What is Pharmachology?

1. Correct or decrease the severity of an illness or injury
2. Manage life threatening conditions
3. Substantially reduce patient discomfort

Off-Label drugs are approved by the FDA for one use but are often used for a purpose other than what they were approved. Could be route of administration, dose or diagnosis.

These applications should only be used when approved by a Service Medical Director or by regional protocol

Schedule I medications are not perscribed, dispensed or used for medicinal purposes. They have high abuse potential and have no recognized medical purposes.

Heroin, Marijuana, LSD

Schedule II medications require locked storage, record keeping and controlled waste procedures. They have a high potential for abuse but have legitimate medical purpose.

Fentanyl (Sublimaze), Methylphenidate (Ritalin), Cocaine, Morphine Sulphate

What are 4 sources of medication?

Give an example of each

1. Plant - Atropine, aspirin, morphine, digoxine
2. Animal (endocrine system)- Heparin, Antivenom, insulin
3. Microorganisms (bacteria, fungus, mold) - streptkinase, antibiotics
4. Minerals - Iron, magnesium sulphate, lithium, calcium

1. Concentration
2. Purity
3. Preservatives

1. Capusule - gelatin shell
2. Tablet - round shape
3. Powder - dissolved or mixed in solution
4. Drops - nose or ear
5. Skin - gel, ointment, paste, patch
6. Suppository - wax material
7. Liquid - disolved or suspended for oral use
8. Inhaler/Spray - gas or fine mist for airway

1. Chemical name - used in clinical practice
2. Generic name - proposed by manufacturer and regulated internationally to promote consistency and avoid duplication in drug names
3. Brand name - chose by manufacturer and approved by the FDA. Selected for marketing purposes

1. Direct sunlight
2. Extreme heat or cold (55 to 85 degrees is good)
3. Physical damage to medication containers

The process by which a medication begins to alter a function or process within the body

A desired effect is produced

1. Administered in the wrong route
2. When route of administration malfunctions
3. Inadequate dose
4. Excessive dose

1. Absorption into the body
2. Distribution throughout the body
3. Biotransformation - working
4. Elimination out of the body

The action of the body on a medication

The fate of a medication in the body such as distribution and elimination

A specialized area in the tissues that initiates certain actions after specific stimulations

Receptors exist in various protiens that are connected to cells throughout the body

1. Channels permitting the passage of ions (positive charged particles) in cells may be opened or closed
2. A biochemical messanger becomes activated intiating other chemical reations within the cells
3. A normal cell function is prevented
4. A normal or abnormal function of the cell begins

Agonist medications initiate a response. They can alter cellular activity by attaching to receptor sites and prompting cell response

*Morphine stimulates opiate receptors

Antagonist medications stop a reaction or response. They prevent agonist chemicals from reaching the cell receptor sites and initiating or altering particular cellular activity.

*Narcan - blocks receptor from agonist (opiate)

As the concentration of a medication increases and crosses the the Threshhold level, initiation or alteration of cellular activity begins.

Increasing concentrations of medication cause increased effects until all receptor sites become occupied or the maximum capability of the cell is reached.

The concentration of medication required to initiate a cellular response.

As the potency of a medication increases the concentration or the dose required for a particular cellular response decrease.

Efficacy is the ability to initiate or alter cell activity in the therapeutic desired manner.

Once the cellular receptors become bound with the agonist cellular activity plateaus and no change or further activity is possible. Additional or increase doses will not change the cellular activity.

1. Insulin restriction
2. Glucagon secretion 
3. Inhibition of noreponephrine release 

*Glucagon raises blood sugar and increase liver secretion

What 4 things do Beta I receptors govern?

HEART

1. Chronotropic effect - increased heart rate
2. Inotropic effect - increased myocardial contractility (heart beats harder)
3. Dromotropic effect - increased myocardial conduction (electrical activity in the heart)
4. Renin (hormone secreted when BP is low) secretion for urinary retention

What 4 things do Beta II govern?

LUNGS

1. Bronchodialate - bronchus and bronchiole dialation
2. Insulin secretion
3. Uterine relaxation
4. Arterial dilation in certain key organs

What do Dopaminergic receptors govern?

(receptor subtypes)

1. Competative antagonists
2. Non competative antagonists
3. Partial agonists

They temporarily bind with cellular receptor sites displacing agonist chemicals. They will wear off eventually.

Like Narcan, as the antagoist is eliminated through the kidneys the agonist can pick up strength and continue to bind to the receptor cells. The efficacy of the antagonist is related to its affinity (ability to bind to the receptor)

1. Age
2. Weight
3. Environment
4. Genetic Factors
5. Pregnancy
6. Psychosocial Factors

1. Water - Infants have the most H2O, Elderly the least
2. Lipids/fats - Infants the least, Elderly the most
3. Protien - varies, Elderly dont metabolize well

For a man 50 + (2.3 x inches over 5 ft)

For a woman 45.5 + (2.3 x inches over 5ft)

1. Class A - no risk in 1st trimester
2. Class B - animal studies found no risk or adverse effect to fetus in 1st trimester but not tested in women
3. Class C - animal studies revealed adverse effects but not tested on women or no tests available
4. Class D - Fetal risk to be used in life threatening situation for the mother
5. Class X - Contraindicated

They are clinical changes caused by a medication that are not desired and may cause some degree of harm or discomfort to the patient

1.  Range in severity
2. Can be unexpeccted (idiosyncratic)
3. Adverse reactions can be helpful

TThe amount of medications needed to maintain a desired amount in the body while factoring elimination.

The more substance in the body, the more the body works to eliminate the substance

Determined by manufacturers, a particular adverse effect meaning that 50% of the animals tested had a toxic effect at or above the weight based dose

The process in which a mechanism reducing available cell receptors for a particular medication results in tolerance (decrease efficacy/potency)

Increased metabolism or elimination

1. Increased heart rate
2. Increase blood pressure
3. Activate the sympathetic nervous system

1. Reduce sympathetic and CNS functioning
2. Respiratory depression
3. Bradycardia
4. Hypotention

1. Addition or summation
2. Synergism
3. Potentiation
4. Altered absorption
5. Altered metabolism
6. Altered distribution
7. Altered elimination
8. Physiological antagonism
9. Neutralization

The time a medication concentration can be expected to remain above the minimum level needed to provide the intended action

Depends on the dose, route and clinical status of a patient

The chosen route of administration determines the % of  unchanged medication that reaches systemic circulation

IV administration has 100% bioavailability

1. Physical and chemical properties of a medication
2. Route of administration available with a patient
3. How quickly the effects of the medication are needed

The movement of a solvent (H2O) from an area of low solute concentration to one of high concentration through semipermeable membranes to equalize concentrations of solute on both sides of the membrane

The body strives for homeostatis (balance in the body). Salt decides the balance, H20 follows the salt

Metabolite

A chemical change by the body on a medication (pharmacokenetics)

1. An inactive substance can become active (Active metabolite)
2. An active medication can be change into another active medication (active metabolite)
3. An active medication can become inactive (inactive metabolite)
4. A medication can be transformed into a substance that is easier for the body to eliminate (Active/Inactive Metabolite)

A system in the liver that uses complex enzyme based process to alter the chemical structure of a medication of other chemical. This process occurs in the liver.

Responsible for the metabolism of different medication groups.

1. Zero order elimination
2. First order elimination

1. Choice of Medication
2. Dose/Efficacy
3. Route
4. Timing
5. Manner of administration
6. Monitoring (vitals)

1. Dose is based on size and not age
2. Need to be able to convert lbs to kgs
3. Most meds are based on an ideal weight
4. Size effects the elimination of a medication

* Max dose of a med for a pediatric patient is the adult dose

1. Cardiac output increases
2. Hemocrit (%RBC) decrease
3. Tidal volume and Minute volume increase
4. Inspiration and experation decrease
5. Renal blood flow and urination increase

1. Onset - absorbtion and distribution - the amount of time it takes to work
2. Peak- Highest point between Onset and Duration of Effect
3. Duration of Effect - metabolism and elimination - amount of time the effect of the medication lasts

1. Can be left in for up to 24 hours
2. 100% bioavailability
3. Bones are vascular

1. Slower absorption rate
2. Can prevent adverse cardiac effects

1. Pain
2. Nicotine
3. Nausea/vomiting

Large amounts of medication over a long duration of effect

1. Physical properties
2. Chemical propertied
3. Patient clinical factors

1. Nonionic -uncharged - small and easily pass
2. Lipophilic - attracted to fats and lipids - easily pass
3. Hydrophilic/ionic - attracted to water molecules - have to find a different route through the barrier

1. Blood-brain barrier
2. Blood-placenta barrier
3. Blood-testes barrier

They form a capillary cell barrier preventing the passage of medication molecules through openings in the capillary walls.

1.  Right Patient
2. Right Medication
3. Right Dose
4. Right Route
5. Right Time
6. Right Documentation

1. Antiseizure
2. Anxiolytic (relief of anxiety)
3. Sedative

1. Competative depolarizing
2. Non-depolarizing

It reaches the neuromuscular junction, binds with nicotinic receptors on muscles, causes a brief reaction known as fasciculation and prevents activation by ACh.

Succinycholine - rapid onset

receptor sites on muscle cells that cause contractions

Agents that bind and block drugs that produce muscle relaxation by interfering with nerve impulses between nerve endings and muscle receptors

They occupy but do not activate receptor sites preventing activation of ACh

The process of discharging resting cardiac muscle fibers by electric impluse that causes them to contract

Alters electronic charge present in the cell

1. Not using leading zeroes
2. Not using trailing zeroes
3. Not spelling out magnesium sulphate and morphine sulphate
4. Not spelling out subcutaneous and intranasal

1. Asthma
2. COPD
3. Acute bronchospasm

Atrovent (Ipratropium)

Antagonizes muscarinic receptors causing bronchodilation and decreased mucous in the upper and lower airways

"Fight or Flight"

1. Increase heart rate
2. Increased blood to muscles
3. Increased respiratory
4. Pupil dialation
5. Agonist stimulated

"Feed or Breed"

1. Increased gastric motility
2. Increase blood to digestion
3. SLUDGUM - salivation, lacrimation, urination, defecation, gastric upset and emisis

What do corticosteroids treat?

Name three

Airway inflammation, oxygenation and ventilation

1. Methylprednisolone (Solu-medrol)
2. Dexamethasone (decadron)
3. Prednisone

The early phase of cardiac repolarization where in the heart muscle can not be stimulated to depolarize

Protection limits the potential maximum heart rate by ensuring that a certain amount of time elapses between myocardial contractions

Immediately following the absolute refractory period there is a brief window for an unusually powerful stimulus to initiate depolarization

The period in the cell firing cycle at which it is possible but difficult to restimulate the cell to fire another impulse

 Four classifications of antidysrythmia medications based on the mechanism of an action rather that on specific medications group

Certain medications have a MOA that occurs in more than one class

Phase 4 (Start): cardiac cells are at rest waiting for the generation of a spontaneous impulse from within or transfer of an impulse from an adjacent cardiac cell - coincides with diastole
Phase 0- Rapid influx of sodium ions, K ions exit cell; depolarization occurs
Phase 1 - Sodium decreases, K exits slowly
Phase 2 - Calcium enters cell, K exts
Phase 3 - Calcium ceases, K continues to exit

* During phases 0,1,2, and 3 no additional depolarization may occur due to external stimuli. This protection limits the potential maximum heart rate by ensuring that a certain amount of time elapses between myocardial contractions (absolute refractory period)

1. Ventrical specific
2. Slows sodium in cardiac cells
3. Suppresses ectopic foci (pace maker cells)
4. Resolves V-fib originating in the ventricles
5. Lidocaine

Beta Blockers

1. Competetively Inhibit catecholamine (epinephrine) activation of beta receptor sites
2. Affect Beta 1 moderately affecting Beta 2 (bronchospasm)
3. Calcium blockers may cause massive conduction abnormalities
   
4. Metoprolol (-lol) reduces heart rate during MI and artrial tachycardias - decreases heart rate, reduces BP and lowers myocardial o2 consumption

1. Increase phases 1, 2, and 3 of the cardiac cycle
2. Prolongs the absolute refractory period that treats atrial and ventricular tachycardias
3. Cordarone and amiodarone are used
4. Lengthens the time of each heart beat

Calcium Channel Blockers

1. Reduce BP, control HR and may increase myocardial o2 delivery during ischemia
2. Inhibit uterine contractions during labor,Treat migraines, Cardiomyopathy
3. Decrease velocity of cardiac contraction, slows electrical SA node, pumps more o2 to blood
4. Verapamil (longer shelf life) /Cardizem controls heart rate of pts with A-fib or atrial flutter