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PM3B: Autumn > Diabetes Lecture 3: Parenteral Drug Delivery > Flashcards

Diabetes Lecture 3: Parenteral Drug Delivery Flashcards

1
Q

What does parenteral mean

A

Method to deliver the drug directly to the blood outside of GI tract

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2
Q

What does Ka, Kd, Km and Ke stand for

A

Ka- absorption

Kd- distribution

Km- Metabolism

Ke- excretion

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3
Q

What are the advantages of injection

A

Rapid and complete absorption

Able to predict the pharmacokinetic profile of drug: control drug and frequency

Useful in unconscious patient, uncooperative patient, nausea and vomiting patient, unable to swallow

Useful for giving small dose

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4
Q

What are the disadvantages of injection

A

Aseptic precautions must be followed

Expensive to manufacture

Once administered, impossible to remove from blood stream

Pain and infection at site of injection

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5
Q

What are the different angles for the intramuscular, subcutaneous and intradermal

A

Intramuscular: 72 or 90 degrees

Subcutaneous: 45 or 90 degrees

Intradermal: 15 degrees

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6
Q

Why shouldn’t you administer larger volume intravenous route into the vein at a fast rate

A

Can lead to sudden osmotic pressure and electrolytes can lead to risk of shock or acute renal failure

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7
Q

What complications are associated with IV delivery and describe them

A

Air embolism- injection of air bubble to vessel can prove fatal if it reaches brain

Thrombosis- formation of clot in blood vessel

Haemolysis- breakdown of red cells lead to relate of haemoglobin

Phlebitis- inflammation of vein wall due to irritation from formulation

Extravasation- leakage of the injection from the vein into surrounding tissue

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8
Q

What are the typical areas of intramuscular injection and advantage it has

A

Deltoid
Gluteal
Vastus lateralis

Quick onset of action

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9
Q

What is subcutaneous injection route

A

Used into the fat layer

Beneath dermis and epidermis and above muscle tissue: typically at arm, abdomen or legs

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10
Q

Give examples of subcutaneous injection use

A

Local anaesthetics: lidocaine 5% with adrenaline

Used to administer antigens or vaccines (small pox)

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11
Q

How does the administer subcutaneous drug gain assess to the blood stream

A

Absorbed into the blood vessels directly, but subcutaneous tissues often adipose and poorly perfused

Interstital fluid is collected by lymphatic capillaries and these drain into the regional lymph nodes and into bloodstream

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12
Q

What are the four insulin delivery methods available (devices)

A

Insulin syringe- vial

Insulin Pen- can carry insulin discreetly with cartridges and a fine needle

Insulin pump or pod- worn on belt, has needle inserted under skin, pump provides basal insulin throughout day and bolus doses at meal times

Jet Injector- sends spray of insulin through skin by high pressure

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13
Q

Describe the use of rapid acting insulin and give examples

A

Acts within 10 to 15 minutes, used to treat high blood sugar level to match or cover a rise in food glucose levels following intake of food

Referred to as bolus insulin

Examples: Homolog, Novolog, Apidra

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14
Q

Describe the use of short acting insulin (regular)

A

Used like rapid acting insulin- used to treat high blood sugar level or cover a rise in food glucose levels following intake of food

Has a longer duration of acting and delayed peak

Referred to as bolus insulin

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15
Q

Describe the use of intermediate and long acting insulin and provide examples

A

Provides basal insulin concentrations and doses that are adjusted based on pattern of blood glucose

Not used for acute treatment of high blood glucose and generally not given before meals

Referred to as basal insulin

Controls the blood glucose in a fasted state

Intermediate example: NPH

Long acting example: Glargine (lantus) and Deter (Lever)

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16
Q

What are the types of insulin normally used in pumps

A

Aspart (Novolog)

Lisper (Homolog)

Glulisine (Apidra)

17
Q

Describe what basal insulin is

A

Steady drip of insulin that matches glucose release by liver

Meets body’s basic energy needs

18
Q

Describe what bolus insulin is

A

Given to cover carbohydrates consumed in meals and snacks

Used to correct high blood glucose levels

19
Q

What is Intrathecal delivery

A

Injection into the subarachnoid space to reach cerebrospinal fluid

20
Q

What is epidural delivery

A

Delivery of drug into the dural membrane surrounding the spinal cord

21
Q

What are the three requirements for parenteral drug delivery

A

Sterile

Pyrogen free- endotoxin that induces fever (produced by deactivation of bacteria)

Homogenous- delivers reproducible dose, physically and chemically stable

22
Q

What must you consider when formulating an intravenously delivered drug

A

Sterile

Small fragments of dust and glass or rubber excluded

Small volume (100ml or below) must be formulated at range of 4 to 10 (considerably hypo/hypertonic)

Large volume- closely matched to properties of blood- pH rarely outside 6 to 8 limit

23
Q

Define plasma extender

A

IV parenteral infused via peripheral vein with closely matched tonicity

24
Q

What are suitable vehicles for injection

A

Water- has to be pure and sterile

Non aqueous vehicles:
Used for non water soluble APIS
Typically are oils

25
Q

State some co-solvents that can be used in formulation

A 
Ethanol
PEG
Glycerine
Soybean Oil
Castor oil
26
Q

State some surfactants that can be used

A

Tween 80
Sorbitan monooleate
Tween 20
Lecithin

27
Q

Which parenteral drug delivery should preservatives be avoided and give an example of preservatives

A

AVOIDED IN: single dose IV

Examples:
Phenol (0.25 to 0.5% w/v)
Chlorocrasol (0.1 to 0.3% w/v)

28
Q

How do you correct hypotonicity

A

Dextrose
Glycerine
NaCl

29
Q

Give examples of commonly used buffers

A

Acetic acid/sodium acetate

Citric acid/sodium citrate

Sodium phosphate and disodium phosphate

30
Q

How do you render a solution isotonic

A

Addition of Dextrose or sodium chloride solution to increase osmotic pressure of solution

31
Q

How do you change viscosity and what do you add

A

Change when adding polymeric stabiliser

example: PVP or aluminimum stearate

32
Q

What are the advantages of increasing viscosity in a dosage form

A

Stability

Steric hinderance

Decrease flocculation of suspensions

DVLO

33
Q

What are the steps involved in intramuscular deliver

A

release of the drug from the dosage form into intracellular fluids

Absorption from intracellular fluids into the blood and lymphatic system

transport from the local blood volume into the general circulation

metabolism

34
Q

What are the advantages of injection in general capillary membrane

A

It is highly permeable and not rate limiting

35
Q

What are the key points you have to know for release rate: hydrophobic/phillic, ionisation and protein bound

A

Highly hydrophobic will not dissolve in the intracellular fluid

Strongly ionised or very water soluble- will not cross capillary membrane

Strongly protein bound will be slowly absurd as activity in solution is reduced

36
Q

What is intramuscular delivery contraindicated in patients with cardiac failure

A

Absorption will be extremely slow as muscle perfusion will be small

PM3B: Autumn (19 decks)

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