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Semester 5- Pharmacology > 2.2 Pharmacodynamics, DDIs and Toxicology > Flashcards

2.2 Pharmacodynamics, DDIs and Toxicology Flashcards

1
Q

What are the 4 principal classes of receptor site?

A

Receptors
Ion channels
Carriers/transporters
Enzymes

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2
Q

What is the active state?

A

Receptor which carries out a specific task

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3
Q

What is the inactive state?

A

Not active- no receptor activation

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4
Q

What is an agonist?

A

Ligand which binds to a receptor to move it into the active state

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5
Q

What is an antagonist?

A

Ligand which binds to a receptor but keeps it in the inactive state

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6
Q

What is a partial agonist?

A

Ligand bound to a receptor but the receptor action is not at 100%

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7
Q

What is a partial antagonist?

A

Ligand bound to a receptor and the receptor action is low but not at 0%

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8
Q

What is the affinity of a drug?

A

The tendency of a drug to bind to a specific receptor type

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9
Q

What is the efficacy of a drug?

A

The maximal effect of a drug when bound to a receptor

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10
Q

What is the agonist potency?

A

The drug concentration at which 50% of the maximal response is obtained

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11
Q

What is the antagonist potency?

A

Concentration of the drug which reduces maximal response by 50%

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12
Q

What is the therapeutic window?

A

The concentration range at which drugs produce a clinically useful effect without exerting toxic effects.

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13
Q

How can DDIs affect the absorption of a drug?

A

Oral drugs can be affected by drugs which alter gut motility and passive absorption

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14
Q

How can DDIs affect the distribution of a drug?

A

Can be affected by competition of drugs at protein/lipid binding sites.

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15
Q

How can DDIs affect the metabolism of a drug?

A

Affected by induction or inhibition of enzymes in the liver

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16
Q

How can DDIs affect the elimination of a drug?

A

Affected by changes in protein binding, inhibition of tubular secretion and changes in urine/pH

17
Q

What does inhibition of CYP450 enzymes do to a drug’s half life?

A

Increases

18
Q

What does induction of CYP450 enzymes do to a drug’s half life?

A

Decreases

19
Q

What does inhibition of CYP450 enzymes do to a drug’s clearance?

A

Decrease

20
Q

What does induction of CYP450 enzymes do to a drug’s clearance?

A

Increase

21
Q

How can DDIs be useful?

A

Some DDIs can enhance the clinical effects of a specific drug

22
Q

Give 5 classes of drugs that have common DDIs

A 
Anticonvulsants
Anticoagulants
Antidepressants
Antibiotics
Antiarrhythmics
23
Q

How does renal disease affect drug pharmacology?

A

Reduction in clearance of renally excreted drugs

Some drugs are nephrotoxic or can create electrolyte imbalances

24
Q

How does hepatic disease affect drug pharmacology?

A

Reduced metabolism of drugs in the liver causing the half lives of the drugs to increase

25
Q

How does cardiac disease affect drug pharmacology?

A

Falling cardiac output leads to lower organ perfusion so metabolism in the liver and clearance in the kidneys is reduced.

26
Q

How does hypoalbuminaemia affect drug pharmacology?

A

Less albumin means there are less drug binding sites so the free drug concentration is in a higher concentration

27
Q

What is an ‘on-target’ ADR?

A

An exaggerated therapeutic effect, usually caused by a drug working on the same receptor in a different area of the body

28
Q

What is an ‘off-target’ ADR?

A

Drugs reacting with other receptor types to the one intended
When a build up of metabolites become toxic

29
Q

Give 6 examples of CYP450 inducers

A 
Phenytoin 
Carbamazepine 
Rifampicin 
Alcohol (Chronic)
Barbiturates
Sulphonylureas
30
Q

Give 8 examples of CYP450 inhibitors

A 
Omperazole
Disulfiram 
Erythromycin 
Valproate
Isoniazid
Ciprofloxacin 
Ethanol 
Sulphonamides

Semester 5- Pharmacology (12 decks)

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