Nasal Delivery Flashcards

1
Q

Why is nasal delivery used

A
  1. local effects
  2. systemic effects
    - where oral route is not available
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2
Q

what is the main nasal passage

A

turbinates and meatuses (air spaces)

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3
Q

what are the functions of the nasal passage

A
  1. air conditioning
    - can increase temperature from 23 degrees to about 32
  2. can increase humidity
  3. filtration by vibrissae and mucociliary clearance
  4. olfaction
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4
Q

describe the deposition and clearance of a nasal spray from the nasopharynx

A

deposition increases as time increases
- platueu

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5
Q

describe the deposition and clearance of a nasal spray from the turbinates

A

deposition decreases as time increases
- platueus

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6
Q

what is systemic delivery

A

a route of administration into the circulatory system so that the entire body is affected

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7
Q

what are the anatomical and physiological factors affecting nasal absorption

A
  1. large surface area
  2. highly vascularized so avoids first pass hepatic metabolism
  3. mucociliary clearance decreases contact time
  4. metabolic activity
  5. immunological clearance
  6. mucus barrier
  7. epithelial barrier
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8
Q

what is transcellular transport

A

active transport mechanism where solutes pass through the cell passing through both the apical membrane and basolateral membrane

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9
Q

what is paracellular transport

A

transfer of substances across an epithelium by passing through the intercellular space (tight junctions) between the cells

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10
Q

what are the drug factors affecting nasal absorption

A
  1. molecular weight
    - absorption decreases when molecular weight >1000Da
    - limited diffusion of molecules >3.6 Angstroms
    - negligible diffusion of molecules >15 angstroms
  2. lipophilicity- absorption increases with increased lipophilicity
  3. charge- absorption best if molecules are unionised
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11
Q

what is breakthrough pain

A

A sudden increase in pain that may occur in patients who already have chronic pain
- usually lasts a short period of time
- can be given rescue dose of a rapid acting opioid of relatively short duration

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12
Q

give an example of a drug that can be used for breakthrough pain

A

fentanyl/pecfent

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13
Q

what is the half life of fentanyl

A

12-15 mins

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14
Q

describe the effectiveness of PecFent

A
  1. more effective than placebo in reducing pain 30 min after use
  2. patients satisfied or very satisfied with 90% of breakthrough pain episodes
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15
Q

what can be used as treatment of accidental overdose of opioid

A

IV and IM naloxone
Narcan nasal spray

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16
Q

describe when overdose occurs

A

occurs when too much of an opioid fits in too many receptors slowing and then stopping the breathing

17
Q

describe how naloxone reverses an overdose

A

naloxone has a stronger affinity to the opioid receptors than opioids, so it knocks the opioids off the receptors for a short time
- this allows the person to breathe again and reverse the overdose

18
Q

describe how naloxone nasal spray can be used

A

used by many first responders and primary caregivers
- nasal spray formulation of naloxone is easier to deliver, and eliminates the risk of a contaminated needle stick

19
Q

which people are likely to witness an opioid overdose

A
  1. people at risk of an opioid overdose, their friends and families
  2. people whose work brings them into contact with people who overdose
    - healthcare workers, police, emergency service workers
20
Q

when is a nasal spray recommended

A

opioid overdose in non medical and medical settings

21
Q

compare the nasal and oral bioavailability of desmopressin

A

oral bioavailability= 0.08-0.16%
nasal bioavailability= 10%

22
Q

what are the formulation factors affecting nasal absorption

A
  1. pH
  2. osmolarity
  3. viscosity
  4. concentration
  5. volume
  6. dosage form
  7. penetration enhancers
23
Q

give an example of a penetration enhancer

A

chitosan
- cationic polysaccharide
- increases the absorption of polar molecules and acts as a bioadhesive
- transiently opens tight junction

24
Q

give examples of therapeutic areas suitable for IN administration

A
  1. breakthrough cancer pain- fentanyl, morphine
  2. emergency situation medicines- naloxone for opioid overdose
25
Q

what are the patient factors affecting nasal absorption

A
  1. acceptable to patient
    - non invasive, comfort and compliance
    - simple dosage forms, drops and sprays
  2. variability of dosing
  3. disease
    - inflammation
    - common cold