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Journal of Pharmaceutical Sciences Mar 1986The absolute bioavailability and pharmacokinetic parameters of two methylprednisolone formulations (methylprednisolone sodium succinate and methylprednisolone acetate)...
The absolute bioavailability and pharmacokinetic parameters of two methylprednisolone formulations (methylprednisolone sodium succinate and methylprednisolone acetate) were determined in five dogs. Plasma concentrations of methylprednisolone, methylprednisolone sodium succinate, and methylprednisolone acetate were measured by sensitive and specific high-performance liquid chromatographic methods. After intravenous methylprednisolone sodium succinate administration, methylprednisolone was released rapidly but the extent of availability was rather low (43.6%). This has been tentatively explained in terms of its subsequent single-pass metabolism in the liver, i.e., hepatic hydrolysis of methylprednisolone sodium succinate followed by immediate hepatic elimination of the released methylprednisolone. After intramuscular administration of methylprednisolone acetate, its absorption was slow (half-time of absorption, 69.04 h) and the availability of the released methylprednisolone was low (42.7%). Therapeutic implications of these results are discussed, especially those which are relevant to shock therapy.
Topics: Animals; Biological Availability; Dogs; Half-Life; Injections, Intramuscular; Injections, Intravenous; Kinetics; Male; Methylprednisolone; Methylprednisolone Acetate; Methylprednisolone Hemisuccinate; Models, Biological
PubMed: 3517294
DOI: 10.1002/jps.2600750309 -
Journal of Pharmacokinetics and... Dec 1983This study was conducted to evaluate the influence of route of administration upon the bioavailability and pharmacokinetics of methylprednisolone sodium succinate....
This study was conducted to evaluate the influence of route of administration upon the bioavailability and pharmacokinetics of methylprednisolone sodium succinate. Fourteen healthy adult male volunteers received 40 mg doses of methylprednisolone as the following treatments after an overnight fast in a 4-way crossover design: (a) as a 1 ml i.v. bolus; (b) as a 1 ml i.m. injection; (c) administered as an oral solution; and (d) as 5 X 8 mg oral tablets. Both the ester and free methylprednisolone were determined in plasma and urine. Study results indicate that the ester is rapidly and extensively converted to free methylprednisolone after all routes. The extent of methylprednisolone absorption was equivalent after i.v. and i.m. administration. Both orally administered treatments resulted in a lower extent of absorption attributed to a first-pass effect. Although a slightly lower extent of absorption was demonstrated following the oral administration of the methylprednisolone sodium succinate solution relative to the methylprednisolone oral tablets, this average difference of 9% would probably be of minimal therapeutic importance.
Topics: Absorption; Administration, Oral; Adult; Biological Availability; Humans; Injections, Intramuscular; Injections, Intravenous; Kinetics; Male; Methylprednisolone
PubMed: 6678310
DOI: 10.1007/BF01059057 -
The Journal of Neuroscience Nursing :... Aug 1992Treatment with high-dose intravenous methylprednisolone is safe and may be associated with significant neurologic improvement in acute spinal cord injury patients....
Treatment with high-dose intravenous methylprednisolone is safe and may be associated with significant neurologic improvement in acute spinal cord injury patients. Accurate calculation and administration of the prescribed therapy and identification and assessment of complications should be incorporated into the overall standard of care for the acute spinal cord injury patient.
Topics: Acute Disease; Humans; Infusions, Intravenous; Injections, Intravenous; Methylprednisolone; Spinal Cord Injuries
PubMed: 1517672
DOI: 10.1097/01376517-199208000-00012 -
Lancet (London, England) Mar 1977
Topics: Drug Evaluation; Humans; Infusions, Parenteral; Injections, Intravenous; Methylprednisolone
PubMed: 66434
DOI: No ID Found -
Bulletin of Experimental Biology and... Apr 2023We studied the neuroprotective effect of local application of methylprednisolone in combination with a block copolymer after contusion spinal cord injury in rats....
We studied the neuroprotective effect of local application of methylprednisolone in combination with a block copolymer after contusion spinal cord injury in rats. Histological analysis of the spinal cord showed that delivery of a complex of methylprednisolone with a block copolymer reduced the volume of white and gray matter lesions. An increase in the amplitude of the evoked response of the gastrocnemius muscle was observed during epidural stimulation of the spinal cord 6 h after the injury. The maximum amplitude of the muscle response was greater in the group with local delivery of the methylprednisolone complex with the polymer 72 h after the injury. The obtained results demonstrate the neuroprotective effect of the local administration of the complex and allow to make positive prognosis for the recovery of the sensorimotor functions in rats.
Topics: Rats; Animals; Methylprednisolone; Neuroprotective Agents; Spinal Cord; Spinal Cord Injuries; Contusions
PubMed: 37160795
DOI: 10.1007/s10517-023-05795-1 -
Annals of Internal Medicine Aug 1983
Topics: Adult; Female; Humans; Methylprednisolone; Peritonitis
PubMed: 6881794
DOI: 10.7326/0003-4819-99-2-282_1 -
Zeitschrift Fur Arztliche Fortbildung Nov 1994
Review
Topics: Dose-Response Relationship, Drug; Humans; Methylprednisolone; Receptors, Glucocorticoid; Rheumatic Diseases
PubMed: 7839711
DOI: No ID Found -
Annals of the Rheumatic Diseases Oct 2022
Topics: Antibodies, Monoclonal, Humanized; Humans; Methylprednisolone; COVID-19 Drug Treatment
PubMed: 32816700
DOI: 10.1136/annrheumdis-2020-218788 -
Pharmaceutical Research Aug 1988The pharmacokinetics of methylprednisolone and two methylprednisolone esters, the phosphate and the hemisuccinate, were investigated after intravenous administration of... (Comparative Study)
Comparative Study
The pharmacokinetics of methylprednisolone and two methylprednisolone esters, the phosphate and the hemisuccinate, were investigated after intravenous administration of the esters to 12 healthy male subjects in two different doses (250 and 1000 mg). Methylprednisolone was formed more rapidly from phosphate than from hemisuccinate. During the first 30 min methylprednisolone levels were three to four times higher after phosphate administration than after hemisuccinate. The mean residence time of the hemisuccinate was significantly longer and the total-body clearance lower than those of the phosphate. Whereas very little of the phosphate (mean, 1.7%) was eliminated unchanged into the urine, there were significant amounts of hemisuccinate (mean, 14.7%) excreted renally and therefore not bioavailable. Methylprednisolone saliva levels paralleled plasma levels; the average saliva/plasma ratio was 0.22. Neither phosphate nor hemisuccinate could be detected in saliva. An average of 7.2% of the administered dose was eliminated in the form of methylprednisolone in urine. Renal clearance was 24 ml/min and not dose or prodrug dependent. For both doses endogenous hydrocortisone levels were lowered after 24 hr. For the 1000-mg dose the depression was still significant after 48 hr. The results indicate that methylprednisolone phosphate results in a faster and more efficient conversion to its active form, methylprednisolone, than methylprednisolone hemisuccinate.
Topics: Adolescent; Adult; Humans; Hydrocortisone; Male; Methylprednisolone; Methylprednisolone Hemisuccinate; Saliva
PubMed: 3072558
DOI: 10.1023/a:1015921408870 -
Archives of Neurology Dec 1985Corticosteroids have been useful in the management of myasthenia gravis (MG), but their efficacy has been limited by the slow onset of improvement, initial worsening of...
Corticosteroids have been useful in the management of myasthenia gravis (MG), but their efficacy has been limited by the slow onset of improvement, initial worsening of MG, refractoriness of some patients, and side effects of large daily doses. High-dose intravenous methylprednisolone pulses have been reported to produce rapid improvement in several immunologic disorders. In this study we administered 2 g of methylprednisolone intravenously every five days to 15 consecutive patients who had exacerbation of generalized MG. Satisfactory improvement occurred in ten of 15 patients after two courses and in two of five patients after a third course. Onset of improvement began a mean (+/- SD) of 3 +/- 1.1 days after the first infusion, 2.1 +/- 1 days after the second, and 2.4 +/- 1 days after the third, and reached its maximum level 8.9 +/- 6.1 days after the last infusion. A decrease in strength occurred in three patients 1.43 +/- 1.30 days after each infusion, was not marked, and lasted three days, following which improvement generally occurred. Side effects were minimal. After improvement, a daily dose of prednisone (30 mg) was used to maintain improvement. Use of pulse therapy at five-day intervals for the management of severe MG seems to have an advantage in that it produces less initial worsening and more rapid improvement in MG, enabling smaller daily maintenance doses to be employed, with fewer side effects.
Topics: Adult; Aged; Female; Humans; Infusions, Parenteral; Male; Methylprednisolone; Middle Aged; Myasthenia Gravis
PubMed: 4062612
DOI: 10.1001/archneur.1985.04060110031011