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Pharamology
The study of drugs and their actions on the body
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Therapeutics
The study of drugs used to cure, treat, or prevent disease
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Pharmacotherapy
A combination term for pharmacology and therapeutics
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Disease management
Collective of all aspects of disease and not just the pharmacotherapy
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Therapeutic classification
- Drugs are classed or grouped according to the drug use
- For example, therapeautic classification of bronchodilators can have several drug classes (xanthines, beta adrenergics, parasympatholytics)
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Pharmacologic classification
Drugs with similar characteristics
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How are drug developed?
- drugs are derived from a variety of sources:
- Plants
- animals
- minerals
- chemicals
- Recombinant DNA
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Most drugs are now...
Chemically synthesized, but in the future may be bioengineered
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Chemical name
- Describes the chemical structure and is long and very complicated
- This has little clinical use but is needed to make the drug
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Generic name
- Given by United States Adopted Names (USAN) council
- Not owned by a particular company, called the nonproprietary name, and usually writted in lowercase
- Example: albuterol sulfate
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Brand or Trade name
- Owned by company that discovered and produced the drug
- Example: Sudafed^registered is the trade name for generic psudoephedrine
- Trade names are usually capitalized and have the regestered trademark symbol
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Bioavailability
Measures the amount of drug absorbed into circulation
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What are the influence factors of bioavailability?
- Drug solubility
- Dosage form
- Route of administration
- pH
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Different routes of adminstration!
- Oral
- Sublingual
- Rectal
- Nasogastric tube
- Intravenous
- Intramuscular
- Transdermal
- Inhalation
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Pharmacokinetics
Kinesis means movement, and this literally means what happens to a drugfrom the time it enters the body to the time it leaves the body
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What are the different phases of pharmacokinetics?
- Absorption
- Distrubtion
- Metabolism
- Elimination
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Absorption
- This is the rate limiting step
- In other words, how fast it takes the drug to dissolve determines the rate of effect
- IV is the fastest because it bypasses the absorption process by going directly into the bloodstream
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Distrubtion
Major vehicle for distrubtion is the bloodstream
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What effects distrubtion of a drug?
- Blood fat
- Fat
- Water solubility
- Protein binding
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Metabolism
After the drug has been absorbed and distributed, the body works to break it down via metabolism into several components called metabolites
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What is the major organ for metabolism?
The liver
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Elimination
This is the last step of pharmacokinetics, where the drug is excreted from the body
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What are the different ways drugs can be elimenated?
- Urine
- Feces
- Pulmonary system
- Skin
- Hair
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Half life or T(1/2)
- Time it takes for the concentration of the drug to decrease by one-half after adminstration
- Drugs with short half lives don't stay in the bosy long
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First pass effect
- After being absorbed, some drugs do not go directly into circulation but pass threw the liver first, where enzymes can begin to inactivate.
- This is one reason why equivalent oral doses are higher than IV doses
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Steady State
- A continuous infusion gives a regulated, consistent dosage over time of drug concentration in the plasma
- Maximum concentration in the body
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Variables that affect passage of drugs across plasma membranes!
- A size of the drug molecule
- Ionization of drug
- Lipid solubility across the lipid cell membrane
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Drugs with a high ED 50 are...
More potent than drugs with a low ED 50
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Therapeutic Index
The ration between the minimun effective dose and the maximun tolerated dose
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Affinity
The stregth of binding between a drug and a receptor
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Agonist
- Binds with receptor (affinity) and causes a response
- In other words, it activates the receptor
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Antagonist
Binds with receptor (affinity) but has little or no response
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Additive interaction
- The sum of the effect of two drugs given together is equal to each of them given separately but at the same time
- 1 + 1= 2
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Synergistic interaction
- Giving two drugs together results in a greater effect than expected if given seperately
- 1 + 1= 3
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Potentiation Interaction
- One of the drugs has no direct effect yet increases the effect of the other drug
- 1 + 0= 3
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The nervous system consist of...
- Central nervous system
- Perpheral nervous system
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Central Nervous System
Comprised of the brain and spinal cord
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Peripheral Nervous System
- Comprised of all the nerves outside the brain and spinal cord
- Afferent and Efferent nerves
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Afferent nerves
Carry sensory information from parts of the body to the brain for processing
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Efferent nerves
- Carry impulses away from the brain and spinal cords
- Also known as motor nerves
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The peripheral nervous system is divided into...
- Somatic nervous system
- Autonomic nervous system
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Somatic nervous system
Controls skeletal muscle movement during voluntary movement and is under concious control
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Autonomic nervous system
- The involuntary or automatic respons
- Regulates the cardiopulmonary and digestive systems
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The autonomic nervous system is divided into...
- Sympathetic
- Parasympathetic
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Sympathetic branch
- Alert system for stressful situations
- Fight or fight response
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Parasymapthetic branch
- Concerned with daily body maintenance and maintaining a homeostatic enviroment
- Sleep and Eat system
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Aersol
Supension of solid or liquid particles within a gas
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Aersol therapy
Delievery of either solid or liquids into the respiratory tract for therapeutic purposes
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Goals of Aerosol therapy!
- To humidify inspired gas, which may be dry or humidity deficient
- To improve the mobilization and elimination of secretions
- To deliever medications to the respiratory tract
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Advantages of aersol therapy!
- Smaller requried doses
- Quick drug response
- Fewer less sever side effects
- Painless and convenient
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Disadvantages of aersol therapy!
- Difficult to delivery percise dose
- Requries patient compliance and education
- Equipment maintenance
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10 to 15 micron particle size
These particles get stuck in the upper airways (nose and mouth)
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5 to 10 micron particle size
These particles penetrate to larger bronchi
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1 to 5 micron particle size
These particles pentrate to lower airways, where most bronchodilators are needed
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Less than 0.5 micron particles size
- These particles penetrate to the alveoli
- May also be breathed right back out
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Ultrasonic nebulizers
- Are quite efficient
- They have a very low dead volume and may not need diluent, which shortens treatment time
- However they are very expensive
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Antiasthmatics or mast cell stabilizers
- Desensitize the allergic response
- Which then prevents or decreases the incidence of asthma
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Dead space volume
- The portion of the dose that cannot be nebulized
- Can be as little as 1 to 3 ml
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What percentages of patients uses a MDI correctly?
60 to 70% of patients do not use the MDI correctly
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Dry powder inhaler (DPI)
- Devices that deliver the drug in powder form to the lungs for absorption
- Have no propellant or external power source
- Small self generating devices
- Patient must generate greater than 50 liters per minute for the device to properly aerosolize the dry powder
- Difficult for small children and someone in acute respiratory distress to use
- Works well in cold weather unlike MDI
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Nicotinic receptors
- Found at the skeletal muscles in the somatic system and at all preganglionic sites in the parasympathetic and sympathetic nervous system
- These receptors simply pass the signal on to the postsynaptic neuron
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Muscarinic receptors
- Found at the postganglionic site of the parasympathetic nervous system
- ACh binds found on involuntary muscles or glands
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Acetylcholine (ACh) is metabolized by...
Acetychlinestrase (AChE)
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What drugs will stimulate or mimic the parasympathetic system?
- Cholinergics
- Parasympathomimetics
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Drugs that stimulate the parasympathetic receptors...
Causes slowing of the heart and bronchonstruction
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Drugs that stimulate the sympathetic receptors...
Beta1 speed up the heart rate and beta2 causes bronchoconstruction
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Alpha stimulation causes...
- Smooth muscle of the blood vessels
- Vasoconstriction
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Beta1 stimulation causes...
- Found primarily in cardiac muscle
- increase in heart rate
- increase in conduction
- increase in contraction
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Beta2 stimulation causes...
- Smooth muscle of airways and certain muscles
- Vasodilation
- bronchodilation
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Acetylcholine is the main neurotrasmitter in...
- All autonomic preganglionic and at parasympathetic postganglionic synapses
- Somatic system or preganglionic sites
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Cholinergics
- Drugs that stimulate parasympathetic receptor
- Responses cause slow heart rate and bronchoconstruction
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