Zubsolv: 7 things you should know

Medically reviewed by Carmen Pope, BPharm. Last updated on May 23, 2024.

1. How it works

• Zubsolv is a brand (trade) name for a combination buprenorphine/naloxone sublingual tablet that may be used for the treatment of opioid dependence.
• Buprenorphine is an opioid (narcotic) that has a unique and complex mechanism of action, which includes incomplete binding to mu-opioid receptors and complete binding to kappa opioid receptors. Opioid receptors have three main effects: reducing breathing (respiratory depression), producing euphoria (feelings of intense happiness or excitement), and decreasing pain. The way buprenorphine binds means it can satisfy opioid cravings without producing strong feelings of euphoria or causing significant respiratory depression. In addition, while it is bound to opioid receptors, other opioids (such as heroin and oxycodone) cannot bind. It also stays on the receptors for longer - about three days; which makes it a good choice for use in opioid addiction treatment programs.
• Naloxone is present in this combination tablet to discourage misuse. Naloxone is a very strong blocker of mu-opioid receptors and will precipitate people into opioid withdrawal if drug misusers attempt to convert the tablet into an injectable form. Naloxone has virtually no other effect when taken sublingually.
• Zubsolv belongs to the class of medicines known as combination opioid/opioid antagonists. It may also be called a narcotic analgesic combination.

2. Upsides

• May be used to treat opioid dependence (opioid misuse disorder).
• Zubsolv is used as part of a complete treatment program that includes counseling and psychosocial support.
• Given as a single daily dose. Treatment should be initiated under clinical supervision and progress to unsupervised administration as the patient's clinical stability permits. The amount of take-home medication should take into account the patient's stability as well as their home security and other factors.
• Dosage can be progressively adjusted until the correct dosage is found that holds the patient in treatment and suppresses opioid withdrawal symptoms.
• Zubsolv is available in six dosage strengths of buprenorphine/naloxone: Zubsolv 0.7mg/0.18mg; Zubsolv 1.4mg/0.36mg; Zubsolv 2.9mg/0.71mg; Zubsolv 5.7mg/1.4mg; Zubsolv 8.6mg/2.1mg; and Zubsolv 11.4mg/2.9mg.
• May be used as initial therapy in patients dependent on heroin and other short-acting opioids instead of buprenorphine monotherapy. Zubsolv should be started when signs of opioid withdrawal appear but not less than six hours after the last opioid use to avoid precipitating opioid withdrawal syndrome. Patients dependent on methadone or long-acting opioids may be more susceptible to precipitated and prolonged withdrawal during induction of Zubsolv and instead should be initiated on buprenorphine monotherapy. Following buprenorphine monotherapy induction, the patient can be transitioned to once-daily Zubsolv. See the product information for induction and maintenance dosage recommendations.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• A headache, gastrointestinal disorders (eg, constipation, nausea, or vomiting), pain, withdrawal syndrome, infection, insomnia, sweating, and rhinitis are the most common side effects reported. Liver enzyme elevation (eg, alanine aminotransferase, aspartate aminotransferase, gamma-glutamyl transferase), and blood creatine phosphokinase elevations have also been reported.
• Has the potential to cause serious, life-threatening breathing problems. This is more likely in people who misuse Zubsolv, or when it is used in combination with other medications that also affect breathing, such as benzodiazepines. Children, the elderly or debilitated, and those with pre-existing breathing problems are also at higher risk.
• May be habit-forming, even at the dosage prescribed by your doctor. Zubsolv is a Schedule III controlled substance and it must be prescribed and dispensed with appropriate precautions to minimize the risk of misuse, abuse, or diversion.
• Allergic reactions (including breathing difficulties, rash, and anaphylactic shock) and liver damage (hepatitis) have been reported. Do not use Zubsolv in patients with a history of hypersensitivity to buprenorphine.
• May cause sleepiness or dizziness and affect a person's ability to drive or operate machinery. Alcohol should be avoided
• May cause a severe lowering of blood pressure, or a sudden drop in blood pressure when going from sitting to standing.
• Risk of heart rhythm disorders (such as QT prolongation), particularly at higher dosages.
• Dosage adjustments may be necessary when switching between Zubsolv and other buprenorphine/naloxone formulations. For example, from Zubsolve to Suboxone, differences in bioavailability require different strengths to be given. One Zubsolve 5.7mg/1.4mg sublingual tablet is equivalent to one Suboxone 8mg/2mg sublingual tablet. Monitor for signs of over-medication as well as withdrawal or under-dosing when switching brands.
• Misuse of Zubsolv can cause addiction, overdose, or death. Refer patients who continue to misuse, abuse, or divert opioid products to more intensive, structured treatment.
• Zubsolv should be tapered off if the decision is made to discontinue it to avoid the occurrence of withdrawal signs and symptoms.
• May not be suitable for some people such as those with liver disease, cardiac arrhythmias, the elderly or frail, with a history of drug or alcohol abuse, with psychiatric disorders, previous head injury or raised intracranial pressure, a history of seizure disorders, with certain gastrointestinal conditions, respiratory disease, liver disease, physically dependent on full agonists, or certain other concomitant conditions. Use during pregnancy may cause withdrawal symptoms in the newborn baby.
• May interact with several other drugs including other opioids, benzodiazepines, and other central nervous system depressants resulting in profound sedation, respiratory depression, and sometimes death. May also interact with drugs metabolized through several CYP hepatic enzyme systems (such as CYP3A4 or CYP2D6) or drugs that also release serotonin (such as antidepressants, antipsychotics, and tramadol). There is a risk of heart rhythm disorders (such as QT prolongation) associated with Zubsolv, particularly when used with other drugs that prolong the QT interval.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

Zubsolv is a combination buprenorphine/naloxone sublingual tablet that helps to suppress opioid withdrawal symptoms and is used for the maintenance treatment of opioid drug dependence as part of a complete treatment program that includes counseling and psychosocial support. Dosage adjustments are required when switching from Zubsolv to other combination buprenorphine/naloxone formulations.

5. Tips

• Never share Zubsolv with another person, particularly those with a history of drug abuse or addiction.
• Zubsolv must be administered whole. Do not cut, chew, or swallow Zubsolv. Place Zubsolv sublingual tablets under the tongue and allow them to dissolve; swallowing the tablets reduces how much buprenorphine is absorbed. The average dissolution time is 5 minutes. If you are required to take more than one sublingual tablet at a time, place all tablets in different places under the tongue at the same time.
• Do not eat or drink anything until Zubsolv has completely dissolved.
• Zubsolv is not directly interchangeable with other brands of buprenorphine/naloxone, such as Suboxone; dosage adjustments are necessary. Talk with your doctor.
• Always keep your appointments with your healthcare provider. Your frequency of visits will depend on your clinical stability but should be at least weekly during the first month of treatment because this allows your clinician to determine the effectiveness of your treatment plan and overall progress.
• Continued treatment with Zubsolv usually depends on compliance with all elements of the treatment plan and abstinence from illicit drug use. When used to treat drug addiction, take advantage of any social support and counseling services offered to you as withdrawal from opioids is a long and often difficult process and a successful outcome is dependent upon a multi-targeted approach.
• Seek immediate medical help if you develop blurred vision, are excessively sleepy or uncoordinated, have slurred speech, have slowed reflexes or breathing, or have significant problems thinking.
• Rise carefully from a sitting to a standing position to minimize the blood pressure-lowering effects of Zubsolv which may result in dizziness increasing your risk of falls.
• Zubsolv may cause constipation. Talk to your doctor about taking laxatives as a preventive against constipation if you are prescribed Zubsolv.
• Zubsolv has been associated with androgen deficiency which may cause symptoms such as low libido, impotence, erectile dysfunction, amenorrhea, or infertility. Talk to your doctor if this happens to you.
• Zubsolv can cause sedation and affect your ability to drive or operate machinery.
• Do not drink alcohol while you are taking Zubsolv.
• Always talk to your doctor or pharmacist before buying anything over-the-counter to check if it is compatible with Zubsolv. If Zubsolv is administered with other drugs that also release serotonin, such as tramadol, lithium, or antidepressants, a condition called serotonin syndrome may develop. Symptoms include agitation or restlessness, sweating, diarrhea, headache, confusion, rapid heart rate, high blood pressure, dilated pupils, loss of muscle coordination, twitching muscles, or muscle rigidity. See your doctor immediately.
• Keep out of reach of children and pets because even one dose can be fatal.
• Tell other health providers including dentists that you are being treated with Zubsolv.
• If you are a woman of childbearing age you should use adequate contraception to ensure you do not become pregnant while being administered Zubsolv. If you inadvertently become pregnant, tell your doctor straight away as there is a risk your baby may be born with neonatal withdrawal syndrome which will need to be treated. Do not breastfeed while being administered Zubsolv.

6. Response and effectiveness

• The tolerability of Zubsolv, when compared with buprenorphine therapy, was evaluated in two blinded randomized trials that showed a 93% retention by day 3 in the Zubsolv group (n=383) compared to a 92% retention in the generic buprenorphine group (n=375) in one trial and an 85% (n=155) retention in the Zubsolv group compared to a 95% retention in the generic buprenorphine group (n=155) in the other trial. The lower rate of retention in the second trial may have been due to the infrequent use of divided dosing in the Zubsolv group.

7. Interactions

Medicines that interact with Zubsolv may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with Zubsolv. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Common medications that may interact with Zubsolv include:

• 5-hydroxytryptophan
• albuterol
• antibiotics, such as azithromycin, clarithromycin, erythromycin, and norfloxacin
• antidepressants, such as tricyclic antidepressants (eg, amitriptyline), monoamine oxidase inhibitors (eg, isocarboxazid, phenelzine, and tranylcypromine), or SSRIs (eg, fluoxetine, sertraline)
• antifungal agents, such as itraconazole and ketoconazole
• anticonvulsants, such as brivaracetam, carbamazepine, divalproex, lamotrigine, phenytoin, phenobarbital, or primidone
• antipsychotics (such as butyrophenones, phenothiazines, or thioxanthenes) and atypical antipsychotics (eg, aripiprazole, olanzapine, quetiapine, ziprasidone)
• any medication that may cause drowsiness, such as benzodiazepines (eg, alprazolam, diazepam, lorazepam), sleeping pills (such as zolpidem or ziprasidone), or first-generation antihistamines (such as doxylamine or promethazine)
• bisacodyl
• bupropion
• buspirone
• busulfan
• cannabis
• cyclosporine
• dapsone
• dasatinib
• droperidol
• echinacea
• flucloxacillin
• heart medications such as amlodipine, atenolol, or candesartan
• HIV medications, such as delavirdine or ritonavir
• metoclopramide
• muscle relaxants, such as baclofen or cyclobenzaprine
• opioids such as codeine, fentanyl, or morphine
• pregabalin
• rifampin
• sodium oxybate
• valerian
• other medications that affect serotonin, such as amphetamines, lithium, tramadol, or triptans (eg, almotriptan, eletriptan, or sumatriptan).

Avoid grapefruit products, drinking alcohol, or taking illegal or recreational drugs while taking Zubsolv.

Note that this list is not all-inclusive and includes only common medications that may interact with Zubsolv. You should refer to the prescribing information for Zubsolv for a complete list of interactions.

References

• Zubsolv (buprenorphine hydrochloride and naloxone hydrochloride). Updated 12/2023. Orexo US, Inc. https://www.drugs.com/pro/zubsolv.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Zubsolv only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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