Term
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Definition
| results from injury to tissues: somatic and visceral |
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Term
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Definition
| results from injury to peripheral nerves |
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Term
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Definition
results from injury to tissues - bones joints, muscles
localized and sharp in quality |
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Term
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Definition
| results form injury to visceral organs - vaguely localized with a diffuse aching quality |
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Term
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Definition
| opium poppy; resin from the poppy is collected and processed into opium |
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Term
| general affect of opioids on pain |
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Definition
-most efficacious drug at blocking transmission of pain
-no effect on inflammatory processes
-all decrease respiratory rate, even at therapeutic levels
-elevate mood, covering the emotional aspect of pain |
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Term
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Definition
1. morphine: chiefly responsible for pharmacological actions of opium
2. codeine: methylmorphine, weaker actions
3. thebain: no analgesic activity, provides synthetic route for hydroxylated opioids |
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Term
| opioid molecular structure |
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Definition
1. 3 spots for attachment
2. changing the methyl group on the N can get rid of analgesic power
3. attached to C3 or C6 reduce analgesic activity
4. CH3 group attached to C3 will decrease first pass metabolism in GI tract when taken orally |
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Term
| codeine molecular structure |
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Definition
| methoxy group on C3 - can be taken orally |
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Term
| thebaine molecular structure |
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Definition
| 2 methoxy groups (on C3 and C6), no therapeutic activity |
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Term
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Definition
1. treatment of opioid toxicity, especially respiratory depression; small doses IM or IV promptly reverse effects of μ-opioid agonists; induces withdrawal syndrome
2. used in diagnosis of physical dependence on opioids - withdrawal symptoms begin in 2 mins and subside in 2 hours |
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Term
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Definition
A: absorbed well IM, SC, and oral and nasal mucosa
D: rapid from blood into highly perfused tissues, less to brain bc of BBB
M: first pass in liver inactivates many opioids (undergoes conversion to polar entity)
E: polar metabolites excreted in urine |
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Term
| Actions of morphine on CNS |
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Definition
MERMAN C
miosis
euphoria
respiratory depression
mood altering/rewarding properties
analgesia
nausea/vomiting
cough suppression |
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Term
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Definition
-relief of moderate to severe acute pain
-continuous dull pain is relieved more effectively than sharp intermittent pain
-in patients suffering from pain, induces a feeling of well being and tranquility (euphoria) |
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Term
| morphine and dyspnea associated with LVF and pulmonary edema |
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Definition
depresses respiration, which is difficult and painful
reduces urge to suck in more air - reduces rate and depth of breathing |
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Term
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Definition
due to excitation of the parasympathetic nerve innervating the pupil
->pathognomonic of opioid use (can use to check if patient is using meds) |
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Term
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Definition
-depresses respiration due to decreased sensitivity of brain stem to increases in Pco2 and H+ (dec. chemical sensory drive)
-main stimulus for breathing becomes hypoxia
-effect increased by concurrent use of other CNS -active drugs (alcohol, barbiturates, benzodiazepines)
-voluntary breathing not blocked |
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Term
| mechanism of increased intracranial pressure |
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Definition
| dec. respiration -> inc. pCO2 -> arteriolar dilatation ->inc. CSF pressure |
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Term
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Definition
suppressess cough reflex that originates in the medulla oblongata
morphine molecule can be modified to select for just this property - dextromethorphan |
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Term
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Definition
cough suppressant
-no analgesic or addictive properties
-acts centrally to increase threshold for coughing with no drowsiness or GI disturbances
-does not act through opioid receptors |
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Term
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Definition
stimulates the CTZ (chemosensitive trigger zone) in the medulla to cause nausea and vomiting
-only feel nausea when lying down - vestibular component? |
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Term
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Definition
-blunts baroreceptor reflex
-causes peripheral arteriolar and venous dilatation (partly from morphine-induced release of histamine)
-orthostatic hypotension and fainting |
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Term
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Definition
-decreases propulsive peristalsis, leading to constipation
-suppresses awareness of bowel stimuli
-tone of anal sphincter is increased |
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Term
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Definition
-causes urinary hesitancy and urgency - increased tone of bladder smooth muscle (detrusor) and of sphincter muscle - muscles contracting against each other
-suppresses awareness of bladder stimuli |
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Term
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Definition
can cause spasm of lower end of the common bile duct (sphincter of Oddi), causing increased pressure within the biliary tract
-morphine can intensify pain in patients with pre-existing biliary colic so know cause of pain before administration |
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Term
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Definition
develops to analgesia and respiratory depression, but not to constipation and pupillary miosis
patient will need higher doses
relapses in abusive drug use can die from respiratory effects - no longer tolerant but take dose they took while using |
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Term
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Definition
triad of signs:
1. coma
2. pinpoint pupils
3. depressed respiration |
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Term
| treatment of opioid poisoning |
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Definition
-maintain patent airway and ventilate
-treat with antagonist to reverse CNS effects - naloxone (pure antagonist) |
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Term
| morphine receptor mechanism of action |
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Definition
-morphine binds to a specific receptor
-binding is stereospecific and involves 3 binding sites
-regions of highest binding are associated with the limbic system, cortex, and brainstem
-opiate receptors are concentrated within pain and reward pathways
-work both presynaptically and postsynaptically
-receptors are G-protein coupled and activation reduces Ca++ influx during AP, leading to less neurotransmitter release from nociceptive primary afferents |
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Term
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Definition
1. spinal and supraspinal analgesia
2. miosis
3. respiratory depression
4. sedation
5. euphoria
6. physical dependence
7. dec. GI motility
8. hyperpolarize second-order neurons by inc. K+ conductance (IPSP) |
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Term
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Definition
1. spinal analgesia
2. miosis (less intense than μ)
3. respiratory depression (less intense than μ)
4. sedation
5. dysphoria |
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Term
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Definition
1. much less is known
2. main barrier to clinical utility is that most of the δ-receptor agonists are peptides and do not cross the BBB |
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Term
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Definition
endogenous pain suppressing system
1. enkephalins
2. endorphins
3. dynorphins |
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Term
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Definition
-biologically inactive
-converted to MAM (monoacetylmorphine) in the body and then into morphine
-MAM and morphine are responsible for the effects |
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Term
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Definition
μ-agonist with morphine-like activity
prolonged use gives rise to tolerance
-used for relieve of chronic pain and treatment of opioid abstinence and dependence
-oral efficacy |
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Term
| opioid withdrawal syndrome (hours after missing dose) |
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Definition
-intense fear (can be alleviated with placebo)
-8-16 hrs: lacrimation, rhinorrhea, yawning, sweating, mydriasis, anorexia, nervousness, irritability, tremors, anxiety, fear, restless sleep (sympathetic activity) |
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Term
| opioid withdrawal syndrome within 36 hours |
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Definition
1. severe muscle fasciculation and twitch
2. severe cramps in legs and stomach
3. uncontrolled vomiting, salivation, diarrhea, and urination
4. weakness, depression, chills/sweating, gooseflesh, muscle spasms, kicking movements
5. unable to sleep, inc. respiratory rate, inc. blood pressure, inc. temp, inc. blood sugar, inc. basal metabolic rate |
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Term
| length of opioid withdrawal syndrome |
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Definition
| peaks within 48-72 hours and subsides over the next 10 days |
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Term
| intensity of withdrawal syndrome |
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Definition
1. half-life of drug: short - intense but brief, long - prolonged but less intense
2. degree of physical dependence
3. methadone, meperidine, codeine qualitatively the same but less intense than morphine withdrawal |
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Term
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Definition
μ-agonist, actions similar to morphine
decreased constipation and urinary retention problems |
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Term
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Definition
-large, repeated doses can lead to excitatory syndrome: hallucinations, tremors, muscle twitches, dilated pupils, hyperreflexia, convulsions - due to accumulation of normeperidine
-half-life of normeperidine is 20 hrs while meperidine is 3
-not drug of choice for prolonged pain |
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Term
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Definition
μ-agonist, 80x more potent than morphine as an analgesic
for anesthesia and post-op analgesia, duragesic (transdermal patch) releases fentanyl over 72 hours, PCA |
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Term
| mild-to-moderate agonists |
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Definition
1. codeine
2. oxycodone (oxycontin)
3. hydrocodone (vicodin)
*methoxy group results in oral availability
*bind poorly to μ-receptor |
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Term
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Definition
-analgesic efficacy due to conversion to morphine - polymorphisms in cytochrome P450 isoform CYP2D6 can affect metabolism
-dispensed alone or in combination with aspirin or acetaminophen |
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Term
| codeine and gene polymorphisms |
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Definition
can be rapid or slow metabolizers
-use caution with pregnant and breastfeeding women - mother or child could be fast metabolizer (morphine poisoning)
-poor metabolizers - caucasians 7%
-rapid metabolizers - saudi arabia 20%, ethiopia 29% |
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Term
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Definition
-rapid, progressive, and profound sensorineural hearing loss in patients taking vicodin
-can be successfully rehabilitated with cochlear implants |
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Term
| agonist-antagonist opioids |
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Definition
-substances that appear to be agonists at some receptors but antagonists at others
-pentazocine, butorphanol
-partial agonist: buprenorphine |
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Term
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Definition
-weak μ-antagonist
-κ-agonist: responsible for analgesic activity
-actions similar to morphine-like opioids with respect to analgesia, sedation, respiratory depression
-because of antagonist activity, increased doses do not cause proportionate depression of respiration
-high doses increase BP and HR
-may precipitate withdrawal in μ-opioid dependent patient |
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Term
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Definition
(50mg Talwin +0.5mg naloxone)
-oral pentazocine laced with naloxone to prevent abuse potential through injection
-naloxone is degraded in liver, but if pill is powdered and injected it will produce withdrawal |
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Term
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Definition
-more potent than morphine (per weight)
-lowest abuse potential
-actions similar to pentazocine
-increases pulmonary arterial BP, increasing work of heart (watch with CHF and MI) |
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Term
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Definition
-highly lipophilic opioid derivative of thebaine
-partial μ-agonist, 25-50x more potent than morphine
-duration of analgesia longer than morphine
-maintenance drug for opioid-dependent subjects
-used as analgesic |
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Term
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Definition
| used in long-term management of opioid addiction - the long duration (24 hrs) of action serves as a safety valve after detox for patients with high motivation to remain opioid free |
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