Buprenorphine Injection

What is Buprenorphine Injection?

• Buprenorphine Injection (Sublocade; Buprenex), is a partial opioid agonist.

Buprenorphine

Buprenorphine molecule from xtal ball

Buprenorphine molecule from xtal spacefill

What are the uses of this medicine?

Buprenorphine Injection (Sublocade;Buprenex), is a prescription medicine used to treat adults with moderate to severe addiction (dependence) to opioid drugs (prescription or illegal) who:

• have received treatment with an oral transmucosal (used under the tongue or inside the cheek) buprenorphine-containing medicine for 7 days and
• are taking a dose that controls withdrawal symptoms for at least seven days.
• It is part of a complete treatment plan that should include counseling.

How does this medicine work?

• Buprenorphine, a synthetic phenanthrene with narcotic analgesic activity.
• Buprenorphine hydrochloride is a partial agonist at the mu-opioid receptor and an antagonist at the kapa-opioid receptor in the central nervous system.
• However, under the conditions of recommended use it behaves as a classic mu-opioid agonist, mimicking the actions of endogenous peptides at CNS opioid receptors.
• The agonist action results in a raised pain threshold and increased tolerance to pain.
• However, it also causes sedation, physical dependence, and respiratory depressant effects and decreases heart rate and blood pressure.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have been shown to be hypersensitive to buprenorphine or any component of the ATRIGEL delivery system.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• pain medicines
• tranquilizers
• sleeping pills
• anxiety medicines
• antihistamines
• antipsychotics such as aripiprazole (Abilify), asenapine (Saphris), cariprazine (Vraylar), chlorpromazine, clozapine (Versacloz), fluphenazine, haloperidol (Haldol), iloperidone (Fanapt), loxapine, lurasidone (Latuda), molindone, olanzapine (Zyprexa), paliperidone (Invega), perphenazine, pimavanserin (Nuplazid), quetiapine (Seroquel), risperidone (Risperdal), thioridazine, thiothixene, trifluoperazine, and ziprasidone (Geodon)
• benzodiazepines such as alprazolam (Xanax), chlordiazepoxide (Librium), clobazam (Onfi), clonazepam (Klonopin), clorazepate (Gen-Xene, Tranxene), diazepam (Diastat, Valium), estazolam, flurazepam, lorazepam (Ativan), oxazepam, quazepam (Doral), temazepam (Restoril), and triazolam (Halcion)
• diuretics ('water pills')
• erythromycin (E.E.S., Eryc, Erythrocin, others)
• certain HIV medications such as atazanavir (Reyataz, in Evotaz), delavirdine (Rescriptor), efavirenz (Sustiva, in Atripla), etravirine (Intelence), indinavir (Crixivan), nelfinavir (Viracept), nevirapine (Viramune), and ritonavir (Norvir, in Kaletra, in Technivie)
• hypnotics
• ipratropium (Atrovent)
• medications for irritable bowel disease, motion sickness, Parkinson's disease, ulcers, or urinary problems
• ketoconazole
• medications for migraine headaches such as almotriptan (Axert), eletriptan (Relpax), frovatriptan (Frova), naratriptan (Amerge), rizatriptan (Maxalt), sumatriptan (Alsuma, Imitrex, in Treximet), and zolmitriptan (Zomig)
• mirtazapine (Remeron)
• muscle relaxants such as cyclobenzaprine (Amrix), dantrolene (Dantrium), and metaxalone (Skelaxin)
• opiate (narcotic) medications for pain control and cough
• rifampin (Rifadin, Rimactane, in Rifater, in Rifamate)
• medications for seizures such as carbamazepine (Epitol, Tegretol, Teril, others), phenobarbital, and phenytoin (Dilantin, Phenytek)
• sedatives
• 5HT3 serotonin blockers such as alosetron (Lotronex), granisetron (Sancuso, Sustol), ondansetron (Zofran, Zuplenz), or palonosetron (Aloxi)
• selective serotonin-reuptake inhibitors such as citalopram (Celexa), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem, in Symbyax), fluvoxamine (Luvox), paroxetine (Brisdelle, Prozac, Pexeva), and sertraline (Zoloft)
• serotonin and norepinephrine reuptake inhibitors such as duloxetine (Cymbalta), desvenlafaxine (Khedezla, Pristiq), milnacipran (Savella), and venlafaxine (Effexor)
• tramadol (Conzip)
• trazodone
• tricyclic antidepressants ('mood elevators') such as amitriptyline, clomipramine (Anafranil), desipramine (Norpramin), doxepin (Silenor), imipramine (Tofranil), nortriptyline (Pamelor), protriptyline (Vivactil), and trimipramine (Surmontil).

• Also tell your doctor or pharmacist if you are taking or receiving the following monoamine oxidase (MAO) inhibitors or if you have stopped taking them within the past two weeks: isocarboxazid (Marplan), linezolid (Zyvox), methylene blue, phenelzine (Nardil), selegiline (Eldepryl, Emsam, Zelapar), or tranylcypromine (Parnate).

Is this medicine FDA approved?

• Buprenorphine was patented in 1965, and approved for medical use in the United States in 1981.

How should this medicine be used?

Recommended dosage:

• The recommended dose of Sublocade is two monthly initial doses of 300 mg followed by 100 mg monthly maintenance doses.
• Increasing the maintenance dose to 300 mg monthly may be considered for patients in which the benefits outweigh the risks.

Buprenex dose: In Adults and Pediatric Patients over 12 years of age:

• The initial starting dose is 1 mL BUPRENEX (0.3 mg buprenorphine) given by deep intramuscular or slow (over at least 2 minutes) intravenous injection at up to 6-hour intervals, as needed.

In Pediatric Patients:

• BUPRENEX has been used in pediatric patients 2-12 years of age at doses between 2-6 micrograms/kg of body weight given every 4-6 hours.

Administration:

• Buprenorphine extended-release (long-acting) injection comes as a solution (liquid) to be injected subcutaneously (just under the skin) by a health care provider into the stomach area.
• It is usually given once monthly with at least 26 days in between doses.
• Each buprenorphine injection slowly releases the drug into your body over a month.
• After you receive a dose of buprenorphine extended-release injection, you may notice a lump at the injection site for several weeks, but it should decrease in size over time. Do not rub or massage the injection site. Be sure that your belt or waistband does not put pressure on the place where the medication was injected.
• Be sure to tell your doctor how you are feeling during your treatment with buprenorphine extended-release injection.
• If buprenorphine extended-release is to be discontinued, your doctor will probably decrease your dose gradually.
• You may experience withdrawal symptoms including restlessness, teary eyes, sweating, chills, widening of the pupils (black circles in the middle of the eyes), irritability, anxiety, backache, weakness, stomach cramps, difficulty falling asleep or staying asleep, nausea, loss of appetite, vomiting, diarrhea, fast breathing, or fast heartbeat. These withdrawal symptoms may occur 1 month or longer after your last buprenorphine extended-release injection dose.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Injection: 100 mg/0.5 mL and 300 mg/1.5 mL
• BUPRENEX (buprenorphine hydrochloride) is supplied in cartons containing five clear glass snap-ampules of 0.3 mg/mL buprenorphine).

This medicine is available in fallowing brand namesː

• Sublocade; Buprenex

What side effects can this medication cause?

The most common side effects of this medicine may include:

• constipation
• headache
• nausea
• injection site itching
• vomiting
• increase in liver enzymes
• tiredness
• injection site pain
• affect fertility in males and females

Less common, but serious side effects may include:

• Trouble breathing
• Sleepiness, dizziness, and problems with coordination
• Physical dependence
• Liver problems
• Allergic reaction
• Opioid withdrawal
• Decrease in blood pressure

What special precautions should I follow?

• Buprenorphine can be abused in a manner similar to other opioids. Monitor patients for conditions indicative of diversion or progression of opioid dependence and addictive behaviors.
• Life-threatening respiratory depression and death have occurred in association with buprenorphine. Warn patients of the potential danger of self-administration of benzodiazepines or other CNS depressants while under treatment with Sublocade.
• Buprenorphine has been associated with life-threatening respiratory depression and death. Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose.
• Inform patients and caregivers that potentially fatal additive effects may occur if Sublocade is used with benzodiazepines or other CNS depressants, including alcohol. Counsel patients that such medications should not be used concomitantly unless supervised by a healthcare provider.
• Inform patients that Sublocade could cause a rare but potentially life-threatening condition resulting from concomitant administration of serotonergic drugs. Warn patients of the symptoms of serotonin syndrome and to seek medical attention right away if symptoms develop. Instruct patients to inform their healthcare providers if they are taking, or plan to take serotonergic medications.
• Inform patients that Sublocade could cause adrenal insufficiency, a potentially life-threatening condition. Adrenal insufficiency may present with non-specific symptoms and signs such as nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure. Advise patients to seek medical attention if they experience a constellation of these symptoms.
• Inform patients that anaphylaxis has been reported with buprenorphine. Advise patients how to recognize such a reaction and when to seek medical attention.
• Caution patients that Sublocade may impair the mental or physical abilities required for the performance of potentially dangerous tasks such as driving or operating hazardous machinery. Instruct patients not to drive or operate hazardous machinery until they are reasonably certain that Sublocade does not adversely affect their ability to engage in such activities.
• Inform patients that Sublocade can cause drug dependence and that withdrawal signs and symptoms may occur when the medication is discontinued.
• Inform patients that, like other opioids, Sublocade may produce orthostatic hypotension in ambulatory individuals.
• Inform patients that they may have detectable levels of buprenorphine for a prolonged period of time after treatment with Sublocade. Considerations of drug-drug interactions, buprenorphine effects, and analgesia may continue to be relevant for several months after the last injection.
• Instruct patients to inform their healthcare providers of any other prescription medications, over the-counter medications, or herbal preparations that are prescribed or currently being used.
• Advise women that if they are pregnant while being treated with Sublocade, the baby may have signs of withdrawal at birth and that withdrawal is treatable.
• Advise women of childbearing potential who become pregnant or are planning to become pregnant to consult their healthcare provider regarding the possible effects of using Sublocade during pregnancy.
• Warn patients that buprenorphine passes into breast milk. Advise the nursing mother taking buprenorphine to monitor the infant for increased drowsiness and breathing difficulties.
• Inform patients that chronic use of opioids may cause reduced fertility. It is not known whether these effects on fertility are reversible.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• pinpoint pupils, sedation, hypotension, respiratory depression, and death

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• In the event of overdose, the respiratory and cardiac status of the patient should be monitored carefully.
• When respiratory or cardiac functions are depressed, primary attention should be given to the re-establishment of adequate respiratory exchange through provision of a patent airway and institution of assisted or controlled ventilation.
• Oxygen, IV fluids, vasopressors, and other supportive measures should be considered as indicated.
• Naloxone may be of value for the management of buprenorphine overdose.
• Higher than normal doses and repeated administration may be necessary.

Can this medicine be used in pregnancy?

• Sublocade should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• The safety and effectiveness of Sublocade have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

• Active ingredient: buprenorphine
• ATRIGEL® delivery system: biodegradable 50:50 poly(DL-lactide-co-glycolide) polymer and a biocompatible solvent, N-methyl-2-pyrrolidone (NMP).

Who manufactures and distributes this medicine?

• Sublocade® is a registered trademark of Indivior UK Limited.
• Manufactured by Curia Global Inc. Albany, NY

What should I know about storage and disposal of this medication?

• Store refrigerated at 2 - 8°C (35.6 - 46.4°F).
• Once outside the refrigerator this product may be stored in its original packaging at room temperature, 15 – 30°C (59 – 86°F), for up to 7 days prior to administration.
• Discard Sublocade if left at room temperature for longer than 7 days.
• Sublocade is a Schedule III drug product.
• Handle with adequate security and accountability.
• After administration, syringes should be properly disposed, per facility procedure for a Schedule III drug product, and per applicable federal, state, and local regulations.

• Dailymed label info on Buprenorphine Injection
• FDA Buprenorphine Injection

Buprenorphine Injection Resources
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The following are antidepressant subclasses and drugs

MAO Inhibitors Isocarboxazid, Phenelzine, Tranylcypromine

SNRIs Duloxetine, Levomilnacipran, Venlafaxine

SSRIs Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Vilazodone, Vortioxetine

Tricyclics Amitriptyline, Amoxapine, Clomipramine, Desipramine, Doxepin, Imipramine, Nortriptyline, Protriptyline, Trimipramine

Miscellaneous Bupropion, Flibanserin, Mirtazapine, Nefazodone, Trazodone