Prednisolone hemisuccinate

GLUCOCORTICOID DRUGS

Toolkit

First aid for an attack

When the first signs of anaphylactic shock appear, a person should be provided with emergency medical care, which consists of performing the following algorithm of actions:

1. The patient is placed in a horizontal position.
2. It is necessary to free the victim’s neck and chest from clothing, the impact of which may complicate the act of breathing.
3. A tourniquet should be applied above the area of ​​the body where the drug was injected, a poisonous insect bite occurred, or exposure to another potential allergen occurred.
4. Introduce adrenaline and glucocorticoids, which have anti-shock and anti-allergic effects, into the patient's body.
5. Organize the patient's inhalation with an additional source of oxygen.

In the absence of medical equipment and increasing respiratory failure, artificial respiration is performed. At this stage of emergency care, the patient may require urgent intubation with connection to a ventilator.

When artificial ventilation is not possible, tracheostomy is used. The walls of the victim’s larynx are pierced with 6 injection needles, which have a wide lumen diameter.

CHARACTERISTICS OF INDIVIDUAL DRUGS

Depending on their structure, glucocorticoids differ in duration of action, severity of anti-inflammatory, mineralocorticoid, metabolic and immunosuppressive activity (Table 5). Moreover, there is no direct correlation between their immunosuppressive and anti-inflammatory effects. For example, dexamethasone has a powerful anti-inflammatory effect and relatively low immunosuppressive activity.

CORTISONE

The drug is a natural glucocorticoid, biologically inactive. Activated in the liver, turning into hydrocortisone. Has a short-term effect. Compared to other glucocorticoids, it has more pronounced mineralocorticoid activity, that is, it has a significant effect on water-electrolyte metabolism.

Features of application

Mainly used for replacement therapy

adrenal insufficiency in patients with normal liver function.

Release forms:

• tablets of 25 and 50 mg (cortisone acetate)
  .

HYDROCORTISONE

A natural glucocorticoid, its glucocorticoid activity is 4 times weaker than prednisolone, but its mineralocorticoid activity is slightly superior. As with cortisone, there is a high risk of edema, sodium retention, and potassium loss.

Features of application

Hydrocortisone, like cortisone, is not recommended for pharmacodynamic therapy

, especially in patients with edema, hypertension, and heart failure.
It is used
mainly
for replacement therapy
for primary and secondary adrenal insufficiency. In acute adrenal insufficiency and other emergency conditions, the drug of choice is hydrocortisone hemisuccinate.

Release forms:

• hydrocortisone hemisuccinate, dry substance or solution in ampoules and bottles of 100 and 500 mg (hydrocortisone-meva, panukort, solu-cortef)
  ;
• hydrocortisone acetate, suspension in ampoules and vials of 25 mg/ml.

PREDNISOONE

Synthetic glucocorticoid, most often used in clinical practice for pharmacodynamic therapy

and is considered as a standard drug. In glucocorticoid activity it is 4 times stronger than hydrocortisone, and in mineralocorticoid activity it is inferior to it. Refers to glucocorticoids with an average duration of action.

Release forms:

• tablets of 5, 10, 20 and 50 mg (ano-prednisone, decortin N, tednisol);
• prednisolone phosphate, 1 ml ampoules, 30 mg/ml;
• prednisolone hemisuccinate, powder in ampoules of 10, 25, 50 and 250 mg (decortin salt);
• prednisolone acetate, suspension in ampoules of 10, 20, 25 and 50 mg ( prednihexol).

PREDNISONE

In terms of activity and other parameters it is close to prednisolone. Initially, prednisone is a metabolically inactive drug (prodrug). Activated in the liver by hydroxylation and conversion to prednisolone. Therefore, it is not recommended to use it for severe liver diseases. The main advantage of prednisone is its lower cost.

Release forms:

• 5 mg tablets (prednisone).

METHYLPREDNISOLONE

Compared to prednisolone, it has slightly greater (20%) glucocorticoid activity, minimal mineralocorticoid effect, and is less likely to cause undesirable reactions (especially changes in the psyche, appetite, ulcerogenic effect). It has a higher cost than prednisolone.

Features of application

Just like prednisolone, it is used mainly for pharmacodynamic therapy. It is preferable in patients with mental disorders, obesity, peptic ulcer disease, as well as during pulse therapy.

Release forms:

• tablets of 4 and 16 mg (Medrol, Metypred, Urbazon, Prednol);
• methylprednisolone succinate, dry substance in ampoules and vials of 8, 20, 40, 125, 250, 500 mg, 1.0 and 2.0 g (metipred, prednol-L, solu-medrol);
• methylprednisolone acetate, suspension in 40 mg bottles (depo-medrol, metypred);
• methylprednisolone suleptanate, ampoules of 50 and 100 mg/ml (promedrol).

TRIAMCINOLONE

It is a fluorinated glucocorticoid. It has a stronger (20%) and longer-lasting glucocorticoid effect than prednisolone. Has no mineralocorticoid activity. More often causes undesirable reactions, especially from muscle tissue (“triamcinolone” myopathy) and skin (striae, hemorrhages, hirsutism).

Release forms:

• tablets of 2, 4 and 8 mg ( berlicort, delficort, kenacort, polcortolone
  );
  triamcinolone acetonide, suspension in ampoules of 40 mg/ml ( kenalog, tricort
  );
• triamcinolone hexacetonide, suspension in ampoules of 20 mg/ml ( Lederspan
  ).

DEXAMETHASONE

Just like triamcinolone, it is a fluorinated drug. One of the most powerful glucocorticoids: 7 times stronger than prednisolone in glucocorticoid activity. Does not have mineralocorticoid effect. It causes severe depression of the hypothalamic-pituitary-adrenal system, severe disturbances of carbohydrate, fat, calcium metabolism, and a psychostimulating effect, therefore it is not recommended to prescribe it for a long period.

Features of application

The drug has some special indications for use: bacterial meningitis; cerebral edema; in ophthalmology (keratitis, uveitis and others); prevention and treatment of nausea and vomiting during chemotherapy; treatment of severe withdrawal syndrome in alcoholism; prevention of respiratory distress syndrome in premature infants (dexamethasone stimulates the synthesis of surfactant in the alveoli of the lungs); leukemia (replacing prednisolone with dexamethasone in acute lymphoblastic leukemia significantly reduces the incidence of damage to the central nervous system).

Release forms:

• tablets of 0.5 and 1.5 mg (daxin, dexazone, cortidex);
• dexamethasone phosphate, ampoules of 1 and 2 ml, 4 mg/ml (daxin, dexabene, dexazone, sondex).

BETAMETHASONE

A fluorinated glucocorticoid, similar in strength and duration of action to dexamethasone. Glucocorticoid activity is 8-10 times higher than that of prednisolone. Does not have mineralocorticoid properties. It has a somewhat weaker effect on carbohydrate metabolism than dexamethasone. The best known drug is betamethasone phosphate/dipropionate, intended for intramuscular, intra-articular and periarticular administration. It consists of two esters, one of which - phosphate - is quickly absorbed from the injection site and gives a quick (within 30 minutes) effect, and the other - dipropionate - is absorbed slowly, but provides a prolonged effect - up to 4 weeks or more. It is a fine-crystalline suspension that cannot be administered intravenously. Water-soluble betamethasone phosphate is administered intravenously and subconjunctivally.

Signs of anaphylactic shock

The clinical manifestations of anaphylactic shock largely depend on the exposure to which allergen that provoked the acute allergic reaction.

This type of pathological condition of the body is accompanied by the occurrence of the following symptoms:

• redness of the skin in the area of ​​contact of the body with a potential irritant;
• severe itching of the epithelial tissues and mucous membrane of the oral cavity, larynx, which only intensifies;
• a sharp decrease in blood pressure;
• a feeling of severe pain that appears immediately after contact with the allergen;
• dizziness;
• nausea;
• attacks of spasmodic pain inside the abdomen;
• diarrhea;
• vomiting if the allergen gets inside the gastrointestinal tract;
• multiple swelling of the mucous membranes;
• feeling of suffocation and lack of air;
• loss of consciousness;
• a burning sensation in the chest area (this symptom of anaphylactic shock occurs in the case of an allergic reaction to a drug that was administered intravenously);
• narrowing of the lumen of the bronchi, which leads to disruption of the gas exchange process;
• pale facial skin;
• cyanosis of the surface of the lips, fingers and toes;
• collapse of all life support systems of the body.

The above symptoms of anaphylactic shock can appear within 1-2 minutes. In most cases, people who are in close proximity to the victim do not always have time to understand the reason for the patient’s unsatisfactory state of health.

Precautions when using Prednisolone

During therapy with the drug Prednisolone, the following precautions must be taken to maintain health:

• periodic observation by an ophthalmologist;
• control over the cellular composition of peripheral blood, as well as glucose levels;
• checking blood pressure;
• maintaining a stable electrolytic balance;
• dosed intake of antacids and drugs containing potassium ions, which minimize the risk of side effects;
• refuse vaccination, since Prednisolone suppresses the occurrence of an adequate immune response (artificial immunization of the body should be carried out later, after discontinuation of the medication);
• carry out x-ray monitoring of the preservation of the mineral structure of the bones of the spine, upper and lower extremities.

During long-term therapy with Prednisolone, it should be taken into account that this drug increases the concentration of 11- and 17-hydroxyketocorticosteroids. In patients who have previously suffered a myocardial infarction or suffer from liver cirrhosis, these diseases may progress with further destruction of the affected tissues.

Dosages

The prednisolone dosage regimen for patients with signs of anaphylaxis is established by the attending physician, taking into account the severity of the patient's condition.

For adults

For patients of the adult age group who are in a state of anaphylactic shock, jet intravenous administration of Prednisolone is indicated in a dosage of 50 to 150 mg of the active substance. In particularly severe cases, this dose can be increased to 400 mg.

After stabilizing the patient’s condition and normalizing blood pressure, further administration of Prednisolone is carried out intravenously, but as part of a drip solution. Repeated use of this drug is possible within a time interval of 3-4 hours.

For adult patients, the average daily dose of Prednisolone ranges from 300 to 1200 mg, with its subsequent reduction as health improves. It is important to remember that abrupt cessation of therapy with this drug may provoke withdrawal symptoms.

For children by age

For children of all age groups, whose bodies are still growing, the use of Prednisolone is possible only in extreme cases, when there is a real threat to the child’s life.

The dose of glucocorticoid is determined individually by the attending physician, who assesses the severity of anaphylaxis. After the injection of the drug, the child remains in the inpatient department of the hospital under round-the-clock supervision of medical personnel.