Safertine

Safertine Uses, Dosage, Side Effects, Food Interaction and all others data.

Safertine is a pyridine derivative that is in clinical use as a nonopioid analgesic. It was approved for the treatment of pain in 1984 in Europe. It is not approved for use in the U.S. or Canada, but is currently in phase II trials for the treatment of fibromyalgia.

Table Of contents

• Safertine
• Uses
• Dosage
• Side Effect
• Precautions
• Interactions
• Uses during Pregnancy
• Uses during Breastfeeding
• Accute Overdose
• Food Interaction
• Half Life
• Volume of Distribution
• Clearance
• Interaction With other Medicine
• Contradiction
• Storage

Trade Name	Safertine
Generic	Flupirtine
Flupirtine Other Names	Flupirtine, Flupirtino, Flupirtinum
Weight	100mg
Type	Capsule
Formula	C15H17FN4O2
Weight	Average: 304.3195 Monoisotopic: 304.133554013
Groups	Investigational
Therapeutic Class
Manufacturer	Applied Communication And Controls
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

Investigated for use/treatment in fibromyalgia.

How Safertine works

Safertine upregulates Bcl-2, increases glutathione levels, activates an inwardly rectifying potassium channel, and delays loss of intermitochondrial membrane calcium retention capacity. Safertine acts like a NMDA receptor antagonists, but does not bind to the receptor. One study concluded that the discriminative effects of flupirtine are neither of opioid nor of alpha-1 adrenergic type, but are primarily mediated through alpha-2 adrenergic mechanisms [PMID: 2901483].

Toxicity

Oral, mouse: LD50 = 300 mg/kg; Oral, rabbit: LD50 = 3200 mg/kg; Oral, rat: LD50 = 980 mg/kg.

Elimination Route

Bioavailability: 90% (oral), 70% (rectal)

Half Life

6.5 hrs (average), 11.2-16.8 hrs (average 14 hrs) (elderly), 8.7-10.9 hrs (average 9.8 hrs) (in those with moderate-level renal impairment).

Elimination Route

72% of flupirtine and its metabolites appear in urine and 18% appear in faeces.

Innovators Monograph

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