Robin D Pharmacology For Nursing

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Pharmacology

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The study of substances that interact with living systems through chemical processes

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Pharmacotherapy

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The application of pharmacologic principles and products for the benefit of individual patients

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Drug

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Chemicals that exert an effect on a biological process

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Rx

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Latin: take

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Anti-infective durgs

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Drugs that don't speed up, slow down, or mimic a process in the body. Act as poisons against bacteria, viruses, and fungi while having minimal effect on the host

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Clinical effect

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When a drug acts as expected to for a known purpose. Ex. Benadryl as an antihistamine works to stop runny nose and itchy eyes

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Idiosyncratic effect

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When a drug acts differently than expected. Rare, usually genetic. Ex. Benadryl usually causes drowsiness, but sometimes the opposite occurs

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Side effect

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The effects of a drug other than its main clinical effect. Common, but may be different between individuals. Tylenol PM = Tylenol + Benadryl

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Toxicology

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The study of hte harmful effects of chemicals

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Renaissance physician: "a lot kills, a little heals"

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Paracelsus

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Chemical

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Specific chemical structure of the drug

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Generic name

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Official, non-proprietary name

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Patent life

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20 years

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Roles of the FDA

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Monitor the use of existing drugs, oversee the development of new drugs, approve new drugs.

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Concerns of the FDA

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Safety, efficacy

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Pure food and Drug Act of 1906

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Food safety

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*Food Drug and Cosmetic Act of 1938

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Drug safety (sulfadrug antifreeze)

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Durham-Hunphrey Amendment of 1951

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OTC v. Rx

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Kefauver-Harris Amendment of 1969

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Clinical trial efficacy, pregnancy safety

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Dietary Supplements Health and Education Act (DSHEA) of 1994

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Herbal products

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Orphan drugs

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Drugs that meet requirements for safety and efficacy, but the number of patients who need them is small

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Pregnancy category A

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No problem

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Pregnancy category B

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Does a little good

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Pregnancy category C

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Don't know

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Pregnancy category D

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Little bit bad

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Pregnancy category X

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Known teratogens

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Major teratogens

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Ace inhibitors - renal damage
Androgens - Masculinization of female fetus
Carbamazepine - Neural tube defects
Isotretinoin - CNS, face, ear malformations
Statin drugs - multiple malformations
Tetracycline - teeth discoloration
Thalidomide - shortened, absent limbs
Warfarin - CNS defects
Cancer chemotherapy agents - multiple defects

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Iatrogenicity

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Greek: brought forth by healer. E. complications following surgery/adverse drug affects

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Phase III

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Large croup clinical trials

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Preclinical

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Animal tests, investigating new drugs

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Over the counter

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May be purchased directly by consumer. Safe for use without medical supervision

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Prescription Rx or legend drugs

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Must be ordered by a physician or authorized practitioner. Bottles contain federal legend statement

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Controlled Substances Act

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Drugs with abuse potential placed into specific categories "schedules"

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Schedule I drugs

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Highest abuse potential. NO accepted medical use. heroin, LSD, Marijuana.

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Schedule II drugs

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High abuse potential. Morphine, methadone, amphetamines

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Class III

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Moderate abuse potential. Codeine, hydrocodone

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Schedule IV

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Lower abuse potential. Benzodiazepines, propoxyphene, hypnotics

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Schedule V

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Lowest abuse potential. Cough syrups with small amounts of Codeine.

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Basis of pharmacology

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Receptor theory

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Pharmacodynamics

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Actions of a drug in the body. Agonist or antagonist

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Pharmacokinetics

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Actions of the body on the drug. ADME

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Must have the following ot bind to a receptor

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Appropriate size, electrical charge, and atomic composition

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Appropriate size

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Most drugs are 100 - 1000 MW

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Agonists

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A drug that mimics the activity of the endogenous molecule. Brings about same physiological effect. Does what hormone or NT would have done. Ex. Morphine, Beta agonists, Dopamine

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Antagonists

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A drug that blocks the action of the endogenous molecule. Blocks the activity of an endogenous molecule. Ex. Beta blockers, antihistamines, naloxone reverses the effects of narcotic overdose.

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Modulators

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Drugs that have agonistic effects at receptors in some tissues but antagonistic effects effects in other tissues. Ex. SERMS (selective Estrogen Receptor Modulators)

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Inert binding sites

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Drugs may bind with sites in the body that are not receptors. Ex. protein binding

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Dose

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Amount of a drug required to allow for an adequate concentration at target site

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Efficacy

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The maximum response a drug can produce

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Potency

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Amount of drug required to achieve effect.

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Pharmacogenetics

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Genetic factors. Number of receptor types. Metabolizing factors.

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Do plasma proteins increase/decrease during pregnancy?

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Plasma proteins increase during pregnancy. Doses must be increased because less of the drug is available in the blood.

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ADME

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Absorption, Distribution, Metabolism, Elimination

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Permeation

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A drug moves from one body compartment to another and must pass barriers along hte way

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Aqueous diffusion

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Driven by concentration gradient of the drug, downhill movement described by FIck's law

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Lipid diffusion

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Many lipid barriers separating bodily compartments.

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Special carriers

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Necessary for substances too large or insoluble for diffusion (peptides, amino acids, glucose)

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If a drug's desired effect is LOCAL, the most common routes of administration include

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Topical (skin, nasal, rectal, vaginal), inhillation (lungs), Instillation (eyes, ears)

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If the drug's desired effect is SYSTEMIC, common routes include:

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Enteral (oral, sublingual, rectal), parenteral (not using GI tract) intravaneous, subcutaneous, transdermal, insuffiation (snorting)

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A - Absorption

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Process of a drug entering body. ABsorption into the blood straeam is hte goal of drugs with systemic effects

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Oral advantages

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Easiest for self-administration, relatively safe

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Oral disadvantages

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Adequate absorption?, Gastric irritation, acidic environment and drug stability, "first pass" effect

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First pass effect

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Liver can clear out drug immediately

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Most commonly used medications

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Oral

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Sublingual advantages

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Absorbed through oral mucosa into venous system, avoids "first pass", good for patients with difficulty swallowing

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Sublingual disadvantages

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Only for small amounts of drugs

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Sublingual drug example

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Nitroglycerine

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Buccal

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Placing drig between cheek and gume

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Buccal advantages

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Similar to sublingual. NO first pass, good for patients with difficulty swallowing

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Buccal disadvantages

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Similar to sublingual. Only used for small amounts

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Buccal examples

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Nicorette gum, oral disintegrating tablets for nausea

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Rectal (P.R) advantages

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Severe nausea prevents oral, topical effet desired, Drugs may be administered to unconscience patients

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Rectal disadvantages

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Inconvenient, aesthetically undesireable, drugs may be poorly absorbed

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Inhalation definition

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Suspending drugs in aerosol for for use in the lungs

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Inhalation advantages

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Directly affects the air passages with limited systemic effecs

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Inhalation disadvantages

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Must be administered with proper technique

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Subcutaneous injection

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Beneath the skin, small amount, insulin

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Intramuscular injection

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Larger amounts, vaccines

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Intravenous injection

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Allows for accurate amounts of drug to be placed directly into circulation, emergencies

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Topical and transdermal definition

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Applying drug directly to skin. Local effect only, Ex. lidocane patches

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Bioavailability

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Free fraction of unchanged drug reaching systemic circulation following administration

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Factors affecting distribution

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Tissue permeability, blood flow, plasma proteins

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Volume distribution

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the measure of apparent space in the body availible to contain a drug. Reflects balance between blood in plasma and its binding to tissue. Important for dosing and monitoring

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Malnutrition increases/decreases plasma proteins?

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Malnutrition decreases plasma proteins

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Metabolism

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Biotransformation

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Metabolism

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Body's attempt to prepare ingested substances for elimination from the body (often via kidneys). Transform from lipophilic to hydrophilic

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Most biotransformation occurs in the

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Liver. Metabolism can also take place in the gut

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Metabolism phaze I:

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Reactions add or unmask functional groups like OH or NH2

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Metabolism phaze II

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Reactions are also referred to as conjugations

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First pass metabolism

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After oral administration, drugs are absorbed into the portal venoius system. Before entering general circulation, drugs may undergo significant first pass metabolism. Some drugs first pass rate so great that bioavailibility drops to zero: Ex. nitroglycerin, lidocane

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Cytochrome P-450

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Liver microsomal enzyme for metabolizing xenobiotics

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Saint John's wart, smoking, charcoal broiled foods

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Increases enzymes and liver metabolism. Cna lead to innefective drugs/endogenous agents Ex. birth control/warfarrin

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Erythromycin/grapefruit juice

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Decreases liver metabolism. Can increase availabilities to statin drugs.

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Factors affecting metabolism

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Individual differences (genetics), Liver size and functionality, diet and environmental factors, Afe and sex, Drug-drug interaction, Drug-disease interactions

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Pharmacogenetics

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Genetic polymorphisms influence the expression of phase I and II enzymes, can alter metabolism

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Salicates/Asprin in children

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Reyes syndrome

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Improtant drugs to remember for age/sex metabolism differences

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Ethanol, benzodiazepines, propranolol, salicylates

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Chronic liver disease may...

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affect the hepatic metabolism of drugs (alcoholic cirrhosis, hepatitis)

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Hypo-hyperthyroidism can have effects on the metabolism of...

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Warfarin, digoxin, insulin

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hypothyroid patients may need higher/lower than expected doses of digoxin and insulin, and higher/lower than expected dosages of warfarin

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hypothyroid patients should receive higher doses of digocin and insulin but lower dosages of warfarin.

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Elimination

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The intrinsic ability fo the body to remove a drug from circulation (= excretion)

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Routes of elimination

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Sweat, tears, exhaled air via the lungs, Bile via the liver, Urine via hte kidneys

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Clearance

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The measure of the body's ability to eliminate a drug. Closely related to renal physiology. Based on creatin clearance.

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Elimination half life

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Time required to decrease concentration of the drug by one-half
t 1/2 x 5 = effective clearance from body