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Levetiracetam

 
Drug Info:

Levetiracetam

Brand names: Keppra®

Chemical formula:



Levetiracetam Oral solution

What is this medicine?

LEVETIRACETAM (lee ve tye RA se tam) is an antiepileptic drug. It is used with other medicines to treat certain types of seizures.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•kidney disease
•suicidal thoughts, plans, or attempt; a previous suicide attempt by you or a family member
•an unusual or allergic reaction to levetiracetam, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth. Follow the directions on the prescription label. Use a specially marked spoon or container to measure your medicine. Ask your pharmacist if you do not have one. Household spoons are not accurate. You may take this medicine with or without food. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking this medicine except on the advice of your doctor or health care professional. Stopping your medicine suddenly can increase your seizures or their severity.
 
Contact your pediatrician or health care professional regarding the use of this medication in children. While this drug may be prescribed for children as young as 4 years of age for selected conditions, precautions do apply.
 
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

•sevelamer

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for a regular check on your progress. Wear a medical identification bracelet or chain to say you have epilepsy, and carry a card that lists all your medications.
 
It is important to take this medicine exactly as instructed by your health care professional. When first starting treatment, your dose may need to be adjusted. It may take weeks or months before your dose is stable. You should contact your doctor or health care professional if your seizures get worse or if you have any new types of seizures.
 
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.
 
The use of this medicine may increase the chance of suicidal thoughts or actions. Pay special attention to how you are responding while on this medicine. Any worsening of mood, or thoughts of suicide or dying should be reported to your health care professional right away.
 
Women who become pregnant while using this medicine may enroll in the North American Antiepileptic Drug Pregnancy Registry by calling 1-888-233-2334. This registry collects information about the safety of antiepileptic drug use during pregnancy.

What side effects may I notice from receiving this medicine?

Side effects you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•dark urine
•general ill feeling or flu-like symptoms
•problems with balance, talking, walking
•unusually weak or tired
•worsening of mood, thoughts or actions of suicide or dying
•yellowing of the eyes or skin

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•diarrhea
•dizzy, drowsy
•headache
•loss of appetite

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from heat and light. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Oxford A-Z of Medicinal Drugs:

levetiracetam

Top

An antiepileptic drug (see anticonvulsant drugs) that is used alone or as an adjunct to treat partial seizures and as an adjunct to treat tonic-clonic seizures and myoclonic seizures (in which sudden muscle spasms occur between seizures). It is available, on prescription only, as tablets, an oral solution, and a form for intravenous infusion.

Side effects:
include dizziness, sleepiness, liver or kidney disease, headache, nausea, vomiting, and indigestion.

Precautions:
levetiracetam is not recommended for pregnant or breastfeeding women.

Interactions with other drugs:

Antidepressants and antimalarial drugs: there may be an increased risk of convulsions if some of these drugs are taken with levetiracetam.

Proprietary preparation:
Keppra.

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Wikipedia on Answers.com:

Levetiracetam

Top
Levetiracetam
Systematic (IUPAC) name
(S)-2-(2-oxopyrrolidin-1-yl)butanamide
Clinical data
Trade names Keppra
AHFS/Drugs.com monograph
MedlinePlus a699059
Pregnancy cat. C(US)
Legal status Prescription only
Routes Oral, intravenous
Pharmacokinetic data
Bioavailability ~100%
Protein binding <10%
Metabolism Enzymatic hydrolysis of acetamide group
Half-life 6 - 8 hr
Excretion Urinary
Identifiers
CAS number 102767-28-2 YesY
ATC code N03AX14
PubChem CID 5284583
DrugBank DB01202
ChemSpider 4447633 YesY
UNII 44YRR34555 YesY
KEGG D00709 YesY
ChEMBL CHEMBL1286 YesY
Chemical data
Formula C8H14N2O2 
Mol. mass 170.209 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

Levetiracetam (INN) (play /lɛvɨtɪˈræsɨtæm/) is an anticonvulsant medication used to treat epilepsy.[1] It is the S-enantiomer of etiracetam, structurally similar to the prototypical nootropic drug piracetam.

Levetiracetam is marketed under the trade name Keppra. Keppra is manufactured by UCB Pharmaceuticals Inc. Since November of 2008 the drug has been available as a generic brand in the United States.

Contents

Medical uses

Levetiracetam has been approved in the European Union as a monotherapy treatment for epilepsy in the case of partial seizures, or as an adjunctive therapy for partial, myoclonic and tonic-clonic seizures.[2] It is also used in veterinary medicine for similar purposes.

Levetiracetam has potential benefits for other psychiatric and neurologic conditions such as Tourette syndrome, autism, bipolar disorder and anxiety disorder, but its most serious adverse effects are behavioral and its benefit-risk ratio in these conditions is not well understood.[3]

Along with other anticonvulsants like gabapentin, it is also sometimes used to treat neuropathic pain. It has not been found to be useful for essential tremors.[4]

Adverse effects

Levetiracetam is, in general, well tolerated[5] but may cause drowsiness, weakness, unsteady gait, coordination problems, headache, pain, forgetfulness, anxiety, irritability or agitation, dizziness, mood changes, nervousness, loss of appetite, vomiting, diarrhea, constipation, and changes in skin pigmentation (color).

Some serious side effects can be depression, hallucinations, suicidal thoughts, seizures that are worse or different, fever, sore throat, and other signs of infection, double vision, itching, rash, swelling of the face. A study published in 2005 suggests that the addition of pyridoxine (vitamin B6) may curtail some of the psychiatric symptoms.[6]

Measurement in bodily fluids

Assay of Levetiracetam[7]

There are only a few papers published reporting therapeutic drug monitoring methods of levetiracetam. Three of them employed HPLC with UV-detection [8], [9] , [10], and two methods were using GC with NPD-detection [11], [12]. Microemulsion electrokinetic chromatography with UV-detection was utilized in one method [13]. Two methods facilitating chiral separation of the S- and Renantiomer of levetiracetam, one utilizing GC–MS and the other HPLC–UV, were published [14], [15]. These methods were designed to investigate in dogs the pharmacokinetic and pharmacodynamic properties of the two enantiomers separately. For routine therapeutic drug monitoring in men, these methods were not appropriate. In all but one of the methods [16], sample preparation with SPE or liquid–liquid extraction is necessary. Pucci et al. [17] evaluated the feasibility of protein precipitation as the only sample preparation step in comparison to SPE. They concluded, that protein precipitation is a suitable and fast sample preparation for measuring routine patient samples.

Various HPLC[18], [19], [20], [21], [22], [23], [24], and LC-MS [25], [26], [27]methods have been reported for the determination of levetiracetam in pure and pharmaceutical dosage forms.

Mechanism of action

The exact mechanism by which levetiracetam acts to treat epilepsy is unknown. However, the drug binds to a synaptic vesicle protein, SV2A,[28] which is believed to impede nerve conduction across synapses.[29]

Available forms

  • ready-to-administer bags of Sodium Chloride Injection, at concentrations of 500 mg/100 mL, 1000 mg/100 mL and 1500 mg/100 mL[30]

See also


References

  1. ^ Abou-Khalil B (June 2008). "Levetiracetam in the treatment of epilepsy". Neuropsychiatr Dis Treat 4 (3): 507–23. PMC 2526377. PMID 18830435. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2526377. 
  2. ^ BNF 59. BMA & RPSGB. 2010. 
  3. ^ Farooq MU, Bhatt A, Majid A, Gupta R, Khasnis A, Kassab MY (2009). "Levetiracetam for managing neurologic and psychiatric disorders". Am J Health Syst Pharm 66 (6): 541–61. doi:10.2146/ajhp070607. PMID 19265183. 
  4. ^ http://www.neurology.org/content/early/2011/10/18/WNL.0b013e318236f0fd.abstract
  5. ^ Gambardella A, Labate A, Colosimo E, Ambrosio R, Quattrone A (February 2008). "Monotherapy for partial epilepsy: focus on levetiracetam". Neuropsychiatr Dis Treat 4 (1): 33–8. PMC 2515905. PMID 18728811. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2515905. 
  6. ^ "Clinical Epilepsy: Pediatrics". Epilepsia 46 (s8): 142–67. 2005. doi:10.1111/j.1528-1167.2005.460801_16.x. http://www3.interscience.wiley.com/journal/118734483/abstract. 
  7. ^ Prafulla Kumar Sahu, M. Mathrusri Annapurna; Analytical Method development by Liquid Chromatography, LAP LAMBERT Academic Publishing GmbH & Co. KG, Germany, ISBN: 978-3-8443-2869-1.
  8. ^ N. Ratnaraj, H.C. Doheny, P.N. Patsalos, Ther. Drug Monit. 18 (1996) 154.
  9. ^ T.A. Vermeij, P.M. Edelbroek, J. Chromatogr. B Biomed. Appl. 662 (1994) 134.
  10. ^ V. Pucci, F. Bugamelli, R. Mandrioli, A. Ferranti, E. Kenndler, M.A. Raggi, Biomed. Chromatogr. 18 (2004) 37.
  11. ^ T.A. Vermeij, P.M. Edelbroek, J. Chromatogr. B Biomed. Appl. 662 (1994) 134.
  12. ^ R. Coupez, R. Straetemans, G. Sehgal, A. Stockis, Z.S. Lu, J. Clin. Pharmacol. 43 (2003) 1370.
  13. ^ M. Ivanova, A. Piunti, E. Marziali, N. Komarova, M.A. Raggi, E. Kenndler, Electrophoresis 24 (2003) 992.
  14. ^ N. Isoherranen, M. Roeder, S. Soback, B. Yagen, V. Schurig, M. Bialer, J. Chromatogr. B Biomed. Sci. Appl. 745 (2000) 325.
  15. ^ N. Isoherranen, B. Yagen, S. Soback, M. Roeder, V. Schurig, M. Bialer, Epilepsia 42 (2001) 825.
  16. ^ V. Pucci, F. Bugamelli, R. Mandrioli, A. Ferranti, E. Kenndler, M.A. Raggi, Biomed. Chromatogr. 18 (2004) 37.
  17. ^ V. Pucci, F. Bugamelli, R. Mandrioli, A. Ferranti, E. Kenndler, M.A. Raggi, Biomed. Chromatogr. 18 (2004) 37.
  18. ^ Prafulla Kumar Sahu*, Dillip Kumar Sahoo, M.M.Annapurna, M.E.Bhanoji Rao, Development and validation of an RP-HPLC method for determination of Levetiracetam in Bulk and Pharmaceutical Dosage Forms, Analytical Chemistry: An Indian Journal, 2009, 8(1).
  19. ^ C. Manuela, M. Susan, A. Fiorenzo, R. Roberto and B. Agostino, J chromatogr B., 2008, 873(1), 129.
  20. ^ N. Appala Raja, J. Venkateswara Rao, K. Vanitha Prakash, K. Mukkanti and K. Srinivasu, E Journal of Chemistry, 2008, 5(S2), 1098.
  21. ^ J. Valarmathy, L. Samueljoshua, G. Rathinavel, C. Selvin Thanija and T. Sivakumar,Research J Pharm and Tech., 2008, 1(3), 395.
  22. ^ J. Marten Lobenhoffer and S.M. Bode Boger, J Chromatogr B., 2005, 815, 197.
  23. ^ N. Ratnaraj, C. Doheny Helen and N. Patsalos Philip, Ther Drug Monit, 1996, 18(2), 154.
  24. ^ A.C. Vermeij and P.M. Edelbroek, J Chromatogr B., 1994, 662,134.
  25. ^ M. Kamal Matar, J Pharm Biomed Anal., 2008, 48(3), 822.
  26. ^ G. Saravanan, G. Jhothy, Y. Suresh, A. Annerao, M. Ramakrishna, M. Yogeshwar Reddy and B. Ravibabu, Chromatographia, 2008, 67, 173.
  27. ^ Tiedong Guo, M. Lisa Oswald, M. Damodara Rao and J. Steven Soldin, Clinica Chimica Acta, 2007, 375, 115.
  28. ^ Lynch BA, Lambeng N, Nocka K, et al. (June 2004). "The synaptic vesicle protein SV2A is the binding site for the antiepileptic drug levetiracetam". Proc Natl Acad Sci USA. 101 (26): 9861–6. doi:10.1073/pnas.0308208101. PMC 470764. PMID 15210974. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=470764. 
  29. ^ Rogawski, MA (June 2006). "Diverse mechanisms of antiepileptic drugs in the development pipeline". Epilepsy Research 69 (3): 273–94. doi:10.1016/j.eplepsyres.2006.02.004. PMC 1562526. PMID 16621450. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1562526. 
  30. ^ "Mylan Inc. (MYL) Launches Innovative Version of Antiepileptic Drug Levetiracetam", ClinicaSpace (Mylan), 20 Jan 2012, http://www.clinicaspace.com/news_story.aspx?NewsEntityId=246929, retrieved 22 Jan 2012 

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Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
 Oxford A-Z of Medicinal Drugs. Market University Press. © 2000, 2003, 2010 An A-Z of Medicinal Drugs. All rights reserved.  Read more
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