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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
Concentration in zero order/saturable/michealis menten decreases ______ over time
Linearly
26
Drugs that display Zero Order Elimination kinetics?
WHAT PET ``` Warfarin Heparin Aspirin Tolburamide Phenytoin Ethanol Theophylline ```
27
It is the maximal effect available with increasing concentration of a drug
Efficacy (Emax)
28
It is the dose required to produce 50% of the max effect
Potency (EC50)
29
Concentration required to bind 50% of the receptors
Kd
30
Smaller the Kd, the ____ the affinity
Greater
31
Maximum percentage of receptors with increasing concentration of a drug Maximal number of receptors bound
Bmax
32
Minimum dose required to produce a specified response is determined in each member of a population
Quantal Dose-Response Curve
33
Formula for therapeutic index
TD 50 divided by ED50
34
Efficacy is measured through _____ dose response curves
Graded
35
Receptors that do not bind when the drug concentration is sufficient to produce maximal effect
Spare receptors
36
In the presence of an agonist, a partial agonist can act as _______
Antagonist
37
Effects of competitive antagonists can be overcome by
Adding more agonist
38
Competitive antagonists shift the dose response curve to the
Right
39
Non competitive antagonists causes a ____ shift to the dose response curve
Downward shift
40
This type of antagonist binds to q different receptor and produces an effect opposite to that produced by the drug it is antagonizing
Physiologic antagonists
41
This type of antagonist directly interacts with the drug to remove it or prevent it from reaching the target
Chemical antagonist
42
Responsiveness diminishes rapidly after administration of a drug
Tachyphylaxis
43
What drugs display tachyphylaxis?
MEDical students Love to watch CNN in HD! ``` Metoclopramide Ephedrine Dobutamine LSD Calcitonin Nitroglycerin Nicotine Hydralazine Desmopressin ```
44
The concentration of a drug at the receptor site
Effective Drug Concentration
45
The concentration at the receptor site is proportional to the drug concentration in the plasma at equilibrium except in?
Topical agents
46
Pharmacokinetic parameter that can be altered by liver and kidney disease
Volume of distribution | Clearance
47
Most important pharmacokinetic parameter to be considered in defining a rational steady state during dose regimen
Clearance
48
Condition in which the average total amount of drug in the body does not change over multiple dosing intervals
Steady state
49
Steady state is reached in?
4-5 half lives
50
Cockroft Gault Equation
(140-Age) x kg ------------------- 72 x serum crea (X 0.85 females)
51
Long term reduction in receptor number due to continuous exposure to agonist
Downregulation
52
Receptor activation is blocked for prolonged periods
Upregulation
53
Fraction of the administered dose that reaches the systemic circulation
Bioavailability
54
Bioequivalence is determined by
AUC Cmax Tmax
55
This is when the drug is 85-125% of the innovator
Bioequivalence
56
Pharmacokinetics: | Equal to the rate of elimination arlt steady state
Maintenance dose
57
This is given when the therapeutic concentration must be achieved rapidly and volume of distribution is large
Loading dose
58
Formula for adjustment of dose in renal impairment
Crea clearance. X ave dose ---------------- 100ml/min
59
Computation of the amount of drug in the body at any time:
Vd x plasma concentration
60
What are the Phase 1 reactions?
HORD Hydrolysis Oxidation Reduction Deamination
61
Most important organ for drug metabolism
Liver
62
Primary determinant of clearance
Drug Biotransformation
63
Cytochrome P450 INDUCERS: Ethel Booba takes Phen Phen and Refuses Greasy Carb Shakes
``` Ethanol Barbiturates Phenytoin Rifampicin Griseofulvin Carbamazepine St. John's Wort ```
64
This type of inhibitors bind irreversibly to metabolizing enzymes
Suicide inhibitors
65
Cytochrome P450 INHIBITORS Inhibitors Stop Cyber Kids from Eating GRApefruit QV
``` Isoniazid Sulfinamides Cimetidine Ketoconazole Erythromycin Grapefruit juice Ritonavir Amiodarone Quinidine Valproic acid ```
66
These types of Phase 2 reactions are used for inactivation
Acetylation | Methylation
67
Typical Drugs that use acetylation: HIPS
Hydralazine Isoniazid Procainamide Sulfonamide
68
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
Category A
69
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
Category B
70
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
Category C
71
FDA category Positive evidence of human fetal risk but the benefits may be acceptable despite the risk
Category D
72
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
Category X
73
Common Teratogens | Valproic acid Anti epileptics
Neural tube defects
74
All anticonvulsants are CYP450 INDUCERS except:
Valproic acid
75
All antidepressants are CYP450 INHIBITORS except
St. John's Wort
76
Teratogen | Phenytoin
Fetal hydantoin syndrome
77
Teratogen | Diethylstilbestrol (DES)
Vaginal clear cell adenoCA
78
Teratogen | Lithium
Ebstein's anomaly
79
Teratogen | Isotretinoin
Craniofacial malformation
80
Teratogen | Misoprostol
Möbius sequence
81
Teratogen | Penicillamine
Cutis laxa
82
Teratogen | Thalidomide
Phocomelia
83
Teratogens | Tetracycline
Tooth discoloration
84
Teratogens | Streptomycin
Ototoxicity
85
Teratogens | Methimazole
Aplasia cutis congenita
86
Teratogens | Sulfonamides
Kernicterus
87
Teratogens | Fluoroquinolones
Cartilage damage
88
Teratogens | Warfarin 1st trimester
Chondrodysplasia
89
Teratogens | Warfarin 2nd trimester
CNS malformation
90
Teratogens | Warfarin 3rd trimester
Bleeding diasthesis
91
Standard in vitro test for mutagenicity Uses special strain of Salmonella
Ames Test
92
In vivo mutagenicity test carried out in mice where males are exposed to substance before mating
Dominant lethal test
93
Includes all preclinical data collected up to the time of submission and the detailed proposal for clinical trials
Investigational new drug
94
What clinical trial phase is decribed when there is evaluation of the dose response relationship and pharmacokinetics among NORMAL volunteers?
Phase 1
95
How many test subjects are included in Phase 1?
25-100 normal | 20-50 chemo
96
Phase of the clinical trial where evaluation of the drug is done in patients with the target disease under controlled conditions.
Phase 2
97
Phase of clinical trial where desired efficacy at tolerated doses is tested
Phase 2
98
Phase of the clinical trial where a large design involing many patients that include special populations
Phase 3
99
Phase of clinical trial where they explore the spectrum further and compare it to older therapies and to discover infrequent toxicities
Phase 3
100
This is also called the postmarketing surveillance phase
Phase 4
101
This is the right to market the drug without competition from other firms
Drug patents
102
How many years is allowed in a drug patent?
20 years

Pharma (15 decks)

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