Pharm1 Intro
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| True or false: Typically a drugs that is a racemic mixture, only one of the forms will work. However in a large number of cases the other enatiomer will be responsible for many SE. | True.
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| Covalent bond: | sharing electrons. Very strong. It is usually the way we store energy. These covalent bonds are often irreversible-it is difficult for the body to break covalent bonds. DNA alkalating drugs stop DNA replication of cancer cells.
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| Electrostatic bond: | Weaker than covalent. More common than covalent in drug-receptor reactions.
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| Three types of electrostatic bonds and their relative strengths: | Strong: interactions between permanently charged ionic molecules. Weaker: hydrogen bonding. Weakest: induced-dipole interactions, like Van der Waal's or London forces.
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| True or false: hydrophobic interactions are strong. | False. They are generally weak
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| Hydrophobic interactions are probably significant in driving what reactions? | 1. Between lipophilic drugs and biological membranes, 2. between drugs and relatively nonpolar (not charged) receptor sites.
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| What are the only three possible hydrogen bonds? Why? | H-O, H-N, and H-F. Because of the strong electronegativity of those molecules.
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| What is the Henderson-Hasselbach equation? | pH = pKa + log(UP/P)
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| Acid vs base: what is charged/uncharged when protonated/unprotonated? | Acid: unprotonated is the ionized and protonated is unionized. Acid = (A-)/(HA)Base: unprotonated is unionized and protonated is ionized. Acid = (B)/(HB+)
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| What is the body's most important buffer? | Bicarb.
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| What do we use the Henderson-Hasselbach equation for? | This equation will tell you how much of the drug is present in the protonated and unprotonated form at a certain pH.
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| Drug ionization reduces a drug's ability to... | Cross a lipid bilayer.
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| pKa stands for... | Minus the log of the Ka.
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| What is Ka? | The acid constant.
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| What is Le Chatelier's Principle? | This states that “a system at equilibrium will respond in such a way as to oppose any change made to it.”
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| What is absorption? | Movement of a drug across a membrane.
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| Why don't IV drugs have an absorption phase? | Because they don't cross a membrane, they enter directly into the central(plasma) compartment.
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| Most drugs are weak... | Bases.
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| Where are most PO drugs absorbed? | In the small intestine.
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| Why are most PO drugs best absorbed in the small intestine? | Because of the villi, there is a much greater surface area. Even acidic drugs are better absorbed in the small intestine, because the large SA makes up for the less-than-optimum pH. Basic drugs are absorbed VERY well in the small intestine.
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| Why is SQ absorption phase slower than IM absorption phase? | There is much more blood flow to the muscle than to the skin. This means that in the muscle as the blood goes by it is not carrying much of the drug and it has a better diffusional pressure to take up the drug more rapidly.
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| Distributive phase: Once drug is in plasma (which is the highway that is mostly used to distribute drugs) it has to travel to its... | Site of action.
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| When a drug is converted from its parent form into another form, that is no longer the <blank>. The <blank> has been eliminated. | Parent drug.
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| Elimination can occur in two ways: | Metabolism of the parent drug into another form, or excretion of the parent drug in its original form.
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| In the central compartment(plasma compartment): <blank> molecules are normally the only molecules that can elicit a response. | Free drug.
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| In plasma, what is the number one protein that free drug binds to? | Albumin.
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| If a drug is 99% protein bound, and you inject 1000 molecules of drug you would only have <blank> free molecules. | 10.
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| Can albumin cross membranes? | No.
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| Metabolism generally makes a drug more... | Polar.
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| Drugs that are metabolized into more non-polar form the FDA will not approve it because it will... | Accumulate in the body.
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| Define pharmacodynamics: | The effect of the drug on the body. Relates the drug concentration to its effect.
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| Define pharmacokinetics: | How the drug is handled by the body. Involves entire ADME.
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| Agonist: | Is a substance that interacts usually at a receptor to elicit a response.
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| Antagonist: | Is a substance that blocks response usually at a receptor.
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| Competitive antagonist: | There is a competitor for the binding site. If there is more of a drug(agonist or antagonist, drug or endogenous ligand), the higher number will have a competitive advantage.
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| What is affinity? | The ability of a substance to interact at a receptor.
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| What is intrinsic activity? | The ability of a substance to elicit a response at a receptor.
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| What is a compound with good affinity and good intrinsic activity? | An agonist.
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| What is a compound with good affinity and no intrinsic activity? | A good antagonist.
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| What is a substance with good affinity and poor intrinsic activity, that is, less affinity than the endogenous ligand. | A partial agonist.
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| A partial agonist is always also... | A partial antagonist.
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| What are non-competitive interactions? | The antagonist does not act at the same binding site as the agonist. By binding at that secondary site causes an alteration in the site of the normal agonist site and the agonist can’t bind.
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| What is an allosteric interaction? | A non-competitive interaction. The binding of the drug at the secondary site.
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| What do adrendergic receptors interact with? | Norepinephrine.
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| Where are some usual receptor sites on the cell? | Cellular membrane(inside and outside), cytoplasm, nuclear envelope.
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| What are some examples of drugs that have non-receptor mediated responses? | Mannitol(an osmotic diuretic), Methyl cellulose(an osmotic laxative), Dextrans(when used IV, expand blood volume by pulling water from tissues into blood)
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| Most drugs act on receptors, except: | Some anesthetics, hypnotics, and sedatives;
Alcohols; Osmotically-active drugs; Acidifying/alkalinizing agents; Antiseptics.
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| Receptors can be blocked by receptor antagonists (affinity, but low-to-no intrinsic activity). For example, Atropine blocks... | Muscarinic Ach receptors.
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| The affinity of drug binding is referred to as the... | Association constant, KA
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| What is the Association Constant formula? | KA = Kon/Koff
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| What is the dissociation constant (KD)? | The concentration at which 50% of the receptors are occupied.
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| What is the dissociation constant (KD) equation? | 1/KA (or Koff/Kon).
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