Opioids by m
of 10
Transcript of Opioids by m
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OPIOIDS
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ENDOGENEOUS OPIOIDPEPTIDES
ENDORPHIN
ENKEPHALIN
DYNORPHIN
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ACTIONS OF OPIOID RECEPTORSµ (Mu)
Physical dependence Euphoria
Analgesia supra spinal &
Spinal Respiratory depression
Constipation
Growth hormone Prolactin Secretion ACH Release
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(Kappa)
Sedation
Analgesia spinal & Supra spinal
Miosis
Dysphoria
Disorientation
ADH release
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(Delta)– AAnalgesia (spinal & supra spinal)nalgesia (spinal & supra spinal)
– ReRelease oflease of ggrowthrowth hhormoneormone
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OPIOID ANALGESICS
STRONG AGONISTS
Morphie
Meperi!ie
Metha!oe
Feta"l
Su#etailRe$i#etail
Al#etail
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MODERATE AGONIST
Co!eie
O%"&o!oe
Propo%"phee
PARTIAL AGONIST
'upreorphie'utorphaol
Petaoie
Nal*uphie
ANTAGONISTS
Nalo%oe
Naltre%oe
Nal$e#ee
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Mech Of ActionMech Of Action
Ca++
channels K +Channels open
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OPIOID PEPTIDESOPIOID PEPTIDESµ
ENDORPHINENDORPHIN ++++++ ++++++ ++++++
ENKEPHALINENKEPHALIN ++++ ++++++ ,,
DYNORPHINDYNORPHIN ++++ ++ ++++++
OPIOID DR-GSOPIOID DR-GS
MORPHINEMORPHINE ++++++ ++ ++++
ETORPHINEETORPHINE ++++++ ++++++ ++++++
PETHIDINEPETHIDINE ++++ ++ ++
PHENA.OCINEPHENA.OCINE ++++ ++++ ++++
ANTAGONISTSANTAGONISTSNALORPHINENALORPHINE ++++ ++++ ++++
NALO/ONENALO/ONE ++++++ ++++ ++++
AFFINITY OF OPIOIDS FOR RECEPTORS
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Pharmacological Actions
(Central) Analgesia Euphoria e!ation
"ecrease! respiration rate uppression of Cough re#e$ Miosis
%ausea & omiting 'runcal rigi!it
Continu
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Pharmacological Actions
(Peripheral)*'
iliar tract C
%euroen!ocrine
,istamine release uterus
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'olerance 'olerance
'olerance- re.ersi/letarts after the 0rst !ose
(clinicall 123 wee4s)
(constipation5 Miosis5 Con.ulsions)
Phsical !epen!ence
A/stinence n!rome
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CO%'6A *%"*CA'*O%
o HEAD IN+UR
o COPD
o USE O% PURE AGONIST -ITH -EA.
PARTIA# AGONISTo HPOTHROIDISM, ADDISON/S DISEASE
o IN PTS -ITH RENA# OR HEPATIC %AI#URE
o DURING PREGNANC
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A"E6E E77EC'
'eha0ioral !itur*a&e
NAUSEA & $OMITING
POSTURA# HPOTENSION
URINAR RETENSION
INCREASED INTRACRANIA# PRESSURE
HPOTHERMIA
ITCHING, URTICARIA
CONTIPATION
TO#ERANCE & DEPENDENCE
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MEPERIDINE ( Pe'hi"ine)
Phen!liei"ine "ei*a'i*e
Po'en! 012344mg 5 34mg Mohine
T1/2 3 hrs
Me'aolism 'o no2meei"ine a s'ong CNSs'imulan' Marked anticholinergic (Mydriasis, Tachycardia)
No an'i'ussi*e e6e'
Dug "een"ene ommon in heal'h 7o8es
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Metha!oneMetha!one
"ipheno$late5"ifeno$in58oprami!e"ipheno$late5"ifeno$in58oprami!e
8e.opropo$phen58e.opropo$phen5"e$tromethorphane"e$tromethorphane
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Pre.entionPre.ention
8OMO'*88OMO'*8 (!ipheno$late 19:mg + atropine ;9;1:mg)(!ipheno$late 19:mg + atropine ;9;1:mg) MO6P,*%E + %A8O
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COMMON OPIOID ANALGESICS
Hi1hHi1hHi1hHi1h,234,23455,264,264PareteralPareteral
Ol"Ol"Al#etailAl#etail
Hi1hHi1hHi1hHi1h7755724724PareteralPareteral
Ol"Ol"Su#eta"lSu#eta"l
Hi1hHi1hHi1hHi1h7755724724PareteralPareteral
Ol"Ol"Feta"lFeta"l
Hi1hHi1hHi1hHi1h335588Me!iu$Me!iu$Meperi!ieMeperi!ie
Hi1hHi1hHi1hHi1h885599Hi1hHi1hMetha!oeMetha!oe
Hi1hHi1hHi1hHi1h::5588Lo;Lo;O%"$orphoeO%"$orphoeHi1hHi1h
Hi1hHi1h
88
5544
Lo;Lo;
H"!ro$orphoeH"!ro$orphoe
Hi1hHi1hHi1hHi1h885544Lo;Lo;MorphieMorphie
A!!i&tioA!!i&tio
A*ueA*ueLia*ilit"Lia*ilit"
Ma%i$u$Ma%i$u$
E##i&ie&"E##i&ie&"
Duratio o#Duratio o#
Aal1eiaAal1eia
(Hour)(Hour)
OralOral
PareteralPareteralPote&"Pote&"
RatioRatio
Na$eNa$e
(Cot!)
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Hi1hHi1hHi1hHi1h885544Hi1hHi1hLe0orphaolLe0orphaol
Lo;Lo;Hi1hHi1h::5588PareteralPareteral
ol"ol"
'utorphaol'utorphaol
Lo;Lo;Hi1hHi1h8855
