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Product Name
:
TRAMADOL-ELSaad
Chemical Name
:
Tramadol HCl
Therapeutic Category
:
Analgesic & Anesthetic
Pharmacologic Category
:
Analgesic, Opioid
Pharmaceutical Form
:
Ampoule
Composition
:
Tramadol HCl 100mg/2ml
Monitoring Parameters
Dosing
 
Dosing: Adult
Moderate pain : for adults and adolescents above 14 years of age receive 50 mg of Tramadol injection as a single dose. If there is no pain-relieving effect after 30-60 minutes, a further 50 mg can be administered. In severe pain a higher dose is necessary, 100 mg Tramadol injection are administered as a single dose.

For the treatment of severe pain : after operations, on demand pain relief may require even higher doses in the first few hours. In general, over 24 hours more than the normal daily doses of Tramadol injection are not necessary. Depending on the pain, the effect lasts for 4 to 8 hours. In general, 400 mg of Tramadol injection per day need not to be exceeded.
However, for the treatment of cancer pain much higher doses may be necessary.

Dosing: Pediatric
Dosage for children : Children aged 1 to 13 years receive 1-2 mg Tramadol injection per kg body weight as a single dose. In this case Tramadol injection is diluted in water for injection. As in the following table : Water for Injection Gives the following concentrations: 2 ml + 2 ml 25.0 mg / ml 2 ml + 4 ml 16.7 mg / ml 2 ml + 6 ml 12.5 mg / ml 2 ml + 8 ml 10.0 mg / ml 2 ml + 10 ml 8.3 mg / ml 2 ml + 12 ml 7.1 mg / ml 2 ml + 14 ml 6.3 mg / ml 2 ml + 16 ml 5.6 mg / ml 2 ml +18 ml 5.0 mg / ml Dose adjustment when the duration of action is prolonged : When kidney or liver function is impaired, it is not necessary to adjust the dose of Tramadol injection in acute pain conditions, because the preparation is only given once or occasionally. In chronic ( long –lasting ) pain, however, the intervals between doses should be extended on account of the risk of accumulation due to delayed excretion. Even if there is no recognizable restriction of liver or kidney function, excretion may be delayed in elderly patients ( over 75 years of age), and therefore the intervals between doses may have to be extended. Tramadol injection is administered intravenously, intramuscularly or subcutaneously ( on intravenous injection Tramadol injection is mostly injected into a surface blood vessel of the arm, on intramuscular injection into the buttocks and on subcutaneous injection under the skin). Intravenous injection is carried out slowly by injecting 50 mg Tramadol injection per minute. Tramadol injection must not be administered for longer than absolutely necessary . if long-term treatment is necessary, your doctor should check at regular short intervals as to whether and with what dose Tramadol injection should be continued if necessary, with breaks in treatment.
Use
 
Relief of moderate to moderately-severe pain
Adverse Reactions
 
>10%:
Cardiovascular: Flushing (8% to 16%)
Central nervous system: Dizziness (10% to 33%), headache (4% to 32%), somnolence (7% to 25%), insomnia (2% to 11%)
Dermatologic: Pruritus (3% to 12%)
Gastrointestinal: Constipation (9% to 46%), nausea (15% to 40%), vomiting (5% to 17%), dyspepsia (1% to 13%)
Neuromuscular & skeletal: Weakness (4% to 12%)
1% to 10%:
Cardiovascular: Postural hypotension (2% to 5%), chest pain (1% to <5%), hypertension (1% to <5%), peripheral edema (1% to <5%), vasodilation (1% to <5%)
Central nervous system: Agitation (1% to <5%), anxiety (1% to <5%), apathy (1% to <5%), chills (1% to <5%), confusion (1% to <5%), coordination impaired (1% to <5%), depersonalization (1% to <5%), depression (1% to <5%), euphoria (1% to <5%), fever (1% to <5%), hypoesthesia (1% to <5%), lethargy (1% to <5%), nervousness (1% to <5%), pain (1% to <5%), pyrexia (1% to <5%), restlessness (1% to <5%), malaise (<1% to <5%), fatigue (2%), vertigo (2%)
Dermatologic: Dermatitis (1% to <5%), rash (1% to <5%)
Endocrine & metabolic: Hot flashes (2% to 9%), hyperglycemia (1% to <5%), menopausal symptoms (1% to <5%)
Gastrointestinal: Diarrhea (5% to 10%), xerostomia (3% to 13%), anorexia (1% to 6%), abdominal pain (1% to <5%), appetite decreased (1% to <5%), weight loss (1% to <5%), flatulence (<1% to <5%)
Genitourinary: Pelvic pain (1% to <5%), prostatic disorder (1% to <5%), urine abnormalities (1% to <5%), urinary tract infection (1% to <5%), urinary frequency (<1% to <5%), urinary retention (<1% to <5%)
Neuromuscular & skeletal: Arthralgia (1% to 5%), back pain (1% to <5%), creatine phosphokinase increased (1% to <5%), myalgia (1% to <5%), hypertonia (1% to <5%), neck pain (1% to <5%), rigors (1% to <5%), paresthesia (1% to <5%), tremor (1% to <5%)
Ocular: Blurred vision (1% to <5%), miosis (1% to <5%)
Respiratory: Bronchitis (1% to <5%), congestion (nasal/sinus) (1% to <5%), cough (1% to <5%), dyspnea (1% to <5%), nasopharyngitis (1% to <5%), pharyngitis (1% to <5%), rhinitis (1% to <5%), rhinorrhea (1% to <5%), sinusitis (1% to <5%), sneezing (1% to <5%), sore throat (1% to <5%), upper respiratory infection (1% to <5%)
Miscellaneous: Diaphoresis (2% to 9%), flu-like syndrome (1% to < 5%), withdrawal syndrome (1% to <5%), shivering (<1% to <5%)
<1% (Limited to important or life-threatening): Abnormal gait, allergic reaction, amnesia, anaphylactoid reactions, anaphylaxis, anemia, angioedema, appendicitis, ALT increased/decreased, AST increased/decreased, bradycardia, bronchospasm, BUN increased, cataracts, cellulitis, cholecystitis, cholelithiasis, clamminess, cognitive dysfunction, concentration difficulty, creatinine increased, deafness, disorientation, diverticulitis, dreams abnormal, dysphagia, dysuria, ear infection, ECG abnormalities, edema, fecal impaction, gastroenteritis, gastrointestinal bleeding, GGT increased, gout, hallucination, hematuria, hemoglobin decreased, hepatitis, hypotension, hypersensitivity, irritability, joint stiffness, libido decreased, liver enzymes increased, liver failure, menstrual disorder, MI, migraine, muscle cramps, muscle spasms, muscle twitching, myocardial ischemia, night sweats, orthostatic hypotension, palpitation, pancreatitis, peripheral edema, peripheral ischemia, pneumonia, proteinuria, pulmonary edema, pulmonary embolism, sedation, seizure, serotonin syndrome, sleep disorder, speech disorder, Stevens-Johnson syndrome, stomatitis, suicidal tendency, syncope, taste perversion, tachycardia, thrombocytopenia, tinnitus, toxic epidermal necrolysis, urticaria, vesicles, visual disturbance
A withdrawal syndrome may include anxiety, diarrhea, hallucinations (rare), nausea, pain, piloerection, rigors, sweating, and tremor. Uncommon discontinuation symptoms may include severe anxiety, panic attacks, or paresthesia.
Contraindications
 
Hypersensitivity to tramadol, opioids, or any component of the formulation
Canadian product labeling:
Tramadol is contraindicated during or within 14 days following MAO inhibitor therapy
Warnings / Precautions Drug
 
Concerns related to adverse effects:
• Anaphylactoid reactions: Rare but serious anaphylactoid reactions (including fatalities) often following initial dosing have been reported. Pruritus, hives, bronchospasm, angioedema, toxic epidermal necrolysis (TEN), and Stevens-Johnson syndrome also have been reported with use. Previous anaphylactoid reactions to opioids may increase risks for similar reactions to tramadol.
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• Seizures: Even when taken within the recommended dosage seizures may occur; risk is increased in patients receiving serotonin reuptake inhibitors (SSRIs or anorectics), other opioids, tricyclic antidepressants or other cyclic compounds (including cyclobenzaprine, promethazine), neuroleptics, MAO inhibitors, drugs which may lower seizure threshold, or drugs which impair metabolism of tramadol (ie, CYP2D6 and 3A4 inhibitors). Patients with a history of seizures, or with a risk of seizures (head trauma, metabolic disorders, CNS infection, malignancy, or during alcohol/drug withdrawal) are also at increased risk.
Disease-related concerns:
• Abdominal conditions: May obscure diagnosis or clinical course of patients with acute abdominal conditions.
• Drug abuse: Use with caution in patients with a history of drug abuse or acute alcoholism; potential for drug dependency exists.
• Ethanol use: Use with caution in heavy alcohol users.
• Head trauma: Use with extreme caution in patients with head injury, intracranial lesions, or elevated intracranial pressure; exaggerated elevation of ICP may occur.
• Hepatic impairment: Use with caution and reduce dosage in patients with mild-to-moderate hepatic impairment; extended release formulations should not be used in severe hepatic impairment (Child-Pugh class C); Ryzolt™ (extended release tablet) should not be used in any degree of hepatic impairment.
• Renal impairment: Use with caution and reduce dosage in patients with mild-to-moderate renal impairment; extended release formulations should not be used in severe renal impairment Clcr <30 mL/minute.
• Respiratory disease: Patients with respiratory disorders (eg, significant chronic obstructive pulmonary disease (COPD), cor pulmonale, hypoxia, hypercapnia) may be at greater risk of respiratory depression.
• Suicide risk: Suicide risk: Avoid use in patients who are suicidal; use with caution in patients taking tranquilizers and/or antidepressants, or those with an emotional disturbance including depression.
Concurrent drug therapy issues:
• CNS depressants: Use with caution and reduce dosage when administering to patients receiving other CNS depressants; may cause CNS depression and/or respiratory depression.
• Serotonin syndrome: Avoid, if possible, use with serotonergic agents such as TCAs, MAO inhibitors (use with extreme caution; contraindicated in Canadian product labeling), triptans, venlafaxine, trazodone, lithium, sibutramine, meperidine, dextromethorphan, St John’s wort, SNRIs, and SSRIs; use caution with drugs which impair metabolism of tramadol (ie, CYP2D6 and 3A4 inhibitors); concomitant use may increase the risk of serotonin syndrome.
Special populations:
• Debilitated patients: Use with caution in debilitated patients; there is a greater potential for critical respiratory depression, even at therapeutic dosages.
• Elderly: Extended-release formulation should be used with extreme caution in the elderly (particularly >75 years of age); may be more sensitive to adverse effects. Reduce initial dose.
Dosage form specific issues:
• Extended release tablets: Caution patients to swallow tablets whole. Rapid release absorption of tramadol from tablets that are broken, crushed, or chewed may lead to a potentially-lethal overdose.
• Phenylalanine: Some products may contain phenylalanine.
Other warnings/precautions:
• Abuse/misuse/diversion: Healthcare provider should be alert to problems of abuse, misuse, and diversion.
• Withdrawal: Tolerance or drug dependence may result from extended use (withdrawal symptoms have been reported); abrupt discontinuation should be avoided. Tapering of dose at the time of discontinuation limits the risk of withdrawal symptoms.
Metabolism/Transport Effects
Substrate of CYP2D6 (major), 3A4 (major)
Interactions
 
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Alvimopan: Analgesics (Opioid) may enhance the adverse/toxic effect of Alvimopan. This is most notable for patients receiving long-term (i.e., more than 7 days) opiates prior to alvimopan initiation. Management: Alvimopan is contraindicated in patients receiving therapeutic doses of opioids for more than 7 consecutive days immediately prior to alvimopan initiation. Risk D: Consider therapy modification
Ammonium Chloride: May increase the excretion of Analgesics (Opioid). Risk C: Monitor therapy
Amphetamines: May enhance the analgesic effect of Analgesics (Opioid). Risk C: Monitor therapy
Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of Analgesics (Opioid). Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Risk X: Avoid combination
CYP2D6 Inhibitors (Moderate): May diminish the therapeutic effect of TraMADol. These CYP2D6 inhibitors may prevent the metabolic conversion of tramadol to its active metabolite that accounts for much of its opioid-like effects. Risk C: Monitor therapy
CYP2D6 Inhibitors (Strong): May diminish the therapeutic effect of TraMADol. These CYP2D6 inhibitors may prevent the metabolic conversion of tramadol to its active metabolite that accounts for much of its opioid-like effects. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Risk D: Consider therapy modification
Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Desmopressin: Analgesics (Opioid) may enhance the adverse/toxic effect of Desmopressin. Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
MAO Inhibitors: TraMADol may enhance the neuroexcitatory and/or seizure-potentiating effect of MAO Inhibitors. TraMADol may enhance the serotonergic effect of MAO Inhibitors. Management: Consider alternatives to combined treatment with tramadol and monoamine oxidase inhibitors due to an increased risk of serotonin syndrome and seizures. Avoid transdermal selegiline. Risk D: Consider therapy modification
Mixed Agonist / Antagonist Opioids: May diminish the analgesic effect of Analgesics (Opioid). Management: Seek alternatives to mixed agonist/antagonist opioids in patients receiving pure opioid agonists, and monitor for symptoms of therapeutic failure/high dose requirements (or withdrawal in opioid-dependent patients) if patients receive these combinations. Risk D: Consider therapy modification
Pegvisomant: Analgesics (Opioid) may diminish the therapeutic effect of Pegvisomant. Risk C: Monitor therapy
Selective Serotonin Reuptake Inhibitors: May enhance the neuroexcitatory and/or seizure-potentiating effect of TraMADol. TraMADol may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: Analgesics (Opioid) may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Risk C: Monitor therapy
Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Risk D: Consider therapy modification
Sibutramine: May enhance the serotonergic effect of Serotonin Modulators. This may cause serotonin syndrome. Risk X: Avoid combination
Succinylcholine: May enhance the bradycardic effect of Analgesics (Opioid). Risk C: Monitor therapy
Thiazide Diuretics: Analgesics (Opioid) may enhance the orthostatic hypotensive effect of Thiazide Diuretics. Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Tricyclic Antidepressants: May enhance the neuroexcitatory and/or seizure-potentiating effect of TraMADol. Risk C: Monitor therapy
Vitamin K Antagonists (eg, warfarin): TraMADol may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Pregnancy
 
C
Pregnancy Implications
Adverse events were observed in animal studies. Tramadol has been shown to cross the human placenta when administered during labor. Postmarketing reports following tramadol use during pregnancy include neonatal seizures, withdrawal syndrome, fetal death, and stillbirth. Not recommended for use during labor and delivery.
Lactation
 
Enters breast milk/not recommended
Breast-Feeding Considerations
Sixteen hours following a single 100 mg I.V. dose, the amount of tramadol found in breast milk was 0.1% of the maternal dose. Use is not recommended by the manufacturer for postdelivery analgesia in nursing mothers.
Mechanism of Action
 
Tramadol and its active metabolite (M1) binds to μ-opiate receptors in the CNS causing inhibition of ascending pain pathways, altering the perception of and response to pain; also inhibits the reuptake of norepinephrine and serotonin, which also modifies the ascending pain pathway
Pharmacodynamics / Kinetics
 
Onset of action: Immediate release: ~1 hour
Duration: 9 hours
Distribution: Vd: 2.5-3 L/kg
Protein binding, plasma: ~20%
Metabolism: Extensively hepatic via demethylation (mediated by CYP3A4 and CYP2B6), glucuronidation, and sulfation; has pharmacologically active metabolite formed by CYP2D6 (M1; O-desmethyl tramadol)
Half-life elimination: Tramadol: ~6-8 hours; Active metabolite: 7-9 hours; prolonged in elderly, hepatic or renal impairment
Excretion: Urine (30% as unchanged drug; 60% as metabolites)
 
   
 
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