What Is Flupirtine?

Flupirtine, flupirtine is an aminopyridine as a centrally acting non-opioid analgesic. It first went on sale in Europe in 1984 and is mainly sold under the names Katatolon, Trancolong, Awegal, Efiret, Trancopal Dolo and Metanor. Like Nefopam, it is unique among analgesics because it is a non-opioid, non-NSAID, non-steroidal central-acting analgesic. The clinical analgesic effect is slightly weaker than methadone, which is caused by hand surgery, trauma, and burns.

Chinese name: Flupirtine
Foreign name: Flupirtine

Drug alias: KATADOLON
Drug type: Capsule

Flupirtine Basic Information

Chinese name: flupirtine

Chinese alias: N- [2-amino-6-[(4-fluorophenyl) methylamino] pyridin-3-yl] urethane; fluoropyridine; 2-amino-6-[(P-fluorobenzyl Propyl) amino] -3-pyridinecarbamate;

English name: Effirma;

English alias: ethylN- [2-amino-6-[(4-fluorophenyl) methylamino] pyridin-3-yl] carbamate; Flupirtine;

CAS number: 56995-20-1

Molecular formula: C15H17FN4O2

Structural formula:

Molecular weight: 304.31900

Exact mass: 304.13400

PSA: 89.27000

LogP: 3.71060

Physical and chemical properties

Density: 1.35g / cm

Melting point: 115-116ºC

Boiling point: 434.9ºC at 760mmHg

Flash point: 216.8ºC

Refractive index: 1.661 ^[1]

Flupirtine

Flupirtine drug fact sheet general information

Indications for flupirtine

It is mainly used for postoperative pain, headache, trauma and burn-induced pain.

Flupirtine dosage

1 oral: 100 mg each time, 3 to 4 times a day, severe cases 200 mg each time, 3 times a day, the maximum dose is 600 mg per day. Pediatric 100mg / time. TID.

2. External use: suppositories, 150 mg each time, 3 to 4 times a day, severe cases 6 times a day, the maximum dose of 900 mg a day for 8 consecutive days. Pediatric 75mg / time, extreme dose 300mg / d.

Flupirtine dosage forms and specifications

1. Capsule: 100mg;

2. Suppository: 150mg.

Flupirtine contraindications

1. Cholestasis is prohibited.

2. Pregnant and lactating women are prohibited.

3. Those who are allergic to flupirtine, renal insufficiency, and hypoalbuminemia are prohibited.

Flupirtine precautions

Use with caution for the elderly and children.

Flupirtine adverse reactions

See fatigue, dizziness, nausea, vomiting, upset stomach, diarrhea, constipation, sweating, dry mouth, visual impairment, elevated AST or ALT.

Flupirtine drug interactions

Combination with anticoagulant drugs can increase the latter's anticoagulant effect.

Pharmacological effects of flupirtine

It has a direct contraction effect on smooth muscle, shrinks the extracranial arteries, restores the excessive expansion and pulsation of cerebral arteries, and reduces headache symptoms. Its role is related to activation of serotoninergic receptors in the vessel wall.

Similar to clonidine, it acts on the norepinephrine down-regulation pain regulator and produces analgesic effects, and is not antagonized by naloxone. The analgesic potency is equal to pentazocine, about 50% of morphine. No respiratory depression, no constipation, urinary retention and other adverse reactions, long-term use does not produce tolerance and dependence. Oral absorption is easy. ^[2-3]

Flupirtine pharmacokinetics

Oral absorption is good, after 20 to 30 minutes after taking effect, the effect lasts 3 to 5 hours, the peak time of plasma drug concentration is 0.5 to 1 hour, plasma t _1/2 is 2 to 11 hours, mainly excreted from urine. ^[4]

Flupirtine Expert Reviews

Flupirtine mainly acts on the central nervous system, without opioid effects such as inhibition of breathing or antitussive. Its analgesic effect lies between methadone and acetaminophen. Oral absorption is rapid, the effect is fast, the effect lasts 3 to 5 hours.