This presentation deals with buprenorphine drug profile, from a clinical pharmacist perspective. Summarized version of drug, including chief ADRs, interactions, and patient and health-care professional counselling tips have been mentioned.

1. DR. VISHNU R NAIR,
PharmD, Dip. (Neuroplasticity), Dip. (Keto Dietary Advisor), Dip.
(Psychotherapy), Nutrition Coach,
Assistant Professor (Dept. of Pharmacy Practice),
NIMS Institute of Pharmacy, NIMS University.

2. Drug  opioid in nature  mandates prescription use of drug!
Comes under “controlled substance”

3. Injection
Transdermal patch
Buccal film
Subcutaneous implants
Sublingual tablets.

4. In refractory, severe pain
Opioid dependence
Opioid withdrawal in heroin dependence.

5. Buprenorphine  acts on µ-opioid receptors (Agonistic effect) 
alters perception of pain (central & neuropathic)
Drug  weak kappa-antagonist
Pregnancy category: “C”
Use with caution, if benefits outweigh risks !

6. DOSING PRINCIPLES

7. Indicated in age group 2-12 years
Indicated for moderate-severe pain
Dose: 2-6 µg/kg, every 4-6 hours (i.m/ slow i.v)

8. CIRCUMSTANCE DOSING PRINCIPLE
Usual dose 0.15-0.6 mg, every 4-8 hours (as required)
For acute pain 0.3 mg i.m/ i.v, Q6-Q8H (as required)
For chronic pain:
 Transdermal patch
 Buccal film
 5-20 µg/hr, apply once every week
 75 µg, once daily.
For opioid dependence 16 mg/day (sublingual) [ Maintenance dose]
For opiate withdrawal in heroin-dependence 0.3-0.9 mg; i.v; Q6-Q12H
In hepatic impairment For severe impairment  reduce dose by 50% (for
sublingual and buccal dosages).

9. ADVERSE EFFECTS

10. Sedation
Hypotension
Dizziness
Nausea & vomiting
Headache
Respiratory depression
Constipation
If patient using patch/ implants  application-site rashes!

11. Respiratory depression (especially in overdose)
QTc- prolongation  risk of Torsades de pointes!
Hepatotoxicity:
• Drug  CV collapse  shock  ischemic liver injury  liver
damage!
Severe allergic reactions!

12.  Drug + CNS depressants (including alcohol)  high risk of sedation & dizziness
 Drug + CYP3A4 inhibitors (amiodarone, erythromycin, INH)  reduced
metabolism of buprenorphine  high risk of buprenorphine toxicity!
 Drug + CYP3A4 inducers (Rifampin, CBZ, fosphenytoin)  increased metabolism
of buprenorphine  reduced efficacy of buprenorphine!
 Drug + amiodarone, fluoroquinolones, erythromycin  high risk of QTc-
prolongation  high risk of Tdp!
 Drug + MAO-inhibitors  high risk of sedation!

13. Severe respiratory disease
Severe depression
Acute asthmatic attacks
Paralytic ileus:
- Drug  impairs GI motility  can worsen paralytic ileus!
If using transdermal patch:
- Management of mild, acute/intermittent pain
- Management of pain requiring short-term opioid analgesia
- Management of post-operative pain.
CNS depressive effects of
buprenorphine!

14. CNS depression
B.P (hypotension)
Liver enzymes
Pain response.

15. Never use drug with BZDs & CNS depressants :
- High risk of sedation, respiratory depression, coma & death!
Implants  not used properly (inserted/ removed abruptly)  high
risk of nerve damage / embolism  be careful when inserting in upper
arm!
[Buprenorphine + naloxone] combination tablets  preferred over
buprenorphine monotherapy for opioid dependence
- Naloxone  unabsorbed opiate antagonist
- Naloxone  blocks effects of buprenorphine  reduces risk of
buprenorphine abuse!!

16. Patch dose> 20 µg/hr  high risk of QTc-prolongation!
Drug  lowers seizure threshold  use cautiously in patients with
seizure history or currently under treatment!

17.  Avoid alcohol consumption
 Drug  causes drowsiness  impairs ability to focus, operate machinery 
careful!
 Drug  may cause constipation  report to physician/ pharmacist if it gets severe
 Prolonged drug use  high risk of physical/ psychological dependence  use, only
as directed by physician/ pharmacist!
 Do not place direct heat on patch!!!!!
 Report any allergic reactions (especially with patches/ implants)
 Never cut the patches by yourself!
 Apply patches on hairless, dry area
 Keep used & unused patches away from children!

18. THANK YOU!!!