Helpex® anticold neo ginger sugar free

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT HELPEX® ANTICOLD NEO GINGER sugarfree (HELPEX® ANTICOLD NEO GINGER sugarfree)

Composition:

Active substances: paracetamol, levocetirizine dihydrochloride;

1 sachet of 2.5 g contains 500 mg of paracetamol, 1.25 mg of levocetirizine dihydrochloride;

Excipients: aspartame (E 951), mannitol (E 421), honey flavor, ginger flavor, colloidal anhydrous silicon dioxide, sodium lauryl sulfate, anhydrous citric acid, tartrazine (E 102), erythritol, ginger root extract (6:1).

Pharmaceutical form. Oral powder for solution.

Main physicochemical characteristics: powder from white to light yellow color.

Pharmacotherapeutic group. Analgesics and antipyretics. Anilides. Paracetamol, combinations without psychotropic agents.

ATC code N02BE51.

Pharmacological Properties

Pharmacodynamics

A combined medicinal product for symptomatic treatment of acute respiratory viral infections, influenza, and common cold. Possesses antipyretic, analgesic, antiallergic, and mild anti-inflammatory properties. Relieves symptoms of nasal congestion, rhinorrhea, lacrimation, sneezing, headache, and body aches.

Paracetamol exerts analgesic, antipyretic, and mild anti-inflammatory effects.

The mechanism of action of paracetamol is associated with its effect on the thermoregulatory center in the hypothalamus, its ability to inhibit the synthesis of prostaglandins and inflammatory mediators (kinins, serotonin), and an increase in the pain sensitivity threshold.

Levocetirizine dihydrochloride is a non-sedating antihistamine, the active and stable R-enantiomer of cetirizine, belonging to the group of competitive histamine antagonists. Its pharmacological action is due to blockade of H1-histamine receptors. The affinity for H1-histamine receptors is twice higher with levocetirizine than with cetirizine. It affects the histamine-dependent phase of allergic reaction development, reduces eosinophil migration, vascular permeability, and limits the release of inflammatory mediators. Prevents the development and suppresses the progression of allergic reactions, exerting anti-exudative, anti-pruritic, and anti-inflammatory effects. It does not exhibit anticholinergic or anti-serotonin activity and does not penetrate the central nervous system.

Levocetirizine inhibits the late phase of inflammation reaction induced by intradermal administration of kallikrein in patients. It also reduces the expression of adhesion molecules such as ICAM-1 and VCAM-1, which are markers of allergic inflammation. By reducing ICAM-1 adhesiveness, an indirect antiviral effect is achieved, since cellular resistance to rhinovirus increases. Additionally, levocetirizine reduces the level of secondary adhesion of Staphylococcus aureus and Haemophilus influenzae to nasopharyngeal epithelial cells infected with rhinovirus.

Pharmacokinetics

Paracetamol is rapidly and almost completely absorbed in the gastrointestinal tract. The elimination half-life is 1–4 hours. It is evenly distributed throughout all body fluids. Plasma protein binding is variable. It is primarily excreted by the kidneys in the form of conjugated metabolites.

Levocetirizine dihydrochloride. Pharmacokinetic parameters show linear dependence and are almost identical to those of cetirizine. It is rapidly absorbed after oral administration; food does not affect the extent of absorption but reduces its rate. Bioavailability is 100%. There is no available information on the distribution of levocetirizine in human tissues or its penetration through the blood-brain barrier. The volume of distribution is 0.4 L/kg. Plasma protein binding is 90%.

In humans, metabolism accounts for less than 14% of the administered dose of levocetirizine. Excretion occurs mainly via glomerular filtration and active tubular secretion. The elimination half-life (T1/2) is 7.9 ± 1.9 hours, and total clearance is 0.63 mL/min/kg. It does not accumulate and is completely eliminated from the body within 96 hours. 85.4% of the active substance dose is excreted unchanged in urine, and approximately 12.9% in feces.

In patients with impaired renal function (creatinine clearance < 40 mL/min), levocetirizine clearance is reduced and elimination half-life (T1/2) is prolonged (for example, in patients undergoing hemodialysis, total clearance is reduced by 80%), necessitating appropriate dose adjustment. During a standard 4-hour hemodialysis session, only a small fraction (less than 10%) of levocetirizine is removed. Levocetirizine passes into breast milk.

Clinical characteristics.

Indications.

Treatment of symptoms associated with acute viral respiratory infections and influenza (to reduce elevated body temperature, relieve rhinitis, reduce nasal mucosal swelling, alleviate headache, and eliminate body aches).

Contraindications.

Hypersensitivity to any component of the medicinal product or to piperazine derivatives in medical history. Blood disorders (including severe anemia, leukopenia). Severe impairment of liver and/or kidney function (creatinine clearance < 10 mL/min). Congenital hyperbilirubinemia, glucose-6-phosphate dehydrogenase deficiency, alcoholism.

Interaction with other medicinal products and other forms of interaction.

When used concomitantly with paracetamol, the following interactions may occur:

• may slow down elimination of antibiotics from the body;
• barbiturates reduce the antipyretic effect of paracetamol;
• concomitant use of paracetamol with hepatotoxic agents increases hepatotoxic effects;
• inducers of hepatic microsomal enzymes (anticonvulsants (phenytoin, barbiturates, carbamazepine), rifampicin), alcohol, and isoniazid enhance the hepatotoxicity of paracetamol;
• metoclopramide and domperidone increase, while cholestyramine, antacids, and food decrease absorption of paracetamol;
• salicylamide prolongs the elimination period of paracetamol;
• tetracycline increases the risk of anemia and methemoglobinemia caused by paracetamol;
• paracetamol reduces the effectiveness of diuretics;
• paracetamol intake may affect test results for blood glucose and uric acid levels.

Prolonged concomitant use enhances the anticoagulant effect of coumarins (e.g., warfarin), increasing the risk of bleeding.

Concomitant use of paracetamol with nonsteroidal anti-inflammatory drugs increases the risk of impaired kidney function.

Concomitant use with flucloxacillin may lead to metabolic acidosis with a high anion gap due to pyroglutamic acidosis, especially in patients with risk factors (see section "Special precautions").

Studies on levocetirizine regarding drug interactions have not been conducted. Studies with cetirizine (racemic mixture) showed that concomitant administration with antipyrine, pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide, or diazepam does not result in clinically significant adverse interactions. When used concomitantly with theophylline (400 mg/day), a slight reduction (by 16%) in total clearance of levocetirizine was observed (theophylline distribution remained unchanged). In a study involving multiple doses of ritonavir (600 mg twice daily) and cetirizine (10 mg daily), cetirizine exposure increased by approximately 40%, while ritonavir distribution was slightly reduced (-11%) with concomitant cetirizine use.

Food intake does not affect the extent of drug absorption but reduces the rate of its absorption.

Concomitant use of cetirizine or levocetirizine with alcohol or other central nervous system depressants in susceptible patients may result in additional reduction in alertness and ability to perform tasks.

Special precautions for use.

Do not exceed the recommended dose; do not take the medicine simultaneously with other products containing paracetamol, as this may lead to paracetamol overdose, which can cause liver failure.

Consult a physician if symptoms persist and/or are accompanied by high fever lasting more than 3 days; if headache becomes persistent.

Do not use concurrently with alcohol.

Patients should consult a doctor before use if they are taking analgesics daily for mild forms of arthritis; patients taking warfarin or similar anticoagulant drugs; patients with liver disease (increased risk of hepatotoxic effects of paracetamol) or kidney disease.

Cases of liver failure/dysfunction have been reported in patients with reduced glutathione levels, such as in severe malnutrition, anorexia, low body mass index, or chronic alcoholism. In patients with reduced glutathione levels, for example during severe infections such as sepsis, the use of paracetamol increases the risk of metabolic acidosis. Symptoms of metabolic acidosis include deep, rapid, or labored breathing, nausea, vomiting, and loss of appetite. Immediate medical attention should be sought if these symptoms occur.

Cases of high anion gap metabolic acidosis (HAGMA) due to 5-oxoproline (pyroglutamic) acidosis have been reported in patients with severe underlying conditions such as severe renal failure and sepsis, or in patients with malnutrition or other sources of glutathione deficiency (e.g., chronic alcoholism), who were treated with paracetamol at therapeutic doses for prolonged periods or in combination with flucloxacillin. If HAGMA due to pyroglutamic acidosis is suspected, paracetamol should be discontinued immediately and close monitoring initiated. Measurement of urinary 5-oxoproline levels may be helpful in identifying pyroglutamic acidosis as the underlying cause of HAGMA in patients with multiple risk factors.

Use with caution in patients with chronic renal insufficiency (dose adjustment required) and in elderly patients with renal impairment (possible reduction in glomerular filtration rate).

Sugar-free formulation; therefore, suitable for patients with diabetes and individuals on a low-calorie diet. The main excipient by weight is erythritol—a natural sugar substitute containing no calories, which does not affect blood glucose levels, tooth enamel, or metabolism.

Contains a natural extract of medicinal ginger (Zingiber officinale), known to reduce blood glucose and glycated hemoglobin levels.

Use with caution in patients predisposed to urinary retention (e.g., due to spinal cord injury, benign prostatic hyperplasia), as levocetirizine may increase the risk of urinary retention; and in patients at risk of seizures or with epilepsy.

There are no data on enhanced effects of sedatives when used at therapeutic doses. However, concomitant use of sedatives should be avoided during treatment with this medicine.

Antihistamines suppress skin allergic reactions; therefore, the medicine should be discontinued at least 3 days before skin allergy testing (elimination period).

Tartrazine (E 102) may cause allergic reactions.

Aspartame (E 951) is a phenylalanine derivative and poses a risk for patients with phenylketonuria.

Use during pregnancy or breastfeeding.

Pregnancy

Not recommended during pregnancy, as levocetirizine dihydrochloride is contraindicated in pregnancy.

Breastfeeding

Since the active ingredients of the medicine pass into breast milk to some extent, the medicine should not be used during breastfeeding. If treatment is necessary, breastfeeding should be discontinued.

Fertility

There are no data on the effect of the medicine on fertility.

Ability to affect reaction speed when driving or operating machinery.

During treatment, patients should refrain from activities requiring high concentration (e.g., driving vehicles or operating potentially hazardous machinery).

Method of Administration and Dosage.

Adults and children aged 12 years and older: 1 sachet up to 4 times daily. 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.

Maximum duration of use without medical consultation – 3 days.

Children.

Do not use in children under 12 years of age.

Overdose.

Hepatic injury is possible in adults who have ingested 10 g or more of paracetamol, or 5 g in the presence of risk factors, and in children who have ingested more than 150 mg/kg body weight.

In paracetamol overdose, symptoms within the first 24 hours may include pallor, nausea, vomiting, loss of appetite, and abdominal pain.

Initial clinical and biochemical signs of liver damage may appear 12–48 hours after overdose. Disturbances in glucose metabolism, hypokalemia, and metabolic acidosis (including lactic acidosis) may occur, along with elevated liver transaminase activity, increased bilirubin levels, prolonged prothrombin index, and hemorrhages.

Occasionally, nephrotoxicity has been observed, including renal colic, interstitial nephritis, and acute renal failure with acute tubular necrosis, which may manifest as severe lumbar pain, hematuria, and proteinuria, and may develop even in the absence of severe liver injury.

In severe cases, liver damage (hepatocellular necrosis) and worsening liver function may occur, potentially progressing to hepatic encephalopathy, hepatic coma, cerebral edema, and may be fatal.

In patients with risk factors (long-term treatment with carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St. John's wort, or other drugs inducing liver enzymes; alcoholism; glutathione depletion (digestive disorders, cystic fibrosis, HIV infection, fasting, cachexia)), ingestion of 5 g or more of paracetamol may lead to liver injury.

Cardiac arrhythmias and acute pancreatitis have also been reported, typically accompanied by liver function disturbances and hepatotoxicity.

With large doses, central nervous system effects may include disorientation.

With prolonged use of the drug in high doses, blood-forming organs may develop aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, or thrombocytopenia.

Treatment of overdose: In case of overdose, prompt medical assistance is required. The patient should be immediately transported to a hospital, even if early symptoms of overdose are absent.

Symptoms may be limited to nausea and vomiting and may not reflect the severity of overdose or risk of organ damage. Gastric lavage should be performed within the first hours after suspected overdose. Activated charcoal may be beneficial if the excessive dose of paracetamol was ingested within the past hour.

Plasma paracetamol concentration should be measured 4 hours or later after ingestion (earlier concentrations are unreliable). Intravenous administration of N-acetylcysteine should be initiated within 24 hours after paracetamol ingestion according to current guidelines. Maximum antidotal effect is achieved within 8 hours after paracetamol intake; thereafter, antidote efficacy decreases sharply. In the absence of vomiting, oral methionine may be used as an appropriate alternative in remote areas outside hospital settings.

Symptoms of levocetirizine dihydrochloride overdose may include drowsiness in adults and initial excitation and increased irritability followed by drowsiness in children.

Treatment of overdose. There is no specific antidote for levocetirizine. In case of overdose symptoms, symptomatic and supportive therapy is recommended. Gastric lavage may be considered shortly after drug ingestion. Hemodialysis is ineffective for removing levocetirizine from the body.

Adverse Reactions

Immune system disorders: hypersensitivity reactions, including itching, urticaria, skin and mucous membrane rashes, angioneurotic edema, anaphylactic shock, erythema multiforme, Stevens–Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

Nervous system disorders: drowsiness, headache, increased fatigue, weakness, asthenia, tremor, seizures, paresthesia, dizziness, fainting, dysgeusia, sleep disturbances, aggression, excitement, insomnia, suicidal thoughts, hallucinations, depression.

Eye disorders: visual disturbances, blurred vision.

Cardiac disorders: palpitations, tachycardia.

Renal and urinary system disorders: dysuria, urinary retention.

Ear and labyrinth disorders: vertigo.

Respiratory system disorders: bronchospasm in patients sensitive to aspirin and other nonsteroidal anti-inflammatory drugs, dyspnea.

Gastrointestinal disorders: nausea, vomiting, dry mouth, abdominal pain, diarrhea, constipation, increased appetite.

Hepatobiliary disorders: liver function abnormalities, elevated liver enzyme activity, usually without development of jaundice, hepatitis.

Endocrine disorders: hypoglycemia, up to hypoglycemic coma.

Blood and lymphatic system disorders: anemia, including hemolytic anemia, bruising or bleeding; sulfhemoglobinemia and methemoglobinemia (cyanosis, dyspnea, chest pain); agranulocytosis, thrombocytopenia.

Musculoskeletal and connective tissue disorders: myalgia, arthralgia.

Metabolism and nutrition disorders: metabolic acidosis with a high anion gap.

General disorders: edema, weight gain.

Description of selected adverse reactions

Cases of metabolic acidosis with a high anion gap due to pyroglutamic acidosis have been observed in patients with risk factors who used paracetamol (see section "Special precautions"). Pyroglutamic acidosis may occur due to low glutathione levels in these patients.

Reporting suspected adverse reactions

Reporting suspected adverse reactions after the medicine has been authorized is important. It allows continued monitoring of the benefit-risk balance of the medicine. Healthcare professionals and patients, as well as their legal representatives, should report any suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 4 years.

Storage conditions.

Store in the original packaging out of reach of children at a temperature not exceeding 25 °C.

Packaging.

2.5 g of powder in sachets; 10 sachets in a cardboard box.

Availability category. Over-the-counter.

Manufacturer. Alpex Pharma SA.

Manufacturer’s address and place of business.

Via Cantonale, 6805 Mezzovico-Vira, Switzerland.