Term
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Definition
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Term
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Definition
mu agonist
USE: -Mild pain relief
KINET: -Much less 1st pass metabolism than morphine |
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Definition
mu agonist
KINET: -100X potency of Morphine |
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Definition
mu agonist
USE: Abuse
NOTES: -Schedule 1 Drug (no medical use allowed) |
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Definition
mu agonist
USE: -most widely used opioid
NOTES: -component of Vicadin (also contains Acetominophen) and loritab |
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Definition
mu agonist
USE: -similar to morphine |
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Definition
mu agonist
NOTES: -Rarely used |
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Definition
mu agonist
USE: -Tx of heroin withdrawal, chronic severe pain |
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Definition
mu agonist
USE: -chronic Tx of severe pain
NOTES: -"percocet" OxyContin (slow release, widely abused; "hillbilly heroin") |
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Definition
mu agonist
NOTES: -low abuse potential, not much better than placebo |
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Definition
mu partial agonist (agonist/antagonist) -- Stronger KAPPA agonist ;. decreased pain
USE: Tx of moderate pain
NOTES: Stimulates kappa receptor. Less abuse potential because it stimulates mu recptors less |
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Definition
partial mu agonist (agonist/antagonist)
USE: Tx of moderate pain & Tx of opioid addiction
NOTES: -highly used right now. Enough Mu agonist activity to prevent withdrawal effects |
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Definition
mu partial agonist (agonist/antagonist)
USE: -moderate pain |
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Definition
mu partial agonist (agonist/antagonist)
USE: -moderate pain
MECH: -partial mu agonsist, NT-RI activity (similar to antidepressant activity)
NOTES: -Newer drug |
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Definition
mu antagonist
USE: Tx of opioid poisoning
MECH: Mu antagonist (No agonist activity)
KINET: Fast acting (IV admin) |
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Definition
mu antagonist
USE: Tx of addiction (poor results)
KINET: Longer acting oral admin |
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Definition
mu antagonist
USE: Prevents opioid-induced constipation
MECH: Quaternary opioid antagonist (;. no CNS activity)
NOTE: New drug |
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Term
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Definition
Antiepiletic Drug (old standard)
Mech: Inhibits voltage gated Na channels
Use: Monotherapy for Tonic/clonic Sz & Partial Sz
Kinetics: 90% plasma protein bound
-dose increases disproportionately increase the available amount of drug
-must monitor levels to ensure proper blood doses
-95% liver metabolism (CYP2C9, -2C10, -2C19)
SE: Gingival hyperplasia (20% PTs on long term therapy)
-Steven Johnson Syndrome (blistering of skin & mucous membranes) - not restricted to anticonvulsants
-severe for of SJS called Toxic epidermal necrosis
--Cease Tx if occurs! |
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Term
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Definition
Antiepiletic Drug (old)
-inhibits voltage gated Na channels
-also Tx of Neuropathic pain
Kinetics: -metabolism difficult to predict (like Phenytoin
SE: -Stupor coma hyperirritability & Increased |
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Term
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Definition
Antiepiletic Drug (old)
-Inhibits 'T-type calcium channels' (Absence Sz ONLY)
-Few drug drug interactions |
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Term
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Definition
Antiepiletic Drug (old)
USE: -Treats ALL types of Sz (including Absence)
-inhibits voltage gated Na channels, also...
-Inhibits 'T-type calcium channels'
SE: -Causes heptotoxicity |
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Term
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Definition
Antiepiletic Drug (old)
-Enhance GABA-A's inhibitory effects (post-synaptic)
-controls status epilepticus
--Used as ADJUNCTIVE Tx (Not monotherapy) |
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Term
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Definition
| Antiepiletic Drug (Benzodiazepine - old) |
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Term
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Definition
| Antiepiletic Drug (Benzodiazepine - old) |
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Term
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Definition
Antiepiletic Drug (New)
USE: -Tx of Partial Sz
-used in Tx of Neuropathic Pain
--Adjunctive Tx
MECH: -Mimics gaba shape, not action
KINET: Excreted unchanged in urine (:. Check urine function)
Factoid: - Whistleblower for off-label promotion |
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Definition
Antiepiletic Drug (New)
-inhibits voltage-gated Na channels |
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Term
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Definition
Antiepiletic Drug (New)
USE: -Mono or Adjunctive Tx for partial and general Tonic/Clonic
-Tx of LGS
MECH: -Slow recovery of voltage-gated Na channels (ie phenytoin)
-Inhibit some Ca channels
KINET: Alters other drugs' T1/2
- Long T1/2 (~24 hours)
SE: SJS (adjunctive Tx), Dizziness, Ataxia |
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Definition
Antiepiletic Drug (New)
-Also Tx of Bipolar Disorder |
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Definition
Ergot alkyloid/Act on 5-HT receptor
USE: -
MECH: -
KINET: Taken orally, sublingually, or by suppository
SE: - |
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Definition
Ergot alkyloid/Act on 5-HT receptor
USE: -
MECH: -
KINET: -
SE: - |
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Term
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Definition
Ergot alkyloid/Act on 5-HT receptor
USE: -
MECH: -
KINET: -
SE: - |
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Term
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Definition
| 5-HT (1B/1D) Agonist USE: - MECH: - KINET: - SE: - |
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Term
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Definition
5-HT (1B/1D) Agonist
USE: -
MECH: -
KINET: -
SE: - |
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Term
| "-triptan" refers to which drugs? |
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Definition
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Term
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Definition
Dopmine ANTagonist (Antiemetic)
USE: -
MECH: -
KINET: -
SE: - |
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Term
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Definition
Dopmine ANTagonist (Antiemetic)
USE: -
MECH: -
KINET: -
SE: - |
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Term
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Definition
Analgesic (acetominophen + steroid + synpathomimetic)
USE: Tx of migraines (1st line)
MECH: - multiple, includes vasoconstriction
KINET: - 1/hr, up to 6/day
SE: - Very few |
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Term
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Definition
USE: -
MECH: -
KINET: -
SE: - |
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Term
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Definition
Antidepressant
USE: -
MECH: -
KINET: -
SE: - |
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Term
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Definition
Antiseizure Drug
USE: -
MECH: -
KINET: -
SE: - |
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Term
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Definition
Antiseizure Drug
USE: - Migraine prophylaxis
MECH: -
KINET: -
SE: - |
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Term
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Definition
Antiseizure Drug
USE: -
MECH: -
KINET: -
SE: - |
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Term
| What effect does mu receptor signaling produce? |
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Definition
Strong analgesia
Abuse potential
respiratory depression |
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Term
Mu Opioid Receptor
(Location & Effects) |
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Definition
Brainstem, spinal, and limbic
EFFECTS: Limbic Effects, some spinal effects, Supraspinal effects, sedation, resp. depression, dependence |
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Term
Kappa Opioid Receptor
(Location & Effects) |
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Definition
Brainstem & Spinal
EFFECTS: Some spinal, some supraspinal, sedation, & Dysphoria |
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Term
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Definition
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Term
Endorphins & Enkephalins
-How do they trigger receptors? |
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Definition
| Structurally similar to Opioids |
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Term
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Definition
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Term
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Definition
| Use: Suppress acute attack of gout |
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Term
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Definition
| USE: Suppress acute attack of gout |
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Term
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Definition
| USE: Suppress acute attack of gout |
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Term
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Definition
| USE: Suppress acute attack of gout |
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Term
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Definition
| USE: Increase excretion of Uric Acid |
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Term
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Definition
| USE: Inhibit the formation of uric acid |
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Term
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Definition
| USE: Inhibit the formation of Uric Acid |
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Term
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Definition
USE: -Analgesia (acute - trauma & chronic - cancer)
-Sedation & mental clouding (not classic sedative effects)
---Easily aroused from "floating dream-like" sleep
---OD can lead to stupor, coma or death
-Antitussive Effects (ie codeine) however they can degranulate mast cells which is VERY BAD for asthmatics
-Adjunct to surgical anesthesia
-Antidiarrheal derivatives (Loparamide - immodium)
-Abuse
NOTE: Administered as infusion, PCA (gold standard for pain management), or spinal anesthesia admin |
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Term
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Definition
KINET: ~75% 1st pass metabolism if oral therefore usually parenteral administration (usually sustained release)
-*Standard dose: 10 mg subQ or IM* (lower amount when IV)
-Rapid onset of action, short duration (4-6hrs)
-Glucuronide metabolism
-Cross BBB & placental barrier (abuse affects fetus) |
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Term
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Definition
SE: -Euphoria (typically) via reward centers. Rarely dysphoria, affecting mainly females
-Nausea via CRTZ activation (sometimes treatable), which reduces w/ tolerence
---vestibular component of nausea may exist
-Respiratory depression (rate & depth) at therapeutic dose (may exacerbate resp. problems)
-Decreases sensitivity of chemo CO2 receptors (reduced drive to breath) ;. respiration is based solely on hypoxic response---;. can stop breathing if O2 is administered
-Constriction of pupils ("pin point pupils") - not affected by tolerance
-Antitussive Effects
-Histamine release causes itch over the skin (;. antihistamines (diphenhydramine) used to alleviate itch)
-Increased risk of seizures
-Chronic high dose - endocrine, and other effects
-Deceased bowel motility (constrict circular, relaxed longitudinal) = constipation;. laxatives (osmotic laxatives like miralax or milk of magnesia) may help
-urine retention (another smooth muscle effect) - may need to catheter for drainage
-Bronchoconstriction (via histamine effect, not mu receptor)
-Constriction of sphincter of oddi (decreased bile bladder contraction) - helps with pain, exacerbates cholistitis
-Cardiovascular effects (postural hypotension - histamine mediated)
-Cutaneous vasodilation (flushing) - Cold turkey skin with withdrawal
-increase ICP (hi CO2 --> vasodilation) ;. don't use with closed head injuries if avoidable
-Immunosuppression w/ chronic use (assumed to be effect of heroin early in Hx of AIDS) |
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Term
Morphine
(Miscelaneous Notes) |
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Definition
NOTES: -A Classic drug
-Rage attacks in cats
-Re Pulmonary Edema w/ MI: decreases anxiety which is exacerbating cardiopulm. problems
---also some vasodilation effects |
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Term
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Definition
Interactions:
-CNS depressants have additive effects
-cocaine/heroin + morphine = speedball (Belushi)
-Useful when given with painkillers of different types (ie - mu & COX effects)
-Increased analgesia when given with antihistamines
-Tricyclic antidepressants also enhance effects of opioids |
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Term
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Definition
Overdose: Opioid Antagonist - can't hurt the patient if wrongly diagnosed. ALso give respiratory support
Toxidrome: Stupor, bradypnea, Pin-point pupils
---fixed and dilated pupils indicate hypoxia and imminent death |
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