ﺑﺎﺯﮔﺸﺖ ﺑﻪ ﺻﻔﺤﻪ ﻗﺒﻠﯽ
خرید پکیج
تعداد آیتم قابل مشاهده باقیمانده : 3 مورد
نسخه الکترونیک
medimedia.ir

Methohexital: Drug information

Methohexital: Drug information
(For additional information see "Methohexital: Patient drug information" and see "Methohexital: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
ALERT: US Boxed Warning
Appropriate administration:

Use methohexital only in hospital or ambulatory care settings that provide for continuous monitoring of respiratory (eg, pulse oximetry) and cardiac function. Ensure immediate availability of resuscitative drugs and age- and size-appropriate equipment for bag/valve/mask ventilation and intubation and personnel trained in their use and skilled in airway management. For deeply sedated patients, a designated individual other than the practitioner performing the procedure should be present to continuously monitor the patient.

Brand Names: US
  • Brevital Sodium
Pharmacologic Category
  • Barbiturate;
  • General Anesthetic
Dosing: Adult
General anesthesia

General anesthesia: IV: Usual dosing range: 1 to 1.5 mg/kg for induction; titrate to response and tolerability.

Procedural sedation

Procedural sedation (off-label dose): IV: Usual dosing range: 0.75 to 1 mg/kg; redose with 0.5 mg/kg every 2 to 5 minutes based on response and tolerability (Bahn 2005).

Rapid sequence intubation outside the operating room

Rapid sequence intubation outside the operating room (off-label use): Note: May cause hypotension; consider alternative agent in patients who are hemodynamically unstable (Stollings 2014).

IV: Usual dosing range: 0.75 to 1.5 mg/kg; redose with 0.5 mg/kg based on response and tolerability (Diaz-Guzman 2010; Farrell 2020; Roberts 2019; Stollings 2014).

Wada test

Wada test (off-label use): Intracarotid (off-label route): 3 to 4 mg over 3 seconds; a second dose may be administered at 2 mg over 2 seconds based on response and tolerability (Buchtel 2002; Conradi 2020; Patel 2011).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling; use with caution.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling. However, adjustment may be necessary due to hepatic metabolism. Use with caution.

Dosing: Older Adult

Refer to adult dosing. Reduce dose or administer at the low end of the dosage range.

Dosing: Pediatric

(For additional information see "Methohexital: Pediatric drug information")

Note: Doses must be titrated to effect.

Induction

Induction :

IM: Infants and Children: 5% (50 mg/mL) solution: 6.6 to 10 mg/kg/dose

IV: Limited data available: Infants, Children, and Adolescents: 1% (10 mg/mL) solution: 1 to 2.5 mg/kg/dose; usual adult dose is 70 mg (ie, 1 mg/kg); if patient is premedicated, dose should be decreased (Björkman 1987; Coté 2013)

Rectal: Infants and Children: 1% (10 mg/mL) solution or 10% (100 mg/mL) solution: 25 mg/kg/dose; reported maximum dose: 500 mg/dose (Quaynor 1985)

Preoperative sedation

Preoperative sedation: Infants and Children:

IM: 5% (50 mg/mL) solution: 5 to 10 mg/kg/dose (Coté 2013)

Rectal: 1% (10 mg/mL) solution or 10% (100 mg/mL) solution: Usual dose: 25 mg/kg/dose; range: 20 to 40 mg/kg/dose; maximum dose: 500 mg/dose (Björkman 1987; Coté 2013; Liu 1980; Pomeranz 2000)

Procedural sedation

Procedural sedation:

IM: Infants and Children: 5% (50 mg/mL) solution: 10 mg/kg/dose (Varner 1985). Note: Some experts do not suggest routine use due to slower onset (Coté 2013).

IV: Limited data available: Infants, Children, and Adolescents: 1% (10 mg/mL) solution: Initial: 0.5 to 1 mg/kg/dose administer immediately prior to procedure; titrate additional doses to achieve level of sedation as needed in increments of 0.5 mg/kg to a maximum total dose: 2 mg/kg total. In the prospective phase of a trial including 20 infants and children (mean age: 26 ± 17 months) undergoing CT scans, a mean dose of 1 ± 0.5 mg/kg/dose was reported (Krauss 2006; Sedik 2001)

Rectal: Infants and Children: 10% (100 mg/mL) solution: Usual: 25 mg/kg/dose; range: 20 to 35 mg/kg/dose; maximum dose: 500 mg/dose; administer 5 to 15 minutes prior to procedure (Manuli 1993; Pomeranz 2000)

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling; use with caution.

Dosing: Hepatic Impairment: Pediatric

All patients: There are no dosage adjustments provided in the manufacturer's labeling. However, adjustment may be necessary due to hepatic metabolism. Use with caution.

Adverse Reactions

The following adverse drug reactions are derived from product labeling unless otherwise specified.

Frequency not defined:

Cardiovascular: Circulatory depression, circulatory shock, tachycardia

Dermatologic: Erythema of skin, pruritus, urticaria

Gastrointestinal: Abdominal pain, salivation

Hepatic: Abnormal hepatic function tests

Local: Injection-site reaction (injury to nerves adjacent to injection-site)

Nervous system: Headache, postanesthetic shivering

Neuromuscular & skeletal: Muscle twitching

Respiratory: Bronchospasm, dyspnea, rhinitis

Postmarketing:

Cardiovascular: Hypotension (Whitwam 1978), thrombophlebitis (Whitwam 1978)

Gastrointestinal: Hiccups (Whitwam 1978), nausea (Whitwam 1978), vomiting (Whitwam 1978)

Hypersensitivity: Anaphylaxis, hypersensitivity reaction (Whitwam 1978)

Local: Pain at injection site (Whitwam 1978)

Nervous system: Seizure (Rockoff 1981), tremor (Whitwam 1978)

Neuromuscular & skeletal: Laryngospasm (Whitwam 1978), muscle movements (Whitwam 1978)

Respiratory: Apnea (Whitwam 1978, Yemen 1991), cough (Whitwam 1978), respiratory depression (Whitwam 1978)

Contraindications

Hypersensitivity to methohexital or any component of the formulation; porphyria (latent or manifest); patients in whom general anesthesia is contraindicated

Warnings/Precautions

Concerns related to adverse effects:

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving); however, the duration of action is <10 minutes when used for procedural sedation (Bahn 2005).

• Hypotension/tachycardia: May cause temporary hypotension and tachycardia; use with caution in hemodynamically unstable patients (hypotension or shock) or severe hypertension.

Disease-related concerns:

• Anemia: Use with caution in patients with severe anemia; respiratory depression may occur leading to further inadequate tissue oxygenation.

• Cardiovascular disease: Use with caution in patients with cardiovascular disease including heart failure; consider monitoring cardiac function. Methohexital may enhance preexisting circulatory depression, severe cardiovascular instability, or a shock-like condition; consider using another induction agent in these patients.

• Hepatic impairment: Use with caution in patients with hepatic impairment; may prolong or potentiate hypnotic effect.

• Obesity: Use with caution in patients with extreme obesity.

• Pulmonary disease: May cause respiratory depression; use with caution in patients with pulmonary disease. Use with caution in patients with asthma and chronic obstructive pulmonary disease. Use with extreme caution in patients with ongoing status asthmaticus; hiccups, coughing, laryngospasm, and muscle twitching have occurred impairing ventilation.

• Renal impairment: Use with caution in patients with renal impairment; may prolong or potentiate hypnotic effect.

• Seizure disorder: Use with caution in patients with a history of seizure disorder.

Special populations:

• Debilitated patients: Use with caution in debilitated patients.

• Older adult: Use with caution in the elderly.

• Pediatric neurotoxicity: In pediatric and neonatal patients <3 years and patients in third trimester of pregnancy (ie, times of rapid brain growth and synaptogenesis), the repeated or lengthy exposure to sedatives or anesthetics during surgery/procedures may have detrimental effects on child or fetal brain development and may contribute to various cognitive and behavioral problems. Epidemiological studies in humans have reported various cognitive and behavioral problems including neurodevelopmental delay (and related diagnoses), learning disabilities, and ADHD. Human clinical data suggest that single, relatively short exposures are not likely to have similar negative effects. No specific anesthetic/sedative has been found to be safer. For elective procedures, risk vs benefits should be evaluated and discussed with parents/caregivers/patients; critical surgeries should not be delayed (FDA 2016).

Other warnings/precautions:

• Appropriate administration: [US Boxed Warning]: Should only be administered in hospitals or ambulatory care settings with continuous monitoring of respiratory (eg, pulse oximetry) and cardiac function. Immediate availability of resuscitative drugs and age- and size-appropriate intubation equipment and trained personnel experienced in handling their use should be immediately available and personnel trained in their use and skilled in airway management should be assured. For deeply sedated patients, a designated individual other than the healthcare provider performing the procedure should be present to continuously monitor the patient. Maintenance of a patent airway and adequacy of ventilation must be ensured during use. Laryngospasm is common during induction with all barbiturates.

• Cumulative effect: Repeated dosing or continuous infusions may cause cumulative effects.

• Intravenous (IV) administration: Prior to IV administration, ensure patient has adequate IV access; extravasation or intra-arterial injection causes necrosis.

Warnings: Additional Pediatric Considerations

In pediatric and neonatal patients <3 years of age and patients in third trimester of pregnancy (ie, times of rapid brain growth and synaptogenesis), the repeated or lengthy exposure to sedatives or anesthetics during surgery/procedures may have detrimental effects on the child's or fetus' brain development and may contribute to various cognitive and behavioral problems; the FDA is requiring warnings be included in the manufacturer's labeling for all general anesthetic/sedative drugs. Multiple animal species studies have shown adverse effects on brain maturation; in juvenile animals, drugs that potentiate GABA activity and/or block NMDA receptors for >3 hours demonstrated widespread neuronal and oligodendrocyte cell loss along with alteration in synaptic morphology and neurogenesis. Epidemiological studies in humans have reported various cognitive and behavioral problems including neurodevelopmental delay (and related diagnoses), learning disabilities, and ADHD. Human clinical data suggest that single, relatively short exposures are not likely to have similar negative effects. Further studies are needed to fully characterize findings and ensure that these findings are not related to underlying conditions or the procedure itself. No specific anesthetic/sedative has been found to be safer. For elective procedures, risk vs benefits should be evaluated and discussed with parents/caregivers/patients; critical surgeries should not be delayed (FDA 2016).

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution Reconstituted, Injection, as sodium [preservative free]:

Brevital Sodium: 500 mg (1 ea); 2.5 g (1 ea [DSC])

Generic Equivalent Available: US

No

Pricing: US

Solution (reconstituted) (Brevital Sodium Injection)

500 mg (per each): $110.83

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Controlled Substance

C-IV

Administration: Adult

IM administration: Use 5% (50 mg/mL) solution.

IV: Dilute to a maximum concentration of 1% prior to IV use.

Induction of anesthesia: 1% (10 mg/mL) solution is administered IV at a rate of ~1 mL/5 seconds or ~2 mg/second.

Intracarotid (off-label route): Wada test (off-label use): 0.1% (1 mg/mL) solution has been used; administer dose at a rate of 1 mg/second into the internal carotid artery (Buchtel 2002; Patel 2011).

Rectal administration: Use 1% (10 mg/mL) solution; 10% (100 mg/mL) solution has also been used (Pomeranz 2000).

Administration: Pediatric

Parenteral:

IM: Use 5% solution (50 mg/mL)

IV:

Bolus: For induction, infuse a 1% solution (10 mg/mL) at a rate of ~1 mL/5 seconds (ie, ~2 mg/second, or 12 mL/minute [120 mg/minute] depending upon pump setting)

Continuous IV infusion: Adults: Use a 0.2% solution (2 mg/mL)

Rectal: Use a 1% solution (10 mg/mL); a 10% solution (100 mg/mL) has also been given rectally (Björkman 1987; Pomeranz 2000)

Use: Labeled Indications

General anesthesia: Induction of anesthesia prior to the use of other general anesthetic agents; to supplement other anesthetic agents for longer surgical procedures.

Procedural sedation: Short surgical, diagnostic, or therapeutic procedures associated with minimal painful stimuli.

Use: Off-Label: Adult

Rapid sequence intubation, outside the operating room; Wada test

Medication Safety Issues
Sound-alike/look-alike issues:

Brevital may be confused with Brevibloc

High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs which have a heightened risk of causing significant patient harm when used in error.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider therapy modification

Blood Pressure Lowering Agents: Barbiturates may enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Risk C: Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromopride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

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 D: Consider therapy modification

Cannabinoid-Containing Products: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

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 D: Consider therapy modification

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy

Daridorexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

DexmedeTOMIDine: CNS Depressants may enhance the CNS depressant effect of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider therapy modification

Difelikefalin: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Doxycycline: Barbiturates may decrease the serum concentration of Doxycycline. Risk C: Monitor therapy

Doxylamine: CNS Depressants may enhance the CNS depressant effect of Doxylamine. Risk C: Monitor therapy

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. Risk D: Consider therapy modification

Esketamine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. Risk X: Avoid combination

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider therapy modification

Hemin: Barbiturates may diminish the therapeutic effect of Hemin. Risk X: Avoid combination

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider therapy modification

Ixabepilone: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kava Kava: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kratom: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

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 D: Consider therapy modification

Lisuride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider therapy modification

Methoxyflurane: Barbiturates may enhance the nephrotoxic effect of Methoxyflurane. Barbiturates may increase the metabolism of Methoxyflurane. Risk X: Avoid combination

Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy

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. Risk X: Avoid combination

Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Multivitamins/Minerals (with ADEK, Folate, Iron): May decrease the serum concentration of Barbiturates. Risk C: Monitor therapy

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Olopatadine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

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 D: Consider therapy modification

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination

Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Oxybate Salt Products: CNS Depressants may enhance the CNS depressant effect of Oxybate Salt Products. Management: Consider alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants (including the oxybate salt product) should be considered. Interrupt oxybate salt treatment during short-term opioid use Risk D: Consider therapy modification

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 D: Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy

Procarbazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Ropeginterferon Alfa-2b: CNS Depressants may enhance the adverse/toxic effect of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider therapy modification

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy

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 D: Consider therapy modification

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination

Theophylline Derivatives: Barbiturates may decrease the serum concentration of Theophylline Derivatives. Risk C: Monitor therapy

Tricyclic Antidepressants: Barbiturates may increase the metabolism of Tricyclic Antidepressants. Management: Monitor for decreased efficacy of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. Tricyclic antidepressant dose adjustments are likely required. Risk D: Consider therapy modification

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Valerian: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Valproate Products: May increase the serum concentration of Barbiturates. Barbiturates may decrease the serum concentration of Valproate Products. Risk C: Monitor therapy

Vitamin K Antagonists (eg, warfarin): Barbiturates may increase the metabolism of Vitamin K Antagonists. Management: Monitor INR more closely. Anticoagulant dose increases of 30% to 60% 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. Risk D: Consider therapy modification

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 D: Consider therapy modification

Zuranolone: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider therapy modification

Pregnancy Considerations

Methohexital crosses the placenta.

Based on animal data, repeated or prolonged use of general anesthetic and sedation medications that block N-methyl-D-aspartate (NMDA) receptors and/or potentiate gamma-aminobutyric acid (GABA) activity may affect brain development. Evaluate benefits and potential risks of fetal exposure to methohexital when duration of surgery is expected to be >3 hours (Olutoye 2018).

Use of methohexital in obstetric anesthesia has been described (Holdcroft 1974; Lee 1966; Verma 1985). However, other agents are more commonly used (ACOG 209 2019; Devroe 2015).

The ACOG recommends that pregnant women should not be denied medically necessary surgery, regardless of trimester. If the procedure is elective, it should be delayed until after delivery (ACOG 775 2019).

Breastfeeding Considerations

Methohexital is present in breast milk (Borgatta 1997).

Breast milk concentrations of methohexital were highest ~1 hour following induction of anesthesia in nine women undergoing sterilization ≥1 months postpartum. Methohexital was not measurable in the maternal breast milk of four women 8 to 10 hours after the dose. None of the women had detectable milk or serum concentrations ≥24 hours after the dose (Borgatta 1997).

The manufacturer recommends that caution be exercised when administering methohexital to breastfeeding women. The Academy of Breast Feeding Medicine recommends postponing elective surgery until milk supply and breastfeeding are established. Milk should be expressed ahead of surgery when possible. In general, when the child is healthy and full term, breastfeeding may resume, or milk may be expressed once the mother is awake and in recovery. For children who are at risk for apnea, hypotension, or hypotonia, milk may be saved for later use when the child is at lower risk (ABM [Reece-Stremtan 2017]).

Monitoring Parameters

Respiratory (eg, pulse oximetry and capnography), cardiovascular (eg, cardiac monitoring, BP, heart rate), CNS status (when used for anesthesia and/or procedures, monitor sedation level).

Mechanism of Action

Methohexital is an ultra short-acting IV barbiturate anesthetic. Barbiturates depress the sensory cortex, decrease motor activity, and alter cerebellar function producing drowsiness, sedation, and hypnosis.

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: IV: Immediate; IM (pediatrics): 2 to 10 minutes; Rectal (pediatrics): 5 to 15 minutes

Duration: Single dose:

IM: 1 to 1.5 hours

IV: Time to clinical recovery (ie, awake time, sitting and standing steadily, duration of amnesia): 5 to 15 minutes (psychomotor impairment may continue for up to 8 hours) (Barash 2009; Fredman 1994; Korttila 1975)

Rectal (pediatrics): 45 to 60 minutes (Cote 1994)

Metabolism: Hepatic via demethylation and oxidation

Bioavailability: Rectal: 17%

Half-life elimination: 1.6 to 3.9 hours (Ghoneim 1985)

Excretion: Urine

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (CZ) Czech Republic: Brietal sodium;
  • (DE) Germany: Brevimytal natrium;
  • (EE) Estonia: Brietal;
  • (FI) Finland: Brietal;
  • (LT) Lithuania: Brietal;
  • (NO) Norway: Brevital;
  • (NZ) New Zealand: Brevimytal hikma | Brevital;
  • (PL) Poland: Brietal sodium;
  • (PR) Puerto Rico: Brevital;
  • (RU) Russian Federation: Brietal;
  • (TW) Taiwan: Brietal sodium
  1. American College of Obstetricians and Gynecologists (ACOG). ACOG committee opinion no. 775: nonobstetric surgery during pregnancy. Obstet Gynecol. 2019;133(4):e285-e286. [PubMed 30913200]
  2. American College of Obstetricians and Gynecologists (ACOG). ACOG practice bulletin no. 209: obstetric analgesia and anesthesia. Obstet Gynecol. 2019;133(3):e208-e225. [PubMed 30801474]
  3. Bahn EL and Holt KR, "Procedural Sedation and Analgesia: A Review and New Concepts," Emerg Med Clin North Am, 2005, 23(2):503-17. [PubMed 15829394]
  4. Barash PG, Cullen BF, Stoelting RK, et al, eds, Clinical Anesthesia, 6th ed, Philadelphia, PA; Lippincott Williams & Wilkins, 2009.
  5. Beimer NJ, Buchtel HA, Glynn SM. One center's experience with complications during the Wada test. Epilepsia. 2015;56(8):e110-113. [PubMed 26046456]
  6. Bjorkman S, Gabrielsson J, Quaynor H, et al, “Pharmacokinetics of I.V. and Rectal Methohexitone in Children,” Br J Anaesth, 1987, 59(12):1541-7. [PubMed 3426908]
  7. Borgatta L, Jenny RW, Gruss L, Ong C, Barad D. Clinical significance of methohexital, meperidine, and diazepam in breast milk. J Clin Pharmacol. 1997;37(3):186-192. [PubMed 9089420]
  8. Brevital (methohexital sodium) [prescribing information]. Chestnut Ridge, NY: Par Pharmaceutical; October 2020.
  9. Buchtel HA, Passaro EA, Selwa LM, et al, “Sodium Methohexital (Brevital) as an Anesthetic in the Wada Test,” Epilepsia, 2002, 43(9):1056-61. [PubMed 12199731]
  10. Conradi N, Rosenberg F, Biermann L, et al. Advantages of methohexital over amobarbital in determining hemispheric language and memory lateralization in the Wada test - a retrospective study. Epilepsy Behav. 2020;113:107551. doi:10.1016/j.yebeh.2020.107551 [PubMed 33246234]
  11. Coté CJ, “Sedation for the Pediatric Patient,” Pediatr Clin North Am, 1994, 41(1):31-58. [PubMed 8295806]
  12. Coté CJ, Lerman J, Anderson B, eds.A Practice of Anesthesia for Infants and Children. 5th ed. Elsevier; 2013.
  13. Devroe S, Van de Velde M, Rex S. General anesthesia for caesarean section. Curr Opin Anaesthesiol. 2015;28(3):240-246. doi: 10.1097/ACO.0000000000000185. [PubMed 25827280]
  14. Diaz-Guzman E, Mireles-Cabodevila E, Heresi GA, Bauer SR, Arroliga AC. A comparison of methohexital versus etomidate for endotracheal intubation of critically ill patients. Am J Crit Care. 2010;19(1):48-54. doi: 10.4037/ajcc2010562 [PubMed 20045848]
  15. Dionne RA, Yagiela JA, Moore PA, et al, “Comparing Efficacy and Safety of Four Intravenous Sedation Regimens in Dental Outpatients,” Am Dent Assoc, 2001, 132(6):740-51. [PubMed 11433853]
  16. Elman DS and Denson JS, "Preanesthetic Sedation of Children With Intramuscular Methohexital Sodium," Anesth Analg, 1965, 44(5):494-8. [PubMed 5890378]
  17. Farrell NM, Killius K, Kue R, Langlois BK, Nelson KP, Golenia P. A comparison of etomidate, ketamine, and methohexital in emergency department rapid sequence intubation. J Emerg Med. 2020;59(4):508-514. doi:10.1016/j.jemermed.2020.06.054 [PubMed 32739131]
  18. Folkerts H, “Spontaneous Seizure After Concurrent Use of Methohexital Anesthesia For Electroconvulsive Therapy and Paroxetine: A Case Report,” J Nerv Ment Dis, 1995, 183(2):115-6. [PubMed 7844577]
  19. Food and Drug Administration. FDA Drug Safety Communication: FDA review results in new warnings about using general anesthetics and sedation drugs in young children and pregnant women. https://www.fda.gov/Drugs/DrugSafety/ucm532356.htm. Published December 14, 2016. Accessed May 26, 2017.
  20. Forbes RB, Murray DJ, Dillman JB, et al, “Pharmacokinetics of Two Percent Rectal Methohexitone in Children,” Can J Anaesth, 1989, 36(2):160-4. [PubMed 2650897]
  21. Fredman B, d'Etienne J, Smith I, Husain MM, White PF. Anesthesia for electroconvulsive therapy: effects of propofol and methohexital on seizure activity and recovery. Anesth Analg. 1994;79(1):75-79. [PubMed 8010457]
  22. Ghoneim MM, Chiang CK, Schoenwald D, et al. The pharmacokinetics of methohexital in young and elderly subjects. Acta Anaesthesiol Scand. 1985;29(5):480-482. [PubMed 4036532]
  23. Holdcroft A, Robinson MJ, Gordon H, Whitwam JG. Comparison of effect of two induction doses of methohexitone on infants delivered by elective caesarean section. Br Med J. 1974;2(5917):472-475. [PubMed 4834097]
  24. Johns FR, Sandler NA, Buckley MJ, et al, “Comparison of Propofol and Methohexital Continuous Infusion Techniques for Conscious Sedation,” J Oral Maxillofac Surg, 1998, 56(10):1124-27. [PubMed 9766535]
  25. Korttila K, Linnoila M, Ertama P, Häkkinen S. Recovery and simulated driving after intravenous anesthesia with thiopental, methohexital, propanidid, or alphadione. Anesthesiology. 1975;43(3):291-299. [PubMed 1163829]
  26. Krauss B and Green SM, “Procedural Sedation and Analgesia in Children,” Lancet, 2006, 367(9512):766-80. [PubMed 16517277]
  27. Lee PF. Anaesthesia for Caesarean section with methohexital. Acta Anaesthesiol Scand Suppl. 1966;23:138-143. [PubMed 4952997]
  28. Lihua P, Su M, Ke W, Ziemann-Gimmel P. Different regimens of intravenous sedatives or hypnotics for electroconvulsive therapy (ECT) in adult patients with depression. Cochrane Database Syst Rev. 2014;(4):CD009763. [PubMed 24723301]
  29. Liu LM, Goudsouzian NG, Liu PL. Rectal methohexital premedication in children, a dose-comparison study. Anesthesiology. 1980;53(4):343-345. [PubMed 7425360]
  30. Loddenkemper T, Möddel G, Dinner DS, et al. Language assessment in Wada test: comparison of methohexital and amobarbital. Seizure. 2009;18(9):656-659. [PubMed 19800265]
  31. Manuli MA, Davies L. Rectal methohexital for sedation of children during imaging procedures. AJR Am J Roentgenol. 1993;160(3):577-580. [PubMed 8430557]
  32. Miller JR, Grayson M, and Stoelting VK, "Sedation With Intramuscular Methohexital Sodium for Office and Clinic Ophthalmic Procedures in Children," Am J Ophthalmol, 1966, 62(1):38-43. [PubMed 5936524]
  33. Olutoye OA, Baker BW, Belfort MA, Olutoye OO. Food and Drug Administration warning on anesthesia and brain development: implications for obstetric and fetal surgery. Am J Obstet Gynecol. 2018;218(1):98-102. [PubMed 28888583]
  34. Patel A, Wordell C, Szarlej D. Alternatives to sodium amobarbital in the Wada test. Ann Pharmacother. 2011;45(3):395-401. doi:10.1345/aph.1P476 [PubMed 21325100]
  35. Pomeranz ES, Chudnofsky CR, Deegan TJ, et al, “Rectal Methohexital Sedation for Computed Tomography Imaging of Stable Pediatric Emergency Department Patients,” Pediatrics, 2000, 105(5):1110-14. [PubMed 10790471]
  36. Quaynor H, Corbey M, Björkman S. Rectal induction of anaesthesia in children with methohexitone. Patient acceptability and clinical pharmacokinetics. Br J Anaesth. 1985;57(6):573-577. [PubMed 4005094]
  37. Reece-Stremtan S, Campos M, Kokajko L; Academy of Breastfeeding Medicine. ABM clinical protocol #15: analgesia and anesthesia for the breastfeeding mother, revised 2017. Breastfeed Med. 2017;12(9):500-506. [PubMed 29624435]
  38. Roberts J. Roberts and Hedges’ Clinical Procedures in Emergency Medicine and Acute Care. 7th ed. Elsevier; 2019.
  39. Rockoff MA, Goudsouzian NG. Seizures induced by methohexital. Anesthesiology. 1981;54(4):333-335. doi:10.1097/00000542-198104000-00015 [PubMed 7212335]
  40. Sedik H, “Use of Intravenous Methohexital as a Sedative in Pediatric Emergency Departments,” Arch Pediatr Adolesc Med, 2001, 155(6):665-8. [PubMed 11386953]
  41. Schwanda AE, Freyer DR, Sanfilippo DJ, et al, “Brief Unconscious Sedation for Painful Pediatric Oncology Procedures,” Am J Pediatr Hematol Oncol, 1993, 15(4):370-6. [PubMed 8214358]
  42. Stollings JL, Diedrich DA, Oyen LJ, Brown DR. Rapid-sequence intubation: a review of the process and considerations when choosing medications. Ann Pharmacother. 2014;48(1):62-76. doi:10.1177/1060028013510488 [PubMed 24259635]
  43. Urquhart ML and White PF, “Comparison of Sedative Infusions During Regional Anesthesia-Methohexital, Etomidate, and Midazolam,” Anest Analg, 1989, 68(3):249-54. [PubMed 2919762]
  44. Varner PD, Ebert JP, McKay RD, Nail CS, Whitlock TM. Methohexital sedation of children undergoing CT scan. Anesth Analg. 1985;64(6):643-645. [PubMed 4003782]
  45. Verma R, Ramasubramanian R, Sachar RM. Anesthesia for termination of pregnancy: midazolam compared with methohexital. Anesth Analg. 1985;64(8):792-794. [PubMed 3160263]
  46. Wells D, Davies G, and Wagner D, “Accidental Injection of Epidural Methohexital,” Anesthesiology, 1987, 67(5):846-8. [PubMed 3674498]
  47. Whitwam JG. Adverse reactions to i.v. induction agents. Br J Anaesth. 1978;50(7):677-687. doi:10.1093/bja/50.7.677 [PubMed 354663]
  48. Yemen TA, Pullerits J, Stillman R, Hershey M. Rectal methohexital causing apnea in two patients with meningomyeloceles. Anesthesiology. 1991;74(6):1139-1141. doi:10.1097/00000542-199106000-00024 [PubMed 2042766]
Topic 9629 Version 300.0

آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟