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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
What is the role of the Sigma receptors?
PCP receptor - causes dysphoria, rage, and hallucinations when activated
26
What is the function of Synthetic Opiate Agonists?
The mimic endogenous peptides at the dorsal horn, suppressing Substance P.
27
What is another term for Synthetic Opiate Agonists?
Mu agonists (mimic endogenous peptide activity at the Mu receptors)
28
What are the 7 most common SPECIFIC Mu agonists?
1) Morphine 2) Diacetylmorphine (DAM) 3) Codeine 4) Hydrocodone 5) Hydromorphine 6) Oxycodone 7) Meperidine
29
What are the specific characteristics of Morphine?
- Mu agonist - Analgesic (short and long term) - An alkaloid (plant derived - from opium)
30
Which Mu agonist has a 10mg dose that is considered the prototype for which all others are compared?
Morphine - 10mg dose
31
What is the main problem with morphine?
it has a 50% first-pass effect, which is why it is IV administered. ***Oral doses would need to be very high
32
What is the common name for Diacetylmorphine?
heroin
33
What differentiates Diacetlymorphine from Morphine?
DAM has an acetyl group attached in place of hydroxyl group. - more carbons - increased lipid solubility due to acetyl group
34
What is the result of the increased lipid solubility of heroin (DAM)?
Increased lipid solubility allows it to pass more rapidly through the Blood Brain Barrier and converted to morphine.
35
What are side effects of morphine?
- pneumonia - skin abcesses - collapsed veins - heart valve disease - addiction - hepatitis C
36
What class of controlled substance is codeine?
Schedule 2
37
What is codeine used for most commonly?
Moderate pain control in ambulatory patients (still mobile)
38
What is the first pass effect of codeine in relation to morphine?
Decreased first pass effect compared to morphine
39
What is a secondary use for codeine?
It is an excellent anti-tussin (cough suppressant)
40
What is the common name for Hydrocodone?
Vicodin | Tylenol 3
41
How does hydrocodone compare to codeine and morphine?
stronger than codeine, 1/10th as strong as morphine
42
What is another name for hydromorphone?
dilaudid
43
What advantage does hydromorphone have over morphine?
10 times the oral dosing potency of morphine due to hydrolization...increased water solubility
44
What is vicodin a combination of?
hydrocodone and acetaminophen
45
What is a side effect of hydromorphone (dilaudid)?
hyperglycemia
46
What are the brand names of oxycodone?
- Roxicodone - Percocet (oxycodone & acetaminophen) - Percodan (oxycodone & aspirin) - Oxycontin (12hr oxycodone)
47
What is the brand name of meperidine?
Demerol
48
What is the side effect of meperidine?
metabolized into meperedinic acid - causes seizures
49
What are the two Delta Receptor Opiate receptor agonists?
1) Loperamide | 2) Diphenoxylate & atropine
50
What is the common name and use for loperamide?
Immodium A-D | - specific Delta receptor agonist that treats diarrhea
51
What is lomotil (dephenoxylate and atropine) used for?
Diarrhea
52
What is the side effect of high doses of atropine?
hallucinations and drastic change in BP
53
What are common administrations of Fentanyl used for?
IV: analgesic prior to operation for amnesia and pain relief Transdermal: ambulatory patients Lozenges
54
What is the secondary effect of Tramadol besides Mu agonist for pain relief?
Increases serotonin levels (serotonin raises endogenous peptide levels)
55
What is the contraindication for tramadol due to its effect on serotonin levels?
Increased risk of seizures | Potentially harmful with SSRI's
56
What is the MOA for methadone?
It's an opiate agonist substitute that occupies Mu receptor with minimal pain relief, but good withdrawal prevention.
57
What is suboxone a combination of?
Buprenorphine - partial Mu receptor agonist with high affinity but low intrinsic activity. Prevents withdrawal without euphoria. - Naltrexone - blocks heroin and other opiates
58
What is the advantage/disadvantage of suboxone over methadone?
suboxone blocks opiates, but is expensive
59
What are the effects of opiate analgesics on the body?
``` 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
What causes withdrawal?
Body stops releasing endogenous peptides
61
What are withdrawal symptoms?
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
What happens with acute overdose?
Triad: pinpoint pupils respiratory depression coma
63
What types of non-opiates are used in pain control?
1) anti-convulsants 2) tri-cyclic antidepressants 3) SSRI's
64
What is the MOA for anti-convulsants in pain relief?
sodium channel blockage (prevents action potential)
65
What is the MOA for TC anti depressants?
increased serotonin and norepinephrine levels | - increased endogenous peptide levels
66
What is the MOA for SSRI's in pain relief?
increased serotonin levels at dorsal horn

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