Database : HANSEN
Search on : INTERACOES DE MEDICAMENTOS [Subject descriptor]
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Id:18426
Author:Teo, Steve K; Colburn, Wayne A; Tracewell, William G; Kook, Karin A; Stirling, David I; Jaworsky, Markian S; Scheffer, Michael A; Thomas, Steve D; Laskin, Oscar L
Title:Clinical pharmacokinetics of thalidomide ..-
Source:s.l; s.n; 2004. 17 p. ilus, tab, graf.
Abstract:Thalidomide is a racemic glutamic acid derivative approved in the US for erythema nodosum leprosum, a complication of leprosy. In addition, its use in various inflammatory and oncologic conditions in being investigated. Thalidomide interconverts between the (R)- and (S)-enantiomers in plasma, with protein binding of 55% and 65%, respectively. More than 90% of the absorbed drug is excreted in the urine and faeces within 48 hours. Thalidomide is minimally metabolised by the liver, but is spontaneously hydrolysed into numerous renally excreted products. After a single oral dose of thalidomide 200mg (as the US-approved capsule formulation) in healthy volunteers, absorption is slow and extensive, resulting in a peak concentration (Cmax) of 1-2mg/L at 3-4 hours after administration, absorption lag time of 30 minutes, total exposure (AUCoo) of 18mg - h/L, apparent elimination half-life of 6 hours and apparent systemic clearence of 10 L/H. Thalidomide pharmacokinetics are best described by a one-comportment model with first-order absorption and elimination. Because of the low solubility of the drug in the gastrointestinal tract, thalidomide exhibits absorption rate-limited pharmacolinetics (the 'flip-flop' phenomenon), with its elimination rate being faster than in absorption rate. The apparent elimination half-life of 6 hours therefore represents absorption, not elimination. The 'true' apparent volume of distribution was estimated to be 16L by use of the faster elimination-rate half-life. Multiple doses of thalidomide 200 mg/day over 21 days cause no change in the pharmacokinetics, with a steady-state Cmax (Cssmax) of 1.2 mg/L. Simulation of 400 and 800 mg/day also shows no accululation, with Css of 3.5 and 6.0 mg/L, respectively. Multiple-dose studies in cancer patients show pharmacokinetics comparable with those in healthy populations at similar dosages. Thalidomide exhibits a dose-proportional increase in AUC at doses from 50 to 400mg. Because of the low solubility of thalidomide Cmax is less than proportional to dose, and tmax is prolonged with increasing dose. Age, sex and smoking have no effect on the pharmacokinetics of thalidomide, and the effect of food is minimal. Thalidomide does not alter the pharmacokinetics of oral contraceptives, and is also unlikely to interact with warfarin and grapefruit juice. Since thalidomide is mainly hydrolysed and passively excreted, its pharmacokonetics are not expected to change in patients with impaired liver...(AU).
Descriptors:TALIDOMIDA/admin
TALIDOMIDA/sint quim
TALIDOMIDA/contra
TALIDOMIDA/hist
TALIDOMIDA/isol
TALIDOMIDA/farmacocin
TALIDOMIDA/normas
TALIDOMIDA/tox
TALIDOMIDA/uso terap
TALIDOMIDA/metab
ERITEMA NODOSO HANSENICO/quimioter
 ERITEMA NODOSO/etiol
 SINDROME DE IMUNODEFICIÊNCIA ADQUIRIDA FELINA/terap
 ADMINISTRACAO ORAL
 INTERACOES DE MEDICAMENTOS/fisiol
 RIFAMPINA/antag
 FENOBARBITAL/antag
 CIMETIDINA/antag
 DILTIAZEM/antag
 WARFARIN/antag
Limits:HUMANO
Location:BR191.1; 00948/s


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Id:13728
Author:DeRossi, Scott S; Hersh, Elliot V
Title:Antibiotics and oral contraceptives ..-
Source:s.l; s.n; 2002. 7 p. ilus, graf.
Abstract:With the exception of rifampin-like drugs, there is a lack of scientific evidence supporting the ability of commonly prescribed antibiotics, including all those routinely employed in outpatient dentistry, to either reduce blood levels and/or the effectiveness of oral contraceptives. To date, all clinical trials studying the effects of concomitant antibiotic therapy (with the exception of rifampin and rifabutin) have failed to demonstrate an interaction. Like all drugs, oral contraceptives are not 100 per cent effective with the failure rate in the typical United States population reported to be as high as 3 per cent. It is thus possible that the case reports of unintended pregnancies during antibiotic therapy may simply represent the normal failure rate of these drugs. Considering that both drug classes are prescribed frequently to women of childbearing potential, one would expect a much higher rate of oral contraceptive failure in this group of patients if a true drug:drug interaction existed. On the other hand, if the interaction does exist but is a relatively rare event, occurring in, say, 1 in 5000 women, clinical studies such as those described in this article would not detect the interaction. The pharmacokinetic studies of simultaneous antibiotic and oral contraceptive ingestion, and the retrospective studies of pregnancy rates among oral contraceptive users exposed to antibiotics, all suffer from one potential common weakness, i.e., their relatively small sample size. Sample sizes in the pharmacokinetic trials ranged from 7 to 24 participants, whereas the largest retrospective study of pregnancy rates still evaluated less than 800 total contraceptive users. Still, the incidence of such a rare interaction would not differ from the accepted normal failure rate of oral contraceptive therapy. The medico-legal ramifications of what looks like at best a rare interaction remains somewhat "murky." On one hand, we have medico-legal experts advising the profession to exercise caution and warn all oral contraceptive users of a potential reduction in efficacy during antibiotic therapy. These opinions are not evidence-based and rely heavily on one or two legal proceedings that cannot even be substantiated. On the other hand, there is one recently published legal proceeding in which the outcome was in favor of the oral surgeon. There is clearly...(AU).
Descriptors:VIES (EPIDEMIOLOGIA)
DISPONIBILIDADE BIOLOGICA
ANTIBIOTICOS/farmacocin
ANTIBIOTICOS/uso terap
ESTUDOS RETROSPECTIVOS
ABSORCAO INTESTINAL/ef drogas
RIFABUTINA/uso terap
RIFAMPINA/uso terap
ANTICONCEPCIONAIS ORAIS/antag
ANTICONCEPCIONAIS ORAIS/farmacocin
ANTICONCEPCIONAIS ORAIS/uso terap
INTERACOES DE MEDICAMENTOS
 ENSAIOS CLINICOS
 JURISPRUDÊNCIA
 TAMANHO DA AMOSTRA
Limits:HUMANO
FEMININO
GRAVIDEZ
Electronic Medium:http://www.ilsl.br
Location:BR191.1; 09018/s


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Id:13195
Author:George, Joseph; Balakrishnan, S; Bhatia, V. N
Title:Drug interaction during multidrug regimens for treatment of leprosy ..-
Source:s.l; s.n; feb. 1988. 6 p. tab.
Abstract:The influence of concurrently rifampicin and clofazimine on the metabolism of 4,4'-diaminodiphenyl sulfone (dapsone, DDS) has been studied in 30 subjects on multidrug regimens for treatment of leprosy. Plasma and urinary levels of drugs were determined on days 2,8 and 15 after administration of the drug, while cretinine levels in urine were also determined to overcome the effect of diuresis. During concurrent administration of rifampicin the plasma levels of DDS gradually fell from day 2 to day 15 of rifampicin administration and the decrease was most significant on day 15. Clofazimine did not exert any such influence on DDS metabolism. A comparison of urine and plasma levels of DDS during the course of treatment. The findings suggest that during concurrent administration of DDS and rifampicin, the intake of DDS shoud be regular and uninterrupted.(AU).
Descriptors:HANSENIASE/quimioter
QUIMIOTERAPIA COMBINADA
ESQUEMA DE MEDICACAO
DAPSONA/admin
DAPSONA/metab
INTERACOES DE MEDICAMENTOS
CLOFAZIMINA/uso terapeutico
RIFAMPINA/uso terapeutico
Limits:HUMANO
SUPPORT, NON-U.S. GOV'T
Electronic Medium:http://www.ilsl.br
Location:BR191.1; 02088/s


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Id:9449
Author:Garrelts, James C
Title:Clofazimine: a review of its use in leprosy and Mycobacterium avium complex infection ..-
Source:s.l; s.n; 1991. 7 p. ilus, tab.
Descriptors:SINDROME DE IMUNODEFICIENCIA ADQUIRIDA
CLOFAZIMINA
CLOFAZIMINA
INTERAÇOES DE MEDICAMENTOS
GASTROENTEROPATIAS
HANSENIASE
HANSENIASE
DERMATOPATIAS
INFECÇAO POR MYCOBACTERIUM AVIUM-INTRACELLULARE
INFECÇAO POR MYCOBACTERIUM AVIUM-INTRACELLULARE
Location:BR191.1; 06311/s


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Id:8368
Author:Joshi, J. V; Maitra, A; Sankolli, G; Bhatki, S; Joshi, U. M
Title:Norethisterone and ethinyl estradiol kinetics during dapsone therapy ..-
Source:s.l; s.n; 1984. 3 p. tab, graf.
Descriptors:DAPSONA
INTERAÇOES DE MEDICAMENTOS
ETINIL ESTRADIOL
ETINIL ESTRADIOL
HANSENIASE
NORETINDRONA
NORETINDRONA
NORETINDRONA
Location:BR191.1; 02415/s


  6 / 6 HANSEN  
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Id:7644
Author:Fader, Darrel J; Johnson, Timothy M
Title:Medical issues and emergencies in the dermatology office ..-
Source:s.l; s.n; 1997. 16 p. ilus, tab.
Abstract:We review the medical issues and emergencies potentially encountered in the practice of general or surgical dermatology. Traditional guidelines have largely consisted of dated extrapolations from the nondermatologic literature concerning procedures that are primarily irrelevant to dermatology. This article outlines a rational approach to organizing an office emergency plan for anaphylaxis, stroke, status epilepticus, myocardial infarction, and hypertensive crisis. We discuss the literature that has influenced current office behavior regarding endocarditis prophylaxis, the use of electrosurgery with pacemakers, arrhythmogenic drug interactions, vasovagal syncope, lidocaine "allergy," and bleeding complications from oral anticoagulants. Recommendations for managing these issues in a dermatologic context are provided..
Descriptors:ANTICOAGULANTES/efeitos adversos
TRANSTORNOS CEREBROVASCULARES/terapia
DERMATOLOGIA
DOENCA
INTERACOES DE MEDICAMENTOS
HIPERSENSIBILIDADE A DROGAS/etiologia
HIPERSENSIBILIDADE A DROGAS/terapia
ELETROCIRURGIA/efeitos adversos
EMERGENCIAS
SERVICOS MEDICOS DE EMERGENCIA
ENDOCARDITE BACTERIANA/prevenção e controle
DIRETRIZES
HEMORRAGIA/terapia
HIPERTENSAO/terapia
LIDOCAINA/efeitos adversos
INFARTO DO MIOCARDIO/terapia
MARCA-PASSO ARTIFICIAL
CONSULTORIOS MEDICOS
DERMATOPATIAS/cirurgia
DERMATOPATIAS/terapia
ESTADO EPILEPTICO/terapia
SINCOPE/terapia
Limits:HUMANO
Location:BR191.1; 0194/cme



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