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Biochemistry > Target based drug discovery > Flashcards

Target based drug discovery Flashcards

1
Q

What is target based drug discovery?

A

This means that a certain biomolecule has been identified as problematic, and a drug will be developed to change its behaviour, with the aim of certain final effect.

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2
Q

What is pharmacokinetics?

A

Pharmacokinetics (How does the body deal with drugs?)
- Fate of drugs once they have been ingested
- Variability of response between patients
- How drugs move through the body in the processes of absorption, distribution, metabolism, and excretion - (ADME).

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3
Q

What is pharmacodynamics?

A

Pharmacodynamics (What effect drugs have on the body?)
- Is the study of how a drug binds to its binding site
- The drug not only has to bind to its target, it has to reach it in the first place
- For an oral drug that involves a long journey with many hazards to be overcome.

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4
Q

Drugs may be…

A
  • Acidic
  • Neutral
  • Basic
  • Small organic molecules
  • Large polymers
  • Other compounds with completed chemistries
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5
Q

What does the route of administration depend on?

A
  • Physical & chemical property of the drug (e.g. pH, solid, liquid, solubility)
  • Site of desired action – localised or generalised
  • Effect of digestive juices and first pass metabolism of drug
  • Accuracy of dosage required
  • Condition of the patient e.g. unconscious, vomiting, etc.
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6
Q

What are the different types of local routes?

A
  • Topical
  • Deeper tissue
  • Arterial supply
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7
Q

What are examples of topical administration?

A
  • Lotion
  • Cream
  • Spray
  • Drops
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8
Q

What are examples of deeper tissue administration?

A
  • Intra-articular (joint)
  • Intra-medullary (bone marrow or spinal cord)
  • Intrathecal pump (spinal fluid)
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9
Q

What are examples of arterial supply administration?

A
  • Angiography
  • Anti-cancer drugs
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10
Q

What is topical administration?

A

External application of the drug to the surface

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11
Q

What is deeper tissue administration?

A

Certain deep areas can be approached by syringe and neede

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12
Q

What is arterial supply administration?

A

Closed intra arterial injection

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13
Q

What are local routes?

A

When you put the drug where you want it to go.

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14
Q

What are systemic routes?

A

Getting the drug into the whole system

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15
Q

What are the different types of systemic routes?

A
  • Oral
  • Sublingual
  • Inhalation
  • Intradermal & subcutaneous
  • Intravenous
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16
Q

What is sublingual?

A
  • Kept under the tongue or crushed and spread over the mouth
  • Absorption through mucous membrane with good access to arteries
17
Q

What are the advantages od sublingual?

A
  • Rapid absorption (< 1 minute)
  • Liver is by passed – directly in the systemic circulation
  • Can be used on unconscious patients
18
Q

What are the disadvantages of sublingual?

A
  • Can only be lipid and saliva soluble drugs
  • Uncooperative patients
  • Irritate the mucosa
19
Q

What is intravenous?

A

Its injected directly into the vein

20
Q

What are the advantages of intravenous?

A
  • Quick action – good for emergencies
  • Desired concentration easily obtained
  • Doesn’t pass through the liver so it won’t be metbolised
  • Can be used on unconscious and uncooperative patients
  • Onset of action between 15-30 seconds.
21
Q

What are the disadvantages of intravenous?

A
  • Costly – special apparatus
  • Local irritation
  • Self medication not possible
  • Action cannot be stopped
  • Aseptic and antiseptic measures must be maintained
  • Extravasation (escape of drug into tissue )may cause severe irritation
22
Q

What are intradermal, subcutaneous, and intramuscular?

A

Other types of injections

23
Q

What is intradermal?

A
  • Least invasive
  • Involves getting into the layers between the skin
  • Used for testing allergies
  • Onset of action between 10-30 mins
24
Q

What is subcutaneous?

A
  • Deeper than intradermal
  • Below the skin but not reaching the muscle.
  • Used for insulin
  • Can be done themselves.
  • Onset of action between 10-30 mins
25
Q

What is intramuscular?

A
  • Deepest of the 3
  • Where RNA vaccines go
  • Onset of action between 10-30 mins
26
Q

What are the advantages of oral?

A
  • Self medication possible
  • Large area for absorption
  • Procedure simple- no additional cost
  • Slow action – safe for some risky drugs
  • Both solid and liquid forms of drugs can be administered
27
Q

What are the disadvantages of oral administration?

A
  • Irritant and unpalatable drugs cannot be administered
  • May induce nausea and vomiting
  • Not useful when vomiting and diarrhoea present
  • Or patient unconscious
  • Can be destroyed by gastric juices e.g. penicillin G and insulin
28
Q

What does Lipinski’s rule of 5 state?

A

States that in general an orally active compound has no more than one violation of the following criteria.
< 5 hydrogen bond donors (typically NH + OH)
< 10 hydrogen bond acceptors (all N and O atoms)
A molecular weight < 500
Octanol-Water partition coefficient (log P < 5)
P = [Aorg]/[Aaq]

Biochemistry (18 decks)

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