B. 26. Semisynthetic and synthetic opiates

Question 1

list the synthetic opiates

Answer 1

Fentanyl
Tramadol
Meperidine 
Loperamide
Diphenoxylate 
Methadone

Question 2

what is Naloxone?

Answer 2

semi-synthetic opioid antagonist

strong

Question 3

what is Naltrexone?

Answer 3

synthetic opioid antagonist

strong

Question 4

list the semisynthetic opiates

Answer 4

oxycodone
dihydrocodeine
Buprenorphine
Nalbuphine

Question 5

which agent has the highest potency- morphine or fentanyl?

Answer 5

fentanyl is 100x more potent than morphine

Question 6

what are the strong agonists

Answer 6

Fentanyl
Meperidine
Oxycodone
Methadone

Question 7

what are the weak agonists

Answer 7

Tramadol
Loperamide
Diphenoxylate
codeine
dihydrocodeine

Question 8

which agent has the highest potency- morphine or Buprenorphine?

Answer 8

Buprenorphine has 25-50x more potent than morphine

Question 9

which agents have mixed activity?

Answer 9

Buprenorphine
Nalbuphine
ᴋ antagonist
µ agonist (partial)

Question 10

what are the uses of Fentanyl?

Answer 10

analgesic (post-operative pain, chronic pain syndromes)–> transdermal (chronic pain-25-100µg)/sublingual
anesthesia –>IV

Question 11

what is the duration of action and max daily dose of Tramadol?

Answer 11

6 hours

max. 400mg

Question 12

what are the uses of Tramadol?

Answer 12

analgesic (neuropathic pain, dentistry)

Question 13

what are the SE’s of Tramadol

Answer 13

nausea- vomiting
dizziness
sweating
dry mouth 
sedation
epilepsy
respiratory depression

Question 14

what causes serotonin syndrome when giving Tramadol?

Answer 14

Tramadol inhibits NE and 5-HT reuptake
shouldn’t be combined with MAO inhibitors
can cause epilepsy

Question 15

what is Meperidine used for?

Answer 15

analgesic use (emergency care, pre-operative)

Question 16

what might lead to serotonin syndrome when giving Meperidine?

Answer 16

has serotonergic activity

antimuscarinic effect–>antagonizes the smooth muscle effects of opioids –>no constipation or urinary retention

Question 17

which agent is a potential drug of abuse?

Answer 17

oxycodone

Question 18

which opiates are anti-diarrheal agents?

Answer 18

Loperamide

Diphenoxylate

Question 19

when do we use oxycodone?

Answer 19

analgesic use (post-operative pain, chronic pain syndromes)

Question 20

what are the indications for giving Codeine and Dihydrocodeine?

Answer 20

antitussive (suppress coughing)

analgesic effect in combination with NSAID’s or acetaminophen

Question 21

what can Codeine and Dihydrocodeine cause?

Answer 21

epileptic seizures

Question 22

which agent is safer than Morphine?

Answer 22

Nalbuphine

less cardiovascular effects

Question 23

which agent is used for spinal anesthesia?

Answer 23

Nalbuphine

Question 24

what are the indications for giving Methadone and Buprenorphine

Answer 24

management of opioid withdrawal syndrome

maintenance programs for addicts (heroin, morphine)

Question 25

which opiates have a long serum T1/2?

Answer 25

methadone | Buprenorphine

Question 26

which opiate has good absorption?

Answer 26

buprenorphine

Question 27

when do we give Naloxone?

Answer 27

management of acute opioid overdose (IV administration)

Question 28

Naloxone dose

Answer 28

0.4mg

Question 29

why combine Naloxone with OXYCODONE?

Answer 29

may reduce opioid bowel syndrome --> antagonizes constipation

Question 30

what is the indications for giving Naltrexone?

Answer 30

management of opioid withdrawal syndrome -->oral 50 mg | management of alcohol withdrawal syndrome

Question 31

what is the T1/2 of Naltrexone and SE's

Answer 31

Long T1/2--> up to 48h' | hepatotoxic

Question 32

what is Methylnaltrexone?

Answer 32

peripheral opioid antagonist | can't enter the brain

Question 33

what is Methylnaltrexone usually used for?

Answer 33

avoid constipation from opioid bowel syndrome | without affecting pain relief