Quait

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT KVAJT® (QUIET)

Composition:

Active substances: guaifenesin, complex sedative extract;

1 ml of solution contains: complex sedative extract, dry, from a mixture of hawthorn flowers and leaves (Crataegi folium cum flore), hops strobiles (Lupuli flos), St. John's wort herb (Hyperici herba), lemon balm leaves (Melissae folium), passionflower herb (Passiflorae herba), elder flowers (Sambuci flos), valerian root (Valerianae radix) (2-4:1), extracted with 30% ethanol – 77.5 mg; guaifenesin calculated as 100% substance – 40 mg;

Excipients: fructose; glucose monohydrate; xanthan gum; sodium saccharin; maltodextrin; sodium cyclamate; sodium citrate; citric acid monohydrate; ethanol 96%; propylene glycol; sodium benzoate (E 211); orange oil; purified water.

Pharmaceutical form. Oral solution.

Main physicochemical characteristics: syrup-like, clear or slightly cloudy liquid ranging from reddish-brown to brown in color, with a characteristic odor and taste. A slight sediment may form during storage.

Pharmacotherapeutic group. Hypnotics and sedatives. ATC code N05CM.

Pharmacological properties.

Pharmacodynamics.

The pharmacologically active components of the drug are guaifenesin and herbal extract, which exert predominantly sedative effects. The sedative effect of the extract combines with the myorelaxant and anxiolytic action of guaifenesin (relaxes smooth muscles).

Pharmacokinetics.

Guaifenesin is rapidly absorbed from the gastrointestinal tract, metabolized in the liver via conjugation with glucuronic acid, and excreted primarily in the form of inactive metabolites in the urine.

The biological half-life is approximately 1 hour.

Clinical characteristics.

Indications.

Mild form of neurasthenia, especially when accompanied by anxiety, fear, sadness, restlessness, irritability, decreased concentration, or fatigue; mild form of insomnia, exhaustion, or neurotic memory disorders.

Supportive therapy in migraine, headache due to nervous tension, psychosomatic vascular disorders with neurocirculatory dystonia, neurogenic tetany, facial pain, and climacteric syndrome.

Functional gastrointestinal disorders, dyspeptic syndrome without organic lesions, irritable bowel syndrome, and adjunctive therapy in organic gastrointestinal diseases with a pronounced neurotic component.

Psychosomatic dermatoses accompanied by pruritus (urticaria, atopic eczema).

Contraindications.

Hypersensitivity to the active components or to any excipients of the drug; myasthenia gravis; epilepsy; depression and other conditions associated with depression of central nervous system (CNS) activity; bradycardia; concomitant use of cyclosporine or tacrolimus; use in HIV-positive patients taking protease inhibitors.

Interaction with other medicinal products and other forms of interactions.

Guaifenesin

Guaifenesin enhances the analgesic effect of paracetamol and acetylsalicylic acid, and potentiates the effects of alcohol, sedative antihistamines, and other substances that depress the CNS. The central action of muscle relaxants may enhance the adverse effects of guaifenesin, particularly muscle weakness.

Hypericum perforatum (St. John's wort)

Hypericum perforatum may induce CYP3A4, CYP1A2, and CYP2C9 isoenzymes of cytochrome P450, which may lead to reduced efficacy of other concurrently administered drugs metabolized by these isoenzymes. Hypericum perforatum also induces P-glycoprotein. This interaction was first observed in healthy volunteers receiving indinavir and Hypericum perforatum. A similar interaction can also be expected with other antiretroviral protease inhibitors (amprenavir, nelfinavir, ritonavir, saquinavir) and non-nucleoside reverse transcriptase inhibitors (delavirdine, efavirenz, nevirapine) used in the treatment of HIV-positive patients. Clinically significant interactions with Hypericum perforatum have also been reported with concomitant use of cyclosporine, tacrolimus, digoxin, and warfarin. This interaction may lead to decreased plasma concentrations of these drugs and, consequently, reduced therapeutic efficacy.

Clinically proven drug interactions have been demonstrated between Hypericum perforatum and theophylline, amitriptyline, and oral contraceptives. There is also a potential for interaction with antiepileptic drugs. Potential interactions between Hypericum perforatum and many other drugs metabolized by cytochrome P450 3A4 isoenzyme, including grapefruit juice, are expected.

Patients receiving treatment with indinavir or other antiretroviral drugs should avoid using Hypericum perforatum, as the interaction may reduce their efficacy and potentially lead to resistance.

Hypericum perforatum must not be used with cyclosporine. If a patient is taking cyclosporine, Hypericum perforatum should be discontinued and cyclosporine dosage adjusted based on plasma cyclosporine levels. Close monitoring for any signs of tissue rejection is necessary in transplant patients.

Concomitant use of Hypericum perforatum and tacrolimus may lead to subtherapeutic concentrations of tacrolimus, potentially causing transplant rejection. Patients should avoid concomitant use of Hypericum perforatum and tacrolimus. If concomitant use occurs, Hypericum perforatum should be discontinued and plasma levels of tacrolimus monitored, as dose adjustment of tacrolimus may be necessary.

Concomitant administration of Hypericum perforatum with digoxin is not recommended. If administration of Hypericum perforatum is necessary, monitoring of digoxin plasma levels should be performed and the dose adjusted accordingly. When increasing the digoxin dose, the dose of Hypericum perforatum remains unchanged; regarding discontinuation of therapy, consultation with a physician is advised.

Concomitant use of Hypericum perforatum with warfarin is not recommended. If administration of Hypericum perforatum is necessary, prothrombin time should be monitored during warfarin therapy and the dose adjusted accordingly. When increasing the warfarin dose, the dose of Hypericum perforatum remains unchanged; regarding discontinuation of therapy, consultation with a physician is advised.

Hypericum perforatum may significantly reduce the efficacy of theophylline; therefore, concomitant use is not recommended. If Hypericum perforatum must be used, theophylline plasma levels should be monitored and the dose adjusted as needed, without changing the dose of Hypericum perforatum.

Concomitant use with oral contraceptives may lead to abnormal uterine bleeding (menorrhagia, hypermenorrhea, metrorrhagia). A reduced contraceptive effect may occur. It is recommended to use combined oral hormonal contraceptives in combination with other contraceptive methods (barrier methods) during therapy with Hypericum perforatum.

Concomitant therapy with amitriptyline is not recommended.

Concomitant therapy with Hypericum perforatum and antiepileptic drugs (carbamazepine, phenobarbital, phenytoin) is not recommended. A decreased plasma level of the antiepileptic drug and occurrence of seizures may occur. If administration of Hypericum perforatum is necessary, monitoring of antiepileptic drug plasma levels and symptoms of reduced efficacy (e.g., increased seizure activity) should be performed. Upon discontinuation of Hypericum perforatum therapy, a reduction in the dose of antiepileptic drugs may be necessary; monitoring for signs of antiepileptic drug toxicity should be conducted.

Clinically significant interactions have been observed between Hypericum perforatum and SSRIs and triptans. Due to the increased risk of adverse reactions associated with these interactions, Hypericum perforatum should not be used concomitantly with these drugs.

Use of Hypericum perforatum is not recommended in patients taking antibiotics, sulfonamides, calcium channel blockers, female sex hormones, or hypolipidemic agents (statins).

Passiflora

When used concomitantly with CNS depressants such as barbiturates, tranquilizers, the sedative and hypnotic effects of the drug are enhanced. Concomitant intake with benzodiazepines is not recommended. Concomitant use with disulfiram should be avoided. During treatment with the drug, consumption of alcoholic beverages should be avoided.

Valeriana

Potentiates the effects of alcohol, sedatives, hypnotics, antihypertensives, anxiolytics, and spasmolytics.

Hawthorn

Enhances the effects of sedatives, hypnotics, antiarrhythmic agents, and cardiac glycosides.

Melissa

Concomitant use may enhance the effects of other sedatives and hypnotics.

Effect on laboratory test results.

Guaifenesin may cause false-positive results in diagnostic tests for 5-hydroxyindoleacetic acid (using nitrosonaphthol as reagent in the photometric method) and vanillylmandelic acid in urine. In view of this, treatment with the drug should be discontinued 48 hours before urine collection for these tests.

Special precautions.

The drug should be used with caution in patients with severe liver or kidney diseases and in cases of intoxication with substances that depress the central nervous system (CNS).

During treatment, patients, especially those with fair skin, should avoid prolonged and intense exposure to ultraviolet radiation (sunbathing, being in the sun at high altitudes, tanning beds).

Patients receiving indinavir or other antiretroviral drugs should avoid using Hypericum perforatum (St. John's wort), as this may lead to the development of resistance to antiretroviral drugs and reduced treatment efficacy.

Due to the potential for drug interactions, concomitant use of Hypericum perforatum-containing products should be discontinued in patients taking SSRIs, triptans, theophylline, digoxin, antiepileptic drugs, warfarin, or oral contraceptives.

Use with caution in patients with severe organic gastrointestinal disorders.

Elderly patients should start treatment with the minimum dose.

Alcohol consumption should be avoided during treatment.

Specific sensitivity to the smell of valerian may occur.

Guaifenesin should be discontinued 48 hours before urine collection for the analysis of vanillylmandelic acid and 5-hydroxyindoleacetic acid in urine when using nitrosonaphthol as a reagent (see section "Interaction with other medicinal products and other forms of interaction").

The drug contains 11.72% (v/v) ethanol; one dose (5 mL) contains 0.462 g of ethanol, which should be considered when administering the drug during pregnancy, breastfeeding, in children, and in patients at risk (patients with liver disease, epilepsy). One dose (5 mL) of the solution is equivalent to 4.9 mL of wine or 11.5 mL of beer. Due to its ethanol content, the medicinal product is harmful for patients with alcoholism.

One dose (5 mL) of the drug contains 0.25 g of fructose and 1.0 g of glucose. This should be considered when treating patients with diabetes mellitus. The drug should not be used in patients with hereditary fructose intolerance or glucose-galactose malabsorption.

This medicinal product contains 1.616 mmol/dose (or 37.12 mg/dose) of sodium, which corresponds to 11.15% of the WHO recommended maximum daily intake of sodium for adults (2 g). Caution is advised when administering to patients on a sodium-restricted diet.

Use during pregnancy or breastfeeding.

Due to insufficient safety data, the drug is contraindicated during pregnancy and breastfeeding.

Ability to affect reaction speed when driving or operating machinery.

Because the drug contains ethanol and guaifenesin, its use may lead to impaired reaction time, with individual variability in each patient (see "Adverse reactions of the nervous system"). Therefore, potentially hazardous activities requiring high attention, such as driving a vehicle or operating machinery, should be avoided.

Dosage and Administration.

The usual dose is 5 ml (1 teaspoonful) of the medication 3 times daily. If necessary, the dose may be increased to 10 ml 3 times daily or reduced to 2.5 ml in the morning and afternoon and 5 ml in the evening. The dose may be adjusted according to the patient's condition. The interval between each individual dose should be 4 to 6 hours. Maximum daily dose – 30 ml.

Elderly patients

Dosage is the same as for adult patients.

The individual dose can be measured using the dosing cup provided.

The medication may be mixed with beverages (juice, except grapefruit juice, tea).

Children.

The medication may be administered to children aged 12 years and older.

Overdose.

Overdose initially manifests as central nervous system depression and drowsiness. Later, these symptoms may be accompanied by nausea, mild muscular weakness, joint pain, and a sensation of heaviness in the stomach.

Other possible symptoms include bitter taste in the mouth, discomfort in the liver area, headache, dizziness, lethargy, general weakness, hand tremor, dilated pupils, chest tightness, abdominal pain, decreased hearing and visual acuity, tachycardia, decreased blood pressure, bradycardia, and reduced concentration.

With guaifenesin overdose, cases of nephrolithiasis have been reported.

Treatment is purely symptomatic and follows general principles of overdose management. There is no specific antidote.

Side effects.

Immune system: hypersensitivity reactions, vasculitis.

Nervous system: dizziness, drowsiness, suppression of emotional responses, depression.

Gastrointestinal tract: discomfort in the gastrointestinal tract, nausea, vomiting, spasms, heartburn, diarrhea or constipation.

Skin and subcutaneous tissue: exanthema, pruritus, rash, urticaria, photosensitization (during treatment, avoid UV radiation), hyperemia, skin swelling.

Musculoskeletal and connective tissue: muscle weakness.

Respiratory system: dyspnea.

Cardiovascular system: increased blood pressure, tachycardia, bradycardia, ventricular tachycardia.

General disorders: increased fatigue, general weakness, decreased mental and physical performance.

Shelf life. 4 years.

Do not use the medicinal product after the expiry date stated on the packaging.

Storage conditions.

Store at a temperature not exceeding 25 °C. Do not freeze.

Keep out of reach of children.

Packaging.

100 ml in a bottle. 1 bottle with a measuring cup/dosing cup in a carton.

Availability. Over-the-counter.

Manufacturer.

JSC "Farmak".

Manufacturer's location and address of operations.

74, Kyrylivska Street, Kyiv, 04080, Ukraine.