Basic Principles Flashcards by Clyde Silverio

____ actions of a drug on the body

Pharmacodynamics

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___ actions of the body on the drug

Pharmacokinetics

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Arrange to according to decreasing strength

Covalent, Hydrophobic, Electrostatic bonds

Covalent
Electrostatic
Hydrophobic bonding

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[Type of diffusion]

passive movement of non-protein bound drugs

Aqueous diffusion

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[Type of diffusion]

affected by the drug concentration and charge

Aqueous diffusion

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[Type of diffusion]

governed by Fick’s Law of Diffusion

Aqueous diffusion, Lipid Diffusion

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[Type of diffusion]

movement of drugs through lipid membranes from ECF to the ICF

lipid diffusion

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[Type of diffusion]

most important limiting factor for permeation

Lipid diffusion

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[Type of diffusion]

important for the diffusion of weak acids and weak bases

Lipid diffusion

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[Type of diffusion]

for drugs that do not readily cross through membranes; transported across barriers by mechanisms that carry similar endogenous substances

transport by special carriers

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[Type of diffusion]

not governed by Fick’s law of diffusion is capacity-limited

transport by special carriers

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[Type of diffusion]

vitamin B12 bound to intrinsic factor is a type of _____

endocytosis

pinocytosis

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[Type of diffusion]

iron bound to transferrin

endocytosis and pinocytosis

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[Water/Lipid Solubility of Drugs]

____ is directly proportional to electrostatic charge

directly proportiona

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[Water/Lipid Solubility of Drugs]

ionized and polar drugs _____ (water/lipid soluble)

water soluble

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[Water/Lipid Solubility of Drugs]

this is associated with an increased clearance

water soluble

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[Water/Lipid Solubility of Drugs]

inversely proportional to electrostatic charge

inversely proportional

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What are the 3 dependent factors for permeation?

Solubility
Concentration gradient
Surface area and vascularity

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[Water/Lipid Solubility of Drugs]

unprotonated weak acid

more water-soluble, better clearance

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[Water/Lipid Solubility of Drugs]

protonated weak acid

more lipid soluble, more likely to cross biological membranes

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[Water/Lipid Solubility of Drugs]

unprotonated weak base

more lipid soluble, cross biological membrane

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[Water/Lipid Solubility of Drugs]

protonated weak base

more water soluble, better clearance

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[Absorption/Excretion]

if a compound is placed in a solution above its pKa

this favors? (Absorption/excretion)

favors absorption

Above its pKa, unprotonated form predominates, which favors absorption

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[Absorption/Excretion]

if a compound is s placed in a solution below its pKa

this favors? (Absorption/excretion)

favors excretion

Below its pKa, protonated form predominates, which favors absorption

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[Absorption/Excretion] if a weak base is placed in an acidic environment? this favors? (Absorption/excretion)

favors excretion Again, basic drugs are excreted in an acidic environment

[Absorption/Excretion] if an acidic compound is placed in an alkalitic environment this favors? (Absorption/excretion)

favors excretion

What are the 3 major factors that affect drug absorption>

1. Route of administration 2. Blood flow 3. Concentration

[Route of drug administration] highest first pass effect?

oral route

[Route of drug administration] potentially more dangerous

IV route

[Route of drug administration] bypasses first pass effect

IV IM SQ Buccal/Sublingual

[Route of drug administration] anticoagulants cant be given by this route

[Route of drug administration] IM injection to buttocks is safest at

superolateral

[Route of drug administration] inferomedial buttock IM injection can result to this complication

sciatica

[Route of drug administration] superomedial buttock IM injection is associated with this gait

gluteus medius gait

[Route of drug administration] Offers direct absoprtion to systemic venous circulation, bypasses the FPE

Buccal/Sublingual

[Route of drug administration] trace the route of the drug via the sublingual route before reaching the heart

lingual, IJV, Brachiocephalic, SVC, RA

[Route of drug administration] partial avoidance of the FPE, used for large amounts of drugs with unpleasant tase

Racta

[Route of drug administration] offers delivery closes to target

inhalational

[Drug distribution] What are the factors that affect drug distribution?

1. Size of the organ 2. Blood flow 3. Solubility 4. Protein binding

[Drug distribution] Basic drugs are bound to these proteins ____

orosomucoid and alpha 1 acid glycoprotein

[Drug distribution] acidic drugs are bound to this protein

albumin

Drug with the lowest molecular weight, can cross BBB

lithium

Drug that is water soluble, but can cross the BBB because it has a low molecular weight

ethanol

the duration of drug action is determined by?

1. dose administered | 2. rate of elimination following last dose

[Drug elimination] rate of elimination is proportionate to the concentration

first order

[Drug elimination] rate of elimination is constant regardless of concentration

Zero-order

What drugs display zero order elimination kinetics?

1. Warfarin 2. Heparin 3. Aspirin 4. Tolbutamide 5. Phenytoid 6. Ethanol 7. Theophylline

What are the characteristics of a receptor?

1. Selective in their ligand-binding 2. modifiable 3. most are proteins

[Graded dose-response relationship] ___ concentration required to bind 50% of the receptors

[Graded dose-response relationship] A ____ kd is associated with greater affinity for its receptor

smaller Kd

[Graded dose-response relationship] ____ is the maximal effect achievable with increasing concentration of a drug

Emax

[Graded dose-response relationship] ____ concentration of drug wherein half of the maximal effect is achieved

EC50

[Graded dose-response relationship] ___ maximum percentage of receptors with increasing concentration of a drug/maximal number of receptors boudn

Bmax

[Type of dose response curve] response of a particular receptor-effector mechanism measured against increasing drug concentration

dose response

[Type of dose response curve] fraction of the population that response at each dose against the log of the dose administered

quantal dose-reponse curve

[Type of dose response curve] Efficacy and potency are derived from this curve

graded dose-response curve

[Type of dose response curve] Median effective, median toxic, median lethal doses are derived from this curve

quantal dose-response curve

What is the formula to determine the therapeutic index?

TI = TD50/ED50

___ refers to the dose range between the most effective dose and the most toxic dose

Therapeutic index

___ refers to the amount of drug needed to produce a given effect

potency

___ is determined by the affinity of the receptor for the drug (efficacy/potency)

potency

Noncompetitive antagonist causes ____ shift of the DRC

downward

competitive antagonist causes _____ shift of DRC

right shift

_____ continuous activation may lead to depletion of essential substrates

tolerance

____ responsiveness diminishes rapidly after administration of a drug; frequent or continuous exposure to agonist results in short-term diminution of the receptor

tachyplaxis

[Volume of distribution] a low Vd distributes in?

blood

[Volume of distribution] a high Vd distributes in?

tissues

___ most important pharmacokinetic parameter to be considered in defining rational steady state during dosage regimen

clearance1

Steady state is achieved after how many half-lives?

4-5

___ are also called mixed function enzyme

Cyt P450

____ is a standard in vitro test for mutagenicity

Ames test

____ is an in vivo mutagenicity test carried out in mice

dominant lethal test

[Clinical trial] ____ preclinical data collected up to time ofsubmission

investigation

[Clinical trial] ____ request for approval of general marketing of the agent for prescription use

new drug application

[Clinical trial] evaluation of the dose-response relationship and pharmakokinetics among normal human volunteers (20-100 volunteers)

Phase 1 Trial

[Clinical trial] in phase 1 trial of a cancer drug, how many volunteer patients are needed

20-50

[Clinical trial] 100-200 patients with target disease, done in hospital ward

phase 2

[Clinical trial] 1000-5000 patients; double-blind crossover design

phase 3

[Clinical trial] post marketing surveillance

phase 4