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FM1 > Pharm Block 2 Kinetics > Flashcards

Pharm Block 2 Kinetics Flashcards

1
Q

Prednisone

A

PO doses from 5-100mg QD

Metabolized in the liver to prednisolone

t 1/2 ~ 18-36 hr

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2
Q

Cyclosporine

A

PO or IV for immunosuppression at 2.5-15 mg/kg QD; narrow therapeutic window

Opthalmic formulation 0.05% or 0.1% is used to increase tear production that has been suppressed by inflammation

CYP3A4 (drug interactions!); metabolites excreted in bile

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3
Q

Tacrolimus

A

IV or PO; PO absorption is highly variable (needs individualized regimens)

Extensively metabolized by CYP3A4 (drug interactions!)
Metabolites excreted in bile

Concentrated in the pancreas and may INHIBIT PANCREATIC INSULIN SECRETION

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4
Q

Sirolimus

A

Solution or tablets for PO administration (2-5 mg QD)

Cypher is a sirolimus-eluting stent used to inhibit restenosis after stenting to treat coronary artery occlusion; 80% of sirolimus is released in 30 days and the rest in 90 days

CYP3A4 substrate (drug interactions!)
Metabolites excreted in bile

Long t 1/2 - 60 hrs

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5
Q

Azathioprine

A

PO or IV, good oral absorption
Maintenance does is 1-3 mg/kg QD

6-MP is inactivated by oxidation (by xanthine oxidase) and methylation (by thiopurine S-methyltransferase)

Excretion is mostly renal

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6
Q

Mycophenolate mofetil

A

PO or IV; both routes offer essentially complete bioavailability of mycophenolic acid

Usual dose is 1g BID for kidney and liver transplants, 1.5 g BID for heart transplants

Inactive phenolic glucuronide is main metabolite; excreted almost entirely in urine

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7
Q

Muromonab-CD3

A

1 mg/mL solution for IV bolus administration

Usual does is 5 mg QD for 10-14 days

T cells begin to disappear from blood within minutes and reappear 1 week after therapy is halted

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8
Q

Basiliximab

A

Lyophilized powder that is reconstituted for IV administration

20 mg given IV as bolus injection or infusion over 20-30 min
First 20 mg dose given 2 hr prior to surgery
Second 20 mg dose is given 4 days after transplantation
Elimination half-life is 7 days; normal T cell numbers return in 7-14 days

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9
Q

Adalimumab

A

Prefilled syringes containing 20 or 40 mg for SC injection

Maintenance dose is 40 mg Q 2 weeks

Elimination half-life is 10-20 days (mean 14 days)

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10
Q

Carbachol

A

0.01% solution that is instilled into anterior chamber of the eye

Miosis is maximal 2-5 min after administration

Not susceptible to AChE inactivation

Duration of miosis - 24 hrs

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11
Q

Methacholine

A

Lyophilized powder is reconstituted in isotonic saline for inhalation via nebulizer

3-fold more resistant to AChE than acetylcholine

Most subjects return to baseline pulmonary function after 30-45 min

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12
Q

Bethanechol

A

PO tablets 10-50 mg TID-QID

Onset occurs 60-90 min and duration is 60 min

Not susceptible to AChE inactivation

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13
Q

Pilocarpine

A

0.5-6% opthalmic solution, duration 4-14 hrs
PO dose 5-10 mg TID, 3-5 hr duration

Ocusert delivers pilocarpine for 7 days via contact lens-like system

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14
Q

Nicotine

A

Gum, lozenge, inhaler, nasal spray, transdermal patch

Widely distributed in body tissues, especially CNS

Mostly metabolized in liver; unchanged nicotine and metabolites are excreted by kidney

t 1/2 = 30-120 min

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15
Q

Varenicline

A

0 .5 mg and 1 mg tablets for PO, usually 1 mg BID after 1 week ramp-up

Peak plasma concentration reached in 3-4 hr; half-life = 24 hr

Minimal metabolism, 92% is excreted unchanged in urine

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16
Q

Physostigmine

A

0.1% solution via IV injection or applied topically to eye

Duration of action 1-2 hr when given IV, 12-36 hr on eye

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17
Q

Neostigmine

A

15 mg tablets for PO
Average dose is 10 tabs QD with individualized dosing interval

Duration of action 2-4 hr

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18
Q

Edrophonium

A

IV or IM

Duration of action ranges from 5-10 min (IV) and 5-30 min (IM)

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19
Q

Echothiophate

A

0.03% topical opthalmic solution, 1 qtt QD-BID

Membrane penetration is poor due to high polarity

Duration of action = 100hr

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20
Q

Pralidoxime

A

1-2g IV, PO, IM
Infuse in 100mL of saline given over 15-30 min with additional doses PRN

Distributes throughout extracellular water

Metabolized by liver with half-life of 74-77 min

Both unchanged drug and metabolite are excreted by kidneys

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21
Q

Atropine

A

PO tabs or IV, IM or SC solution

0.5-1 mg as antisialagogue, 2-3mg for AChE inhibitor or muscarinic agonist poisoning

Well absorbed, widely distributed throughout body

Metabolized in liver
t 1/2 = 2-4 hr
Excreted renally

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22
Q

Oxybutynin

A

Topically (transdermal patch) or PO (5mg BID-TID)

Widely distributed to body tissues

Onset within 30-60 min of PO, duration 6-10 hrs

CYP3A4 (enteric and hepatic)

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23
Q

Ipratropium

A

Oral inhalation or 0.03% nasal spray
Effect lasts 4-6 hrs

Quaternary amine, doesn’t cross BBB very well

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24
Q

Mecamylamine

A

PO as 2.5 mg tablets, daily dose 2.5-25mg given TID or QID

Almost completely absorbed and excreted unchanged in urine

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25
Q

Epinephrine

A

IV or intracardiac injection, inhalation, topically to eye

Poor PO availability; metabolized by COMT and MAO in liver and other tissues

Duration varies, generally 1-4 hrs

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26
Q

Phenylephrine

A

Injection, PO, intranasally, opthalmically

Metabolized by MAO in liver and other tissues

Active for 30 min to 4 hr

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27
Q

Clonidine

A

Epidurally, PO, transdermal patch

PO bioavailability near 100%

Highly lipid soluble, distributes widely throughout the tissues including CNS

Antihypertensive effects last up to 8hrs (PO) and up to 7 days with transdermal patch

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28
Q

Isoproterenol

A

For cardiac arrests, IV infusion or IV bolus
For bronchodilation, aerosol

COMT metabolism

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29
Q

Dobutamine

A

Continuous IV for

30
Q

Albuterol

A

Oral inhilation
Bronchodilation occurs within 7 min; peaks 0.5-2 hrs, lasts 2-6 hr

Liver metabolism

Excretion through urine and feces

31
Q

Salmeterol

A

Oral inhalation with BID dosing

Therapeutic effects in 14 min, peak effects 3-4 hr, effects last 12 hr

Excretion in feces

32
Q

Phentolamine

A

Lyophilized powder that is reconstituted in NS and used immediately

IV for BP control or SC as multiple injections for necrosis prevention

t 1/2 19 min

33
Q

Phenoxybenzamine

A

Oral absorption is variable, 20-30%

Distribution is extensive because of high lipophilicity and may accumulate in fatty tissues

Can last up to 7 days after discontinuation

Given days before surgery

34
Q

Prazosin

A

2-5mg TID

Antihypertensive effects peak at 2-4 hr, but complete antihypertensive effects may not occur for 4-6 weeks

Metabolized in liver by demethylation and conjugation (majority eliminated via biliary excretion in feces)

35
Q

Tamsulosin

A

Long-acting, dosing 0.4-0.8mg QD

Food decreases peak plasma concentration and bioavailability ~30%

Protein binding is 94-99% by alpha1-glycoprotein

Metabolized in liver by CYP3A4 and CYP2D6

36
Q

Yohimbine

A

PO

Bioavailability is highly variable, 7-87%

1% of unchanged drug is excreted renally

t1/2 = 36 min

37
Q

Carvedilol

A

PO, 6.25-25mg BID, take with food to reduce incidence of orthostatic hypotension

Extensively metabolized by CYP2D6 and CYP2C9

38
Q

Propranolol

A

PO or IV, highly lipophilic, widely distributed

Extensively metabolized upon first pass through liver
Metabolites excreted renally

39
Q

Timolol

A

0.25-0.5% gel-forming opthalmic solution; 1 gtt QD

Some systemic absorption

Partially metabolized by liver; metabolites and parent drug are excreted renally

40
Q

Metoprolol

A

100-450mg PO QD

Quickly absorbed but bioavailability of 0.5 because of first-pass metabolism

Moderately lipid-soluble; widely distributed

Liver CYP2D6; t1/2 = 3-4 hr

Excretion mainly thru kidney as metabolites; 5% unchanged

41
Q

Pindolol

A

5-30mg PO BID

Rapidly absorbed, little or no first pass effect

35-40% excreted unchanged in urine and 60-65% metabolized into hydroxy-metabolites (excreted as glucuronides and sulfates)

42
Q

Alpha-Methyltyrosine

A

250mg PO QID

BP decreases progressively for first 2 days of therapy; after withdrawal BP increases gradually to pretreatment values within 2-3 days

Well-absorbed and 69% is excreted in urine unchanged

43
Q

Alpha-Methyldopa

A

PO 500-2000mg QD-BID

Peak effects in 4-6 hr; duration 24 hrs

44
Q

Reserpine

A

Absorbed rapidly from GI tract following oral administration
Hypotensive effects not observed for 2-3 weeks

Widely distributed, completely metabolized in liver to inactive compounds

Antihypertensive effects can last for weeks following DC of therapy

45
Q

Botulinum Toxin A

A

IM or intradermally for local effect

Onset 2 days, duration 3-4 months

46
Q

Amphetamine

A

PO, 10-30mg OM, immediate or extended

CYPS and MAO, excreted in urine

Excretion is highly sensitive to urine pH

47
Q

Cocaine

A

Topically

Onset within 1 min, peak effect in 5 min, duration 20-60 min

48
Q

Paroxetine

A

PO, 20-50mg QD

Well-absorbed from gut, food has no effect on absorption

Metabolism in liver CYP2D6 and CYP3A4 and conjugation with glucuronic acid or sulfate, only 2% unchanged

Excretion via urine and feces

Onset 1-4 weeks

49
Q

Atomoxetine

A

PO, 0.5-1.2 mg/kg QD, increased over days or weeks

Extensive hepatic metabolism CYP2D6,

50
Q

Phenelzine

A

PO, 20-30mg TID

Well absorbed in gut

Plasma half-life is short and unrelated to duration of enzyme inhibition, which is prolonged

Onset of antidepressant action can take anywhere from 1-8 weeks

51
Q

Cyclophosphamide

A

PO or IV

Oral F= 0.87-0.96

Metabolized by CYPs, 10-20% excreted in urine unchanged

t1/2 = 3-12 hrs

52
Q

Temozolomide

A

PO or IV

Initial TX is daily for 42 days w/ concomitant focal radiotherapy
Maintenance phase is a dose for 5 days then 23 days with no drug (6 cycles)

Crosses BBB (used mainly for brain caners)

53
Q

Carboplatin

A

IV infusion over 15 min, once every 21-28 days x 6 cycles

Mostly eliminated by renal excretion within 24 hr unchanged

54
Q

Bleomycin

A

IV, IM, SC, or instilled in bladder for local TX of bladder cancer

Excreted primarily by kidneys

55
Q

Doxorubicin

A

IV as single injection Q 21-28 days

Distributes throughout body and extensively binds DNA with levels proportional to DNA content of tissue

Obesity can decrease clearance by 35%

56
Q

5-Fluorouracil

A

IV (low and inconsistent oral F)

5-FU metabolizes by dihydropyrimidine dehydrogenase in liver, mucosa, tumor cells

57
Q

Gemcitabine

A

IV over 30 min

21-28 day cycle. Doses given on days 1, 8, 15

t1/2 = 15 min

58
Q

Methotrexate

A

PO or IV

Renal excretion; glomerular filtration and active tubular secretion

59
Q

Vincristine

A

IV or weekly or longer intervals

Elimination half-life = 23-85 hrs

60
Q

Paclitaxel

A

IV (high rate of hypersensitivity rxns)

Extensive hepatic metabolism by CYP2C8, CYP3A4

70-80% dose eliminated in feces in 1 week

61
Q

Etoposide

A

IV

97% bound to serum albumin, toxicity correlates to hepatic health

56% excreted in urine, 44% excreted in feces after 5 days

62
Q

Irinotecan

A

IV infusion

Metabolized by hepatic CYPs that are induced by antiseizure drug

63
Q

Bevacizumab

A

IV

t1/2 = 20 days

64
Q

Cetuximab

A

IV

t1/2 = 7.5 days

65
Q

Rituximab

A

IV usually given 4-8 weeks

Time of onset = 50 days
Duration of response = 10-12 months

After completion of TX, can be detected in patient’s serum for 3-6 months

66
Q

Trastuzumab

A

IV for 12-18 weeks

t1/2 = 6-16 days

67
Q

Temsirolimus

A

25mg diluted and given by weekly IV

Metabolized to sirolimus by CYP3A4
Eliminated in feces

Temsirolimus t1/2 = 30 hr
Sirolimus t 1/2 = 60 hr

68
Q

Erlotinib

A

PO

Hepatic CYP3A4
Eliminated in feces

t 1/2 = 36 hr

69
Q

Imatinib

A

PO

Hepatic CYP3A4

Single dose of ketoconazole increases maximal concentration in plasma

t 1/2 imatinib and major metabolite N-desmethyl derivative = 18, 40 hrs respectively

70
Q

Sunitinib

A

PO for 4 weeks followed by 2 weeks without drug

Hepatic CYP3A4

FM1 (6 decks)

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