Centrally acting Analgesics

Question 1

Name Morphine Analogues.

Answer 1

Morphine, Heroin, Codeine.

Question 2

Heroin.

Answer 2

Diamorphine.

Question 3

Synthetic Derivatives of Morphine?

Answer 3

Methadone, Fentanyl, Pethidine, Pentazocine.

Question 4

Stuff that act like opoids in the body?

Answer 4

Endorphins, Enkephanlins and Dynorphins.

Question 5

Types of receptors affected by opoids?

Answer 5

Mu, Delta and Kappa.

Question 6

How does morphine work?

Answer 6

Two components in action

Spinal - Inhibits dorsal horn pain transmission.
Supraspinal - Sends inhibitory impulses through descending pathways.

Inhibit release of excitatory transmitters from primary afferents.

Question 7

What happens when a opoid receptor is activated?

Answer 7

Inhibition of Nuerotransmitter release.
Presynaptic - Inactivation of Ca2+ ion channels.
Post synaptic - Increased Potassium conductance (hyperpolarization).

Activation of descending gaba neurones.

Question 8

Mu receptors.

Answer 8

Gets you high, addicted, sedated and can kill you (respiratory depression).

Question 9

Kappa receptors

Answer 9

Modest analgesia with no addiction. Feel like shit and sedated.

Question 10

Delta receptors.

Answer 10

Very small analgesic effect.

Question 11

Pure Agonists at Mu and Kappa?

Answer 11

Morphine, Methadone, Fentanyl, Codeine.

Question 12

Pure Antagonist?

Answer 12

Naloxone.

Question 13

A mixed Agonist-Antagonist?

Answer 13

Buprenorphine.

Question 14

Partial Agonist?

Answer 14

Pentazocine, Nalbuphine.

Question 15

Effects of Opoids.

Answer 15

Analgesia, Sedation, Euphoria, Respiratory and Cough depression, Tranquility.

Nausea, Constipation, Low blood pressure, Urticaria and bronchoconstriction - release of histamines.

Question 16

How can you clinically examine whether the patient may be suffering from an overdose of opoids?

Answer 16

Miosis - pinpoint pupils.

Question 17

Codeine.

Answer 17

Weaker than morphine, mild-moderate pain and cough (depression of cough reflex).

Question 18

Pure Agonists at Mu and Kappa?

Answer 18

Morphine, Methadone, Fentanyl, Codeine.

Question 19

Pure Antagonist?

Answer 19

Naloxone.

Question 20

A mixed Agonist-Antagonist?

Answer 20

Buprenorphine.

Question 21

Partial Agonist?

Answer 21

Pentazocine, Nalbuphine.

Question 22

Tramadol.

Answer 22

Weak acting at Mu. Spinal inhibition of pain. Re-uptake inhibitor of NA and 5-HT.

Oral, IM and IV.

Question 23

How can you clinically examine whether the patient may be suffering from an overdose of opoids?

Answer 23

Miosis - pinpoint pupils.

Question 24

Morphine.

Answer 24

Distributes widely in body and enters brain slowly. Cross to placenta, dependance in foetus.

In the liver it becomes more potent

Question 25

Pethidine.

Answer 25

Fast. Moderate - severe pain.

Question 26

Fentanyl.

Answer 26

Moderate - severe, Lipophilic.

Question 27

Methadone.

Answer 27

Weak and longer lasting. Can give orally, Powerful, Cross tolerance with heroin.

Question 28

Etorphine.

Answer 28

VERRRY powerful, more potent than morphine (1000 to 80000 times).

Question 29

Tramadol.

Answer 29

Weak acting at Mu. Spinal inhibition of pain. Re-uptake inhibiitor of NA and 5-HT.

Question 30

Why is tramadol easy to prescribe?

Answer 30

Less side effects, well tolerated and low abuse potential. Better for MODERATE pain compared to morphine.

Question 31

Morphine.

Answer 31

Distributes widely in body and enters brain slowly. Cross to placenta, dependance in foetus.

Question 32

How long would morphine last?

Answer 32

2-3 hours.

Question 33

When will morphine be completely removed?

Answer 33

In one day.

Question 34

Effects of Opioids in general?

Answer 34

Analgesia, Euphoria/Dysphoria, Respiratory depression (most common cause of death) and decreased gastric motility. Relaxation, hypothermia, Hypotension, Reduced sex drive, Drying of secretion, flushed warm skin, Tranquilization.

Question 35

Contraindications of Opioids?

Answer 35

Pregnancy, Head Injury, Pulmonary, hepatic or renal dysfunction.

Question 36

Do not use a Pure Agonist with,

Answer 36

A weak partial agonist.

Question 37

What's the difference between Dependance and Addiction?

Answer 37

Dependance is physical, Addiction is psychological. Dependance lasts only for a few days whereas psychological can go on for years.

Question 38

Naloxone.

Answer 38

Antagonist at all 3 receptors.Used to treat respiratory depression, precipitate withdrawal syndrome.

Question 39

Morphine over dosage triad.

Answer 39

Pinpoint pupil, Coma, Respiratory depression