Freenos SR

Pseudoephedrine hydrochloride, loratadine.

Each sustained-release capsule contains: Immediate release pellets: Loratadine 5 mg, Pseudoephedrine HCl 60 mg.
Sustained-release pellets: Pseudoephedrine HCl 60 mg.

Pharmacology: Loratadine is a long-acting tricyclic antihistamine with selective, peripheral H₁-receptor activity.
Pseudoephedrine HCl, one of the naturally occurring alkaloids of Ephedra and an orally administered vasoconstrictor, produces a gradual but sustained decongestant effect facilitating shrinkage of congested mucosa in upper respiratory areas. The mucous membrane of the respiratory tract is decongested through the action of the sympathetic nerves.

For relief of nasal and ocular symptoms of upper respiratory mucosal congestion, such as in allergic rhinitis. They are intended for short term use only unless taken under medical supervision.

Adults and children ≥ 12 years: 1 capsule twice daily.

In the event of overdosage, treatment, which should be started immediately, is symptomatic and supportive. Discontinuation of use, gastric lavage and support of vital functions are advised.
Manifestations: They may vary from CNS depression (sedation, apnea, diminished mental alertness, cyanosis, coma, cardiovascular collapse) to stimulation (insomnia, hallucination, tremors, or convulsions) to death. Other signs and symptoms may be euphoria, excitement, tachycardia, palpitations, thirst, perspiration, nausea, dizziness, tinnitus, ataxia, blurred vision and hypertension or hypotension. Stimulation is particularly likely in children, as are atropine-like signs and symptoms (dry mouth; fixed, dilated pupils; flushing; hyperthermia; and gastrointestinal symptoms).
In large doses sympathomimetics may give rise to giddiness, headache, nausea, vomiting, sweating, thirst, tachycardia, precordial pain, palpitations, difficulty in micturition, muscular weakness and tenseness, anxiety, restlessness, and insomnia. Many patients can present a toxic psychosis with delusions and hallucinations. Some may develop cardiac arrhythmias, circulatory collapse, convulsions, coma, and respiratory failure.
Treatment: Emergency treatment should be started immediately. There is no specific antidote. Treatment of overdosage consists of single-dose activated charcoal. Use should be considered in a patient who presents within 1 hour of ingestion. Activated charcoal is contraindicated in a patient with diminished level of consciousness unless airway is protected. In some rare situations, gastric lavage may be appropriate if initiated within 1 hour of ingestion, though this technique has not been proven to be beneficial and is thus rarely used due to risks of complications and lack of efficacy. Its use is contraindicated in patients with unprotected airways, in patients where use would increase risk and severity of aspiration, and in patients at risk of hemorrhage or GI perforation. Ipecac has not been shown to be beneficial based on experimental and clinical studies.
Loratadine is not cleared by hemodialysis to any appreciable extent. It is not known if loratadine is removed by peritoneal dialysis.
After emergency treatment, the patient should continue to be medically monitored. Treatment of the signs & symptoms of overdosage is symptomatic and supportive. Stimulants (analeptic agents) should not be used. Vasopressors may be used to treat hypotension. Short-acting barbiturates, diazepam or paraldehyde may be administered to control seizures. Hyperpyrexia, especially in children, may require treatment with tepid water sponge baths or hypothermic blanket. Apnea is treated with ventilatory support.

Patients who have shown hypersensitivity to loratadine and pseudoephedrine or idiosyncrasy to their components including the metabolite descarboethoxy-loratadine, to adrenergic agents or to other drugs of similar chemical structure.
Patients receiving monoamine oxidase (MAO) inhibitor therapy or within 14 days of discontinuing such treatment and in patients with narrow-angle glaucoma, urinary retention, hypertension, severe coronary artery disease and hyperthyroidism.

Sympathomimetic agents should be used with caution in patients with stenosing peptic ulcer, pyloroduodenal obstruction, prostatic hypertrophy or bladder neck obstruction, cardiovascular disease, increased intraocular pressure or diabetes mellitus.
Sympathomimetic agents should be used with caution in patients receiving digitalis.
Sympathomimetic agents may cause central nervous system (CNS) stimulation, excitability, convulsions and/or cardiovascular collapse with accompanying hypotension.
Acute generalized exanthematous pustulosis (AGEP), a form of severe skin reaction, may occur with pseudoephedrine containing products in isolated cases. If signs and symptoms such as the sudden occurrence of small (generalized) pustules, erythema, or fever are observed, patients should discontinue using the drug.
Pseudoephedrine, like other CNS stimulants, has been abused. At high doses, patients commonly experience mood elevation, decreased appetite and a sense of increased energy, physical strength, mental capacity and alertness. Anxiety, irritability, and loquacity also have been reported. With continued use, tolerance develops; the user increases the dose and ultimately toxicity occurs. Depression may follow rapid withdrawal.
Patients with severe liver impairment should be administered a lower initial dose because they may have reduced clearance of loratadine, an initial dose of one tablet daily is recommended.
Dependence liability: there are no data available to indicate that abuse or dependency occurs with loratadine.
Because of the lack of experience with long-term use of this drug, its use should be limited to three months unless recommended by a physician.
Use in elderly: In patients 60 years or older, sympathomimetic agents may cause confusion, hallucinations, convulsions, CNS depression and death. Consequently, caution should be exercised when administering a repeat action formulation to this patient group.
Use in children: Safety and efficacy in children younger than 12 years of age have not yet been established.

Pregnancy: Caution: Safe use of this product in pregnancy has not been established. The use of FREENOS SR during pregnancy is therefore not recommended.
Lactation: Loratadine and its active metabolite are eliminated in the breast milk of lactating women with milk concentrations being similar to plasma concentrations. Through 48 hours after dosing, only 0.029% of the loratadine dose is eliminated in the milk as unchanged loratadine and its active metabolite, descarboethoxy-loratadine. Pseudoephedrine has been reported to be excreted into breast milk of lactating women. The use of FREENOS SR in nursing mothers is therefore not recommended.

Frequently reported adverse reactions included dizziness, dry mouth, fatigue, headache, insomnia, nervousness and sedation.
Rare adverse reactions in decreasing order of frequency included nausea, abdominal distress, anorexia, thirst, tachycardia, pharyngitis, rhinitis, acne, pruritus, rash, urticaria, arthralgia, confusion, dysphonia, hyperkinesia, hypoesthesia, decreased libido, paresthesia, tremor, vertigo, flushing, postural hypotension, increased sweating, eye disorders, earache, tinnitus, taste abnormality, agitation, apathy, depression, euphoria, paroniria, increased appetite, change in bowel habits, dyspepsia, eructation, hemorrhoids, tongue discoloration, tongue disorder, vomiting, transient abnormal hepatic function, dehydration, increased weight, hypertension, palpitation, migraine, bronchospasm, coughing, dyspnea, epistaxis, nasal congestion, sneezing, nasal irritation, dysuria, micturition disorder, nocturia, polyuria, urinary retention, asthenia, back pain, leg cramps, malaise and rigors.
As with other sympathomimetic amines, CNS stimulation, muscular weakness, tightness in the chest and syncope may also be encountered.
Alopecia, anaphylaxis (including angioedema), abnormal hepatic function, dizziness, palpitations and tachycardia have been reported rarely during the marketing of loratadine. Very rare adverse events include convulsions or seizures have been reported during the postmarketing of loratadine.

When administered concomitantly with alcohol, loratadine has no potentiating effect as measured by psychomotor performance studies.
When sympathomimetic agents are given to patients receiving MAO inhibitors, hypertensive reactions, including hypertensive crises, may occur.
The antihypertensive effects of methyldopa, mecamylamine, reserpine and veratrum alkaloids may be reduced by sympathomimetic agents.
Beta-adrenergic blocking agents may also interact with sympathomimetic agents.
Antacids increase the rate of pseudoephedrine absorption; kaolin decreases it.
Increased ectopic pacemaker activity can occur when pseudoephedrine is used concomitantly with digitalis.
The antibacterial agent, furazolidone, is known to cause a dose-related inhibition of MAO. Although there are no reports of a hypertensive crisis caused by the concurrent administration of pseudoephedrine and furazolidone, they should not be taken together.
Care should be taken in the administration of FREENOS SR concomitantly with other sympathomimetic amines because the combined effects on the cardiovascular system may be harmful to the patient.
Increases in plasma concentrations of loratadine have been reported after concomitant use with ketoconazole, erythromycin or cimetidine, but without clinically significant changes (including electrocardiographic).
Other drugs known to inhibit hepatic metabolism should be coadministered with caution.
Loratadine should be discontinued approximately 48 hours prior to skin testing procedures since antihistamines may prevent or diminish otherwise positive reactions to dermal reactivity indicators.
The in vitro addition of pseudoephedrine to sera containing the cardiac isoenzyme MB of serum creatine phosphokinase progressively inhibits the activity of the enzyme. The inhibition becomes complete over six hours.

Store at temperatures below 30°C.

Cough & Cold Preparations

R01BA02 - pseudoephedrine ; Belongs to the class of systemic sympathomimetic preparations used as nasal decongestants.
R06AX13 - loratadine ; Belongs to the class of other antihistamines for systemic use.

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