PHENYTOIN

Inhibition of Na channel function:

It stabilizes the excitable
membranes of neuronal and
cardiac cells
Pharmacokine
Administered orally (normal route)
tics
or by IM or by IV injection.
Slow absorption and inactivated by
liver microsomal enzymes.
Uses
First line therapy for all types of

epilepsy except absence

seizures.
Dose: 150 300 mg/day, gradually
increase to maximal 600 mg/day
Phenytoin combined with Dz (Drug
of choice in the maintenance of
patients with status epilepticus)
Mechanism of
action

Carbamazepine
Similar to phenytoin.

Slow absorption.
Metabolized in liver.
Excreted in urine.

Valproate
Similar to phenytoin.

Rapid absorption.
Metabolized in liver.
Excreted in urine.

For all types of epilepsy

Broad spectrum
anticonvulsant
Drug of choice for partial
Dose: 600 mg daily
seizures and tonic clonic
seizures
Trigeminal neuralgia (a painful
inflammation of the
trigeminal nerve; fifth
cranial nerve)
glossopharyngeal
neuralgias.
Dose : 100 400 mg BD
Adverse
Narrow therapeutic index (even
1. CNS:
1.Xerostomia
effects
small fluctuations in plasma levels
Drowsiness, blurred vision 2.Inhibition of platelet
can cause toxicity)
(reversible), dizziness,
aggregation
diplopia, ataxia,
3.GI complaints
1.CNS:
nystagmus, headache.
4.Weight gain
Cerebello vestibular effects,
2. Hypersensitivity reactions: 5.Hair loss
ataxia, nystagmus, lethargy,
Rash, dyspepsia.
6.Drowsiness
tremor, dystonia, confusion.
3. Water retention,
7.Tremor
2.Long term effects:
leucopenia, aplastic
Gum hypertrophy, gingivitis,
anaemia.
gingival hyperplasia, slurred
speech, hirsutism, coarsening of
facial features.
3.IV route:
Cardiac arrhythmias, CNS
depression
4.Haematological effects:
Thrombocytopenia, interfere
with platelet aggregation,
increase the prothrombin time
5.Hypersensitivity reactions and
Stevens-Johnson Syndrome
6.Overdose:
Coma, apnoea
Drug
Inhibition of phenytoin metabolism CBZ increases metabolism of
Interactions Valproate
Phenytoin
Cimetidine
Warfarin
Cotrimoxazole
Theophylline
Doxycycline
Oral contraceptives
Isoniazid
Doxycycline
Chloramphenicol
Oral contraceptives
Do not administer together
Contraindicati 1.Teratogenic causing fetal
1. Severe hepatotoxic
on
hydantoin syndrome
reactions
2.Deficiency in prenatal growth,
2. Teratogenic effects
mental retardation, cleft palate,
such as neural tube
heart deformities
defects
3. Life threatening
pancreatitis