Active Ingredient History

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Buprenorphine is an opioid analgesic, used to treat opioid addiction, moderate acute pain, and moderate chronic pain. Buprenorphine is a partial agonist at the mµ-opioid receptor and an antagonist at the kappa-opioid receptor. One unusual property of buprenorphine observed in vitro studies is its very slow rate of dissociation from its receptor. This could account for its longer duration of action than morphine, the unpredictability of its reversal by opioid antagonists, and its low level of manifest physical dependence. The principal action of the therapeutic value of buprenorphine is analgesia and is thought to be due to buprenorphine binding with high affinity to opioid receptors on neurons in the brain and spinal cord. Buprenorphine produces respiratory depression by direct action on brain stem respiratory centers. The respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to both increases in carbon dioxide tension and electrical stimulation. Buprenorphine causes a reduction in motility associated with an increase in smooth muscle tone in the antrum of the stomach and duodenum. Digestion of food in the small intestine is delayed and propulsive contractions are decreased. Buprenorphine produces peripheral vasodilation, which may result in orthostatic hypotension or syncope. Manifestations of histamine release and/or peripheral vasodilation may include pruritus, flushing, red eyes, sweating, and/or orthostatic hypotension.   NCATS

  • SMILES: CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]4Cc5ccc(O)c6O[C@@H]2[C@]3(CCN4CC7CC7)c56
  • InChIKey: RMRJXGBAOAMLHD-CTAPUXPBSA-N
  • Mol. Mass: 467.65
  • ALogP: 4.41
  • ChEMBL Molecules:
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Drug Pricing (per unit)

United States

$0.4832 - $1205.9000

Australia

$0.6479 - $286.5509
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Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Combination drugs

( buprenorphine, naloxone (narcan) - other names: bunavail, cassipa, zubsolv )
17-cyclopropylmethyl-4,5alpha-epoxy-7alpha-((s)-1-hydroxy-1,2,2-trimethylpropyl)-6-methoxy-6,14-endo-ethanomorphinan-3-ol | 21-cyclopropyl-7alpha-[(s)-1-hydroxy-1,2,2-trimethylpropyl]-6,14-endo-ethano-6,7,8,14-tetrahydrooripavine | 2-[3-cyclopropylmethyl-11-hydroxy-15-methoxy-(14r)-13-oxa-3-azahexacyclo[13.2.2.12,8.01,6.06,14.07,12]icosa-7,9,11-trien-16-yl]-3,3-dimethyl-2-butanol | 2-(n-cyclopropylmethyl-4,5alpha-epoxy-3-hydroxy-6-methoxy-6,14-endo-ethanomorphinan-6alpha-yl)-3,3-dimethyl-2-butanol | bupeaze | buplast | buprenex | buprenophine | buprenorfina | buprenorfine | buprenorphine | (-)-buprenorphine | (−)-buprenorphine | buprenorphine hcl | buprenorphine hydrochloride | buprenorphine hydrochloride, naloxone hydrochloride dihydrate | buprenorphine mixture with naloxone | buprenorphine / naloxone | buprenorphine/naloxone | buprenorphinum | butec | cam2038 | cl-112302 | espranor | gabup | hapoctasin | natzon | nih-8805 | norspan | panitaz | prefibin | prenotrix | probuphine | reletrans | rx-6029m hcl | sevodyne | subutex | temgesic | tephine | transtec | u- 952

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