Nervous System depressant
 Usually taken throughout person’s lifetime but
may be discontinued if there has not been a
seizure for the past 3-5 years
 Also known as anti-epileptic
 Two most common seizures

1. Tonic-Clonic Seizure – also called grand

mal seizure; most common form of
seizures. In the tonic phase, the skeletal
muscles contract or tighten in a spasm,
lasting3 to 5 seconds. In the clonic phase,
there is a dysrhythmic muscular
contraction, or jerkiness, of the legs and
arms, lasting 2 to 4 minutes.
2. Absence seizure – also called petit
mal seizure; brief loss of
consciousness lasting less than 10
seconds; fewer than three spike
waves on the electroencephalogram
(EEG) printout, usually occurs in
children.
 Action of Anticonvulsants
 By suppressing sodium influx through the drug binding
to the sodium channel when it is inactivated, thus
prolonging the channel inactivation and thereby neuron
firing
 By suppressing the calcium influx, thus preventing the
electric current generated by the calcium ions to the T-
calcium channel
 By increasing the action of gammaaminobutyric acid
(GABA), which inhibits neurotransmitter throughout the
brain
 Types of Anticonvulsant

1. Hydantoins
– First anticonvulsant used to treat seizures
– Discovered in 1938 and is still the most
commonly used drug for controlling seizures
– Has the least toxic effects, has a small effect on
general sedation, an is nonaddicting
– Should not be used during pregnancy because it
can have a teratogenic effect on the fetus
 Client Teachings when taking
Phenytoins
 Instruct client to the suspension form well before
pouring
 Advice client not to drive or perform other
hazardous activities when beginning
anticonvulsant therapy. Until client adapts to drug
dosage, drowsiness is likely to occur.
 Alert female clients contemplating pregnancy to
consult with the health care provider because
phenytoin and valproic acid may have teratogenic
effect.
 During pregnancy, seizures frequently increase because
of increased metabolism rates, and serum phenytoin
levels should be closely monitored. Most
anticonvulsants are classified pregnancy category D.
 Inform client that alcohol and other CNS depressants
can cause an added depressive effect on the body and
should be avoided.
 Teach the client not to abruptly stop the drug therapy
but rather to withdraw the prescribed drug gradually
under medical supervision to prevent the seizure
rebound (recurrence of seizure)
 Teach the client not to take the OTC drugs without first
consulting the health care provider.
 Instruct the client with diabetes to monitor serum
glucose levels more closely than usual because
phenytoin may inhibit insulin release, thus causing an
increase in blood sugar.
 DIET
 Educate client to take the anticonvulsant at the
same time everyday with food or milk. If liquid
form is used, shake well before ingesting the
drug.
 Side Effects
 Urine must be pinkish or reddish brown.
 Maintain good oral hygiene and use a soft
toothbrush to prevent gum irritation and bleeding
 Report symptoms of sore throat, bruising, and
nosebleeds, which may indicate a blood dyscrasia.
 Inform any the health care provider of adverse
reactions such as gingivitis, nystagmus
( involuntary movement of the eyeballs) slurred
speech, rash, and dizziness.
 Pharmacokinetics

Phenytoin s slowly absorbed from the small

intestine. It is a highly protein bound (85-95%)
drug; a decrease in serum protein or albumin ca
increase the free phenytoin serum level. With a
mall amount to average drug dose, the half-life of
phenytoin is approximately 22 hours; however, the
range can be from 6-45 hours. Phenytoin is
metabolized to inactive metabolites, and that
portion is excreted in urine.
 Pharmacodynamics

The pharmacoynamics of orally administered

phenytoin include on set of action within 30
minutes to 2 hrs, peak serum concentration
on 1.5 to 3 hurs, steady state of serum
concentrationnin 7-10 days, and a duration
of action dependent to half-life. Oral
phnytoin is most commonly ordered as a
sustained-release capsule. The peak
concentration time is 4-12hours .
 Pharmacodynamics
Intravenous (IV) infusion of phenytoin should be
administered by a direct injection into a large vein.
The drug may be diluted in a saline solution;
however, dextrose solution should be avoided
because of drug precipitation. Continuous IV
infusion of phenytoin should not be used. IV
phenytoin, 50 mg in faction thereof, should be
administered over a period of 1 minute for adults
and, when the client is elderly, at a rate of 25 mg
per minute.
Infusion rates of more than 50 mg per
minute may cause hypotension or
cardiac dysrhythmias, especially
with older and debilitated clients
Local irritation at injection site of
phenytoin irritates tissues and may
cause damage. For this reason and
because of its erratic absorption rate,
IM administration of phenytoin is
discouraged.
 2. Barbiturates
 Phenobarbital, a long acting barbiturate, is still
prescribed to treat grand mal seizures and acute
episodes of status epilepticus seizures (rapid
succession epileptic seizures), meningitis, toxic
reactions, and eclampsia.
 Problems associated with Phenobarbital include its
cause of general sedation and clients tolerance to
drug.
 3. Succinimides
 The succinimides drug groups is used to treat
absence or petit mal seizures, and it may be used in
combination with other anticonvulsants to treat
seizures.
 Ethosuximide (Zarontin)- succinimide of choice
 Methsuximide (Cebuntin) and Phensuximide
(Milontin)- used mainly for petit mal refractory
seizures
 4. Oxazolidones or
Oxazolodinedione
 Oxazolidones, trimethadione, and
paramethadione are prescribed to treat petit
mal seizures.
– Prescribed more frequently than
paramethadione
– May be used in combination with other drugs
or singly to treat refractory mal seizures
 5. Benzodiazipines
 3 benzodiapines that have anticonvulsants effects:
 Clonazepam- effective in controlling petit mal
(absence) seizures.
 2. Clorazepate dipotassium- frequently
administered in adjunctive therapy for treating
partial seizures.
 Diazepam- primarily described for treating acute
status epilepticus and must e administered IV to
adhere the desired response
 - has short term effect.
 6. Iminostilbenes
 Carbamazepine- an iminostibene, is effective in
treating refractory seizures disorder that have not
responded to other convulsant therapies.
– Use to control grand mal and partial seizures and
combination of these seizures.
– Use also for psychiatric disorders, tnigeminal neuralgia,
and alcohol withdrawal.
– Not approved by FDA for treatment of the above
mentioned disorder.
 7. Valproate

 Valproic acid has been prescribed for petit

mal, grand mal and mixed types of seizures.
 Care should be taken when giving this drug
to very young children and clients with liver
disorders because of hepatoxicity is one of
the possible adverse reactions
 Anticonvulsants and
Pregnancy
 During pregnancy, seizure episodes increase 25%
in women with epilepsy.
 Hypovia that may occur during seizures places
woman with epilepsy and her fetus at risk.
 Anticonvulsant drugs increase the loss of folate
(folic acid) in pregnant women.
 Tend to act as inhibitors of Vitamin K, which
contributes to hemorrhaging in infants shortly
after birth.
 Anticonvulsants and
Pregnancy
 Some anticonvulsants drugs have teranogenic properties
that increase the risk for fetal malformation.
1.Phenytoin and carbamazepine
- Linked to fetal anomalies such as cardiac defects and
cleft palate.
2. Trimethadione
- should not be given to women bearing of child because
of its strong teratogenic effect.
3. Valproic acid
- causes neural tubal effect (spinal bifida) in 2% to 3% of
pregnant women who take the drug
 Anticonvulsant and Febrile
Seizures
 Seizures associated with fever usually occur in
children between the ages of 3 months and 5
years. Epilepsy develops in app. 2.5% of children
who have had one or more febrile seizures.
 Prophylactic anticonvulsants such as
Phenobarbital or diazepam may be indicated for
high risk client.
 Valproic acid should not be given to children
because of its possible hepatotoxic effects.
 Anticonvulsants and Status
Epilepticus
 Status Epilepticus- a continuous seizure state,
considered a medical emergency.
 The choices of pharmacologic agents are
diazepam (Valium) administered IV or lorazepam
(Ativan) followed by IV administration of
phenytoin (Dilantin).
 For continued seizures, midazoleum (Versed) or
propofol (Diprivan), then high-dose barbiturates
are used. These drugs should be administered
slowly to avoid respiratory depression.
 Selected Anticonvulsants for
Seizure Disorders
 Tonic-Clonic (Grand Mal) – Phenytoin,
Carbamazepine, Fosphenytoin,
Lamotrigine, Primidone, Phenobarbital

 Absence (Petit Mal) – Ethosuximide,

Valproic Acid, Lamotrigine, Clonazepam
 Reporters

Judimer S. Bendita
Rafael C. Catbagan, Jr.
BSN 3B