TDM - THERAPEUTIC DRUG MONITORING Flashcards by CHARLENE SAN JOSE

Typical Effectiveness of Route of Exposure

intravenous > inhalation > intraperitoneal injection
> intramuscular injection > ingestion > topical

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intravenous route of administration is associated with ___ % bioavailability

100

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orally administered drug should achieve % bioavailability

70% 0.7 fraction

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5 pharmacological parameters that determine serum drug concentration

liberation
absorption
distribution
metabolism
excretion

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refers to the release of the drug

liberation

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is the transport of drug from the site of administration to the blood

absorption

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refers to the delivery of the drug to the tissues

distribution

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is the process of chemical modification of the drug by cells

metabolism

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is the process by which the drug and its metabolites are excreted from the body

excretion

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most drugs are absorbed in what way

passive diffusion

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tablets and capsules require dissolution before being absorbed; liquid solutions are rapidly absorbed

true or false

true

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weak acids are absorbed in ___ while weak bases are in ___

stomach; intestine

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the process wherein the drugs are effective in the body tissues, not generally in the blood

distribution

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the relationship between distribution of substances between tissue and blood levels is termed as

distribution space

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the rate at which a particular drug is cleared from the circulation is dependent not only on the type of drug itself, but also on a patient’s capacity to metabolize and excrete it

excretion

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causes of drug toxicity

elevated concentration of free drug
abnormal response to drug after administration
the presence of active drug metabolites

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these drugs are used for treatment of arrhythmias and congestive heart failure

cardioactive drugs

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classification of cardioactive drugs

class I (rapid sodium channel blockers)
class II (beta receptor blockers)
class III (potassium channel blockers)
class IV (calcium channel blockers)

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class 1 cardioactive drugs example

quinidine, procainamide, lidocaine

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class II cardioactive drugs example

PROPANOLOL

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class III cardioactive drugs example

AMIODARONE

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class IV cardioactive drugs example

VERAPAMIL

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is a cardiac glycoside for treatment of atrial arrhythmia and congestive heart failure

digoxin

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digoxin, when taken in large doses it inhibits Na-K-ATPase thus it decreases ___

K and Mg, and increase Ca

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effect of digoxin to hyperthyroid individuals

resistant

toxic effects of digoxin

nausea, vomiting, visual disturbances, premature ventricular contractions, and atrioventricular bode blockage

therapeutic level of digoxin

0.5-2 ng/ml

toxic level of digoxin

> 2 ng/ml

is used to correct ventricular arrhythmia for treatment of acute myocardial infarction

lidocaine (xylocaine)

it is administered by continuous IV infusion after a loading dose

lidocaine (xylocaine )

lidocaine is also known as

xylocaine

cardioactive drugs that can be used as a local anaesthetic

lidocaine(xylocaine)

lidocaine(xylocaine) is can't be administered ___ due to almost complete hepatic removal of the absorbed drug

orally

toxic effect of lidocaine(xylocaine)

congestive heart failure and heart block

toxicity level of lidocaine(xylocaine)

> 4 -8 ug/ml

a naturally occurring drug for the treatment of arrhythmia

quinidine

quinidine is almost ___ protein bound

85%

quinidine's elimination

hepatic metabolism

route of delivery of quinidine

oral administration

quinidine's common formulation

quinidine sulfate and quinidine gluconate

toxic level of quinidine

>5 ug/ml

toxic effects of quinidine

cinchonism, blood dyscrasia, hepatitis

procainamide is also called as

pronestyl

describe the absorption of procainamide(pronestyl) in GIT

rapid and complete

elimination of procainamide(pronestyl)

renal filtration hepatic metabolism

route of delivery of procainamide(pronestyl)

oral

toxic level of procainamide(pronestyl)

> 12 ug/ml

toxic effects of procainamide(pronestyl)

reversible lupus-like syndrome (ANA) nephrotic syndrome urticaria

it is used to treat cardiac arrhythmias and used as a substitute for quinidine

disopyramide

route of disopyramide

orally

describe the absorption of disopyramide in GIT

rapid and complete

elimination of disopyramide

renal filtration

toxic level of disopyramide

10 ug/ml

toxic effects of disopyramide

bradychardia and atrioventricular node blockage

a beta-receptor-blocking drug

propanolol

propanolol is used in the treatment of

angina pectoris, hypertension, and coronary artery disease

propanolol's effect to thyroid hormones

suppresses the conversion of T4 to T3

it is used in the treatment of thyrotoxicosis

propanolol

therapeutic range of propanolol

50-100 ng.ml

toxic effects of propanolol

bradycardia, arterial insufficiency (raynaud's type), platelet disorder, and pharyngitis

amiodarone is also called as

cordarone

it blocks potassium channel in the cardiac muscle

amiodarone (cordarone)

amiodarone (cordarone) is used for treatment of

ventricular arrhythmia

it is an iodine containing drug which can cause hyperthyroidism or hypothyroidism

amiodarone (cordarone)

toxic level of amiodarone (cordarone)

>2.5 ug/ml

toxic effects of amiodarone (cordarone)

bradychardia, hepatitis, photodermatitis, and thyroid dysfunction

is used for treatment of angina, hypertension, and supraventricular arrhythmia

verapamil

therapeutic range of verapamil

80-400 ng/ml

verapamil's toxic effects

hypotension, peripheral edema, and ventricular fibrillation

list down the aminoglycosides antibiotics

gentamicin tobramycin amikacin kanamycin neomycin streptomycin

purpose of aminoglycosides

treatment of gram-negative bacterial infections;

route of aminoglycosides

intramuscular or intravenous

absorption of aminoglycosides in GIT

not well absorbed from the GIT

aminoglycosides can cause damage to which cranial nerve

8th cranial nerve (hearing loss )

aminoglycosides' elimination

renal filtration

toxic effects of aminoglycosides

nephrotoxicity and ototoxicity

toxic levels of amikacin and kanamycin

> 30 ug/ml

toxic levels of gentamicin and tobramycin

12-15 ug/ml

it is the antibiotic and glycopeptide against gram positive cocci and bacilli

vancomycin

vancomycin's route of administration

IV infusion

describe the oral absorption of vancomycin

poor oral absorption

its toxic side effects occur in the therapeutic range (5-10 ug/ml)

vancomycin

elimination of vancomycin

renal filtration and excretion

toxic effects of vancomycin

"red man syndrome" nephrotoxicity ototoxicity

this antibiotic is distributed to all tissues and concentrates in the CSF

chlorampenicol

chlorampenicol is ___% protein bound

50%

describe the GIT absorption of chlorampenicol

rapidly absorbed

toxic level of chlorampenicol

>25 ug/ml

toxic effects of chlorampenicol

blood dyscrasia and cytoplasmic vacuolation (erythroid and myeloid cells )

it is a long-acting barbiturate that controls grand mal tonic-clonic seizure and focal epileptic

phenobarbital

this anti epileptic drug is not used for petit mal seizure

phenobarbital

used for treating withdrawal symptoms in infant whose mothers are addicted to opiate or barbiturate

phenobarbital

an anti epileptic drug that is used to treat cases of congenital hyperbilirubinemia

phenobarbital

majority of phenobarbital taken is stored in

brain

elimination of phenobarbital

hepatic metabolism

therapeutic level of phenobarbital

20-40 ug/ml

toxic effects of phenobarbital

nystagmus stupor ataxia respiratory depression

phenytoin is also called as

phenytoin (dilantin )

it controls tonic clonic and simple partial seizures

phenytoin (dilantin )

phenytoin (dilantin) is not used for what type of seizure

petit mal and atomic seizures

route of phenytoin (dilantin)

intravenous

describe the GIT absorption of phenytoin (dilantin)

incomplete

elimination of phenytoin (dilantin)

hepatic pathway (zero order kinetics )

major toxicity effect of phenytoin (dilantin)

initiation of seizures tetragonic action (cleft lip and palate) nystagmus

therapeutic range of phenytoin (dilantin)

10-20 ug/ml

toxic level of phenytoin (dilantin)

>20 ug/ml

phenytoin (dilantin) 's injectable proform

fosphenytoin

valproic acid is also called as

depakene

used for treatment of petit mal (absence seizure ), atomic, and grand mal seizures

valproic acid (depakene)

valproic acid (depakene)'s route of administration

orally

describe the GIT absorption of valproic acid (depakene)

rapid and complete

valproic acid (depakene) protein bound percentage

93%

why do valproic acid (depakene) needs monit0ring after 6 months of therapy

hepatic dysfunction is observable

valproic acid (depakene)'s elimination

hepatic metabolism

therapeutic level of valproic acid (depakene)

50-100 ug/ml

valproic acid (depakene) toxic level of > 100 ug/ml will cause

nausea lethargy weight gain

valproic acid (depakene) toxic level of > 200 ug/ml will cause

pancreatitis hallucinations hyperammonemia

carbamazepine is also called as

tegretol

a tricyclic compound related to imipramine

carbamazepine (tegretol)

effective for grand mal seizures and for treating seizures accompanied by pain

carbamazepine (tegretol)

route of carbamazepine (tegretol)

orally

elimination of carbamazepine (tegretol)

hepatic metabolism

idiosyncratic effect of carbamazepine (tegretol)

rashes leukopenia nausea vertigo febrile reactions

therapeutic level of carbamazepine (tegretol)

4-16 ug/ml

toxic level of carbamazepine (tegretol)

> 12 ug/ml

toxic effects of carbamazepine (tegretol)

hematologic dyscrasias aplastic anemia irregular pulse ataxia

this antiepileptic drug has antineuralgic action and is 70-805 protein bound

carbamazepine (tegretol)

drug of choice for controlling petit mal (absence of seizure )

ethosuximinde (zarontin)

route of ethosuximinde (zarontin)

orally administered

how many percent is ethosuximinde (zarontin) protein bound?

free in the serum and not protein bound

toxic level of ethosuximinde (zarontin)

> 100 ug/ml

toxic effects of ethosuximinde (zarontin)

GIT disturbances ataxia SLE aplastic anemia pancytopenia

this anti epileptic drug is similar to neurotransmitter gamma aminobutyric acid (GABA)

gabapentin (neurontin)

gabapentin (neurontin) is used in

partial seizures and as an adjunctive therapy

route of gabapentin (neurontin)

orally

percent of gabapentin (neurontin) being bound to protein

not bound to plasma proteins

elimination of gabapentin (neurontin)

unchanged in urine and not metabolized in humans

toxic effects of gabapentin (neurontin)

ataxia and somnolence (drowsiness )

other seizure drugs of interest that is used as an adjunct drug for partial seizures

topiramate lamotrigine (lamictal ) felbamate

psychoactive drug that is used for treatment of manic-depressive illness (bipolar disorders )

lithium

psychoactive drugs that is a drug of choice for the prevention of chronic cluster headache

lithium

effect of psychoactive drugs - lithium, to thyroid hormone

inhibits thyroid hormone synthesis and release, inhibits iodine update causing hypothyroidism

psychoactive drug that is a cationic metal that does not bind to proteins

lithium

lithium's route of administration

orally and absorption is rapid and complete

psychoactive drug that go along with lithium, together, they inhibit the action of ADH on the kidneys

demeclocycline

elimination of lithium

renal filtration

toxic effects of lithium

severe dehydration nephrotoxicity hypothyroidism

toxic effect of lithium if 1.2-2 mmol/l

apathy, lethargy, speech difficulties

toxic effect of lithium if >2 mmol/l

seizures muscle rigidity coma

psychoactive drug that is used for the treatment of depression, insomnia, extreme apathy, and loss of libido

tricyclic antidepressants

route of tricyclic antidepressants

orally administered

example of tricyclic antidepressants

imipramine, amitriptyline, doxepin, nortriptyline, trazadone

elimination of tricyclic antidepressants

hepatic metabolism

toxic effects of tricyclic antidepressants

drowsiness blurred vision memory loss seizure cardiac arrhythmia Parkinsonsian syndrome unconsciousness

this psychoactive drug has the ability to block the re-uptake of serotonin in central serotonergic pathways

fluoxetine (prozac)

this psychoactive drug is used for treatment of obsessive-compulsive disorders

fluoxetine (prozac)

toxic effects of fluoxetine (prozac)

attempted suicide, decreased libido, and sexual function

the only bronchodilator in the book of rodriguez

theophylline

theophylline belongs to the ___ class

methylated xanthine

theophylline its action is specific to the relaxation of ___

bronchial smooth muscle

theophylline is used for the treatment of

asthma and chronic obstructive pulmonary disease

it is therapeutic for primary apnea of prematurity

theophylline

used to treat the absence of respiratory effort in newborn infants

theophylline

effect of theophylline to histamine and proinflammatory agents

inhibitor

route of administration of theophylline

initially administered intravenously then orally

percent of theophylline of protein bound

50%

can theophylline cross placenta?

yes, and teratogenic in pregnant females

theophylline the best predictor of toxicity is the

the blood level of the drug and not the early signs or symptoms of toxicity

elimination of theophylline

renal filtration and hepatic metabolism

toxic level of theophylline

> 20 ug/ml

toxic effects of theophylline

GI bleeding seizures tachycardia syncope

an immunosuppressive drug that inhibits the cellular immune response by clocking production of interleukin 2

cyclosporine

an immunosuppressive drug that is used to prevent the rejection of allogenic organ transplants

cyclosporine

an immunosuppressive drug that is utilized for suppression of acute graft-versus-host disease

cyclosporine

what are the organs that require high dosage of cyclosporine

heart liver pancreas

an immunosuppressive drug that has marked affinity with RBC

cyclosporine

erythrocyte-cyclosporine is ___ dependent

temperature-dependent

cyclosporine's route of administration

orally with 5-50% absorption

elimination of cyclosporine

hepatic metabolism

best sample of cyclosporine determination

whole blood (with lysis of RBC to yield the total amount )

toxic level of cyclosporine

>500 ng/ml

toxic effects of cyclosporine

renal tubular and glomerular dysfunction gi disturbances hirsutism hemotologic dyscrasias

an immunosuppressive drug that is 100x more powerful than cyclosporine

tacrolimus ()

tacrolimus is also known as

tacrolimus (prograf/fk-506)

an immunosuppressive drug that is a macrolide lactone antibiotic

tacrolimus (prograf/fk-506)

tacrolimus (prograf/fk-506) elevated level are observed in

cholestasis

elimination of tacrolimus (prograf/fk-506)

hepatic metabolism

specimen of choice for

whole blood

toxic effects of tacrolimus (prograf/fk-506)

thrombus formation nephrotoxicity neurotoxicity

this immunosuppressive drug is similar to tacrolimus (prograf/fk-506)

rapamycin

rapamycin is also known as

rapamycin (sirolimus)

rapamycin (sirolimus)'s major side effects

lipid abnormalities and thrombocytopenia

other immunosuppressive drug that decreases renal allograft rejection

mycophenolate mofetil

other immunosuppressive drug that inhibits lymphocyte proliferation

leflunomide (LFM)

other immunosuppressive drug that is used for treatment of rheumatoid arthritis

leflunomide (LFM)

the 2 antineoplastic drugs in rodriguez book

methotrexate busulfan

it is an effective therapy for a variety of neoplastic conditions

methotrexate

the antineoplastic drug that works as well as immunosuppressive drug

methotrexate

methotrexate's effect to DNA synthesis

inhibitory in all cells by blocking dihydrofolate reductase

is used to reverse the action of methotrexate

leucovorin

the reversal of action of methotrexate by leucovorin is known as

leucovorin rescue

toxic level of methotrexate

0.01 umol/l

toxic effects of methotrexate

leicopenia GI ulceration thrombocytopenia cirrhosis

is an alkalyting agent used to treat leukemia and lymphomas prior to bone marrow transplantation

busulfan

busulfan's overdosage may cause

hepatic occlusive disease

this is a sub item under inflammatory/analgesics