Methadone

Methadone Brand Names- Dolophine | Methadose

What is Methadone

Methadone is a potent synthetic opiate agonist of the phenylheptylamine class and is structurally unrelated to morphine.

Methadone is a racemic mixture; the l-isomer is responsible for the drug’s analgesic effects. The d-isomer exhibits significantly less analgesic action and lacks respiratory depression activity and addiction liability, but it does have antitussive effects.

Methadone is the most frequently used agent in medically supervised opiate withdrawal and maintenance programs. Federal, state, and local guidelines strictly regulate methadone treatment of opiate dependence.

Effective methadone treatment requires individualized and comprehensive psychosocial support and access to medical and rehabilitative services. Heroin-dependent individuals have better outcomes when they are maintained on methadone than when they are not treated at all, acutely detoxified and released, expelled from treatment programs or when the treatment program is closed.

A study by the National Institute on Drug Abuse (NIDA), the Drug Treatment Outcome Study (DATOS), found that in those patients treated by outpatient methadone centers, weekly heroin use decreased 69%, cocaine use decreased by 48%, illegal activity decreased by 52%, and full time work increased by 24%. There is evidence that methadone treatment is effective in reducing transmission of HIV and hepatitis B and C infections by reducing intravenous drug use and needle sharing. 

Indications

  1. moderate pain
  2. opiate agonist dependence
  3. opiate agonist withdrawal
  4. severe pain

Side Effects

  1. abdominal pain
  2. adrenocortical insufficiency
  3. agitation
  4. amenorrhea
  5. anaphylactoid reactions
  6. anorexia
  7. anxiety
  8. apnea
  9. asthenia
  10. biliary obstruction
  11. blurred vision
  12. bone fractures
  13. bradycardia
  14. cardiac arrest
  15. cardiomyopathy
  16. confusion
  17. constipation
  18. diaphoresis
  19. dizziness
  20. drowsiness
  21. dysphoria
  22. dyspnea
  23. edema
  24. euphoria
  25. flushing
  26. glossitis
  27. gonadal suppression
  28. hallucinations
  29. headache
  30. heart failure
  31. hyperamylasemia
  32. hypertension
  33. hyperthyroidism
  34. hypokalemia
  35. hypomagnesemia
  36. hyponatremia
  37. hypotension
  38. hypoventilation
  39. hypoxia
  40. impotence (erectile dysfunction)
  41. infertility
  42. injection site reaction
  43. insomnia
  44. libido decrease
  45. miosis
  46. nausea
  47. neonatal opioid withdrawal syndrome
  48. oliguria
  49. orthostatic hypotension
  50. osteoporosis
  51. palpitations
  52. pancreatitis
  53. peripheral vasodilation
  54. phlebitis
  55. physiological dependence
  56. pruritus
  57. psychological dependence
  58. pulmonary edema
  59. QT prolongation
  60. rash
  61. respiratory arrest
  62. respiratory depression
  63. restlessness
  64. seizures
  65. serotonin syndrome
  66. SIADH
  67. sinus tachycardia
  68. ST-T wave changes
  69. syncope
  70. thrombocytopenia
  71. thrombocytosis
  72. tolerance
  73. torsade de pointes
  74. urinary retention
  75. urticaria
  76. ventricular fibrillation
  77. ventricular tachycardia
  78. vomiting
  79. weakness
  80. weight gain
  81. withdrawal
  82. xerostomia

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • abrupt discontinuation
  • accidental exposure
  • adrenal insufficiency
  • alcoholism
  • angina
  • anxiety
  • asthma
  • biliary tract disease
  • bladder obstruction
  • bradycardia
  • brain tumor
  • breast-feeding
  • cardiac arrhythmias
  • cardiac disease
  • 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
  • females
  • geriatric
  • GI disease
  • GI obstruction
  • head trauma
  • heart failure
  • hepatic disease
  • hypertension
  • hypocalcemia
  • hypokalemia
  • hypomagnesemia
  • hypotension
  • hypothyroidism
  • hypovolemia
  • hypoxemia
  • ileus
  • increased intracranial pressure
  • infants
  • infertility
  • inflammatory bowel disease
  • intracranial mass
  • labor
  • long QT syndrome
  • malnutrition
  • MAOI therapy
  • myocardial infarction
  • myxedema
  • neonatal opioid withdrawal syndrome
  • neonates
  • obesity
  • obstetric delivery
  • oliguria
  • opiate agonist hypersensitivity
  • opioid overdose
  • opioid use disorder
  • opioid-naive patients
  • orthostatic hypotension
  • pain
  • pancreatitis
  • potential for overdose or poisoning
  • pregnancy
  • prostatic hypertrophy
  • pulmonary disease
  • QT prolongation
  • renal disease
  • reproductive risk
  • requires an experienced clinician
  • respiratory depression
  • respiratory insufficiency
  • scoliosis
  • seizure disorder
  • seizures
  • sleep apnea
  • status asthmaticus
  • substance abuse
  • surgery
  • thyroid disease
  • ulcerative colitis
  • urethral stricture
  • urinary retention

Interactions

  • Abacavir
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