Pharmacokinetics 1 Flashcards

1
Q

What is pharmacokinetics? Why is it important?

A

What the body does to the drug. It is important as is will vary hugely in patients. It can identify drug interaction, predict the influence of diseases of drugs.

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2
Q

What does (L)ADME stand for? and what is it?

A

Liberation, Absorption, Distribution, Metabolism and Excretion. It is the 4/5 steps of pharmacokinetics

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3
Q

What are the advantages and disadvantages of oral route?

A

A - Convenient and safe.

D - First-pass effect, many variables and barriers

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4
Q

What are the advantages and disadvantages of sublingual route?

A

A - No first pass effect.

D - inconvenient, small dose limit and taste.

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5
Q

What are the advantages and disadvantages of Inhalation route?

A

A - Fast, rapid delivery to blood.

D - Requires special properties of drug

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6
Q

What are the advantages and disadvantages of topical route?

A

A - convenient, localised.

D - only localised

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7
Q

What are the advantages and disadvantages of transdermal route?

A

A - Prolonged release.

D - The skin is a very effective barrier

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8
Q

What are the advantages and disadvantages of intramuscular route?

A

A - rapid for aqueous, slow for oil.

D - painful and requires a trained professional.

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9
Q

What are the advantages and disadvantages of intravenous route?

A

A - direct, total dose and rapid.

D - Requires professional, injection risk and rapid response (Risk of anaphalxis)

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10
Q

What is bioavailabilty?

A

It is the fraction of unchanged drug that reaches the systemic circulation. IV bioavailability = 100% but oral can vary.

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11
Q

What are the four ways small molecules can cross cell membranes?

A
  • Diffusing directly through lipid.
  • Diffusing through aqueous pores.
  • Transmembrane carrier protein.
  • Pinocytosis (endocytosis of small molecules)
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12
Q

Features of hydrophilic and lipophilic drugs

A

Hydrophilic - soluble in aqueous, polar media.

Lipophilic - Soluble in fats and non-polar solutions so can pass through membranes

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13
Q

The ratio of ionised to unionised drugs depends on what? What pH are weak acids/bases less likely to become ionised in?

A

The pH.
- Weak acis are less likely to become ionised in acidic environments. A weak base is more likely to become ionised in an acid environment. (ionised drugs cannot cross membranes)

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14
Q

What are the main properties that affect drug absorption?

A

Lipophilicity and ionisation

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15
Q

What factors affect distribution?

A

Degree of drug ionisation

Lipid solubility

pH of compartments

Cardiac output and blood flow (low BF then less drug travailing to tissue)

Capillary permability

Plasma binding protein.

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16
Q

What is the compartment model?

A

The central compartment (compartment 1) consists of the plasma and tissues where the distribution of the drug is practically instantaneous. The peripheral compartment (compartment 2) consists of tissues where the distribution of the drug is slower.

17
Q

What are Bisphosphonates used to treat?

A

Osteoporosis

18
Q

What do phosphonates have a high affinity for?

A

Calcium so they are quickly distributed to the skeleton and can be stored there so you do not often need to give the injections.

19
Q

Name the main plasma proteins drugs bind to

A

Albumin (main one) but also Alpha-1 acid glycoprotein

lipoproteins

Globulins.

20
Q

Competition for binding sites can cause?

A

Big increases in free drug concentrations

21
Q

Describe the effects of aspirin on warfarin?

A

Aspirin and warfarin are weak bases so they can only bind to one site on albumin. Aspirin has a high affinity for albumin so can displace warfarin, increasing the amount of unbound warfarin in the body.

22
Q

The distribution of drugs between compartments in the body depends on?

A

Tissue and drug dependent factors.

23
Q

How can side effects of drugs be minimised

A

Limiting their distribution via the route of administration

24
Q

What are the clinical uses of bethanechol?

A

Bladder and GI hypotonia