The concentrations of methylergometrine (M) in the plasma were determined by a new radioimmunoassay after a single intravenous and intramuscular administration of two brands. Methergin (Sandoz Pharmaceuticals, Inc, East Hanover, NJ, USA) and Myomergin (Leiras Pharmaceuticals, Turku, Finland). No significant differences between the two brands were found. After the intravenous injection, M distributed quickly from the plasma to the tissues, and according to the elimination phase half-life M has no cumulative properties. After the intramuscular injection, M was absorbed quickly with peak plasma concentrations at one-half hour.

Abortion, Induced↗

PubMedDate not supplied

Pharmacokinetics of glycopyrrolate in children.

STUDY OBJECTIVE: To investigate the pharmacokinetics of glycopyrrolate in children. DESIGN: Open study with three parallel groups. SETTING: Pediatric surgery department at a university hospital. PATIENTS: 26 healthy ASA physical status I children undergoing minor surgery. INTERVENTIONS: Patients were assigned to 1 of 3 groups: under 1 year of age (Group 1, n = 8), between 1 and 3 years of age (Group 2, n = 7), and over 3 years of age (Group 3, n = 11). Glycopyrrolate 5 micrograms/kg was given as a single intravenous (i.v.) injection before induction of general anesthesia. Blood samples (for determination of drug concentrations in plasma) were collected via venous cannula inserted into the contralateral antecubital vein. MEASUREMENTS AND MAIN RESULTS: ECG was observed continuously, blood pressure was measured with an automatic noninvasive device, and blood samples were taken just before and at 2, 4, 6, 10, 15, 30, 60, 120, 180, 240, 360, and 480 minutes after injection of glycopyrrolate. Glycopyrrolate concentrations in plasma were determined with a radioreceptor assay. The only significant difference in the pharmacokinetic parameters was the shortened elimination half-life in patients between 1 and 3 years of age. Glycopyrrolate 5 micrograms/kg i.v. did not cause any significant alterations in heart rate. CONCLUSIONS: There were no significant changes in the distribution volume or clearance of glycopyrrolate in children of different ages. The shortened elimination half-life in children between 1 and 3 years of age is of minor clinical importance.

Anesthesia, Intravenous↗

PubMedDate not supplied

The effect of metoclopramide on the contraction of the human gallbladder.

In a double blind study 45 patients were given either an i.v. injection of 20 mg Primperan (20 mg metoclopramide, Lundbeck, n = 15), 20 mg Metopram (20 mg metoclopramide, Leiras, n = 15) or a corresponding amount of physiological saline (n = 15) and the effect of metoclopramide on the human gallbladder was studied in x-ray examination of gallbladder. The gallstones do not appear to be a contraindication for the clinical use of metoclopramide as an antiemetic drug. No contraction of the gallbladder was demonstrated, even though metoclopramide has been shown to contact intestinal smooth muscle. Primperan caused more side effects than Metopram. Sedation seems to be the most common side effect of metoclopramide.

Cholecystography↗

PubMedDate not supplied

Risk-benefit assessment of anaesthetic agents in the puerperium.

A critical evaluation of anaesthetic agents in the puerperium is difficult because systematic, relevant studies are still lacking. Current knowledge of the effects of different agents used in labour and caesarean section indicates that significant residual effects on the mother and newborn are limited. In the early puerperium, based on physiological and/or hormonal changes, the mother could be more sensitive to inhalational anaesthetic agents and local analgesics. To date there is no evidence that any anaesthetic agent is excreted in breast milk in clinically significant amounts when given as a single dose. The only exception is perhaps in the case of very premature neonates whose mothers have had multidrug therapy before labour. Even then the importance of breast milk should be carefully assessed against possible adverse drug effect. However, repeated administration of long-acting benzodiazepines and continuous epidural administration of pethidine (meperidine) can have adverse effects on the neonate. The essential conclusion of this review is that breast-feeding is best. The different anaesthetic agents are excreted in the milk in amounts so low that detrimental effects on the neonate should not be expected.

Anesthesia, Obstetrical↗

PubMedDate not supplied

Clinical pharmacokinetics of cerebrospinal fluid.

The distribution of drugs into the cerebrospinal fluid has long been considered a challenging field of investigation in 2 major respects: (a) understanding how the physicochemical properties (molecular weight, pKa, plasma protein binding) of various molecules influence their movements across such a specific structure as the blood-brain barrier; and (b) defining the relationship between cerebrospinal fluid concentrations of various drugs and their central (side) effects. An attempt has been made to review the very dispersed information presently available to offer a clinically orientated picture of this area of pharmacokinetics. Drugs acting on the central nervous system (benzodiazepines, tricyclic antidepressants, anticonvulsants, opioids), antibacterial agents, cardiovascular drugs (beta-adrenoceptor blockers and digoxin), antineoplastic drugs (mainly methotrexate), and other miscellaneous agents (corticosteroids, cimetidine, methylxanthines) are reviewed. The available evidence seems to support the conclusion that only for methotrexate and antibacterial agents does knowledge of cerebrospinal fluid pharmacokinetics have direct therapeutic implications, while the mosaic of information available for other drugs does little more than provide a partially satisfactory picture.

Anti-Infective Agents↗

PubMedDate not supplied

Obstetric analgesia. Clinical pharmacokinetic considerations.

All drugs used in obstetric analgesia are more or less lipophilic, their site of action is in the central nervous system, and they have good membrane penetrability in the fetomaternal unit. Thus the dose and method of administration as well as the duration of treatment are important clinical determinants of drug effects in the fetus and newborn. In the past, too much emphasis has been placed on fetomaternal blood concentration ratios of different agents; it is now appreciated that the extent of fetal tissue distribution and the neonatal elimination rate are pharmacokinetically much more important. Extensive fetal tissue distribution is reflected in a low fetomaternal drug concentration ratio, which may be followed by prolonged neonatal elimination of the drug. Currently, the most effective and safest method for obstetric analgesia is regional epidural administration of bupivacaine or lignocaine (lidocaine); only low doses are needed and the newborn is able to handle these agents efficiently. On the basis of pharmacokinetic and neurobehavioural assessments, inhalational anaesthetic agents appear to be more attractive than pethidine (meperidine) or benzodiazepines. Intermittent administration and fast pulmonary elimination of inhalational agents ensure that long-lasting residual effects are unlikely to occur. The kinetics of epidural and intrathecal opiates explain the problems associated with their use in obstetrics. Among the newer drugs used in obstetric analgesia, the properties of meptazinol and isoflurane appear interesting and these agents warrant further study. All drugs used in obstetric analgesia have a potentially detrimental effect on the neonate and, therefore, knowledge of fetal and neonatal pharmacokinetics is of importance to the clinician.

Anesthesia, Obstetrical↗

PubMedDate not supplied

Pre-operative preparation.

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Cesarean Section↗

PubMedDate not supplied

Anxiety and endocrine responses to surgery.

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Anxiety↗