opiates nsaids benzos 2016

8/19/2019 Opiates NSAIDs Benzos 2016

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Analgesics & MuscleRelaxants:

Primum non nocere Kenneth McCall, BSPharm, PharmD

Associate Professor

UNE College of Pharmacy


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ObjectiesClassify o!ioi"s base" #!on agonist, !artial

agonist, or antagonist rece!tor e$ects%

Classify ben&o"ia&e!ines base" #!on theirhalf'life an" "#ration of action%

Classify NSA(Ds accor"ing to theircycloo)ygenase selectiity%

("entify the DEA sche"#le for a gien "r#g% *ecogni&e the !harmacologic e$ects of

o!ioi"s, ben&o"ia&e!ines, non'ben&o m#sclerela)ants, an" NSA(Ds%


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Outline: The Duality of Analgesics O!ioi"s

Ben&o"ia&e!ines

Non'ben&o M#scle *ela)ants NSA(Ds


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O!ioi"s in Nat#reO!i#m Po!!y

En"or!hins

Decrease a!!etiteDecrease stress

*e"#ce !ain

Ma+e yo# ha!!y


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Classication of O!ioi"sAgonists

Mor!hine, co"eine, hy"roco"one , metha"one,me!eri"ine, fentanyl, o)yco"one

Partial agonistsB#!renor!hine -reach a !late#., !enta&ocine

Antagonists

Nalo)one -reerse oer"ose from an o!ioi"s.,naltre)one


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PharmacologyAgonist / "r#gs that occ#!y a rece!tor an" actiate themAntagonist / "r#gs that occ#!y a rece!tor an" bloc+ rece!tor

actiation%

Agonist alone Antagonist alone

0U11 AC2(3A2(ON 1ESS actiationNo actiation

Agonist 4 AntagonistStim#lates an" bloc+s

- Creates a !late# in the !harmalogic e$ect


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Before O!ioi" *ece!tor Actiation


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After O!ioi" *ece!tor Actiation


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After O!ioi" *ece!tor Actiation


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O!ioi" Pharmacologic

E$ectsM#'5 an" M#'6 *ece!tor Me"iate"

Analgesia

Se"ation' can "eelo! a tolerance to if on for a

7hileE#!horia

*es!iratory "e!ression

Co#gh s#!!ression

MiosisNa#sea 8 omiting

Consti!ation

2olerance, !hysical "e!en"ence, an" 7ith"ra7al


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Pharmaco"ynamicsDose'*es!onse C#re


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O!ioi" (n"icationsAc#te an" chronic !ain

Malignant an" nonmalignant !ain

Scientic ei"ence for malignant !ain -cancer.No ei"ence for long term o!ioi" #se for

nonmalignant !ain

Ne#ro!athic an" m#s+#los+eletal !ain


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DEA ClassicationSche"#le (

9igh !otential for ab#se an" no c#rrently acce!te"me"ical #se in the US -heroin, MDMA, marij#ana.

Sche"#le ((

9igh !otential for ab#se an" c#rrently acce!te" me"ical#se in the Unite" States -!#re o!iates, am!hetamines,

barbit#rates, hy"roco"one.%

Sche"#le (((Potential for ab#se less than the "r#gs in sche"#les (

an" (( -co"eine mi)e" 7ith NSA(D or APAP,b#!renor!hine.%

Sche"#le (31o7 !otential for ab#se relatie to the "r#gs in sche"#le

((( -ben&o"ia&e!ines, :&'"r#gs; &ol!i"em, trama"ol.%


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Categori&e hy"roco"one@APAPaccor"ing to the DEA Classication%

5% Sche"#le (

6% Sche"#le ((

>% Sche"#le (((?% Sche"#le (3


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Ben&o"ia&e!ine Mechanism of

ActionBen&o"ia&e!ines enhance the e$ect of the

ne#rotransmitter gamma'aminob#tyric aci"-ABA.% -inhibitory.

htt!@@!harmacologycorner%com@animation'ben&o"ia&e!ines'"ia&e!am'lora&e!am'al!ra&olam@

http://pharmacologycorner.com/animation-benzodiazepines-diazepam-lorazepam-alprazolam/http://pharmacologycorner.com/animation-benzodiazepines-diazepam-lorazepam-alprazolam/http://pharmacologycorner.com/animation-benzodiazepines-diazepam-lorazepam-alprazolam/http://pharmacologycorner.com/animation-benzodiazepines-diazepam-lorazepam-alprazolam/


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Classication of Ben&osShort acting

mi"a&olam, tria&olam

(nterme"iate actingal!ra&olam, lora&e!am, tema&e!am

1ong actingDia&e!am -ale#m., chlor"ia&e!o)i"e,

#ra&e!am


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Ben&o Pharmacologic

E$ectsSe"ation

9y!notic

An)iolyticAnticon#lsant

M#scle rela)ant

Amnesia

2olerance, !hysical "e!en"ence, an"7ith"ra7al

"r#gs -&ol!i"em etc. only ca#se se"ation an" "o not

hae an)iolytic, anticon#lsant an" m#scle rela)ant e$ect


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Ben&o"ia&e!ine

(n"ications(nsomnia F short term #se

An)iety

Seire "isor"ersM#scle s!asm

Pre's#rgical retrogra"e amnesia


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6G56 Beers Criteria '

Ben&os*ecommen"ation Aoi" ben&o"ia&e!ines of

any ty!e for treatment of insomnia, agitation,or "eliri#m%

*ationale Ol"er a"#lts hae increase"sensitiity to ben&os an" slo7er metabolismof long'acting agents% (n general, all ben&osincrease ris+ of cognitie im!airment,"eliri#m, falls, fract#res, an" motor ehicleacci"ents%

H Am eriatr Soc 6G56%


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6G56 Beers Criteria F

"r#gs*ecommen"ation Aoi" chronic #se -IJG

"ays.

*ationale Ben&o"ia&e!ine rece!tor agonistshae a"erse eents similar to those ofben&o"ia&e!ines in ol"er a"#lts -"eliri#m,falls, fract#res.%


Ben&o"ia&e!ines are classie" base" on


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Ben&o"ia&e!ines are classie" base" ontheir half'life%


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Com!are the !harmacological e$ects of al!ra&olaman" &ol!i"em%


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Non'Ben&o"ia&e!ine M#scle

*ela)antsmeta)alone -S+ela)in.

cycloben&a!rine -0le)eril.

cariso!ro"ol -Soma.methocarbamol -*oba)in.


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Centrally Acting M#scle *ela)ants

Mechanism of ActionDecrease m#scle tone an" alleiate m#scle

s!asm, !ain an" hy!er'ree)ia%

Central nero#s system rela)ation is achiee"in general by mimic+ing or enhancing thee$ects of s#bstances s#ch as ABA%


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Centrally Acting M#scle *ela)ants

Pharmacologic E$ectsSe"ation

(m!aire" motor coor"ination

De!en"enceDry mo#th, consti!ation, bl#rre" ision


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6G56 Beers Criteria F M#scle

*ela)ants*ecommen"ation Aoi"%

*ationale Most m#scle rela)ants are !oorlytolerate" by ol"er a"#lts beca#se ofanticholinergic a"erse eents, se"ation, an"ris+ of fract#res%



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Avoid Anticholinergics

Arch Intern Med. 2008;168(5):508-513

A id A ti


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Avoid Anti-cholinergics

9ighest *is+Amitri!tyline, atro!ine, ben&tro!ine, carisoprodol,

chlor!heniramine, cy!rohe!ta"ine, "icyclomine,"i!henhy"ramine -Bena"ryl., #!hena&ine,

hy"ro)y&ine, hyoscyamine, imi!ramine, mecli&ine,o)yb#tynin, !er!hen&a&ine, !rometha&ine,thiori"a&ine, thiothi)ene, ti&ani"ine, tri#o!era&ine

9igh *is+

Amanta"ine, baclofen, cetiri&ine, cimeti"ine,clo&a!ine, cyclobenzaprine, "esi!ramine,lo!erami"e, lorata"ine, nortri!tyline, olan&a!ine,!rochlor!era&ine, !se#"oe!he"rine, toltero"ine

Arch Intern Med. 2008;168(5):508-513

A id A ti


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Avoid Anti-cholinergics

Me"i#m *is+Carbi"o!a'leo"o!a, entaca!one, halo!eri"ol,

ethocarbaol, metoclo!rami"e,

mirta&a!ine, !aro)etine, !rami!e)ole,#etia!ine, raniti"ine, ris!eri"one, selegiline,tra&o"one, &i!rasi"one

Arch Intern Med. 2008;168(5):508-513


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%1ora&e!am?% 1#nesta


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Non'steroi"al Anti'inammatory

Dr#gs


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NSA(Ds Mechanism of

Action*e"#ce !rostaglan"in !ro"#ction by inhibiting

cyclo'o)ygenase -COL'5, COL'6. en&ymes%

Decrease" !rostaglan"in !ro"#ctionAnalgesia

Anti!yresis -re"#ce feer.

Anti'inammation


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NSA(Ds Mechanism of

ActionCell membrane !hos!holi!i"s

En"oli!ase F corticosteroi"s

Arachi"onic aci"Cycloo)ygenase F NSA(Ds

2hrombo)ane

Prostaglan"ins

Prostacyclin


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COL'5 s% COL'6Cycloo)ygenase 5

Platelet actiation an" aggregation

A$erent arteriole "ilation an" increase"glomer#lar ltration

(ncrease" ( m#co#s !ro"#ction

Cycloo)ygenase 6

Analgesia an" inammatory res!onse


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NSA(D Classication s

APAPNon'selectie(b#!rofen, na!ro)en, +eto!rofen, in"omethacin, as!irin,

eto"olac, !iro)icam, +etorolac

*is+ of (, *enal si"e e$ects an" eleate" Bloo" Press#re

Selectie COL'6 (nhibitorsCeleco)ib, al"eco)ib, rofeco)ib

1ess ( ris+

Same renal ris+ an" eleate" bloo" !ress#re as non'selectie

Acetamino!henAnalgesia, b#t no anti'inammatory !ro!erties

1ess (, bloo" !ress#re an" renal ris+s

1ier to)icity F aoi" "aily "oses I > grams in a"#lts

5 ca#se of he!atic inj#ry "#e to oer"ose


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6G56 Beers Criteria F NSA(Ds, non'

selectie*ecommen"ation Aoi" chronic #se #nless

other alternaties are not e$ectie an"!atient can ta+e gastro!rotectie agent -PP( F

ome!ra&ole.*ationale (ncreases ris+ of ( blee"ing an"

!e!tic #lcer "isease in high'ris+ gro#!sincl#"ing those I, ta+ing oralcorticosteroi"s, anticoag#lants, or anti!lateletagents% (n"omethacin an" +etorolac haehighest rate of a"erse e$ects%



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Acetamino!hen% % Acetamino!hen

?% Celebre)


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CASE Disc#ssion? year'ol" man% 2hree years ago,

sym!tomatic beginning of lubar pain 7henthe !atient, s!en"ing a lot of time seate" in

his oQce, com!laine" of !ain in his bac+ 7henstan"ing #! from the chair%

2he or"ere" l#mbar M*( at that time sho7e"s!on"ylosis an" "egeneratie "isc "iseasemostly in the 1>'? an" 1?' segments 7ithright 1?' "isc herniation%

Me"ical O!inion F Me"ical Case St#"ies


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CASE Contin#e" 2he !ain 7as !ersisting on an" o$ #ntil fo#r7ee+s ago, 7hen the a)ial lo7 bac+ !ainincrease" 7ith lo7er e)tremities ra"iation,

!arasthesias an" tingling% 2he !ain is constant, #ct#ating at a 5'

R@5G !A" level% 2he !ain increases 7ith!rolonge" sitting an" getting #! from thechair% (t im!roes in supine position an"resoles 7ith an injection of 3oltaren%


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CASE Contin#e"

2he l#mbar M*(, that 7as re!eate",7as consistent 7ith s!on"ylosis an"

"egeneratie "isc "isease%


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CASE Contin#e"


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#estions===

As+ yo#r !harmacist%

opiates nsaids benzos 2016

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