Term
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Definition
| The fraction of drug that reaches systemic circulation after a particular route of administration |
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Term
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Definition
| The drugs (generic and parent) are considered equal to each other in containing same active ingredients, dosage form, and route. They must act the same way in the body. All other parts of the drug may be different (additives/lots) Ranges and tolerances vary Generic drugs are as good as the parent. Made to same standards as regular drugs. |
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Term
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Definition
| Describes the drug's chemical composition and molecular structure |
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Term
| Bioavailability depends on route |
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Definition
| IV=100% bioavailable Oral=affected by 1st pass, solubility, formulation, competition, |
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Term
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Definition
| Detoxifies, Makes fat soluble compounds more water soluble, |
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Term
| Dosing pattern by route (dosing curve) |
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Definition
IV = Concentration starts high and decreases
Oral drugs = concentrations starts low and increases, peaks, plateaus, and metabolized off
(same curve for all drugs that are absorbed) |
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Term
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Definition
| Amount of drug you need to get a certain effect |
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Term
| Factors that affect absorption |
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Definition
| Route, Molecular nature of the drug, Food, Dosage formulation, status of the absorptive surface, Rate of blood flow, acidity of stomach, status of motility |
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Term
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Definition
| Enteral (GI), Parenteral, Topical (can have local or systemic effect) |
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Term
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Definition
| The amount absorbed is related to the amount administered. particles travel along concentration gradient |
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Term
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Definition
| A drug given via the oral route may be extensively metabolized by the liver before reaching the systemic circulation (high first-pass effect) |
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Term
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Definition
| The transport of a drug in the body by the bloodstream to its site of action |
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Term
| What factors affect distribution |
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Definition
Size of drug molecule
Polarity (large positively charged molecules cannot be absorbed ie aminoglycocides and must be delivered IV except neomycin tabs for c-diff or gent eye drops)
Water soluble vs. fat soluble
Blood flow
Capillary permeability (blood brain barrier)
Binding to proteins |
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Term
*Important concept r/t distribution
(hint, r/t protein binding) |
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Definition
Only "free" drug is pharmacologically active
Only free drugs can have an effect
Only free drugs can be metabolized |
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Term
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Definition
| drugs bound to proteins are not available nor are they able to be metabolized. Proteins are too big to leave the blood vessels and drugs bound to proteins will also not be able to leave the blood vessel |
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Term
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Definition
| One drug may out-compete the other drug or substance |
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Term
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Definition
Conduction of an action potential down the axon of the cell
• Drugs that act on axonal conduction are not very selective as they will affect conduction in all nerves they have access
• Local anesthetics are the only drugs that work by altering axonal conductions |
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Term
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Definition
Information is carried across the gap between the neuron and the postsynaptic cell
Drugs can elicit selective responses |
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Term
| 5 steps of synaptic transmission |
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Definition
| 1. transmitter synthesis 2. Transmitter storage 3. Transmitter release 4. |
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Term
| What is the location and response to activation of the receptor, Nicotinic N? (peripheral cholinergic) |
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Definition
Location: All autonomic nervous system ganglia and the adrenal medulla
Response to activation: Stimulation of parasympathetic and sympathetic postganglionic nerves and release of epinephrine from the adrenal medulla |
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Term
| What is the location and response to activation of the receptor, Nicotinic M (peripheral cholinergic) |
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Definition
Location: Neuromuscular junction
Response to activation: Contraction of skeletal muscle |
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Term
| What is the location and response to activation of the receptor, Muscarinic (peripheral cholinergic) |
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Definition
Location: All parasympathetic target organs:
Eye: contraction of the ciliary muscle focuses the lens for near vision. Contraction of the iris sphincter muscle causes miosis
Heart: Decreased rate
Lung: Constriction of bronchi and promotion of secretions
Bladder: voiding
GI tract: Salvation, increased gastric secretions, increased intestinal tone and motility, and defecation
Sweat glands: sweating (ACt supply from sympathetic nervous system)
Sex organs: Erection
Blood vessels: Vasodilation (receptors not part of nervous system however) |
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Term
| What is the location and response to activation of the receptor, Alpha 1 (peripheral adrenergic) |
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Definition
Location:
Eye: Contraction of the radial muscle of the iris causes mydraisis
Arterioles: Constriction
Veins: Constriction
Sex organs: Ejaculation
Bladder neck and prostatic capsule: Contraction |
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Term
| What is the location and response to activation of the receptor, Alpha 2 (peripheral adrenergic) |
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Definition
Location: Presynaptic nerve terminals
Response to receptor activation: Inhibition of transmitter release |
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Term
| What is the location and response to activation of the receptor, Beta 1 (peripheral adrenergic) |
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Definition
Location: Heart: Increased rate force of contraction, and increased AV conduction velocity
Kidney: Renin release |
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Term
| What is the location and response to activation of the receptor, Beta 2 (peripheral adrenergic) |
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Definition
Arterioles (heart, lung, and skeletal muscle): Dilation
Bronchi: Dilation
Uterus: Relaxation
Liver: Glycogenolysis (breakdown of glycogen to glucose)
Skeletal muscle: Enhanced contraction, glycogenolysis |
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Term
| What is the location and response to activation of the receptor, Dopamine receptors in the PNS |
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Definition
Location: Vasculature of the kidney
Activation: Dilates renal blood vessels |
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Term
| Receptor specificity of adrenergic transmitters |
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Definition
Epinephrine: can activate all alpha and beta receptors but not dopamine
Norepinephrine: Can activate alpha 1, alpha 2, and beta 1, but not beta 2 or dopamone
Dopamine: Can activate alpha 1, beta 1, and dopamine receptors |
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Term
| Seven regulatory functions of the parsympathetic nervous system |
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Definition
| ➢ Slows heart ➢ Increases GI secretions ➢ Constrict bronchiole smooth muscle ➢ Emptying bladder ➢ Emptying bowel ➢ Constriction of the pupil ➢ Focusing the eyes for near vision |
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Term
| Principle functions of the sympathetic nervous system |
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Definition
➢ Regulation of the cardiovascular system
➢ Regulation of body temperature
➢ Implementation of the “fight-or-flight” reaction |
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Term
| Six categories of cholinergic drugs |
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Definition
1. Muscarinic agonists: Bethanechol
2. Muscarinic antagonists: atropine
3. Ganglionic stimulating agents: Nicotine (Nicotinic N)
4. Ganglionic blocking agents: Trimethaphan
5. Neuromuscular blocking agents: d-tubocurarine and succinylcholine (block ACh @ Nicotinic M)
6. Cholinesterase inhibitors: Neostigmine, physostigmine (indirectly activate all cholinergic receptors) |
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Term
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Definition
| Describes the drug's chemical composition and molecular structure |
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Term
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Definition
| Name given by the US Adopted Name Council |
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Term
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Definition
| The drug has a registered trademak; use of the name is restricted by the drug's patent owner |
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Term
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Definition
| Any chemical that affects the physiologic processes of a living organism (not a food) |
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Term
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Definition
| The study or science of drugs |
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Term
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Definition
| The use of drugs and the clinical indications for drugs to prevent and treat diseases |
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Term
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Definition
| The process drugs of entering the body |
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Term
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Definition
| Drug movement includes Absorption, distribution, metabolism, and excretion |
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Term
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Definition
Drug effect
The study of what the drug does to the body |
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Term
| Volume of drug distribution (Vd) |
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Definition
| how much plasma you would need to have if the drug was present and accounted for in plasma. (Normally 4-5L) Gives an estimate of how the drug is being distributed. A volume of less than 0.071 L/Kg means that the drug is staying in circulation. A volume greater than 0.071 L/Kg means that the drug has left the circulatory system (or that you would have needed to have much more volume to account for the amount of drug measured) Lithium has small Vd and loves to stay in blood and could be dialized out. Pheno has a huge Vd and is out in tissues and cannot be dialized out. |
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Term
| Metabolism (biotransformation) |
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Definition
The biologic transformation of a drug into a more water soluble (polar) compound; Usually into an inactive metabolite, or a less potent metabolite (however may be more potent metabolite ie prodrug)
CYP 450 enzymes are responsible for most of drug metabolism
Codeine is transformed into morphine by enzymes in the liver. Some people do not have the enzyme that metabolizes codeine and do not experience pain relief |
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Term
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Definition
Cytoxin (chemo drug) is completely inactive when given and is made into the active form by enzymes in the liver.
Toxicity of drugs can be affected by metabolism ie Demerol is metabolized into an agent that causes seizures |
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Term
| Phases of drug metabolism |
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Definition
| Phase I: conversion to less lipophilic compound involves the cytochrome P-450 system Phase II: Conjugation |
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Term
| Factors that decrease metabolism |
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Definition
| Cardiovascular dysfunction, renal insufficiency, hepatic disease, genetics, drug therapy, toxins |
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Term
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Definition
| The elimination of drugs from the body |
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Term
| Factors affecting excretion |
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Definition
| Age, gender, body weight and composition, protein binding, kidneys (GFR, tubular reabosorption, tubular secretion), Pulmonary, Bowel |
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Term
| Crockcroft-Gault Equation to Predict GFR |
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Definition
Clcr (cc/min) = [140-age] x IBW/72 x Scr X [0.85 if female]
Creatinine comes from lean muscle. Lost over time
greater than 80 cc/min normal
Less than 50 cc/min impaired renal function
Take general body weight unless pt is third spacing to significant degree |
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Term
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Definition
The time it takes for one half of the original amount of a drug in the body to be removed
Measures the rate drugs are removed
This is a kinetics term, and does not refer necessarily to the duration of the therapeutic effect
Takes approximately 5 half-lives to clear drug |
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Term
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Definition
| The amount of drug administered is equal to the amount of drug eliminated within one dosing interval resulting in a plateau or constant serum drug level |
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Term
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Definition
| Use of a loading dose helps one achieve desired therapeutic effect sooner. It does not alter the time required to achieve steady-state |
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Term
| Linear (First-Order) Pharmacokinetics |
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Definition
Half-life remains constant no matter how high the concentration
Amount of metabolism changes with concentration |
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Term
| Non-Linear Pharmacokinetics (Zero-order) |
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Definition
Fixed amount metabolized per Unit time
Half-life changes with concentration |
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Term
| Michaelis-Menten Kinetics |
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Definition
| Follows linear kinetics until enzymes become saturated |
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Term
| Question: Drug X = renal toxic in patients with impaired renal function, given 100mg, if you get 50mg in renal impairment, med has 0 bioavailability. Will this drug cause toxic effect? |
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Definition
| No. Drug is not bioavailable. Must be available to cause toxic effects |
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Term
| Pharmacokinetics help clinician determine a drugs: |
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Definition
| Onset (time it takes for drug to elicit a therapeutic response), Peak (the time it takes for a drug to reach its maximum therapeutic response), Duration (the time a drug concentration is sufficient to elicit a therapeutic response) |
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Term
Pharmacodynamics
Action vs. Effect |
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Definition
The study of what the drug does to the body
Action is how the drug works (enhancing or inhibiting)
Effect is consequence of drug action on body |
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Term
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Definition
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Term
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Definition
| Liver-like enzymes (CYP) in intestinal tract that like to chew on grapefruit juice (substrate) and are not available to chew on drugs that would normally be broken down thus making more drug available to be absorbed and metabolized. |
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Term
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Definition
| may account for the drugs toxicity, duration of action, side effects etc. |
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Term
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Definition
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Term
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Definition
Action that occurs at therapeutic dose (due to pharmacologic actions of the drug)
May be predictable
May be used to produce a desired therapeutic effect (benadryl = drowsiness)
May decrease over time |
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Term
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Definition
| an unexpected or unintended response to a therapeutic dose of a drug |
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