Prednisolone is a synthetic analogue of the hormones cortisone and hydrocortisone. It has anti-inflammatory, antiallergic, antiexudative, antishock, anti-toxic effects.
Generic name: Prednisolone.
Brand name: Millipred, Orapred.
What is prednisolone?
Prednisolone is a synthetic adrenal corticosteroid. prednisolone, the active metabolite of prednisone (generic Deltasone), was measured in his plasma using a high-pressure liquid chromatography technique. Corticosteroid is a class of chemicals. This medication affects the immunity making people vulnerable to various infections.
The study of adrenal function began in the 19th century, but it was not until 1936 that Kendall and Wintersteiner in the USA and Reinstein in Switzerland simultaneously isolated steroids in crystalline form from extracts of adrenal cortex. In 1948 cortisone was obtained in quantities sufficient for clinical studies, and later hydrocortisone. Today, there is a wide range of synthetic glucocorticosteroids (GCS) used in clinical practice. During the synthesis of new GCSs, the efforts were aimed at creating drugs with a more selective action than that of hydrocortisone. A significant decrease in mineralocorticoid activity of synthetic GCSs was achieved. For example, prednisolone is almost devoid of mineralocorticoid properties.
The chemical structure of prednisolone is a modified hydrocortisone molecule with the introduction of a double bond between the 1st and 2nd atoms of the steroid nucleus, which allowed to reduce the mineralocorticoid activity and, in addition, significantly increase its anti-inflammatory activity. Thus, a small structural change caused a significant increase in the biological activity of the hormone.
GCSs are used in medical practice mainly as anti-inflammatory, anti-shock, antiallergic agents and immunosuppressants.
GCS, especially prednisolone, has many effects on the body, regulates protein and fat metabolism, affects carbohydrate metabolism.
Prednisolone regulates insulin and glucagon synthesis, stimulates gluconeogenesis by inducing the enzymes that regulate it, increases glycogen content in liver by stimulating glycogen synthetase activity, inhibits glucose uptake by lipocytes, stimulating lipolysis.
GCS have a catabolic effect and can cause dystrophic changes in the lymphoid and connective tissue, muscles, subcutaneous and fatty tissue and skin.
The mechanism of anti-inflammatory action of GCS is associated with their influence on the number, distribution and function of leukocytes. After a single injection of prednisolone, the number of T- and B-lymphocytes, monocytes, eosinophilic and basophilic granulocytes decreases in peripheral tissue, while the content of neutrophilic granulocytes increases. This is due to two factors: increased intake of neutrophilic granulocytes from the bone marrow and decreased migration from the blood, which leads to a decrease in their numbers in the focus of inflammation. Decrease of lymphocytes, monocytes, eosinophilic and basophilic granulocytes in peripheral blood is a consequence of their transfer from blood to lymphoid tissue.
Prednisolone inhibits the function of leukocytes and tissue macrophages. Its effect on tissue macrophages is to limit their ability to phagocytosis, as well as the production of pyrogens, collagenase, elastase and plasminogen activators. Inhibiting the function of leukocytes, prednisolone can affect other mechanisms of inflammation: it reduces capillary permeability by inhibiting the activity of kinins and hyaluronidase, inhibits the release of histamine from mast cells.
The immunosuppressive effect of prednisolone is due, in addition to its effect on the migration and interaction of T- and B-lymphocytes, to its effect on the complement system, as well as to inhibition of the production and effects of interleukin-2.
Prednisolone has anti-shock, anti-allergic and anti-inflammatory effects. With prolonged use, it inhibits the synthesis and secretion of ACTH by the pituitary gland and secondary secretion of GCS by the adrenal glands.
After intravenous administration prednisolone binds to blood plasma globulin – transcortin. Maximum plasma concentration of free prednisolone is reached 10 min after intravenous and 60 min after intramuscular administration.
Prednisolone is a medium duration of action GCS. The elimination half-life is about 3 hours. It is actively metabolized in many tissues, especially intensively in liver, excreted as metabolites, mainly in urine.
Medical Use:
Prednisolone is used to fight with inflammation in many inflammatory and allergic conditions. prednisolone treats blood cell cancers and lymph gland cancers. Buy prednisolone to treat such cases. prednisolone 5 mg is very useful for treating such conditions as: asthma, hypodermal gangrenous, ulcerative colitis, temporal arthritis, cluster headaches, acute leukemia and others.
Prednisolone is indicated:
- as an emergency treatment for burns, traumatic, transfusion, infectious-toxic shock;
- in endocrinology – in primary or secondary adrenal insufficiency, including acute; non-pulmonary thyroiditis;
- in rheumatology and therapy – in rheumatoid arthritis and systemic lupus erythematosus;
- In dermatology – in severe erythema multiforme, exfoliative dermatitis;
- in severe allergic diseases, resistant to adequate therapy with antihistamines, contact and atopic dermatitis, serum sickness, drug allergy, transfusion reactions, asthmatic status, acute laryngeal edema of non-infectious
- etiology;
- in hematology – in idiopathic thrombocytopenic purpura, acute and chronic leukemia;
- in neurology – in multiple sclerosis;
- in transplantology – to suppress transplant rejection reaction;
- in infectious clinic – infectious-toxic shock (in case of simultaneous antibiotic therapy);
- in pediatrics – allergic reactions, including anaphylaxis;
- laryngitis, laryngotracheitis;
- severe forms of bronchial asthma, asthmatic status.
In case of shock, prednisolone is administered intravenously slowly or by intravenous drip in a dose of 30-90 mg. For other indications, 30-45 mg intravenously slowly. If intravenous administration is difficult, the drug can be administered deeply intramuscularly.
Wide introduction of prednisolone, especially injectable dosage forms, into medical practice has saved more than one human life. Along with new and active GCSs, prednisolone is an effective, proven and available drug that is still relevant today.
Form and how to use:
Prednisolone may be more often found in the form of tablets, they are prednisolone 5 mg, prednisolone 10 mg, prednisolone 20 mg and prednisolone 40 mg.
You should take this prednisolone by mouth and with food it is necessary, because food helps to prevent stomach upset. The dosage and duration of taking this medication depends on medical conditions. Take prednisolone 1 to 4 times per day.
Prednisolone tablets are prescribed orally. The dose is selected individually. When prescribing, the daily secretory rhythm of glucocorticosteroids should be taken into account: most (or all) of the dose is prescribed in the morning. Treatment is stopped slowly, gradually reducing the dose.
When administered orally as substitution therapy, the initial dose for adults is 20-30 mg/day (4-6 tablets), the maintenance dose is 5-10 mg/day (1-2 tablets). If necessary, the initial dose may be 15-100 mg/day (3-20 tablets), the maintenance dose is 5-15 mg/day (1-3 tablets). The daily dose should be reduced gradually. For children, the initial dose is 1-2 mg/kg/day in 4-6 doses, the maintenance dose is 0.3-0.6 mg/kg/day.
The highest daily dose for adults is 0.1 g.
Treatment with prednisolone should be performed in case of clear indications and under close medical supervision.
After discontinuation of treatment, withdrawal syndrome, adrenal insufficiency may occur, as well as exacerbation of the disease for which prednisolone was prescribed.
Taking prednisolone 5 mg without prescription may lead to nausea, increased sweating, insomnia, dizziness, shortness of breath, vision changes or other eye problems, increased hunger and many others not listed here. Call a doctor if you noticed such or other cases.
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Side effects
Side effects and contraindications for the use of prednisolone are the same as for other GCS intended for systemic corticosteroid therapy.
The frequency and severity of side effects depend on the duration of use and the size of the used dose of the drug.
Endocrine system disorders: Icenko-Cushing’s syndrome, weight gain, hyperglycemia up to the development of steroid diabetes, depletion (up to atrophy) of adrenal cortex function, delayed sexual development in children.
Digestive system: nausea, vomiting, increased gastric acidity, ulcerogenic effect, increased or decreased appetite, flatulence, hiccups.
Metabolic disorders: increased potassium excretion, sodium retention in the body with the formation of edema, negative nitrogen balance.
Cardiovascular system: arterial hypertension, arrhythmias, bradycardia.
Blood coagulation system: increased blood clotting.
Musculoskeletal system: “steroid” myopathy, decreased muscle mass, osteoporosis, aseptic necrosis of bones, growth retardation and ossification processes in children.
Skin and mucous membranes: delayed wound healing, petechiae, ecchymoses, skin thinning, hyper- or hypopigmentation, acne, stretch marks, tendency to pyoderma and candidiasis.
Eye: steroid cataract, provocation of latent glaucoma.
Nervous system disorders: mental disorders.
Allergic reactions: generalized (skin rash, skin itching, anaphylactic shock), local allergic reactions.
Other: decreased resistance to infection, “withdrawal” syndrome.
Contraindications
Hypersensitivity, gastric or 12 duodenal ulcer in the acute phase, decompensated diabetes, severe arterial hypertension, osteoporosis, Icenko-Cushing’s disease, vaccination period, active tuberculosis, glaucoma, systemic mycoses, acute viral infection, productive symptoms in mental disorders, viral and bacterial eye diseases, primary glaucoma, corneal diseases with damaged epithelium, bacterial, fungal, viral skin lesions, tuberculosis, syphilis, skin tumors.
The drug does not affect the ability to drive vehicles and machinery.
Precautions
1) If you have allergy to any ingredient of prednisolone, you should not take it. 2) Consult a doctor if you decided to buy prednisolone. 3) You should remember about possible side effects 4) You should not take more than prescribed. 5) Try not to miss doses, if it happened take it as soon as possible. 6) Avoid contact with people who have recently received live vaccines.7) If you are pregnant you should buy prednisolone only if it is necessary.
During the treatment (especially prolonged) it is necessary to supervise ophthalmologist, control arterial pressure and water-electrolyte balance, as well as peripheral blood picture, blood glucose. In order to reduce the side effects, potassium intake into the body may be increased (diet, potassium supplements).
Caution is used in patients with a history of psychosis; in nonspecific infections with simultaneous chemotherapy or antibiotic therapy.
In diabetes mellitus the use is possible only in absolute indications or to prevent suspected insulin resistance. In latent forms of tuberculosis, prednisolone may be used only in combination with antituberculosis drugs. In Addison’s disease, concomitant use with barbiturates should be avoided.
Pregnancy and lactation
During pregnancy (especially during the first trimester) it is used only for vital indications. If it is necessary to use during lactation, the expected benefits of the treatment for a mother and risks for a child should be carefully weighed.
Interations:
- With the simultaneous use of prednisolone with NSAIDs, the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding increases (in combination with NSAIDs in the treatment of arthritis, a decrease in the GCS dose is possible due to the summation of therapeutic effects).
- Oral contraceptives increase the level of prednisone in the blood, with the possible increase in therapeutic and side effects.
- Possible pharmaceutical incompatibility of prednisolone in the form of a solution for intravenous administration with other intravenous injected drugs – it is recommended to inject it separately from other drugs (intravenously bolus (jet) or through another dropper, as a second solution).
- The simultaneous use of prednisolone with diuretics can lead to increased excretion of potassium from the body and an increased risk of developing heart failure.
- The simultaneous use of prednisolone with thiazide diuretics can lead to an increase in the excretion of potassium from the body and an increase in the risk of developing heart failure.
- The simultaneous use of prednisolone with carbonic anhydrase inhibitors can lead to increased excretion of potassium from the body and an increase in the risk of developing heart failure.
- With the simultaneous use of prednisolone with carbonic anhydrase inhibitors, the risk of osteoporosis may increase.
- The simultaneous use of prednisolone with tricyclic antidepressants can increase the severity of depression caused by the use of GCS (tricyclic antidepressants are not indicated for the treatment of this side effect).
- The simultaneous use of prednisolone with tricyclic antidepressants with m-anticholinergic activity increases IOP.
- Hypokalemia caused by prednisone may increase the degree and duration of muscle blockade by muscle relaxants.
- The simultaneous use of prednisolone with antihypertensive drugs can cause a decrease in the antihypertensive effect due to sodium and water retention.
- The simultaneous use of prednisolone with fluoroquinolones increases the risk of tendinitis, in rare cases it can lead to tendon rupture.
- The simultaneous use of prednisolone with inducers of liver microsomal enzymes leads to a decrease in its concentration in the blood.
- The simultaneous use of prednisolone with sodium-containing drugs can lead to the development of edema and an increase in blood pressure.
- With the simultaneous use of prednisolone with cardiac glycosides, their tolerance worsens and the likelihood of developing arrhythmias increases, incl. ventricular premature beats (due to hypokalemia caused by prednisolone).
- The simultaneous use of prednisolone with indirect anticoagulants weakens (less often – enhances) their effect. Coagulation indicators should be monitored to maintain the desired anticoagulant effect – it may be necessary to adjust the doses of simultaneously used DV.
- With the simultaneous use of prednisolone with thrombolytics, the risk of bleeding ulcers in the gastrointestinal tract increases.
- With the simultaneous use of prednisolone with anticoagulants, the risk of bleeding from ulcers in the gastrointestinal tract increases.
- With the simultaneous use of prednisolone with insulins, their effectiveness decreases (GCS can increase the concentration of glucose in the blood). Dose adjustment of concomitant insulin may be required.
- With the simultaneous use of prednisolone with oral hypoglycemic drugs, their effectiveness decreases (GCS can increase the concentration of glucose in the blood). Dose adjustment of concurrent oral hypoglycemic drugs may be required.
- With the simultaneous use of prednisolone with vitamin D, the effect of the latter on the absorption of calcium ions in the intestine decreases.
- The simultaneous use of prednisolone with m-anticholinergics increases IOP.
- The simultaneous use of prednisolone with antihistamine drugs increases IOP.
- The simultaneous use of prednisolone with nitrates increases IOP.
- With the simultaneous use of prednisolone with loop diuretics, the risk of osteoporosis may increase.
- The simultaneous use of androgens with prednisone promotes the development of peripheral edema and hirsutism, the appearance of acne.
- The simultaneous use of steroid anabolic drugs with prednisone promotes the development of peripheral edema and hirsutism, the appearance of acne.
- Estrogens reduce the clearance of prednisolone, which may be accompanied by an increase in its action. It may be necessary to adjust the dose of prednisolone when increasing or decreasing the dose of concurrently used estrogens.
- Oral estrogen-containing contraceptives reduce the clearance of prednisolone, which may be accompanied by an increase in its action.
- Inhibitors of adrenal cortex function may necessitate an increase in the dose of prednisolone.
- Antipsychotics increase the risk of developing cataracts when used concomitantly with prednisolone.
- When used concomitantly with vaccines, prednisolone increases the risk of virus activation and infection.
- When used simultaneously with live antiviral vaccines, prednisolone increases the risk of viral activation.
- When used concomitantly with prednisolone, immunosuppressants increase the risk of developing infections and lymphoma or other lymphoproliferative disorders caused by the Epstein-Barr virus.
- The simultaneous use of antacids reduces the absorption of prednisolone in the form of tablets for oral administration.
- With simultaneous use with antithyroid drugs, the clearance of prednisolone decreases.
- With simultaneous use with thyroid hormones, the clearance of prednisolone increases.
- Prednisolone is metabolized by the CYP3A4 isoenzyme. With the simultaneous use of prednisolone with inhibitors of the isoenzyme CYP3A4, PCF is possible (decreased metabolism of prednisolone).
- Prednisolone is metabolized by the CYP3A4 isoenzyme. With the simultaneous use of prednisolone with inducers of the CYP3A4 isoenzyme, PCF is possible (increased metabolism of prednisolone).
- It is possible to develop severe weakness with the simultaneous use of anticholinesterase drugs and corticosteroids in patients with severe pseudoparalytic myasthenia gravis. If possible, anticholinesterase therapy should be discontinued 24 hours before starting treatment with prednisone.
- With simultaneous use with barbiturates, the metabolism of prednisolone increases. An increase in the dose of prednisolone may be required.
- The simultaneous use of prednisolone with non-potassium-sparing diuretics can lead to an increase in the potassium-excreting effect of GCS – it is necessary to monitor the possible development of hypokalemia.