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CRP 108 Trial Design and Pharmacology > Lecture 2 > Flashcards

Lecture 2 Flashcards

1
Q

Pharmacokinetics

A

study of movement of drugs throughout body
-ADME

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2
Q

oral administration

A

safe, self-administered, economical, must be resistant to stomach enzmes and acid
-absoprtion affected by food intake, physcial activity
-harmful chemical processed by the liver

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3
Q

Intravenous

A

most rapid and accurate, cannot be removed from body easily if overdosed or allergic

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4
Q

Intramuscular

A

slower, more even absorption

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5
Q

Rectal administration

A

may avoid first-pass liver metabolism, used for vominting or those unable to take oral medication, or infants

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6
Q

Intraperitoneal

A

common for lab animals, injetion through abdominal wall into spce surrounding organs, used for cancer drugs

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7
Q

Subcuteaneous

A

injection just below skin, slow and varibale absorption, can be slowed with oil or impant

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8
Q

Inhalation

A

abosroption through lungs, rapid due to large surfae area

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9
Q

Topical

A

applied to mucous membranes, local effect, could be absorbed into bloodstream

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10
Q

Intranasal

A

Can pass blood-brain barrier, or for local effects in nasal passage

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11
Q

Transdermal

A

through the skin using patches, controlled and sustained delivery of drug

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12
Q

Epidural

A

spinal anesthetis to cerebrospinal fluid, pass blood-brain barrier

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13
Q

Infusion pump

A

impant under skin of scalp, constant antibiotic dose into cerebral ventricles

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14
Q

Gene therapy

A

application of DNA that encodes specific protein, used to increase or block gene expression to correct clinical condition, vectr needed to carry gene to cell nuclei, often viral vectors

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15
Q

Absorption factors (3)

A

primarily dictated by rate of passage into blood stream of drug through cell membrane. Phospholipids of the membrne have a hydrophilic head and two hydrophobic tails in a bilayer. Only lipid soluble drugs can pass freely, others need receptor or channel or pores in capillaries
-also affected by rate stomach empties and size and sex of the person

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16
Q

CSF

A

cerebralspinal fluid, fills subarachnoid space around brain and spinal cord. Many drugs cannot enter the CSF from the bloodstream

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17
Q

Brain capillaries

A

have distinct morphology that limits movement of water soluble molecules

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18
Q

blood brain barrier

A

separation between the brain capillaries and the brain/CSF

19
Q

Distribution

A

drug is distributed fastest to tissues with high blood flow and are vascular
slowe to low blood flow (muscle) and fat
slowest to tissues with lowest bloodflow (bone) and tendons

20
Q

Distribution depends on (3)

A

-cardiac blood flow
-degree of protein building
-volume of distribution
sometimes biological barriers such as blood brain barrier

21
Q

Drug transport

A

transporter proteins on cell membrane mediate drug concentrations in cells, uptake or efflux

22
Q

efflux transporters

A

remove drug from inside the cell, critical determinant of drug conentration inside cell, source of multii drug resistance

23
Q

uptake transporters

A

bring drugs into cell, critical determinant of drug concentration inside cell

24
Q

Drug depots

A

binding at inactive sites where no biological effect is initiated
-plasma proteins, fat, muscle
-cannot reach active sites or metabolism by liver
-reversible
-affects magnitude and duration of drug action -delays effects
-people vary in amount of depot binding
-nonselective, can bind different drugs
-can cause overdose, or higher expected blood levels of drug
-drugs reamin detectable in body for long times

25
Q

three routes of clearing drug from body

A

-hepatic metabolism
-bile
-urine

26
Q

drug metabolism

A

process of turning drug into its metabolites
-increase water solubility and prepare for elimination
-takes place in liver, minor metabolism in kidney, brain, skin and lungs

27
Q

Cytochrome p (CYP) 450

A

major role in drug metabolism
variable acitivity between people
cause of many drug drug interactions
different types of CYP 450

28
Q

CYP 3A4

A

most abundant p450, metabolism of about half of drugs on the market

29
Q

CYP 450 induction and inhibition

A

drugs can induce or inhibit CYP enzymes, increasing or decreasing metabolism

30
Q

drug activation

A

sometimes metabolism actives a drug (prodrug)
biotransformation into active compound

31
Q

kidneys

A

elimnation of drugs from blood into urine, pH of urine affects reabosrtion into kidney, also removes waste and excess salts from blood

32
Q

other routes of elimination

A

faeces, bile into faeces, lungs in air, breast milk, sweat

33
Q

Clearance (Cl)

A

total body clearance is sum of clearance from various metabolism pathways

34
Q

Pharmacodynamics

A

study of physiological and biochemical interaction of drug molecules with cell receptors in target tissue

35
Q

Neuropharmacology

A

drugs act on neurotransmitter receptors to enhance or reduce normal functioning of cell

36
Q

hormones

A

most hormones act on brain by binding receptors in cytoplasm or nucleus. alters cell function by triggering changes in gene expression

37
Q

receptor agonist

A

highest affinity for receptor and produce significant biologicl effect

38
Q

receptor antagonist

A

fits receptors but produces no cellular effect
partial agonists hgave intermediate efficacy (partially bind receptor)
inverse agonsis initiate biological affect that is opposite to agonist

39
Q

dose-response curve

A

describe extent of effect produced by given drug concentration

40
Q

threshold dose

A

smallest dose that exhibits measurable effect

41
Q

ED50

A

dose that produces half the maximal effect (50% effective dose)
-tell you about potency of a drug

42
Q

maximum response

A

assume all receptors are bound to drug (ED100)

43
Q

drug tolerance

A

diminished response to drug after repeated exposure
-increasing dosage needed to see same magnitude of biologial effect
cross tolerance: tolerance to one drug an diminish effectiveness of other drugs

44
Q

pharmacogenetics

A

study of genetic basis of variability in drug response amoung individuals
-goal: genetics that affect side effects and predict therpeutic response
-i.e. differences in p450 enzyme genes, recpetors, transporters, signalling cascade proteins
-some people may require different doses

CRP 108 Trial Design and Pharmacology (6 decks)

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