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Lernmaterialien für Pharma an der Medical University Varna

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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

Indications of opioid analgesics


Lösung anzeigen
TESTE DEIN WISSEN


Pains of high intensity:

  • malignant pain
  • post surgical pain
  • other pain syndromes
    • trauma, burns
    • labor
    • AMI (acute myocardial infarction)
    • Biliary / renal colic

Other indications

  • dry-non-productive cough
    • codeine
  • Cardiac asthma (morphine, IV)
    • Venodilation
    • soothing the over-irritated respiratory center
    • disputavle benefit
  • diarrhea- peripheral agonists
    • loperamide
Lösung ausblenden
TESTE DEIN WISSEN

Piascledine 


Lösung anzeigen
TESTE DEIN WISSEN

Antibacterial & inflamm. drugs

-avocado soya extract 

-antiinflamm.

Lösung ausblenden
TESTE DEIN WISSEN

Angiotensin converting enzyme inhibitors (ACEIs )

(prils)

Lösung anzeigen
TESTE DEIN WISSEN
  • ​enalapril
  • perindopril
  • lisinopril
  • ramipril
Lösung ausblenden
TESTE DEIN WISSEN


Opioid analgesics 



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


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

PD of opioid analgesics

  • central effects
  • peripheral effects
  • phenomena associated with chronic administration
Lösung anzeigen
TESTE DEIN WISSEN

Central effects

  •  Analgesia
  •  Euphoria
  •  Respiratory depression 
  •  Sedation
  •  Miosis (pupil constriction)
  •  Cough suppression
  • Endocrine effects
    •  ↑ ADH, prolactin
    •  ↓ FSH, LH; CRH (=corticotropin-releasing hormone)
  •  Immunosuppression



Peripheral effects

  •  Constipation
  •  Spasmogenic effects on biliary and urinary tract, urinary bladder
  •  Histamine release – itching, bronchoconstriction (in asthmatic patients)



Phenomena associated with chronic

administration

  •  Tolerance
  •  Dependence (psychological and physical)




Lösung ausblenden
TESTE DEIN WISSEN

Dobutamine (B1 selective agonist)

(=synthetic catecholamine)

  • PK
  • PD
  • clinical use
  • ADR
Lösung anzeigen
TESTE DEIN WISSEN

PK

  • IV infusion

PD

  • Effects:
  • Cardiac stimulation
    ◦ (+)inotropiceffect
    ◦ (+)bathmotropiceffect

clinical use

  • Cardiogenic shock
  • Acute heart failure


ADR

  • Arrhythmia
  • ↑ myocardial O2 consumption



Lösung ausblenden
TESTE DEIN WISSEN

Calcium Channel blockers (calcium antagonists)

-non-dihydropyridines

Lösung anzeigen
TESTE DEIN WISSEN

Verapamil

Lösung ausblenden
TESTE DEIN WISSEN

Antithrombotic Drugs

Fibrinolytics

Lösung anzeigen
TESTE DEIN WISSEN

Streptokinase

Lösung ausblenden
  • 29858 Karteikarten
  • 254 Studierende
  • 18 Lernmaterialien

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

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:

Indications of opioid analgesics


A:


Pains of high intensity:

  • malignant pain
  • post surgical pain
  • other pain syndromes
    • trauma, burns
    • labor
    • AMI (acute myocardial infarction)
    • Biliary / renal colic

Other indications

  • dry-non-productive cough
    • codeine
  • Cardiac asthma (morphine, IV)
    • Venodilation
    • soothing the over-irritated respiratory center
    • disputavle benefit
  • diarrhea- peripheral agonists
    • loperamide
Q:

Piascledine 


A:

Antibacterial & inflamm. drugs

-avocado soya extract 

-antiinflamm.

Q:

Angiotensin converting enzyme inhibitors (ACEIs )

(prils)

A:
  • ​enalapril
  • perindopril
  • lisinopril
  • ramipril
Q:


Opioid analgesics 



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


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)



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:

PD of opioid analgesics

  • central effects
  • peripheral effects
  • phenomena associated with chronic administration
A:

Central effects

  •  Analgesia
  •  Euphoria
  •  Respiratory depression 
  •  Sedation
  •  Miosis (pupil constriction)
  •  Cough suppression
  • Endocrine effects
    •  ↑ ADH, prolactin
    •  ↓ FSH, LH; CRH (=corticotropin-releasing hormone)
  •  Immunosuppression



Peripheral effects

  •  Constipation
  •  Spasmogenic effects on biliary and urinary tract, urinary bladder
  •  Histamine release – itching, bronchoconstriction (in asthmatic patients)



Phenomena associated with chronic

administration

  •  Tolerance
  •  Dependence (psychological and physical)




Q:

Dobutamine (B1 selective agonist)

(=synthetic catecholamine)

  • PK
  • PD
  • clinical use
  • ADR
A:

PK

  • IV infusion

PD

  • Effects:
  • Cardiac stimulation
    ◦ (+)inotropiceffect
    ◦ (+)bathmotropiceffect

clinical use

  • Cardiogenic shock
  • Acute heart failure


ADR

  • Arrhythmia
  • ↑ myocardial O2 consumption



Q:

Calcium Channel blockers (calcium antagonists)

-non-dihydropyridines

A:

Verapamil

Q:

Antithrombotic Drugs

Fibrinolytics

A:

Streptokinase

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