Phil Pharmawealth/Karnataka Tramadol Hydrochloride

Tramadol hydrochloride.

Each ml contains Tramadol Hydrochloride 50 mg.

Pharmacology: Tramadol is an effective pain reliever (analgesic). Its mode of action resembles that of narcotics, but ii has significantly less potential for abuse and addiction than the narcotics. Tramadol is as effective as narcotics in relieving pain but does not depress respiration. a side effects of most narcotics. Tramadol is not a nonsteroidal anti-inflammatory drug (NSAID) and does not have the increased risk of stomach ulceration and internal bleeding that can occur with the use of NSAIDs.
Pharmacokinetics: Distribution: The volume of distribution of Tramadol is 2.6 and 2.9 liters/kg in male and female subjects respectively following a 100 mg intravenous dose. The binding of Tramadol to human plasma protein is approximately 20% and binding also appears to be independent of concentration up to 10 mg/ml. Saturation of plasma protein binding occurs only at concentrations outside the clinically relevant range.
Although not confirmed in humans. Tramadol has been shown in rats to cross the blood-brain barrier.
Metabolism: Approximately 30% of the dose is excreted in the urine as unchanged drug. whereas 60% of the dose is excreted as metabolites. The remainder is excreted either as unidentified or an unextractable metabolites. The major metabolic pathways appear to be N-and O-demethylation and glucuronidation or sulfation in the liver. Only the one metabolite (mono-O-desmethyltramadol denoted M1) is pharmacologically active. Production of M 1 is dependent on the CYP2D6 isoenzyme of cytochrome P-450.
Elimination: The mean terminal plasma elimination half-lives of racemic Tramadol and racemic M1 are 6.3+1.4 and 7.4+1.4 hours respectively.
The plasma elimination half-life of racemic Tramadol increases from approximately six hours to seven hours upon multiple dosing.
Special Populations: Renal: Impaired renal function results in a decreased rate and extent of excretion of Tramadol and its active metabolite M1. In patients with creatinine clearances of less than 30 mL/min, adjustment of the dosing regimens is recommended (see Dosage & Administration). The total amount of Tramadol and M1 removed during dialysis period is less than 7% of the administered dose.
Hepatic: Metabolism of Tramadol and M1 is reduced in patients with advanced cirrhosis of the liver. resulting in a both larger area under the concentration lime curve for Tramadol and longer Tramadol and M1 elimination half-lives (13 hours for Tramadol and 19 hours for M1). In cirrhotic patients, adjustment of the dosing regimen is recommended. Healthy elderly subjects aged 65 to 75 years have plasma Tramadol concentrations and elimination half-lives comparable to those observed in healthy subjects less than 65 years of age. In subjects over 75 years, maximum serum concentration are slightly elevated (208 vs. 162 mg/ml.) and the elimination half-life is slightly prolonged (7 vs. 6hours) compared to subjects 65 to 75 years of age. Adjustment of the daily dose is recommended for patients older than 75 years. The absolute bioavailability of Tramadol is 73% in males and 79% in females. The plasma clearance is 6.4 mL/min/kg in males and 5. 7 mL/min/kg in females following a 100 mg IV dose of Tramadol.

Opioid analgesics are mainly used for the relief of moderate to severe pain. They are also used as anesthesia for premedication, induction, or maintenance. In balanced anesthesia, they are used in conjunction with an anesthetic gas and muscle relaxant. When used with a compound such as droperidol, they can produce a state of mild sedation with analgesia called neuroleptanalgesia. Morphine is generally the standard against which other opioids are compared and is considered by many to be the analgesic of choice for severe pain associated with terminal illness. Opioids with a quicker onset and shorter duration of action like alfentanil are preferred for use in anesthesia.
Moderate to severe acute or chronic pain and in pain measure & surgery. Arthralgia, musculoskeletal pain, colics, lower back pain, pain associated with fractures and dislocations, confusion, and osteoarthritis indicated for the management of moderate to moderately severe pain.

Tramadol hydrochloride is an opioid analgesic.
Usual doses are 5010 100 mg by injection.
Total daily dosage should not exceed 400 mg.
For the treatment painful conditions, Tramadol hydrochloride 50 mg to 100 mg can be administered as needed for relief every four to six hours, not to exceed 400 mg per day. For moderate pain, Tramadol 50 mg may be adequate as the initial dose, and for severe pain Tramadol 100 mg is usually more effective as the initial dose.
Individualization of Dose: Available data do not suggest that a dosage adjustment is necessary in elderly patients 65 to 75 years of age unless they also have renal or hepatic impairment. For elderly patients over 75 years old not more than 300 mg/day in divided doses as above is recommended. In all patients with creatinine clearance less than 30 mL/min, ii is recommended that the dosing interval of Tramadol be increased to12 hours with a maximum daily dose of 200 mg. Since only 7% of an administered dose is removed by haemodialysis, dialysis patients can receive their regular dose on the day of dialysis. The recommended dose for patients with cirrhosis is50 mg every 12 hours. Patients receiving chronic carbamazepine doses up to 800 mg daily required up to twice the recommended dose of Tramadol.

The euphoric activity and other similar compounds has led to their abuse. Larger doses produce respiratory depression and hypotension, with circulatory failure and deepening coma. Convulsions may occur, especially in infants and children. Rhabdomyolysis progressing to renal failure has been reported in overdosage.
Death may occur from respiratory failure. Toxic doses vary considerably with the individual and regular users may tolerate large doses. The triad of coma, pin point pupils, and respiratory depression is considered indicative of overdosage; dilatation of the pupils occurs as hypoxia develops. Pulmonary oedema after overdosage is a common cause of fatalities among opioid addicts.
Should not be administrated to patients who have previously demonstrated hypersensitivity to Tramadol or in cases of acute intoxication with alcohol, hypnotics, centrally acting analgesics, opioids or psychotropic drugs.
Generally contraindicated in respiratory depression, especially in the presence of cyanosis and excessive bronchial secretion.

Delayed respiratory depression may occur following an epidural or intrathecal administration. It should be used with extreme caution in patients with decreased respiratory reserve and should not be given during attack of bronchial asthma or in heart failure secondary to chronic lung disease. Opioid analgesics should be used with caution in patients with myasthenia gravis.
Special cautions in use: Few cases of overdoses with Tramadol have been reported. Estimates of ingested doses in foreign fatalities have been in the range of 3 to 5 g. A 3 g intentional overdose in a patient in the clinical studies produced emesis and no sequelae. The lowest dose reported to be associated with fatality was possibly between 500 and1000 mg in a 40 kg women, but details of the case are not completely known. Serious potential consequences of overdosage are respiratory depression and seizure. Nalaxone will reverse some, but not all symptoms caused by overdosage with Tramadol so general supportive treatment is recommended. Primary attention should be given to the assurance of adequate respiratory exchange. Haemodialysis is not expected to be helpful because ii removes only a small percentage of the administered dose. Convulsions occurring in mice following the administration of toxic doses of Tramadol could be suppressed with barbiturates or benzodiazepines, but were increased with naloxone. Naloxone did not change the lethality of an overdose in mice.

In normal doses, the most common side-effects of opioid analgesics are nausea, vomiting, constipation, drowsiness, and confusion; tolerance generally develops with long-term use, but not to constipation. Micturition may be difficult and there may be ureteric or biliary spasm; there is also an anti diuretic effect. Dry mouth, sweating, facial flushing, vertigo, bradycardia, palpitations, orthostatic hypotension, hypothermia, restlessness, changes of mood, hallucinations, and miosis may also occur. These effects tend to occur more commonly in ambulant patients than n those at rest in bed and in those without severe pain. Raised intracranial pressure occurs in some patients.
Muscle rigidity has been reported following high doses.
Tramadol Hydrochloride was administrated to 550 patients during the double-blind or open-label extension periods in US studies of chronic non malignous pain. The most frequently reported events were in the central nervous system and gastrointestinal system.
Body as a whole: Malaise, Allergic reaction, Accidental injury, weight loss, anaphylaxis, Suicide tendency.
Cardiovascular: Vasodilation, Syncope, Orthostatic Hypotension, Tachycardia, Abnormal ECG, Hypertension, Hypotension, Myocardial ischemia, palpitations.
Central nervous system: Anxiety, confusion, coordination disturbance, Euphoria, Nervousness, Sleep Disorder, Seizure, Migraine, speech disorders.
Gastrointestinal: Abdominal pain, Anorexia, Flatulence, Gastrointestinal bleeding, Hepatitis, Stomatitis.
Musculoskeletal: Hypertonia.
Skin: Rash, Urticaria, Vesicles, Steven-Johnson Syndrome/Toxic epidermal necrolysis.
Special Senses: Visual Disturbances, Dysgeusia.
Urogenital: Urinary retention, Urinary frequency, Menopausal symptoms, Dysuria, Menstrual disorder.
Respiratory: Dyspnea.

Store at temperatures not exceeding 30°C.

Analgesics (Opioid) / Supportive Care Therapy

N02AX02 - tramadol ; Belongs to the class of other opioids. Used to relieve pain.

Rx