Instructions for Helpex Anticold Neo powder for oral solution sachet 4 g with lemon flavor No. 10
Composition
active ingredients: paracetamol, levocetirizine dihydrochloride, phenylephrine hydrochloride;
1 sachet of 4 g contains paracetamol 500 mg, levocetirizine dihydrochloride 1.25 mg, phenylephrine hydrochloride 10 mg;
excipients:
Helpex® Anticold NEO with lemon flavor: colloidal anhydrous silicon dioxide, aspartame (E 951), mannitol (E 421), sucralose, sucrose, tartrazine (E 102), lemon flavoring, citric acid anhydrous;
Helpex® Anticold NEO with raspberry flavor: colloidal anhydrous silicon dioxide, aspartame (E 951), mannitol (E 421), sucralose, sucrose, betanin (E 162), raspberry flavoring.
Dosage form
Powder for oral solution.
Main physicochemical properties:
Helpex® Anticold NEO with lemon flavor: pale yellow to yellow powder;
Helpex® Anticold NEO with raspberry flavor: almost white powder with a pale pink tint, dark red particles may be present.
Pharmacotherapeutic group
Analgesics and antipyretics. Anilides. Paracetamol, combinations without psycholeptics.
ATX code N02B E51.
Pharmacological properties
Pharmacodynamics.
Combined drug for the symptomatic treatment of acute respiratory viral infections, flu and colds. Has antipyretic, analgesic, antiallergic and weak anti-inflammatory properties. Eliminates symptoms of nasal congestion, runny nose, tearing, sneezing, headache, body aches.
Paracetamol has analgesic, antipyretic and weak anti-inflammatory effects.
The mechanism of action of paracetamol is associated with the drug's effect on the thermoregulation center in the hypothalamus, its ability to inhibit the synthesis of prostaglandins and inflammatory mediators (kinin, serotonin), and an increase in the pain threshold.
Levocetirizine dihydrochloride is a non-sedating antihistamine, an active stable R-enantiomer of cetirizine, belonging to the group of competitive histamine antagonists. The pharmacological action is due to the blocking of H1-histamine receptors. The affinity for H1-histamine receptors of levocetirizine is 2 times higher than that of cetirizine. It affects the histamine-dependent stage of the development of an allergic reaction, reduces eosinophil migration, vascular permeability, limits the release of inflammatory mediators. It prevents the development and suppresses the manifestation of allergic reactions, has antiexudative, antipruritic, anti-inflammatory effects, does not have anticholinergic and antiserotonin effects, does not penetrate the central nervous system.
Levocetirizine inhibits the late phase of the inflammatory response induced in patients by intradermal administration of kallikrein. It also reduces the expression of adhesion molecules such as ICAM-1 and VCAM-1, which are markers of allergic inflammation. By reducing the adhesion of ICAM-1, an indirect antiviral effect is exerted, since cell resistance to rhinovirus increases. Levocetirizine also reduces the level of secondary adhesion of Staphylococcus aureus and Haemophilus influenzae to nasopharyngeal epithelial cells that have been infected with rhinovirus.
Phenylephrine hydrochloride is a relatively selective α1-adrenomimetic. It has a weak effect on α2- and β-adrenergic receptors. Due to its vasoconstrictor effect, phenylephrine reduces swelling of the nasal mucosa, the volume of nasal secretions and improves nasal breathing due to easier passage of air through the nose. Use for temporary relief of nasal congestion in acute respiratory viral infections and colds.
Pharmacokinetics.
Paracetamol is rapidly and almost completely absorbed from the gastrointestinal tract. The half-life is 1–4 hours. It is evenly distributed in all body fluids. Binding to plasma proteins is variable. It is excreted mainly by the kidneys in the form of conjugated metabolites.
Levocetirizine dihydrochloride. Pharmacokinetic parameters have a linear relationship and are almost the same as those of cetirizine. Rapidly absorbed when administered orally, food intake does not affect the extent of absorption, but reduces its rate.
There is no information on the distribution of levocetirizine in human tissues, as well as on its penetration through the blood-brain barrier. The volume of distribution is 0.4 l/kg. Plasma protein binding is 90%.
About 14% of levocetirizine is metabolized in the body. Given the low degree of metabolism and the lack of increased inhibitory effect, the interaction of levocetirizine with other substances (and vice versa) is unlikely.
Excretion of the drug occurs mainly due to glomerular filtration and active tubular secretion. The half-life (T1/2) is 7.9 ± 1.9 hours, total clearance is 0.63 ml/min/kg. It does not accumulate, it is completely excreted from the body in 96 hours. 85.4% of the dose of the active substance is excreted unchanged in the urine, about 12.9% in the feces.
Phenylephrine hydrochloride. The action occurs quickly and lasts about 20 minutes. It is metabolized in the liver or in the gastrointestinal tract, excreted by the kidneys.
Indication
Treatment of symptoms that occur during acute respiratory viral infections, influenza (to reduce elevated body temperature, reduce runny nose, relieve swelling of the nasal mucosa, relieve headaches, eliminate body aches).
Contraindication
Hypersensitivity to any component of the drug, piperazine derivatives in history. Arterial hypertension, cardiovascular diseases, conduction disorders, severe ischemic heart disease, atherosclerosis, heart failure. Hyperthyroidism, pheochromocytoma. Severe liver and/or kidney dysfunction (creatinine clearance < 10 ml/min). Acute hepatitis. Pancreatitis. Thrombosis, thrombophlebitis, increased blood clotting and tendency to thrombus formation, tendency to vasospasm. Congenital hyperbilirubinemia, glucose-6-phosphate dehydrogenase deficiency. Alcoholism. Blood diseases (including severe anemia, leukopenia). Prostatic hypertrophy with difficulty urinating, bladder neck obstruction. Diabetes mellitus. Angle-closure glaucoma. Simultaneous use with tricyclic antidepressants; with MAO inhibitors and for 2 weeks after stopping their use; beta-blockers and other antihypertensive drugs, sympathomimetics, drugs that suppress or increase appetite; amphetamine-like psychostimulants. Pregnancy and breastfeeding. Do not use in children under 12 years of age. Epilepsy, increased excitability, sleep disorders. Bronchial asthma.
Interaction with other medicinal products and other types of interactions
When used simultaneously with paracetamol, the following types of interactions may occur:
the elimination of antibiotics from the body may be slowed down;
barbiturates reduce the antipyretic effect of paracetamol;
with simultaneous use of paracetamol with hepatotoxic agents, the toxic effect on the liver increases;
Inducers of liver microsomal enzymes, anticonvulsants, including phenytoin; carbamazepine, barbiturates, rifampicin, alcohol and isoniazid, may enhance the hepatotoxicity of paracetamol;
metoclopramide and domperidone increase, and cholestyramine, antacids and food reduce the absorption of paracetamol;
salicylamide prolongs the elimination period of paracetamol;
tetracycline increases the risk of developing anemia and methemoglobinemia caused by paracetamol;
the half-life of chloramphenicol increases (up to 5 times);
Paracetamol reduces the effectiveness of diuretics.
With simultaneous long-term use, the anticoagulant effect of coumarins (e.g. warfarin) is enhanced, increasing the risk of bleeding. Periodic use has no significant effect.
Concomitant use of paracetamol with nonsteroidal anti-inflammatory drugs increases the risk of renal dysfunction.
When used simultaneously with flucloxacillin, there is a risk of metabolic acidosis with a high anion gap, especially in patients with risk factors (see section "Special instructions").
No interaction studies have been conducted with levocetirizine. Studies with cetirizine (racemic mixture) have shown that concomitant use with antipyrine, pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide or diazepam does not reveal clinically significant adverse interactions. When co-administered with theophylline (400 mg/day), a small decrease (by 16%) in the total clearance of levocetirizine was observed (theophylline distribution was not changed). In a study of multiple doses of ritonavir (600 mg twice daily) and cetirizine (10 mg daily), the exposure of cetirizine increased by approximately 40%, while the distribution of ritonavir was slightly impaired (–11%) with concomitant use of cetirizine.
Food intake does not affect the extent of absorption of the drug, but reduces the rate of its absorption.
Regular use of paracetamol simultaneously with zidovudine may lead to the development of neutropenia and an increased risk of liver damage; simultaneous use with azidothymidine may lead to the development of neutropenia.
The use of phenylephrine hydrochloride with MAO inhibitors (including moclobemide), indomethacin and bromocriptine can cause severe arterial hypertension; with tricyclic antidepressants (amitriptyline) increases the risk of cardiovascular side effects; may reduce the effectiveness of ß-blockers and other antihypertensive drugs (debrizoquine, guanethidine, reserpine, methyldopa) with an increased risk of arterial hypertension and adverse reactions from the cardiovascular system; with sympathomimetic amines, digoxin and cardiac glycosides increases the risk of arrhythmias and myocardial infarction. Rauwolfia alkaloids reduce the therapeutic effect of phenylephrine hydrochloride; α-blockers (phentolamine), phenothiazines, furosemide and other diuretics prevent vasoconstriction. With the simultaneous use of phenylephrine and ganglioblockers, adrenoblockers, rauwolfia alkaloids or methyldopa, a decrease in blood pressure is possible.
Application features
Do not exceed the indicated dose; do not take the drug simultaneously with other drugs containing paracetamol, as paracetamol overdose is possible. In case of overdose, you should immediately consult a doctor, even if the patient feels well, because of the risk of delayed serious liver damage (see section "Overdose").
The risk of paracetamol overdose increases in alcoholic liver disease. Do not use simultaneously with alcohol.
You should consult a doctor if symptoms persist, worsen, or persist for more than 3 days, and if the headache becomes persistent.
Before using the drug, patients with liver disease (the risk of hepatotoxic effects of paracetamol increases) or kidney disease, and patients who use warfarin or similar drugs with anticoagulant effects and who take analgesics every day for mild arthritis should consult a doctor.
Cases of liver failure/dysfunction have been reported in patients with reduced glutathione levels, such as those with severe wasting, anorexia, low body mass index or chronic alcoholism. Patients with reduced glutathione levels, such as those with severe infections such as sepsis, are at increased risk of developing metabolic acidosis when taking paracetamol. Symptoms of metabolic acidosis include deep, rapid or labored breathing, nausea, vomiting, loss of appetite. You should seek medical attention immediately if these symptoms occur.
Caution is advised when using paracetamol concomitantly with flucloxacillin due to an increased risk of high anion gap metabolic acidosis (HAGMA), particularly in patients with severe renal insufficiency, sepsis, malnutrition and other sources of glutathione deficiency (e.g. chronic alcoholism), and in patients taking the maximum daily dose of paracetamol. Close monitoring, including measurement of urinary 5-oxoproline, is recommended.
Caution should be exercised when prescribing the drug to patients with Raynaud's disease. The drug may affect the results of laboratory tests for blood glucose and uric acid.
Use with caution in patients with chronic renal failure (dosage regimen adjustment required) and in elderly patients with renal failure (possible reduction in glomerular filtration).
Use with caution in patients prone to urinary retention; in patients at risk of seizures, as the use of the drug may lead to increased seizures (see section "Contraindications").
Phenylephrine may cause an attack of angina.
Antihistamines suppress the skin allergy test, so before performing it, the drug should be stopped 3 days before the test (withdrawal period). The dye tartrazine (E 102) may cause allergic reactions.
Aspartame (E 951) is a derivative of phenylalanine, which is dangerous for people with phenylketonuria.
Helpex® Anticold NEO contains sucrose, therefore patients with known intolerance to some sugars should consult their doctor before taking this medicine.
Use during pregnancy or breastfeeding
Pregnancy
The safety of the drug during pregnancy has not been established, therefore the drug is not used in pregnant women (see the "Contraindications" section).
Breast-feeding
Since the active substances of the drug penetrate into breast milk to some extent, breastfeeding should be discontinued during treatment with the drug.
Fertility
There are no data on the effect of the drug on fertility.
Ability to influence reaction speed when driving vehicles or other mechanisms
During treatment with the drug, you should refrain from activities that require increased concentration of attention (for example, driving a vehicle or working with other potentially dangerous mechanisms).
Method of administration and doses
Adults and children over 12 years of age: 1 sachet up to 4 times a day. The intervals between doses should be at least 4 hours. Dissolve the contents of the sachet in a glass of hot water and drink.
The duration of treatment should not exceed 5 days.
The maximum period of use without consulting a doctor is 3 days.
Do not use in children under 12 years of age.
Overdose
Liver damage is possible in adults who have taken 10 g or more of paracetamol or 5 g in the presence of risk factors, and in children who have taken more than 150 mg/kg of body weight.
In case of paracetamol overdose, symptoms develop in the first 24 hours: pallor, nausea, vomiting, loss of appetite, abdominal pain.
Clinical and biochemical signs of liver damage appear 12–48 hours after overdose.
Cardiac arrhythmias and pancreatitis have been reported, usually accompanied by liver dysfunction and hepatotoxicity.
Hypoglycemic coma, thrombocytopenia, impaired glucose metabolism and metabolic acidosis, hypokalemia, increased hepatic transaminase activity, increased bilirubin levels and increased prothrombin index, and hemorrhage may occur.
Occasionally, nephrotoxicity has been observed from the urinary system, including renal colic, interstitial nephritis, and acute renal failure with acute tubular necrosis, which may present with severe lower back pain, hematuria, and proteinuria and may occur even in the absence of severe liver damage. High doses may lead to hepatocellular necrosis with encephalopathy and impaired consciousness, hepatic coma, acute renal failure, and death.
In patients with risk factors [long-term treatment with carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St. John's wort or other drugs that induce liver enzymes; alcoholism; glutathione cachexia (digestive disorders, cystic fibrosis, HIV infection, starvation, cachexia)], the use of 5 g or more of paracetamol may lead to liver damage.
When taking large doses, the central nervous system experiences disorientation.
With prolonged use of the drug in high doses, aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, and thrombocytopenia may develop on the part of the hematopoietic organs.
Treatment of overdose: In case of suspected overdose, the patient should be taken to hospital, even if there are no early symptoms of overdose. Symptoms may be limited to nausea and vomiting and may not reflect the severity of the overdose or the risk of organ damage. Gastric lavage should be performed in the first hours after a suspected overdose. Treatment with activated charcoal may be appropriate if the overdose of paracetamol was taken within 1 hour.
The concentration of paracetamol in the blood plasma should be measured 4 hours or later after ingestion (earlier concentrations are unreliable). Intravenous N-acetylcysteine is administered within 24 hours after ingestion of paracetamol according to current recommendations, the maximum effect of the antidote occurs within 8 hours after ingestion of paracetamol, and thereafter the effectiveness of the antidote decreases sharply.
In the absence of vomiting, oral methionine may be used as a suitable alternative in remote areas outside the hospital.
Symptoms of levocetirizine dihydrochloride overdose may include drowsiness in adults and initial agitation and increased irritability followed by drowsiness in children.
Treatment of overdose. There is no specific antidote for levocetirizine. In case of symptoms of overdose, symptomatic and supportive therapy is recommended. Gastric lavage may be considered shortly after ingestion. Hemodialysis is not effective in removing levocetirizine from the body.
Phenylephrine overdose is manifested by symptoms from the cardiovascular system with respiratory depression. Nervousness, headache, dizziness, insomnia, nausea, vomiting, increased blood pressure or reflex bradycardia, tachycardia, palpitations, urinary retention may be present.
Treatment of overdose. Intravenous α-blockers are used to eliminate hypertensive effects; in case of convulsions, diazepam.
Adverse reactions
Immune system disorders: hypersensitivity reactions including pruritus, urticaria, rash (generalized, erythematous), angioedema, anaphylactic shock; erythema multiforme exudative, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
On the part of the organs of vision: visual and accommodation disorders, blurred vision, oculogyration (involuntary circular movements of the eyeball), mydriasis, increased intraocular pressure.
From the nervous system: sedative effect, drowsiness when exceeding the therapeutic dose, insomnia, dizziness, fainting, weakness, asthenia, increased fatigue, decreased mental and physical performance, mood changes, dysphoria, headache, paresthesia, seizures, tremor, tic, dysgeusia, dyskinesia, memory impairment, anxiety, restlessness.
On the part of the psyche: sleep disorders, psychomotor agitation, hallucinations, apathy, depression, aggression, insomnia, suicidal thoughts, nightmares, nervousness, irritability, feelings of fear, disorientation.
Respiratory system: bronchospasm in patients sensitive to aspirin and other nonsteroidal anti-inflammatory drugs, shortness of breath, pharyngitis, rhinitis.
On the part of the kidneys and urinary system: spasm of the urethral canals and vesical sphincters, dysuria, enuresis, urinary retention, difficulty urinating, renal colic, nephrotoxicity.
On the part of the digestive tract: nausea, vomiting, dry mouth, gastrointestinal discomfort, epigastric pain, diarrhea, constipation, increased appetite, heartburn, flatulence, hypersalivation.
From the organs of hearing and balance: vertigo, tinnitus.
From the hepatobiliary system: impaired liver function, increased activity of liver enzymes, hepatitis, liver failure.
On the part of the endocrine system: hypoglycemia, up to hypoglycemic coma.
From the blood and lymphatic system: thrombocytopenia, agranulocytosis, anemia, including hemolytic anemia (bruising or bleeding); sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), leukopenia, pancytopenia, neutropenia.
Musculoskeletal system: myalgia, arthralgia.
General disorders: malaise, edema, weight gain, fever.
If any adverse reactions occur, discontinue use of the drug and consult a doctor.
Reporting of suspected adverse reactions
Reporting of suspected adverse reactions occurring after the marketing authorisation of a medicinal product plays an important role. This allows for continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals should report any suspected adverse reactions through the national pharmacovigilance system.
Expiration date
4 years.
Storage conditions
Store out of the reach of children in the original packaging at a temperature not exceeding 25 °C.
Packaging
4 g of powder in a sachet; 10 sachets in a cardboard box.
Vacation category
Without a prescription.
Producer
Alpex Pharma SA.
Location of the manufacturer and address of its place of business
Via Cantonale, 6805 Mezzovico-Vira, Switzerland.
