ACTION AND MECHANISM - Antitussive. Cloperastine is an antitussive structurally related to ethanolamine antihistamines. Its mechanism of action in cough is unknown, although a possible depression of the cough center has been suggested, accompanied by a bronchodilator and local anesthetic effect on the bronchi. It does not cause dependence or significant nervous system depression, unlike opioid antitussives. It has mild antihistamine activity. SENIORS No specific problems have been described in elderly patients that would require a dosage adjustment. However, elderly patients may be more sensitive to the anticholinergic effects of cloperastine and may also have underlying conditions that could be exacerbated by the drug, such as glaucoma or benign prostatic hyperplasia. PATIENT ADVICE - Avoid drinking alcohol during treatment. - Tell your doctor and/or pharmacist if symptoms continue or worsen after 7 days of treatment, as well as if they are accompanied by fever, severe headache or skin rashes. - Inform your doctor and/or pharmacist if you have conditions such as prostate enlargement, high blood pressure, other cardiovascular diseases, or glaucoma. - If you are going to undergo allergy diagnostic tests, stop taking cloperastine at least 3 days before the test. - Tell your doctor and/or pharmacist if you experience symptoms such as: * Dry mouth, constipation, drowsiness, insomnia or the onset of nightmares, as well as sudden loss of vision or eye pain. CONTRAINDICATIONS - Hypersensitivity to cloperastine, other antihistamines, or any other component of the medication. - Patients undergoing treatment with MAOIs. - Children < 2 years, pregnancy and breastfeeding. EFFECTS ON DRIVING Cloperastine does not appear to have significant effects on the ability to drive, although in rare cases it may cause drowsiness or dizziness. PREGNANCY Animal safety : cloperastine was not teratogenic in animals. Safety in humans : There are no adequate and well-controlled studies in humans. Manufacturers advise against its use during pregnancy. Effects on fertility : no specific studies have been conducted in humans. PHARMACOKINETICS Oral route: - Absorption: good and rapid oral absorption, with tmax 1-1.5 h. The effects appear within 20-30 min and last for 3-4 h. Effect of food : does not affect the absorption of cloperastine. - Distribution: no data available. - Metabolism: extensive hepatic metabolism. Enzyme inducing/inhibiting capacity : does not appear to have significant effects. - Excretion: in urine, in the form of metabolites. Elimination is complete within 24 hours. Pharmacokinetics in special situations : There are no specific pharmacokinetic data in children, the elderly, or patients with renal or hepatic impairment: INDICATIONS - Symptomatic treatment of dry and unproductive cough, such as irritative or nervous cough, in adults and children from 2 years of age. INTERACTIONS - Alcohol and sedatives (other H1 antihistamines, benzodiazepines, antipsychotics, opiates). Risk of increased sedation. - Anticholinergic drugs. The anticholinergic effects could be potentiated when combined with other drugs such as certain antihistamines, antiparkinsonian drugs, antipsychotics or antidepressants. - Expectorants and mucolytics. Inhibition of the cough reflex could lead to pulmonary obstruction in cases of increased volume or fluidity of bronchial secretions. LACTATION Animal safety : no data available. Safety in humans : It is unknown whether it is excreted in breast milk, and the potential consequences for the infant. Manufacturers advise against its use during breastfeeding. CHILDREN Cloperastine can be used in children from 2 years of age, adjusting the dose according to the childs age. However, it should be borne in mind that children may be more sensitive to anticholinergic effects. Its use is contraindicated in children under 2 years of age. GUIDELINES FOR PROPER ADMINISTRATION - Syrup, oral suspension: shake before use. POSOLOGY Flutox syrup, Sekisan : Doses are expressed in mg of cloperastine fendizoate. 3.45 mg of cloperastine fendizoate is equivalent to 2 mg of cloperastine hydrochloride. - Adults: 10 ml (approx. 35 mg), 3 times a day. - Children and adolescents < 18 years: * Adolescents > 12 years: 10 ml (approx. 35 mg), 3 times a day. * Children aged 7-12 years: 5 ml (approx. 17.5 mg), twice a day. * Children 5-6 years: 3 ml (approx. 10 mg), twice a day. * Children 2-4 years: 2 ml (approx. 7 mg), twice a day. * Children < 2 years: contraindicated. - Elderly: no specific dosage recommendations have been made. Duration of treatment : prolong treatment while the cough persists, and up to a maximum of 7 days, unless otherwise recommended by a doctor. Missed dose : Take the next dose at the usual time. Do not double the next dose. DOSAGE IN HEPATIC INSUFFICIENCY No specific dosage recommendations have been made. DOSAGE IN RENAL INSUFFICIENCY No specific dosage recommendations have been made. PRECAUTIONS - Anticholinergic effects. Cloperastine has anticholinergic effects, so it could aggravate conditions such as [CONSTIPATION], [INTESTINAL OBSTRUCTION] (including [INTESTINAL ATONY], [ILEUS], stenosing [PEPTIC ULCER]), [HIGH PRESSURE], [HEART FAILURE], [ISCHEMIC HEART DISEASE], [CARDIAC ARRHYTHMIA], conditions that lead to [URINARY RETENTION] such as [PROSTATIC HYPERPLASIA], [MYASTHENIA GRAVIS], [GLAUCOMA] or [HYPERTHYROIDISM], among others. In addition, a reduction in salivation may occur, with a risk of dental caries. - Persistent cough. Extreme caution is advised in patients with chronic cough, such as that associated with smoking, emphysema, or asthma, or in cases of productive cough, because by inhibiting the cough reflex, it could impair expectoration and increase airway resistance. Furthermore, due to anticholinergic effects, the volume of bronchial secretions could decrease, increasing their viscosity and worsening these conditions. You should see a doctor if the cough persists for more than a week, or if it is accompanied by a high fever, skin rashes, or persistent headache. - Skin tests for hypersensitivity to allergenic extracts. Due to their antihistamine effects, these extracts could produce false negatives in diagnostic tests. It is recommended to discontinue administration at least 72 hours before performing the test. PRECAUTIONS RELATING TO EXCIPIENTS - Because it contains methyl parahydroxybenzoate, it may cause allergic reactions (possibly delayed). ADVERSE REACTIONS Adverse reactions are described according to each frequency interval, being considered very common (>10%), common (1-10%), uncommon (0.1-1%), rare (0.01-0.1%), very rare (<0.01%) or of unknown frequency (cannot be estimated from the available data). - Digestive: infrequent [DRY MOUTH]. - Neurological/psychological: infrequent [DROWSY], [DYSTONIA], [TREMOR], [DIZZINESS]. - Respiratory: frequency unknown [EPISTAXIS]. - Dermatological: very rare [URTICARIA]. - Allergic reactions: very rare [ANAPHYLAXIS]. OVERDOSE Symptoms : Cloperastine poisoning may cause initial excitability, followed by CNS depression. An exacerbation of anticholinergic symptoms may also occur, although it is not a potent anticholinergic. Measures to be taken : - Antidote: Severe anticholinergic symptoms, if they occur, could be treated with physostigmine. However, severe poisoning does not appear likely. - General elimination measures: perform gastric lavage and administer activated charcoal if the poisoning is recent, the patient is conscious and the airway can be protected. - Monitoring: monitor electrolyte levels and blood pH. - Treatment: symptomatic. COMPOSITION CLOPERASTINE: 3.54 MILLIGRAMS - PHENDIZOATE SUCROSE (EXCIPIENT): 450 MILLIGRAMS METHYL PARAHYDROXYBENZOATE (E-218) (EXC): 1.22 MILLIGRAMS PROPYL PARAHYDROXYBENZOATE (E-216) (EXC: 0.18 MILLIGRAMS