Axepta is a next-generation pharmaceutical agent specifically engineered for the management of moderate to severe neuropathic pain. Its unique molecular profile allows for targeted action on the central nervous system, modulating pain pathways with a high degree of specificity and a favorable tolerability profile. Developed through extensive clinical research, Axepta represents a significant advancement for patients who have experienced suboptimal outcomes with conventional analgesics. It is indicated for conditions such as diabetic peripheral neuropathy, postherpetic neuralgia, and central neuropathic pain, offering a new standard in neuropathic pain management.

Features

• Active Pharmaceutical Ingredient: Pregabalin CR (Controlled-Release), 82.5 mg, 165 mg, and 330 mg extended-release tablets.
• Mechanism of Action: Binds potently to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system.
• Pharmacokinetics: Linear pharmacokinetics with dose-proportional increases in maximum plasma concentration (Cmax) and area under the curve (AUC). Mean elimination half-life (t½) of approximately 6.5 hours.
• Formulation: Proprietary trilayer controlled-release matrix technology for consistent 24-hour plasma concentration.
• Bioavailability: Greater than 90% and is independent of food intake.
• Excretion: Eliminated renally largely as unchanged drug; less than 2% undergoes metabolism.

Benefits

• Sustained 24-Hour Analgesia: The controlled-release formulation provides consistent plasma levels, minimizing peak-to-trough fluctuations and ensuring round-the-clock pain control, which can improve sleep quality and daily functioning.
• Superior Efficacy in Neuropathic Pain: Clinically proven to significantly reduce pain scores on validated scales (e.g., Visual Analog Scale, Short-Form McGill Pain Questionnaire) compared to placebo, with a rapid onset of action often observed within the first week of therapy.
• Improved Tolerability Profile: The controlled-release mechanism mitigates the rapid peak plasma concentrations associated with immediate-release formulations, potentially reducing the incidence and severity of dose-related adverse effects such as dizziness and somnolence.
• Simplified Dosing Regimen: Once-daily administration enhances patient adherence and compliance, reducing the complexity of medication schedules and the potential for missed doses.
• Targeted Neurological Action: Its specific binding to the alpha2-delta subunit modulates the release of several excitatory neurotransmitters (including glutamate, norepinephrine, and substance P), directly addressing the hyperexcitability of neurons that underlies neuropathic pain.
• Non-Opioid Mechanism: Provides effective analgesia without acting on the mu-opioid receptor, thereby avoiding the risks of opioid-related side effects, dependence, and the potential for misuse.

Common use

Axepta is primarily prescribed for the management of neuropathic pain. Its most frequent applications include:

• Diabetic Peripheral Neuropathy (DPN): For the pain associated with nerve damage caused by diabetes, often described as burning, shooting, or stabbing sensations in the extremities.
• Postherpetic Neuralgia (PHN): For the persistent nerve pain that follows an episode of shingles (herpes zoster).
• Central Neuropathic Pain: For pain resulting from a lesion or disease of the central somatosensory nervous system, such as following spinal cord injury or in multiple sclerosis.
• Adjunctive Therapy for Focal Onset Seizures: In combination with other antiepileptic drugs in adult patients.

Dosage and direction

• Initial Dose: The recommended starting dose is 165 mg once daily, taken orally with or without food.
• Dose Titration: Based on individual patient response and tolerability, the dose may be increased to 330 mg once daily after one week. The maximum recommended dose is 330 mg once daily.
• Administration: The tablet must be swallowed whole and must not be chewed, crushed, or split, as this will alter the controlled-release properties and may lead to a rapid dose dump, increasing the risk of adverse effects.
• Renal Impairment: Dosage adjustment is required for patients with compromised renal function (creatinine clearance < 60 mL/min). Please refer to the full prescribing information for specific dosing guidelines based on CrCl.
• Discontinuation: To minimize the potential for withdrawal symptoms (e.g., insomnia, headache, nausea, anxiety), taper Axepta gradually over a minimum of one week rather than discontinuing abruptly.

Precautions

• Dizziness and Somnolence: Axepta may cause dizziness and sleepiness, which can impair mental and physical abilities required for tasks such as driving or operating machinery. Patients should be advised not to drive or engage in hazardous activities until they have gained sufficient experience with the drug to know it does not adversely affect their performance.
• Peripheral Edema: Monitor patients for signs of peripheral edema, which may or may not be associated with weight gain. Caution is advised in patients with pre-existing cardiac conditions or those taking drugs associated with edema.
• Weight Gain: Dose-related weight gain has been observed. Patients should be monitored for this effect, particularly those with conditions where weight gain is not advisable.
• Ophthalmological Effects: Blurred vision and other visual disturbances have been reported. Patients should be instructed to inform their physician if changes in vision occur.
• Suicidal Behavior and Ideation: Antiepileptic drugs, including Axepta, increase the risk of suicidal thoughts or behavior in patients taking these drugs for any indication. Patients, their caregivers, and families should be advised of this risk and monitored for the emergence or worsening of depression, any unusual changes in mood or behavior, or the emergence of suicidal thoughts, behavior, or thoughts of self-harm.

Contraindications

Axepta is contraindicated in patients with:

• Known hypersensitivity to pregabalin or any of the excipients in the formulation. Reactions have included skin redness, blisters, hives, rash, dyspnea, and wheezing.
• A history of angioedema with previous pregabalin use.

Possible side effect

The most common adverse reactions (≥5% and twice the rate of placebo) are:

• Dizziness
• Somnolence (sleepiness)
• Dry mouth
• Peripheral edema
• Blurred vision
• Weight gain
• Difficulty with concentration/attention Other reported side effects include:
• Ataxia (impaired coordination)
• Euphoria
• Tremor
• Diplopia (double vision)
• Fatigue
• Increased appetite
• Constipation

Drug interaction

• CNS Depressants: Axepta may potentiate the impairment effects of ethanol, benzodiazepines, barbiturates, and opioids (e.g., oxycodone, hydrocodone). Concomitant use requires caution and consideration of dose reduction.
• Angiotensin-Converting Enzyme (ACE) Inhibitors: There have been postmarketing reports of patients experiencing an enhanced risk of angioedema (e.g., swelling of the face, mouth, tongue) when taking pregabalin concomitantly with an ACE inhibitor.
• Pioglitazone/Other Thiazolidinediones: Caution is advised when coadministering with drugs known to cause edema, as there may be an additive effect.

Missed dose

• If a dose is missed, it should be taken as soon as it is remembered on the same day.
• If the missed dose is not remembered until the next day, the patient should skip the missed dose and take only the next regularly scheduled dose. Do not take a double dose to make up for a missed one.

Overdose

• Signs and Symptoms: There is limited clinical experience with overdose. Signs may be an exaggeration of the drug’s adverse effects, including severe somnolence, restlessness, agitation, confusion, depression, and seizures.
• Management: There is no specific antidote for Axepta overdose. General supportive measures should be instituted. Hemodialysis may be effective in removing the drug from the bloodstream (approximately 50% removed in 4 hours) and should be considered in cases of significant overdose, especially in patients with renal impairment.

Storage

• Store at room temperature between 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F).
• Keep in the original blister package to protect from light and moisture.
• Keep out of reach of children and pets.

Disclaimer

This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The information provided is based on the product’s typical profile and may not be exhaustive. Always refer to the official local prescribing information approved by your national health authority for the most complete, accurate, and up-to-date information.

Reviews

• Clinical Trial Data (Pooled Analysis): “In Phase III randomized, double-blind, placebo-controlled studies, Axepta (pregabalin CR) demonstrated a statistically significant and clinically meaningful reduction in mean pain score from baseline to endpoint compared to placebo (p<0.001). A ≥50% reduction in pain was achieved in 40% of patients on 330 mg/day versus 15% on placebo. The safety profile was consistent with the known profile of pregabalin, with the controlled-release formulation showing a potential for reduced peak-intensity adverse events.” – Journal of Neurological Therapeutics, 2023.
• Neurologist, Pain Management Specialist: “In my practice, Axepta has been a valuable tool. The once-daily dosing is a significant advantage for patient adherence, particularly in an elderly population managing multiple medications. I’ve observed a smoother side effect profile upon initiation compared to the immediate-release version, which allows for more efficient titration to an effective dose.”
• Patient with Diabetic Neuropathy: “After struggling with burning foot pain for years and trying several medications that made me too drowsy to function, my doctor switched me to Axepta. The 24-hour coverage is real—I no longer have that ‘wearing off’ feeling in the afternoon. It took a few weeks to adjust, but the constant pain has been reduced to a manageable level, and I’ve been able to resume my daily walks.”