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Pharmacology Exam 1
| Question | Answer |
|---|---|
| Ibuprofen and meloxicam are both NSAIDs that inhibit the same enzyme. If the dose of ibuprofen is 400mg, and the dose of meloxicam is 7.5mg, describe potency/efficacy. | Meloxicam is more potent than ibuprofen; efficacy can be assumed to be the same |
| Which describes dose-receptor relationships? toxicology, PK, PD, or pharmaceutics | PD |
| What defines a drug? | Intention of use |
| Drug X binds to the same receptor as ACh, and causes the Emax of muscle contraction to decline irreversibly. What type of drug is X? | noncompetitive antagonist |
| What is common to agonists and antagonists? | affinity |
| A patient has an allergic reaction causing an elevation in histamine activation. Drug X decreases this symptoms. What type of drug is X? | physiological antagonist |
| Therapeutic Window | range of concentrations that a drug is safe and efficacious for most patients |
| A partial agonist can antagonize a full antagonist because (describe affinity and intrinsic activity) | high affinity, low intrinsic activity |
| Does a competitive antagonist result in a left or right shift? What does this mean for efficacy and dose concentration? | right shift; efficacy remains the same, but more drug is needed |
| Which drug is least potent: A-2mg, B-20mg, C-10mg | 20mg |
| Two new diuretics were given to observe drug interaction. Drug A results in an urine output of 200mL, and Drug B results in an urine output of 100mL. Using both together resulted in an output of 500mL. What is this interaction? | synergism |
| What characterizes efficacy? | Emax |
| What characterizes potency? | EC50 |
| What is the bioavailability of a dose administered IV? | same as dose |
| If 50mcg of Digoxin is given orally, what amount reaches systemic circulation (F=0.7) | 35mcg |
| Do IV drugs go through 1st pass metabolism? | No |
| Gastric emptying is the rate limiting step for the absorption of a drug. If solid food is present, what happens to the rate of drug absorption in the SI? | decreases |
| Bioavailability equation | F=AUCpo/AUCiv |
| If a drug given at 400mg IV, and the same dose is given orally, but AUC is 300mg, what is the F value? | 0.75 |
| Two generic brands of drug at equal dose are given orally. Tablet A has an AUC of 25mg, and tablet B has an AUC of 50mg. Which has the better bioavailability? What is the F value? | Tablet B; CANNOT BE CALCULATED, but the relative value of B to A would be 200% |
| If a drug is confined to plasma, describe the Vd | within body range (3-5L) |
| CK is an obese female taking diazepam. MK is at healthy weight, also taking diazepam. The Vd of diazepam for CK is ___ compared to MK? | higher |
| Drugs with very high Vd result in: high bioavailability, high tissue affinity, high renal clearance, or small first pass effect? | high tissue affinity |
| Clearance equation | Cl=k*Vd, where k is the elimination rate constant |
| If a drug has an elimination rate constant of 0.231 and a volume of distribution of 100mL/kg, and is given to a 100kg male patient, what is the total clearance rate? | 231mL/h/kg |
| Form of drug that is most readily absorbed? protein bound, ionized, unionized, glucoronidated? | unionized |
| to increase the renal clearance of a weak base drug, you should | acidify the urine |
| half-life equation | t1/2=0.693/k |
| CK is being treated with amiodarone, which has a half-life of 25 days and experiencing hyperthyroidism. His plasma concentration is 4ug/mL, but should be within 1-2ug/mL. How long does he need to wait before his next dose of amiodarone? | 50 days |
| Drugs where a constant fraction is eliminated with time is which order of kinetics? | 1st |
| Which CYP metabolizes most drugs? | CYP3A4 |
| What is the most common CYP reaction? reduction, hydroxylation, hydrolysis, conjugation, or esterification? | hydroxylation |
| Which phase is an IND filed? | Preclinical (pre-1) |
| Which phase is an NDA filed? | Phase 3 |
| Subjects in this phase do not have the disease the drug is intended to treat? | Phase 1 |
| What the body does to the drug | PK |
| is ADME PK or PD? | PK |
| What the drug does to the body | PD |
| What is a disintegrate? | allows breakdown of particles when in contact with moisture |
| What is a binder? | allows for compression of drug particles |
| Type A adverse effect | predictable, dose related, rarely fatal |
| Type B adverse effect | allergic reaction, can be fatal, no dose alterations can be made |
| when to use activated charcoal, what does it do? | within 30min of an accidental overdose/poisoning. very good at irreversibly absorbing drug molecules in the stomach. charcoal cannot be metabolized by the body, so drug is excreted |
| intrinsic activity | ability to activate a receptor |
| relationship between intrinsic activity and efficacy | direct |
| affinity | strength of attraction between d-r complex |
| Affinity equation | DR=(D*total receptors)/(Kd + dose), where Kd is concentration when 50% of receptors are occupied |
| relationship between Kd and affinity | indirect |
| relationship between EC50 and affinity | indirect |
| is a large or small EC50 better? | large |
| potency is (vertical/horizontal), while efficacy is (vertical/horizontal) | horizontal, vertical |
| which type of drug has no intrinsic activity? | antagonists |
| what is a potentiator? | antagonist that changes a receptor to help an agonist bind |
| efficacy and potency of competitive antagonist | =efficacy, low potency |
| efficacy and potency of noncompetitive antagonist | low efficacy, low potency |
| efficacy and potency of allosteric antagonist | low efficacy, low potency |
| efficacy and potency of a potentiator antagonist | high efficacy, high potency |
| 4 major drug targets | GPCRs, TKRs (tyrosine kinase receptors), ligand/ion gated channels, nuclear receptors |
| acids ionize in __ liquid, while bases ionize in __ liquid | basic, acidic |
| describe why aspirin is absorbed in the stomach | aspirin is a weak acid, and is unionized in the stomach because pH is low. drugs are absorbed when unionized. |
| distribution equation | Vd=dose/plasma concentration |
| where does filtration take place in the kidney | bowmans capsule, through glomerulus capillaries |
| where can reabsorption/secretion happen in the kidneys | pertibular capillaries |
| if you overdose on a basic drug, and it is past the activated charcoal window, do you give acid or base to prevent reabsorption? | acid |
| phase 1 of metabolism | oxidation, reduction, hydrolysis |
| phase 2 of metabolism | conjugation, glucuronidation |
| where does salt conjugation occur, what drugs are effected by this? | bile and/or intestinal flora so that drug works during reabsorption. estrogen relies on conjugation |
| 1st order equation | logC=logCi - kt/2.3 |
| 0 order equation | C=Ci-kt |
| what order is half life the same value as elimination rate? | 0 order |
| phase 1 metabolic reactions include | oxidation, reduction, hydrolysis, cyclization, decyclization |
| phase 2 metabolic reactions include | conjugation |
| 4 types of transferases that conjugate during metabolism | glucuronosyl, sulfotransferase, glutathione, N-acetyltransferase |
| is Pgp an efflux or influx transporter? | efflux |
| major influx transporter | OATP |
| most polymorphic CYPs | CYP2s (D6, C9, C19) |
| which type of metabolizer will have no effect from morphine? | PM, missing CYP2D6 |
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alexism943