Naltrexone

Naltrexone Brand Names

Depade | ReVia | Vivitrol

What is Naltrexone

Naltrexone is an oral opiate receptor antagonist. It is derived from thebaine and is very similar in structure to oxymorphone.

Like parenteral naloxone, naltrexone is a pure antagonist (i.e., agonist actions are not apparent), but naltrexone has better oral bioavailability and a much longer duration of action than naloxone.

Clinically, naltrexone is used to help maintain an opiate-free state in patients who are known opiate abusers.

Naltrexone is of greatest benefit in patients who take the drug as part of a comprehensive occupational rehabilitative program or other compliance-enhancing program.

Unlike methadone or LAAM, naltrexone does not reinforce medication compliance and will not prevent withdrawal. Naltrexone has been used as part of rapid and ultrarapid detoxification techniques. These techniques are designed to precipitate withdrawal by administering opiate antagonists. These approaches are thought to minimize the risk of relapse and allow quick initiation of naltrexone maintenance and psychosocial supports.

Ultrarapid detoxification is performed under general anesthesia or heavy sedation. While numerous studies have been performed examining the role of these detoxification techniques, a standardized procedure including appropriate medications and dose, safety, and effectiveness have not been determined in relation to standard detoxification techniques.

Naltrexone supports abstinence, prevents relapse, and decreases alcohol consumption in patients treated for alcoholism.

Naltrexone is not beneficial in all alcoholic patients and may only provide a small improvement in outcome when added to conventional therapy. The FDA approved naltrexone in 1984 for the adjuvant treatment of patients dependent on opiate agonists.

FDA approval of naltrexone for the treatment of alcoholism was granted January 1995.

The FDA approved Vivitrol, a once-monthly intramuscular naltrexone formulation used to help control cravings for alcohol in April 2006, and then in October 2010, the FDA approved Vivitrol for the prevention of relapse to opioid dependence after opioid detoxification.

Indications

  1. alcohol dependence
  2. opiate agonist dependence
  3. opiate agonist withdrawal induction
  4. pruritus
  5. tobacco cessation

Side Effects

  1. abdominal pain
  2. acne vulgaris
  3. agitation
  4. alopecia
  5. anaphylactoid reactions
  6. angina
  7. angioedema
  8. anorexia
  9. anxiety
  10. appetite stimulation
  11. arthralgia
  12. asthenia
  13. atrial fibrillation
  14. back pain
  15. bleeding
  16. blurred vision
  17. chest pain (unspecified)
  18. chills
  19. cholecystitis
  20. cholelithiasis
  21. colitis
  22. confusion
  23. conjunctivitis
  24. constipation
  25. cough
  26. dehydration
  27. dental pain
  28. depression
  29. diarrhea
  30. dizziness
  31. drowsiness
  32. dysgeusia
  33. dyspnea
  34. dysuria
  35. ecchymosis
  36. edema
  37. ejaculation dysfunction
  38. elevated hepatic enzymes
  39. eosinophilia
  40. eosinophilic pneumonia
  41. epistaxis
  42. euphoria
  43. fatigue
  44. fever
  45. flatulence
  46. gastroesophageal reflux
  47. GI bleeding
  48. hallucinations
  49. headache
  50. heart failure
  51. hematoma
  52. hemorrhoids
  53. hepatitis
  54. hoarseness
  55. hot flashes
  56. hyperbilirubinemia
  57. hypercholesterolemia
  58. hyperhidrosis
  59. hyperkinesis
  60. hypertension
  61. ileus
  62. increased urinary frequency
  63. infection
  64. influenza
  65. injection site reaction
  66. insomnia
  67. irritability
  68. laryngitis
  69. lethargy
  70. libido decrease
  71. libido increase
  72. lymphadenopathy
  73. malaise
  74. migraine
  75. muscle cramps
  76. myalgia
  77. myocardial infarction
  78. nasal congestion
  79. nausea
  80. night sweats
  81. nightmares
  82. ocular inflammation
  83. ocular irritation
  84. otalgia
  85. palpitations
  86. pancreatitis
  87. paranoia
  88. paresthesias
  89. peptic ulcer
  90. phlebitis
  91. photophobia
  92. polydipsia
  93. pruritus
  94. pulmonary embolism
  95. purpura
  96. rash
  97. restlessness
  98. rhinorrhea
  99. seizures
  100. sinus tachycardia
  101. sinusitis
  102. sneezing
  103. stroke
  104. suicidal ideation
  105. syncope
  106. thrombosis
  107. tinnitus
  108. tissue necrosis
  109. tremor
  110. urticaria
  111. visual impairment
  112. vomiting
  113. weight gain
  114. weight loss
  115. withdrawal
  116. xerostomia
  117. yawning

Monitoring Parameters

  • LFTs

Contraindications

  • acute opioid withdrawal
  • breast-feeding
  • children
  • coagulopathy
  • depression
  • driving or operating machinery
  • females
  • hemophilia
  • hepatic disease
  • hepatitis
  • infants
  • intravenous administration
  • neonates
  • obesity
  • potential for overdose or poisoning
  • pregnancy
  • renal impairment
  • respiratory depression
  • subcutaneous administration
  • suicidal ideation
  • surgery
  • thrombocytopenia
  • tissue necrosis

Interactions

  • Acamprosate
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Codeine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Pentazocine
  • Acetaminophen; Propoxyphene
  • Acetaminophen; Tramadol
  • Alfentanil
  • Alvimopan
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
  • Atropine; Difenoxin
  • Atropine; Diphenoxylate
  • Bremelanotide
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Buprenorphine
  • Buprenorphine; Naloxone
  • Butorphanol
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Disulfiram
  • Dronabinol
  • Fentanyl
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Homatropine; Hydrocodone
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Ibuprofen; Oxycodone
  • Levomethadyl
  • Levorphanol
  • Lofexidine
  • Meperidine
  • Meperidine; Promethazine
  • Methadone
  • Methylnaltrexone
  • Morphine
  • Morphine; Naltrexone
  • Nabilone
  • Nalbuphine
  • Naldemedine
  • Naloxegol
  • Opiate Agonists-Antagonists
  • Oxycodone
  • Oxymorphone
  • Pentazocine
  • Pentazocine; Naloxone
  • Phenothiazines
  • Propoxyphene
  • Remifentanil
  • Sufentanil
  • Tapentadol
  • Tramadol
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