Drugs Pharma an der Universität Jena | Karteikarten & Zusammenfassungen

Lernmaterialien für Drugs Pharma an der Universität Jena

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Nondepolarizing neuromuscular blockers

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  • For muscle relaxation in tracheal intubation and surgical anesthesia
  • assisted respiratory always necessary
  • highly water soluble(quarternary nitrogen)—> excreted via urine
  • Substances: Tubocurarine, Rocuronium
Lösung ausblenden
TESTE DEIN WISSEN
Succinylcholin
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TESTE DEIN WISSEN
=suxamethonium
  • depolarising blocker
  • agonist for nicotinic Ach-receptor
  • short term muscle relaxation: onset 2 min, duration 5-10 min —> in anesthesia and intensive care, facilitation of endotracheal intubation
  • Quickly degraded by plasma butyrylcholinesterase
  • blockage prolonged by decreased concentration of butyrylcholinesterase because of liver desease, pragnancy or age
  • blockage prolonged by genetic variants of butyrylcholinesterase
  • side effects:
    • muscle pains due to unsynchronized contractions of muscle fibres before onset of paralysis
    • sinus bradycardia+ dysrhythmias
    • Hyperkalemia(elevated level of potassium in blood)
    • malignant hyperthermia
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TESTE DEIN WISSEN

What are side effects of ligands for β3 receptors?

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TESTE DEIN WISSEN
  • example Mirabegron/ Vibebegron (β3 agonist/ detrusor muscle relaxation in bladder): infections of the urethra, tachycardia, increased blood pressure (as β1 heart may be targeted)


=generally, β3 ligands lack specificity (β3 over β1) àcardiovascular side effects: Tachycardia

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TESTE DEIN WISSEN

Bladder: important receptors/ location/ function 

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TESTE DEIN WISSEN

SNS: 

- M. detrusor: b3 (causes dilation to allow filling) 

-internal urethral spincter: a1 (keep liquid)


PNS: 

- M. detrusor: m3 (causing contration to allow emptying) 



- skeletal muscle: nAChR (voluntary control)

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TESTE DEIN WISSEN
Tubocurarine
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TESTE DEIN WISSEN
  • blocker of nicotinic Ach-receptor—> no depolarisation
  • Called nondepolarizing neuromuscular blocker
  • competetive
  • quarternary ammonium binds carboxylgroup (Glu, Asp)
  • Assisted respiratory necessary
Lösung ausblenden
TESTE DEIN WISSEN

Yohimbine

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TESTE DEIN WISSEN
  • Targets α2-adrenoceptor as Antagonist =increases NE/E signaling at the synapse
    1. influences the catecholaminergic synapse: acts as adrenergic receptor agonist as indirect sympatholytic
  • Found in the bark of the African tree pausinystalia yohimbe and is commercially sold with the slogan “longer life, better sex”: used as a used as aphrodisiac and for erectile dysfunction
  • Ingredient in many weight loss products, no proven effect on weight loss though
  • Passes BBB: when entering the CNS it causes an increased Noradrenalin, Serotonin and Dopamin release > psychotic effect, increased heart rate and blood pressure, can cause severe tremors

          >severe side effects

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TESTE DEIN WISSEN

Levomethamphetamine 

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TESTE DEIN WISSEN


  • there are different types of Amphetamines: Amphetamine, Methamphetamine (Crystal: improved BBB permeability used in 2nd world war to increase alertness/ concentration and decrease fatigue/appetite and Levomethamphetamine (reduced potential for euphoria and addiction)
  • Levomethamphetamine is a different stereoisomere than Meth (less effective [dopamine] rise)


>influences the catecholaminergic synapse: False substrates for plasma membrane and vesicular transporters (like all Amphetamines)


  • can be available as therapeutic drug (such as a vapor inhaler as nasal decongestant)


Lösung ausblenden
TESTE DEIN WISSEN

Dantrolene

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TESTE DEIN WISSEN
  • ryanodine receptor antagonist
  • inhibita calcium release from SR
  • myotrop muscle relaxant --> reduced contraction
  • treatment of malignant hyperthermia, spasticity
Lösung ausblenden
TESTE DEIN WISSEN

Botulinum toxin (Botox)

Lösung anzeigen
TESTE DEIN WISSEN
  • binds to nerves that use Ach--> endocytosis, then released into cytosol of synaptic endings
  • light chain acts as an endoprotease to degrade SNAREs(synaptic fusion complex does not form) -->reduction in the amount of Ach --> reduction of muscle activity
  • BTX injections useful for diseases with incoluntary muscle activity: strabismus, facial spasm, stuttering
  • botulism=intoxication with toxin -->muscle paralysis
Lösung ausblenden
TESTE DEIN WISSEN

Amphetamine

Lösung anzeigen
TESTE DEIN WISSEN
  • influences the catecholaminergic synapse: False substrates for plasma membrane and vesicular transporters
    1. transported into the presynapse via NET (and DAT) (NET/DAT are responsible for removal of catecholamines from the synaptic cleft)
    2. Inhibition of Norepinephrine uptake into vesicles by VMAT (vesicular monoamine transporter)
    3. makes plasma membrane transporters operate in opposite direction
    4. non-exocytotic release of NA, DA (monoamines)
    5. Increased Norepinephrine + Dopamine concentrations in the synaptic cleft
  •   their derivates also occur naturally (Amphetamine, Ephedrine, Cathione) (while Methamphetamines are synthetic)


Lösung ausblenden
TESTE DEIN WISSEN
Nicotin
Lösung anzeigen
TESTE DEIN WISSEN
  • Non-specific nAch-receptor agonist
  • highly toxic(lethal dosis 60mg-1g)
  • Can also be regarded as antagonist—> stimulates ganglia, then blocks due to desensitization of the receptor
  • low dose:stimulating effects on sympathetic and parasympathetic system and on CNS
    • stimulates adrenal glands to produce epinephrine(symp.)
      • increased heart rate and blood pressure (constriction of blood vessels)
      • increased degradation of fats and glycogen
      • increased basal energy rate
    • stimulates motility of gastointestinal system(parasymp.)
    • dopamine production-->> anxiety relief, enhanced attention& memory
    • reduced appetite, nausea
Lösung ausblenden
TESTE DEIN WISSEN

Tyramine 


Lösung anzeigen
TESTE DEIN WISSEN
  • drug that influences the catecholaminergic synapse by acting as false substrates for plasma membrane and vesicular transporters
  • Unable to pass the BBB (only non-psychoactive peripheral sympathomimetic effects)
  • Tyramine are biogenic amines, which are normally metabolized by MAO (monoamine oxidase)
    1. in different foods, e.g. cheese. („Tyros“ greek word for cheese))
  • Increased uptake can cause migraine
  • Ingestion of cheese can cause „tyramine crisis“, if patients take MAO inhibitors (which degrade catecholamines) > it can lead to increased systolic blood pressure
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  • 65562 Karteikarten
  • 1426 Studierende
  • 87 Lernmaterialien

Beispielhafte Karteikarten für deinen Drugs Pharma Kurs an der Universität Jena - von Kommilitonen auf StudySmarter erstellt!

Q:
Nondepolarizing neuromuscular blockers

A:
  • For muscle relaxation in tracheal intubation and surgical anesthesia
  • assisted respiratory always necessary
  • highly water soluble(quarternary nitrogen)—> excreted via urine
  • Substances: Tubocurarine, Rocuronium
Q:
Succinylcholin
A:
=suxamethonium
  • depolarising blocker
  • agonist for nicotinic Ach-receptor
  • short term muscle relaxation: onset 2 min, duration 5-10 min —> in anesthesia and intensive care, facilitation of endotracheal intubation
  • Quickly degraded by plasma butyrylcholinesterase
  • blockage prolonged by decreased concentration of butyrylcholinesterase because of liver desease, pragnancy or age
  • blockage prolonged by genetic variants of butyrylcholinesterase
  • side effects:
    • muscle pains due to unsynchronized contractions of muscle fibres before onset of paralysis
    • sinus bradycardia+ dysrhythmias
    • Hyperkalemia(elevated level of potassium in blood)
    • malignant hyperthermia
Q:

What are side effects of ligands for β3 receptors?

A:
  • example Mirabegron/ Vibebegron (β3 agonist/ detrusor muscle relaxation in bladder): infections of the urethra, tachycardia, increased blood pressure (as β1 heart may be targeted)


=generally, β3 ligands lack specificity (β3 over β1) àcardiovascular side effects: Tachycardia

Q:

Bladder: important receptors/ location/ function 

A:

SNS: 

- M. detrusor: b3 (causes dilation to allow filling) 

-internal urethral spincter: a1 (keep liquid)


PNS: 

- M. detrusor: m3 (causing contration to allow emptying) 



- skeletal muscle: nAChR (voluntary control)

Q:
Tubocurarine
A:
  • blocker of nicotinic Ach-receptor—> no depolarisation
  • Called nondepolarizing neuromuscular blocker
  • competetive
  • quarternary ammonium binds carboxylgroup (Glu, Asp)
  • Assisted respiratory necessary
Mehr Karteikarten anzeigen
Q:

Yohimbine

A:
  • Targets α2-adrenoceptor as Antagonist =increases NE/E signaling at the synapse
    1. influences the catecholaminergic synapse: acts as adrenergic receptor agonist as indirect sympatholytic
  • Found in the bark of the African tree pausinystalia yohimbe and is commercially sold with the slogan “longer life, better sex”: used as a used as aphrodisiac and for erectile dysfunction
  • Ingredient in many weight loss products, no proven effect on weight loss though
  • Passes BBB: when entering the CNS it causes an increased Noradrenalin, Serotonin and Dopamin release > psychotic effect, increased heart rate and blood pressure, can cause severe tremors

          >severe side effects

Q:

Levomethamphetamine 

A:


  • there are different types of Amphetamines: Amphetamine, Methamphetamine (Crystal: improved BBB permeability used in 2nd world war to increase alertness/ concentration and decrease fatigue/appetite and Levomethamphetamine (reduced potential for euphoria and addiction)
  • Levomethamphetamine is a different stereoisomere than Meth (less effective [dopamine] rise)


>influences the catecholaminergic synapse: False substrates for plasma membrane and vesicular transporters (like all Amphetamines)


  • can be available as therapeutic drug (such as a vapor inhaler as nasal decongestant)


Q:

Dantrolene

A:
  • ryanodine receptor antagonist
  • inhibita calcium release from SR
  • myotrop muscle relaxant --> reduced contraction
  • treatment of malignant hyperthermia, spasticity
Q:

Botulinum toxin (Botox)

A:
  • binds to nerves that use Ach--> endocytosis, then released into cytosol of synaptic endings
  • light chain acts as an endoprotease to degrade SNAREs(synaptic fusion complex does not form) -->reduction in the amount of Ach --> reduction of muscle activity
  • BTX injections useful for diseases with incoluntary muscle activity: strabismus, facial spasm, stuttering
  • botulism=intoxication with toxin -->muscle paralysis
Q:

Amphetamine

A:
  • influences the catecholaminergic synapse: False substrates for plasma membrane and vesicular transporters
    1. transported into the presynapse via NET (and DAT) (NET/DAT are responsible for removal of catecholamines from the synaptic cleft)
    2. Inhibition of Norepinephrine uptake into vesicles by VMAT (vesicular monoamine transporter)
    3. makes plasma membrane transporters operate in opposite direction
    4. non-exocytotic release of NA, DA (monoamines)
    5. Increased Norepinephrine + Dopamine concentrations in the synaptic cleft
  •   their derivates also occur naturally (Amphetamine, Ephedrine, Cathione) (while Methamphetamines are synthetic)


Q:
Nicotin
A:
  • Non-specific nAch-receptor agonist
  • highly toxic(lethal dosis 60mg-1g)
  • Can also be regarded as antagonist—> stimulates ganglia, then blocks due to desensitization of the receptor
  • low dose:stimulating effects on sympathetic and parasympathetic system and on CNS
    • stimulates adrenal glands to produce epinephrine(symp.)
      • increased heart rate and blood pressure (constriction of blood vessels)
      • increased degradation of fats and glycogen
      • increased basal energy rate
    • stimulates motility of gastointestinal system(parasymp.)
    • dopamine production-->> anxiety relief, enhanced attention& memory
    • reduced appetite, nausea
Q:

Tyramine 


A:
  • drug that influences the catecholaminergic synapse by acting as false substrates for plasma membrane and vesicular transporters
  • Unable to pass the BBB (only non-psychoactive peripheral sympathomimetic effects)
  • Tyramine are biogenic amines, which are normally metabolized by MAO (monoamine oxidase)
    1. in different foods, e.g. cheese. („Tyros“ greek word for cheese))
  • Increased uptake can cause migraine
  • Ingestion of cheese can cause „tyramine crisis“, if patients take MAO inhibitors (which degrade catecholamines) > it can lead to increased systolic blood pressure
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