Buprenorphine and naloxone sublingual tablets

Description

Addiction to drugs and opioids is one of the public health crises in the contemporary world that affects not only the body but also the psyche and the foundation of families. In recent years, numerous studies have been conducted to find effective methods for treating this addiction, and new drugs have entered the market, one of which is the sublingual buprenorphine-naloxone combination. Kish Medipharm Pharmaceutical Company, relying on modern technology and international standards, has succeeded in producing this drug in two formulation models:

• 2 mg buprenorphine hydrochloride + 0.5 Naloxone hydrochloride mg
• 8 mg buprenorphine hydrochloride + 2 Naloxone hydrochloride mg

This product is produced with the official license of the Ministry of Health, Treatment and Medical Education and under strict quality supervision, and forms part of maintenance treatments for patients with drug use disorder.

Medicinal ingredients and function of components

Buprenorphine hydrochloride: partial receptor agonist μ

Buprenorphine, a partial agonist at the μ-opioid receptor, acts to block the pleasure of opioids while reducing withdrawal symptoms. Unlike full agonists such as heroin or methadone, the drug has a ceiling effect and does not increase in intensity with increasing dose. This feature significantly reduces the risk of overdose.

Naloxone hydrochloride: opioid receptor antagonist

Naloxone binds to the same μ receptors, blocking the effects of buprenorphine when administered by injection. When administered sublingually, naloxone has little absorption and no significant effect, but if attempted to abuse via injection, naloxone is activated and causes severe withdrawal symptoms, preventing the person from continuing to abuse.

Main uses of buprenorphine and naloxone

It is important to know the main uses of buprenorphine-naloxone because this drug combination is designed only for the treatment of opioid dependence and its misuse can be dangerous. Knowing the exact use will prevent abuse, unwanted interactions and side effects and make treatment more effective under the supervision of a physician.

Drug Dependence Treatment: Buprenorphine-naloxone sublingual tablet is used to treat addiction to substances such as heroin, opium, morphine, codeine, fentanyl, and oxycodone. Regular use of the drug is an important part of the treatment plan for dependent patients by reducing cravings for drugs, improving psychophysical stability, and restoring daily functioning.

Use in MMT programs: In Medication-Assisted Treatment (MMT) programs, this pill is considered a safer and more controllable alternative to methadone and is often prescribed in addiction treatment centers under the supervision of a psychiatrist and a specialist physician.

How to use and how to use sublingual buprenorphine and naloxone tablets

The method of administration of sublingual buprenorphine and naloxone tablets plays a vital role in the effectiveness of the treatment. The drug must be completely placed under the tongue to be properly absorbed; swallowing it will reduce absorption and effectiveness. Proper administration not only helps control withdrawal symptoms, but also prevents complications and treatment failure. Due to the presence of naloxone, there is a possibility of sudden and severe withdrawal symptoms if injected or used incorrectly. Therefore, adherence to the correct method of administration is a fundamental condition for the success of the treatment and maintaining the patient's safety in the addiction cessation process.

Sublingual form: fast absorption, long-lasting effect

The buprenorphine and naloxone sublingual tablet is designed to enter the bloodstream directly through the oral mucosa. This absorption route, unlike swallowing the drug and passing through the digestive tract, avoids the "first-pass effect" and allows the drug to enter the bloodstream more quickly and begin its therapeutic effect.

When the tablet is completely placed under the tongue and dissolved, buprenorphine binds to μ-opioid receptors in the brain, inhibiting withdrawal symptoms and reducing cravings. At the same time, naloxone is not absorbed by this route (as it is poorly absorbed sublingually) and is only activated when the drug is used improperly, such as by injection.

If the tablet is swallowed before it is completely dissolved, the drug must pass through the digestive tract, be metabolized in the liver, and ultimately a large portion of its active compound is degraded; as a result, the therapeutic effect is reduced and may even become ineffective.

For this reason, proper patient education on the use of the sublingual form is crucial. This method not only maximizes the effectiveness of the treatment, but also prevents side effects and drug failure. It is also clinically safer and less abuse-prone than injectable forms.

Dosage and treatment adjustment

At the beginning of treatment, a lower dose (2 mg/0.5 mg) is used to assess the patient's response, and the dose is gradually increased depending on the severity of the dependence and the clinical situation. The maximum daily dose is often adjusted to 24 mg of buprenorphine.

Benefits of sublingual buprenorphine and naloxone: A deeper look

Below, we will provide a comprehensive and expert review of the key benefits of sublingual buprenorphine and naloxone. These benefits play an effective role in improving the treatment process of addiction, reducing cravings, controlling withdrawal symptoms, and preventing abuse, paving the way for patients to recover.

Reducing cravings for drugs: One of the main challenges in treating drug addiction is the sudden and intense craving for the drug; a craving that is not only physical, but also psychological and behavioral. By partially saturating the μ (mu) receptors in the brain, buprenorphine activates the same receptors that are stimulated by drugs such as heroin, morphine, or fentanyl without producing an intense "high." This partial saturation signals to the brain that the "need" has been satisfied, while preventing pathological pleasure seeking.

In fact, the brain feels that it has received enough, so the obsessive desire to consume decreases. This effect makes it easier for the patient to overcome environmental or stressful stimuli and maintain the decision to abstain during the critical phase of early treatment.

Controlling physical and psychological withdrawal symptoms: Drug withdrawal without medical treatment can lead to severe and sometimes unbearable symptoms, including muscle pain, tremors, nausea, insomnia, anxiety, depression, and extreme irritability. Buprenorphine plays the role of a “gradual reliever.” By controlling the stimulation of opioid receptors, it balances neurotransmitters and prevents the body from experiencing the sudden shock of withdrawal.

On the other hand, controlling psychological symptoms such as restlessness or anxiety not only provides physical relief but also strengthens the person's psychological motivation to stay on the path to quitting. This psychological stability is an important factor in preventing relapse and relapse.

Reducing the likelihood of abuse: Buprenorphine alone, when injected or taken illicitly, can produce a certain euphoric feeling. But when combined with naloxone, the situation becomes completely different. Naloxone is an opioid receptor antagonist that has little activity when taken orally but is rapidly activated when injected, neutralizing the effects of buprenorphine or any other opioid.

As a result, if someone were to inject the sublingual tablet, the naloxone in it would cause sudden withdrawal symptoms—an unpleasant and very difficult state. This feature makes the drug safe from the risk of “abuse” and “compulsory use” and keeps the patient on the path to treatment. Such clever design in the formulation distinguishes it from methadone and many other treatments.

Possible side effects of buprenorphine and naloxone sublingual tablets: a complete and detailed description

Buprenorphine and naloxone tablets, like any effective medication, may be associated with some side effects. It is important for patients and healthcare providers to be aware of these side effects, as early recognition of adverse reactions can prevent serious problems. These side effects are usually divided into two categories: common and rare:

Common side effects

These side effects usually appear in the first few days of use or when adjusting the dose, and in many cases, they decrease with time or dose adjustment:

• Nausea and vomiting: This is a normal reaction of the body to the introduction of a new substance into the digestive system. It is recommended to take the tablet on a half-full stomach to reduce the severity of this symptom.
• Constipation: One of the most common side effects of opioid medications, which can be controlled with fluid intake, a high-fiber diet, and physical activity.
• Excessive sweating: May occur due to the drug's effect on the autonomic nervous system and may subside over time.
• Headache: caused by chemical changes in the brain or mild disturbances in sleep and blood pressure. The use of mild painkillers is allowed with a doctor's prescription.
• Mild anxiety or restlessness: May occur early in treatment or when the dose is reduced. This is usually temporary and subsides as treatment stabilizes.
• Itchy skin: In some patients, a mild skin reaction such as redness or itching is observed on the face or body, which often does not require specific treatment.

Rare and serious complications

These are much less common, but due to the severity of the risk, awareness and immediate action are essential if they occur:

• Respiratory depression: Especially when taken with alcohol, benzodiazepines, or other sedatives. This condition can be life-threatening and requires immediate medical intervention.
• Severe allergic reactions: Symptoms such as swelling of the lips, tongue, throat, hives, or shortness of breath may indicate an anaphylactic reaction, which requires emergency treatment.
• Hallucinations or psychotic states: Although rare, they may occur in some patients with a history of mental illness or hypersensitivity to opioids. In these cases, the drug should be stopped immediately and the psychiatrist should be informed.

Important drug interactions of buprenorphine and naloxone sublingual tablets: a comprehensive explanation

Drug interactions are one of the most important points that should be paid special attention to when taking any medication. Buprenorphine and naloxone sublingual tablets are no exception to this rule, and their simultaneous use with some medications can lead to serious and even dangerous side effects. In this section, we will examine the most important drug interactions of this combination.

Central nervous system depressants (CNS)

One of the most important and dangerous groups of drugs that interact with buprenorphine and naloxone are sedatives and hypnotics. This group includes benzodiazepines such as diazepam and lorazepam, alcohol, and other anti-anxiety or sedative medications. Taking these drugs with buprenorphine-naloxone can cause severe respiratory depression.

Respiratory depression is a severe decrease in the rate and depth of breathing, which can lead to a lack of oxygen in the body and, in severe cases, cause unconsciousness, brain damage, and even death. The risk of this complication increases when the dose of the drugs is high or the patient has respiratory or liver disease.

Therefore, it is recommended that patients discuss any sedatives or alcohol they are taking with their doctor to avoid dangerous interactions. It is especially important to adjust the dosage and timing of medications carefully.

Psychiatric medications

SSRI antidepressants such as fluoxetine and sertraline, as well as antiepileptic drugs, may interact with buprenorphine-naloxone. These interactions may cause two serious side effects:

Serotonin syndrome: This condition is caused by too much serotonin in the brain and has symptoms such as severe anxiety, excessive sweating, increased heart rate, muscle tremors, and in more severe cases, impaired consciousness and seizures. Taking buprenorphine and drugs that increase serotonin levels at the same time can trigger this syndrome.

Seizures: Some antiepileptic or psychiatric medications may lower the seizure threshold. Combining these medications with buprenorphine should be done with great care and under the supervision of a physician to reduce the risk of seizures.

Key points in managing drug interactions:

• Fully inform your doctor about all medications you are taking, even herbal remedies and supplements.
• Close monitoring of clinical symptoms during treatment, especially in the initial days of drug use.
• Adjust the dosage of medications and avoid taking medications with similar effects at the same time.
• If you experience unusual symptoms such as shortness of breath, dizziness, seizures, or severe anxiety, seek medical attention immediately.

Absolute and relative contraindications for sublingual buprenorphine and naloxone tablets

The use of combination drugs such as buprenorphine and naloxone requires special attention to the patient's clinical condition. There are some situations where the use of this drug can be dangerous or requires close care and monitoring. Below we will discuss the absolute and relative contraindications to the use of this drug.

Pregnancy and breastfeeding

Buprenorphine is transferred to the fetus through the placenta and can cause neonatal abstinence syndrome. These symptoms include persistent crying, breathing problems, tremors, restlessness, and feeding disorders in the newborn. Therefore, the administration of this drug during pregnancy should be done with great caution and under the supervision of an obstetrician. In cases where there is a need for addiction treatment, the benefits and risks should be carefully weighed.

During breastfeeding, buprenorphine may pass into breast milk and have effects on the infant. Although the rate of transfer is lower than some other medications, it is recommended that breastfeeding mothers consult a doctor and, if necessary, continue taking the medication carefully and under supervision.

Severe liver failure

Buprenorphine is primarily metabolized in the liver. In people with severe liver failure, the processing and excretion of the drug is significantly reduced. This can lead to accumulation of the drug in the body and increased side effects, including respiratory depression and toxicity.

Therefore, patients with moderate to severe liver problems should use this drug with extreme caution and under the close supervision of their physician. In some cases, it may be necessary to reduce the dose or choose an alternative treatment method.

Chronic respiratory diseases

Patients with chronic respiratory diseases such as severe asthma or COPD (chronic obstructive pulmonary disease) are at high risk of respiratory depression. Buprenorphine can slow breathing by reducing the activity of the central nervous system, and in these patients, whose lungs are already functioning poorly, this may lead to worsening breathing problems, respiratory failure, and even death.

For this reason, the use of this drug in such patients is either prohibited or must be done with great care and special care. Doctors usually carefully evaluate the patient's respiratory status and, if necessary, suggest alternative medications or less risky treatment methods.

Conclusion | Kish Medipharm Buprenorphine and Naloxone Sublingual Tablets

The buprenorphine-naloxone sublingual tablet produced by Kish Medipharm Company, with its balanced and scientific combination of two powerful pharmaceutical molecules, has revolutionized the treatment of opioid addiction. With its dual function of controlling cravings and preventing abuse, this drug has high safety and significant therapeutic efficacy.

Despite its extensive benefits, its use should only be done under the supervision of a specialist physician, with careful monitoring and full adherence to treatment instructions. When used correctly, this medication can be an effective step in the path of treatment, rehabilitation, and return of patients to an addiction-free life.