Excegran
Excegran - General Information
Excegran is a sulfonamide anticonvulsant approved for use as an adjunctive therapy in adults with partial-onset seizures. Excegran may be a carbonic anhydrase inhibitor although this is not one of the primary mechanisms of action. Excegran may act by blocking repetitive firing of voltage-gated sodium channels leading to a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may inhibit the uptake of the inhibitory neurotransmitter GABA while enhancing the uptake of the excitatory neurotransmitter glutamate.
Pharmacology of Excegran
Excegran is an antiseizure drug chemically classified as a sulfonamide and unrelated to other antiseizure agents. The precise mechanism by which zonisamide exerts its antiseizure effect is unknown, although it is believed that the drug blocks sodium channels which leads to the suppression of neuronal hypersynchronization (i.e. convulsions). Likewise zonisamide has also been found not to potentiate syanptic activity by GABA (gamma amino butyric acid).
Excegran for patients
LEAFLET
Questions and Answers about ZONEGRAN (zonisamide) capsules
What is the most important information I should know about ZONEGRAN?
Some people taking ZONEGRAN (ZON-uh-gran) can get serious reactions. If you get any of the following symptoms, call your doctor right away:
* Rash (may be a sign of a dangerous condition)
* Fever, sore throat, sores in your mouth, or bruising easily (may be signs of a blood problem)
* Sudden back pain, abdominal (stomach area) pain, pain when urinating, bloody or dark urine (may be signs of a kidney stone)
* Decreased sweating or a rise in body temperature (especially in patients under 17 years old)
* Depression
* Thoughts that are unusual for you
* Speech or language problems
* Severe muscle pain and/or weakness
ZONEGRAN can cause drowsiness and coordination problems.
Do not drive or operate dangerous machinery until you know how ZONEGRAN affects you.
What Is ZONEGRAN?
ZONEGRAN is a medicine to treat partial seizures in adults. It is taken with other seizure medicines to help control your seizures.
Who should not take ZONEGRAN?
Talk to your doctor first before stopping ZONEGRAN.
Tell your doctor if you are allergic to sulfa drugs. Do not take ZONEGRAN if you are allergic to any sulfa drugs (for example, BactrimTM or Septra) or ZONEGRAN.
How should I take ZONEGRAN?
Be sure to follow your doctorís directions. Starting a new medicine can be confusing. If you have any questions, call your doctor.
Start with one ZONEGRAN capsule each day (100 mg). Swallow the capsule whole. Do not bite into or break the capsule. You may take this medicine with or without food.
After a week or so, your doctor may increase your dose of ZONEGRAN. This may occur more than once. It is done to get the best control for your seizures. Take only the number of ZONEGRAN capsules you were told to take.
Talk to your doctor about what to do if you miss a dose.
If you think you have overdosed on your medicine, call your local poison control center or emergency room right away.
Drink 6-8 glasses of water a day. This may help prevent kidney stones.
Talk to your doctor before stopping ZONEGRAN or any other seizure medicine. Stopping a seizure medicine all at once can cause status epilepticus, a serious problem.
What shoud I avoid while taking ZONEGRAN?
ZONEGRAN may make you drowsy. Do not drive a car or operate complex machinery until you know how ZONEGRAN may affect you.
Tell your doctor about any other medicines you may be taking, including non-prescription medicines.
Tell your doctor right away if you are pregnant or plan to become pregnant. You and your doctor can decide if the benefits of taking ZONEGRAN outweigh the risks. ZONEGRAN may cause birth defects.
It is not known whether ZONEGRAN is passed through breast milk to the baby. Before taking ZONEGRAN, tell your doctor if you are nursing or planning to nurse your baby.
What are the possible or reasonably likely side effects of ZONEGRAN?
The most common side effects are drowsiness, loss of appetite, dizziness, headache, nausea, agitation, and irritability. These side effects could occur at any time, but most often occur in the first 4 weeks.
Contact your doctor right away if:
* you develop skin rash
* your seizures worsen
* you develop signs of kidney stones (sudden back pain, abdominal pain, blood in your urine)
* you develop signs of a blood problem (fever, sore throat, sores in your mouth, or bruising easily)
* you get depressed
* you start having thoughts that are unusual for you
* you are very drowsy, have difficulty concentrating, or have coordination problems
* you develop speech or language problems
Other information about ZONEGRAN:
Medicines are sometimes prescribed for purposes other than those listed in a patient leaflet. Use ZONEGRAN only for the reason your doctor told you. Do not use it for another reason. Do not share your ZONEGRAN with others.
This is a summary of information about ZONEGRAN. Call your healthcare professional with any questions. Your doctor or pharmacist can give you the complete information about ZONEGRAN that is written for health professionals. You can also get information about ZONEGRAN at www.elan.com. You can get information and help from the Epilepsy Foundation at 800-EFA-1000 or www.efa.org.
Distributed by: Elan Biopharmaceuticals, a business unit of Elan Pharmaceuticals, Inc.
San Diego, CA 92121, ZONEGRAN is a trademark licensed exclusively to Elan Pharmaceuticals, Inc., All other product names may be trademarks of the respective companies with which they are associated., © 2000 Elan Pharmaceuticals, Inc.
Excegran Interactions
Effects of ZONEGRAN on the pharmacokinetics of other antiepilepsy drugs (AEDs): Zonisamide had no appreciable effect on the steady state plasma concentrations of phenytoin, carbamazepine, or valproate during clinical trials. Zonisamide did not inhibit mixed-function liver oxidase enzymes (cytochrome P450), as measured in human liver microsomal preparations, in vitro. Zonisamide is not expected to interfere with the metabolism of other drugs that are metabolized by cytochrome P450 isozymes.
Effects of other drugs on ZONEGRAN pharmacokinetics:
Drugs that induce liver enzymes increase the metabolism and clearance of zonisamide and decrease its half-life. The half-life of zonisamide following a 400 mg dose in patients concurrently on enzyme-inducing AEDs such as phenytoin, carbamazepine, or phenobarbital was between 27-38 hours; the half-life of zonisamide in patients concurrently on the non-enzyme inducing AED, valproate, was 46 hours. Concurrent medication with drugs that either induce or inhibit CYP3A4 would be expected to alter serum concentrations of zonisamide.
Interaction with cimetidine: Zonisamide single dose pharmacokinetic parameters were not affected by cimetidine (300 mg four times a day for 12 days).
Excegran Contraindications
ZONEGRAN is contraindicated in patients who have demonstrated hypersensitivity to sulfonamides or zonisamide.
Additional information about Excegran
Excegran Indication: For use as adjunctive treatment of partial seizures in adults with epilepsy.
Mechanism Of Action: Excegran binds to sodium channels, voltage sensitive calcium channels and to a lesser extent carbonic anhydrase. This blocks or suppresses neuronal depolarization and hypersynchronization.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Zonisamide
Synonyms: Zonisamida [Spanish]; Zonisamidum [Latin]
Drug Category: Antioxidants; Anticonvulsants
Drug Type: Small Molecule; Approved
Other Brand Names containing Zonisamide: Exceglan; Excegram; Excegran; Zonegran;
Absorption: Variable, yet relatively rapid rate of absorption with a time to peak concentration of 2.8-3.9 hours. Food has no effect on the bioavailability of zonisamide.
Toxicity (Overdose): Symptoms of overdose include diminished breathing, loss of consciousness, low blood pressure, and slow heartbeat.
Protein Binding: 40% (at concentrations of 1.0-7.0 µg/mL)
Biotransformation: Primarily hepatic through cytochrome P450 isoenzyme 3A4 (CYP3A4). Undergoes acetylation and reduction, forming N-acetyl zonisamide, and the open-ring metabolite 2–sulfamoylacetyl phenol, respectively.
Half Life: 63 hours
Dosage Forms of Excegran: Capsule Oral
Chemical IUPAC Name: 1,2-benzoxazol-3-ylmethanesulfonamide
Chemical Formula: C8H8N2O3S
Zonisamide on Wikipedia: https://en.wikipedia.org/wiki/Zonisamide
Organisms Affected: Humans and other mammals
