Buprenorphine Buprenorfin adalah suatu derivat semisintetik dari morfin alkaloid, thebaine, dengan derajat lipofilik yang tinggi

, dan merupakan agonis opioida parsial pada reseptor opioida µ dalam sistem saraf, dan juga antagonis reseptor opioida k (kappa). Aktivitas agonis intrinsiknya rendah, hanya mengaktifkan sebagian reseptor opioida µ, oleh sebab itu efek maksimal yang dapat dihasilkan ibuprenorfin akan selalu lebih ringan dibandingkan agonis opioida penuh seperti heroin, morfin dan metadon. Buprenorfin memiliki afinitas tinggi terhadap reseptor opioida µ, berikatan dengan reseptor ini lebih kuat daripada agonis opioida penuh. Buprenorfin juga memiliki afinitas tinggi dan memiliki sifat antagonis pada reseptor k, sehingga pada keadaan tertentu buprenorfin dosis tinggi dapat menimbulkan sindrom putus obat opioida (opioida withdrawal syndrome) dengan gejala dan tanda yang serupa secara kualitatif tetapi tidak sama secara kuantitatif dibandingkan akibat antagonis penuh seperti nalokson atau naltrekson. Profil farmakologis yang unik ini membuat buprenorfin memberikan beberapa keuntungan dibandingkan terapi gabungan agonis – antagonis yang digunakan dalam terapi ketergantungan opioida. Keuntungan ini antara lain indeks keamanan yang lebih besar terhadap terjadinya depresi pernafasan, tanda otonom dari putus obat opioida yang lebih ringan, dan efek psikomimetik atau disforik yang lebih ringan. Dengan efek respon opioida ganda maka ketika menghambat efek

dan risiko overdosis Kombinasi tersebut dapat membahayakan.e. morphine. Penekanan khusus harus diberikan untuk menilai tingkat neuroadaptasi terhadap opioida. benzodiazepin atau antidepresi. gangguan motorik dan kognitif. buprenorphine yields those same effects.. but with less intensity than heroin. By stimulating the receptor only partially. khususnya obat sedatif seperti alkohol. buprenorfin juga mengurangi penggunaan heroin sendiri.When the mu receptor is stimulated. Buprenorphine is a partial agonist at (i. all of which stimulate the receptor fully (Johnson and . it sets in motion a chain of nerve cell activities that underlies most of the familiar opioid effects. pain reduction. feelings of wellbeing or pleasure. stimulator of ) the mu receptor.penggunaan heroin sampingan. depresi saluran pernapasan. pada keadaan yang menggunakan obat sedatif lain secara terus menerus. bahkan overdosis yang berujung pada kematian. for example. meliputi efek sedative. and respiratory suppression. Semua terapi substitusi opioida harus dipertimbangkan dengan hati-hati pada individu yang menggunakan obat-obat lainnya. or methadone.

the abrupt stripping of the other opioid from the mu receptor can precipitate withdrawal. and when he or she last administered an abused opioid. the medication will block it from reaching the receptors and producing the desired strong effects. While buprenorphine’s manner of interacting with the mu receptor gives rise to its most important attributes and advantages in addiction treatment. Pevnick. more so than abused opioids and methadone do. •Buprenorphine has high affinity for the mu receptor. the patient’s level of physical dependence. if buprenorphine is given to an individual who has already taken another opioid.That is. the medication also has a significant action at a second receptor: .This characteristic probably accounts for buprenorphine’s long duration of action in the treatment of opioid dependence. Whereas those drugs can cause powerful euphoria. 1994).Strain. if a patient takes an abused opioid on top of buprenorphine. buprenorphine binds tightly to mu receptors. buprenorphine provides a positive but moderate psychoactive effect that reduces craving and helps patients comply with their medication regimens (Jasinski. This effect necessitates care when a clinician initiates buprenorphine therapy. Consequently. Walsh et al. and Griffith. Moreover. it displaces the other opioid from the receptors. 1978. motivating continued abuse.. 1999). depending on the dosage of buprenorphine. •Buprenorphine disassociates (detaches) from the mu opioid receptor slowly.

prevents stimulation) of the kappa opioid receptor(Cowan. 1977).. 1988. Mendelson and Jones. and Macfarlane. and Liebson. such as chronic depression. Pickworth et al.g. Both tablets produce similar clinical effects when administered sublingually (Stoller et al. Lewis.. however.. Preston. Singh et al. 1999. when injected by an opioid-addicted person. 1993. 1998. 2000) There are two formulations of buprenorphine for treating opioid dependence.e. 1997) and has been abused in other countries (O’Connor et al.. and Liebson.. Suboxone was developed because buprenorphine alone has potential for abuse (e. Preston. 2003. 1992. Bigelow. buprenorphine may induce positive mood and feelings of wellbeing (Rothman et al. 1996. 1988).. 1990). Varescon et al. By attaching to the kappa receptor and slowing its activity. 2001). a buprenorphine hydrochloride (HCl) tablet (Subutex) and a combination tablet (Suboxone) containing buprenorphine HCl plus naloxone HCl in a ratio of 4:1 (Fudala et al. Bigelow. 1997b.. 2002). Unlike buprenorphine. Mendelson et al....• Buprenorphine is an antagonist (i. naloxone is poorly absorbed and has little effect when taken sublingually (Chiang and Hawks. 2003. Strain et al.. naloxone can precipitate an opioid withdrawal syndrome—a strong deterrent to diversion of Suboxone and its abuse by injection . Stimulation of the kappa opioid receptor plays a role in producing some of the major symptoms associated with opioid withdrawal.