What are the common side effects of long-term prednisone use. How does prednisone interact with other medications. What are the potential risks associated with prolonged prednisone therapy.

Understanding Prednisone: A Powerful Corticosteroid Medication

Prednisone is a widely prescribed corticosteroid medication known for its potent anti-inflammatory and immunosuppressive properties. Healthcare providers often prescribe this drug to treat a variety of conditions, including rheumatoid arthritis, severe allergic reactions, lupus, and multiple sclerosis. Available in both immediate-release and delayed-release formulations, prednisone can be taken orally as a tablet or liquid solution.

While prednisone is undoubtedly effective in managing numerous medical conditions, its use comes with a range of potential side effects, especially when taken in large doses or for extended periods. These side effects can vary from mild to severe and may worsen over time, particularly with higher doses of the medication.

Common Side Effects of Long-Term Prednisone Use

Patients taking prednisone for extended periods may experience a variety of side effects. Some of the more common ones include:

• Mood and personality changes
• Insomnia
• Headaches and dizziness
• Fatigue and muscle weakness
• Increased hair growth
• Heartburn
• Weight gain and changes in fat distribution
• Skin changes (thinning, fragility, and discoloration)
• Excessive sweating
• Acne
• Slower wound healing
• Menstrual irregularities in women
• Decreased libido

Is long-term prednisone use associated with more severe side effects? Indeed, prolonged use of prednisone can lead to more serious health complications. These may include:

• Hyperglycemia (elevated blood sugar levels)
• Dyslipidemia (abnormal blood lipid levels)
• Increased susceptibility to infections
• Bone loss, osteoporosis, and heightened fracture risk
• Stunted growth in children
• Gastrointestinal inflammation and ulcers
• Severe hypertension
• Eye problems, including blurred vision
• Neurological symptoms such as numbness, tingling, and muscle twitching
• Depression and psychotic symptoms

Prednisone’s Impact on the Endocrine System

One of the most significant concerns with long-term prednisone use is its effect on the endocrine system. How does prednisone influence hormone production and regulation? Prednisone, being a synthetic form of cortisol, can suppress the body’s natural production of this crucial hormone. This suppression can lead to adrenal insufficiency, a condition where the adrenal glands cannot produce adequate amounts of cortisol.

Prolonged use of prednisone may also interfere with the hypothalamic-pituitary-adrenal (HPA) axis, which is responsible for regulating various bodily functions, including stress response, metabolism, and immune system function. This interference can result in:

• Cushing’s syndrome (characterized by weight gain, facial rounding, and other symptoms)
• Diabetes mellitus or worsening of existing diabetes
• Thyroid function abnormalities
• Growth retardation in children

Prednisone and Bone Health: A Critical Concern

Long-term prednisone use can have detrimental effects on bone health. How does this medication impact bone density and fracture risk? Prednisone interferes with calcium absorption and bone formation while simultaneously increasing bone resorption. This combination of effects can lead to:

• Osteoporosis
• Increased risk of fractures, particularly in the spine and hip
• Avascular necrosis (death of bone tissue due to lack of blood supply)

To mitigate these risks, healthcare providers often recommend calcium and vitamin D supplementation for patients on long-term prednisone therapy. In some cases, bisphosphonates or other bone-protecting medications may be prescribed to prevent or treat osteoporosis.

Prednisone’s Effects on the Immune System and Infection Risk

While prednisone’s immunosuppressive properties make it valuable in treating autoimmune disorders, they also increase the risk of infections. How does long-term prednisone use affect the immune system? Prednisone suppresses both innate and adaptive immune responses, leading to:

• Increased susceptibility to bacterial, viral, and fungal infections
• Reactivation of latent infections, such as tuberculosis or hepatitis B
• Slower wound healing and increased risk of post-operative complications
• Masking of infection symptoms, potentially delaying diagnosis and treatment

Patients on long-term prednisone therapy should be vigilant about infection prevention and promptly report any signs of infection to their healthcare provider. In some cases, prophylactic antibiotics may be recommended to reduce the risk of certain infections.

Cardiovascular and Metabolic Effects of Long-Term Prednisone Use

Prolonged use of prednisone can have significant impacts on the cardiovascular system and metabolism. What are the potential cardiovascular and metabolic consequences of long-term prednisone therapy? Some of the effects include:

• Hypertension (high blood pressure)
• Fluid retention and edema
• Dyslipidemia (abnormal blood lipid levels)
• Increased risk of atherosclerosis and cardiovascular events
• Weight gain and redistribution of body fat (typically to the face, neck, and abdomen)
• Insulin resistance and diabetes mellitus

To minimize these risks, healthcare providers may recommend regular monitoring of blood pressure, lipid levels, and blood glucose. Lifestyle modifications, such as a heart-healthy diet and regular exercise, may also be advised to counteract some of these effects.

Drug Interactions and Prednisone: What You Need to Know

Prednisone can interact with various medications, both over-the-counter and prescription drugs. These interactions can alter the effectiveness of prednisone or increase the risk of side effects. What are some important drug interactions to be aware of when taking prednisone?

• NSAIDs (e.g., aspirin, ibuprofen): Increased risk of gastrointestinal ulceration
• Antidiabetic medications: May require dose adjustments due to prednisone’s effect on blood sugar levels
• Cyclosporine: Potential increased risk of seizures
• Anticoagulants (e.g., warfarin): Prednisone may inhibit the body’s response to these medications
• Oral contraceptives: May increase the effects of prednisone
• Vaccines: Prednisone may reduce the effectiveness of certain vaccines

It’s crucial for patients to inform their healthcare providers about all medications, supplements, and herbal products they are taking to avoid potential interactions with prednisone.

Managing Side Effects and Risks of Long-Term Prednisone Use

While the side effects and risks associated with long-term prednisone use can be significant, there are strategies to minimize them. How can patients and healthcare providers manage the potential complications of prolonged prednisone therapy?

• Use the lowest effective dose for the shortest duration possible
• Consider alternate-day dosing or delayed-release formulations to reduce side effects
• Implement bone-protecting measures, such as calcium and vitamin D supplementation
• Monitor and manage blood pressure, blood sugar, and lipid levels
• Be vigilant about infection prevention and promptly treat any infections that occur
• Regularly assess the need for continued prednisone therapy and explore alternative treatments when possible
• Gradually taper the dose when discontinuing prednisone to avoid adrenal insufficiency

Patients should work closely with their healthcare providers to develop a personalized plan for managing the risks associated with long-term prednisone use.

Balancing Benefits and Risks: The Prednisone Dilemma

For many patients with chronic inflammatory conditions, prednisone can be a life-changing medication, providing relief from debilitating symptoms. However, the potential for long-term side effects creates a challenging dilemma for both patients and healthcare providers. How can one balance the benefits of prednisone against its potential risks?

The decision to use prednisone long-term should be made on a case-by-case basis, considering factors such as:

• The severity and nature of the underlying condition
• The availability and effectiveness of alternative treatments
• The patient’s individual risk factors for potential side effects
• The patient’s quality of life with and without prednisone therapy

In some cases, the benefits of prednisone may outweigh the risks, particularly when it is the only effective treatment option for a severe or life-threatening condition. In other situations, healthcare providers may explore alternative therapies or combination treatments to minimize the need for long-term prednisone use.

The Importance of Patient Education and Shared Decision-Making

Given the complex nature of long-term prednisone therapy, patient education and shared decision-making are crucial. How can healthcare providers ensure that patients are well-informed about the risks and benefits of prednisone?

• Provide comprehensive information about potential side effects and long-term risks
• Discuss alternative treatment options and their pros and cons
• Encourage patients to ask questions and express their concerns
• Involve patients in the decision-making process regarding their treatment plan
• Regularly reassess the treatment plan and adjust as needed

By fostering open communication and shared decision-making, healthcare providers can help patients make informed choices about their treatment and actively participate in managing the risks associated with long-term prednisone use.

Future Directions: Improving Long-Term Corticosteroid Therapy

As research continues to shed light on the long-term effects of prednisone and other corticosteroids, efforts are being made to develop safer and more targeted therapies. What are some promising developments in the field of corticosteroid treatment?

• Selective glucocorticoid receptor modulators (SEGRMs): These compounds aim to retain the anti-inflammatory benefits of corticosteroids while reducing side effects
• Improved drug delivery systems: Novel formulations and delivery methods may help optimize the therapeutic effects of prednisone while minimizing systemic exposure
• Combination therapies: Researchers are exploring combinations of prednisone with other medications to allow for lower doses and reduced side effects
• Personalized medicine approaches: Genetic and biomarker studies may help identify patients most likely to benefit from prednisone therapy or at higher risk for side effects

These advancements hold promise for improving the long-term management of conditions requiring corticosteroid therapy, potentially offering patients more effective and safer treatment options in the future.

Side Effects of Prednisone | Laguna Treatment Hospital

Written by: Editorial Staff

Edited by: Amanda Lautieri

Reviewed by: Scot Thomas, M.D.

Updated: Aug 02, 2022

Prednisone is a widely used prescription corticosteroid. It is a commonly used anti-inflammatory and immunosuppressive medication. It may be used in the treatment of conditions such as rheumatoid arthritis, severe allergic reactions, lupus, and multiple sclerosis, among other conditions.¹

The medication is taken by mouth, either as a tablet or oral solution,¹ and it is available in both immediate-release or delayed-release formulations.^2,3

What Are the Side Effects of Prednisone?

Though it’s a valuable pharmacotherapeutic used in a number of medical situations, prednisone has several significant side effects—especially if used in large amounts or for sustained periods of time. Side effects can range from mild to severe, and they may worsen over time, especially with higher doses of the medication. ⁴

Side effects may include:^1,5

• Personality/mood changes.
• Insomnia.
• Headache.
• Dizziness.
• Fatigue.
• Muscle weakness.
• Increased growth of hair.
• Heartburn.
• Weight gain.
• Changes in fat distribution through the body.
• Skin changes (increased thinness and fragility and/or red or purple blotches or lines under the skin).
• Sweating.
• Onset of acne.
• Slower healing of wounds.
• Irregular periods or amenorrhea in women.
• Lowered sexual interest.

Some side effects may be more serious, including:^1,5,6

• Hyperglycemia (increased blood glucose level).
• Dyslipidemia.
• Increased susceptibility to infections.
• Bone loss, osteoporosis, and increased fracture risk.
• Stunted growth (in children).
• Gastrointestinal inflammation.
• Nausea and/or vomiting.
• Stomach pain.
• Ulcers.
• Hacking cough.
• Very high blood pressure, which may lead to:
  • Severe headache.
  • Shortness of breath.
  • Confusion.
  • Arrhythmias.
  • Eye problems, including blurred vision.
• Numbness or tingling in face and extremities.
• Twitching of the muscles.
• Uncontrollable shaking of the hands.
• Seizures.
• Depression.
• Psychotic symptoms/loss of touch with reality.

How Does Prednisone Interact with Other Drugs?

Prednisone may negatively interact with other medications, both over-the-counter and prescription. Because prednisone is associated with a risk of gastrointestinal ulceration, patients are advised to avoid taking it in combination with aspirin or other NSAIDs.^4,6 Other drug interactions include the following:

• Because prednisone may increase blood sugar, individuals taking diabetic agents may require a dose adjustment of the antidiabetic medication. ⁴
• Patients taking both cyclosporine, an immunosuppressant, and prednisone have been reported to suffer convulsions.⁴
• Prednisone can inhibit the body’s response to anticoagulants, such as warfarin.⁴
• Oral birth control may increase the effects of prednisone.⁴

Prednisone may also interfere with the body’s normal response to vaccines, making them less effective. ⁴ Your doctor can evaluate the potential impact of these drug combinations to make a recommendation for your specific treatment plan needs.

What Risks Are Associated with Use?

There may be some negative risks associated with even short-term use of corticosteroids like prednisone. One study noted that over a 3-year period, approximately 1 in 5 Americans used an oral corticosteroid for less than 30 days. This short-term use of corticosteroids increased the risk of sepsis, venous thromboembolism, and bone fractures even at low doses. ⁷

Another concern with the use of prednisone is that some of the conditions that the drug treats are long-term chronic conditions, such as rheumatoid arthritis or asthma, but long-term use of prednisone continues to increase the risk of negative side effects. This puts many patients and doctors in a difficult position, as they need the medication to manage the symptoms of chronic conditions, but they may end up with other problems due to long-term use of the drug.⁷

Corticosteroid therapy is the first line of treatment for several inflammatory conditions and, in some cases, may be the only appropriate treatment option. Your doctor can discuss the risks and benefits of prednisone with you.

References:

1. U.S. National Library of Medicine. (2015). Prednisone.
2. (n.d.). Prednisone (Rx).
3. Alten R, Grahn A, Holt RJ, et al. Delayed-release prednisone improves fatigue and health-related quality of life: findings from the CAPRA-2 double-blind randomised study in rheumatoid arthritis. RMD Open 2015(1), e000134.
4. Horizon Pharma. (2012). Rayos (prednisone), Highlights of Prescribing Information.
5. Puckett Y, Bokhari AA. Prednisone. [Updated 2019 Apr 2]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2019 Jan-.
6. University of Maryland Medical Center. (n.d.). Taking Prednisone.
7. Waljee Akbar K, Rogers Mary A M, Lin Paul, Singal Amit G, Stein Joshua D, Marks Rory M et al. (2017). Short term use of oral corticosteroids and related harms among adults in the United States: population based cohort study. BMJ, 357:j1415.

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Prednisolone | healthdirect

Key facts

• Prednisolone is a medicine that belongs to a group of medicines called corticosteroids.
• Prednisolone helps reduce inflammation in your body, treating many conditions, but not curing them.
• Prednisolone is commonly used to treat some types of arthritis, asthma, skin problems and autoimmune diseases.
• If you take prednisolone for a long time, especially at a high dose, you may experience significant side effects.
• If you want or need to stop taking prednisolone, ask your doctor how to reduce the dose gradually to avoid serious side effects.

Looking for a medicine?

Visit healthdirect’s list of medicines that contain prednisolone to find out more about a specific medicine.

What is prednisolone?

Prednisolone is a medicine that belongs to a group of medicines called corticosteroids. Corticosteroids are synthetic (manufactured) versions of a natural body chemical called cortisol. This medicine helps reduce inflammation in your body or suppress your immune system.

Prednisone is a different medicine that is related to prednisolone and works in the same way to treat inflammatory diseases. Your doctor will prescribe the medicine and dose that is most suitable for your condition.

What is prednisolone used for?

Prednisolone helps reduce inflammation in your body.

Symptoms of inflammation may include:

• swelling
• redness
• pain or tenderness
• itching

Inflammation can affect any part of your body.

Prednisolone is used to treat many different conditions, including:

• severe allergies
• asthma
• some types of arthritis
• skin problems
• inflammatory diseases of the bowel
• autoimmune diseases — where your immune system mistakenly attacks normal cells in your body

How does prednisolone work?

Prednisolone enters the cells that cause inflammation and blocks the body’s inflammatory reaction. It reduces the symptoms of some conditions, but is doesn’t cure them.

What forms of prednisolone are available?

Prednisolone is the name of the active ingredient. It is available in many different brands, which have different:

• names
• appearances (size, shape or colour)
• forms (tablets, liquid, eye drops and suppositories)
• strengths

No matter which brand you are prescribed, prednisolone works in the same way to treat your condition.

In Australia, you need a doctor’s prescription to buy prednisolone.

What are the possible side effects of prednisolone?

Prednisolone helps most people who take it, but some people experience side effects.

Generally, the risk of side effects is low if you take prednisolone for a short time. Your risk increases if you take high doses of prednisolone for a long time.

Common side effects of prednisolone, especially with high doses for long periods, include:

• fluid retention including bloating of the face and swelling of the abdomen
• weight gain
• irregular periods
• muscle cramps
• thin skin that bruises easily, and acne
• osteoporosis (thinning of the bones)
• high blood pressure

Some psychological side effects include:

• trouble sleeping
• irritability, agitation or depression

In children, prolonged use of prednisolone can cause slowed growth.

Prolonged use of prednisolone in children and adults can increase your chance of developing some infections. It can also cause thyroid problems.

Some side effects can only be noticed by your doctor. If you take prednisolone for long periods of time, you should have regular check-ups.

See your doctor immediately or go to the emergency department of your nearest hospital if you experience any of these serious side effects:

• severe abdominal pain
• seizures
• sudden changes in your vision
• symptoms such as severe dizziness, fainting, weakness, chest pain or irregular heart beat
• abnormal changes in your mood or behaviour

If you experience a serious or life-threatening side effect, call triple zero (000) and ask for an ambulance.

This is not a full list of side effects. For more information about the risks of side effects, read the Consumer Medicines Information (CMI) for the brand of prednisolone you are taking or speak to your doctor or pharmacist. Although there are many possible side effects, you may not experience any of them.

What should I be careful of when taking prednisolone?

It is important to take prednisolone as prescribed. Talk with your doctor if you would like to lower your dose or stop taking prednisolone. Stopping it suddenly might cause serious side effects and can be dangerous.

Make sure to tell your doctor, surgeon or dentist that you are taking prednisolone, as surgery or illness may affect the dose you need to take.

When should I speak to my doctor?

Speak to your doctor if you:

• experience side effects that trouble you
• have signs of an allergic reaction
• have a health condition or are taking medication that may affect how your body reacts to prednisolone
• become pregnant or start breastfeeding

See the Consumer Medicines Information (CMI) for full details about when to speak with your doctor before or after you have started taking prednisolone.

Your doctor or pharmacist can provide more information to improve some possible side effects. For example, ask them if taking prednisolone with food can reduce indigestion or heartburn, or if taking corticosteroids in the morning can help prevent sleep disturbances.

ASK YOUR DOCTOR — Preparing for an appointment? Use the Question Builder for general tips on what to ask your GP or specialist.

Are there alternatives to prednisolone?

Because prednisolone is used for many medical conditions, its alternatives depend on the condition you’re taking it for. Discuss options with your doctor.

Resources and support

Asking about your treatment or medication is important to help you understand your options. Read our guide to important questions to ask your pharmacist or doctor before taking a medicine.

You can also visit healthdirect’s list of medicines that contain prednisolone to read the CMI for the brand of prednisolone prescribed.

Learn more here about the development and quality assurance of healthdirect content.

PREDNISOLONE TAB. 5MG No. 100

Composition

1 tablet contains:

active ingredient: prednisolone 5 mg

excipients: colloidal silicon dioxide, potato starch, stearic acid, magnesium stearate, talc, povidone, corn starch, lactose mono hydrate.

Dosage form

tablets

Description

White or off-white flat-cylindrical tablets, beveled and engraved with “P” on one side.

Action

GKS. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of ​​inflammation. Violates the ability of macrophages to phagocytosis, as well as to the formation of interleukin-1. Contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of ​​inflammation. Reduces capillary permeability due to the release of histamine. Suppresses the activity of fibroblasts and the formation of collagen.
Inhibits the activity of phospholipase A2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce the production of prostaglandins.
Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue, inhibits the formation of antibodies.
Prednisolone inhibits the release of pituitary ACTH and ?-lipotropin, but does not reduce the level of circulating ?-endorphin. Inhibits the secretion of TSH and FSH.
When applied directly to the vessels, it has a vasoconstrictor effect.
Prednisolone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, and increases the activity of gluconeogenesis enzymes. In the liver, prednisolone enhances the deposition of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from protein metabolism products. An increase in blood glucose stimulates the secretion of insulin.
Prednisolone inhibits the uptake of glucose by fat cells, which leads to the activation of lipolysis. However, due to an increase in insulin secretion, lipogenesis is stimulated, which contributes to the accumulation of fat.
Has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone, it affects the processes of water-electrolyte metabolism: it promotes the excretion of potassium and calcium ions, the retention of sodium and water ions in the body. Osteoporosis and Itsenko-Cushing’s syndrome are the main factors limiting long-term therapy with corticosteroids. As a result of the catabolic action, growth suppression in children is possible.
In high doses, prednisolone can increase the excitability of brain tissue and help lower the seizure threshold. Stimulates excess production of hydrochloric acid and pepsin in the stomach, which leads to the development of peptic ulcers.
When used systemically, the therapeutic activity of prednisolone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.
With external and local application, the therapeutic activity of prednisolone is due to anti-inflammatory, anti-allergic and anti-exudative (due to the vasoconstrictor effect) action.
Compared with hydrocortisone, the anti-inflammatory activity of prednisolone is 4 times greater, the mineralocorticoid activity is 0.6 times less.

Pharmacodynamics

Prednisolone is a synthetic glucocorticoid drug, a dehydrated analogue of hydrocortisone. It has anti-inflammatory, anti-allergic, desensitizing, anti-shock, anti-toxic and immunosuppressive effects.

Interacts with specific cytoplasmic receptors and forms a complex that penetrates into the cell nucleus, stimulates the synthesis of matrix ribonucleic acid (mRNA), the latter induces the formation of proteins, incl. lipocortin mediating cellular effects. Lipocortin inhibits phospholipase A2, inhibits the release of arachidonic acid and inhibits the synthesis of endoperoxides, prostaglandins, leukotrienes, which promote inflammation, allergies, etc.

Suppresses the release of adrenocorticotropic hormone by the pituitary gland and, secondarily, the synthesis of endogenous glucocorticosteroids. It inhibits the secretion of thyroid-stimulating and follicle-stimulating hormones.

Reduces the number of lymphocytes and eosinophils increases – erythrocytes (stimulates the production of erythropoietins).

Protein metabolism: reduces the amount of protein in plasma (due to globulins) with an increase in the albumin / globulin ratio, increases the synthesis of albumins in the liver and kidneys: increases protein catabolism in muscle tissue.

Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.

Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract increases the activity of glucose-6-phosphatase, leading to an increase in glucose from the liver into the blood, increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, leading to the activation of gluconeogenesis.

Water-electrolyte metabolism: retains sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, “washes” calcium from the bones, increases its excretion by the kidneys.

The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils and mast cells, induction of the formation of lipocortin and a decrease in the number of mast cells that produce hyaluronic acid with a decrease in capillary permeability, stabilization of cell membranes and organelle membranes (especially lysosomal).

The anti-allergic effect develops as a result of suppression of the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, a decrease in the number of circulating basophils, suppression of the development of lymphoid and connective tissue, and a decrease in the number of T- and B-lymphocytes. mast cells, reducing the sensitivity of effector cells to allergy mediators, inhibition of antibody production. changes in the body’s immune response.

In obstructive diseases of the respiratory tract, the action is mainly based on inhibition of inflammatory processes, inhibition of the development or prevention of mucosal edema, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium and deposition of circulating immune complexes in the bronchial mucosa. There is inhibition of erosion and desquamation of the mucous membrane. Prednisolone increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by inhibiting or reducing its production.

Antishock and antitoxic action is associated with an increase in blood pressure (due to an increase in the concentration of circulating catecholamines and restoration of sensitivity to them by adrenoreceptors, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane-protective properties, and activation of liver enzymes involved in the metabolism of endo- and xenobiotics.

The immunosuppressive effect is due to the inhibition of the proliferation of lymphocytes (especially T-lymphocytes), the suppression of B-cell migration and the interaction of T- and B-lymphocytes. inhibition of the release of cytokines (interleukin-1, interleukin-2 gamma-interferon) from lymphocytes and macrophages and a decrease in the formation of antibodies.

Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Pharmacokinetics

Absorption – high, the maximum concentration in the blood when taken orally is reached after 1-1. 5 hours. In plasma, up to 90% of prednisolone binds to proteins: transcortin (cortisol-binding globulin) and albumin.

Metabolized in the liver, kidneys, small intestine, bronchi. The oxidized forms are glucuronidated or sulfated. Metabolites are inactive. The half-life is 2-4 hours. It is excreted in bile and urine by glomerular filtration and by 80-90% is reabsorbed by the tubules. 20% is excreted by the kidneys unchanged.

Indications for use

Endocrine disorders: primary and secondary adrenal insufficiency (including the condition after removal of the adrenal glands) congenital adrenal hyperplasia: subacute thyroiditis, hypoglycemic conditions.

Systemic connective tissue diseases: rheumatoid arthritis: systemic lupus erythematosus dermatomyositis scleroderma: periarteritis nodosa.

Acute rheumatism, acute carditis, chorea minor.

Acute and chronic educational diseases of the joints humeroscapular periarthritis ankylosing spondylitis (Bekhterev’s disease) gouty and psoriatic arthritis osteoarthritis (including post-traumatic) polyarthritis juvenile arthritis, Still’s syndrome in adults bursitis nonspecific tendosynovitis synovitis epicondylitis.

Acute and chronic allergic diseases: allergic reactions to drugs and food drug exanthema serum sickness urticaria pollinosis angioedema allergic rhinitis.

Bronchial asthma, status asthmaticus.

Diseases of the blood and the hematopoietic system: autoimmune hemolytic anemia; acute lympho- and myeloid leukemia; lymphogranulomatosis; thrombocytopenic purpura; agranulocytosis; panmyelopathy; secondary thrombocytopenia in adults;

Skin diseases: pemphigus eczema, psoriasis, exfoliative dermatitis atopic dermatitis diffuse neurodermatitis contact dermatitis (with damage to a large surface of the skin) toxidermia seborrheic dermatitis toxic epidermal necrolysis (Lyell’s syndrome) bullous dermatitis herpetiformis malignant exudative erythema ma (Stevens-Johnson syndrome).

Allergic and inflammatory diseases of the eye: allergic corneal ulcers allergic forms of conjunctivitis sympathetic ophthalmia severe indolent anterior and posterior uveitis optic neuritis.

Diseases of the gastrointestinal tract: ulcerative colitis, Crohn’s disease, hepatitis, local enteritis.

Lung cancer (in combination with cytotoxic drugs).

Myeloma.

Lung diseases: acute alveolitis, pulmonary fibrosis, stage II-III sarcoidosis.

Kidney diseases of autoimmune origin (including acute glomerulonephritis), nephrotic syndrome.

Tuberculous meningitis, pulmonary tuberculosis.

Aspiration pneumonia (in combination with specific chemotherapy).

Berylliosis, Loeffler’s syndrome (not amenable to other therapy).

Multiple sclerosis.

Cerebral edema (including on the background of a brain tumor or associated with surgery, radiation therapy or head trauma) after prior parenteral use.

Prevention of transplant rejection in organ transplants.

Hypercalcemia due to oncological diseases. Nausea and vomiting during cytostatic therapy.

Contraindications

The only contraindication for short-term use for health reasons is hypersensitivity to prednisolone or drug components.

In children during the period of growth, glucocorticosteroids should be used only if absolutely indicated and under the most careful supervision of the attending physician.

Use in pregnancy and lactation

Prednisolone may be used during pregnancy if the expected benefit to the mother outweighs the potential risk to the fetus.

In the first trimester of pregnancy, prednisolone is used only for health reasons.

With long-term therapy during pregnancy, the possibility of impaired fetal growth is not excluded. In the case of use in the III trimester of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

Since glucocorticosteroids pass into breast milk, if necessary, the use of the drug during breastfeeding is recommended to stop breastfeeding.

Use in children

In children during the period of growth, GCS should be used only according to absolute indications and under the close supervision of a physician.
Contraindication for external use: children’s age (up to 2 years, with itching in the anus – up to 12 years).

Side effects

The frequency and severity of side effects depend on the duration of use, the size of the dose used and the ability to comply with the circadian rhythm of prednisolone administration.

From the endocrine system: suppression of adrenal function, decreased glucose tolerance, “steroidal” diabetes mellitus or manifestation of latent diabetes mellitus, Itsenko-Cushing’s syndrome (moon face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis , striae), growth retardation and delayed sexual development in children.

Gastrointestinal tract: oral candidiasis, nausea, vomiting, pancreatitis, “steroid” gastric and duodenal ulcer, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases, an increase in the activity of “liver” transaminases and alkaline phosphatase.

From the side of the cardiovascular system: increased blood pressure, arrhythmias, bradycardia, development (in predisposed patients) or increased severity of chronic heart failure, ECG changes characteristic of hypokalemia, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction – the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.

From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, cerebellar pseudotumor, headache, convulsions.

From the sensory organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos.

From the side of metabolism: hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating.

Side effects due to mineralocorticoid activity – fluid and sodium retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, weakness and fatigue).

On the part of the musculoskeletal system: growth retardation and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely – pathological bone fractures, aseptic necrosis of the head of the humerus and femur), rupture of muscle tendons, “steroid” myopathy a decrease in muscle mass (atrophy).

On the part of the skin and mucous membranes: delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, acne, striae, a tendency to develop pyoderma and candidiasis.

Diseases of the kidneys and urinary tract: frequent nocturnal urination, urolithiasis due to increased excretion of calcium and phosphate.

Diseases of the immune system: generalized (skin rash, skin itching, anaphylactic shock) and local allergic reactions.

Other: the development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia.

Interaction

Phenobarbital, phenytoin, rifampicin, ephedrine, aminoglutethimide, aminophenazone (inducers of “liver” microsomal enzymes) reduce the therapeutic effect of glucocorticosteroid hormones.

An increase in the dose of insulin and oral hypoglycemic agents may be required due to the weakening of the hypoglycemic effect.

Both an increase and a decrease in the anticoagulant effect are possible when taking indirect anticoagulants (dose adjustment is required).

Anticoagulants and thrombolytics – increased risk of bleeding from ulcers in the gastrointestinal tract.

Non-steroidal anti-inflammatory drugs:

Acetylsalicylic acid – prednisolone accelerates its excretion and reduces the concentration in the blood. After the abolition of glucocorticosteroid drugs, an increase in the concentration of salicylates and the development of intoxication are possible due to the ulcerogenic effect of salicylates, the risk of developing gastrointestinal bleeding and ulceration increases.

Indomethacin – increases the risk of side effects of prednisolone (displacement of prednisolone by indomethacin from albumin bonds).

The risk of hypokalemia increases when taking amphotericin B, diuretics, theophylline, cardiac glycosides.

Carbonic anhydrase inhibitors and loop diuretics may increase the risk of osteoporosis.

When taking estrogens and oral estrogen-containing contraceptives, the clearance of glucocorticosteroids is reduced, the half-life is prolonged, and the therapeutic and toxic effects of prednisolone are enhanced.

Hemotoxicity of methotrexate increases.

Reduces the stimulating effect of somatropin on growth.

Vitamin D – its effect on calcium absorption in the intestine is reduced.

Praziquantel – its concentration decreases.

M-anticholinergics (including antihistamines and tricyclic antidepressants) and nitrates – increases intraocular pressure.

Isoniazid and mexiletine – prednisolone increases their metabolism (especially in “slow” acetylators), which leads to a decrease in their plasma concentrations.

Adrenocorticotropic hormone enhances the action of prednisone.

Ergocalciferol and parathormone prevent the development of prednisolone-induced osteopathy.

Cyclosporine and ketoconazole, by slowing down the metabolism of prednisolone, can in some cases increase its toxicity.

Glucocorticosteroids reduce the hypotensive effect of antihypertensive drugs.

Simultaneous administration of androgens and anabolic steroid drugs with prednisolone contributes to the development of peripheral edema and hirsutism, the appearance of acne.

Mitotane and other inhibitors of adrenal function may necessitate an increase in the dose of prednisolone.

When used simultaneously with live antiviral vaccines and against the background of other types of immunization, it increases the risk of virus activation and the development of infections.

Immunosuppressants increase the risk of developing infections and lymphoma or other lymphoproliferative disorders associated with the Epstein-Barr virus.

Antipsychotics (neuroleptics) and azathioprine increase the risk of developing cataracts when prednisolone is prescribed.

Simultaneous administration of antacids reduces the absorption of prednisolone.

With simultaneous use with antithyroid drugs, it decreases, and with thyroid hormones, the clearance of prednisolone increases.

Method of administration and doses

The dose and duration of treatment is selected by the doctor on an individual basis, depending on the indications and severity of the disease.

Usually take a single daily dose or take a double dose every other day, in the morning, between 6 and 8 am.

The high daily dose can be divided into 2-4 doses, with the larger dose taken in the morning. Tablets should be taken during or immediately after a meal with a small amount of liquid.

In acute conditions and as replacement therapy for adults, the initial dose is 20-30 mg/day, the maintenance dose is 5-10 mg/day. In some diseases (nephrotic syndrome, some rheumatic diseases), higher doses are prescribed. Treatment is stopped slowly, gradually reducing the dose. If there is a history of psychosis, high doses are prescribed under the strict supervision of a physician.

Doses for children: initial dose – 1-2 mg/kg/day in 4-6 divided doses, maintenance – 0.3-0.6 mg/kg/day.

When prescribing, the daily secretory rhythm of glucocorticosteroids should be taken into account: most (or all) of the dose is prescribed in the morning.

Overdose

If side effects occur, reduce the dose of prednisolone. There is no specific antidote, treatment is symptomatic. It is necessary to control blood electrolytes.

Special instructions

Before starting treatment, the patient should be examined for possible contraindications. Clinical examination should include examination of the cardiovascular system, X-ray examination of the lungs, examination of the stomach and duodenum, urinary system, and organ of vision. Before and during steroid therapy, it is necessary to control the complete blood count, the concentration of glucose in the blood and urine, and electrolytes in the plasma. During the period of treatment with glucocorticosteroids, especially in high doses, it is not recommended to vaccinate due to a decrease in its effectiveness.

Medium and high doses of glucocorticosteroids may cause an increase in blood pressure.

In tuberculosis, the drug can only be administered in conjunction with anti-tuberculosis drugs.

Intercurrent infections, septic conditions require simultaneous antibiotic therapy.

In long-term treatment with glucocorticosteroids, potassium should be given to avoid hypokalemia.

In Addison’s disease, the drug should not be taken simultaneously with barbiturates because of the risk of developing acute adrenal insufficiency (Addisonian crisis).

Glucocorticosteroid hormones may cause growth retardation in children and adolescents. Prescribing the drug every other day usually avoids or minimizes the likelihood of developing such a side effect.

In old age, the frequency of adverse reactions increases.

With sudden withdrawal, especially in the case of high doses, there is a syndrome of “withdrawal” of glucocorticosteroids: loss of appetite, nausea, lethargy, generalized musculoskeletal pain, asthenia.

The likelihood of drug-related adrenal insufficiency and associated complications can be reduced by gradual withdrawal of the drug. After discontinuation of the drug, adrenal insufficiency can last for months, therefore, in any stressful situation during this period, hormone therapy should be resumed.

In hypothyroidism and liver cirrhosis, the effect of glucocorticosteroid hormones may increase.

Patients should be warned in advance that that they and their loved ones should avoid contact with patients with chicken pox, measles, herpes. In cases where systemic treatment with glucocorticosteroids is carried out or treatment with glucocorticosteroid drugs was carried out in the next 3 months, and the patient was not vaccinated, specific immunoglobulins should be prescribed.

Treatment with glucocorticosteroids requires medical supervision for diabetes mellitus (including a family history), osteoporosis (higher risk in postmenopausal periods), hypertension, chronic psychotic reactions (glucocorticosteroid hormones can cause mental disturbances and increase emotional instability), tuberculosis history, glaucoma, steroid myopathy, gastric and duodenal ulcer, epilepsy, herpes simplex eye (danger of corneal perforation).

Due to the weak mineralocorticoid effect, prednisolone is used with mineralocorticoids for replacement therapy in adrenal insufficiency.

In diabetic patients, blood glucose levels should be monitored and therapy adjusted if necessary.

Influence on the ability to drive vehicles and control mechanisms

A similar effect of the drug is unknown.

Presentation

Tablets, 5 mg.

100 tablets in a polypropylene bottle with a tamper-evident cap.

One bottle in a carton box with attached instructions for use.

Pharmacy conditions

Prescription

Storage conditions

Store at a temperature not exceeding 25°C.

Keep out of reach of children.

Shelf life

5 years.

Do not use after the expiration date.

Manufacturer and consumer complaints organization

GEDEON RICHTER

Prednisolone side effects to watch out for

The medical drug Prednisolone belongs to the group of synthetic glucocorticoids, which has all the properties inherent in the compounds of this group. Long-term use of the drug in high doses causes side effects of Prednisolone.

Contents:

• 1 Storm Therapy
• 2 Clinical Observations of Prednisolone
• 3 Metabolic Side Effects of Prednisolone
  • 3.1 Cardiovascular Side Effects
  • 3.2 Side effects on the endocrine system
  • 3.3 Side effects on the gastrointestinal tract
  • 3.4 Side effects on the immune system
  • 3. 5 Side effects on the musculoskeletal system
  • 3.6 Side effects face-to-face effects on the organs of vision
  • 3.7 Other side effects effects

“Assault” therapy drug

Prednisolone – a drug of the hormonal group

The drug is prescribed only in emergency cases, when the main therapy does not lead to the proper result, or the treatment begins to take a protracted character. With an ineffective clinical picture, the appointment is carried out in a short course using high doses of the drug. Long-term use of a large volume of Prednisolone can cause a protein deficiency in the blood plasma, which threatens to toxic release of free progesterone. Reasons why Prednisolone is classified as a hormonal drug:

1. Deficiency of progesterone in the plasma protein, as a rule, leads to impaired growth and sexual development of adolescents during maturation, or at a transitional age.
2. Prednisolone causes an increase in blood sugar levels in diabetic patients.
   In addition, the drug is capable of simultaneous actions to enhance the decay and neoplasm of fat cells deposited in tissues, which leads to a transient process of obesity.
3. An excess of Prednisolone leads to a violation of mineral metabolism, since the drug is able to remove potassium from the body, thereby reducing myocardial contractility. This leads to myocardial infarction and the risk of a heart attack.
4. Prednisolone depletes calcium from the body, leading to osteoporosis, or thinning of the bones. The bones become brittle and may break from slight bruising.
5. The action of the drug in the cells of the body retains water and sodium, causing severe swelling.

Prednisolone is produced in various forms, according to the formulation: powder, injection solution, suspension injection, oral liquid, oral suspension, oral syrup, oral tablets, dissolving tablets for oral use.

Clinical observations of the action of Prednisolone

Patients who received an average of 10 mg per day of Prednisolone for several months had 50% less infection with infectious diseases compared with patients who received an average of 20 mg per day of the drug. Significantly fewer episodes of aseptic necrosis were noted, with a trend towards fewer complications in patients with low doses of the drug.

Prednisolone – release form: solution for injection

At the same time, side effects of Prednisolone were observed, manifested when using minimal doses, but their manifestation was presented in an insignificant amount. Doses greater than 10 mg per day have been associated with an increase in side effects in a significant subset of patients. Side effects from taking Prednisolone can be divided into those associated with short-term therapy, lasting up to three weeks, and manifestations after long-term therapy, conducted over three weeks.

Short-term courses of the drug included effects associated with increased accumulation of sodium weight parts and fluid accumulation. These may include hyperglycemia, glucose intolerance, hypokalemia, gastrointestinal disturbances with ulceration, and reversible depression of the hypothalamic-pituitary-adrenal axis. On the part of the psychomotor and nervous system, patients experienced a sharp change in mood – from euphoria to insomnia.

Frequent cases of nervousness, anxiety, mania of several modifications, catatonia, depression, delusions, hallucinations and aggressive behavior have been reported among patients taking large doses of prednisolone.

Long-term use of the drug has led to such long-term side effects as depressed appearance and confusion, hirsutism or virilism, impotence, menstrual irregularities, peptic ulcer, cataracts and increased intraocular pressure, the development of glaucoma, myopathy, osteoporosis, up to compression fractures of the spine.

Metabolic side effects of Prednisolone

When observing the metabolic side effects of Prednisolone, hypernatremia, hypokalemia, fluid retention in the body, a negative nitrogen balance and an increased concentration of urea nitrogen in the blood have been reported. In the course of research, it turned out that glucocorticoids significantly reduce the secretion of thyrotropin.

Side effects on the cardiovascular system

Prednisolone: ​​formulation – ointment

On the part of the cardiovascular system, hypertensive syndrome, persistent heart failure due to long-term storage of fluid in the cells, as well as a direct effect of vascular contraction were observed. Studies have shown that patients may develop systolic hypertension. It turned out to be susceptible to 12% of the total number of observed patients. As it turned out, hypertension was associated with long-term corticosteroid therapy and, the researchers believe, due to fluid retention. In some cases, changes in blood pressure occurred due to the advanced age of patients.

Endocrine side effects

Endocrine side effects included glucose intolerance and hyperglycemia. Diabetes, as a symptom, can develop in people prone to this disease, or suffering from a heredity factor. Hypothalamic-pituitary-adrenal suppression may be extended up to a calendar year after long-term therapy with prednisolone. The observed effect of the manifestation of Itsenko-Cushing’s disease was most likely associated with the therapy of a chronic disease. In addition, hirsutism or virilism, impotence, and menstrual irregularities may also be a reflection of prednisolone therapy for chronic conditions.

Corticosteroid therapy can induce glucose intolerance by decreasing sugar utilization in liver tissues and increasing glucose output. Patients on long-term therapy may exhibit significantly higher serum glucose levels if the test was taken on the day of taking prednisolone. For example, it has been observed in patients with diabetes mellitus requiring treatment with a modified diet using glucose-regulating and hypoglycemic drugs.

Adrenal suppression may persist up to twelve months after long-term corticosteroid therapy. Adrenal suppression can be reduced by reducing the use of corticosteroids to once a day or every other day. Perdnisolone treatment may be used as adjunctive corticosteroid therapy during times of stress, infectious disease, surgery, or serious injury.

Gastrointestinal side effects

Gastrointestinal side effects from the use of Prednisolone included gastrointestinal disturbances, nausea, vomiting and peptic ulcer. There were also manifestations of pancreatitis, and in isolated cases, the manifestation of gastrointestinal bleeding and perforation of the walls of the stomach. The most common side effect of Prednisolone is gastrointestinal upset, with nausea, vomiting, indigestion, and anorexia. Rare manifestations of peptic ulcer, as the researchers suggest, have been associated with long-term corticosteroid therapy.

Immune system side effects

Immune system side effects included impairment of cellular immunity. This results in an increased susceptibility of patients to bacterial, viral, fungal and parasitic infections. In addition, the immune response to skin tests may be suppressed.

Side effects on the musculoskeletal system

On the part of the musculoskeletal system during corticosteroid therapy, manifestations of myopathy were observed in the form of weakness and wasting of the proximal limbs and muscle belt. As a rule, such processes are reversible after cessation of therapy. Corticosteroids inhibit calcium absorption in the intestine. The resulting increase in urinary calcium excretion leads to bone resorption and bone loss. Bone loss of more than 3% in one year was a demonstration of taking Prednisolone at the appointment of 10 mg of the drug per day.

Postmenopausal women are particularly at risk for bone loss. Elderly patients, 16% of the total number of people studied, received corticosteroids for 5 years. These people are at risk for spinal compression fractures because they have experienced bone loss. Studies have shown bone loss in women with concomitant therapy with prednisolone 7.5 mg daily plus tamoxifen occurring within two years of drug initiation.

Adverse events affecting the musculoskeletal system included myopathy, osteoporosis, spinal compression and fractures, and avascular necrosis of the bone. Aseptic necrosis is the most common factor in damage to the femoral head.

Side effects on the organs of vision

Prednisolone – dosage form: tablets

On the part of the visual system, there is an increase in eye pressure and the development of cataracts. In kidney transplant patients who were prescribed prednisolone at a dosage of 10 mg per day, 33% of patients developed posterior subcapsular cataracts. The median time for cataract development is 26 months. In this case, the cataract developed in less than a year. An increase in intraocular pressure was observed in 5% of patients. Also, glaucoma was included in the side effect on the part of the organs of vision.

Other manifestations of side effects

Other side effects included:

1. Glucocorticoid withdrawal syndrome. It is observed as a result of an abrupt cessation of taking Prednisolone. Typically causes adrenal suppression syndrome.
2. Rheumatoid arthritis, or glucocorticoid withdrawal syndrome. The syndrome may occur after discontinuation of corticosteroids.