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MD1010 > CTL week 9 > Flashcards

CTL week 9 Flashcards

1
Q

sources of drugs?

A

sources of drugs?

  • microorganism
  • plants
  • animals
  • minerals
  • synthesised in laboratories.
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2
Q

what is the difference between the Approved and Proprietary name of a drug?

A

what is the difference between the Approved and Proprietary name of a drug?

Answer:
Approved -> generic name (non-capital letters)
Proprietary -> brand/trade name

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3
Q

what is the molecular target of drugs?

A

what is the molecular target of drugs?

Answer:

  • Proteins (R.I.C.E) [Receptors, Ion-channels, Carriers, Enzymes]
  • nucleic acids
  • miscellaneous targets.
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4
Q

an Agonist drug possess ?

A

an Agonist drug that possess ?

Answer: high Affinity and Efficacy for the receptor

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5
Q

an antagonist drug possess ?

A

an antagonist drug that possess ?

Answer: high affinity but no efficacy. It blocks the receptor

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6
Q

what is an Allosteric Modulators?

A

what is an Allosteric Modulators?

Answer: binds to modulatory site on receptor and either increases or inhibits the response.

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7
Q

what is the name for a drug that inhibits ion flow in ion-channels?

A

what is the name for a drug that inhibits ion flow in ion-channels?

Answer: Blockers

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8
Q

GABA is what kind of transmitter?

A

GABA is what kind of transmitter?

Answer: an antagonists that opens Chlorine channels to cause the membrane to hyperpolarize, thus relaxing.

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9
Q

3 kinds of drugs used by enzymes?

A

3 kinds of drugs used by enzymes?

  • Inhibitor
  • False substrate, converted to something else.
  • Pro-drug, is converted by enzyme into active form.
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10
Q

2 kinds of drugs for Carrier molecules (transporters)

A

2 kinds of drugs for Carrier molecules (transporters)

Answer:

  • drugs that inhibit transport
  • drugs that act as false substrates
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11
Q

molecular targets for drugs (extended version)?

hint: LCDMSG

A

molecular targets for drugs (extended version)?

Lipid components of cell membrane (genral anaesthetics)
Cell surface proteins 
DNA nuclei acids (chemotherapy) 
Metal ions 
Structural proteins (like tubulin)
Gastrointestinal contents (antacids)
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12
Q

what are the 4 classes of receptors?

what kind of molecules (neurotransmitter/hormones) bind to which receptors?

A

what are the 4 classes of receptors?

  • Ligand-gated ion channels (exp: nicotinic, GABA, Glutamate, 5-HT3)
  • G-protein coupled receptors (exp: muscarinic, adrenoceptors, dopamine, opioid, 5-HT)
  • Kinase-linked receptors (exp: cytokines, insulin, leptin, GH, IGF-1)
  • nuclear receptors (exp: Oestrogen, steroids, Thyroid hormones)
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13
Q

what are the receptors for Epinephrine and Norepinephrine?

A

Epinephrine and Norepinephrine receptors are?

α1, α2, β1, β2

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14
Q

what are the receptors for Acetylcholine?

A

what are the receptors for Acetylcholine?

Answer: Muscarinic and nicotinic

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15
Q

_________ is the study of the interaction between a drug and its molecular target and the pharmacological response.

A

___Pharmacodynamics______ is the study of the interaction between a drug and its molecular target and the pharmacological response.

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16
Q

_____ measure of the ability of drug to bind to a receptor?

A

___Affinity___ measure of the ability of drug to bind to a receptor?

17
Q

_____ ability of a drug, once bound to a receptor, to activate the receptor and produce a pharmacological response.

A

___Efficacy___ ability of a drug, once bound to a receptor, to activate the receptor and produce a pharmacological response.

18
Q

are Efficacy and Affinity related?

A

are Efficacy and Affinity related?

Answer: no

19
Q

the concentration that produces a certain pharmacological response is?

A

the concentration that produces a certain pharmacological response is?

Answer: potency (and it is determined by both Efficacy and Affinity).

The more potent the drug, the lower the concentration required to produce a big impact.

20
Q

what is EC50?

A

what is EC50?

Effective concentration: the concentration of agonist which produces 50% of the maximal response. The lower the EC50, the more potent the drug

21
Q

what is the difference between full and partial agonist?

A

what is the difference between full and partial agonist?

Answer:
full agonist has high efficacy
low agonist has low efficacy (will never reach max response even at high concentrations)
(note: full and partial agonist can have same affinity)

22
Q

does an antagonist have an effect on the constitutive activity?

A

does an antagonist have an effect on the constitutive activity?

Answer: No, but it inhibits the effect of an agonist.

23
Q

what is constitutive activity?

A

what is constitutive activity?

Answer: the continuous activity of receptors even in the absence of ligand.

24
Q

what is an inverse agonist?

A

what is an inverse agonist?

Answer: it decreases constitutive activity.

25
Q

Reversible competitive antagonism are?

A

Reversible competitive antagonism are?

Answer:

  • Compete with agonist to bind to receptor.
  • Increasing the concentration of the agonist will overcome the antagonist effect.
  • Result, the log curve is pushed to the right
26
Q

Irreversible competitive antagonism are?

A

Irreversible competitive antagonism are?

answer:
- Forms a strong chemical bond with receptor.
- Cannot be broken (increasing agonist concentration will not overcome antagonist).
- Result, reduces the response of the receptor.

27
Q

non-competitive agonist are?

A

non-competitive agonist are?

Answer:
Bind to allosteric site
Inhibit agonist from producing effect
Are not surmountable

28
Q

is Drug specificity concentration-dependent?

A

is Drug specificity concentration-dependent?

answer: Yes
At low concentration it will act on specific receptors.
At high concentrations it will act on other receptors or other cells.

29
Q

Effects of a drug will often lessen if given continuously because?

(hint: ChIA PIE)

A

Effects of a drug will often lessen if given continuously because?

Answer: 
Change in receptors 
Internalization of receptors 
Active extrusion of drug from cells 
Physiological adaptation 
Increased drug breakdown 
Exhaustion of mediators

MD1010 (40 decks)

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