Term
| adverse effects of opioids |
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Definition
respiratory depression
miosis
constipation
urinary retention
nausea, vomiting
mental clouding
possible dysphoria
physical dependence
CNS depression
pruritis for some
euphoria
sedation |
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Term
| absorption and distribution of opioids |
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Definition
Absorbed readily, significant first-pass effect, delays oral absorption of other drugs by decrease acid and decrease gastric emptying
Distributes rapidly, onset and duration is influenced by each drug's lipophilicity (low - slower onset, longer duration; high - rapid onset, short duration) |
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Term
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Definition
Class: analgesic, opioid, schedule II
Mechanism: agonist at mu opioid receptor, some effect at delta and kappa
Indication: analgesia, suppression of cough
Contraindication: chronic kidney disease, neonates (not full metabolism capabilities)
Adverse effects: nausea, vomiting, histamine release (hypotension and pruritis), respiratory depression, constipation, potential for abuse
Absorption: many routes and formulations, extended release forms
Distribution: hydrophilic --> slow onset of action, longer duration
Metabolism: high first pass, glucuronide, active metabolites as analgesisc (M6G) or toxic (M3G) |
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Term
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Definition
Class: analgesic, opioid
aka Dilaudid
Mechanism: agonist at mu receptor, some effects at delta and kappa
Indications: moderate to severe pain
Adverse Effects: similar to morphine but less histamine release and no opioid-active metabolites (preferred in patients with renal impairment of hemodynamic instability) |
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Term
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Definition
Class: analgesic, opioid
Mechanism: agonist at mu receptor, some effects at delta, more potent than morphine
Indications: analgesia; popular for postoperative or labor analgesia, chronic pain, anesthetic adjuvant
Adverse effects: respiratory depression, constipation, potential for abuse
Absorption: transdermal patch and others
Distribution: very lipid s
oluble, easily passes through skin and mucus, fast onset, short duration |
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Term
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Definition
Class: analgesics, opioids
Mechanism: mu receptor agonist, rapid onset 1-5min after IV, ester linkage, susceptible to plasma esterases, short half-life 5min
Indications: moderate to severe pain; adjunct to general anesthesia
Adverse effects: respiratory depression |
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Term
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Definition
Class: analgesics, opiods
Mechanism: mu agonist, some effects at delta and kappa; inhibit NE and 5HT transporters
Indications: ~pain declining usage; often in labor b/c does not decrease force of uterine contractions
Adverse effects: respiratory depression, constipation, abuse potential, negative inotropic on heart, antimuscarinic effects, tachycardia, potential for seizures, serotonin syndrome
Metabolism: to normeperidine which has significant antimuscarinic effects (dilate pupils) and assoc with seizures |
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Term
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Definition
Class: analgesics, opiods
Mechanism: AGONIST at kappa opioid receptor, ANTAGONIST at mu
Indications: moderate to severe pain, preoperative medication and supplement for pain relief
Adverse effects: limited respiratory depression, increased heart rate and BP at high doses, DYSPHORIA due to kappa action
[when combined with naloxone, decreases use as injectable, naloxone metabolized when taken orally] |
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Term
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Definition
Class: analgesics, opioid
Mechanism: pro-drug, metabolized to morphine, agonist at mu receptor, some action at delta and kappa, less effect than morphine
Indications: mild-moderate pain, esp. combined with aspirin or acetaminophen; antitussive, antidiarrheal
Adverse effects: constipation, respiratory depression RARE
Metabolism: high first pass, 50-70% to codeine6glucuronide, 0-15% to morphine by CYP2D6 |
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Term
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Definition
Class: analgesics, opiod
Mechanism: mu agonist
Indications: mild to moderate pain
Adverse effects: constipation, respiratory depression, potential for abuse
Absorption: available with acetaminophen and ibuprofen; extended release w/ more drug/pill - abuse issues, reformulated in 2010 to be non-crushable |
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Term
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Definition
Class: analgesics, opioid
Mechanism: mild to moderate pain; antitussive
Adverse effects: constipation, respiratory depression, abuse potential, hepatic toxicity when combined with acetaminophen
Absorption: until 2014 always formulated with another drug (NSAID) |
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Term
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Definition
Class: opioid antagonist
Mechanism: antagonize opioid action, given IV due to large first pass effect, short duration of action 1-2h
Indication: acute opioid overdose (esp. respiratory depressed)
Adverse effects: relapse due to short duration of action, much higher doses needed for buprenorphine reversal due to slow dissociation
Absorption: formulated with buprenorphine and pentazocine to prevent abuse, auto-injectory approved in 2014 |
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Term
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Definition
Class: opioid antagonist
Mechanism: antagonize opioid action, long duration
Indication: decrease cravings for alcohol in chronic alcoholics
Absorption: very well, 10hr duration |
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Term
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Definition
Class: analgesic, opioid
Mechanism: agonist at mu receptor
Indication: mild to moderate pain, often after dental surgery
Adverse effects: FATAL HEART ARRHYTHMIAS AT THERAPEUTIC DOSES; constipation, respiratory depression, etc. |
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Term
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Definition
coma
pinpoint pupils
respiratory depression
TX: establish airway and ventilate, naloxone (trigger withdrawal, eventual rebound) |
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Term
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Definition
Inc. vigilance: hepatic disease (bioavailability), impaired renal fx (accumulation of active metabolites), compromised resp. fx (potential depression of), asthma (histamine-induced bronchoconstriction)
Totally: Pregnant and post-partum (may cross placenta and milk), Neonates and very young children (metabolic differences), Geriatric (drowsy, confusion, delirium, inc risk of falls, they take lots of meds - interactions) |
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Term
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Definition
sedative-hypnotics - increase CNS depression
antipsychotics tranquilizers - increase sedation, accentuate CV effects
MAO-I - hyperpyrixic coma |
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Term
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Definition
Class: "analgesic"
Mechanism: pro-drug, metabolized to morphine, very lipid soluble
Effects: warmth, taste, high or intense pleasure, period of sedation and tranquility
Indication: none
Half-life: 3min |
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Term
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Definition
gradual loss in effectiveness (days-to-weeks process)
larger dose required to produce same effect
parallel shift to right in dose-response curve
does NOT predict addiction
to: euphoria, analgesia, sedation, resp. depression, N/V
not to: miosis, constipation
cross-tolerance to other opioid agonists (partial or incomplete) |
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Term
| opioid physical dependence |
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Definition
withdrawal upon discontinuation does NOT predict addiction,
antagonist can precipitate |
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Term
| opioid psychological dependence |
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Definition
euphoria, indifference to stimuli, sedation
proclivity to return to drug use even after acute withdrawal has abated
DA pathways in the nucleus accumbens involved in mediating opioid-induced reward |
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Term
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Definition
pupillary dilation
sweating
piloerection (gooseflesh)
vomit, diarrhea
increased BP
yawning
fever |
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Term
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Definition
maladaptive use leading to significant impairment and distress
fundamental element is drug-seeking behavior
longer use --> inc. likelihood of tolerance and dependence --> inc. likelihood of addiction |
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Term
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Definition
Class: analgesic, opioid
Mechanism: mu agonist, racemic mixture blocks NMDA receptors and monoamine reuptake transporters, binds extravascularly and slowly released back into plasma (24hr half-life)
Indication: difficult to treat pain (neuropathic, cancer), opioid dependence (lessens highs and lows of withdrawal, cross tolerance to heroin, dec. addiction-reinforcing effects, dec. drive to obtain illegally)
Adverse effects: respiratory depression, prolonged QT interval (arrhythmias), 1/3rd of all prescription opioid-related deaths (overestimation of tolerance and polysubstance abuse) |
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Term
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Definition
Class: analgesic, opioid
Mechanism: partial agonist at mu, antagonist at kappa, long duration due to slow dissociation
Indication: especially difficult to treat pain (neuropathic, cancer); opioid dependence (as effective as methaone)
Adverse effects: limited respiratory depression and constipation; resistant to naloxone reversal (due to b's slow dissociation)
Absorption: formulated with naloxone, proper use as sublingual- b better absorbed and n not; injected naloxone absorbed and precipitates withdrawal instead of high |
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Term
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Definition
Class: opioid, non-analgesic
Mechanism:
Indications: diarrhea
Absorption: low solubility, limited use for parenteral injection; combined with low-dose atrophine to lessen risk of abuse |
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Term
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Definition
Class: opioid, non-analgesic
Mechanism:
Indication: diarrhea
Absorption: limited and access to brain is low so less abuse potential; available w/o perscription |
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Term
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Definition
Class: analgesic, non-opioid
Mechanism: orally active with lots of metabolites, weak mu agonist, inhibits NE and 5HT reuptake, activates alpha receptors
Indications: mild-moderate pain, modulate emotional aspects of pain
Adverse effects: assoc. w/ seizuires, risk of serotonin syndrome w/ MAOIs SSRIs or TCAs, assoc. w/ inc. risk of suicide
Positives: low risk of respiratory depression, constipation or abuse |
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Term
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Definition
Class: analgesic, non-opioid
Mechanism: inhibit 5HT and NE reuptake, dirty drugs (inhibit muscarinic, histamine, alpha1 receptors)
Indication: depression, NEUROPATHIC PAIN, adjuvant for INFLAMMATORY PAIN, anxiety disorders
Contraindications: coadmin w/MAOIs
Adverse effects: anticholinergic effects, sedation from H1 block, orthostatic hypotension from alpha1 block, CV toxicities, potential suicidal thoughts/behavior in children/young adults |
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Term
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Definition
Class: analgesic, non-opioid
Mechanism: inhibit 5HT and NE reuptake
Indication: depression, NEUROPATHIC PAIN, anxiety disorders
Adverse effects: potential for suicidal thoughts/behaviors in children/young adults; increase BP, serotonin syndrome, hepatitis |
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Term
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Definition
Class: analgesic, anticonvulsant
Mechanism: bind voltage-gated calcium channels in CNS to inhibit NT release
Indications: NEUROPATHIC PAIN, FIBROMYALGIA, epilepsy
Adverse effects: minor |
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Term
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Definition
Class: analgesics
Mechanism: decrease sodium channel activity, decrease calcium channel currents; increase GABA activity to decrease AP propagation and cellular excitability
Indications: epilepsy, NEUROPATHIC PAIN
Adverse effects: varied and drug-dependent |
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Term
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Definition
Class: analgesic, non-opioid
Mechanism: blocks N-type Ca++ channels thus block neurotransmitter release
Indication: severe chronic pain refractory to other therapies
Adverse effects: psychosis, cognitive impairment, hallucinations, changes in mood or consciousness, nausea |
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