Prednisone

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Prednisone
Systematic (IUPAC) name
17-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl- 7,8,9,10,12,13,14,15,16,17-decahydro-6H- cyclopenta[a]phenanthrene-3,11-dione
Identifiers
CAS number	53-03-2
ATC code	A07EA03 H02AB07
PubChem	5865
DrugBank	APRD00340
Chemical data
Formula	C21H26O5
Mol. mass	358.428 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	70%
Metabolism	prednisolone (liver)
Half life	1 hour
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C
Legal status	Prescription only
Routes	Oral, Nasal, Rectal, Injection, IV

Prednisone is a synthetic corticosteroid drug that is usually taken orally but can be delivered by intramuscular injection and can be used for a great number of different conditions. It has a mainly glucocorticoid effect. Prednisone is a prodrug that is converted by the liver into prednisolone, which is the active drug and also a steroid.

[edit] Uses

Prednisone is particularly effective as an immunosuppressant, and affects virtually all of the immune system. It can, therefore, be used in autoimmune diseases, inflammatory diseases (such as severe asthma, severe allergies, severe poison ivy dermatitis, systemic lupus erythematosus, ulcerative colitis, rheumatoid arthritis, Bell's Palsy, Crohn's disease, pemphigus and sarcoidosis), various kidney diseases including nephrotic syndrome, and to prevent and treat rejection in organ transplantation. This medicine may also reduce the sex drive. Prednisone has also been used in the treatment of migraine headaches and cluster headaches.

Furthermore, the pharmaceutical industry uses prednisone tablets for the calibration of dissolution testing equipment according to the United States Pharmacopeia (USP).

Intravenous application may be employed for cerebral inflammation, as in the period attacks caused by multiple sclerosis.

[edit] History

Prednisone was invented in the early 1950s when Arthur Nobile at Schering demonstrated that the side-effects of cortisone, such as water retention, high blood pressure and muscle weakness, could be removed by oxidisation of the drug through exposure to microbes. The drug was introduced by Schering in the mid-1960s.

[edit] Dependency

Adrenal suppression occurs if prednisone is taken for longer than 7 days, a condition wherein the body is unable to synthesize natural corticosteroids and becomes dependent on the prednisone taken by the patient. For this reason, prednisone should not be stopped abruptly if taken for longer than seven days; rather the dosage must be reduced slowly. This reduction may be over a few days if the course of prednisone was short, but may take weeks or months if the patient had been on long-term treatment. Abrupt withdrawal may lead to an Addisonian crisis, which may be life-threatening. For those on chronic therapy, alternate-day dosing may preserve adrenal function, thereby reducing side-effects (see "Dosing Considerations").

[edit] Side-effects

Short-term side-effects, as with all glucocorticoids, include high blood glucose levels, especially in patients that already have diabetes mellitus or are on other medications that increase blood glucose (such as tacrolimus), and mineralocorticoid effects such as fluid retention (although it is worth noting, however, that the mineralocorticoid effects of prednisone are very minor; this is why it is not used in the management of adrenal insufficiency unless a more potent mineralocorticoid is administered concomitantly). Additional short-term side-effects include insomnia, euphoria, and, rarely, mania. Long-term side-effects include Cushing's syndrome, weight gain, osteoporosis, glaucoma, type II diabetes mellitus, and depression upon withdrawal.

[edit] Major

• weight gain
• facial swelling
• depression, mania, or other psychiatric symptoms
• unusual fatigue or weakness
• mental confusion / indecisiveness
• blurred vision
• abdominal pain
• peptic ulcer
• infections
• painful hips or shoulders
• osteoporosis
• insomnia
• severe joint pain
• cataracts
• osteonecrosis
• anxiety

[edit] Minor

• stretch marks
• nervousness
• acne
• rash
• increased appetite
• hyperactivity
• frequent urination
• diarrhea
• removes intestinal flora

[edit] External links

• Prednisone-related growth impairment persist in children with CF