Centrally acting Analgesics Flashcards

1
Q

Name Morphine Analogues.

A

Morphine, Heroin, Codeine.

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2
Q

Heroin.

A

Diamorphine.

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3
Q

Synthetic Derivatives of Morphine?

A

Methadone, Fentanyl, Pethidine, Pentazocine.

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4
Q

Stuff that act like opoids in the body?

A

Endorphins, Enkephanlins and Dynorphins.

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5
Q

Types of receptors affected by opoids?

A

Mu, Delta and Kappa.

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6
Q

How does morphine work?

A

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.

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7
Q

What happens when a opoid receptor is activated?

A

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

Activation of descending gaba neurones.

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8
Q

Mu receptors.

A

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

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9
Q

Kappa receptors

A

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

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10
Q

Delta receptors.

A

Very small analgesic effect.

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11
Q

Pure Agonists at Mu and Kappa?

A

Morphine, Methadone, Fentanyl, Codeine.

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12
Q

Pure Antagonist?

A

Naloxone.

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13
Q

A mixed Agonist-Antagonist?

A

Buprenorphine.

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14
Q

Partial Agonist?

A

Pentazocine, Nalbuphine.

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15
Q

Effects of Opoids.

A

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

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

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16
Q

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

A

Miosis - pinpoint pupils.

17
Q

Codeine.

A

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

18
Q

Pure Agonists at Mu and Kappa?

A

Morphine, Methadone, Fentanyl, Codeine.

19
Q

Pure Antagonist?

A

Naloxone.

20
Q

A mixed Agonist-Antagonist?

A

Buprenorphine.

21
Q

Partial Agonist?

A

Pentazocine, Nalbuphine.

22
Q

Tramadol.

A

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

Oral, IM and IV.

23
Q

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

A

Miosis - pinpoint pupils.

24
Q

Morphine.

A

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

In the liver it becomes more potent

25
Q

Pethidine.

A

Fast. Moderate - severe pain.

26
Q

Fentanyl.

A

Moderate - severe, Lipophilic.

27
Q

Methadone.

A

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

28
Q

Etorphine.

A

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

29
Q

Tramadol.

A

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

30
Q

Why is tramadol easy to prescribe?

A

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

31
Q

Morphine.

A

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

32
Q

How long would morphine last?

A

2-3 hours.

33
Q

When will morphine be completely removed?

A

In one day.

34
Q

Effects of Opioids in general?

A

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.

35
Q

Contraindications of Opioids?

A

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

36
Q

Do not use a Pure Agonist with,

A

A weak partial agonist.

37
Q

What’s the difference between Dependance and Addiction?

A

Dependance is physical, Addiction is psychological.

Dependance lasts only for a few days whereas psychological can go on for years.

38
Q

Naloxone.

A

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

39
Q

Morphine over dosage triad.

A

Pinpoint pupil, Coma, Respiratory depression