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<Product Name> 7.5 Mg Tablets 2. QUALITATIVE AND SUMMARY OF PRODUCT CHARACTERISTICS 1. NAME OF THE MEDICINAL PRODUCT <Product name> 7.5 mg tablets 2. QUALITATIVE AND QUANTITATIVE COMPOSITION Each tablet contains 6,7 mg levomethadone as 7.5 mg levomethadone hydrochloride. For the full list of excipients, see section 6.1. 3. PHARMACEUTICAL FORM Tablet Formal comment Information on the size of the tablet should be added. White to off-white, oblong, uncoated tablet with break scores on both sides, with a length of approximately 12 mm and a width of approximately 5.5 mm. The tablet can be divided into equal doses. 4. CLINICAL PARTICULARS 4.1 Therapeutic indications Severe pain in adults. 4.2 Posology and method of administration Levomethadone must be titrated individually. In general, the lowest effective analgesic dose should be chosen. The following recommended doses should be used as guidance. In case of severe pain conditions (e.g. cancer pain) doses may vary. It is recommended that the patient should rest during levomethadone’s duration of action. Posology Adults For adults a single dose of 7.5 mg levomethadone hydrochloride is recommended. In certain cases the initial dose might be 2.5 mg levomethadone hydrochloride. In case of decreasing efficacy administration can be repeated after 4-6 hours. In order to avoid a cumulative effect generally the second and all following doses should be lower than the initial dose. For the total daily dose it is recommended not to exceed 4 to 6 times the single dose. For the treatment of chronic pain administration following a fixed dose schedule should be preferred. 1 Notes Levomethadone is roughly twice as effective as the methadone racemate. There are indications that levomethadone degradation is enhanced when the methadone racemate is administered, thereby possibly altering this ratio. This must be taken into account when dosing. Special populations Elderly patients Reduction of the dose is recommended in elderly patients. Patients with renal and/or hepatic impairment Reduction of the dose is recommended in patients with renal diseases or severe chronic liver diseases. Paediatric population The safety and efficacy of levomethadone in children and adolescents aged <18 years have not been established. Method of administration For oral use. The tablets should be taken with a sufficient amount of liquid (e.g. ½ glass of water). 4.3 Contraindications Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. During the first trimester of pregnancy levomethadone must not be used (see section 4.6). Treatment with MAO inhibitors or within two weeks after their discontinuation. Narcotic antagonists or other narcotic agonists/antagonists (e.g. pentazocine and buprenorphine) must not be used during treatment with levomethadone, except for treatment of overdose. 4.4 Special warnings and precautions for use Strict indication and particularly close medical surveillance are required in case of: presence of impaired consciousness concomitant use of other central nervous system and/or respiratory depressant medicinal products and substances conditions where depression of the respiratory centre must be avoided raised intracranial pressure hypotension in case of hypovolaemia prostatic hypertrophy with residual urine formation pancreatitis biliary tract disorders obstructive and inflammatory bowel disease phaeochromocytoma hypothyroidism moderate to severe impairment of the respiratory centre and respiratory function bradycardia treatment with classes I and III antiarrhythmics opioid dependence acute abdominal conditions: Treatment with levomethadone, in common with other μ-agonists, may hamper diagnosis or mask the clinical progression in patients with acute abdominal conditions. Therefore, patients with signs of acute abdomen during treatment should be monitored closely until an exact diagnosis has been established. infants, children and adolescents <18 years of age. 2 Lung and respiration Levomethadone should be used with caution in patients with: asthma chronic obstructive pulmonary disease cor pulmonale substantially impaired respiratory reserve pre-existing impairment of respiratory function hypoxia or hypercapnia Even at usual therapeutic doses, respiratory activity may be reduced in these patients, while simultaneously airway resistance may increase resulting in apnoea. In patients predisposed to such atopic phenomena, exacerbation of pre-existing asthma, skin eruptions and blood dyscrasias (eosinophilia) may occur. Intracranial pressure The respiratory-depressant effect of opioids and their capacity to raise the cerebrospinal fluid pressure may be enhanced clinically relevant in case of pre-existing raised intracranial pressure. In view of the efficacy profile of levomethadone as a μ-agonist, it should be used with extreme caution and only when deemed essential for the treatment of such patients. Potential for dependence Levomethadone has a primary dependence potential and may produce addiction. With prolonged use physical and psychological dependence as well as tolerance develops. When used as directed in patients with chronic pain the risk of developing physical or psychological dependence is markedly reduced or needs to be assessed in a differentiated manner. Upon abrupt discontinuation severe and sometimes life-threatening withdrawal symptoms are to be expected. There is a cross-tolerance to other opioids. Risk from concomitant use of sedative medicinal products such as benzodiazepines or related medicinal products: Concomitant use of <Product name> and sedative medicinal products such as benzodiazepines or related medicinal products may result in sedation, respiratory depression, coma and death. Because of these risks, concomitant prescribing with these sedative medicinal products should be reserved for patients for whom alternative treatment options are not possible. If a decision is made to prescribe <Product name> concomitantly with sedative medicinal products, the lowest effective dose should be used, and the duration of treatment should be as short as possible. The patients should be followed closely for signs and symptoms of respiratory depression and sedation. In this respect, it is strongly recommended to inform patients and their caregivers to be aware of these symptoms (see section 4.5). Cardiac diseases Levomethadone should be administered with special caution to patients with known or suspected prolonged QT interval or an electrolyte imbalance, especially hypokalaemia/cardiac arrhythmias. During treatment with μ-opioid receptor agonists prolongation of QT interval and subsequent polymorphic ventricular tachycardia (torsade de pointes) has to be expected. In principle, all patients must be asked about their cardiac medical history and about any unexplained syncope prior to initiation of therapy. The patient should be informed about the possibility of cardiac arrhythmias. Prior to initiation of therapy and after two weeks of treatment, an ECG must be taken to establish and quantify the effect of the substitution substance on the QT interval. Similarly, it is advisable to take an ECG before any dose increase, as well as a follow-up at least once a year. In the event of unexplained syncope, the possibility of a cardiac cause should be considered. If there is any change in co- medication, the possibility of interaction affecting the QT interval must be considered. 3 Adrenal insufficiency Opioids may cause reversible adrenal insufficiency requiring monitoring and glucocorticoid replacement therapy. Symptoms of adrenal insufficiency may include nausea, vomiting, loss of appetite, fatigue, weakness, dizziness, or low blood pressure. Hypoglycaemia Hypoglycaemia has been observed in the context of methadone (a racemic mixture of levomethadone and dextromethadone) overdose or dose escalation. Regular monitoring of blood sugar is recommended during dose escalation (see section 4.8 and section 4.9). Decreased Sex Hormones and increased prolactin Long-term use of opioids may be associated with decreased sex hormone levels and increased prolactin. Symptoms include decreased libido, impotence or amenorrhea. Doping test Athletes must be aware that this medicinal product may cause a positive reaction to ‘anti-doping’ tests. Use of levomethadone as doping agent may become a health hazard. <Product name> contains sodium This medicine contains less than 1 mmol sodium (23 mg) per tablet, that is to say essentially ‘sodium- free’. 4.5 Interaction with other medicinal products and other forms of interaction The effects of levomethadone can be influenced both by pharmacodynamic and pharmacokinetic interactions. Depending on the clinical picture, the dose of levomethadone and/or concomitant medicinal products will have to be adjusted in the event of interactions described in the following section. The following combinations are contraindicated (see section 4.3): Use of MAO inhibitors within the last 14 days prior to opioid administration (e.g. pethidine) can lead to life-threatening effects, with both depressant and excitatory symptoms on the central nervous system, respiration and on circulatory function. Such reactions cannot be excluded for levomethadone. Pentazocine and buprenorphine (except for treatment of levomethadone hydrochloride overdose). When co-administering levomethadone with other medicinal products or substances, the following interactions must be taken into consideration: With central nervous system and respiratory function depressant medicinal products and substances mutual
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