Hydrocortisone + Lidocaine (Suspension) Instructions for Use

ATC Code

H02AB09 (Hydrocortisone)

Active Substances

Lidocaine (Rec.INN registered by WHO)

Hydrocortisone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Corticosteroids for intra-articular and periarticular administration

Pharmacotherapeutic Group

Glucocorticoids for systemic use. Glucocorticoids. Hydrocortisone

Pharmacological Action

Hydrocortisone is a glucocorticoid agent (GCS). It has anti-inflammatory and anti-edematous effects.

It inhibits the release of cytokines (interleukins and interferon) from lymphocytes and macrophages, suppresses the release of inflammatory mediators by eosinophils, disrupts arachidonic acid metabolism and prostaglandin synthesis.

It reduces inflammatory cellular infiltration, decreases leukocyte migration, including lymphocytes, to the inflammation site.

When administered intra-articularly, the therapeutic effect occurs within 6-24 hours and lasts for several days or weeks.

Lidocaine is a local anesthetic with a membrane-stabilizing effect and a rapid analgesic effect.

Pharmacokinetics

Hydrocortisone

Absorption

After intra-articular and periarticular administration, the absorption of hydrocortisone occurs slowly. When administered intra-articularly, hydrocortisone slowly penetrates into the systemic circulation.

Distribution

More than 90% of hydrocortisone binds to plasma proteins. Hydrocortisone crosses the placental barrier.

Metabolism

It is metabolized in the liver to form tetrahydrocortisone and tetrahydrocortisol metabolites.

Excretion

Metabolites, mainly in the form of glucuronides, as well as a small amount of unchanged hydrocortisone, are excreted by the kidneys.

Lidocaine

Absorption

Lidocaine is well and rapidly absorbed from the surface of mucous membranes and damaged skin.

Distribution, metabolism and excretion

Lidocaine is extensively bound to plasma proteins. It is metabolized mainly in the liver. T_1/2 is 1-2 hours. Lidocaine passes into breast milk and crosses the placental and blood-brain barriers.

Indications

• Osteoarthritis involving multiple joints;
• Monoarthrosis (knee, elbow, hip joints);
• Arthritis of rheumatic or other etiology (except for tuberculous and gonorrheal arthritis);
• Scapulohumeral periarthritis;
• Bursitis;
• Epicondylitis;
• Tenosynovitis;
• For preoperative preparation during interventions on ankylosed joints;
• As local therapy in addition to systemic glucocorticosteroid therapy.

ICD codes

Dosage Regimen

Suspension

Adults

5-50 mg of Hydrocortisone-Richter preparation, depending on the size of the joint and the severity of the disease.

Special patient groups

Elderly patients

In elderly patients, it is recommended to use the same doses as in younger adult patients. In elderly patients, adverse effects may be more pronounced.

Children

5-30 mg of Hydrocortisone-Richter preparation per day, divided into several doses. It is recommended to prescribe the drug at the lowest effective therapeutic dose and, if possible, for a short course.

On one day, the drug can be administered in no more than 3 joints; a repeat injection is possible after a 3-week interval. Administration of the drug directly into the joint can adversely affect the hyaline cartilage, so the drug can be administered into the same joint no more than 3 times a year.

Method of administration

For local use. The drug is not intended for systemic use.

The Hydrocortisone-Richter preparation should be administered intra- and periarticularly, depending on the size of the joint and the severity of the disease.

For tendinitis, the injection should be made into the tendon sheath; the drug must not be injected directly into the tendon. The drug should not be used to treat Achilles tendon diseases.

Shake the vial before use.

The injection is administered in compliance with the rules of antisepsis and asepsis.

Adverse Reactions

Data on the frequency of adverse reactions are not available.

Frequency unknown (frequency cannot be estimated from the available data).

Under certain conditions, in particular, with prolonged local use and/or use of high doses of hydrocortisone and lidocaine, both substances can enter the systemic circulation and cause systemic adverse reactions.

Infections and infestations opportunistic infections, exacerbation of latent tuberculosis.

Blood and lymphatic system disorders leukocytosis.

Immune system disorders hypersensitivity.

Endocrine disorders with long-term treatment and/or use in high doses, suppression of adrenal cortex function is possible.

Metabolism and nutrition disorders increased appetite, fluid and sodium retention, hypokalemic alkalosis. Increased protein catabolism may cause negative nitrogen balance. GCS reduce glucose tolerance and increase the need for hypoglycemic drugs.

Psychiatric disorders insomnia, mental disorder.

Nervous system disorders increased intracranial pressure with papilledema, convulsions, dizziness, headache.

Eye disorders corneal ulceration, glaucoma, exophthalmos, chorioretinopathy, blurred vision.

Cardiac disorders entry of lidocaine injected into the joint area into the systemic circulation (in significant quantities) can cause conduction disturbances and peripheral vasodilation; heart failure.

Vascular disorders thromboembolism, arterial hypertension.

Gastrointestinal disorders peptic ulcer (in some cases with perforation and bleeding), gastric bleeding, pancreatitis, esophagitis, nausea.

Skin and subcutaneous tissue disorders delayed wound healing, skin atrophy, skin striae, acneiform rash, itching, folliculitis, hirsutism, hypopigmentation, skin irritation, dry skin, thin and sensitive skin, telangiectasia.

Musculoskeletal and connective tissue disorders osteoporosis, steroid myopathy, aseptic osteonecrosis, myalgia, arthralgia.

General disorders and administration site conditions fever, malaise. As with other local injections, administration of hydrocortisone into a joint may cause pain and swelling at the injection site. As a rule, such reactions disappear spontaneously after a few hours.

Investigations decreased blood potassium, increased intraocular pressure.

After discontinuation of GCS treatment a “withdrawal” syndrome occurs: fever, myalgia, arthralgia, adrenal insufficiency.

Children and adolescents under 18 years

Endocrine disorders slowed growth and development in children and adolescents.

Eye disorders children and adolescents are more likely to develop cataracts.

Reporting of suspected adverse reactions

It is important to report suspected adverse reactions after registration of the medicinal product in order to ensure continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are recommended to report any suspected adverse drug reactions through the national adverse reaction reporting systems of the member states of the Eurasian Economic Union.

Contraindications

• Hypersensitivity to hydrocortisone and/or lidocaine, or any of the excipients;
• Intra-articular infection;
• Cushing’s syndrome;
• Tendency to thrombosis;
• Systemic infection (sepsis) without specific antibacterial treatment;
• Achilles tendon diseases;
• First trimester of pregnancy.

With caution

Gastric and duodenal ulcer, herpes simplex, including ocular herpes (risk of corneal perforation), arterial hypertension, diabetes mellitus (or family history burdened by this disease); osteoporosis (increased risk of osteoporosis in postmenopausal women); chronic psychotic reactions; history of tuberculosis; glaucoma; steroid myopathy; epilepsy; chickenpox; chronic heart failure; elderly age (over 65 years), second and third trimesters of pregnancy, breastfeeding period.

Use in Pregnancy and Lactation

Pregnancy

Due to the lack of sufficient safety data for the drug in pregnant women, the use of hydrocortisone in the first trimester of pregnancy is contraindicated. In the second and third trimesters of pregnancy, the use of hydrocortisone is possible when the intended benefit to the mother outweighs the potential risk to the fetus (the risk of congenital malformations (e.g., cleft palate) and intrauterine growth retardation is low).

Breastfeeding period

Hydrocortisone and lidocaine pass into breast milk. The use of GCS during breastfeeding can lead to impaired adrenal function and developmental delay in infants.

Use in Hepatic Impairment

Data on the use of the drug in patients with impaired liver function are not provided.

Use in Renal Impairment

Data on the use of the drug in patients with impaired renal function are not provided.

Pediatric Use

Children should be prescribed the drug at the lowest therapeutic doses and, if possible, for the shortest duration.

Geriatric Use

Use with caution in elderly patients over 65 years of age.

Special Precautions

With intra-articular administration of GCS, there is an increased risk of an inflammatory response in the joint. To avoid the development of bacterial infection, the administration of the drug into the joint should be carried out in compliance with the rules of asepsis and antisepsis.

During treatment with GCS (especially in high doses), vaccination should be avoided due to the risk of neurological complications and suppression of antibody production. During treatment, the immune response and the ability to localize infection may be impaired. Treatment with hydrocortisone in standard or high doses can provoke an increase in blood pressure, retention of water and salts, and also increase the excretion of potassium.

GCS increase calcium excretion. To reduce the risk of increased catabolism and the risk of developing osteoporosis, basic therapy (calcium preparations, vitamin D) or bisphosphonates, or anabolic drugs may be prescribed.

In the latent form of tuberculosis, hydrocortisone should be used only in combination with anti-tuberculosis drugs. If a systemic infection develops, hydrocortisone should be used only in combination with specific (e.g., antibacterial) therapy.

GCS, including hydrocortisone, can increase blood glucose concentration, worsen the course of existing diabetes, or increase the predisposition to developing diabetes with their long-term use.

When using GCS, it is advisable to adjust the dose of oral hypoglycemic drugs and anticoagulants.

When used in combination with diuretics, the electrolyte balance should be carefully monitored. During long-term treatment with GCS, the addition of potassium preparations to therapy is justified to prevent hypokalemia.

Concomitant use with inhibitors of the CYP3A isoenzyme, including drugs containing cobicistat, contributes to an increased risk of systemic adverse reactions. This combination of drugs should be avoided. An exception is cases where the possible benefit of use outweighs the increased risk of systemic adverse reactions of GCS. In such cases, the patient should be carefully monitored for the detection of systemic adverse reactions of GCS.

Visual impairment

Visual impairment may occur with systemic and local use of GCS. If a patient experiences symptoms such as blurred vision or other visual disturbances, the patient should be referred to an ophthalmologist for examination to identify possible causes, including cataracts, glaucoma, or rare diseases, such as central serous chorioretinopathy (CSCR), cases of which have been reported after systemic and local use of GCS.

During treatment, it is recommended to regularly monitor blood pressure, urine and stool for occult bleeding. The frequency of adverse reactions is higher in elderly patients.

Use in pediatrics

Against the background of GCS intake, a slowdown in the growth rate of children and adolescents is observed. It is recommended to prescribe the drug at the lowest effective therapeutic dose and, if possible, for a short course. The dose of GCS should be reduced gradually, up to complete withdrawal of the drug.

Excipients

The Hydrocortisone-Richter preparation, suspension for intra-articular and periarticular injection, contains propylparahydroxybenzoate (E216) and methylparahydroxybenzoate (E218). These substances can cause allergic reactions (possibly delayed) and in rare cases, bronchospasm.

This medicinal product contains 30.48 mg of sodium in one dose. This fact must be taken into account when using the drug in patients on a sodium-restricted diet.

Effect on ability to drive and operate machinery

The Hydrocortisone-Richter preparation, suspension for intra-articular and periarticular injection, does not affect the ability to drive vehicles and work with machinery.

Overdose

Symptoms depending on the amount of GCS and lidocaine that entered the systemic circulation, local or systemic manifestations may be observed.

Treatment there is no specific antidote. Treatment is symptomatic.

Drug Interactions

In patients with Addison’s disease, hydrocortisone should not be injected into the joint area simultaneously with the intake of barbiturates, since this combination can provoke acute adrenal insufficiency.

Caution should be exercised when using GCS concomitantly with the drugs listed below

• Barbiturates, phenylbutazone, phenytoin, rifampicin, carbamazepine, primidone, aminoglutethimide (these drugs may reduce the effects of GCS);
• Inhibitors of the CYP3A isoenzyme, including some drugs for the treatment of HIV infection, for example, ritonavir, cobicistat (contribute to an increased risk of systemic adverse reactions);
• Oral hypoglycemic drugs (an increase in the dose of oral hypoglycemic drugs may be required, since GCS cause hyperglycemia);
• Anticoagulants (with simultaneous use of GCS, the effectiveness of anticoagulants may increase or decrease);
• Salicylates (when GCS are discontinued, serum concentrations of salicylates may increase significantly and the risk of intoxication may increase. Since both salicylates and GCS have an ulcerogenic effect, simultaneous use of these drugs may increase the risk of gastrointestinal bleeding and ulcer formation);
• Amphotericin, diuretics, theophylline, digoxin, cardiac glycosides (increased risk of hypokalemia);
• Oral contraceptives (increased serum concentration of GCS);
• Antihypertensive drugs (GCS reduce the effectiveness of antihypertensive drugs);
• Mifepristone (reduced effectiveness of GCS).

Incompatibility

Due to the lack of compatibility studies, this medicinal product should not be mixed with other medicinal products.

Storage Conditions

The drug should be stored out of the reach of children, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 2 years. Do not use after the expiration date.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.