Prednisolone

Prednisolone uses

• Pharmacological action
• Pharmacokinetics
• Why is Prednisolone prescribed?
• Dosage and administration
• Prednisolone side effects, adverse reactions
• Prednisolone contraindications
• Using during pregnancy and breastfeeding
• Special instructions
• Prednisolone drug interactions
• Prednisolone in case of emergency / overdose
• Prednisolone reviews

Pharmacological action

Prednisolone is a glucocorticosteroid. This medication inhibits the function of leukocytes and tissue macrophages. Prednisolone restricts the migration of leukocytes in the area of inflammation. This drug violates the ability of macrophages to phagocytosis and the formation of interleukin-1. Prednisolone contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in inflammation. This medicine decreases capillary permeability caused by histamine release. Prednisolone inhibits the activity of fibroblasts and collagen formation.

Prednisolone inhibits the activity of phospholipase A2 which leads to suppression of the synthesis of prostaglandins and leukotrienes. This medication inhibits the release of COX (especially COX-2), which also helps reduce the production of prostaglandins.

Prednisolone reduces the number of circulating lymphocytes (T-and B-cells), monocytes, eosinophils and basophils as a result of their displacement from the bloodstream into lymphoid tissue; suppresses the formation of antibodies.

Prednisolone inhibits the release of pituitary ACTH and beta-lipotropina but it does not reduces the level of circulating beta-endorphin. This drug also inhibits the secretion of TSH and FSH.

Prednisolone has a vasoconstrictor effect with direct application to the vessels.

Prednisolone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. It stimulates gluconeogenesis, amino acid contributes to the capture of the liver and kidneys and increases the activity of enzymes of gluconeogenesis. In the liver, Prednisolone enhances the deposition of glycogen by stimulating the activity of glikogensintetazy and synthesis of glucose from the products of protein metabolism. This medicine increases blood glucose activates the secretion of insulin.

Prednisolone inhibits glucose uptake by fat cells that leads to the activation of lipolysis. However, due to an increase in insulin secretion is stimulated lipogenesis which contributes to the accumulation of fat.

Prednisolone also has catabolic effects in lymphoid and connective tissue, muscle, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone Prednisolone affects the processes of water and electrolyte metabolism: promotes the excretion of potassium and calcium, delay in the body of sodium and water. Osteoporosis and Itsenko-Cushing's syndrome are the main factors limiting the long-term therapy with corticosteroids. As a result of the catabolic actions it may suppress growth in children.

In high doses prednisone can increase the excitability of brain tissue and contributes to lowering the threshold of convulsive readiness. This medication stimulates the excessive production of hydrochloric acid and pepsin in the stomach which leads to the development of peptic ulcers.

When systemic use the therapeutic activity of Prednisolone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.

For external and local application the therapeutic activity of Prednisolone is due to anti-inflammatory, antiallergic and antiexudative (due to vasoconstrictor effect) effect.

As compared with hydrocortisone the anti-inflammatory activity of Prednisolone is 4 times greater, the mineralocorticoid activity is 0.6 times smaller.

Pharmacokinetics

After oral administration Prednisolone is well absorbed from the gastrointestinal tract. C_max in plasma observed after 90 min. In plasma most of Prednisolone is associated with transcortin (cortisol binding globulin). This drug metabolized primarily in the liver.

T_1/2 is about 200 minutes.

Why is Prednisolone prescribed?

For oral and parenteral use: rheumatism; rheumatoid arthritis, dermatomyositis, periarteritis nodosa, scleroderma, ankylosing spondylitis, asthma, asthmatic status, acute and chronic allergic diseases, anaphylaxis, Addison's disease, acute adrenal insufficiency, adrenogenital syndrome; hepatitis, hepatic coma, hypoglycemic states, lipid nephrosis; agranulocytosis, various forms of leukemia, lymphoma, thrombocytopenic purpura, hemolytic anemia; chorea; pemphigus, eczema, pruritus, exfoliative dermatitis, psoriasis, pruritus, seborrheic dermatitis, SLE, erythroderma, alopecia.

For intra-articular administration: chronic arthritis, post-traumatic arthritis, osteoarthritis of large joints, rheumatic destruction of individual joints, arthritis.

For the introduction of infiltration in the tissue: epicondylitis, tenosynovitis, bursitis, frozen shoulder, keloids, sciatica, Dupuytren's contracture, rheumatism and similar lesions of joints and various tissues.

For use in ophthalmology: allergies, chronic and atypical conjunctivitis and blepharitis; inflammation of the cornea with intact mucosa; acute and chronic inflammation of the anterior segment of the choroid, sclera and episcleritis; sympathetic inflammation of the eyeball; after injuries and operations during prolonged stimulation of eyeballs.

Dosage and administration

When Prednisolone administered orally for replacement therapy in adults the initial dose is 20-30 mg, maintenance dose is 10.5 mg / day. If necessary, the initial dose is may be 15-100 mg / day, the maintenance one is 5-15 mg / day. The daily dose should be reduced gradually. For children the starting dose is 1-2 mg / kg in 4-6 receptions, the maintenance one is 300-600 mg / kg / day.

For IM or IV dose administration the multiplicity and duration of application are determined individually.

When intra-articular administration in large joints it used a dose of 25-50 mg, for medium-sized joints - 10-25 mg for small joints - 5-10 mg. For the introduction of infiltration into the tissues depending on disease severity and magnitude of the defeat use doses from 5 mg to 50 mg.

Prednisolone used topically in ophthalmology 3 times / day, course of treatment is no more than 14 days; in dermatology - 1-3 times / day.

Prednisolone side effects, adverse reactions

Endocrine system: menstrual irregularities, suppression of adrenal function, Itsenko-Cushing's syndrome, suppression of pituitary-adrenal system, reduced tolerance to carbohydrates, steroid diabetes, or a manifestation of latent diabetes, growth retardation in children, delayed sexual development in children.

Digestive system: nausea, vomiting, steroid ulcer and duodenal ulcer, pancreatitis, esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases - elevated liver transaminases and alkaline phosphatase.

Metabolism: the negative nitrogen balance due to protein catabolism, increased excretion of calcium from the body, hypocalcemia, weight gain, increased sweating.

Cardiovascular system: the loss of potassium, hypokalemic alkalosis, arrhythmia, bradycardia ; steroid myopathy, heart failure (the development or worsening of symptoms), ECG changes typical of hypokalemia, increased blood pressure, hypercoagulability, thrombosis. In patients with acute myocardial infarction - the spread of necrosis, slowing the formation of scar tissue that can lead to rupture of the heart muscle.

Musculoskeletal system: slowing growth and ossification processes in children (premature closure of epiphyseal growth zones) and osteoporosis (very rarely - pathological fractures, aseptic necrosis of the humeral head and femoral), rupture of tendons of muscles, muscle weakness, steroid myopathy, loss of muscle mass (atrophy).

CNS: headache, increased intracranial pressure, delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor cerebellum, and seizures.

Vision: the rear subcapsular cataracts, increased intraocular pressure (with the possible damage to the optic nerve), trophic changes of the cornea, exophthalmos, the propensity to develop secondary infections (bacterial, fungal, viral).

Dermatological reactions: petechiae, ecchymosis, thinning and fragility of the skin, hyper- or hypopigmentation, acne, stretch marks, susceptibility to the development of pyoderma and candidiasis.

Reactions due to immunosuppressive effect: slow process of regeneration, reduced resistance to infections.

For parenteral administration: in rare cases of anaphylactic and allergic reactions, hyper- or hypopigmentation, atrophy of skin and subcutaneous tissue, exacerbation after intrasinovialnogo applications such as Charcot arthropathy, sterile abscesses, when injected into pockets on the head - blindness.

Prednisolone contraindications

For short-term use for health reasons - increased sensitivity to Prednisolone.

For intra-articular injection and injection directly into the lesion: previous arthroplasty, abnormal bleeding (endogenous or caused by the use of anticoagulants), intra-articular fracture, infection (sepsis) inflammation in the joints and periarticular infections (including in history), as well as general infectious disease marked juxta-articular osteoporosis, lack of signs of inflammation in the joints ("dry" joint, such as osteoarthritis without synovitis), severe bone destruction and deformity of the joint (a sharp narrowing of joint space, ankylosis), the instability of the joint as a result of arthritis, aseptic necrosis of the epiphyses of bones forming the joint.

For external use only: bacterial, viral, fungal skin diseases, tuberculosis, skin, cutaneous manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), children's age (up to 2 years, with itching in the anal area - up to 12 years), rosacea, acne vulgaris, perioral dermatitis.

For use in ophthalmology: bacterial, viral, fungal eye diseases, tuberculosis eye disease, trachoma, violating the integrity of ocular epithelium.

Using during pregnancy and breastfeeding

During pregnancy Prednisolone is used only for health reasons. If necessary use of Prednisolone during lactation should carefully weigh the potential benefits of treatment for both mother and child at risk.

Special instructions

With care use for parasitic and infectious diseases of viral, fungal or bacterial origin - herpes simplex, herpes zoster (viraemic phase), chicken pox, measles, amoebiasis, strongyloidiasis, systemic mycosis, active and latent tuberculosis.

Be wary of up to 8 weeks before and 2 weeks after vaccination, and lymphadenitis after BCG, with immunodeficiency (including AIDS or HIV infection).

Be wary of diseases in gastrointestinal tract: gastric ulcers and duodenal ulcers, esophagitis, gastritis, acute or latent peptic ulcer, the newly created anastomosis intestinal ulcerative colitis with the threat of perforation or abstsedirovaniya, diverticulitis. Be wary of Prednisolone use in diseases of the cardiovascular system, including after recent myocardial infarction, with decompensated congestive heart failure, hypertension, hyperlipidemia, with endocrine diseases - diabetes mellitus, hyperthyroidism, hypothyroidism, pituitary basophilia, with severe chronic renal and / or liver failure, nefrourolitiaze, with hypoalbuminemia, with systemic osteoporosis, myasthenia gravis, acute psychosis, obesity III-IV stage, in poliomyelitis, open- and closed-angle glaucoma.

If necessary, intra-articular injection with caution in patients with severe general condition, failure (or brevity) of the 2 previous injections (with regard to individual properties apply GCS). During treatment (especially long-term) it needed to monitor at eye specialist, blood pressure control and water-electrolyte balance, and the pattern of peripheral blood glucose levels; to reduce the side effects can be assigned anabolic steroids, antibiotics, and increase the flow of potassium in the body (diet, potassium containing medications).

It is recommended to clarify the need for injection of ACTH after treatment with prednisone (after a skin test).

When Addison's disease should avoid the simultaneous use of barbiturates.

After cessation of treatment it may be experience a withdrawal syndrome, adrenal insufficiency and exacerbation of the disease, about which he was appointed Prednisolone Rotexmedica.

When intercurrent infections, septic conditions, and tuberculosis, must be simultaneous antibiotic therapy.

The children in the period of growth GCS should be used only if absolutely indicated and under close medical supervision.

Externally Prednisolone should not be used for more than 14 days. In case of application for ordinary or pink acne perhaps exacerbation.

Prednisolone drug interactions

Simultaneous administration of Prednisolone with: