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Flashcards in Basics Deck (92):
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Monitor PT/INR
Inhibits Vit K dependen5 factors

Warfarin

1

Monitor PTT
Activates anti-thrombin III

Heparin

2

Warfarin antidote

Vit K
FFP

3

Heparin antidote

Protamine sulfate

4

Antidote for Organophosphate poisoning

Pralidoxime

First line is Atropine

5

Most important limiting factor for permeation

Lipid diffusion

6

Predicts rate of movement of molecules across a barrier

Fick's law of diffusion

7

What molecules are more water soluble, leading to increased clearnace?

Ionized (charged) and polar

8

What molecules are more lipid soluble, leading to increased capacity to cross biological membranes?

Non-ionized (uncharged) and non polar

9

PH= pKa + log of A?/B?

A: Unprotonated
B: Protonated

10

Weak acid can be excreted faster by __________ the urine with __________.

Alkalinizing
Bicarbonate HCO3

To make ACIDIC BASIC, give BICARB

ABB

11

Weak base can be excreted faster by __________ the urine with __________.

Acidifying
Ammonium chloride (NH4Cl) or KCl

To make BASIC ACIDIC, give AMMONIUM CHLORIDE

BAA

12

Identify: Site of drug metabolism is in the gut wall, portal circulation and liver, usually noted in oral drugs

First Pass Effect

13

Bypasses first pass effect

IV
IM
Sublingual
Transdermal

14

Anticoagulants cannot be given via _____ route

IM
Can cause hematomas

15

Order based on superiority
Oral, IV, IM, SubCu, Buccal/Sublingual, Rectal

IV
IM
SubCu
Buccal/Sublingual
Rectal
Oral

16

Partial avoidance of first pass effect in ________ route

Rectal

17

Which of the 3 veins of the rectum exhibits first pass effect?

Superior Rectal Vein

18

Order based on decreasing evaporation:

Ointment
Gel
Lotion
Cream

Lotion
Gel
Cream
Ointment

19

Acute inflammation of the skin:
Use drugs with Increased or decreased evaporation?

Increased

20

Chronic inflammation of the skin:
Use drugs with Increased or decreased evaporation?

Decreased

21

Can bound drugs cross membranes?

No
Only unbound drugs can cross
Acidic and basic drugs are BOUND

22

Drugs that are not modified by the body and continue to act until excreted

Drugs?

Mannitol
Lithium

23

Concentration decreases 50% for every half life
Concentration decreases exponentially
Most common

Type of elimination

First Order

24

Rate of elimination is constant for every half life
Concentration decreases linearly

Zero order

25

Drugs that display Zero Order Kinetics

WHAT PET

Warfarin
Heparin
Aspirin
Tolbutamide
Phenytoin
Ethanol
Theophylline

26

In the presence of a full agonist, a ___________ agonist can act as an inhibitor

Partial

27

These do not provoke a biological response by themselves upon binding to a receptor
Blocks or dampens drug response in the presence of an agonist

Antagonist

28

Irreversible antagonist
Not overcome by adding more agonist

Non-competitive

29

Reversible antagonist
Overcome by adding more agonist

Competitive

30

Shifts dose response curve to the right

Competitive antagonist

31

Shifts dose response curve to the left

Non-competitive antagonist

32

Binds to a different receptor producing an effect that is opposite to the effect of the drug it is antagonizing

I.e. Histamine and epinephrine

Physiologic antagonists

33

Reduces constituitive activity
Opposite effects are produced by the agonist

I.e. Propranolol, thyroid hormone

Inverse agonist

34

Antagonist that interacts directly with the drug to remove it or prevent it from reaching its target

Doesn't depend on interaction with agonist receptors

I.e. Dimercaprol for lead poisoning
Pralidoxime for organophosphate poisoning

Chemical antagonists

35

Drugs that exhibit Tachyphylaxis
DELaMar watches CNN in HD

Dobutamine
Ephedrine
LSD
Metoclopramide
Calcitonin
Nitroglycerin
Nicotine
Hydralazine
Desmopressin

36

Define: Drug input equals rate of elimination

Steady state

37

Number of half lives to reach steady state

4-5

38

Plasma drug concentration is inversely proportional to_______

Vd and Clearance

39

Vd is __________ proportional to half life

Directly

40

Clearance is ___________ proportional to half life

Inversely

41

Area under the curve (AUC ) is a measure of_________

Bioavailability

42

Clearance is __________ proportional to Maintenance dose

Directly

43

Desired plasma concentration is _______ proportional to maintenance dose

Directly

44

Bioavailability is ___________ proportional to maintenance dose

Inversely

46

Trough determinines the minimum ___________ concentration

Effective

47

Peak determines the minimum ___________ concentration

Toxic

48

Effect of renal disease and reduced CO on drug clearance

Decrease

49

Phase I reactions that convert a parent drug to a more polar or water soluble product
Not highly selective of substrates

HORD

Hydroxylation
Oxidation
Reduction
Deamination

50

75% of drugs are metabolized by Cytochrome______

CYP 3A4
CYP 2D6

51

Phase II reactions that makes original drug more polar (water soluble) less lipid soluble
Not very selective

GAG GSM

Glucuronidation
Acetylation
Glutathione conjugation
Glycine conjugation
Sulfation
Methylation

52

Asians are ______ acetylators

Fast

Must increase drug

53

Caucasians are ________ acetylators

Slow

54

Cytochrome P450 inducers

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

Ethel Booba takes PHEN-phen and Refuses Greasy Carb Shakes

55

Cytochrome P450 Inhibitors

Isoniazid
Sulfonamides
Cimetidine
Ketoconazole
Erythromycin
Grapefruit Juice
Quinidine
Valproic Acid
Ritonavir
Amiodarone

ISO Santa Claus Kissing Every Girl, Quickly Vanishing Right After

56

Class of Drugs:
Safe in pregnant human
Safe in pregnant animal

Folic acid, thyroid hormone

A

57

Class of Drugs:
No studies in pregnant human, Safe in pregnant animal
OR
Safe in pregnant human, unsafe in pregnant animal

Zidovudine

B

58

Class of Drugs:
No studies in pregnant human, Unsafe in pregnant animal
OR No studies in both human and pregnant animals

Aspirin

C

59

Class of Drugs:
Unsafe in pregnant human
Unsafe in pregnant animal

ACE inhibitors, Anticonvulsants

D

60

Class of Drugs:
Unsafe in pregnant human
Unsafe in pregnant animal

Statins, OCPs, Chlomiphene, Misoprostol, High Dose Vit A
Teratogenic

X

61

Fetal-renal damage

ACE inhibitors

62

Neural Tube Defects

ADR of which drug?

Anti-epileptic drugs

63

Fetal Hydantoin Syndrome

ADR of which drug?

Phenytoin

64

Neonatal hypoglycemia

ADR of which drug?

Oral hypoglycemic agents

65

Neonatal dependence

ADR of which drug?

Barbiturates

66

Vaginal Clear Cell AdenoCA

ADR of which drug?

Diethylstilbestrol (DES)

67

Fetal Alcohol syndrome

ADR of which drug?

Ethanol

68

Ebstein's anomaly

ADR of which drug?

Lithium

69

Craniofacial malformations

ADR of which drug?

Isotretinoin

70

Congenital hypothyroidism

ADR of which drug?

Iodide

71

Mobius sequence

ADR of which drug?

Misoprostol

72

Cutis laxa

ADR of which drug?

Penicillamine

73

Phocomelia

ADR of which drug?

Thalidomide

74

IUGR

ADR of which drug?

Smoking

75

Tooth discoloration

ADR of which drug?

Tetracycline

76

Ototoxicity

ADR of which drug?

Streptomycin

77

Aplasia Cutis Congenita

ADR of which drug?

Methimazole

78

Kernicterus

ADR of which drug?

Sulfonamides

79

Cartilage damage

ADR of which drug?

Fluoroquinolones

80

Chondrodysplasia

ADR of which drug?

Warfarin 1st trimester

81

CNS malformations

ADR of which drug?

Warfarin 2nd trimester

82

Bleeding diatheses

ADR of which drug?

Warfarin 3rd trimester

83

In vitro test for mutagenicity

Ames test

84

In vivo mutagenicity test in mice

Dominant lethal test

85

Preclinical data up to proposal for clinical trials

Investigational New Drug

86

Includes preclinical and clinical testing
Request for approval of general marketing of drug for prescription use

New Drug Application

87

Phases of Drug Trial:
Among normal human volunteers (25-50)
Is it safe?

Phase I Trial

88

Phases of Drug Trial:
Among volunteers with target disease (100-300)
Is it effective?

Phase II Trial

89

Phases of Drug Trial:
Among many patients and clinicians (1000-5000)
Compare with older therapies and discover toxicities

Phase III Trial

90

Detects infrequent toxicities
Post-marketing surveillance

Phase IV Trial

91

Drug for a rare disease, affecting fewer than 1 every 200,000 people

Orphan drug

110

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

Therapeutic window