Pharmaceutics Flashcards

1
Q

What are the 4 main functions of the kidneys?

A

Regulate body fluids

Electrolyte balance

Remove metabolic waste

Drug Excretion

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2
Q

What are 6 common causes of kidney faliure?

A

Pyelonephritis –> Inflammation

Hypertension

Diabetes

Nephrotoxic drugs

Hypovolemia –> Reduction in renal blood flow

Neophroallergens –> Things that stimulate an immune response in the kidneys

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3
Q

What is uremia?

And what affect does this have?

A

Nitrogen in the blood (urea)

Will reduce glomerular filtration….and so reduce drug clearance and other PK paramaters….such as an increase in Vd (as the total body water volume has increased…so hydrophillic drugs will accumulate more)

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4
Q

What are the assumptions made when trating patients with kidney faliure?

A
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5
Q

Name 3 possible GFR markers, and what the requirments are to be one

A

Inulin, Creatinine and Blood Urea Nitrogen (BUN)

They must be….

Freely filtered by the glomerulus

Not be reabsorbed or secreted by renal tubules

Not be metabolised

Not have significant protein binding

Not have an effect on filtration rate or alter renal function

Non-toxic

Infused in a sufficient dose

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6
Q

What are the 5 assumptions that we make when using CrCl?

A

Daily anabolic production of creatinine in the liver is constant

Daily anabolic conversion in striatal muscle is constant, and no other sources of creatinine exist –> Larger in those with large muscle mass, and can change with drugs like trimethoprim

Creatinine is freely filtered by the kidney and is not secreted or reabsorbed –> Does undergo tubular secretion

The measurement of of creatinine in serum and urine is accurate

Urine collection is complete –> It often complete…or overcollected!

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7
Q

What’s the difference between hemoperfusion and hemofiltration?

A

Hemoperfusion –> Passing blood through an adsorbant material and back to the patient (mainly used to remove drugs in overdose)

Hemofiltration –> A low pressure flow is used through hollow artificial fibres or flat plate membranes (replacement fluids)

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8
Q

Why cant the IV route be used to supplement patients with nutrients when they are nil by mouth?

What is the alternative?

A

As you cant add enough calories in without them going into fluid overload or damaging the blood vessles

Instead we use the enteral route or the nasogastic route (less likely to become clogged)

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9
Q

Why is Enteral Nutrition better than Pareteral Nutrition?

A

They are cheaper

Less chance of a medical mistake

Maintain a healthy gut until normal feeding is resumed

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10
Q

When is parenteral nutrition given?

And what is the difference between TPN and PPN?

A

When feeding is needed for over 7 days and….

Patient cannot be fed orally or enterally

They have severe gut dysfunction –> No GI absorption

TPN –> Total Parenteral Nutrition….given centrally

PPN –> Partial Parenteral Nutrition…..given peripherally (IV)

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11
Q

In TPN, what is the recommended level of fluid?

And when is this increased/decreased?

A

2-3L

Increased –> In fever and diarrhoea, vomiting and wound drains

Decreased –> Renal faliure, CHF, Cirrhotic ascities and pulmonary disease

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12
Q

In PN, what are the requirements for the following?

Energy

Sugar (Dextrose)

Lipids

Protein (Nitrogen)

A

Energy –> 23-35kcal/kg/day….. this increases for children/adolcescents/infants

Sugar –> 4-5mg/kg/min

Lipds –> No actual amount, but used to carry fat soluble drugs/vitamins

Protein –> 0.2g/kg/day…..for all commercial AA solutions the total amount must not differ by more than 10%

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13
Q

What are the 2 types of TPN?

A

Pharmacy Made –> Must be used within a couple of hours

Multi Chamber Bags –> The three main components are seperated, extending the shelf-life. Also means not all 3 compartments need to be used at the same time (more personalised)

Both are still fairly instable

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14
Q

A lipid emulsion containing AAs and lipids is best made under what conditions to ensure stability?

A

pH of 8 and a surface potential of -35mV

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15
Q

What vitamin is the most unstable substance in TPN?

A

Ascorbic acid –> Readily oxidised to dehydroascorbic acid (DHAA)

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16
Q

What do the following stand for?

ESPEN

ASPEN

JSPEN

BAPEN

A

ESPEN –> European Society for Parenteral and Enteral Nutrition

ASPEN –> American Society for Parenteral and Enteral Nutrition

JSPEN –> Japanese Society of Parenteral and Enteral Nutrition

BAPEN –> British Association for Parenteral and Enteral Nutrition

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17
Q

What are some physiological changes that occur during pregnancy?

A

Changes in body weight and body fat –> Changes lipophillic distribution

Delayed gastric emptying and prolonged GI transit time –> Slower absoption

Increased cardiac output/HR/SV

Increased total water volume

Decreased plasma proteins (albumin) –> Bad for highly bound drugs

Increased GFR –> Higher excretion

Changed hepatic enzymes (such as CYPs) –> Changes in metabolism, meaning increases or decreases in doses or certain drugs

18
Q

When can you not take B-lactams in pregnancy?

A

2nd/3rd trimesters and 6 weeks postpartum

19
Q

In pregnancy, what does the increase Vd cause us to do?

A

Decrease the dose and so Cmax also

This occurs if the Cl is decreased, whereas the dose can be maintained if Cl has increased alongside the Vd

20
Q

Why do obese patients often need more drug than normal weighted people?

A

Because they have more fat and a bigger liver

More Fat = More lipophillic distribution

Larger Liver –> Greater metabolic rate (glucoronidation)

21
Q

Is the CrCl in obese patients greater or smaller than that of normal people?

A

It is increased

22
Q

What is the major barrier to compliance in oral liquid in the paediatric population?

A

Taste! –> So taste masking is vital

23
Q

How small must a tablet be to be deemed a ‘mini tablet’?

A

<3mm

24
Q

What is the major diasadvantage of chewable/orodisperable tablets?

A

Stability

25
Q

What are the 2 main excipients in chewable tablets?

A

Mannitol (sweetener) and Xylitol (sugar-free)

26
Q

Where are the 3 parts of the body that the API in orodispersable tablets can be absorbed?

A

Pre-Gastric –> Oromucosal tissues

Gastic –> The stomach

Post-Gastric –> Small and large intestines

27
Q

What are the 3 ways of formulating orodisperable tablets?

A

Direct Compression –> DuraSolv

Lyophillization (Zydis) –> Water is removed via sublimation. It is then freeze-dried to form the highly porous and water-soluble mix

Moulding –> WOWTAB

28
Q

What is Amniotic Fluid?

A

Fluid in the stomach with a pH of 6-8, which is present at birth in the child

This increases the BA of basic drugs, and decreases that of acidic drugs

29
Q

Is Gastric Emptying Time increased or decreasing in neonates?

A

Increased

30
Q

What is the effect of Pepsin and Bile levels in neonates?

A

Pepsin –> Increases drastically over a short period after birth

Bile –> Lower in neonates

This means non-water soluble drugs are solubilsed as well, so are absorbed less

31
Q

Why do we need to be careful when using intra-ocular drugs in neonates?

What about nasal/skin preperations?

A

The eye of a newborn is 2/3 of the size of an adult, with much thinner membranes. This means that drugs are absorbed much quicker

The same applies for nasal preperations (skin is thinner)

32
Q

What type of inhaler can only be used by children ages 4-5yrs and older?

A

DPIs

As a minimum inspiratory volume is needed, which young children will not have!

33
Q

What is the benefits and problems of using suppositories in children?

A

Benefits –> Easy to administer if the oral route in unavaliable

Also great when the child is being sick (N+V)

Problems –> Adult sizes will often be too big, so they need to be made smaller by ourselves. This is problematic as the API isn’t uniformlly distributed!

34
Q

What are the ages of the following…

Neonate

Infant

Children

Adolescent

A

Neonate –> Birth to 1 month

Infant –> 1 month to 2 years

Children –> 2 to 12 years

Adolescent –> 12 to <16 years

35
Q

At what stage of childhood is there excessive interpatient variability…with different things happening at different rates?

A

Infant

36
Q

Which drugs (that are absorbed via the GI) will have a lower BA in paediatrics?

And why ones will have an increased BA?

A

Those that are dependent on transporters/carrier uptake systems, as these are not mature yet

Those that dont need them will have a greater BA due to immature metabolism

37
Q

How is the Vd affected in the paediatric population?

A

They have a high water content and low fat content….so…..

Water soluble drugs –> Higher Vd

Fat soluble drugs –> Lower Vd

38
Q

Do paediatrics have higher or lower protein binding?

A

Lower, so greater unbound fraction of the drug

39
Q

What is the change in body composition that occurs in the elderly?

A

Weight is lost, which causes a relative increase in body fat

40
Q

Name some of the physiological changes that occur in the elderly

A

Less HCl/Pepsin secretion

Atrophy of the small intestines (villi) –> Decreasing SA and so absorption

Lipase and Typsin secretion decreases (amylase constant)–> Lipid encapsulated drugs will be broken down slower!

Reduction in liver size and blood flow –> Less metabolism

41
Q

Why is GFR not an accurate measure of renal function in the elderly?

A

As plasma creatinine decreases with age, so GFR also changes (not due to changes in kidney function)