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Drugs and Discovery > Vocabulary > Flashcards

Vocabulary Flashcards

Learn Vocabulary for Pharmaceutical Chemistry

1
Q

Clearance (Clint)

A

A fundamental Pharmacokinetic term that refers to the ability of the body to eliminate a drug. Clearance = (rate of elimination)/(concentration of drug in biofluid). Total body clearance ius actually the sum of clearance by renal, liver, and other mechanisms

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2
Q

Total Body Clearance

A

Sum of clearance by renal, liver, and other mechanisms

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3
Q

cLogP or cLogD

A

Calculated or theoretical LogP; @ single pH value, or across pH spectrum

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4
Q

CYP’s

A

Cytochrome p450 enzymes that oxidatively metabolize drugs in the liver, subtypes; 1a@, 2C9, 2C19, 2D6 and 3A4

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5
Q

Distribution

A

A pharmacokinetic term that refers to the movement of a drug from the site of administration into the various tissues and organ systems of the body. In most cases, distribution is used to describe the passage of a drug out of the vascular system to other compartments of the body

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6
Q

EC50

A

The molar concentration of an agonist which produces 50% of the maximum possible response for that agonist

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7
Q

Efficacy

A

Describes the way in which agonists vary in the response they produce, even when they occupy the same number of receptors

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8
Q

Excretion

A

A pharmacokinetic term that refers to the irreversible removal of a drug in the unchanged form. Excretion is one of two processes (metabolism, excretion) that account for the elimination of a drug from the body. The kidney is the typical site of drug excretion, although excretion may occur at the liver, lungs, etc.

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9
Q

First pass metabolism

A

Drugs which are absorbed from the gut travel directly to the liver where some are extensively metabolized before they can reach their intended site of action

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10
Q

Fu

A

Fraction unbound, see protein binding

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11
Q

GLP

A

Good Laboratory Practices

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12
Q

GMP

A

Good Manufacturing Practices

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13
Q

Hepatic Clearance

A

The hepatic clearance is the amount of drug removed by the liver as calculated by determinining the amount of drug presented to the liver by the hepatic artery and the portal vein and the amount of drug found leaving the liver in the hepatic vein. It should be noted that the liver has the greatest metaboli capacity of any organ

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14
Q

HTL

A

Hit-to-lead

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15
Q

HTS

A

High throughput screening

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16
Q

ia

A

Intra-arterial; in to the lumen of the artery

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17
Q

ic

A

intracerebral; into the brain

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18
Q

IC50

A

Where an agonist causes an inhibitory response, the IC50 is the molar concentratoin which produces 50% of its maximum possible inhibition

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19
Q

icv

A

Intracerebroventricular administration; into the ventricles of the brain

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20
Q

id

A

Intradermal; into the dermal layer of the skin

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21
Q

im

A

intramuscular; into a skeletal muscle

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22
Q

IND

A

Investigational New Drug

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23
Q

Intrinsic Activity

A

A term used to describe the mathematical relationship between a receptor occupancy and a tissue response. (Term exchangeable with Efficacy)

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24
Q

Inverse Agonist

A

A drug which produces an effect opposite to that of an agonist, yet acts at the same receptor

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25
Q

ip

A

intraperitoneal; into the peritoneal cavity

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26
Q

it

A

Intrathecal; into the spinal canal

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27
Q

iv

A

Intravenous; into a vein

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28
Q

IVT

A

In Vivo Toleration

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29
Q

LogP

A

A measure of the lipophilicity of a compound; its partition coefficient between an organic solvent (usually octantal) and an aqueous buffer.

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30
Q

Mechanism of Action (MOA)

A

This refers to the specific biochemical actions of a drug on a biological system that account for the effects produced by the drug

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31
Q

MW

A

Molecular Weight

32
Q

NCE

A

New Chemical Entity

33
Q

NDA

A

New Drug Application

34
Q

Nocte

A

At night dosing

35
Q

Non-hepatic Clearance

A

Clearance of a drug which is not mediated by the liver

36
Q

Parenteral

A

Any route other than alimentary canal, usually means injected into body

37
Q

Partial Agonist

A

An agonist, which, no matter how high the concentration is applied, is unable to produce maximal activation of the receptors

38
Q

PCP

A

Physical Chemical Property

39
Q

pd

A

Pharmacodynamic

40
Q

Pharmacodynamics

A

The branch of pharmacology that deals wit the effects produced by a drug

41
Q

Pharmacokinetics

A

The branch of pharmacology that deals with the administration, uptake, distribution, and elimination of drugs from the body

42
Q

pk

A

pharmacokinetics

43
Q

pka

A

pH at which 50% of an acid is dissociated into H= and base. High pKa values indicate a weak acid

44
Q

Placebo

A

A dummy treatment in a clinical trial, designed to assess the extent to which fators other than the drug under test affect the outcome

45
Q

PO

A

Oral, by mouth

46
Q

POC

A

Proof of concept

47
Q

potency

A

A measure of the concentration of a drug at which it is effective (vague term; clarify with EC50, IC50, etc)

48
Q

Protein Binding

A

The process in which substances endogenous or exogenous bind to proteins, peptides, or enzymes

49
Q

qd

A

quaque die, once a day dosing

50
Q

QSAR

A

Quantitative Structure-Activity Relationships

51
Q

SAR

A

Structure Activity Relationships

52
Q

sc

A

Subcutaneous, under the skin

53
Q

T1/2

A

Term used to represent various biological half-lives fora drug, including; the kinetic or metabolic half-life, i.e. the time for the concentration of drug in plasma to decline to half of its original level. Or can also be expressed as the half-life of the effect of a drug, i.e. the time necessary for the response to decline to half of the original response.

54
Q

TI

A

Therapeutic Index; Ratio of the toxic dose of the drug to the doe which causes the desired therapeutic effect

55
Q

tid

A

Thrice-daily dosing

56
Q

Topical

A

Onto a surface such as skin

57
Q

tPSA

A

Topological Polar Surface Area

58
Q

Volume of distribution (Vd)

A

his is a hypothe1cal number expressed in liters which provides informa1on on the degree to which a drug is distributed. The Vd is the ra1o of the absolute amount of drug (e.g. mg) in the body to the concentra1on (e.g. mg/ml) as typically determined in plasma. If a drug (100mg) is administered i.v. and its Vd (100L) is large then its concentra1on in plasma is low (e.g. .001mg/ml) and it is widely distributed out of the plasma water compartment. If the concentra1on is rela1vely high (0.1mg/ml) then the Vd is low (10L) then the drug is retained in the plasma compartment. That the Vd can take on values that are clearly hypothe1cal is made clear by considering that Vd values can range far in excess of the actual fluid volume of a normal individual.

59
Q

Absorption

A

The sum of all the processes that are entailed in the movement of the drug from the site of administra1on to the inside of the body is considered to be absorp1on. For most prac1cal purposes, administra1on is considered to be complete when all of the drug has entered the circulatory system and is thus being distributed to the rest of the body. By this guideline, intravenous administra1on does not involve absorp1on since the drug is placed directly into the circulatory system.

60
Q

Acute Dosing

A

Single Dose

61
Q

ADME

A

Absorption, distribution, metabolism, excretion

62
Q

Affinity

A

The iaffinity of a compound for a receptor describes the avidity with which the compound binds to the receptor. Affinity is typically quantified by the kd

63
Q

KD

A

the kd is the concentration at which half of all the receptors are occupied by the copound. The lower the Kd, the greater the affinity of the compound for the receptor.Affinity is a property of the compound, not of the rector. Thus, two comounds could bind at the same receptor, but one can have a greater affinity for the receptor

64
Q

Agonist

A

A ligand or drug that when bound to a receptor induces a response or signal that mimics the natural endogenous ligand for that receptor.

65
Q

Full agonist

A

A ligand or drug that produces the same maximal response as the natural (endogenous) ligand.

66
Q

Partial Agonist

A

A ligand or drug that produces less than the maximal response of a full agonist even if all the receptors are bound at high concentrations

67
Q

Allosteric Binding Site

A

a site on a receptor/protein where the natural endogenous ligand does not bind. Drug/receptor interac1ons at allosteric binding sites may induce 3D‐conforma1onal changes in the structure of the receptor/protein that indirectly alter the binding of a ligand in the active site.

68
Q

Antagonist

A

A ligand or drug that when bound to a receptor does not provoke a biological response itself but blocks or dampens agonist‐mediated responses. In other words, an antagonist has affinity but no efficacy for a given target. It blocks or inhibits the func1onal of an agonist (natural or synthetic).

69
Q

Competitive antagonists

A

reversibly bind to receptors at the same binding site as the endogenous ligand or agonist. The degree of antagonism is dependent on the rela1ve concentra1ons of the agonist and antagonist (a competion between the two for the active site).

70
Q

Non‐competive antagonists

A

diminishes the maximum response of an agonist but is independent on the concentra1on of the agonist. This could occur via an irreversible interac1on with the ac1ve site or through an allosteric binding site.

71
Q

bid

A

bis in die, twice daily dosing

72
Q

Bioavailability

A

The amount of administered drug that is actually therepeutically available to the animal or patient. Bioavailability implies that the amount of drug that is bioavailable has access to its site of action

73
Q

Bioisostere

A

subs1tuents or func1onal groups with similar physical and chemical proper1es that impart similar biological responses within a given compound. Exchanging one bioisostere for another is a common tac1c in drug design to enhance the biological ac1vity or improve physiochemical proper1es of a compound without dras1cally changing the overall structure of the compound.

74
Q

Blood Brain Barrrier (BBB)

A

The endothelial cells of the capillaries of the brain and spinal cord are linked by tight junctions which prevent direct contact between plasma and cells of the central nervous system

75
Q

Chronic Dosing

A

Repeated dosing

76
Q

CIM

A

Confidence in Mechanism

Drugs and Discovery (1 decks)

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