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PHARMACOLOGY > PMOC M3 > Flashcards

PMOC M3 Flashcards

magaral

1
Q

 Compound of significant pharmacological activity [API] - need makuha yung desirable effect but not always

A
  1. Finding the Lead
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2
Q

6 parts in Finding the Lead

A
  1. Choose a disease
  2. Choose a drug target
  3. Identify a bioassay
  4. Find[identify] a ‘lead compound’
  5. Isolate and purify the lead compound if necessary
  6. Determine the structure of the lead compound if necessary
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2
Q

Ways to discover a LEAD compound:

A

1.Natural Products Screening
2. Medical Folklore
3. Screening Synthetic Compound Libraries

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3
Q

 Ancient people used ——- products as drugs - however, many of the products were very ——–

A

natural toxic

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4
Q

banned in Paris on 1566

A

Tartar emetic

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5
Q

 The search to find less toxic substances than those based on natural sources resulted in the introduction of synthetic substances as drugs

A

LEADS API

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6
Q

 Compound of significant pharmacological activity [API] - need makuha yung desirable effect but not always

A

Finding the Lead

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7
Q

Market first then science follows

A
  1. Choose a disease
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8
Q
  • A huge investment has to be made in the research and development of a new drug
A
  1. Choose a disease
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9
Q
  1. Choose a disease
    Considerations:
A
  • Economic – kikita k aba sa paggawa ng drugs na ito
  • Medical – if you know the disease ano yung gamot for it [therapeutic use]
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10
Q
  • You know the target you will know the applicable medication
A
  1. Choose a drug target
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11
Q
  • An understanding of which biomacromolecules are involved in a particular disease state is clearly important.
A
  1. Choose a drug target
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12
Q
  • The test should be simple, quick, and relevant, as there are usually a large number of compounds to be analyzed.
A
  1. Identify a bioassay
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13
Q
  • Human testing is not possible at such an early stage
A
  1. Identify a bioassay
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14
Q

do not involve live animals

A

In vitro Tests

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15
Q

specific tissues, cells, or enzymes are used

A

In vitro Tests

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16
Q

Often needed to check whether drugs have the desired pharmacological activity and also to monitor their pharmacokinetic properties.

A

In vivo tests

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17
Q

On animals often involve inducing a clinical condition in the animal to produce observable symptoms

A

In vivo tests

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18
Q
  • Lead compound is a compound which shows the desired pharmacological activity
    o Leads - has desirable effect
  • has undesirable effect
  • The lead compound provides a start for the drug design and development process.
A
  1. Find[identify] a ‘lead compound’
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19
Q

o Most biologically active natural products are secondary metabolites with quite complex structures and several chiral centers

A
  1. Natural Products Screening
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20
Q

o The study of medicines derived from natural sources is known as

A

pharmacognosy in Natural Products Screening

21
Q

pharmacognosy sources

A
  • Plants
  • Microorganisms [antibiotic ex penicillin and cephalosporin]
  • Marine life [aquatic samples ex tilapia can rejuvenate your skin]
  • Animals
  • Venoms and toxins.
22
Q

o Traditional/folkloric claims [medical herms to explore as therapeutic use]

A
  1. Medical Folklore
23
Q

o Companies will research further/explore the mini research of a person kasi sila maybadget

A
  1. Screening Synthetic Compound Libraries
24
Q

o Pharmaceutical companies often try to diversify their range of structures by purchasing novel compounds prepared by research groups elsewhere.

A
  1. Screening Synthetic Compound Libraries
25
Q

o Pharmaceutical companies often screen their library of compounds whenever they study a new target.

A
  1. Screening Synthetic Compound Libraries
26
Q

“Me too” and “Me Better” Drugs

A
  1. Existing Drugs
27
Q

Revise the compound to make it better

A
  1. Existing Drugs
28
Q

Many companies use established drugs from their competitors as lead compounds

A
  1. Existing Drugs
29
Q
  • AIM: To modify the structure sufficiently such that it avoids patent restrictions, retains activity, and, ideally, has improved therapeutic properties.
A
  1. Existing Drugs
30
Q

Captopril is example in ——- then explain

A

Existing Drugs
* Captopril has incompatibilities that cause GI disturbance/ irritation in stomach lining
* So kung maiimprove at matatangal ang GI disturbance na ito the drug will become much better
* Walang nalalabag na law/ or copy right

31
Q

 Benzodioxanes is example in ——- then explain

A

 Benzodioxanes major action is on the nervous system but it can also inhibit histamine receptor [having effect on the histamine1 receptor that will effect as anti-allergy] that will produce Ethanolamine, and from Ethanolamine na produce si Ethylenediamines [effect ay anti-allergy]
 They modify the stracture of Ethanolamine that came from Benzodioxanes to produce Diphenhydramine there for na produce yung anti-allergy therefore it will prevent the production of histamine/ prevent allergic reaction
 Produce and revise result in the Ethylenediamines then produce Tripelennamine use as anti-allergy it is same function but different drug
 But the 2 drug has side effect which is drowsiness which is not good but you can use a therapeutic use for sleeping which is anesthetic
 From that you can produce Promethazine [anesthetic agent] then revise and produce Chlorpromazine [Tranquilizer]

32
Q

o Molecular modelling software programs can be used to study the binding site and to design molecules which will fit and bind to the site (de novo drug design)

A

Computer-aided Design

33
Q

o binding site is important para doon magfit yung substate + active site = enzyme
o need ng courses of attraction in the binding side [so need iidentify yung binding site]

A

Computer-aided Design

34
Q

define different bonding

A
  1. Ionic Bond – opposite charge / nitrogen
  2. Hydrogen Bond - OH group
  3. Van der waals – Carbon / non-polar
35
Q

o Accidental drugs discovery / chance discovery
- Ex. Penicillin

A

Serendipity

36
Q

o Frequently, lead compounds are found as a result of serendipity (i.e. chance).

A

Serendipity

37
Q
  • Isolated and purified which of those components would be your API
A

Isolate and purify the lead compound if necessary

38
Q
  • If the lead compound (or active principle) Is present in a mixture of compounds from a natural source or a combinatorial synthesis, it has to be isolated and purified because you need to remove the toxic substance to pure substance.
A

Isolate and purify the lead compound if necessary

39
Q
  • Structure determination is a relatively straightforward process and it is only when the natural product is obtained in minute quantities that a full synthesis is required to establish its structure.
A

Determine the structure of the lead compound if necessary

40
Q

– NEED TO TRANSFOR INTO CRYSTALINE FORM
o requires & suitable crystal of the sample

A

X-ray crystallography
Determine the structure of the lead compound if necessary

41
Q

– BEST USE
o used more commonly in the Philippines, as it can be carried out on any sample, whether it be a solid, oil, or liquid.

A

NMR spectroscopy
Determine the structure of the lead compound if necessary

42
Q

 raw materials guaranty to have a desirable effect and there properties to be modify therefore in modification of the compound trying to the drug designing.

A

Drug Design

43
Q

METHODS Drug Design

A
  1. Identify structure-activity relationships (SARS)
  2. Identify the pharmacophore
  3. Improve target interactions (pharmacodynamics)
  4. Improve pharmacokinetic properties
44
Q
  • relationship of how structural features of the molecule contribute to, or take away from, the desired biologic activity
A

1) Structure Activity Relationship (SAR)

45
Q
  • Kailangan mag fit ng neurotransmitter doon sa binding site that will apply the —-
  • So dapat mag fit yung structure ng gamot mo and yung structure ng target mo
A

1) Structure Activity Relationship (SAR)

46
Q
  • AIMS of this is to Identify those part of the molecule that are importance in the biological activity and those are not active [titignan kung ano yung magkakaroon ng activity and non activity]
A

1) Structure Activity Relationship (SAR)

47
Q
  • SAR Studies are essential in ——-
A

drug optimization

48
Q

2 SAR Studies are essential in drug optimization

A

o to find analogues with better activity and selectivity
o remember Pharmacodynamics – powerful and selective enough

49
Q
  • summarizes the important binding groups that are required for activity, and their relative positions in space with respect to each other.
  • Not modify as it is na yun
A

2) Pharmacophore

50
Q
  • Pharmacodynamics optimization
  • Pharmacokinetic optimization
  • We want to enhance the intramolecular bonds within the target in order for a drug to powerful and selective enough
A

3) Drug Optimization

51
Q

Explain Drug development

A

Drug discovery, Drug design, Drug trials [phase1,2,3,4] , Drug manufacturing/process

PHARMACOLOGY (16 decks)

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