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Pharmacology basic knowledge > PED2001 Absorption > Flashcards

PED2001 Absorption Flashcards

1
Q

What does ADME stand for?

A

Absorption, Distribution, Metabolism, Excretion

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2
Q

How do drug molecules primarily move around the body?

A

Through bulk flow and diffusion

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3
Q

What is bulk flow in the context of drug transport?

A

Transport through the bloodstream, lymphatics, cerebrospinal fluid, or GI tract

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4
Q

What factors influence diffusion of drug molecules?

A

Molecular size and lipid solubility

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5
Q

What is the significance of aqueous diffusion?

A

Crucial for drug transport, especially for large MW drugs

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6
Q

What is the diffusion coefficient dependent on?

A

1/SQR of molecular weight (MW)

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7
Q

What is the typical molecular weight range for small molecules that can pass through compartments easily?

A

200-1000 kDa

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8
Q

What are the three ways small molecules cross the cell membrane?

A
  • Diffusing directly through the lipid
  • Combination with solute carrier (SLC) or other membrane transporter
  • Diffusing through aqueous pores formed by membrane glycoproteins (AQPs)
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9
Q

What is pinocytosis?

A

The process of invagination of the cell membrane to trap extracellular constituents in a vesicle

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10
Q

True or False: Nonpolar molecules can dissolve freely in membrane lipids.

A

True

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11
Q

What determines the rate of permeation across a membrane?

A

Permeability coefficient and concentration difference

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12
Q

What is the partition coefficient?

A

Expresses solubility for a substance distributed between the membrane phase and aqueous environment

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13
Q

What does diffusivity measure?

A

Mobility within the lipid, expressed as a diffusion coefficient

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14
Q

What is ‘ion trapping’?

A

The process where ionisation and membrane permeability affect drug permeation and steady state distribution

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15
Q

What is the Henderson-Hasselbalch equation used for?

A

To determine the ratio of ionised to unionised forms of weak acids or bases depending on pH

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16
Q

What effect does urinary acidification have on weak bases?

A

Accelerates excretion

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17
Q

What is the primary role of carrier-mediated transport?

A

Regulate entry and exit of important molecules across cell membranes

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18
Q

What are ATP-binding cassette (ABC) transporters?

A

Membrane proteins that couple substrate transport to ATP hydrolysis

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19
Q

What is the role of P-glycoprotein (P-gp)?

A

To protect the body against xenobiotics and regulate drug transport

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20
Q

What is the main function of BSEP (Bile Salt Export Pump)?

A

Transport bile salts across the canicular membrane of hepatocytes

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21
Q

What condition is associated with mutations in the ABCC2 gene?

A

Dublin Johnson syndrome

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22
Q

What are the implications of BCRP (Breast Cancer Resistance Protein) in drug transport?

A

Secretion of xenobiotics into milk, affecting breast-fed infants

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23
Q

What do SLC transporters primarily do?

A

Facilitate the transport of a variety of substrates across cell membranes

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24
Q

What types of transporters exist within SLC transporters?

A
  • Facilitative transporters
  • Secondary active transporters
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25
Q

What is the role of MRP1 (Multidrug Resistance Associated Protein 1)?

A

Facilitates extrusion of numerous glutathione, glucuronate, and sulphate conjugates

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26
Q

What is the primary role of MRP2?

A

Eliminates drug glucuronides in bile

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27
Q

What is the significance of pH partition in drug absorption?

A

Affects steady-state distribution of weak acids or bases across compartments

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28
Q

What genetic mutation in Collie dogs leads to neurotoxicity from ivermectin?

A

Lack of MDR1 gene encoding P-glycoprotein

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29
Q

What compound is generated by purine metabolism and can cause effects in joints and kidneys?

A

Uric acid

High levels of uric acid in synovial fluid can lead to joint issues, while accumulation can cause uric acid kidney stones.

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30
Q

What is the effect of the mutation H155A on proteins?

A

Makes an unstable protein

31
Q

How many different gene families do SLC transporters have?

A

52 different gene families

32
Q

What are the two types of proteins classified under SLC transporters?

A
  • Facilitative transporters
  • Secondary active transporters
33
Q

What do facilitative transporters do?

A

Allow substrates to flow downhill with their electrochemical gradients

34
Q

What do secondary active transporters do?

A

Allow substrates to flow uphill against their electrochemical gradient by coupling transport to that of a co-substrate

35
Q

Are secondary active transporters ATP dependent?

A

No, they are not ATP dependent

36
Q

What is the OATP family responsible for?

A

Transporting organic anions across membranes

37
Q

Which genes encode the OATP family?

A

SLOC1 to SLOC6 genes

38
Q

Which OATP proteins are most important for drug disposition?

A
  • OATP1B1
  • OATP1B3
  • OATP2B1
39
Q

What type of substrates do OATP1B1 typically transport?

A
  • Statins
  • Rifampicin
  • Benzylpenicillin
40
Q

What is the OAT family?

A

A separate family from OATPs, members of the SLC22A subfamily

41
Q

Where are OAT1, OAT2, and OAT3 located?

A

Basolateral membrane of proximal tubule cells, facing blood vessels

42
Q

What is the role of OAT4?

A

Located on the apical membrane of proximal tubule, facing urine

43
Q

What is the substrate coupling mechanism for OAT1 to OAT3?

A

Coupled to dicarboxylic acid transport

44
Q

What types of drugs are likely substrates for OAT transporters?

A
  • Sulphated conjugates
  • Glucuronide conjugates
45
Q

Give an example of a substrate for OAT1.

A

Tetracycline

46
Q

What are OCTs?

A

Organic cation transporters

47
Q

Which OCTs are the most important in human drug disposition?

A
  • OCT1
  • OCT2
48
Q

What types of substrates does OCT1 transport?

A
  • Metformin
  • Cisplatin
49
Q

What is the role of PEPT transporters?

A

Transport peptides and are involved in drug reabsorption in the kidney

50
Q

Which family do PEPT transporters belong to?

A

POT protein family

51
Q

What types of drugs do PEPT1 and PEPT2 transport?

A
  • Penicillins
  • ACE inhibitors
  • Valacyclovir
52
Q

What is the function of MATE transporters?

A

Export pumps that contribute to biliary and renal excretion of cations

53
Q

What are the two MATE genes identified?

A
  • MATE1
  • MATE2
54
Q

Where is MATE1 expressed?

A

In the kidney and liver

55
Q

Where is MATE2 expressed?

A

Only in the kidney

56
Q

What is the role of transporter proteins in the liver and kidney?

A

Transport xenobiotics into hepatocytes for metabolism and excretion

57
Q

What is the function of the basolateral membrane in drug transport?

A

Excretion by tubular secretion or reabsorption into circulation

58
Q

What happens to compounds at the brush border membrane?

A

They enter the lumen for final renal excretion

59
Q

What is the role of CYP2C9 and UGT2B7 in drug metabolism?

A

Metabolizes diclofenac to acyl glucuronide (DF-AG)

60
Q

What is the effect of OAT2 and OAT4 on DF-AG?

A

They excrete DF-AG

61
Q

What can cause drug-drug interactions involving transporters?

A

Inhibition of transport in OAT and P-glycoprotein (P-gp)

62
Q

What is a consequence of OAT inhibition by probenecid?

A

Slower clearance of penicillin

63
Q

What is the impact of P-gp on digoxin?

A

Excretion affected by various drugs, potentially causing toxicity

64
Q

What does OATP1B1 polymorphism lead to?

A

Higher plasma levels of some statins due to impaired hepatocyte entry

65
Q

What condition can arise from OCT2 linked nephrotoxicity?

A

Fanconi syndrome

66
Q

What is the proportion of free drug to bound drug when drugs are bound to plasma proteins?

A

Free drug fraction is less than 1%, bound fraction is 99%

67
Q

What is the most important protein for drug binding in plasma?

A

Albumin

68
Q

What types of drugs does albumin mainly bind?

A
  • Acidic drugs (e.g. warfarin)
  • Basic drugs (e.g. TCAs)
69
Q

What factors influence the amount of drug bound to protein?

A
  • Concentration of free drug
  • Affinity for binding sites
  • Concentration of protein
70
Q

What is the significance of fat in drug accumulation?

A

Acts as a reservoir for non-polar drugs

71
Q

What can lead to significant drug accumulation in fat?

A

High administration of benzodiazepines (BZDs)

72
Q

What is the partition coefficient of morphine?

A

0.4

73
Q

Which drug accumulates in bones and teeth and should not be used in children?

A

Tetracyclines

74
Q

What can amiodarone lead to during long-term use?

A

Hepatitis and pulmonary fibrosis

Pharmacology basic knowledge (10 decks)

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