ABSTRAL 100mcg Tablets/Sublingual

What is ABSTRAL 100mcg

ABSTRAL 100mcg is a potent opioid analgesic available as sublingual tablets designed to rapidly relieve breakthrough pain in patients who are already receiving and tolerant to around-the-clock opioid therapy for chronic cancer pain. The active ingredient in ABSTRAL is fentanyl citrate, a synthetic opioid that is significantly stronger than morphine.

• It belongs to the class of strong opioid analgesics used for the management of severe pain.
• ABSTRAL tablets are placed under the tongue (sublingual administration) for quick absorption into the bloodstream, resulting in rapid onset of pain relief.
• This medication is specifically indicated for breakthrough pain, which is a sudden, transient flare of pain that occurs despite baseline pain control.
• ABSTRAL should only be used in patients who are opioid tolerant due to its potency and risk of serious adverse effects including respiratory depression.
• It is a prescription-only medicine and requires careful monitoring by healthcare professionals.
• Because of its rapid action, ABSTRAL is useful in situations where quick control of acute pain episodes is needed.

Overall, ABSTRAL 100mcg is an essential medication for managing episodic severe pain in selected patients with chronic cancer-related pain, improving quality of life by controlling otherwise disabling pain flares.

How to use ABSTRAL 100mcg

Correct administration of ABSTRAL 100mcg sublingual tablets is crucial for effective pain control and safety. Important instructions include:

• Route: Place the tablet under the tongue and allow it to dissolve completely without chewing, swallowing, or sucking it.
• Do not eat or drink: Avoid eating or drinking until the tablet is fully dissolved to ensure optimal absorption.
• Dosage initiation: The initial dose should be prescribed by a specialist, usually starting with the lowest strength available, as dosing is highly individualized.
• Frequency: Use ABSTRAL only as needed for breakthrough pain, and never exceed the prescribed maximum daily dose.
• Opioid tolerance: Only patients who are opioid tolerant (i.e., already on significant doses of opioids for chronic pain) should use ABSTRAL.
• Avoid alcohol and CNS depressants: These can increase sedation and respiratory depression risk.
• Storage: Keep the tablets in the original blister pack until use to protect from moisture.
• Missed dose: Do not take an extra dose if a dose is missed; wait until breakthrough pain occurs again before using ABSTRAL.
• Disposal: Dispose of unused tablets safely as per local guidelines due to risk of misuse or accidental ingestion.

Proper adherence to these instructions helps ensure safe and effective relief of breakthrough pain episodes.

Mode of Action ABSTRAL 100mcg

The active component of ABSTRAL, fentanyl citrate, is a synthetic opioid agonist that acts primarily on the central nervous system (CNS) to relieve pain. Its mode of action includes:

• Opioid receptor binding: Fentanyl selectively binds to the mu-opioid receptors located in the brain, spinal cord, and other parts of the body.
• Inhibition of pain pathways: Activation of mu-opioid receptors inhibits ascending pain signals by reducing neurotransmitter release and altering neuronal excitability.
• Rapid absorption: Sublingual administration allows fentanyl to bypass the gastrointestinal tract and first-pass metabolism, enabling quick entry into systemic circulation and fast onset of analgesia.
• Potency: Fentanyl is approximately 50-100 times more potent than morphine, making it suitable for severe pain control.
• Duration of action: Its effects typically begin within minutes and last for 1-2 hours, suitable for transient breakthrough pain episodes.

This targeted action at opioid receptors results in effective suppression of breakthrough cancer pain with rapid onset and relatively short duration, matching the episodic nature of the pain.

ABSTRAL 100mcg Interactions ABSTRAL 100mcg

ABSTRAL (fentanyl citrate) has important drug interactions that may affect its safety and efficacy. Key interaction points include:

• CNS depressants: Concomitant use with benzodiazepines, alcohol, sedatives, or other opioids may cause profound sedation, respiratory depression, coma, or death.
• Monoamine oxidase inhibitors (MAOIs): Use with MAOIs or within 14 days of stopping them is contraindicated due to risk of serotonin syndrome or enhanced opioid effects.
• CYP3A4 inhibitors: Drugs like ketoconazole, erythromycin, ritonavir can increase fentanyl plasma concentrations, raising overdose risk.
• CYP3A4 inducers: Agents such as carbamazepine, phenytoin, rifampin may reduce fentanyl levels, decreasing effectiveness.
• Anticholinergic drugs: May increase risk of urinary retention or severe constipation when combined with fentanyl.
• Serotonergic drugs: Caution with SSRIs, SNRIs, or triptans to avoid serotonin syndrome.
• Muscle relaxants and anesthetics: Enhanced sedation and respiratory depression risk when co-administered.

Patients must inform their healthcare provider of all current medications to avoid potentially dangerous interactions with ABSTRAL.

Dosage of ABSTRAL 100mcg

Dosage of ABSTRAL must be individualized carefully under strict medical supervision, typically by a pain specialist. Key dosing considerations include:

• Initial dosing: Usually starts at the lowest available strength (100 mcg) for opioid-tolerant patients to assess individual response and tolerance.
• Titration: Dose adjustments are made cautiously based on effectiveness and side effects, with careful monitoring to avoid overdose.
• Maximum daily dose: Depends on total opioid use and breakthrough pain frequency; patients should not exceed prescribed limits.
• Frequency: ABSTRAL is taken only as needed for breakthrough pain, not for baseline pain control.
• Not for opioid non-tolerant patients: Use in non-tolerant patients is contraindicated due to risk of fatal respiratory depression.
• Discontinue other breakthrough opioids: When starting ABSTRAL, other rapid-acting opioids should be stopped to avoid additive effects.
• Special populations: Elderly, hepatic or renal impairment patients require close monitoring and possible dose adjustments.

Strict adherence to prescribed dosage and regular follow-ups are critical to maximize safety and efficacy.

Possible side effects of ABSTRAL 100mcg

ABSTRAL use can cause a range of side effects, some of which may be serious. Common and important side effects include:

• Common Side Effects: Drowsiness, dizziness, nausea, vomiting, constipation, dry mouth, headache, weakness, sweating.
• Respiratory Depression: Serious and potentially fatal slowing of breathing, especially in non-opioid tolerant patients or with overdose.
• Hypotension: Low blood pressure causing fainting or dizziness.
• Central Nervous System Effects: Confusion, hallucinations, sedation, or mood changes.
• Allergic reactions: Rash, itching, swelling, or anaphylaxis in rare cases.
• Withdrawal Symptoms: If abruptly discontinued after prolonged use, symptoms like agitation, sweating, and muscle pain may occur.
• Serotonin Syndrome: Rare but serious if combined with serotonergic agents; symptoms include agitation, hallucinations, rapid heartbeat, and fever.

Any new or worsening symptoms should be reported to a healthcare provider immediately. Respiratory depression requires urgent medical attention.

ABSTRAL 100mcg Contraindications ABSTRAL 100mcg

ABSTRAL is contraindicated in the following situations:

• Non-opioid tolerant patients due to high risk of fatal respiratory depression.
• Known hypersensitivity to fentanyl or any component of the tablet.
• Severe respiratory depression or acute asthma attacks.
• Paralytic ileus or severe gastrointestinal obstruction.
• Concurrent use of MAO inhibitors or within 14 days of their discontinuation.
• Use in patients with significant CNS depression or coma.
• Patients with known or suspected head injury or increased intracranial pressure without appropriate monitoring.

Strict patient selection and screening are mandatory to avoid life-threatening complications.

Storage of ABSTRAL 100mcg

Proper storage ensures ABSTRAL’s stability and safety:

• Store tablets in the original blister pack until use to protect from moisture and light.
• Keep at room temperature, ideally between