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What is Pharmacology?
The study of drugs.
What is a Drug?
Any substance or chemical that effects processes of an organism.
What are the 3 different types of names for drugs?
- Generic: short/simple (Ibuprofen, Acetaminophen)
- Trade: (proprietary) Registration, patented & owned. (Motrin, Tylenol)
- Chemical: Molecular structure & chemistry (propionic acid: Motrin)
Name some "prils" (ACE inhibitors).
- Lisinopril (Prinivil)
- Benazapril (Lotensin)
- Enalapril (Vasotec)
"Prils" are ACE Inhibitors, how do they work?
ACE Inhibitors: Angiotensin-converting enzyme inhibitors. They cause vasodialation, which <BP by decreasing tension in the blood vessles.
"Sartans" are ARBs, how do they work?
- ARBs: Angiotensin II Receptor Blockers
- they cause vasodilation & <Peripheral resistance.
Name some "sartans" (ARBs)
- Losartan (Cozaar)
- Valsartan (Diovan)
- Telmisartan (Micardis)
What are "triptans"?
- Seritonin Agonists
- ie: Mirtazapine (Remeron)
"Prazoles" are PPIs, Explain how they work.
PPIs are Proton Pump Inhibitors, they suppress gastric acid secretions by inhibiting the hydrogen/potassium adenosine triphosphate (ATPase) enzyme system located in the gastric parietal cells.
Name some "prazole" drugs
- Omeprazole (Prilosec)
- Lansoprazole (Prevacid)
- Rabeprazole (Aciphex)
- Pantoprazole (Protonix)
Olols, alols, & ilols are Beta Blockers, explain how they work.
They block the beta1 & beta2 receptor sites. They <the effects of the sympathetic nervous system by blocking the axn of the catecholamines epinephrine & norepinephrine, therby <HR & BP.
Name some olols, alols, and ilols.
- Atenolol (Tenormin)
- Metoprolol Tartrate (Toprol XL, Lopressor)
- Nadolol (Corgard)
"Dipines" are CCBs (Calcium Channel Blockers), explain how they work.
Calcium activates myocardial contraction, ^ workload of the heart & the need for more O2. CCBs relax coronary artery spasm & relax peripherial arteriols <cardiac O2 demand.
Name some "dipines".
"Tidines" are H2 blockers, explain how they work.
they block the H2 receptors of the parietal cells in the stomach, thus reducing gastric acid secretion & concentration.
Name some "tidine" drugs.
- Cimentidine (Tagamet)
- Ranitidine (Zantac)
- Famotidine (Pepcid)
"Zepams" or "Zolams" are Bensodiazepines, explain how they work.
^ the axn of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) to the GABA receptors. Neuron excitability is <
Name some benzodiazapines (zepams & zolmas)
- Alprazolam (Xanax)
- Temazepam (Restoril)
- Lorazepam (Ativan)
- Diazepam (Valium)
- These are Schedule IV meds
"Statins" are Antihyperlipidemic drugs, how do they work?
- They are hepatic HMG-CoA reductase inhibitors.
- they inhibit cholesterol synthesis in the liver which <concentration of cholesterol, <LDL & ^HDL
Name some "statins"
- Atrovastatin (Lipitor)
- Pravastatin sodium (Pravachol)
- Simvastatin (Zocor)
Explain these acronyms...ER, XL, SR, CD, LA.
Extended Release, Extended Length, Sustained Release, Controlled Release, Long Acting.
Name some drugs that indicate how often it is taken.
- Nitro-bid (Take BID)
Where do drugs come from?
List forms that drugs come in.
- Tablets: timed, enteric-coated, SR
- Solutions, suspensions
- Topical: Dermatological, patches
- IV, IM, SC, Intrathecal
List drug forms from fastest to slowest for onset of axn
IV, IM, SC, Intradermal, Inhalents, solutions/suspensions, emulsions, topical, lozenges, implants, tablets, capsules, suppositories.
Name the Parenteral routes
IV, SC, IM, Intradermal
What are the 5 patient rights?
- Right: Patient
What are the 5 extra rights of a patient?
- Right: Documentation
- Right to educate
- To Refuse
Guidelines for correct MED administration.
- Read Dr's orders carefully
- Verify the identity of the patient
- Read the Med label carefully
- Verify dosage calculations
- Implement any special handling
- Know the reason why drug is being given
What is required of a nurse to give a PRN med?
- Reason for drug use
- ASSESSMENT of pt's needs
List the 3 ways drugs move.
- Passive Diffusion
- Facilitated Diffusion
- Active Transport
Explain Passive Diffusion
Moving from an area of higher concentration to an area of lower concentration. No Energy required.
Explain Facilitated Diffusion.
Moving from an area of higher concentration to an area of lower concentration, drug is carried by an enzyme of protein.
Explain Active Transport.
Moving from an area of lower concentration to an area of higher concentration. (against the concentration gradient) *REQUIRES ENERGY
What does drug movement depend on?
The drugs ability to cross cell membranes.
How do lipid-soluble drugs move?
They cross the cell membrane by dissolving in the lipid layer.
How do water-soluble drugs move into a cell?
They cross thru via pores and channels.
- Lipid-soluble drugs cross the cell membrane better than water-soluble
- Most drugs are lipid-soluble
What is the 1st phase of drug action?
- Pharmaceutic (Dissolution)
What is the 2nd phase of drug action?
- ADME (Absorption, Distribution, Metabolism, Excretion)
What is Pharmacokinetics?
The process of drug movement to achieve drug action.
What are the 4 basic processes of Pharmacokinetics?
- Metabolism (Biotransformation)
Explain the Pharmacokinetic phase of Absorption.
The movement of drug particles from the GI tract to body fluids by passive absorption, active absorption or pinocytosis.
What is pinocytosis?
When cells carry a drug across their membrane by engulfing the drug particles.
What does absorption depend on?
- Dosage form & route
- Fxn, & PH of GI tract & if theres food in it
- Drug solubilty & ionization
- *drugs that are lipid-soluble & non-ionized are absorbed faster.
What affects absorption?
- Blood flow
- PH of stomach acid
- Poor circulation
- Route of Administration
List the most acidic organ to the least.
- Stomach: ph 1-3
- Duodenum: 6
- Jejunum & ileum: 7-8
How will a low pH affect the absorption of acidic drugs?
it will ^ absorption
How can a low pH affect certain drugs?
Can destroy the potency
Bioavailability is the % of an administered drug that is available in the body to produce an effect.
What factors can alter bioavailability?
- Drug form & route
- GI mucosa & motility
- Food & other drugs
- Changes in liver metabolism
What is the % of bioavailability of oral, IV, & IM/SC routes?
- Oral is always <100%
- IV is 100%
- IM/SC: High bioavailability
Explain the First-pass effect
The rapid inactivation (by rapid metabolism) of some oral drugs by the liver before reaching the systemic circulation.
Do IV drugs have a First-pass effect?
NO, they bypass the liver = ^drug in circulation.
Process by which a drug is moved from the circulation to its site of action.
Name areas of rapid distribution.
- (d/t having ^blood supply to those areas)
Distribution is influenced by what factors?
- Blood flow
- Water soluble vs fat soluble
- Blood-brain barrier
- Protein-binding effect
Name areas of slow distribution.
Explain "Free Drugs"
Drugs NOT bound to a protein, they are ACTIVE & can cause pharmacologic responses.
What happens when the amount of free drug in circulation decreases?
More bound drug is released from the protein to maintain the balance of Free drug.
Explain protein binding.
An interaction in which a drug binds to proteins in the body.
Explain what happens when a drug has a High First-pass effect.
It means that the amount of available drug is reduced.
List some factors of Protein-binding.
- Drug that is attached to a protein can not act. It allows for storage and release of the drug as needed for longer duration of axn.
- Unattached drug is free to act.
- this reduces risk of toxicity.
With protein bound drugs there can be interactions when what occurs?
When two or more protein bound drugs are competing for protein binding sites.
Explain Metabolism (Biotransformation).
A process by which the body inactivates drugs.
Where is the primary site for metabolism?
Drugs that are inactivated by liver enzymes become?
- Inactive metabolites
- Water-soluble substances
- Active metabolites
Metabolism can effect toxicity by either ______ or _______ it.
Increasing or decreasing it.
What is Cytochrome P450?
A liver enzyme: breaks down drugs
Explain an enzyme inducer.
Drug that causes liver to synthesize more enzymes -->increasing the rate of biotransformation--> reducing the drug level in the blood.
Explain an enzyme inhibitor.
Drug that blocks the effects of the enzymes --> reducing the rate of biotransformation --> Increasing drug levels in blood
Biotransformation can be influenced by what things?
- Age Enzyme induction
- Body weight Nutritional status
- Genetics Drug Competition
- Metabolic rate First-pass effect
- Illness Half Life
- Tolerance Dependence
- Concurrent use of other drugs
Factors that decrease metabolism (biotransformation).
- Enzyme inhibitor
- Liver Dysfunction
- Cardiovascular dysfunction
- Erythromycin or Ketoconazole drug thereapy
Factors that increase metabolism (biotransformation).
- Enzyme inducer
- Barbiturate therapy
- Rifampin therapy
Delayed drug metabolism can result in what?
- Accumulation of drugs in system
- Prolonged action of drugs
Stimulating drug metabolism causes what?
Diminished pharmacologic effects
What is excretion?
Elimination of drug and metabolites from the body.
What are the two primary routes of elimination/excretion?
- GI tract (feces)
- Kidneys (urine)
What are other routes of excretion?
Sweat, breast milk, breathing, saliva
How does the creatinine clearance test work?
By comparing the level of creatinine in the urine w/the level of creatinine in the blood.
What is creatinine?
A metabolic byproduct of muscle that is excreted by the kidneys
What is the most accurate test to determine renal fxn?
Kidney disease can result in what & how does this effect excretion?
Decreased GFR or decreased renal tubular secretion, causing drug excretion to be slowed or impaired. Drug accumulation w/possible severe adverse reactions can result.
What is the Half-life of a drug
The time it takes for one 1/2 of the original amount of drug in the body to be removed.
The Half-life of a drug is a measure of what?
The rate at which drugs are removed from the body which is determined by the rate of metabolism & excretion.
Most drugs are considered effectively removed after how many Half-lives?
What does the Half-life help the doctor determine?
Dose amount, frequency & duration of therapy.
What is a Peak Level?
The highest plasma concentration of drug at a specific time.
What is a Trough Level?
The lowest plasma concentration of a drug, & it measures the rate at which the drug is eliminated.
Explain Therapeutic Range of drug concentration in plasma.
It should be between the minimum effective concentration in the plasma for obtaining desired drug action & the minimum toxic concentration.
Explain duration of action
The length of time the drug has a pharmacologic effect.
Explain Peak Action.
Occurs when the drug reaches its highest blood or plasma concentration.
What is MEC?
Minimum effective concentration
What is Onset of Action?
The time it takes to reach the MEC