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Toxicology & TDM

The Drugs!

Antibiotics--Aminoglycosides -used to treat infections w/ gram-____ bacteria that are resistant to less toxic antibiotics gram-negative
Types of Aminoglycoside Drugs (x3AGT) Amikacin Gentamicin Tobramycin
Antibiotics--Aminoglycosides: TRUE or FALSE Drugs are very polar & poorly absorbed by the intestines. True
Antibiotics--Aminoglycosides -Distributed in what fluid? -Do they cross the Cell Membrane? -Do they bind to plasma proteins? Distributed in the extracellular fluid but do not cross cell membranes nor do they bond to plasma proteins
Antibiotics--Aminoglycosides -Hours for elimination of half lives 2-3 hours
Antibiotics--Aminoglycosides -Clearance is dependent on... Renal function
Antibiotics--Aminoglycosides -Trough measurements (monitors what?) Trough--monitors Toxicity
Antibiotics--Aminoglycosides -values exceeding trough levels predict what? renal damage
Antibiotics--Aminoglycosides -Peak values are measuring? Therapeutic Levels
Antibiotics--Aminoglycosides -what deactivates gentamicin by creating an inactive complex? Heparin
Glycopeptide Antibiotics--Vancomycin -can damage what? Auditory Nerve & Kidneys
Glycopeptide Antibiotics--Vancomycin -effective against what type of bacteria? Gram-[+] cocci & bacilli
Antiepileptic Drugs -3 first generation drugs (PPV) Phenobarbital Phenytoin (Dilantin) Valproic Acid (Depakene or Depakote)
Antiepileptic Drugs -Phenobarbital is a slow acting barbiturate that effectively controls several types of seizures
Antiepileptic Drugs -Phenytoin (Dilantin) is commonly used for treatment of seizure disorders
Antiepileptic Drugs -Phenytoin (Dilantin) is used short-term in ____ to prevent_____ brain injury to prevent loss of functional tissue
Antiepileptic Drugs -Valproic Acid (Depakene) is used as a ______ for treatment of _____ & _____ seizures used as a monotherapy for treatment of petit mal & absense seizures
Antiepileptic Drugs-Phenobarbital -eliminated how and is dependent on what? Hepatic elimination & age dependent Children 70 hrs, Adults 100 hrs
Antiepileptic Drugs-Phenobarbital -reduced liver function ______ half life increases
Antiepileptic Drugs-Phenobarbital -when should you collect the sample? late in the dose interval (trough preferred)
Antiepileptic Drugs -what is used in the treatment of tonic-clonic and complex-partial seizures? Primidone aka Mysoline
Antiepileptic Drugs -what is the major metabolite of primidone? phenobarbital
Antiepileptic Drugs -what drug is used in the treatment of primary or secondary generalized tonic-clonic seizures? Phenytoin aka Dilantin
Antiepileptic Drugs -what % of phenytoin is protein bound? 90%
Antiepileptic Drugs -what will give higher free drug levels of phenytoin? Hypoalbuminemia
Antiepileptic Drugs-Phenytoin -small dosage increments result in ____ changes in blood concentration large
Antiepileptic Drugs-Phenytoin -how many hours after dose will you see toxic symptoms? 4-5 hrs
Antiepileptic Drugs -which drug is rapidly and almost completely absorbed after oral dose? Valproic Acid aka Depakene or Depakote
Antiepileptic Drugs-Valproic Acid -Half life is variable--dependent on? dosage and age
Antiepileptic Drugs -what % of valproic acid is protein bound? 93% of drug is protein bound
Antiepileptic Drugs-Valproic Acid -more free drug is available in hepatic disease, uremia or altered protein states
Antiepileptic Drugs-Valproic Acid -free drug is influenced by..... other protein bound meds (such as phenytoin)
Antiepileptic Drugs -which drug is used for treatment of tonic-clonic and complex-partial seizures as a last resort? Caramazepine aka Tegretol
Antiepileptic Drugs-Caramazepine -chronic therapy induces _____ which will shorten the half life liver enzymes
Antiepileptic Drugs-Caramazepine -decreased liver functions _____ levels increase
Antiepileptic Drugs-Caramazepine -drug can induce (x3) leukopenia, thrombocytopenia & aplastic anemia
Antiepileptic Drugs-Caramazepine -trough is used to measure therapy unless intoxication is suspected--then measure how many hours after dose? 2-4 hours after oral dose
Antiepileptic Drugs- -which drug is used to manage acute lymphoblastic leukemia in children, choriocarcinoma & trophoblastic tumors in women Methotrexate
Antiepileptic Drugs-Methotrexate -decreases _____ nucleotide synthesis by inhibiting the enzyme _____ reductase decreases pyrimidine nucleotide synthesis by inhibiting the enzyme dihydrofolate reductase
Antiepileptic Drugs-Methotrexate -treatment is followed by _____ to rescue cells from methotrexate inhibition Leucovorin
Antiepileptic Drugs-Methotrexate -what 3 cytotoxic effects can PT develop? Myelosuppression, Gastrointestional mucositis and hepatic cirrohsis
Antiepileptic Drugs-Methotrexate -high dose methotrexate followed by leucovorin rescue is an effective therapy for.... neoplastic conditions
Antipsychotic Drugs -what drug treats manic depression? Lithium
Antipsychotic Drugs-Lithium -values exceeding ____ after 12 hrs indicates risk of intoxication 1.5 meg/L
Antipsychotic Drugs-Lithium -Lithium excretion parallels what? Sodium
Antipsychotic Drugs-Lithium -standard methodology ion-specific electrode or flame emission
Tricyclic Antidepressants -treats (x4) depression insomnia extreme apathy loss of libido
Tricyclic Antidepressants--Name the metabolites of Amitriptyline Doxepin Imipramine Nortriptyline Nordoxepin Desipramine
Tricyclic Antidepressants-methods should address the following -sensitive to concentrations as low as 25 mg/ml
Tricyclic Antidepressants-methods should address the following -distinguish and measure both parent and metabolite
Tricyclic Antidepressants-methods should address the following -discriminate b/t tricyclic & tetracyclinc (many OTC meds)
Bronchodilators -relaxes bronchial smooth muscle to relieve or prevent asthma Theophylline
Bronchodilators-Theophylline -absorption rates: what are the peaks with and without food with 3-5 without 2
Bronchodilators-Theophylline -half lives of children/smokers & normal adults children/smokers 3-4 hrs normal adults 9hrs
Bronchodilators-Theophylline -clearance is _____ dependent dose
Bronchodilators-Theophylline-Clearance -level >20 mg/ml: small increases in dose gives _____ in serum disproportionate increase in serum
Bronchodilators-Theophylline -Optimal levels 15 mg/ml
Bronchodilators-Theophylline -what is a minor metabolite? Caffenine
Cardioactive -what two drugs need to be measure at the same time for cardio issues? Procainamid & N-acetylprocainamide (NAPA)
Cardioactive--NAPA -accumulates in PTs with... impaired renal function
Cardioactive--NAPA + Procainamide -should not exceed ____mg/ml 30 mg/ml
Cardioactive drugs requiring TDM-Cardiac Glycosides -which drug inhibits membrane Na-K-ATPase? Digoxin
Cardioactive drugs requiring TDM-Cardiac Glycosides -Digoxin absorption is variable and influenced by dietary factors GI motility Formulation of drug
Cardioactive drugs requiring TDM-Cardiac Glycosides -Digoxin half life in plasma 38 hrs in average adult
Cardioactive drugs requiring TDM-Cardiac Glycosides -Digoxin is measured by immunoassays to determine total concentration in serum
Cardioactive drugs requiring TDM-Cardiac Glycosides -Digoxin: increased sensitivity seen in (x3) Hypokalemia Hypercalcemia Hypomagnesemia
Cardioactive drugs requiring TDM-Antiarrhytmics -what three types? (QPD) Quinidine Procainamide Disopyramide
Cardioactive drugs requiring TDM-Cardiac Glycosides -Digoxin: peak levels in plasma and tissues plasma: 2-3hrs after ingestion tissues: 6-10 hrs
Cardioactive drugs requiring TDM-Cardiac Glycosides -Digoxin: tissue levels correlate with ___ & ____ values therapeutic and toxic values
Cardioactive drugs requiring TDM-Cardiac Glycosides -Digoxin: what two things may give similar clinical symptoms toxicity & under treatment
Cardiac Drugs -what has a high degree of first-pass hepatic metabolism that results in widely variable bioavailability for individuals? Propranolol (Inderal)
Cardiac Drugs -only given by IM or IV b/c undergoes first pass hepatic metabolism when given orally Lidocaine
Cardiac Drugs-Lidocaine -two metabolites that can be toxic monoethylglycinexylidide (MEGX) glycinexylidide (GX)
Cardiac Drugs-Lidocaine -testing in early therapy for adequate concentration is done _____ min after loading dose 30 min
Cardiac Drugs--Lidocaine -if no loading dose is used, ____hrs after start of therapy 5-7 hrs
Cardiac Drugs-Lidocaine -bound by _____ -increased after_____ & _____ free drug bound by a-acid-glycoprotein increased after MI & reduces free drug
Cardiac Drugs -used to treat rapid & irregular heart beats? Quinidine
Cardiac Drugs-Quinidine -plasma peak reached in how many hrs after oral dose? 1.5-2hrs
Cardiac Drugs-Quinidine -what cross reacts w/ metabolites that gives slightly higher values that GLC? EMIT & FPIA antibodies
Cardiac Drugs-Quinidine -trough specimen usually is used to document what? adequate dosage
Immunosuppressive Drugs -what selectively inhibits proliferation & activation of CD4+ cells? Cyclosporin A
Immunosuppressive Drugs -Cyclosporin A is used to prevent what? graft vs host rejection in organ transplants
Immunosuppressive Drugs -Cyclosporin A inhibits proliferation of lymphocytes while results in.... the suppression of humoral and cellular immunity
Immunosuppressive Drugs-Cyclosporin A -Specimen Requirement - % bound in ____ Whole Blood 90% bound in RBC
Immunosuppressive Drugs-Cyclosporin A -concentration in RBC is _____ dependent in vitro temperature
Immunosuppressive Drugs -what is found in the soil in N.Japan (fungus) FK 506 aka Tacrolimus
Immunosuppressive Drugs -FK506 is _____X more potent than cyclosporin 100x
Immunosuppressive Drugs-FK506 - ____% bound to ____ 99% bound to albumin
Immunosuppressive Drugs-FK506 -what can be caused w/ continual use? renal failure
Immunosuppressive Drugs-FK506 -_____Interference T-Helper Interference
Created by: haley.gooch



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