Buprenorphine

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