DEXTENZA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DEXTENZA (DEXTENZA).
Dexamethasone is a corticosteroid with glucocorticoid activity that binds to the glucocorticoid receptor, leading to inhibition of inflammatory mediators such as prostaglandins and leukotrienes, and suppression of immune cell migration and activation.
| Metabolism | Primarily hepatic via CYP3A4; dexamethasone is a substrate of CYP3A4 and induces CYP3A4 and P-glycoprotein. |
| Excretion | Dextenza (dexamethasone ophthalmic insert) is administered intracanalicularly; systemic absorption is minimal. Following release into the tear film, the drug is primarily eliminated via nasolacrimal drainage and subsequent gastrointestinal absorption with hepatic metabolism. Renal excretion accounts for <5% of the dose as unchanged drug; biliary/fecal elimination is negligible. |
| Half-life | The terminal elimination half-life of dexamethasone from plasma after systemic absorption is approximately 3-4 hours. However, Dextenza provides sustained local delivery to the ocular surface; the insert releases dexamethasone over 30 days, with therapeutic levels maintained throughout. |
| Protein binding | Dexamethasone is approximately 77-80% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | The apparent volume of distribution (Vd) for dexamethasone is approximately 0.75 L/kg, indicating distribution into total body water and tissues. Locally, the insert concentrates drug at the ocular surface. |
| Bioavailability | Bioavailability after intracanalicular administration is high at the target site (ocular surface) due to direct release. Systemic bioavailability is negligible (less than 5%), as the drug is primarily retained locally and eliminated via nasolacrimal drainage. |
| Onset of Action | After intracanalicular placement, onset of clinical effect (reduction of ocular inflammation and pain) is observed within 24-48 hours as dexamethasone is released into the tear film. |
| Duration of Action | Each insert delivers dexamethasone continuously for up to 30 days, providing sustained anti-inflammatory and analgesic effects. The insert dissolves over time, with complete resorption typically occurring within 30 days. |
| Molecular Weight | 392.46 |
Insert 0.4 mg intracanalicularly (into the lacrimal punctum) as a single dose; releases dexamethasone over 30 days.
| Dosage form | INSERT |
| Renal impairment | No dose adjustment required based on renal function. |
| Liver impairment | No specific guidelines; use with caution in severe hepatic impairment. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment; use with consideration for age-related ocular conditions. |
| 1st trimester | No adequate studies in pregnant women; animal studies have shown fetal harm. Use only if potential benefit justifies potential risk to fetus. |
| 2nd trimester | No adequate studies; consider risk of systemic corticosteroid exposure. Use only if clearly needed. |
| 3rd trimester | Avoid near term due to potential for neonatal adrenal suppression. |
Clinical note
Comprehensive clinical and safety monograph for DEXTENZA (DEXTENZA).
| Placental transfer | Dexamethasone crosses the placenta; limited data for ophthalmic route but systemic absorption minimal. |
| Breastfeeding | Systemic absorption is minimal, but caution is advised. Consider risk of infant exposure to corticosteroids. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to dexamethasone or any componentActive ocular infection (e.g., fungal, viral, bacterial) without concurrent therapyCorneal epithelial defects or ulceration
| Precautions | May increase intraocular pressure; monitor in patients with glaucoma., May delay wound healing., May increase risk of secondary ocular infections, including fungal infections., Use with caution in patients with corneal thinning or perforation., Systemic effects possible with prolonged use. |
| Food/Dietary | No specific food interactions with this drug. |
| Clinical Pearls |
Loading safety data…
| L3 - Moderately Safe |
| Teratogenic Risk | Corticosteroids are known teratogens in animal studies. Dextenza (dexamethasone ophthalmic insert) has limited systemic absorption, but fetal risk cannot be completely excluded. Use during pregnancy only if potential benefit justifies potential risk to the fetus. Preclinical data suggest increased risk of cleft palate and intrauterine growth restriction with systemic corticosteroids in pregnancy. |
| Fetal Monitoring | Monitor intraocular pressure if used for more than 10 days. In pregnancy, routine prenatal care, fundal height measurements, and fetal growth assessment via ultrasound if prolonged use. Monitor for signs of corticosteroid adverse effects such as elevated blood pressure, blood glucose, and weight gain. |
| Fertility Effects | No specific fertility studies with Dextenza. Systemic corticosteroids may affect ovulation and menstrual cycle regularity. Corticosteroids may suppress hypothalamic-pituitary-adrenal axis. Use with caution in women attempting conception. |
| DEXTENZA (dexamethasone ophthalmic insert) is a corticosteroid indicated for postoperative ocular inflammation and pain. It is inserted into the inferior canaliculus and releases dexamethasone over 30 days. Avoid use in patients with active ocular infections or corneal epithelial defects. Monitor for elevated intraocular pressure (IOP) and posterior subcapsular cataract formation. Instruct patients to avoid rubbing the eye to prevent dislodging the insert. |
| Patient Advice | Do not rub or touch the eye, as this may dislodge the insert. · The insert may be felt in the eye but should not cause pain; report any severe discomfort. · Avoid swimming or getting water in the eye while the insert is in place. · Continue prescribed eye drops as directed; the insert does not replace other medications. · Seek immediate medical attention if you experience vision changes, eye pain, or signs of infection. |