Opioids are powerful pain relievers that work by binding to opioid receptors in the brain and body. Friedrich Sertürner first isolated morphine from opium in 1803. Opioids include natural opiates derived from the opium poppy like morphine and codeine, semi-synthetic drugs like heroin, and fully synthetic drugs like fentanyl. They act primarily on mu, kappa, and delta opioid receptors and their effects include analgesia, sedation, respiratory depression, and constipation. Common opioids used in anesthesia include morphine, fentanyl, pethidine, and tramadol. While opioids are effective analgesics, their use can cause side effects and risks of dependence, addiction,
https://gettreatment.com/blog
Opium is the dried latex obtained from the opium poppy. The immature seed pod are cut (scored), which makes the latex leak out. It dries into opium.
Prof. Mridul M. Panditrao has added another of his very important, useful and in vogue topic to his collection. This is his well acclaimed andwell received faculty lecture at recently concluded International conference on Pain... ISSPCON 2014, at Mumbai/ Bombay from 6th to 9th Feb. 2014.
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Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journeygreendigital
Tom Selleck, an enduring figure in Hollywood. has captivated audiences for decades with his rugged charm, iconic moustache. and memorable roles in television and film. From his breakout role as Thomas Magnum in Magnum P.I. to his current portrayal of Frank Reagan in Blue Bloods. Selleck's career has spanned over 50 years. But beyond his professional achievements. fans have often been curious about Tom Selleck Health. especially as he has aged in the public eye.
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Introduction
Many have been interested in Tom Selleck health. not only because of his enduring presence on screen but also because of the challenges. and lifestyle choices he has faced and made over the years. This article delves into the various aspects of Tom Selleck health. exploring his fitness regimen, diet, mental health. and the challenges he has encountered as he ages. We'll look at how he maintains his well-being. the health issues he has faced, and his approach to ageing .
Early Life and Career
Childhood and Athletic Beginnings
Tom Selleck was born on January 29, 1945, in Detroit, Michigan, and grew up in Sherman Oaks, California. From an early age, he was involved in sports, particularly basketball. which played a significant role in his physical development. His athletic pursuits continued into college. where he attended the University of Southern California (USC) on a basketball scholarship. This early involvement in sports laid a strong foundation for his physical health and disciplined lifestyle.
Transition to Acting
Selleck's transition from an athlete to an actor came with its physical demands. His first significant role in "Magnum P.I." required him to perform various stunts and maintain a fit appearance. This role, which he played from 1980 to 1988. necessitated a rigorous fitness routine to meet the show's demands. setting the stage for his long-term commitment to health and wellness.
Fitness Regimen
Workout Routine
Tom Selleck health and fitness regimen has evolved. adapting to his changing roles and age. During his "Magnum, P.I." days. Selleck's workouts were intense and focused on building and maintaining muscle mass. His routine included weightlifting, cardiovascular exercises. and specific training for the stunts he performed on the show.
Selleck adjusted his fitness routine as he aged to suit his body's needs. Today, his workouts focus on maintaining flexibility, strength, and cardiovascular health. He incorporates low-impact exercises such as swimming, walking, and light weightlifting. This balanced approach helps him stay fit without putting undue strain on his joints and muscles.
Importance of Flexibility and Mobility
In recent years, Selleck has emphasized the importance of flexibility and mobility in his fitness regimen. Understanding the natural decline in muscle mass and joint flexibility with age. he includes stretching and yoga in his routine. These practices help prevent injuries, improve posture, and maintain mobilit
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Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
These simplified slides by Dr. Sidra Arshad present an overview of the non-respiratory functions of the respiratory tract.
Learning objectives:
1. Enlist the non-respiratory functions of the respiratory tract
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5. Describe the cough and sneeze reflexes
Study Resources:
1. Chapter 39, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 34, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 17, Human Physiology by Lauralee Sherwood, 9th edition
4. Non-respiratory functions of the lungs https://academic.oup.com/bjaed/article/13/3/98/278874
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Prix Galien International 2024 Forum ProgramLevi Shapiro
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Microteaching is a unique model of practice teaching. It is a viable instrument for the. desired change in the teaching behavior or the behavior potential which, in specified types of real. classroom situations, tends to facilitate the achievement of specified types of objectives.
1. OPIOIDS
DR. SURAJ KURMI (INTERN)
DEPARTMENT OF ANESTHESIOLOGY
“Among the remedies which it has pleased
Almighty God to give to man to relieve his
sufferings, none is so universal and so efficacious
as opium.”
2. OBJECTIVES
• INTRODUCTION/ TERMINOLOGY
• HISTORY
• CLASSIFICATION
• OPIOIDS RECEPTORS AND ITS DISTRIBUTION
• MECHANISM OF ACTIONS
• SYSTEMIC EFFECTS
• USES IN ANESTHESIA
• IMPORTANT OPIOIDS AND ITS USES AND EFFECTS
• OPIOD WITHDRAWAL SYNDROME
3. INTRODUCTION/TERMINOLOGY
• Opioids:
It includes all the natural and semisynthetic alkaloid
derivatives from opium as well as their synthetic
surrogates with the action that mimic those of
morphine.
It includes:
1. Opiates
2. Synthetic opioids( agonist, mixed agonist-
antagonist and antagonist)
3. Endogenous opioids
4. • Opiates
opiates are taken to those opiod drugs that are derived from
alkaloids of the opium poppy( papaver somniferum)
Opium is a Greek word meaning “juice,” or the exudate from
the poppy
Opium is obtained from the opium poppy by incision of the
seed pod after the petals of flower have dropped. The
white latex that oozes out on incision turns brown and
hardens on standing. This sticky brown gum opium. It
contains 20 alkaloids. The principle alkaloid in opium is
morphine(10%), codeine is present in <0.5%
7. Endogenous opiods
• Enkephalins (act through delta receptor)
• Endorphins( act through mu receptor)
• Dynorphins( act through kappa receptor)
Enkephalins and endorphins mediate
supraspinal control of pain while dynorphins
mediate pain control at spinal level.
enkephalins are responsible for producing
acupuncture mediated analgesia
8. Opioid - History
• Friedrich Wilhelm Serturner
– A German Pharmacist
– Isolated Morphine in 1803 and named it after the
Greek god of Dreams “MORPHEUS”
• Used for thousands of years to produce:
– Euphoria
– Analgesia
– Sedation
– Relief from diarrhea
– Cough suppression
9. Opioid- history
• Used medicinally and recreationally from early Greek
and Roman times
• Opium and laudanum (opium combined with alcohol)
were used to treat almost all known diseases
• Invention of the hypodermic needle in 1856 produced
drug abusers who self administered opioids by
injection
• Controlling the widespread use of opioids has been
unsuccessful because of the euphoria, tolerance and
physiological dependence that opioids produce
10. Classification of Opioids
Low efficacy for mild and moderate pain High efficacy for severe pain
Codeine
Dihydrocodeine
Pentazocine
Morphine
Pethidine
Methadone
phenazocine
NATURALLY OCCURING SEMI-SYNTHETIC SYNTHETIC
• Morphine
• Codeine
• Thebaine
• Heroin
• Dihydromorphone
• Oxymorphone
• Pentamorphone
• Butorphanol
• Levorphanol
• Pethidine
• Fentanyl,
alfentanil,sufentanil
• Tramadol
• Buprenorphine
11. CLASSIFICATION ON BASIS OF
RECEPTOR INTERACTION
PURE AGONIST AGONIST ANTAGONIST PURE ANTAGONIST
•Morphine
•Fentanyl
•Alfentanil
•Sulfentanil
•Pethidine
•Pentazocine
•Butorphanol
•Nalorphine
•Buprenorphine
•Dezocine
•Naloxone
•Naltrexone
•Nalmefene
•Diprenorphine
•Methylnaltrexone
1. Pure agonist: are agonist to all opioid receptors with highest propensity for
mu receptors
2. Agonist-antagonist: All agonist and antagonist (except buprenorphine and
dezocine) are agonist at kappa and sigma receptor and antagonist at mu
receptor.. Buprenorphine and dezocine are classified as partial agonist
antagonist as at low dose they are agonist at mu receptor whereas at high
dose become antagonist. Produces ceiling effect.
3. Pure antagonist: antagonist to all receptor
12. OPIOID RECEPTORS
• Mainly 3 (three) types of receptors – μ (mu), κ (kappa)
and δ (delta)
• Subtypes: μ1, μ2, κ1, κ2, κ3, δ1 and δ2
• Location: Peripheral Nerve endings, SG in spinal chord,
Periaqueductal gray (PAG) in midbrain and Brain stem
(medulla, hypothalumus and also amygdala
• Sigma receptors are not considered as opioid receptors
as they are not activated by morphine and not blocked
by naloxone. Actions mediated by it are : dysphoria,
hallucination,tachycardia and htn
• Nociceptin(orphanin FQ) has been identified as new
opiod receptor through which endogenous opiod act.
13. Distribution of opiod receptors
• Dorsal horn of spinal cord
• Subcortical regions of brain
Thalamus
Midbrain periaqueductal gray
Rostral ventral medulla sites(nucleus raphe
magnus)
• Locus ceruleus of brainstem
• Hypothalamic nuclei
17. MECHANISM OF ACTION OF OPIOIDS
SUPRASPINAL: opioids binds with receptors in rostroventral
region of medulla and cause stimulation of off cells present
there, thereby blocking nociceptive stimuli transmission
SPINAL LEVEL: act in substantia gelatinosa of dorsal horn cells
and inhibit the release of excitatory transmitters
Cellular level: opioids bind with the receptors and stimulate G
protein synthesis and increases cAMP which causes:
Increase K+: hyperpolarization of membrane
Decreases calcium: decreases excitability
18. Mechanism
All are G protein coupled receptors
• inhibit adenylyl cyclase
• Associated with ion channels,
1. ↑ postsynaptic K+ efflux
(hyperpolarization)
2. ↓ presynaptic Ca+2 influx leading
to inhibition of excitatory
neurotransmitter release
19. Uses in anesthesia
Mainly used for analgesia, for both intraoperative and
postoperative
Blunting cardiovascular reponse to intubation. Fentanyl is
most commonly used but sulfentanil is the agent of choice
Painless labour (fentanyl+bupivacaine by epidural route)
Sedation in ICU
Pulmonary edema ( morphine is the agent of choice)
Intraoperative myocardial ischemia( morphine is used)
To abolish shivering( pethidine ad tramadol)
For day care surgery( propofol+remifentanil is the
combination of choice)
20. Systemic effects
CARDIOVASCULAR SYSTEM
HYPOTENSION: due to decreased central sympathetic
tone.(minimum with fentanyl) . Pethidine and
pentazocine causes hypertension
BRADYCARDIA,( except pentazocine and pethidine
causes tachycardia)
Shifting of blood from pulmonary to systemic
circulation( Rx of left ventricular failure)
Vasolidation,
Decrease peripheral vascular resistance,
Decrease pulmonary vascular resisitance
21. RESPIRATORY SYSTEM
•Respiratory depression
•Medulla: mu2 receptor
•Decreases both the rate and volume
•Usual cause of death in opioid poisoning
•Bronchospasm
•Morphine, pethidine: histamine release
•Directly acting on bronchial muscle opiods
are bronchodilator but can cause
bronchoconstriction by release of histamine
•Inhibits airway and tracheal reflex(so used in
intubation and laryngoscopy and used in cough
syrups(codeine))
22. Central nervous system
•Analgesia, visceral pain more relieved than somatic
pain
•Sedation: sedation at lower dose which progress to
deep coma in high dose
•Decrease cerebral metabolic rate(cmr), cbf(cerebral
blood flow) and icp in resting brain but increses in head
injury and icsol
•EEG: produces high voltage slow waves( delta) but
cannot cause flattening due to ceiling effect
•Nausea and vomiting due to stimulation of CTZ
•Mood changes and mental clouding
•Hypothermia
•Convulsions
23. Systemic effects
• Muscular system:can cause muscle rigidity which can sometime
severe in thoracic muscle that hypoxia occurs.( wooden chest
syndrome or stiff chest syndrome)
• GIT: Decrease peristalsis
• Ileus
• Constipation
• Constriction of sphincter of oddi and Increase of biliary duct
pressure
• Urinary system: urinary retention due to relaxation of urinary
bladder
• Eye: causes miosis, decreases IOP
24. Systemic effects
• Endocrine: stress hormones decresed like
ACTH,FSH,LH and cortisol. Whereas ADH, GH
and prolactin synthesis increased
• Decrease effect of shivering: pethidine
• Tolerance, physical dependence and
addiction
27. Opioid agonist
MORPHINE
• Clearance mainly by hepatic biotransformation
• M-3-glucuronide (inactive)
• M-6-glucuronide,highly active metabolite
• Metabolites cleared by kidney
• Plasma half life:2 hr duration of analgesia: 4-6hrs
• Dose: 0.1-0.2mg/kg
• Route: iv, im, subcutaneous, oral, epidural, intrathecal
• Respiratory depression in renal failure
• Death from morphine poisoning : respiratory arrest
28. Morphine
Indications:
As analgesic in visceral pain, following operation, terminal illness(cancer), burn
Myocardial infarction
Travelers diarrhea
To suppress cough
Acute LVF and pulmonary edema
Contrainication
Respiratory depression
Nausea. Vomiting
Constipation, biliary and ureteric spasm
Hypotension
Bronchospasm
29. Pethidine(meperidine)
• It is a synthetic morphine
• 1/10th potent than morphine
• Short duration of action(2-3hr).
• Large dose shows anticholinergic effect: mydriasis, antispasmodic
action, atropine like side effects
• Histamine release is less than morphine
• Metabolic producxt of pethidine noepethidine can cause convulsion
and delirium.
• Pethidine abolishes shivering so drug of choice in shivering.
• Contraindicated in mao inhibitor therapy and in patient with
myocardial ischemia(as it depresses myocardium)
• Dose is 0.1-1mg/kg
30. Fentanyl
• 100 times more potent than morphine
• Due to high lipid solubility it has rapid onset( 2-5 minute) and rapid
recovery(1-2hrs)
• Can be given im, iv, tranmucosal(fentanyl lollipop),
transdermal(fentanyl patch), intrathecal and epidural route
• Cardiac stability
• With bupivacaine used epidurally for painless labour
• Fentanyl can produce significant muscle rigidity
• Dose: 2-5mcg/kg
• Sulfentanil analogue of fentanyl is 500 times more potent than
morphine, agent of choice for inhibiting stress response to
laryngoscopy and intubation
31. Tramadol
• Synthetic derivative of codeine
• Produces analgesia by dual mechanism: first by acting on
opioid receptor and secondly by increasing serotonin levels
• 2nd drug of choice in shivering
Other opioid agonist
Codeine: used for suppressing cough
Heroin: highest addiction potential
Methadone: used in prevention of opiod withdrawal
symptoms
32. Agonist -antagonist
Produces ceiling to respiratory depression.
PENTAZOCINE( FORTWIN)
Agonist at kappa and delta receptor and antagonist at mu receptor
Mainly acts on kappa receptors at spinal level
Causes tachycardia and hypertension
Depress respiration but has ceiling effect on respiratory depression
Less nausea/vomiting
Less addiction potential than morphine
Dose: 1mg/kg can be given iv, im, routes
Pentazocine is used for sequential analgesic anesthesia. Th this
technique pentazocine is administered after fentanyl is given in
moderate doses
33. Buprenorphine
• mu agonist at low dose but become
antagonist at high dose(after 1.2mg in adults),
so respiratoey depression which may be seen
intially is reversed and there is increased
ventilation.
• 25 times more potent than morphine
• Dose: 0.3mg
34. Opioid antagonist
Naloxone
Acts on all receptors with maximum propensity for mu receptors
Reverses the action of all opioIds with partial reversal of
buprenorphine
Onset of action is 1-2 minutes and duration of action is 30-60
minutes
Metabolized in liver
Systemic effects: cvs- causes sympathetic stimulation and produces
severe hypertension and tachycardia and in cns causes incresed
metabolic rate, oxygen consumption and blood flow(increse icp)
35. Naloxone
Contraindication
Myocardial ischemia
Intracranial lesion
Pheochromocytoma
Uses of naloxone:
• Acute Morphine Poisoning (0.4 – 0.8 mg IV 2-3 min, maximum 10 mg.
• Reverse the effect of diazepam, barbiturates(though GABA receptor),
nitrous oxide, endogenous opioids, alcohol, ketamine
• Diagnosis of opioid dependence
• Treating neonatal asphyxia if opioid are used during labour
• Treatment of septicemia, hypovolemic and spinal shock
• In treating alzheimer’s disease. schizophrenia.
38. Drug interactions
• The depressant actions of morphine are
enhanced by phenothiazines, MAOIs, and TCAs.
• Analgesia enhanced by: Low doses of
amphetamine & hydroxyzine.
Editor's Notes
Inhibits release of transmitters – NA, DA, 5-HT, GABA and Glutamate