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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
Epinephrine
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
26
Phenylephrine
Injection, PO, intranasally, opthalmically Metabolized by MAO in liver and other tissues Active for 30 min to 4 hr
27
Clonidine
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
28
Isoproterenol
For cardiac arrests, IV infusion or IV bolus For bronchodilation, aerosol COMT metabolism
29
Dobutamine
Continuous IV for
30
Albuterol
Oral inhilation Bronchodilation occurs within 7 min; peaks 0.5-2 hrs, lasts 2-6 hr Liver metabolism Excretion through urine and feces
31
Salmeterol
Oral inhalation with BID dosing Therapeutic effects in 14 min, peak effects 3-4 hr, effects last 12 hr Excretion in feces
32
Phentolamine
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
Phenoxybenzamine
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
Prazosin
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
Tamsulosin
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
Yohimbine
PO Bioavailability is highly variable, 7-87% 1% of unchanged drug is excreted renally t1/2 = 36 min
37
Carvedilol
PO, 6.25-25mg BID, take with food to reduce incidence of orthostatic hypotension Extensively metabolized by CYP2D6 and CYP2C9
38
Propranolol
PO or IV, highly lipophilic, widely distributed Extensively metabolized upon first pass through liver Metabolites excreted renally
39
Timolol
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
Metoprolol
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
Pindolol
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
Alpha-Methyltyrosine
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
Alpha-Methyldopa
PO 500-2000mg QD-BID Peak effects in 4-6 hr; duration 24 hrs
44
Reserpine
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
Botulinum Toxin A
IM or intradermally for local effect Onset 2 days, duration 3-4 months
46
Amphetamine
PO, 10-30mg OM, immediate or extended CYPS and MAO, excreted in urine Excretion is highly sensitive to urine pH
47
Cocaine
Topically Onset within 1 min, peak effect in 5 min, duration 20-60 min
48
Paroxetine
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
Atomoxetine
PO, 0.5-1.2 mg/kg QD, increased over days or weeks Extensive hepatic metabolism CYP2D6,
50
Phenelzine
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
Cyclophosphamide
PO or IV Oral F= 0.87-0.96 Metabolized by CYPs, 10-20% excreted in urine unchanged t1/2 = 3-12 hrs
52
Temozolomide
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
Carboplatin
IV infusion over 15 min, once every 21-28 days x 6 cycles Mostly eliminated by renal excretion within 24 hr unchanged
54
Bleomycin
IV, IM, SC, or instilled in bladder for local TX of bladder cancer Excreted primarily by kidneys
55
Doxorubicin
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
5-Fluorouracil
IV (low and inconsistent oral F) 5-FU metabolizes by dihydropyrimidine dehydrogenase in liver, mucosa, tumor cells
57
Gemcitabine
IV over 30 min 21-28 day cycle. Doses given on days 1, 8, 15 t1/2 = 15 min
58
Methotrexate
PO or IV Renal excretion; glomerular filtration and active tubular secretion
59
Vincristine
IV or weekly or longer intervals Elimination half-life = 23-85 hrs
60
Paclitaxel
IV (high rate of hypersensitivity rxns) Extensive hepatic metabolism by CYP2C8, CYP3A4 70-80% dose eliminated in feces in 1 week
61
Etoposide
IV 97% bound to serum albumin, toxicity correlates to hepatic health 56% excreted in urine, 44% excreted in feces after 5 days
62
Irinotecan
IV infusion Metabolized by hepatic CYPs that are induced by antiseizure drug
63
Bevacizumab
IV t1/2 = 20 days
64
Cetuximab
IV t1/2 = 7.5 days
65
Rituximab
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
Trastuzumab
IV for 12-18 weeks t1/2 = 6-16 days
67
Temsirolimus
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
Erlotinib
PO Hepatic CYP3A4 Eliminated in feces t 1/2 = 36 hr
69
Imatinib
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
Sunitinib
PO for 4 weeks followed by 2 weeks without drug Hepatic CYP3A4

FM1 (6 decks)

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