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Intro Classes > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

pharmacotherapeutics

A

the rational clinical use of drugs to prevent, diagnosed, and treat medical conditions

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2
Q

three aspects of pharmacotherapy

A

1) clinical presentation (knowledge about your patient)
2) pathophysiology (knowledge of medical conditions)
3) pharmacology (knowledge of drug action)

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3
Q

therapeutics

A

the whole spectrum of modalities intended to manage medical conditions (e.g. surgery, radiation, chemotherapy)

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4
Q

drug

A

contains a known quantity of an identified pure biologically active substance

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5
Q

crude medicinal

A

an inconsistent mix of different biologically active substances, such as opium

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6
Q

nutrients

A

chemical compounds in food that are used by the body to function properly and maintain health

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7
Q

pharmacokinetics

A

the study of what the body does to a drug

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8
Q

pharmacodynamics

A

the study of what drugs do to the body

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9
Q

four stages of pharmacokinetics

A

absorption

distribution

biotransformation

excretion

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10
Q

absorption (drug)

A

the unidirectional movement of drug from the site of administration to the general blood circulation (the central compartment)

(i.e. the rate and extent that the parent drug reaches the general circulation)

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11
Q

two dimensions of absorption and units

A

rate (how fast); slope of blood concentration (C) over time (t)

extent (how much); area under the C/t curve

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12
Q

plasma

A

the fluid remaining after blood cells are removed from blood

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13
Q

parent drug

A

the chemically unchanged form of the drug

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14
Q

bioavailability definition and abbreviation

A

the fraction of the dose that reaches the general circulation (100% for IV drugs, oral drugs face barriers to absorption)

abbreviated as “F” (for fraction)

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15
Q

Bioavailability formula

A

Bioavailability (F) = (AUC oral/AUC IV)

Determined by measuring blood concentrations at several points after IV injection and measuring concentrations at several points after giving the same dose by any other route

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16
Q

Dose

A

The amount of drug taken at any one time

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17
Q

Dosage

A

The amount of drug taken over a chronological period (per day, per treatment cycle, etc.), and maybe comprised of several doses

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18
Q

Distribution

A

The (reversible) movement of drug between body compartments

19
Q

Volume of distribution

A

How much blood the dose appears to dissolve in

Volume = drug dose/plasma concentration

20
Q

Biotransformation

A

The body’s attempt to get rid of the parent molecule and its metabolites (primarily through the liver)

21
Q

Excretion

A

The rate that the body gets rid of drugs and drug metabolites; may occur via urine, bile, feces, sweat, or breath

22
Q

First-order elimination

A

The fraction of the drug concentration in plasma decreases by a constant proportion, regardless of the drug concentration (inverse log)

23
Q

Zero-order elimination

A

The fraction of the drug concentration in plasma decreases by a constant amount determined by the capacity of the elimination pathway (linear slope)

24
Q

Agonist

A

A drug that binds receptors that are active, and thus increase biological activity

25
Q

Antagonist

A

A drug that binds receptors that are inactive, blocking an agonist from interacting with the receptor and thus decreases biological activity

26
Q

Partial agonist

A

A drug that binds active and inactive receptors, increasing biological activity when the receptor equilibrium is mostly inactive, and decreasing biological activity when the receptor equilibrium is mostly active

27
Q

Inverse agonist

A

A drug that binds to a receptor that is normally always active, but unlike an antagonist that merely blocks an agonist from binding, the receptor, and inverse agonist reverses the receptor activity

28
Q

Drug receptor states

A

Active and inactive

29
Q

Reversible binding

A

The drug combined to the receptor and, part over and over again, usually using non-covalent bonds

30
Q

Irreversible binding

A

The drug covalently binds the receptors and does not dissociate unless the bond is broken by enzyme or other disassociating agents

31
Q

Orthosteric binding site

A

The drug binds to the usual site where it corresponded ligand usually binds to

32
Q

Allosteric binding site

A

The drug binds to any sites beside the usual ligand binding site

33
Q

Ligand-gated ion channels

A

Ionotropic receptors; drugs bind to these channels to alter ion conductance, either leading to hyperpolarization or depolarization (e.g. local anesthetics, sulfonylureas)

Happens in milliseconds, e.g. nicotinic ACh receptor

34
Q

G-protein coupled receptors

A

Metabotropic receptors; The drugs bind to the extracellular domain of a transmembrane receptor which acts on a regulatory GTP binding protein which then generates a second messenger (e.g. beta2 agonist)

Happens in seconds, e.g. Muscarinic ACh receptor

35
Q

Kinase-linked receptors

A

Drugs bind to the extracellular domain of a transmembrane receptor to activate the enzymatic activity of its cytosolic tail (e.g. insulin)

Happens in hours, e.g. cytokine receptors

36
Q

Nuclear receptors

A

Lipid soluble drugs diffuse across the membrane and activate these intracellular receptors [e.g. steroids (estrogen, testosterone), sterols (Vitamin D)]

Happens in hours, e.g. ostrogen receptor

37
Q

Competitive

A

A molecule binds to an enzyme’s active site, which prevents the original substrate binding and it’s effects can be modulated by changing the substrate concentration

38
Q

Non-competitive

A

A molecule binds to an enzyme’s allosteric site and causes a confirmational change to the enzyme’s active site. Increasing the original substrate levels does not reduce the inhibitor’s effect

39
Q

One Compartment Model Ratios

A

Solid:Fluid = Men - 40:60, Women - 45:55

ECF:ICF = (1/3)%:(2/3)%

Plasma:Interstitial Fluid = 20%:80%

40
Q

concentration of a drug at the active site is a function of what

A

concentration of the drug in the blood

41
Q

the most important factor affecting the rate of oral drug absorption

A 
stomach emptying
(absorption will be minimal until a drug gets past the stomach into the intestine)
42
Q

pre-hepatic blood is comprised of what

A

the splanchnic (portal) circulation that combines with the blood returning to the liver via the hepatic artery

43
Q

the first-pass effect

A

the extent that the liver prevents a fraction of the dose (when taken orally, rectally, or through skin) from reaching the systemic circulation is called the hepatic first-pass effect

44
Q

hepatic first-pass extraction vs bioavailability

A

inverse relationship

when hepatic first-pass extraction is 100%, bioavailability is 0

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