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STEP 1 Pharm > Pharm Basics > Flashcards

Pharm Basics Flashcards

1
Q

Km

A

The concentration at which the reaction is half of maximum. Lower the Km, the higher the affinity.

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2
Q

Michaelis-Menten Equation

A

Vmax*S/Km+S

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3
Q

Michaelis-Menten Equation

A

Vmax*S/Km+S

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4
Q

Lineweaver Burk Plot

A

Plots against 1/V and 1/s

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5
Q

X intercept on lineweaver burk?

A

-1/Km. The further to the right (closer to zero), the lower the affinity

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6
Q

Y intercept on lineweaver burk

A

1/Vmax.

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7
Q

Slope on lineweaver burk

A

Km/Vmax

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8
Q

Slope on lineweaver burk

A

Km/Vmax

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9
Q

Characteristics of a reversible competitive inhibitor

A

Resemble substate, overcome by increasing S, bind active site, DO NOT CHANGE VMAX, increase Km.

Decrease potency of an enzyme

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10
Q

Characteristics of an irreversible competitive inhibitor

A

Resemble substate, not overcome by increasing S, bind active site, decrease Vmax, don’t change Km.

Decrease efficacy of an enzyme

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11
Q

Characteristics of an irreversible competitive inhibitor

A

Resemble substate, not overcome by increasing S, bind active site, decrease Vmax, don’t change Km.

Decrease efficacy of an enzyme

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12
Q

Noncompetitive inhibitor characteristics

A

Don’t resemble substrate, not overcome by increasing S, don’t bind active site,

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13
Q

Bioavailability

A

Fraction of administered drug that reaches systemic circulation unchanged. IV dose, F=100. For oral dose, F

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14
Q

Volume of distribution equation

A

Amount of drug in the body/plasma drug concentration

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15
Q

Drugs with low Vd

A

Remain mostly in blood, these include large/charged molecules

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16
Q

Drugs with medium Vd

A

Mostly in EFC. Include small hydrophilic molecules

17
Q

Drugs with large Vd

A

Mostly in tissues including fat. Small lipophilic molecules especially if bound to tissue protein

18
Q

Half-life equation

A

(0.693 x Vd)/CL

19
Q

How many half-lives does it take to reach steady state?

A

3.3 to reach 90%. 4 or 5 to reach full steady state.

20
Q

Clearance equation

A

Rate of elimination of the drug/plasma drug concentration.

VdXke (elimination constant)

21
Q

Loading dose

A

(Cp X Vd)/ F

Cp is target plasma concentration

22
Q

Maintenance dose

A

(CpXCLxt)/F

23
Q

Zero order elimination

A

Rate of elimination is constant and not based on the amount of drug in the body. Includes Phenytoin, ethanol, aspirin (at high doses)

24
Q

First order elimination

A

Rate of elimination is directly proportional to the drug concentration. There is a constant fraction of drug eliminated per unit time.

This is flow-dependent elimination

25
Q

Weak acids

A

Treat overdose with bicarbonate, because are ionized in basic environment.

Phenobarbital, methotrexate, aspirin

26
Q

Weak bases

A

Trapped in acidic environments, treat overdose with ammonium chloride.

27
Q

Weak bases

A

Trapped in acidic environments, treat overdose with ammonium chloride.

28
Q

Phase 1 metabolism

A

Oxidation/reduction/hydrolysis (usually cyp450)

29
Q

Phase 2 metabolism

A

Glucuronidation, acetylation, sulftation. Yields very polar, inactive metabolites that are renally excreted.

30
Q

Phase 2 metabolism

A

Glucuronidation, acetylation, sulftation. Yields very polar, inactive metabolites that are renally excreted.

31
Q

Efficacy of a drug

A

The maximal effect a drug can produce.

High efficacy drugs include analgesics, antibiotics, antihistamines, and decongestants.

32
Q

Potency of a drug

A

The amount of drug needed for a given effect. Increased affinity for receptors.

Include chemotherapeutics, antihypertensives, and cholesterol drugs

33
Q

Competitive antagonist effect on curve

A

Shifts to the right, decreases the potency. Flumazenil (on gaba)

34
Q

Noncompetitive antagonist/irreversible competitive antagonist effect on curve

A

Shifts it down. Prevents maximal effect. (ketamine is noncompetitive, phenoxybenzamine is irreversible competitive on alpha receptors

35
Q

Therapeutic index

A

A measurement of drug safety.

TD50/ED50 = median toxic dose/ median effective dose.

Safe drugs have high TIs.

Low TI drugs include theophylline, digoxin, lithium

36
Q 
Receptor and g protein class
A1
A2
B1
B2
M1
M2
M3
D1
D2
H1
H2
V1
V2
A 
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s
s
q
i
q
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i
q
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STEP 1 Pharm (17 decks)

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