Pharmacology2

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additives in aerosols

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1)Preservatives
2)propellants
3)surfactants
4)carrier agents with dry powder inhalants

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Preservative and ph adjuster in the neb

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1)benzalkonium chloride
2)sulfuric acid

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Propellant and dispersing agent in the MDI

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1)chloroflourocarbons
2)oleic acid is the dispersing agent

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Enteral

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Route of administration referring to the small intestine

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First pass effect

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If a drug is highly metabolized by the liver enzymes and is administered orally, most of the drug's activity will be terminated in its passage through the liver before it ever reaches the general circulation and the rest of the body.

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Routes that avoid first pass metabolism

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1)injection
2)sublingual
3)transdermal
4)rectal
5)inhalation

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Factors in the time-plasma curve

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kinetic factors of:
1) absorption
2)DISTRIBUTION
3)metabolism
4)elimination

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Inhaled aerosols

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are deposited on the surface of the upper or lower airway, and are considered topical
2)are intended for local or systemic effect

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L/t ratio

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1)Quantifies the efficiency of drug aerosol delivery to the lung, and is based on the distibution to the airway and gastrointestinal tract
2)proportion of the drug available to the lung, out of the total systemically available drug
3)Any action that reduces the swallowed portion of the inhaled drug, such as resovoir device, can increase the L/t ratio
4)perfectly efficient aerosol would have an L/t ratio of 1

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Total systemic drug level

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1)Is due to airway absorption, plus the amount absorbed from the gastrointestinal tract

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What determines the L/t ratio?

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1)by the rate of first pass metabolism, and the efficiency of the inhalation device in placing the drug in the airway

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Two drugs with the same first pass metabolism_______

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can have different l/t ratios even if the airway deposition or delivery device is the same

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Systemic effects depend on

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1)the amount of active drug absrobed into the system
2)the reactivity of the drug in the oropharnx

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pharmacodynamic phase

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the mechanism of drug action by which a drug molecule causes its effects on the body

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Most drugs exert their effects by___

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binding to protein targets, and sunsequently modulating the normal function of these proteins
-relevant protein targets include receptors, enzymes, ion channels, and carrier molecules

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Catecholamines are metabolized by____

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COMT

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Albuterol is metabolized by

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substrate conjugation

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transmembrane signalling for glucocorticoid, such as inhaled flunisolide or oral prednisone

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diffuses across the cell membrane and attaches to a receptor in the cytoplasm. Complex binds to GRE, which intiates or represses transcription

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Three main compenents of G protein linked receptors

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1)drug receptor
2)G protein
3)effector system

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Stages of G protein interactions

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1)Drug couples to the receptor at the site surrounded by the transmembrane regions of the cell
2)receptor then activates a g protein on the cytoplasmic surface of the cell membrane

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G proteins are so called because____

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They are a family of guanine nucelotide binding proteins

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Beta receptors and GS proteins

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Beta receptors couple with beta-adrenergic receptors, and activate GS proteins

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Potency

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Refers to the dose or concentration at which the drug will produce 50 percent of the desired effect

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Maximal effect

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The greatest reponse that can be produced by a drug, a dose above which no further reponse can be elicted

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two drugs can have the same potency but different____

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Maximal responses

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ED 50 on a therapeutic index curve

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Dose at which half of the subjects improve

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LD 50 on a therapeutic index curve

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Lethal dose for 50 percent of the test population

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Chemical anatagonism

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a direct chemical interaction between a drug and a biologic mediator

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Functional antagonism

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Can occur when two drugs each produce an effect, but the effects cancel each other out.

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Competitive antagonism

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Occurs when a drug has an affinity for a receptor, but no efficacy, and at the same time blocks the active agonist from binding to and stimulating the receptor

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pharmacogenetics

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The study of hereditary or genetic differences

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Stability

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Describes the tendency of aerosol particles to remain in suspension

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Aerosol

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suspension of liquid orsolid particles

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Stability

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Describes the tendency pf particles to remain in suspension

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Penetration

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Refers to the depth within the lung reached by the particles

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Deposition

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Process of particles depositing out of suspension to remain in the lung

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count mode

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the most frequently occuring particle size in a distribution

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count median diameter

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The particle size above and beyond which fifty percent of the particles are found

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Mass median diameter

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the particle size above and below which fifty percent of the mass of the particles is found