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PMP101 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What is pharmacology?

A

A branch of science that deals with the study of drugs and their actions on living systems.

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2
Q

What is a drug?

A

A chemical with a selective therapeutic action.

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3
Q

What is Pharmacodynamics (PD)?

A

What the drug does to the body.
Drug action and mechanisms.

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4
Q

What is Pharmacokinetics (PK)?

A

What the body does to the drug.
Barriers (ADME).

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5
Q

What is biological specificity?

A

Right target

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6
Q

What is chemical specificity?

A

Right target binding site.

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7
Q

What does the B1 receptor do?

A

Increases heart rate; Increasing cardiac muscle’s force of contraption.

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8
Q

What does the B2 receptor do?

A

Relaxes the airway.
Dilatate smooth muscles.

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9
Q

What do target binding sites provide?

A

The selectivity for the specific binding of drugs/ligands (LOCK and KEY system).

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10
Q

What are the 3 key drug binding sites?

A
  1. Drugs targeting enzymes.
  2. Drugs targeting transporters.
  3. Drug targeting voltage-gated ion channels.
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11
Q

Drugs as enzyme inhibitors.

A

Intracellular breakdown - phosphodiesterase- sildenafil.
Neurotransmitter degradation - acetylcholine esterase - neostigmine.
Messenger synthesis - cyclo-oxygenase - ibuprofen (reversable) aspirin (irreversible).

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12
Q

Drugs as enzyme substrates

A

dopamine precursor L-DOPA for Parkinson’s disease.

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13
Q

What is meant by competitive binding?

A

Drug competes for the ligand active site.

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14
Q

What is meant by non-competitive binding?

A

Drug binds at different site.

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15
Q

Therapeutic action

A

Biological: right target.
Chemical: right target binding site.

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16
Q

Adverse/Side effects

A

Biological: non-specific target.
Chemical: non-specific binding site.

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17
Q

What is an agonist?

A

A drug that binds to the same active site as adrenaline and activates the B2 like adrenaline.

18
Q

What is an antagonist?

A

Drugs that oppose the agonist function.
Block the B1 receptor.

19
Q

What is Affinity?

A

How well a drug/ligand binds to it’s receptor.

20
Q

What is Efficacy?

A

How well a drug/ligand activates the receptor.

21
Q

Do agonists have affinity and efficacy?

A

Agonists have both affinity and efficacy.

22
Q

Do antagonists have affinity and efficacy?

A

Antagonists only have affinity.
THEY PRODUCE NO RESPONSE.

23
Q

What is kD?

A

The concentration req. to occupy 50% of receptor.

24
Q

What is EC50?

A

The effective concentration of agonist for 50% response.

25
Q

Which is usually higher, affinity(kD) or potency(EC50)?

A

Affinity (kD).

26
Q

What is antagonism?

A

Drug/ligand that reduces/blocks the agonist response

27
Q

Name a type of antagonism?

A

Receptor antagonism

28
Q

Why do antagonists only have affinity?

A

Binds to receptors, Null response, i.e. blocks agonist response.

29
Q

Competitive antagonism.

A

Orthosteric - same binding site of the endogenous hormone.
Block the drug by occupying the B1 binding site.

30
Q

Non-competitive antagonism.

A

Blocks the response by by binding at a different binding site to the agonist.
No need for them to have identical structures.

31
Q

Reversable and non-reversable

A

Reversable can dissociate from the receptor and binding sites can be re-occupied.
Non-reversable antagonists cannot dissociate from the receptor.

32
Q

Reversable competitive antagonists

A

Max. response can still be achieved (surmountable antagonism).

33
Q

Irreversible competitive antagonists.

A

Form covalent link with receptor.
Reduces the number of receptors available for the agonist to stimulate the response.

34
Q

Non-surmountable antagonism

A

EC50 declines as receptor reserves decrease.
agonists maximum response drops.

35
Q

Receptor Tyrosine Kinase (RTK)

A

Receptors for growth factors (EGF, VEGF, Insulin etc.).
Activation: Cell proliferation, differentiation, survival and metabolism.
Hyperactivation: Polyps, tumours and cancer.

36
Q

Receptors for growth factors
EGF, VEGF, IGF, PDGF

A

Epidermal growth factor.
Vascular endothelial growth factor.
Insulin-like growth factor.
Platelet-derived growth factor

37
Q

RTK

A

Growth factor binding RTK leads dimerization and autophosphorylation

38
Q

RTK

A

One tyrosine kinase activates autophosphorylation of its partner and vice versa.
signalling proteins recruited to RTK.
Signalling proteins contains SH2 domain to sense and bind specific RTK.

39
Q

SH2 domain

A

some SH2 proteins are enzymes (phospholipase C)
Some SH2 domain proteins are adaptors (Grb2).

40
Q

RTK - drugs

A

Very limited
Insulin
Many neurotrophin analogues couldn’t pass through clinical trials.
Monoclonal antibodies.

41
Q

Guanynyl cyclase receptors

A

Limited membrane bound
released from atria, promotes vasodilation and urinary sodium excretion.

PMP101 (1 decks)

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