Flupirtine
Mechanism :
Flupirtine is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. 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.
Indication :
- Analgesic for acute and chronic pain
- Muscle relaxant for back pain
Contraindications :
Established hypersensitivity to flupirtine maleate. Flupirtine should not be given to patients at risk of a hepatic encephalopathy nor to patients. Suffering from cholestasis, since an encephalopathy or ataxia may develop or deteriorate. As flupirtine maleate loosens muscle tenseness patients suffering from myasthenia gravis should not be treated with flupirtine. Since flupirtine maleate is mostly metabolized in the liver, patients with a liver disease and alcohol abusers should not be given Flupirtine.
Dosing :
>6 years:
Oral 50 mg, thrice or four times a day.
Adverse Effect :
Gastric & abdominal discomfort, blurred vision, constipation, diarrhea, nausea, dry mouth, thrombocytosis, flu-like symptoms, heartburn, pruritus, vomiting, arrhythmias, anxiety, weakness, disorientation, insomnia, headache, elevated mood, depression, fatigue, hallucinations, impaired concentration, paresthesia, sedation/somnolence, tremors, dizziness/light-headedness.
Interaction :
Anticoagulants: Flupirtine may interact with anticoagulants such as warfarin. A blood test called the PT is needed to monitor this potential interaction.
Alcohol or other Sedatives: Such as benzodiazepines can increase the tiredness and dizziness that you may experience with flupirtine.
Hepatic Dose :
Dose of flupirtine should be reduced to 50% in patients with hepatic impairment.