DEXAMETHASONE INTENSOL
Clinical safety rating: avoid
CYP3A4 inducers (eg phenytoin) may decrease efficacy and inhibitors may increase effects Can cause hyperglycemia and adrenal suppression with prolonged use.
Corticosteroid that binds to the glucocorticoid receptor, leading to anti-inflammatory and immunosuppressive effects via inhibition of phospholipase A2, reduction of prostaglandins and leukotrienes, and modulation of gene transcription.
| Metabolism | Primarily hepatic via CYP3A4; metabolites are excreted renally. |
| Excretion | Renal (approximately 65-80% as metabolites, <10% as unchanged drug); biliary/fecal (minor). |
| Half-life | Terminal elimination half-life: 36-54 hours (adults); clinically, biological half-life (duration of HPA axis suppression) is longer (24-72 hours). |
| Protein binding | 77-84%, primarily to albumin and corticosteroid-binding globulin (transcortin). |
| Volume of Distribution | 0.75-1.0 L/kg; indicates extensive tissue distribution with high intracellular penetration. |
| Bioavailability | Oral: 80-90% (immediate-release); IM: approximately 100%. |
| Onset of Action | Oral: 1-2 hours; IV: immediate (within minutes); IM: 2-4 hours. |
| Duration of Action | Duration of anti-inflammatory effect: 18-36 hours; duration of HPA suppression: 24-72 hours after single dose. |
| Molecular Weight | 392.46 |
0.75-9 mg/day orally in divided doses every 6-12 hours; for anti-inflammatory/immunosuppressive effects, initial dose 0.75-9 mg/day; for cerebral edema, 10 mg IV then 4 mg IM/IV every 6 hours.
| Dosage form | CONCENTRATE |
| Renal impairment | No dose adjustment required for GFR >30 mL/min; for GFR 10-30 mL/min, consider dose reduction by 25%; for GFR <10 mL/min, avoid use or reduce dose by 50% due to accumulation of metabolites. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: reduce dose by 75% or consider alternative. |
| Pediatric use | 0.02-0.3 mg/kg/day orally in divided doses every 6-12 hours; maximum 0.5 mg/kg/day; for induction of diuresis in nephrotic syndrome, 2 mg/kg/day. |
| Geriatric use | Initiate at lowest effective dose (e.g., 0.75 mg/day) and titrate slowly; monitor for hyperglycemia, osteoporosis, and fluid retention; avoid prolonged use due to increased risk of adverse effects. |
| 1st trimester | Crosses placenta; associated with increased risk of cleft palate (odds ratio 1.3-3.3) when used in first trimester. Use only if clearly needed. |
| 2nd trimester | Use only if clearly needed; monitor for fetal growth restriction. Adrenal suppression may occur with prolonged use. |
| 3rd trimester | Use only if clearly needed; may cause neonatal adrenal suppression and hypoglycemia if given near term. |
Clinical note
CYP3A4 inducers (eg phenytoin) may decrease efficacy and inhibitors may increase effects Can cause hyperglycemia and adrenal suppression with prolonged use.
| FDA category | Positive |
| Placental transfer | Readily crosses the placenta; metabolized to a lesser extent than prednisolone. Fetal concentrations may reach 10-30% of maternal levels. |
■ FDA Black Box Warning
No FDA black box warning is applicable.
| Common Effects | immunosuppression |
| Serious Effects |
Systemic fungal infectionsHypersensitivity to dexamethasone or any component
| Precautions | Increased risk of infections due to immunosuppression, Adrenal suppression with prolonged use; taper dose when discontinuing, Masking of signs of infection, Exacerbation of fungal infections; avoid in systemic fungal infections, Increased intraocular pressure; monitor in glaucoma patients, Corticosteroid-induced osteoporosis with long-term use, Growth suppression in children, Kaposi sarcoma has been reported; discontinue if diagnosed, Live or live-attenuated vaccines are contraindicated during therapy |
| Food/Dietary | Grapefruit and grapefruit juice may increase dexamethasone levels; avoid concurrent use. High-sodium foods may exacerbate fluid retention; consider a low-sodium diet. Alcohol can increase gastric irritation; limit or avoid. |
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| Breastfeeding |
| Enters breast milk in low concentrations. At maternal doses up to 5 mg/day, amounts are unlikely to cause systemic effects in the infant. Avoid high-dose, prolonged therapy if breastfeeding. |
| Lactation Rating | L2 |
| Teratogenic Risk | First trimester: Increased risk of oral clefts (odds ratio ~3). Second/third trimester: Fetal adrenal suppression, intrauterine growth restriction, low birth weight. Chronic use may cause fetal hypothalamic-pituitary-adrenal axis suppression. |
| Fetal Monitoring | Maternal: Blood glucose, blood pressure, signs of infection, bone density with prolonged use. Fetal: Ultrasound for growth restriction, amniotic fluid volume, and biophysical profile. Neonatal: Observe for adrenal insufficiency. |
| Fertility Effects | No direct impairment. However, treatment of underlying conditions (e.g., autoimmune disorders) may improve fertility. Chronic high doses may disrupt menstrual cycles. |
| Clinical Pearls | Dexamethasone Intensol is a concentrated oral solution (1 mg/mL) for patients who cannot swallow tablets. Due to its high potency, use a calibrated dropper for accurate dosing. Monitor for hyperglycemia, especially in diabetic patients, and for signs of adrenal suppression with prolonged use. Avoid abrupt discontinuation; taper dose. Can cause immunosuppression; watch for infections. |
| Patient Advice | This medication is highly concentrated; measure each dose carefully using the dropper provided. · Take with food or milk to reduce stomach upset. · Do not stop taking this medication suddenly without consulting your doctor; the dose may need to be tapered. · Report any signs of infection (fever, sore throat), mood changes, or vision problems to your healthcare provider. · Carry a medical ID card indicating you are taking corticosteroids. |