- May 31, 2023
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Brand Name :
Belbuca
Synonyms :
buprenorphine buccal
Class :
Analgesics, Opioid Partial Agonist
Dosage Forms & Strengths
buccal film: Schedule III
75mcg
150mcg
300mcg
450mcg
600mcg
750mcg
900mcg
Indicated for chronic severe pain:
Apply the buccal film to the buccal mucosa every 12 hours
Opioid naïve
Initial dose-75mcg buccal film every day
If tolerated, apply the film every 12 hours for four days.
Patients should be titrated up to a dosage that works best for them regarding analgesia and side effects at 150 mcg every 12hr intervals at most every four days.
Maximum dose-450mcg every 12 hours.
Conversion from other opioids
buprenorphine may cause opioid withdrawal in patients.
Before starting buprenorphine buccal, taper patients ≤30 mg oral morphine sulfate equivalents (MSE) daily to minimize opioid withdrawal.
After the analgesic taper, base the beginning dosage on the patient's previous daily opioid dose, as stated.
<30 mg/day oral morphine equivalent: Begin with 75 mcg daily or every 12 hours.
30 to 89 mg/day equivalent of oral morphine : Begin with 150 mcg every 12 hours.
90-160 mg/day oral morphine equivalent: Begin with 300 mcg every 12 hours.
>160 mg/day oral morphine equivalent: Consider using a different analgesic.
buprenorphine buccal dosages of 600 mcg, 750 mcg, and 900 mcg are only used after titration from lower doses.
Individual titration should be done in increments of 150 mcg every 12 hours, no more than every four days.
methadone Conversion
methadone to buprenorphine buccal conversion requires close monitoring.
Previous dosage exposure affects methadone-opioid agonist ratios.
methadone's lengthy half-life allows plasma accumulation.
Maintenance and titration dose
The minimum titration period is four days based on the pharmacokinetic profile and steady-state plasma levels.
Individual titration should be at most 150 mcg every 12hr.
Do not exceed 900 mcg every 12hr due to QTc interval lengthening.
Consider a substitute analgesic if buprenorphine buccal 900 mg is insufficient to control pain.
Breakthrough pain may need buprenorphine dosage modification or rescue therapy with a suitable immediate-release painkiller.
Dose Adjustments
Renal impairment
No dosage adjustment is necessary
Hepatic impairment
Mild (Child-Pugh A): No dose change is needed.
Moderate (Child-Pugh B): No dosage change is needed, but monitor for toxicity or overdose symptoms.
Severe (Child-Pugh C): From 150 mcg to 75 mcg, half the beginning and titration dosage of individuals with normal liver function.
Safety and efficacy not established
Caution is needed
may increase the adverse effect of Opioid Agonists
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of Buprenorphine
may increase the CNS depressant effect of Buprenorphine
may increase the CNS depressant effect of Buprenorphine
may increase the CNS depressant effect of Buprenorphine
may increase the CNS depressant effect of Buprenorphine
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may decrease the therapeutic effect of Opioid Agonists
may increase the serotonergic effect of Opioid Agonists
may increase the CNS depressant effect of Buprenorphine
may increase the CNS depressant effect of Buprenorphine
may increase the adverse effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may diminish the serum concentration of buprenorphine
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may increase the constipating effect of Opioid Agonists
may increase the serum concentration of CYP3A4 Substrates
may increase the serum concentration of CYP3A4 Substrates
may increase the adverse effect of Buprenorphine
may increase the adverse effect of Buprenorphine
may increase the adverse effect of Buprenorphine
may increase the adverse effect of Buprenorphine
may increase the adverse effect of Buprenorphine
may decrease the therapeutic effect of Opioid Agonists
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may decrease the therapeutic effect of Opioid Agonists
may increase the CNS depressant effect of CNS Depressants
may increase the adverse effect when combined
may increase the CNS depressant effect of CNS Depressants
may increase the analgesic effect of Opioid Agonists
may increase the analgesic effect of Opioid Agonists
may increase the analgesic effect of Opioid Agonists
may increase the analgesic effect of Opioid Agonists
may increase the analgesic effect of Opioid Agonists
may increases the adverse effect of Opioid Agonists
may increases the adverse effect of Opioid Agonists
may increases the adverse effect of Opioid Agonists
may increases the adverse effect of Opioid Agonists
may increases the adverse effect of Opioid Agonists
may enhance the serum concentration of Buprenorphine
may enhance the serum concentration of Buprenorphine
may enhance the serum concentration of Buprenorphine
may enhance the serum concentration of Buprenorphine
may enhance the serum concentration of Buprenorphine
may increase the hyponatremic effect of Opioid Agonists
may increase the CNS depressant effect of CNS Depressants
may increase the CNS depressant effect of CNS Depressants
may decrease the therapeutic effect of Opioid Agonists
may decrease the therapeutic effect of Opioid Agonists
may decrease the therapeutic effect of Opioid Agonists
may decrease the therapeutic effect of Opioid Agonists
may decrease the therapeutic effect of Opioid Agonists
spironolactone and hydrochlorothiazide
may increase the adverse/toxic effect of Opioid Agonists
may increase the adverse/toxic effect of Opioid Agonists
may increase the adverse/toxic effect of Opioid Agonists
may increase the adverse/toxic effect of Opioid Agonists
may increase the adverse/toxic effect of Opioid Agonists
it may diminish the metabolism when combined with diosmin
Actions and Spectrum:
Mechanism of Action:
Spectrum of Activity:
Frequency defined
>10%
Open-label titration phase
Nausea, both opioid-naïve and opioid-tolerant (33%)
Constipation, opioid-naïve (13%)
Nausea, opioid-naive (50%)
Nausea, opioid-tolerant (17%)
Constipation, opioid-naïve and opioid-tolerant (11%)
1-10%
Open-label titration phase
Dizziness (6%)
Constipation, opioid-tolerant (8%)
Somnolence (6%)
Headache (8%)
Drug withdrawal syndrome: (1%)
Vomiting (7%)
Post-marketing reports
Hepatotoxicity
Anaphylaxis
Adrenal insufficiency
Serotonin syndrome
Androgen deficiency
Black box warning:
Contraindications/caution:
Contraindications:
Caution:
Pregnancy consideration: Opioids, including buprenorphine, can cross the placenta, leading to respiratory depression and psychophysiological effects in neonates. The use of opioids is generally not recommended in women immediately before and during labor.
Lactation: Excretion of the drug in human breast milk is known. Caution should be exercised when administering opioid therapy to nursing women.
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
<b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
buprenorphine binds to and activates mu-opioid receptors in the brain, spinal cord, and other areas of the central nervous system. It acts as a partial agonist, producing opioid effects but with a ceiling effect, limiting its maximal effect even at higher doses. This property reduces the risk of respiratory depression compared to full opioid agonists.
Pharmacodynamics:
The pharmacodynamics of buprenorphine buccal:
Pharmacokinetics:
Absorption
When administered via the buccal route, buprenorphine is absorbed through the mucous membranes of the oral cavity. It undergoes rapid absorption, with a portion of the drug entering the bloodstream through the oral mucosa. The buccal route provides a relatively high bioavailability for buprenorphine.
Distribution
buprenorphine is extensively distributed throughout the body. It has a high lipid solubility, allowing it to cross the blood-brain barrier and distribute into various tissues, including the central nervous system. Buprenorphine binds extensively to plasma proteins, primarily to albumin.
Metabolism
buprenorphine is extensively metabolized in the liver primarily through hepatic metabolism. The main metabolic pathway is N-dealkylation, catalyzed by the cytochrome P450 enzyme system, particularly CYP3A4. The major metabolite formed is norbuprenorphine, which has partial agonist activity at the mu-opioid receptor.
Elimination and Excretion
The metabolites of buprenorphine, including norbuprenorphine, are primarily eliminated through urine and, to a lesser extent, through feces. Only a tiny fraction of the parent drug is excreted unchanged. The elimination half-life of buprenorphine is variable and can range from 20 to 73 hours, depending on individual factors and dosing.
Administration:
buprenorphine buccal is a formulation of buprenorphine designed for administration through the buccal mucosa, which refers to the area inside the cheek. Here’s a general overview of the administration of buprenorphine buccal:
Patient information leaflet
Generic Name: buprenorphine buccal
Why do we use buprenorphine buccal?
buprenorphine buccal is primarily used for the management of moderate to severe pain. It is a formulation of buprenorphine designed to be administered through the buccal mucosa (inside the cheek).
