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104 Cards in this Set
- Front
- Back
Pharmaco dynamics
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Study of the mechanism of action of drugs within the body and how the drugs produce their effects in the body
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Pharmaco genetics
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STUDY of drug reactions in the body that are unanticipated or unusual, and may have a hereditatary basis for the response
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Pharmaco kinetics
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study of drug actions as they move through the body; the way the body absorbs, distributes, metabolizes and excretes drugs; mathematical study of drugs based on time and dose
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Pharmaco Theraputics
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study of drugs used to prevent, treat or diagnose treatment
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Pharmacology
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Study of biology active compounds, how they react to the body and how the body reacts to them
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Pharmacopeia:
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Lists all of the authorized drugs in a country.
Contains: descriptions, recipes, strengths, purity standards, and dosage forms. |
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Efficacy:
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Degree that drug acts as expected.
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Safety:
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Degree to which it lacks harmful effects. No drug completely safe.
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Selectivity:
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Exerts only the effect for which it is given. There would be no side effects. No drug is completely selective.
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Pharmacokinetics:
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How the body acts on the drug. Effects drug concentration at site of action.
Absorption Distribution Metabolism Excretion |
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1938
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Comprehensively Amended the Pure Food and Drug Act:
Established the Food and Drug Administration (FDA) ***Very significant Required government approval prior to marketing a drug Identified required elements for drug labels |
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Efficacy
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Degree to which a drug acts as expected
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Selectivity
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Excerts only the effect for which it is given. There would be no side effects, There is no such thing
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Predictability
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Can determine the exact response
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Federal Food drug and cosmetic act 1938
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Established the FDA
Requires government approval prior to marketing a drug Identifies required elements for drug labels |
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Durham Humprey Amendment 1952
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Specified how prescription drugs can be ordered and refilled.
Acknowledged over the counter drugs as second category drugs |
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Kefauver Harris Amendment 1962
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Required manufacturesa to provide efficacy and safety before marketing a product.
All drugs from 1938 had to be evaluated Ineffective drugs where removed from market |
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Orphan Drug Act 1983
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FDA can provide grants to pharmaceutical to research chronic disease
500 new drugs discovered |
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FDA Modernazation act 1997
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Fast track for AIDS and CAncer drugs
6 mo notice to stop making drug CAn require to test drug in children Clinical database for drugs treating life threatening illnesses Drug company can tout off labell uses |
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Controlled drugs substance act 1970
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Schedules I - V
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Schedules I
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High abuse
Heroin Marijuana LSD |
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Schedules II
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High abuse potential
Morphine Codeine opoids |
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Schedules III
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Less abuse, script expires in 6 Mo Only 5 refills
Vicodin anabolic steroids |
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Schedules IV
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Less abuse, script expires in 6 Mo Only 5 refills
Barbituates benzodiazepines |
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Schedules V
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May or may not require script, depends on State
AntiDiarrheal like litimil |
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Development of New Drugs
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Need pre-clinical Human studies Phase I -III
-Submit Investigational New Drug IND application to FDA - |
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Phase 1
Investigator must get new FDA approval after each new phase before proceeding |
Phase 1 Initial eval small # of normal volounteers Eval metabolism & effect on humans
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Phase II
Investigator must get new FDA approval after each new phase before proceeding |
Limited controlled eval ( double blind studies) given in gradualy higher doses to people with diseases
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Phase III
Investigator must get new FDA approval after each new phase before proceeding |
Extended clinical eval (500 - 5000)( double blind studies) establish safety & Effacacy Lasts 3 -6 mo
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Therapeutic index
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measure drug's safety
50% of animals survives |
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Phase IV. Postmarketing Surveilance
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Prescribed to general public
Previously unknown side effects may be discovered Relies on voluntary reporting by health profs even when not sure FDA Medwatch and USP practitioners Reporting Network |
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Names of Drugs
Chemical |
describes drugs using exact chemical nomenclature to show atomic & molucular structure
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Names of Drugs
Generic |
Non- Propierietary
First letter NOT Capitalized |
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Names of Drugs
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Propierietary
First letter Capitalized |
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Absorbtion
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what gets into the bloodstream. Concerned with the progress of a drug from a dosage form to a biological active form that can pass across tissues to the systemic circulation
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Bioavailability
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% absorbed into systemic circulation after administerion.
depends on route of administration as well as the drugs ability to cross memberanes and reach its target |
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First Pass effect
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Drug absorbed through the stomach ans small intestine must pass through liver before circulating systemically.
Liver can Inactivate drug making less of the drug available to reach the target organ |
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Absorption
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At cellular level occurs through passive transport, active transport, pinocytosis and facilitated diffusion IV is 100% bioavailable
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Distribution
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Tissiue permeability
Blood floww Plasma proteis binding (can bind to that will render the drug inactive, pH, binding to subcelular componant) |
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Drug storage sites
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1.Adipose tissiue- Lipid soluble, drugs tend to rmain for long time due to metabolic rate drug and poor blood perfusion
2. Bone. Toxic agents like heavy metals 3.Muscle 4. Organs. Liver and Kidney |
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First Order excretion
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Rate of removal of drug from body is proportional to the concentration of the drug in the plasma
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Half Time excretion
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Time required for drug concentration in body to reduce by 50%
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Steady State
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Plateau between that administered and that eliminated
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Tolerance
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Decreased response after repeated dose
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0rgans that excrete drugs
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Kidneys, lungs, sweat glands, mammary glands, salvary glands, skin an GI tract
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Therapeutic Index
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Index ratio of the LD50/ED50 Represents an estimate i=of safety of drug
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Route of administration
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Enteral : GI tract
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Route of administration
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Parenteral: Usual meaning injectable- IV. IM, SC, SQ, ID
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Route of administration
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Other - Topical
Inhalation Transdermal |
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Route of administration
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Absorbtion. From stomach or
small intestine (most common) Must cross barriers , epithelial cells lining th GI tract and capillary wall |
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absorption?
What is the most common method for a drug to pass the cell membrane? |
small intestine
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absorption?
What will enhance absorption? |
Most frequently used enteral route
Ease of use Self-Care Least expensive route Can possibly be retrieved if needed. Or can be bound with activated charcoal. Safer |
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absorption?
What will impair absorption? |
Variable absorption:
Solubility factors pH Emptying time Presence of food Drug coatings Inactivation by gastric acid or first pass effect Usually must be swallowed Can cause local irritation |
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Oral preparations
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Tablets
Enteric coated Sustained release |
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Drug Distribution: Passage of drug from blood to interstitial fluid
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Influenced by:
Blood flow to the tissues Ability to of drug leave the vascular system Lipid solubility Amount of protein binding (usually albumin) in the blood Blood brain barrier |
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What impact does protein binding have on distribution?
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Many drugs bind to plasma proteins
When a drug is bound to protein it is not pharmacologically active. Only unbound drug can exert an effect. If the amount of free drug increases there will an increased drug effect even without a change in dose. |
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What is the definition of metabolism?
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Changes drug from its pharmacologically active form to a more water soluble form to enhance excretion
Percentage of drug metabolized each time the drug is circulated to the liver varies from drug to drug |
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What is the significance of first pass metabolism?
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When drugs are highly metabolized during the first circulation to the liver (first pass) little or no active drug is sent to the general circulation.
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How does the CYP 450 enzyme system impact metabolism?
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This system has many substrates.
Most drugs are metabolized by at least one of the P450 isoenzymes. Some drugs may either inhibit or stimulate the P450 enzyme system and result in increased or decreased levels of other drugs. Also can activate prodrugs |
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Results of metabolism
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Facilitates renal clearance
Inactivates the drug Improves therapeutic action Creates prodrugs Can either increase or decrease toxicity |
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3 Processes in Kidney effecting Excretion
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Glomerular filtration: moves drugs from blood to urine. Protein bound drugs cannot pass
Passive tubular reabsorption - lipid soluble drugs move back to blood Active tubular excretion “pumps” move drugs back from blood to urine |
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Loading Dose:
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Larger temporary starting dose
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Maintenance Dose:
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Smaller routine dose
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Plasma Drug Concentration
Minimal effective concentration: |
plasma level of drug below which the drug will not achieve a therapeutic effect
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Plasma Drug Concentration
Toxic concentration: |
level at which toxic effects occur
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Plasma Drug Concentration
Therapeutic range: |
between the Toxic concentration and the Minimal effective concentration:
. Goal of drug therapy |
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What is the significance of drug half-life?
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Plateau (Steady state)
Depends on half-life Achieved in about 4 half lives Peak concentration – highest level should not exceed toxic [] Trough concentration – lowest concentration Should not go below MEC Once achieved it would take about 4 half-lives to eliminate drug if discontinued |
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MEC
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Minimal Effective Concentration
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What is a placebo response?
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An inactive "dummy" medication made up to resemble the active investigational formulation as much as possible
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Pharmacodynamics
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Most drug action occurs as the result of an interaction of the drug with a chemical receptor in the body.
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Drug Effects: Mechanism of Action
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Drug-receptor interactions (agonist/antagonist effects) This is the most common effect.
Drug-enzyme interactions Nonspecific drug interactions |
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Agonist-
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a drug that has affinity, (attraction) binds with and stimulates the receptor
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Antagonist –
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a drugs that has affinity, binds with and blocks action at the receptor.
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Drug Interactions
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Can occur when more than 2 drugs are used.
OTC drugs and substances can interact. Can increase or decrease response of other drug or create yet another response. |
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Drug Interactions
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Can effect Pharmacokinetics through:
Altered absorption Altered distribution Altered metabolism (P450 enzyme system) Altered excretion |
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Drug - Food
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Altered metabolism
Grapefruit juice inhibits metabolism of some drugs. Inhibits one of the P450 isoenzymes (CYP3A4) in the liver AND THE INTESTINES. There is a dose dependent relationship. Can inhibit metabolism for 3 days after last glass of GFJ if taken daily. Increased toxicity: MAOI inhibitors and foods high in tyramine. |
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Adverse drug reaction (ADR):
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harmful, unwanted effect. Occurs at normal doses.
Runs the continuum from bothersome to life-threatening. Greatest risk to elderly and very young |
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Idiosyncratic effect
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Unusual unexpected effect. Genetically determined.
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Iatrogenic disease
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produced by therapy or drug
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Physical dependence:
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with long term use the body has adapted to the drug and abstinence syndrome (physical withdrawal symptoms) will occur if drug is stopped
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Carcinogenic effect:
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can produce a cancer
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Teratogenic effect:
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drug-induced birth defect.
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Hepatotoxicity:
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acute liver failure – rare but life-threatening.
Check liver function tests (LFTs) at periodic intervals Watch for signs of hepatic damage |
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Cardiotoxicity:
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Prolonged QT interval
Some drugs have been withdrawn New drugs need to be tested. www.QTdrugs.org www.fda.gov/medwatch |
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Tolerance
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Decreased responsiveness to a drug due to repeated drug administration
Pharmacodynamic: adaptive response from long-term administration Metabolic: accelerated metabolism from induction of P450 Tachyphylaxis: decreased responsiveness with short term repeated dosing. |
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Herbal (Botanical Medicine) Some Key Points
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About 25% of Drugs are Plant Based but if labeled as a drug are under FDA rules for drugs.
If labeled as a dietary supplement FDA only intervenes after it has been released and shown to be harmful or ineffective. There are many quality control issues. |
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Teratogenic
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An effect on the utero development of an organism resulting in abnormal structure or function. Not generally heritable
Critical periods First 2 weeks preimplantation 3-10 weeks Embryonic lots of development |
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Why are Drugs Used During Pregnancy
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To treat a preexisting condition or one that occurs during pregnancy.
To treat complications of pregnancy such as: Hyperemesis gravidarum Preeclampsia Eclampsia Thrombus formation |
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Placental transfer of drug
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Molecular weight
Protein binding Chemical configuration Lipid solubility – crosses more easily Longer time in bloodstream greater potential for transfer Later in pregnancy because of increase blood flow to placenta Discard idea of placental barrier |
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FDA Pregnancy Categories
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A no risk in controlled studies in women
B no risk in animal studies not validated in humans. Most likely carry little or no risk to the fetus. C animal studies teratogenic no studies in humans. Most likely some fetal risk. D positive evidence of fetal risk X Definite evidence- contraindicated during pregnancy. |
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Drug Dosage
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To administer the correct prescribed dose it may be necessary may need to calculate the amount from available supply.
Two nurses should always check drug dosage calculations in order to prevent overdosage from math errors. Most accurate means for prescriber or for nurse to check to be sure dose prescribed is in safe range is to calculate dose using body surface area (BSA). Get that from a nomogram and use calculation BSA in square meters (from nomogram x Adult dose ______________________________ 1.73 |
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Pharmacokinetic differences with children
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Neonates (1st 4 weeks after birth) have immature livers and kidneys
Infants bodies 75% water IV and sc injections have higher levels and prolonged duration of action Changed ADME with neonates and infants |
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Pharmacokinetic differences with children
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Increased gastric pH Increased bioavailability of most drugs. Decrease acidic drugs.
Variable motility leads to unpredictable bioavailbility Decrease bile acids in neonates |
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Distribution children
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Increased total body water and increased extracellular water in neonates and infants leads to increased volume of distribution of water soluble drugs. Lower volume of distribution of fat soluble drugs.
Decrease in albumin and protein binding can lead to increased free drug |
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Volume of distribution children
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The ratio of the amount of drug in the body to its concentration in the plasma or blood.
Vd = amount of drug in the body plasma drug concentration |
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Metabolism in children
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Decreased P450 enzymes in neonates and infants leads to prolonged half-life and decreased renal clearance.
Implications require lower dosage of some drugs. This changes in young children |
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Excretion: Neonates and Infants
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Decreased glomerular function and
Decreased tubular function Leads to prolonged half-life for elimination. Need dosage decrease. |
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Pharmacokinetic Changes Older adult
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Altered absorption more likely caused by disease processes. Also impacted by
Increased gastric pH Altered peristalsis and decreased intestinal blood flow |
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Pharmacokinetic Changes older adult
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Metabolism is slowed. There is a decrease in hepatic blood flow and decrease in P 450 activity.
Decreased hepatic blood flow may lead to decreased first pass metabolism Decreased cardiac function may lead to decreased metabolism Excretion Renal function is decreases about 10% each decade after age 50. Keep in mind that serum creatinine levels remain normal even though kidney function is impaired. Renal function needs to be measured by Creatinine clearance not serum creatinine. |
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Increased Risks of Adverse Effects and Drug Interactions Older adult
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Polypharmacy
With greater than 4 drugs the possibility of drug interactions increase geometrically. ***Polypharmacy problems are often overlooked by health professionals. Nonadherence Lifestyle |
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White Americans cultural beliefsystem
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Less tolerant to pain which some other cultures accept
Greater expectations for cure or good management Expect to leave office with a prescription Accepting of American Medical Model More accepting of side effects |
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Some Examples cultural beliefsystem
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Hispanics, Chinese and Asians may expect rapid symptom relief but proceed with caution and tend to decrease dosages to avoid even minimal side efects.
Chinese believe in American medicine to relieve symptoms but value Chinese medicine for permanent cure. |
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Pharmacogenetic Influences on Drug Therapy some examples
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G6PD deficiency (x-linked recessive) Common in individuals of African, Mediterranean, Asiatic origin
May get a hemolytic response after administering analgesics, sulfonamides, antimalarials, nitrofurantoin and other drugs |
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Genetic Alteration in debrisoquine-sparteine polymorphism
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Analgesic impact – causes about 5-10% of population especially Chinese to be poor metabolizers of codeine to morphine so lessened therapeutic effect.
Those of African descent may be less responsive to beta blocking agents. May have prolonged drug toxicity to certain drugs if a poor metabolizer. May have increased drug interactions if an extensive metabolizer. |