A.18

Question 1

Semisynthetic and synthetic opioids

Answer 1

1. Semisynthetic- Hydromorphone, Oxycodone, Dihydrocodein, Buprenorphine, Nalbuphine, Naloxone, Methyl-naltrexone
2. Synthetic- Methadone, Meperidine (=pethidin), Fentanyl, Tramadol, Diphenoxylate, Loperamide

Question 2

serotonin syndrome

Answer 2

acute, life threatening situation that can lead to hyperthermia, epileptiform seizures, acidosis, hemodynamic changes (caused by combining drugs together)

Question 3

“ceiling” effect

Answer 3

if you increase the dose most effects will not increase after a certain point

Question 4

Breakthrough pain

Answer 4

A sudden increase in pain that may occur in patients who already have chronic pain from cancer, arthritis, fibromyalgia, or other conditions. Breakthrough pain usually lasts for a short time.

Question 5

Hydromorphone

Answer 5

MOA: Semi-synthetic strong μ-OR agonist;
Analgestic potency: 8X more potent than morphine; Effect: similar to morphine (CNS effects and Peripheral effects);
ROA: p.o

Question 6

Oxycodone

Answer 6

MOA: Semi-synthetic strong μ-OR agonist, Codeine derivative;
Effects: similar to morphine;
IND: used in cancer associated pain and chronic musculoskeletal pain;
SEs: constipation;
ROA: p.o combined with naloxone (naloxone antagonizes the constipation)

Question 7

Methadone

Answer 7

MOA: synthetic strong μ-OR agonist;
IND: management of opioid withdrawal syndrome, maintenance programs for addicts;
DOA: 20-30h;
Extra: good BAp.o; ROA: p.o

Question 8

Meperidine

Answer 8

Analgestic potency: 0.1;
MOA: synthetic strong μ-OR agonist, κ-OR agonist, M-AChR antagonist;
IND: opioid analgestic, easy to use (ER, preoperative); Effect: weaker sedative and miotic effect than morphine, no antitussive effect, Anti-M effect (↑HR), weaker uterus relaxant+biliary effect;
DOA: 2-4h;
SEs: toxic metabolite (Norpethidine) no chronic use

Question 9

Fentanyl

Answer 9

MOA: synthetic strong μ agonist;
AP: 100X more than morphine;
T1/2: 1-2h;
ROA: i.v, T.D patch, buccal film, lollypop, nasal spray; IND: General anesthesia, ICU: analgosedation, Emergency: painful situations, chronic cancer patients (t.d. patch);
Extra: the buccal film and nasal spray are used in break-through pain

Question 10

Dihydrocodein

Answer 10

MOA: semisynthetic weak μ-OR agonist;
Extra: Codeine derivative;
AP: more than codeine;
IND: antitussive effect, stronger analgestic effect than codeine

Question 11

Tramadol

Answer 11

MOA: synthetic weak μ-OR agonist, inhibitor of NE +5-HT reuptake;
ROA: i.v, p.o;
IND: neurophatic pain;
DOA: 6h;
SEs: nausea, vomiting, in elderly-severe confusion;
Contra-IND: cannot be used with other serotonergic agents (can lead to serotonin syndrome)

Question 12

Diphenoxylate, Loperamide

Answer 12

MOA: synthetic weak μ-OR agonist;
IND: anti-diarrheal agents (↓GI motility+secretions); Extra: Loperamide penetrates BBB with difficulty (no CNS effect)

Question 13

Buprenorphine

Answer 13

MOA: weak μ-OR agonist, κ-OR antagonist (has high affinity for OR);
AP: 0.4-0.5 (weak analgestic);
IND: opioid addiction, respiratory depression (less than morphine);
SEs: precipitation of withdrawal symptoms in morphine addicts;
Extra: usually given in a pill with Naloxone;
ROA: p.o, sublingual t.d

Question 14

Nalbuphine

Answer 14

MOA: semisynthetic μ-OR partial agonist, κ-OR agonist; AP: 0.8-1;
Effect: analgesia, dysphoria, sedation, “ceiling” effect, naloxone antagonism is weaker;
IND: spinal anesthesia;
SEs: sedation, dysphoria, sweating

Question 15

Naloxone

Answer 15

MOA: semisynthetic strong NS-OR antagonist;
ROA: I.V, i.m, I.O, p.o is given with oxycodone;
IND: opioid intoxication;
SEs: agitation, rage;
Extra: no oral BA, very fast effect;
DOA: 20min

Question 16

Methyl-Naltrexone

Answer 16

MOA: peripherally acting OR antagonist;
IND: opioid induced constipation;
Extra: cannot cross the BBB