Search results for "Pharmacokinetics"
showing 10 items of 458 documents
Pharmacokinetics of Intravitreal Anti-VEGF Drugs in Age-Related Macular Degeneration
2019
Intravitreal administration of anti-vascular endothelial growth factor (VEGF) antibodies has become the standard treatment for Age-Related Macular Degeneration; however, the knowledge of their pharmacokinetics is limited. A comprehensive review of the preclinical and clinical pharmacokinetic data that were obtained in different studies with intravitreal bevacizumab, ranibizumab, and aflibercept has been conducted. Moreover, the factors that can influence the vitreous pharmacokinetics of these drugs, as well as the methods that were used in the studies for analytical determination, have been exposed. These anti-VEGF drugs present different charge and molecular weights, which play an importan…
A multicenter phase 1 study of solitomab (MT110, AMG 110), a bispecific EpCAM/CD3 T-cell engager (BiTE®) antibody construct, in patients with refract…
2018
ABSTRACT We assessed the tolerability and antitumor activity of solitomab, a bispecific T-cell engager (BiTE®) antibody construct targeting epithelial cell adhesion molecule (EpCAM). Patients with relapsed/refractory solid tumors not amenable to standard therapy received solitomab as continuous IV infusion in a phase 1 dose-escalation study with six different dosing schedules. The primary endpoint was frequency and severity of adverse events (AEs). Secondary endpoints included pharmacokinetics, pharmacodynamics, immunogenicity, and antitumor activity. Sixty-five patients received solitomab at doses between 1 and 96 µg/day for ≥28 days. Fifteen patients had dose-limiting toxicities (DLTs): e…
Bone targeting compounds for radiotherapy and imaging: *Me(III)-DOTA conjugates of bisphosphonic acid, pamidronic acid and zoledronic acid
2016
Background Bisphosphonates have a high adsorption on calcified tissues and are commonly used in the treatment of bone disorder diseases. Conjugates of bisphosphonates with macrocyclic chelators open new possibilities in bone targeted radionuclide imaging and therapy. Subsequent to positron emission tomography (PET) examinations utilizing 68Ga-labelled analogues, endoradiotheraphy with 177Lu-labelled macrocyclic bisphosphonates may have a great potential in the treatment of painful skeletal metastases. Methods Based on the established pharmaceuticals pamidronate and zoledronate two new DOTA-α-OH-bisphosphonates, DOTAPAM and DOTAZOL(MM1.MZ) were successfully synthesized. The ligands were labe…
Distribution and depletion of sulfadiazine after a multiple per os dosing in gilthead sea bream (Sparus aurata) fed two different diets
2013
The distribution and depletion profile of sulfadiazine (SDZ) were investigated in gilthead sea bream (Sparus aurata) fed on fish oil (FO) or plant oil-based (PO) diets. Fish averaging 230 g were given medicated feed containing 25 mg SDZ kg-1 fish for 5 days at 24-26°C. Blood and muscle plus skin were sampled on days 1, 3, 5, 6, 8 and 9. Differences in plasma and fillet SDZ levels between the two groups were statistically insignificant. The maximum drug concentrations in plasma were 3.2 ± 1.9 μg mL-1 and 2.9 ± 1.2 μg mL-1 in the PO and FO groups, respectively. In post-medicated samples depletion rapidly reached concentrations close to the level of quantification at 72 h post medication. With…
Essential Oil Composition of Alluaudia procera and in Vitro Biological Activity on Two Drug-Resistant Models
2019
Drug resistance is a major obstacle in antibiotic and antitumor chemotherapy. In response to the necessity to find new therapeutic strategies, plant secondary metabolites including essential oils (EOs) may represent one of the best sources. EOs in plants act as constitutive defenses against biotic and abiotic stress, and they play an important role in the pharmacology for their low toxicity, good pharmacokinetic and multitarget activity. In this context, natural products such as EOs are one of the most important sources of drugs used in pharmaceutical therapeutics. The aim of this paper was to identify the chemical composition of the essential oil of Alluaudia procera leaves, obtained by hy…
Accumulation and Adverse Effects of Metoprolol and Propranolol After Concurrent Administration of Cimetidine
1983
Pharmacokinetics of metoprolol, propranolol and atenolol were investigated in six healthy volunteers following 7 days of oral monotherapy with these drugs and after 7 days concurrent administration of each of these betareceptor antagonists with cimetidine. Application of cimetidine did not lead to any interaction with atenolol, whereas mean peak plasma levels of metoprolol were increased by 70%, and those of propranolol by 95% due to concurrent administration of cimetidine (p < 0.05). The AUC of the two last mentioned beta blockers behaved similarly (p < 0.05). Measurement of exercise-induced tachycardia on the 6th day of administration showed no differences between monotherapy with the bet…
Effect of aging on pain relief in the older cancer patients: pharmacokinetic and pharmacodynamic aspects.
2016
The prevalence of cancer rises with advancing age. A large number of cancer patients are aged over 65 years, and it is expected that even more patients will develop cancer as a consequence of the g...
Serum Levels of Sulpiride Enantiomers after Oral Treatment with Racemic Sulpiride in Psychiatric Patients: a Pilot Study1
2001
Sulpiride (SULP), a substituted benzamide with high selectivity for D 2 -like dopamine receptors, has a chiral structure and is used in most countries as the racemate. In an open pilot study, we investigated 26 inpatients (13 female, 13 male) with schizophrenic or depressive disorder treated with SULP (mean daily dosage 64-1062 mg) administered orally, either as a monotherapy or as an add-on treatment to a stable and unchanged medication for 3-60 days. Serum levels of total SULP and of its enantiomers were measured by high-performance liquid chromatography (HPLC) procedures. Clinically relevant indicators of hepatic and renal function as well as retrospectively assessed clinical outcome par…
Clinical management of drug-drug interactions in HCV therapy: Challenges and solutions.
2013
Contains fulltext : 118153.pdf (Publisher’s version ) (Open Access) Hepatitis C virus (HCV) infected patients often take multiple co-medications to treat adverse events related to HCV therapy, or to manage other co-morbidities. Drug-drug interactions associated with this polypharmacy are relatively new to the field of HCV pharmacotherapy. With the advent of the direct-acting antivirals telaprevir and boceprevir, which are both substrates and inhibitors of the cytochrome P450 (CYP) 3A iso-enzyme, knowledge and awareness of drug-drug interactions have become a cornerstone in the evaluation of patients starting and continuing HCV combination therapy. In our opinion, an overview of conducted dr…
Does the Intrapelvic Compartment Syndrome Exist?
1998
Pelvic compartment syndrome is a rare condition. As in other musculoskeletal localizations, the intra-compartmental pressure raises above a critical level. In the pelvic compartment syndromes, the gluteal compartments are mainly concerned. We report on three patients with bilateral ureteral obstruction, due to compression by a massive retroperitoneal haematoma as a complication of an unstable pelvic ring or acetabular fracture. Anuria with renal organ failure, due to compression of the ureters in the small true pelvis represents an intrapelvic compartment syndrome. Anuria, due to ureteral compression, mostly developing 24 to 48 hours after injury, has to be differentiated from anuria due to…