Buprenorphine

Registered South African indications:

• Opioid dependance

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients 
• Breastfeeding
• Severe hepatic impairment 
• Children < 16 years 
• Severe respiratory insufficiency
• Acute alcoholism or delirium tremens

Cautions

• Pregnancy
• Severe renal impairment
• Mild to moderate hepatic impairment 
• Elderly
• Debilitated patients 
• Children
• Suboptimal treatment
• Non-opioid dependent individuals 
• Chronic obstructive pulmonary disease
• Asthma
• Cor pulmonale
• Decreased respiratory reserve
• Hypoxia
• Hypercapnia
• Mild to moderate respiratory insufficiency 
• Kyphoscoliosis
• Abrupt withdrawal 
• Pre-existing hepatic enzyme abnormalities
• Hepatitis B or C virus
• Alcohol abuse
• Anorexia
• Head injury
• Intracranial lesions
• Suspected increased cerebrospinal pressure
• History of seizures
• Hypotension
• Prostatic hypertrophy
• Urethral stenosis
• Myxoedema
• Hypothyroidism
• Adrenal cortical insufficiency
• Biliary tract dysfunction 
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: slt

Substitution treatment for opioid drug dependence
- Within a framework of medical, social and psychological treatment

• Oral (slt): Initial: 0.8-4mg, as a single dly dose; Titrate according to clinical response; Maintenance: 12-16mg, dly; Max: 16mg/24hrs

For patients dependent on heroin or short-acting opioids, the first dose of buprenorphine should be started when objective signs of withdrawal appear, but not less than 4-6 hours after the patient last used opioids

For patients receiving methadone, the dose of methadone should be reduced to a maximum of 30mg/day before initiating treatment with buprenorphine

After a satisfactory period of stabilisation has been achieved, the dosage may be reduced gradually to a lower maintenance dose

Not indicated for use in children below 16 years

Pregnancy

• FDA Pregnancy Category C

Breastfeeding

• Contraindicated

Renal Impairment

• Severe: Caution; dose adjustment recommended 

Hepatic Impairment

• Mild to moderate: Caution; no dose adjustment recommended 
• Severe: Contraindicated

Elderly

• Caution; no information available 

Porphyria Information

• Not porphyrinogenic (NP)

Drugs in Sport

• Prohibited - In competition

Central Nervous System Disorders

• Insomnia
• Agitation
• Anxiety
• Depression
• Hostility
• Nervousness
• Paranoia
• Abnormal thinking 
• Drug dependence
• Headache
• Dizziness
• Hypertonia
• Migraine
• Paraesthesia
• Somnolence
• Syncope
• Tremor
• Drug withdrawal syndrome
• Neonatal drug withdrawal syndrome
• Asthenia

Cardiovascular Disorders

• Palpitations
• Vasodilatation
• Chest pain 

Respiratory Disorders

• Bronchitis
• Pharyngitis
• Rhinitis
• Cough
• Dyspnoea
• Yawning

Gastrointestinal Disorders

• Nausea and vomiting 
• Abdominal pain
• Constipation
• Tooth disorder 
• Flatulence 
• Diarrhoea
• Dry mouth
• Dyspepsia

Genitourinary Disorders

• Dysmenorrhoea

Endocrine and Metabolic Disorders

• Decreased appetite

Musculoskeletal Disorders

• Arthralgia
• Back pain
• Bone pain
• Muscle spasms
• Myalgia
• Neck pain

Skin and Subcutaneous Tissue Disorders

• Hyperhidrosis
• Rash
• Peripheral oedema 

Immune, Blood and Lymphatic System Disorders

• Lymphadenopathy
• Infection
• Influenza
• Fever
• Chills 

Sensory Disorders

• Lacrimal disorder
• Mydriasis

• Central nervous system depressants
• Opioid analgesics
• Naltrexone
• CYP3A4 inhibitors
• CYP3A4 inducers
• Monoamine oxidase inhibitors

• Blood pressure 
• Hepatic function
• Neurological examination 
• Respiratory examination 

Buprenorphine is an opioid partial agonist and antagonist. It attaches itself to the mu and kappa receptors of the brain. Its activity in opioid maintenance treatment is attributed to its slowly reversible link with the mu receptors which, over a prolonged period, minimises the need of the opioid-dependent patient.

Tablet sublingual 2mg

• Subutex sublingual (Adcock Ingram) originator

Tablet sublingual 8mg

• Subutex sublingual (Adcock Ingram) originator

COMBINATION PREPARATIONS

Buprenorphine/ Naloxone

Tablet sublingual 2mg/0.5mg

• Suboxone (Indivior South Africa) originator

Tablet sublingual 8mg/2mg

• Suboxone (Indivior South Africa) originator