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Manufacturers: Dr. Reddy's Laboratories Ltd.
Active ingredients
- Astemizole
Disease class
- Conjunctivitis
- Acute atopic conjunctivitis
- Vasomotor and allergic rhinitis
- Hives
- Angioedema
- Allergy unspecified
Clinical and pharmacological group
- Not indicated. See instructions
Pharmacological action
- Antiallergic
Pharmacological group
- H1-antihistamines
Oral tablets Histalong (Histalong)
Instructions for medical use of the drug
Description of pharmacological action
Reduces capillary permeability and tissue swelling caused by histamine, prevents the development and facilitates the course of allergic reactions. Does not have a pronounced sedative effect.
Indications for use
Allergic rhinitis, conjunctivitis, urticaria, Quincke's edema and other allergic diseases.
Release form
tablets 10 mg; contour packaging 10 cardboard pack 2; dispersible tablets for children 5 mg; contour cell packaging 10 with measuring spoon (scoop) cardboard pack 2;
Pharmacodynamics
II generation histamine H1 receptor blocker, piperidine derivative. It has an antihistamine effect, which is due to competition with histamine for binding sites with H1 receptors on effector cells. Prevents the occurrence and facilitates the course of allergic reactions. Reduces itching and exudation. It has virtually no anticholinergic activity and does not have a sedative effect.
Pharmacokinetics
After oral administration, astemizole is rapidly absorbed from the gastrointestinal tract, absorption decreases in the presence of food. Subject to intensive metabolism during the “first pass” through the liver. Metabolism of astemizole in the liver occurs with the participation of the cytochrome P450 enzyme system, mainly the CYP3A4 isoenzyme and, to a lesser extent, the CYP2D6 and CYP2A6 isoenzymes. Css in plasma of astemizole and its metabolites is achieved within 4-8 weeks. Desmethylastemizole, the main metabolite of astemizole, has antihistamine activity. The binding of unchanged astemizole to plasma proteins is 96%. Practically does not penetrate the BBB. T1/2 of astemizole and its metabolites at steady state is 19 days. Astemizole is excreted in the form of metabolites in the urine and through the intestines.
Use during pregnancy
Adequate and strictly controlled studies of the safety of astemizole during pregnancy have not been conducted. Experimental studies revealed the embryotoxic effect of astemizole. It is not known whether astemizole is excreted into breast milk in humans. Experimental studies have found that astemizole is excreted in the milk of lactating dogs. It should be borne in mind that astemizole metabolites can remain in the mother's body for up to 4 months after cessation of therapy.
Contraindications for use
Liver dysfunction, cardiac arrhythmia (ARI), simultaneous use of azole antifungals, macrolide antibiotics (except for azithromycin azalide), selective serotonin reuptake inhibitors, HIV protease inhibitors, quinidine in therapeutic doses, children under 2 years of age, pregnancy , lactation period, hypersensitivity to astemizole.
Side effects
From the central nervous system and peripheral nervous system: rarely - nausea, dizziness. From the cardiovascular system: ventricular arrhythmias (including arrhythmias) are possible. Other: increased appetite, tendency to increase body weight.
Directions for use and doses
Adults and children over 12 years old - 10 mg 1 time / day. Children aged 6-12 years - 5 mg 1 time / day, 2-6 years - 200 mcg / kg 1 time / day.
Interactions with other drugs
With the simultaneous use of astemizole and itraconazole, ketoconazole and other antifungal agents imidazole and triazole derivatives, macrolides clarithromycin, erythromycin, triacetoleandomycin, terfenadine, serotonin reuptake inhibitors, HIV protease inhibitors (ritonavir, indinavir), the risk of developing ventricular arrhythmias increases due to impaired metabolism of astemizole in liver and increasing its concentration in the blood plasma.
Precautions for use
Use with caution in case of prolongation of the QT interval (on ECG), hypokalemia, severe liver dysfunction.
Storage conditions
In a dry place, protected from light, at a temperature not exceeding 25 °C.
Best before date
36 months
ATX classification:
R Respiratory system
R06 Antihistamines for systemic use
R06AX Other antihistamines for systemic use
R06AX11 Astemizole
Instructions for use INDALONG
Undesirable combinations
With the simultaneous use of thiazide diuretics and lithium preparations
There may be an increase in the concentration of lithium in the blood plasma, accompanied by the appearance of signs of overdose. If necessary, diuretics can be used in combination with lithium preparations, and the dose of the drugs should be carefully selected, constantly monitoring the lithium content in the blood plasma.
With the simultaneous use of drugs that can cause arrhythmias
(astemizole, erythromycin for intravenous administration, pentamidine, sultopride, terfenadine, vincamine, halofantrine, bepridil) and thiazide diuretics, the development of arrhythmias is possible (provoking factors include hypokalemia, bradycardia or a prolonged QT interval). For hypokalemia, it is necessary to use drugs that do not cause aritis.
Combinations requiring caution
When used simultaneously with NSAIDs (for systemic use)
with significant fluid loss, acute renal failure may develop (due to decreased glomerular filtration). It is necessary to compensate for fluid loss and carefully monitor renal function at the beginning of treatment.
When used simultaneously with drugs that can cause hypokalemia
(amphotericin B (for intravenous administration), corticosteroids and mineralocorticoids (for systemic administration), tetracosactide, drugs that stimulate intestinal motility) increases the risk of developing hypokalemia due to an additive effect. Constant monitoring of potassium levels in the blood serum is necessary, and appropriate treatment should be prescribed if necessary. Particular attention should be paid to patients concomitantly receiving cardiac glycosides.
When used simultaneously with baclofen
There is an increase in the antihypertensive effect. It is necessary to compensate for fluid loss and carefully monitor renal function at the beginning of treatment.
Hypokalemia enhances the toxic effect of cardiac glycosides
. When using thiazide diuretics and cardiac glycosides simultaneously, serum potassium levels and ECG readings should be carefully monitored.
Combination with potassium-sparing diuretics
(amiloride, spironolactone, triamterene) is effective in some categories of patients, but the possibility of developing hypokalemia or hyperkalemia cannot be excluded, especially in patients with diabetes mellitus and patients with renal failure. It is necessary to monitor the potassium content in the blood serum, ECG parameters and, if necessary, modify the course of therapy.
Reduced serum sodium concentration in patients receiving ACE inhibitors
, increases the risk of sudden arterial hypotension and/or acute renal failure (especially with renal artery stenosis).
Class IA antiarrhythmic drugs
(quinidine, hydroquinidine, disopyramide),
amiodarone, bretylium, sotalol
, can cause arrhythmias in the presence of risk factors (hypokalemia, bradycardia and initially prolonged QT interval). Plasma potassium levels and the QT interval should be carefully monitored, adjusting the course of treatment if necessary.
Lactic acidosis occurring while taking metformin
, is often a consequence of functional renal failure caused by the action of diuretics (especially “loop” diuretics). Metformin should not be used if creatinine levels exceed 15 mg/L (135 µmol/L) in men and 12 mg/L (110 µmol/L) in women.
Dehydration during the use of diuretics increases the risk of developing acute renal failure. This risk is especially high when using iodinated contrast agents.
in high doses. Before using iodine-containing contrast agents, it is necessary to compensate for fluid loss.
Combinations requiring special attention
Tricyclic antidepressants and antipsychotics
enhance the antihypertensive effect of thiazide diuretics and increase the risk of orthostatic hypotension (additive effect).
With the simultaneous administration of diuretics and calcium salts
it is possible to increase the concentration of calcium ions in the blood plasma due to a decrease in their excretion in the urine.
With simultaneous use of thiazide diuretics with cyclosporine
it is possible to increase the creatinine content in the blood plasma without changing the concentration of circulating cyclosporine, even with normal fluid and sodium ion levels.
Corticosteroid drugs, tetracosactide (for systemic use)
reduce the antihypertensive effect due to fluid and sodium ion retention.
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GISTALONG Tablets 10 mg No. 20
General information International name: Astemizole Group affiliation: H1-histamine receptor blocker
Description of the active substance (INN): Astemizole
Pharmacological action: Long-acting antihistamine. Blocks peripheral H1-histamine receptors, eliminates smooth muscle spasms caused by histamine, and reduces capillary permeability. Relieves bronchospasm caused by physical activity and hyperventilation. Has weak antiserotonin activity. It has virtually no sedative or anticholinergic effects. The effect develops within 24 hours (sometimes for 2-3 days) and reaches a maximum after 9-12 days. The duration of effect depends on the duration of previous therapy (suppression of skin tests may persist for several weeks after discontinuation of treatment).
Indications: Allergic rhinitis (seasonal and year-round), allergic conjunctivitis, allergic skin reactions (chronic idiopathic urticaria, etc.), angioedema (treatment and prevention). Anaphylactic and anaphylactoid reactions, bronchial asthma (auxiliary therapy).
Contraindications: Hypersensitivity, pregnancy, lactation, early childhood (up to 2 years), prolongation of the QT interval on the ECG (including history), simultaneous use with ketoconazole and itraconazole, clarithromycin, erythromycin, troleandomycin, mibefradil, liver failure .With caution. Hypokalemia.
Side effects: Sedation (more pronounced when used in high doses), dryness of the mucous membrane of the mouth, nose and throat, increased appetite and body weight, tachycardia, when used in high doses - drowsiness, palpitations, prolongation of the QT interval, arrhythmia (in including ventricular pirouette type), collapse. Overdose. Symptoms: headache, nausea, confusion, prolongation of the QT interval on the ECG, ventricular dysrhythmia (including pirouette type), ventricular fibrillation, convulsions, collapse, cardiac arrest, death. Treatment: gastric lavage, cardiac monitoring for 24 hours, symptomatic and supportive therapy.
Directions for use and dosage: Orally, on an empty stomach, 1 hour before or 2 hours after meals. Adults and children over 12 years old - 10 mg 1 time per day. Children aged 6-12 years - 5 mg 1 time per day; under 6 years - 2 mg/10 kg in one dose only in the form of a suspension. The maximum treatment period is 7 days.
Special instructions: It is not recommended to take grapefruit juice at the same time (suppresses metabolism and increases concentration in the blood). Do not exceed recommended doses. Patients should be warned about the potential for anticholinergic effects (dry mucous membranes). If fainting occurs while taking astemizole, you should immediately stop taking it and examine the patient to identify cardiac arrhythmias. It is recommended to discontinue use at least 4 weeks before performing a skin test for allergens. Adequate and strictly controlled studies of the safety of astemizole during pregnancy have not been conducted. Experimental studies revealed the embryotoxic effect of astemizole. It is not known whether astemizole is excreted into breast milk in humans. Experimental studies have found that astemizole is excreted in the milk of lactating dogs. It should be borne in mind that astemizole metabolites can remain in the mother’s body for up to 4 months after cessation of therapy. During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Interaction: Ethanol and other drugs that depress the central nervous system may enhance the inhibitory effect on the central nervous system. The administration of other drugs that have an anticholinergic effect enhances the anticholinergic effect of astemizole. Azithromycin, clarithromycin, erythromycin, troleandomycin; Medicines that prolong the QT interval (tricyclic antidepressants, BMCCs, especially bepridil, cisapride, disopyramide, maprotiline, phenothiazines, pimozide, procainamide, quinidine, sparfloxacin) are at risk of developing cardiotoxic effects (prolongation of the QT interval, development of arrhythmias and other ventricular arrhythmias). Fluconazole, itraconazole, ketoconazole, metronidazole, miconazole and other inhibitors of the cytochrome P450 system, mifebradil - increase the plasma concentration of astemizole and the risk of developing cardiotoxic effects. HIV protease inhibitors, serotonin reuptake inhibitors: fluvoxamine, nefazodone, ritonavir and sertraline reduce the metabolism of terfenadine in vitro, however, the clinical significance of these data has not been established, therefore, until a final assessment of these data is established and given the similar chemical structure of astemizole and terfenadine, simultaneous use astemizole and the listed drugs are not recommended.
