ANALAB CAPSULES: Each capsule contains Tramadol Hydrochloride 50.00 mg.
Pharmacodynamics: Tramadol hydrochloride is a synthetic, centrally active analgesic. The drug (and its active M1 metabolite) acts as an opiate agonist, apparently by selective activity at the μ-receptor. In addition to its opiate agonist activity, tramadol hydrochloride inhibits reuptake of certain monoamines (norepinephrine, serotonin), which appears to contributes to the drug's analgesic effect.
Pharmacokinetics: Absorption: The duration of effects of tramadol hydrochloride and its active metabolite, O-desmethyltramadol (M1), is 2 and 3 hours respectively.
Distribution: Tramadol hydrochloride is 20% bound to plasma proteins. Its volume of distribution is 2.6 - 2.9 L/kg.
Metabolism: Tramadol hydrochloride is metabolized in liver via CYP2D6 and CYP3A4. It is metabolized in the liver to O-desmethyltramadol (M1) as an active metabolite via CYP2D6.
Elimination: Tramadol hydrochloride is eliminated as parent drug and metabolites through the urines in 6.3 and 7.4 hours respectively.
ANALAB CAPSULES is administered orally. Since food does not affect substantially the rate or extent of absorption of tramadol hydrochloride administered alone, it can be administered without regard to meal.
Patients 17 years of age and older with moderate to moderately severe chronic pain not requiring rapid onset of analgesic effect may initially receive ANALAB CAPSULES using a dosage titration regimen;
the recommended initial dosage is 25 mg daily in the morning, increased by increments of 25 mg every 3 days as separate doses up to a dosage of 25 mg 4 times daily. Thereafter, daily dosage may be
increased as tolerated by 50 mg every 3 days, up to 50 mg 4 times daily. Following titration, 50 - 100 mg may be administered every 4 - 6 hours as needed.
Patients 17 years of age and older requiring rapid of analgesia, and in whom the benefit of rapid onset of analgesia outweighs the risk of drug discontinuance secondary to adverse effects associated with higher initial dosage, may receive a ANALAB CAPSULES dosage of 50 - 100 mg every 4 - 6 hours. Do not exceed 400 mg/day.
Dosage in Renal Function Impairment: Impaired renal function results in a decreased rate and extent of excretion of tramadol hydrochloride and its active metabolite, M1. In patients with a creatinine clearance (CrCl) less than 30 mL/min, adjustment of the dosing regimen is recommended. Patients may receive an oral ANALAB CAPSULES dosage of 50 - 100 mg and increase the dosing interval to 12 hours, with a maximum daily dose of 200 mg. Because hemodialysis only removes 7% of an administered dose, dialysis patients can receive their regular dose on the day of dialysis.
Dosage in Hepatic Function Impairment: Metabolism of tramadol hydrochloride and M1 is reduced in patients with advanced cirrhosis of the liver, resulting in both a larger AUC for tramadol hydrochloride and longer tramadol hydrochloride and M1 elimination half-lives (13 hours for tramadol hydrochloride and 19 hours for M1). In cirrhotic patients, adjustment of the dosing regimen is recommended. The recommended dosage for adults with hepatic cirrhosis is 50 mg every 12 hours.
Manifestation: In severe overdosage, mainly by the IV route, apnea, circulatory collapse, convulsions, cardiac arrest, pulmonary edema, and death may occur. The less severely poisoned patient often has a triad of CNS depression, miosis, and respiratory depression. Serious overdosage is characterized by respiratory depression, extreme somnolence progressing to stupor or coma, constricted pupils, skeletal muscle flaccidity, and cold and clammy skin. Hypotension, bradycardia, hypothermia, pulmonary edema, pneumonia, or shock occurs in 40% or less of patients.
Treatment: Administer a narcotic antagonist (e.g. naloxone). The duration of respiratory depression following overdosage may be longer than the duration of the opioid antagonist, so repeated administration of the antagonist may be necessary; keep the patient under surveillance. Do not give an antagonist in the absence of clinically significant respiratory or cardiovascular depression. Naloxone is the antagonist of choice. If necessary to give an antagonist to an opioids-tolerant patient, administer with extreme caution and by titration with smaller than usual doses.
When treating tramadol hydrochloride overdosage, primary attention should be given to maintaining adequate ventilation along with general supportive treatment. Although an opiate antagonist (e.g., naloxone) will reverse some, but not all, manifestations of tramadol hydrochloride overdosage, the risk of seizures also is increased with naloxone administration. Hemodialysis is unlikely to be helpful in a tramadol hydrochloride overdosage because it removes less than 7% of the administered dose in a 4 hours dialysis period.
In cases of oral overdose, evacuate the stomach by emesis or gastric lavage if treatment can be instituted within 2 hours following ingestion. Do not induce emesis. Absorption of drugs from the GI tract may be decreased by giving activated charcoal which, in many cases, is more effective than lavage. Observe the patient for a rise in temperature or pulmonary complications that may require antibiotic therapy.
Hypersensitivity to the drug or known intolerance to other opioids or any components of the products, acute intoxication with alcohol, hypnotics, narcotics, centrally acting analgesics, opioids, or psychotropic drugs.
Seizures: Seizure have occurred during tramadol hydrochloride therapy with recommended dosages. Seizure can occur following the first dose. Naloxone administration in patients with tramadol hydrochloride overdose also may increase the risk of seizure.
Sensitivity reactions: Serious and rarely fatal anaphylactoid reactions have been reported in patients receiving tramadol hydrochloride. These reactions often occur following the first dose. Other reported hypersensitivity reactions include pruritus, hives, bronchospasm, urticaria, angioedema, toxic epidermal necrolysis, and Stevens-Johnson syndrome. Patients with a history of anaphylactoid reactions to codeine and other opioids may be at increased risk and therefore should not receive tramadol hydrochloride.
Respiratory depression: Tramadol hydrochloride should be administered with caution to patients at risk for respiratory depression. Respiratory depression may result when large doses of tramadol hydrochloride are administered with anesthetic medications or alcohol, and should be treated as a tramadol hydrochloride overdose.
Increased intracranial pressure or head injury: Tramadol hydrochloride should be used with caution in patients with increased intracranial pressure or head injury, since the respiratory depressant effects of opiate agonists include carbon dioxide retention and secondary elevation of cerebrospinal fluid pressure, and such effects may be markedly exaggerated in these patients. Also, pupillary changes (miosis) from tramadol hydrochloride may obscure the existence, extent, or course of intracranial pathology. Clinicians also should maintain a high index of suspicion for adverse drug reaction when evaluating altered mental status in these patients if they are receiving tramadol hydrochloride.
Withdrawal: Withdrawal symptoms may occur if tramadol hydrochloride is discontinued abruptly. Symptoms may include anxiety, sweating, insomnia, rigors, pain, nausea, tremors, diarrhea, upper respiratory symptoms, piloerection, and rarely hallucinations. Clinical experience suggests that withdrawal symptoms may be relieved by tapering the dosage.
Acute abdominal conditions: Tramadol hydrochloride administration also may complicate the clinical assessment of patients with acute abdominal conditions.
Renal and hepatic impairment: Impaired renal function results in a decreased rate and extent of excretion of tramadol hydrochloride and its active metabolite, M1. Tramadol hydrochloride and M1 metabolism are reduced in patients with advanced hepatic cirrhosis; therefore, dosage reduction also is recommended in these patients
Category C.
Use in pregnancy: Although there are no adequate and controlled studies to date in humans, tramadol hydrochloride has been shown to be embryotoxic and fetotoxic in mice, rats, and rabbits at maternally toxic doses. Safe use of tramadol hydrochloride in pregnancy has not been established. Tramadol hydrochloride should be used during pregnancy only if the potential benefits justify the possible risks to the fetus. Tramadol hydrochloride also should not be used in pregnant women prior to or during labor unless the potential benefits outweigh the risks.
Use in nursing mother: Tramadol hydrochloride is distributed into milk. Because the safety of tramadol hydrochloride in infants and neonates has not been evaluated, the drug is not recommended for obstetrical preoperative medication or for post-delivery analgesia in nursing women.
Nervous system: Dizziness, vertigo, headache, somnolence, nervousness, anxiety, agitation, tremor, spasticity, euphoria, emotional lability, hallucinations, asthenia, confusion, amnesia, depression, paresthesia, seizure, hypertonia.
GI: Constipation, nausea, vomiting, dyspepsia, dry mouth, diarrhea, abdominal pain, anorexia, flatulence, weight loss.
Sensitivity reactions: Pruritus, rash, urticaria, Stevens-Johnson syndrome, toxic epidermal necrolysis.
Cardiovascular: Vasodilation, orthostatic hypotension, syncope, tachycardia, hypotension.
Genitourinary and renal: Menopausal symptoms, urinary frequency, dysuria, menstrual disorder, increased serum creatinine concentrations, proteinuria.
Others: Malaise, visual disturbance, dyspnea, dysgeusia, respiratory depression.
CYP2D6 inhibitors: Tramadol hydrochloride is extensively metabolized by a number of pathways including CYP2D6 and CYP3A4. The formation of M1 (active metabolite) is dependent upon CYP2D6 and as such is subject to inhibition, which may affect the therapeutic response. Therefore, coadministration of tramadol hydrochloride with a CYP2D6 inhibitor (eg, fluoxetine, paroxetine, quinidine, amitriptyline) may increase concentrations of tramadol hydrochloride and reduce concentrations of M1.
CYP3A4 inhibitors: Coadministration of tramadol hydrochloride with CYP3A4 inhibitors (eg, macrolide antibiotics,
azole antifungals, protease inhibitors) may decrease tramadol hydrochloride clearance. Coadministration may produce increased tramadol hydrochloride concentrations. Carefully monitor patients receiving potent CYP3A4 inhibitors (eg, ritonavir, ketoconazole, clarithromycin) for an extended period of time and adjust the dosage as need.
CYP3A4 inducers: CYP3A4 inducers (eg, rifampin, carbamazepine, phenytoin) may produce increased clearance of tramadol hydrochloride, use with caution.
Carbamazepine: Because carbamazepine increases tramadol hydrochloride metabolism and because of the seizure risk associated with tramadol hydrochloride, concomitant administration is not recommended.
SSRIs: SSRIs (Nefazodone, Venlafaxine, fluvoxamine) may inhibit tramadol hydrochloride metabolism and therefore increase toxicity. Use with caution. The serotonergic effects of tramadol hydrochloride and serotonin reuptake effects of tramadol hydrochloride and serotonin reuptake nhibitors may be additive, increasing the risk for adverse effects such as seizures and serotonin syndrome.
Warfarin: The oral anticoagulant effect of warfarin may be increased. Monitor coagulation tests and adjust dose as needed.
Store at temperature not exceeding 30°C.
N02AX02 - tramadol ; Belongs to the class of other opioids. Used to relieve pain.
Analab cap 50 mg
10 × 10's
Analab inj 50 mg/mL
10 × 1's
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