Version May 2024
Sodium oxybate is a CNS depressant. In clinical trials at recommended doses, obtundation and clinically significant respiratory depression occurred in adult patients treated with sodium oxybate. Many patients who received sodium oxybate during clinical trials in narcolepsy were receiving CNS stimulants.
Sodium oxybate is the sodium salt of gamma hydroxybutyrate (GHB). Abuse or misuse of illicit GHB, either alone or in combination with other CNS depressants, is associated with CNS adverse reactions including seizure, respiratory depression, decreases in the level of consciousness, coma, and death.
Because of the risks of CNS depression, abuse, and misuse, sodium oxybate is only available through a restricted program under a Risk Evaluation and Mitigation Strategy (REMS) called the Lumryz REMS or Xywav and Xyrem REMS.
Narcolepsy: Oral:
ER suspension (Lumryz): 4.5 g as a single dose at bedtime. May increase nightly dose by 1.5 g at weekly intervals based on efficacy and tolerability; recommended dosage range: 6 to 9 g once daily at night. Maximum dose: 9 g/night.
IR solution (Xyrem): Initial: 2.25 g at bedtime after the patient is in bed, and 2.25 g administered 2.5 to 4 hours later (4.5 g/night). May increase nightly dose by 1.5 g (0.75 g at bedtime and 0.75 g administered 2.5 to 4 hours later) at weekly intervals based on efficacy and tolerability; usual effective dosage range: 6 to 9 g per night. Maximum dose: 9 g/night.
Missed second dose: Skip dose and resume usual dosing schedule the next day. Do not administer 2 doses at the same time.
Switching from IR solution (Xyrem) to ER suspension (Lumryz): Administer the nearest total equivalent dose in grams once per night.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
ER suspension (Lumryz): Do not use as initial therapy in patients with hepatic impairment; patients who have been titrated to a maintenance dose on IR solution may be switched to the ER suspension if the appropriate dosage strength is available.
IR solution (Xyrem): Reduce initial dose(s) by 50%.
Refer to adult dosing; use with caution.
(For additional information see "Sodium oxybate (gamma hydroxybutyrate): Pediatric drug information")
Narcolepsy (excessive daytime sleepiness/cataplexy): Note: Nightly, 2 doses are administered; some patients may require unequal doses to achieve optimal response. Dosing is present in mg/kg and grams; use precaution.
Children ≥7 years and Adolescents:
Immediate-release oral solution (Xyrem):
<20 kg: Oral: Limited data available: Initial: 60 to 90 mg/kg/night (total dose) in 2 divided doses; the first dose administered at bedtime after the patient is in bed, then 2.5 to 4 hours later, administer the second dose; titrate every 1 to 2 weeks until efficacy or development of intolerable side effects. Reported maximum daily dose: 180 mg/kg/night (Ref).
20 to <30 kg: Oral: Initial: ≤1 g at bedtime after the patient is in bed, then 2.5 to 4 hours later, administer second dose of ≤1 g. After 1 week, titrate dose based on efficacy and tolerability at weekly intervals; increase dose in ≤0.5 g/dose (≤1 g/night) increments per week; maximum single dose: 3 g/dose; maximum daily dose: 6 g/night.
30 to <45 kg: Oral: Initial: ≤1.5 g at bedtime after the patient is in bed, then 2.5 to 4 hours later, administer second dose of ≤1.5 g. After 1 week, titrate dose based on efficacy and tolerability at weekly intervals; increase dose in ≤0.5 g/dose (≤1 g/night) increments per week; maximum single dose: 3.75 g/dose; maximum daily dose: 7.5 g/ night.
≥45 kg: Oral: Initial: ≤2.25 g at bedtime after the patient is in bed, then 2.5 to 4 hours later, administer second dose of ≤2.25 g . After 1 week, titrate dose based on efficacy and tolerability at weekly intervals; increase dose in ≤0.75 g/dose (1.5 g/night) increments per week; maximum single dose: 4.5 g/dose; maximum daily dose: 9 g/night.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Children ≥7 years and Adolescents: Immediate-release oral solution (Xyrem): Reduce initial total nightly dose by 50% and administer in 2 divided doses.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults unless otherwise indicated.
>10%:
Endocrine & metabolic: Weight loss (children and adolescents: 13%; adults: 1% to 4%)
Gastrointestinal: Nausea (children, adolescents, and adults: 6% to 20%), vomiting (children, adolescents, and adults: 2% to 18%)
Genitourinary: Urinary incontinence (children and adolescents: 19%; adults: 2% to 9%)
Nervous system: Confusion (2% to 17%), dizziness (children, adolescents, and adults: 4% to 15%), headache (children and adolescents: 17%; adults: 7%)
1% to 10%:
Cardiovascular: Peripheral edema (3%)
Dermatologic: Hyperhidrosis (1% to 3%)
Gastrointestinal: Decreased appetite (children and adolescents: 9%; adults: 3% to 4%), diarrhea (3% to 4%), upper abdominal pain (3%)
Nervous system: Anxiety (2% to 8%), depression (children, adolescents, adults: 1% to 7%), disorientation (2% to 3%), disturbance in attention (1% to 4%), drowsiness (2% to 8%), intoxicated feeling (3%), irritability (3%), pain (3%), paresthesia (2% to 3%), severe central nervous system depression (2%), somnambulism (children, adolescents, and adults: 1% to 6%), tremor (2% to 5%)
Neuromuscular & skeletal: Limb pain (3%)
<1%: Nervous system: Suicidal ideation (children, adolescents, adults), suicidal tendencies
Frequency not defined (all populations):
Hematologic & oncologic: Oxygen desaturation
Nervous system: Delirium, emotional disturbance (including obsessive thoughts), obtundation
Respiratory: Respiratory depression
Postmarketing (any population):
Cardiovascular: Hypertension
Endocrine & metabolic: Fluid retention
Genitourinary: Nocturia
Hypersensitivity: Hypersensitivity reaction
Nervous system: Aggressive behavior, agitation, drug abuse, falling, hallucination, hangover effect, memory impairment, panic attack, paranoid ideation, parasomnias (sleep driving, sleep eating) (Wallace 2011), psychosis (including acute psychosis) (Langford 2011)
Neuromuscular & skeletal: Arthralgia
Ophthalmic: Blurred vision
Respiratory: Sleep apnea (Hartley 2011)
Concomitant use with alcohol or sedative-hypnotic agents; succinic semialdehyde dehydrogenase deficiency
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to sodium oxybate or any component of the formulation
Concerns related to adverse effects:
• Behavioral and psychiatric effects: Use has been associated with aggression, agitation, anxiety, confusion, depression, paranoia, psychosis, suicidality, and hallucinations; use caution in patients with history of depression and/or suicide attempt.
• CNS depression: Sodium oxybate may impair physical or mental abilities. Patients must be instructed not to engage in hazardous activities requiring mental alertness or motor coordination for at least 6 hours after taking sodium oxybate.
• Parasomnias: Parasomnias, including sleepwalking, may occur with use. Evaluate episodes of sleepwalking and implement appropriate interventions.
• Respiratory depression: [US Boxed Warning]: In clinical trials at recommended doses, obtundation and clinically significant respiratory depression occurred in sodium oxybate-treated adult patients. Many of the patients who received sodium oxybate during clinical trials in narcolepsy were receiving CNS stimulants. Use with caution in patients with compromised respiratory function.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with heart failure or hypertension; contains significant amounts of sodium.
• Hepatic impairment: Use with caution in patients with hepatic impairment; dosage adjustment is recommended.
• Renal impairment: Use with caution in patients with renal impairment due to significant amounts of sodium in the product.
• Sleep-related breathing disorders: Sleep-related breathing disorders (eg, sleep apnea) may occur during therapy; may be more common in patients that are obese, male, postmenopausal (not on hormone-replacement therapy), or narcoleptic. In pediatric patients, central sleep apnea and oxygen desaturation has been reported.
Special populations:
• Older adult: Although limited data exists, headache was observed at a higher incidence in older adults ≥65 years of age compared to younger adults. Older adults may also be at increased risk for other CNS effects; use with caution and monitor cognitive/motor function closely.
Other warnings/precautions:
• Abuse/misuse/diversion: [US Boxed Warning]: Sodium oxybate (the sodium salt of gamma hydroxybutyrate [GHB]) is a CNS depressant controlled substance with abuse potential. Seizures, respiratory depression, decreases in level of consciousness, coma, and death have been reported when GHB, either alone or in combination with other CNS depressants, has been abused. Health care providers should be alert to problems of abuse, misuse, and diversion. Patients should be evaluated for a history of drug abuse and should be monitored for signs of misuse, abuse, and substance use disorder.
• Sodium: Contains high sodium content: Use with caution in patients sensitive to high sodium intake (eg, renal impairment, heart failure, hypertension).
• Tolerance/withdrawal: Tolerance to sodium oxybate, or withdrawal following its discontinuation, has not been clearly defined in controlled clinical trials, but has been reported at larger doses used for illicit purposes.
Sodium content for various doses:
|
Total nightly sodium oxybate dose |
Sodium content |
|---|---|
|
3 g |
550 mg |
|
4.5 g |
820 mg |
|
6 g |
1,100 mg |
|
7.5 g |
1,400 mg |
|
9 g |
1,640 mg |
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Packet, Oral:
Lumryz: 4.5 g (7 ea, 30 ea); 6 g (7 ea, 30 ea); 7.5 g (7 ea, 30 ea); 9 g (7 ea, 30 ea) [contains carrageenan]
Solution, Oral:
Xyrem: 500 mg/mL (180 mL)
Generic: 500 mg/mL (180 mL)
May be product dependent
Pack (Lumryz Oral)
4.5 g (per each): $366.66
6 g (per each): $488.88
7.5 g (per each): $611.10
9 g (per each): $733.32
Solution (Sodium Oxybate Oral)
500 mg/mL (per mL): $40.13 - $41.63
Solution (Xyrem Oral)
500 mg/mL (per mL): $44.27
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.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Oral:
Xyrem: 500 mg/mL (180 mL)
C-I (illicit use); C-III (medical use)
Access to sodium oxybate is restricted under the Lumryz REMS or the Xywav and Xyrem REMS. The programs are intended to ensure health care providers are specially certified and is dispensed only by specially certified pharmacies. Patients must also enroll in the program and have documentation of safe use conditions. Further information regarding the Lumryz REMS program may be obtained at 1-877-453-1029 or for the Xywav and Xyrem REMS at 1-866-997-3688 or http://www.xywavxyremrems.com.
In Canada, access to sodium oxybate is restricted under the Xyrem Success Program. The program is intended to educate prescribers, pharmacists, and patients on the safe use, storage, and handling of the drug, to maintain a registry of trained physicians, pharmacies, and patients, and to limit distribution through a single wholesaler to pharmacies on an as-needed basis after a prescription is received by the pharmacy. Initial dispensing of prescriptions should occur only after the prescriber, pharmacist, and patient have received and read the educational materials. Further information regarding the program may be obtained at 1-866-599-7365.
Oral: Administer on an empty stomach, ≥2 hours after eating. Administer while patient is in bed; patient should lie down immediately after dose and remain in bed.
ER suspension (Lumryz): Administer at bedtime. Prepare dose prior to bedtime. Prior to ingestion, suspend dose in ~1/3 cup (~80 mL) of water in provided mixing cup; do not use hot water. Administer within 30 minutes of mixing.
IR solution (Xyrem): Administer first dose at bedtime. Administer second nightly dose 2.5 to 4 hours after the first dose; an alarm clock may need to be set for the second dose. Prepare both doses prior to bedtime. Prior to ingestion, dilute each dose with ~1/4 cup (60 mL) water in provided empty pharmacy containers.
Oral: Immediate-release oral solution (Xyrem): Administer on an empty stomach (at least 2 hours after eating); administration at similar times each night is preferred. Each nightly dose should be administered while patient is sitting up in bed; then patient should lie down and remain in bed; sleep generally occurs within 5 to 15 minutes (generally abruptly without patient feeling drowsy). Both doses should be prepared prior to bedtime. The first dose is administered at bedtime and the second dose 2.5 to 4 hours later; an alarm clock may need to be set for the second dose. For patients who sleep >8 hours per night the first dose may be administered at bedtime or after an initial period of sleep. After use, rinse containers with water.
Missed dose: If the second dose is missed, skip that dose and resume therapy the next night; do not administer both doses at the same time. Diluted doses that are not used should be properly and promptly disposed.
An FDA-approved patient medication guide, which is available with the product information and at https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/021196s042lbl.pdf#page=26, must be dispensed with this medication.
Narcolepsy: Treatment of cataplexy or excessive daytime sleepiness in adult patients with narcolepsy and pediatric patients ≥7 years of age with narcolepsy (Xyrem only).
Sodium oxybate may be confused with oxybate salts (calcium, magnesium, potassium, and sodium).
Xyrem may be confused with Xywav.
None known.
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): May enhance the CNS depressant effect of Oxybate Salt Products. Alcohol (Ethyl) may increase the serum concentration of Oxybate Salt Products. Specifically, alcohol may increase concentrations of the sodium oxybate extended release suspension. Risk X: Avoid combination
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
Benzodiazepines: May enhance the CNS depressant effect of Oxybate Salt Products. 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
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 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
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
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
Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. 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
Hypnotics (Nonbenzodiazepine): May enhance the CNS depressant effect of Oxybate Salt Products. Risk X: Avoid combination
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
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
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
Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. 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
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
Rilmenidine: Oxybate Salt Products may enhance the CNS depressant effect of Rilmenidine. Risk X: Avoid combination
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
Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination
Valerian: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Valproate Products: May increase the serum concentration of Sodium Oxybate. Management: Decrease the dose of sodium oxybate immediate release oral solution by at least 20% when initiating therapy with valproate products. No dose adjustment recommended when sodium oxybate extended release suspension is combined with valproate products. 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
Administration immediately after a high-fat meal delays absorption and decreases peak serum gamma-hydroxybutyrate level. Management: Administer on an empty stomach ≥2 hours after eating.
The injection formulation, when used as an anesthetic during labor and delivery, was shown to cross the placenta; a slight decrease in Apgar scores due to sleepiness in the neonate was observed.
Gamma hydroxybutyrate is endogenous to breast milk; concentrations increase following oral administration of sodium oxybate. Based on initial studies, breastfeeding should be avoided between the 2 bedtime doses and for 6 to 8 hours following the second nighttime dose to limit exposure to the infant (Barker 2017; Busardò 2016). According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.
Contains a high sodium content; limit dietary intake of sodium.
Signs and symptoms of depression or suicidality; emergence of anxiety, confusion, thought disorders, or behavior abnormalities; drug abuse, misuse, and substance use disorder.
The active moiety of sodium oxybate is gamma-hydroxybutyrate (GHB). The therapeutic effects of GHB, a metabolite of gamma aminobutyric acid (GABA), are hypothesized to be mediated by GABAB receptor activity at noradrenergic, dopaminergic, and thalamocortical neurons.
Note: Pharmacokinetic parameters in pediatric patients 7 to 17 years were reported as being similar to adult patients.
Onset: Rapid (≤5 to 15 minutes).
Absorption: Rapid; high-fat meals delay absorption (average Tmax increased 1 hour [extended release] and 1.25 hours [immediate release]) and reduce the Cmax by a mean 33% (extended release), 59% (immediate release) and AUC by 14% (extended release), 37% (immediate release).
Distribution: 190 to 384 mL/kg.
Protein binding: <1%.
Metabolism: Primarily via the Krebs cycle to form water and carbon dioxide; secondarily via beta oxidation; significant first-pass effect; no active metabolites; metabolic pathways are saturable.
Bioavailability: ~88%.
Half-life elimination: 30 to 60 minutes.
Time to peak: Extended release: 90 minutes; Immediate release: 30 to 75 minutes.
Excretion: Primarily pulmonary (as carbon dioxide); urine (<5% as unchanged drug); feces (negligible).
Hepatic function impairment: AUC is doubled, elimination half-life is longer, and oral clearance is reduced in cirrhotic patients (Child-Pugh class A and C).
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