From: paprcutr@aol.com (PaprCutr) Subject: Re: Tradol (Ultram) Date: 1995/08/21 newsgroups: alt.drugs.hard I just recently returned from Mexico and Tradol was the only OTC analgesic worth trying. I even brought an American bottle of Klonopin for them to refill, and wouldn't without a mexican doctor's script. The new law was instated Jun 30. Anyway Tradol he told me was for "mucho dolar" much pain, and suggested a dosage of two before bedtime. I took 6 and in 90 minutes got very high. I don't remember what the dosage was, but it should be understood to cause euphoria and nodding in high doses. ================================================================== From: (Timelord95) Subject: Re: Ultram or 569 Date: 1995/11/03 newsgroups: alt.drugs.hard IF IT IS ULTRAM, STAY AWAY FROM IT. Ultram is a mu-opioid agonist which also happens to lower the seizure threshold about 40% on average. I've had a seizure thanks to this shit- AVOID it. The Timelord ================================================================== From: smisch Subject: Ultram Date: 1996/05/28 newsgroups: alt.drugs,alt.drugs.hard Someone recently asked about this drug. The following has been nicked in full from http://pharminfo.com and should answer more than a few questions: --------- --------- Tramadol for Pain Reprinted from the April 1995 issue of Medical Sciences Bulletin , published by PharmaceuticalInformation Associates, Ltd. (www.pharminfo.com) Indication: Moderate to severe pain Drug Tradename: Ultram Manufacturer: Johnson & Johnson Johnson & Johnson has received marketing approval for its prescription analgesic tramadol (Ultram) for management of moderate to severe pain. The manufacturer claims that the drug is less likely than nonsteroidal antiinflammatory drugs (NSAIDs) to cause serious gastrointestinal side effects and less likely than opioids to produce physical dependence. Tramadol is scheduled to become available to physicians about mid-April. It is manufactured by R. W. Johnson and marketed by Ortho-McNeil. Tramadol hydrochloride is a centrally acting, synthetic analgesic that is not derived from natural sources and is not chemically related to opiates. Its chemical name is (+)cis-2-[(dimethylamino)methyl]-1-(3-methoxyphenyl) cyclohexanol. The mechanism of action of tramadol is not fully understood. The drug, however, appears to have two modes of action. It binds with low affinity to mu-opioid receptors (the principal active metabolite has a greater affinity for these receptors); this blocks pain impulses from reaching the brain, in the same way as with NSAIDs and opioids. Tramadol, in addition, inhibits reuptake of norepinephrine and serotonin, altering the way the brain monitors pain signals. The effect in pain relief is said to be equivalent to that of Tylenol(R) with Codeine #3. Tramadol does not inhibit production of prostaglandins, so the risk of gastrointestinal bleeding and renal toxicity is reduced. The drug is believed to carry low potential for abuse and thus has not been designated a controlled substance, but the manufacturer will be required to conduct postmarketing studies of abuse potential. Racemic tramadol is rapidly absorbed after oral administration. Bioavailability is about 75%, and food does not alter the rate or extent of absorption. Peak plasma concentration is reached about 2 hours after a single dose, and the peak concentration of the principal active metabolite occurs after 3 hours. Steady state is achieved after 2 days of treatment. The plasma half-life is 5 hours after a single dose and 7 hours with multiple doses. Tramadol is extensively metabolized, primarily by N- and O-demethylation and glucuronidation or sulfation in the liver. Three long-term, controlled clinical trials involving 820 subjects (530 receiving tramadol) have examined the efficacy of tramadol for chronic low back pain and pain associated with cancer, neuropathy, and orthopedic and joint conditions. Researchers found that approximately 250 mg tramadol a day, in divided doses, produced pain relief equivalent to that produced by five doses of acetaminophen 300 mg with codeine phosphate 30 mg, five doses of aspirin 325 mg with codeine phosphate 30 mg, or two to three doses of acetaminophen 500 mg with oxycodone hydrochloride 5 mg. The most frequently reported side effects have been dizziness, nausea, constipation, headache, and somnolence. These occurred at rates similar to those for codeine- containing analgesics. Tramadol is contraindicated for patients with hypersensitivity to the drug and in cases involving acute intoxication with alcohol, hypnotics, centrally acting analgesics, opioids, or psychotropic drugs. Seizures have been observed in laboratory animals receiving the drug in excessive doses. Tramadol should be used with caution in patients receiving monoamine oxidase inhibitors and in those with respiratory distress, intracranial pressure or head injury, acute abdominal conditions, or renal or hepatic disease. Ultram is an oral preparation available in 50-mg white, film-coated, capsule-shaped tablets. The recommended dose is 50 to 100 mg as needed every 4 to 6 hours, with the total dose not to exceed 400 mg a day. According to the manufacturer, the 50-mg dose should be adequate for moderate pain. More severe pain may require the 100-mg dose. The dosage does not need to be adjusted for elderly patients, but for those with creatinine clearance less than 30 mL/min, lengthening the dose interval to 12 hours is recommended, with a maximum daily dose of 200 mg. Dialysis patients can take a normal dose, because dialysis removed only about 7% of the drug from the blood. For patients with hepatic cirrhosis, the recommended dose is 50 mg every 12 hours. The normal dose may need to be doubled for patients who are also taking carbamazepine. (FDC Reports. 1995; Mar 13:8-9. Lee CR et al. Drugs. 1993; 46: 313-340. Additional information from the manufacturer.)