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The antiemetic activity of droperidol administered by intramuscular injection during cisplatin chemotherapy: a pilot study.

The antiemetic activity of escalating doses of droperidol was evaluated in ten patients undergoing chemotherapy with cisplatin regimens. Major antiemetic activity was achieved in five patients, two patients had less nausea and vomiting as compared with prior prochlorperazine therapy, and three patients were refractory to droperidol. No dose-response relationship was observed. Sedation occurred in nine patients, and two patients experienced dystonic reactions. Droperidol is a relatively safe and effective antiemetic for patients undergoing chemotherapy with cisplatin.

Adult↗

Changes in insulin-like growth factors I and II and their binding protein after a single intramuscular injection of growth hormone.

The concentrations of insulin-like growth factors I and II (IGF-I and IGF-II) and their binding proteins in serum were measured in 10 GH-deficient patients before and after a single 6-IU injection of GH. Serum IGF-I concentrations were initially low, increased significantly by 8 and 24 h, and decreased to pretreatment levels 48 and 72 h after GH administration. Serum IGF-II concentrations also were low initially and did not increase by 8 and 24 h, but were, however, significantly higher 48 and 72 h after GH administration. In GH-deficient patients before GH administration, binding of IGF-I or IGF-II to serum proteins was restricted primarily to proteins of 50K mol wt. Little or no binding to proteins of 150,000 mol wt was found. By 8 and 24 h after GH injection, IGF-I, but not IGF-II, bound primarily to a protein(s) of 150K mol wt, as in normal subjects. IGF-II remained bound to a 50K mol wt protein. By 48 and 72 h after administering GH, however, the binding pattern was reversed, and IGF-II, but not IGF-I, bound predominantly to a protein(s) of 150K mol wt. Our data demonstrate both a temporal dissociation in the responses of IGF-I and IGF-II to GH and a similar temporal dissociation in the binding of IGF-I and IGF-II to the large mol wt (150K) binding protein. This dissociation, particularly the latter, may provide a means for better characterization of protein fractions in binding IGF, particularly in terms of specificity.

Adolescent↗

Serum interferon beta-1a (Avonex) levels following intramuscular injection in relapsing-remitting MS patients.

BACKGROUND: The pharmacokinetics of IFNbeta-1a in MS patients are poorly understood. We have previously reported an ELISA sensitive and specific for measuring serum IFNbeta-1b levels in patients with MS. OBJECTIVE: We describe an ELISA to measure interferon beta-1a (Avonex) in the serum of MS patients following IM administration. METHODS: We have developed an ELISA for detecting serum IFNbeta-1a in MS patients receiving 6 million units (MU) of IFNbeta-1a, IM once weekly. The specificity of this ELISA was confirmed by the lack of cross-reactivity with other cytokines except for IFNbeta-1b. RESULTS: Serum IFNbeta-1a levels were measured at 3 and 6 months after initiating treatment with IFNbeta-1a in 10 MS patients. At 3 months, all 10 patients had detectable levels ranging from 68 to 86 IU/mL. At 6 months, IFNbeta-1a could be detected in the serum of all but three patients, with levels ranging from 64 to 81 IU/mL. A kinetic study of IFNbeta-1a serum levels in a separate group of six MS patients who had been receiving IFNbeta-1a for several months was carried out. Blood was drawn before and 2, 4, 6, 8, and 24 hours after IFNbeta-1a injection. Peak serum IFNbeta-1a levels were observed at 8 hours and became undetectable at 24 hours after injection. CONCLUSION: The described ELISA may have useful clinical applications in examining the correlation between serum IFNbeta-1a levels and clinical efficacy.

Enzyme-Linked Immunosorbent Assay↗

The dose-response relationship and regional distribution of lactate after intramuscular injection of halothane and caffeine in malignant hyperthermia-susceptible pigs.

We hypothesized that IM halothane and caffeine injection increases local lactate concentration dose-dependently in malignant hyperthermia-susceptible (MHS) and nonsusceptible (MHN) pigs and that the hypermetabolic reaction measured by regional distribution of lactate and carbon dioxide is limited to a small muscle volume. Microdialysis probes were placed in the hindlimbs of 7 MHS and 7 MHN pigs and perfused with Ringer's solution. After equilibration, boluses of increasing halothane and caffeine concentrations were injected. For the second hypothesis regarding regional distribution, microdialysis probes were positioned in 7 MHS and 6 MHN pigs at the injection site for halothane and caffeine and at a distance of 10 mm and 25 mm. Lactate was measured in the dialysate by spectrophotometry. In addition, PCO2 was measured in the halothane experiments. Halothane and caffeine increased IM lactate dose-dependently in MHS pigs significantly more than in MHN pigs. Lactate and PCO2 were increased only at the injection site but not at 10 mm and 25 mm distance. MH susceptibility leads to a leftward shift of the dose-response curve for IM lactate after local injection of halothane and caffeine. The increase of lactate and carbon dioxide levels after local MH trigger injection is limited to a small area around the probe.

Anesthetics, Inhalation↗

Polyacrylamide gel electrophoretic serum protein patterns of acute inflammation induced by intramuscular injection of turpentine in young broiler chickens.

Changes in the serum protein patterns accompanying inflammation in young broilers were examined by polyacrylamide gradient gel electrophoresis. Sera were obtained from blood of 4-week-old male broilers after induction of acute inflammation by an injection of 0.5 ml/kg turpentine. Electrophoretic patterns at 48 hr after injection, showed an increase in transferrin (Tf) and a segment containing albumin (Alb) with multiple peaks. The unbound iron binding capacity (UIBC) increased by 10 times, and the serum iron (SI) concentration in acute inflammation was reduced to one-half its initial value. These are considered to be typical changes in serum proteins and iron after acute inflammation.

Animals↗

Intramuscular injection of testosterone undecanoate for the treatment of male hypogonadism: phase I studies.

OBJECTIVE: In the search for long-acting testosterone preparations suited for substitution therapy of hypogonadal men, testosterone undecanoate (TU) dissolved in either tea seed oil or castor oil was investigated. DESIGN: In study I, 1000 mg TU in tea seed oil (125 mg/ml) were injected in equal parts into the gluteal muscles of seven hypogonadal men. In study II, 1000 mg TU in castor oil (250 mg/ml) were injected into one gluteal muscle of 14 patients. RESULTS: In comparison with published data on testosterone enanthate, most widely used for i.m. injections, the kinetic profiles of both TU preparations showed extended half-lives and serum levels not exceeding the upper limit of normal. The castor oil preparation had a longer half-life than TU in tea seed oil (33.9+/-4.9 vs 20.9+/-6.0 days (mean pm S.E.M.)). CONCLUSION: The longer half-life and the smaller injection volume make TU in castor oil a strong candidate for further applications in substitution therapy and in trials for male contraception.

Adult↗

Induction of the synthesis of the pregnancy-specific protein p70 in the endometrium by intramuscular injection of recombinant bovine interferon-alpha I1 in nonpregnant ewes.

We examined the effect of recombinant bovine interferon-alpha I1 (rboIFN-alpha I1) or recombinant bovine trophoblast protein-1 (rbTP-1) on protein synthesis by endometrial explants from Day-13 cyclic ewes and studied the ability of rboIFN-alpha I1 injected i.m. to influence subsequent protein secretion by endometrial tissue explants. In Expt 1, ewes were injected with either 2 mg rboIFN-alpha I1 or vehicle alone at 12 h intervals beginning on Day 11 of the oestrous cycle and ending on the morning of Day 13; 8 h after the last injection, ewes were hysterectomized and endometrial explant cultures were prepared. Explants were cultured for 24 h in leucine-deficient medium supplemented with 250 microCi L-[3H]leucine per culture. For Expt 2, additional explants were prepared from Expt 1 controls. Explants were cultured in the presence of 0, 20 or 200 ng/ml of either rboIFN-alpha I1 or rbTP-1 for 24 h in leucine-deficient medium supplemented with 250 microCi L-[3H]leucine per culture. Secreted proteins were analysed by two-dimensional electrophoresis and fluorography. There was a marked enhancement of a 70 kDa acidic protein, p70, in explants cultured in the presence of rboIFN-alpha I1 or rbTP-1. This polypeptide is a product of the gravid uterine horn from Day 14 to Day 20 of pregnancy and is a useful marker of the action of interferon-alpha (IFN-alpha) on endometrium. Enhanced production of p70 also occurred in ewes injected i.m. with rboIFN-alpha I1.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗