ESPRANOR 8MG ORAL LYOPHILISATE
BUPRENORPHINE HYDROCHLORIDE
What it does
Buprenorphine is an opioid medication used to relieve pain and help with addiction treatment.
Commonly used for: pain relief, opioid addiction treatment
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
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Source: Pharmacy and Poisons Board · fetched 2026-01-28 20:26:11 · updated 2026-09-18 02:29:03
Drug Interactions
74Pharmacodynamic Warnings
Buprenorphine appears in TABLE 11: Drugs with CNS depressant effects
Severe (7)
Buprenorphine - increases exposure
Selpercatinib is predicted to increase the exposure to opioids (alfentanil, buprenorphine). Avoid.
Opioids - decreases concentration
Brigatinib potentially decreases the concentration of opioids (alfentanil, fentanyl). Avoid. Also see TABLE 6 p. 1518
Opioids - increases exposure
Ceritinib is predicted to increase the exposure to opioids (alfentanil, fentanyl). Avoid. Theoretical → Also see TABLE 6 p. 1518
Opioids - increases risk of cnstoxicity
Ritonavir increases the risk of CNS toxicity when given with opioids (pethidine). Avoid.
Opioids - decreases exposure
Lorlatinib is predicted to decrease the exposure to opioids (alfentanil, fentanyl). Avoid.
Opioids - increases risk of adverse effects
Selegiline increases the risk of adverse effects when given with opioids (pethidine). Avoid. Also see TABLE 13 p. 1520
Opioids - increases exposure
Selpercatinib is predicted to increase the exposure to opioids (alfentanil, buprenorphine). Avoid.
Moderate (44)
Buprenorphine - increases exposure
Dronedaroneispredictedtoincreasetheexposuretoopioids (alfentanil,buprenorphine,fentanyl,oxycodone).Monitorand adjustdose.oStudy →AlsoseeTABLE6p.1518
Buprenorphine - increases exposure
Antifungals, azoles (fluconazole, isavuconazole, posaconazole) are predicted to increase the exposure to opioids (alfentanil, buprenorphine, fentanyl, oxycodone). Monitor and adjust dose.
Buprenorphine - increases exposure
Cobicistat is predicted to increase the exposure to opioids (alfentanil, buprenorphine, fentanyl, oxycodone). Monitor and adjust dose.
Buprenorphine - increases exposure
Crizotinibispredictedtoincreasetheexposuretoopioids (alfentanil,buprenorphine,fentanyl,oxycodone).Monitorand adjustdose.oStudy →AlsoseeTABLE6p.1518
Buprenorphine - increases exposure
Idelalisib is predicted to increase the exposure to opioids (alfentanil, buprenorphine, fentanyl, oxycodone). Monitor and adjust dose.
Unknown (23)
Drugs That Cause Serotonin Syndrome - increases risk of serotonin syndrome
Opioids (tapentadol) are predicted to increase the risk of serotonin syndrome when given with drugs that cause serotonin syndrome (see TABLE 13 p. 1520). Theoretical drugs that reduce serum potassium.
Opioids - additive effect
Clozapine can cause constipation, as can opioids; concurrent use might increase the risk of developing intestinal obstruction. Also see TABLE 11 p. 1519
Opioids - increases exposure
Asciminibispredictedtoincreasetheexposuretoopioids (alfentanil).rTheoretical
Opioids - increases exposure
Bictegravirispredictedtoincreasetheexposuretoopioids (methadone).oTheoretical
Opioids - increases exposure
Bulevirtideispredictedtoincreasetheexposuretoopioids (alfentanil).oTheoretical
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: exact
About this medicine
Buprenorphine is an opioid medication used to relieve pain and help with addiction treatment.
What it treats
- pain relief
- opioid addiction treatment
How it works
It works by changing the way the brain and nervous system respond to pain.
Who it's for
It is for adults who need help with severe pain or are undergoing treatment for opioid addiction.
Drug class
Opioids
Cautions
- • Be careful if you are taking other medications that can cause drowsiness or breathing problems.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Buprenorphine
BNF-referencedBuprenorphine is a semi-synthetic opioid used primarily as an analgesic for moderate to severe pain and as a part of a treatment regimen for opioid dependence. It acts as a partial agonist at the mu-opioid receptor, providing analgesic effects while also having antagonist properties that can prevent the effects of other opioids.
Indications
- Moderate to severe pain
- Opioid dependence treatment
Dosage
Children: For children aged 6 months to 11 years, buprenorphine is administered at a dose of 3-6 micrograms/kg every 6-8 hours
Adults: For moderate to severe pain, buprenorphine may be administered as a sublingual tablet or by injection. Typical dosing involves 200-400 micrograms every 6-8 hours, adjusting based on clinical response and patient tolerance.
Mechanism of action
Buprenorphine exerts its effects by binding to the mu-opioid receptors in the central nervous system, activating them to produce analgesia. As a partial agonist, it activates the receptor but to a lesser extent than full agonists like morphine. This property not only alleviates pain but also reduces the risk of respiratory depression compared to full agonists. Additionally, buprenorphine has a ceiling effect, reducing the potential for misuse and overdose.
Pharmacodynamics
Buprenorphine demonstrates a complex pharmacodynamic profile due to its partial agonist activity at the mu-opioid receptors and antagonist effects at the kappa-opioid receptors. It leads to effective pain management with a lower risk of side effects such as sedation and respiratory depression. The drug's affinity for the mu-opioid receptor allows it to displace full agonists, which is beneficial in treating opioid dependence.
Pharmacokinetics
Buprenorphine is well-absorbed through the sublingual route, with peak plasma concentrations typically reached within 1 to 2 hours. It has a high volume of distribution and is extensively metabolized in the liver, primarily by CYP3A4, leading to various metabolites. The elimination half-life is variable, ranging from 24 to 60 hours, allowing for once daily dosing in dependence treatment. Renal impairment may prolong the effects of the drug, while liver function should be monitored during therapy.
Contra-indications
- Severe respiratory depression
- Acute or severe bronchial asthma
- Known or suspected gastrointestinal obstruction, including paralytic ileus
- Hypersensitivity to buprenorphine or any of its excipients
Adverse effects
- Nausea
- Vomiting
- Constipation
- Drowsiness
- Dizziness
- Headache
- Sweating
- Hypotension
- Withdrawal syndrome in opioid-dependent patients
- Respiratory depression
Interactions
- Selpercatinib increases exposure to buprenorphine (severe interaction)
- Dronedarone increases exposure to buprenorphine (moderate interaction)
- Antifungals (azoles) increase exposure to buprenorphine (moderate interaction)
- Cobicistat increases exposure to buprenorphine (moderate interaction)
- Crizotinib increases exposure to buprenorphine (moderate interaction)
- Idelalisib increases exposure to buprenorphine (moderate interaction)
- Imatinib increases exposure to buprenorphine (moderate interaction)
- Letermovir increases exposure to buprenorphine (moderate interaction)
- Clarithromycin increases exposure to buprenorphine (moderate interaction)
- Erythromycin increases exposure to buprenorphine (moderate interaction)
Precautions
- Caution in patients with impaired consciousness
- Monitor liver function regularly during treatment
- Consider the effects of concomitant medications that may enhance sedation or respiratory depression
- Avoid use in patients with severe renal impairment unless necessary
Pregnancy
Buprenorphine should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus. It is a category C drug, meaning risk cannot be ruled out. Close monitoring is recommended.
Breast-feeding
Buprenorphine is excreted in breast milk; caution should be exercised when administering to breastfeeding women. Monitoring of the infant for sedation and respiratory depression is advisable.
Storage
Store in a cool, dry place, away from direct sunlight. Keep out of reach of children.
Formulations
- Sublingual tablets
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: Buprenorphine
PubChem CID 644073Molecular formula: C29H41NO4
Mechanism of action
Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. It demonstrates a high affinity for the mu-opioid receptor but has lower intrinsic activity compared to other full mu-opioid agonists such as [heroin], [oxycodone], or [methadone]. This means that buprenorphine preferentially binds the opioid receptor and displaces lower affinity opioids without activating the receptor to a comparable degree. Clinically, this results in a slow onset of action and a clinical phenomenon known as the "ceiling effect" where once a certain dose is reached buprenorphine's effects plateau. This effect can be beneficial, however, as dose-related side effects such as respiratory depression, sedation, and intoxication also plateau at around 32mg, resulting in a lower risk of overdose compared to [methadone] and other full agonist opioids. It also means that opioid-dependent patients do not experience sedation or euphoria at the same rate that they might experience with more potent opioids, improving quality of life for patients with severe pain and reducing the reinforcing effects of opioids which can lead to drug-seeking behaviours. Buprenorphine's high affinity, but low intrinsic activity for the mu-opioid receptor also means that if it is started in opioid-dependent individuals, it will displace the other opioids without creating an equal opioid effect and cause a phenomenon known as "precipitated withdrawal" which is characterized by a rapid and intense onset of withdrawal symptoms (i.e. anxiety, restlessness, gastrointestinal distress, diaphoresis, intense drug cravings, and tachycardia). Individuals must therefore be in a state of mild to moderate withdrawal before starting therapy with buprenorphine. Buprenorphine is commercially available as the brand name product Suboxone which is formulated in a 4:1 fixed-dose combination product along with [naloxone], a non-selective competitive opioid receptor antagonist. Combination of an opioid agonist with an opioid antagonist may seem counterintuitive, however this combination with naloxone is intended to reduce the abuse potential of Suboxone, as naloxone is poorly absorbed by the oral route (and has no effect when taken orally), but would reverse the opioid agonist effects of buprenorphine if injected intravenously.
Pharmacodynamics
Buprenorphine interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissues. In clinical settings, buprenorphine exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Buprenorphine depresses the respiratory centers, depresses the cough reflex, and constricts the pupils. **Dependence** Buprenorphine is a partial agonist at the mu-opioid receptor and chronic administration produces physical dependence of the opioid type, characterized by withdrawal signs and symptoms upon abrupt discontinuation or rapid taper. The withdrawal syndrome is typically milder than seen with full agonists and may be delayed in onset. Buprenorphine can be abused in a manner similar to other opioids. This should be considered when prescribing or dispensing buprenorphine in situations when the clinician is concerned about an increased risk of misuse, abuse, or diversion. **Withdrawal** Abrupt discontinuation of treatment is not recommended as it may result in an opioid withdrawal syndrome that may be delayed in onset. Signs and symptoms may include body aches, diarrhea, gooseflesh, loss of appetite, nausea, nervousness or restlessness, anxiety, runny nose, sneezing, tremors or shivering, stomach cramps, tachycardia, trouble with sleeping, unusual increase in sweating, palpitations, unexplained fever, weakness and yawning. **Risk of Respiratory and Central Nervous System (CNS) Depression and Overdose** Buprenorphine has been associated with life-threatening respiratory depression and death. Many, but not all, post-marketing reports regarding coma and death involved misuse by self-injection or were associated with the concomitant use of buprenorphine and benzodiazepines or other CNS depressant, including alcohol. Use buprenorphine and naloxone sublingual tablets with caution in patients with compromised respiratory function (e.g., chronic obstructive pulmonary disease, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression). **Risk of Overdose in Opioid Naïve Patients** There have been reported deaths of opioid-naïve individuals who received a 2 mg dose of buprenorphine as a sublingual tablet for analgesia. Buprenorphine and naloxone sublingual tablets are not appropriate as an analgesic in opioid-naïve patients. **Precipitation of Opioid Withdrawal Signs and Symptoms** If buprenorphine is started in opioid-dependent individuals, it will displace the other opioids and cause a phenomenon known as "precipitated withdrawal" which is characterized by a rapid and intense onset of withdrawal symptoms. Individuals must therefore be in a state of mild to moderate withdrawal before starting therapy with buprenorphine. Because it contains naloxone, buprenorphine and naloxone sublingual tablets are also highly likely to produce marked and intense withdrawal signs and symptoms if misused parenterally by individuals dependent on full opioid agonists such as heroin, morphine, or methadone. **Gastrointestinal Effects** Buprenorphine and other morphine-like opioids have been shown to decrease bowel motility and cause constipation. Buprenorphine may obscure the diagnosis or clinical course of patients with acute abdominal conditions and should be administered with caution to patients with dysfunction of the biliary tract. **Effects on the Endocrine System** Opioids inhibit the secretion of adrenocorticotropic hormone (ACTH), cortisol, and luteinizing hormone (LH) in humans. They also stimulate prolactin, growth hormone (GH) secretion, and pancreatic secretion of insulin and glucagon. Chronic use of opioids may influence the hypothalamic-pituitary-gonadal axis, leading to androgen deficiency that may manifest as low libido
Biological pathways
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
This drug in other countries
The same active ingredient registered across other registries we cover - including different brands.