Dsuvia (sufentanil citrate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Sufentanil citrate is a synthetic phenylpiperidine-derivative opiate agonist.
Sufentanil citrate is an opioid agonist with high affinity and selectivity for the micro-opiate receptor in the CNS; the drug reportedly is more selective and binds more tightly to this receptor than fentanyl. Partial occupancy of the micro-receptor by naloxone (an opiate antagonist) has been shown to substantially decrease the analgesic effect of sufentanil.
Sufentanil produces dose-related analgesia; at doses up to 8 mcg/kg, the drug has a potent analgesic effect. Higher doses usually produce substantial CNS depression resulting in hypnosis and anesthesia; however, hypnosis may occur at doses of 1.5 mcg/kg. The analgesic potency of sufentanil appears to be 5-12 times that of fentanyl on a weight basis.
Sufentanil doses of 8 mcg/kg or greater result in EEG patterns indicative of a deep level of anesthesia; the drug induces a shift to the left in EEG amplitude and frequency that is consistent with central anesthetic activity.
Following IV administration, sufentanil has a more rapid onset of action than does morphine or fentanyl. The onset of action of sufentanil as determined by time to unconsciousness (i.e., loss of response to voice command) reportedly ranges from 1.2-3 minutes following total mean doses of 4.9-30 mcg/kg. The mean duration of anesthesia is reportedly 40 minutes following initial doses of 0.4 mcg/kg of sufentanil; the mean duration of anesthesia of additional doses of 0.1 mcg/kg of sufentanil is reportedly 41-44 minutes.
Following a single sublingual administration, sufentanil has a bioavailability of approximately 53% relative to a 1-minute IV sufentanil infusion of 30 mcg. Compared to IV administration, sublingual maximum concentration values were 17-fold lower. The sublingual route of administration of sufentanil avoids intestinal and hepatic first-pass effects.
Following a single dose of sufentanil sublingual tablets, maximum concentrations occur at a median time of 1 hour. After 12 multiple hourly doses over 11 hours, the geometric mean for the AUC within a dosing interval (AUC0-60min) and maximum concentration values were increased by 3.7-fold and 2.3-fold greater compared to single-dose administration, respectively. Steady-state plasma concentrations were achieved after 7 doses.
Distribution of sufentanil injectioninto human body tissues and fluids has not been fully characterized; however, the drug is highly lipophilic and is rapidly and extensively distributed in animals. The drug is approximately 93% bound in plasma in healthy males, mainly to albumin; alpha-, alpha1-, beta-, and gamma-globulins; and alpha1-acid glycoprotein. Plasma concentrations of sufentanil decline rapidly secondary to redistribution and appear to decline in a triphasic manner.
In adults with normal renal and hepatic function, the plasma half-life of sufentanil citrate injectionin the initial (distribution) phase averages 0.72-1.2 minutes, the plasma half-life in the second (redistribution) phase averages 13.7-17 minutes, and the plasma half-life in the terminal (elimination) phase averages 140-158 minutes. The elimination half-life is longer (434 minutes) in neonates but shorter in infants and children (97 minutes), compared with adults (164 minutes). Following a single dose of sufentanil sublingual tablets, the mean terminal half-lfe is 13.4 hours.
The clearance of sufentanil in healthy neonates is approximately one-half that reported in adults and children, and the clearance may be further reduced by up to one-third in neonates with cardiovascular disease.
The major sites of biotransformation of sufentanil are the liver and small intestine via N-dealkylation at the piperidine nitrogen and O-demethylation. The O-demethylated metabolite appears to have about 10% of the analgesic activity of the unchanged drug. Sufentanil and its metabolites are excreted principally in urine and also in feces via biliary elimination; approximately 80% of the administered dose is excreted in urine and feces within 24 hours after administration.
Only 2% of the dose is excreted unchanged in urine and feces.
Generic name: sufentanil citrate
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Dsuvia
Indications
The following indications are listed for Dsuvia:
- Acute Pain
Dosing
Dosage of sufentanil citrate is expressed in terms of sufentanil. Dosage must be carefully adjusted according to body weight, individual requirements and response, physical status and underlying pathologic condition, premedication or concomitant medication(s), the anesthetic(s) being used, and the nature and duration of the surgery.
Sufentanil is administered IV or epidurally, oras sublingual tablets (Dsuvia(R)).
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No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Hypersensitivity to sufentanil.
*Significant respiratory depression (sufentanil sublingual tablets).
*Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment (sufentanil sublingual tablets).
*Known or suspected GI obstruction, including paralytic ileus (sufentanil sublingual tablets).
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse reactions associated with sufentanil citrate injection were respiratory depression, apnea, rigidity, and bradycardia.
The most common adverse reactions (>=2%) associated with sufentanil sublingual tablets were nausea, headache, vomiting, dizziness and hypotension.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of sufentanil citrate injection in children as young as 1 day of age have been documented in a limited number of patients undergoing cardiovascular surgery. Safety and efficacy of sufentanil sublingual tablets in pediatric patients have not been established; use is not recommended in these patients because of the risk of noncompliance with sublingual dosing instructions.
The clearance of sufentanil in healthy neonates is approximately one-half that in adults and children. The clearance rate of sufentanil can be further reduced by up to a third in neonates with cardiovascular disease, resulting in an increase in the elimination half-life.
Prolonged use of opioids during pregnancy may cause neonatal opioid withdrawal syndrome. Data on sufentanil in pregnant women are insufficient to inform a drug-associated risk for major birth defects and miscarriage.
In animal studies, embryolethality and maternal toxicity occurred in rabbits with IV sufentanil administration at 0.9 times the human procedural dose of 30 mcg/kg during organogenesis. Decreased live fetuses and pup survival were noted in rats treated with sufentanil late in gestation and throughout lactation at doses below the human procedural dose. No malformations were observed in either rats or rabbits at doses below the human procedural dose. Sufentanil should be used during pregnancy only when the potential benefits justify the possible risks to the fetus.
Sufentanil injectionis not recommended for use in pregnant women during or immediately prior to labor, when other analgesic techniques are more appropriate. Monitor neonates exposed to opioid analgesics during labor for signs of excess sedation and respiratory depression.
Epidural administration of sufentanil in combination with bupivacaine 0.125% with or without epinephrine is indicated for labor and delivery. Sufentanil is not recommended for IV use or for use of larger epidural doses during labor and delivery because of potential risks to the newborn infant after delivery.
Consider the developmental and health benefits of breastfeeding along with the mother's need for sufentanil and any potential adverse effects on the breastfed infant or from the underlying maternal condition. Monitor infants exposed to sufentanil through breast milk for excess sedation and respiratory depression.
In general, use caution when selecting a dosage for an elderly patient, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy. Titrate the dosage of sufentanil injection slowly in geriatric patients and monitor closely for signs of CNS and respiratory depression. Because the dose of sufentanil sublingual tablets cannot be titrated, monitor geriatric patients closely for signs of CNS and respiratory depression or consider an alternate medication that can be titrated.
Elderly patients may have increased sensitivity to sufentanil. No special population studies in geriatric patients have been performed for sufentanil sublingual tablets. In patients who received sublingual sufentanil, the overall rate of adverse events and most common adverse events tended to increase with age, although vomiting was less common in patients aged >=75 years than in younger patients.
In general, use caution when selecting a dosage for an elderly patient, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy. Titrate the dosage of sufentanil citrate injection slowly in geriatric patients and monitor closely for signs of CNS and respiratory depression. Because the dose of sufentanil sublingual tablets cannot be titrated, monitor geriatric patients closely for signs of CNS and respiratory depression or consider an alternate medication that can be titrated.
ICD codes
No ICD codes are available for this drug.
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Last reviewed · Source: First Databank (FDB) drug data
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