Information about Zonisamide
Zonisamide is a sulfonamide anticonvulsant approved for use as an adjunctive therapy in adults with partial-onset seizures. It was discovered by researchers at Dainippon Sumitomo Pharma (大日本住友製薬 Dainippon Sumitomo Seiyaku) (formerly Dainippon Pharmaceutical (大日本製薬 Dainippon Seiyaku)), who launched it in 1989 as Excegran in Japan.[1] It was marketed by Élan in the United States starting in 2000 as Zonegran, before Élan transferred their interests in zonisamide to Eisai (エーザイ) in 2004.[2] Eisai also markets Zonegran in Asia (China, Taiwan, and fourteen others)[3] and Europe (starting in Germany and the United Kingdom).[4]
Additionally, the metabolism of zonisamide is inhibited by ketoconazole, ciclosporin, miconazole, fluconazole and carbamazepine in descending order.[24]
Uses
Epilepsy
Zonisamide is approved in the United States,[5] United Kingdom,[6] for adjunctive treatment of partial seizures in adults and in Japan for both adjunctive and monotherapy for partial seizures (simple, complex, secondarily generalized), generalized (tonic, tonic-clonic (grand mal), and atypical absence) and combined seizures.[7]Parkinson's
An open trial on zonisamide in seven Parkinson's disease patients had positive results, according to this 2001 report.[8] Since then, it has been reported to treat the resting tremor that other therapies may leave behind.[9] By early November of 2005, Dainippon Sumitomo had filed a NDA for the use of zonisamide in Parkinson's disease; it is to be marketed as Tremode.[10]Obesity
It has also been studied for obesity[11] with significant positive effects on body weight and there are three ongoing clinical trials for this indication.[12][13][14]Migraines
Zonisamide has been studied for and used as a migraine preventative medication, and has also been shown to be effective in some cases of neuropathic pain. It has also been used by psychiatrists as a mood stabilizer.[15][16]Metabolism
Zonisamide is metabolized mostly by the CYP3A4 isoenzyme, but also CYP3A7 and CYP3A5,[17] to 2-(sulphamoylacetyl)-phenol via reductive cleavage of the 1,2-benzisoxazole ring.[18]Mechanism of action
The exact mechanism of action is not known for zonisamide. According to Leppik, while zonisamide may be a carbonic anhydrase inhibitor like acetazolamide, this is not one of the primary mechanisms of action, which might be blocking repetitive firing of voltage-gated sodium channels and reduction of T-type calcium channel currents,[19] or by binding allosterically to GABA receptors like the benzodiazepines and muscimol,[20],[21] or increasing the levels of the glutamate transport protein in the brain while decreasing the amount of GABA transport protein, in other words, inhibiting the uptake of the inhibitory neurotransmitter GABA while enhancing the uptake of the excitatory neurotransmitter glutamate.[22]Side effects
The most common side effects include drowsiness, loss of appetite, dizziness, headache, nausea, and agitation/irritability.Interactions
Zonisamide and other carbonic anhydrase inhibitors such as topiramate, furosemide, and hydrochlorothiazide have been known to interfere with amobarbital, which has led to inadequate anesthetization during the Wada test.[23]Additionally, the metabolism of zonisamide is inhibited by ketoconazole, ciclosporin, miconazole, fluconazole and carbamazepine in descending order.[24]
References and end notes
1. ^ Dainippon Sumitomo Pharma Co., Ltd. (2005). Company History. Company Information. Dainippon Sumitomo Co., Ltd.. Retrieved on 12 November, 2005.
2. ^ Dainippon Pharmaceutical Co., Ltd. (2004). Transfer of Rights Agreement for North America and Europe Reached on Zonegran. News Releases for Dainippon Pharmaceutical in 2004. Dainippon Sumitomo Pharma Co., Ltd. Retrieved on 12 November, 2005.
3. ^ Dainippon Pharmaceutical Co., Ltd. (2005). Dainippon Pharmaceutical and Eisai Conclude Agreement for the Development, Manufacture and Marketing of the Anti-Epileptic Agent Zonisamide in Asia. Dainippon Pharmaceutical News Releases for 2005. Dainippon Sumitomo Pharma Co., Ltd.. Retrieved on 12 November, 2005.
4. ^ Eisai Co., Ltd. (2005). Eisai Announces Launch of Zonegran (zonisamide), Treatment For Epilepsy In the UK and Germany. Eisai 2005 News Releases. Eisai Co., Ltd.. Retrieved on 12 November, 2005.
5. ^ Élan Pharmaceuticals Inc (2003). NDA 20-789/S-001; Zonegran (zonisamide) Capsules 25, 50, 100 mg FDA Approvable Labeling Text - August 22] 2003] (PDF). Zonisamide Approval History. Food and Drug Administration. Retrieved on 2005-11-13.
6. ^ Eisai Ltd. (2005). Zonegran Summary of Product Characteristics. electronic Medicines Compendium. Medicines.org.uk. Retrieved on 2005-11-13.
7. ^ Dainippon Pharmaceutical Co., Ltd. (2004). EXCEGRAN Tablets 100 mg & EXCEGRAN Powder 20% (English). Retrieved on 2006-03-13.
8. ^ Murata, Miho; Horiuchi Emiko and Kanazawa Ichiro (December 2001). "Zonisamide has beneficial effects on Parkinson's disease patients". Neuroscience Research 41 (4): 397–9. PubMed.
9. ^ Nakanishi, I; Kohmoto J, Miwa H, Kondo T (August 2003). "[Effect of zonisamide on resting tremor resistant to antiparkinsonian medication]". No To Shinkei 55 (8): 685–9. PubMed.
10. ^ Dainippon Sumitomo Pharma Co., Ltd. (2005). New Drugs in the R&D Pipeline (under development by DSP) (PDF). List of Product Development Project. Retrieved on 2005-11-21.
11. ^ Gadde, Kishore M.; Deborah M. Franciscy, H. Ryan Wagner, II; K. Ranga R. Krishnan (April 2003). "Zonisamide for Weight Loss in Obese Adults: A Randomized Controlled Trial". Journal of the American Medical Association 289 (14): 1820–1825. PubMed.
12. ^ University of Cincinnati (2005). Zonegran in the Treatment of Binge Eating Disorder Associated With Obesity. ClinicalTrials.gov. Retrieved on 2006-05-04.
13. ^ Tuscaloosa Research & Education Advancement Corporation (2005). Zonegran for the Treatment of Weight Gain Associated With Psychotropic Medication Use: A Placebo-Controlled Trial. ClinicalTrials.gov. Retrieved on 2006-05-04.
14. ^ National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) (2006). Zonisamide for Weight Reduction in Obese Adults. ClinicalTrials.gov. Retrieved on 2006-05-04.
15. ^ Dr. Brian D. Loftus (2004). Zonegran. Retrieved on 2006-11-29.
16. ^ Hasegawa, Hisanori (May 2004). "Utilization of zonisamide in patients with chronic pain or epilepsy refractory to other treatments: a retrospective, open label, uncontrolled study in a VA hospital". Curr Med Research Opinion 20 (5): 577–580. PubMed.
17. ^ Ohmori, S.; Nakasa H, Asanome K, Kurose Y, Ishii I, Hosokawa M, Kitada M (1998 May 8). "Differential catalytic properties in metabolism of endogenous and exogenous substrates among CYP3A enzymes expressed in COS-7 cells". Biochimica et Biophysica Acta 1380 (3): 297-304. PubMed.
18. ^ Stiff, D. D.; Robicheau JT, Zemaitis MA. (January 1992). "Reductive metabolism of the anticonvulsant agent zonisamide, a 1,2-benzisoxazole derivative". Xenobiotica 22 (1): 1-11. PubMed.
19. ^ Leppik, Ilo E. (December 2004). "Zonisamide: chemistry, mechanism of action, and pharmacokinetics". Seizure 13 (Suppl 1): S5-9; discussion S10. DOI:10.1016/j.seizure.2004.04.016. PubMed.
20. ^ Mimaki, T.; Suzuki Y, Tagawa T, Karasawa T, Yabuuchi H (March 1990). "Interaction of zonisamide with benzodiazepine and GABA receptors in rat brain". Medical Journal of Osaka University 39 (1-4): 13-7. PubMed.
21. ^ Mimaki, T.; Suzuki Y, Tagawa T, Karasawa T, Yabuuchi H (1990 March). "[3H]zonisamide binding in rat brain". Medical Journal of Osaka University 39 (1-4): 19-22. PubMed.
22. ^ Ueda, Yuto; Doi Taku, Tokumaru Jun, and L. James Willmore (2003 August 19). "Effect of zonisamide on molecular regulation of glutamate and GABA transporter proteins during epileptogenesis in rats with hippocampal seizures". Molecular Brain Research 116 (1-2): 1-6. DOI:10.1016/S0169-328X(03)00183-9. PubMed.
23. ^ Bookheimer, Susan; Schrader, Lara M.; Rausch, Rebecca; Sankar, Raman; Engel, Jerome Jr. (February 2005). "Reduced anesthetization during the intracarotid amobarbital (Wada) test in patients taking carbonic anhydrase-inhibiting medications". Epilepsia 46 (2): 236. DOI:10.1111/j.0013-9580.2005.23904.x.
24. ^ Nakasa, H.; Nakamura H, Ono S, Tsutsui M, Kiuchi M, Ohmori S, Kitada M. (April 1998). "Prediction of drug-drug interactions of zonisamide metabolism in humans from in vitro data". European Journal of Clinical Pharmacology 54 (2): 177–83. PubMed.
2. ^ Dainippon Pharmaceutical Co., Ltd. (2004). Transfer of Rights Agreement for North America and Europe Reached on Zonegran. News Releases for Dainippon Pharmaceutical in 2004. Dainippon Sumitomo Pharma Co., Ltd. Retrieved on 12 November, 2005.
3. ^ Dainippon Pharmaceutical Co., Ltd. (2005). Dainippon Pharmaceutical and Eisai Conclude Agreement for the Development, Manufacture and Marketing of the Anti-Epileptic Agent Zonisamide in Asia. Dainippon Pharmaceutical News Releases for 2005. Dainippon Sumitomo Pharma Co., Ltd.. Retrieved on 12 November, 2005.
4. ^ Eisai Co., Ltd. (2005). Eisai Announces Launch of Zonegran (zonisamide), Treatment For Epilepsy In the UK and Germany. Eisai 2005 News Releases. Eisai Co., Ltd.. Retrieved on 12 November, 2005.
5. ^ Élan Pharmaceuticals Inc (2003). NDA 20-789/S-001; Zonegran (zonisamide) Capsules 25, 50, 100 mg FDA Approvable Labeling Text - August 22] 2003] (PDF). Zonisamide Approval History. Food and Drug Administration. Retrieved on 2005-11-13.
6. ^ Eisai Ltd. (2005). Zonegran Summary of Product Characteristics. electronic Medicines Compendium. Medicines.org.uk. Retrieved on 2005-11-13.
7. ^ Dainippon Pharmaceutical Co., Ltd. (2004). EXCEGRAN Tablets 100 mg & EXCEGRAN Powder 20% (English). Retrieved on 2006-03-13.
8. ^ Murata, Miho; Horiuchi Emiko and Kanazawa Ichiro (December 2001). "Zonisamide has beneficial effects on Parkinson's disease patients". Neuroscience Research 41 (4): 397–9. PubMed.
9. ^ Nakanishi, I; Kohmoto J, Miwa H, Kondo T (August 2003). "[Effect of zonisamide on resting tremor resistant to antiparkinsonian medication]". No To Shinkei 55 (8): 685–9. PubMed.
10. ^ Dainippon Sumitomo Pharma Co., Ltd. (2005). New Drugs in the R&D Pipeline (under development by DSP) (PDF). List of Product Development Project. Retrieved on 2005-11-21.
11. ^ Gadde, Kishore M.; Deborah M. Franciscy, H. Ryan Wagner, II; K. Ranga R. Krishnan (April 2003). "Zonisamide for Weight Loss in Obese Adults: A Randomized Controlled Trial". Journal of the American Medical Association 289 (14): 1820–1825. PubMed.
12. ^ University of Cincinnati (2005). Zonegran in the Treatment of Binge Eating Disorder Associated With Obesity. ClinicalTrials.gov. Retrieved on 2006-05-04.
13. ^ Tuscaloosa Research & Education Advancement Corporation (2005). Zonegran for the Treatment of Weight Gain Associated With Psychotropic Medication Use: A Placebo-Controlled Trial. ClinicalTrials.gov. Retrieved on 2006-05-04.
14. ^ National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) (2006). Zonisamide for Weight Reduction in Obese Adults. ClinicalTrials.gov. Retrieved on 2006-05-04.
15. ^ Dr. Brian D. Loftus (2004). Zonegran. Retrieved on 2006-11-29.
16. ^ Hasegawa, Hisanori (May 2004). "Utilization of zonisamide in patients with chronic pain or epilepsy refractory to other treatments: a retrospective, open label, uncontrolled study in a VA hospital". Curr Med Research Opinion 20 (5): 577–580. PubMed.
17. ^ Ohmori, S.; Nakasa H, Asanome K, Kurose Y, Ishii I, Hosokawa M, Kitada M (1998 May 8). "Differential catalytic properties in metabolism of endogenous and exogenous substrates among CYP3A enzymes expressed in COS-7 cells". Biochimica et Biophysica Acta 1380 (3): 297-304. PubMed.
18. ^ Stiff, D. D.; Robicheau JT, Zemaitis MA. (January 1992). "Reductive metabolism of the anticonvulsant agent zonisamide, a 1,2-benzisoxazole derivative". Xenobiotica 22 (1): 1-11. PubMed.
19. ^ Leppik, Ilo E. (December 2004). "Zonisamide: chemistry, mechanism of action, and pharmacokinetics". Seizure 13 (Suppl 1): S5-9; discussion S10. DOI:10.1016/j.seizure.2004.04.016. PubMed.
20. ^ Mimaki, T.; Suzuki Y, Tagawa T, Karasawa T, Yabuuchi H (March 1990). "Interaction of zonisamide with benzodiazepine and GABA receptors in rat brain". Medical Journal of Osaka University 39 (1-4): 13-7. PubMed.
21. ^ Mimaki, T.; Suzuki Y, Tagawa T, Karasawa T, Yabuuchi H (1990 March). "[3H]zonisamide binding in rat brain". Medical Journal of Osaka University 39 (1-4): 19-22. PubMed.
22. ^ Ueda, Yuto; Doi Taku, Tokumaru Jun, and L. James Willmore (2003 August 19). "Effect of zonisamide on molecular regulation of glutamate and GABA transporter proteins during epileptogenesis in rats with hippocampal seizures". Molecular Brain Research 116 (1-2): 1-6. DOI:10.1016/S0169-328X(03)00183-9. PubMed.
23. ^ Bookheimer, Susan; Schrader, Lara M.; Rausch, Rebecca; Sankar, Raman; Engel, Jerome Jr. (February 2005). "Reduced anesthetization during the intracarotid amobarbital (Wada) test in patients taking carbonic anhydrase-inhibiting medications". Epilepsia 46 (2): 236. DOI:10.1111/j.0013-9580.2005.23904.x.
24. ^ Nakasa, H.; Nakamura H, Ono S, Tsutsui M, Kiuchi M, Ohmori S, Kitada M. (April 1998). "Prediction of drug-drug interactions of zonisamide metabolism in humans from in vitro data". European Journal of Clinical Pharmacology 54 (2): 177–83. PubMed.
External links
- Official Zonegran Website
- Dainippon Sumitomo Prescribing Information for Excegran (Japanese version)
- Official Dainippon Sumitomo Pharma Website (English version)
Sulfonamide may refer to:
..... Click the link for more information.
- Sulfonamide (chemistry) - the sulfonamide functional group (organic chemistry)
- Sulfonamide (medicine) - the group of sulfonamide antibacterial drugs
..... Click the link for more information.
The anticonvulsants, sometimes also called antiepileptics, belong to a diverse group of pharmaceuticals used in prevention of the occurrence of epileptic seizures. More and more, anticonvulsants are also finding ways into the treatment of bipolar disorder, since many seem to
..... Click the link for more information.
..... Click the link for more information.
seizure is a temporary abnormal electro-physiologic phenomenon of the brain, resulting in abnormal synchronization of electrical neuronal activity. It can manifest as an alteration in mental state, tonic or clonic movements, convulsions, and various other psychic symptoms (such as
..... Click the link for more information.
..... Click the link for more information.
Élan Corporation plc
Public
Founded Athlone, County Westmeath, Ireland (1969)
Headquarters Dublin 2, Dublin, Ireland
Key people Kelly Martin, President & CEO
Paul Breen, Global Services & Operations
Richard T.
..... Click the link for more information.
Public
Founded Athlone, County Westmeath, Ireland (1969)
Headquarters Dublin 2, Dublin, Ireland
Key people Kelly Martin, President & CEO
Paul Breen, Global Services & Operations
Richard T.
..... Click the link for more information.
Editing of this page by unregistered or newly registered users is currently disabled due to vandalism.
If you are prevented from editing this page, and you wish to make a change, please discuss changes on the talk page, request unprotection, log in, or .
..... Click the link for more information.
If you are prevented from editing this page, and you wish to make a change, please discuss changes on the talk page, request unprotection, log in, or .
..... Click the link for more information.
MeSH D014202
Tremor is an unintentional, somewhat rhythmic, muscle movement involving to-and-fro movements (oscillations) of one or more parts of the body.
..... Click the link for more information.
- ''For the film see Tremors (film). For other uses, see Tremor (disambiguation).
Tremor is an unintentional, somewhat rhythmic, muscle movement involving to-and-fro movements (oscillations) of one or more parts of the body.
..... Click the link for more information.
The New Drug Application (NDA) is the vehicle in the United States through which drug sponsors formally propose that the FDA approve a new pharmaceutical for sale and marketing.
..... Click the link for more information.
..... Click the link for more information.
Obesity
Classification & external resources
Silhouettes representing healthy, overweight, and obese.
ICD-10 E 66.
ICD-9 278
DiseasesDB 9099
MedlinePlus 003101
eMedicine med/1653
MeSH C23.888.144.699.
..... Click the link for more information.
Classification & external resources
Silhouettes representing healthy, overweight, and obese.
ICD-10 E 66.
ICD-9 278
DiseasesDB 9099
MedlinePlus 003101
eMedicine med/1653
MeSH C23.888.144.699.
..... Click the link for more information.
Migraine
Classification & external resources
ICD-10 G 43.
ICD-9 346
OMIM 157300
DiseasesDB 8207
MedlinePlus 000709
eMedicine neuro/218
MeSH D008881
Migraine
..... Click the link for more information.
Classification & external resources
ICD-10 G 43.
ICD-9 346
OMIM 157300
DiseasesDB 8207
MedlinePlus 000709
eMedicine neuro/218
MeSH D008881
Migraine
..... Click the link for more information.
Neuropathy
Classification & external resources
ICD-10 G 56. - G 63. ,
G 90.0 , G 99.0
ICD-9 337.0 - 337.1 ,
356 - 357 , 377
eMedicine topic list Neuropathy is usually short for peripheral neuropathy
..... Click the link for more information.
Classification & external resources
ICD-10 G 56. - G 63. ,
G 90.0 , G 99.0
ICD-9 337.0 - 337.1 ,
356 - 357 , 377
eMedicine topic list Neuropathy is usually short for peripheral neuropathy
..... Click the link for more information.
Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14.13.97 ), a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body.
..... Click the link for more information.
..... Click the link for more information.
Isozymes (also known as isoenzymes) are enzymes that differ in amino acid sequence but catalyze the same chemical reaction. These enzymes usually display different kinetic parameters (i.e. different KM values), or different regulatory properties.
..... Click the link for more information.
..... Click the link for more information.
CYP3A7 is a member of the cytochrome P450 family. It serves in fetuses a role similar to the role CYP3A4 serves in adults.
..... Click the link for more information.
External links
- MeSH CYP3A7+protein,+human
..... Click the link for more information.
Benzisoxazole is an aromatic organic compound with a molecular formula C7H5NO containing a benzene-fused isoxazole ring structure. Benzisoxazole has no household use. It is used primarily in industry and research.
..... Click the link for more information.
..... Click the link for more information.
Carbonic anhydrase (carbonate dehydratase) is a family of metalloenzymes (enzymes that contain one or more metal atoms as a functional component of the enzyme) that catalyze the rapid conversion of carbon dioxide to bicarbonate and protons, a reaction that occurs rather
..... Click the link for more information.
..... Click the link for more information.
Acetazolamide, sold under the trade name Diamox, is a carbonic anhydrase inhibitor that is used to treat glaucoma, epileptic seizures, benign intracranial hypertension, altitude sickness, cystinuria, and dural ectasia.
..... Click the link for more information.
..... Click the link for more information.
Sodium channels (also known as "voltage-gated sodium channels") are integral membrane proteins that conduct sodium ions (Na+) through a cell's plasma membrane. Many of the ionotropic receptors are also able to conduct sodium ions.
..... Click the link for more information.
..... Click the link for more information.
This article or section may be confusing or unclear for some readers.
Please [improve the article] or discuss this issue on the talk page. This article has been tagged since December 2006.
..... Click the link for more information.
Please [improve the article] or discuss this issue on the talk page. This article has been tagged since December 2006.
..... Click the link for more information.
In biochemistry, allosteric regulation is the regulation of an enzyme or protein by binding an effector molecule at the protein's allosteric site (that is, a site other than the protein's active site).
..... Click the link for more information.
..... Click the link for more information.
The GABA receptors are a class of receptors that respond to the neurotransmitter γ-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system.
..... Click the link for more information.
..... Click the link for more information.
The benzodiazepines (pronounced [ˌbɛnzəʊdaɪˈæzəpiːnz], or "benzos" for short) are a class of psychoactive drugs considered minor tranquilizers with varying hypnotic, sedative, anxiolytic,
..... Click the link for more information.
..... Click the link for more information.
Muscimol (Agarin, Pantherine) is the major psychoactive alkaloid present in many mushrooms of the Amanita genus. Unlike psilocybin, a tryptamine, muscimol is a potent, selective agonist of the GABAA receptor.
..... Click the link for more information.
..... Click the link for more information.
Glutamic acid or glutamate (abbreviated as Glu or E; Glx or Z represents either glutamic acid or glutamine), is the protonated form of glutamate (the anion). Glutamate is one of the 20 proteinogenic amino acids.
..... Click the link for more information.
..... Click the link for more information.
Transport protein can refer to:
..... Click the link for more information.
- Membrane transport protein
- Vesicular transport protein
- Water-soluble carriers of small molecules
..... Click the link for more information.
In animals, the brain or encephalon (Greek for "in the skull"), is the control center of the central nervous system, responsible for behavior. The brain is located in the head, protected by the skull and close to the primary sensory apparatus of vision, hearing,
..... Click the link for more information.
..... Click the link for more information.
Carbonic anhydrase (carbonate dehydratase) is a family of metalloenzymes (enzymes that contain one or more metal atoms as a functional component of the enzyme) that catalyze the rapid conversion of carbon dioxide to bicarbonate and protons, a reaction that occurs rather
..... Click the link for more information.
..... Click the link for more information.
Topiramate (brand name Topamax) is an anticonvulsant drug produced by Ortho-McNeil Neurologics, a division of Johnson & Johnson. It is used to treat epilepsy in both children and adults.
..... Click the link for more information.
..... Click the link for more information.
Furosemide (INN) or frusemide (former BAN) is a loop diuretic used in the treatment of congestive heart failure and edema. It is most commonly marketed by Sanofi-Aventis under the brand name Lasix.
..... Click the link for more information.
..... Click the link for more information.
Hydrochlorothiazide, sometimes abbreviated HCT, HCTZ, or HZT is a popular diuretic drug that acts by inhibiting the kidneys' ability to retain water. This reduces the volume of the blood, decreasing blood return to the heart and thus cardiac output and, by
..... Click the link for more information.
..... Click the link for more information.
Amobarbital (formerly known as amylobarbitone) is a drug that is a barbiturate derivative. It has sedative-hypnotic and analgesic properties. It is a white crystalline powder with no odor and a slightly bitter taste.
..... Click the link for more information.
..... Click the link for more information.
This article is copied from an article on Wikipedia.org - the free encyclopedia created and edited by online user community. The text was not checked or edited by anyone on our staff. Although the vast majority of the wikipedia encyclopedia articles provide accurate and timely information please do not assume the accuracy of any particular article. This article is distributed under the terms of GNU Free Documentation License.
Herod_Archelaus
