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Year 2 LCRS Pharmacology > 2+3: Drug Receptor+ Drug mechanics > Flashcards

2+3: Drug Receptor+ Drug mechanics Flashcards

1
Q

What does Pharmacokinetics discribe?

A

What the body does to/with the drug

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2
Q

Wht does Pharmacodynamics discribe?

A

What the drug does the the body (what the effect is)

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3
Q

What are the prinicpal target sited of drugs?

A

Proteins:

  • Receptors
  • Ion channels
  • Transport systems
  • Enzymes
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4
Q

Which signals does a receptor respond to?

A
  • Neurotransmitters
  • Hormones
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5
Q

Where are receptors located

A

Type 1-3: in cell membrane (usually)

Type 4: intracellular steroid receptors

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6
Q

Which Sub-Types of Receptors are there?

A
  1. Type 1: ionotropic (ion channel linked)
  2. Type 2: G-protein coupled
  3. Type 3: Kinase linked
  4. Type 4: intracellular steroid receptors
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7
Q

What are the characteristics of a Type 1 receptor?

A

Ionotropic receptors (ion channel coupled)

  • very fast response (milli sec.)
  • e.g. nAChR, GABA
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8
Q

Which type of receptor is an ionotrypic receptor?

A

Type 1

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9
Q

Whar are the characteristics of a Type 2 receptor?

A

G-protein coupled –> set off intracellular messenger system

  • seconds of response
  • e.g. ß1 adrenergic receptor in heart
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10
Q

What are the characteristics of a Type 3 receptor?

A

Kinase linked

  • response within minutes
  • e.g. insulin, Growth factor
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11
Q

Whar are the characteristics of Type 4 receptors?

A

Intracellular steroid hormones

  • regulate DNA transcription
  • response within hours
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12
Q

Which signals does an ion chanel respond to?

Which example drugs target ion channels?

A
  1. Change in voltage (voltage gated)
  2. Receptor binding (Receptor linked)

e.g. Local Anesthetics, Calcium channel blockers

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13
Q

How can transport systems be exploited as drug target?

A

By blocking transport systems that transport substanced against their concentration gradient ( are specific for substance + ATP dependant)

  • e.g. Neurotransmitter uptake (blocking of reuptake of Noradrenaline used in antidepressants)
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14
Q

In which ways can drugs target Ezymes?

A
  1. Enzyme inhibitors
    • inhibit enzyme action and slows reaction down
  2. False substrate
    • Derivate von enzym substaten lassen “False transmitters” entstehen (e.g. Methylnoradrenaline from Methyldopa which has a less powerful effect)
  3. Produgs
    • umwandlung des Medikaments durch Enzym
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15
Q

What is a False transmitter? What is a true transmitter?

A

False transmitter: Transmitter that closely immitates the action of a transmitter but act a bit different

  • e.g. Methyldopa (False transmitter) giving Methylnoradrenaline binding weaker to target –> causing muscle relaxation
  • DOPA would be the true transmitter
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16
Q

What are Non-specific drug actions?

A

Drugs that work via theit physiochemical properties

  • anitacids (bases)
  • osmotic purgatives (abführmittel)
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17
Q

What is an agonist?

A

Something that enhances receptor action

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18
Q

What is an antagonist?

A

Something that blocks/ decreased receptor action

19
Q

Which factors does the potency of a drug depend on?

A
  1. Affinity –> how strong/easy does the drug bind to the target
  2. Efficacy –> how strong is the effect of the drug on the target
20
Q

What is the Affinity of a Drug?

A

How strongly/easy the drug binds to its target

21
Q

What is teh effecacy of a drug?

A

How strong the effect is on the target

(e.g. conformatin change in receptor)

22
Q

What are the characteristics of a full agoinst?

A

It binds to and activate a receptor with the maximum response that an agonist can elicit at the receptor

23
Q

Whar are the charcteristics of a partial agonist?

A

Bind to and activate the receptor but only have a partial efficacy in comparison to full agonist

–> can have antagonist property in presence of a full agonist

24
Q

What is the selectivity of a drug?

A

How selective the drug is to its target (will be overlap, often resulting in side-effects)

25
Q

What does the structure-activity relationship descibe?

A

Small changes in structure can have major effects on results (because of lock-and key modell)

26
Q

Descibe/draw a dose-response curve of a full agonist in comparison to a partial agonist

A
27
Q

Describe /draw how a log- dose response curve of a full agonist with high efficacy, full agonist with low efficacy and partial agonist would look like

A
28
Q

How efficiant are antagonist?

A

Not at all –> have affinity but no efficacy (don’t do anything)

29
Q

What two types of Antagonists are there?

A
  1. Competitive
    • same binding site as substrate
    • Shifts Dose-response curve to the right
    • surmountable (überwindbar bei hohen Substratkonenztrationen)
  2. Irreversible
    • different binding site or binds tighly
    • –> incativate enzyme/receptor
30
Q

What are the characteristivs of competitive antagonist binding?

A

Competitive

  • same binding site as substrate
  • Shifts Dose-response curve to the right
  • surmountable (überwindbar bei hohen Substratkonenztrationen)
31
Q

What are the characteristics of irreversible antagonsit binding?

A

Irreversible

  • different binding site or binds tighly
  • –> incativate enzyme/receptor
  • insurmountable (unüberwindbar bei hohen Substratkonzentration)
32
Q

How would a log dose response curve look like in presence of

  • agonist alone
  • with competitve agonist
  • with irreversible agonist
A
33
Q

Explain the concept of receptor blockage antagonism

A

Competitive binding or Irreversible binding

34
Q

Through which mechanisms can a drug act as an antagonist?

A
  1. Receptor blockage
    • competitive
    • irreversible
  2. Physiological antagonism
    • opposite effect in same tissue
  3. Chemical antagonism
    • reduces concentration of agonist by forming chemical complexes
  4. Pharmacokinietic antagonism
    • reduce concentration by: decreasing absorbtio, increasing metabolism/excretion
35
Q

Explain the conecegt of physiological antagonism

A

A drug has the opposite effect as the agonist in the same tissue

e.g. Noradrenaline is an antagonist of histamine in blood vessel (dilation vs. constriction)

36
Q

Explain the conept of chemical antagonism

A

Antagonist reduces concentration by reducing formin chemical complex with agonist

e.g. Dimercaprol with heavy metals

37
Q

Explain the concept of pharmacokinetic antagonism

A

decrease concentration of agonist at site of action by

  • decreasing absorbtion
  • increasing excretion
  • increasing metabolism
38
Q

What is drug tolerance?

A

A gradual decrease to drug afer longer time of administration

39
Q

Which concepts can lead to drug tolerance?

A
  1. Pharmacokinetic factors
    • adaptive increase in metabolism (e.g. enzymes)
  2. Receptor loss/increase
  3. Change in receptor (desensitisation)
  4. Exhaution of mediator store
  5. Physiological adaption (to side effects)
40
Q

Explain the concept of pharmacokinetic in drug tolerance

A

Ther ecan be an adaptive increase in drug metabolites etc. e.g. enzmyes

41
Q

Explain the concept of receptor loss/increase with drug tolerance

A

Receptors can be lossed by plasma endocytosis

less receptors —> less action

42
Q

What happens at receptor desensitzation in drug tolerances?

A

Conformation change in receptor leading to desensitization

43
Q

Explain the concept or exhaution of mediator site in the context of drug tolerance

A

E.g. Amphitamines cause release of amines

–> Amine storages get exhaused –> can’t be released

44
Q

Explain the concept of physiological adaptation in the context of drug tolerance

A

it is a homeostatic response

often a tolerance to the drug side effects

Year 2 LCRS Pharmacology (38 decks)

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