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At least 19 recordsLinked to original sources
PubMed1988

Second trimester abortion with ethacridine lactate plus carboprost--which is the best time to administer the carboprost?

Extra-amniotic ethacridine lactate plus intramuscular prostaglandin has become a popular method for terminating second trimester pregnancies. In this study, intrauterine pressure was continuously monitored in order to objectively compare the efficacy of 3 different times of administration of Carboprost (15-methyl PGF2 alpha) - at 2 hours, 4 hours and 8 hours after the instillation of ethacridine lactate. The best results were obtained with the administration of Carboprost 8 hours after the instillation of the extra-amniotic ethacridine lactate. The synergistic effect of ethacridine lactate and Carboprost is optimal after this time. This is probably because the ethacridine lactate will have produced sufficient cervical ripening to ensure optimal efficacy of the prostaglandin-induced uterine contractions in expelling the products of conception.

Abortifacient Agents↗
PubMed1980

Comparison of two high-pressure liquid chromatographic assays for carboprost, a synthetic prostaglandin.

A high-pressure liquid chromatographic assay for carboprost tromethamine as the bulk drug and in a sterile solution formulation is described. The procedure involves derivatization of the prostaglandin to form the UV-absorbing naphthacyl ester, which then is chromatographed on a silica gel column using methylene chloride-1,3-butanediol-water (496:4:0.25) as the mobile phase. This procedure is compared with a nonderivatization procedure with refractive index detection. Both procedures separate the 15R-epimer of carboprost from carboprost, but only the derivatization procedure separates the 5-trans-isomer of carboprost. Possible reasons for the better separation using the derivatization procedure are discussed. Both procedures gave a coefficient of variation of approximately 1% for carboprost. The derivatization procedure gave a coefficient of variation of approximately 7% for the 15R-epimer and 5-trans-isomer when present at 2% of the carboprost level.

Carboprost↗
PubMed1992

Prophylactic and therapeutic carboprost tromethamine bladder irrigation in rats with cyclophosphamide-induced hemorrhagic cystitis.

Recently, prostaglandins have been shown to be effective agents for the treatment of cyclophosphamide-induced hemorrhagic cystitis. Among the prostaglandins studied is carboprost tromethamine, a PGF2a analog. To determine the effectiveness of carboprost tromethamine therapy on the urothelium, we induced hemorrhagic cystitis in 81 rats. These were divided into two treatment arms. One arm was treated prophylactically at the time of cyclophosphamide injection, and the other started treatment only after hemorrhagic cystitis was established. Animals were divided equally into groups receiving 0, 0.4, 0.8, and 1.6 mg.% carboprost tromethamine in 0.9% normal saline by continuous bladder irrigation. All bladders were examined grossly for edema and hemorrhage, then histologically for mucosal ulceration, congestion, and perivascular hemorrhage. Results from the prophylactic arm, as compared to those for controls, revealed that all groups except those treated only with 0.9% normal saline had a lower incidence of hemorrhagic cystitis (p less than 0.05). In the established hemorrhagic cystitis arm, the group treated with 1.6 mg.% carboprost tromethamine showed the best response (p less than 0.05), whereas the group treated with 0.9% normal saline showed the poorest response. This study reveals that hemorrhagic cystitis in the rat model may be prevented by prophylactic continuous bladder irrigation with carboprost tromethamine, whereas established hemorrhagic cystitis may be treated effectively with intravesical instillation of carboprost tromethamine. Although the mechanism of action of this prostaglandin on the urothelium is unknown, it appears grossly and histologically to decrease ulceration, perivascular hemorrhage, and congestion in the mucosa and submucosa.

Animals↗
PubMed1993

Treatment of cyclophosphamide-induced hemorrhagic cystitis with intravesical carboprost tromethamine.

We review our experience with 18 consecutive patients who received intravesical carboprost tromethamine, an F2-alpha prostaglandin, for severe hemorrhagic cystitis following cyclophosphamide chemotherapy. Of the patients 16 were given cyclophosphamide for conditioning before bone marrow transplantation and 2 received the drug as cytotoxic therapy alone (dose range 3.6 to 15.8 gm.). All patients had severe gross hematuria that was refractory to forced diuresis and to continuous saline bladder irrigation. The intravesical prostaglandin therapy was initiated only after significant transfusion requirements (greater than 1 unit packed red blood cells per day) and/or numerous catheter manipulations for relief of clot retention. Eligible patients underwent complete clot evacuation followed by intravesical instillation of 0.4 to 1.0 mg.% carboprost tromethamine for 2 hours 4 times per day, alternating with continuous saline bladder irrigation for 2 hours. Six patients attempted an alternate protocol of 0.8 to 1.0 mg.% carboprost tromethamine given by continuous saline bladder irrigation. Complete resolution of gross hematuria occurred in 9 patients (50%). Eight patients had a partial response, with decreased transfusion requirements noted. However, complete resolution ultimately required an alternative therapy (for example formalin or urinary diversion). One patient (6%) failed to respond and required formalin therapy on day 4 of carboprost tromethamine therapy. Decreased red blood cell transfusion requirements were noted during and after therapy when compared to pretreatment values. No changes in renal or bladder function were noted during the mean followup of 17 weeks (range 1 to 64 weeks). There were 3 cases of recurrent hematuria. Side effects were limited to bladder spasm in 14 of the 18 patients (78%), with no systemic complications. The results suggest that carboprost tromethamine is a useful bedside therapy for hemorrhagic cystitis due to cyclophosphamide, and treatment appears to have minimal toxicity.

Administration, Intravesical↗
PubMed1993

Carboprost trometamol in the management of the third stage of labor.

OBJECTIVE: To compare carboprost trometamol with methylergometrine in managing the third stage of labor. METHOD: One hundred and fifty parturient women were randomly assigned to use carboprost trometamol or methylergometrine immediately after delivery. RESULT: Both the duration of the third stage and the mean blood loss were significantly less in the carboprost group than the methergine group (P < 0.001). CONCLUSION: Carboprost trometamol is a more potent uterotonic drug than methylergometrine. Reducing blood loss in parturient women is very important especially in cases where there is the likelihood of anemia.

Adult↗
PubMed1995

Intravesicular carboprost for the treatment of hemorrhagic cystitis after marrow transplantation.

OBJECTIVES: To determine the minimal active dose and extent of activity of intravesicular carboprost for the treatment of hemorrhagic cystitis after marrow transplantation. METHODS: Twenty-four adults with grade 3 or 4 hemorrhagic cystitis were treated. All but 2 had failed other local therapy. Treatment was initiated at a median of 32 days post-transplant. Eleven patients received carboprost intravesicularly at 0.2 mg/dL for 60 minutes every 6 hours, and the dose was escalated every 24 hours until a dose of 1.0 mg/dL was reached unless a response was achieved. Thirteen additional patients were treated at an initial dose of 0.8 mg/dL, with escalation to 1.0 mg/dL after four doses in the absence of a response. RESULTS: Overall, 15 of the 24 patients responded. In the dose-escalation setting, 0.8 mg/dL was the minimal active dose. The total response rate was 62% with doses at or above 0.8 mg/dL and 18% at lower doses. All but one response occurred with 7 or fewer days of therapy, and 9 patients relapsed later. Four additional patients were salvaged following cystoscopy with clot evacuation with or without alum or formalin instillation. In all but 1 patient, bladder spasms developed during treatment with carboprost, but were not sufficiently severe to discontinue therapy. CONCLUSIONS: Intravesicular carboprost at 1.0 mg/dL every 6 hours for no more than 7 days should be considered for a randomized study for treatment of refractory hemorrhagic cystitis. Cystoscopic examination and evacuation of clots prior to therapy may be required to achieve the full benefit of this treatment.

Administration, Intravesical↗
PubMedDate not supplied

Second trimester pregnancy termination in primigravidas by double application of dinoprostone gel and intramuscular administration of carboprost tromethamine.

A randomized study of legal pregnancy termination in the second trimester has been performed in primigravidas by endocervical application of Prepidil gel (dinoprostone gel) in combination with intramuscular application of Prostin 15 M (carboprost tromethamine). The study comprised 97 patients. The control group (N = 35) included patients in whom pharmacologic preparation of the cervix was performed by a singleton endocervical application of 0.5 mg dinoprostone gel and intramuscular administration of Prostin 15 M (Carboprost Tromethamine) (1 ml/2 h) 10 h later and until abortion. The investigated group A (N = 31) underwent pharmacologic preparation of the cervix by endocervical application of 0.5 dinoprostone gel, 2 times during an interval of 4 hours. Intramuscular injection of Prostin 15 M (Carboprost Tromethamine) (1 ml/h) was administered 6 hours after the second application of gel and until abortion. The investigated group B (N = 31) underwent pharmacologic preparation of the cervix by a singleton double-dose endocervical application of 0.5 mg dinoprostone gel and intramuscular treatment by 1 ml/2 h of Prostin 15 M (Carboprost Tromethamine) applied 10 hours later and until abortion. On the basis of obtained results, a conclusion was made that the NEW combination of endocervical and intramuscular application of prostaglandins gives statistically significantly shortened abortion interval (the control group x = 9.97; SD = 5.22 versus investigation group: A-x = 6.80; SD = 4.31 and investigation group: B-x = 5.55; SD = 3.48). Better pharmacologic preparation of the uterine cervix resulted in shorter abortion interval and decreased amount of systemically applied prostaglandins. A shortened abortion interval significantly decreases the rate of immediate, early and late complications. A decreased amount of systemically applied prostaglandins results in significantly lower rate of unwanted side-effects caused by prostaglandins, making this method of pregnancy termination significantly cheaper.

Abortion, Induced↗
PubMed1990

Evaluation of carboprost tromethamine in the treatment of cyclophosphamide-induced hemorrhagic cystitis.

The treatment of cyclophosphamide-induced hemorrhagic cystitis has been difficult, with overall poor results using intensive and costly therapy. The authors evaluated the treatment of this problem in four patients with prostaglandin intravesical therapy. Each patient had failed to respond to conservative management. Carboprost tromethamine (Hemabate) was instilled into the bladder, with dwell times ranging from 45 to 60 minutes, three to four times a day for 4 to 5 days. Two of the patients required a second course with carboprost tromethamine at an increased concentration. A third patient's treatment was stopped after the first 5-day course because of intractable bladder spasms and persistent hematuria. In the three patients who completed the full course of therapy the hematuria resolved completely. The only side effect noted was bladder spasms, which were controlled in three of the four patients with oxybutynin chloride. This preliminary evaluation suggests that carboprost tromethamine may be a safe and effective bedside treatment of cyclophosphamide-induced hemorrhagic cystitis.

Adult↗
PubMed1984

High-performance liquid chromatographic determination of acid-catalyzed degradation products of methyl carboprost in a polymeric controlled-release device.

A normal-phase high-performance liquid chromatographic method was used for the determination of methyl carboprost and acid-catalyzed degradation products in a polymer-based, controlled release dosage form. A reversed-phase method was used to isolate sufficient quantities of the degradation products to determine their identity. Degradation of methyl carboprost under acidic conditions results in epimerization and dehydration, to several isomers, at the tertiary allylic hydroxyl group. Mass balance was 94% for a sample allowed to degrade 50%. These compounds were observed to form in the polymer-based, controlled release dosage form. For the determination of methyl carboprost in the dosage form, the method was found to be linear, precise with a relative standard deviation of 2% and to have an average recovery of 99.2%.

Carboprost↗
PubMed1990

Prophylactic intramyometrial carboprost tromethamine does not substantially reduce blood loss relative to intramyometrial oxytocin at routine cesarean section.

The influence of intramyometrial injection of 125 micrograms of 15-s-15-methyl prostaglandin F2 alpha (carboprost tromethamine, Prostin/15M) versus 20 U of oxytocin immediately after delivery of placenta on blood loss at cesarean section was investigated by means of a double-blinded, randomized trial. Hematocrit decrease from the day before operation to the third postoperative day was used as an index of blood loss. Decreases in hematocrit were comparable for the oxytocin and carboprost tromethamine groups. Excess blood loss (hematocrit decrease more than 6 vol. %) was significantly associated with the indication for cesarean section (three of four for cephalopelvic disproportion versus 9 of 42 others, p less than 0.01), but not with age, parity, number of prior cesarean sections, or birthweight. Carboprost tromethamine does not appear to be more effective than oxytocin when given by intramyometrial injection at this dose for routine cesarean section; its prophylactic utility in higher doses or in cases at risk for hemorrhage from uterine atony remains to be investigated.

Adult↗
PubMed2004

Use of carboprost to facilitate hysteroscopic resection of submucous myomas.

Ten women with submucous myomas that could not be completely resected hysteroscopically were treated with intracervical carboprost. This caused uterine contraction and extrusion of the unresectable intramural component into the endometrial cavity. Eleven of 13 myomas in these patients could then be completely resected. One intramural myoma extruded into the endometrial cavity after injection of carboprost and was also completely resected.

Adult↗
PubMed1999

Carboprost exposure in a newborn with recovery.

BACKGROUND: This case describes a newborn who was accidentally given carboprost (Hemabate) 250 micrograms intramuscularly, the largest amount ever reported in a normal newborn. CASE REPORT: A full-term newborn was inadvertently given carboprost rather than his prescribed hepatitis vaccine. Within 15 minutes, he was tachypneic and hypertensive followed by bronchospasms and dystonic movements and/or seizure activity of his upper extremities. He also was hyperthermic and had diarrhea stools. He recovered within 18 hours and was discharged. CONCLUSION: The manufacturer reports 2 infants who received lesser amounts and remained asymptomatic. This child exhibited symptoms associated with an overdose of a prostaglandin F2a, although complete recovery occurred within 18 hours.

Carboprost↗
PubMed1997

[Dose study of methyl carboprost suppository for planned delivery at term].

OBJECTIVE: To investigate clinical reasonable dose of methyl carboprost suppository (15-methyl-PGF2 alpha) for induction of labor. METHOD: A total of 150 gravidas with singleton pregnancy and cephalic presentation, accepted for induction of labor, were randomly allocated into 3 groups: group 1, 15-methyl-PGF2 alpha 0.100 mg (n = 50); group 2, 0.125 mg (n = 50); and group 3, 0.200 mg (n = 50). RESULTS: The success rates of induction were 90.0%, 94.0% and 100.0% for group 1, 2 and 3, respectively. As cervical Bishop score < or = 5, the cases needed oxytocin intravenous infusion during the active phase were 48.5%, 40.7% and 5.0%, respectively; cervical Bishop score > or = 6, the cases were 11.8%, 13.0% and 0.0%, respectively. There were 3 cases of precipitate delivery in group 2 and 3. No uterine hyperstimulation occurred in group 1 and 2, while 3 cases of uterine hyperstimulation in group 3. CONCLUSION: (1) A single maximum dose of 15 methyl-PGF2 alpha for term labor induction should be < 0.200 mg. (2) The different dose was chosen according to cervical Bishop score, i.e. 0.200 mg or 0.125 mg for Bishop score < or = 5, and 0.100 mg for Bishop score > or = 6.

Adult↗
PubMedDate not supplied

[Abortion in the 2d trimester using carboprost tromethamine].

The authors present their own experience (1980-1985) in the application (im. so called "monotone rhythm and doses") of Prostin 15-M (Upjohn) in legal abortions in the second trimester (14th-20th gestational weeks). This preparation was applied in 470 patients divided into 3 groups for the purpose of differential treatment and analysis: A--gravidae juvenae 13-18 years of age, B--gravidae adultae (19-40 years of age) C--gravidae vetustae 41-46 years of age. The mean age of patients by age groups was: A-16 years + 8 months; B-26 years + 3 months; C-42 years + 7 months. Indications for abortion were: medical in 53.83%, eugenic in 30.21%, medico-social in 14.25%, and ethico-legal in 1.70%. The percentage of primigravidae was 40.42 and of multigravidae 59.76%. The average length of the abortion interval and the average dose of Prostin 15-M (in ml) were as follows: group A 28 h 30' and 8.92 ml; group B 23 h 23' and 8.23 ml. and group C 16 h and 4.97 ml. All recorded side-effects and complications were analysed. Significant complications occurred in 5 cases (1.06%): cervical rupture in 3 cases and massive postabortal haemorrhage in 2 cases. No deaths occurred. The authors elaborated a system of the differential evaluation of the efficacy of this method and its advantages over other methods previously applied. The method has proved to be very simple, efficacious, suitable from the medico-clinical point of view, with a relatively low percentage of complications, and economical (costs of treatment and hospitalisation).

Abortion, Induced↗
PubMed1984

Menses induction in rhesus monkeys using a controlled-release vaginal delivery system containing (15S) 15-methyl prostaglandin F2 alpha methyl ester.

Polymeric controlled-release vaginal delivery systems were designed for (15S)15-methyl prostaglandin (PG)F2 alpha methyl ester (carboprost methyl). The drug was incorporated into a highly permeable reservoir membrane that was bound to a relatively nonpermeable support membrane. The rate of drug release was controlled by coating the reservoir membrane with a less permeable rate-controlling membrane. Vaginal devices were prepared with in vitro steady-state release rates from 5 to 180 microgram/hour. The release curves were characterized by an initial, transient rapid release of the drug, followed by a linear zero-order release phase. Pregnancy was terminated in rhesus monkeys following a 24-hour treatment with vaginal devices having release rates of carboprost methyl of 45 microgram/hour or greater. Successful menses induction was associated with peripheral plasma concentrations of (15S)15-methyl PGF2 alpha between 2000 and 3000 pg/ml. Peripheral plasma concentrations of progesterone declined very rapidly to less than 1.0 ng/ml in monkeys in which pregnancy was terminated. These studies demonstrate the feasibility of manufacturing controlled-release vaginal delivery systems containing carboprost methyl for use in early pregnancy termination.

Abortion, Induced↗
PubMed2005

Ovulatory response and embryo yield in Jakhrana goats following treatments with PMSG and FSH.

Superovulatory response and embryo production efficacy were investigated in adult (age 2-4 years, average body weight: 27-43 kg) cycling Jakhrana goats (n = 15) under semi-arid environmental conditions of India by administering different superovulatory regimens. Goats were reared under semi-intensive system of management in established farm conditions. To synchronize oestrus, a luteolytic dose of carboprost tromethamine (Upjohn, UK) was administered intramuscularly to all does at the dose rate of 5 microg per kg body weight in a double dose schedule with an interval of 11 days. For superovulation, 750 IU of PMSG (Folligon, Intervet, Boxmeer, Holland) per goat was administered intramuscularly 24 h before administering a second dose of luteolytic agent in five does (treatment 1). FSH (Sigma, St. Louis, MO, USA) 12.50 IU per goat was administered intramuscularly in a decreasing daily dose schedule (2.50, 2.50; 1.875, 1.875; 1.25, 1.25; 0.625, 0.625) at 12 h intervals over four days, initiated 48 h before administering second dose of carboprost tromethamine in 5 does (treatment 2). FSH (Super-Ov, Ausa Intern, USA) was administered at a uniform dose rate of 8.33 units per goat intramuscularly at 24 h intervals over three consecutive days (total dose was 25 units), initiated 48 h before administering a second dose of carboprost tromethamine in 5 does (treatment 3). To synchronize ovulation in responders, human chorionic gonadotrophin (hCG, Chorulon, Intervet) was injected intramuscularly at a dose rate of 500 IU in each goat on the day of oestrus appearance. Goats were laparotomized 72-82 h following the onset of synchronized oestrus and their genitalia were flushed using a standard collection procedure. Variability (p > 0.05) in superovulatory response (number of established corpora lutea) was observed: FSH (Sigma), 11.8 +/- 2.9; FSH (Super-Ov), 11.6 +/- 4.5; PMSG (Intervet), 8.4 +/- 2.3. A similar pattern was reflected in mean embryo and transferable embryo recovery, respectively (p > 0.05): FSH (Sigma), 8.0 +/- 1.8, 5.2 +/- 1.7; FSH (Super-Ov), 6.6 +/- 2.4, 5.4 +/- 2.4; PMSG, 5.8 +/- 1.9, 3.8 +/- 2.2. In PMSG-treated does, comparatively more unfertilized ova or retarded embryos were recovered than in FSH-treated does. The superiority of FSH preparations over PMSG was reflected in terms of total and transferable embryo production (p > 0.05). On average, five transferable embryos (excellent and good quality) were recovered per doe treated with FSH of either source. The mean ova/embryo recovery was satisfactory (55-68%). Results indicated that Jakhrana goats can be superovulated for embryo production using FSH of either source to augment productivity.

Animals↗