Kenalog
Kenalog (active ingredient - triamcinolone) belongs to the group of glucocorticosteroids. The drug has antipruritic, anti-inflammatory, immunosuppressive and antiallergic effects and can be used both locally and systemically, which determines a wide range of its use: from chronic obstructive diseases of the respiratory tract to dermatological diseases, from various forms of joint damage to hay fever (hay fever).
Kenalog suppresses the activity of tissue macrophages and leukocytes, preventing the latter from penetrating into the site of inflammation. Interferes with the processes of interleukin-1 synthesis and phagocytosis, “disarming” macrophages. Stabilizes lysosome membranes, thereby reducing the level of proteolytic enzymes at the site of inflammation. Reduces the permeability of small blood vessels caused by the release of the mediator of allergic reactions, histamine. Inactivates connective tissue cells fibroblasts, thereby suppressing collagen formation. Kenalog inhibits the synthesis of inflammatory mediators prostaglandins and leukotrienes by suppressing the activity of phospholipase A2 and the release of cyclooxygenase-1. Reduces the number of lymphocytes, monocytes, basophils and eosinophils circulating in the blood by moving them into the lymphoid tissue, suppresses the process of antibody formation.
Kenalog is available in two dosage forms: suspension for injection (in this case, “40” is added to the name of the drug, indicating its dosage:) and tablets. Before using the injection form, the ampoule with its contents must be shaken. The suspension is not administered intravenously: only intramuscularly (systemic action) and inside the joint (locally). In all cases, the dose of the drug is determined individually: it depends on the pathogenesis of the disease and must strictly correspond to the goals of treatment.
When using Kenalog systemically in adults and adolescents over 16 years of age, the injection is made deep into the buttock. The drug is administered slowly, the standard dose in such cases is 1 ampoule (40 mg), in severe cases it can be doubled. With this method of administering the drug, it is necessary to prevent possible tissue atrophy. Immediately after the injection, a sterile napkin is pressed to the injection site for several minutes. To eliminate hay fever, as a rule, a one-time use of kenalog during the season of mass flowering of allergenic plants is sufficient. If one injection is not enough, then the next one is allowed to be given no earlier than after 1 month.
The dose of Kenalog for intra-articular administration is determined by the degree of damage and the size of the joint. If it is necessary to quickly eliminate symptoms, Kenalog can be combined with local anesthetics with mandatory observance of aseptic conditions. Suffice it to say that the injection site should be prepared as if a surgical procedure was planned. Repeated use of the drug in case of local use is allowed no earlier than after 14 days. Another option is to inject Kenalog under the skin. In such cases, local anesthesia is also used (in the same syringe with Kenalog). When injecting, the syringe should be held horizontally so that its contents are injected into the area between the skin and the subcutaneous layer. The duration of use of Kenalog is determined by the doctor and varies from a single administration for hay fever to courses lasting several years, as for bronchial asthma. When using Kenalog systemically, the patient's diet should be rich in proteins and vitamins.
Kenalog – suspension
GCS inhibits the release of interleukin1, interleukin2, interferon gamma from lymphocytes and macrophages. It has anti-inflammatory, antiallergic, desensitizing, antishock, antitoxic and immunosuppressive effects.
Suppresses the release of ACTH and beta-lipotropin by the pituitary gland, but does not reduce the concentration of circulating beta-endorphin. Inhibits the secretion of TSH and FSH.
Increases the excitability of the central nervous system, reduces the number of lymphocytes and eosinophils, increases the number of red blood cells (stimulates the production of erythropoietins).
Interacts with specific cytoplasmic receptors and forms a complex that penetrates the cell nucleus and stimulates the synthesis of mRNA; the latter induces the formation of proteins, incl. lipocortin, mediating cellular effects. Lipocortin inhibits phospholipase A2, suppresses the formation of arachidonic acid and inhibits the synthesis of endoperoxides, Pg, leukotrienes, which contribute to inflammation, allergies, etc.
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; enhances protein catabolism in muscle tissue.
Lipid metabolism: increases the synthesis of higher fatty acids and TG, redistributes fat (fat accumulation 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 the flow of 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 Na+ and water in the body, stimulates the excretion of K+ (MCS activity), reduces the absorption of Ca2+ from the gastrointestinal tract, “washes out” Ca2+ from the bones, increases the excretion of Ca2+ by the kidneys.
The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils; inducing the formation of lipocortin and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes and organelle membranes (especially lysosomal ones).
The antiallergic effect develops as a result of suppression of the synthesis and secretion of allergic 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, a decrease in the number of T- and B-lymphocytes, mast cells, reducing the sensitivity of effector cells to allergy mediators, inhibiting antibody formation, changing the body's immune response.
In COPD, the action is based mainly on inhibition of inflammatory processes, inhibition of development or prevention of swelling of the mucous membranes, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucous membrane. Increases the sensitivity of beta-adrenergic receptors of small and medium-caliber bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by inhibiting or reducing its production.
Antishock and antitoxic effects are associated with an increase in blood pressure (due to an increase in the concentration of circulating catecholamines and restoration of the sensitivity of adrenergic receptors to them, 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 inhibition of the release of cytokines (interleukin1, interleukin2; interferon gamma) from lymphocytes and macrophages.
Suppresses the synthesis and secretion of ACTH and, secondarily, the synthesis of endogenous corticosteroids. Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
In terms of anti-inflammatory activity, triamcinolone is close to hydrocortisone; triamcinolone acetonide is 6 times more active. There is virtually no activity on the ISS.
After intramuscular administration, the maximum effect is observed after 24-48 hours, the duration of action with intramuscular administration is 1-6 weeks, in the joint cavity - several weeks.
Kenalog 40, 5 pcs., 1 ml, 40 mg/ml, suspension for injection
Kenalog® 40 is not intended for intravenous, intradermal, intraocular, epidural or intrathecal use. Serious adverse events have been reported with epidural and intrathecal routes of administration.
To prevent tissue atrophy at the site of intramuscular injection, Kenalog® 40 should be injected deep into the gluteal muscle.
Kenalog® 40 has a therapeutic effect for a long period of time after administration, but it is not intended for use in emergency situations.
When using the drug topically, it is necessary to evaluate its compatibility with simultaneously administered local anesthetics.
It is allowed to mix with an equal volume of solutions of local anesthetics (1% procaine solution or 1% lidocaine solution) in a syringe, but not in an ampoule.
Before and during GCS therapy, it is necessary to monitor a general blood count, glycemia, and the content of electrolytes in the blood plasma.
With long-term use of GCS, the risk of developing subcapsular cataracts and glaucoma increases, sometimes with damage to the optic nerve. The incidence of secondary eye infections may also increase.
It is necessary to study the synovial fluid in each joint to exclude a septic process. A significant increase in pain, accompanied by local swelling, further limitation of joint mobility, fever and malaise, suggests the development of septic arthritis. If sepsis is confirmed, appropriate antimicrobial therapy is necessary. When treating during intercurrent infections, septic conditions, tuberculosis, antibiotic treatment is carried out simultaneously.
It should not be injected into “unstable” joints, in the area of the Achilles tendon (risk of rupture).
Vaccination with live viral vaccines is contraindicated during GCS therapy. Immunization with killed viral or bacterial vaccines during the use of GCS does not provide the expected increase in the number of antibodies and does not provide the expected protective effect. Therefore, such drugs should not be prescribed 8 weeks before and 2 weeks after vaccination.
In patients who have not had chickenpox and are receiving treatment with corticosteroids, the risk of developing chickenpox or herpes infection increases due to accidental contact with infected persons. In such cases, passive immunization is recommended.
Caution is necessary in patients after surgery and bone fractures, since GCS can slow down the healing of wounds and fractures due to increased excretion of calcium ions from the body.
The effect of GCS is enhanced in patients with liver cirrhosis or hypothyroidism.
The use of Kenalog® 40 may alter the performance of hypersensitivity tests.
GCS can mask some signs of existing infectious diseases, as well as the appearance of infection during treatment. When using them, there may be a decrease in immunity and a weakening of the process of localizing the infection.
The use of GCS can provoke a deterioration of the condition and increased migration of larvae in patients with strongyloidiasis, which can lead to severe enterocolitis and death due to gram-negative septicemia.
When using corticosteroids (especially high and medium doses of hydrocortisone and cortisol), increased blood pressure, fluid and salt retention, and increased excretion of potassium ions may be observed. Although these phenomena are less pronounced when prescribing synthetic corticosteroids (such as the drug Kenalog® 40), it may be necessary to limit salt in food and additionally take potassium supplements. With long-term use of the drug, it is necessary to ensure sufficient consumption of protein foods necessary to maintain the nitrogen balance of the body.
If a patient has a gastric ulcer, its exacerbation during treatment with corticosteroids may be asymptomatic until the ulcer perforates or bleeding begins.
Considering also the fact that long-term use of corticosteroids causes increased acidity of gastric juice, which can lead to the formation of gastric ulcers, an appropriate treatment regimen for peptic ulcer should be prescribed.
In children during the growth period, GCS should be used only according to absolute indications and under the particularly careful supervision of the attending physician.
Menstrual irregularities and vaginal bleeding may occur in postmenopausal women. It should be noted that they are likely to develop in women, but this should not limit the doctor when conducting the necessary examination depending on the indications.
Due to the risk of severe allergic reactions (up to anaphylactic shock) during parenteral administration of GCS, special care should be taken when treating patients with a history of allergies.
Special information on excipients
Kenalog® 40 contains benzyl alcohol, which can cause serious (including fatal) adverse reactions, especially in children. This should be taken into account when prescribing high doses of Kenalog® 40 and long courses of treatment to patients (especially children).
Visual impairment
Visual impairment may occur with systemic and local use of GCS. If blurred vision or other visual disturbances occur, you should consider consulting an ophthalmologist to rule out causes such as cataracts, glaucoma, or rare diseases such as central serous chorioretinopathy (CSCR), which have been reported after systemic and topical use of corticosteroids.
Impact on the ability to drive vehicles and machinery
No special studies have been conducted on the effect of the drug on the ability to drive vehicles or operate machinery. However, during the treatment period, caution should be exercised when driving and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions, due to the possibility of developing undesirable reactions from the nervous system.