Basic Principles Flashcards

1
Q

Any substance that brings about a change in biologic function

A

Drug

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2
Q

Actions of a drug on the body

A

Pharmacodynamics

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3
Q

Actions of the body on the drug

A

Pharmacokinetics

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4
Q

Movement of drug molecules into and within biologic environments

A

Permeation

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5
Q

Most important limiting factor for permeation

A

Lipid diffusion

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6
Q

Aqueous solubility is __________ proportional to electrostatic charge

A

Directly

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7
Q

Lipid solubility is __________ proportional to electrostatic charge

A

Inversely

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8
Q

In weak acids, ___________ form is more water soluble an undergoes better clearance

A

Unprotonated

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9
Q

In weak bases, ___________ form is more water soluble an undergoes better clearance

A

Protonated

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10
Q

Excretion of a weak acid may be accelerated by alkalinizing the urine with _________

A

Bicarbonate

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11
Q

Excretion of a base acid may be accelerated by acidifying the urine with _________

A

Ammonium chloride

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12
Q

Transfer of a drug from its site of administration to the bloodstream

A

Absorption

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13
Q

Most common route of drug administration

A

Oral route

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14
Q

Slowest route of drug administration

A

Topical

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15
Q

Undergoes significant first pass effect

A

Oral route

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16
Q

Partially bypass the first pass effect

A

Rectal

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17
Q

Distribution depends on 4 factors

A

Size of the organ
Blood flow
Solubility
Binding

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18
Q

Drugs may undergo 3 metabolic fates

A

Termination of drug action
Drug activation
Elimination without metabolism

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19
Q

Termination of drug action

A

Elimination

20
Q

Release of drugs or their metabolites in the urine, stool, bile

A

Excretion

21
Q

Rate of elimination is proportionate to the concentration

A

First order elimination

22
Q

Rate of elimination is constant regardless of concentration

A

Zero order elimination

23
Q

What drugs display zero order kinetics?

A
WHAT PET
Warfarin
Heparin
Aspirin
Tolbutamide
Phenytoin
Ethanol
Theophylline
24
Q

Translate the drug-receptor interaction into a change in cellular activity

A

Effectors

25
Q

Response of a particular receptor-effector system measured against increasing drug concentrations

A

Dose response curve

26
Q

Denotes the amount of drug needed to produce a given effect

A

Potency

27
Q

Responsiveness diminishes rapidly after administration of a drug

A

Tachyphylaxis

28
Q

What drugs display tachyphylaxis?

A
MED Loves CNN in HD
Metoclopramide
Ephedrine
Dobutamine
LSD
Calcitonin
Nitroglycerin
Nicotine
Hydralazine
Desmopressin
29
Q

Continuous activation may lead to depletion of essential substrates

A

Tolerance

30
Q

Relates the rate of elimination to the plasma concentration

A

Clearance

31
Q

Condition in which the average total amount of drug in the body does not change over multiple dosing intervals. Rate of drug input is equal to the rate of elimination.

A

Steady state

32
Q

Fraction of the administered dose that reaches the systemic circulation

A

Bioavailability

33
Q

Results in the achievement of therapeutic levels of the drug in the blood without exceeding the minimum toxic concentration

A

Dosage regimen

34
Q

Safe range between the minimum therapeutic concentration and the minimum toxic concentration of a drug

A

Therapeutic window

35
Q

Phase I reactions

A
HORDe
Hydrolysis
Oxidation
Reduction
Deamination
36
Q

Arrange according to decreasing order of strength:
Electrostatic bonds
Hydrophobic bonds
Covalent bonds

A

Covalent bonds
Electrostatic bonds (ionic bonds, hydrogen bonds, van der Waals)
Hydrophobic bonds

37
Q

Fick’s Law of Diffusion

A

(Difference in concentration x permeability coefficient x area)/thickness

38
Q

(Volume of distribution x desired plasma concentration)/Bioavailability

A

Loading dose

39
Q

(Clearance x desired plasma concentration)/Bioavailability

A

Maintenance dose

40
Q

Standard in vitro test for mutagenicity

A

Ames test

41
Q

Phase of clinical trial that deals with the careful evaluation of dose-response relationship and pharmacokinetics among normal human volunteers

A

Phase 1 trial

42
Q

Phase of clinical trial that deals with evaluation of drug in a moderate number of patients with target disease

A

Phase 2 trial

43
Q

Phase of clinical trial that explore further the spectrum of beneficial actions of the new drug, compare it to standard of treatment and discover toxicities

A

Phase 3 trial

44
Q

Postmarketing surveillance phase

A

Phase 4 trial

45
Q

Cytochrome P450 inducers

A
Ethanol
Barbiturates
Phenytoin
Phenobarbital
Rifampicin
Griseofulvin
Carbamazepine
St. John's Wort
Smoking
46
Q

Cytochrome P450 inhibitors

A
Isoniazid
Sulfonamides
Valproic acid
Venlafaxine
Cimetidine
Ketoconazole
Erythromycin
Grapefruit juice
Ritonavir
Amiodarone