prednisolone(redirected from Orapred)
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prednisolone sodium phosphate
Pharmacologic class: Corticosteroid (intermediate-acting)
Therapeutic class: Anti-inflammatory, immunosuppressant
Pregnancy risk category C
Exerts potent anti-inflammatory (glucocorticoid) and weak sodium-retaining (mineralocorticoid) activity. Glucocorticoid activity causes profound and varied metabolic effects.
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.
• 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)
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).
☞ 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.
☞ In systemic therapy, don't discontinue drug abruptly, even if inhaled steroid is added.
• Know that additional corticosteroids are needed during stress or trauma.
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, thrombo-embolism, 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
Metabolic: sodium and fluid retention, hypokalemia, hypocalcemia, hyper-glycemia, decreased carbohydrate tolerance, growth retardation (in children), diabetes mellitus, cushingoid effects (with long-term use), hypothal-amic-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, bron-chospasm
Skin: urticaria, rash, pruritus, contact dermatitis, acne, striae, poor wound healing, thin fragile skin, bruising, hir-sutism, 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
Drug-drug. Amphotericin B, mezlocillin, piperacillin, thiazide and loop diuretics, ticarcillin: additive hypokalemia Anticholinesterase drugs: decreased anticholinesterase effect (when prednisolone is used for myasthenia gravis)
Aspirin, other nonsteroidal anti-inflammatory drugs: increased risk of GI discomfort and bleeding
Cardiac glycosides: increased risk of digitalis toxicity due to hypokalemia
Cyclosporine: therapeutic benefits in organ transplant recipients, but with increased risk of toxicity
Erythromycin, indinavir, itraconazole, ketoconazole, ritonavir, saquinavir: increased prednisolone blood level and effects
Hormonal contraceptives: impaired metabolism and increased effects of prednisolone
Isoniazid: decreased isoniazid blood level
Live-virus vaccines: decreased antibody response to vaccine, increased risk of adverse effects
Oral anticoagulants: reduced anticoagulant requirement, opposition to anticoagulant action
Phenobarbital, phenytoin, rifampin: decreased prednisolone efficacy Salicylates: reduced salicylate blood level
Somatrem: inhibition of somatrem's growth-promoting effects
Theophylline: altered pharmacologic effects of either drug
Skin tests: suppressed results
Drug-diagnostic tests. Calcium, potassium, thyroid 131I uptake, thyroxine, tri-iodothyronine: decreased levels
Cholesterol, glucose: increased levels Nitroblue tetrazolium test for bacterial infection: false-negative result
Skin tests: suppressed results
Drug-herbs. Alfalfa: activation of quiescent systemic lupus erythematosus
Echinacea: increased immune-stimulating effects
Ephedra (ma huang): decreased drug blood level
Ginseng: potentiation of immunomodulating effect
Licorice: prolonged drug activity
Drug-behaviors. Alcohol use: increased risk of gastric irritation and GI ulcers
• 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.
☞ Monitor 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.
• 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-the-counter 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.
prednisolone/pred·nis·o·lone/ (pred-nis´ah-lōn) a synthetic glucocorticoid derived from cortisol, used in the form of the base or the acetate, sodium phosphate, or tebutate ester in replacement therapy for adrenocortical insufficiency, as an antiinflammatory, and as an immunosuppressant.
prednisoloneA semisynthetic corticosteroid drug derived from the natural steroid hormone cortisol and used in the treatment of a wide range of inflammatory disorders. Prednisolone may be given by mouth or injection, but many preparations are formulated for application to the skin or the eyes or ears and the drug may also be given as an enema. The drug is on the WHO official list. Brand names are Deltacortril, Deltastab, Minims prednisolone, Precortisyl Forte, Pred Forte, Predenema, Predfoam, Prednesol, and Predsol.
glucocorticoidsthe group of corticosteroid hormones (mainly cortisol syn hydrocortisone, of which cortisone is the precursor) produced by the adrenal cortex, under the control of adrenocorticotrophic hormone (ACTH) from the anterior pituitary. Their major actions on nutrient metabolism have the net effect of promoting glucose and free fatty acid availability as fuels. Also vital for normal cellular processes as diverse, for example, as excitation-contraction coupling and the health of connective tissues. Synthetic steroids such as prednisolone and dexamethasone have similar actions and are used in the treatment of, for example, asthma and rheumatic conditions. Banned in sport due to their powerful anti-inflammatory action and effect of producing euphoria and masking pain. (Not to be confused with anabolic steroids). See also adrenal glands, hormones; Table 1.
|Site of production||Name of hormone||Main targets||Involved in regulating:||Secretion controlled by:|
|Hypothalamus||Releasing and inhibiting hormones||Anterior pituitary (via local blood vessels)||Secretion of anterior pituitary hormones||Other brain regions; feedback re regulated hormones and their actions|
|Neurohormones released from posterior pituitary:|
|Oxytocin||Uterus, breasts||Labour and lactation||Afferent information from target organs|
|Antidiuretic hormone (ADH, vasopressin)||Kidneys||Water loss: ECF volume and osmolality||Hypothalamic osmoreceptors|
|Anterior pituitary||(Human) growth hormone (H)GH||Most cells||Growth and metabolism||Hypothalamic releasing and inhibiting hormones via local blood vessels|
|Thyroid-stimulating (TSH)||Thyroid gland||Thyroid secretions|
|Gonadotrophins||Ovary or testis||Germ cell maturation and hormone secretions|
|Adrenocorticotrophic (ACTH)||Adrenal cortex||Cortisol secretion|
|Pineal body||Melatonin||Widespread, including brain, thymus, etc.||Hypothalamus; varying light input from retina|
|Parathyroids||Parathormone||Bone, kidneys, gut||ECF [Ca2+]|
|Medulla||Heart, smooth muscle, glands||Cardiovascular and metabolic adjustments to activity and stress||Sympathetic nervous system|
|Atrial wall||Atrial natriuretic hormone||Kidneys||Blood volume; increases sodium (therefore also water) loss in urine||Stretch of atrial wall by venous pressure|
|Gonads: Testis||Androgens (mainly testosterone)||Genitalia and other tissues||Reproductive function and sex characteristics||Anterior pituitary gonadotrophins|
|Ovary||Uterus, breasts and other tissues||Menstrual cycle, pregnancy, lactation|
|Pancreas||Blood levels, storage and cellular uptake of nutrients, notably glucose, but also proteins and fats||Blood levels of nutrients; autonomic nervous system; other gastrointesinal hormones|
|Stomach||Gastrin||Gastric acid-secreting cells||Gastrointestinal functions: motility, digestive juices and other secretions||Local chemical and mechanical factors in the alimentary tract|
|Small intestine||Several GI functions including bile flow, pancreatic enzyme and exocrine secretions||Ingestion of food, distension of GI tract|