Prednisone

ATC CodeA07EA03, H02AB07
CAS number53-03-2
PUB number5865
Drugbank IDDB00635
Empirical formulaC21H26O5
Molar mass (g·mol−1)358,4281
Physical statesolid
Melting point (°C)230-235
PKS value12,58
Solubility77.54 mg/L

Basics

Prednisone is an active ingredient that has an anti-inflammatory and anti-allergic effect. It also regulates our immune defense (immunosuppressive) if it is too strong (allergy) or if this is necessary, as is the case with organ transplants.

Prednisone is a prodrug, which means that it is inactive and is only converted into its active form, i.e. prednisolone, in the body where it is supposed to work. Prednisone is a steroid hormone and belongs to the group of glucocorticoids.

Prednisone is used to treat allergic symptoms, inflammatory skin diseases, inflammatory bowel diseases(Crohn's disease, ulcerative colitis), arthritis, lupus, psoriasis, bronchial asthma, chronic obstructive pulmonary disease (COPD), rheumatic diseases, pseudo-croup, adrenal insufficiency, allergic or inflammatory eye diseases and tumor diseases.

Graphic structural formula of the active substance prednisone

Effect

Prednisone is converted to prednisolone in the liver. Prednisolone, also a glucocorticoid, binds to the glucocorticoid receptors and thus suppresses inflammatory processes in the body by preventing the migration of inflammatory cells into damaged tissue. This is achieved by reducing the fluid permeability of the smallest vessel walls (capillaries). This makes it difficult for inflammatory cells to migrate into the tissue. In addition, vascular enlargement (vasodilation) is suppressed. This has the advantage that the inflammatory cells cannot move through the blood vessels as quickly and therefore an inflammatory reaction takes place more slowly. In addition, the release of inflammatory mediators, i.e. substances that control inflammatory processes in the body, is suppressed.

Prednisone is absorbed in the intestine, converted to prednisolone in the liver, broken down and excreted via the kidneys. The half-life, i.e. the time the body needs to break down half of the active ingredient, is 2-3 hours. Less than half of prednisone is bound to plasma proteins.

It is important to note that prednisone also increases susceptibility to infection by regulating our immune system (immunosuppressive).

Dosage

Always take prednisone exactly as described in the package leaflet or as advised by your doctor.

The usual dose for hormone replacement treatment is 5-7.5 mg per day. This is divided into 2 single doses per day. The dose should be increased by the doctor if particular physical stress occurs (e.g. infection, operation).

Tablets in different dosages are available for the treatment of various other illnesses.

In general, however, the following guidelines apply to adults:

  • high dose - 80-100 mg/day
  • medium dose - 40-80 mg/day
  • low dose - 10-40 mg/day
  • very low dose - 1.5-7.5 mg/day

For children, the following general guidelines apply:

  • high dose - 2-3 mg/kg body weight (bw)/day
  • medium dose - 1-2 mg/kg bw/day
  • maintenance dose - 0.25 mg/kg bw/day

The dosage in children should be as low as possible!

The dose should be reduced as soon as the desired effect has been achieved (tapering) and adjusted to a maintenance dose or stopped completely. Dose reduction (tapering) is only ever done by your doctor and should never be carried out independently.

In the case of high doses over a few days, it is possible to dispense with tapering. However, this is also only decided by your doctor!

For a few diseases such as non-Hodgkin's lymphoma, chronic lymphocytic leukemia, Hodgkin's disease and multiple myeloma, only a single dose is usually administered. In these cases, it is not necessary to taper the dose.

Prednisone should be taken with sufficient liquid and during or immediately after a meal.

Treatment with prednisone should always be mentioned to other doctors, specialists or in hospital, as prednisone interacts with other frequently used medications.

Side effects

Side effects when taking prednisone are highly dependent on the dose and duration of therapy.

In general, the following side effects may occur:

  • viral, fungal and bacterial infections
  • parasitic infections
  • Dwarf threadworm infections
  • blood count changes
  • Hypersensitivity reactions (e.g. skin rash)
  • severe allergic reactions (anaphylaxis)
  • cardiac arrhythmia
  • convulsions
  • fluctuations in blood pressure
  • circulatory collapse
  • cardiac arrest
  • Weakening of the immune system
  • Hormonal disorders (Cushing's syndrome, inactivity or atrophy of the adrenal cortex)
  • Increase in appetite and weight gain
  • Increased blood sugar levels
  • Diabetes (diabetes mellitus)
  • Increased blood lipids (cholesterol and triglycerides)
  • Water retention (oedema)
  • potassium deficiency
  • depression
  • irritability
  • euphoria
  • Increased drive
  • psychoses
  • mania
  • hallucinations
  • Mood instability
  • feelings of anxiety
  • sleep disorders
  • suicidal tendencies
  • increased intracranial pressure
  • epilepsy
  • Cataracts
  • Glaucoma
  • Worsening of corneal ulcers
  • Eye infections caused by viruses, bacteria or fungi
  • Blurred vision
  • High blood pressure (hypertension)
  • Increased risk of arteriosclerosis and thrombosis
  • vascular inflammation
  • increased vascular fragility
  • gastrointestinal ulcers
  • gastrointestinal bleeding
  • pancreatitis
  • stretch marks
  • Thinning of the skin ("parchment skin")
  • Dilated skin vessels
  • Increased tendency to bruise
  • skin bleeding
  • Increased body hair
  • acne
  • Inflammatory skin changes on the face (incl. mouth, nose and eyes)
  • changes in skin pigmentation
  • muscle weakness
  • Muscle atrophy, bone atrophy (osteoporosis) and bone loss
  • Tendon inflammation and tendon ruptures
  • Fat deposits in the spinal column (epidural lipomatosis)
  • Growth retardation in children
  • Disorders of sex hormone secretion
  • Absence of menstruation (amenorrhea)
  • Male pattern baldness in women (hirsutism)
  • impotence
  • Scleroderma-related (autoimmune disease) renal crisis (signs of increased blood pressure and reduced urine production)
  • Delayed wound healing

Interactions

Interactions may occur if the following medicines are taken at the same time:

  • Medication to strengthen the heart (cardiac glycosides) can be increased
  • Diuretics (saluretics) and laxatives can increase potassium excretion
  • Medication to increase eye pressure (atropine and anticholinergics) can be increased
  • Prednisone in combination with drugs to suppress the immune system (immunosuppressive drugs) can increase susceptibility to infections or worsen existing infections
  • Prednisone in combination with ciclosporin can increase the risk of seizures
  • Prednisone in combination with fluoroquinolones can increase the risk of tendon problems or ruptures
  • Blood sugar-lowering agents (oral antidiabetics, insulin) can be weakened
  • "Blood thinners" (oral anticoagulants, coumarin derivatives) can be weakened
  • Medication for muscle relaxation (non-polarizing muscle relaxants) can be attenuated
  • Medication for the treatment of worm diseases (praziquantel) can be weakened
  • Growth hormones(somatropin) can be attenuated
  • Prednisone in combination with protirelin can attenuate the increase in thyroid stimulating hormone (TSH)
  • Prednisone in combination with certain drugs to lower blood pressure (ACE inhibitors) can cause changes in the blood count
  • Prednisone can cause stomach ulcers and/or gastrointestinal bleeding in combination with drugs for the treatment of inflammation and rheumatism
  • In combination with drugs for the treatment of malaria or rheumatic diseases(chloroquine, hydroxychloroquine, mefloquine), prednisone can cause muscle or heart muscle disorders (myopathies, cardiomyopathies)

The following medicines weaken the effect of prednisone:

The following medicines increase the effect of prednisone:

Prednisone can suppress skin reactions to allergy tests!

Prednisone can lead to a positive result in doping tests!

Prednisone is not recommended as a doping agent as it can endanger your health!

The effect of vaccinations from killed pathogens (inactivated vaccine) can be weakened by high doses of prednisone.

Contraindications

Prednisone must not be taken in the following cases:

  • in the case of an allergy to the active substance prednisone

Long-term therapy with prednisone can lead to an increased susceptibility to infections , even from pathogens that only rarely cause illness.

Age restriction

In children and adolescents, prednisone should only be used if this is absolutely necessary from a medical point of view. Due to the risk of growth retardation, longitudinal growth should be monitored regularly. The dose should be as low as possible and limited in time.

In older patients, the risk of a decrease in bone density (osteoporosis) increases. In this case, the risk-benefit profile should be carefully weighed up by the attending physician .

Pregnancy & breastfeeding

According to the package leaflet of various medications, the following applies to prednisone:

During pregnancy and breastfeeding , prednisone should only be taken on the advice of a doctor , as malformations and/or growth disturbances may occur and prednisone passes into breast milk.

The Pharmacovigilance and Advisory Center for Embryonal Toxicology of the Charité-Universitätsmedizin (www.embryotox.de) recommends

Pregnancy

In the first trimester of pregnancy (1st trimester), a risk of cleft lip and palate cannot be ruled out despite extensive studies. Especially between the 8th and 11th week of pregnancy, prednisone should therefore be avoided if possible. However, it is assumed that the risk of cleft lip and palate depends on the dose.

In the last two trimesters of pregnancy (2nd and 3rd trimester), there may be an increased risk of premature birth with low birth weight, depending on the duration and dose. According to current knowledge, this risk increases with long-term therapy with 10 mg/day or higher.

In late pregnancy, hypoglycemia or electrolyte imbalances may occur in the unborn baby. Adrenal insufficiency is also possible, but appears to depend on the dose.

The growth of the baby in the mother's womb should therefore be monitored by ultrasound for weeks during high-dose prednisone therapy. If therapy lasts until birth, adrenal insufficiency should be considered and possibly treated.

Breastfeeding

Prednisone therapy poses only very limited risks during breastfeeding . Prednisone does pass into breast milk, but only less than 10%. In the case of therapy with up to 10 mg/day, the amount absorbed via breast milk is below the detection limit. Even with a high-dose short-term therapy of up to 1 g, there is no risk for the breastfed infant. However, if this high-dose therapy lasts longer, you should wait three to four hours before breastfeeding.

Prednisone is the drug of choice in both pregnancy and breastfeeding. There are therefore no alternatives.

Thomas Hofko

Thomas Hofko

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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