flupirtine

Action and Spectrum

Actions and Spectrum: 

Actions: 

flupirtine is a non-opioid analgesic drug that functions differently from conventional painkillers due to its distinct mode of action. It is helpful in the treatment of both acute and chronic pain since its primary mechanism of action is its modulation of neuronal excitability. flupirtine’s specific activities include opening the potassium channel, relieving pain, relaxing muscles, having an anti-excitatory effect, and decreasing the use of opioids. 

Spectrum: 

flupirtine’s spectrum of action mainly consists of its usage as a non-opioid analgesic for pain relief, especially when dealing with specific pain problems such as neuropathic pain, chronic pain, musculoskeletal pain, pain sparing, and pain syndromes with limited available treatments. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Sleep disturbance 

Nausea 

Tremors 

Vomiting 

Abdominal pain 

Constipation 

Fatigue 

Dryness in mouth 

Dizziness 

Heartburn 

Depression 

Abdominal discomfort 

Increased sweating 

Nervousness 

Diarrhea 

Flatulence 

Headache 

Restlessness 

Black Box Warning

Black Box Warning: 

It is important to remember that flupirtine carries specific safety concerns and possible hazards, especially in relation to hepatotoxicity (liver damage) and other adverse effects. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Pediatrics 
• History of alcohol abuse 
• Hepatic impairment 

Cautions 

• Thyroid disorders 
• Geriatrics 
• Renal impairment 
• Hepatic impairment 
• Drug interactions 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

Limited data is available regarding the administration of the drug during pregnancy. 

Breastfeeding warnings:  

Limited data is available regarding the excretion of drug in breast milk. 

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

flupirtine is a non-opioid analgesic medication with a unique mechanism of action that sets it apart from traditional pain relievers. Because it primarily acts by modulating neural excitability, it can be used to treat both acute and chronic pain. The unique actions of flupirtine include activating the potassium channel, reducing the need for opioids, alleviating pain, relaxing muscles, and having an anti-excitatory impact. 

Pharmacodynamics: 

Kv7 (KCNQ) potassium channels are a particular type of potassium channel that is preferentially opened by flupirtine. These channels are present in neurons and are essential for controlling the excitability of neurons. flupirtine causes the potassium ions to flow out of the cell by activating these channels, which causes the membrane of the neuron to become hyperpolarized. 

The main pharmacodynamic impact of flupirtine is the decrease in neuronal excitability. Hyperpolarized neurons are less likely to produce action potentials, which are the electrical impulses in the nervous system that carry information, because they are less sensitive to excitatory cues. The transmission of pain signals from peripheral nerves to the central nervous system is effectively dampened by this decrease in excitability. 

Pharmacokinetics: 

Absorption 

The bioavailability is 90% 

The time to achieve peak effect is 1-4 hours 

Distribution 

Protein-bound is 95-99% 

The volume of distribution of flupirtine is 99 L/kg 

Metabolism 

Hepatic metabolism occurs to flupirtine, mainly in the liver. flupirtine is metabolized by a number of enzymatic mechanisms that result in the production of several metabolites.

Elimination and Excretion 

The half-life is 6-8 hours 

Renal excretion is the body’s primary method of eliminating flupirtine. Excreted in the urine is a considerable portion of the medication and its metabolites. Individual differences may exist in the precise excretion %, which may also be influenced by metabolism, dosage, and general health. 

Adminstartion

Administration: 

Typically, tablets or capsules containing flupirtine are taken orally. A healthcare professional should decide on the dose and schedule that is particular to each patient depending on their condition, the kind and intensity of their pain, and other specific considerations.

Typically, doses of flupirtine are given several times a day at different intervals to ensure steady pain relief. Meals are not necessary when taking flupirtine. In order to reduce the chance of experiencing withdrawal symptoms or a relapse of pain, it is usually advised to taper the dosage of flupirtine gradually while under the supervision of a medical professional. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: flupirtine 

Pronounced: fluh-PEER-teen 

Why do we use flupirtine? 

The primary purpose of flupirtine is to relieve pain because of its analgesic qualities. The management of many types of pain, such as neuropathic pain, musculoskeletal pain, migraines and headaches, and other pain conditions, is generally advised for its usage.