Name of the Glucocorticoid Drugs
Glucocorticoids drugs are synthetic versions of naturally occurring steroid hormones produced by the adrenal cortex. They’re widely used in medicine for their powerful anti-inflammatory and immunosuppressive effects
- Prednisolone
- Methyl prednisolone
- Triamcinolone
- Deflazacort
1.Prednisolone
| Prednisolone |
| Availability Oral solution: 5 mg/ml Suspension for injection (acetate): 25 mg/ml, 40 mg/ml, 50 mg/ml Suspension (ophthalmic): 0.12%, 0.125%, 1% Syrup: 5 mg/5 ml, 15 mg/5 ml Tablets: 5 mg Tablets (orally disintegrating, sodium phosphate): 10 mg, 15 mg, 30 mg |
| Indications and dosages ➣ Severe inflammation; immunosuppression Adults: Dosage individualized based on diagnosis, severity of condition, and response. Usual dosage ranges from 5 to 60 mg P.O. (prednisolone) daily in two to four divided doses, or 4 to 60 mg I.M. (acetate) daily in divided doses, or 5 to 50 mg P.O. (sodium phosphate) daily in divided doses. ➣ Acute exacerbation of multiple sclerosis Adults: 200 mg P.O. daily for 1 week, followed by 80 mg every other day for 1 month ➣ Refractory bronchial asthma Children: 1 to 2 mg/kg/day (sodium phosphate) as a single dose or in divided doses; may continue for 3 to 10 days or until symptoms resolve or patient achieves peak expiratory flow rate of 80% of personal best ➣ Nephrotic syndrome in children Children: 60 mg/m2 P.O. (sodium phosphate solution) daily in three divided doses for 4 weeks, then 4 weeks of alternate-day therapy at single doses of 40 mg/m2 ➣ Various allergic conditions and dermatologic, endocrine, GI, hematologic, neoplastic, nervous system, ophthalmic, respiratory, and rheumatic disorders Adults: Variable and individualized depending on condition being treated and patient response. Initially, 10 to 60 mg (ODT) P.O. daily. Children: Variable and individualized depending on condition being treated. Initial dosage range is 0.14 to 2 mg/kg/day P.O. in three or four divided doses. ➣ Steroid-responsive inflammatory eye conditions Adults: In severe cases, initially one to two drops (acetate or sodium phosphate) instilled into conjunctival sac q hour during day and q 2 hours at night. In mild or moderate inflammation or in severe cases that respond favorably, one to two drops q 3 to 12 hours. |
Mechanism of Action
- Binds to intracellular glucocorticoid receptors and suppresses inflammatory and immune responses by:
- Inhibiting neutrophil and monocyte accumulation at inflammation site and suppressing their phagocytic and bactericidal activity
- Stabilizing lysosomal membranes
- Suppressing antigen response of macrophages and helper T cells
- Inhibiting synthesis of inflammatory response mediators, such as cytokines, interleukins, and prostaglandins
Pharmacokinetics
- Protein bound: 65-91% (lower in elderly)
- Peak plasma time: 5 min (IV); 1 hr (PO)
- Extensively metabolized in liver
- Half-life: 3.6 hr (normal renal function); 3-5 hr (end-stage renal disease)
- Excretion: Urine (mainly)
Administration
- Be aware that prednisolone has many different formulations that may be given by various routes: P.O., I.M., or ophthalmic. Before administering, make sure formulation can be given by prescribed route.
- Don’t break ODT tablets.
- Place ODT tablet on tongue and either swallow tablet whole or allow it to dissolve in mouth with or without water.
- Inject I.M. form deep into gluteal muscle. Rotate injection sites.
- Avoid subcutaneous injection. 2In systemic therapy, don’t discontinue drug abruptly, even if inhaled steroid is added.
- Know that additional corticosteroids are needed during stress or trauma
Contraindications
- Hypersensitivity to drug, other corticosteroids, alcohol, bisulfite, or tartrazine (with some products)
- Systemic fungal infections
- Active untreated infections (except in selected patients with meningitis)
- Acute superficial herpes simplex, keratitis, fungal or viral eye diseases, tuberculosis of eye, or after uncomplicated removal of superficial corneal foreign body (ophthalmic use)
- Idiopathic thrombocytopenic purpura (with I.M. use)
- Live-virus vaccines (with immunosuppressive prednisolone dosages)
Precautions Use cautiously in:
- Diabetes mellitus, glaucoma, renal or hepatic disease, hypothyroidism, cirrhosis, diverticulitis, nonspecific ulcerative colitis, recent intestinal anastomoses, inflammatory bowel disease, thromboembolic disorders, seizures, myasthenia gravis, heart failure, hypertension, osteoporosis, ocular herpes simplex, immunosuppression, emotional instability
- Pregnant or breastfeeding patients
- Children younger than age 6 (younger than age 2 when treated for nephrotic syndrome; younger than age 1 month when treated for aggressive lymphomas and leukemias with ODT form).
Adverse reactions
- CNS: headache, nervousness, depression, euphoria, personality changes, psychosis, vertigo, paresthesia, insomnia, restlessness, seizures, meningitis, increased intracranial pressure, hypertrophic cardiomyopathy in premature infants
- CV: hypotension, hypertension, vasculitis, thrombophlebitis, thromboembolism, fat embolism, arrhythmias, heart failure, shock
- EENT: cataracts, glaucoma, visual disturbances, exacerbation of ocular infection, secondary ocular infections, globe perforation at corneal or scleral thinning site, transient stinging or burning of eyes, dry eyes, corneal ulcers, mydriasis (all with ophthalmic use); posterior subcapsular cataracts (especially in children), glaucoma, nasal irritation and congestion, rebound congestion, sneezing, epistaxis, nasopharyngeal and oropharyngeal fungal infections, perforated nasal septum, anosmia, dysphonia, hoarseness, throat irritation (with long-term use)
- GI: nausea, vomiting, abdominal distention, rectal bleeding, dry mouth, esophageal candidiasis, esophageal ulcer, pancreatitis, peptic ulcer
- GU: amenorrhea, irregular menses
- Hematologic: purpura
- Metabolic: sodium and fluid retention, hypokalemia, hypocalcemia, hyperglycemia, decreased carbohydrate tolerance, growth retardation (in children), diabetes mellitus, cushingoid effects (with long-term use), hypothalamic-pituitary-adrenal suppression (with systemic use longer than 5 days), adrenal suppression (with high-dose, long-term use)
- Musculoskeletal: muscle weakness or atrophy, myalgia, myopathy, osteoporosis, aseptic joint necrosis, spontaneous fractures (with long-term use), osteonecrosis, tendon rupture
- Respiratory: cough, wheezing, bronchospasm
- Skin: urticaria, rash, pruritus, contact dermatitis, acne, striae, poor wound healing, thin fragile skin, bruising, hirsutism, petechiae, subcutaneous fat atrophy, urticaria, angioedema
- Other: aggravation or masking of infections, increased or decreased appetite, weight gain (with long-term use), facial edema and erythema, edema, hypersensitivity reaction
Patient monitoring
- Monitor weight, blood pressure, and electrolyte levels.
- Watch for cushingoid effects (moon face, central obesity, buffalo hump, hair thinning, high blood pressure, frequent infections).
- Assess patient for depression and psychosis.
- Monitor blood glucose level carefully in diabetic patient.
- Evaluate for signs and symptoms of infection, which drug may mask or exacerbate. 2Monitor for signs and symptoms of early adrenal insufficiency (fatigue, weakness, joint pain, fever, anorexia, shortness of breath, dizziness, syncope).
- Assess musculoskeletal status for joint, tendon, and muscle pain.
Patient teaching
- Tell patient to take oral dose with food or milk to reduce GI upset.
- Instruct patient to remove ODT tablet from blister just before taking.
- Instruct patient to place ODT tablet on tongue and either swallow tablet whole or allow it to dissolve in mouth with or without water. Caution patient not to cut, split, or break tablet.
- Teach patient to recognize and immediately report cushingoid effects and signs and symptoms of early adrenal insufficiency.
- Advise patient and significant other to immediately report depression or psychosis.
- Explain that drug increases risk of infection. Instruct patient to contact prescriber at first sign of infection.
- Caution patient not to suddenly stop drug (including ophthalmic forms). Instruct him to discuss any changes in therapy with prescriber.
- Tell patient to immediately report bleeding or joint, muscle, tendon, or abdominal pain.
- Inform patient that he may need higher dosage during periods of stress. Encourage him to wear or carry medical identification stating this.
- Tell patient to avoid vaccinations during therapy. Mention that others in household shouldn’t receive oral polio vaccine because they could pass poliovirus to him.
- Caution patient not to take over-thecounter drugs or herbs during therapy.
- Teach patient how to use eye drops. Caution him not to touch dropper tip to eye or any other surface.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above
Nursing Considerations
- Give once-daily doses in the morning to mirror body’s normal cortisol secretion.
- Inspect injectable form for particulates and discoloration before administering.
- For I.M. injection, shake suspension well before withdrawing. Keep in mind that I.M. injections are contraindicated in patients with idiopathic thrombocytopenic purpura.
- For intra-articular injection, attach a 20G to 24G needle to empty syringe, using aseptic technique, so prescriber can remove a few drops of synovial fluid to confirm that needle is in the joint. The aspirating syringe is then exchanged with a prenisolone-filled syringe to inject drug into joint.
- Because prednisolone can produce many adverse reactions, assess patient regularly for evidence of such reactions, including heart failure and hypertension. Also monitor patient’s intake, output, and daily weight.
- Monitor growth pattern in children; prednisolone may retard bone growth.
- Prolonged use may cause hypothalamic pituitary-adrenal suppression
- Be aware that patient may be at risk for emotional instability or psychic disturbance while taking prednisolone, especially if predisposed to them or taking high doses
2.Methyl prednisolone
| Methyl prednisolone |
| Availability Solution for injection: 40 mg, 125 mg, 500 mg, 1 g, 2 g Suspension for injection: 20 mg/ml, 40 mg/ml, 80 mg/ml Tablets: 2 mg, 4 mg, 8 mg, 16 mg, 24 mg, 32 mg |
| Indications and dosages ➣ Diseases and disorders of endocrine system, collagen, skin, eye, GI tract, respiratory system, or hematologic system; neoplastic diseases; allergies; edema; multiple sclerosis; tuberculous meningitis; trichinosis; rheumatic disorders; osteoarthritis; bursitis; localized inflammatory lesions Adults: Methylprednisolone—4 to 160 mg P.O. daily in four divided doses, depending on disease or disorder. Acetate—40 to 120 mg I.M., or 4 to 80 mg by intra-articular or soft-tissue injection, or 20 to 60 mg by intralesional injection (depending on type, size, and location of inflammation); may be repeated at 1 to 5 weeks. Sodium succinate high-dose therapy— 30 mg/kg I.V. over at least 30 minutes. May be repeated q 4 to 6 hours for 48 hours. |
Mechanism of Action
Binds to intracellular glucocorticoid receptors and suppresses inflammatory and immune responses by inhibiting accumulation of neutrophils and monocytes at inflammation sites, stabilizing lysosomal membranes, suppressing the antigen response of macrophages and helper T cells, and inhibiting the synthesis of inflammatory response mediators, such as cytokines, interleukins, and prostaglandins.
Pharmacokinetics
- Peak plasma time: PO: 2.1 ± 0.7 hr; IV (succinate): 0.8 hr
- Extensively metabolized in liver
- Half-life (adults): Oral: 2.5 ± 1.2 hr; IV (succinate): 0.25 ± 0.1 hr
- Dialyzable: Hemodialysis, slightly
- Excretion: Urine (mainly, as metabolites), feces (minimally)
Administration
- As needed and prescribed, give prophylactic antacids to prevent peptic ulcers in patients receiving high doses.
- When methylprednisolone acetate is substituted for oral form, know that I.M. dosage should equal oral dosage and should be given once daily.
- Know that methylprednisolone acetate is not for I.V. use. It may be given I.M. or by intra-articular, intralesional, or soft-tissue injection.
- Be aware that methylprednisolone sodium succinate may be given I.M. or I.V. Reconstitute with bacteriostatic water for injection containing 0.9% benzyl alcohol, per manufacturer’s instructions.
- In long-term methylprednisolone therapy, alternate-day therapy should be considered.
- For direct I.V. injection, inject each 500-mg dose over 2 to 3 minutes or more. For I.V. infusion, further dilute in compatible I.V. solution (such as 5% dextrose, 0.9% sodium chloride, or 5% dextrose in 0.9% sodium chloride injection) and give over 10 to 20 minutes.
- Maintain patient on lowest effective dosage, to minimize adverse effects.
Contraindications
- Hypersensitivity to drug or its component
- Systemic fungal infections
- Use in premature infants (with sodium succinate form, which contains benzyl alcohol)
Precautions:
- Cardiovascular, hepatic, renal, or GI disease; active untreated infections; thromboembolitic tendency; idiopathic thrombocytopenic purpura; osteoporosis; myasthenia gravis; hypothyroidism; glaucoma; ocular herpes simplex; vaccinia or varicella; seizure disorders; metastatic cancer
- Pregnant or breastfeeding patients
- Children
Adverse reactions
- CNS: headache, restlessness, nervousness, depression, euphoria, personality changes, psychoses, vertigo, paresthesias, insomnia, adhesive arachnoiditis, conus medullaris syndrome, increased intracranial pressure, seizures, meningitis
- CV: hypotension, hypertension, arrhythmias, heart failure, shock,fat embolism, thrombophlebitis, thromboembolism EENT: cataracts, glaucoma, increased intraocular pressure, nasal irritation, nasal septum perforation, sneezing, epistaxis, nasopharyngeal or oropharyngeal fungal infection, dysphonia, hoarseness, throat irritation
- GI: nausea, vomiting, abdominal distention, rectal bleeding, dry mouth, anorexia, esophageal candidiasis, esophageal ulcer, peptic ulcer, pancreatitis
- GU: amenorrhea, irregular menses Respiratory: cough, wheezing, bronchospasm
- Metabolic: decreased growth (in children), reduced carbohydrate tolerance, diabetes mellitus, hyperglycemia, sodium and fluid retention, hypokalemia, hypocalcemia, cushingoid state (with long-term use), hypothalamic-pituitary-adrenal suppression (with systemic use beyond 5 days), adrenal suppression (with longterm, high-dose use), acute adrenal insufficiency (with abrupt withdrawal)
- Musculoskeletal: muscle wasting, osteoporosis, osteonecrosis, tendon rupture, aseptic joint necrosis, muscle pain and weakness, steroid myopathy, spontaneous fractures (with long-term use)
- Skin: facial edema, rash, pruritus, urticaria, contact dermatitis, acne, decreased wound healing, bruising, hirsutism, thin and fragile skin, petechiae, purpura, striae, subcutaneous fat atrophy, skin atrophy, acneiform lesions, angioedema
- Other: anosmia, bad taste, increased appetite, weight gain (with long-term use), Churg-Strauss syndrome, increased susceptibility to infection, aggravation or masking of infections, impaired wound healing, atrophy at injection site, local pain and burning, irritation, hypersensitivity reaction
Patient monitoring
- Monitor fluid and electrolyte balance, weight, and blood pressure.
- With long-term or high-dose use, assess for cushingoid effects, such as moon face, central obesity, acne, abdominal striae, hypertension, osteoporosis, myopathy, hyperglycemia, fluid and electrolyte imbalances, and increased susceptibility to infection.
- Check for signs and symptoms of steroid-induced psychosis (delirium, euphoria, insomnia, mood swings, personality changes, and depression).
- Monitor growth and development in children on prolonged therapy.
- Know that therapy beyond 6 months increases risk of osteoporosis. Obtain baseline bone density mass and provide teaching about lifestyle factors (such as weight-bearing exercise, proper diet, moderation of alcohol intake, and smoking cessation) and possible need for calcium, vitamin D, or bisphosphonate therapy.
- With long-term use, withdraw drug gradually.
- After dosage reduction or drug withdrawal, monitor patient for signs and symptoms of adrenal insufficiency
Patient teaching
- Tell patient to take with food to minimize GI upset.
- Advise patient on chronic therapy to have periodic eye exams and to carry medical identification that states he’s taking drug.
- Inform patient that drug increases risk for infection. Urge him to avoid exposure to people with infections such as measles and chickenpox. Tell him to contact prescriber if exposure occurs.
- Advise patient to report unusual weight gain, swelling, muscle weakness, black tarry stools, vomiting of blood, menstrual irregularities, sore throat, fever, or infection.
- Tell patient to immediately report signs or symptoms of adrenal insufficiency (including fatigue, appetite loss, nausea, vomiting, diarrhea, weight loss, weakness, and dizziness) after dosage reduction or drug withdrawal.
- Advise diabetic patient to monitor blood glucose level carefully.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above
Nursing Considerations
- Use cautiously in patients with congestive heart failure or renal insufficiency because sodium retention and edema can occur in patients taking a corticosteroid. Also use cautiously in patients with peptic ulcer, diverticulitis, fresh intestinal anastomoses, or nonspecific ulcerative colitis; these conditions increase risk of perforation during corticosteroid therapy.
- Give methylprednisolone tablets with food to minimize indigestion and GI irritation. For once-daily dosing, give in the morning to coincide with normal cortisol secretion. Expect prescriber to add an antacid or H2- receptor antagonist to regimen.
- Discard parenteral products that are discolored or contain particles. Discard any remaining Depo-Medrol suspension after prescribed dose is drawn from vial.
- Inject I.M. form deep into gluteal muscle. Avoid injecting into deltoid muscle because of risk of subcutaneous atrophy.
- Arrange for low-sodium diet with added potassium, as prescribed.
- Protect patient from falling, especially elderly patient at risk for fractures from osteoporosis.
- Closely monitor patient for signs of infection because drug may mask them or may worsen systemic fungal infections or active latent disease. Be aware that chickenpox and measles can become life-threatening in patients taking a corticosteroid.
- Assess for possible depression or psychotic episodes during therapy.
- Monitor blood glucose level; dosage of insulin or oral antidiabetic drug may need to be adjusted in diabetic patient.
- Be aware that changes in thyroid function such as development of hypothyroidism or hyperthyroidism may require dosage adjustment in chronic therapy because metabolic clearance of methylprednisolone is affected by thyroid activity.
- Avoid skin testing during methylprednisolone therapy because drug may suppress reaction.
3.Triamcinolone
| Triamcinolone |
| Availability triamcinolone acetonide Cream: 0.025%, 0.1%, 0.5% Injectable suspension: 10 mg/ml, 40 mg/ml Lotion: 0.025%, 0.1% Ointment: 0.025%, 0.1%, 0.5% Suspension: 55 mcg/metered spray triamcinolone hexacetonide Injectable suspension: 5 mg/ml, 20 mg/ml |
| Indications and dosages ➣ Allergic rhinitis Adults and children older than age 12: 220 mcg (two sprays of acetonide suspension) in each nostril daily. When maximum benefit has been achieved and symptoms have been controlled, reduce dosage to 110 mcg/day (one spray in each nostril daily). Children ages 6 to 12: Initially, 110 mcg (two sprays of acetonide suspension) as one spray in each nostril once daily. Use 220 mcg (two sprays in each nostril) daily in children not responding adequately to 110 mcg daily. Children ages 2 to 5: Recommended and maximum dosage is 110 mcg as one spray in each nostril once daily. ➣ Severe inflammation; immunosuppression Adults and children older than age 12: 60 mg (acetonide) I.M. at 6-week intervals. For intralesional or sublesional use, 1 mg at each injection site, repeated one or more times weekly; for intra-articular, intrasynovial, or softtissue injection, 2.5 to 40 mg, repeated when symptoms recur. Or 0.5 mg/square inch of affected skin (hexacetonide) by intralesional or sublesional injection or 2 to 20 mg by intraarticular injection; may repeat at 3- to 4-week intervals. Children ages 6 to 12: 0.03 to 0.2 mg/kg or 1 to 6.25 mg/m2 I.M. at intervals of 1 to 7 days ➣ Corticosteroid-responsive dermatoses Adults and children older than age 12: Apply cream, ointment, or lotion sparingly to affected area two to four times daily |
Mechanism of Action
- Inhibits the release of prostaglandins and leukotrienes, thus reducing immediate and late-phase allergic responses in chronic asthma. Triamcinolone also:
- Decreases peribronchial edema and mucus secretion by inhibiting the binding of allergens to immunoglobulin E antibodies on the surface of mast cells, thereby inactivating the release of chemotactic substances
- Decreases inflammation by interfering with leukocyte adhesion to capillary walls
- Inhibits the release of leukocytic acid hydrolases, preventing macrophage accumulation at the infection site
- Inhibits histamine and kinin release, preventing the formation of scar tissue.
Pharmacokinetics
- Bioavailability: Complete with intra-articular injection
- Protein bound: 68%
- Metabolized in liver
- Half-life: Plasma, 2-3 hr; biologic, 18-36 hr
- Renal clearance: 9.5 mL/min
- Excretion: Urine (40%), feces (60%)
Contraindications
- Hypersensitivity to drug, tartrazine, chlorofluorocarbon propellants, alcohol, propylene glycol, or polyethylene glycol
- Systemic fungal infections (parenteral use)
- Idiopathic thrombocytopenic purpura (I.M. use)
- Administration of live-virus vaccines (with immunosuppressant doses of triamcinolone)
Precautions :
- Active untreated infection, systemic infection, immunosuppression, hypertension, osteoporosis, diabetes mellitus, glaucoma, renal disease, hypothyroidism, cirrhosis, diverticulitis, nonspecific ulcerative colitis, recent intestinal anastomoses, thromboembolic disorders, seizures, myasthenia gravis, heart failure, ocular herpes simplex, emotional instability
- Pregnant or breastfeeding patients
- Children younger than age 2 (safety not established).
Adverse reactions
- CNS: headache, vertigo, paresthesia, syncope, personality changes, pseudotumor cerebri, seizures
- CV: hypertension, thrombophlebitis, arrhythmias, thromboembolism, heart failure
- EENT: cataract, glaucoma, increased intraocular pressure, exophthalmos, otitis, nasal or sinus congestion, rhinitis, epistaxis, sneezing, dry mucous membranes, pharyngitis, throat discomfort
- GI: nausea, vomiting, dyspepsia, abdominal distention or pain, peptic ulcer, ulcerative esophagitis, oral candidiasis, dry mouth, pancreatitis
- GU: cystitis, urinary tract infection, glycosuria, menstrual irregularities, vaginal candidiasis Metabolic: fluid retention, hypernatremia, hypokalemia, hyperglycemia, hypocalcemia, decreased growth (in children), carbohydrate intolerance, exacerbation of latent diabetes mellitus, cushingoid appearance (moon face, buffalo hump), hypokalemic alkalosis, acute adrenal insufficiency (with abrupt withdrawal or acute stress in long-term use)
- Musculoskeletal: muscle weakness; steroid myopathy; loss of muscle mass; myalgia; bursitis; tenosynovitis; osteoporosis; fractures; aseptic necrosis; with intra-articular injection—osteonecrosis, tendon rupture, post-injection flare
- Respiratory: cough, wheezing, chest congestion
- Skin: delayed wound healing; thin and fragile skin; petechiae; bruising; with topical use—local eruptions, pruritus, hypopigmentation or hyperpigmentation, scarring, stinging, skin maceration, secondary infection, cutaneous or subcutaneous atrophy, diaphoresis, facial erythema
- Other: toothache, weight gain, fever, pain, voice alteration, hypersensitivity reaction
Patient monitoring
- Monitor respiratory status. Watch for worsening signs and symptoms.
- With long-term use, assess for adverse endocrine and musculoskeletal reactions.
- Monitor carefully for signs and symptoms of infection, which drug may mask.
Patient teaching
- Teach patient correct use of drug. Make sure he has received manufacturer’s patient information sheet.
- Inform patient that drug can affect many body systems. Urge him to report serious adverse effects promptly.
- Tell parents drug may make child more vulnerable to childhood infections, such as chicken pox and measles.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.
Nursing Considerations
- Be aware that high doses of corticosteroids such as trimcinolone aren’t recommended for patients with cranial trauma who don’t require a corticosteroid for another conditions because of increased risk of death.
- Triamcinolone should be administered with extreme caution, if at all, in patients who have active or quiescent tuberculosis infection of the respiratory tract, untreated fungal or bacterial infection, systemic viral or parasitic infection, or ocular herpes simplex because this drug can make these infections worse.
- Give oral form of triamcinolone with meals to minimize GI distress.
- Use calibrated device to measure liquid doses.
- If necessary, crush tablets and mix with food or fluids.
- Shake I.M. suspension thoroughly before drawing it into syringe.
- Be aware that specialized training may be needed to administer parenteral triamcinolone.
- Don’t administer parenteral forms of triamcinolone I.V.
- Be aware that triamcinolone may reactivate tuberculosis in patients who have a history of it.
- Monitor patients, especially infants, closely for gasping syndrome because parenteral triamcinolone contains benzyl alcohol. Exposure to high doses may result in toxicity evidenced by life-threatening hypotension and metabolic acidosis
- Be aware that, although rare, bone mineral density loss and osteoporosis may occur, which may increase risk of fractures, especially in patients on prolonged triamcinolone therapy
5.Deflazacort
| Deflazacort |
| Availability Tablet 6mg,18mg,30mg,36mg oral suspension 22.75mg/mL |
| Indications and dosages Duchenne Muscular Dystrophy 0.9 mg/kg/day PO qDay |
Mechanism of Action
Corticosteroid prodrug, whose active metabolite, 21-desDFZ, acts through the glucocorticoid receptor to exert anti-inflammatory and immunosuppressive effects
The precise mechanism by which deflazacort exerts its therapeutic effects in patients with DMD is unknown
Pharmacokinetics
- Peak plasma time: ~1 hr (fasting); ~2 hr (high-fat meal)
- Protein bound: 40%
- Rapidly converted to the active metabolite 21-desDFZ by esterases after oral administration
- Excretion: Predominantly urinary (~68% [active metabolite accounts for 18% of this]); elimination is nearly complete by 24 hr post dose
Side effects
Increased appetite, Weight gain, Abdominal pain, Mood changes, Cushingoid syndrome, Excessive hair growth on face, Central obesity, Polyuria, Constipation, Irritability, Fever, Back pain, Erythema (skin redness), Rash, Nausea, Nosebleeds, Stretch marks
Contraindications
Hypersensitivity to or any of the ingredients. Patients receiving live virus immunization.
Precautions & Warnings
- Cardiac disease or congestive heart failure (except in the presence of active rheumatic carditis), hypertension, thromboembolic disorders. Glucocorticoids can cause salt and water retention and increased excretion of potassium. Dietary salt restriction and potassium supplementation may be necessary.
- Gastritis or oesophagitis, diverticulitis, ulcerative colitis if there is the probability of impending perforation, abscess or pyogenic infections, fresh intestinal anastomosis, active or latent peptic ulcer.
- Diabetes mellitus or family history, osteoporosis, myasthenia gravis, renal insufficiency.
- Emotional instability or psychotic tendency, epilepsy.
- Previous corticosteroid-induced myopathy.
- Liver failure.
- Hypothyroidism and cirrhosis, which may increase the glucocorticoid effect.
- Ocular herpes simplex because of possible corneal perforation.
REFERENCES
- Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
- McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
- April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
- Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
- Nursebro.com, Search – Nursebro
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