One of the most commonly prescribed anti-inflammatory drugs is Prednisolone. In some cases, this tool is indispensable, and in some - even able to save a person’s life. They can treat both children and adults. Prednisolone is available in various dosage forms and dosages. And every patient should know not only about the merits of the drug and its indications, but also its minuses and side effects.
Prednisolone is a synthetic analogue of the hormone of the adrenal glands - hydrocortisone and has a similar effect to it. The main functions of the drug:
The mechanism of action of the drug in many ways still not exactly installed. We can only say that it affects almost all stages of the inflammatory process, inhibits the synthesis of inflammatory mediators - cytokines and histamine, and prevents the migration of immune system cells.
Any medication that contains prednisolone acts on specific glucocorticosteroid receptors located in various tissues. Especially many of these receptors in the liver.
Prednisolone reduces the permeability of cell walls and has a moderate vasoconstrictor effect. It also affects the metabolism - lipids, proteins, carbohydrates, sodium ions and calcium, retains water in the body.
The effect of the drug on protein metabolism is that it reduces the amount of albumin in the plasma and increases their amount in the composition of the liver, reduces protein synthesis in muscle tissue.
Impact on lipid metabolism is to enhance the synthesis of higher fatty acids and triglycerides, the redistribution of adipose tissue.
The effect on carbohydrate metabolism is expressed in enhancing the absorption of glucose from the gastrointestinal tract, stimulating the flow of glucose from the liver into the blood. For these reasons, prednisone contributes to hyperglycemia.
Prednisolone retains sodium in the body, but stimulates the excretion of potassium, reduces bone mineralization and slows down the absorption of calcium from the gastrointestinal tract.
The mechanism by which the anti-inflammatory effect of the drug is realized is versatile. First of all, prednisone prevents the release of inflammatory mediators from mast cells, reduces capillary permeability, stabilizes cell membranes. In addition, prednisolone violates the synthesis of prostaglandins from arachidonic acid, cytokines (interleukins, a special protein - tumor necrosis factor).
Also, prednisone has an immunosuppressive effect. It interferes with the interaction of various types of lymphocytes and their migration, reduces the intensity of the formation of antibodies, blocks the release of interferons.
The antiallergic effect is due to a decrease in the secretion of inflammatory mediators, inhibition of the release of histamine from mast cells, and suppression of the activity of lymphocytes in the blood. Prednisolone reduces the sensitivity of receptors in various tissues to inflammatory mediators.
The therapeutic effect of the drug in obstructive processes in the airways is due to the effect on inflammatory processes, a decrease in the swelling of the mucous membranes and viscosity of mucus, an increase in the sensitivity of adrenoreceptors to sympathomimetics. In case of shock, prednisolone increases blood pressure, reduces the permeability of vascular walls, has a membrane-protective effect, activates liver enzymes involved in metabolic processes.
Also, the drug prevents the development of lymphoid and connective tissue.
Prednisolone in the form of an ointment, in addition to anti-inflammatory, anti-allergic and anti-edema effects, also prevents the occurrence of itching.
By its anti-inflammatory activity, prednisolone is 4 times as high as hydrocortisone. However, prednisone is not the strongest of the synthetic glucocorticosteroid hormones. In addition, it is 40% inferior to the natural adrenal hormone hydrocortisone in mineralocorticoid activity.
The drug is able to inhibit the synthesis of corticotropin and endogenous glucocorticosteroids.
When administered as a pill, the maximum plasma concentration is observed after 90 minutes, with intravenous administration - after 30 minutes. The active substance may be in the composition of the blood for a long time. The half-life is 200 minutes.
When should you take Prednisone?
The use of the drug is extremely wide, and it is often necessary to use it in different dosage forms in different situations. This means that the patient is not always free to switch from pills to injections, and then, for example, to ointment.
In general, the drug is most often used to relieve symptoms of inflammatory processes of moderate and high severity. These processes can be localized in the following parts of the body:
- musculoskeletal system
- blood system
- gastrointestinal tract
- nervous system
Also one of the main directions of the drug is to combat systemic allergic reactions, such as angioedema and anaphylactic shock, especially when they take a scale that threatens the functioning of the body. And the use of the drug in the form of an injection or taking a pill in such a situation can save a person’s life.
Another important area of use of the drug in which it is able to prevent the development of life-threatening processes is anti-shock therapy. Often, Prednisolone is prescribed for various shock conditions. This may be cardiogenic, burn, surgical, toxic, traumatic shock. Here Prednisolone is most often used in case of ineffectiveness of vasoconstrictor agents and other symptomatic therapy.
The drug is used in such a dangerous complication as brain swelling. This condition may occur as a result of injuries, infectious and inflammatory processes, and surgical intervention.
Prednisolone is often prescribed for severe injuries, burns, including the gastrointestinal tract, and upper respiratory tract, poisoning.
Also, the drug is used in severe bronchial asthma, systemic connective tissue diseases (systemic lupus erythematosus, scleroderma, rheumatoid arthritis).
Acute and chronic diseases of the joints, in which the doctor may prescribe Prednisone:
- arthritis (gouty, psoriatic, juvenile)
- osteoarthritis (including post-traumatic)
- ankylosing spondylitis
- still's syndrome
Often, Prednisolone is also prescribed for skin diseases:
- dermatitis (contact, seborrheic, exfoliative, bullous herpetiform)
- lyell syndrome
- stevens-Johnson syndrome
Indications for taking the drug also include eye diseases of an allergic and inflammatory nature - allergic conjunctivitis, sympathetic ophthalmia, uveitis, optic neuritis. And the use of medication for such diseases helps not only to relieve swelling and inflammation, but also often to avoid vision loss.
Prednisolone is also prescribed for congenital adrenal hyperplasia, berylliosis, Lefler syndrome, multiple sclerosis, thyrotoxicosis, acute hepatitis, hepatic coma, and severe kidney disease.
An extensive scope of the drug - diseases of the circulatory system and blood. The diagnoses for which specialists can prescribe prednisone are:
- anemia (autoimmune hemolytic, erotrotsitarnaya, congenital hypoplastic)
- lymphocytic leukemia
- myeloid leukemia
Prednisolone is also prescribed for some types of oncological diseases, for example, in case of lung cancer, multiple myeloma. In addition, the drug is useful in the treatment of complications of cancer, for example, hypercalcemia. Also, prednisone is prescribed to reduce nausea and vomiting during treatment with cytotoxic agents.
The ability of the drug to suppress the immune response is not only useful in the treatment of autoimmune diseases. Due to this feature, Prednisolone is prescribed for the prevention of rejection of transplanted donor organs.
It is necessary to note one important circumstance - because many people forget about this minus of the drug. Despite the fact that the main purpose of Prednisolone is to combat inflammation, this does not mean that the remedy will be effective in infectious diseases. Moreover, for diseases caused by bacteria or viruses, taking the drug is not recommended. Here it should be remembered that one of the properties of the drug is immunosuppression. And the use of the medication can lead to the fact that the bacteria and viruses in the body subjected to the action of Prednisolone, will feel at ease. Therefore, if one cannot do without a drug in such a case, then it should be used as part of a complex therapy, which should also include measures aimed at eliminating the causative agents of the disease, for example, taking antibiotics.
Often, Prednisolone is prescribed during replacement therapy, in case of insufficient functional activity of the adrenal glands. However, in this case, it should be borne in mind that the mineralocorticoid activity of the drug is lower than that of hydrocortisone. Therefore, patients with insufficient adrenal function should be treated not only with prednisone, but also mineralocorticoids.
It also acts on the adrenal glands, inhibiting the production of their natural hormones. Therefore, with prolonged administration of the drug, adrenal dysfunction may be observed, which becomes noticeable after the end of treatment. Over time, this phenomenon usually passes.
Tablets have the widest range of indications. They are used for:
- endocrine pathologies
- connective tissue diseases, joint inflammations
- chronic and acute allergic reactions
- bronchial asthma, blood diseases, and the blood system
- skin diseases
- eye diseases
- diseases of the gastrointestinal tract and lungs
- autoimmune kidney disease
- swelling of the brain (after parenteral therapy)
- for the prevention of vomiting during cytostatic therapy
- for the prevention of transplant rejection
Prednisolone injection is used for:
- shock conditions
- allergic reactions, especially in severe and acute forms
- swelling of the brain
- connective tissue diseases, rheumatoid arthritis, systemic lupus erythematosus
- severe bronchial asthma
- thyrotoxic crisis
- acute hepatitis, hepatic coma
- acute adrenal insufficiency
Prednisolone ointment is mainly used in case of dermatological problems. These may be the following diseases:
- lupus erythematosus
In this case, it is important that skin diseases are not caused by infectious causes. Otherwise, the drug can lead to inhibition of immunity and its use will only encourage the development of the disease. That is why prednisone is not prescribed as an ointment for skin infections.
The tool in the form of drops is used in ophthalmology. Indications for the use of eye drops are:
- eye injuries
- chronic allergic blepharoconjunctivitis
- eye irritation in the postoperative period
The pharmaceutical industry produces prednisone in a variety of forms, each of which is intended for use in certain diseases and situations in which the patient finds himself. For example, tablets are best suited for the treatment of chronic inflammatory or allergic processes. For the treatment of skin diseases it is best to use a local dosage form - ointment. For eye problems, use special eye drops. And in acute conditions, such as injuries, swelling of the brain or anaphylactic shock, only injections can help you - jet or drop.
Prednisolone tablets has two dosage options - 1 and 5 mg. The tablets also contain milk sugar, povidone, starch, stearic acid.
The solution for intravenous injection has a dosage of 30 and 15 mg per 1 ml. In the composition of the solution can be found some excipients:
- sodium metabisulphite
- disodium edetat
- sodium hydroxide
- sodium hydroxide
Drops for use in eye diseases and skin ointment have a concentration of 0.5%. This means that 1 g of the drug contains 5 mg of active ingredient. The composition of the ointment contains a number of auxiliary components:
- stearic acid
- propyl paraben
- purified water
The tool can be used not in all cases. However, here we must take into account the seriousness of the situation in which it is assigned. If we are talking about stopping a severe allergic reaction, such as anaphylactic shock, then all possible prohibitions fade into the background. After all, it is a state that threatens life. Such evidence is called life. With vital indications, the only case where it is impossible to take a remedy is its individual intolerance.
However, if we are talking about long-term therapy with prednisone, then here the situation when it can not be taken, are much more common. A weighty list of contraindications should be attributed to the disadvantages of the drug.
As with indications, contraindications for different dosage forms may not be the same. The most extensive list of contraindications for tablets and solution.
In general, the list of prohibitions is based on the types of effects that prednisone produces on the body. For example, despite the fact that the agent is prescribed for certain cardiovascular diseases, it cannot be used for acute or subacute myocardial infarction. This is due to the fact that prednisone blocks the formation of scar tissue on the heart. As a result, the area of necrosis in the heart may expand, and a heart failure may even occur.
You should also consider that prednisone affects the production of glucose in the body. This means that it can contribute to an increase in body weight. Therefore, people with obesity should also not be used. In addition, it stimulates the production of pepsin and hydrochloric acid in the stomach, which predetermines its prohibition in case of peptic ulcer of this organ and duodenum.
With caution appoint a means in the form of tablets and solution for:
- renal and hepatic failure
- Itsenko-Cushing disease
- grade 3-4 obesity
- systemic osteoporosis
- psychoses, including, in the anamnesis
The disadvantage of the remedy (unlike other glucocorticosteroids) is that it is prohibited in violation of the arachidonic acid metabolism.
Among the diseases of the gastrointestinal tract, in which the drug is appointed with caution, include:
- peptic ulcer and duodenal ulcer
- ulcerative colitis with the threat of perforation
- peptic ulcer
Not recommended for use in acute or chronic infections of viral or bacterial nature, parasitic diseases. And it is not surprising, because prednisone inhibits many immune mechanisms, making the disease takes a heavy or protracted nature. Particular caution should be observed with tuberculosis, various types of herpes, mycoses, amebiasis. In some cases, the use of tools in infectious diseases is permissible, however, subject to the simultaneous implementation of adequate etiotropic therapy.
Do not use the drug in patients undergoing vaccination, because the weakening of the immunity caused by the drug may make it difficult to form resistance to the disease against which the vaccine is directed. The ban period lasts for 2 months before vaccination and 2 weeks after this procedure.
It is not recommended to use the drug in immunodeficient states, including AIDS.
Long-term use in children is also not recommended, since an excess amount of prednisone can negatively affect the formation of a young body. In pediatric practice, the tool can be used only under strict medical supervision, in the minimum effective dose and minimally short courses. Even local forms should be used with care in children, since they are more likely to enter the systemic circulation than in adults, due to the larger ratio of body area to its mass in children
The number of contraindications for ointment and eye drops is less than that of tablets and solution. And this is not surprising, because the medicine in the form of ointment and drops acts only locally, without penetrating into the systemic circulation. Therefore, the disadvantages with this use of the drug is much less.
However, Prednisolone ointment should not be used with:
- bacterial, viral and fungal skin lesions
- skin tumors
- open wounds
- skin post-vaccination reactions
- trophic ulcers
Do not use the ointment for the treatment of infants (up to a year).
A woman should use ointment with caution if she is pregnant or is breastfeeding a baby.
Drops are not recommended for use with:
- increased intraocular pressure
- keratitis, caused by the herpes virus
- viral diseases of the cornea and conjunctiva
- infectious eye diseases
- corneal epitheliopathy
Due to the fact that the drug is not allowed in a large number of cases, before starting therapy, the patient should be examined for the presence of pathologies in which its reception can lead to negative consequences. The study should include examination of the cardiovascular system, stomach, urinary organs, eyes, blood tests (the amount of glucose and electrolytes), chest x-rays. During the period of therapy, periodic monitoring of electrolyte level, blood pressure, glucose level, and the state of the organs of vision is necessary. X-ray monitoring of bones and joints is recommended.
Use during pregnancy and lactation
Many probably wondered whether it is possible to use the tool during pregnancy. This is not highly recommended. The fact is that, in its composition, prednisone penetrates the fetus, and as shown by animal studies, it is capable of producing a teratogenic effect, that is, negatively affecting the development of the fetus. This effect is particularly pronounced at the very beginning of pregnancy, in its first trimester. However, during other periods of pregnancy, reception is also undesirable. In particular, adrenal atrophy may develop in the third trimester.
However, in cases where the medication is not enough, it is still prescribed to women awaiting addition to the family. But it should be remembered that during pregnancy, treatment is necessarily carried out under the supervision of a physician. After birth, a child whose mother has taken prednisone may experience adrenal suppression.
Although a very small dose of the drug penetrates into breast milk (approximately 1% of the blood concentration), however, this is enough to have a negative effect on the body of the newborn. Therefore, in such cases, mothers are encouraged to stop breastfeeding.
The drug affects various biochemical and physiological processes in the body. And this means that it affects various body systems and groups of organs.
The main systems on the part of which the appearance of side effects is possible while taking the medication:
- gastrointestinal tract
- respiratory system
On the part of the endocrine system, the following types of side effects are possible:
- reduced glucose tolerance
- steroid diabetes
- adrenal suppression
- Itsenko-Cushing syndrome
- delayed sexual development in children
On the part of the gastrointestinal tract, the following negative phenomena are possible:
- decrease in appetite
- gastric and duodenal ulcer
Side effects from the cardiovascular system:
- changes in ECG parameters
- arterial hypertension
On the part of the psyche and the nervous system, the following disorders are possible:
- affective insanity
- increased intracranial pressure
The following pathological phenomena associated with the eyes may also be observed:
- increased intraocular pressure up to damage the optic nerve
- bacterial, viral or fungal infections of the eye
- trophic changes of the cornea
- sudden loss of vision due to crystallization of the active substance in the eye vessels after parenteral administration to the head area
In addition, while taking the medication, the following pathologies associated with metabolic disorders are encountered:
- the acceleration of excretion of potassium from the body
- weight gain
- fluid and sodium retention in the body
- weight loss
When taking the medication often occurs hypokalemia syndrome, expressed in arrhythmias, severe fatigue and weakness, muscle pain. In children, ossification can slow down and growth slows down. Therefore, the attending physician should monitor the growth dynamics of the child in case of long-term therapy.
Other adverse events:
- bone necrosis
- excessive sweating
- tendon rupture
- delayed wound healing
- steroid acne
- skin rash
- exacerbation of infections
- increased blood clotting
In tablets and injection, the likelihood of systemic side effects is much higher than that of the local forms - drops and ointments. In addition, with injections, such phenomena as pain, the development of infections and numbness at the injection site are possible. With intramuscular injection, atrophy of subcutaneous tissue is possible.
When applying the ointment may cause steroid acne, burning, itching, irritation and dry skin.
The most dangerous side effect that occurs with long-term use of eye drops is an increase in intraocular pressure. For this reason, drops containing prednisone are not recommended for more than 10 days. The development of posterior capsule cataract is also possible.
Of course, the number of cases when, after taking a patient would appear severe reactions, is a small percentage. Nevertheless, such a situation is possible, and we should be prepared for it.
Also, to ensure the minimum number of negative manifestations during therapy, the patient should follow a diet. The diet should include a minimum of fat, salt and carbohydrates, a large amount of protein and vitamins.
After the end of long-term therapy during the year, the development of acute adrenal insufficiency is possible.
In old age, the number of adverse reactions increases.
Overdose when taking pills or parenteral administration is manifested in increased side effects. Symptomatic therapy and gradual withdrawal of the drug are recommended. In case of overdose of ointment and eye drops, hypersensitivity reactions are possible. In the case of an ointment, it is possible to completely stop using the product.
Means in the form of tablets or solution for injection may cause side effects in the form of dizziness, so patients are not recommended during the course of therapy to drive vehicles or perform work requiring concentration of attention. After instillation of suspension into the eyes, tearing is possible, so immediately after this procedure, the patient should also refrain from such exercises.