Drug information of Sufentanil

Sufentanil


An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.

Mechanism of effect

Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase.

Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Sufentanil's analgesic activity is, most likely, due to its conversion to morphine. Opioids open calcium-dependent inwardly rectifying potassium channels (OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.

Pharmacodynamic

Sufentanil is a synthetic opioid analgesic. Sufentanil interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissues. In clinical settings, sufentanil exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation.

Sufentanil may increase the patient's tolerance for pain and decrease the perception of suffering, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Sufentanil depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.

Pharmacokinetics

 Absorption, Volume of distribution, Protein binding, Metabolism and Route of elimination are not Available. Half life is 265 minutes.

Dosage

Surgical analgesia (as a component of balanced anesthesia) (surgery expected to last: 1 to 2 hours): IV: Total dose: 1 to 2 mcg/kg with N2O/O2; ≥75% of total dose may be administered by slow injection or infusion prior to intubation (titrate to individual response)

Maintenance:

Incremental dosing: According to the manufacturer, 10 to 25 mcg may be administered as needed when movement and/or changes in vital signs indicate surgical stress or lightening of analgesia. May also administer doses in the range of 5 to 20 mcg as needed or 0.1 to 0.25 mcg/kg as needed. Total dose should not exceed 1 mcg/kg/hour of expected surgical time.

Continuous infusion: May also be administered as a continuous infusion with the infusion rate based on the induction dose used. Maximum infusion rate according to the manufacturer: 1 mcg/kg/hour. May also administer doses in the range of 0.3 to 0.9 mcg/kg/hour or 0.5 to 1.5 mcg/kg/hour .

Surgical analgesia (as a component of balanced anesthesia) (surgery expected to last 2 to 8 hours): Total dose: 2 to 8 mcg/kg with N2O/O2; ≤75% of total dose may be administered by slow injection or infusion prior to intubation (titrate to individual response).

Maintenance:

Incremental dosing: According to the manufacturer, 10 to 50 mcg may be administered as needed when movement and/or changes in vital signs indicate surgical stress or lightening of analgesia. Total dose should not exceed 1 mcg/kg/hour of expected surgical time.

Continuous infusion: May also be administered as a continuous infusion with the infusion rate based on the induction dose used. Maximum infusion rate according to the manufacturer: 1 mcg/kg/hour. May also administer doses in the range of 0.3 to 0.9 mcg/kg/hour or 0.5 to 1.5 mcg/kg/hour.

Surgical anesthesia: Total dose: 8 to 30 mcg/kg as a slow injection, infusion, or injection followed by infusion; titrate to individual patient response.

Maintenance:

Incremental dosing: 0.5 to 10 mcg/kg as needed in anticipation of surgical stress

Continuous infusion: Base infusion rate on the induction dose so that the total dose for the procedure does not exceed 30 mcg/kg

Analgesia for labor and delivery: Epidural: 10 to 15 mcg with bupivacaine 0.125% with/without epinephrine. Dose can be repeated twice (for a total of 3 doses) at not less than 1-hour intervals until delivery.

Alerts

Sufentanil Citrate Injection contains Sufentanil, a Schedule II controlled substance. As an opioid, Sufentanil Citrate Injection exposes users to the risks of addiction, abuse, and misuse.

Serious, life-threatening, or fatal respiratory depression has been reported with the use of opioids, even when used as recommended. Respiratory depression, if not immediately recognized and treated, may lead to respiratory arrest and death. 

Sufentanil Citrate Injection should be administered only by persons specifically trained in the use of anesthetic drugs and the management of the respiratory effects of potent opioids, including respiration and cardiac resuscitation of patients in the age group being treated. 

Monitor such patients closely including vital signs, particularly when initiating and titrating Sufentanil Citrate Injection and when Sufentanil Citrate Injection is given concomitantly with other drugs that depress respiration. To reduce the risk of respiratory depression, proper dosing and titration of Sufentanil Citrate Injection are essential. 

Concomitant use of Sufentanil Citrate Injection with a CYP3A4 inhibitor, such as macrolide antibiotics (e.g., erythromycin), azole-antifungal agents (e.g., ketoconazole), and protease inhibitors (e.g., ritonavir), may increase plasma concentrations of Sufentanil and prolong opioid adverse reactions, which may exacerbate fatal respiratory depression. 

Intravenous administration or unintentional intravascular injection during epidural administration of Sufentanil Citrate Injection may cause muscle rigidity, particularly involving the muscles of respiration. The incidence and severity of muscle rigidity is dose related. These effects are related to the dose and speed of injection. 

When benzodiazepines or other CNS depressants are used with Sufentanil Citrate Injection, pulmonary arterial pressure may be decreased. This fact should be considered by those who conduct diagnostic and surgical procedures where interpretation of pulmonary arterial pressure measurements might determine final management of the patient. 

Profound sedation, respiratory depression, coma, and death may result from the concomitant use of Sufentanil Citrate Injection with benzodiazepines or other CNS depressants (e.g., nonbenzodiazepine sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, other opioids, alcohol). 

Sufentanil Citrate Injection may cause severe bradycardia, severe hypotension including orthostatic hypotension, and syncope. There is increased risk in patients whose ability to maintain blood pressure has already been compromised by a reduced blood volume or concurrent administration of certain CNS depressant drugs (e.g., phenothiazines or general anesthetics). 

Cases of serotonin syndrome, a potentially life-threatening condition, have been reported during concomitant use of Sufentanil Citrate Injection with serotonergic drugs. 

Proper placement of the needle or catheter in the epidural space should be verified before Sufentanil is injected to assure that unintentional intravascular or intrathecal administration does not occur. Unintentional intravascular injection of Sufentanil could result in a potentially serious overdose, including acute truncal muscular rigidity and apnea. 

In patients who may be susceptible to the intracranial effects of CO2 retention (e.g., those with evidence of increased intracranial pressure or brain tumors), Sufentanil Citrate Injection may reduce respiratory drive, and the resultant CO2 retention can further increase intracranial pressure. 

Sufentanil may cause spasm of the sphincter of Oddi. Opioids may cause increases in serum amylase. 

Sufentanil may increase the frequency of seizures in patients with seizure disorders, and may increase the risk of seizures occurring in other clinical settings associated with seizures. 

Sufentanil Citrate Injection may impair the mental or physical abilities needed to perform potentially hazardous activities such as driving a car or operating machinery.

Points of recommendation

To make sure this medicine is safe for you, tell your doctor if you have:

  • If you have an allergy to sufentanil or any other part of sufentanil.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you have any of these health problems: Lung or breathing problems like asthma, trouble breathing, or sleep apnea; high levels of carbon dioxide in the blood; or stomach or bowel block or narrowing.
  • If you are taking any of these drugs: Buprenorphine, butorphanol, nalbuphine, or pentazocine.
  • If you have taken certain drugs used for low mood (depression) like isocarboxazid, phenelzine, or tranylcypromine or drugs used for Parkinson's disease like selegiline or rasagiline in the last 14 days. Taking sufentanil within 14 days of those drugs can cause very bad high blood pressure.
  • If you are taking any of these drugs: Linezolid or methylene blue.

To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.

This medicine has an opioid drug in it. The use of opioid drugs along with a benzodiazepine drug or other drugs that may make you drowsy or slow your actions has led to very bad side effects. Side effects that have happened include slowed or trouble breathing and deaths. Benzodiazepine drugs include drugs like alprazolam, diazepam, and lorazepam. Benzodiazepine drugs are used to treat many health problems like anxiety, trouble sleeping, or seizures. Talk with the doctor.

Many drugs interact with sufentanil and can raise the chance of side effects like deadly breathing problems. Talk with your doctor and pharmacist to make sure it is safe to use sufentanil with all of your drugs.

Do not take with alcohol or products that have alcohol. Unsafe and sometimes deadly effects may happen.

This medicine may raise the chance of seizures in some people, including people who have had seizures in the past. Talk to your doctor to see if you have a greater chance of seizures while taking sufentanil.

If you are 65 or older, use sufentanil with care. You could have more side effects.

This medicine may cause harm to the unborn baby if you take it while you are pregnant. If you are pregnant or you get pregnant while taking sufentanil, call your doctor right away.

Using sufentanil for a long time during pregnancy may lead to withdrawal in the newborn baby. This can be life-threatening. Talk with the doctor.

Tell your doctor if you are breast-feeding or plan to breast-feed. This medicine passes into breast milk and may harm your baby.

Pregnancy level

C


Ask a Pharmacist


User's questions
    No comments yet.