It is crucial to keep yourself and your loved ones safe during the COVID-19 outbreak. Yet addiction may pose even a higher danger than the virus.

Learn about recovery during the pandemic:

GHB Uses And Dosage. Xyrem Mechanism Of Action

ghb uses, dosages, and MOA

Important InformationThis information is for educational purposes only. We never invite or suggest the use, production or purchase of any these substances. Addiction Resource and it’s employees, officers, managers, agents, authors, editors, producers, and contributors shall have no direct or indirect liability, obligation, or responsibility to any person or entity for any loss, damage, or adverse consequences alleged to have happened as a consequence of material on this website. See full text of disclaimer.

Being a psychoactive drug, gamma-hydroxybutyrate is used for treating sleeping disorders in patients with narcolepsy. GHB medical use also includes off-label indications such as alcohol and opioid withdrawal and fibromyalgia. However, recently the substance has become more popular among bodybuilders and youngsters at the parties as a drug of abuse. The information in this article is determined to examine what purposes Xyrem is used for, its label and off-label indications, and appropriate dosages for different age groups.

Help Line Woman

Hope Without Commitment

Find the best treatment options. Call our <strong>free and confidential</strong> helpline

Most private insurances accepted

Marketing fee may apply

Learn About GHB Uses & MOA:

Illegal Uses Of GHB

GHB as Date Rape Drug

GHB is a date rape drug. Among other features, GHB is easily soluble and does not have any smell, only slightly salty taste; that is why it is usually mixed with alcoholic beverages for stronger sedative and amnesic effects. Sexual predators use GHB as a party drug for its quick effect on the victims that help to relax their muscles voluntarily and induce prolonged amnesia for events that occur under the influence of the drug.

In the case of being involved in such a situation, one should immediately call the police and visit the hospital for health monitoring and drug testing. If a victim addressed the police over a long time, the GHB hair test still can be conducted to prove the presence of a drug.

GHB Use In Bodybuilding

Another illicit use of sodium oxybate is spread among athletes and bodybuilders to improve their performance. Some users take GHB for bodybuilding activities because the drug activates the dopamine release, increases hormone release, invokes restful sleep, and stimulates fat metabolism, which tends to become causes of further abuse. Such hormone growth leads to increased muscle mass and decreased fat mass. However, GHB and bodybuilding should not be considered as a solution for extra muscles. On the contrary, the substance provides a temporary spike on muscle growth and does not work as anabolic. Users should take into account dangerous side effects and both physical and psychological dependence.

GHB Use At Party Raves

Some users report about GHB recreational use as doping at nightlife occasions and raves, mostly accompanied by electronic music and Rampal dancing. GHB produces a feeling of euphoria and increases sociability and is used instead of ecstasy or even with it. According to the information from users, the drug is popular within the LGBT+ community. Often, patients are transported from night clubs to hospitals with severe intoxication resulted from polydrug use. Such conditions require substance abuse treatment under medical supervision.

xyrem for sleep

GHB Medical Uses

Xyrem For Sleep Disorders In Patients With Narcolepsy

Sodium oxybate use is associated with dose-related improvements in treating symptoms of narcolepsy, in particular, cataplexy in narcolepsy and excessive daytime sleepiness. Xyrem for narcolepsy showed a reduction in the number of attacks of cataplexy. Comparing to other drugs such as antidepressants and stimulants typically used to treat the disorder, only using Xyrem for insomnia helps to deal with both symptoms of narcolepsy with a lower chance of developing tolerance and unwelcome side effects. The use of Xyrem for sleep is an FDA-approved approach of narcolepsy treatment.

Xyrem For Alcohol Withdrawal

According to clinical studies, a prescription of gamma-hydroxybutyric acid may ease the symptoms of alcohol withdrawal and restrain from alcohol consumption. Only about 10-15% of patients had craving episodes within the treatment program. During three months of the research on how to use GHB for alcohol withdrawal symptoms, the drug showed much better results than a placebo in the total number of abstinent days and alcohol craving. Moreover, Xyrem was more effective than diazepam in treating alcohol withdrawal symptoms and as equally efficient as clomethiazole. On the other hand, there is still more research that needs to be done to confirm the prevalence of GHB prescription effectiveness over its harm.

Xyrem For Opioid Withdrawal

In double-blind placebo-controlled research, GHB medical use showed positive results in suppressing opioid withdrawal in 14 heroin and 13 methadone users. The effect from gamma-hydroxybutyric acid occurred 15 minutes after the oral administration and lasted for 2 and 3 hours, respectively. Later the patients received the dose every 2 to 4 hours for the first 2 days and 4 to 6 hours for the following 6 days. Such an approach suppressed the most abstinence symptoms and improved patients’ overall state. After 8 days of treatment, users reported the absence of withdrawal symptoms, and their program was changed with an intravenous injection of 0.4 mg naloxone. So, doctors issue a recipe for GHB off-label for treating alcohol withdrawal.

xyrem for pain

Xyrem For Fibromyalgia

Several research papers investigated the use of Xyrem for fibromyalgia. They showed the efficiency of GHB use to deal with fibromyalgia symptoms, reducing pain, sleep disturbances, and fatigue over time.

A 14-week, randomized, controlled trial studied the effect of GHB versus placebo in 548 patients with fibromyalgia. There were more than 30% less pain in 54.2% and 58.5% of patients treated with sodium oxybate 4.5g and 6g per night, respectively, versus 35.2% for placebo. Improvements in physical condition were also much better after GHB use than placebo. However, a number of the adverse effects occurred in 5% of the patients treated with GHB; it is twice higher than after the placebo treating program.

Despite proven efficiency, FDA Panel rejects Xyrem as fibromyalgia treatment because of high abuse potential and possible GHB withdrawal treatment.

GHB Dosage For Excessive Daytime Sleepiness

Xyrem Dosage For Adults

According to the FDA guide, the starting GHB dosage for adults is 4.5 grams (g) per night administered orally. The dosage should be divided into 2 parts taking 2.25 g at the bedtime and 2.25 g taken 2.5-4 hours later. In order to reach the most effective result, the dose can be increased by 1.5 g per night every week (additional 0.75 g at bedtime and 0.75 g taken 2.5-4 hours later). The most efficient results of treatment were obtained after taking the dose of 6 g to 9 g per night. There is a lack of investigation about taking GHB in larger amounts; that is why the dosage more than 9 g should not be used.

Patients with hepatic impairment should be prescribed to take one-half of the starting dose per night, administered orally, and also divide it into two doses. Patients sensitive to salt intake should consider the amount of daily sodium intake in each dose of Xyrem dosage because of the high salt content in GHB.

Xyrem Dosage & Schedule For Pediatric Patients

There is a strict determination for pediatric patients on how much GHB to take. The liquid GHB dose is calculated by weight and taken twice per night (the dosage should be divided into 2 parts taking one part at the bedtime and second part 2.5-4 hours later). The dosage may be gradually increased and/or unequally divided based on efficacy and tolerability.

Child weightInitial doseTitration (max weekly increase)Maximal dose
20-30 kg≤2 g1 g6 g
30-45 kg≤3 g1 g7.5 g
45 kg and more≤4.5 g1.5 g9 g
For patients who sleep more than 8 hours per night, the first dose of Xyrem may be given at bedtime or after an initial period of sleep. If the patient is under 7 years old and weighs less than 20 kilos, the lower Xyrem dosing should be considered during the treatment period.

How To Administer Xyrem

  • The first GHB dosage should be taken at least 2 hours after eating.
  • Before the ingestion, each dose of the medicine should be mixed with approximately ¼ cup (approximately 60 mL) of water in the provided container.
  • Patients have to prepare both dosages before bedtime and take them while in the bed and lie down immediately because Xyrem acts fast, and the patient may suddenly fall asleep without first feeling dozy. Usually, patients fall asleep in 5-15 minutes after the administration; however, the time depends on the person and varies from night-to-night.
  • It is recommended to set the alarm to awaken for the second dose.
If the Xyrem dosage schedule is disrupted and the second dosage is missed, the patient should delay taking another dose until next night. Both dosages should never be taken simultaneously.

Contraindications & Warnings

It is important to remember how GHB is used. Due to the rapid influence on the central nervous system, sodium oxybate should be administered only at bedtime while being in bed. For at least 6 hours after the ingestion, the user should not be involved in any activities that need complete mental alertness or motor coordination. At the beginning of taking Xyrem, the patient should monitor the possible side effects of GHB or after-action of GHB the next day. If any symptom appears, one should avoid activities connected with full mental alertness or motor coordination.

Users should stay away from taking Xyrem in combination with other CNS depressants (including alcohol) and sedative-hypnotics because of the increased risk of respiratory depression, hypotension, profound sedation, syncope, and even GHB overdose death. If any of CNS depressants or opioids are necessary for treatment, GHB use should be discussed with the attending physician. Also, taking GHB can cause suicidal thoughts and attempts. If a patient has a history of mental disorders, it is important to let the treating physician know. Abuse and consequently developed addiction are also possible. In such cases, treatment in a professional rehabilitation center for substance abuse is required.

xyrem MOA

Sodium Oxybate Mechanism Of Action

What Does GHB Do?

Oxybate (GHB) is a metabolite of γ-aminobutyric acid (GABA), which is synthesized and accumulated by neurons in the brain. Xyrem mechanism of action is bringing about ‘delta’ (slow) brain waves and night-time sleep. With the appropriate amount of GHB taken in bedtime, a person gets a deeper sleep, and the duration of the sleeping session prolongs. However, the full sodium oxybate mechanism of action is not studied completely; the fact is that its therapeutic effects are caused by influencing noradrenergic, dopaminergic, and thalamocortical neurons.

How Long Does GHB Last?

Generally, the effect of using Xyrem occurs in 5-15 minutes and lasts for about 3 hours. The absolute bioavailability is approximately 88%, and the most effective results are achieved in 30.7-51.9 minutes. However, GHB duration depends on the dose and person themself. The patient should be careful about the dosage one takes, because even a small amount under some circumstances may switch the desired effect to the overdose.

How To Prevent GHB Misuse

Despite the range of research, the Xyrem pharmacology is complex and needs to be studied more. Even being used for clinical treatment, Xyrem prescription form should be supervised by a doctor according to the health indications. Any improper use of the drug may cause intoxication, severe adverse effects, and even death. An insatiable desire to use the substance for recreational purposes signals for dependence. In such cases, one need should immediately address rehab for GHB abuse to get professional help.

Help Line Woman

Hope Without Commitment

Find the best treatment options. Call our <strong>free and confidential</strong> helpline

Most private insurances accepted

Marketing fee may apply

View Sources
  1. Takahara J, Yunoki S, Yakushiji W, Yamauchi J, Yamane Y. Stimulatory effects of gamma-hydroxybutyric acid on growth hormone and prolactin release in humans. The Journal of Clinical Endocrinology and Metabolism. 1977; 44(5): 1014‐1017. doi:10.1210/jcem-44-5-1014. https://pubmed.ncbi.nlm.nih.gov/858775/.
  2. Kapoor P, Deshmukh R, Kukreja I. GHB acid: A rage or reprive. Journal of Advanced Pharmaceutical Technology & Research. 2013; 4(4): 173‐178. doi:10.4103/2231-4040.121410. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3853692/.
  3. Mayer G. The use of sodium oxybate to treat narcolepsy. Expert Review of Neurotherapeutics. 2012; 12(5): 519‐529. doi:10.1586/ern.12.42. https://pubmed.ncbi.nlm.nih.gov/22550980/.
  4. Scharf MB. Sodium oxybate for narcolepsy. Expert Review of Neurotherapeutics. 2006; 6(8): 1139‐1146. doi:10.1586/14737175.6.8.1139. https://pubmed.ncbi.nlm.nih.gov/16893342/.
  5. Caputo F, Vignoli T, Maremmani I, Bernardi M, Zoli G. Gamma hydroxybutyric acid (GHB) for the treatment of alcohol dependence: a review. International Journal of Environmental Research and Public Health. 2009; 6(6): 1917‐1929. doi:10.3390/ijerph6061917. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2705225/.
  6. Gallimberti L, Cibin M, Pagnin P, et al. Gamma-hydroxybutyric acid for treatment of opiate withdrawal syndrome. Neuropsychopharmacology. 1993; 9(1): 77‐81. doi:10.1038/npp.1993.45. https://pubmed.ncbi.nlm.nih.gov/8397726/.
  7. Russell IJ, Holman AJ, Swick TJ, et al. Sodium oxybate reduces pain, fatigue, and sleep disturbance and improves functionality in fibromyalgia: results from a 14-week, randomized, double-blind, placebo-controlled study. Pain. 2011; 152(5): 1007‐1017. doi:10.1016/j.pain.2010.12.022. https://pubmed.ncbi.nlm.nih.gov/21397402/.
  8. Spaeth M, Bennett RM, Benson BA, Wang YG, Lai C, Choy EH. Sodium oxybate therapy provides multidimensional improvement in fibromyalgia: results of an international phase 3 trial. Annals of the Rheumatic Diseases. 2012; 71(6): 935‐942. doi:10.1136/annrheumdis-2011-200418. https://pubmed.ncbi.nlm.nih.gov/22294641/.
  9. XYREM® (sodium oxybate) oral solution, CIII: HIGHLIGHTS OF PRESCRIBING INFORMATIO. Jazz Pharmaceuticals, Inc. 2002. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021196s030lbl.pdf.
Olivier George

About Author

Olivier George, Ph.D.

Olivier George is a medical writer and head manager of the rehab center in California. He spends a lot of time in collecting and analyzing the traditional approaches for substance abuse treatment and assessing their efficiency.

Comments

Leave a comment