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Sports Pharmacology > 2.1 Opiates and Opiate Receptor Agonists > Flashcards

2.1 Opiates and Opiate Receptor Agonists Flashcards

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1
Q

What is pain?

A

A signal that an offensive stimuli may be harmful.

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2
Q

What is a nociceptor?

A

A nociceptor is a peripheral neuron that responds to offensive stimuli that may damage our tissue, by converting this stimuli into a chemical message that travels up the spinal cord and brain via nociceptive nerve fibers.

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3
Q

What is the name of the chemical message that travels up nerves to signal pain?

A

Substance P

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4
Q

What area of the brain translates the message from Substance P into what we know as “pain”?

A

The Somatosensory Cortex

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5
Q

What are the two types of pain?

A
  • Somatic pain

- Visceral pain

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6
Q

What type of nociceptive nerve fiber is responsible for somatic pain?

A

Myelinated “type A” nociceptive nerves

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7
Q

What type of pain is transmitted via Type A myelinated fibers?

A

Somatic…Fast conducting, finger in the door, abrupt pain.

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8
Q

How fast does a Substance P signal travel through somatic, type A, myelinated nerve fibers?

A

30m/sec

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9
Q

What type of nociceptive nerve fiber is responsible for visceral pain?

A

Non-myelinated, “type C” nociceptive nerves

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10
Q

What type of pain is transmitted via Type C, non-myelinated fibers?

A

Visceral…dull, aching pain

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11
Q

How fast does a substance P signal travel through visceral, Type C, non-myelinated fibers?

A

2m/sec

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12
Q

What are the two types of pain pathways?

A
  • Afferent

- Efferent

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13
Q

What happens in the afferent pathway when the nociceptor is activated?

A
  • Substance P travels from site of injury to the CNS via nociceptive nerve fibers.
  • These fibers enter the spinal cord via the dorsal root and synapse with other neurons in the dorsal horn.
  • Secondary nerve fibers then carry Substance P across the spinal cord and up the spinothalamic tract to the thalamus and then the cortex (pain) and limbic system (emotions).
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14
Q

What areas of the brain are affected by substance P?

A
  • Thalamus
  • Cortex (pain)
  • Limbic system (emotions)
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15
Q

What pathway carries response signals following pain activation in the brain?

A

Efferent pathways

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16
Q

What happens in the efferent pathway following pain signaling?

A
  • endogenous peptides (endorphins, dynomorphins, and enkephalins) travel from the medular area of the brain down to the dorsal horn.
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17
Q

What is the role of endogenous peptides in the efferent pathways?

A
  • to interfere with Substance P transmission at the dorsal horn, thereby suppressing the chemical message that signals the brain that there is pain.
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18
Q

Where do endogenous peptides interfere with the transmission of Substance P?

A

At the synapses of the afferent pathway of the dorsal horn.

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19
Q

How do endogenous peptides interfere with the transmission of Substance P at the synapses?

A

The peptides complex with the Mu receptors at the Pre-synaptic terminal of the nerve fibers located at the dorsal horn.

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20
Q

What happens when peptides complex with the Mu receptors at the pre-synaptic terminal of the dorsal horn?

A

They inhibit the influx of Ca+ into the cells of the nerve fibers, preventing an action potential.

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21
Q

What is the result of preventing the action potential at the presynaptic terminal?

A

This prevents Substance P from transmitting from one nerve cell to the next, effectively blocking the pain signal from reaching the brain.

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22
Q

What are the 3 Endogenous Opiate Peptide Receptor types?

A

1) Mu receptor
2) Delta Receptor
3) Sigma receptor

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23
Q

What is the role of the Mu receptors when activated and their location?

A
  • Pain relief at the dorsal horn synapse
  • causes Euphoria in the limbic system via dopamine release
  • causes Addiction
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24
Q

What is the role and location of the Delta Receptors when activated?

A

Located in GI tract - causes constipation

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25
Q

What is the role of the Sigma receptors?

A

PCP receptor - causes dysphoria, rage, and hallucinations when activated

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26
Q

What is the function of Synthetic Opiate Agonists?

A

The mimic endogenous peptides at the dorsal horn, suppressing Substance P.

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27
Q

What is another term for Synthetic Opiate Agonists?

A

Mu agonists (mimic endogenous peptide activity at the Mu receptors)

28
Q

What are the 7 most common SPECIFIC Mu agonists?

A

1) Morphine
2) Diacetylmorphine (DAM)
3) Codeine
4) Hydrocodone
5) Hydromorphine
6) Oxycodone
7) Meperidine

29
Q

What are the specific characteristics of Morphine?

A
  • Mu agonist
  • Analgesic (short and long term)
  • An alkaloid (plant derived - from opium)
30
Q

Which Mu agonist has a 10mg dose that is considered the prototype for which all others are compared?

A

Morphine - 10mg dose

31
Q

What is the main problem with morphine?

A

it has a 50% first-pass effect, which is why it is IV administered.

***Oral doses would need to be very high

32
Q

What is the common name for Diacetylmorphine?

A

heroin

33
Q

What differentiates Diacetlymorphine from Morphine?

A

DAM has an acetyl group attached in place of hydroxyl group.

  • more carbons
  • increased lipid solubility due to acetyl group
34
Q

What is the result of the increased lipid solubility of heroin (DAM)?

A

Increased lipid solubility allows it to pass more rapidly through the Blood Brain Barrier and converted to morphine.

35
Q

What are side effects of morphine?

A
  • pneumonia
  • skin abcesses
  • collapsed veins
  • heart valve disease
  • addiction
  • hepatitis C
36
Q

What class of controlled substance is codeine?

A

Schedule 2

37
Q

What is codeine used for most commonly?

A

Moderate pain control in ambulatory patients (still mobile)

38
Q

What is the first pass effect of codeine in relation to morphine?

A

Decreased first pass effect compared to morphine

39
Q

What is a secondary use for codeine?

A

It is an excellent anti-tussin (cough suppressant)

40
Q

What is the common name for Hydrocodone?

A

Vicodin

Tylenol 3

41
Q

How does hydrocodone compare to codeine and morphine?

A

stronger than codeine, 1/10th as strong as morphine

42
Q

What is another name for hydromorphone?

A

dilaudid

43
Q

What advantage does hydromorphone have over morphine?

A

10 times the oral dosing potency of morphine due to hydrolization…increased water solubility

44
Q

What is vicodin a combination of?

A

hydrocodone and acetaminophen

45
Q

What is a side effect of hydromorphone (dilaudid)?

A

hyperglycemia

46
Q

What are the brand names of oxycodone?

A
  • Roxicodone
  • Percocet (oxycodone & acetaminophen)
  • Percodan (oxycodone & aspirin)
  • Oxycontin (12hr oxycodone)
47
Q

What is the brand name of meperidine?

A

Demerol

48
Q

What is the side effect of meperidine?

A

metabolized into meperedinic acid - causes seizures

49
Q

What are the two Delta Receptor Opiate receptor agonists?

A

1) Loperamide

2) Diphenoxylate & atropine

50
Q

What is the common name and use for loperamide?

A

Immodium A-D

- specific Delta receptor agonist that treats diarrhea

51
Q

What is lomotil (dephenoxylate and atropine) used for?

A

Diarrhea

52
Q

What is the side effect of high doses of atropine?

A

hallucinations and drastic change in BP

53
Q

What are common administrations of Fentanyl used for?

A

IV: analgesic prior to operation for amnesia and pain relief
Transdermal: ambulatory patients
Lozenges

54
Q

What is the secondary effect of Tramadol besides Mu agonist for pain relief?

A

Increases serotonin levels (serotonin raises endogenous peptide levels)

55
Q

What is the contraindication for tramadol due to its effect on serotonin levels?

A

Increased risk of seizures

Potentially harmful with SSRI’s

56
Q

What is the MOA for methadone?

A

It’s an opiate agonist substitute that occupies Mu receptor with minimal pain relief, but good withdrawal prevention.

57
Q

What is suboxone a combination of?

A

Buprenorphine - partial Mu receptor agonist with high affinity but low intrinsic activity. Prevents withdrawal without euphoria.
- Naltrexone - blocks heroin and other opiates

58
Q

What is the advantage/disadvantage of suboxone over methadone?

A

suboxone blocks opiates, but is expensive

59
Q

What are the effects of opiate analgesics on the body?

A 
CNS - analgesia
drowsiness
Mood changes - mu euphoria; sigma dysphoria
Mental clouding
Nausea
Lower seizure threshold
Constipation - delta receptor
Contracted pupils
Histamine release - itching
Vasodilation
Respiratory Depression - primary cause of death due to respiratory failure
60
Q

What causes withdrawal?

A

Body stops releasing endogenous peptides

61
Q

What are withdrawal symptoms?

A

6-12 hrs - sweating, restlessness, rhinorrhea
12-24 - dilated pupils, twitching, tremors
1-3 days - intestinal spasms, depression, increased bp & hr, hot-cold flashes

62
Q

What happens with acute overdose?

A

Triad:
pinpoint pupils
respiratory depression
coma

63
Q

What types of non-opiates are used in pain control?

A

1) anti-convulsants
2) tri-cyclic antidepressants
3) SSRI’s

64
Q

What is the MOA for anti-convulsants in pain relief?

A

sodium channel blockage (prevents action potential)

65
Q

What is the MOA for TC anti depressants?

A

increased serotonin and norepinephrine levels

- increased endogenous peptide levels

66
Q

What is the MOA for SSRI’s in pain relief?

A

increased serotonin levels at dorsal horn

Sports Pharmacology (4 decks)

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