Pharmacology Flashcards

1
Q

What are the 4 types of molecular targets?

A
  1. Transporter proteins
  2. Ion channels
  3. Enzymes
  4. Receptors
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2
Q

What are the 4 types of receptors?

A
  1. Ligand gated
  2. G-protein coupled
  3. Catalytic
  4. Nuclear
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3
Q

How do agonist drugs work?

A

They produce a functional response in the same way as an endogenous agonist.

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4
Q

What do antagonist drugs do?

A

They block the binding sites.

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5
Q

What does EC50 refer to?

A

Potency - the drug concentration at which the drug produces 50% of the maximal response.

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6
Q

Optimal therapeutic effect is seen between — to — % drug concentration.

A

20 to 80

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7
Q

What 5 factors effect absorption?

A
Absorption surface
Blood flow
Solubility of the drug
Ionisation
Formulation
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8
Q

What is the approximate pH of the stomach?

A

2

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9
Q

Why is the duodenum more alkaline than the stomach?

A

The pancreas secretes bicarbonate ions into the duodenum.

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10
Q

Acids in a basic environment become ——- and won’t move across ——— easily.

A

ionised

membranes

(and vice versa)

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11
Q

Most absorption occurs in the ——–

A

intestines.

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12
Q

What is the first pass effect?

A

Percentage of hepatic excretion of an oral drug prior to it reaching the systemic circulation.

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13
Q

Define drug distribution.

A

Irreversible transfer of a drug from one location to another.

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14
Q

What 6 factors effect drug distribution?

A
Blood flow
Cardiac output 
Organ/ tissue perfusion
Lipid solubility
Presence of drug transporters
Plasma protein binding
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15
Q

Other than protein-binding, what tissues can drugs bind to?

A

Bone matrix and adipose tissue.

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16
Q

What 4 mechanisms are involved in drug clearance?

A

Kidney excretion
Biliary/ faecal excretion
Hepatic metabolism
Pulmonary excretion

17
Q

What are the two main ways that drugs are metabolised?

A

Functionalisation and conjugation

18
Q

What is functionalisation?

A

One of the ways drugs are metabolised.

Enzymes, usually of the P450 family, are added to the drug which makes them more water soluble.

19
Q

What is conjugation?

A

One of the ways a drug is metabolised.

A chemical group present in the drug is added to the polar group of an endogenous substance.

20
Q

What is the role of genetics in metabolism?

A

Genes are required for enzyme production to metabolise drugs.

21
Q

What are the 3 ways in which the kidneys eliminate drugs?

A

Filtration
Reabsorption
Secretion

22
Q

What is enzyme induction, and why is it significant?

A

Increased expression of enzyme protein. (ie., one drug can increase production of another enzyme).

Can result in increased metabolism of another drug.

23
Q

What is enzyme inhibition, and why is it significant?

A

Two drugs competing for the same enzyme.

Results in decreased metabolism of at least one of them.

24
Q

What is hepatic uptake?

A

Drug has to enter hepatocytes to undergo metabolism.

25
Q

What is enterohepatic cycling?

A

Drug and drug metabolites present in bile that enter duodenum become available for reabsorption.

26
Q

Define half-life.

A

The time taken for the plasma drug concentration to fall by one half (50%).

27
Q

What 2 factors influence half-life?

A

Distribution and clearance.