Pharmacodynamics/kinetics Flashcards by Shirica Shaw

What are the 4 ways a drug binds to a receptor? How do they work?

Ion: one atom transfers an electron

Hydrogen: attracted to nearby electronegative atoms

Van der Waals: weak fluctuating bonds

Covalent: shared electrons

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What is another name for ion bonding?

Electrocovalent

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Competitive antagonists shift the dose curve to the ______

Right

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What is an inverse agonist? Give examples

A drug that competes for the same site as an agonist but produces the opposite effect.

Propranolol
Metoprolol
Cetirizine
Loratadine
Prazosin
Naloxone

“Pro met sneezing cat named Lora, who praised Nala”

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Inverse agonist were once called _______

Antagonist

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T/F: the amount of receptors that we have can increase or decrease depending on comorbidities and drug therapies

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How are receptors classified?

By location

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What are the three types of receptors? What do they consist of?

Lipid bilayer: opioids benzos, beta blockers, catecholamines, NMBD
Intracellular proteins: insulin, steroids, Milrinone
Circulating proteins: anticoagulant (warfarin)

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What are your vessel rich groups?

Parts of the body that have a high cardiac output; in a 1 compartment model, blood flows here after the aorta

Heart
lungs
liver
kidney
brain

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What is the more realistic model?

2 compartmet model

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What type of drugs are able to leave the central compartment and go to the peripheral compartment?

Fat soluble drugs (lipid solube)

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Which drugs have a larger volume of distribution, fat/lipid soluble, or water soluble?

Fat soluble

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Where do water soluble drugs normal stay?

Plasma

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Can narcotics cross the bilayer?

Yes

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What are the 2 things that affect volume of distribution?

changes in blood volume
# of carrier proteins

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Almost all drugs we give are bound to ________

plasma proteins

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What type of protein do acidic drugs primarily bind to? Alkalotic drugs?

Acidic drugs: albumin

Alkalotic drugs: A-1 acid glycoprotein

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What are conditions that decrease albumin? Would affect does this have on anesthesia?

Malnutrition
Burns
Liver failure
Acidosis

This increases the free drug which can cross into membranes and increase concentration/potency.

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What can cause decreased plasma proteins in general?

Pregnancy
Age
Hepatic disease
Renal failure

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What does it mean when a drug has poor protein binding and is lipophilic? What are some examples?

This drug is free and can cross lipid bilayers

This drug will have a big volume of distribution

ex) Thiopental, Diazepam

Highly protein bound to plasma, protein drugs have a _________ volume of distribution. What are some examples?

Small

Ex) warfarin

What drugs have active metabolites?

Diazepam
Propranolol
Morphine (has 2)
Prodrugs like codeine

What happens during metabolism?

Convert active, lipid, soluble drugs to inactive drugs that are able to be excreted

What are the ways that drugs are metabolized?

CYP450 enzyme in the liver (liver main way)
Kidney
Tissue esterase (GI, Placenta)

What is phase 1 of metabolism consist of?

Oxidation Reduction Hydrolysis ** all drugs and bonds are getting ready to be water soluble**

What is phase 2 of metabolism consist of?

Conjugation ** covalently links, a highly polar molecule to become water soluble**

Describe CYP450

-Large family with 10 isoforms -Membrane bound -contains a heme cofactor -involves oxidation and reduction

What is the most common Phase 1 enzyme for anesthesia drugs?

CYP3A4

What is the difference between something that induces and inhibits the CYP450 enzyme? Give examples.

Induces: increases the amount of enzyme --> increases metabolism ex) phenobarbital Inhibits: decreases amount of enzyme --> increases concentration of drug ex) grapefruit juice

T/F: Hepatic aesthetic drugs clearance is constant

Differentiate between flow llimited and capacity limited hepatic clearance

Flow limited: rate is proportional to concentration Capacity limited: metabolism is exceeded since liver capability is not unlimited

What is Context Sensitive Half-Time?

Time to a 50% decrease after an infusion at a constant concentration is discontinued

What does it mean when the PK & the pH are identical?

50% of the drug is ionized and 50% of the drug is non-ionized

What's the main difference between ionized drugs, and non-ionized drugs?

Drugs that are ionized are more likely to stay water soluble and not cross barriers

Most drugs are ______ acids & bases

weak ex) acids: barbs bases: LA; opioids

Elderly populations have _________ cardiac output and __________ protein binding

Decreased Decreased

Define efficacy versus potency

Efficacy: the ability of a drug to produce a clinical effect Potency: less drug with more affect. Concentration versus response.

T/F: plasma is a site of effect for anesthetic drugs

F CNS

What is lag time?

Time between administration and effect in the CNS

The therapeutic index =

Lethal dose 50% / effective dose 50%

What are enantiomers?

Structures that are chemically identical & are mirror images

What are chiral compounds?

Molecules with asymmetric centers

What are optical isomers?

Enantiomers

Describe rotation of light in optical isomers

rotates light in solution If right: Dextrorotatory left: levorotatory

Describe molecule sequence in optical isomers

R: rectus S: sinister

Describe Racemic mixtures

50/50 mixtures of 2 optical isomers/enantiomers 1 enantiomer is active the other is inactive of has adverse side effects

The enantiomer for Albuterol is ______

Xopenex

_______ is the enantiomer for Atracurium. What does it do?

Nimbex Lacks histamine effects

PCN is ________ the PT cap

secreted from

Pharmacodynamics/kinetics Flashcards

Test 1