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PMS-TRAMADOL-ACET is a brand name for Acetaminophen (also known as Paracetamol), supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: AND CLINICAL USE ............................................................................ 3 CONTRAINDICATIONS ................................................................................................. 4 WARNINGS AND PRECAUTIONS.................................................................................…
Verbatim from this product's HC label. Tap a section to expand.
, Cardiovascular; ADVERSE REACTIONS, Other Clinically Significant Adverse Experiences Previously Reported in Clinical Trials or Post- Marketing Reports with Tramadol; DRUG INTERACTIONS, QTc Interval-Prolonging Drugs; DOSAGE AND ADMINISTRATION, Recommended Dose and Dosage Adjustment; OVERDOSAGE).
pms-TRAMADOL-ACET Product Monograph Page 36 of 70 Concentration – Efficacy Relationships The minimum effective analgesic concentration will vary widely among patients, especially among patients who have been previously treated with potent opioid agonists.
The minimum pms-TRAMADOL-ACET Product Monograph Page 37 of 70 effective analgesic concentration of tramadol for any individual patient may increase over time due to an increase in pain, the development of a new pain syndrome and/or the development of analgesic tolerance.
Concentration – Adverse Reaction Relationship There is a relationship between increasing tramadol plasma concentration and increasing frequency of dose-related opioid adverse reactions such as nausea, vomiting, CNS effects, and respiratory depression.
In opioid-tolerant patients, the situation may be altered by the development of tolerance to opioid-related adverse reactions (see DOSAGE AND ADMINISTRATION). Pharmacokinetics Tramadol Tramadol is administered as a racemate and both the (-) and (+) forms of both tramadol and M1 are detected in the circulation.
3. Tramadol has a slower absorption and longer half-life when compared to acetaminophen. 6) a For acetaminophen, Cmax was measured as mcg/mL. A single-dose pharmacokinetic study of tramadol hydrochloride and acetaminophen in volunteers showed no drug interactions between tramadol and acetaminophen.
Upon multiple oral dosing to steady state, however, the bioavailability of tramadol and metabolite M1 was lower for the combination tablets compared to tramadol administered alone. 2% for (-)-M1. The cause of this reduced bioavailability is not clear.
Following single or multiple dose administration of tramadol hydrochloride / acetaminophen, no significant change in acetaminophen pharmacokinetics was observed when compared to acetaminophen given alone. pms-TRAMADOL-ACET Product Monograph Page 38 of 70 Absorption The absolute bioavailability of tramadol from tramadol hydrochloride and acetaminophen tablets has not been determined.
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
Other brands of Acetaminophen in Canada.
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Tramadol hydrochloride has a mean absolute bioavailability of approximately 75% following administration of a single 100 mg oral dose of tramadol HCl tablets. The mean peak plasma concentration of racemic tramadol and M1 after administration of two tramadol hydrochloride and acetaminophen tablets occurs at approximately two and three hours, respectively, post-dose.
Peak plasma concentrations of acetaminophen occur within one hour and are not affected by co-administration with tramadol. Oral absorption of acetaminophen following administration of tramadol hydrochloride and acetaminophen tablets occurs primarily in the small intestine.
Food Effects When tramadol hydrochloride and acetaminophen tablets were administered with food, the time to peak plasma concentration was delayed for approximately 35 minutes for tramadol and almost one hour for acetaminophen. However, peak plasma concentration and the extent of absorption of either tramadol or acetaminophen were not affected.
The clinical significance of this difference is unknown. 9 L/kg in male and female subjects, respectively, following a 100 mg intravenous dose. The binding of tramadol to human plasma proteins is approximately 20%, and binding also appears to be independent of concentration up to 10 mcg/mL.
Saturation of plasma protein binding occurs only at concentrations outside the clinically relevant range. Acetaminophen appears to be widely distributed throughout most body tissues except fat. 9 L/kg. A relatively small portion (~ 20%) of acetaminophen is bound to plasma protein.
Metabolism Following oral administration, tramadol is extensively metabolized by a number of pathways, including CYP2D6 and CYP3A4, as well as by conjugation of parent and metabolites. Approximately 30% of the dose is excreted in the urine as unchanged drug, whereas 60% of the dose is excreted as metabolites.
The major metabolic pathways appear to be N- and O-demethylation and glucuronidation or sulfation in the liver. Metabolite M1 (O-desmethyltramadol) is pharmacologically active in animal models. Patients who are CYP2D6 ultra-rapid metabolizers convert tramadol to its active metabolite (M1) more rapidly and completely than other patients.
, debrisoquine, dextromethorphan, and tricyclic antidepressants) (see Special Populations and Conditions, Race). pms-TRAMADOL-ACET Product Monograph Page 39 of 70 Based on a population PK analysis of Phase I studies in healthy subjects, concentrations of tramadol were approximately 20% higher in “CYP2D6 poor metabolizers” versus “extensive CYP2D6 metabolizers”, while M1 concentrations were 40% lower.
In vitro drug interaction studies in human liver microsomes indicate that inhibitors of CYP2D6 […]