Nature, Sources, and
Drug Dosage:
Inhalation
Introduction: History on Inhalation of
Drugs
● Very old method of drug delivery
● In the 20th century: “aerosol therapy” - mainstay of
respiratory care
● 1929: inhaled epinephrine for asthma relief
○ Early version of dry powder inhaler (DPI) -
Aerohalor
■ Administer penicillin dust to treat
respiratory infections
● 1950: Wright Nebulizer - precursor of the modern hand
held jet venturi nebulizer
● 1956: Metered- dose inhaler (MDI)
● 1971: SpinHAler DPI for cromolyn sodium
Introduction: Drug Absorption
● The drug is inhaled and absorbed in the lungs
○ Its features include:
■ large surface area
■ Rapid absorption
○ Avoids first pass-metabolism
○ Volatile and gaseous drugs
● Absorption site: Lung alveoli
FLOW:
● Drugs (gas/spray) → absorbed in the
bloodstream
● Drug is inhaled → lungs → alveoli (where
particles will diffuse into the bloodstream) →
body
Introduction: Delivery of Drugs via
inhalation
● While small molecules seems to be absorbed from airways, it is alveolated regions that provide a large
absorptive surface.
● Lungs - portal for systemic delivery of substances (anesthetics, nicotine, and other illicit drugs)
● Deposition of small molecules in the “deep lung” → High absorption rate ⇒ inhalation delivery
attractive for drugs with intended rapid onset of action
● Therapeutics (peptides and proteins) that cannot be delivered systematically and non invasively are
absorbed with different degrees of systemic bioavailability - inhalation
● Lung deposition - critical factor for efficient and systemic delivery
○ Depends on:
■ drug particle properties
➢ Size, shape, density, velocity, charge, hygroscopicity
■ State of the respiratory system
➢ Age, sex disease, lung volume, and anatomy of individual
PROPER DRUG ADMINISTRATION
OF INHALATION PRODUCTS
Dry powder inhaler
How do I prepare the DPI?
1. Hold the DPI(Diskus) in your left hand. Place the thumb of your right hand in the thumb grip. Push your thumb
as far away from you as it will go. This action opens the diskus to expose the lever underneath.
2. Slide the lever away from you until it clicks. This action loads the dose of medication. You will see the dose
counter decrease by one.
Inhaling the medication
Once you have your DPI loaded, follow these steps to inhale the medication:
3. Turn your head away from the DPI and breathe out as much air as you comfortably can.
4. Place the DPI mouthpiece in your mouth and breathe in strong and steady but not too fast, and fill your lungs
completely.
5. Hold your breath for up to 10 seconds.
6. Remove the DPI from your mouth and exhale slowly.
7. Close the DPI by placing your thumb in the thumb grip and sliding the grip back toward you, as far as it will go.
This action resets the inhaler so it is ready to use for the next treatment.
8. If more than one dose is prescribed, repeat steps 1 through 7 for each dose.
Dry Powder Inhalation
DISKUS
Dry Powder Inhalation
Nebulizer solution or suspension
The basic steps to set up and use your nebulizer are as follows:
1. Wash your hands well.
2. Connect the hose to an air compressor.
3. Fill the medicine cup with your prescription. To avoid spills, close the medicine cup tightly and always hold the
mouthpiece straight up and down.
4. Attach the hose and mouthpiece to the medicine cup.
5. Place the mouthpiece in your mouth. Keep your lips firm around the mouthpiece so that all of the medicine goes
into your lungs.
6. Breathe through your mouth until all the medicine is used. This takes 10 to 15 minutes. If needed, use a nose clip so
that you breathe only through your mouth. Small children usually do better if they wear a mask.
7. Turn off the machine when done.
8. Wash the medicine cup and mouthpiece with water and air dry until your next treatment.
Nebulizer solution or suspension
Metered dose inhaler
1. Remove the cap from the MDI and shake well.
2. Breathe out all the way.
3. Place the mouthpiece of the inhaler between your teeth and seal your lips tightly around it.
4. As you start to breathe in slowly, press down on the canister one time.
5. Keep breathing in as slowly and deeply as you can. (It should take about 5 seconds for you to
completely breathe in.)
6. Hold your breath for 10 seconds (count to 10 slowly) to allow the medication to reach the airways of
the lung.
7. Repeat the above steps for each puff ordered by your doctor. Wait about 1 minute between puffs.
8. Replace the cap on the MDI when finished.
9. If you are using a corticosteroid MDI, rinse your mouth and gargle using water or mouthwash after
each use.
Metered dose inhaler
Advantages and disadvantages
ADVANTAGES
DISADVANTAGES
◇ Very rapid absorption due to the large surface
area of the respiratory endothelium ● Bioavailability depends on
◇ Rapid onset of action takes place patient’s inhaler technique and
◇ Bronchodilators and inhaled steroids can be the size of drug particles
targeted to lungs with low levels of systemic generated by the delivery
absorption technique
◇ Direct delivery of active components to the ● Special apparatus is required
diseased organs and cells ● Irritation of the respiratory tract
◇ Prevention of potentially toxic therapeutics may take place
from entering bloodstream, therefore limiting
possible adverse effects upon other healthy
organs
◇ Minimum side effects
◇ No first pass effect takes place
◇ Fewer doses are required
◇ Easy method
Nasal Spray
Types of Nasal Sprays
1. Decongestants - narrows blood vessels in the lining of your
nose, which shrinks swollen tissues
2. Salt-water solutions - also called "saline" nasal sprays which
loosen up your mucus and keep it from getting crusty
3. Steroid nasal sprays - help clear a stuffed-up nose that comes
from a sinus infection by relieving allergy symptoms
How to use a Nasal Spray?
◇ Block one nostril by pressing a finger against it lightly.
◇ Put your thumb at the bottom of the pump bottle. The hole
at the top of the bottle should be underneath your open
nostril.
◇ Squeeze the pump and breathe in gently. Then switch to
the other side and repeat the process.
Nasal Spray
Nasal Spray
Advantages Disadvantages
◇ Large nasal mucosal surface area ◇ Not feasible for high molecular weight
◇ Rapid onset of action ◇ Volume restriction of 25-100 U/L
◇ Bypass the BBB ◇ Drug permeability affected due to ciliary
◇ Improved bioavailability movement and enzymatic inhibition
◇ Ease of administration, noninvasive
References:
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on_Treatment_of_Lung_Diseases
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