Аллергоферон плюс
Аллергоферон плюс Uses, Dosage, Side Effects, Food Interaction and all others data.
Interferon alpha 2b (human leukocyte clone hif-sn 206 protein moiety reduced). A type I interferon consisting of 165 amino acid residues with arginine in position 23. This protein is produced by recombinant DNA technology and resembles interferon secreted by leukocytes. It is used extensively as an antiviral or antineoplastic agent.
Upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also induce the synthesis of several key antiviral mediators, including 2'-5' oligoadenylate synthetase (2'-5' A synthetase) and protein kinase R.
Loratadine is a non-sedating antihistamine. It works by selectively binding to peripheral histamine H1-receptors on effector cells.
Like other 2nd generation antihistamines, loratadine is selective for peripheral H1 receptors. Loratadine does not penetrate effectively into the central nervous system and has poor affinity for CNS H1-receptors. These qualities result in a lack of CNS depressant effects such as drowsiness, sedation, and impaired psychomotor function.
Xylometazoline is a sympathomimetic agent with marked alphaadrenergic activity, and is intended for use in the nose. It constricts the nasal blood vessels, thereby decongesting the mucosa of the nose and neighboring regions of the pharynx. This enables patients suffering from colds to breathe more easily through the nose. The effect of Xylometazoline begins within a few minutes and persists for several hours. Xylometazoline is generally well tolerated and does not impair the function of ciliated epithelium. Systemic absorption may occur following nasal application of Xylometazoline.
Xylometazoline is a sympathomimetic agent that causes vasoconstriction of the nasal mucosa. In one study comprising subjects with nasal congestion associated with the common cold, the median time of onset of subjective relief of nasal congestion was about 1.7 minutes and the time of subjective peak relief of nasal congestion was 30 minutes. Previous studies reported rebound swelling, rebound nasal congestion, rhinitis medicamentosa, and shorter duration of decongestant effect from the long-term use of xylometazoline in healthy volunteers, suggesting that the drug is most effective if used temporarily.
An early in vitro study demonstrated xylometazoline to exert anti-oxidant actions, where it inhibited microsomal lipid peroxidation and mediated hydroxyl radical scavenging activity. This suggests that xylometazoline has a beneficial effect against oxidants, which play a role in tissue damage in inflammation.
| Trade Name | Аллергоферон плюс |
| Generic | Interferon Alfa-2b + Loratadine + Xylometazoline |
| Type | |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Interferon alfa-2b is a form of recombinant human interferon used to treat hepatitis B and C infection, genital warts, hairy cell leukemia, follicular lymphoma, malignant melanoma, and AIDs-related Kaposi's sarcoma.
For the treatment of hairy cell leukemia, malignant melanoma, and AIDS-related Kaposi's sarcoma.
Loratadine provides faster relief from the symptoms of hay fever, allergic rhinitis such as sneezing, nasal discharge, itching, ocular itching and burning, nasal and ocular sign and symptoms are relieved rapidly after oral administration.
Loratadine is also effective in idiopathic chronic urticaria. In children over 2 years, Loratadine is used for the symptomatic relief of seasonal allergic rhinitis and allergic skin conditions such as urticaria nettle rash.
For the symptomatic relief of nasal congestion, perennial allergic rhinitis (including hay fever), sinusitis.
Аллергоферон плюс is also used to associated treatment for these conditions: Chronic Hepatitis C Virus (HCV) Infection, Hairy Cell Leukemia (HCL), Kaposi’s sarcoma, Melanoma, MalignantAllergic Dermatologic Disorders, Allergic Rhinitis (AR), Allergies, Chronic Urticaria, Common Cold, Eye pruritus, Fever, Nasal Congestion, Nasal Itching, Pain, Perennial Allergic Rhinitis (PAR), Perennial Rhinitis, Pollen Allergy, Pruritus, Rhinorrhoea, Seasonal Allergic Rhinitis, Sneezing, Sensation of burning in the eyes, Watery eyes, Watery itchy eyesAllergic Rhinitis (AR), Nasal Congestion, Seasonal Allergic Rhinitis
How Аллергоферон плюс works
Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which upon dimerization activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers and activators of transcription)which dimerize and activate multiple (~100) immunomodulatory and antiviral proteins. Interferon alpha binds less stably to type I interferon receptors than interferon beta.
Histamine release is a key mediator in allergic rhinitis and urticaria. As a result, loratadine exerts it's effect by targeting H1 histamine receptors.
Loratadine binds to H1 histamine receptors found on the surface of epithelial cells, endothelial cells, eosinophils, neutrophils, airway cells, and vascular smooth muscle cells among others. H1 histamine receptors fall under the wider umbrella of G-protein coupled receptors, and exist in a state of equilibrium between the active and inactive forms. Histamine binding to the H1-receptor facilitates cross linking between transmembrane domains III and V, stabilizing the active form of the receptor. On the other hand, antihistamines bind to a different site on the H1 receptor favouring the inactive form.
Hence, loratadine can more accurately be classified as an "inverse agonist" as opposed to a "histamine antagonist", and can prevent or reduce the severity of histamine mediated symptoms.
Nasal congestion is caused by various etiologies, such as rhinosinusitis and allergic or non-allergic rhinitis, leading to congestion of the venous sinusoids lining the nasal mucosa. Activation of α-adrenergic receptors leads to vasoconstriction of the blood vessels of the nasal mucosa and resumption of nasal airflow. As the most abundantly expressed in the human nasal mucosa, α1A- and α2B-adrenoceptors may play the most important role in vasoconstriction of the human nasal mucosa. Xylometazoline is a more selective agonist at α2B-adrenoceptors, with affinity at α1A-, α2A-, α2C-, α1B-, and α1D-adrenoceptors. Xylometazoline decreases nasal resistance during inspiration and expiration and increases the volume of nasal airflow. Compared to oxymetazoline, another imidazoline nasal decongestant, xylometazoline had a slightly faster onset of action although they had a similar duration of action. In one study, subjects with nasal congestion reported relief of earache and sore throat in addition to nasal decongestion: it is speculated that oxymetazoline mediates this effect by causing vasoconstriction of the nasal mucosa that contains the venous sinuses and nasal decongestion allows breathing through the nose, providing relief from sore throat caused by mouth breathing that dries and irritates the throat.
Dosage
Аллергоферон плюс dosage
Adult & children over 12 years of age: One Loratadine 10 mg tablet once daily (usually in the morning).
Children:
- 2-12 years (body weight more than 30 Kg): 10 mg Loratadine once daily.
- 2-12 years (body weight less than 30 Kg): 5 mg Loratadine once daily.
- Below 2 years of age: Safety and efficacy of Loratadine have not been established.
Liver & renal impairment: Patients with liver impairment and renal insufficiency (GFR <30 ml/min) should be given a lower initial dose (10 mg every other day).
Adults: 2 or 3 drops of Xylometazoline Adult formula (0.1%) two to three times daily. This adult formula should not be used for children under the age of 12 years.Children under 12 years: 1 or 2 drops of the Xylometazoline children's formula (0.05%) in each nostril once or twice daily. Not to be used in infants less than 3 months.
Side Effects
Fatigue, nausea and headache were reported rarely. Scientific studies showed that Loratadine does not cause drowsiness. It does not affect performance and ability to drive or tasks requiring concentration.
The following side effects have occasionally been encountered: a burning sensation in the nose and throat, local irritation, nausea, headache, and dryness of the nasal mucosa. Systemic cardiovascular effects have occurred, and this should be kept in mind when giving Xylometazoline to people with cardiovascular disease.
Toxicity
There is limited experience with overdosage. Postmarketing surveillance includes reports of patients receiving a single dose as great as 10 times the recommended dose. In general, the primary effects of an overdose are consistent with the effects seen with therapeutic doses of interferon alfa-2b. Hepatic enzyme abnormalities, renal failure, hemorrhage, and myocardial infarction have been reported with single administration overdoses and/or with longer durations of treatment than prescribed. Toxic effects after ingestion of interferon alfa-2b are not expected because interferons are poorly absorbed orally.
Second generation antihistamines such as loratadine have very few adverse effects; however, insomnia, headache, fatigue, drowsiness and rash have been reported. Symptoms of loratadine overdose include gastrointestinal side effects, agitation, drowsiness, tachycardia, and headache. It is advised to obtain an ECG in the event of loratadine overdose.
The oral LD50 is 230 mg/kg in rats and 75 mg/kg in mice. The subcutaneous LD50 is 90 mg/kg in rats and 53 mg/kg in mice. The intraperitoneal LD50 is 43 mg/kg in rats.
Xylometazoline poisoning is documented in three pediatric patients who were exposed to a drug concentration 40 times above the adequate dosage for children due to a compounding error: these patients experienced bradypnea and sinus bradycardia with supraventricular extrasystoles and were managed with fluid management.
Precaution
Patients with liver impairment and renal insufficiency (GFR <30 ml/min) should be given a lower initial dose (10 mg every other day).
Each Xylometazoline pack should be used by one person only to prevent any cross-infection. Patients are advised not to take decongestants for more than seven consecutive days.
Interaction
When administered concurrently with alcohol, Loratadine has no potentiating effect as measured by psychomotor performance studies. Interactions with other drugs have not been reported.
No drug interactions have been reported.
Volume of Distribution
The volume of distribution of loratadine is 120 L/Kg.
No information is available on xylometazoline pharmacokinetics.
Elimination Route
Absorption is high (greater than 80%) when administered intramuscularly or subcutaneously.
Loratadine is rapidly absorbed and achieves peak plasma concentration in 1-2 hours, while it's main metabolite achieves peak plasma concentration in 3-4 hours.
In the rapid dissolve formulation, the pharmacokinetic parameters of loratadine are as follows: Cmax = 2.56 ng/ml, Tmax = 1.14 hrs, AUC = 6.14 ng x hr/ml.
In the rapid dissolve formulation, the pharmacokinetic parameters of descarboethoxyloratadine are as follows: Cmax = 3.72 ng/ml, Tmax = 1.97 hr, AUC = 49.1 ng x hr/ml.
In the conventional formulation, the pharmacokinetic parameters of loratadine are as follows: Cmax = 2.11 ng/ml, Tmax = 1.00 hr, AUC = 4.64 ng x hr/ml
In the conventional formulation, the pharmacokinetic parameters of descarboethoxyloratadine are as follows: Cmax = 3.66 ng/ml, Tmax = 1.97 hr, AUC = 48.4 ng x hr/ml
No information is available on xylometazoline pharmacokinetics.
Half Life
The elimination half-life following both intramuscular and subcutaneous injections was approximately 2 to 3 hours. The elimination half-life was approximately 2 hours following intravenous injection.
The elimination half life is approximately 10 hours for loratadine and 20 hours for descarboethoxyloratadine.
No information is available on xylometazoline pharmacokinetics.
Clearance
The clearance of loratadine after single oral doses of 20 mg and 40 mg are 12 L/h/kg and 9 L/h/kg respectively. P-glycoprotein is involved in the clearance of many 2nd generation antihistamines, including loratadine, from the central nervous system. 1st generation antihistamines are not cleared by P-glycoprotein, which may help explain why they have a different central nervous system adverse effect profile compared to their 2nd generation counterparts. It appears that an antihistamine with higher affinity for p-glycoprotein will have a lower incidence of CNS adverse effects.
No information is available on xylometazoline pharmacokinetics.
Elimination Route
Over a 10 day period, 40% of loratadine is excreted in the urine, and 42% is eliminated in the faeces.
No information is available on xylometazoline pharmacokinetics.
Pregnancy & Breastfeeding use
Use in pregnancy: There is no experience of the use of Loratadine in human pregnancy, hence it should not be used during pregnancy.
Use in lactation: Loratadine is excreted in breast milk, so it should not be administered to lactating mother.
No foetal toxicity or fertility studies have been carried out in animals. In view of its potential systemic vasoconstrictor effect, it is advisable to take the precaution of not using Xylometazoline during pregnancy
Contraindication
Loratadine is contraindicated in patients who have shown hypersensitivity or idiosyncracy to their components.
Xylometazoline nasal drops is contraindicated in patients with trans-sphenoidal hypophysectomy or surgery exposing the dura mater. It is also contraindicated in patients who are hypersensitive to Xylometazoline.
Acute Overdose
Symptoms: Somnolence, tachycardia headache, drowsiness, extrapyramidal manifestations and palpitations.
Management: Symptomatic and supportive treatment. Immediately empty stomach by inducing emesis with ipecac syrup. Admin of activated charcoal after emesis may be useful. If induction of vomiting is unsuccessful or contraindicated (e.g. patient is comatose, having seizures or lacks gag reflex), gastric lavage with NaCl 0.9% soln may be performed to prevent aspiration of gastric contents. Saline cathartics may be useful to rapidly dilute bowel contents.
Storage Condition
Store between 20-25° C.
Protect from heat. For reasons of hygiene, do not use the bottle more than 28 days after opening it.
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