Meprobamate (Andaxin) - Uses, Dose, MOA, Brands, Side effects

Meprobamate (Andaxin) is a non-benzodiazepine tranquilizer that is used in the short-term treatment of anxiety disorders.

Meprobamate Uses:

  • Anxiety:

    • Used for treating anxiety disorders
    • Limitations of use:
      • According to recommendations from the American Psychiatric Association, World Federation of Societies of Biologica Psychiatry, and British Association for Psychopharmacology, meprobamate is not a first line therapy option  for  anxiety disorders.

Meprobamate (Andaxin) Dose in Adults:

Meprobamate (Andaxin) Dose in the treatment of Anxiety:

  • Oral: 1.2 to 1.6 g/day in divided doses;
  • The maximum: 2.4 g/day

Discontinuation:

  • When used for prolonged periods must be tapered off slowly over 2 weeks before discontinuation, due to potential for withdrawal symptoms like anorexia, insomnia, and anxiety.

Meprobamate (Andaxin) Dose in Childrens:

Meprobamate (Andaxin) Dose in the treatment of Anxiety:

  • Children ≥6 years:

    • 200 to 600 mg/day orally in 2 to 3 divided doses
    • Discontinuation:
    • When used for prolonged periods must be tapered off slowly over 2 weeks before discontinuation, due to potential for withdrawal symptoms like anorexia, insomnia, and anxiety.
  • Adolescents:

    • Same as adult dosing.

Pregnancy Risk Category: D/ X

  • Contraindicated during pregnancy
  • It can cross the placenta, and could cause congenital malformations.

Use during breastfeeding

  • Contained in breast milk.

Dose in Kidney Disease:

  • No dose adjustment recommended by the manufacturer however following guidelines may be used:
    • CrCl 10 to 50 mL/minute:
      • Administer every 9 to 12 hours
    • CrCl <10 mL/minute:
      • Administer every 12 to 18 hours
    • Hemodialysis:
      • No dosage adjustment is needed.
    • Peritoneal dialysis:
      • Administer every 12 to 18 hours
    • Continuous renal replacement therapy (CRRT):
      • Administer every 9 to 12 hours

Dose in Liver disease:

No dose adjustment is required.


Side effects of Meprobamate (Andaxin):

  • Cardiovascular:

    • Abnormal electroencephalogram
    • Tachycardia
    • Cardiac arrhythmia
    • Peripheral edema
    • Palpitations
    • Severe hypotension
    • Syncope
  • Central nervous system:

    • Slurred speech
    • Chills
    • Paradoxical excitation
    • Drowsiness Euphoria
    • Overstimulation
    • Headache
    • Paresthesia
    • Dizziness
    • Vertigo
    • Ataxia
  • Dermatologic:

    • Dermatitis Erythema multiforme
    • Skin rash
    • Stevens-Johnson syndrome
  • Endocrine & metabolic:

    • Exacerbation of porphyria
  • Gastrointestinal:

    • Diarrhea
    • Nausea
    • Proctitis
    • Stomatitis
    • Vomiting
  • Genitourinary:

    • Anuria
    • Oliguria
  • Hematologic & oncologic:

    • Bruise
    • Agranulocytosis
    • Purpura
    • Aplastic anemia
    • Leukopenia
    • Immune thrombocytopenia
    • Petechia
    • Eosinophilia
  • Hypersensitivity:

    • Angioedema
    • Anaphylaxis
    • Hypersensitivity reaction
  • Neuromuscular & skeletal:

    • Weakness
  • Ophthalmic:

    • Accommodation disturbance
  • Respiratory:

    • Bronchospasm
  • Miscellaneous:

    • Fever

Contraindications to Meprobamate (Andaxin):

  • Allergy or sensitivity to meprobamate, any component of the formulation.

Warnings and precautions

  • Allergy reactions:

    • Pre-existing dermatological conditions may cause allergic reactions, especially if the fourth dose is taken.
  • Depression in the CNS:

    • Use with caution before using this product to cause CNS depression or drowsiness.
    • Concomitant use of alcohol or other sedatives can increase the risk of developing CNS depression.
  • Depression

    • Patients with depression or suicidal thoughts need to be treated with care.
  • Use of drugs:

    • Patients who have previously used or been dependent on drugs may be at risk for addiction.
    • This may lead to psychological tolerance.
  • Hepatic impairment

    • Pre-existing hepatic impairment should be treated with care
  • Renal impairment

    • Pre-existing renal dysfunction must be considered.
  • Seizure disorder

    • Preventive measures should be taken if you have a seizure disorder.

Meprobamate: Drug Interaction

Risk Factor C (Monitor therapy)

Alcohol (Ethyl

CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl).

Alizapride

May enhance the CNS depressant effect of CNS Depressants.

Brexanolone

CNS Depressants may enhance the CNS depressant effect of Brexanolone.

Brimonidine (Topical)

May enhance the CNS depressant effect of CNS Depressants.

Bromopride

May enhance the CNS depressant effect of CNS Depressants.

Cannabidiol

May enhance the CNS depressant effect of CNS Depressants.

Cannabis

May enhance the CNS depressant effect of CNS Depressants.

Chlorphenesin Carbamate

May enhance the adverse/toxic effect of CNS Depressants.

CNS Depressants

May enhance the adverse/toxic effect of other CNS Depressants.

Dimethindene (Topical)

May enhance the CNS depressant effect of CNS Depressants.

Doxylamine

May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended.

Dronabinol

May enhance the CNS depressant effect of CNS Depressants.

Esketamine

May enhance the CNS depressant effect of CNS Depressants.

HydrOXYzine

May enhance the CNS depressant effect of CNS Depressants.

Kava Kava

May enhance the adverse/toxic effect of CNS Depressants.

Lofexidine

May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.

Magnesium Sulfate

May enhance the CNS depressant effect of CNS Depressants.

MetyroSINE

CNS Depressants may enhance the sedative effect of MetyroSINE.

Minocycline (Systemic)

May enhance the CNS depressant effect of CNS Depressants.

Nabilone

May enhance the CNS depressant effect of CNS Depressants.

Piribedil

CNS Depressants may enhance the CNS depressant effect of Piribedil.

Pramipexole

CNS Depressants may enhance the sedative effect of Pramipexole.

ROPINIRole

CNS Depressants may enhance the sedative effect of ROPINIRole.

Rotigotine

CNS Depressants may enhance the sedative effect of Rotigotine.

Rufinamide

May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced.

Selective Serotonin Reuptake Inhibitors

CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced.

Tetrahydrocannabinol

May enhance the CNS depressant effect of CNS Depressants.

Tetrahydrocannabinol and Cannabidiol

May enhance the CNS depressant effect of CNS Depressants.

Trimeprazine

May enhance the CNS depressant effect of CNS Depressants.

Yohimbine

May diminish the therapeutic effect of Antianxiety Agents.

Risk Factor D (Consider therapy modification)

Blonanserin

CNS Depressants may enhance the CNS depressant effect of Blonanserin. Risk

Buprenorphine

CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Risk

Chlormethiazole

May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk

Droperidol

May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Risk

Flunitrazepam

CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Risk

HYDROcodone

CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk

Lemborexant

May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk

Methotrimeprazine

CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk

Opioid Agonists

CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk

OxyCODONE

CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk

Perampanel

May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Risk

Sodium Oxybate

May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. Risk

Suvorexant

CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk

Tapentadol

May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk

Zolpidem

CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk

Risk Factor X (Avoid combination)

Azelastine (Nasal)

CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal).

Bromperidol

May enhance the CNS depressant effect of CNS Depressants.

Orphenadrine

CNS Depressants may enhance the CNS depressant effect of Orphenadrine.

Oxomemazine

May enhance the CNS depressant effect of CNS Depressants.

Paraldehyde

CNS Depressants may enhance the CNS depressant effect of Paraldehyde.

Thalidomide

CNS Depressants may enhance the CNS depressant effect of Thalidomide.

 

Monitoring parameters:

  • symptoms of anxiety
  • mental status
  • Signs of overdose

How to administer?

It may be administered after meals.


Mechanism of action of Meprobamate (Andaxin):

It suppresses multi-neuronal spinal reflexes, involves the thalamus and limbic system.

The onset of action:

  • Sedation: about 1 hour

Metabolism:

  • Hepatic

Half-life elimination:

  • 10 hours

Excretion:

  • Urine (8% to 20% as unchanged drug);
  • feces (10% as metabolites)

International Brand Names of Meprobamate:

  • Andaxin
  • Centryl
  • Ecuanil
  • Equanil
  • Koligin
  • Meprate
  • Mepro
  • Meprobamat
  • Meprodil
  • Miltaun
  • Oasil
  • Pertranquil
  • Praol
  • Probamato
  • Probamyl
  • Procalmadiol
  • Quaname
  • Quanil
  • Reposo-Mono
  • Restenil
  • Sanobamat
  • Tranquilin
  • Visano

Meprobamate Brand Names in Pakistan:

No Brands Available in Pakistan.

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