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Levetiracetam is used to treat epilepsy-related seizures. Epilepsy is a chronic illness in which sufferers experience recurrent fits. It is used to describe an epileptic condition in which fits affect only one side of the brain but can spread to wider areas on both sides. It works by slowing the aberrant brain messages that trigger seizures. It works by suppressing specific brain areas responsible for aberrant activity and preventing the spread of electrical signals that cause seizures. It lowers seizures but does not cure epilepsy. It was initially approved for usage in the United States in 1999 and has no structural or mechanistic similarities to other anti-epileptic medications.

BRAND NAMES:

Keppra - It contains the active ingredients of levetiracetam. It is available in tablets and oral solutions used to treat seizures.

Roweepra– It contains the active ingredients of levetiracetam. It is available as extended-release tablets used to treat adjunctive therapy.

Elepsia – It contains the active ingredients of levetiracetam. It is available in the form of extended-release tablets used to treat partial-onset seizures.

Spritam – It contains the active ingredients of levetiracetam. It is available in the form of oral disintegration tablets used to treat seizures.

Matever – It contains the active ingredients of levetiracetam.  It is available in the form of tablets used to treat epilepsy.

MECHANISM OF ACTION:

The mechanisms by which levetiracetam exerts its anti-epileptic effects are not clearly defined. The most relevant mechanism, of action is to be binding to a unique synaptic vesicle protein 2A. SV2A protein is a part of the secretory vesicle membrane that mediates calcium-dependent vesicular neurotransmitter release. Levetiracetam binding to SV2A appears to decrease the rate of vesicular release.

PHARMACOKINETICS:

Absorption: Levetiracetam is rapidly and virtually entirely absorbed after oral administration, with a reported absolute oral bioavailability of almost 100%. Co-administration of levetiracetam with food delays Tmax by around 1.5 hours and reduces Cmax by 20%.

Distribution: Levetiracetam has a distribution volume of about 0.5 to 0.7L/kg.

Metabolism: The key metabolic process is the acetamide group's enzymatic hydrolysis. Metabolites have no pharmacological effect and are eliminated by the kidneys. The hepatic cytochrome P450 system plays just a minor role.

Excretion: Approximately 66% of the administered dose of levetiracetam is eliminated as unaltered medication in the urine, with only 0.3% excreted in the feces.

PHARMACODYNAMICS:

Levetiracetam has a wide therapeutic index, making it unique among anti-epileptic drugs. It appears to prevent seizure activity by selectively inhibiting hyper-synchronized epileptiform burst firing without altering normal neuronal transmission, though the precise mechanism by which this occurs is unknown. Patients using levetiracetam should be monitored for the onset or worsening of depressive symptoms, suicidal ideation, and behavioral abnormalities.

DOSAGE AND ADMINISTRATION:

These are available in the form of tablets, solutions, and injections

  • Immediate release of tablets having the strengths of 250mg, 500 mg, 750 mg, and 1000mg.

  • 3-D tablet immediate release has the strengths of 250mg, 500mg, 750mg, and 1000mg.

  • Extended-release tablets have the strengths of 500mg, 750mg, 1000mg, and 1500mg.

  • Oral solution having the strength of 100mg/ml.

  • Injectable solutions with the strengths of 5mg/ml, 10mg/ml, 15mg/ml, and 100mg/ml.

Levitiracetam is available in several forms, including a solution, an immediate-release tablet, an extended-release tablet, and an oral suspension tablet. The solution is immediate-release tablets and tablets for suspension are typically taken twice daily. Once in the morning and again at night, with or without food. The extended-release tablets are typically taken once a day, with or without food. The extended-release tablets are typically taken once a day, with or without food. Try to take levetiracetam at roughly the same time each day.

DRUG INTERACTIONS:

Drug interactions with levetiracetam may include 

  • Anti-epileptic medicines- carbamazepine, phenytoin and phenobarbital

  • Anti-HIV drugs- ritonavir

  • Acidity medicine – cimetidine

  • Chronic alcoholism – disulfiram

  • Anti-tuberculosis drug – rifampin

  • Anti-Parkinson drug – levodopa

  • Asthma drug - theophylline

CONTRAINDICATIONS:

Levetiracetam is contraindicated to a hypersensitivity reaction to the drug or any excipients contraindicated to levetiracetam. Levitiracetam should be stopped permanently if the clinician can not establish an alternative etiology for the hypersensitivity reaction.

SIDE EFFECTS:

Levetiracetam may cause side effects

  • Weakness

  • Unsteady walking

  • Dizziness

  • Confusion

  • Irritability

  • Aggression

  • Headache 

  • Loss of appetite

  • Vomiting

  • Diarrhea

  • Constipation

  • Joint pain

  • Neck pain

  • Double vision

  • Nasal congestion

Some side effects can be serious

  • Rash, fever, swollen lymph nodes

  • Seizures

  • Fever

  • Blisters on skin

  • Itching

  • Swelling  of the face

  • Loss of balance or coordination

  • Hives

OVERDOSE:

Symptoms of overdose may include 

  • Drowsiness

  • Agitation

  • Aggression

  • Decreased consciousness

  • Difficulty breathing

TOXICITY:

General supportive measures, airway protection, and monitoring of vital signs are done on overdose patients. Hemodialysis may be needed in patients with significant renal impairment. A four-hour hemodialysis session can remove almost 50% of the drug.

STORAGE:

Keep out of children's reach. Maintain at an ambient temperature between 15° and 30°C (59° to 86°F).

Image
Levetiracetam
Levetiracetam EP Impurity A

Levetiracetam EP Impurity A

CAS Number
67118-31-4
Levetiracetam USP Related Compound B

Levetiracetam USP Related Compound B

CAS Number
7682-20-4