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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Buprenorphine Hydrochloride And Naloxone Hydrochloride Dihydrate
Brand Name
Buprenorphine Hydrochloride And Naloxone Hydrochloride Dihydrate
Generic Name
Buprenorphine Hydrochloride And Naloxone Hydrochloride Dihydrate
Active Ingredient
BuprenorphineCategory
Partial Opioid Agonist [EPC]
Variants
18
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Buprenorphine Hydrochloride And Naloxone Hydrochloride Dihydrate, you must consult a qualified healthcare professional.
| 2 mg/1 | TABLET | SUBLINGUAL | 16729-549 |
| 8 mg/1 | TABLET | SUBLINGUAL | 58118-8020 |
| 8 mg/1 | TABLET | SUBLINGUAL | 67296-2191 |
| 2 mg/1 | TABLET | SUBLINGUAL | 70518-3862 |
| 2 mg/1 | TABLET | SUBLINGUAL | 71335-1720 |
| 2 mg/1 | TABLET | SUBLINGUAL | 58118-8005 |
| 8 mg/1 | TABLET | SUBLINGUAL | 71335-1858 |
| 2 mg/1 | TABLET | SUBLINGUAL | 71335-1653 |
| 8 mg/1 | TABLET | SUBLINGUAL | 71335-1725 |
+ 6 more variants
Detailed information about Buprenorphine Hydrochloride And Naloxone Hydrochloride Dihydrate
Buprenorphine is a potent partial opioid agonist and kappa-opioid antagonist used for the treatment of opioid use disorder (OUD) and chronic pain management. It belongs to the class of medications known as partial opioid agonists.
Dosage of buprenorphine is highly individualized and depends entirely on the condition being treated and the specific formulation used.
Buprenorphine is generally not approved for use in pediatric patients for the treatment of opioid use disorder. For pain management, its safety and efficacy in children under the age of 18 have not been established for most formulations. Some specific injectable forms may be used in children over 2 years old for acute pain in a hospital setting, but this is rare and requires expert pediatric anesthesia oversight.
No specific dose adjustment is typically required for patients with renal impairment, as only a small fraction of the drug is cleared by the kidneys. However, metabolites can accumulate, so cautious monitoring is advised.
Since buprenorphine is extensively metabolized by the liver, patients with moderate to severe hepatic impairment (Child-Pugh Class B and C) require careful monitoring. In some cases, the use of buprenorphine/naloxone combination products is avoided in severe hepatic impairment because naloxone levels can increase significantly, potentially causing precipitated withdrawal.
Older adults should be started at the lower end of the dosing range. They are more susceptible to the sedative effects, respiratory depression, and confusion associated with opioids. Close monitoring for fall risk and cognitive changes is essential.
Proper administration is vital for the medication to work correctly:
If you miss a dose, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and resume your regular schedule. Do not double the dose to catch up. If you miss multiple doses, contact your healthcare provider, as you may need to restart the induction process to avoid precipitated withdrawal.
Signs of buprenorphine overdose include extreme sleepiness, pinpoint pupils, slowed or shallow breathing (hypoventilation), and profound muscle weakness. While buprenorphine has a ceiling effect on respiratory depression, an overdose can still be fatal, especially when combined with alcohol, benzodiazepines, or other CNS depressants. If an overdose is suspected, call 911 or emergency services immediately. Naloxone (Narcan) can be used to reverse the effects, though higher doses or continuous infusions may be required because of buprenorphine's high receptor affinity.
> Important: Follow your healthcare provider's dosing instructions precisely. Do not adjust your dose or stop taking the medication without medical guidance, as this can lead to relapse or severe withdrawal symptoms.
Most patients taking buprenorphine will experience some mild to moderate side effects, particularly during the first few weeks of treatment as the body adjusts to the medication. Common side effects include:
Buprenorphine is a high-alert medication that requires strict adherence to safety protocols. It should only be used under the direct supervision of a healthcare provider experienced in pain management or the treatment of opioid use disorder. Patients must be honest with their doctors about all other substances they are using, including alcohol and recreational drugs, as these can create lethal combinations.
As detailed in the side effects section, buprenorphine carries critical warnings regarding Addiction, Abuse, and Misuse; Life-threatening Respiratory Depression; Accidental Ingestion; Neonatal Opioid Withdrawal Syndrome; and Interactions with Benzodiazepines. These warnings emphasize that while buprenorphine is a life-saving medication for many, it possesses the same fundamental risks as other opioid medications if not managed with extreme care.
There are certain substances that should never be combined with buprenorphine due to the extreme risk of fatal outcomes:
There are specific scenarios where the use of buprenorphine is strictly prohibited because the risks clearly outweigh any potential benefits:
Buprenorphine is often considered a preferred treatment for opioid use disorder during pregnancy, as the risks of untreated addiction (including overdose and lack of prenatal care) are significantly higher than the risks of the medication.
Buprenorphine’s unique profile stems from its high affinity and low intrinsic activity at the mu-opioid receptor. It binds to the receptor so strongly that it 'outcompetes' other opioids. However, once bound, it only partially activates the receptor (partial agonism). This creates a ceiling on effects like euphoria and respiratory depression. Simultaneously, it acts as a potent antagonist at the kappa-opioid receptor, which may contribute to its efficacy in treating mood disorders and reducing the 'anti-reward' signals associated with addiction. It also has weak antagonist activity at the delta-opioid receptor.
The dose-response curve for buprenorphine is bell-shaped for some effects but plateaued for others. Its analgesic effect increases with dose up to a point, while its effect on breathing plateaus, making it safer than full agonists. The duration of its effect is much longer than its plasma half-life would suggest because it dissociates (detaches) from the mu-receptor very slowly.
Common questions about Buprenorphine Hydrochloride And Naloxone Hydrochloride Dihydrate
Buprenorphine is primarily used for two distinct medical purposes: the treatment of opioid use disorder (OUD) and the management of chronic, severe pain. In the context of OUD, it acts as a maintenance medication that reduces cravings and withdrawal symptoms, allowing individuals to stabilize their lives and engage in counseling. For pain management, it is available in patches or films that provide long-acting relief for patients who require continuous opioid therapy. It is often preferred over other opioids because of its lower risk of overdose and misuse. Always use this medication only for the specific condition for which it was prescribed by your doctor.
The most common side effects experienced by patients taking buprenorphine include headaches, nausea, constipation, and increased sweating. Many patients also report trouble sleeping (insomnia) or feeling dizzy, especially when they first start the medication or increase their dose. Because it is an opioid, it can cause some drowsiness, though this is usually less intense than with full agonists like oxycodone. Most of these side effects are manageable and may diminish as your body becomes accustomed to the drug. However, if you experience severe abdominal pain or yellowing of the eyes, you should contact your healthcare provider immediately.
No, you should strictly avoid drinking alcohol while taking buprenorphine. Alcohol is a central nervous system depressant, and when combined with buprenorphine, it can dangerously slow down your heart rate and breathing. This combination significantly increases the risk of a fatal overdose, even if you are taking your medication exactly as prescribed. Many drug-related deaths involving buprenorphine also involve alcohol or other sedatives. If you have a history of alcohol use, it is vital to discuss this with your doctor before starting treatment.
Buprenorphine is considered one of the standard treatments for pregnant women with opioid use disorder. While it can cause Neonatal Opioid Withdrawal Syndrome (NOWS) in the newborn, this condition is manageable and often less severe than the withdrawal seen with methadone or illicit opioids. Untreated opioid addiction during pregnancy poses much greater risks to both the mother and the baby, including premature birth and fetal death. Therefore, the benefits of staying on buprenorphine usually outweigh the risks. If you are pregnant or planning to become pregnant, your doctor will help you manage your treatment to ensure the best outcome for your baby.
The time it takes for buprenorphine to work depends on the form you are using and the condition being treated. For withdrawal symptoms, sublingual films or tablets typically begin to provide relief within 30 to 60 minutes, with peak effects occurring within 2 to 3 hours. For chronic pain, the transdermal patch may take 24 to 72 hours to reach a steady level of pain relief in your system. Because buprenorphine stays in the body for a long time, it provides a stable effect throughout the day once you reach a maintenance dose. Your doctor will guide you through the initial 'induction' phase to find the timing that works best for you.
You should never stop taking buprenorphine suddenly, as this can trigger unpleasant withdrawal symptoms. While buprenorphine withdrawal is often described as less intense than heroin or methadone withdrawal, it can still cause significant discomfort, including muscle aches, diarrhea, anxiety, and sweating. Furthermore, stopping the medication abruptly increases the risk of relapse for those being treated for addiction. If you wish to discontinue the medication, your healthcare provider will create a gradual tapering schedule. This process involves slowly reducing your dose over weeks or months to allow your brain and body to adjust safely.
If you miss a dose of buprenorphine, you should take it as soon as you remember. However, if it is almost time for your next scheduled dose, you should skip the missed dose and simply take your next one at the regular time. Do not take two doses at once to make up for a missed one, as this can increase the risk of over-sedation. If you miss several days of your medication, do not restart your full dose without calling your doctor first. You may need to restart with a smaller dose to avoid getting sick or experiencing precipitated withdrawal.
Weight gain is not a commonly listed side effect of buprenorphine in clinical trials, but some patients do report changes in weight during long-term treatment. This can be due to several factors, such as improved appetite and health as a person stabilizes their life during recovery from addiction. Opioids can also slow down the digestive system and occasionally cause fluid retention, which might feel like weight gain. Additionally, changes in hormone levels (like decreased testosterone) caused by long-term opioid use can sometimes affect metabolism. If you are concerned about weight changes, discuss your diet and activity level with your healthcare provider.
Buprenorphine can interact with many other medications, some of which can be very dangerous. You must tell your doctor about everything you take, especially benzodiazepines, sleep aids, muscle relaxants, or other opioids. Certain antidepressants and antifungal medications can also change how your body processes buprenorphine, leading to either too much or too little of the drug in your blood. Even herbal supplements like St. John's Wort can interfere with your treatment. Your pharmacist and doctor will check for these interactions to ensure that your medication regimen is safe and effective for you.
Yes, buprenorphine is available in several generic forms, which are typically more affordable than brand-name versions like Suboxone or Butrans. Generic versions are available for sublingual tablets, sublingual films, and transdermal patches. The FDA requires generic medications to have the same active ingredient, strength, and dosage form as the brand-name drug, so they are considered equally effective. However, the appearance or inactive ingredients might differ slightly. If you have concerns about the cost of your medication, ask your doctor or pharmacist if a generic version is appropriate for your specific treatment plan.
Other drugs with the same active ingredient (Buprenorphine)
> Warning: Stop taking Buprenorphine and call your doctor immediately if you experience any of these serious symptoms:
With prolonged use, patients may experience persistent constipation, hormonal imbalances (low testosterone or estrogen), and potential changes in sleep architecture. There is also a risk of developing a physical dependence on buprenorphine itself; while this is different from the 'addiction' seen with illicit drugs, it means the medication must be tapered slowly to avoid withdrawal. Dental health must be monitored closely for the duration of treatment.
Buprenorphine products carry several significant FDA Black Box Warnings, which are the highest level of warning for prescription drugs:
Report any unusual symptoms to your healthcare provider immediately. Regular follow-ups are necessary to monitor for these potential complications.
Patients on long-term buprenorphine therapy require regular clinical monitoring:
Buprenorphine may impair the mental or physical abilities required for performing potentially dangerous tasks, such as driving a car or operating machinery. This is especially true during the first few days of treatment or after a dose increase. Do not drive until you are certain the medication does not make you drowsy or confused.
Do not drink alcohol while taking buprenorphine. Alcohol significantly increases the risk of severe respiratory depression, coma, and death. Even small amounts of alcohol can interact dangerously with the sedative properties of buprenorphine.
Abruptly stopping buprenorphine can lead to withdrawal symptoms, although these are typically less severe than withdrawal from full agonists like heroin or methadone. Symptoms include body aches, diarrhea, goosebumps, loss of appetite, runny nose, sneezing, tremors, and shivering. If you wish to stop taking buprenorphine, your doctor will provide a slow tapering schedule to minimize discomfort and the risk of relapse.
> Important: Discuss all your medical conditions, including any history of liver disease, heart rhythm problems, or lung disease, with your healthcare provider before starting Buprenorphine.
Buprenorphine can cause false-positive results on some standard urine drug screens for opioids. Specific 'buprenorphine-only' tests are required to accurately detect the drug. It may also cause asymptomatic elevations in liver enzymes (ALT and AST) and amylase/lipase levels in some patients.
For each major interaction, the management strategy usually involves dose adjustment, increased monitoring, or choosing an alternative medication.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including those you only take occasionally.
These are conditions where the medication may be used, but only with extreme caution and frequent monitoring:
Patients who are allergic to other thebaine-derived opioids (such as oxycodone or oxymorphone) should be closely monitored when starting buprenorphine, as there is a theoretical risk of cross-reactivity, although it is clinically rare.
> Important: Your healthcare provider will evaluate your complete medical history, including your respiratory health and liver function, before prescribing Buprenorphine.
Buprenorphine and its metabolite, norbuprenorphine, are excreted in human milk in small amounts. In women stabilized on buprenorphine maintenance, the amount of drug the infant receives via breast milk is very low and generally considered safe. Breastfeeding is encouraged for women on stable MOUD, as it can actually help reduce the severity of NOWS in the infant. Monitor the infant for increased sleepiness or breathing difficulties.
Safety and effectiveness in pediatric patients have not been established. The primary concern in this population is accidental exposure; a single tablet can be fatal to a small child. If used off-label for pain in older adolescents, it must be done with extreme caution and at much lower doses than adults.
Older patients (65+) are at increased risk for side effects. They often have reduced renal or hepatic function and may be taking multiple other medications (polypharmacy). There is a higher risk of respiratory depression and falls. Clinicians typically 'start low and go slow' with dosing in this population.
While the kidneys are not the primary route of elimination, renal failure can lead to the accumulation of metabolites. No specific dose adjustments are provided in the labeling, but clinical monitoring for increased sedation is recommended. Buprenorphine is not significantly removed by hemodialysis.
As the liver is the primary site of metabolism, hepatic impairment significantly affects buprenorphine levels.
> Important: Special populations require individualized medical assessment and more frequent clinical follow-ups.
|---|---|
| Bioavailability | 30% - 50% (Sublingual), 15% (Buccal) |
| Protein Binding | 96% (Alpha/Beta globulins) |
| Half-life | 24 - 42 hours (Sublingual), 26 hours (Transdermal) |
| Tmax | 40 - 120 minutes (Sublingual) |
| Metabolism | Hepatic (CYP3A4 to Norbuprenorphine) |
| Excretion | Fecal 70%, Renal 30% |
Buprenorphine is the primary representative of the Partial Opioid Agonist class. In the context of addiction, it is grouped with methadone and naltrexone as MOUD. In the context of pain, it is considered an 'atypical opioid' due to its complex pharmacology compared to traditional Schedule II opioids.