DSUVIA
Clinical safety rating
cautionComprehensive clinical and safety monograph for DSUVIA (DSUVIA).
Selective, high-affinity agonist at the mu-opioid receptor, resulting in analgesia via activation of G-protein coupled inwardly rectifying potassium channels and inhibition of voltage-gated calcium channels in the central nervous system.
| Metabolism | Primarily metabolized by CYP3A4 and CYP3A5 to fentanyl and other inactive metabolites; also undergoes metabolism by amide hydrolysis. |
| Excretion | Primarily renal elimination of metabolites; unchanged drug accounts for <1% of the dose. Fecal excretion is minimal. Total recovery: ~70% in urine, ~20% in feces. |
| Half-life | Terminal elimination half-life is approximately 23.4 hours (range 17–30 h), supporting once-daily dosing. Due to rapid redistribution, clinical effects may wane before elimination is complete. |
| Protein binding | Approximately 7–8% bound to plasma proteins (primarily albumin). Minimal binding ensures high free fraction. |
| Volume of Distribution | Mean Vd is approximately 1.5 L/kg, indicating extensive extravascular distribution. The large Vd reflects rapid and widespread tissue uptake. |
| Bioavailability | Sublingual: 100% bioavailable (systemic). Oral ingestion (swallowing) reduces bioavailability due to first-pass metabolism; for optimal effect, must be administered sublingually. |
| Onset of Action | Sublingual: 5–15 minutes to first perceptible analgesia; peak effect at 30–60 minutes. |
| Duration of Action | Analgesic effect lasts 4–6 hours with single sublingual dose, related to redistribution rather than elimination half-life. Duration is dose-dependent and may be prolonged in hepatic impairment. |
| Molecular Weight | 386.55 |
30 mcg sublingual tablet as a single dose; may repeat once after 1 hour if needed. Maximum 2 doses per 24 hours.
| Dosage form | TABLET |
| Renal impairment | No adjustment recommended for mild to moderate impairment (CrCl >=30 mL/min). Avoid use in severe impairment (CrCl <30 mL/min) or ESRD due to lack of data. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh C). Caution in moderate impairment (Child-Pugh B); consider alternative therapy. |
| Pediatric use | Not approved for use in patients under 18 years of age. Safety and efficacy not established. |
| Geriatric use | No specific dose adjustment recommended; use caution due to increased sensitivity to opioids and higher risk of respiratory depression. Consider lower starting doses if opioid-naive. |
| 1st trimester | No adequate human studies; animal studies show no risk in first trimester? Not applicable as DSUVIA (sufentanil sublingual) is not indicated in pregnancy. Avoid use. |
| 2nd trimester | No adequate human studies; animal studies show no risk? Avoid use due to potential fetal opioid dependence/withdrawal. |
| 3rd trimester | Use may cause neonatal opioid withdrawal syndrome; avoid use. Prolonged use may cause respiratory depression in neonate. |
Clinical note
Comprehensive clinical and safety monograph for DSUVIA (DSUVIA).
| Placental transfer | Sufentanil readily crosses the placenta; rapid equilibrium between maternal and fetal circulation. |
| Breastfeeding | Sufentanil is excreted in human milk; use caution. Due to short half-life, minimal exposure is expected, but monitor infant for respiratory depression and sedation. |
| Lactation Rating | L3 - Moderately Safe |
| Teratogenic Risk | Insufficient human data; animal studies show embryo-fetal toxicity at maternal exposures ≥2x MRHD. Avoid in 1st trimester due to risk of neural tube defects; 2nd/3rd trimester risk of fetal opioid dependence and neonatal abstinence syndrome. Not recommended during pregnancy unless benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal respiratory rate, oxygen saturation, sedation level. Fetal heart rate monitoring during prolonged use. Assess for neonatal withdrawal after delivery. |
| Fertility Effects | Animal studies show reduced fertility at high doses; human data insufficient. May cause menstrual irregularities and hormonal changes. |
■ FDA Black Box Warning
WARNING: SERIOUS AND LIFE-THREATENING RISKS FROM USE OF DSUVIA; ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING RESPIRATORY DEPRESSION; ACCIDENTAL EXPOSURE; NEONATAL OPIOID WITHDRAWAL SYNDROME; and RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS.
| Serious Effects |
Hypersensitivity to sufentanil or any componentSignificant respiratory depressionAcute or severe bronchial asthma in an unmonitored settingKnown or suspected gastrointestinal obstruction (including paralytic ileus)Concurrent use of MAO inhibitors or within 14 daysPostoperative pain management in children <18 years (specific to DSUVIA label)
| Precautions | Addiction, abuse, and misuse, Life-threatening respiratory depression, Accidental exposure, Neonatal opioid withdrawal syndrome, Risks from concomitant use with benzodiazepines or other CNS depressants, Severe hypotension, Adrenal insufficiency, Severe injection site reactions (not applicable for this formulation but product-specific: application site reactions) |
| Food/Dietary | Avoid grapefruit and grapefruit juice during treatment as they may increase opioid levels. No other known food interactions. |
| Clinical Pearls | Administer sublingually at the base of the tongue or between the cheek and gum; do not crush or chew; each unit contains a single dose; monitor for respiratory depression, especially in opioid-naïve patients; avoid in patients with severe hepatic impairment. |
| Patient Advice | Place the tablet under the tongue or between your cheek and gum and allow it to dissolve completely; do not swallow, crush, or chew the tablet. · Do not eat or drink anything until the tablet has completely dissolved. · Keep DSUVIA out of reach of children and away from others; accidental use can cause fatal overdose. · Do not stop taking this medication suddenly without talking to your doctor. · Avoid alcohol and other central nervous system depressants while taking DSUVIA. |
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