Buprenorphine

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Buprenorphine Brand Names

Belbuca | Buprenex | Butrans | Probuphine | Sublocade | Subutex

What is Buprenorphine

Buprenorphine is a semisynthetic mixed opiate agonist-antagonist. Buprenorphine, a partial mu-receptor agonist, exhibits a ceiling to its pharmacological effects; thus, the danger of overdose, abuse liability, and toxicity from buprenorphine may be less than with full opioid agonists.

The immediate-release parenteral formulation of buprenorphine was first approved by the FDA in 1981 and is used for the relief of moderate to severe pain; subsequent FDA approvals of the transdermal and buccal formulations are used for the management of chronic severe pain in patients who require daily, around-the-clock, long-term opioid treatment.

A sublingual formulation (e.g., Subutex), a 6-month subdermal implant (Probuphine), and an extended-release monthly subcutaneous injection (Sublocade) are used for the treatment of opioid dependence.

Buprenorphine was the first medication approved for in-office treatment of opioid dependence under the federal Drug Addiction Treatment Act (DATA), and practitioners using buprenorphine products approved for the treatment of opiate dependence must comply with the requirements of DATA.

In a study, comparable reductions in illicit opioid usage were found with 3 treatments for opioid dependence: buprenorphine, methadone, and levomethadyl acetate.

The dosages were individually optimized within a range of 16 to 48 mg 3 times a week for buprenorphine, 60 to 100 mg daily for methadone, and 75 to 161 mg 3 times a week for levomethadyl acetate.

Indications

  1. moderate pain
  2. neonatal abstinence syndrome
  3. opiate agonist dependence
  4. opiate agonist withdrawal
  5. severe pain

Side Effects

  1. abdominal pain
  2. adrenocortical insufficiency
  3. agitation
  4. amblyopia
  5. amenorrhea
  6. anaphylactic shock
  7. anaphylactoid reactions
  8. anemia
  9. angina
  10. angioedema
  11. anorexia
  12. anxiety
  13. apnea
  14. arthralgia
  15. asthenia
  16. atrial fibrillation
  17. AV block
  18. back pain
  19. blurred vision
  20. bradycardia
  21. bronchospasm
  22. chest pain (unspecified)
  23. chills
  24. cholecystitis
  25. coma
  26. confusion
  27. conjunctivitis
  28. constipation
  29. cough
  30. cyanosis
  31. dehydration
  32. depression
  33. diaphoresis
  34. diarrhea
  35. diplopia
  36. dizziness
  37. drowsiness
  38. dysarthria
  39. dysgeusia
  40. dyspepsia
  41. dysphagia
  42. dysphoria
  43. dyspnea
  44. ecchymosis
  45. edema
  46. elevated hepatic enzymes
  47. emotional lability
  48. epiphora
  49. erythema
  50. euphoria
  51. fatigue
  52. fever
  53. flatulence
  54. flushing
  55. gonadal suppression
  56. hallucinations
  57. headache
  58. hematoma
  59. hepatic encephalopathy
  60. hepatic failure
  61. hepatic necrosis
  62. hepatitis
  63. hiccups
  64. hyperbilirubinemia
  65. hyperhidrosis
  66. hypertension
  67. hyperventilation
  68. hypoesthesia
  69. hyponatremia
  70. hypotension
  71. hypoventilation
  72. hypoxia
  73. ileus
  74. impaired cognition
  75. impotence (erectile dysfunction)
  76. increased intracranial pressure
  77. infection
  78. infertility
  79. injection site reaction
  80. insomnia
  81. jaundice
  82. lethargy
  83. libido decrease
  84. malaise
  85. memory impairment
  86. migraine
  87. miosis
  88. musculoskeletal pain
  89. myalgia
  90. nausea
  91. neonatal opioid withdrawal syndrome
  92. neonatal respiratory depression
  93. nightmares
  94. orthostatic hypotension
  95. pallor
  96. palpitations
  97. paresthesias
  98. peripheral edema
  99. peripheral vasodilation
  100. pharyngitis
  101. physiological dependence
  102. pruritus
  103. psychological dependence
  104. psychosis
  105. QT prolongation
  106. rash
  107. respiratory depression
  108. restlessness
  109. rhinitis
  110. rhinorrhea
  111. seizures
  112. serotonin syndrome
  113. SIADH
  114. sinus tachycardia
  115. sinusitis
  116. skin irritation
  117. stroke
  118. syncope
  119. tinnitus
  120. tremor
  121. urinary incontinence
  122. urinary retention
  123. urticaria
  124. vertigo
  125. visual impairment
  126. vomiting
  127. weakness
  128. weight loss
  129. wheezing
  130. withdrawal
  131. xerophthalmia
  132. xerostomia

Monitoring Parameters

  • LFTs

Contraindications

  • abrupt discontinuation
  • accidental exposure
  • acute abdomen
  • acute heart failure
  • acute intoxication of CNS depressants
  • acute myocardial infarction
  • adrenal insufficiency
  • alcoholism
  • anxiety
  • asthma
  • atrial fibrillation
  • biliary cirrhosis
  • biliary obstruction
  • biliary tract disease
  • bladder obstruction
  • bradycardia
  • breast-feeding
  • bronchitis
  • cardiac arrhythmias
  • cardiac disease
  • children
  • chronic obstructive pulmonary disease (COPD)
  • CNS depression
  • coadministration with other CNS depressants
  • coma
  • constipation
  • cor pulmonale
  • coronary artery disease
  • dental work
  • depression
  • diabetes mellitus
  • diarrhea
  • driving or operating machinery
  • emphysema
  • ethanol intoxication
  • females
  • fever
  • gallbladder disease
  • geriatric
  • GI obstruction
  • head trauma
  • heart failure
  • heating pad
  • hepatic disease
  • hepatic encephalopathy
  • hepatitis
  • hypertension
  • hypocalcemia
  • hypokalemia
  • hypomagnesemia
  • hypotension
  • hypothyroidism
  • hypovolemia
  • hypoxemia
  • ileus
  • implant insertion and removal complications
  • increased intracranial pressure
  • infants
  • infection
  • infertility
  • inflammatory bowel disease
  • intracranial mass
  • intramuscular administration
  • intravenous administration
  • jaundice
  • labor
  • long QT syndrome
  • malnutrition
  • myocardial infarction
  • myxedema
  • neonatal opioid withdrawal syndrome
  • neonates
  • obesity
  • obstetric delivery
  • oliguria
  • opiate agonist hypersensitivity
  • opioid-naive patients
  • orthostatic hypotension
  • pain
  • pancreatitis
  • potential for overdose or poisoning
  • pregnancy
  • prostatic hypertrophy
  • psychosis
  • pulmonary disease
  • QT prolongation
  • renal failure
  • renal impairment
  • reproductive risk
  • requires an experienced clinician
  • respiratory depression
  • respiratory insufficiency
  • scleroderma
  • scoliosis
  • seizure disorder
  • seizures
  • sleep apnea
  • status asthmaticus
  • substance abuse
  • sunlight (UV) exposure
  • surgery
  • thyroid disease
  • toxic megacolon
  • ulcerative colitis
  • urethral stricture
  • urinary retention
  • urinary tract obstruction

Interactions

  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Codeine
  • Acetaminophen; Dextromethorphan
  • Acetaminophen; Dextromethorphan; Doxylamine
  • Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
  • Acetaminophen; Dextromethorphan; Phenylephrine
  • Acetaminophen; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Diphenhydramine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Pentazocine
  • Acetaminophen; Propoxyphene
  • Acetaminophen; Tramadol
  • Aclidinium; Formoterol
  • Acrivastine; Pseudoephedrine
  • Albuterol
  • Albuterol; Ipratropium
  • Alfentanil
  • Alfuzosin
  • Almotriptan
  • Alosetron
  • Alprazolam
  • Amifampridine
  • Amiloride
  • Amiloride; Hydrochlorothiazide, HCTZ
  • Amiodarone
  • Amitriptyline
  • Amitriptyline; Chlordiazepoxide
  • Amoxapine
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amprenavir
  • Anagrelide
  • Anticholinergics
  • Apalutamide
  • Apomorphine
  • Aprepitant, Fosaprepitant
  • Arformoterol
  • Aripiprazole
  • Arsenic Trioxide
  • Artemether; Lumefantrine
  • Asenapine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atomoxetine
  • Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Atropine; Difenoxin
  • Atropine; Diphenoxylate
  • Azithromycin
  • Baclofen
  • Barbiturates
  • Bedaquiline
  • Belladonna; Opium
  • Benzhydrocodone; Acetaminophen
  • Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Boceprevir
  • Bosentan
  • Brexpiprazole
  • Brompheniramine
  • Brompheniramine; Carbetapentane; Phenylephrine
  • Brompheniramine; Dextromethorphan; Guaifenesin
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Brompheniramine; Pseudoephedrine
  • Budesonide; Formoterol
  • Bumetanide
  • Buprenorphine; Naloxone
  • Bupropion; Naltrexone
  • Buspirone
  • Butorphanol
  • Cannabidiol
  • Capsaicin; Metaxalone
  • Carbamazepine
  • Carbetapentane; Chlorpheniramine
  • Carbetapentane; Chlorpheniramine; Phenylephrine
  • Carbetapentane; Diphenhydramine; Phenylephrine
  • Carbetapentane; Guaifenesin
  • Carbetapentane; Guaifenesin; Phenylephrine
  • Carbetapentane; Phenylephrine
  • Carbetapentane; Phenylephrine; Pyrilamine
  • Carbetapentane; Pseudoephedrine
  • Carbetapentane; Pyrilamine
  • Carbidopa; Levodopa; Entacapone
  • Carbinoxamine
  • Carbinoxamine; Dextromethorphan; Pseudoephedrine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Carbinoxamine; Phenylephrine
  • Carbinoxamine; Pseudoephedrine
  • Cariprazine
  • Carisoprodol
  • Cenobamate
  • Ceritinib
  • Cetirizine
  • Cetirizine; Pseudoephedrine
  • Chlophedianol; Dexchlorpheniramine; Pseudoephedrine
  • Chloral Hydrate
  • Chloramphenicol
  • Chlorcyclizine
  • Chlordiazepoxide
  • Chlordiazepoxide; Clidinium
  • Chloroquine
  • Chlorpheniramine
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dextromethorphan
  • Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Phenylephrine
  • Chlorpheniramine; Pseudoephedrine
  • Chlorpromazine
  • Chlorzoxazone
  • Cimetidine
  • Ciprofloxacin
  • Cisapride
  • Citalopram
  • Clarithromycin
  • Class IA Antiarrhythmics
  • Clemastine
  • Clobazam
  • Clofazimine
  • Clomipramine
  • Clonazepam
  • Clorazepate
  • Clozapine
  • Cobicistat
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • COMT inhibitors
  • Conivaptan
  • Crizotinib
  • Cyclizine
  • Cyclobenzaprine
  • Cyproheptadine
  • Daclatasvir
  • Dalfopristin; Quinupristin
  • Dantrolene
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Dasatinib
  • Degarelix
  • Delavirdine
  • Desflurane
  • Desipramine
  • Desvenlafaxine
  • Deutetrabenazine
  • Dexchlorpheniramine
  • Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Dexmedetomidine
  • Dextromethorphan
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Dextromethorphan; Guaifenesin
  • Dextromethorphan; Guaifenesin; Phenylephrine
  • Dextromethorphan; Guaifenesin; Potassium Guaiacolsulfonate
  • Dextromethorphan; Guaifenesin; Pseudoephedrine
  • Dextromethorphan; Promethazine
  • Dextromethorphan; Quinidine
  • Diazepam
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diltiazem
  • Dimenhydrinate
  • Diphenhydramine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Diphenhydramine; Phenylephrine
  • Dofetilide
  • Dolasetron
  • Dolutegravir; Rilpivirine
  • Donepezil
  • Donepezil; Memantine
  • Doxepin
  • Doxylamine
  • Doxylamine; Pyridoxine
  • Dronabinol
  • Dronedarone
  • Droperidol
  • Duloxetine
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elagolix
  • Elbasvir; Grazoprevir
  • Eletriptan
  • Elexacaftor; tezacaftor; ivacaftor
  • Eliglustat
  • Elvitegravir
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Emtricitabine; Rilpivirine; Tenofovir alafenamide
  • Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
  • Encorafenib
  • Enflurane
  • Entacapone
  • Entrectinib
  • Enzalutamide
  • Eribulin
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Escitalopram
  • Esketamine
  • Eslicarbazepine
  • Estazolam
  • Eszopiclone
  • Ethacrynic Acid
  • Ethanol
  • Etomidate
  • Etravirine
  • Ezogabine
  • Fedratinib
  • Fentanyl
  • Fingolimod
  • Flecainide
  • Flibanserin
  • Fluconazole
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluphenazine
  • Flurazepam
  • Fluticasone; Salmeterol
  • Fluticasone; Umeclidinium; Vilanterol
  • Fluticasone; Vilanterol
  • Fluvoxamine
  • Formoterol
  • Formoterol; Mometasone
  • Fosamprenavir
  • Foscarnet
  • Fosphenytoin
  • Fospropofol
  • Frovatriptan
  • Furosemide
  • Gabapentin
  • Gemifloxacin
  • Gemtuzumab Ozogamicin
  • Gilteritinib
  • Glasdegib
  • Glycopyrrolate; Formoterol
  • Goserelin
  • Granisetron
  • grapefruit juice
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Halogenated Anesthetics
  • Haloperidol
  • Halothane
  • Histrelin
  • Homatropine; Hydrocodone
  • Hydrochlorothiazide, HCTZ; Spironolactone
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Hydroxychloroquine
  • Hydroxyzine
  • Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate
  • Ibuprofen; Oxycodone
  • Ibutilide
  • Idelalisib
  • Iloperidone
  • Imatinib
  • Imipramine
  • Indacaterol
  • Indacaterol; Glycopyrrolate
  • Indapamide
  • Indinavir
  • Inotuzumab Ozogamicin
  • Isavuconazonium
  • Isoflurane
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Ivacaftor
  • Ivosidenib
  • Ketamine
  • Ketoconazole
  • Lapatinib
  • Lasmiditan
  • Lefamulin
  • Lenvatinib
  • Lesinurad
  • Lesinurad; Allopurinol
  • Letermovir
  • Leuprolide
  • Leuprolide; Norethindrone
  • Levalbuterol
  • Levocetirizine
  • Levofloxacin
  • Levomethadyl
  • Levomilnacipran
  • Levorphanol
  • Linezolid
  • Lithium
  • Lofexidine
  • Loop diuretics
  • Loperamide
  • Loperamide; Simethicone
  • Lopinavir; Ritonavir
  • Lorazepam
  • Lorlatinib
  • Lumacaftor; Ivacaftor
  • Lumacaftor; Ivacaftor
  • Lumateperone
  • Lurasidone
  • Macimorelin
  • Magnesium Salts
  • Maprotiline
  • Meclizine
  • Mefloquine
  • Meperidine
  • Meperidine; Promethazine
  • Meprobamate
  • Metaproterenol
  • Metaxalone
  • Methadone
  • Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine
  • Methocarbamol
  • Methylene Blue
  • Metronidazole
  • Midazolam
  • Midostaurin
  • Mifepristone
  • Milnacipran
  • Minocycline
  • Mirtazapine
  • Mitotane
  • Molindone
  • Monoamine oxidase inhibitors
  • Morphine
  • Morphine; Naltrexone
  • Moxifloxacin
  • Nabilone
  • Nalbuphine
  • Nalmefene
  • Naloxone
  • Naltrexone
  • Naproxen; Sumatriptan
  • Naratriptan
  • Nefazodone
  • Nelfinavir
  • Netupitant, Fosnetupitant; Palonosetron
  • Nevirapine
  • Nilotinib
  • Norfloxacin
  • Nortriptyline
  • Octreotide
  • Ofloxacin
  • Olanzapine
  • Olodaterol
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Ondansetron
  • Oritavancin
  • Orphenadrine
  • Osimertinib
  • Oxaliplatin
  • Oxazepam
  • Oxcarbazepine
  • Oxycodone
  • Oxymorphone
  • Palbociclib
  • Paliperidone
  • Panobinostat
  • Paroxetine
  • Pasireotide
  • Pazopanib
  • Pentamidine
  • Pentazocine
  • Pentazocine; Naloxone
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenylephrine; Promethazine
  • Phenytoin
  • Pimavanserin
  • Pimozide
  • Pirbuterol
  • Pitolisant
  • Posaconazole
  • Potassium-sparing diuretics
  • Pramipexole
  • Pregabalin
  • Primaquine
  • Prochlorperazine
  • Promethazine
  • Propafenone
  • Propoxyphene
  • Protriptyline
  • Quazepam
  • Quetiapine
  • Quinine
  • Ramelteon
  • Ranolazine
  • Rasagiline
  • Remifentanil
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifabutin
  • Rifampin
  • Rifamycins
  • Rifapentine
  • Rilpivirine
  • Risperidone
  • Ritonavir
  • Rizatriptan
  • Romidepsin
  • Ropinirole
  • Rotigotine
  • Rufinamide
  • Salmeterol
  • Saquinavir
  • Serotonin-Receptor Agonists
  • Sertraline
  • Sevoflurane
  • Short-acting beta-agonists
  • Simeprevir
  • Siponimod
  • Solifenacin
  • Sorafenib
  • Sotalol
  • Spironolactone
  • St. John’s Wort, Hypericum perforatum
  • Streptogramins
  • Sufentanil
  • Sumatriptan
  • Sunitinib
  • Suvorexant
  • Tacrolimus
  • Tamoxifen
  • Tapentadol
  • Tasimelteon
  • Telaprevir
  • Telavancin
  • Telithromycin
  • Telotristat Ethyl
  • Temazepam
  • Terbutaline
  • Tetrabenazine
  • Tezacaftor; Ivacaftor
  • Thiazide diuretics
  • Thiethylperazine
  • Thioridazine
  • Tiotropium; Olodaterol
  • Tipranavir
  • Tizanidine
  • Tolcapone
  • Tolterodine
  • Toremifene
  • Torsemide
  • Tramadol
  • Trandolapril; Verapamil
  • Trazodone
  • Triamterene
  • Triazolam
  • Tricyclic antidepressants
  • Trifluoperazine
  • Trimethobenzamide
  • Trimipramine
  • Triprolidine
  • Triptorelin
  • Trospium
  • Umeclidinium; Vilanterol
  • Vandetanib
  • Vardenafil
  • Vemurafenib
  • Venlafaxine
  • Verapamil
  • Vigabatrin
  • Vilazodone
  • Voriconazole
  • Vorinostat
  • Vortioxetine
  • Zafirlukast
  • Zaleplon
  • Ziconotide
  • Ziprasidone
  • Zolmitriptan
  • Zolpidem

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