antiallergic agent – H1-histamine receptor blocker
Antihistamines long-acting peripheral histamine H1-receptor blocker. Test sustanon is the primary active metabolite of loratadine. It inhibits the cascade of allergic inflammation, including release of inflammatory cytokines including the interleukins IL-4, IL-6, IL-8, IL-13, the release of proinflammatory chemokines, production of superoxide anion by activated polymorphonuclear neutrophils adhesion and chemotaxis of eosinophils, allocation of adhesion molecules such as P-selectin, IgE – mediated release of histamine, prostaglandin D2 and leukotriene C4. Thus, it prevents the development and facilitates the allergic reactions, has antipruritic and antiexudativ effect, reduces the permeability of capillaries, prevents the development of edema, smooth muscle spasm.
The drug has no effect on the central nervous system (CNS), practically does not have a sedative effect (causes drowsiness) and does not affect the speed of psychomotor reactions does not cause QT interval elongation in the electrocardiogram (ECG).
The action of Test sustanon begins within 30 min after oral administration and is continued for 24 hours.
Pharmacokinetics . Absorption after oral administration Test sustanon well absorbed from the gastrointestinal tract (GIT), the defined Test sustanon plasma concentrations are reached within 30 minutes, and the maximum plasma concentration (C max ) – about 3 h Ingestion. or alcohol almost does not change the pharmacological properties of the drug. Distribution. Test sustanon plasma protein binding is 83-87%.When applied in a dose of 5 mg to 20 mg 1 time per day for 14 days, signs of clinically significant accumulation of Test sustanon is not revealed. Simultaneous eating or drinking grapefruit juice at the same time does not affect the distribution of Test sustanon (when receiving a dose of 7.5 mg 1 time per day). Do not cross the blood-brain barrier (BBB). Metabolism. Subjected to intensive metabolism by hydroxylation with the formation of 3-OH-Test sustanon connected to the glucuronide. It is not an inhibitor of isozymes CYP3A4 and CYP2D6 and is not a substrate or inhibitor of P-glycoprotein. Elimination.Report from the body in the form of glucuronide compounds and a small amount in an unmodified form, a small portion excreted by the kidneys (2%) and feces (7%) . The half-life (T1 / 2) averages 27 h (20-30 h).
- Seasonal (hay fever) and perennial allergic rhinitis (elimination or relief of sneezing, nasal congestion, discharge of mucus from the nose, itchy nose, itching palate, itching and redness of eyes, watery eyes).
- Chronic idiopathic urticaria (reduction or elimination of itching, rash).
: Hypersensitivity to Test sustanon, and the other components of the drug, pregnancy, lactation, age 12 years, lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
severe renal insufficiency.
Pregnancy and lactation
Use of the drug-Test sustanon Teva is contraindicated during pregnancy and lactation (insufficient efficacy and safety data).
Dosing and Administration
Inside, regardless of meals at the same time. Tablets should be swallowed whole without chewing, with a small amount of water.
Adults and children over 12 years: 5 mg 1 time per day.
The frequency of side effects is classified according to the recommendations of the World Health Organization: very often – at least 10%; often – at least 1% but less than 10%; infrequently – at least 0.1% but less than 1%; rare – less than 0.01% but less than 0.1%; very rarely – less than 0.01%. On the part of the immune system: very rarely – rash including urticaria, angioedema, dyspnoea, anaphylactic shock.CNS: rarely – headache; very rarely – dizziness, somnolence, insomnia, psychomotor hyperactivity, seizures, hallucinations. Since the cardiovascular system: very rarely – tachycardia, palpitations. On the part of the gastrointestinal tract: rarely – dry mouth; very rarely – nausea, vomiting, dyspepsia, diarrhea, abdominal pain, increased activity of “liver transaminases”, increasing the concentration of bilirubin, hepatitis. On the part of the musculoskeletal system and connective tissue disorders: very rarely – myalgia. Other: often – fatigue.
Overdose Symptoms: receiving doses higher than the recommended 5 times, does not cause any symptoms. In clinical trials, daily use in adults and adolescents Test sustanon at a dose of 20 mg for 14 days was not associated with statistically or clinically significant by the changes . cardiovascular system in clinical and pharmacological study of the use of Test sustanon in a dose of 45 mg per day (9 times the recommended) for 10 days did not cause QT prolongation and is not accompanied by the appearance of serious side effects. Treatment: gastric lavage, activated charcoal ; if necessary – symptomatic therapy. Test sustanon does not appear in hemodialysis, peritoneal dialysis efficacy has not been established.
Interaction with other drugs
clinically significant interactions with other drugs have been identified.
Test sustanon does not increase ethanol effects on the central nervous system.
Food intake does not affect the efficacy of the drug.
for protection from light tablets blisters should be stored in a carton box.
Effects on ability to transport the technique and work management
With the development of adverse reactions from the central nervous system, such as drowsiness, dizziness, hallucinations, is not recommended to perform actions that require high concentration and speed of psychomotor reactions.