ABSTRAL 400mcg Tablets/Sublingual

What is ABSTRAL 400mcg

ABSTRAL 400mcg is a fast-acting sublingual tablet formulation of Fentanyl (as citrate), a potent synthetic opioid analgesic. It is specifically indicated for the management of breakthrough cancer pain (BTcP) in adult patients who are already receiving and are tolerant to opioid therapy for their underlying persistent cancer pain.

• Form: Sublingual tablet
• Strength: 400 micrograms of fentanyl as citrate
• Packaging: 10 tablets per blister
• Therapeutic class: Opioid analgesic

This formulation allows for rapid onset of pain relief, typically within 10 to 15 minutes after administration. ABSTRAL is designed for use under the tongue, where it dissolves quickly and enters the bloodstream rapidly via the oral mucosa, bypassing the gastrointestinal tract and first-pass metabolism.

Due to its high potency, ABSTRAL 400mcg is prescribed only for opioid-tolerant patients and is not suitable for opioid-naïve individuals due to the risk of potentially fatal respiratory depression.

How to use ABSTRAL 400mcg

ABSTRAL must be used precisely as prescribed by a healthcare provider trained in pain management and opioid therapy. Correct administration is critical to achieve optimal pain relief and to minimize the risk of overdose.

• Place the tablet under the tongue as far back as comfortable.
• Do not chew, crush, or swallow the tablet whole.
• Allow the tablet to dissolve completely. This typically takes about 1–2 minutes.
• Do not eat or drink anything until the tablet is fully dissolved.

Patients should wait at least 2 hours before treating another breakthrough pain episode with ABSTRAL. If pain relief is not adequate, the healthcare provider may adjust the dose or titrate gradually to find the effective dose.

ABSTRAL should not be used more than four times a day for breakthrough pain. Patients must continue their regular opioid regimen for chronic background cancer pain alongside ABSTRAL.

Mode of Action ABSTRAL 400mcg

Fentanyl, the active ingredient in ABSTRAL, is a potent opioid agonist that primarily acts on the mu-opioid receptors in the central nervous system (CNS). These receptors are involved in pain perception, emotional response to pain, and the modulation of nociceptive signals.

• Mu-opioid receptor agonism: Fentanyl binds with high affinity to these receptors, producing analgesia, sedation, euphoria, and respiratory depression.
• Rapid absorption: The sublingual route enables rapid mucosal absorption directly into systemic circulation, bypassing first-pass hepatic metabolism.
• Onset of action: Pain relief typically begins within 10–15 minutes of administration, making it ideal for breakthrough pain episodes.
• Duration: Short-acting; provides pain relief for approximately 1–2 hours.

Because of this quick onset and high potency, ABSTRAL is effective for the rapid control of breakthrough pain episodes in opioid-tolerant cancer patients.

ABSTRAL 400mcg Interactions ABSTRAL 400mcg

ABSTRAL can interact with many medications and substances, some of which may enhance its effects, particularly the risk of respiratory depression, while others may reduce its efficacy or increase its side effects.

• Other CNS depressants: Combining ABSTRAL with benzodiazepines (e.g., diazepam), sedatives, alcohol, or antipsychotics can increase the risk of profound sedation, respiratory depression, coma, or death.
• Cytochrome P450 3A4 inhibitors: Drugs like ketoconazole, erythromycin, and ritonavir may increase fentanyl levels by inhibiting its metabolism, leading to toxicity.
• Inducers of CYP3A4: Rifampin, phenytoin, or carbamazepine may reduce fentanyl levels and analgesic effect.
• Serotonergic drugs: Co-administration with SSRIs, SNRIs, or MAOIs can increase the risk of serotonin syndrome, a potentially life-threatening condition.

Patients must inform their healthcare provider of all medications they are taking, including over-the-counter drugs, herbal products, and dietary supplements, to avoid harmful interactions.

Dosage of ABSTRAL 400mcg

The dosing of ABSTRAL must be individualized and titrated under strict medical supervision. The goal is to determine the lowest effective dose that provides adequate relief of breakthrough pain.

• Initial Dose: Patients starting ABSTRAL therapy must undergo dose titration. The initial dose is not necessarily 400mcg — it starts at 100mcg and is adjusted based on clinical response.
• Titration: If 100mcg is not effective, the dose may be increased in steps (100 → 200 → 300 → 400mcg, etc.) until adequate pain relief is achieved.
• Maintenance Dose: Once the effective dose is identified, patients use that specific dose for subsequent BTcP episodes. 400mcg may be the final titrated dose in some patients.
• Frequency: No more than 4 doses per day should be used.

Note: ABSTRAL is not interchangeable on a microgram-per-microgram basis with other fentanyl products. Each formulation has its own unique pharmacokinetic profile, so switching requires retitration.

Possible side effects of ABSTRAL 400mcg

Like other opioids, ABSTRAL may cause a range of side effects. Some are common and manageable, while others may be severe and require immediate medical attention.

• Common side effects:
  • Drowsiness or sedation
  • Dizziness
  • Nausea or vomiting
  • Constipation
  • Dry mouth
• Serious side effects:
  • Respiratory depression (slowed or shallow breathing)
  • Bradycardia (slow heart rate)
  • Severe hypotension
  • Serotonin syndrome (if used with serotonergic drugs)
  • Allergic reactions: rash, swelling, anaphylaxis (rare)

Patients and caregivers should be educated to recognize early signs of respiratory depression and seek emergency help if symptoms occur. Monitoring is especially critical during the initial dose titration phase.

ABSTRAL 400mcg Contraindications ABSTRAL 400mcg

ABSTRAL is not appropriate for all patients. Its use is contraindicated in certain clinical situations due to the high risk of serious adverse effects.

• Opioid-naïve patients: Due to the high potency of fentanyl, ABSTRAL should only be used in individuals already tolerant to regular opioid therapy.
• Acute or postoperative pain: ABSTRAL is not indicated for the management of short-term, acute, or surgical pain.
• Severe respiratory depression: Pre-existing conditions affecting respiration may be worsened by fentanyl.
• Hypersensitivity: Known allergy to fentanyl or any tablet excipient.
• Use of MAO inhibitors: Concomitant or recent (within 14 days) use increases risk of fatal reactions.

ABSTRAL should be used with extreme caution in patients with head injury, liver or kidney impairment, or in elderly and debilitated patients, due to increased sensitivity to opioids.

Storage of ABSTRAL 400mcg

Proper storage of ABSTRAL is essential due to the high potency of fentanyl and the risk of accidental exposure, especially in children and pets.

• Temperature: Store at room temperature between 20°C to 25°C (68°F to 77°F).
• Keep in original blister: Do not remove tablets from their packaging until ready to use to prevent degradation and contamination.
• Secure storage: Store in a locked cabinet or location away from children, pets, and unauthorized individuals.
• Disposal: Unused tablets must be disposed of safely. Follow your local pharmacy or regulatory guidance for disposal of opioids.
• Avoid moisture and heat: Keep away from direct sunlight and humid environments like bathrooms.

Accidental ingestion of ABSTRAL can be fatal, especially in children. Always ensure tablets are stored securely and used with caution.