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Intro Flashcards

1
Q

Which type of drug permeation is not governed by Fick’s Law and is capacity limited?

A

Transport by special carriers

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2
Q

Ionized and polar drugs are more _____ soluble and with ______ clearance

A

Water soluble

Increased clearance

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3
Q

Absorption is faster with:

_____ surface area and ____ membranes

A

Larger surface area and thinner membranes

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4
Q

What predicts the rate of movement of molecules across a barrier?

A

Fick’s law of diffusion

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5
Q

Which quadrant of the buttocks if the safest for IM drugs?

A

Superolateral

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6
Q

Through which blood vessels do sublingual drugs pass?

A

Lingual vein– IJV– brachiocephalic– SVC– right atrium

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7
Q

What route has a partial avoidance of the first pass effect?

A

Rectal

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8
Q

What route offers the closest delivery to the target in respiratory diseases?

A

Inhalational

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9
Q

Which route of administration is the slowest?

A

Topical

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10
Q

Arrange topical route from more evaporation to less:

A 
Tincture
Wet dressings
Lotion
Gel
Aerosol
Powder
Paste
Cream
Foam
Ointment
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11
Q

4 factors that determine drug distribution:

A

Organ size
Blood flow
Solubility
Protein binding

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12
Q

Influences the concentration of the drug in the extracellular fluid surrounding the blood vessel

A

Solubility

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13
Q

Acidic drugs are bound to this protein

A

Albumin

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14
Q

Basic drugs bind to this protein

A

Orosomucoid

A1 acid glycoprotein

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15
Q

What protein binds NT and hormones?

A

Globulin

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16
Q

Type of drug metabolism where the drugs are metabolized into biologically inactive derivatives

A

Termination of drug action

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17
Q

Drug metabolism where prodrugs are metabolized to become active

A

Drug activation

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18
Q

Metabolism:

Some drugs are not modified by the body and continue to act until they are excreted

A

Elimination without metabolism

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19
Q

Give examples of drugs that undergo elimination without metabolism

A

Mannitol
Lithium
Electrolytes

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20
Q

Duration of drug action is determined by

A

Dose administered

Rate of elimination following last dose

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21
Q

This is the most common type of elimination

A

First order elimination

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22
Q

This type of elimination is proportionate to the concentration

A

First order elimination

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23
Q

Constant fraction is being eliminated over time

A

First order elimination

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24
Q

Rate of elimination is constant regardless of concentration

A

Zero order elimination

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25
Q

Concentration in zero order/saturable/michealis menten decreases ______ over time

A

Linearly

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26
Q

Drugs that display Zero Order Elimination kinetics?

A

WHAT PET

Warfarin
Heparin
Aspirin
Tolburamide
Phenytoin
Ethanol
Theophylline
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27
Q

It is the maximal effect available with increasing concentration of a drug

A

Efficacy (Emax)

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28
Q

It is the dose required to produce 50% of the max effect

A

Potency (EC50)

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29
Q

Concentration required to bind 50% of the receptors

A

Kd

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30
Q

Smaller the Kd, the ____ the affinity

A

Greater

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31
Q

Maximum percentage of receptors with increasing concentration of a drug

Maximal number of receptors bound

A

Bmax

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32
Q

Minimum dose required to produce a specified response is determined in each member of a population

A

Quantal Dose-Response Curve

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33
Q

Formula for therapeutic index

A

TD 50 divided by ED50

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34
Q

Efficacy is measured through _____ dose response curves

A

Graded

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35
Q

Receptors that do not bind when the drug concentration is sufficient to produce maximal effect

A

Spare receptors

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36
Q

In the presence of an agonist, a partial agonist can act as _______

A

Antagonist

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37
Q

Effects of competitive antagonists can be overcome by

A

Adding more agonist

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38
Q

Competitive antagonists shift the dose response curve to the

A

Right

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39
Q

Non competitive antagonists causes a ____ shift to the dose response curve

A

Downward shift

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40
Q

This type of antagonist binds to q different receptor and produces an effect opposite to that produced by the drug it is antagonizing

A

Physiologic antagonists

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41
Q

This type of antagonist directly interacts with the drug to remove it or prevent it from reaching the target

A

Chemical antagonist

42
Q

Responsiveness diminishes rapidly after administration of a drug

A

Tachyphylaxis

43
Q

What drugs display tachyphylaxis?

A

MEDical students Love to watch CNN in HD!

Metoclopramide
Ephedrine
Dobutamine
LSD
Calcitonin
Nitroglycerin 
Nicotine 
Hydralazine
Desmopressin
44
Q

The concentration of a drug at the receptor site

A

Effective Drug Concentration

45
Q

The concentration at the receptor site is proportional to the drug concentration in the plasma at equilibrium except in?

A

Topical agents

46
Q

Pharmacokinetic parameter that can be altered by liver and kidney disease

A

Volume of distribution

Clearance

47
Q

Most important pharmacokinetic parameter to be considered in defining a rational steady state during dose regimen

48
Q

Condition in which the average total amount of drug in the body does not change over multiple dosing intervals

A

Steady state

49
Q

Steady state is reached in?

A

4-5 half lives

50
Q

Cockroft Gault Equation

A

72 x serum crea (X 0.85 females)

51
Q

Long term reduction in receptor number due to continuous exposure to agonist

A

Downregulation

52
Q

Receptor activation is blocked for prolonged periods

A

Upregulation

53
Q

Fraction of the administered dose that reaches the systemic circulation

A

Bioavailability

54
Q

Bioequivalence is determined by

A

AUC
Cmax
Tmax

55
Q

This is when the drug is 85-125% of the innovator

A

Bioequivalence

56
Q

Pharmacokinetics:

Equal to the rate of elimination arlt steady state

A

Maintenance dose

57
Q

This is given when the therapeutic concentration must be achieved rapidly and volume of distribution is large

A

Loading dose

58
Q

Formula for adjustment of dose in renal impairment

59
Q

Computation of the amount of drug in the body at any time:

A

Vd x plasma concentration

60
Q

What are the Phase 1 reactions?

A

HORD

Hydrolysis
Oxidation
Reduction
Deamination

61
Q

Most important organ for drug metabolism

62
Q

Primary determinant of clearance

A

Drug Biotransformation

63
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
64
Q

This type of inhibitors bind irreversibly to metabolizing enzymes

A

Suicide inhibitors

65
Q

Cytochrome P450 INHIBITORS

Inhibitors Stop Cyber Kids from Eating GRApefruit QV

A 
Isoniazid 
Sulfinamides
Cimetidine
Ketoconazole
Erythromycin
Grapefruit juice 
Ritonavir
Amiodarone
Quinidine
Valproic acid
66
Q

These types of Phase 2 reactions are used for inactivation

A

Acetylation

Methylation

67
Q

Typical Drugs that use acetylation:

HIPS

A

Hydralazine
Isoniazid
Procainamide
Sulfonamide

68
Q

FDA drug category?
Controlled studies in women fail to demonstrate a risk to the fetus in the first trimester. Possibility of fetal harm appears remote

A

Category A

69
Q

FDA Category

Either animal reproduction studies have not demonstrated a fetal risk

No controlled studies in PREGNANT WOMEN

Animal studies shown adverse effect but not confirmed in women in 1st trimester

A

Category B

70
Q

FDA Category
Studies in animals have revealed adverse effects in fetus and no controlled studies in WOMEN

Or no studies are available

Should be given only when benefit outweighs risk

A

Category C

71
Q

FDA category

Positive evidence of human fetal risk but the benefits may be acceptable despite the risk

A

Category D

72
Q

FDA Category
Studies in animals or human beings have demonstrated fetal abnormalities

Or there is evidence of fetal risk based on human experience or both

Risk clearly outweighs benefit

A

Category X

73
Q

Common Teratogens

Valproic acid
Anti epileptics

A

Neural tube defects

74
Q

All anticonvulsants are CYP450 INDUCERS except:

A

Valproic acid

75
Q

All antidepressants are CYP450 INHIBITORS except

A

St. John’s Wort

76
Q

Teratogen

Phenytoin

A

Fetal hydantoin syndrome

77
Q

Teratogen

Diethylstilbestrol (DES)

A

Vaginal clear cell adenoCA

78
Q

Teratogen

Lithium

A

Ebstein’s anomaly

79
Q

Teratogen

Isotretinoin

A

Craniofacial malformation

80
Q

Teratogen

Misoprostol

A

Möbius sequence

81
Q

Teratogen

Penicillamine

A

Cutis laxa

82
Q

Teratogen

Thalidomide

A

Phocomelia

83
Q

Teratogens

Tetracycline

A

Tooth discoloration

84
Q

Teratogens

Streptomycin

A

Ototoxicity

85
Q

Teratogens

Methimazole

A

Aplasia cutis congenita

86
Q

Teratogens

Sulfonamides

A

Kernicterus

87
Q

Teratogens

Fluoroquinolones

A

Cartilage damage

88
Q

Teratogens

Warfarin 1st trimester

A

Chondrodysplasia

89
Q

Teratogens

Warfarin 2nd trimester

A

CNS malformation

90
Q

Teratogens

Warfarin 3rd trimester

A

Bleeding diasthesis

91
Q

Standard in vitro test for mutagenicity

Uses special strain of Salmonella

92
Q

In vivo mutagenicity test carried out in mice where males are exposed to substance before mating

A

Dominant lethal test

93
Q

Includes all preclinical data collected up to the time of submission and the detailed proposal for clinical trials

A

Investigational new drug

94
Q

What clinical trial phase is decribed when there is evaluation of the dose response relationship and pharmacokinetics among NORMAL volunteers?

95
Q

How many test subjects are included in Phase 1?

A

25-100 normal

20-50 chemo

96
Q

Phase of the clinical trial where evaluation of the drug is done in patients with the target disease under controlled conditions.

97
Q

Phase of clinical trial where desired efficacy at tolerated doses is tested

98
Q

Phase of the clinical trial where a large design involing many patients that include special populations

99
Q

Phase of clinical trial where they explore the spectrum further and compare it to older therapies and to discover infrequent toxicities

100
Q

This is also called the postmarketing surveillance phase

101
Q

This is the right to market the drug without competition from other firms

A

Drug patents

102
Q

How many years is allowed in a drug patent?

Pharma (15 decks)

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