Pharmacokinetics- Administration and Absorption Flashcards

1
Q

How are drugs administered?

A

Enteral formulations, parenteral formulations, topical formulations

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2
Q

Give examples of enteral formulations

A
  • Tablet
  • Capsule
  • Liquid
  • Suppository
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3
Q

Describe a tablet

A
  • Compressed, contains 5-10% active ingredient
  • > 90% fillers (binders, lubricants, disaggregants)
  • Aqueous solubility is dependent on particle size and crystal form
  • Has enteric coating which prevents disintegration until passage through stomach into intestine
  • Sustained/extended/modified release of drug
  • Osmotic core, permeable coating allows slow release of drug
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4
Q

What is the effect of extended release drug formulation?

A

Reduces the frequency of dosing

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5
Q

Describe a capsule

A
  • Gelatinous envelope
  • Controllable disintegration speed
  • Slow and fast dissolving particles
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6
Q

Describe a liquid/syrup formulation (enteral)

A
  • Possibly faster absorption
  • Sugar/sugar-free
  • Often paediatric
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7
Q

Describe a suppository formulation

A
  • Rectal
  • Torpedo shape
  • Used for vomiting patients
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8
Q

Give examples of parenteral formulations

A

Liquid, Lyophilised

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9
Q

Describe a liquid formulation (parenteral)

A
  • Vials, ampoules, cartridges, pre-filled syringes

- May need diluting (e.g. IV bag)

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10
Q

What does parenteral mean?

A

Not by gut, i.e. injectable

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11
Q

Describe a lyophilised formulation

A
  • Freeze-dried
  • Produces dry powder
  • Needs reconstituting with liquid
  • Vials, ampoules, dual chamber syringes, etc.
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12
Q

What are topical formulations?

A

Local action- on the surface

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13
Q

What are enteral formulations?

A

By the gut

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14
Q

Give examples of topical formulations

A
  • Cutaneous

- Inhaled

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15
Q

Describe cutaneous formulations

A
  • Cream- mixture of oil/water to penetrate skin
  • Ointment- oilier, reduces water loss
  • Gel-liquefies on contact with skin
  • Paste-powder suspended in a cream
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16
Q

Described inhaled formulations

A
  • For lower airways
  • MDI- metred dose inhaler
  • Breath actuated device
  • Nebulisers
17
Q

Give examples of other administration methods

A
  • Eye drops
  • Nasal sprays
  • Vaginal, urethral suppositories
18
Q

What are the different routes of absorption?

A
  • Oral
  • Parenteral
  • Topical
19
Q

Describe oral absorption

gastric

A
  • Greatest absorption in the small intestine, not in stomach
  • Gastric phase delays drug absorption in intestine
  • Drug absorption may be affected by GI contents
20
Q

What slows down gastric emptying?

A
  • Solid meal (distension)
  • High fat meal
    High protein meal
  • Low gastric meal
  • Low gastric pH
21
Q

Describe oral absorption (hepatic portal circulation)

A

Some oral drugs undergo variable degrees of metabolism in stomach, gut and liver before reaching systemic circulation (1st pass metabolism)

22
Q

Give a summary of oral absorption

A
  • Convenient but delay in drug onset
  • Drug exposed to gastric acid and bacterial and digestive enzymes
  • Portal vein –> liver before reaching site of action
  • Some drugs undergo significant 1st pass metabolism, adjusted doses may be required
  • Enteral routes that avoid 1st pass metabolism include buccal, sublingual and rectal
23
Q

What does parenteral absorption involve?

A
  • Avoids GI tract and first pass metabolism
  • Used against pain, local trauma and infection
  • Requires injection
  • Trained healthcare staff required
24
Q

Give examples of parenteral absorption

A
  • Intravenous
  • Intramuscular
  • Subcutaneous
25
Q

Describe intravenous absorption

A
  • Instant access, high peak concentration

- Bolus; continuous IV infusion used to control rate

26
Q

Describe intramuscular absorption

A
  • Intermediate-onset; smallish volumes only

- Oil based depot formulations give very long duration

27
Q

Describe subcutaneous absorption

A
  • Very slow onset

- Small volumes only

28
Q

Give examples of topical absorption

A
  • Transdermal

- Inhaled

29
Q

Describe transdermal absorption

A
  • Creams/patches
  • Very slow onset; prolonged action
  • Requires a highly lipophilic drug
  • May cause local irritation
30
Q

Describe inhaled absorption

A
  • Rapid delivery
  • No first-pass metabolism
  • Most inhaled drugs act locally (in lungs)
  • Allows low dose to local site
  • Rarely used for systemic drugs