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Pharmacology > Lecture 10 and 11 > Flashcards

Lecture 10 and 11 Flashcards

1
Q

What are the 4 main compartments that water exits in the body?

A
  • Extracellular (blood plasma, interstitial fluid, lymph)
  • Intracellular
  • Transcellular
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2
Q

What is Volume of distribution (Vd)?

A

Volume that would contain the total body content of the drug at a concentration equal to that is present in the plasma

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3
Q

What is the equation for Volume of distribution (Vd)?

A

Vd = Q/Cp

Cp - Plasma
Q - Drug

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4
Q

What is the purpose of Volume of distribution?

A

Relative affinity of the compound for plasma/blood constituents and tissue constituents

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5
Q

What affects Volume of distribution?

A

Lipid solubility due to cell peentration
- Plasma protein binding reduces Vd
- Tissue binding increases Vd

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6
Q

What influences a drug distribution?

A

Albumin, acid glycoprotein and beta-globulin

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7
Q

What form does drugs exist in therapeutic concentrations within plasma?

A

Bound form

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8
Q

What are the functions of plasma protein binding?

A
  • Binding is rapidly reversible and non specific
  • Forms a reservoir of drug
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9
Q

What are unexpected effects in plasma protein binding/

A
  • Surge or drop in cocnentration leading to side effects or OD
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10
Q

How isthe treatments to Parkinson’s disease handled?

A
  • To increase dopaminergic activity
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11
Q

Dopa is a drug. How is it adminstered and what its effect?

A

Adminstered with Carbidopa
- Increases plasma levels and half life

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12
Q

What are the side effects of Dopa on non targeted delivery?

A

Hypotension, caridac arrythmias

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13
Q

What is the side effect of Dopa on the CNS?

A
  • Depression, anxiety, insomnia, hallucinations
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14
Q

What is drug elimination

A

Irreversible loss of drug from the body

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15
Q

What is Metabolism?

A

Enzymatic converison of one chemical entity to another within the body

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16
Q

What is Excretion?

A

Elimination from the body

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17
Q

What are the main excetory routes?

A
  • Kidney
  • The hepatobiliary system
  • Lungs
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18
Q

What drugs are elimintated efficiently by the kidneys?

A

Lipophilic drugs

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19
Q

What are Xenobiotics?

A

Foreign chemical agent that comes into the bdoy

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20
Q

What are examples of Xenobiotics?

A
  • Drugs
  • Toxins
  • Emissions (e.g motor vehicle, CO2 fuels)
  • Lifestyle (e.g vaping, alcohol)
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21
Q

What are molcecules that are not well metabolised?

A

Heterocyclic aromatic amines

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22
Q

What are the two main classes of Heterocyclic aromatic amines?

A

Prolysis of amino acids and sugars

Cancer

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23
Q

What are Polycyclic Aromatic Hydrocarbons?

A

Chemicals that occur naturally in coal, crude oil and gasoline
- Found in Cigarettes

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24
Q

Example of an inorganic xenobiotic

A

Asbestos

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25
Q

Reduced reabsoprtion by the kidney, ehanced billary and renal excretion is caused by?

A

Transforming a lipophililic drug to polar metabolites

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26
Q

5 fluourouracil is activated by metabolism. What drug is it?

A

Prodrug

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27
Q

What are the sites of metabolism?

A
  • Liver
  • Plasma
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28
Q

How does metabolism occur in the liver?

A

Drugs absorbed via the Gl tract pass through the liver before entering cirulation

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29
Q

Example of drug that is absorbed in the plasma?

A

Suxamethonium

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30
Q

What is the function of Suxamethonium ?

A

Depolarising neuromuscular blocker

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31
Q

How does Suxamethonium have effect in the body?

A

Persistently over stimulate the receptor Metabolised by plasma cholinesterases

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32
Q

What drug has an effect on the metabolism in the lungs?

A

Epoprostenol

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33
Q

What drug has an affect on the metabolism in the intestines?

A

Monoamine oxidases metabolise Tyramie (amino acid), MAOI inhibits the enzyme

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34
Q

What are drugs that undergo substantial first pass eliminaiton?

A

Salbutamol, Lidocaine, Aspirin. Morphine

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35
Q

What does the first pass effect refer to?

A

Combined effect of metabolism by the liver and in the gut

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36
Q

Significant inter-individual variation can occur due to first pass effect. What are the effects?

A

• Unpredictable efficacy
• Chance of toxic side effects / adverse reactions

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37
Q

What are the results of metabolism?

A

Duration of exposure and biological activity is reduced
• Biological activity of a drug may be changed (prodrugs)
• Biological half life is reduced
• Accumulation in the body is avoided

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38
Q

Where can CYP enzymes be found?

A

Membrane of the smooth endoplasmic reiculum

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39
Q

Where are polar drugs excreted?

A

Urine

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40
Q

What are the differences within the P450 enyzmes?

A
  • Amino acid sequence
  • Sensitivity to inhibitors and inducing agents
  • Specificity of the reactions that they catalyse
41
Q

What does CYP450 enyzms work parallel with?

A

Electron donors

42
Q

How many CYP enzymes account for 93% of known drug metabolising reactions?

A

12

43
Q

Where DH is a drug, what is the name for NADH or NAPH?

A

Reduced nicotinamide adenine dinucleotide cofactor

44
Q

Where DH is a drug, what type of cofactor is NAD or NADP?

A

Oxidised

45
Q

What is the final electron acceptor?

A

Oxygen

46
Q

Role of metabolsim?

A

Abolish drugs/potentially harmful substances from the body

47
Q

What are the phase one reactions?

A

Catabolic, Oxidation, Reduction or Hydrolysis

48
Q

What is Rate of reaction in Michaelis-Menten kinetics proportional to?

A

Concentration of enzymes

49
Q

What factors can effect phase 1 metabolism?

A

Inhibition of CYP450
- Competitive inhibitor - quinidine - CP2D6
- Noncompetitive injibitor - Ketoconazole - Complexes with Fe3+

50
Q

What effect does Phenobarbitol and 3,4 bezo[α]pyrene have on the rate of oxidative metabolism of zoxazolamine?

A

Increase the rate

51
Q

What drug is coverted into morphine by CYP2D6?

A

Codeine

52
Q

What does poort metabolisers face when coverting codeine to morphine?

A

Inadequate pain relief

53
Q

What does rapid metabolisers face when coverting codeine to morphine?

A

Morphine OD

54
Q

Example of drug interaction in affecting enzyme effectiveness?

A

Seizures – Anticonvulsant
• Pregnancy – Oral contraceptive
• Graft / organ rejection - Immunosuppressants

55
Q

What are phase II reactions?

A

Conjugation/ anabolic reactions

56
Q

How does Conjugation reaction occur?

A

Attachment of a substituent group - causing inactive product

57
Q

Phase II reactions require insertion of glucuronyl, sulphate, methyl or acetyl group. Why?

A

Reaction sequence requires activation of the groups being coupled through energy transfer from high-energy phosphate compounds

58
Q

What is the purpose of Glucoronic acid in Phase II reactions?

A

Reacts with high energy UTP forming UDP

59
Q

What is Transferases??

A

Transfer small polar molecules onto the drug

60
Q

How does Paracetamol OD occur?

A
  • Glucuronide and sulphate pathways become saturated
  • More NADPQI is produced by Phase I reactions
  • Glutathione becomes depleted, NADPQI remains cytotoxic – hepatocyte damage and death
61
Q

What are the four stages of Paracetamol OD?

A

• Stage 1 – asymptomatic – GI upset
• Stage 2 – Nausea and vomiting
• Stage 3 Hepatic failure – jaundice, encephalopathy
• Stage 4 – Death from liver failure

62
Q

What are the routes of excretion?

A
  • Kidney - Urine
  • Bile - Faces
  • Expelled air
  • Sweat/Saliva
63
Q

What are the roles of the Kidney?

A
  • Maintaining internal environment
  • Regulate volume of water in the body
    -Excreting metabolic waste
  • Producing erythropoietin and renin
  • Coverting Vitamin D
64
Q

Where does Glomerular filtration occur?

A

Renal corpuscle

65
Q

What type of process is used in Glomerular filtration between the Glomercular capsule and the Peritubular capillary?

A

Passive diffusion

66
Q

What are not filtered in Glomerular filtration?

A

Plasma proteins and drug protein complexes

67
Q

How small does a molecular need to be to pass throught he glomeruli?

A

20 kDA

68
Q

What is Creatinine?

A

A waste product of creatine phosphate

69
Q

What factors affect glomercular filtration?

A
  • Protein binding
  • Size
  • Renal disease, renal blood flow, age
70
Q

What is the Glomercular filtration rate?

A

A test used to check how well the kidneys are working (how much blood pass throught he glomeruli)

71
Q

What does high creatinine levels show?

A

Low glomerular filtration

72
Q

What are Peritubular absorption?

A

Substances move fromt he subule into the tubular capillaries

73
Q

What is Peritubular secretion?

A

Substance moves from the capillaries into the tubule

74
Q

What is Renal Clearance?

A

Volume of plasma containing the amount of substance that is removed from the body by the kidneys in unit time

75
Q

What is the equation for Renal Clearance?

A

CLren = Cu x Vu / Cp

Cp - plasma concentration
Cu - the urinary concentration
Vu - the rate of flow of urine
CLren - varies greatly for different drugs

76
Q

What is Ion trapping?

A

Basic drugs more readily excreted in acidic urine

77
Q

What drug is used in the treatment of recurrent urinar tract infections?

A

Hiprex

78
Q

What effect does Diuretics have on the kidney?

A
  • Increase the excretion of Na+ and water
  • Decreas the reabsorption of Na+ and CL- from the filtrate
79
Q

What sites does Diuretics affect?

A
  • Loop of Henle
  • Distal tubule
  • Collecting tubule and ducts
80
Q

What is Enteropepatic recycling?

A

Feedback mechanism involving the intestine and the liver

81
Q

How is drug absorption occur in Enterohepatic recycling?

A

Intestine into the portal circulation

82
Q

What happens to drugs when they enter the Enterohepatic recycling?

A

• Uptake of drug by hepatocytes
• Remaining drug and conjugated metabolites are secreted into the bile and back into the intestine
• Drug and conjugates can be reabsorbed into the systemic and hepatic circulation

83
Q

What is the Enterohepatic cycle of bile acids?

A

Cholic acid and chenodeoxycholic acid – formed in the liver from cholesterol
• Conjugated with taurine or glycine – enhances detergent properties – stored in gall bladder until after a meal
• Bile acids facilitate digestion and absorption of nutrients, lipid-soluble vitamins, lipids
• Metabolised by intestinal microbiota, actively reabsorbed in the distal ilium and recycled by transport back to the liver

84
Q

What prevents overgorwing of interstinal bacteria and cause antimicrobial peptide secretion?

A

Bile acids

85
Q

What is Glucurondiation?

A

Excretion into the bile

86
Q

What durgs undergo glucuronidaion during metabolism?

A
  • Morphine
  • Propofol
  • Sex hormones
  • Cardiac glycosides
87
Q

How can Glucurondiated chemicals be de-conjugated by intestinal bacteria?

A

Via hydrolysis

88
Q

What is Digoxin?

A

Cardiac glycoside, slows down the heart rate making it easier for the heart to pump blood around the body

89
Q

What happens when small variations to Digoxin is made?

A

Toxic side effects

90
Q

What is Digoxin is excreted as into the bile?

A

O-glucuronide

91
Q

What metabolises O-glucuronide back into active digoxin?

A

GIT bacteria

92
Q

What happens if the blood concentration of digoxin is high?

A

Enterohepatic recirulation can be blocked

93
Q

What is Cholestyamine?

A

– binds digoxin stopping high enterohaptic recirulation and reducing blood concentrations

94
Q

What is the Hepatic and biliary clearance equation?

A

CLbiliary = Bile flow x Cbile / Cp

95
Q

How is Triethylaminuria involved in excretion?

A

Excreted through sweat to cause a unpleasant odour

96
Q

What happens in Phase 1 to CYP450 enzymes?

A

Making them more polar

97
Q

What is the purpose of Phase II enyzmes?

A

Adding another subtitiuent (conjugation)

98
Q

Where does the loop diuettics affect?

A

Loop of Henle

99
Q

What must happen in MEC?

A

minimum concentration of drug must be reached in the plasma before the desired therapeutic effect is achieved

Pharmacology (7 decks)

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