Flashcards in Leffler-1 Deck (24)
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1
Q
Non-opioid analgesics vs Opioid Analgesics
A
- Non-opioid Analgesics:
- act in:
- peripheral tissues (primarily)
- inhibit formation of pain producing substances
- prostaglandins
- inhibit formation of pain producing substances
- Act In the CNS:
- reduce prostaglandin production involved in temperature regulation
- Anti-inflammatory
- peripheral tissues (primarily)
- act in:
- Opioid Analgesics
- Acts primarily in the CNS (Spinal cord and brain)
- inhibit Neurotransmission of pain
2
Q
Opioids differs from NSAIDs:
A
Opioids:
- Significant:
- abuse potential
- tolerance, physical and psychological dependence
- First pass metabolism
- oral has less analgesic effect than parenteral doses
- Have to be injected
- abuse potential
- More powerful analgesic
- Lack anti-inflammatory and antipyretic effects
- Antipyretic (reduce fever)
- Site of action: CNS
3
Q
Opiate
A
- Drug derived from the alkaloids of the opium poppy
4
Q
Opioid
A
- Classs of drugs
- includes:
- opiates
- Opiopeptins
- all synthetic and semisnthetic drugs
- mimic action of opiates
5
Q
Opioid peptides
A
- Endogenous peptides that act on opioid receptors
6
Q
Narcotic
A
- Any psychoactive compound with sedative properties
- used in legal context to refer to substances with abuse or addictive potential
- applies to more than just opioids
7
Q
Endogenous Opioid Peptides
A
- 3 famillies of peptides:
- Enkephalins
- Endorphins
- Dynorphins
- Opioid receptors have overlapping affinities for these 3 peptides
- All implicated in pain modulation
- Analgesic role
- Released upon stressful stimuli and diminish sensation
- Dynorphin A
- may increase pain
- Pronociceptive action
8
Q
Source of Opium
A
- Poppy plant
9
Q
What is the principle alkaloid?
A
- Morphine
10
Q
Opioid Receptors
A
- Inhibitory G-coupled protein receptor (Gi)
- Limbic System
- 3 types:
- Mu
- Kappa
- Delta
- Binding site for endogenous ligans and opioid drugs
- all 3 coupled to adenylyl cyclase:
- inhibition=Inhibition of NT release
11
Q
Where are opioid receptors expressed?
A
-
Expressed in pain-modulating descending pathway
- Periaqueductal gray area
- Also expressed in limbic, midbrain, and cortical structures
12
Q
When opioid receptors are activated what happens?
A
- Direct inhibition of:
- neurons
- spinal cord pain transmission
13
Q
Opioid Receptors: Mechanism of Action
A
- Modulate Ca2+ and K+ ion channels
- actions can occur at the level of the:
- spinal cord (spinal analgesia)
- CNS (supraspinal analgesia)
- Net Result:
- Raise the threshold to pain
14
Q
Mu receptor:
A
- Function:
- Supra spinal and spinal analgesia
- sedation
- inhibition of respiration
- slowed GI transit (constipation)
- High affinity for Endorphins (primary opioid peptide)
- Primary receptor for opioid drugs
15
Q
Kappa receptor
A
- Function:
- psychotomimetic effects
16
Q
Delta Receptor
A
- Function:
- Supraspinal and spinal analgesai
17
Q
Physiological effects to receptor types:
- Mu Receptors
- Kappa Receptors
- Delt Receptors
A
- Mu Receptor:
- Analgesia
- Respiratory Depression
- Euphoria (pleasure, well-being, elation)
- Sedation
- Physical Dependence
- Slowed GI Transit (Constipation)
- Miosis
- Modulation of Hormone and NT release
- Kappa Receptor:
- Analgesia
- Dysphoria (unease, Dissatsifaction)
- Sedation (some to little)
- Slowed GI transit
- Miosis
- Psychomimetic effects
- Delta receptor:
- Modulation of Hormone and NT release
18
Q
Overall systemic effects of opioid receptor activation:
CNS vs Periphery
A
Some are desired effects, some are undesired
Overdose can lead to death
CNS:
- Analgesia
- Euphoria
- Sedation
- Respiratory depression
- Cough Suppresion
- Miosis
- Truncal rigidity
- Nausea and Vomiting
- Body temperature-reduce shivering
- May increase ICP
Periphery:
- Bradycardia
- Hypotension (in cardiovascular-stressed patients)
- Constipation
- Biliary colic (contraciton of biliary smooth muscles)
- Decreased renal function (or urinary retention)
- Prolong labor (reduce uterine tone)
- Stimulate release of ADH, prolactin, somatotropin and inhibit release of LH
- Pruritus (hives)
19
Q
Clinical uses for opioids
A
- Analgesia
- moderate to severe pain
- refractory pain
- Acute Pulmonary Edema
- relieves pain associated with dyspnea
- Cough Suppression
- Ciarrhea
- Shivering (Reduced by meperidine)
- Applications in Anesthesia
- Pre-op
- Intraoperativiely
- Anesthetic regimen
20
Q
Clinical Uses: Opioids for specific types of pain
A
- Postoperative pain
- effective in post-op
- can facilitate early movement (positive outcomes)
- Obstetric pain
- Monitor respiration in neonate
- can use naloxone if necessary
- Myocardial infarction
- Morphine=drug of choice
- Head Injury
- use with caution
- opioids can incrase ICP
- Cancer-related pain
- Patient should be given as much meds as need for analgesia
- Chronic Non-Cancer pain
21
Q
Tolerance
A
- compensatory changes in number and sensitivity of CNS receptors
- Need more of the drug to achieve the same effect
- time it takes-varies
22
Q
Minimal or no degree of tolerance to opioid effects
A
- Miosis
23
Q
Dependence
A
- Can develop dependence without addiction
- Occurs with the development of tolerance
-
physical dependence
- abstinence syndrome (withdrawal) will occur if drug is discontinued or antagonist if administered
- Once dependence develops, the desire to avoid withdrawal becomes motivator for continued drug use
24
Q
A