Triamcinolone
Triamcinolone
Generic Name
Triamcinolone
Mechanism
Triamcinolone is a synthetic glucocorticoid that exerts its therapeutic effects by
• Binding to cytoplasmic glucocorticoid receptors → complex translocates to the nucleus.
• Modulating gene transcription: up‑regulates anti‑inflammatory proteins (annexin‑1, lipocortin) and down‑regulates pro‑inflammatory cytokines (IL‑1, IL‑6, TNF‑α).
• Inhibiting phospholipase A₂ → ↓ arachidonic acid → ↓ prostaglandin & leukotriene synthesis.
• Stabilizing lysosomal membranes → ↓ mast cell and neutrophil degranulation.
These actions reduce edema, vascular permeability, and inflammatory cell recruitment in tissues.
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Pharmacokinetics
| Parameter | Typical Values |
| Absorption | Oral: ~60–70 % (max 2 h). Topical/ocular: ~10–15 % depending on vehicle; intramuscular ~80 % (peak 1–4 h). |
| Distribution | Widely distributed; high protein binding (~70 %). Lipophilic → penetrates skin, mucosa, CNS. |
| Metabolism | Hepatic via CYP3A4, and non‑catalyzed deacetylation. Metabolites are inactive. |
| Elimination | Renal (urine) and biliary routes. Half‑life ~8–12 h (systemic), much shorter for topical preparations. |
| Drug Interactions | CYP3A4 inhibitors (e.g., ketoconazole) ↑ plasma levels; inducers (e.g., rifampin) ↓ efficacy. High‑dose systemic use may suppress the hypothalamic‑pituitary‑adrenal axis. |
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Indications
| Formulation | Indications |
| Topical (cream, ointment, lotion) |
• Mild‑to‑moderate eczema, psoriasis, dermatitis, post‑operative inflammation. • Insect bites, allergic contact dermatitis. |
| Ocular (ointment, suspension) | • Allergic conjunctivitis, uveitis, keratitis. |
| Intramuscular/I.m. & Subcutaneous | • Localized rheumatic pain, bursitis, tendonitis. |
| Sublingual/Oral (tablet/gel) | • Severe asthma exacerbations, chronic obstructive pulmonary disease (COPD) flare‑ups. |
| Intravenous (IV) | • Severe systemic inflammatory states (e.g., allergic reactions, transplant rejection). |
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Contraindications
- Absolute: hypersensitivity to triamcinolone or any component.
- Relative: systemic fungal infection, uncontrolled diabetes, active viral infections (e.g., HSV), osteoporosis with concurrent potent steroids, pregnancy (B–C, but avoid systemic exposure during first trimester).
- Warnings:
- Systemic use may cause adrenal suppression, myopathy, dyslipidemia, hypertension.
- Topical over large body surface area increases systemic absorption.
- Ophthalmic use caution in patients with glaucoma or ocular hypertension.
- Use cautiously in immunocompromised patients – risk of infection.
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Dosing
| Route | Adult Dose (Typical) | Notes |
| Topical (cream/ointment) | 0.5–2 % twice daily for 1–4 weeks; taper as symptoms resolve. | Avoid occlusion >2 weeks; apply thin layer. |
| Ocular (ointment) | 0.1 % eye drops, 4–6 times/day for 2–4 weeks. | Use after dilating pupil if needed. |
| Intramuscular | 20–80 mg single dose; repeat every 12–24 h for ≤2 days. | Use aseptic technique; rotate sites. |
| Subcutaneous | 5–10 mg daily for 1–2 weeks. | Monitor blood glucose. |
| Oral (tablet/gel) | 10–20 mg/day divided doses; taper over 2–3 weeks. | Assess for adrenal suppression with prolonged use. |
| IV | 4–20 mg/kg/day in divided doses; total daily dose ≤80 mg. | Continuous infusion for severe reactions. |
(Refer to institutional protocols; adjust for pediatric dosing, renal/hepatic impairment, and specific indications.)
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Adverse Effects
- Common
- Exacerbation of diabetes; hyperglycemia.
- Skin atrophy, striae, telangiectasia (topical).
- Hypertension, edema.
- Mood changes, insomnia.
- Localized burning, pruritus (ocular/Topical).
- Serious
- Systemic adrenal suppression → secondary adrenal insufficiency.
- Osteoporosis, osteoporosis‑related fractures (long‑term systemic use).
- Immunosuppression → opportunistic infections (CMV, fungal).
- Peptic ulceration/bleeding (with concurrent NSAIDs).
- Cataract formation, glaucoma (ocular).
- Hypersensitivity/anaphylactic reactions.
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Monitoring
| Parameter | Frequency | Rationale |
| Blood glucose | Baseline; every 2–3 days on >5 mg/day for >1 week | Steroid‑induced hyperglycemia. |
| Blood pressure | Baseline; weekly | Steroids may elevate BP. |
| Weight, BMI | Every visit | Fluid retention & bone health. |
| Bone density (DEXA) | After 6 months >6 mo of systemic use | Osteoporosis risk. |
| Eye exam (glaucoma, cataract) | Baseline; biannual for ocular preparations | Steroid ocular complications. |
| Adrenal axis (ACTH, cortisol) | Before taper >10 mg/day; within 1 week of cessation | Prevent adrenal crisis. |
| Liver function tests | Baseline; every 2 weeks if prolonged therapy | Metabolism via CYP3A4. |
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Clinical Pearls
- “Topical Triage”: Use the lowest effective potency and apply for the shortest duration to avoid systemic absorption. A 0.5 % cream suffices for most mild dermatitis; reserve 2 % cream for recalcitrant lesions.
- “Eye‑Care Hack”: For ocular irritation, instill a drop, wait 2–3 min with eyes closed; this improves penetration and alleviates burning.
- “Systemic Taper”: When tapering systemic dosing, reduce by 5 mg per day after 1 week; avoid abrupt discontinuation to prevent adrenal insufficiency.
- “Contra‑Indication Check”: In diabetics, pre‑screen with HbA1c; if >8 %, consider dose reduction or alternative therapy.
- “Drug Interaction Clue”: Patients on oral contraceptives show increased oral bioavailability of triamcinolone; monitor for breakthrough bleeding.
- “Sublingual Splint”: For oral sore ulcers, keep the gel under the tongue for 10 min before swallowing to reduce gastric irritation.
- “Pediatric Precaution”: In children <5 yrs, limit systemic exposure <1 mg/kg/day; topical use may be at higher concentrations (up to 2 %) but for <5 % of body surface.
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• *This drug card is for educational purposes only. Always verify with up‑to‑date clinical guidelines and institutional protocols.*