Analgesics
Tramadol Hydrochloride 50 mg
20Coated Tablets
T103
203/2014
21/8/2014
Excipients | Hypromellose , Magnesium stearate , Microcrystalline cellulose , Polyethylene glycol , Polysorbate 80 , Corn starch , Pregelatinized corn starch , Carnauba wax , Sodium starch glycolate , Titanium dioxide , Lactose . |
Mechanism Of Action | Tramadol Hydrochloride is a centrally acting synthetic analgesic compound. It is a non-selective pure agonist at mu, delta and kappa opioid receptors with a higher affinity for the mu receptor. Other mechanisms which may contribute to its analgesic effect are inhibition of neuronal reuptake of noradrenaline (norepinephrine) and enhancement of serotonin release. tramadol does not show respiratory depression when given within the analgesic dosage interval. The gastrointestinal motility is not affected. |
INDICATIONS | Tramadol is indicated for the treatment of moderate to severe pain. |
CONTRAINDICATIONS | • Hypersensitivity to the active substance or any of the other ingredients in the preparation. • Acute intoxication with central nervous system depressants (alcohol, hypnotics, centrally acting analgesics, opioids, psychotropic drugs). • Patients receiving monoamine oxidase inhibitors or within two weeks of their withdrawal. • Severe hepatic impairment. • Severely impaired kidney function (creatinine clearance less than 10ml/min). • Severe respiratory impairment. • Epilepsynot controlled by adequate treatment. • Tramadol must not be administered during breastfeeding if long term treatment, i.e more than 2 to 3 days, is necessary. • For use in narcotic withdrawal treatment |
Side EFFECTS | cardiovascular regulation (palpitation, tachycardia, postural hypotension or cardiovascular collapse),dizziness , headache, somnolence, nausea ,vomiting, constipation, dry mouth,retching; gastrointestinal irritation (a feeling of pressure in the stomach, bloating),diarrhea , sweating,dermal reactions (e.g. pruritus, rash, urticaria), fatigue. |
WARNINGS | Care should be taken and the risk/benefit of treatment determined prior to administration of tramadol in thefollowing situations: • Withdrawal symptoms: At therapeutic doses tramadol has the potential to cause withdrawal symptoms. • Drug dependence and abuse: Reports of these are rare and less frequent than withdrawal reactions. The clinical need for analgesic treatment should be reviewed regularly. Tramadol has a low dependence potential. On long-term use tolerance, psychic and physical dependence may develop. In patients with a tendency to drug abuse or dependence, Treatment should only be for short periods and under medical supervision. • Opioid-dependent patients: Tramadol is not suitable as a substitute in these patients and cannot suppress morphine withdrawal symptoms. • In patients sensitive to opiates the product should only be used with caution. • Tramadol should be used with caution in patients with head injury, increased intracranial pressure, impairment of hepatic (metabolism of tramadol and active metabolite is reduced) and renal (decreased rate and extent of excretion of tramadol and the active metabolite) function, decreased level of consciousness and in patients prone to convulsive disorder or in shock. • Patients prone to convulsive disorders. Convulsions have been reported at therapeutic doses and the risk may be increased at doses exceeding the usual upper daily dose limit. Patients with a history of epilepsy or those susceptible to seizures should only be treated with tramadol if there are compelling clinical reasons. The risk of convulsions may increase in patients taking tramadol and concomitant medication that lowers the seizure threshold . • Care should be taken when treating patients with respiratory depression, or if concomitant CNS depressant drugs are being administered ,or if the recommended dosage is significantly exceeded as the possibility of respiratory depression cannot be excluded in these situations. • The concomitant use of carbamazepine or concomitant intake of alcohol with tramadol is not recommended . • As there have been fatal cases of unintended overdose with tramadol associated with the use of psych-active medicines or substances including alcohol, tramadol should be prescribed with care in alcoholics and users of other psycho-active drugs. • After long term treatment (> 3 months) of analgesics with use every second day or more frequently, headache may develop or aggravate. Headache caused by overuse of analgesics (MOH - medication-overuse headache) should not be treated by increasing the dose. In such cases the use of analgesics should be discontinued in consultation with a doctor. |
DRUG INTERACTIONS | • Tramadol should not be combined with MAO inhibitors. Concomitant administration of Tramadol with other centrally depressant medicinal products including alcohol maypotentiate the CNS effects . • The results of pharmacokinetic studies have so far shown that on the concomitant or previous administration of cimetidine (enzyme inhibitor) clinically relevant interactions are unlikely to occur. Simultaneous or previous administration of carbamazepine (enzyme inducer) may reduce the analgesic effect and shorten the duration of action. • The combination with mixed agonist/antagonists (e.g. buprenorphine, nalbuphine, pentazocine) and tramadol is not advisable, because the analgesic effect of a pure agonist may be theoretically reduced in such circumstances. • Tramadol can induce convulsions and increase the potential for selective serotonin re-uptake inhibitors (SSRIs). serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic anti-depressants, anti-psychotics and other seizure threshold lowering medicinal products (such as bupropion, mirtazapine, tetrahydrocannabinol) to cause convulsions. • Concomitant therapeutic use of tramadol and serotonergic drugs, such as selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), MAO inhibitors, tricyclic antidepressants and mirtazapine may cause serotonin toxicity. Signs of serotonin syndrome may be for example confusion, agitation, fever, sweating, ataxia, hyperreflexia, myoclonus and diarrhoea. • Withdrawal of the serotoninergic medicinal products usually brings about a rapid improvement. Treatment depends on the nature and severity of the symptoms. • Caution should be exercised during concomitant treatment with tramadol and coumarin derivatives (e.g. warfarin) due to reports of increased INR with major bleeding and ecchymoses in somepatients. • Other active substances known to inhibit CYP3A4, such as ketoconazole and erythromycin, might inhibit the metabolism of tramadol. |
Pregnancy And lactations | Tramadol crosses the placenta. There is inadequate evidenceavailable on the safety of tramadol in human pregnancy. Therefore tramadol should not be used in pregnant women. During lactation about 0.1 % of the maternal dose is secreted into the milk. Tramadol is not recommended during breast-feeding. After a single administration of tramadol it is not usually necessary to interrupt breast-feeding. |
Dosage And Administration | The dose should be adjusted to the intensity of the pain and the sensitivity of the individual patient. The lowest effective dose for analgesia should generally be selected. Adults and children over 12 years: Acute pain: Adults and children over age 12 years: 50-100mg 3-4 times daily. Patients with low weight should use 0.7mg/kg bodyweight. Duration of therapy depends upon clinical need. Chronic pain: An initial dose of 50mg or 100mg is followed by doses of 50mg or 100mg, every 4 to 6 hours, according to pain severity. A total daily dose of 400mg should not be exceeded. Older people, A dose adjustment is not usually necessary in patients up to 75 years without clinically manifest hepatic or renal insufficiency. In elderly patients over 75 years elimination may be prolonged. Therefore, if necessary the dosage interval is to be extended according to the patient's requirements. Patients with renal impairment/renal dialysis: The elimination of tramadol may be prolonged in these patients. The usual initial dosage should be used. In these patients prolongation of the dosage intervals should be carefully considered according to the patient's requirements. For patients with creatinine clearance <30ml/min, the dosage interval should be increased to 12 hours. Tramadol is not recommended in patients with severe renal impairment (creatinine clearance <10ml/min). Patients with hepatic impairment The elimination of tramadol may be prolonged. The usual dosage should be divided in 2, or the dosage interval should be extended to 12 hours. In these patients prolongation of the dosage intervals should be carefully considered according to the patient's requirements. In severe hepatic impairment, the product is contraindicated. Pediatric population: Children under 12 years: Not recommended. |
OVERDOSE | Symptoms of overdosage are typical of other opioid analgesics and include miosis, vomiting, cardiovascular collapse, sedation and coma, seizures and respiratory depression. Supportive measures such as maintaining the patency of the airway and maintaining cardiovascular function should be instituted; naloxone should be used to reverse respiratory depression; fits can be controlled with diazepam. Gastrointestinal decontamination with activated charcoal or by gastric lavage is only recommended within 2 hours after tramadol intake. Tramadol is minimally eliminated by haemodialysis and haemofiltration. Therefore treatment of acute intoxication with tramadol by haemodialysis or haemofiltration is not recommended. |
Storage Conditions | Store at room temperature between 20 – 25 ° c Keep out of reach of children Prescription only medicine |