Drug Handling Of The Body Flashcards

1
Q

What are the advantages of oral administration?

A

Convenient for patient

Absorption from small intestine- large surface area

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2
Q

What are the disadvantages of oral administration?

A
Not appropriate for all patients
Absorption can be variable 
Absorption can depend of stomach contents
Rate of gastric emptying 
Degradation in the stomach
First pass metabolism
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3
Q

What does degradation in the stomach mean?

A

Parenteral cells secrets HCL

Chief cells secrete digestive enzymes this means the drug could have low bioavailability

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4
Q

What does bioavailability mean?

A

The amount of drug that reaches the circulation as intact drug

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5
Q

Want does first pass metabolism mean?

A

Drug gets lost in the liver due to hepatic first pass effect, low bioavailability

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6
Q

What are the advantages of topical administration?

A

Convenient

Poorly absorption means minimum risks of overdosing

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7
Q

What are the disadvantages of topical administration?

A

Negative effect on the skin- thinning of the skin

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8
Q

What are the advantages of transdermal administration?

A

Long acting
Useful for when you want low blood levels for a long period of time
Suitable for a wide range of patient groups

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9
Q

What are the disadvantages of transdermal administration?

A
Skin effects
Variable absorption
Lipid solubility 
Potent 
Expensive
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10
Q

What are the advantages of rectal administration?

A

Local effect

Useful for patient who cannot swallow

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11
Q

What are the disadvantages of rectal administration?

A

Need to be trained

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12
Q

Example of rectal drugs

A

Analgesics
Diazepam
Prednisolone
Antifungals

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13
Q

What are the advantages of inhalation?

A

Rapid changes in the plasma concentration of drug because of the high surface area of the lungs and good blood flow to area

Local or systemic effect

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14
Q

What are the disadvantages of inhalation?

A

Difficulties in ensuring the drug reaches the site of action

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15
Q

Example of inhalation drugs

A

Halothane
Salabutomol
Nitric oxide
GTN

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16
Q

What are Parenteral routes?

A

IV- thiopental, heparin
IM-pre-Meds
Intradermal- dentistry, local anaesthesia, allergy screening
SC- insulin
INTRATHECAL- antiviral agents, chemo drugs
Epidural- nerve blockers used during labour

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17
Q

What are the advantages of parenteral administration?

A

Rapid action
By pass stomach and liver
Lower doses is required
Patent controlled for analgesia- syringe drivers

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18
Q

What are the disadvantages of Parenteral administration?

A

Trained person needed
Extreme care required
Accidental overdose?
IM- painful

19
Q

Explain the different types of formation of drugs

A

Tablets, gels, locations, aresols, suspensions. Powders. Granules. Capsules, lotions, patches, Inhalations, pastes, sprays, syrup, creams, gases

Can impact upon the bioavailability and sustained release

20
Q

Explain the oral drug absorption

A

From tablet to granules to fine particles to solutions, then absorbed through stomach and small intestine

21
Q

How does the drug cross the cell membrane?

A

If they are lipid soluble- can cross through the epithelial cell in the small intestine to get to the blood stream through diffusion

If water soluble cannot cross through

22
Q

How is the drug absorbed whole it moves across membranes?

A

1 passage through water channels
2 endocytosis
3 passive diffusion
4 facilitated of active transport

23
Q

What is facilities transport?

A

Drug moves down concentrated gradient
Proteins provide channels
No energy required
Staturable, selective, competitive inhibition by other substances

24
Q

What is active transport?

A

Drug moves against the concentration gradient
Energy is required
Saturable, selective, competition inhibition
Example:lithium, levodapa, methyldopa

25
Q

What happens when the drug has been absorbed?

A

Distributed via blood stream

Transferred into and out of various tissues in the body

26
Q

Want affects extent of distribution?

A

Lipid solubility of drugs
Blood flow to organ/tissue
Binging of drugs to proteins

27
Q

Explain the blood flow in these organs/tissues: liver, kidney, CNS, myocardium, fat, other I.e. Muscles

A

Liver: 680ml/min/kg
Kidney: 3,333 ml/min/kg: received the most blood flow
CNS: 615ml/min/kg
Myocardium: 833ml/min/kg
Fat and other: 25ml/min/kg each: here drugs are not distributed

28
Q

Where does protein binding occurs?

A

Free drugs can bind to proteins in the plasma I.e. Albumin

Only free drugs can diffuse across membranes and have an effect

29
Q

How is drug removed from the body?

A

Through metabolism and excretion
Most drugs are lipophilic and so will recirculate around the body
We excited water soluble drugs

30
Q

Define drug metabolism

A

It is the enzyme-mediated conversion of a lipid soluble compound into a more water soluble one, ready for excretion

31
Q

Where does metabolism take place?

A
Mainly in the liver : smooth endoplasmic reticulum 
Kidneys 
Lung
GI tract
Brain
Plasma
32
Q

What are the phases of metabolism?

A

There are two phases. Usually occur in a sequence, phase 1 then phase 11, however phase 11 can precede phase 1

33
Q

What happens in phase 1?

A

Modify the chemical structure of drug
Makes drugs slightly more water soluble
Prepare for phase 11
Products can be more chemically reactive than the parent drug

34
Q

What are pro-drugs?

A

Some drugs when metabolised can even more active than the original drug

Example: prednisone becomes prednisolone
Codeine become morphine
GTN becomes nitric oxide

35
Q

What happens on phase 11 of metabolism?

A

Conjugate drug into large molecules- amino acid, sulphate groups

Product become water soluble and easily excreted
Increased molecular weight
Inactive , decrease receptor affinity and enhance excretion

36
Q

Explain a how drugs interact.

A

Drugs metabolising enzymes can be a) induced I.e alcohol and carbamazepine induce liver enzymes and b) inhibited such as fluoxetine and grape juice

This will result in decrease of the duration of drug action

37
Q

Explain the role of excretion

A

Removal of drugs: drug metabolic and water soluble drugs

Urine, bile, faeces, lungs, skin

To increase drug exception, increase blood flow to the kidneys, decrease plasma protein binding

38
Q

Explain the dosage regimens

A

The therapeutic response of most drugs is related to the level of the drug in the plasma
We need to know the half life of a drug, this is the time it takes for the amount of drug to decrease to one half of the peak level
The rate at which drugs are eliminated from the body

39
Q

How much drug remains if the half life is 2hours for 20mg drug?

A
After 2 hours: 10mg drug will remain
4hrs: 5mg
6hrs: 2.5mg
8hrs: 1.25mg
10hrs: 0.625mg
After 10 hrs sufficient to say all the drug has gone
40
Q

How much of the drug is eliminated in 5 half lives?

A

97%

41
Q

Why do we care about half lives?

A

To avoid drug interactions

Estimating how long it will take for toxic concentration to be eliminated from body

42
Q

What is drug disposition?

A

What the body does to the drug compared to what the drug does to the body
Intake–>absoprtion–>distribution–>drug-cell interaction–>metabolism –> excretion

43
Q

Explain the therapeutic window

A

A range of doses that produces therapeutic response without causing any significant adverse effect in patients.
Generally therapeutic window is a ratio between minimum effective concentrations (MEC) to the minimum toxic concentration (MTC).

I.e. Warfarin and phenytoin have narrow therapeutic window and so need close monitoring

44
Q

What happens if a patient has renal or hepatic disease?

A

The plasma half life increase and drug concentrations may reach a toxic level