Pharm exam 1 FINAL REVIEW Flashcards

1
Q

Chiral

A

something that has chiral center that can rotate around center, has mirror image of itself.

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2
Q

Enantiomer

A

2 mirror images

e.g. racemic mixtures, may have both compounds present

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3
Q

Isomer

A

Same chemical formula but different structure

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4
Q

Kd

A

Drug concentration at which 1/2 of receptors are bound

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5
Q

Low k/d = ?

A

High drug/receptor affinity

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6
Q

k/d does not equal?

A

EC50, two different concepts

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7
Q

Receptors can spontaneously

A

shift into active configuration

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8
Q

Tachyphylaxis

A

quick tolerance

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9
Q

Conventional hybridoma technology antibodies

A

Takes cancer protein, inject to mouse, mouse makes antibodies, isolate splenic antibodies, combine with tumor cells, makes the antibodies proliferate.

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10
Q

Purple denotes

A

human

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11
Q

IND, NDA

A

Investigational new drug, new drug application

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12
Q

Receptors can be ___ or _____ the cell

A

inside or outside

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13
Q

Receptors that we dont know what they do

A

orphan receptors

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14
Q

Inert receptors

A

Drug carriers, albumin, don’t transmit signal but they hold drug.

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15
Q

What does Albumin, alpha-1 acid glycoprotein, and lipoproteins bind to

A

Albumin: Acidic
a1-acid: basic
Lipoproteins: neutral drugs

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16
Q

Cell surface receptors

A

Catalytic, ion, GPCRs

17
Q

Intracellular receptors are

A

lipid soluble drugs

18
Q

GPCRs have ______ desensitization and a _______ response.

A

rapid; fast

19
Q

Catalytic cell surface receptor example

A

Tyrosine kinase (TKR)

20
Q

TKRs

A

Two monomers, dimerize, dimer then activates, using 6 ATPs, tyrosines become phosphorylated, interacts with relay proteins to make a response

21
Q

Hydrophobic molecules binding inside the cell membrane

A

NO and steroids

22
Q

Permeation

A

Aqueous diffusion, lipid diffusion, special carriers, endo/exocytosis.

23
Q

Whole blood/plasma volume

A

5.6L/2.8L per 70kg person.

24
Q

Most important factor of therapeutic monitoring is

A

clearance

25
Q

Drugs that do not penetrate fat well, you use

A

IBW

26
Q

Phase 1 reactions

A

take off groups

Oxidation, reduction, hydrolysis, hydrogenation

27
Q

Types of CYP450 (oxidation)

A

3a4 50%, 2D6 20%, 2B6 8%

28
Q

CYP450 pathway

A

-drug binds to p450
- Series of oxidation reduction reactions
-NADPH oxidizes to NADP+
-flavoprotein is reduced/oxidized,
-p450 is reduced, FE3+ to FE2+
-Oxygen binds to CYP450
-oxygen reduced to water
-Drug has hydroxyl group on it
-Drug becomes more water soluble, from lipophilic to hydrophilic+

29
Q

Phase 2 reactions

A

attach larger molecules to drug

e.g. glucuronidation, sulfation, glutathione conjugation, glycine

30
Q

Acetaminophen pathway

A

Glucuronidation, then sulfation if more of it.

if toxic dose ingested, phase 1 reactions come in. Glutathione conjugation can occur to deactive. Toxic reagent nucleophilic binds to proteins in cell and destroys liver cells, leading to liver cell death.

31
Q

how many DNA codes for proteins

A

1-2%

32
Q

Examples of drugs that need adjustments for genetics

A

6-MP: TPMT mutations
Warfarin: CYP2C9, poor or rapid metabolizer
Herceptin: tumor overexpressing HER2, target for herceptin therapy.

33
Q

What % of membrane proteins are carrier proteins

A

15-30%

34
Q

ABC uses

A

ATP

35
Q

SLC21 uses ______ transport

A

passive