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Biomedical subjects

A Rane

Publications and source records attributed to A Rane.

At least 217 records · Page 12Linked to original sources
PubMed1982

Extradural and parenteral morphine: kinetics and effects in postoperative pain. A controlled clinical study.

In a controlled clinical study of 20 patients undergoing arthrotomy a single dose of morphine 0.05 mg kg-1 administered extradurally resulted in more pronounced and prolonged pain relief than morphine 0.1 mg kg-1 i.m. in the period immediately after operation. This difference was significant between 2 and 11 h after morphine administration. The maximum analgesic effect for nine patients in the extradural group was obtained about 2 h after injection. Two of 10 in the extradural group experienced urinary retention. Other side-effects were mild for both groups. Plasma concentrations of morphine were measured in five patients in each group. Four hours after administration, morphine was not detectable in plasma in any of the extradural group and in two of the i.m. group. Our study gives further support for the theory that extradural morphine acts on the spinal cord.

Adult↗
PubMed1982

Extradural pethidine with and without adrenaline during labour: wide variation in effect.

The pain-relieving effect of a single extradural dose of pethidine 25 mg with and without adrenaline was studied in 20 healthy women during labour. The study was open regarding the effects of pethidine but double-blind regarding the addition of adrenaline. In 14 of 19 women good or excellent analgesia was achieved for a period of 50-160 min. Pethidine with adrenaline 25 micrograms was not more effective than pethidine alone. Eight of the 14 women showed signs of regional analgesia to pin-prick and temperature discrimination. The patients had small (45-188 ng ml-1) concentrations of pethidine in plasma. In eight patients the plasma concentrations of pethidine were maintained for at least 1.5 h. Extradural pethidine thus induces analgesia of short and variable duration. Repeated doses may be needed, resulting in accumulation of the drug in plasma with the risk of respiratory depression in mother or child.

Anesthesia, Epidural↗
PubMed1982

Phenytoin excretion in human breast milk and plasma levels in nursed infants.

Phenytoin excretion into human breast milk was studied in six nursing women with epilepsy. The average ratio between the areas under the plasma (and milk) concentration versus time curves (AUC) was 0.13. There was a good (r = 0.97) correlation between the mean plasma and milk concentrations of phenytoin, and an even better relation (r = 0.99) between the AUC for phenytoin in plasma and the mean milk concentration. The ratio between unconjugated and conjugated 4-OH-phenytoin (the main metabolite) in plasma was 0.08-0.09. The corresponding ratio in milk was considerably higher. The present data do not argue against breast feeding during phenytoin therapy, not even when weighed against the potential risks for toxicity of the parent compound. Only two of six infants had a measurable, yet very low plasma concentration of phenytoin. The calculated body weight--related doses of phenytoin secreted into milk will be less than 5% of the dose to infants and small children.

Adult↗
PubMed1982

Maternal kinetics and transplacental passage of pethidine during labour.

1 Pethidine is commonly used in single doses as an analgesic in obstetrics. Plasma concentration-time profiles of pethidine after intramuscular administration of 1.5 mg/kg body weight to 16 pregnant women during labour were investigated. There was only a two-fold variation in peak plasma concentration (300-650 ng/ml). The mean (+/- s.d.) value of the apparent plasma half-life of pethidine was 3.4 (+/- 1.0) h which is not different from that in healthy controls. norpethidine plasma levels were not measurable (less than 10 ng/ml). 2 The placental transfer transfer of pethidine was studied at delivery in samples from the umbilical cord vessels and from a maternal peripheral vein. In another 14 patients serial determinations of pethidine concentration were made in foetal scalp blood and maternal venous blood simultaneously during the different stages of labour. The foeto-maternal drug ratio varied between 0.35 and 1.5 with a positive correlation between ratio and dose delivery time interval. The concentration of pethidine in umbilical cord plasma or blood varied between 60 and 400 ng/ml with dose-delivery time intervals of 30 min to 10.5 h. The foetal concentration of pethidine reached a peak-plateau value between 1-5 h after dose.

Female↗
PubMed1982

Clindamycin passage into human milk.

1 The clindamycin bioactivity was measured during the dosage interval in the plasma of women with puerperal infections and in their breast milk. 2 There was a marked interindividual variation in the peak levels. The clindamycin bioactivity in the milk ranged from 1/10 to several times the corresponding bioactivity in the plasma that was collected at the same time. 3 The concentration of clindamycin in the milk (bioactivity) at the end of the dosage interval correlated with the area under the plasma concentration v time curve. 4 Clindamycin is thus transferred into human breast milk. Although the actual amounts secreted are small, the wellknown side effects and the lack of knowledge about the disposition and effects of clindamycin in newborn infants are strong arguments against nursing during treatment with this drug.

Adult↗
PubMed1982

Glucuronidation of morphine in human liver and interaction with oxazepam.

Morphine is primarily metabolized through glucuronidation by a microsomal UDP-glucuronyltransferase. With the use of 14C-morphine the activity of this enzyme was measured in hepatic microsomes from ten kidney transplant donors with total cerebral infarction and four icteric patients with pancreatic carcinoma. In the former livers the rate of glucuronidation varied from 1.08 to 8.67 nmol per mg microsomal protein per min, with a mean value of 3.83. These values were somewhat higher than in the liver biopsies from the four cancer patients. Oxazepam, at 1/10 the concentration of morphine, inhibited the morphine glucuronidation by 35%. The inhibition was competitive. Salicylamide also inhibited the morphine glucuronidation but only at concentrations considerably higher than morphine. The relevance of the in vitro data for the in vivo situation is unclear, since the concentrations employed in this study are several-fold higher than those encountered in the plasma of patients treated with these drugs.

Drug Interactions↗
PubMed1982

Clinical evaluation of oral methadone in treatment of cancer pain.

A dose-adjustment program for oral methadone and the long-term effects of the analgesic therapy have been evaluated in 15 patients with incurable cancer. Rapid and continuous pain relief without serious side-effects was achieved by "ad libitum" dosage in the first 3-5 days. Thereafter, a dosage based on each patients's subjective need was instituted. The mean daily dose was 44 during the first day and it decreased to 22 mg daily at the end of the dose-adjustment week. Three patients did not complete the program because of insufficient effect or severe nausea. Among the 12 patients who chose to continue the methadone treatment after the initial dose-adjustment period, four continued the therapy to their death, three discontinued the therapy due to insufficient effect, and three due to adverse reactions. In one case it was possible to stop the treatment due to decreased pain. The treatment period in these 12 patients varied between 8 and 270 days. Oral methadone offers good pain relief for long periods of time in this group of patients and has obvious advantages as compared to long term parenteral therapy with narcotic analgesics.

Administration, Oral↗
PubMed1982

Regional epidural analgesia: kinetics of pethidine.

Low intrathecal doses of opiates produce dose-dependent long-wasting elevation of the pain threshold in rats. The effect is postulated to be mediated by a direct action on the substantia gelatinosa of the spinal cord. Eight uncontrolled and two controlled studies in man showed a long duration of analgesia for most patients in the postoperative period. The duration of effect differs widely within and between studies. Using a double-blind design, we compared the relative efficacy of epidural and parenteral pethidine to control postoperative pain after total hip replacement. Preliminary pharmacokinetic data from six patients show that epidural doses of 20 or 60 mg pethidine give a similar pattern of absorption and elimination in plasma as 2 mg pethidine/kg body weight intramuscularly. The terminal elimination half-lives of pethidine in plasma are 5-7 h for all routes of administration. The possibility cannot be excluded that the analgesic effect of epidural pethidine is partly systemically mediated.

Anesthesia, Conduction↗
PubMed1982

Renal glucuronidation of morphine in the human foetus.

The glucuronidation of morphine was investigated in kidney microsomes from human foetuses. This reaction was found to be catalyzed in all specimens investigated and the UDP-glucuronyltransferase activities varied between 0.18 and 0.30 nmol per min. per mg microsomal protein. Intraindividual comparisons with the hepatic glucuronidation rates revealed the renal enzyme rate to be about 50 percent of the hepatic. Oxazepam, and to a lesser extent salicylamide, inhibited the glucuronidation of morphine in kidney microsomes in similarity to what previously was shown in human foetal liver microsomes.

Female↗
PubMed1982

Sulphate and glucuronic acid conjugation of harmol in human fetal and adult liver tissue.

Glucuronidation of harmol in microsomal preparations and sulphate conjugation in hepatic 105,000 g supernatant fractions were studied comparatively in human fetal and adult liver subcellular preparations. The formation of harmol sulphate in the fetal liver was slightly lower than in the adult liver and considerably lower than in rat liver. No glucuronidation of harmol was found in fetal liver, while the activity in adult liver was 30-80 nmol glucuronide formed/2 mg/20 min. In an ontogenic perspective, our in vitro findings are consistent with drug metabolic studies in the human neonate in whom negligible glucuronidation but well-developed sulphate conjugation of paracetamol has been demonstrated.

Adult↗