Butabarbital (Butisol) - A rapid acting hypnotic drug.

Butabarbital is a hypnotic medicine that belongs to the barbiturates group. It has a fast onset of action and a short duration of action. It is used as a sedative and a hypnotic medicine.

Butabarbital Dose in Adults

For Daytime sedation:

  • 15 - 30 mg orally 3 or  4 times a day.

Use as a Hypnotic:

  • 50 - 100 mg orally at bedtime.
  • It may be used for the short term as it loses its efficacy after 2 weeks.

For Preoperative sedation:

  • 50 - 100 mg orally 60 - 90 minutes before the surgery.

Butabarbital Dose in Children

Dose for sedation Preoperatively:

  • Children and Adolescents:
    • 2 - 6 mg/kg orally 60 - 90 minutes prior to surgery to a maximum dose of 100 mg.

Pregnancy Risk Factor D

  • It corsses placental barriers and fetal tissues.
  • Use of it during pregnancy can lead to neonatal withdrawal symptoms, which may manifest as irritability or seizures in the neonate.

Use of butabarbital during lactation

  • It can be excreted in breastmilk and should therefore be avoided by lactating mothers.

Butabarbital Dose in Renal Disease:

  • The dose should be reduced in patients with renal disease.
  • The manufacturer, however, has not recommended any dose adjustment in patients with renal disease.

Butabarbital Dose in Liver Disease:

  • The dose should be reduced in patients with liver disease.
  • The manufacturer, however, has not recommended any dose adjustment in patients with liver disease.

Common Side Effects Of Butabarbital Include:

  • Central nervous system:
    • Drowsiness

Contraindication to Butabarbital include:

  • Allergy reactions to barbiturates and any component of the formulation
  • Porphyria

Warnings and precautions

  • Abnormal thinking and behavior changes:
    • There may be neuropsychiatric symptoms that can include abnormalities in thought and behavior, worsening insomnia, or other psychotic symptoms. This may need to be carefully evaluated.
  • Depression in the CNS:
    • The drug may cause depression in the central nervous system, so caution should be taken when operating heavy machinery or driving.
  • Hypersensitivity reactions
    • Very rare allergic reactions have been reported.
    • This includes cases of angioedema of the tongue, glottis or larynx as well as nausea, vomiting and hypotension.
    • Butarbital should not be used on patients with angioedema.
  • Paradoxical answers:
    • Patients who are simultaneously being treated for pain may sometimes experience a paradoxical response.
  • Activities that are sleep-related:
    • It may be used to cause sleep-driving or cooking, eating, phone calls, sleeping, talking, and even walking while you're asleep.
    • The events may be lost on the patients.
    • Patients who use other CNS depressants, such as alcohol, are more likely to suffer from sleep-related disorders.
    • Patients who have reported sleep-driving should stop receiving treatment.
  • Depression
    • Patients suffering from depression should be cautious when taking the drug, as it can cause suicidal thoughts and tendencies.
  • Use of drugs:
    • Patients can develop a psychological and physical dependence.
    • Patients with a history or drug dependence should be cautious when using it.
  • Hepatic impairment
    • Patients with mild or moderate hepatic impairment should adjust the dose.
    • The drug should not be recommended to anyone with severe hepatic impairment or those who have signs that suggest hepatic dysfunction.
  • Renal impairment
    • Patients with severe renal impairment should have their dose adjusted.
  • Respiratory disease
    • It can cause respiratory depression. Patients who are at high risk for respiratory depression should be cautious when using the drug.

Butabarbital: 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.

Beta-Blockers

Barbiturates may decrease the serum concentration of Beta-Blockers. Exceptions: Atenolol; Levobunolol; Metipranolol; Nadolol.

Blood Pressure Lowering Agents

Barbiturates may enhance the hypotensive effect of Blood Pressure Lowering Agents.

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.

Calcium Channel Blockers

Barbiturates may increase the metabolism of Calcium Channel Blockers. Management: Monitor for decreased therapeutic effects of calcium channel blockers with concomitant barbiturate therapy. Calcium channel blocker dose adjustments may be necessary. Nimodipine Canadian labeling contraindicates concomitant use with phenobarbital. Exceptions: Clevidipine.

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.

Felbamate

May increase the serum concentration of Barbiturates. Barbiturates may decrease the serum concentration of Felbamate. Management: Monitor for elevated barbiturate concentrations/toxicity if felbamate is initiated/dose increased, or reduced concentrations/effects if felbamate is discontinued/dose decreased. Refer to phenobarbital dosing guidelines for patients receiving that agent.

Griseofulvin

Barbiturates may decrease the serum concentration of Griseofulvin.

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

May enhance the CNS depressant effect of CNS Depressants.

Mirtazapine

CNS Depressants may enhance the CNS depressant effect of Mirtazapine.

Multivitamins/Minerals (with ADEK, Folate, Iron)

May decrease the serum concentration of Barbiturates.

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.

Primidone

May enhance the adverse/toxic effect of Barbiturates. Primidone is converted to phenobarbital, and thus becomes additive with existing barbiturate therapy.

Propacetamol

Barbiturates may increase the metabolism of Propacetamol. This may 1) diminish the desired effects of propacetamol; and 2) increase the risk of liver damage.

Pyridoxine

May increase the metabolism of Barbiturates. Apparent in high pyridoxine doses (eg, 200 mg/day)

Rifamycin Derivatives

May increase the metabolism of Barbiturates.

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.

Theophylline Derivatives

Barbiturates may decrease the serum concentration of Theophylline Derivatives. Exceptions: Dyphylline.

Thiazide and Thiazide-Like Diuretics

Barbiturates may enhance the orthostatic hypotensive effect of Thiazide and Thiazide-Like Diuretics.

Trimeprazine

May enhance the CNS depressant effect of CNS Depressants.

Valproate Products

May increase the serum concentration of Barbiturates. Barbiturates may decrease the serum concentration of Valproate Products.

Risk Factor D (Consider therapy modification)

Blonanserin

CNS Depressants may enhance the CNS depressant effect of Blonanserin.

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 patches (Butrans brand) at 5 mcg/hr in adults when used with other CNS depressants.

Chloramphenicol (Systemic)

May decrease the metabolism of Barbiturates. Barbiturates may increase the metabolism of Chloramphenicol (Systemic).

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.

CycloSPORINE (Systemic)

Barbiturates may increase the metabolism of CycloSPORINE (Systemic).

Doxycycline

Barbiturates may decrease the serum concentration of Doxycycline.

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.

Estrogen Derivatives (Contraceptive)

Barbiturates may diminish the therapeutic effect of Estrogen Derivatives (Contraceptive). Contraceptive failure is possible. Management: Use of a non-hormonal contraceptive is recommended.

Flunitrazepam

CNS Depressants may enhance the CNS depressant effect of Flunitrazepam.

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.

HydrOXYzine

May enhance the CNS depressant effect of Barbiturates. Management: Consider a decrease in the barbiturate dose, as appropriate, when used together with hydroxyzine. With concurrent use, monitor patients closely for excessive response to the combination.

LamoTRIgine

Barbiturates may decrease the serum concentration of LamoTRIgine. Management: See lamotrigine prescribing information for specific age-dependent dosing guidelines regarding concurrent use with a barbiturate, as well as for adjusting lamotrigine dosing if concurrent barbiturate therapy is discontinued.

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.

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.

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.

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.

Progestins (Contraceptive)

Barbiturates may diminish the therapeutic effect of Progestins (Contraceptive). Contraceptive failure is possible. Management: Use of alternative, nonhormonal contraceptives is recommended.

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.

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.

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.

Teniposide

Barbiturates may decrease the serum concentration of Teniposide. Management: Consider alternatives to combined treatment with barbiturates and teniposide due to the potential for decreased teniposide concentrations. If the combination cannot be avoided, monitor teniposide response closely.

Tricyclic Antidepressants

Barbiturates may increase the metabolism of Tricyclic Antidepressants.

Vitamin K Antagonists (eg, warfarin)

Barbiturates may increase the metabolism of Vitamin K Antagonists. Management: Monitor INR more closely. An anticoagulant dose increase may be needed after a barbiturate is initiated or given at an increased dose. Anticoagulant dose decreases may be needed following barbiturate discontinuation or dose reduction.

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 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.

Hemin

Barbiturates may diminish the therapeutic effect of Hemin.

Methoxyflurane

Barbiturates may enhance the nephrotoxic effect of Methoxyflurane. Barbiturates may increase the metabolism of Methoxyflurane.

Mianserin

May enhance the CNS depressant effect of Barbiturates. Mianserin may diminish the therapeutic effect of Barbiturates. Barbiturates may decrease the serum concentration of Mianserin.

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.

Somatostatin Acetate

May enhance the adverse/toxic effect of Barbiturates. Specifically, Somatostatin Acetate may enhance or prolong Barbiturate effects, including sedative effects.

Thalidomide

CNS Depressants may enhance the CNS depressant effect of Thalidomide.

Ulipristal

Barbiturates may decrease the serum concentration of Ulipristal.

Voriconazole

Barbiturates may decrease the serum concentration of Voriconazole.

Monitoring Parameters:

 With prolonged therapy, Liver and renal functions should be monitored.

How to take Butabarbital?

  • It is administered orally 60 to 90 minutes before the surgery.

Mechanism of action of Butabarbital:

  • Butabarbital, a fast-acting barbiturate that has a short duration of effect, is available. 
  • It blocks impulses from the cortex to the thalamus and the reticular activating systems.

It has beenThe beginning of actionbetween 45-60 minutes.Duration of the actionIt can take between 6 and 8 hours. It is quickly absorbed by the body and is then metabolized in the liver. It has been aEliminating half-lifeAbout 100 hours.ExcretedPrimarily via urine

Butabarbital international brands:

  • Butisol Sodium
  • Brevinarcon

Butabarbital Brands in Pakistan:

 No brands available in Pakistan

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