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Opiod Analgesics Flashcards

1
Q

What type of receptors are opioid receptors

A

G protein- coupled receptors

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2
Q

Where are G protein coupled receptors located

A

Located primarily in the brain and spinal cord regions (CNS)

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3
Q

What are G protein-coupled receptors involved in

A

transmission and modulation of pain

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4
Q

Four well characterized classes of opioid receptors

A

Mu
Kappa
Delta
Nociception/Orphanin FQ (NOP)

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5
Q

What receptor is primarily targeted by morphine and most of the clinically used opioid agonists

A

Mu receptor and some also interact with the kappa receptor

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6
Q

What receptor typically does not respond to agonists that interact with the classical opioid receptors

A

NOP receptor

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7
Q

What are endogenous opioid peptides

A

natural ligands for the opioid receptors

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8
Q

What are the endogenous opioid peptides

A

Enkephalins, dynorphins, endorphin, and NOP

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9
Q

What are each endogenous opioid peptides derived from

A

Enkephalins: proenkephalin protein
Endorphin: POMC
Dynorphins: prodynorphin
Nociception/Orphanin FQ: Pronociceptin/ OFQ

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10
Q

Activation of the opioid receptors results in three well-characterized actions results in what

A

inhibition of the overall activity of the neurons where the receptors are located

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11
Q

What are the three mechanisms of opioids

A

Inhibition of Ca2+ channels
Activation of K+ channels
Activation of the inhibitory G proteins, Gi/Go

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12
Q

What does the inhibition of Ca2+ channels cause

A

a decrease in intracellular Ca2+
concentrations, which blocks neurotransmitter release

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13
Q

What does activation of K+ channels cause

A

increased K+ efflux, which results in
hyperpolarization and decreased firing of the neurons

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14
Q

What does activation of the inhibitory G proteins cause

A

inhibit adenylate cyclase activity, resulting in a decrease in cyclic AMP (cAMP) production and decreased phosphorylation of downstream targets.

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15
Q

What are the dual components of pain

A

sensory (intensity of perception) and emotional (unpleasantness/reaction)

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16
Q

What’s cutaneous or somatic pain

A

*comes from the skin or close to the surface of the body
* intense pain
* has a minimal emotional component.

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17
Q

What’s deeper (visceral) pain

A
  • tends to be poorly localized
  • has autonomic responses (e.g. sweating, nausea)
  • has a strong emotional component (anguish)
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18
Q

Why are opioids beneficial as analgesics

A

they reduce both the sensory and emotional
components of pain

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19
Q

What is the most dangerous side effect of opiate administration/overdose

A

respiratory depression

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20
Q

True/false: Heroin has greater abuse potential than morphine because it enters the brain more readily

A

True

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21
Q

What properties does Codeine have

A

antitussive properties (stops coughing) with reduced analgesic properties

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22
Q

What two opioids can be considered safer for some patients

A

Pentazocine and Buprenorphine

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23
Q

What do pentazocine and buprenorphine do

A

retain analgesic effects and lower respiratory depression potential, making them safer for some patients

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24
Q

What are the therapeutic effects of opioids

A
  • Analgesia
  • Sedation
  • Euphoria (relief of emotional components of pain)
  • Anti-tussive
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25
What are the adverse effects
* Nausea (most-common adverse effect) * Histamine release (itching, rashes) * GI transit slowed (constipation) * Miosis (pin-point pupils) * Bradycardia (slow heart rate) * Respiratory depression (most dangerous adverse effect) * Dysphoria (kappa agonists) * Psychotomimetic effects (kappa agonists) * Physical dependence and tolerance
26
What is the most common adverse effect of opioids
Nausea
27
What are the clinical signs of opioid over-dose
Coma Pin-point pupils (miosis) Respiratory depression Decreased blood pressure Decreased body temperature Convulsions (with some opioids)
28
What are the treatments for opioid over-dose
Naloxone i.v. (or nasal spray) Produces rapid reversal, but rapid offset. May require repeated administration. Ventilate. Drugs to control hypotension
29
What could happen if patients in shock are given opioids
patients in shoch may exhibit severe hypotension
30
What could happen if head trauma patients are given opioids
(a) The hypercapnia (increased CO2 in the blood) and respiratory depression may dilate cerebral vessels and increase intracranial pressure. (b) The miosis (constriction of the pupil) present following opioid administration may also mask pupillary dilation present with brain injury use opioids with extreme caution**
31
What could happen if patients with renal insufficiency are given opioids
the drug could accumulate in their system
32
True/false: opioids synergize with CNS depressants
TRUE Morphine and other opioids exhibit intense sedative effects and increased respiratory depression when combined with other sedatives, such as alcohol, benzodiazepines or barbiturates
33
What drugs are opioid receptor agonists
Morphine Heroin Codeine Tramadol Fentanyl, Sufentanil, Alfentanil Methadone Oxycodone Oxymorphone Hydrocodone
34
Mixed Agonists/Antagonists
Pentazocine Butorphanol Buprenorphine
35
Opioid Receptor Antagonists
Naloxone Nalmefene (Revex) Naltrexone
36
What drugs are use to help with opioid abstinence
Methadone Buprenorphine + Naloxone Naltrexone
37
Consequences of repeated opioid use
Tolerance Metabolic tolerance Cellular tolerance Cross tolerance
38
What is metabolic tolerance
increased ability of the liver to metabolize a drug results in decreased blood levels of the drug.
39
Cellular tolerance
adaptations in the target cells (e.g. receptor inactivation) produce a weaker response to same blood levels
40
Cross tolerance
the development of tolerance to one drug results in tolerance to other drugs with similar pharmacological actions
41
Tolerance develops to most effects of opioid drugs except:
*miosis *constipation
42
What are withdrawal symptoms
*hypertension *tachycardia *intestinal cramping *emesis (vomiting) *diarrhea *cold sweats
43
True/false: Dependence is equivalent to Addiction
FALSE: one can be physically dependent on an opioid but not addicted
44
What is acute treatment for withdrawal symptoms
Clonidine: alpha-2 adrenergic receptor agonist 2. Clonidine is usually prescribed to lower blood pressure. 3. Clonidine has been found to be helpful in decreasing some of the adrenergic effects of opiate withdrawal, such as hypertension, tachycardia and sweating
45
What is abuse
use of a drug that causes physical, psychological, economic, legal or social harm to the individual or to others
46
What is addiction
behavioral pattern characterized by compulsive use, interest in obtaining drug, high tendency to relapse
47
Morphine
Used for severe and chronic pain Drug of choice for pain associated with myocardial infarction (heart attack) Oldest known opioid drug **Agonist
48
Heroin
Produces pain relief faster than morphine because it crosses BBB faster than morphine ***Agonists
49
Codeine
**Agonists Anti-tussive (relieves coughs) Useful for mild to moderate pain; approximately 12 times weaker than morphine Orally active
50
Tramadol
**Agonists Contraindicated in patients with a history of uncontrolled seizures Can act as an SRI: serotonin reuptake inhibitor, which promotes increased levels of serotonin in the synapse. A combination of tramadol with an MAOI (monoamine oxidase inhibitor) anti-depressant can lead to fatal consequences through serotonin syndrome
51
Fentanyl, Sufentanil, Alfentanil
Agonists** Used as adjuncts to anesthesia, transdermally as analgesics (Fentanyl only) and in oral lozenge form (Fentanyl only) for the induction of anesthesia. Fentanyl is 50-100 times stronger than morphine. *Sufentanil is 5- to 7-fold stronger than fentanyl (about 700 times stronger than morphine) *Alfentanil is approximately 20 times stronger than morphine and very short acting. Fentanyl has a short action of duration, 1-2 hours and a very rapid onset (<20 minutes)
52
Methadone
Agonists* Equivalent to morphine in strength, but orally active Longer onset and offset than morphine Commonly used in opioid maintenance and detoxification programs
53
Oxycodone
Agonists** Similar to morphine in effectiveness of controlling pain and in the duration of its effect More effective as an oral drug than morphine (retains about 60-70% of its parenteral effect when given orally)
54
Butorphanol
Mixed Agonists/ Antagonists* Similar in action to pentazocine (weak mu antagonist/kappa agonist) Shows ceiling effect for its analgesic The side effects and signs of toxicity are similar to those produced by pentazocine
54
Pentazocine
Mixed agonists/Antagonists Pentazocine is contraindicated in patients with myocardial infarction because it increases heart rate and cardiac load. It is contraindicated in epileptic patients because it decreases seizure threshold
55
Hydrocodone
10 times weaker than morphine in effectiveness of controlling pain More effective as an oral drug than morphine (retains about 70-80% of its parenteral effect when given orally)
56
Buprenorphine
Mixed** Because of the reduced maximal effect of the drug on mu receptors it shows a ceiling effect for respiratory depression making it safer than morphine when over-dosed
57
Naloxone
Antagonists* Administered I.V. or with intranasal spray for overdose Naloxone will rapidly reverse the effects of opioid agonists and is used to treat respiratory depression caused by opioid overdose, as might occur when fentanyl is used during surgery for anesthesia or in the emergency room when a patient is suspected to be comatose from heroin overdose Rapid onset and short duration of action. *Re-administration may be necessary in cases of opioid over-dose until the opioid agonist has been cleared from the body First-pass metabolism is so extensive that naloxone is essentially inert when taken orally (used to advantage in Suboxone® (buprenorphine/naloxone combination drug)
58
Nalmefene
A long acting, injectable, pure opioid antagonist. The half-life of 11 hours is about 5 times that of naloxone. *This means that re-administration during treatment of opioid over-dose is less necessary compared with naloxone but provides less flexibility in treatment options Indications for the drug include use in post-operative settings to reverse respiratory depression and use in opioid overdose
59
Naltrexone
Antagonists* Has a very long duration of action (48-72 hours) Oral administration is effective and is used for opioid abstinence programs
60
Methadone
Long acting Mu receptor agonist Used to replace a short-acting I.V. drug like heroin with a slow, orally-acting drug. Once substituted, the dose of methadone is decreased until the patient can dispense with it entirely
61
Buprenorphine + Naloxone
Combination of mixed opioid receptor agonist plus an orally-inert antagonist As with methadone, used to replace abused opioids in a dependent individual
62
Naltrexone
Long-lasting opioid receptor antagonist Oral or long acting depo-injection

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