Flupirtine maleate information from DrugsUpdate
Flupirtine, a non-opioid analgesic, is indicated for the management of moderate to severe forms of acute and chronic pain including migraine, dysmenorrhoea, post-traumatic pain, post-surgical pain and injuries. Flupirtine possess moderate muscle relaxant property.
Pharmacodynamics
Flupirtine is a centrally-acting and non-opioid analgesic. The drug activates G-protein-coupled receptors that stimulate K+ channels of neuronal cells. The drug acts as an indirect N-methyl-D-Aspartate (NMDA) antagonist. Flupirtine inhibits neuronal excitability and reduce calcium Ca2+ influx into the cells. The mechanism is vital for neuronal transmission of pain signals to motor neurons.
Pharmacokinetics
After oral absorption, Flupirtine is well absorbed in the GIT. The apparent Vss of Flupirtine is about 150 L. The Cmax is about 1.5-2 hours after oral administration. Flupirtine is metabolized by the liver. The drug is excreted by biliary route as drug metabolites. The terminal half-life is about 7 hours.
Flupirtine maleate Indications / Flupirtine maleate Uses
No information available
Flupirtine maleate Adverse Reactions / Flupirtine maleate Side Effects
The adverse events of Flupirtine are dose-dependent. Some of the commonly reported adverse events are vomiting, flatulence, rashes, constipation, anorexia, dizziness, abdominal pain, allergic reactions, confusion, GI disorders, sleep disturbances, dry mouth, tremors and headache. Some of the rare and serious adverse events of Flupirtine are iatrogenic hepatitis with elevated levels of serum transaminases and other parameters of liver function tests.
Precautions
Flupirtine is contraindicated in patients with hepatic encephalopathy, cholestasis, myasthenia gravis and ataxia.
Special Precautions
No information available
Other Drug Interactions
Flupirtine may interact with other drugs including sedatives, hypnotics, anticoagulants and benzodiazepines.
Other Interactions
Do not consume alcohol while taking Flupirtine. It can increase the adverse events of Flupirtine.
Dosage
For pain (Adults):
Start with an initial oral dose of 200 mg/day. The dosage can be titrated to 100 mg, thrice daily, depending on pain intensity.
For pain (Pediatrics):
For children over six years, consider oral administration of 50 mg, thrice or four times a day.
For renal-impaired patients:
The dosage should be reduced by 50% of the recommended adult dosage.
Food(before/after)
Can be taken before or after meals intake
List of Contraindications
Flupirtine maleate and Pregnancy
Flupirtine has not been classified under USFDA pregnancy category. However, caution should be exercised before taking Flupirtine during pregnancy.
Flupirtine maleate and Lactation
Nursing mothers should consult a physician before taking Flupirtine.
Flupirtine maleate and Children
No information available
Flupirtine maleate and Geriatic
No information available
Flupirtine maleate and Other Contraindications
No information available
Storage
Store in a cool and dry place protected from light and moisture
Lab interference
Store in a cool and dry place protected from light and moisture
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