How many years does it take to complete 3 phases?
This phase determines the max does with toxicities that are well defined
How much of NDA is clinical data?
Phase determines, health/benefits ratio, verifies efficacy, safety, and dosage?
How many drugs pass efficacy trials of phase 3?
How many drugs pass the dose ranging trials of phase 2?
How many drugs pass the safety studies of phase 1?
safety + efficacy
2 criteria for NDA approval?
Use of a label drug that is not FDA approved?
3 & 4
What schedule(s) do optometrist prescribe?
Food, drugs, cosmetics, biologics, radiation, 25% consumer dollar
What 5 things does the FDA regulate?
Key to FDA approval?
Oral, sublingual, rectal
3 routes of ENTERAL ?
IV, IM, & subcutaneous
3 routes of PARENTERAL?
How long it takes for the drug to start working?
Weak acids (Uncharged) in acidic enviroment are _____ soluble allowing them to pass through biological membranes
a weak base in an alkalinic enviroment will be un/charged?
a weak base in charged(protanated) is less/more lipid soluble?
Process by which RX enters systemic circulation?
blood flow, Ph, solubility
3 factors that effect absortion?
Portion of adminstered dose that is absorbed into the circulation, & works?
1st pass metabolism & RX solubility
2 things influence bioavailabilty?
1st pass loss or eliminination
Overall process that contributes to bioavailability reduction?
inhalation, transdermal, & sublingual, lower rectum
What 4 things can avoid first pass metabolism?
RX unstable in gut wall?
RX metabolized by digestive enzymes?
RX metabolized by intestinal wall enzymes?
Two Rx have same efficacy & safety?
Two RX have same bioavailabilty & peak blood concentrations?
B globulin + acid glycoprotein
2 plasma proteins that bind BASIC drugs?
Plasma protein that binds ACIDIC drugs?
The less albumin your body has the _____ likely the drug will bind?
diffuse thru membranes, metabolized, excreted, or cause therapeutic effects
When a RX molecule is bound to plasma protein it CAN NOT?(4)
free rx conc, protein conc, & affinity for binding sites, competion of other RX
Amount of RX bound depends on?
renal failure, inflamation, fasting, malnutrition
Name 4 conditions that will effect how much plasma protein is bound to drug?
Binding of drug molecules is usually ?
Give an ex. of a drug that displaces another drug from plasma protein binding?
Warfarin is a strong anticoagulant because it has ___% bound?
The relationship between concentration & amt of drug in body?
Rx pka, binding protein coefficient of rx on fat
2 factors influencing volume distribution?
Controls half life and excretion?
Ionic trapping, tissue barriers, & protein binding
Name the 3 factors that influence Tissue Distribution?
The shorter the half life the _____the drug gets out?
If the drug is in a lg volume the half life will be ___>
RAte of ellimination proportional to plasma concentrations?
zero order (non-linear)
Constant rate of ellimination irregardless of plasma concentration.
Less drug the _____ the elimination?
Phase 1 drugs
Kind of drug that utilizes the P-450 system?
What phase of drug turns lipophilic drugs into polar drugs making them easier to eliminate?
hydoylsis, oxidation, methlyation, demethlyation, reduction, alcohol dehydrogenase
List the 6 Phase 1 rxn types?
phase 2 drugs result in _____polarity of drug?
sulfate conjugation, glycine conjugation, glucuromide conjugation
Name the 3 phase 2 rxn types?
A drug that inhibits the metabolism of many other drugs
Topical, Periocular injections, & Systemicly
Name the 3 ways to treat ocular pathology?
non invasive, simple instillation, self admister, increased drug at infection site
What are the 4 benefits of topical admistration?
Normal tear layer volume?
Amount eyelids can hold?
Normal drop size?
ideal drop size?
tear flow, tear volume
2 things on the ocular surface that can decrease absortion?
for maximal corneal drug penetration a molecule must have an optium ration of _____&_____?
Noniodized molecules penetrate the ____&____ of the eye?
Ionized molecules penetrate what part of the trilaminar permiability barrier?
what kind of drugs does the iris pigment store?
Acts as a resevoir for drugs/
Make up the retinal blood barrier because they have zona ocludens?
gels, ointment, sprays, emulsions, solutions, oral, injections, solutions/supspensions, unit-dose-dispersers, solid delivery devices
Name all ten ocular ocular formulations of medicine?
Pilocarapine (.25) is an ex of a ___?
lamolin, mineral oil, petrolatum
3 things which are added to ointments to increase CONTACT time?
Most common type of injection?
an examply of an IV injection procedure?
Fastest absorption rate of ocular meds?
Best for cyclopleging kids
Unit does dispensors
Great for patients that have hypersensitivity rxns to preservatives or on a chronic therapy?
HCl, Bitartarate, Borate
3 buffers that control pH?
Most stable buffer?
Least stable buffer?
Which is tolerated better hyper/hypotonic drugs ?
Name the 2 agents that alter Tonicity?
Polyvinylprrolidone povidine, polyvinly alcohol, cellulose gums
Name the 3 Agents that alter Viscosity?
Increasing _____ leads to increase retention time, bioavailability, lubrication, and reduction in draining rate?
One of the worse preservatives can cause SLK disease in contact lens wearers?
surface & intracellular
Name 2 receptors?
What drugs bind to intracellular receptors?
Most drugs bind to ____Receptors?
Cell surface, nuclear, enzyme activators, & ion channel openers
Name 4 types of receptor agonist?
Name an ex of enzyme inhibiition that is a Key RXN in Aqueous in eye?
If you want to slow the aqueous then you would inhibit?
Noncompetitive Antagonists bind _____from receptors?
Super sensitzed (up-regulated)
IF you keep blocking a receptor then a receptor will become?
Only way to achieve a steady state is with ?
which drug would reach a steady state first, shorter or longer half life drug?
How many half lifes does it take to reach a steady state?
Time required for serum plasma concentrations to decrease by 50%?
How many days will it take for drug to reach steady state, if the drug is 24 hrs?
Amt of drug administered is equal to drug eliminated?
allow rapid achievement of steady state and is usually 2x of regular does?
Z - pak
An example of a medicine with a loading does?
NO, but plasma rx levels increase
By doubling the infusion rate time does the steady state change?
What is the equation for therapeutic index?
_____is an example of a drug with a small TI & _____is an ex. of a drug with a high TI?
BAD!!! not treating the disease, costly
Is sub therapeutic levels good or bad?
The larger the TI levels the _____the drug is?
Reflects the safety of a drug & how likely will there be an overdose?
2 or less
A therapeutic index levels is considered bad if it is below?
The study of the biochemical & physiological process underlying drug actions
Most drugs cause there effect through ____interactions?
Determines drug action selectivity?
____determines relationship of rx dose & effect, drug action selectivity, & mediates antagonist + agonist effects?
NA/K, ATpase pump, dioxin
Name 3 ex's of tranport protein receptors?
Name a structural protein receptor for anticancer therapies/anti-inflamation drugs?
Name a drug that reacts with multiple receptors, like histamin + ach?
Affinity & efficacy
NAme the 2 properties of agonists?
The comparison of ED50's of 2 or more drugs that cause the same responses via interating with same receptors. Both drugs must have same efficiacy?
An agoninst with less than maximal efficacy?
IF max efficiacy is less than endogenous compound then partial agonist is actually an______?
Interact with receptor but do not cause change in the receptor therefore they have affiity but no EFFICACY?
Competitive, noncompetitive, irreversible
Name the 3 types of Antagoninsts?
Dextral shift to the right
How will an Antagonist displace the agonist DR curve?
Lungs, kidney, Bile, mothers milk, saliva, sweat
Name the 6 ways to elliminate drugs?
Increase toxicity and half life
A patient having poor kidney function will respond to a drug by?
Ellimination using enterohepatic circulation/active transport?
Distal tubules reabsorb ?
How small does a drug have to be to pass through glomerular filtration?
This can be used to increase excretion rate by trapping drug in filtrate?
clearence * plasma concentration
Excretion rate formula?
Volume of plasma cleared of drug per unit time NOT amt of drug leaving the body?
Rate of elimination /plasma concentration
if you decrease clearance then you ___half life?
Drinking more water
How can you increase clearance?
clearance & volume distribution
What two things are half life of elimination dependent on?
Most control of ANS is manifested by?
Neurotransmitter in both sympathetic & parasympathetic ganglia?
What kind of agoinst is Pilocarpine?
What kind of antagonist is Tropicamide?
Muscarinic & nicotinic
Two types of Cholinergic receptors?
sketal mm & EOMS
Where are nicotinic receptors found?
What enzyme breaks down excess of Acetylcholine?
If pt has a red face we can assume he's taking for hypertension?
In order for a NTM to bind it needs influx of Ca this theory is called?
Parasympathetic effects on lacrimal gland due to what CN?
Muscaric type found at neuroeffector junctions innervated by parasympathetic NS?
Muscarinic type found at autonomic gangnlia & CNS?
speen, sweat gland, piloerector mm, bld vessels
Name 4 organs that are ONLY receive sympathetic integration?
Patients body temp increased, red, and cant sweat, what drug was given?
NMT will never be released if its in a ?
Bind reversibly to cholinergic receptors but do not activate it, preventing a response?
Inhibit acetlycholinesterase enzyme so there is more Ach in synapse?
Direct acting agents
Act directly on cholinergic receptors on the post synaptic membrane?
Acetlycholine, Bethanechol, Carbachol, pilocarpine
Name the 4 direct acting Cholinergic Agonists?
Direct acting muscarnic parasympathomimetic ?
Causes, contractions of longitudinal fibers of CB, opening TM and increasing aq drainage.
Increase the permiability of the blood/aq barrier?
2 , 8
Pilocarapine has max effect in ___hr and lasts for ___hrs?
Pilopine gel 4% are more gentle causing less myopia but could result in?
Salvation, lacrimation, sweating, nausa, vomiting, diarrehea, bronchilor spasm, pulmonary edema worsens parkinsoism
If taken in excess Pilocarpine can cause ?
Atropine & ipratropium
Name two Antimuscarinnic drugs?
Name one ganglion blocker?
Vecuronium, tubocuarine, pancuronium
Name the three neuromuscular blockers?
fast but short duration acting indirect cholinergic agonist that is used for diagnosis of MG?
pyridostigmine, neostigmine, physostigmine
Name the 3 indirect cholinergic agonist for treating MG?
antidote for organophosphate?
Physotigmine, pyridotigmine, neostigmine, edrophonium
Name the 4 Anticholinesterases/ Indirect acting cholinergic agoninsts reversible?
Irreversible Indirect acting cholinergic agonist?
USEd for accomadative esotropia & breaking synechia?
Miotic drugs (echothiophate)
This type of drug increases incidence of retinal detachment with strong?
Drug causes, eyelid myokymia, bronchiolar constriction, parkinsoism, paralysis with succinylcholine
PAM(pralidoximine) + Atropine
Antidote to Irreversible cholinergic agonist?
decrease aqueous humor
atropine, scopolamine, ipratropium, homatropine
Name the 4 antimuscarinic agents?
Fatal doses of atropine in adults/kids?
Duration of atropine?
drowsiness, dizziness, constipation, dry mouth, impaired judgement, headaches
list some side effects associated with anticholinergic drugs?
Used during surgeries to relax muscles?
Depolarizing agonist, resistant to depolarizing and flaccid paralyis?
Block entire output to ANS?
Nicotine, Trimethaphan, mesamylamine
List the 3 Ganglionic blockers?