Ezogabine- Potiga - @-Anti-convulsant (June 2011)
Drug Name:Ezogabine- Potiga - @-Anti-convulsant (June 2011)
List Of Brands:
Indication Type Description:
Drug Interaction
Indication
Adverse Reaction
Contra-Indications
Dosages/ Overdosage Etc
Patient Information
Pharmacology/ Pharmacokinetics
Pregnancy and lactation
Drug Interaction:
Ezogabine plasma levels may be reduced by concomitant administration
of phenytoin or carbamazepine. An increase in dosage of POTIGA
should be considered when adding phenytoin or carbamazepine.
N-acetyl metabolite of ezogabine may inhibit renal clearance of digoxin,
a P-glycoprotein substrate. Monitor digoxin levels.
Indication:
POTIGA (ezogabine) Tablets, CV
Initial U.S. Approval: 2011
WARNING:
RETINAL ABNORMALITIES
AND POTENTIAL VISION LOSS
See full prescribing information for complete boxed warning.
POTIGA can cause retinal abnormalities with funduscopic features simila
to those seen in retinal pigment dystrophies, which are known to result in damage to
the photoreceptors and vision loss.
Some patients with retinal abnormalities have been found to have abnormal visual
acuity. It is not possible to determine whether POTIGA caused this decreased
visual acuity.
The rate of progression of retinal abnormalities and their reversibility are unknown.
Patients who fail to show substantial clinical benefit after adequate titration should
be discontinued from POTIGA.
All patients taking POTIGA should have baseline and periodic (every 6 months)
systematic visual monitoring by an ophthalmic professional.
Testing should include visual acuity and dilated fundus photography.
If retinal pigmentary abnormalities or vision changes are detected,
POTIGA should be discontinued unless no other suitable treatment options
are available and the benefits of treatment outweigh the potential risk of
vision loss.
Drug Name- Potiga
Active Ingredient - Ezogabine
For use as on add-on medication to treat seizures associated with
epilepsy in adults
Indication-
For use as on add-on medication to treat seizures associated with
epilepsy in adults
Approved by FDA on 10-6-2011 (Ref- FDA approved List- 2011)
Adverse Reaction:
The most common adverse reactions (incidence 4% and approximately
twice placebo are-
dizziness, somnolence, fatigue, confusional state, vertigo, tremor,
abnormal coordination, diplopia, disturbance in attention, memory impairment,
asthenia, blurred vision, gait disturbance, aphasia, dysarthria, and
balance disorder.
Contra-Indications:
CONTRAINDICATIONS
None.
WARNINGS AND PRECAUTIONS
Urinary retention: Patients should be carefully monitored for urologic symptoms.
POTIGA can cause skin discoloration: If a patient develops skin discoloration,
serious consideration should be given to an alternative treatment.
Neuropsychiatric symptoms: Monitor for confusional state, psychotic
symptoms, and hallucinations.
Dizziness and somnolence: Monitor for dizziness and somnolence.
QT prolongation: QT interval should be monitored in patients taking
concomitant medications known to increase the QT interval
or with certain heart conditions.
Suicidal behavior and ideation: Monitor for suicidal thoughts or behaviors.
Dosages/ Overdosage Etc:
Indication-
For use as on add-on medication to treat seizures associated with
epilepsy in adults
INDICATIONS AND USAGE
POTIGA is a potassium channel opener indicated as adjunctive treatment of
partial-onset seizures in patients aged 18 years and older who have responded
inadequately to several alternative treatments and for whom the benefits outweigh
the risk of retinal abnormalities and potential decline in visual acuity.
DOSAGE AND ADMINISTRATION
Administer in 3 divided doses daily, with or without food.
The initial dosage should be 100 mg 3 times daily (300 mg per day) for 1 week.
Titrate to maintenance dosage by increasing the dosage at weekly intervals by no
more than 150 mg per day.
Optimize effective dosage between 200 mg 3 times daily (600 mg per day)
to 400 mg 3 times daily (1,200 mg per day).
In controlled clinical trials, 400 mg 3 times daily (1,200 mg per day) showed
limited improvement compared to 300 mg 3 times daily (900 mg per day) with
an increase in adverse reactions and discontinuations.
When discontinuing POTIGA, reduce the dosage gradually over a period of
at least 3 weeks.
POTIGA may cause retinal abnormalities with long-term use; therefore, treatment
should be discontinued if patients fail to show substantial clinical benefit after
adequate titration.
Testing of visual function should be done at baseline and every 6 months
during therapy with POTIGA
If retinal pigmentary abnormalities or vision changes are detected,
POTIGA should be discontinued unless no other suitable treatment options
are available and the benefits of treatment outweigh the potential
risk of vision loss.
Dosing adjustments are required for geriatric patients and patients with
moderate to severe renal or hepatic impairment.
DOSAGE FORMS AND STRENGTHS
-Tablets:50 mg, 200 mg, 300 mg, and 400 mg.
Patient Information:
PATIENT INFORMATION
1.Retinal Abnormalities and Potential Vision Loss
Inform patients of the risk of retinal abnormalities and possible risk of vision loss, which
may be permanent .
All patients taking POTIGA should participate in baseline and periodic ophthalmologic
monitoring of vision by an ophthalmic Professional. Inform patients that if they suspect
any vision changes, they should notify their physician immediately.
2.Urinary Retention
Patients should be informed that POTIGA can cause urinary retention (including urinary
hesitation and dysuria). If patients experience any symptoms of urinary retention, inability to
urinate, and/or pain with urination, they should be instructed to seek immediate medical
assistance
3.Skin Discoloration
Inform patients that POTIGA can cause discoloration of nails, lips, skin, palate, and parts
of the eye and that it is not known if the discoloration is reversible upon drug discontinuation
. Most skin discoloration has been reported after at least 2 years of treatment with POTIGA,
4. Psychiatric Symptoms
Patients should be informed that POTIGA can cause psychiatric symptoms such as
confusional state, disorientation, hallucinations, and other symptoms of psychosis.
Patients and their caregivers should be instructed to notify their physicians if they
experience psychotic symptoms
5. Central Nervous System Effects
Patients should be informed that POTIGA may cause dizziness, somnolence, memory
impairment, abnormal coordination/balance, disturbance in attention, and
ophthalmological effects such as diplopia or blurred vision.
Patients taking POTIGA should be advised not to drive, operate complex machinery,
or engage in other hazardous activities until they have become accustomed to any
such effects associated with POTIGA
6. Suicidal Thinking and Behavior
Patients, their caregivers, and families should be informed that AEDs, including
POTIGA, may increase the risk of suicidal thoughts and behavior and should be
advised of the need to be alert for the emergence or worsening of symptoms
of depression, any unusual changes in mood or behavior, or the emergence
of suicidal thoughts, behavior, or thoughts about self harm. Behaviors of concern
should be reported immediately
7.Pregnancy
Patients should be advised to notify their physicians if they become pregnant
or intend to become pregnant during therapy. Patients should be advised to notify
their physicians if they intend to breastfeed or are breastfeeding an infant.
8. Nursing Mothers
It is not known whether ezogabine is excreted in human milk. However, ezogabine
and/or its metabolites are present in the milk of lactating rats. Because of the
potential for serious adverse reactions in nursing infants from POTIGA, a decision
should be made whether to discontinue nursing or to discontinue the drug,
taking into account the importance of the drug tothe mother.
9. Pediatric Use
The safety and effectiveness of POTIGA in patients under 18 years of age have
not been established
Pharmacology/ Pharmacokinetics:
1. Mechanism of Action
The mechanism by which ezogabine exerts its therapeutic effects has not been fully
elucidated. In vitro studies indicate that ezogabine enhances transmembrane potassium
currents mediated by the KCNQ (Kv7.2 to 7.5) family of ion channels.
By activating KCNQ channels, 433 ezogabine is thought to stabilize the resting
membrane potential and reduce brain excitability. In 434 vitro studies suggest
that ezogabine may also exert therapeutic effects through augmentation of
GABA-mediated currents.
2. Pharmacokinetics
The pharmacokinetic profile is approximately linear in daily doses between 600 mg and
1,200 mg in patients with epilepsy, with no unexpected accumulation following repeated
administration. The pharmacokinetics of ezogabine are similar in healthy volunteers
and patients with epilepsy.
Pregnancy and lactation:
1 Pregnancy
Pregnancy Category C.
There are no adequate and well-controlled studies in pregnant women
POTIGA should be used during pregnancy only if the potential benefit justifies the
potential risk to the fetus
2. Nursing Mothers
It is not known whether ezogabine is excreted in human milk. However, ezogabine
and/or its metabolites are present in the milk of lactating rats.
Because of the potential for serious adverse reactions in nursing infants
from POTIGA, a decision should be made whether to discontinue nursing
or to discontinue the drug,taking into account the importance of the drug to
the mother.
3. Pediatric Use
The safety and effectiveness of POTIGA in patients under 18 years
of age have not been established
4.Geriatric Use
There were insufficient numbers of elderly patients enrolled in partial-onset
seizure controlled trials (n = 8 patients on ezogabine) to determine the
safety and efficacy of POTIGA in this population.
Dosage adjustment is recommended in patients aged 65 years and older
