Nasal

M3O15. The nose is divided into two equal part (nostrils), by the .

Septum

M3O15. The nose provides protection from _ and __.

foreign particles and pathogens

M3O15. The nasal septum is made of what 3 things?

1. bone
2. cartilage
3. epithelium

M3O15. Anterior nasal cavity

Vestibule segment

M3O15. Middle nasal cavity

Atrium segment

M3O15. Posterior nasal cavity

Respiratory segment

M3O15. The vestibule is composed of ___ and __.

• stratified squamous keratinized cells

• sebaceous glands

M3O15. The atrium is composed of

• stratified squamous

• pseudostratified columnar w/microvilli

M3O15. The respiratory segment is composed of what sections?

superior, middle and inferior turbinates

M3O15. The respiratory segment is composed of what cells?

ciliated/nonciliated columnar w/microvilli and goblet cells

M3O15. Located at the roof of the nasal cavity above the superior turbinate with a direct connection to the CNS

Olfactory region

M3O16. Cilia and mucus move posteriorly to the nasopharynx and eventually to the GI tract.

Mucocilliary clearance (MCC)

M3O16. The beating of the cilia at 1000 strokes per minute

Ciliary beat frequency (CBF)

M3O16. What 3 things is the CBF influenced by?

1. infection
2. pollution
3. drugs

M3O16. What is a physical barrier to drug delivery in the nose?

a lipoidal cell layer with aqueous pores

M3O16. allows hydrophilic drugs that are smaller than 1 kilodalton.

Paracellular transport

Lipophilic drugs such as fentanyl, progesterone, and propranolol permeate ___ and RAPIDLY

Transcellularly transport

M3O16. The enzymatic barrier in the nasal mucosa contains , , , and __

• oxidative/conjugate enzymes

• proteases and peptidases

M3O16. The nasal mucosa has a P450 dependent monooxygenase system in the nose that degrades

nasal decongestants and nicotine

M3O16. Things stay in the nasal cavity _ (shorter/longer) than in the ocular cavity.

longer

M3O16. The clearance half-life of drugs in the nasal cavity is around .

21 minutes

M3O16. _ and _ will decrease MCC

↑ viscosity and ↓ CBF

M3O16. Mucocilliary clearance (MCC) creates a _ barrier.

temporal

M3O16. Mucocilliary clearance (MCC) affects (polar/nonpolar) drugs

polar

M3O16. A drug that has low bioavailability due to chemical degradation is due to what barrier in the nasal cavity?

enzyme degradation

M3O17. Nasal sprays can treat both and _ diseases.

systemic and local

M3O17. One of the oldest delivery systems for nasal administration

Nasal drops

M3O17. Nasal drops require ___.

calibration

M3O17. Squeezed bottles are mainly used for products.

saline

M3O17. Squeezed bottles require __.

calibration

M3O17. Nasal inhalers are used for .

volatile drugs

M3O17. Saline is good for what 3 nasal dosage forms?

1. nasal drops
2. squeezed bottles
3. metered dose nasal sprays

M3O17. Provided as a single dose, typically for systemic use

Single metered dose nasal sprays

M3O17. What nasal dosage forms gives the most accurate dose (25 micro/L)?

metered dose nasal sprays

M3O18. With formulation requirements for nasal dosage forms, we want to avoid affecting the and _.

cilia and CBF

M3O18. Nasal dosage forms are (required/not required) to be sterile if not going into lungs.

not required

M3O18. Is isotonicity more important for nasal dosage forms or ophthalmic dosage forms?

ophthalmic dosage forms

M3O18. Nasal dosage forms have to be (isotonic/near isotonic).

near isotonic

M3O18. The usual pH for nasal formulations is _.

4-8

M3O18. benzalkonium chloride is used for _ in nasal sprays.

preservative

M3O18. Can you use eye drops in the nose?

yes

M3O18. Can you use nasal drops in the eye?

no

M3O18. Metered dose nasal sprays can give doses as small as _.

25 microliters

M3O19. Patients should blow their nose _ (before/after) administration.

before

M3O19. After administered a nasal spray, the patient should __ immediately after.

hold their breath for a few seconds

M3O19. Immediately after the administration of a nasal spray, patients should breathe out of their _ (nose/mouth).

mouth

M3O20. What are the 4 advantages of Nasal drug administration?

1. good for local delivery
2. bypass 1st pass effect
3. rapid onset of action
4. easy to use

M3O20. What are the 3 disadvantages of Nasal drug administration?

1. patient acceptance
2. potential for systemic absorption
3. irritation

List the structures of the nose from the anterior to posterior regions. (4)

1. vestibule
2. atrium
3. respiratory/olfactory region
4. nasopharynx

In the nasal cavity, what kind of drugs can be absorbed trancellularly?

• positive log P

• smaller than 400 daltons

In the nasal cavity, what kind of drugs can be absorbed paracellularly?

• negative log P

• smaller than 400 daltons

In the nasal cavity, what kind of drugs are not absorbed systemically?

peptides and larger than 1,000 daltons

What 4 diseases can be treated locally with nasal dosage forms?

1. seasonal allergic rhinitis
2. perenial allergic rhinitis
3. hayfever
4. sinusitis

What 4 diseases can be treated systemically with nasal dosage forms?

1. osteoporosis
2. von willebrand's disease
3. migraine headaches
4. central diabetes insipidus

Drug absorption in the nasal cavity is most like what kind of administration?

IV