Pulmonary

Pulmonary drugs can be 

 

Local

 

or Systemic

 

Local= Asthma, Mucolytes, Cystic Fibrosis, Respiratory Distress syndrome

 

Systemic=Afrezza(insulin powder inhaler recomb human insulin), ADASUVE (loxapine restricted use for schizo)

2 main methods drug delivery

 

[image]

Intratracheal

[rare,,,,drug liquid instilled into trachea fro deeper distribution]

 

Aerosol Inhalation [intartracheally or oral inahaled]

Inhalers can be
dry powder or propellant driven
nebulizers can be
air jet or ultrasonic
Respiratory tract

upper air way[nose and nasal cavity]

 

tracheo-bronchial tree[gas exchange]

Pulmonary Epithelia

ciliated epithelia

[pseudostratified ciliated columnar/w/ goblet cells]

 

mucus= similar composition and func to that of nasal cavity

[prevents dehydration,traps foreign particles]

[MUCOCILIARY ESCALATOR]

SURFACE LINING LAYER COVERS __________WHERE MACROPHAGES ROAM FREELY
ALVEOLI
tHESE REGIONS ARE LINED WITH PSEUDOSTRATIFIED CILIATED COLUMNAR EPITHELIAL PULMONARY CELLS AND GOBLET CELLS

LARYNX

TRACHEA

NASOPHARYNX

NASAL CAVITY

BRONCHI

fATE OF RX AT THESE SITES

 

OROPHARYNX

 

TRACHEOBRONCHIAL REGION

 

ALVEOLI

OROPHARYNX= SOME ABSORPTION POSSIBLE,SOME RX WILL GO TO GI TRACT[***SUBJECT TO HEPATIC 1ST PASS]

 

TRACHEOBRONCHIAL REGION= NO HEPATIC 1ST PASS,TO PHARYNX THEN GI.RX DEPOSITS IN MUCUS,SOME SYS ABS

 

ALVEOLI= DRUG DEPOSITS IN SLL[SURFACE LINING LAYER]

WHICH PULMONARY REGION IS SUBJECT TO HEPATIC FIRST PASS?????
OROPHARYNX

SMALLER AERODYNAMIC DIAMETER WILL

[BASED ON SIZE,SHAPE DENSITY]

PENETRATE FURTHER IN LUNGS

 

EXTRATHOCIC=>10

UPPER TRACHEOBRONCHIAL=5-10

BRONCHIOLES,ALVEOLAR DUCT,ALVEOLI= 1-5

ALVEOLAR OR EXHALATION OF PARTICLE= SUBMICRON

INC PARTICLE VELOCITY MEANS_________

INCREASED IMPACTION

(particle not able to bend with airstream,,,just goes straight)

RAPID SHALLOW BREATHING FAVORS _____ DEPOSIION

 

 

SLOW DEEP BREATHING FAVORS 

TRACHEOBRONCHIAL PENETRATION

 

DEEPER PENETRATION

HOLDING THE BREATH FAVORS
SEDIMANTATION AND DIFFUSION
PULMONARY = POOR DRUG EFFICIENCY _____ ENDS UP IN ____________

80-95%

 

 

gI TRACT

PROPELLANTS AR NONPOLAR

 

EX: OF PROPELLANTS ARE>>>>>

HFA 134

 

CFC(NOT USED ANYMORE,BREAKS DOWN FASTER IN ATMOSPHERE)

PRESSURE IN MDI

3 ATM

 

[COME IN SOL AND SUSP]

SOL COSOLVENT = ETHANOL

SUSP

[MORE COMMON DUE TO POOR SOLUBLE DRUGS]

[MUST BEMICRONIZED]

EXCIPIENTS OF MDI:

dISPERSING AGENTS AND SUSPENDING AGENTS

SURFACTANTS: OLEIC ACID, SOYA LECITHIN(CAN PREVENT PARTICLE ADHESION)

POVIDONE

 

COSOLVENTS:ETHANOL

DOSE REDUCTION CAN OCCUR WHEN____

INHALER [HFA] IS DROPPED

 

(2-4 SPRAYS TO PRIME INHALER)

PRIME INHALER WHEN_____

1ST USE

 

AFTER DROPPING

 

AFTER CLEANING

SPACERS SLOW ACTUATION TO ABOUT ______
10 m/sec
SPACERS

REDUCE PARTICLE SIZE

PRODUCE BETTER CLOUD FOR RESPIRATION

REDUCE AEROSOL VELOCITY

MAKE MDI EASIER TO USE FOR PT

REDUCE OROPHARYNG DEPOSITION

[SOUND WHEN INHALING INDICATES BREATING IS TOO FAST]

FEATURES OF SPACERS

ANTISTATIC 

FLOW INDICATOR(SOUND IF TOO FAST)

VOLUME

ANTISTATIC COATING

PRESENCE OF VALVES

 

VORTEX(AEROCHAMBER)

AEROCHAMBER-HC

AEROMASK ES

AEROCHAMBER VALVE HOLDING DEVICE

 

SPACERS

 

ADVAIR

FLUTICASONE PROPIONATE & SALMETEROL XINAFOATE

 

MICRONIZED SUSP 

NO EXCIPIENTS

COMBIVENT AND SPIRIVA ARE _____ AND ___________

RESPIMAT INHALERS

LIQUID METERED DOSE INHALERS

 

cOMBIVENT=IPRATROPIUM BROMIDE & ALBUTEROL

SPIRIVA=TIOTROPIUM BROMIDE

 

[SOFTER AND SLOWER AEROSOL THAN pMDI]

[SPRING MECH]

 

SMALL POWDERS TEND TO _________

GET MORE ADHESIVE AND COHESIVE

(THIS IS PROBLEM WITH DPIs)

DPIs ARE _______ TO THE APPROPRIATE SIZE THEN HAVE A CARRIER POWDER USUALLY______&____

MICRONIZED

 

LACTOSE & GLUCOSE

(LARGE AND LESS RESPIRABLE)

UNIT DOSE DPIs=hard gel capsule with powder punctured

ROTAHALER=CAPSULE BROKEN OPEN IN DEVICE [VENTOLIN]

HANDIHALER=CAPSULE PUNCTURED ON SIDE INSIDE DEVICE [SPIRIVA]

AEROLIZER= CAP PUNCTURED ON EACH END IN DEVICE

[FORADIL=formoterolfumarate]

MULTI UNIT- DOSE INHALERS = several doses loaded in at same time[PIERCED BEFORE INHALED]

DISKHALER= CONTAINS CIRCULAR DISK THAT CONTAINS POWDER CHARGES PACKED SEPERATE IN ALUMINUM

[RELENZA=zanamivir w/ lactose]

 

DISKUS = powders contained w/in a blister strip

[SEREVENT=salmeterol xinafoate w/ lactose]

[ADVAIR DISKUS= fluticasone propionate & salmeterol xinafoate w/ lactose]

MULTIPLE DOSE DPI

pulmicort flexhaler[micronized budesonide w/micronized lactose]

 

foradil certihaler[formoterol furoate]

 

asmanex twisthaler[micronized mometasone furoate w/ lactose] 45 day shelf life

 

small volume nebulizer tx

Tx time 7-10 mins

 two type=

[air jet nebs=air mist EX:PARI LL NEBULIZER]

[ultrasonic= piezoelectric crystals vibrate when electrically excited.waves make geysers]

small volume nebulizer tx

Tx time 7-10 mins

 two type=

[air jet nebs=air mist EX:PARI LL NEBULIZER]

[ultrasonic= piezoelectric crystals vibrate when electrically excited.waves make geysers]

nebulizer (generally isotonic solutions)

1-10% rx make it to lungs

 

lot of rx adheres to device

 

may denature protein drugs

 

between brands generate diff particle sizes

 

 

 

 

nebulizer cosolvents

glycerin

 

propylene glycol

neb pH

above 5

inc risk of bronchiospasm below 5

 

solutions w/out preservatives are for single use

 

neb must be sterile

pt populations

 

MDI

 

DPI

 

NEBULIZER

MDI=OLDER THAN 3 YRS W/ SPACER,,,,

OLDER THAN 7 W/OUT SPACER

 

DPI=3-4 YRS OLD

 

NEBULIZER=VERY YOUNG OR VERY OLD

DRUGS SHUD BE THIS SIZE TO GET INTO THE LUNGS

 

1-5 MICRONS

 

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