sufentanil

Action and Spectrum

Actions and Spectrum: 

sufentanil is a potent opioid analgesic medication in the class of drugs known as fentanyl analogs. It is a synthetic opioid primarily used for anesthesia and pain management in medical settings. Here are the critical aspects of its action and spectrum: 

• Action: sufentanil acts on the central nervous system (CNS) by binding to opioid receptors, predominantly the mu-opioid receptors. Activation of these receptors produces various effects, including analgesia (pain relief), sedation, respiratory depression, and euphoria. 
• Potency: sufentanil is highly potent, with a potency approximately 5 to 10 times greater than that of fentanyl and up to 1,000 times greater than that of morphine. This high potency makes it suitable when requiring rapid and intense analgesia or anesthesia. 
• Analgesia: sufentanil provides potent analgesia, making it helpful in managing severe pain. Its quick onset of action and short duration of effect make it particularly suitable for surgical procedures and acute pain management. 
• Anesthesia: sufentanil is commonly used as an adjunct to general anesthesia during surgeries. It can be administered intravenously or via epidural or intrathecal routes to provide analgesia and maintain stable anesthesia during the procedure. 
• Duration of action: sufentanil has a relatively short duration of action compared to other opioids. Its effects typically last for around 30 to 60 minutes, which allows for precise control over the level of analgesia or sedation. 
• Side effects: Like other opioids, sufentanil can cause various side effects, including respiratory depression, sedation, nausea, vomiting, constipation, itching, and potential dependence or addiction with long-term use. These side effects should be closely monitored and managed by healthcare professionals. 
• Dosage: The sufentanil dosage should be carefully individualized based on the patient’s age, weight, and medical condition. It is typically administered and monitored by trained healthcare professionals in a controlled medical environment. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Pruritus 

Anticholinergic effects 

Dizziness 

Seizures 

Urticaria 

Weakness 

Agitation 

Visual disturbances 

Restlessness 

Respiratory depression 

Circulatory depression 

Euphoria 

Faintness 

Nervousness 

Depression 

Sedation 

Dysphoria 

Vomiting 

Coma 

Bradycardia 

Flushing 

Constipation 

Sweating  

Nausea 

Black Box Warning

Black Box Warning: 

It’s important to note that opioids, including sufentanil, have the possibly for abuse, addiction, and misuse. Prolonged or inappropriate use of opioids can lead to dependence and addiction. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

sufentanil has several contraindications, which are conditions or circumstances in which the medication is not recommended due to the potential risks outweighing the benefits. Here are some common contraindications for sufentanil: 

• Hypersensitivity: sufentanil should not be used in individuals with known hypersensitivity or allergic reactions to sufentanil or other opioid medications. 
• Respiratory Depression: sufentanil can cause significant respiratory depression, slowing down or suppressing breathing. It is generally contraindicated in patients with severe respiratory insufficiency, acute or severe bronchial asthma, or hypercarbia. 
• Paralytic Ileus: sufentanil may cause or worsen paralytic ileus, a condition characterized by the slowing or cessation of bowel movements. It is contraindicated in individuals with suspected or known gastrointestinal obstruction. 
• Acute or Severe Hepatic Impairment: sufentanil is metabolized in the liver, and individuals with severe hepatic impairment may have difficulties metabolizing the drug. It is contraindicated in patients with acute or severe hepatic dysfunction. 
• Acute or Severe Renal Impairment: sufentanil is primarily eliminated through the kidneys, and individuals with severe renal impairment may have difficulties eliminating the drug. It is contraindicated in patients with acute or severe renal dysfunction. 
• Monoamine Oxidase Inhibitors (MAOIs): The concomitant use of sufentanil and MAOIs, a type of antidepressant medication, is contraindicated because of risk of severe and unpredictable reactions, including hypertensive crisis. 
• Obstetric Use: sufentanil is generally not recommended during labor and delivery or in obstetric anesthesia due to concerns about respiratory depression in the newborn. 

Caution 

Specific cautions associated with the use of sufentanil: 

• Respiratory Conditions: sufentanil can cause respiratory depression, potentially life-threatening. Caution should be exercised when administering sufentanil to patients with compromised respiratory function, like those with COPD (chronic obstructive pulmonary disease), asthma, or other respiratory disorders. 
• Cardiovascular Conditions: sufentanil may cause hypotension (low blood pressure) and bradycardia (slow heart rate). It should be generally used cautiously in patients with cardiovascular diseases, including hypovolemia (low blood volume), hypotension, shock, or arrhythmias. 
• Head Trauma or Increased Intracranial Pressure: sufentanil can increase intracranial pressure, and its use should be cautiously used in patients with head trauma, intracranial lesions, or pre-existing increased intracranial pressure. Monitoring of neurological status is essential in such cases. 
• Geriatric or Debilitated Patients: Elderly or debilitated patients may be more sensitive to the respiratory depressant effects of sufentanil. Lower doses and careful titration should be considered, and close monitoring for adverse effects is crucial. 
• Renal or Hepatic Impairment: The kidneys primarily eliminate sufentanil and metabolize it in the liver. Patients with impaired renal/hepatic function may experience prolonged effects or increased sensitivity to the medication. Dose adjustments may be necessary, and careful monitoring is essential. 
• Seizure Disorders: sufentanil can lower the seizure threshold. It should be generally used cautiously in patients with a earlier history of seizure disorders or those at an increased risk of seizures. 
• Pregnancy and Lactation: sufentanil use during pregnancy and lactation should be carefully considered. The potential risks, benefits to the mother and the fetus or newborn should be evaluated, and alternative options may be explored. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned 

Lactation:   

Excreted into human milk: Yes 

Breastfeeding warnings:  

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: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

sufentanil is a potent opioid analgesic that shares pharmacological properties with other opioids. Here are some critical aspects of the pharmacology of sufentanil: 

sufentanil acts primarily on the mu-opioid receptors in the central nervous system. Binding to these receptors produces various pharmacological effects, including analgesia, sedation, respiratory depression, and euphoria. 

Analgesic Effect: sufentanil provides potent analgesia by inhibiting the transmission of pain signals in spinal cord and brain. It reduces the perception of pain without significantly affecting other sensory modalities. 

Pharmacodynamics: 

Mechanism of action: sufentanil is a potent opioid analgesic that acts primarily through its interaction with opioid receptors in the central nervous system. Its action is similar to other opioids, such as morphine or fentanyl. Here are the critical aspects of the mechanism of action of sufentanil: 

• Opioid Receptor Binding: sufentanil selectively binds to mu-opioid receptors, which are especially located in the brain, spinal cord, and peripheral tissues. Binding to these receptors produces analgesic effects and mediates many of the pharmacological actions of sufentanil. 
• Modulation of Neurotransmission: By binding to mu-opioid receptors, sufentanil inhibits the release of various neurotransmitters, including P, noradrenaline, dopamine, and serotonin. This modulation of neurotransmitter release reduces the transmission of pain signals, resulting in analgesia. 
• Suppression of Pain Signal Transmission: sufentanil inhibits the conduction of pain signals by blocking the activation of pain-transmitting neurons in the spinal cord and ascending pain pathways. This blockade of pain signal transmission reduces the perception of pain. 
• Central Nervous System Effects: sufentanil affects the central nervous system by enhancing inhibitory signaling and reducing excitatory activity. It hyperpolarizes neurons, decreases neuronal firing, and decreases the release of excitatory neurotransmitters, thereby producing sedation and anxiolysis. 
• Respiratory Effects: Activation of mu-opioid receptors in the brainstem can suppress the responsiveness of the respiratory centers, leading to respiratory depression. sufentanil can reduce the rate and depth of breathing, which can be a dose-dependent effect and a significant concern that requires careful monitoring during administration. 
• Other Effects: sufentanil can cause a range of additional effects, including euphoria, sedation, miosis (constriction of the pupils), gastrointestinal effects (such as constipation and decreased gastrointestinal motility), and cardiovascular effects (such as bradycardia and vasodilation). 

Pharmacokinetics: 

Absorption 

sufentanil can be administered by various routes, including intravenous (IV), epidural, and intrathecal. When given IV, sufentanil is rapidly and completely absorbed into the systemic circulation since its high lipid solubility. The onset of action is usually within minutes. 

Distribution 

sufentanil has a relatively large volume of distribution, indicating extensive distribution throughout the body. It rapidly crosses the blood-brain barrier, resulting in its rapid onset of action in the central nervous system. sufentanil is highly protein-bound (greater than 90%), primarily to alpha-1-acid glycoprotein. 

Metabolism 

sufentanil undergoes hepatic metabolism primarily via cytochrome P450 3A4 enzymes. It undergoes N-dealkylation and hydrolysis to form inactive metabolites, including N-desmethyl sufentanil and N-desmethyl-3-hydroxy sufentanil. These metabolites are further metabolized and eventually eliminated. 

Elimination and Excretion 

The elimination half-life of sufentanil is relatively short, typically ranging from 2 to 4 hours. Most sufentanil and its metabolites are excreted in the urine, with <1% of the administered dose excreted unchanged. Renal clearance is the main route of elimination, with a smaller portion being eliminated in feces. 

Adminstartion

Administration: 

Intravenous administration 

sufentanil is a potent opioid medication typically administered by healthcare professionals in medical settings. The route of administration and dosage of sufentanil depend on the specific situation and the medication’s intended use. Here are some standard methods of administering sufentanil: 

• Intravenous (IV) Administration: sufentanil is commonly administered intravenously. It is typically given as a slow bolus injection or through continuous infusion. Intravenous administration allows for rapid onset of action and precise control of the dosage. 
• Patient-Controlled Analgesia (PCA): sufentanil can be used in patient-controlled analgesia systems, where the patient has control over administering a predetermined dose of medication by pressing a button. PCA is often used for managing post-operative pain, allowing patients to self-administer sufentanil within programmed safety limits. 
• Epidural Administration: sufentanil can be administered via the epidural route, where the medication is injected into the epidural space surrounding the spinal cord. The epidural administration of sufentanil is commonly used for anesthesia and post-operative pain relief. 
• Patient-Controlled Epidural Analgesia (PCEA): Like PCA, PCEA involves patient-controlled administration of sufentanil through an epidural catheter. It allows patients to self-administer controlled doses of sufentanil for pain management following surgery or childbirth. 
• Intrathecal Administration: An intrathecal catheter can administer sufentanil directly into the cerebrospinal fluid. Intrathecal administration is used for anesthesia and pain management during specific surgical procedures or chronic pain management. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: sufentanil 

Pronounced: [ soo-FEN-ta-nil ] 

Why do we use sufentanil? 

sufentanil is a potent opioid medication primarily used for anesthesia and pain management in medical settings. Here are some common uses of sufentanil: 

• Anesthesia: sufentanil is used as an adjunct to general anesthesia during surgical procedures. It provides profound analgesia and sedation, helping to ensure the patient’s comfort and to maintain stable anesthesia during the operation. 
• Post-operative Pain Management: sufentanil may be used for postoperative pain management in the immediate postoperative period. It can be administered intravenously or via patient-controlled analgesia (PCA) systems, allowing patients to self-administer the medication within safe limits to control their pain. 
• Obstetric Analgesia: sufentanil is sometimes used for pain relief during labor and delivery. It can be administered via epidural or intrathecal routes to provide analgesia during childbirth. However, the use of sufentanil in obstetrics is generally limited and carefully considered due to the potential respiratory depression in the newborn. 
• Intensive Care Unit (ICU) Sedation: sufentanil may sedate critically ill patients in the ICU (intensive care unit). It can help manage pain and induce a state of sedation to facilitate patient comfort and provide necessary support during critical conditions. 
• Chronic Pain Management: In some cases, sufentanil may be used to manage chronic pain. This may include conditions such as cancer or severe chronic pain not adequately controlled by other analgesics. However, the use of sufentanil for chronic pain is typically reserved for specialized pain management settings.