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OPIOD
ANALGESICS
-Komal antil
1
GENERAL OBJECTIVES
• describe uses and types of opioids
SPECIFIC OBJECTIVES
• Define pain, pain pathways, types of
pain
• Types of analgesics
• Mechanism of action
• Indications
• Contraindications
• Adverse effects
• Nursing responsibilities
ALGESIA(PAIN):is an unpleasant sensory and
emotional experience associated with actual or
potential tissue damage or described in terms of
such damage.
ANALGESIC: A drug that selectively relieves
pain by acting in the CNS or on peripheral pain
mechanisms, without significantly altering
consciousness
PAIN PATHWAY
TYPES OF PAIN
ACUTE: It is of short duration but it gradually
resolves as the injured tissue heal.
E.g.injury or trauma
CHRONIC: persistent pain that lasts week to
years
E.g. pain may be caused by inflammation or
dysfunctional nerves.
BASED ON ETIOLOGY
NOCICEPTIVE PAIN: Result of activation of
sensory(afferent)receptors (nociceptors)by mechanical,
thermal, chemical stimuli
Functional,physiologic or normal pain
NEUROPATHIC PAIN: Pain resulting from damage to
peripheral nervous or central nervous system tissue or
from altered processing of pain in the CNS
CLASSIFICATION
Analgesics are divided into two groups:
NSAIDS: Non opioid analgesics(mild to
moderate pain)
OPIOIDS: Severe pain
NSAIDS
CLASSIFICATION
WHO PAIN LADDER
OPIOIDS
DEFINITION:
These are those substances used to treat
moderate to severe pain
They are sometimes called narcotics.
CLASSIFICATION
OPIOID RECEPTORS
Opioids exert their action by interacting with specific
receptors present on neurons in CNS&peripheral tissue
Radiological binding studies divided the opioid receptors
into
Each has a specific pharmacological profile,pattern of
anatomic distribution in brain,spinalcord,peripheral tissues
Opioid ligands can interact with diff.opioid receptor as
agonist,partial agonist,competitive antagonist.
OPIOID RECEPTOR
TRANSDUCER MECHANISM
Natural alkaloids
Class of naturally occurring organic nitrogen
containing bases.
This includes compounds with neutral and
even weakly acidic properties.
Well known alkaloids include
morphine,codeine.
MORPHINE
Strong analgesic
Visceral pain is relieved better than somatic pain
Degree of analgesia increase with dose
Nociceptive pain is better relieved than neuretic pain
Associated reactions are also relieved
:apprehension,fear,autonomic effects
Tolerance to pain is better
Mechanism of action
Two components:spinal &supraspinal
Inhibits release of excitatory transmitters from
primary afferents-at substantia gelatinosa of dorsal
horn
Exerted through interneurons-gating of pain
At supra spinal level in cortex ,midbrain&medulla -
alter processing and interpretation and send
inhibitory impulses through descending pathways
Pharmacologic actions
1.CNS
a)analgesia
b)sedation
c)mood and subjective effects
d)respiratory centre
e)cough centre
f)temperature regulating centre
g)vasomotor centre
2.NEURO-ENDOCRINE
2)NEURO-ENDOCRINE
3)CVS
4)GIT
5)Other Smooth muscles
a)biliary tract
b)Urinary bladder
c)Uterus
d)Bronchi
6)ANS
Adverse effects
1)Idiosyncrasy and allergy
2)Apnoea of newborn
3)Acute morphine poisoning
4)Tolerance and dependence
5)Others:Sedation,mental
clouding,lethargy,respiratory dispersion
SPECIFIC ANTIDOTE
Naloxone-0.4-0.8mg i.v. repeated every 2-3 min
till respiration picks up
CONTRAINDICATIONS
1)Infants
2)Patient with respiratory insufficiency
3)Bronchial asthma
4)Head injury
5)Hypotensive states
6)Undiagnosed acute abdominal pain
7)Elderly male
8)Hypothyroidism
CODEINE
Methyl morphine
Converted to morphine by the body
Partial agonist at µ opioid receptor with a low ceiling effect
Available as :
Tablets:15mg,30mg,60mg
Oral solution:15mg/5ml
Injection:30mg,60mg
SIDE EFFECTS
Constipation
Bloating
Indigestion
Dizziness
Nausea&Vomitting
Symptoms of overdose
Bluish lips or skin
Chest pain or discomfort
Constricted,pinpoint or small pupils
Decreased awareness or responsiveness
Extreme sleepiness or unusual drowsiness
Slow or irregular heartbeat
SEMI SYNTHETIC
OPIATES
HEROIN
It is also known as diacetyl morphine or dia morphine.
An illicit opioid synthesized from morphine that can be
a white or brown powder or a black sticky substance
The advantage of diamorphine over morphine is that
diamorphine is more fat soluble and therefore more
potent by inj.,so smaller doses of it are needed for the
same effect on pain.
Available forms: oral :5-10mg orally/IM/SC/IV repeated
every 4 hourly
Children : oral dose-0.6mg/kg/day, IV-0.01mg/kg/hr
INDICATIONS
Physical trauma (bone fractures)
Myocardial infarction
Post surgical pain
Chronic pain
End stage terminal illness
ADVERSE EFFECTS
Respiratory depression
Collapsed vein –long term effect
Dry mouth
Drowsiness
Impaired mental function
Blood borne infection
Pneumonia
Addiction
PHOLCODEINE
It’s a drug which is an opioid cough suppressant
Helps suppress unproductive coughs and also
has a mild sedative effect but has little or no
analgesic effect.
Its average half life is about 2.3 days
Available form: oral solution: 5mg/5ml
ADVERSE EFFECTS
Dizziness
GI disturbances
Constipation
Drowsiness
Excitation
Ataxia
Respiratory depression
CONTRAINDICATION
Hypersensitivity
Asthma
Respiratory failure
Liver failure
COPD,Chronic bronchitis
Alcoholism
HYDROCODONE
Its sold under the brand name hysingla
Its an opioid used to treat severe pain of a prolonged
duration
It is also used as cough suppressant in adults
It is sold as the combination of
acetaminophen+hydrocodone /
ibuprofen+hydrocodone
Dosage :5mg/2.5mg hydrocodone/300mg or 325mg
acetaminophen
The typical dosage is 1-2 tablets taken every 4-6 hrs
as needed
ADVERSE EFFECTS
Abuse
Low blood pressure
Seizures
QT prolongation
Respiratory depression
Serotonin syndrome
CONTRAINDIACTIONS
Hypersensitivity
Respiratory depression
Bronchial asthma
Gastrointestinal obstruction
OXYCODONE
Its sold under brand name as oxycontin
It is usually taken by mouth ,and is available in
immediate release,controlled release
formulations
Onset of pain relief typically begins within 15
mins and lasts for upto 6 hrs.
Dosage : 5mg immediate release form PO every
6 hrs.
ADVERSE EFFECTS
Euphoria
Anxiolysis
Respiratory depression
Reduced sensititivity to pain
constipation
SYNTHETIC OPIATES
PETHIDINE
Chemically unrelated to morphine
Interact with opioid receptor
Well absorbed orally,bioavailability 50%
Effects appear in 10-15 mins after oral absorption
On parenteral administration,action lasts for 2-3 hrs
Metabolized in liver-mepridinic acid and norpethidine
Excreted in urine
INDICATION
Analgesics(substitute of morphine)
Pre anaesthetic medication
Analgesic during labour
Dosage-50-100 mg IM/SC,Oral-50-100 mg tabs
ADVERSE EFFECTS
Similar to morphine
Atropinic effect(dry mouth, blurred vision,
tachycardia)
Overdose-tremors,mydriasis, delirium,
myoclonus, hyperreflexia, convulsions
FENTANYL
80-100 Times more potent than morphine
Fentanyl is 500 times more lipid soluble than morphine,that’s why it is
rapidly distributed in the body because of high lipid solubility,it enters
in brain rapidly and produce peak analgesia in 5min after i.v. injection
Its elimination t1/2 =3.5 hrs
Metabolized in liver in norfentanyl(inactive)
Excreted in urine
Dose- inj in 2& 10 ml ampoules containing 50mcg per ml
Short acting analgesic during operative and
perioperative period
Skeletal muscle relaxant to selected high risk
patient(those undergoing open heart surgery)
Respiratory depression
Transdermal fentanyl frequently used in cancer,
terminal illness pain, chronic pain
Oral route is not used due to high first pass
metabolism
INDICATION
ADVERSE EFFECTS
Redness and irritation on skin wherever apply
the patch
Dizziness
Reduce cardiac contractility & HR
Constipation
TRAMADOL
Centrally acting analgesic
Very low action on opioid receptors
Effective both orally and i.v.(100mg=10mg morphine)
Well tolerated and low abuse potential
High oral bioavailability i.e.70-100% with repeated dosages due to
reduction of first pass effect
Metabolized in liver by demethylation
Its elimination t1/2 =4-6hr
DOSE-50-100 mg IV/IM/oral
INDICATION
Mild to moderate short lasting pain due to
diagnostic procedure
Pain due to Injury
Post operative pain
Chronic pain including cancer pain ( not
effective in severe pain )
ADVERSE EFFECT
Similar to morphine but less prominent
(vomiting , drowsiness)
Sweating
Lowering of seizure threshold(contraindicated
in epileptics)
NURSING
RESPONSIBILITIE
S
Before beginning therapy,perform history
regarding allergies,use of other
medications,health history,and medical history
Caution patient not to chew or crush controlled
release preparations
Keep opioid antagonist and equipment for
assisted or controlled respiration readily
available during iv administration
Direct patient to lie down during IV administration
Dilute and administer IV slowly to minimize likelihood of
adverse effects
Monitor injection sites for irritation ,ex-travasation
Instruct postoperative pt.in pulmonary toilet;drug suppresses
cough reflex
Monitor bowel function and arrange for an thraquinone
laxatives for severe constipation
Institue safety precautions(use side rails,assist with
walking)if CNS,vision effects occur.
Provide frequent small meals if GI upset occurs
Control environment if sweating ,visual difficulties occur
Provide back rubs,positioning ,and other non drug measures
to alleviate pain.
Reassure patient about addiction liability;most patients who
receive opioids for medical reasons do not develop
dependence syndromes
Use caution when injecting IM or SC into
chilled areas or in patients with hypotension or
in shock,impaired perfusion may delay
absorption ;with repeated doses ;an excessive
amt.may be absorbed when circulation is
restored
Follow proper administration guidelines for IM
injections,including site rotation
SUMMARY
Opioids are a group of endogenous and
exogenous substances that act on receptors in
CNS & GIT.
All opioids share crucial chemical and
pharmacologic properties with morphine.
It provides effective analgesia and are used to
treat severe acute or chronic pain
REFERENCES
MEDICAL PHARMACOLOGY,8TH EDITION
BY KD TRIPATHI
WWW.DRUGBANK.CA
THANK YOU

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Opiod analgesics

  • 2. GENERAL OBJECTIVES • describe uses and types of opioids
  • 3. SPECIFIC OBJECTIVES • Define pain, pain pathways, types of pain • Types of analgesics • Mechanism of action • Indications • Contraindications • Adverse effects • Nursing responsibilities
  • 4. ALGESIA(PAIN):is an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage. ANALGESIC: A drug that selectively relieves pain by acting in the CNS or on peripheral pain mechanisms, without significantly altering consciousness
  • 6.
  • 7. TYPES OF PAIN ACUTE: It is of short duration but it gradually resolves as the injured tissue heal. E.g.injury or trauma CHRONIC: persistent pain that lasts week to years E.g. pain may be caused by inflammation or dysfunctional nerves.
  • 8. BASED ON ETIOLOGY NOCICEPTIVE PAIN: Result of activation of sensory(afferent)receptors (nociceptors)by mechanical, thermal, chemical stimuli Functional,physiologic or normal pain NEUROPATHIC PAIN: Pain resulting from damage to peripheral nervous or central nervous system tissue or from altered processing of pain in the CNS
  • 9. CLASSIFICATION Analgesics are divided into two groups: NSAIDS: Non opioid analgesics(mild to moderate pain) OPIOIDS: Severe pain
  • 14. DEFINITION: These are those substances used to treat moderate to severe pain They are sometimes called narcotics.
  • 15.
  • 17. OPIOID RECEPTORS Opioids exert their action by interacting with specific receptors present on neurons in CNS&peripheral tissue Radiological binding studies divided the opioid receptors into Each has a specific pharmacological profile,pattern of anatomic distribution in brain,spinalcord,peripheral tissues Opioid ligands can interact with diff.opioid receptor as agonist,partial agonist,competitive antagonist.
  • 19. Natural alkaloids Class of naturally occurring organic nitrogen containing bases. This includes compounds with neutral and even weakly acidic properties. Well known alkaloids include morphine,codeine.
  • 21. Strong analgesic Visceral pain is relieved better than somatic pain Degree of analgesia increase with dose Nociceptive pain is better relieved than neuretic pain Associated reactions are also relieved :apprehension,fear,autonomic effects Tolerance to pain is better
  • 22. Mechanism of action Two components:spinal &supraspinal Inhibits release of excitatory transmitters from primary afferents-at substantia gelatinosa of dorsal horn Exerted through interneurons-gating of pain At supra spinal level in cortex ,midbrain&medulla - alter processing and interpretation and send inhibitory impulses through descending pathways
  • 23. Pharmacologic actions 1.CNS a)analgesia b)sedation c)mood and subjective effects d)respiratory centre e)cough centre f)temperature regulating centre g)vasomotor centre 2.NEURO-ENDOCRINE
  • 24. 2)NEURO-ENDOCRINE 3)CVS 4)GIT 5)Other Smooth muscles a)biliary tract b)Urinary bladder c)Uterus d)Bronchi 6)ANS
  • 25.
  • 26. Adverse effects 1)Idiosyncrasy and allergy 2)Apnoea of newborn 3)Acute morphine poisoning 4)Tolerance and dependence 5)Others:Sedation,mental clouding,lethargy,respiratory dispersion
  • 27. SPECIFIC ANTIDOTE Naloxone-0.4-0.8mg i.v. repeated every 2-3 min till respiration picks up
  • 28. CONTRAINDICATIONS 1)Infants 2)Patient with respiratory insufficiency 3)Bronchial asthma 4)Head injury 5)Hypotensive states 6)Undiagnosed acute abdominal pain 7)Elderly male 8)Hypothyroidism
  • 30. Methyl morphine Converted to morphine by the body Partial agonist at µ opioid receptor with a low ceiling effect Available as : Tablets:15mg,30mg,60mg Oral solution:15mg/5ml Injection:30mg,60mg
  • 32. Symptoms of overdose Bluish lips or skin Chest pain or discomfort Constricted,pinpoint or small pupils Decreased awareness or responsiveness Extreme sleepiness or unusual drowsiness Slow or irregular heartbeat
  • 35. It is also known as diacetyl morphine or dia morphine. An illicit opioid synthesized from morphine that can be a white or brown powder or a black sticky substance The advantage of diamorphine over morphine is that diamorphine is more fat soluble and therefore more potent by inj.,so smaller doses of it are needed for the same effect on pain. Available forms: oral :5-10mg orally/IM/SC/IV repeated every 4 hourly Children : oral dose-0.6mg/kg/day, IV-0.01mg/kg/hr
  • 36. INDICATIONS Physical trauma (bone fractures) Myocardial infarction Post surgical pain Chronic pain End stage terminal illness
  • 37. ADVERSE EFFECTS Respiratory depression Collapsed vein –long term effect Dry mouth Drowsiness Impaired mental function Blood borne infection Pneumonia Addiction
  • 39. It’s a drug which is an opioid cough suppressant Helps suppress unproductive coughs and also has a mild sedative effect but has little or no analgesic effect. Its average half life is about 2.3 days Available form: oral solution: 5mg/5ml
  • 43. Its sold under the brand name hysingla Its an opioid used to treat severe pain of a prolonged duration It is also used as cough suppressant in adults It is sold as the combination of acetaminophen+hydrocodone / ibuprofen+hydrocodone Dosage :5mg/2.5mg hydrocodone/300mg or 325mg acetaminophen The typical dosage is 1-2 tablets taken every 4-6 hrs as needed
  • 44. ADVERSE EFFECTS Abuse Low blood pressure Seizures QT prolongation Respiratory depression Serotonin syndrome
  • 47. Its sold under brand name as oxycontin It is usually taken by mouth ,and is available in immediate release,controlled release formulations Onset of pain relief typically begins within 15 mins and lasts for upto 6 hrs. Dosage : 5mg immediate release form PO every 6 hrs.
  • 51. Chemically unrelated to morphine Interact with opioid receptor Well absorbed orally,bioavailability 50% Effects appear in 10-15 mins after oral absorption On parenteral administration,action lasts for 2-3 hrs Metabolized in liver-mepridinic acid and norpethidine Excreted in urine
  • 52. INDICATION Analgesics(substitute of morphine) Pre anaesthetic medication Analgesic during labour Dosage-50-100 mg IM/SC,Oral-50-100 mg tabs
  • 53. ADVERSE EFFECTS Similar to morphine Atropinic effect(dry mouth, blurred vision, tachycardia) Overdose-tremors,mydriasis, delirium, myoclonus, hyperreflexia, convulsions
  • 55. 80-100 Times more potent than morphine Fentanyl is 500 times more lipid soluble than morphine,that’s why it is rapidly distributed in the body because of high lipid solubility,it enters in brain rapidly and produce peak analgesia in 5min after i.v. injection Its elimination t1/2 =3.5 hrs Metabolized in liver in norfentanyl(inactive) Excreted in urine Dose- inj in 2& 10 ml ampoules containing 50mcg per ml
  • 56. Short acting analgesic during operative and perioperative period Skeletal muscle relaxant to selected high risk patient(those undergoing open heart surgery) Respiratory depression Transdermal fentanyl frequently used in cancer, terminal illness pain, chronic pain Oral route is not used due to high first pass metabolism INDICATION
  • 57. ADVERSE EFFECTS Redness and irritation on skin wherever apply the patch Dizziness Reduce cardiac contractility & HR Constipation
  • 59. Centrally acting analgesic Very low action on opioid receptors Effective both orally and i.v.(100mg=10mg morphine) Well tolerated and low abuse potential High oral bioavailability i.e.70-100% with repeated dosages due to reduction of first pass effect Metabolized in liver by demethylation Its elimination t1/2 =4-6hr DOSE-50-100 mg IV/IM/oral
  • 60. INDICATION Mild to moderate short lasting pain due to diagnostic procedure Pain due to Injury Post operative pain Chronic pain including cancer pain ( not effective in severe pain )
  • 61. ADVERSE EFFECT Similar to morphine but less prominent (vomiting , drowsiness) Sweating Lowering of seizure threshold(contraindicated in epileptics)
  • 63. Before beginning therapy,perform history regarding allergies,use of other medications,health history,and medical history Caution patient not to chew or crush controlled release preparations Keep opioid antagonist and equipment for assisted or controlled respiration readily available during iv administration
  • 64. Direct patient to lie down during IV administration Dilute and administer IV slowly to minimize likelihood of adverse effects Monitor injection sites for irritation ,ex-travasation Instruct postoperative pt.in pulmonary toilet;drug suppresses cough reflex Monitor bowel function and arrange for an thraquinone laxatives for severe constipation
  • 65. Institue safety precautions(use side rails,assist with walking)if CNS,vision effects occur. Provide frequent small meals if GI upset occurs Control environment if sweating ,visual difficulties occur Provide back rubs,positioning ,and other non drug measures to alleviate pain. Reassure patient about addiction liability;most patients who receive opioids for medical reasons do not develop dependence syndromes
  • 66. Use caution when injecting IM or SC into chilled areas or in patients with hypotension or in shock,impaired perfusion may delay absorption ;with repeated doses ;an excessive amt.may be absorbed when circulation is restored Follow proper administration guidelines for IM injections,including site rotation
  • 67. SUMMARY Opioids are a group of endogenous and exogenous substances that act on receptors in CNS & GIT. All opioids share crucial chemical and pharmacologic properties with morphine. It provides effective analgesia and are used to treat severe acute or chronic pain
  • 68. REFERENCES MEDICAL PHARMACOLOGY,8TH EDITION BY KD TRIPATHI WWW.DRUGBANK.CA