buprenorphine and Renal-Insufficiency

All health professionals should be aware of the importance of evaluating pain - fifth vital sign- in cancer patients. Peripheral and central acting analgesics are widely used to treat moderate to severe pain, particularly cancer pain. Many guidelines have addressed this issue. However, real life patients' have other problems and comorbidities that may raise doubts when prescribing.. Authors made a literature search, trying to clarify same specific situations: loss of oral route, renal impairment (hemodialysis), hepatic impairment, frequent opiod interactions and the availability of short-acting formulations.. The following medicines were included in this analysis: the natural opiates (morphine and codeine), their synthetic and semisynthetic derivatives (hydromorphone, oxycodone, and fentanyl), the partial agonist buprenorphine and finally tramadol and tapentadol. Transdermal systems are only available for buprenorphine and fentanyl. In hepatic impairment, fentanyl is safe, but with the exception of codeine and tramadol; other opioids should be used with caution. In renal failure: fentanyl, hydromorphone, and tapentadol are safe. Morphine should be avoided; other opioids should be used with caution. In hemodialysis, buprenorphine, fentanyl, hydromorphone and tramadol (at doses up to 200 mg/day) may be used.. Failure to recognize the impact of various situations described throughout this work, including the bioavailability due to loss of oral route, due to pharmacokinetics and pharmacodynamics of the various drugs, either in the context of the impaired metabolism or excretion, or in due to pharmacological interactions, conditions a serious risk of subtreatment of pain and consequent impact in terms of quality of life.. Opioid prescription is safe and effective, even in moderate to severe comorbidities such as renal and hepatic impairment and in patients with no oral route available. In this case, as when considering pharmacological interactions, an individualized therapeutic plan is the best solution and the patient should be assessed regularly. Unadjusted doses may relate to bad pain control and a higher prevalence of adverse events.. Introdução: A dor é equiparada a quinto sinal vital e deve ser avaliada de forma sistemática em todas as consultas de um paciente com cancro. Os fármacos utilizados na prática oncológica para tratar os doentes com dor crónica moderada a severa incluem analgésicos de ação periférica e central que têm sido abordados em múltiplas diretrizes nacionais e internacionais. No entanto, na prática clínica há que equacionar outros problemas e eventuais comorbilidades, que podem levantar dúvidas no momento da prescrição.Material e Métodos: Fez-se uma revisão da literatura, tentando refletir sobre algumas situações específicas na utilização de opióides, nomeadamente perda da via oral, insuficiência renal (hemodiálise), insuficiência hepática, interações medicamentosas e formulações de ação imediata.Resultados: Os opiáceos naturais (morfina e codeína) e os seus derivados sintéticos e semissintéticos (hidromorfona, oxicodona, fentanilo), o agonista parcial buprenorfina e finalmente o tramadol e tapentadol foram selecionados para esta análise. Os sistemas transdérmicos estão apenas disponíveis para a buprenorfina e o fentanilo. Na insuficiência hepática, o fentanilo foi considerado seguro, mascom exceção da codeína e do tramadol, podem todos ser usados com precaução. Na insuficiência renal, o fentanilo, a hidromorfona e o tapentadol foram considerados seguros. Deve evitar-se a morfina, e os restantes poderão ser usados com precaução. Em pacientes em hemodiálise pode usar-se buprenorfina, fentanilo, hidromorfona e tramadol (em doses até 200 mg/dia).Discussão: O não reconhecimento do impacto das várias situações descritas ao longo deste trabalho, nomeadamente a alteração da biodisponibilidade por perda de via oral, por alteração da farmacocinética e farmacodinâmica dos vários fármacos, quer no contexto da insuficiência de órgão responsável pelo metabolismo ou excreção, quer no contexto das interações farmacológicas, condiciona umnorme risco de subtratamento da dor e consequente impacto em termos de qualidade de vida.Conclusão: A prescrição de opióides é segura e efetiva, mesmo em situações de comorbilidades moderadas a graves como insuficiência renal e hepática e em doentes sem via oral disponível. Neste caso, como quando considerámos as interações farmacológicas, o plano terapêutico deve ser individualizado e o paciente deve ser avaliado regularmente. A seleção inadequada e/ou dose mal ajustada de um fármaco, o não reconhecimento do impacto dos efeitos adversos, frequente

Topics: Administration, Oral; Analgesics, Opioid; Buprenorphine; Cancer Pain; Codeine; Deglutition Disorders; Fentanyl; Humans; Hydromorphone; Liver Failure; Morphine; Oxycodone; Renal Dialysis; Renal Insufficiency; Tapentadol; Tramadol

Opioid abuse is a devastating, costly, and growing problem in the United States, and one for which treatment can be complicated by barriers such as access to care and legal issues. Only 12% to 15% of the opioid-dependent population is enrolled in methadone maintenance programs. A significant breakthrough occurred with passage of the Drug Addiction Treatment Act of 2000 (DATA 2000). For the first time in approximately 80 years, physicians could legally prescribe opioid medications for the treatment of opioid addiction. The opiate, so designated, was buprenorphine (Subutex).

Topics: Anesthesia; Buprenorphine; Humans; Naloxone; Narcotic Antagonists; Opioid-Related Disorders; Renal Insufficiency

Buprenorphine was not used widely in clinical practice over many years, mainly due to analgesic potency and clinical safety concerns based on misinterpreted animal data. Contrary to previous concerns, however, no analgesic ceiling effect and no antagonism of combined pure mu-opioid receptor agonists is seen within the therapeutic dose range. In recent studies, buprenorphine could be effectively and safely combined with full mu-agonists, and switching between buprenorphine and another opioid provided comparable pain relief based on equianalgesic doses. Moreover, buprenorphine exerts an antihyperalgesic effect, which is due -- at least in part -- to antagonistic activity at kappa-opioid receptors. Buprenorphine pharmacokinetics are not altered by advanced age or renal dysfunction. In addition, the risk of respiratory depression is lower than with other opioids including morphine, hydromorphone, methadone and fentanyl. Unlike morphine and fentanyl, there is no immunosuppressive activity with buprenorphine at therapeutic analgesic doses. Transdermal buprenorphine has significantly improved the clinical use of the drug, providing continuous buprenorphine release for up to 96 h. In clinical trials, patients receiving transdermal buprenorphine experienced significantly greater pain relief, better sleep, and a reduced need for rescue therapy, compared to placebo. Large-scale post-marketing studies have confirmed the effectiveness of transdermal buprenorphine in treating moderate-to-severe cancer and non-cancer pain including neuropathic syndromes. Finally, the comparably low incidence of CNS adverse events and constipation, and the possibility of use in severe renal dysfunction without a need for dose adjustment make buprenorphine well suited for chronic pain management in at-risk patients, such as diabetics, elderly or renally impaired individuals including those requiring haemodialysis.

Topics: Administration, Cutaneous; Analgesics, Opioid; Buprenorphine; Central Nervous System; Drug Interactions; Humans; Pain, Intractable; Receptors, Opioid; Renal Insufficiency; Treatment Outcome