Analgesia (NO neuropathy) Antitussive (BUT NO COPD/ASTHMA (mucus) Antidiarrheal (CONSTIPATION)

Premedication for general anesthesia OR - general anesthetic adjunct - primary general anesthetic (no CV risk) - fentanyl Spine anesthesia - fentanyl+anesthetic (epidural)

Mostly MU RECEPTOR Constipation (no tolerance) N/V (Mu in CTZ + vestibular apparatus). = tx ondansetron Sedation = additive w/ other Rx miosis = (no tolerance, atropine) Pruritis = (NOT MU, from mast cell histamine) Respiratory depression - additive w/ other Rxs, delayed up to 12 hrs) urinary retention

Opioids Flashcards by O lawformonde

High efficacy agonist

Morphine
Meperidine
Methadone
Fentanyl

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Low/Medium efficacy ags

Codeine
Oxycodone
Hydrocodone

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Mixed Ags/Antags

Pentazocine

Buprenorphine

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Antags

Naloxone

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Non-analgesic opioid

Dextromethorphan

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Opiate

Term

Includes non-analgesics

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Opioids

Name

Include synth drugs, endogenous (enkephlins)

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Analgesic

Name

Pain-relieving

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Endogenous Opioid

Mu receptor

Binds

B-endorphin
Enkephalins

MOST OPIOID EFFECTS
*analgesia, Respiratory, euphoria, dependence

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Endogenous Opioids

Delta receptor

Binds

B-endorphins
enkephalins

Analgesia

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Endogenous Opioids

Kappa receptors

Binds
*dynorphins

Analgesia, sedation, endocrine

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Opioid Txs

Analgesia (NO neuropathy)
Antitussive (BUT NO COPD/ASTHMA (mucus)
Antidiarrheal (CONSTIPATION)

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Opioid

Analgesia effects

*threshold (discriminative)

ONLY IN OPIOIDS = *Tolerance (affective /emotion) = care less about pain
*ONLY PAIN = not temp, touch, proprioception (like LOCAL ANALGESICS)

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Opioid Analgesia

Sites

Peripheral = C fiber

Spinal = stop ASCENDING PAIN pathway

Supraspinal = activate DESCENDING PAIN INHIBITORY PATHWAY

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Major receptor for analgesic opioid fact

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Opioids

Uses

Premedication for general anesthesia

OR*
general anesthetic adjunct
primary general anesthetic (no CV risk) - fentanyl
Spine anesthesia*
fentanyl+anesthetic (epidural)

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Antitussive effects

Mediated by (receptor)

DM receptor

NOT OPIATE RECEPTOR

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L stereoisomer activates

Mu (opioid)
+
DM (Anti-tussive)

Natural opioids
Opiates

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D stereoisomer activates

UNNATURAL STEREOISOMER

DM (antitussive ) ONLY
NO MU S.E.

*dextromethorphan

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Opioid Anti-diarrheal effects

*Mu receptor

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Opioid antidiarrheal

S.E

Delayed gastric emptying - other oral Rx slowed

If no cross BBB, no CNS effects

No tolerance

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Opioid

General S.E.

Mostly MU RECEPTOR

Constipation (no tolerance)
N/V (Mu in CTZ + vestibular apparatus). = tx ondansetron
Sedation = additive w/ other Rx
miosis = (no tolerance, atropine)
Pruritis = (NOT MU, from mast cell histamine)
Respiratory depression - additive w/ other Rxs, delayed up to 12 hrs)
urinary retention

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pinpoint pupils
respiratory Depression
decreased consciousness

Opioid OD

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Opioid less common SE

Cardio

Study These Flashcards

Meperidine - TAC (anti-musc)

Most - bradycardia

Opioid tolerance SE change?

SE move with tolerance (except constipation + miosis) = T.I. DOESN'T change

Opioid dosing * Cut back when pt shows... * Switch when...

Lower dose = Higher respiratory effect Switch = SE untenable, equi-analgesia across Rxs

Pt needs analgesia, but is Opioid abuser

Give larger dose than Naive patient

Opioid drug interactions

SSRI + Meperidine = serotonin syndrome + Benzos/Barbituates/alcohol = Respiratory depression

Tx Acute severe pain

IV - morphine/fentanyl

Tx Chronic pain (cancer)

* Underlying pain = extended-release morphine * breakthrough pain = fast/short-acting (fentanyl lolipop, hydromorphone oral, Percocet (oxycodone), vicoden (hydrocodone)

Tx Nociceptive/inflammatory

Opioids

Tx Neuropathic pain

Opioids ADD Anticonvulsants

Change dose if patient :

* opioid dependent * Impaired GI motility * Hepatic/renal impairment * Oral rx ability

High first pass effect

Morphine | only 25% bioavailable

Low first pass effect

Methadone | Almost 100% available

Opioid Analgesia Use against this pain

GOOD **2nd (C fiber - slow) pain = dull/achy LESS**1st (Abeta - fast) pain = sharp, intense WORST **Neuropathic pain (ex. post-herpetic neuralgia)

Non-opioid receptors w/ opioid effects DM receptor

*antitussive effects

Descending pain inhibitory pathway

MOR activated in PAG --> Raphe nucleus --> enkephalin-containing neuron in spinal cord releases enkephalins -->inhibit substance P releasing C-fiber + Hyperpolarize ascending spinothalamic tracts

Morphine * absorption * duration * addiction-resistance * Metab? * SE

*High 1st pass *4-5 hours *slow-release = chronic pain *MS-Contin = crush resistant *metab = glucuronidation *SE= seizure (M3G metabolyte) =renal fail pt (M3G)= lower dose =histamine release = bronchoconstriction, HypoTN,

Hydromorphone *SE

* dilauded * no Histamine = NO bronchoconstriction/hypoTN/pruritis * M3G, NO M6G - So NO dose change w/ renal fail

Fentanyls * onset * forms * SE

* more lipophilic * Fast acting * Can't tolerate oral opioids? --> many forms * Poor cardio function but need surgery antalgesic? - IV fentanyl * No Histamine releases = NO pruritis, bronchoconstriction, hypoTN

Methadone * Uses * absorb * SE

* treat heroin addicts, analgesic * well absorbed in GI * long t 1/2 * non opoid receptor effects --> analgesia * no histamine * PROLONGED QT

Low-medium efficacy opiods * combos * contraindications

All oral NO WITH LIVER DZ Combine with aspirin (=dan) Combine w/ acetaminophen (=cet) *liver toxicity

Ultrametabolizer (CYP2D6) of codeine?

Use alternative: * buprenporphine * hydromorphine

Codeine * uses * SE

* converted by CYP 2D6 to moprhine * antitussive (bind direct to DM - no CYP conversion needed) * histamine release

Oxycodone * efficacy * Metab * slow release

* highest efficacy * CYP2D6 = metab to oxymorphone (NOT AFFECTED BY RECESSIVE CYP FORMS) * slow-release = Oxycontin

Hydrocodone * efficacy * metab * SE

* moderate efficacy * CYP2D6 to hydromorphone = NOT AFFECTED by RECESSIVE CYP FORMS * antitussive, pruritis * most prescribed

Kappa agonists Effects

* kappa agonist = analgesia | * partial/full mu agonist = anagonizes other mus

Misc Opioid Analgesics Buprenorphine * receptors * use * combo

*partial mu ag Kappa antag *sublingual * 1st line - opioid dependence (opioid receptor full-ag blockers) * combo = +naxolone (Suboxone)

Opioid antags Naloxone

*parenteral * Use - Opioid OD * short duration = give multiple doses to OD

Opioid Antags Naltrexone * Duration * use

Long-acting | *use - alcohol addiction + other addiction

Neuropathic pain Fibers

A-beta NOT C + A-delta

Amitriptyline Imipramine Desipiramine * mech * use

NE reuptake inhibitor *neuropathic pain ADDs

Diabetic neuropathy Tx

Carbamazepine | Pregabalin

Postherpetic neuralgia Tx?

Gabapentin | Pregabalin

TX pain 1) Mild pain

Aspirin NSAIDS Acetaminophen

TX Pain 2) Moderate pain

+ low/medium efficacy opioids NEW GUIDELINES CDC = start w/ atypical opioids + lifestyle change

TX pain 3). Severe pain

High efficiacy opioids

Dextromethrophan * receptor * SE

* DM receptor * less addiction = no MU effects Antitussives

Opioids Flashcards

(59 cards)