Dosing & Uses
Dosage Forms & Strengths
powder for injection: Schedule IV
- 500mg
- 2.5g
Anesthesia
Induction: 50-120 mg (70 mg average) IV push at 10 mg ( 1 mL of 1% solution) over 5 seconds, depending on patient response
Maintenance: 20-40 mg (2-4 mL of 1% soluiton) IV push q4-7min PRN, OR 4-6 mg/min IV drip
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (12)
- abemaciclib
methohexital will decrease the level or effect of abemaciclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- benzhydrocodone/acetaminophen
benzhydrocodone/acetaminophen, methohexital. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation. Increased risk of hypotension if ability to maintain blood pressure has been compromised by a reduced blood volume or concurrent administration of certain CNS depressant drugs (eg, phenothiazines or general anesthetics).
- fentanyl
fentanyl, methohexital. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.
- fentanyl intranasal
fentanyl intranasal, methohexital. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.
- fentanyl transdermal
fentanyl transdermal, methohexital. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.
- fentanyl transmucosal
fentanyl transmucosal, methohexital. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration with other CNS depressants, such as skeletal muscle relaxants, may cause respiratory depression, hypotension, profound sedation, coma, and/or death. Consider dose reduction of either or both agents to avoid serious adverse effects. Monitor for hypotension, respiratory depression, and profound sedation.
- hydrocodone
hydrocodone, methohexital. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Profound sedation, respiratory depression, coma, and death may result if coadministered. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation. Increased risk of hypotension if ability to maintain blood pressure has been compromised by a reduced blood volume or concurrent administration of certain CNS depressant drugs (eg, phenothiazines or general anesthetics).
- isocarboxazid
isocarboxazid, methohexital. Other (see comment). Contraindicated. Comment: CNS depressants such as barbiturates should not be used in combination with isocarboxazid.
- metoclopramide intranasal
methohexital, metoclopramide intranasal. Either increases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Avoid use of metoclopramide intranasal or interacting drug, depending on importance of drug to patient.
- ropeginterferon alfa 2b
ropeginterferon alfa 2b and methohexital both increase Other (see comment). Avoid or Use Alternate Drug. Narcotics, hypnotics or sedatives can produce additive neuropsychiatric side effects. Avoid use and monitor patients receiving the combination for effects of excessive CNS toxicity.
- selinexor
selinexor, methohexital. unspecified interaction mechanism. Avoid or Use Alternate Drug. Patients treated with selinexor may experience neurological toxicities. Avoid taking selinexor with other medications that may cause dizziness or confusion.
- sufentanil SL
sufentanil SL, methohexital. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may result in hypotension, profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing of these drugs in patients for whom other treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor closely for signs of respiratory depression and sedation.
Monitor Closely (23)
- abiraterone
methohexital will decrease the level or effect of abiraterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- acrivastine
acrivastine and methohexital both increase sedation. Use Caution/Monitor.
- amifostine
amifostine, methohexital. Either increases effects of the other by anti-hypertensive channel blocking. Use Caution/Monitor. Monitor hemodynamic changes, specifically for signs of hypotension, if using barbiturates with blood pressure lowering medications. .
- amisulpride
amisulpride and methohexital both increase sedation. Use Caution/Monitor.
- asenapine
asenapine and methohexital both increase sedation. Use Caution/Monitor.
- asenapine transdermal
asenapine transdermal and methohexital both increase sedation. Use Caution/Monitor.
- benazepril
methohexital increases toxicity of benazepril by unspecified interaction mechanism. Use Caution/Monitor.
- brexanolone
brexanolone, methohexital. Either increases toxicity of the other by sedation. Use Caution/Monitor.
- bupivacaine implant
methohexital, bupivacaine implant. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Local anesthetics may increase the risk of developing methemoglobinemia when concurrently exposed to drugs that also cause methemoglobinemia.
- buprenorphine, long-acting injection
methohexital increases toxicity of buprenorphine, long-acting injection by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of buprenorphine and benzodiazepines or other CNS depressants increases risk of adverse reactions including overdose, respiratory depression, and death. Cessation of benzodiazepines or other CNS depressants is preferred in most cases. In some cases, monitoring at a higher level of care for tapering CNS depressants may be appropriate. In others, gradually tapering a patient off of a prescribed benzodiazepine or other CNS depressant or decreasing to the lowest effective dose may be appropriate.
- captopril
methohexital, captopril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Both drugs lower blood pressure. Monitor blood pressure.
- daridorexant
methohexital and daridorexant both increase sedation. Modify Therapy/Monitor Closely. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.
- deutetrabenazine
methohexital and deutetrabenazine both increase sedation. Use Caution/Monitor.
- difelikefalin
difelikefalin and methohexital both increase sedation. Use Caution/Monitor.
- ganaxolone
methohexital and ganaxolone both increase sedation. Use Caution/Monitor.
- lasmiditan
lasmiditan, methohexital. Either increases effects of the other by sedation. Use Caution/Monitor. Coadministration of lasmiditan and other CNS depressant drugs, including alcohol have not been evaluated in clinical studies. Lasmiditan may cause sedation, as well as other cognitive and/or neuropsychiatric adverse reactions.
- lemborexant
lemborexant, methohexital. Either increases effects of the other by sedation. Modify Therapy/Monitor Closely. Dosage adjustment may be necessary if lemborexant is coadministered with other CNS depressants because of potentially additive effects.
- lurasidone
lurasidone, methohexital. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Potential for increased CNS depressant effects when used concurrently; monitor for increased adverse effects and toxicity.
- midazolam intranasal
midazolam intranasal, methohexital. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Concomitant use of barbiturates, alcohol, or other CNS depressants may increase the risk of hypoventilation, airway obstruction, desaturation, or apnea and may contribute to profound and/or prolonged drug effect.
- remimazolam
remimazolam, methohexital. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely. Coadministration may result in profound sedation, respiratory depression, coma, and/or death. Continuously monitor vital signs during sedation and recovery period if coadministered. Carefully titrate remimazolam dose if administered with opioid analgesics and/or sedative/hypnotics.
- sparsentan
sparsentan will decrease the level or effect of methohexital by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Sparsentan (a CYP2C19 inducer) decreases exposure of CYP2C19 substrates and reduces efficacy related to these substrates.
- stiripentol
stiripentol, methohexital. Either increases effects of the other by sedation. Use Caution/Monitor. Concomitant use stiripentol with other CNS depressants, including alcohol, may increase the risk of sedation and somnolence.
- suvorexant
suvorexant and methohexital both increase sedation. Modify Therapy/Monitor Closely. Dosage adjustments of suvorexant and concomitant CNS depressants may be necessary
Minor (2)
- probenecid
probenecid increases levels of methohexital by unknown mechanism. Minor/Significance Unknown.
- sulfisoxazole
sulfisoxazole increases levels of methohexital by plasma protein binding competition. Minor/Significance Unknown.
Adverse Effects
Frequency Not Defined
Hiccups, coughing, muscle twitching & laryngospasm, which may impair pulmonary ventilation
Respiratory depression, apnea, dyspnea, cardiorespiratory arrest (which may occur in association with seizures), or hypotension may occur
Circulatory depression, peripheral vasculatory collapse, bronchospasm, postanesthetic shivering, salivation, skeletal muscle hyperactivity (twitching to convulsive-like movements), seizures, restlessness, anxiety (especially in the presence of postop pain), headache, nausea, vomiting, abd pain, & emergence delirium may also occur
Acute allergic reactions including erythema, pruritus, urticaria, rhinitis, hypotension, dyspnea, anxiety, restlessness, abdominal pain & peripheral vascular collapse have been reported
Thrombophlebitis, injection site pain, & injury to nerves adjacent to injection site
Extravasation may cause local irritation manifested as pain, swelling, ulceration, & necrosis
Warnings
Black Box Warnings
Methohexital should be used in hospital or ambulatory care settings that can provide continuous monitoring of respiratory (eg, pulse oximetry) and cardiac function
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 should be readily available
For deeply sedated patients, a designated individual other than the practitioner performing the procedure should be present to continuously monitor the patient
Contraindications
Known hypersensitivity to barbiturates
Patients in whom general anesthesia contraindicated
Patients with latent or manifest porphyria
Cautions
Caution in severe anemia, extreme obesity, debilitated patients
Rapid bolus doses will increase cardiorespiratory effects including laryngospasm, apnea, hypotension, myocardial depression, cardiovascular collapse
Mild sedation may persist 8-12 hr
Patients should be instructed on discharge not to drive or operate heavy machinery
All routes of administration are often associated with hiccups, coughing, and/or muscle twitching, which may also impair pulmonary ventilation; following induction, temporary hypotension and tachycardia may occur
Recovery from methohexital anesthesia is rapid and smooth; the incidence of postoperative nausea and vomiting is low if the drug is administered to fasting patients; postanesthetic shivering has occurred in a few instances
The usual precautions taken with any barbiturate anesthetic should be observed with this drug; the drug should be used with caution in patients with asthma, obstructive pulmonary disease, severe hypertension or hypotension, myocardial disease, congestive heart failure, severe anemia, or extreme obesity
Use with extreme caution in patients in status asthmatics; caution should be exercised in debilitated patients or in those with impaired function of respiratory, circulatory, renal, hepatic, or endocrine systems
This drug should be used only in hospital or ambulatory care settings that provide for continuous monitoring of respiratory (eg. Pulse oximetry) and cardiac function; 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 should be assured
Maintenance of a patent airway and adequacy of ventilation must be ensured during induction and maintenance of anesthesia with methohexital sodium solution; laryngospasm is common during induction with all barbiturates and may be due to a combination of secretions and accentuated reflexes following induction or may result from painful stimuli during light anesthesia; apnea/hypoventilation may be noted during induction, which may impair pulmonary ventilation; the duration of apnea may be longer than that produced by other barbiturate anesthetics; cardiorespiratory arrest may occur
Although the published literature discusses intravenous administration in pediatric patients, the safety and effectiveness of intravenous administration of methohexital sodium in pediatric patients have not been established in well-controlled, prospective studies
Seizures may be elicited in subjects with a previous history of convulsive activity, especially partial seizure disorders
Because the liver is involved in demethylation and oxidation of methohexital and because barbiturates may enhance preexisting circulatory depression, severe hepatic dysfunction, severe cardiovascular instability, or a shock-like condition may be reason for selecting another induction agent
Prolonged administration may result in cumulative effects, including extended somnolence, protracted unconsciousness, and respiratory and cardiovascular depression; respiratory depression in the presence of an impaired airway may lead to hypoxia, cardiac arrest, and death
The CNS-depressant effect of this drug may be additive with that of other CNS depressants, including ethyl alcohol and propylene glycol
Danger of intra-arterial injection
- Unintended intra-arterial injection of barbiturate solutions may be followed by the production of platelet aggregates and thrombosis, starting in arterioles distal to the site of injection; the resulting necrosis may lead to gangrene, which may require amputation
- The first sign in conscious patients may be a complaint of fiery burning that roughly follows the distribution path of the injected artery; if noted, the injection should be stopped immediately and the situation reevaluated; transient blanching may or may not be noted very early; blotchy cyanosis and dark discoloration may then be the first sign in anesthetized patients
- There is no established treatment other than prevention; the following should be considered prior to injection:
- 1. The extent of injury is related to concentration: Concentrations of 1% methohexital will usually suffice; higher concentrations should ordinarily be avoided
- 2. Check the infusion to ensure that the catheter is in the lumen of a vein before injection; injection through a running intravenous infusion may enhance possibility of detecting arterial placement; however, it should be remembered that the characteristic bright-red color of arterial blood is often altered by contact with drugs; the possibility of aberrant arteries should always be considered
- Post injury arterial injection of vasodilators and/or arterial infusion of parenteral fluids are generally regarded to be of no value in altering outcome; animal experiments and publishedindividual case reports concerned with a variety of arteriolar irritants, including barbiturates, suggest that 1 or more of the following may be of benefit in reducing the area of necrosis
- 1. Arterial injection of heparin at the site of injury, followed by systemic anticoagulation
- 2. Sympathetic blockade (or brachial plexus blockade in the arm)
- 3. Intra-arterial glucocorticoid injection at the site of injury followed by systemic steroids
- 4. A case report (nonbarbiturate injury) suggests that intra-arterial urokinase may promote fibrinolysis, even if administered late in treatment
- If extravasation is noted during injection, the injection should be discontinued until the situation is remedied; local irritation may result from extravasation; subcutaneous swelling may also serve as a sign of arterial or periarterial placement of the catheter
Pediatric neurotoxicity
- The clinical significance of these findings is not clear; however, based on available data, the window of vulnerability to these changes is believed to correlate with exposures in the third trimester of gestation through first several months of life but may extend out to approximately three years of age in humans
- Some published studies in children suggest that similar deficits may occur after repeated or prolonged exposures to anesthetic agents early in life and may result in adverse cognitive or behavioral effects; these studies have substantial limitations, and it is not clear if the observed effects are due to the anesthetic/sedation drug administration or other factors such as the surgery or underlying illness
- Anesthetic and sedation drugs are a necessary part of the care of children needing surgery, other procedures, or tests that cannot be delayed, and no specific medications have been shown to be safer than any other; decisions regarding the timing of any elective procedures requiring anesthesia should take into consideration the benefits of the procedure weighed against potential risks
-
Brain development
- Prolonged or repeated exposure may result in negative effects on fetal or young children’s brain development
- Caution with use during surgeries or procedures in children younger than 3 yr or in pregnant women during their third trimester
- Administration of anesthetic and sedation drugs that block NMDA receptors and/or potentiate GABA activity increase neuronal apoptosis in developing brain and result in long-term cognitive deficits when used for longer than 3 hours; assess the risk:benefit ratio in these populations, especially for prolonged procedures (ie, >3 hr) or multiple procedures
Pregnancy & Lactation
Pregnancy
There are no adequate and well-controlled studies in pregnant women; published studies in pregnant primates demonstrate that administration of anesthetic and sedation drugs that block NMDA receptors and/or potentiate GABA activity during the period of peak brain development increases neuronal apoptosis in the developing brain of the offspring when used for longer than 3 hours; clinical significance not clear; however, studies in juvenile animals suggest neuroapoptosis correlates with long-term cognitive deficits
Lactation
Excreted in breast milk; use by nursing mothers should be evaluated carefully
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Ultra short-acting anesthetic barbiturate; no muscle relaxant activity
Pharmacokinetics
Half-Life: 3-6 hr
Onset: Immediate (IV); 2-10 min (IM); 5-15 min (PR)
Duration: 10-20 min (IV); 45 min (PR)
Metabolism: Hepatically conjugated to inactive metabolites; slow
Excretion: Urine; trace amounts of drug &/or metabolites also excreted in feces & sweat
Administration
IV Compatibilities
Solution: D5/LR, D5W in NS, D5W, LR, NS
Additive: chlorpromazine, hydralazine, kanamycin, lidocaine, mechlorethamine, methyldopate, prochlorperazine, promazine, promethazine, streptomycin
Syringe: glycopyrrolate
IV Administration
Do not use diluents containing bacteriostats
Soln should be clear or colorless or it should not be used
Administer by injection or infusion, in concentration no higher than 1%
Avoid intraarterial injection & extravasation
Storage
Store at controlled room temp
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Brevital injection - | 500 mg vial |  | |
| Brevital injection - | 2.5 gram vial |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
methohexital injection
NO MONOGRAPH AVAILABLE AT THIS TIME
USES: Consult your pharmacist.
HOW TO USE: Consult your pharmacist.
SIDE EFFECTS: Consult your pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Consult your pharmacist.
DRUG INTERACTIONS: Consult your pharmacist.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: No monograph available at this time.
MISSED DOSE: Consult your pharmacist.
STORAGE: Consult your pharmacist.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.
Information last revised July 2016. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
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