Pharm: Heme-Onc

Iron

Drug Class: hematinics

MOA: supplement

Indications: iron deficiency

SE/ADRs: Nausea/vomiting; constipation, diarrhea; abdominal cramps, black stools

Contraindications: anaphylaxis, hemochromatosis, hemolytic anemia

Dx-Dx: Antacids, phenytoin, quinolone and tetracycline antibiotics bind Fe

Monitoring: Serum Ferritin, transferrin saturation, Hgb, reticulocytes

Deferoxamine

Desferal

Drug Class: iron chelators

MOA: Chelates iron from hemosiderin, ferritin, transferrin (not

from hgb or cytochromes

Indications: excess serum iron levels

SE/ADRs: Fever, leg cramps, tachycardia, hypotension (IV), allergic drug reactions, pulmonary syndrome, neurotoxicity

Contraindications: Prior anaphylaxis with drug, renal insufficiency, hemochromatosis

Extra

Monitoring: Hgb, serum iron levels

PG: C

Lactation caution, PO (seldom), IV, IM, SQ, usually IV

NOT FOR HEMOCHROMATOSIS TX

Cyanacobalamin

Drug Class: Vitamin (B12)

MOA: Rate limiting cofactor in converting folate to active form and DNA synthesis

Indications: B12 deficiency (megaloblastic anemia, peripheral neuropathy, depression, CVD)

SE/ADRs: painful by injection site

Dx-Dx: Long term acid suppression therapy, metformin, phenytoin

Monitoring: B12, folate serum concentration, homocysteine, methylmalonic acid levels

Replenishment regimens: IM 1000mcg daily for 1-2 weeks, then 1000mcg weekly, then 1000mcg monthly, PO, 1000mcg daily

Folic Acid

Folacin-800

Drug Class: nutritionals

MOA: cofactor in DNA synthesis

Indications: Folate deficiency (megaloblastic anemia, prevention of neural tube defects, CVD)

SE/ADRs: bronchospasm, flushing, pruritus (rare)

Contraindications: hypersensitivity

Dx-Dx: Phenobarbital, phenytoin, primidone levels decreased by

folate, trimethoprim, methotrexate deplete folate levels

Monitoring: Serum folate levels, RBC folate level, variable dosing 1-5mg daily

Epoetin

Epogin

Drug Class: erythrocyte-stimulating agents

MOA: Stimulates erythroid proliferation and differentiation; induces release of reticulocytes

Indications: Low RBC secondary to ESRD, HIV, antineoplastic therapy, RA

SE/ADRs: Secondary impact on iron deficiency, clotting; HTN, thrombosis, seizures

Extra

Contraindications: Hypersensitivity

Monitoring: reticulocyte count, Hgb, Hct, serum ferritin

Iron stores need to be normalized first, may become hypercoagulable with ESA treatment

Filgrastim

Neupogen

Drug Class: Myeloid-growth factors: G-CSF

MOA: Stimulates proliferation and differentiation of myeloid cells; increases phagocytic capacity and prolongs survival of mature neutrophils, mobilizes peripheral neutrophils

Indications: neutropenia secondary to chemotherapy

SE/ADRs: fever, petechiae, bone pain, splenomegaly

Contraindications: hypersensitivity

Dx-Dx:

Monitoring: CBC

Also GM-CSF (granulocyte-macrophage colony-stimulating factor)

Chloroquine

Aralen

Drug Class: anti-malarial agent

MOA: Chloroquine phosphate binds to and inhibits DNA and RNA polymerase inhibiting growth and nucleoprotein synthesis

Indications: Malaria (acute and suppressive tx); extraintestinal amebiasis

SEs/ADRs: Cardiomyopathy, agitation, anxiety, abdominal cramps, hepatitis

Extra

Contraindications: SDO, psoriasis, porphyria, G6PD deficiency, hearing loss, retinopathy, QT prolongation, cardiomyopathy

Dx-Dx: Substrate of CYP2D6, CYP3A4

Monitoring: Ophthalmic exam baseline and periodically

PG: no category listed

Caution in alcoholism or liver disease, is used in PG due to increased seriousness of malaria in PG

Mefloquine

Lariam

Drug Class: anti-malarial agent

MOA: destroys the asexual forms of P. vivax and P. falciparum

Indications: malaria treatment and prophylaxis

SE/ADRs: chills, dizziness, rash, vomiting, tinnitus

EXTRA

Contraindications: Neuropsychiatric disorder, SDO, QT syndrome, hepatitis

Dx-Dx: substrate of CYP3A4

Monitoring: new neuropsych symptoms

PG: B

Approved FDA medication guide; need to consult CDC website for resistance patterns

Doxycycline

Doryx

Drug Class: Tetracycline Antibiotic/Anti-Malarial/Anti-Parasite

MOA: Interferes with bacterial 30S protein production

Indications: CAP, sinusitis, lyme disease, plague, rickettsiae, rosacea, periodontitis, syphilis, cholera, MRSA

SE/ADRs: photosensitivity, alteration of gut flora, enterocolitis, vaginal or oral candidiasis

Contraindications: Hypersensitivity, severe hepatic disease

Dx-Dx: Vit K antagonist levels increase – get more anticoagulation

Monitoring: BUN, CrCl- prolonged use only

PG: unknown

80% excreted in feces, 20% renally, not food dependent but milk/antacids interfere, once daily dosing, PO/IV minocycline, PG unknown but not give to nursing

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Artemether-Lumefantine

Coartem

Drug Class: Anti-Malarial/Artemisinin-based Combination Therapy (ACT)

MOA: inhibition of nucleic acid and protein synthesis

Indications: Treatment of acute, uncomplicated P. falciparum malaria including chloroquine resistant malaria

SE/ADRs: Palpitation, headache, sleep disorders, anorexia, weakness, arthralgia, fever

EXTRA

Contraindications: STRONG CYP3A4 INDUCER (rifampin, phenytoin, carbamazepine, St. John’s wort); QT prolongation; hepatic disease

Dx-Dx: strong CYP3A4 inducers

Monitoring: adequacy of food consumption, ECG

PG: C; AVOID FIRST TRIMESTER

Not for severe or complicated malaria, or for prophylaxis; administer with full meal for bestabsorption

Atovaquone

Mepron

Drug Class: antiprotazoal

MOA: Inhibits electron transport in mitochondria which inhibits key metabolic processes responsible for synthesis of nucleic acids and ATP

Indications: Pneymocystis jirovecii pneumonia, Offlabel Babeosis, toxoplasmosis gondii encephalitis

SE/ADRs: Skin rash, diarrhea, cough, fever

Contraindications: hypersensitivity

Dx-Dx: HIV drugs

Monitoring: LFP, vomiting, diarrhea, clinical improvement

PG: C

Take with a fatty meal; fecal excretion; enterohepatic circulation, t1/2 = 2.2-2.9 days; liquid preparation

Azithromycin

Zithromax

Drug Class: macrolide

MOA: Reversibly bind to 50S subunit of bacterial ribosome and

inhibit protein synthesis

Indications: Penicillin substitute, atypical pneumonia, CAP, chlamydia, PID, AOM, sinusitis, pharyngitis, acute bacterial exacerbations of COPD, pertussis

SE/ADRs: hypersensitivity, minimal N/V/D

Contraindications: hypersensitivity, pre-existing liver disease

Dx-Dx: Vit K antagonists – more anticoagulant Warfarin

Monitoring: symptom response

PG: B

DOES NOT INHIBIT CYP3A4, first line drug, Penetrates most tissues (concentration 10-100 times more than in serum) but not CSF with long T1/2 in tissues, food increases absorption of suspension form (important for pediatric pts), primarily biliary elimination, possible QT prolongation (consider with elder patients with a-fib)

Rifampin

Rifadin

Drug Class: miscellaneous antibiotic/anti-tubercular

MOA: inhibits bacterial RNA synthesis by blocking RNA transcription

Indications: Tuberculosis (in combo with other agents); meningococcal meningitis prophylaxis only; off label anaplasmosis

SE/ADRs: Skin rash, hepatitis, abdominal cramps, flu-like syndrome, thrombocytopenia, leukopenia, anemia

Contraindications: hepatic disorders, alcoholism, diabetes, porphyria

Dx-Dx: Strong CYP3A4, Pgp inducer

Monitoring: Liver function, CBC, mental status, sputum C&S, CXR

PG: C

Dose reduction in renal disease

Quinine

Qualaquin

Drug Class: antimalarial agent

MOA: Depresses oxygen uptake and carbohydrate metabolism; intercalates into DNA, disrupting the parasite’s replication and transcription

Indications: In combination with treatment of chloroquine resistant P. falciparum, P. vivax; off-label treatment for babeosis

SE/ADRs: Arrhythmias, tinnitus, altered mentation, rashes, loss of vision, hypoglycemia

EXTRA

Contraindications: Severe hepatic

disease, long QT,

G6PD deficiency,

optic neuritis,

myasthenia gravis

Dx-Dx: substrate of CYP3A4, Pgp

Monitoring: CBC with platelets, liver function, serum glucose, ECG, ophthalmologic follow up

PG: C

FDA approved medication guide

Clindamycin

Cleocin

Drug Class: lincosamide antibiotic

MOA: Reversibly bind to 50S subunit of bacterial ribosome and inhibit protein synthesis

Indications: Strep, Staph, pneumococci, MRSAca +/-, dental prophylaxis for endocarditis, bacterial vaginosis, dog bite wounds, severe acne, TSS, B. fragilis infections; lung abscess

SE/ADRs: Rashes, neutropenia, impairment of liver function, c. difficile colitis

Contraindications: severe liver disease

Dx-Dx: erythromycin

Monitoring: symptom release

PG: B

Resistance to macrolides can be cross-resistant to clindamycin dependent on mechanism

Ceftriaxone

Rocephen

Drug Class: cephalosporin antibiotics/antiparasitic agent

MOA: Interferes with transpeptidation of bacterial cell wall by binding to PBP

Indications: G+, more G- coverage (citerobactor, s marcescens, Providencia); acute otitis media, sinusitis, LRTI, meningitis, empiric tx serious infections pending C&S

SE/ADRs: Eosinophilia; w/ prolonged use bacterial or fungal superinfection, od neuromuscular hypersensitivity, seizures

Contraindications: Hypersensitivity to cephalosporin, anaphylaxis to penicillin

Dx-Dx: Increased PT/INR with warfarin, may precipitate with Ca containing solutions

Monitoring: PT/INR with Warfarin

PG: B

Primarily biliary tract clearance, t ½ = 7-8 hours, can dose once daily (or twice daily for serious infections); Enterobacter resistance emerges rapidly

Cefuroxime Axetil

Ceftin

Drug Class: cephalosporin antibiotic/antiparasitic agent

MOA: Interferes with transpeptidation of bacterial cell wall by binding to PBP

Indications: G+ and anaerobes, some G- (not enterococci or pseudomonas), b-lactamase producers (H influenza, M Catarrhalis), acute otitis media, sinusitis, CAP, #3DoC for Lyme disease

SE/ADRs: Od neuromuscular hypersensitivity, od seizures

Contraindications: Hypersensitivity to cephalosporins, anaphylaxis to penicillin

Dx-Dx: Increased

PT/INR with

warfarin,

aminoglycosides—> nephrotoxicity

Monitoring: CrCl prolonged use

PG: B

Adjust dose for CKD; administer PO/IV/IM

Cannot substitute on a mg-mg basis for suspension and filmcoated tablets

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