Drug Excretion, Bioavailability, Bioequivalence And Drug Interaction Flashcards

1
Q

Organs of excretion

A

Kidney(urine), tongue( saliva), skin(sweat), breast( breast milk), lungs(breath), rectum/intestine (bile/faeces) , eye( tears) and lastly through hair

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2
Q

Example of drugs passed through large intestine/ rectum

A

Vancomycin $ vincristine

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3
Q

What type of drugs are excreted in the tongue and what is the PH of the saliva

A

Basic drugs
Ph 5.8-8.4

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4
Q

Examples of drugs excreted through the tongue

A

Phenytoin, diazepam, theophylline, caffeine and lithium

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5
Q

What type of transport does the saliva use to excrete drugs

A

Passive diffusion across the cells of the salivary glands and oral epithelium

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6
Q

Examples of drugs the eye excretes

A

Cytarabine

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7
Q

What type of transport does the eye use to excrete drugs

A

Passive transport of lipophilic non protein bound and unionized molecules from plasma across the eccrine and lacrimal glands

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8
Q

Examples of drugs are excreted by the lungs

A

Mainly anaesthetics

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9
Q

Examples of drugs that are excreted by the skin

A

Antipyrine, alchol, benzoic acid, salycitic acid, lead and mercury, cocaine

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10
Q

What type of drugs are excreted by the breast’s

A

Most drugs e.g aspirin

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11
Q

Examples of drugs excreted by the hair

A

Phenobarbital, methamphetamine, methoxyphenamine

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12
Q

What is the most important organ involved in eliminating drugs and their metabolites

A

Kidneys via their functional unit
(Nephron: glomerulus + tubules)

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13
Q

Renal excretion =

A

Glomerular filtration - tubular reabsorption + tubular secretion

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14
Q

Tubular secretion

A

Carrier mediated, independent of size not protein binding
EXCRETES MOST DRUGS (80%)

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15
Q

Where does tubular secretion occur

A

Occurs at both the proximal and distal convulated tubules

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16
Q

What type of drugs are not excreted by glomerular filtration

A

Drugs with high molecular weight like heparin, high molecular weight plasma proteins like albumin(68000) and highly protein bound drugs such as warfarin(98%)

17
Q

Glomerular filtration filters small molecules ( <20,000) such as what

A

Water, Sugar, salt, Unbound drugs via pores at the base of the glomerulus

18
Q

Tubular reabsorption

A

Occurs by passive diffusion from the tubules into the peritubular capillaries, requires lipid solubility

19
Q

What is renal clearance

A

It can be defined as the volume of plasma containing the amount of substance that is excreted by the urine per unit time

20
Q

Formula for renal clearance

A

CLr= Cu/Cp X Vu

21
Q

List the 2 types of half life

A

1) Biological half life
2) plasma half life

22
Q

Define biological half life

A

It is the time taken for a substance to lose half of its physiological, pharmacological and radioactive activity

23
Q

Define plasma t1/2

A

Time taken for a drug to lose half of its plasma concentration

24
Q

Plasma half life depends on what

A

Rate of excretion and metabolism of the drug

25
Q

List the factors affecting drug excretion

A

Lipid solubility
PH
Enterohepatic cycling
Particle size
Protein binding
Drug interaction
Renal disease

26
Q

List the basic drugs

A

Quinine
Probenecid
Morphine
Histamine
Serotonin
Dopamine
Pethidine

27
Q

List the acidic drugs

A

Aspirin
Penicillin
Methotrexate
Indomethacin
Frusemide
Thiazide diuretics

28
Q

List drugs that undergo enterohepatic cycling

A

Tetracycline, Chloramphenicol, Flurbiprofen, leflunomide, colchicine, digitoxin, phenytoin and oestradiol

29
Q

Give an example how drug interaction can affect drug excretion

A

Probenecid inhibits excretion of penicillin by competing with it for tubular secretion at the proximal tubule thereby prolonging its action

30
Q

Normal GFR range
Kidney disease range
Kidney failure range

A

100-130
Kidney disease < 60
Kidney failure <15 ml/min

31
Q

List the substances that alkalize urine

A

Sodium bicarbonate, acetazolamide, potassium citrate

32
Q

List the substances that acidify urine

A

Ammonium chloride, sodium phosphate, potassium phosphate