prednisolone; deltahydrocortisone; metacortandralone (Pred Forte, AK-Pred, Inflamase, Pediapred, Pred Mild, Prelone, Flo-Pred, Veripred 20)
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Introduction
Ophthalmic: (Pred Forte, AK-Pred)
Indications
- adrenal insufficiency
- graft rejection
- acute alcoholic hepatitis associated with encephalopathy
- congenital anomalies
- edema
- cerebral edema
- laryngeal edema
- angioneuroatic edema
- pulmonary edema
- lung disease
- otitis externa
- eye inflammation
- inflammatory infections
- trichinosis
- Loeffler's syndrome
- pneumosystis pneumonia
- Bell's palsy
- musculoskeletal inflammation
- dermatitis
- autoimmune disease
- nephrotic syndrome
- hypersensitivity
- serum sickness
- nasal polyp
- allergic rhinitis
- malignant neoplasms
Dosage
Tabs: 5 mg.
Liquid: 5 mg/5 mL (120 mL), 15 mg/5 mL.
Flo-Pred: viscous, 'spill-proof', oral prednisolone liquid
- ophthalmic
- 1-2 drops every hour during the day & every 2 hours at night
- after response is obtained, 1 drop every 4 hours
- post-operative inflammation
Suspension: (acetate): 0.12% (5 mL, 10 mL) & 1% (5 mL, 10 mL). (phosphate): 0.125% (5 mL), 1% (5 mL).
Storage
- prednisolone acetate oral suspension
Pharmacokinetics
- unlike prednisone, prednisolone does not require activation by hepatic enzymes for activity.
- protein binding 65-91%
- metabolized in the liver by cyt P450 3A4 & in other tissues to inactive compounds
- metabolites eliminated in the urine as conjugates (sulfate, glucuronate)
- elimination 1/2life 3.6 hours
- biological 1/2life is 18-36 hours
- prednisolone is inactivated by the placenta
elimination via liver
1/2life = 3.6 hours
protein binding = 65-91 %
Adverse effects
- common (> 10%)
- less common (1-10%)
- uncommon (< 1%)
- seizures, mood swings, headache, skin atrophy, hyperpigmentation, acne, amenorrhea, sodium & water retention, Cushing's syndrome, hyperglycemia, bone growth suppression, abdominal distension, ulcerative esophagitis, pancreatitis, muscle wasting, hypersensitivity
- ophthalmic agent
Drug interactions
- any drug that inhibits cyt P450 3A4 may increase levels of prednisolone
- any drug that induces cyt P450 3A4 may diminish levels of prednisolone
- drug interaction(s) of methotrexate with biological response modifier
- drug interaction(s) of glucocorticoids with warfarin
- drug interaction(s) of NSAIDs with glucocorticoid
Laboratory
Mechanism of action
- intermediate-potency glucocorticoid
- some mineralocorticoid activity
- mineralocorticoid/glucocorticoid activity (1/156)[7]
More general terms
Additional terms
- cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
- methylprednisolone (Medrol, Solu-Medrol, Depo-Medrol)
- prednisolone/sulfacetamide (Blephamide, Cetapred, Metimyd)
Component of
- prednisolone/trimeprazine
- miconazole/nitrate/polymixin b/prednisolone
- desmoplakin/prednisolone
- prednisolone/sodium phosphate/sulfacetamide
- neomycin/polymixin b/prednisolone
- gentamicin/prednisolone
- prednisolone/sulfacetamide (Blephamide, Cetapred, Metimyd)
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Prescriber's Letter 16(1): 2009 Comparison of Oral Prednisolone Formulations Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=250106&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 5.0 5.1 Deprecated Reference
- ↑ 6.0 6.1 Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=300622&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 7.0 7.1 Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015