sufentanil SL

Action and Spectrum

Actions and spectrum: 

sufentanil sublingual (SL) is a potent opioid analgesic medication. It belongs to the class of fentanyl analogs. sufentanil SL acts primarily as a mu-opioid receptor agonist, binding to the mu-opioid receptors in the central nervous system (CNS) to produce analgesic effects. 

The spectrum of action of sufentanil SL includes powerful pain relief and sedation. It is used in the moderate to severe pain, such as during surgical procedures or in the immediate postoperative period.

Due to its potency, sufentanil SL is often reserved for use in specialized settings, such as in operating rooms, intensive care units, or under the supervision of trained healthcare professionals. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Dizziness (5.6%) 

Vomiting (5.6%) 

Hypotension (4.7%) 

>10% 

Headache (12.1%) 

Nausea (29%)  

<1% 

Gastrointestinal disorders: dyspepsia, diarrhea, eructation, abdominal discomfort, upper abdominal pain, postoperative ileus, Constipation, flatulence, dry mouth, retching, abdominal distension, gastritis, oral hypoesthesia 

connective-tissue and Musculoskeletal disorders: Muscle spasms 

Psychiatric disorders: confusional state, agitation, euphoric mood, mental status changes, Insomnia, anxiety, disorientation, hallucination 

Respiratory, mediastinal, and thoracic disorders: bradypnea, apnea, hypoventilation, respiratory failure, Hypoxia, hiccups, atelectasis, respiratory distress 

Vascular disorders: hypertension, flushing, Hypotension, orthostatic hypotension 

Cardiac disorders: bradycardia, Sinus tachycardia 

Investigations: decreased respiratory rate, decreased urine output, increased AST, increased hepatic enzyme, decreased Oxygen saturation, decreased urine output, abnormal electrocardiogram 

Nervous system disorders: sedation, lethargy, Somnolence, presyncope, memory impairment 

urinary and renal disorders: urinary hesitation, renal failure, Urinary retention, oliguria 

subcutaneous tissue and Skin disorders:  hyperhidrosis, Pruritus, rash   

Post marketing Reports 

Adrenal insufficiency 

Androgen deficiency 

Serotonin syndrome 

Anaphylaxis 

Black Box Warning

Black Box Warning: 

There are no specific black box warnings associated with sufentanil sublingual. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: sufentanil SL is contraindicated in individuals with hypersensitivity or allergic reaction to sufentanil or any of its components. 
• Respiratory Depression: sufentanil SL is contraindicated in patients with severe respiratory depression or severe chronic obstructive pulmonary disease (COPD), as it can further depress respiratory function. 
• Acute or Severe Bronchial Asthma: sufentanil SL is contraindicated in acute or severe bronchial asthma or hypercarbia (increased carbon dioxide levels in the blood), as it may exacerbate respiratory difficulties. 
• Paralytic Ileus: sufentanil SL is contraindicated in patients with paralytic ileus, a condition characterized by the impairment of intestinal movement, as it may further inhibit gastrointestinal motility. 
• Known or Suspected Genetic Variability: sufentanil SL is contraindicated in patients known or suspected to have a genetic variability of the cytochrome P450 3A4 enzyme, as it may affect the metabolism and clearance of the drug.

Caution: 

• Sedation and Impaired Alertness: sufentanil SL may cause sedation, drowsiness, or impaired alertness. Patients should be recommended not to operate machinery, drive, or engage in activities which requires mental alertness. 
• Hypotension: sufentanil SL can cause a drop in blood pressure, especially when administered rapidly or in high doses. Caution should be used in patients with hypovolemia, hypotension, or those who are sensitive to the effects of vasodilators. 
• Dependence and Addiction: sufentanil SL, like other opioid analgesics, has the potential for abuse, addiction, and physical dependence. It should be used under caution in patients with substance abuse or addiction. 
• Interactions with Other Medications: sufentanil SL may interact with other CNS depressants, such as benzodiazepines, sedatives, or alcohol, resulting in additive effects and increased sedation. Caution should be exercised when co-administering sufentanil SL with other medications that can cause respiratory depression or central nervous system depression. 
• Special Populations: sufentanil SL should be used under caution in elderly patients, as they can be more sensitive to the effects of opioids.

Comorbidities: 

• Cardiovascular Disease: Patients with significant cardiovascular disease, such as CHF, CAD, or severe hypertension, may require careful monitoring during the administration of sufentanil SL due to its potential effects on blood pressure and heart rate. 
• Hepatic or Renal Impairment: sufentanil SL is metabolized and eliminated primarily by the liver and kidneys. Patients with significant hepatic or renal impairment may experience altered metabolism and clearance of the drug, which could affect its efficacy and safety. Dose adjustments or alternative pain management strategies may be required in such cases. 
• Substance Abuse or Addiction: Patients with a history of substance abuse or addiction may be at higher risk of developing dependence or experiencing adverse effects with the use of sufentanil SL.  
• Mental Health Disorders: Patients with psychiatric or mental health disorders, particularly those with a history of opioid misuse or dependency, may require specialized management and monitoring when receiving sufentanil SL. 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: sufentanil SL gets excreted into human milk 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>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: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

• Mechanism of Action: sufentanil SL acts as a selective agonist at the opioid receptors in the central nervous system, primarily targeting the mu-opioid receptors. Activation of these receptors produces analgesia, sedation, and respiratory depression. 
• Analgesic Effects: sufentanil SL provides potent analgesia by binding to the mu-opioid receptors. This inhibits the transmission of pain signals, resulting in relief from moderate to severe pain. 
• Respiratory Effects: Like other opioids, sufentanil SL can cause respiratory depression by suppressing the respiratory drive and reducing the responsiveness of the respiratory centers in the brainstem. Careful monitoring of respiratory function is necessary to ensure adequate ventilation during Sufentanil SL administration.

Pharmacodynamics: 

• Mu-opioid Receptor Agonism: sufentanil SL acts as a potent agonist at the mu-opioid receptors, which are widely distributed throughout the spinal cord and brain. Activation of these receptors produces analgesia, sedation, and respiratory depression. 
• Sedation: sufentanil SL has sedative properties and can induce a state of calmness, relaxation, and drowsiness. This sedative effect is primarily mediated by the activation of mu-opioid receptors in the central nervous system. 
• Respiratory Depression: Like other opioids, sufentanil SL can cause respiratory depression. This effect is primarily mediated by the activation of mu-opioid receptors in the brainstem, resulting in the suppression of the respiratory drive. 
• Central Nervous System (CNS) Effects: sufentanil SL can produce various central nervous system effects, including a decrease in alertness, impaired cognitive function, and potential for the development of tolerance and dependence with prolonged use. 
• Cardiovascular Effects: sufentanil SL can cause cardiovascular effects, including decreased blood pressure and heart rate. These effects are primarily due to the activation of mu-opioid receptors in the central and peripheral regions involved in the regulation of cardiovascular function.

Pharmacokinetics: 

Absorption 

sufentanil SL is designed for sublingual administration, where the drug is placed under the tongue and allowed to dissolve. It is rapidly absorbed through the highly vascularized sublingual mucosa and enters the systemic circulation. Sublingual administration bypasses the gastrointestinal tract and hepatic first-pass metabolism, resulting in high bioavailability. 

Distribution 

Once absorbed, sufentanil SL is distributed throughout the body. It has a large volume of distribution, indicating extensive tissue distribution. The drug readily crosses the blood-brain barrier, allowing it to exert its effects on the central nervous system. 

Metabolism 

sufentanil undergoes metabolism primarily in the liver, through the cytochrome P450 enzyme system, particularly CYP3A4. The metabolites formed through metabolism are primarily inactive. However, the contribution of metabolism to the overall clearance of sufentanil is low compared to renal excretion. 

Elimination and excretion 

sufentanil and its metabolites are primarily excreted in the urine. Renal excretion accounts for the majority of the drug elimination, with a small portion of the drug and metabolites being excreted in the feces. 

Adminstartion

Administration: 

• Ensure that the patient’s mouth is clean and free from food or other substances. 
• Wash hands and put on the disposable gloves to maintain proper hygiene. 
• Open the packaging of the Sufentanil SL unit-dose container. 
• Gently place the Sufentanil SL tablet or film under the patient’s tongue. 
• Instruct the patient to avoid chewing, swallowing, or talking while the medication is dissolving. 
• Advise the patient to keep their mouth closed during the administration and to avoid drinking or eating until the medication has completely dissolved. 
• The Sufentanil SL medication will dissolve within a few minutes, and the patient will absorb the medication through the sublingual mucosa. 
• After the medication has dissolved, the patient can swallow any remaining residue. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: sufentanil SL 

Pronounced: (soo-FEN-tuh-nil ess-EL)  

Why do we use sufentanil SL? 

sufentanil sublingual (SL) is primarily used for the management of acute moderate-to-severe pain in medically supervised settings. It is typically used as an analgesic option for breakthrough pain in opioid-tolerant adult patients with cancer. 

The specific uses of sufentanil SL include: 

• Breakthrough Cancer Pain: sufentanil SL is used to treat breakthrough cancer pain in adults and tolerant to opioid treatment for their underlying persistent cancer pain. 
• Opioid-Tolerant Patients: sufentanil SL is intended for use in patients who are considered opioid-tolerant, meaning they have been receiving and can tolerate high doses of opioid medications. It is not suitable for opioid-naïve patients or those who are not already using opioids for their persistent cancer pain.