Trapadol

Light yellow coloured, elongated biconvex, break line on one side and plain on other side, film-coated tablets.
Each film-coated tablet contains: Tramadol HCl 37.5 mg, Paracetamol 325 mg.
Approved colours used.

Analgesic.
Pharmacology: Pharmacodynamics: Tramadol is an opioid analgesic that acts on the central nervous system. Tramadol is a pure non-selective agonist of the μ, δ, and κ opioid receptors with a higher affinity for the μ receptors. Other mechanisms which contribute to its analgesic effect are inhibition of neuronal reuptake of noradrenaline and enhancement of serotonin release. Tramadol has an antitussive effect. Unlike morphine, a broad range of analgesic doses of tramadol has no respiratory depressant effect. Similarly, the gastrointestinal motility is not modified. The cardiovascular effects are generally slight. The potency of tramadol is considered to be one-tenth to one-sixth that of morphine.
The precise mechanism of the analgesic properties of paracetamol is unknown and may involve central and peripheral effects.
Tramadol Hydrochloride/Paracetamol is positioned as a step II analgesic in the WHO pain ladder and should be utilised accordingly by the physician.
Pharmacokinetics: Paracetamol is readily absorbed from the gastrointestinal tract with peak plasma concentrations occurring about 10 to 60 minutes after oral doses. It is distributed into most body tissues. It crosses the placenta and present in breast milk. Plasma-protein binding is negligible at usual therapeutic concentrations but increases with increasing concentrations. The elimination half-life of paracetamol varies from about 1 to 3 hours.
Tramadol is readily absorbed after oral doses but is subject to some first-pass metabolism. Mean absolute bioavailability is about 70 to 75% after oral use and 100% after intramuscular injection. Plasma protein binding is about 20%. Tramadol is metabolised by N- and O-demethylation via the cytochrome P450 isoenzymes CYP3A4 and CYP2D6 and glucuronidation or sulfation in the liver. The metabolite O-desmethyltramadol is pharmacologically active. Tramadol is excreted mainly in the urine, predominantly as metabolites. Tramadol is widely distributed, crosses the placenta, and appears in small amounts in breast milk. The elimination half-life is about 6 hours.

It is indicated for the management of moderate to severe pain.

Adults and children over 16 years: 1 to 2 tablets every 4-6 hours as needed. It can be administered without regard to food or as prescribed by the physician.

Tramadol HCl + Paracetamol (Trapadol) is a fixed combination of active ingredients. In case of overdose, the symptoms may include the signs and symptoms of toxicity of tramadol or acetaminophen or both of these active ingredients.
Symptoms of overdose from tramadol: In principle, an intoxication with tramadol, symptoms similar to those of other centrally acting analgesics (opioids) are to be expected. These include in particular, miosis, vomiting, cardiovascular collapse, consciousness disorders up to coma, convulsions and respiratory depression up to respiratory arrest.
Symptoms of overdose from acetaminophen: An overdose is of particular concern in young children. Symptoms of acetaminophen overdosage in the first 24 hours are pallor, nausea, vomiting, anorexia and abdominal pain. Liver damage may become apparent 12 to 48 hours after ingestion. Abnormalities of glucose metabolism and metabolic acidosis may occur. In severe poisoning, hepatic failure may progress to encephalopathy, coma and death. Acute renal failure with acute tubular necrosis may develop even in the absence of severe liver damage. Cardiac arrhythmias and pancreatitis have been reported.
Liver damage is possible in adults who have taken 7.5-10 g or more of acetaminophen. It is considered that excess quantities of a toxic metabolite (usually adequately detoxified by glutathione when normal doses of acetaminophen are ingested), become irreversibly bound to liver tissue.
Emergency treatment: Transfer immediately to a specialised unit.
Maintain respiratory and circulatory functions.
Prior to starting treatment, a blood sample should be taken as soon as possible after overdose in order to measure the plasma concentration of acetaminophen and tramadol and in order to perform hepatic tests.
Perform hepatic tests at the start (of overdose) and repeat every 24 hours. An increase in hepatic enzymes (ASAT, ALAT) is usually observed, which normalizes after one or two weeks.
Empty the stomach by causing the patient to vomit (when the patient is conscious) by irritation or gastric lavage.
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.
Tramadol is minimally eliminated from the serum by haemodialysis or haemofiltration. Therefore, treatment of acute intoxication with Acetaminophen & Tramadol hydrochloride with haemodialysis or haemofiltration alone is not suitable for detoxification.
Irrespective of the reported quantity of acetaminophen ingested, the antidote for acetaminophen, NAC, should be administered orally or intravenously, as quickly as possible, if possible, within 8 hours following the overdose.

Hypersensitivity to the active substances or to any of the excipients of the medicinal product.
Acute intoxication with alcohol, hypnotic drugs, centrally-acting analgesics, opioids or psychotropic drugs.
Tramadol + Paracetamol should not be administered to patients who are receiving monoamine oxidase inhibitors or within two weeks of their withdrawal.
Severe hepatic impairment.
Epilepsy not controlled by treatment.

Product contains FD & C yellow #5 (Tartrazine) that may cause allergic type reactions (including bronchial asthma) in certain susceptible individuals.

Inappropriate use of this medicine has the potential to cause liver toxicity or severe liver damage. Do not exceed the stated dose. Do not take with any other drug containing paracetamol unless advised by a healthcare professional.

Pregnancy: Since Tramadol HCl + Paracetamol (Trapadol) is a fixed combination of active ingredients including tramadol, it should not be used during pregnancy.
Acetaminophen: Epidemiological studies in human pregnancy have shown no ill effects due to acetaminophen used in the recommended dosage, but patients should follow the advice of their doctor regarding its use.
Tramadol: There are no adequate data from the use of tramadol in pregnant women. Tramadol crosses the placental barrier and chronic use during pregnancy can cause withdrawal symptoms in the newborn baby. Therefore, it should not be used during pregnancy.
Tramadol administered before or during birth does not affect uterine contractility. In neonates, it may induce changes in respiratory rate which are not usually clinically relevant.
Lactation: Since Tramadol HCl + Paracetamol (Trapadol) is a fixed combination of active ingredients including tramadol, it should not be ingested during breast feeding.
Acetaminophen: Acetaminophen is excreted in breast milk but not in a clinically significant amount. Available published data on acetaminophen does not contraindicate it for breast feeding.
Tramadol: Tramadol and its metabolites are found in small amounts in human breast milk. An infant could ingest 0.1% of the dose given to the mother. Tramadol hydrochloride should not be administered during breast feeding.

Nausea, vomiting, constipation, drowsiness, hematological reactions including thrombocytopenia, leukopenia, respiratory depression and hypotension occasionally occurred.

The risk of paracetamol toxicity may be increased in patients receiving other potentially hepatotoxic drugs or drugs that induce liver microsomal enzymes. The absorption of paracetamol may be accelerated by drugs such as metoclopramide. Excretion may be affected and plasma concentrations altered when given with probenecid. Colestyramine reduces the absorption of paracetamol if given within 1 hour of paracetamol.

Store at temperatures not exceeding 30°C.

Analgesics (Opioid)

N02AJ13 - tramadol and paracetamol ; Belongs to the class of opioids in combination with other non-opioid analgesics. Used to relieve pain.

Rx