buprenorphine

Question 1

absorption

Answer 1

readily absorbed through GIT
- but has very poor bioavailability due to first pass metabolism

Question 2

distribution

Answer 2

rapidly and extensively distributed through BBB as highly lipophilic

Question 3

metabolism

Answer 3

hepatic by CYP450 mediated N dealkylation to norbuprenorphine

Question 4

excretion

Answer 4

via faeces and urine

Question 5

MOA

Answer 5

1. an opioid receptor partial agonist at the Mu receptor
2. has weak activity towards Kappa and delta receptors

Question 6

indications

Answer 6

1. moderate to severe pain
2. intraoperative analgesia
3. adjunct in treatment of opioid dependence

Question 7

adverse effects

Answer 7

• constipation
• drug dependence
• confusion

Question 8

interactions

Answer 8

• morphine
• oxycodone

Question 9

contraindications

Answer 9

• acute respiratory depression
• raised intracranial pressure
• severe hepatic impairment