KENALOG-40
Clinical safety rating: caution
Comprehensive clinical and safety monograph for KENALOG-40 (KENALOG-40).
Corticosteroid with anti-inflammatory, immunosuppressive, and antiproliferative properties; suppresses cytokine production, inhibits phospholipase A2, reduces prostaglandin and leukotriene synthesis, and stabilizes lysosomal membranes.
| Metabolism | Primarily hepatic via CYP3A4; undergoes reduction and conjugation to inactive metabolites. |
| Excretion | Primarily hepatic metabolism followed by renal excretion of inactive metabolites. Less than 5% excreted unchanged in urine. Biliary/fecal elimination accounts for approximately 15-20% of total clearance. |
| Half-life | Terminal elimination half-life is approximately 2 to 3 hours after IV administration, but due to the triamcinolone acetonide suspension formulation, the effective half-life following intramuscular or intra-articular administration is prolonged to 2-3 weeks due to slow dissolution from the injection site. |
| Protein binding | 68-80% bound to albumin and corticosteroid-binding globulin (transcortin). |
| Volume of Distribution | Approximately 1.4 L/kg. The large Vd indicates extensive tissue distribution, particularly into adipose tissue and muscle. |
| Bioavailability | Intramuscular: 100% (by definition for IM); Intra-articular: 100% (local); Oral: not applicable (not available orally for systemic use; triamcinolone acetonide has low oral bioavailability due to first-pass metabolism). |
| Onset of Action | Intramuscular: 24-48 hours; Intra-articular: 1-2 days; Local injection: within 24 hours. Systemic effects may be delayed up to 1 week after IM administration. |
| Duration of Action | Intramuscular: 2-3 weeks; Intra-articular: 3-4 weeks (up to 2 months for large joints). Duration depends on dose, injection site, and individual response. |
| Molecular Weight | 434.5 Da |
Intra-articular injection: 10-40 mg for large joints, 5-15 mg for medium joints, 2.5-5 mg for small joints. Intralesional injection: 2.5-5 mg per lesion. Intramuscular injection: 40-80 mg once monthly. Not for IV or subcutaneous use.
| Dosage form | INJECTABLE |
| Renal impairment | No adjustment required for GFR >10 mL/min. In ESRD (GFR<10 mL/min), consider alternative therapy due to increased risk of fluid retention and hypertension. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Use with caution; consider reduced dose of 25-50% of standard. Child-Pugh C: Avoid due to risk of severe side effects; alternative therapy recommended. |
| Pediatric use | Not recommended for children under 1 year. For older children: 0.5-2 mg/kg intramuscularly every 1-4 weeks, up to max 60 mg. Intra-articular doses: 5-15 mg for large joints, 2.5-5 mg for medium joints. Intralesional: 1-2.5 mg per lesion. |
| Geriatric use | Use lowest effective dose due to increased risk of osteoporosis, glucose intolerance, and immunosuppression. Typical starting dose: 25-50% of adult dose; monitor closely for adverse effects. |
| 1st trimester | Corticosteroids cross the placenta. Use only if potential benefit justifies risk to fetus. Studies suggest increased risk of orofacial clefts when used during first trimester. |
| 2nd trimester | Use with caution; associated with potential for intrauterine growth restriction and adrenal suppression in the fetus. |
| 3rd trimester | Use may cause neonatal adrenal suppression; avoid prolonged use near term. |
Clinical note
Comprehensive clinical and safety monograph for KENALOG-40 (KENALOG-40).
| Placental transfer | Corticosteroids cross the placenta; triamcinolone acetonide has moderate placental transfer. The degree is less than prednisolone but greater than dexamethasone due to placental enzyme activity. |
| Breastfeeding | Triamcinolone acetonide is excreted into breast milk in low amounts. High doses or prolonged use may affect the infant's adrenal function. Consider using the lowest effective dose for the shortest duration. |
■ FDA Black Box Warning
Triamcinolone acetonide injectable suspension should not be administered intravenously. Systemic corticosteroids are not approved for epidural or intrathecal administration; serious neurologic events, including spinal cord infarction, paraplegia, and death, have been reported with such routes. Intramuscular administration of triamcinolone is not recommended for children under 2 years of age.
| Serious Effects |
Hypersensitivity to triamcinolone acetonide or any component of the formulationSystemic fungal infectionsIntrathecal administrationAdministration via any route except intramuscular, intra-articular, intrabursal, intralesional, or topical
| Precautions | Increased risk of infections; may mask signs of infection, Adrenal suppression particularly with high doses or prolonged use; taper slowly, Cushing's syndrome with prolonged use, Osteoporosis risk with long-term use, Gastrointestinal perforation especially in patients with inflammatory bowel disease or diverticulitis, Kaposi sarcoma reported in patients on corticosteroid therapy, Myopathy and muscle wasting, Ocular effects: cataracts, glaucoma, increased intraocular pressure, Behavioral and mood disturbances (e.g., euphoria, depression, psychosis), Fluid and electrolyte disturbances (e.g., hypertension, hypokalemia) |
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| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Corticosteroids such as triamcinolone acetonide (Kenalog-40) are associated with an increased risk of orofacial clefts when administered during the first trimester. Use during pregnancy should be avoided unless the benefit clearly outweighs the risk. Second and third trimester exposure may increase the risk of fetal growth restriction, adrenal suppression, and preterm birth. The drug crosses the placenta and can cause fetal hypothalamic-pituitary-adrenal axis suppression. |
| Fetal Monitoring | Monitor maternal blood glucose and blood pressure regularly due to corticosteroid effects. Assess fetal growth via ultrasound in second and third trimesters due to risk of intrauterine growth restriction. Evaluate newborn for signs of adrenal suppression, such as hypoglycemia, lethargy, or poor feeding. |
| Fertility Effects | Systemic corticosteroids may impair fertility by causing menstrual irregularities, ovulatory dysfunction, or suppression of gonadotropin secretion. Triamcinolone acetonide may have similar effects, particularly with prolonged high-dose use. |
| Food/Dietary | No specific food restrictions. However, corticosteroids can cause salt and water retention; patients with hypertension or heart failure should avoid high-sodium foods. May increase appetite and weight gain; advise balanced diet. Grapefruit juice may increase systemic exposure of some corticosteroids (though data limited for triamcinolone); caution with excessive grapefruit intake. Limit alcohol as it may increase risk of gastrointestinal bleeding. |
| Clinical Pearls | Kenalog-40 (triamcinolone acetonide injectable suspension) is a long-acting corticosteroid. Avoid intra-articular injection into unstable joints or joints with infection. Do not inject directly into tendons; risk of tendon rupture. Use caution in patients with diabetes mellitus (may increase blood glucose), tuberculosis, or ocular herpes simplex. Intra-articular injections may cause temporary flare of pain (post-injection flare) within 24-48 hours. Limit frequency of intra-articular injections to every 3-4 weeks. Do not use for epidural injection due to risk of rare but serious neurological events. Sterile technique mandatory to prevent iatrogenic infection. |
| Patient Advice | This medication is a corticosteroid that reduces inflammation and suppresses the immune system. · Do not receive live vaccines while on this medication unless approved by your doctor. · Report any signs of infection (fever, sore throat, pain at injection site) or sudden joint pain/swelling after injection. · If you have diabetes, monitor blood glucose closely; this drug may increase blood sugar. · Avoid abrupt discontinuation after long-term use; dose must be tapered under doctor's supervision. · Protect skin from sun exposure; increased susceptibility to bruising and skin thinning. · Inform all healthcare providers that you are receiving corticosteroid therapy. · Do not drive or operate machinery if you experience dizziness or blurred vision after injection. |