Term
| what are the two ways that a drug can interact? by targeting what? |
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Definition
a macromolecule or receptor
http://www.youtube.com/user/DoctorNajeeb |
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Term
| What are the drugs that produce their therapeutic effects by interacting with a receptor molecule ? |
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Definition
| antacids and osmotic diuretics( inhibit the uptake of sodium and water. for the drugs that do bind to a receptor, there are many chemical interacions that happens between them |
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Term
| How do the antacids TUMS and Maalox work? How do they produce their therapeutic effect? |
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Definition
| by neutralizing the hydrochloric acis in the stomach |
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Term
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Definition
| increased urine formation by diuretics and fluid) may enhance the excretion of certain drugs in urine and is used to treat drug overdose or poisoning of these drugs and hemorrhagic cystitis.[1] |
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Term
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Definition
| increased urine formation by diuretics and fluid) may enhance the excretion of certain drugs in urine and is used to treat drug overdose or poisoning of these drugs and hemorrhagic cystitis.[1] |
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Term
| what happens when osmotic diuretics presence are in the renal tubules? |
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Definition
| creates concentration gradient, leading to elimination of water in the urine |
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Term
| the affinity for a drug for a receptor depends on what kind of factors? |
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Definition
depends on: 1. 3-D shape
2. physico-chemical properties that includes size, sterochemical orientation of its functional groups 4. physical properties. 5. chemical properties |
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Term
| when a receptor makes a covalent bond with the drug, is it reversible? what is an example? |
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Definition
no. It is irreversible.
An example is organophosphate inhibitors |
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Term
| what are the factors that affect drug efficacy and safety? |
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Definition
1. binding affinity to the target protein or receptor.
2. stbiity of the drug in the GIT - ph levels ( the drug has to be stable in there.
3. Absorption from GIT- the faster we absorb, this leads to more toxicity = less effective drug
4. First pass effect ( first pas metabolism) - in order for a drug to work, it has to pass the liver first.The drug is taken by mouth--> into the digestive system--> hepatic portal system --> carries through portal vein and then to the liver then to the -- blood stream.A phenomen of drug metabolism whereby the concentration of the drug is greatly reduced before it reaches the systemic circulation.
5. Distribution- how fat the drug gets distributed to its active location.
6. protein binding- less bound to the protein= better the drug. a drugs efficiency( capacity to produce an effect) maybe afectedby the degree to which it binds to the protein with in blood plasma. he less bound drug is, the more effieciently it can transverse cell membranes or diffuse. the drug binds to proten present in the blod but not at the target site (can be good or bad)
7. Metabolism- how fast a drug gets metabolized. Drug being broken down.
8. Excretion- removel of drug from the boy
9. chemical stability upon storage-drugs last longer when .. how stable is it once it is stored. after we stored it in the freezer, how long from there. ..bottle will state how long is will stay on the shelf. when . it gets 10% less efficacy. (shelf life) experiation dates...slowly goes down...(half life is something else. has to be do with the bottle) 100mg - ... usually 5 half lives usually. )
[3:18:44 PM] navdeep kaur brar: that 90 % that is left now is some toxic compund
[3:19:40 PM] navdeep kaur brar: certain ones u should NOT take them over expiration date
[3:20:36 PM] navdeep kaur brar: someways that you can increase the stability by storing it in ( perservative)
[3:22:00 PM] ravenna: ok
[3:23:34 PM] navdeep kaur brar: how stabe it is once its stored
[3:23:52 PM] navdeep kaur brar: it can go for anything..ice cream,candy
[3:24:21 PM] ravenna: hehe goodie
[3:24:44 PM] navdeep kaur brar: chemical stability of M & M
[3:25:06 PM] navdeep kaur brar: they start to get sticky and change color..
[3:25:11 PM] navdeep kaur brar: same thing as drugs
[3:25:23 PM] navdeep kaur brar: |
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Term
| the functional groups that are within the drug compound, what is their function? |
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Definition
| responsible for the characteristic chemical reactons |
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Term
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Definition
| it is a portion of the drug that contains the functional group that interacts with the receptor active site inorder for a biological activity to result. |
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Term
| can a phrmcophore be composed of more than one functional group? |
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Definition
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Term
| if the pharmacophore i taken way, what would happen? |
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Definition
| the reaactive activity would be gone. |
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Term
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Definition
| a compound that is found before the pharmacophore us found |
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Term
| what can be done to sturtures that are too big? |
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Definition
| we can kep the pharacophore but gett ride of other functional cgroups that are not near the pharacophore |
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Term
| for opiod anagetic what are the pharmacophores? |
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Definition
| pheny group and tertiary amine |
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Term
| if we were to change the addicting efect of cocaine, what would we have to change? |
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Definition
| we would keep the pharmacophore but get rid of the amino alcohol benzoy ester that that contributes to its addiccting effets |
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Term
| Does the lipophilicity increase or decrease as the number of carbons increase? |
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Definition
| as the number of carbons increase,the lipophilicity increases and the hydrophilicity decreases since your increasing the number of carbons. ...(Lipophilicity, (Gr. fat-liking), refers to the ability of a chemical compound to dissolve in fats, oils, lipids, and non-polar solvents such as hexane or toluene) |
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Term
| what is the definition of a bioisosterism what changes and what stay the same? |
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Definition
changing certain things within the group but still retaining the activity.
- example= replacing one atom or another atom.
SAME: nearly equal molecular shapes and volumes. Same distrution of electrons, and similar properties....such as hydrophobicity |
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Term
| when would u ever need to do bioisosteric replacement? |
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Definition
| sometimes a meicinal chemist had a lead compound but there are some lacks in that compound such as bad side effects;therefore,th chemist tries to change those around without changing the desired effect. |
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Term
| what are classical bioisosteres? |
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Definition
they can be single, double, triple, or tetro.
Change: in these classical bioisosteres, the atoms could change but when the atoms do change, tey usally have the same molecular weight. ( trying to find something similar and trying to replace it. there can be a slight difference but not too much) that slight difference usually causes the change. |
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Term
| what is nonclassical bioisoteres? how is it diffferent from classical? |
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Definition
| nonclassical bioisosteres do not have the same number of atoms as the substituent they replace like classical ioisosterism. The non-classical produce agonistic / antagonistic responses. |
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Term
| insulin isolated from different animals is an example of nonclassical bioisosteres or classical? why? |
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Definition
| nonclassical because insulin in different animals differs by many amino acid residues but still produces the same biological effects |
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Term
| what do the nonclassical bioisoterism mimic? |
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Definition
| they mimic spatial arangements, electronic properties, or some other physicchemical property of the molecules or functional gtical for biological group critical for biological activity. |
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Term
| a double bond replacing an essential group into particular configuration critical for activity. nonclassical or classical? |
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Definition
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Term
| true or false, dur to their structual rigidity, double onds can be used in place of rings in order to put functional groups in certain orientation |
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Definition
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Term
| what orientation is better? cis or trans? |
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Definition
| trans because less steric hiderance. |
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Term
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Definition
| study f relative spatial arrrangments of atoms within molecules |
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Term
| what are the similarties with the stereoisomers and what are the differences? |
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Definition
the similarties are that that have the same molecular formula and sequence of atoms
Difference- 3-D orientation of their atoms in space. |
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Term
| what does the activity of a compound depend on thats in vitro? ( in test tube. |
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Definition
| activity of the compound depends on how well it interacts with the target macromolecule/receptor. |
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Term
| what are some of the factors that contribute to the efficacy of a drug molcule in vivo? |
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Definition
| 1. has to be stable at GIT environment 2. should be absorbed from the GIT 3. should survive first pass effect4. should be able to reach the target organ/receptor 5. should be able to excrete |
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Term
| what are some of the requirements for a ood intravenously (IV)? |
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Definition
1. the drug (IV) should be soluable in aqueous media
2. should be sable in solution
3. should be able to distribute to the target organ |
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Term
| what is the difference between vivo and and vitro? |
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Definition
| vivo is within living erson, using a whole person and vitro is in a test tube. |
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Term
| In vivo, what are the several factors that contribute to the efficacy of a drug molecule? |
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Definition
| 1. stable in the GIT environment, 2. absorbed from the GIT 3. should survive the first pass effect 4. should be able to reach the target organ/receptor. |
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Term
| what are the 3 important factors for a drug to be given as an IV ( intravenously)? |
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Definition
| 1. soulable in aqueous media, 2. stable in solution 3. distribute to the target organ |
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Term
| Define oral bioavailiability? |
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Definition
| amount of the drug that reaches the circulation following oral administration |
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Term
| define percentoral bioavailiability? |
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Definition
| percentage of drug that enters the circulation |
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Term
| what are some properties that play a key role in determining bioavailability and overall pharmacological action? |
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Definition
| 1. soluability 2. degree of ionization 3. lipophiliicty 4. diffesivity 5. polymorphism |
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Term
| what are some of the things that the drug has to watch out for when in the GIT? |
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Definition
| 1. being stable in the stomach pH 2. resist degradation from the digestive enzymes |
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Term
| can bacterial enzymes contribute to the metabolism of the drug? |
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Definition
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Term
| why cant Penicillin G be given orally? |
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Definition
| because it is not stable in the acidic stomach pH environment. |
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Term
| what would happen to Penicillin G if it entered the stomach? |
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Definition
| it would be too acidic for it and the acidic environment would hydrolyze it. |
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Term
| After u ingest a drug, what are some of the steps in "drug absorption"? |
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Definition
| the drug must dissolve in the GIT contents, the drug then must cross the membrane, after crossing the membrane, it will go to the blood general system. Drug in formulation --> Drug in Solution --> Drug in blood |
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Term
| There are certain molecules that can pass through the bimolecular lipoid layer? |
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Definition
| only the molecules that are the same size as the pores on the cell |
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Term
| Biological membranes arecomposed of amphipatic molecules, what are they? |
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Definition
| pospholipids and cholestral. |
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Term
| What are the phsiological factors that play a role in the rate andextent of GI absorption? |
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Definition
| 1/ properties of epithelial cells. 2. drgree of vascularity 3. surface area and degree of gastric emptying. |
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Term
| rateof tranfer through the biological membrane id dependent on what? |
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Definition
| lipophilicity. (lipid soluabilty) |
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Term
what is convective absorption?
What is ion-pair absorption? |
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Definition
absorption of small molecules through water-filled pres of biological membranes
- large organic anion can combine with reatively large cation to form an ion pair of neutral properties. |
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Term
| the extent of abosorption from a solution is determined by what? |
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Definition
| dissociation/ionization constant, lipid soluability, and pH of the fluid at the absorption site. |
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Term
| what does the pH-partition theory state? |
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Definition
it states that GI tract and the bilogical membranes act as lipid barriers.
2. un-ionized drugs are absorbed ( prefer)
3. most drugs aborbed by passive diffusion
4. the rate at the drug absorbs is realted to its oil-water partition coefficient |
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Term
| what kind pH drugs will get absorbed in the stomach? |
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Definition
| weak ACIDS and NEUTRAL drugs will be absorbed in the stomach but not basic drugs. |
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Term
| compared to the stomach and the small intestine, where is there a higher pH? |
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Definition
| in the small intestines, there is a higher pH |
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Term
| where are basics likely to be absorbed? |
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Definition
| in the small intestine because of the higher pH. ( exist as mainly unionized) |
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Term
| what is the functional group that basics have? |
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Definition
| they have an amino group (primary, secondary or tertiary) |
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Term
| It is important for the drug to show some lipophilicity to cross the biological membrane but is it also important to have some hydrophilicity? |
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Definition
| yes because your body is 70% water and drugs being hydrophilic is important |
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Term
| what are the factors that affect bioavailability? |
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Definition
| chemical degradation, physical inactivation, incomplete dissoution of the dosage form, microbial metabolism, poorsoulability, first metabolism in the liver |
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Term
| when a drug is directly to the cirulation , the bioavalabily is what percent? |
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Definition
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Term
| during a general circulation, what are the properties that determine the distrbution? |
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Definition
| 1. pka 2. protein binding 3. lipophilicity |
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Term
| there are different areas where distrribution happens, give some examples... |
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Definition
| drugs distribute in the tissues and in the body fluids 2. they may stay in the vascular system is they have a heavy molecular weight or if they are tightly bound to the proteins. Also that certain drus concentrations go to certain locations such as highly soluable lipis goes to the soluable compounds of fat tissues. |
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Term
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Definition
| changing a prodrug to a active drugs |
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Term
| what is a prodrug and what is an active drug? |
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Definition
| prodrug is not active and active drug can be meatabloized. |
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Term
| where are the drug metabolizing enzymes found? |
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Definition
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Term
| the first pass metabolism happens with? |
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Definition
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Term
| what are some ways of admistertating a drug that are not affected by the first pass metabolism? |
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Definition
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Term
| esters and amides are not suceptible to conjugation and excretion, so what are they turned into so we can metabolize esters and amides? |
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Definition
| we change esters and amides to ...carboxlic acids, phenols, and amines because they can easily go through conjudation ( changing a substance into more hydrophilic) |
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Term
| what is the goal of phase 2? |
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Definition
| to make it more polar and water soluable |
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Term
| why is Gluronic acis conjugation the most common conjugative pathway ? |
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Definition
| 1. a radily available supply of glucuronic acid. 2. numerous functional groupscan react with glucuronic acid. 3. the glucuronly moiety greatly enhances water soluabilty due to its ionizable carboxyl group andpolar hydroxyl groups. |
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