Opioids Flashcards
بسم الله الرحمن الرحيم وبه نستعين
What are opioids ?
Drugs with morphine like actions
Anaglesiscs?
Drugs relive pain due to multiple causes.
Opiods : Morphine + synthetics
Non opioids : NSAIDS + Paracetamol
Mild pain
mODERATE Pain uncontrolled
Moderate to severe pain
Comfortable pain free
Non opidods + adjuvants
Weak opioids + non opioids + adjuvantts
Stron opioids + non opioid + adjunatn
Invaseive
Non opioids ?
Adjuvants ?
NSAIDS + Acetamnipohen
Antidepressants + AntiConvulsants
Non opioids ?
Adjuvants ?
NSAIDS + Acetamnipohen
Antidepressants + AntiConvulsants
Weak opioids ?
Termadol + codiene
StRONG OPIOIDS
MOHAB FANTA
Morphine
Oxycodiene
Hydromorphone
Bubronephrine
Fentanayl
Opioids analgesices used in ?
Moderate to severe pain
named dueOPium poppy= Opium ——-10% is morphine
Opioids analgesices used in ?
Moderate to severe pain
named dueOPium poppy= Opium ——-10% is morphine
Codiene also dervied from opium
Opiates and opioids ?
Opiates are derivatves of the alkaloids of opium poppy
Opioids : The class of drugs inculding : Opiate , Opiopepetins , Synthetic and semsyntheic drugs work as Opiates
Narcotic ? why ? opioids
Because of
Stupor +Analgesisa
Stupor = Drowisness and impairment without loss of Consiousness
Narcotic ? why ? opioids
Because of
Stupor +Analgesisa
Stupor = Drowisness and impairment without loss of Consiousness
Narcotic ? why ? opioids
Because of
Stupor +Analgesisa
Stupor = Drowisness and impairment without loss of Consiousness
Mention sourcrs of opioids
S2EP
Plant : Morphine - Codiene
Endogenous : endorphins enkephalins and dynorphins
Synthetic: FTM ( Fentanyl+ tramadol+ Methadone )
Semisynthetic : Heroin + Oxycodiene
Classifiacation of opioids at Function
3As:
-Analgesics + Antitissuves+Antidiarrheal
1-Analgesics وقسمناهم
2-Antitussives CD Codeine - Dextromethorphan
3-Antidiarrheal : LD
Lopramide + Diphenoxylate
Natural opiodis ?
Morphine + codiene agnoists
Semisynthetic :
opioids?
HO HO H !
Hydrocodone
Oxycodone
Hydromprohone
OxyMorphone
Heroin
Classificaion of Synthetics Opioids?>
FT2M2 agonists
Fentaynyl
Tramadlo
Tepentatdol
Mehadone
Mepridine
Partial agonists of opioids ?
Bubrenorp.hin.e
Pentazocine
Nalubuphine
Antagonists of Opioids
عشان نزع السمية
1- Nalxone
2- Nalterxone
Opioids receptors ?
Mu- Delta - kuppa Receptors
Mu most imp resp fort Analgeisa + sedation + respirtaory deprssion !
General explanation of Opioid receptors work
Gi decreasing CAMP Presynaptic
Closing Ca channels
Preventing Glutamate release
Opeining K channels postsynaptic Hyperpolarization and Prevents AP
Opioids receptor activaed ?
Supraspinal : Brainstem + thalamus+cerberal Cortex
Spinal
Pehriphey ? afferent nerves conducting pain
Increasing Dopamine in Nucleus Accumbenes casuing Euphoria and prevent the emotional feel of pain
Ascending pain pathway is ?
Descending pain pathway?
spinothalmic tract
Descending start from periaqudrcta grey area desending to spinal cord releasing Enkephalins + NE + 5HT
repressing spinothalamic Tract of pain
So how opiodes relieve pain ?
Increasing the Opiopepetins : Enkeplains
Working on its Receptors on spinothalmic tract inhibiting pain pahtyway
Termadol
Inhibit reuptake of
Serotonin and NE increaing their inhibitory effect on spinothalamic Tract
And it is Non opioid activity on side to its opioid activity
Classify Opioids Analgesics at its efficay?
Strong :
Agnoists as PFHM
Pethidine
Fentanyl
Heroin
Methadone - Morphine
Partial agonists as Bubrenorphine
______________________
Moderate Codiene and oxycodeine
+ NSAIDS + Antussive activity
_______________________
Weak : Propoxyphene
Analgesics + NSAIDS PARACETAMOL
Main )))))Actions of opioids mention
and classify it to indications and contraindications
Anaglesia+ Sedation + euphoris
1-Analgeisa
I: post operative : acute trauma - MI
CI : Undiagnosed acute abdomen
2-Sedation
I: anaethesia preoperateve preanathrsia medications
CI: casuing Sedation and Narcosis
in dangerous cases
3-Euphroia not indication it is cause of contra indication as casuing dependence
Indication of Opoiids mention
Anglesisc post operative acte reuama cancer MI
Sedation in anathesia and Sugery
Contraindication of Opioids /
Analgesic in Undiagnosed Acute abdomen
Sedation and Narcosis in some situations
Casuing euphoria
How opioids casuing euphoraa?
Inhibite release of Glutamte which inhibit dopamine release casuing
Increased Dopamine in Nucleus accumbnes and Ventral Tegmental Area
Casuing euphoria
Maiinly casue of Death in Case of opioids?
Repiratoy center inhibition by toxicity
Inhbitory effects of Opioids works on?
4 centers + Uterine
Respiratory Center
Cough Center
VMC
thermoregulatory center
Opioids and cough center?
They are antitussive
Codeine + Dextromethorphan
كان بيعمل إدمان
تلاقيهم بيشتروا ازارة ويشربوها مرة واحدة !
Opioids and Respiratory Center
Most common cause of death
due to opioids cuz of respiratory depression .
Make body insensitive to CO2 and Inadqeuate Respiration
Also in Case of Ceaserain section In addicted woman Casuse Asphyxia Neonatorum .
Increasing Co2 casuing Cerberal VD icreasing ICP contraindicatd in head injury
Make body insensitive to CO2 and Inadqeuate Respiration
opioids
in Case of Ceaserain section In addicted woman opioids are CI why ?
Casuse Asphyxia Neonatorum .
Opioids are contraindicatd in head injury why ?
Make respiratorty centers insensitive to Co2 Increasing Co2 casuing Cerberal VD icreasing ICP contraindicatd in head injury
Why Opioids are CI in Labour?
Decrasing Uterine tone +
Ceaseine section casue Ashpyxia Neonatorum
Acute pulmonary edema is indication of Opioids ?
Yes , becasue opioids Repress VMC
Causing Venulodilator and Arteriolodilator effects Causuing decreas in PreLoad and AfterLoad of Heart Decreasing Respiratory distress + Anxiety
But in normal p casues Hypotension
Hypothermia and opioids
Opioids depress the Thermoregulatory centers Causing Hypothermia
Describe inhibitory effects of opioids ?
-Depress the COUGH center so
I: Antitussive Codeine+ Dextrometh
-Depress respiratory center so
CI: Respiratory depression + Asphyxia nenoatrum in CS
-Depress VMC so
I: Acute pulmonary edema
CI : Hypotension
-Depress uterine tone
CI: labour
Depress Thermoregulatory center :
AE CI : Hypothermia
Inhibitory indications of Opioids ?
- Antitussive inhibiting cough cent
-Acute pulmonart edema inhibiting VMC
Inhibitory Contraindications of Opioids ?
-Respiratory depression
-Asphyxia Neonatorum
-Labour delay
-Hypotension
-Hypothermia
المدمن بيتعرف من؟
Miosis
Constipation
Opioids and pupil
Stuimulate occluomotor nucleus or
The parasympathtic nuclerus of third 3rd cranial nerve casuing pin point pupil or called Miosis adverse effect and distingusih addicts
Opioids and Vomiting ?
Stimulating The CTZ
Chemoreceptor Trigger zone
Opioids and diarrhea?
Its antidiarrheal (indications) as it is spsamogenic
Causing closure of Sphincters of anal and urinary of bladder
Stool and urine retention
constioation
Opioids and gall bladder ?
In case of Biliary colic is spamogenic closing the sphincter of oddi and increasing inflammation may casue rupture and peritonins and septic shock
Opioids and Asthma and Hypotension
Opioids release Histamine cassuing bronchoconstriction so CI in Athma
And hypotension VMC - HISTAMINE
Hypotension in opioids is due to ?
Histamine release
vmc depression
Stimulatory indication of opioids ?
Antidiarrheal
Stimulatory Advers effe and CI of opioids
+Occlumotor nucleus Miosis
+CTZ Nausea and Vomiting
Spasmogenic = constpiaton
Spasmogeinc = CI in biliary colic
Histamine releas = CI in Asthma + Hypotension
Stimulatory Advers effe and CI of opioids
+Occlumotor nucleus Miosis
+CTZ Nausea and Vomiting
Spasmogenic = constpiaton
Spasmogeinc = CI in biliary colic
Histamine releas = CI in Asthma + Hypotension
Stimulatory Advers effe and CI of opioids
+Occlumotor nucleus Miosis
+CTZ Nausea and Vomiting
Spasmogenic = constpiaton
Spasmogeinc = CI in biliary colic
Histamine releas = CI in Asthma + Hypotension
Tolerance occurs with all effect except ?
Miosis + Constipation
Stimularoy action of Opioids mention
+Occulmotor nucleus
+CTZ
+Spasmogenic
+Histamine relase
Contraindications of Morphine inspite of Severe pain ?
1-Undiagnosed acute abdomen
2-Labour
3-biliary colic
4-Head Injury
Other side effect of opioids ?
Seizures decreasing threshold of epilepsy in high doses
Othe CI of Opioids
?
Extreme age
Hypothyroidism
Liver dysfunctions
Morphine is given
Parenteral
IV IM SC Epidurally
Morphine is not perefered ?
Orally due to extensive first pass metabolism 20-40 %
Duration of action of Morphine ?
4-6 hOURES
Pehthidine Mepridine
IM + oral
Pethidine in potency and efficacy ?
Potency less than Morphine
Efficacy Equal to Morphine
What is used instead of Morphine in Biliary colic + Labour + why?
Pethidine or Mepridine
in Biliary colic:- less spasmogenic
in Labour :- less repiratory depression not casuing Asphyxia neonatorum
Less Utrein relaxation not delaying labor
Why Pethdine casue less constipation ?
Short action 2-3h
meanwhile Morphine 4-6 h
Blurred Vision and Dry moth appear with ? why?
Pethidine as it has atropine like actions parasympathatic antagonist
May casue mydriasis
Pethdine Increase risk of convulsion especially in / ?
1-Renal failure
2->48 h of acute pain
so its used only in acute not chronic
_____________________
Due to of accumulation of (Normeperidine)
Indications of Pethidine ?
Postopertative pain
Biliary colic +Labour
Advantage of pethidine over morpine are ‘
;
-Less repiratory depression so
less asphyxia neonatrum and death
-less spamogenic less constipation due to low duration and used in biliary colic and labour not causing delay or uterine relaxation
disadvantage of Mepridine pethidine against Morphine are?
Atropine like action
Blurred vision + dry mouth + Mydriasis
Risk of Convulsants due to accumulation of normeperdiine in RF or after 48
هل في تراجع في استخدام البثيدين ؟
اه عشان طلع بيتحول في الكبد ل
Norpethidine toxic metabolite
وده سام للطفل اللي الكبد مش هيقدر يعمل فيه
conjugation + excretion
فهيعمل
Asphyxia Neonatorum \
Desrive Fenatnyl Potency and oneset
and duration
Potency 100 fold than morphine
onset rapid due to lipophilicity 1-5m
Short duration .5 -2 hours
Functions of fentanyel mention
1-Epidural anasthesia + analgesisa:
Posteperatively + during labor
2-Transmucosal + Transdermal patches in chronic pain as cancer
مشاكل Fentanyel ايه ؟
الجرعة العالية بتعمل تخشب في عضلات جدار الصدر فيقلل اتساعية الصدر و يقلل القدرة علي التنفس
decrasing thoracic complicamce+ Ventilation
Indications of Fentanyl
Mention
1-Analgesic :
pre post operative + labor
2-Anasthesia :
Pre-anesthetic medication
3-Conscious sedation + Neuroleptanalgesia+ Neuroleptanethesia
Conscoius sedation mean ?
Amensia+ Analgesia + sedation
without loss of Conscousness
Consous sedation imp ?
In minor and diagnostic procedures as Endoscopy
Conscious sedation is done by ?
Benzodiazpines+Opoid analgesics
MidaZolam+ Fenatnyl
Conscious sedation drug toxiciy can be reversed by ?
Flumazenil + Naloxone
advantage
Neuroleptanalgesisa mean ?
Neurolept = antipsychotic drug + anaglesic
Dorperidol +Fentanyel
Neuroleptanalgesisa mean ?
Neurolept = antipsychotic drug + anaglesic
Dorperidol +Fentanyel
Neuroleptanasthesia is done by adding 65% N2O In O2 to Neuroleptanalgesic patient
Neuroleptanasthesia is done by ?
Neuroleptanasthesia is done by adding 65% N2O In O2 to Neuroleptanalgesic patient
Subgroups or Congenres of Fentanyl
mention 2
1-Sufentanil : more potent
2-Remifentanil : ريمي ريمي ريمي
ultrashot as metabolized in blood and tisse esterases casuing less venilation depression
Remifentanil : ريمي ريمي ريمي
duration and give reasion
ultrashot as IV INFUSION
metabolized in blood and tisse esterases casuing less venilation depression
Heroin is ?
DiacetylMorphine
Diacetyls Increase Lipid Solubility and Crossing BBB 3 times than morphine make it more liable to Euphoria and Addiction due to rapid onset short duration
Is converted in brain into Morphine
How addcits use herioin ?
IS2
Injecting IV / IM after Dissolving in a spoon of Water
Snorting : up by nose by 20$
Smoking : heating up poweder and inhalation of fumes by a small tube of foil
Methadooooooone
Duration ? IMP
24-36 hours
so it is useful in Detocification of Herioin in addicts as It takes longer to leave opioid receptors making the withdrawal smoother and less severe
Methadone Indications ?
Analgesic equal to morphine
detoxification in opioid addicts
long duration less severe and smoother withdrawal
Make a comparsion between methadone and Heroin at
Route
Onset
Duration
Euphoria
Methadone:
Oral only
30 M
24-36H
Absent
Herion:
IV IM INTRA NASAL
IMMEDIATE
MARKED Euphoria
3-6H
Make a comparsion between methadone and Heroin at
Route
Onset
Duration
Euphoria
Methadone:
Oral only
30 M
24-36H
Absent
Herion:
IV IM INTRA NASAL
IMMEDIATE
MARKED Euphoria
3-6H
Mention adverse effects of methadone
As Morphine
QT interval prolongation
Torsade de pointes arrythima
Route of Tramadol
Oral IV IM
Tramadol function
It is mixed opioid and non opioid
Non opioid Anaglesia by inhibiting reuprake of serotinin and NE
Weak Mu agonist
so Partly antgonisted by Naloxone
Used in
Analgesia ( post oper+ chronic pain)+ Neuropathic pain
Bupernophrine is
partial agonist
Bubrenorphine has a property over Morphine explain
Ceiling effect
Has same effective analgesic Effect
but less Euphoria + less Resp. Depression ……
Bubrenrophine how to administrate ?
Sublingual
Parentral
Mention uses of Bubrenorphine /
1-Analgesic in sever pain
2-Detox in Opioid toxicity
as it is used as methadone due to ?
Long duration 24 h and Less severe withdrawal
Mention two drugs help in detox of Morphine and give reason
Methadone
Bubrenorphine
due to long duration of action so less severe and smoother withdraw
Buprenorphine and heroin
بيمنع ان الهروين يمسك في المستقبل لان له ارتباطية قوية بالمستقبل
بيحجب النشوة الناتجة عن الهروين
وله ميزتان هو مفيش نشوة + مفيش تثبيط تنفسي
bubernorpine
في وحود الهيروين يعتبر ؟
antagonist عشان كده مش هنستخدمه في العملية لو الراجل واخذ هيروين لانه يعمل اعراض انسخاب ومش هيشيل الألم
Pethidine or Tramadol + MAOI
interactions
Pethidine increase sertoinin
Tramadol decrease reuptake serotinine and NE AS MAOI
Causing Serotonin Syndrome
Nevere give opioids + CNS depressants
(Sedative+alcohol+antidepress + antipsychotic )
it will add CNS depress
Acute Morphine toxicity apppear as ?
Repsitaroy depression
Pinpoint pupil Miosis
Coma due to CNS depression
Treatment of Acute morphine Toxicity?
Resp Support
Naloxone competitive opioid antagonist
How to treat addiction ?
1-Symptomatic treatment
Pain ; NASIADS
Vomiting: antiemetic
2-Sympatholytic: Clonidine
3-Detox : Methadone +Buprenorhpine
4-Maintanance: naltrexone to prevent relpase by euphoria
وقيل الحمدلله رب العالمين
الحمدلله رب السماوات والأرض رب العالمين
