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Flashcards in PHARM BASICS Deck (56):
1

Time it takes for amount of drug to fall to half of its value, constant in first order kinetics (majority of drugs)

Half-life (T1/2)

2

Relates the amount of drug in the body to the plasma concentration

Volume of distribution (VD)

3

Plasma concentration of a drug at a given time

Cp

4

The ratio of the rate of elimination of a drug to its plasma concentration

Clearance (CL)

5

The elimination of drug that occurs before it reaches the systemic circulation

First pass effect

6

The fraction of unchanged drug that reaches systemic circulation after administration

Bioavailability (F)

7

When the rate of drug input equals the rate of drug elimination

Steady state

8

Different steps of Phase I

Oxidation, reduction, hydrolysis

9

Barbiturates, phenytoin, carbamazepine, and rifampin all do this

Induce CYP450

10

Cimetidine, ketoconazole, isoniazid, and grapefruit all do this

Inhibit CYP450

11

Name 3 Phase II conjugation reactions

Glucuronidation, acetylation, glutathione conjugation, glycine conjugation, sulfation, methylation, water conjugation

12

Constant percentage of drug metabolized per unit time

First order kinetics

13

Constant amount of drug metabolized per unit time

Zero order kinetics

14

Target plasma concentration times (volume of distribution divided by bioavailability)

Loading dose (Cp*(Vd/F))

15

Concentration in the plasma times (clearance divided by bioavailability)

Maintenance dose (Cp*(CL/F))

16

Strength of interaction between drug and its receptor

Affinity

17

Selectivity of a drug for its receptor

Specificity

18

Amount of drug necessary to elicit a biologic effect compared with another drug

Potency

19

Ability of drug to produce the maximal biologic effect

Efficacy

20

Ability of a drug to produce maximal response after binding to the receptor

Full agonist

21

Ability to produce less than maximal response after binding to the receptor

Partial agonist

22

Ability to bind reversibly to the same site as the drug and without activating the effector system

Competitive antagonist

23

Ability to bind irreversibly to the active site or bind to a site distinctly separate from the agonist binding site

Noncompetitive antagonist

24

Mechanism of action (MOA) utilizes intracellular receptors

Steroid and hormones

25

Mechanism of action (MOA) utilizes transmembrane receptors that have intrinsic enzymatic activity

Insulin, EGF, TGFbeta, PDGF, ANP

26

Mechanism of action (MOA) utilizes ligand gated ion channels

Acetylcholine, nicotine

27

Dose which produces therapeutic response in 50% of the population

ED50

28

Dose which is toxic in 50% of the population

TD50

29

Dose which is lethal to 50% of the population

LD50

30

Window between therapeutic effect and toxic effect

Therapeutic index

31

Drugs that have a high margin of safety is indicated by

High therapeutic index

32

Drugs that have a narrow margin of safety is indicated by

Low therapeutic index

33

Antidote used for lead poisoning (without encephalopathy)

Dimercaprol, Edetate calcium disodium, or succimer

34

Antidote used for cyanide poisoning

Nitrites, sodium thiosulfate, hydroxocobalamin (cyanokit)

35

Antidote used for anticholinergic poisoning

Physostigmine

36

Antidote used for organophosphate/anticholinesterase poisoning

Atropine, pralidoxime (2-PAM)

37

Antidote used for iron salt toxicity

Deferoxamine

38

Antidote used for acetaminophen (APAP) toxicity

N-acetylcysteine

39

Antidote for severe lead poisoning (with encephalopathy)

Dimercaprol AND CaEDTA (edetate calcium disodium)

40

Antidote for arsenic, mercury, and gold poisoning

Dimercaprol

41

Antidote used in Wilson's disease (copper poisoning)

Penicillamine

42

Antidote used for heparin toxicity

Protamine Sulfate

43

Antidote used for warfarin toxicity

Vitamin K and Fresh frozen plasma (FFP)

44

Antidote for tissue plasminogen activator (t-PA), streptokinase

Aminocaproic acid

45

Antidote used for methanol and ethylene glycol toxicity

Ethanol

46

Antidote used for opioid toxicity

Naloxone (IV), naltrexone (PO)

47

Antidote used for benzodiazepine toxicity

Flumazenil

48

Antidote used for tricyclic antidepressants (TCA)

Sodium bicarbonate

49

Antidote used for carbon monoxide poisoning

100% O2 and hyperbaric O2

50

Antidote used for digitalis toxicity

Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)

51

Antidote used for beta agonist toxicity (eg. Metaproterenol)

Esmolol

52

Antidote for methotrexate toxicity

Leucovorin

53

Antidote for beta-blocker overdose and hypoglycemia

Glucagon

54

Antidote useful for some drug induced Torsade de pointes

Magnesium sulfate

55

Antidote for hyperkalemia

sodium polystyrene sulfonate (Kayexalate)

56

Method to reduce salicylate intoxication

Alkalinize urine, dialysis