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Neuro 3 > Opioid Analgesics > Flashcards

Opioid Analgesics Flashcards

1
Q

Opitate
Synthetics
Endogenous

A

Opiate - derived from poppy plants…morphine and codeine

Synthetic - fentanyl and oxycodone

Endo - endorphin, enkephalin, dynorphin

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2
Q

Narcotics

A

Originally associated with drugs that induce sleep…now think opioids

Legally associated with any that have abuse potentil

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3
Q

Partial agonist
Mixed agonist
Inverse agonist

A

Exerts effect less than full

Agonist ojn some and antagonist on other

Binds receptor and opposite effect of agonist

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4
Q

POtency vs. efficacy

A

[] needed to acheive half maximumu effect

Amount of effect exerted

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5
Q

Opioid receptors

A

Localized to synapses
Promote release of endogenous opioids
Gi/o protein coupled (reduce neuronal activity)

decrease cAMP (alpha)
Increase K current and decrease Ca influx (beta and gamma)
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6
Q

Types of opioid receptors

A

Mu and kappa - midbrain periaqueductal grau
Gamma - amygdala

Mu is the most common

All three play a role in anagesia

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7
Q

Endogenous expression

A

Pre-pro

endorphins - POMC cleaved to ACTH and B-LPH…B-LPH cleaved to hamma-LPH and B-endorphin

Enkephalins - preproenkephalin cleaved to leu and met enkephalin

Dynorphins - preprodynorphin to dynorphin A, B or Beta neoendorphin

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8
Q

Dynorphins different because

A

Dynorphin A may be involved in spinal cord dorsal horn pain sensation (hyperalgesia)

May be unqiue human

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9
Q

Opioid levels

A 
Periphery
Spinal level (Dorsal horn)
Supraspinal (NRPG and PAG)...these both inhibit dorsal horn
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10
Q

Phenanthrenes

A

Morphine
Codeine
Hydrocodone
Oxycodone

More pheanthrenes arrive COD

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11
Q

Phenypiperidines

A 
Meperidine
Fentanyl
Alfentanil
Sufentanil
Remifentanil

Me feal sure about phenylpiperadines

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12
Q

Phenylhepatanone

A

Methadone alone

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13
Q

If can’t tolerate side ffects

A

Switch to a different class of opioid

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14
Q

Morphine peripheral

A

Analgesia
Constipation
GI spasm

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15
Q

Morphine centrAL

A 
Analgesia
Resp depression
Antitussive
Misosis
Tolerance and dependance
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16
Q

Morphine effectiveness, selectivity, how to administer, divisions, and what type of pain best for

A

Many are as effective, none more

Other sensory modalities are preserved

Best achived by titrating to patient (2/3 adequate with 10mg IM)

Sensory discriminative - ID and localization of pain source
Motivational-affective - subjective reactions

Beetter against continous, dull pian

17
Q

Antitussive, pruritis effects of morhine

A

Suppresses brainstem cough centers…close to breathing centers but not same…occurs at subanalgesic/resp depressing dose

Peripheral mast cell and leukocyte stimulateh istamine reelease

18
Q

Truncal rgidity and N/V with morphine

A

Interferes with ventiilaiton (surgically concomitant NM blocking agents…in overdose, mechanial ventilaiton may be ineffective)

INitally, Stimulate CTZ (worse in ambulatory or oral dosage)

With prolonged high dose could supress BS medullay vomiting center

19
Q

Analgesic, renal, GI, biliary, CV effect of morhpine

A

Efficacy increased with inflammation
Reduced function
Increase smooth muscle tone and decrease propulsion…could lead to spasm that can increase pain
Decrease secretions
Decrease BP (due to histamine release)…can cause orthostatic hypotension
Can be used to treat pulmonary edema

20
Q

Genetics of morhpine

A

People with AA report less pain than GG

21
Q

Absorpition fate and excretion of morphine

A

Not as effective orally
55% as excitotixc mirphine-3-glucuronide
10% as analgesic morphine-6-glucuroine
Metabolites build up in blood over long term exposure

Nearly all excreted in usrine within 24 hours

3-4 half life with enterohepatic recycling

22
Q

Acute toxoicty of morphine

A

Death from profound resp depression (worry about with sleep apnea)

Miosis, decreased respiration, coma

Tx - restore airway physicially or with opioid antagonist (be careful with half life0

23
Q

Tolerance, dep ,and addiction of morhpine

A

Dose and freq dependent (begin at about 1 week and clinically after 2-3)

Dep - only evident when drug withdrawn…drug and drug class selective….neuronal modifications

Addiction - continud use, impaired ocntrol, craving despite harm

24
Q

Morhpine contraindications

A

Mixing any other opioid and with MAO-I (esp meperidine)

25
Q

Cautions of morphine

A

Head injuries…can increase pressure
Pregnancy
Impaired function of pulomanry system, renal system, and hepatic

26
Q

Drug interactions of morphine

A

Sedative hypnotics increase resp depression

Antipsychotic tranquilizers increased sedation

27
Q

Codeine use and cuation

A

Oral analgesic and antitussive

Chemical mod improves 1st pass survivability to 60% via CYP2D6 metab…prodrug metabolized to morphine

BLACK BOX warning for post op pediatric

28
Q

Oxy and hydrocodone origin, use, chemical mod, potency, oxy contin

A

From opium poppy

Oral admin in combination with others

Improves 1st pass survivability

Oxy=hydro»»morphine=codeine

oxycontin - controlled released but higher abuse

29
Q

Meperidine

A

Completely synthetic but structurally dissimilar

Similar to morphine in what it does but 1/10 potency

Used in labor and delivery

Reduced biliary spasms and no misosi

Seizures, termos, convulsions are unique due to normeperidine metabolite (esp renal impaired)

30
Q

Methadone

A

Equipotnet with morphine

Dissimilar

Repeated dosage causes longer lasting effects

Does NOT block opioid actions (full agonist)…also some NMDA antagonist

Considered high risk

31
Q

Fentanyl family

A

Super high potency with a short duration

Repeated do not accummulate and recovery rapid

Highly lipophilic so lollipop good for breakthrough

Used as IV analgesic and balanced anesthesia…use with muscle relaxers

32
Q

Opioid antagoniss

A

Prevent constipiation
Reverse acute opioid toxicity (non-opioid resp depression NOT recovered)
Naltrexone - 48-72 hour, oral, used for addicts
Naloxone - 1-4 hour, NOT oral

33
Q

Suboxone buprenorphine and naloxone

A

Addict maintenance

“Mixed” opioid agents

34
Q

Tramadol

A

5HT release, NE reuptake inhibitor, and weak mu agonist…MOA for analgesia is mu receptor independent

Metabolite stornger mu agonist

Seizures but not resp

35
Q

Tapentadol

A

Moderate mu agonist and NE reuptake inhibitor

36
Q

Key things about codeine and semi syntehtics

A

Pro drug with better bioavailability…metab to morphine

Popular

37
Q

Meperidine, methadone, fentanyl key points

A

Toxicity is CNS, not resp
Equipotent to morphine but better bioavail and can be dosed daily
More potent, lipophilic, and short acting

38
Q

Opioid antagonists and other agents inmportant

A

Recerve intoxication (naltrexone oral but naloxone not)

Others like tramadol and tapentadol have actions on multiple NT system

Neuro 3 (31 decks)

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