Mephobarbital

Mephobarbital Brand Name– Mebaral

What is Mephobarbital

NOTE: This drug is discontinued in the U.S.

Mephobarbital also known as methylphenobarbital) was an oral sedative-hypnotic and anticonvulsant barbiturate agent. It is used for short-term sedation and sleep induction.

Mephobarbital also is used prophylactically to treat tonic-clonic (grand mal) and absence (petit mal) seizures and is often administered with other anticonvulsants.

Mephobarbital is not available in a parenteral formulation and is not used for status epilepticus. Mephobarbital’s actions are secondary to the CNS-depressant properties of the barbiturate class.

Mephobarbital is a long-acting agent with an onset of 30 to 60 minutes and a duration of action of 10 to 16 hours.

Mephobarbital is metabolized to phenobarbital, and most of mephobarbital’s pharmacologic properties are similar to phenobarbital. However, many clinicians prefer mephobarbital over phenobarbital as a seizure medication in children due to an apparently lesser effect on acute cognitive function.

This agent can be habit-forming, causing psychological or physical dependence. As with all anticonvulsants, a warning was in the label regarding an increased risk of suicidal behavior and depression in patients receiving anticonvulstant therapy.

Mephobarbital was in clinical use for decades; the manufacturer discontinued the drug in the UK in 2001, and then the drug was discontinued in the U.S. in 2012.

Indications

  1. absence seizures
  2. sedation induction
  3. sedation maintenance
  4. tonic-clonic seizures

For short term sedation maintenance or sedation induction, to relieve anxiety, tension, and apprehension

Side Effects

  1. agitation
  2. agranulocytosis
  3. anemia
  4. angioedema
  5. anxiety
  6. apnea
  7. asthenia
  8. ataxia
  9. bradycardia
  10. bullous rash
  11. coma
  12. confusion
  13. constipation
  14. depression
  15. diarrhea
  16. dizziness
  17. drowsiness
  18. ecchymosis
  19. elevated hepatic enzymes
  20. emotional lability
  21. erythema
  22. exfoliative dermatitis
  23. fatigue
  24. fever
  25. headache
  26. hepatitis
  27. hypoprothrombinemia
  28. impaired cognition
  29. impotence (erectile dysfunction)
  30. insomnia
  31. interstitial nephritis
  32. irritability
  33. jaundice
  34. lethargy
  35. libido decrease
  36. lupus-like symptoms
  37. maculopapular rash
  38. megaloblastic anemia
  39. miosis
  40. mydriasis
  41. nausea
  42. neonatal abstinence syndrome
  43. neutropenia
  44. nightmares
  45. nystagmus
  46. osteomalacia
  47. osteopenia
  48. photosensitivity
  49. physiological dependence
  50. porphyria
  51. psychological dependence
  52. ptosis
  53. purpura
  54. rash
  55. respiratory depression
  56. seizures
  57. serum sickness
  58. Stevens-Johnson syndrome
  59. suicidal ideation
  60. syncope
  61. teratogenesis
  62. thrombocytopenia
  63. tolerance
  64. toxic epidermal necrolysis
  65. urticaria
  66. vertigo
  67. vomiting
  68. weakness
  69. withdrawal

Monitoring Parameters

  • CBC
  • LFTs
  • serum creatinine

Contraindications

  • abrupt discontinuation
  • alcoholism
  • anuria
  • barbiturate hypersensitivity
  • breast-feeding
  • chronic obstructive pulmonary disease (COPD)
  • CNS depression
  • coadministration with other CNS depressants
  • depression
  • dialysis
  • driving or operating machinery
  • ethanol ingestion
  • geriatric
  • hepatic disease
  • hepatic encephalopathy
  • labor
  • myasthenia gravis
  • myxedema
  • neonates
  • obstetric delivery
  • osteomalacia
  • osteoporosis
  • pain
  • porphyria
  • pregnancy
  • pulmonary disease
  • renal disease
  • renal failure
  • renal impairment
  • respiratory depression
  • respiratory insufficiency
  • sleep apnea
  • status epilepticus
  • substance abuse
  • suicidal ideation

Interactions

  • Abemaciclib
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  • Acetaminophen
  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
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  • Acetaminophen; Caffeine
  • 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; Dichloralphenazone; Isometheptene
  • Acetaminophen; Diphenhydramine
  • Acetaminophen; Guaifenesin; Phenylephrine
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