Term
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Definition
| 17 years total- first 10 in research, development and clinical trials, 7 years for brand name to complete "return on investment" for the company |
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Term
| pharmacokinetics vs. pharmacodynamics |
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Definition
kinetics- what your body does to the drug, includes ADME
dynamics- what the drug does to your body |
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Term
| what organ reduces the bioavailability of a drug due to first pass metabolism? |
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Definition
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Term
| of all the drug routes of administration, which is considered the most dangerous |
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Definition
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Term
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Definition
| a natural product, chemical substance, or pharmaceutical preparation intended for administration to a human or animal to diagnose or treat a disease |
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Term
| name the 5 types of drug sources |
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Definition
1. alkaloids(plant derived, ex. morphine, coke)
2. microbes(ex. antibiotics)
3. animals(ex. hormones)
4. minerals(ex. lithium)
5. synthetic |
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Term
| name the 3 routes of administration |
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Definition
1. enteral: into digestive track- oral, rectal, sublingual, buccal
2. parenteral: non-digestive track- intravenous, intramuscular, subcutaneous, epidural
3. other: vaginal, inhalation, opthalmic, otic |
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Term
| define first-pass metabolism |
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Definition
where the concentration of a drug is greatly reduced before it reaches the systemic circulation.
related mostly to LIVER |
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Term
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Definition
| Absorption, Distribution, Elimination, Metabolism, Excretion |
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Term
| Name the 3 types of Absorption |
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Definition
1. lipid diffusion
2. aqueous diffusion
3. facilitated diffusion(active transport) |
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Term
| 4 effects of pH on absorption |
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Definition
1. drugs are either weak acids(non ionized/ non-protonated) or weak bases(ionized/protonated) that exist as a combo of ionized and non-ionized forms
2. non-ionized forms can cross membranes(can be absorbed)
3. stomach-pH is highly acidic, highly protonated but weak acids are more absorbed
4. intestines- pH is neutral, weak bases and acids more absorbed than in stomach |
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Term
| 3 ways drugs are distributed in tissues/cells |
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Definition
1. diffusion
2. ion-trapping
3. active transport |
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Term
| 4 things that affect distribution |
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Definition
1. organ blood flow
2. plasma protein binding
3. molecular size
4. lipid solubility |
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Term
| biotransformation aka drug metabolism, 5 things to know |
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Definition
1. it is the enzyme-catalyzed conversion of drugs to their metabolites
2. primary site is the liver
3. conjugation- where the drug is attached to groups for more rapid excretion
4. first-pass metabolism
5. bioavailability- F- what fraction of the drug is getting into circulation in its active form |
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Term
| 2 phases of biotransformation |
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Definition
1. phase 1 reactions- oxidation, hydrolysis, reduction
2. phase 2- conjugation |
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Term
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Definition
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Term
| 3 processes of drug excretion |
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Definition
1. filtration
2. secretion
3. reabsorption |
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Term
| 5 steps of enterohepatic recycling |
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Definition
1. drug is conjugated in liver
2. conjugated drug passes into the bile
3. conjugated drug passes into the intestines
4. c. drug is hydrolyzed in the intestines by intestinal bacteria back to the parent compound
5. c. drug is reabsorbed back to the liver |
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Term
| define half life of a drug |
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Definition
| the elimination time it takes to reduce the plasma drug concentration by 50% |
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Term
| what is the equation for a half life drug |
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Definition
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Term
| what is the steady state of drug concentration? |
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Definition
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Term
| define first order kinetics(3 parts) |
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Definition
1. most drugs exhibit this type
2. the amount of drug eliminated over time is proportional to the plasma drug concentration
3. when drug concentration goes up, the rate of elimination goes up |
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Term
| zero order kinetics(3 parts) |
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Definition
1. very few drugs exhibit
2. when the amount of drug eliminated over time is constant
3. does not depend on drug concentration |
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Term
| what drug dose is often given to reach the steady state quicker? |
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Definition
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Term
| pharmacodynamics- mechanism of action |
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Definition
1. ligand receptor binding
2. signal transduction pathway
3. activation of second messenger molecules
4. altered intracellular process |
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Term
| pharmacodynamics- dose responsive curve |
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Definition
| the relationship between the size of the drug dose and the magnitude of pharmacological effect |
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Term
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Definition
1. g-protein-coupled receptors(GPRC's): b-adrenoceptor>stimulation of adenyl cyclase>increased heart rate
2. enzymes: competitive vs. non-competitive
3. membrane transport proteins: ligand gated ion channels, voltage gated ion channels, neurotransmitter transporter proteins
4. steroid hormone receptors |
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Term
| drug receptor interactions(5) |
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Definition
1. reversible bond types- hydrogen, ionic, hydrophobic
2. law of mass action
3. affinity- tendency of a drug to bind with its receptor
4. stereospecificity
5. Kd=[d] required to saturate 50% of the receptors |
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Term
| agonist intrinsic activity(or efficacy) |
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Definition
stimulate receptors
have affinity and intrinsic activity
full, partial, and inverse(negative) agonists |
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Term
| antagonist intrinsic activity(or efficacy) |
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Definition
block receptors
have affinity but DO NOT HAVE intrinsic activity
competitive antagonists- bind reversibly
non-competitive antagonists- bind irreversibly |
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Term
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Definition
desensitization- short term
down-regulation
ex. levadopa-parkinsons disease, morphine-pain control |
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Term
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Definition
supersensitivity
up-regulation
ex. levadopa-parkinsons, morphine-pain control |
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Term
| define competitive inhibitor |
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Definition
| when a drug binds to the same catalytic site as the endogenous substrate |
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Term
| define non-competitive inhibitor |
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Definition
| when a drug binds to a site other than the endogenous substrate and changes the target so the endogenous substrate can't bind there anymore |
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Term
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Definition
1. discovery and characterization of new drug
2. pre-clinical studies
3. IND(investigational new drug) application
4. clinical studies
5. submission of NDA
6. approval of NDA
7. post marketing surveillance |
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Term
| Clinical phases 1-3 of drug development |
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Definition
phase 1- determine pharmacokinetic properties in healthy men and women
phase 2- small number of people with disease intended to treat
phase 3- 1000's of people with double blind studies with drug and placebo |
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Term
| schedule 1 of drug abuse prevention laws |
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Definition
| high abuse potential, no legitimate medical use, distribution and use prohibited- street drugs like heroin, LSD |
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Term
| schedule 2 of drug abuse prevention laws |
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Definition
| high abuse potential, do have a medical use, distribution is highly controlled- adderall, codeine, demerol, methadone, oxycodone |
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Term
| schedule 3-5 of drug abuse prevention laws |
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Definition
| lower abuse potential, less restrictions for distribution- marinol, vicodin, xanax, serax, lunesta, lomotil |
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Term
| 4 adverse effects of drugs |
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Definition
1. excessive pharmacologic effects
2. hypersensitivity reactions- steven johnson syndrome
3. adverse effects on organs- hematopoietic toxicity, hepatotoxicity, nephrotoxicity, other organ toxicities
4. idiosyncratic reactions |
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Term
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Definition
| change in the pharmacological effect of a drug when it is given concurrently with another drug or food |
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Term
| pharmaceutical interactions |
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Definition
| a chemical reaction between drugs that are mixed together prior to administration or absorption |
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Term
| pharmacodynamic interactions |
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Definition
| additive, synergistic, antagonistic |
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Term
| pharmacokinetic interactions |
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Definition
| altered absorption, drug distribution, drug biotransformation, drug excretion |
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Term
| factors affecting drug safety with ADME |
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Definition
AGE!!
A-unchanged
D-infants are full of water, elderly add fat and lose muscle
M- elderly liver function is declining, oxidative
E- elderly reduced |
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Term
| factors affecting drug safety |
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Definition
1. disease- hepatic and renal disease
2. pregnancy and lactation- teratogenic effects: drug induced developmental abnormalities in the fetus |
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Term
| 3 main types of neurotransmitters |
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Definition
1. acetylcholine(Ach)- cholinergenic neurons, all autonomic ganglia, parasympathetic neuroeffector junctions, somatic neuromuscular junctions, a few sympathetic neuroeffector junctions
2. norepinephrine(NE)- adrenergic neurons, most sympathetic postganglionic neuroeffector junctions
3. epinephrine |
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Term
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Definition
1. Ach receptors- Muscarinic receptors(M1-M5) and nicotinic receptors
2. NE and E receptors- called adrenoreceptors: two types of adrenoreceptors; a-adrenoreceptors, b-adrenoreceptors |
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Term
| cholinergenic drugs that affect neurotransmission |
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Definition
black widow spider venom
bethanechol
pilocarpine
botulinum toxin A
cholinesterase inhibitors |
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Term
| adrenergic drugs that affect neurotransmitters |
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Definition
epinephrine and albuterol
cocaine and amphetamines
MAO inhibitors
Beta-blockers |
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Term
| adrenergic drugs that affect neurotransmitters |
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Definition
epinephrine and albuterol
cocaine and amphetamines
MAO inhibitors
Beta-blockers |
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Term
| muscarinic receptors antagonists |
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Definition
| belladonna alkaloids, semisynthetic and synthetic |
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Term
| nicotonic receptor antagonists |
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Definition
| ganglionic blocking agents, neuromuscular blocking agents |
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Term
| 3 types of Belladonna alkaloids(musc) |
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Definition
1. atropine- pupil dilation, sinus bradycardia, decrease secretions in respiratory system, myasthenia gravis
2. scopalamine- motion sickness patch
3. hyoscyamine- relieve intestinal spasms and pain |
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Term
| 3 main types of semisynthetic and synthetic(muscarinic) |
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Definition
1. ipratropium- used for COPD(emphysema, chronic bronchitis)
2. dicyclomine- intestinal cramping and IBS symptoms
3. oxybutynin- overactive bladder |
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Term
| ganglionic blocking agents(nicotinic) |
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Definition
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Term
| neuromuscular blocking agents(nicotinic) |
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Definition
MOA- block nicotine receptors
paralysis of skeletal muscles
non depolarizing- curare
depolarizing- succinylcholine |
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Term
| 3 direct acting acetylcholine receptor agonists |
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Definition
1. choline esters- acetylcholine, bethanechol, carbachol
2. plant alkaloids- muscarine, nicotine, pilocarpine
3. other- cevimeline, varenicline(chantix) |
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Term
| indirect acting Ach agonists |
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Definition
acetylcholinesterase inhibitors
1. reversible- donepezil, edrophoniom, neostigmine, physostigmine, pyridostigmine(mestonin)
2. irreversible- echothiophate
drugst that augment acetylcholine- slidenafil(viagra) |
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