Pharmacokinetics Flashcards

1
Q

What is pharmacokinteticse

A

The effect the body has on the drug

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2
Q

What is pharmacodynamics

A

The effect the drug has on the body

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3
Q

The amount of drug which reaches the site of action depends on what?

A
  • Rate of absorption of drug
  • Rate of distribution around the body
  • Rate of metabolism by the body
  • Rate of excretion by the body
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4
Q

What is the rate of passive diffusion dependent on?

A
  • Solubility of lipid
  • area of the membrane
  • magnitude of concentration gradient across the membrane
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5
Q

Are non-ionised lipid soluble?

A

Yes

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6
Q

Are ionised lipid soluble?

A

No - relatively lipid insoluble

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7
Q

What does a drugs relative proportions (amount of non-ionised drug) depend on?

A

Drug’s intrinsic tendency to ionise & pH of solution

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8
Q

Why do most drugs not ass through the cell membrane via diffusion through aqueous pore?

A

Most drug molecules are too large

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9
Q

What is the paracellular route for drugs to enter a cell?

A

Diffusion through intercellular pores for larger drugs and large proteins e.g. insulin

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10
Q

What molecules enter a membrane via carrier-mediated transport?

A

Relatively insoluble lipids e.g. amino acids, sugars & neurotransmitters.

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11
Q

What factors influence the rate of dissolution?

A
  • particle size
  • pH conditions
  • dosage form
  • influences of additives
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12
Q

Why in inhaltion of anaesthetic likely to cause systemic effects?

A

They are lipophilic molecules that are readily absorbed by passive diffusion through the lungs

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13
Q

What is the absorption of anaesthetic gases dependent on?

A
  • rate of entry to tissues
  • solubility
  • rates of pulmonary blood flow
  • rates of respiration
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14
Q

Where is inhaled anaesthetic excreted?

A

Lungs??

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15
Q

When/ where is percutaneous administration quickest?

A
  • Where skin is thinnest
  • warming skin
  • hydrated skin
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16
Q

Why must drugs be lipid soluble to diffuse quickly into the brain?

A
  • CNS is protected by blood-brain barrier:
  • CNS surrounded by specialised barrier which is an obstacle to the penetration of hydrophilic substances
  • Endothelial cells in the brain do not have intercellular pores but have tight junctions
  • Glial cells associated with capillaries in the brain are another barrier to the diffusion of non-lipid soluble molecules.
17
Q

What is the main factor that influences the rate of drug distribution?

A

How well the molecule crosses the membrane

18
Q

What is a drug interaction?

A

when one drug displaces another drug from a protein it was bound to

19
Q

What protein do most drugs bound to?

A

Albumin (produed by liver)

20
Q

What is meant by drug metabolism?

A

When the body attempts to transform drugs into hydrophilic (water soluble) substance which are usually less pharmacologically active and can be excreted via urine and bile.

21
Q

Name all the organs involved in drug metabolism

A
  • LIVER
  • skin
  • lings
  • kidneys
  • intestine
22
Q

Can drug interactions can occur during drug metabolism?

A

Yes - the metabolism of one drug may affect the metabolism of another drug.

23
Q

Is the metabolite always less pharamolcogically active than the parent compound?

A

No-once metabolised, metabolite is usually less pharmacologically active but can be more active than parent compund can lead to toxicity.

24
Q

What are the 2 phases of drug metabolism?

A

Phase I - chemically reactive groups are added or uncovered (and used up)
Phase II - addition of pharamologically inactive groups (for conjugation reaction)

25
Q

What factors effect the rate of metabolism?

A
  • Genetics
  • Physiological - age
  • Disease -e.g. liver disease
  • Environmental (previous exposure to drug& smoking)
26
Q

How are drugs excreted?

A
  • The liver via hepatic metabolism which secretes them into bile which is secreted in faeces
  • Kidneys play a central role in the excretion of most drugs & metabolites
27
Q

Describe the renal excretion process

A
  • Glomerular filtration: unbound drugs fraction of drug is filtered
  • Active secretion: of acids and bases from plasma. (Active mechanism put in place so drug can be transported against the con. gradient)
  • Resorption: most drugs are subjected to some resorption
28
Q

Why are older people more likely to suffer from drug toxicity?

A

-Declining renal function = glomerular filtration is impaired = poor drug excretion= high drug levels in blood

29
Q

How else can drugs be excreted?

A

Sweat, tears, saliva & lungs