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MPharm2 SL22105 > PK + PC > Flashcards

PK + PC Flashcards

1
Q

What are parenteral medicines?

A

Injections, infusions and implants

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2
Q

What are the three most common routes of injection through the skin?

A

Subcutaneous, intramuscular and intravenous

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3
Q

What are the other 7 parenteral routes?

A
  • intradermal
  • intrathecal (into cerebrospinal fluid)
  • epidural
  • intra-articular (into synovial fluid)
  • intracardiac
  • intra-arterial
  • intraocular
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4
Q

What are the 8 advantages of parenteral formulations?

A
  • Immediate physiological response (IV route) for acute medical situations
  • Drugs which have poor bioavailability or are rapidly degraded within GI tract
  • Unconscious/uncooperative patients, patients with nausea/vomiting
  • Control of dosage and frequency of administration by trained medical staff (an exception being self-administration of insulin)
  • Requirement for localized effect
  • Correction of electrolytes
  • Range of drug release profiles
  • Total parenteral nutrition (TPN)
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5
Q

What are the 5 disadvantages of parenteral formulations?

A
  • More complicated and expensive
  • Skill of administration
  • Pain on administration
  • Allergy to the formulation
  • Difficult to reverse the effects
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6
Q

What are the 6 types of excipients used in paraenteral formulations?

A
  • co-solvents
  • surfactants
  • buffers
  • perservatives
  • anti-oxidants
  • tonicity agents
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7
Q

What are the 4 colligative properties?

A
  • Vapour pressure depression
  • Boiling point elevation
  • Freezing point depression
  • Osmotic pressure
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8
Q

What is vapour pressure depression?

A

Addition of a solute to a solvent, reduces the vapour pressure above the liquid

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9
Q

What is boiling point elevation?

A

The dissolution of a solute in a solvent increases the boiling point of the solution:
ΔTb= Kb m

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10
Q

What is freezing point depression?

A

The dissolution of a solute in a solvent decreases the freezing point of the solution:
ΔTf= Kf m

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11
Q

What is osmotic pressure for non-electrolyte solutions?

A

n R T = c R T
———- .
V

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12
Q

What is osmotic pressure for electrolyte solutions?

A

i c R T

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13
Q

What is osmolality?

A

number of osmoles/kg of solvent (i.e., water)

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14
Q

What is osmolarity?

A

number of osmoles/litre of solution

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15
Q

What is Isosmoticity?

A

if two solutions are separated by a perfect semi-permeable membrane and there is no net movement of solvent, the solutions are Isosmotic

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16
Q

What is Isotonicity?

A

solute conc inside = solute conc outside

17
Q

What is the result of excessive infusion of isotonic formulations?

A

possible increase in extracellular
fluid volume and circulatory overload

18
Q

What is the result of excessive infusion of hypotonic formulations?

A

RBC swelling, haemolysis, water ingress in to cells and tissues, eventually water intoxication (convulsion, oedema)

19
Q

What is the result of excessive infusion of hypertonic formulations?

A

numerous possible complications, e.g. rapid high % dextrose causes hyperglycaemia, glycosuria & intracellular dehydration, osmotic diuresis, water & electrolyte loss, dehydration and coma

20
Q

How do you prepare an isosmotic solution using the freezing point depression method?

A

Using tables, calculate the ΔTf caused by the drug and all other components of the formulation in order to determine the ΔTf required from the adjusting substance

ΔTf (required) = 0.52 – ΔTf (components)

Tables provide experimentally-determined ΔTf values for different concentrations of drugs and excipients

Must be freezing point of -0.52 ºC

21
Q

How do you prepare an isosmotic solution using the NaCl equivalents method?

A

The sodium chloride equivalent (ENaCl) of a solute is the mass of NaCl that lowers the freezing point of a solvent (water) to the same extent as 1 g of the solute
Experimentally-determined ENaCl values for drugs and excipients can be found in tables
Must be 0.9 % NaCl

22
Q

How do you prepare an isosmotic solution using the White-Vincent method?

A

Water is added to the drug and excipients in a sufficient amount to form an isotonic solution
The preparation is then made to its final volume with an isotonic or buffered isotonic diluting vehicle
Must be 285 mOsm/litre

23
Q

What are the 7 most commonly monitored drugs?

A
  • anticonvulsants
  • antiarrhythmics
  • antiasthmatics
  • immunosuppresives
  • antidepressants
  • antineoplasics
  • antibiotics
24
Q

What are the 5 reasons for requesting TDM?

A
  • a narrow therapeutic range
  • assessment of adherence
  • toxicity suspected
  • lack of response
  • no clear observable endpoint to therapeutic success
25
Q

Why is localisation important?

A

P-gp effluxes substrates into the lumen of the organ where is expressed
1. Intestine enterocyte
reduced oral absorption, less F, Less AUC
2. Liver hepatocytes
enhanced biliary elimination more Cl, less AUC
3. Proximal tubule cells of the kidney
enhanced renal excretion, more Cl, less AUC
4. Blood-brain barrier
limit distribution to brain, less V
5. Placenta
limit distribution to foetus, protection by sending drugs back to maternal circulation, less V

26
Q

What is the medical relevence of transporters?

A
  • can ocasionally be drug targets
  • many drugs are substrates for transporters
  • many drugs are also inhibitors and inducers of transporters
27
Q

What 3 effects do transporters have on absorption?

A
  • Intestinal efflux transporters reduce the BA of drugs, including those with good passive permeability
  • Intestinal uptake transporters may enable oral administration of actives with poor passive permeability
  • Gastrointestinal tract efflux and uptake transporters may become saturated
28
Q

What is the effect of transporters on renal excretion?

A

tubular reabsorption can be mediated by transporters

29
Q

What is the effect of transporters on biliary excretion?

A

Transporters into bile tract may rate-control hepatic clearance

30
Q

What is the effect of transporters on hepatic excretion?

A

Transporters into hepatocytes may rate-control hepatic clearance

31
Q

What are the 6 relevancies of DIs?

A
  • cause variability in outcomes of therapy
  • decreased, even eliminate, the efficacy of a treatment
  • cause serious and even fatal adverse events
  • increase hospital admissions and healthcare costs
  • lead to drugs withdrawal from the market
  • Increasing problem due to polypharmacy in aging population
32
Q

What is hepatic clearance?

A

measures the loss of drug across the liver by metabolism and excretion and can be defined as either

33
Q

What is hepatic extraction ratio?

A

the fraction of a drug passing through the liver which is eliminated

34
Q

Which two factors determine hepatic clearance?

A
  • Rate of drug presentation
  • efficiency of drug removal
35
Q

What does a high hepatic extraction ratio mean?

A
  • fast leaving blood cells
  • fast dissociating from plasma proteins,
  • fast being metabolized by enzymes

High EH (>0.7) ClH is primarily rate limited by liver perfusion (QH)

36
Q

What are the 2 reasons a drug has low hepatic extraction ratio?

A
  • slow dissociation from RBC,
  • slow dissociation from plasma proteins
37
Q

How do you calculate extraction ratio?

A

EH = ClH/QH

38
Q

What is AUC in the 2 compartment model?

A

AUC0 = A + B
– –
a b

MPharm2 SL22105 (8 decks)

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