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Section 1
intro
59
Pharmacology
Undergraduate 4
10/19/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
drug patents time frame
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
Term
pharmacokinetics vs. pharmacodynamics
Definition
kinetics- what your body does to the drug, includes ADME

dynamics- what the drug does to your body
Term
what organ reduces the bioavailability of a drug due to first pass metabolism?
Definition
the liver
Term
of all the drug routes of administration, which is considered the most dangerous
Definition
IV
Term
define drugs
Definition
a natural product, chemical substance, or pharmaceutical preparation intended for administration to a human or animal to diagnose or treat a disease
Term
name the 5 types of drug sources
Definition
1. alkaloids(plant derived, ex. morphine, coke)
2. microbes(ex. antibiotics)
3. animals(ex. hormones)
4. minerals(ex. lithium)
5. synthetic
Term
name the 3 routes of administration
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
Term
define first-pass metabolism
Definition
where the concentration of a drug is greatly reduced before it reaches the systemic circulation.

related mostly to LIVER
Term
define ADME
Definition
Absorption, Distribution, Elimination, Metabolism, Excretion
Term
Name the 3 types of Absorption
Definition
1. lipid diffusion
2. aqueous diffusion
3. facilitated diffusion(active transport)
Term
4 effects of pH on absorption
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
Term
3 ways drugs are distributed in tissues/cells
Definition
1. diffusion
2. ion-trapping
3. active transport
Term
4 things that affect distribution
Definition
1. organ blood flow
2. plasma protein binding
3. molecular size
4. lipid solubility
Term
biotransformation aka drug metabolism, 5 things to know
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
Term
2 phases of biotransformation
Definition
1. phase 1 reactions- oxidation, hydrolysis, reduction
2. phase 2- conjugation
Term
define pharmacogenomics
Definition
genetic coding
Term
3 processes of drug excretion
Definition
1. filtration
2. secretion
3. reabsorption
Term
5 steps of enterohepatic recycling
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
Term
define half life of a drug
Definition
the elimination time it takes to reduce the plasma drug concentration by 50%
Term
what is the equation for a half life drug
Definition
t(1/2)= half life
Term
what is the steady state of drug concentration?
Definition
usually 4-5 half lifes
Term
define first order kinetics(3 parts)
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
Term
zero order kinetics(3 parts)
Definition
1. very few drugs exhibit
2. when the amount of drug eliminated over time is constant
3. does not depend on drug concentration
Term
what drug dose is often given to reach the steady state quicker?
Definition
maintenance drug dose
Term
pharmacodynamics- mechanism of action
Definition
1. ligand receptor binding
2. signal transduction pathway
3. activation of second messenger molecules
4. altered intracellular process
Term
pharmacodynamics- dose responsive curve
Definition
the relationship between the size of the drug dose and the magnitude of pharmacological effect
Term
4 types of receptors
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
Term
drug receptor interactions(5)
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
Term
agonist intrinsic activity(or efficacy)
Definition
stimulate receptors
have affinity and intrinsic activity
full, partial, and inverse(negative) agonists
Term
antagonist intrinsic activity(or efficacy)
Definition
block receptors
have affinity but DO NOT HAVE intrinsic activity
competitive antagonists- bind reversibly
non-competitive antagonists- bind irreversibly
Term
agonist tolerance
Definition
desensitization- short term
down-regulation

ex. levadopa-parkinsons disease, morphine-pain control
Term
antagonist tolerance
Definition
supersensitivity
up-regulation

ex. levadopa-parkinsons, morphine-pain control
Term
define competitive inhibitor
Definition
when a drug binds to the same catalytic site as the endogenous substrate
Term
define non-competitive inhibitor
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
Term
7 steps of drug approval
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
Term
Clinical phases 1-3 of drug development
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
Term
schedule 1 of drug abuse prevention laws
Definition
high abuse potential, no legitimate medical use, distribution and use prohibited- street drugs like heroin, LSD
Term
schedule 2 of drug abuse prevention laws
Definition
high abuse potential, do have a medical use, distribution is highly controlled- adderall, codeine, demerol, methadone, oxycodone
Term
schedule 3-5 of drug abuse prevention laws
Definition
lower abuse potential, less restrictions for distribution- marinol, vicodin, xanax, serax, lunesta, lomotil
Term
4 adverse effects of drugs
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
Term
drug interactions
Definition
change in the pharmacological effect of a drug when it is given concurrently with another drug or food
Term
pharmaceutical interactions
Definition
a chemical reaction between drugs that are mixed together prior to administration or absorption
Term
pharmacodynamic interactions
Definition
additive, synergistic, antagonistic
Term
pharmacokinetic interactions
Definition
altered absorption, drug distribution, drug biotransformation, drug excretion
Term
factors affecting drug safety with ADME
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
Term
factors affecting drug safety
Definition
1. disease- hepatic and renal disease
2. pregnancy and lactation- teratogenic effects: drug induced developmental abnormalities in the fetus
Term
3 main types of neurotransmitters
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
Term
2 types of receptors
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
Term
cholinergenic drugs that affect neurotransmission
Definition
black widow spider venom
bethanechol
pilocarpine
botulinum toxin A
cholinesterase inhibitors
Term
adrenergic drugs that affect neurotransmitters
Definition
epinephrine and albuterol
cocaine and amphetamines
MAO inhibitors
Beta-blockers
Term
adrenergic drugs that affect neurotransmitters
Definition
epinephrine and albuterol
cocaine and amphetamines
MAO inhibitors
Beta-blockers
Term
muscarinic receptors antagonists
Definition
belladonna alkaloids, semisynthetic and synthetic
Term
nicotonic receptor antagonists
Definition
ganglionic blocking agents, neuromuscular blocking agents
Term
3 types of Belladonna alkaloids(musc)
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
Term
3 main types of semisynthetic and synthetic(muscarinic)
Definition
1. ipratropium- used for COPD(emphysema, chronic bronchitis)
2. dicyclomine- intestinal cramping and IBS symptoms
3. oxybutynin- overactive bladder
Term
ganglionic blocking agents(nicotinic)
Definition
trimethophan
Term
neuromuscular blocking agents(nicotinic)
Definition
MOA- block nicotine receptors
paralysis of skeletal muscles
non depolarizing- curare
depolarizing- succinylcholine
Term
3 direct acting acetylcholine receptor agonists
Definition
1. choline esters- acetylcholine, bethanechol, carbachol
2. plant alkaloids- muscarine, nicotine, pilocarpine
3. other- cevimeline, varenicline(chantix)
Term
indirect acting Ach agonists
Definition
acetylcholinesterase inhibitors
1. reversible- donepezil, edrophoniom, neostigmine, physostigmine, pyridostigmine(mestonin)
2. irreversible- echothiophate
drugst that augment acetylcholine- slidenafil(viagra)
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