zyduscadila.com

The effect of concentration of hydrophilic (hydroxypropyl methylcellulose [HPMC]) and hydrophobic polymers (hydrogenated castor oil [HCO], ethylcellulose) on the release rate of tramadol was studied. Hydrophilic matrix tablets were prepared by wet granulation technique, while hydrophobic (wax) matrix tablets were prepared by melt granulation technique and in vitro dissolution studies were performed using United States Pharmacopeia (USP) apparatus type II. Hydrophobic matrix tablets resulted in sustained in vitro drug release (>20 hours) as compared with hydrophilic matrix tablets (<14 hours). The presence of ethylcellulose in either of the matrix systems prolonged the release rate of the drug. Tablets prepared by combination of hydrophilic and hydrophobic polymers failed to prolong the drug release beyond 12 hours. The effect of ethylcellulose coating (Surelease) and the presence of lactose and HPMC in the coating composition on the drug release was also investigated. Hydrophobic matrix tablets prepared using HCO were found to be best suited for modulating the delivery of the highly water-soluble drug, tramadol hydrochloride.

Tramadol reference source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14621963&dopt=Abstract tramadol Ultram

tresearch.org

OBJECTIVE: Assess the validity of medical products reporting program (MEDWatch) reports of abuse/dependence and withdrawal associated with Ultram (tramadol). METHODS: Reports of possible abuse/dependence or withdrawal associated with Ultram during 13 quarters following launch were spontaneously reported to the manufacturer Ortho-McNeil Pharmaceutical (OMP) and also solicited from 255 NIDA grantees and addiction treatment professionals by an Independent Steering Committee (ISC). Reports were classified by the ISC using DSM-IV criteria, by the Drug Safety and Surveillance (DSS) units of Robert Wood Johnson Pharmaceutical Research Institute (PRI) using World Health Organization Adverse Reaction Terms (WHOART) terms, and reported to the food and drug administration (FDA) via MEDWatch. Rates of abuse/dependence and withdrawal per 100000 persons exposed were calculated separately for classifications made by the PRI and the ISC, and confidence intervals calculated to determine the degree to which they agreed. RESULTS: For 681 reports submitted to PRI, confidence intervals of ISC ratings contained PRI ratings 12 of 13 times for abuse/dependence, and 12 of 13 times for withdrawal. For 242 reports submitted to the ISC, confidence intervals of ISC ratings contained PRI ratings 10 of 13 times for abuse/dependence, and 12 of 13 times for withdrawal. Proactive surveillance increased the total number of cases of abuse/dependence but not withdrawal. Many cases of withdrawal without signs or symptoms of abuse/dependence were identified. CONCLUSIONS: There was good/excellent concordance between MEDWatch and ISC classifications. Proactive surveillance increased cases of abuse/dependence but not withdrawal. Withdrawal with no signs or symptoms of dependence was common. More use of proactive surveillance is likely to improve assessments of public health risks associated with adverse events.

Tramadol reference source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14636971&dopt=Abstract tramadol Ultram [PubMed - in process]

sina.com

OBJECTIVE: To evaluate the safety and analgesic efficacy of patient controlled intravenous analgesia (PCIA) with tramadol, and to compare its benefits and risks with combined spinal-epidural analgesia (CSEA)+ patient controlled epidural analgesia (PCEA). METHODS: Eighty American Society of Anesthesiologist (ASA) I-II at term parturients in active labor were randomly divided into 3 groups: the control group (n = 30) received no analgesia; group A (n = 30) received spinal administration with ropivacaine 2.5 mg and fentanyl 5 microg, then with PCEA; group B (n = 20) received 1 mg/kg tramadol loading dose i.v. PCIA with 0.75% tramadol and it included: PCA dose 2 ml, lockout time 10 minutes, background infusion 2 ml/h, total dose no more than 400 mg. The intensity of pain was evaluated using Visual Analogue Scale (VAS). RESULTS: Both group A and B showed good pain relief. VAS pain scores were significantly decreased in group A and B compared with those in the control group (P < 0.01). In comparison with group B, the VAS pain scores decreased in group A (P < 0.05). The onset times of analgesia in group A were shorter than those in group B (P < 0.05). Apgar scores in group B were lower than those in group A (P < 0.05). The periods of second stage of labor in group A were longer than those in the control group and group B (P < 0.05). The cesarean delivery rate was significantly higher in the control group (16.7%) than in group A (3.3%) and group B (5.0%), but it did not differ between group A and B. There were no significant differences in vital signs, fetal heart rate, degree of motor block, and uterine contractions among the 3 groups. CONCLUSIONS: PCIA with tramadol is now a useful alternative when patients are not candidates for CSEA for labor, or do not want to have a neuraxial block anesthesia. However, sometimes it may not provide satisfactory analgesic effect.

Tramadol reference source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14642152&dopt=Abstract tramadol Ultram [PubMed - in process]

heinfo.net

AIM: To compare the pharmacokinetics of the enantiomers of trans-tramadol (trans-T) and its active metabolite, trans-O-demethyltramadol (M1), in male and female rats. METHODS: Following a single oral dose of 10 mg/kg trans-T hydrochloride to rats, (+)-trans-T, (-)-trans-T, (+)-M1, and (-)-M1 in plasma were determined by a high performance capillary electrophoresis method. RESULTS: The females showed higher plasma concentrations of (+)-trans-T, (-)-trans-T, and (+)-M1 than the males. The enantiomers of trans-T were absorbed and eliminated more slowly in the females than in the males. (+)-M1 was eliminated more slowly in the females than in the males. All pharmacokinetic parameters but Tmax of the two enantiomers of trans-T were significantly different in both sex rats. The (+)/(-)-enantiomeric ratios of the pharmacokinetic parameters for trans-T in the males were similar to those in the females. The values of Cmax, AUC(0-infinity) of the two enantiomers of M1 were significantly different in both sex rats. The (+)/(-)-enantiomeric ratios of Cmax, AUC(0-infinity) for M1 were lower than 1 in the males, larger than 1 in the females. CONCLUSIONS: Systemic exposure of (+)-trans-T, (-)-trans-T, and (+)-M1 was higher in female rats than in male rats. The stereoselectivity in pharmacokinetics of trans-T was similar, and that of M1 was different in male and female rats.

Tramadol reference source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14653955&dopt=Abstract tramadol Ultram [PubMed - in process]




Minerva Chir. 2003 Dec;58(6):853-5.
[How to control postoperative pain: intravenous route]

[Article in Italian]

Occella P, Vivaldi F.

I Servizio di Anestesia e Rianimazione, Azienda Ospedaliera, San Giovanni Battista, Universita degli Studi di Torino, Torino, Italy.

Intravenous administration of analgesic drugs is one of the most common ways to control post-operative pain. It can be used in almost all kinds of surgical interventions and particularly those of medium and high complexity. Besides, when other techniques are contraindicated because of clinical and/or managing problems, intravenous way finds its best application. Among analgesic drugs NSAID (ketorolac) and opioids (tramadol, morphine, buprenorphine) are most frequently used. As to administration techniques, elastomeric pump is, according to personal experience, a simple-to-manage, practical and precise device with lower cost respect to other administration set. Elastomeric pump is a single use reservoir that allows continuous administration of drugs with a uniform pre-set infusion speed. Finally, guide-lines, showing pre-load and infusion doses of analgesic drugs, based on pain intensity, are presented.

Tramadol reference source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14663417&dopt=Abstract tramadol Ultram [PubMed - in process]