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Pharmacology > Basic Principles > Flashcards

Basic Principles Flashcards

1
Q

Actions of body on the drug

A

Pharmacokinetics

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2
Q

4 components of pharmacokinetics

A

Absorption
Distribution
Metabolism
Excretion

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3
Q

What determines the reversibility of drug effects

A

Strength of bond

Covalent > electrostatic > hydrophobic

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4
Q

Movement of drug molecules into and within biologic environments

A

Permeation

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5
Q

Passive movement of non-protein bound drugs b/w blood and extravascular space through water-filled PORES

A

Aqueous diffusion

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6
Q

Transport NOT governed by Fick’s Law of Diffusion

A

Transport by special carriers

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7
Q

Movement of drugs through lipid membranes;

most important limiting factor for permeation

A

Lipid diffusion

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8
Q

Large drugs bind to receptors, internalized and released after vesicle breakdown

A

Endocytosis

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9
Q

Predicts rate of movement of molecules across a barrier

A

Fick’s Law of Diffusion

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10
Q

Aqueous solubility is _______ proportional to electrostatic charge (ionization, polarity)

A

DIRECTLY

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11
Q

Lipid solubility is _________ proportional to electrostatic charge (ionization, polarity)

A

INVERSELY

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12
Q

fraction of drug molecules charged vs uncharged

A

pH

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13
Q

pH is determined by what equation

A

Henderson-Hasselbalch

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14
Q

Drug route that partially avoids hepatic first-pass effect

A

Rectal route

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15
Q

4 major factors in drug distribution

A 
Size of organ
Blood flow
Solubility
Protein binding
Volume of distribution
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16
Q

Drugs displaying zero-order kinetics (WHATPET)

A 
Warfarin
Heparin
Aspirin
Tolbutamide
Phenytoin
Ethanol
Theophylline
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17
Q

Rate of elimination is proportionate to concentration; uses T1/2

A

First-order elimination

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18
Q

Rate of elimination is CONSTANT regardless of concentration

A

Zero-order elimination

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19
Q

Actions of drug on the body

A

Pharmacodynamics

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20
Q

Has small MW (rarely selective in action); anticoagulant that can cross placenta; inhibits Vit K dependent factors synthesis

A

Warfarin

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21
Q

Antidote for Warfarin

A

Vit K, FFP

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22
Q

Has large MW (poorly absorbed & distributed); cannot cross the placenta; activates anti-thrombin III

A

Heparin (LMWH)

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23
Q

Aspirin intake should be stopped 1 week prior to OR because of what drug-receptor bond?

A

Covalent bond

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24
Q

Antidote for Heparin

A

Protamine sulfate

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25
Q

Why must pralidoxime be given within 6-8 hours after organophosphate poisoning?

A

It will become ineffective if covalent bonds has been formed with the organophosphates.

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26
Q

Activated charcoal is an example of _______ antagonist.

A

chemical antagonist

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27
Q

Slowest form of diffusion; very important among weak acids and weak bases

A

Lipid diffusion

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28
Q

Fick’s law of diffusion:
The greater the difference in conc gradient,
The _______ the rate of diffusion.
(Remember formula)

A

faster

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29
Q

Fick’s law of diffusion:
The greater the surface area,
The ________ the rate of diffusion.

A

faster

e.g. Small intestine’s SA > stomach’s

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30
Q

Fick’s Law of Diffusion:
The higher the permeability coefficient,
the _______ the rate of diffusion.

A

faster

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31
Q

Fick’s law of diffusion:
The greater the thickness of the membrane
The _______ the rate of diffusion

A

slower

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32
Q

The more ionized the drug, the _______ is its kidney CLEARANCE.

A

greater

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33
Q

The more unionized the drug is, the _______ is its absorption.

A

greater

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34
Q

pKa

A 
dissociation constant
(Henderson-Hasselbach equation)
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35
Q

The unprotonated (A-, B) is ______ water-soluble thus undergoes better clearance.

A

more

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36
Q

The protonated (HA, BH+) is _____ lipid soluble thus more likely to cross biological membranes.

A

more

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37
Q

Excretion of a weak acid may be accelerated by…

A

alkalinizing urine with bicarbonate

unprotonate with HCO3- to make A-

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38
Q

Excretion of a weak base may be accelerated by…

A

acidifying the urine with ammonium chloride/ ascorbic acid

protonate to make BH+

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39
Q

Location safest for IM buttock injection

A

superolateral

superomedial: superior gluteal n.; inferomedial: sciatic n.

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40
Q

Suppository safe for preggies with thyroid storm

A

PTU

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41
Q

Anatomy correlate: Rectal suppositories have only partial first-pass effect because the superior rectal vein drains to IMV then to the portal vein. What are the other veins that drain eventually to the IVC?

A

Middle & inferior rectal vein
MRV–> Internal iliac v. –> IVC
IRV –> Internal pudendal v –> IIV –> IVC

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42
Q

Only ____ drugs can be absorbed, distributed, metabolized, excreted and exert pharma effect.

A

free/ unbound

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43
Q

Give examples of drugs that are eliminated without metabolism.

A

Mannitol, lithium

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44
Q

Which type of elimination is faster? (1st-order or 0-order?)

A

Zero-order elimination

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45
Q

The smaller the Kd, the ____ the affinity of a drug to bind to its receptor.

A

greater

Kd = drug conc required to bind 50% of the receptors

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46
Q

TD 50/ ED 50

A

Therapeutic index

measure of drug safety based on 50% of population

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47
Q

Tamoxifen is an example of a _______ agonist.

A

Partial agonist

antagonist to breast, agonist to uterus

48
Q

Maximal effect an agonist can produce if the dose is taken to very high levels; measured only with graded dose-response curves (NOT quantal curves)

A

Emax

49
Q

Concentration of the drug wherein half of the maximal effect is achieved

A

EC50

50
Q

fraction of the population that responds at each dose against the log of the dose administered; where ED50, TD50, LD50 is derived

A

Quantal dose-response curve

51
Q

receptors that do not bind drug when the drug conc is sufficient to produce maximal effect; Kd > EC50

A

Spare receptors

52
Q

agonists that result in all receptors achieving the activated state

A

Full agonist

53
Q

Agonist that produces less than full effect even when it has saturated the receptors; can act as an inhibitor in the presence of another agonist

A

Partial agonist

54
Q

Chemical antagonist for lead poisoning

A

Dimercaprol

55
Q

Antagonist that causes a DOWNWARD shift to the dose-response curve

A

Noncompetitive/ irreversible antagonist

56
Q

Antagonist that acts on the allosteric site causing conformational change; overcome by adding more agonist

A

Competitive/ reversible antagonist

57
Q

Frequent exposure to agonist results in short-term diminution of the receptor response

A

Tachyphylaxis

58
Q

Drugs that display tachyphylaxis

MEDical students Love to watch CNN in HD

A 
Metoclopramide
Ephedrine
Dobutamine
LSD
Calcitonin
Nitroglycerin
Nicotine
Hydralazine
Desmopressin
59
Q

Continuous activation may lead to depletion of substrates

A

Tolerance

60
Q

Long term reduction in receptor number d/t continuous exposure to agonist

A

Downregulation

61
Q

Occurs when receptor activation is blocked for prolonged periods

A

Upregulation

62
Q

Infrequently observed variation in drug response; genetically predertermined
(e.g. cataracts w/ allopurinol, aplastic anemia w/ chloramphenicol, hemolytic anemia w/ methyldopa)

A

Idiosyncratic drug response

63
Q

Vol at w/c drug would be uniformly distributed to produce an observed blood conc; can be altered by liver or kidney dse (low serum albumin)

A

Volume of distribution (Vd)

64
Q

Factors affecting absorption

A

Chemical nature (water/lipid-soluble)
Particle size
Polymorphism (amorphous/crystalline; hydrous/anhydrous)
Form (tablet/enteric-coated)

65
Q

main Vd compartment for High MW & CHON-bound drugs

A

Plasma

66
Q

Main Vd compartment for low MW and hydrophilic drugs

A

ECF

67
Q

Main Vd compartment for low MW and hydrophobic drug

A

Intracellular

68
Q

state where rate of drug administration equals the rate of elimination; reached in 4-5 T1/2 of a drug

A

Steady state

69
Q

Most impt pharmacokinetic parameter to be considered in defining a rational steady state during dosage regimen

A

Clearance

70
Q

fraction of drug reaching the systemic circulation; determined by AUC

A

Bioavailability

71
Q

After oral admin of 500mg of Drug A, only 300mg were absorbed into the systemic circulation. What is the drug’s bioavailability?

A

60% (300/500)

72
Q

Rate of elimination at steady state

=(clearance x desired plasma conc)/bioavailability

A 
Maintenance dose
(Vd not involved in calculating MD)
73
Q

given if therapeutic conc must be achieved rapidly and Vd is large
= (Vd x desired plasma conc)/ bioavailability

A

Loading dose

74
Q

Safe range b/w minimum effective conc (MEC) and minimum toxic conc (MTC)

A

Therapeutic window

75
Q

=average dose x (Crea clearance/ 100mL/min)

A

Corrected dose in renal impairment

76
Q

equation used to calculate Crea clearance

A

Cockroft-Gault equation

= (140-age) x Wt in kg / 72 x serum crea

77
Q

Practice problem for corrected dose:
A drug is 50% cleared by the kidney and 50% cleared by the liver. Its normal dosage is 200 mg/d. What is the corrected dosage in a patient with crea clearance of 20mL/min?

A

120 mg/d

78
Q

Phase I reactions

A HORDe of Phase I reactions

A

Hydrolysis
Oxidation
Reduction
Deamination

79
Q

Type of drug metabolism involving cytochrome P450 enymes; converts parent drug to water-soluble form by inserting a polar FUNCTIONAL group

A

Phase I reaction

functionalism

80
Q

Type of drug metabolism involving conjugation of subgroups to -OH, -NH2, -SH

A

Phase 2 reactions

glucuronidation, acetylation, glutathione conjugation, glycine conjugation, sulfation, methylation

81
Q

Drug that can be metabolized by glucorinidation, glutathione conjugation or sulfation; can cause gray baby syndrome

A

Paracetamol

82
Q

Common drugs that are metabolized by acetylation

HIPS

A 
Hydralazine
INH
Procainamide
Sulfonamides
(HIP: SLE-like sx; Sulfonamide: SJS)
83
Q

Cytochrome P450 inducers

Ethel Booba takes Phen-Phen and Refuses Greasy Carb Shakes

A 
Ethanol
Barbiturates
Phenytoin
Rifampicin
Griseofulvin
Carbamazepine
St. John's Wort/ Smoking
84
Q

Enzyme inhibitors -> dec metabolism

HIV-infected Ami drinks grapefruit juice with fungi, causing tummy ache

A 
amiodarone
cimetidine
furonacoumarins (grapefruit)
azole antifungals
Ritonavir (HIV protease inhibitor)
85
Q

Duration of subacute toxicity

A

2-4 weeks

86
Q

Chronic toxicity

A

6-24 mos.

87
Q

FDA drug category (reproductive toxicity):

preggy human & animal SAFE

A

A

Folic acid, thyroid hormones

88
Q

FDA drug category (reproductive toxicity)

Preggy human: NO STUDY, preggy pet: SAFE

A

B

Zidovudine

89
Q

FDA drug category (reproductive toxicity)

Preggy human SAFE, Preggy pet NOT SAFE

A

B

90
Q

FDA drug category (reproductive toxicity)

Preggy human NO STUDY, preggy pet UNSAFE

A

C

Aspirin

91
Q

FDA drug category (reproductive toxicity)

Preggy human & pet NO STUDIES

A

B

92
Q

FDA drug category (reproductive toxicity)

Preggy human and pet UNSAFE

A

D

ACEI, anticonvulsants

93
Q

FDA drug category (reproductive toxicity)

Preggy human & pet UNSAFE

A

X

Statins, OCPs, clomiphene, misoprostol, high-dose vit A

94
Q

Period of organogenesis

A

3-8 weeks AOG

95
Q

Teratogenic effect of ACEIs

A

fetal RENAL damage

96
Q

Teratogenic effect of Anti-epileptic drugs

A

Neural tube defects

97
Q

Teratogenic effect of OHA

A

neonatal HYPOglycemia

98
Q

Teratogenic effect of barbiturates and opioid abuse

A

Neonatal DEPENDENCE

99
Q

Teratogenic effect of DES (morning after-pill)

A

vaginal clear call adenoCA

100
Q

Teratogenic effect of ethanol

A

Fetal alcohol syndrome

flat philtrum

101
Q

Teratogenic effect of lithium

A

Ebstein’s anomaly

102
Q

Teratogenic effect of isotretinoin

Ganda face mo pero wasak kay baby

A

cranioFACIAL malformation

103
Q

Teratogenic effect of iodide

Wag i-spoil si baby, magiging tamad ant pituitary

A

congenital HYPOTHYroidism

104
Q

Teratogenic effect of Misoprostol

A

Mobius sequence

MOve the MISO

105
Q

Teratogenic effect of penicillamine

Si Peni maganda ang cutis

A

Cutis laxa

106
Q

Teratogenic effect of thalidomide

I-thali mo extremities para ma-amputate

A

Phocomelia

107
Q

Teratogenic effect of smoking

A

IUGR

108
Q

Teratogenic effect of streptomycin

A

Ototoxicity

109
Q

Teratogenic effect of Tetracyclines

A

Tooth discoloration, brittle bones

Tetra colors & break your bones

110
Q

Teratogenic effect of methimazole

A

Aplasia cutis congenita

111
Q

Teratogenic effect of sulfonamide

A

Kernicterus

Remember paracetamol given in neonates undergo sulfation

112
Q

Teratogenic effect of fluroquinolones

Floxacin have limp ears

A

cartilage damage

113
Q

Teratogenic effect of warfarin on the 1st tri

A

Chondrodysplasia

114
Q

Teratogenic effect of heparin on 2nd tri

A

CNS malformation

115
Q

Teratogenic effect of warfarin on 3rd tri

A

Bleeding disorders

Pharmacology (10 decks)

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