Kaplan Chapter 1 Flashcards

1
Q

Name some popular weak acid drugs to remember?

A
  1. aspirin
  2. loops
  3. thiazides
  4. warfarin
  5. pens
  6. many “ate” drugs like valproate
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2
Q

Name some popular drugs that are considered weak bases?

A

Many of the easily abused drugs
1. local anesthetics (cocaine)
2. amphetamines (methamphetamine)
3. PCP
4. morphine
5. narcotics (ex: codeine)

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3
Q

What is the indication for warfarin usually?

A

anti-coagulant

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4
Q

What are some factors that make a drug safer for pregnancy?

A
  1. large
  2. water soluble
  3. highly protein bound
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5
Q

What is the calculation for Volume of distribution?

A

Vd = (amount of drug injected)/(blood concentration extrapolated at t = 0)

Vd= dose/C0

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6
Q

When is Vd low?

A

when bound to plasma protein

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7
Q

When is Vd high?

A

When sequestered in tissue

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8
Q

Give typical plasma volume?

A

3L

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9
Q

Give typical blood V?

A

5L

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10
Q

Give typical extracellular fluid volume?

A

ECF = 12-14 L

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11
Q

Give typical TBW volume?

A

40-42 L

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12
Q

Give common CYP inducers and pneumonic to remember 3 of them.

A

rifampin
St. John’s Wort
carbamazepine
phenytoin

St. John Rifin in the Car

or Chronic Smoker and Chronic Drinking in Barbs Car Ruins Passengers Seats

Chronic smoking
chronic drinking
Barbituates
Carbamazepines
Rifampin (antibiotic)
Phenytoin
St. Johns Wort

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13
Q

Give the most common CYP 450 inhibitors and best pneumonic to remember them.

A

ketoconazole
amiodarone
cimetidine
macrolides (especially erythromycin)
grapefruit juice
omeprazole

Ami’s COKE and Grapefruit juice

or AA CCOKE and Grapefruit Juice w/ Pie

acute alcohol
Amiodarone
Cimetidine
Chloramphenicol/ciprofloxacin as well
Omeprazole
Ketoconazole (azoles/ antimicrobials)
Erythromycin (macrolide/antimicrobials)
Grapefruit Juice
Protease Inhibitor: Ritonavir, indinavir etc.

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14
Q

Give the 3 macrolides azithromycin, erythromycin, and clarithromycin in order of least to greatest P450 inhibitor effect?

A

Remember alphabetical order.
1. azithromycin
2. clarithromycin
3. erythromycin

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15
Q

Suffix to remember macrolides?

A

“thromycin”

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16
Q

Name substances that can acidify urine?

A

NH4Cl (ammonium chloride), Vit. C, cranberry juice

17
Q

Name substances that can alkalinize urine?

A

NaHCO3, acetazolamide

18
Q

What are some drugs that at high doses exhibit zero order kinetics?

A

Zero PEAs

phenytoin
ethanol
salicylate acid (aspirin)

Zero WATT Power

W = warfarin
A = alcohol and aspirin
T = tolbutamide
T = theophylline
P = Phenytoin

19
Q

Formula for volume of distribution.

A

Vd =dose/C0

C0 = conc. at time 0

20
Q

Formula for half-life.

A

t1/2 = 0.7 x (Vd / Cl)

21
Q

Loading dose formula?

A

LD = (Vd x Cp)/f

Cp; concentration in plasma

22
Q

Maintenance dose formula?

A

MD = Cl x Css x † /f

t (tau): dosing interval

23
Q

Infusion rate formula?

A

k0 = Cl x Css

24
Q

Most common class CYPP450 drugs are metabolized?

A

3A4

25
Q

Phase I Metabolism examples?

A

cytochrome P450, MAO, alcohol metabolism

26
Q

What usually takes place in Phase I metabolism?

A

drug goes through either oxidation, reduction, or hydrolysis rxns

27
Q

What usually takes place in Phase II Metabolism?

A

conjugation

28
Q

What are examples of Phase II Metabolism?

A

glucuronidation, acetylation, glutathione

29
Q

Drugs that cause drug induced SLE because of genetic variability in acetylation of the body? (slow acetylators)?

A

hydralazine
procainamide
isoniazid (INH)

SHIPP

sulfasalazine
hydralazine
isoniazid (INH)
procainamide
penicillamine

30
Q

What drug can induce glucuronyl transferase to distinguish Crigler-Najjar Type 1 and Crigler-Najjar Type 2

A

barbituates (ex: phenobarbital)

31
Q

What enzyme is needed to cause Phase II metabolism?

A

transferases

32
Q

What is phase 1 biotransformation?

A

modification of drug molecule via oxidation, reduction, or hydorlysis

33
Q

Describe the process of microsomal metabolism.

A

Usually done by oxidation reactions

Major enzyme systems are involved CYP450 which are localized in SER of cells mostly in liver but can also be found in GI tract, lungs, and kidney.

34
Q

Examples of non microsomal metabolism in Phase I biotransformation?

A

hydrolysis, MAO, alcohol metabolism

35
Q

Describe hydrolysis in non microsomal metabolism?

A

phase I reaction involving addition of water molecule with subsequent bond breakage and includes esterases (pseudocholinesterase) and amidases

36
Q

Glucuronidation requires what major enzyme for conjugation?

A

glucuronyltransferase