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Pharmacology > Basic Principles > Flashcards

Basic Principles Flashcards

0
Q

Arranged according to decreasing order of strength:

Covalent bonds, Electrostatic bonds, Hydrophobic bonding

A

Covalent bonds, Electrostatic bonds, Hydrophobic bonding

Covalent bonds-not reversible

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1
Q

Actions of a drug on the body

A

Pharmacodynamics

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2
Q

It is the most important limiting factor for permeation.

Important for the diffusion of weak acid and weak base

A

Lipid diffusion - concentration only not charged

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5
Q

Heparin activates anti-thrombin III, monitor: aPTT - cannot cross the placenta. Antidote?

A

Protamine sulfate

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7
Q

Aqueous solubility is ___ proportional to electrostatic charge - ionization, polarity

A

Directly proportional - increased aqueous solubility = increased clearance

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8
Q

Aqueous diffusion-passive movement of non-protein bound drugs through small water-filled pores. Affected by what?

A

Drug concentration and charge

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9
Q

Law that predicts the rate of movement of molecules across the barrier. Absorption is faster in organs with larger SA and with thinner membranes

A

Fick’s law of Diffusion

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10
Q

Weak acid: what form is more water soluble and undergoes better clearance?

A

Unprotonated (A-) form - while protonated (HA) form is more lipid soluble and more likely to cross membrane

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12
Q

Excretion of weak acid maybe accelerated by alkalinizing the urine using what?

A

Bicarbonate

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13
Q

pH determines the fraction of drug molecules charged versus uncharged predicted using what equation?

A

Henderson - Hasselbach equation

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14
Q

Actions of the body on the drug - concerned absorption, distribution, metabolism and elimination

A

Pharmacokinetics

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15
Q

Substance that brings a change in biologic function through its chemical action

A

Drugs

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16
Q

Transfer of a drug from site of administration to the bloodstream

A

Absorption

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17
Q

Three factors affecting the drug absorption

A
  1. Route of administration
  2. Blood flow
  3. Concentration
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18
Q

Most common route of drug administration.

A

Oral route - absorption is slow and less complete

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19
Q

drug administration bypasses the first-pass effect, except? Intravenous, Subcutaneous, buccal or rectal

A

Rectal /suppository route - partial avoidance not complete

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20
Q

Slowest route of drug administration

A

Topical route - for local effect , absorption varies with the area of application and drug formulation

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21
Q

Drug distribution depends on major factors

A

Size of organ
Blood flow
Solubility
Binding

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22
Q

True/False: bound drugs can cross membranes and exert their effect.

A

False - bound drugs CANNOT cross membrane

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23
Q

Movement of drug molecules into and within biologic environment

A

Permeation

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24
Q

Refers to chemical alteration of the drug

A

Drug metabolism

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25
Q

Weak base: what form is more lipid soluble and more likely to cross biological membranes?

A

Unprotonated (B) form

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26
Q

For acute inflammation what type of topical agents were used?

A

Drying agents - tinctures, wet dressing and lotions

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28
Q

Acidic drugs are bound to albumin while basic drugs are bound to ____

A

Orosomucoid

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29
Q

Three metabolic fates that a drug may undergo:

A
  1. Temination of drug action
  2. Drug activation
  3. Elimination without metabolism
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30
Q

Refers to termination if drug action

A

Drug elimination

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31
Q

Determines the duration of drug action

A
  1. Dose administered

2. Rate of elimination following the last dose

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32
Q

Refers to characteristic half-life of elimination, most common type of elimination

A

First-Order Elimination - rate if elimination is proportionate to the concentration, decreases exponentially over time

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33
Q

Refers to constant rate of elimination regardless of concentration

A

Zero - Order Elimination - concentration decreases linearly over time

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34
Q

Drugs that display zero order kinetics

A

Warfarin, heparin, aspirin, tolbutamide, phenytoin, ethanol, theophylline - WHAT PET

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35
Q

Specific molecules with which drugs interact to produce changes in the function of the system, most are proteins

A

Receptors

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36
Q

Causes downward shift of the DRC, not overcome by adding more agonist

A

Non-competitive or Irreversible antagonists

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37
Q

Drug reversibly leaves the bloodstream and enters the target organ

A

Distribution

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38
Q

Sigmoid curve, response of a particular receptor-effector system measured against increasing drug concentrations

A

Graded Dose-Response curve

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39
Q

Do not provoke a biological response by themselves, blocks drug response in the presence of an agonist

A

Antagonist

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41
Q

____ and ____ are derived from dose-response curve

A

Efficacy (Emax) and potency (EC50)

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42
Q

Interact directly with the drug being antagonized to remove it or prevent it from reaching its target

A

Chemical antagonists

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43
Q

Refers to concentration required to bind 50% of the receptors

A

Kd - the smaller the Kd, the greater the affinity of a drug for its receptor

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44
Q

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

A

EC50 - potency

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45
Q

Not governed by Fick’s law of Diffusion and is capacity-limited

A

Transport by special carriers - availability of carriers

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46
Q

Capable of fully activating the effector system when it binds to the receptor

A

Full agonists - sufficiently high concentrations result in all the receptors achieving the activated state

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47
Q

Binds to a different receptor, producing an effect opposite to that produced by the drug it is antagonizing

A

Physiologic antagonist

48
Q

It shifts DRCs to the right (increased ED50) but same maximal effect is reached

A

Competitive/Reversible antagonist - effects overcome by adding more agonist

49
Q

Refers to rapidly diminishing responsiveness after administration of a drug

A

Tachyphylaxis

50
Q

Drugs that display tachyphylaxis

A

Metoclopromide, ephedrine, dobutamine, LSD, calcitonin, nitroglycerin, nicotine, hydralazine, desmopressin

51
Q

Refers continuous activation may lead to depletion of essential substrates

A

Tolerance

52
Q

One that is infrequently observed in most patients, not predictable

A

Idiosyncratic drug response

53
Q

Concentration of a drug at the receptor site

A

Effective drug concentration

54
Q

Purely pharmacokinetic parameter with no direct physical equivalent

A

Volume of distribution - can be altered by liver and kidney disease

55
Q

If low Vd = distribute in blood, then medium Vd means?

A

Distribute in extracellular space or body of water

While high Vd - distribute in tissues

56
Q

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

A

Clearance - depends on the drug and the condition of the organ of elimination

57
Q

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

A

Steady state - input rate=elimination rate

58
Q

Constant for drugs following first-order kinetics

A

Half-life

59
Q

Fraction of the administered dose that reaches the systemic circulation

A

Bioavailability

60
Q

Plan for drug administration over a time period

A

Dosage regimen

61
Q

Equal to rate of elimination at steady state, important to maintain concentration above minimum therapeutic level

A

Maintenance dose - Vd is not involved in calculating MD

62
Q

Large Vd for a therapeutic concentration be achieved rapidly

A

Loading dose

63
Q

Refers to the safe range between minimum therapeutic conc and the minimum toxic concentration of a drug

A

Therapeutic window

64
Q

Equation to calculate for patient’s creatinine clearance

A

Cockroft-Gault equation
Clearance = [(140-age)xweight(kg)]/[72xserum creatinine(mg/dL)]
Multiplied by 0.85 in females

65
Q

Metabolism: what phase converts the parent drug to more polar or more reactive product by unmasking or inserting a polar functional group

A

Phase I reactions - example: oxidation, reduction, deamination, hydrolysis

66
Q

Mixed-function oxidases, high conc in smooth endoplasmic reticulum of liver

A

CYP450

67
Q

Metabolism: at what phase involve conjugation of subgroups to -OH, -NH2 and -SH functions on the drug molecule

A

Phase 2 reaction - glucuronate, acetate

68
Q

Most important organ for drug metabolism

A

Liver

69
Q

CYP450 inducers

A

Ethanol, barbiturates, phenytoin, rifampicin, griseofulvin, carbamazepine, st. Johns wort and smoking

70
Q

CYP450 inhibitors

A

Isoniazid, sulfonamides, cimetidine, ketoconazole, erythromycin, grapefruit juice, ritonavir, amiodarone, quinidine and valproic acid

71
Q

Administration of single doses of the agent up to the lethal level in at least 2species

A

Acute toxicity

72
Q

Required for most agents, esp intended for chronic use

A

Subacute/Chronic toxicity

73
Q

FDA drug category: safe for both pregnant human and animal studies

A

Class A

74
Q

FDA drug category: positive evidence of human fetal risk, but benefit from use in pregnant women maybe acceptable despite the risk

A

Class D

75
Q

Teratogen: Fetal renal damage

A

ACE inhibitors

76
Q

SE: antiepileptic drugs

A

Neural tube defect

77
Q

Causes fetal hydantoin syndrome

A

Phenytoin

78
Q

Cause neonatal hypoglycemia

A

Oral hypoglycemic agents

79
Q

Teratogen causes vaginal clear cell adenoCA

A

Diethylstilbestrol / DES

80
Q

Teratogenic effect of alcohol

A

Fetal alcohol syndrome

81
Q

Teratogen causes Ebstein’s anomaly

A

Lithium

82
Q

Teratogen causes craniofacial malformation

A

Isotretinoin

83
Q

Teratogen causes congenital hypothyroidism

A

Iodide

84
Q

Teratogen causes Mobius sequence

A

Misoprostol

85
Q

Preclinical data collected up to the time of submission and detailed proposal for clinical trials

A

Investigational new drug (IND)

86
Q

Produces less than the full effect, act as inhibitor in the presence of an agonist

A

Partial agonist

87
Q

Teratogen causes tooth discoloration

A

Tetracycline

89
Q

Teratogenic effect of Sulfonamides

A

Kernicterus

90
Q

Penicillamine teratogenic effect

A

Cutis laxa

91
Q

Topical preparation used for chronic inflammation

A

Lubricating agents - creams, ointments

92
Q

Thalidomide teratogenic effect

A

Phocomelia

93
Q

Teratogenic effect of warfarin at 1st tri

A

Chondrodysplasia

94
Q

Refer to drug for a rare disease

A

Orphan drug

95
Q

Standard in vitro test for mutagenicity, loss of this dependence signals mutation

A

Ames test - uses Salmonella

96
Q

Teratogenic effect of Streptomycin

A

Ototoxicity

97
Q

Teratogenic effect of smoking

A

IUGR

98
Q

Phase: careful evaluation of dose-response relationship and pharmacokinetics among normal human (25-50)

A

Phase 1 trial

99
Q

Postmarketing surveillance phase

A

Phase 4 trial

100
Q

Teratogenic effect of warfarin at 2nd trimester

A

CNS malformations

101
Q

Teratogenic effect of warfarin 3rd trimester

A

Bleeding diathesis

102
Q

Refer to two related drugs showing comparable bioavailability and similar times to achieve peak blood concentrations

A

Bioequivalence

103
Q

Phase: explore further the spectrum of beneficial actions of the new drug. Large design involving many patients (1000-5000)

A

Phase 3 trial

104
Q

Request for approval of general marketing of new agent for prescription uses

A

New drug application (NDA)

106
Q

Evaluation of drug to moderate number of patients (100-300)

A

Phase 2 trial

109
Q

Warfarin inhibits vitamin K dependent factors synthesis, antidote would be Vitamin K, FFP. What will you monitor in the patient?

A

PT/INR - can cross the placenta

110
Q

Maximal effect achievable with increasing concentration of a drug

A

Emax or efficacy

112
Q

Excretion of weak base maybe accelerated by acidifying the urine using what?

A

Ammonium chloride

128
Q

Preferred route for drugs that has unpleasant taste and for patients who are vomiting

A

Rectal or suppository route

Pharmacology (11 decks)

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