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Lernmaterialien für Pharma an der Medical University Varna

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TESTE DEIN WISSEN


Non-selective inhibitors of cyclooxygenase (СОХ)


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TESTE DEIN WISSEN

Acetyl-salicyl acid (ASA)

Ibuprofen

Diclofenac 

Naproxen


Lösung ausblenden
TESTE DEIN WISSEN


Opioid analgesics 



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TESTE DEIN WISSEN
  • agonists
    • natural
      • morphine hydrochloride/sulfate
      • codeine
    • semisynthetic
      • dihydrocodeine
    • synthtic
      • pethidine
      • fentanyl
      • tramadol
      • methadone
  • antagonists
    • naloxone
Lösung ausblenden
TESTE DEIN WISSEN

Analgesics antipyretics


Clinical use


Lösung anzeigen
TESTE DEIN WISSEN


􏰀 In fever (including in children and

pregnant women – paracetamol

􏰀 To reduce pain (toothache, headache, etc.)


Lösung ausblenden
TESTE DEIN WISSEN

Toxicological characteristics of morphine

  • ADR
  • contraindication
  • acute intoxication
Lösung anzeigen
TESTE DEIN WISSEN


ADR:

  • 􏰀  Respiratory depression )
  • 􏰀  Constipation (=Obstipation)
  • 􏰀  Nausea and vomiting
  • 􏰀  Sedation
  • 􏰀  Pruritus, urticaria, bronchospasm (histamine)
  • 􏰀  ↑ intracerebral pressure
  • 􏰀  Urine retention
  • 􏰀  Tolerance and dependence



Contraindication


  • Cranial trauma
  • Acute abdomen 
  • Bronchial asthma


Acute intox

  • 􏰀 Pinpoint pupils
  • 􏰀 Respiratory depression 
  • 􏰀 Coma → death
  • 􏰀 Treatment: naloxone IV



Lösung ausblenden
TESTE DEIN WISSEN


Other opioid analgesics

  • codeine
  • fentanyl
  • methadone
  • pethidine
  • tramadol
Lösung anzeigen
TESTE DEIN WISSEN

codeine

  • 􏰀  Better oral absorption and penetration in brain
  • 􏰀  Partial conversion to morphine (CYP2D6)
  • 􏰀  Less potent analgesic
  • 􏰀  Pronounced antitussive effect
  • 􏰀  Weaker dependence and respiratory depression
  • 􏰀  Contraindicated in children up to 12-18 years old (for cough)

fentanyl


  • 􏰀  Potent, but short acting analgesic
  • 􏰀  Routes of administration
    • 􏰀 By IV inj.(acute)
    • 􏰀 By transdermal patches (chronic)
    • 􏰀In the spinal canal in anesthesioogy
  • 􏰀  Clinical use
    • 􏰀 In malignant pain
    • 􏰀 In acute severe pain 
    • 􏰀 In surgery

Methadone


  • Long-lasting effect
  • Oral administration
  • Clinical use – replacement therapy of opioid dependence

Pethidine

  • 􏰀 Better oral bioavailability
  • 􏰀 Antimuscarinic(spasmolytic)effects 
  • 􏰀 Used in obstetrics (labor analgesic) 
  • 􏰀 ADR:
    • 􏰀 Excitement and convulsions (toxic metabolite) 
  • 􏰀 Adverse drug interactions with МАОI


Tramadol


  • 􏰀 A weaker analgesic
  • 􏰀 An opioid agonist and a blocker of SERT and NET
  • 􏰀 Good for post-surgical pain 
  • 􏰀 Better tolerated
    • 􏰀 Seizures are possible (toxic metabolite)



Lösung ausblenden
TESTE DEIN WISSEN


Dependence

of opioid analgesics

Lösung anzeigen
TESTE DEIN WISSEN


  • 􏰀 Psychological (addiction) – prominent in abuse
    • 􏰀  Irresistible desire to repeatedly experience the euphoric effects
    • 􏰀  The main factor hindering the attempts of treatment
    • 􏰀  It is rarely a problem with palliative care
  • 􏰀 Physical – pronounced
    • 􏰀 Abstinence syndrome in withdrawal with symptoms opposite of those of morphine
    • 􏰀 Abstinence can be provoked by opioid antagonists or partial agonist


Lösung ausblenden
TESTE DEIN WISSEN


Tolerance 

of opioid analgesics

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TESTE DEIN WISSEN


  • 􏰀 Rapid in development (days), but clinically manifested after 2-3 weeks
  • 􏰀  Dose escalation up to 30-50 fold in addicted persons
  • 􏰀  It is rarely a clinical problem (mostly a social phenomenon)
  • 􏰀  Cross tolerance (incomplete – allows switch to another analgesic)
  • 􏰀  Does not develop to: 
    • 􏰀 Miosis
    • 􏰀 Constipation


Lösung ausblenden
TESTE DEIN WISSEN


Cyclooxygenase(СОХ)


Lösung anzeigen
TESTE DEIN WISSEN


􏰀 The enzyme responsible for the production of prostanoids from AA 

􏰀 Types of COX

    - СОХ-1: constitutive enzyme, involved in the physiological functions of prostanoids:

        -> Prostaglandins (PGs E1/2, F2α) effects:
            􏰀 In the stomach: PGE ↓ gastric acid secretion 

            􏰀 In the uterus: PGE/F cause contraction
            􏰀 In the kidneys PGs E: cause natriuresis

􏰀 Prostacyclin (PGI2)
   - In vascular endothelium: vasodilation, inhibition of platelet aggregation

􏰀 Thromboxane А2 (TxA2)
   - In platelets: aggregation, vasoconstriction

􏰀 СОХ-2:

  • 􏰀  Mainly inducible form, expressed in inflammation:

       - PGs E – edema, reddening, pain

  • 􏰀  Involved also in normal homeostasis (e.g. in the vascular endothelium, kidney, bones, brain)


Lösung ausblenden
TESTE DEIN WISSEN


Pharmacokinetics of NSAIDs


Lösung anzeigen
TESTE DEIN WISSEN


Weak acids
􏰀 Routes of administration

   􏰀 Oral - well absorbed

   􏰀 Rectal
   􏰀 By injection
   􏰀 External

􏰀 Highly and tightly bound to plasma proteins 

      􏰀 Potential to displace other drugs

􏰀 Accumulation in synovial fluid
􏰀 Liver metabolism
􏰀 Urine/bile excretion
􏰀 Plasma half-life - variable (table)


Lösung ausblenden
TESTE DEIN WISSEN


ADRs to NSAIDs



Lösung anzeigen
TESTE DEIN WISSEN


􏰀 Frequent and predictable АDRs (due to COX inhibition)

  - GIT
      ->Gastric discomfort, nausea, ulcers 

       ->Bleeding

􏰀 Renal and cardiovascular

  • -  Sodium and water retention – worsening of hypertension, heart failure

  • -  Thrombotic events (coxibs)

  • -  Reversible acute RF (=rheumatic fever)

          -  „Analgesic nephropathy“ – with chronic, long-term (years) use

􏰀 Bronchoconstriction in „Aspirin- sensitive asthma“


􏰀 Relatively uncommon ADRs 

    - Hepatotoxicity

        -> Nimesulide

         -> ASA – “Ray syndrome” – liver impairment + encephalopathy (in children with viral infections)


􏰀 CNS - ASA at high doses

􏰀 Bone marrow suppression

􏰀 Hypersensitivity reactions


Lösung ausblenden
TESTE DEIN WISSEN

Analgesics antipyretics

Mechanism of action

Lösung anzeigen
TESTE DEIN WISSEN



􏰀Central СОХ inhibition?
􏰀 Other possible mechanisms –

interaction with:

   - Endocannabinoid system

   - Opioid system

   - NO, monoaminergic, cholinergic systems


Lösung ausblenden
TESTE DEIN WISSEN


Clinical use of NSAIDs


Lösung anzeigen
TESTE DEIN WISSEN


􏰀 Inflammatory conditions of the motor system and associated pain

􏰀 Acute or chronic pain of low to modest intensity – headache, toothache, dysmenorrhea, trauma, post-surgery pain


􏰀 In fever – ASA and ibuprofen
􏰀 Prevention of arterial thrombosis (AMI, stroke) –ASA at low doses



Lösung ausblenden
  • 16624 Karteikarten
  • 147 Studierende
  • 5 Lernmaterialien

Beispielhafte Karteikarten für deinen Pharma Kurs an der Medical University Varna - von Kommilitonen auf StudySmarter erstellt!

Q:


Non-selective inhibitors of cyclooxygenase (СОХ)


A:

Acetyl-salicyl acid (ASA)

Ibuprofen

Diclofenac 

Naproxen


Q:


Opioid analgesics 



A:
  • agonists
    • natural
      • morphine hydrochloride/sulfate
      • codeine
    • semisynthetic
      • dihydrocodeine
    • synthtic
      • pethidine
      • fentanyl
      • tramadol
      • methadone
  • antagonists
    • naloxone
Q:

Analgesics antipyretics


Clinical use


A:


􏰀 In fever (including in children and

pregnant women – paracetamol

􏰀 To reduce pain (toothache, headache, etc.)


Q:

Toxicological characteristics of morphine

  • ADR
  • contraindication
  • acute intoxication
A:


ADR:

  • 􏰀  Respiratory depression )
  • 􏰀  Constipation (=Obstipation)
  • 􏰀  Nausea and vomiting
  • 􏰀  Sedation
  • 􏰀  Pruritus, urticaria, bronchospasm (histamine)
  • 􏰀  ↑ intracerebral pressure
  • 􏰀  Urine retention
  • 􏰀  Tolerance and dependence



Contraindication


  • Cranial trauma
  • Acute abdomen 
  • Bronchial asthma


Acute intox

  • 􏰀 Pinpoint pupils
  • 􏰀 Respiratory depression 
  • 􏰀 Coma → death
  • 􏰀 Treatment: naloxone IV



Q:


Other opioid analgesics

  • codeine
  • fentanyl
  • methadone
  • pethidine
  • tramadol
A:

codeine

  • 􏰀  Better oral absorption and penetration in brain
  • 􏰀  Partial conversion to morphine (CYP2D6)
  • 􏰀  Less potent analgesic
  • 􏰀  Pronounced antitussive effect
  • 􏰀  Weaker dependence and respiratory depression
  • 􏰀  Contraindicated in children up to 12-18 years old (for cough)

fentanyl


  • 􏰀  Potent, but short acting analgesic
  • 􏰀  Routes of administration
    • 􏰀 By IV inj.(acute)
    • 􏰀 By transdermal patches (chronic)
    • 􏰀In the spinal canal in anesthesioogy
  • 􏰀  Clinical use
    • 􏰀 In malignant pain
    • 􏰀 In acute severe pain 
    • 􏰀 In surgery

Methadone


  • Long-lasting effect
  • Oral administration
  • Clinical use – replacement therapy of opioid dependence

Pethidine

  • 􏰀 Better oral bioavailability
  • 􏰀 Antimuscarinic(spasmolytic)effects 
  • 􏰀 Used in obstetrics (labor analgesic) 
  • 􏰀 ADR:
    • 􏰀 Excitement and convulsions (toxic metabolite) 
  • 􏰀 Adverse drug interactions with МАОI


Tramadol


  • 􏰀 A weaker analgesic
  • 􏰀 An opioid agonist and a blocker of SERT and NET
  • 􏰀 Good for post-surgical pain 
  • 􏰀 Better tolerated
    • 􏰀 Seizures are possible (toxic metabolite)



Mehr Karteikarten anzeigen
Q:


Dependence

of opioid analgesics

A:


  • 􏰀 Psychological (addiction) – prominent in abuse
    • 􏰀  Irresistible desire to repeatedly experience the euphoric effects
    • 􏰀  The main factor hindering the attempts of treatment
    • 􏰀  It is rarely a problem with palliative care
  • 􏰀 Physical – pronounced
    • 􏰀 Abstinence syndrome in withdrawal with symptoms opposite of those of morphine
    • 􏰀 Abstinence can be provoked by opioid antagonists or partial agonist


Q:


Tolerance 

of opioid analgesics

A:


  • 􏰀 Rapid in development (days), but clinically manifested after 2-3 weeks
  • 􏰀  Dose escalation up to 30-50 fold in addicted persons
  • 􏰀  It is rarely a clinical problem (mostly a social phenomenon)
  • 􏰀  Cross tolerance (incomplete – allows switch to another analgesic)
  • 􏰀  Does not develop to: 
    • 􏰀 Miosis
    • 􏰀 Constipation


Q:


Cyclooxygenase(СОХ)


A:


􏰀 The enzyme responsible for the production of prostanoids from AA 

􏰀 Types of COX

    - СОХ-1: constitutive enzyme, involved in the physiological functions of prostanoids:

        -> Prostaglandins (PGs E1/2, F2α) effects:
            􏰀 In the stomach: PGE ↓ gastric acid secretion 

            􏰀 In the uterus: PGE/F cause contraction
            􏰀 In the kidneys PGs E: cause natriuresis

􏰀 Prostacyclin (PGI2)
   - In vascular endothelium: vasodilation, inhibition of platelet aggregation

􏰀 Thromboxane А2 (TxA2)
   - In platelets: aggregation, vasoconstriction

􏰀 СОХ-2:

  • 􏰀  Mainly inducible form, expressed in inflammation:

       - PGs E – edema, reddening, pain

  • 􏰀  Involved also in normal homeostasis (e.g. in the vascular endothelium, kidney, bones, brain)


Q:


Pharmacokinetics of NSAIDs


A:


Weak acids
􏰀 Routes of administration

   􏰀 Oral - well absorbed

   􏰀 Rectal
   􏰀 By injection
   􏰀 External

􏰀 Highly and tightly bound to plasma proteins 

      􏰀 Potential to displace other drugs

􏰀 Accumulation in synovial fluid
􏰀 Liver metabolism
􏰀 Urine/bile excretion
􏰀 Plasma half-life - variable (table)


Q:


ADRs to NSAIDs



A:


􏰀 Frequent and predictable АDRs (due to COX inhibition)

  - GIT
      ->Gastric discomfort, nausea, ulcers 

       ->Bleeding

􏰀 Renal and cardiovascular

  • -  Sodium and water retention – worsening of hypertension, heart failure

  • -  Thrombotic events (coxibs)

  • -  Reversible acute RF (=rheumatic fever)

          -  „Analgesic nephropathy“ – with chronic, long-term (years) use

􏰀 Bronchoconstriction in „Aspirin- sensitive asthma“


􏰀 Relatively uncommon ADRs 

    - Hepatotoxicity

        -> Nimesulide

         -> ASA – “Ray syndrome” – liver impairment + encephalopathy (in children with viral infections)


􏰀 CNS - ASA at high doses

􏰀 Bone marrow suppression

􏰀 Hypersensitivity reactions


Q:

Analgesics antipyretics

Mechanism of action

A:



􏰀Central СОХ inhibition?
􏰀 Other possible mechanisms –

interaction with:

   - Endocannabinoid system

   - Opioid system

   - NO, monoaminergic, cholinergic systems


Q:


Clinical use of NSAIDs


A:


􏰀 Inflammatory conditions of the motor system and associated pain

􏰀 Acute or chronic pain of low to modest intensity – headache, toothache, dysmenorrhea, trauma, post-surgery pain


􏰀 In fever – ASA and ibuprofen
􏰀 Prevention of arterial thrombosis (AMI, stroke) –ASA at low doses



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