ABIRATERONE (ZYTIGA)
USES: *Castrate-resistant metastatic PCa*
ACTIONS: CYP17 inhibitor;↓ testosterone precursors.
DOSE: 1,000 mg PO qd w/ 5 mg prednisone BID; w/o food 2 hr ac and 1 hr pc; ↓ w/ hepatic impair.
W/P: [X, N/A] w/ severe CHF, monitor for adrenocortical insuff/excess, w/ CYP2D6 substrate/CYP3A4 inhib or inducers; do not use with severe liver insufficiency.
CI: Pregnancy.
DISP: Tabs 250 mg.
SE: Fatigue, joint swelling/discomfort, edema, hot flush, diarrhea, vomiting, cough, ↑ BP, dyspnea, UTI, contusion; common lab abnormalities: Anemia, ↑ alkaline phosphatase, hypertriglyceridemia, lymphopenia, hypercholesterolemia, hyperglycemia, ↓ K+, ↑ AST, ↓ PO4, ↑ ALT.
NOTES: Follow BP, edema status, LFTs, K+; CYP17 inhib may ↑mineralocorticoid SEs; prednisone ↓ACTH limiting SEs (hypokalemia and hypertension); if taken with food excess absorption of drug.
ACETAMINOPHEN [APAP, N-ACETYL-p-AMINOPHENOL] (ACEPHEN, OFIRMEV IV [Rx], TYLENOL, OTHER GENERIC) [OTC]
WARNING: May cause acute liver failure; associated w/ doses > 4,000 mg/d & taking APAP in >1 product.
USES: *Mild–mod pain, HA, fever*
ACTIONS: Nonnarcotic analgesic; ↓ CNS synth of prostaglandins & hypothalamic heat-regulating center.
DOSE:
Adults: 325–650 mg PO or PR q4–6h or 1,000 mg PO 3–4 ×/d; max. 4 g/d. IV: <50 kg: 15 mg/kg IV q6h or 12.5 mg/kg IV q4h; max. 75 mg/kg/d. ≥50 kg: 650 mg IV q4h or 1,000 mg IV q6h; max. 4 g/d.
Peds: <12 y. 10–15 mg/kg/dose PO or PR q4–6h; max. 5 doses/24 h. Administer q6h if CrCl 10–50 mL/min & q8h if CrCl <10 mL/min. IV: 15 mg/kg IV q6h or 12.5 mg/kg IV q4h; max. 75 mg/kg/d.
W/P: [C, +] w/ hepatic/renal impair in elderly & w/ EtOH use (>3 drinks/d); w/ >4 g/d; EtOH liver Dz, G6PD deficiency; w/ warfarin; serious skin rxns (SJS, TEN, AGEP).
CI: Hypersens.
DISP: Tabs melt away/dissolving 80, 160 mg; tabs: 325, 500, 650 mg; chew tabs 80, 160 mg; gel caps 500 mg; liq 160 mg/5 mL, 500 mg/15 mL; drops 80 mg/0.8 mL; Acephen supp 80, 120, 325, 650 mL; Inj 10 mg/mL.
SE: Hepatotoxic; OD hepatotoxic at 10 g; 15 g can be lethal; Rx w/ N-acetylcysteine.
NOTES: No anti-inflammatory or plt-inhibiting action; avoid EtOH; 2014 MedWatch Safety Alert: FDA recommends providers stop using combo products w/> 325 mg APAP/dosage unit. No data that >325 mg APAP/dose is beneficial and this ↑ liver injury risk. ↓ dose also ↓ risk of APAP overdose. Most manufacturers have complied w/ 2011 FDA request to limit APAP to 325 mg/dosage unit; some Rx combos w/ >325 mg of APAP/dosage unit remain available. FDA advisory has rec ↓ in max. dose to 3,000 mg/d.
ACETAMINOPHEN/CODEINE (TYLENOL NO. 2, 3, AND 4) [C-III, C-V]
USES: *Mild–mod pain (No. 2–3); mod–severe pain (No. 4)*
ACTIONS: Combined APAP & narcotic analgesic.
DOSE:
Adults: 1–2 tabs q4–6h PRN or 30–60 mg/codeine q4–6h based on codeine content (max. dose APAP = 4 g/d).
Peds: APAP 10–15 mg/kg/dose; codeine 0.5–1 mg/kg dose q4–6h (guide: 3–6 yr, 5 mL/dose; 7–12 yr, 10 mL/dose) max. 2.6 g/d if < 12 yr; ↓ in renal/hepatic impairment.
W/P: [C, ?] Alcoholic liver disease; G6PD deficiency.
CI: Hypersensitivity.
DISP: Tabs 300 mg APAP + codeine (No. 2 = 15 mg, No. 3 = 30 mg, No. 4 = 60 mg); susp (C-V) APAP 120 mg + codeine 12 mg/5 mL.
SE: Drowsiness, dizziness, N/V.
NOTES: See Acetaminophen note
ACETAZOLAMIDE (DIAMOX)
WARNING: Fatalities due to reactions to sulfonamides (e.g., Stevens–Johnson syndrome [SJS], toxic epidermal necrolysis [TEN], hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias. Sensitizations w/ a sulfonamide is readministration. With serious reactions occur, d/c use. Caution w/ high-dose aspirin and acetazolamide, as anorexia, tachypnea, lethargy, coma, and death have been reported.
USES: *Diuresis, drug and CHF edema, glaucoma, prevent high-altitude sickness, refractory epilepsy*, metabolic alkalosis, resp stimulant in COPD.
ACTIONS: Carbonic anhydrase inhibitor; ↓ renal excretion of hydrogen & ↑ renal excretion of Na+, K+, HCO3-, & H2O.
DOSE:
Adults: Diuretic: 250–375 mg IV or PO q24h. Metabolic alkalosis: 500 mg IV. Diuretic: 5 mg/kg/24 h PO or IV. Alkalinization of urine: 5 mg/kg/dose PO BID–TID; ↓ dose w/ CrCl 10–50 mL/min; avoid if CrCl < 10 mL/min.
W/P: [C, +/−]
CI: ↓ sodium and/or potassium; severe kidney/liver disease, adrenal failure, hyperchloremic acidosis, cirrhosis (hepatic encephalopathy risk), long-term use w/ chronic angle-closure glaucoma.
DISP: Tabs 125, 250 mg; ER caps 500 mg; Inj 500 mg/vial, powder for recons.
SE: Malaise, met allic taste, drowsiness, photosensitivity, hyperglycemia.
NOTES: Follow Na+ & K+; watch for metabolic acidosis; check CBC & plts; SR forms not for epilepsy.
ACETOHYDROXAMIC ACID (LITHOSTAT)
USES: *Adjunct for chronic urea-splitting UTI*, struvite calculi.
ACTION: ↓ Bacterial urease, ↓ ammonia and alkalinity in the urine d/t urea-splitting organisms.
DOSE:
Adults: 250 mg PO 3–4×/d, total 10–15 mg/kg/d; max. 1.5 g/day.
Peds: 10 mg/kg/d PO.
W/P: [X, −]; w/ pre-existing psych disorders.
CI: Patient amenable to definitive surgery; infection with nonurea-splitting organisms, SCr >2.5 mg/dL, females who do not use contraception, pregnancy, component hypersensitivity.
DISP: Tablets 250 mg.
SE: Hemolytic anemia, bone marrow suppression, hepatotoxicity, flushing, rash, nervousness, tremor, anorexia, N/V.
NOTES: Take on empty stomach (follow CBC and LFTs).
ACETYLCYSTEINE (ACETADOTE, MUCOMYST)
USES: *Mucolytic, antidote to acetaminophen hepatotox/OD, adjuvant treat chronic bronchopulmonary diseases & cystic fibrosis* prevent contrast-induced renal dysfunction.
ACTIONS: Splits mucoprotein disulfide linkages; restores glutathione in acetaminophen OD to protect liver.
DOSE: Antidote: PO or NG: 140 mg/kg load, then 70 mg/kg q4h × 17 doses (dilute 1:3 in carbonated beverage or OJ), repeat if emesis w/in 1 hr of dosing. Acetadote: 150 mg/kg IV over 60 min, then 50 mg/kg over 4 hr, then 100 mg/kg over 16 hr. Prevent renal dysfunction: 600–1,200 mg PO BID × 2 day.
W/P: [B, ?].
DISP: Soln, inhaled and oral 10%, 20%; Acetadote IV soln 20%.
SE: Bronchospasm (inhaled), N/V, drowsiness, anaphylactoid reactions w/ IV.
NOTES: Activated charcoal adsorbs PO acetylcysteine for acetaminophen ingestion; start treatment for acetaminophen OD w/in 6–8 hr.
ACYCLOVIR (ZOVIRAX, GENERIC)
USES: *Herpes simplex (HSV) (genital/mucocutaneous, encephalitis, keratitis), Varicella zoster, Herpes zoster (shingles) infections*.
ACTIONS: Interferes w/ viral DNA synth.
DOSE:
Adults: Dose on IBW if obese (>125% IBW) PO. Initial genital HSV: 200 mg PO q4h while awake (5 caps/d) × 10 days or 400 mg PO TID × 7–10 days. Chronic HSV suppression: 400 mg PO BID. Intermittent HSV Treat: As initial, except Treat × 5 days, or 800 mg PO BID, at prodrome. Topical: Initial herpes genitalis: Apply q3h (6×/d) for 7 days. HSV encephalitis: 10 mg/kg IV q8h × 10 days. Herpes zoster: 800 mg PO 5/d for 7–10 days. IV: 10 mg/kg/dose IV q8h 7 days.
Peds: Genital HSV: 3 mo–12 y: 40–80 mg/kg/d divided 3–4 doses (max 1 g); ≥12 yr: 200 mg 5 times day or 400 mg 3 times a day for 5–10 d; IV: 5 mg/kg/dose q8h for 5–7 d Shingles: <12 y: 30 mg/kg/d PO or 1,500 mg/m2/day IV ÷ q8h for 7–10 d; ↓ w/ CrCl <50 mL/min.
W/P: [B, +].
CI: Component hypersens.
DISP: Caps 200 mg; tabs 400, 800 mg; susp 200 mg/5 mL; Inj 500 & 1,000 mg/vial; Inj soln, 50 mg/mL oint 5% and cream 5%.
SE: Dizziness, lethargy, malaise, confusion, rash, IV site inflammation; transient ↑ Cr/BUN.
NOTES: PO better than topical for herpes genitalis.
ALDESLEUKIN [IL-2] (PROLEUKIN)
WARNING: Restrict to pts w/ nl cardiac/pulmonary functions as defined by formal testing. Caution w/ Hx of cardiac/pulmonary disease. Administer in hospital setting w/ physician experienced w/ anticancer agents. Assoc w/ capillary leak syndrome (CLS) characterized by ↓ BP and organ perfusion w/ potential for cardiac/respiratory tox, GI bleed/infarction, renal insufficiency, edema, and mental status changes. ↑risk of sepsis and bacterial endocarditis. Treat bacterial infection before use. Pts w/ central lines are at ↑ risk for infection. Prophylaxis w/ oxacillin, nafcillin, ciprofloxacin, or vancomycin may reduce staphylococcal infection. Hold w/ mod–severe lethargy or somnolence; continued use may result in coma.
USES: *Met RCC & melanoma*.
ACTIONS: Acts via IL-2 receptor; many immunomodulatory effects.
DOSE: 600,000 IU/kg q8h × max. 14 doses days 1–5 and days 15–19 of 28-day cycle (FDA dose/schedule for RCC); other schedules (eg, “high dose” 720,000 IU/kg IV q8h up to 12 doses, repeat 10–15 days later).
W/P: [C, ?/−].
CI: Organ allografts; abnormal thallium stress test or PFT.
DISP: Powder for recons 22 × 106 IU, when reconstituted 18 MIU/mL = 1.1 mg/mL.
SE: Flu-like syndrome (malaise, fever, chills), N/V/diarrhea, ↑ bili; capillary leak syndrome; ↓ BP, tachycardia, pulm & periph edema, fluid retention, & Wt gain; renal & mild hematologic tox (↓Hgb, plt, WBC), eosinophilia; cardiac tox (ischemia, atrial arrhythmias); neurotox (CNS depression, somnolence, delirium, rare coma); pruritic rashes, urticaria, & erythroderma common.
ALENDRONATE (BINOSTO, FOSAMAX, FOSAMAX PLUS D, GENERIC)
USES: *Treat & prevent osteoporosis male & postmenopausal female, Treat steroid-induced osteoporosis, Paget disease*.
ACTIONS: ↓ Nl & abnormal bone resorption, ↓ osteoclast action.
DOSE: Osteoporosis: Treat: 10 mg/d PO or 70 mg qwk; Fosamax plus D 1 tab qwk. Steroid-induced osteoporosis: Treat: 5 mg/d PO, 10 mg/d postmenopausal not on estrogen. Prevention: 5 mg/d PO or 35 mg qwk. Paget disease:40 mg/d PO × 6 mo.
W/P: [C, ?] Not OK if CrCl <35 mL/min, w/ NSAID use.
CI: Esophageal anomalies, inability to sit/stand upright for 30 min, ↓ Ca2+.
DISP: Tabs 5, 10, 35, 40, 70 mg. Fosamax plus D: Alendronate 70 mg w/ cholecalciferol (vit D3) 2,800 or 5,600 IU. Binosto: Effervescent 7 mg tablet.
SE: Abdominal pain, acid regurgitation, constipation, diarrhea/N, dyspepsia, musculoskelet al pain, jaw osteonecrosis (w/ dental procedures, chemo).
NOTES: Take 1st thing in a.m. w/ H2O (8 oz) >30 min before 1st food/beverage of day; do not lie down for 30 min after. Use Ca2+ & vit D supl w/ regular tab; may ↑ atypical subtrochanteric femur fractures.
ALFUZOSIN (UROXATRAL, GENERIC)
USES: *Symptomatic BPH*.
ACTIONS: α-Blocker.
DOSE: 10 mg PO daily immediately after the same meal; do not crush/chew.
W/P: [B, ?/−] w/ any Hx ↓ BP; use w/ PDE5 inhibitors may ↓ BP; may ↑ QTc interval; d/c with angina; intraoperative floppy iris syndrome during cataract surgery; w/ CrCl <30 mL/min.
CI: w/ CYP3A4 inhibitor (eg, ketoconazole, itraconazole, ritonavir); mod–severe hepatic impairment; protease inhibitors for HIV.
DISP: Tabs 10 mg ER.
SE: Postural ↓ BP, dizziness, headache, fatigue, rare priapism.
NOTES: Do not cut or crush.
ALLOPURINOL (ALOPRIM, ZYLOPRIM, GENERIC)
USES: *Gout, hyperuricemia of malignancy, uric acid urolithiasis, recurrent calcium oxalate calculi (w/ urinary uric acid >800 mg/d in males and 750 mg/d in females.*
ACTIONS: Xanthine oxidase inhibitor; ↓ uric acid production.
DOSE:
Adults: PO: Initial 100 mg/d; usual 300 mg/d; max. 800 mg/d; ÷ dose if >300 mg/d. IV: 200–400 mg/m2/d (max. 600 mg/24 h); (after meal w/ plenty of fluid).
Peds: Only for hyperuricemia of malignancy if <10 yr: 10 mg/kg/d PO (max. 800 mg) or 50–100 mg/m2 q8h (max. 300 mg/m2/d); 200–400 mg/m2/d IV (max. 600 mg) ↓ in renal impairment.
W/P: [C, M] Life-threatening syndrome (diffuse desquamative skin rash, fever, hepatic dysfunction, eosinophilia, worsening renal function); 80% have pre-existing renal insufficiency.
DISP: Tabs 100, 300 mg; Inj 500 mg/30 mL (Aloprim).
SE: Rash, N/V, renal impairment, angioedema.
NOTES: Aggravates acute gout; begin after acute attack resolves; IV dose of 6 mg/mL final conc as single daily Inf or ÷ 6-, 8-, or 12-hr intervals
ALPROSTADIL, INTRACAVERNOSAL (CAVERJECT, CAVERJECT IMPULSE, EDEX)
USES: *Erectile dysfunction.*
ACTIONS: A form of prostaglandin E1; relaxes smooth muscles, dilates cavernosal arteries, ↑ lacunar spaces w/ blood entrapment.
DOSE: 2.5–60 μg intracavernosal; titrate in office.
W/P: [X, −].
CI: ↑ risk of priapism (eg, sickle cell, hematologic malignancies); penile deformities/implants; men in whom sexual activity inadvisable.
DISP: Caverject: 5-, 10-, 20-, 40-μg powder for Inj vials ± diluent syringes 10-, 20-, 40-μg amp. Caverject impulse: Self-contained syringe (29G) 10 & 20 μg (volume 0.5 mL), Edex: 10-, 20-, 40-μg cartridges.
SE: Local pain w/ Inj, priapism risk.
NOTES: Counsel about priapism, penile fibrosis, & hematoma risks.
ALPROSTADIL, URETHRAL SUPPOSITORY (MUSE)
USES: *Erectile dysfunction.*
ACTIONS: A form of prostaglandin E1; urethral absorption; vasodilator, relaxes smooth muscle of corpus cavernosa.
DOSE: 125–250 μg PRN to achieve erection (max. 2 systems/24 h) duration 30–60 min.
W/P: [X, −].
CI: ↑ Priapism risk (especially sickle cell, myeloma, leukemia), penile deformities/urethral stricture/implants; men in whom sex inadvisable; component hypersensitivity.
DISP: 125, 250, 500, 1,000 μg w/ transurethral applicator system (microsuppositories 1.4 mm diameter by 3 mm or 6 mm length).
SE: ↓ BP, dizziness, syncope, penile/testicular pain, urethral burning/bleeding, priapism.
NOTES: Titrate dose in office; store in refrigerator; do not expose to temps >86 F; @ room temp max. storage 14 days.
ALVIMOPAN (ENTEREG)
WARNING: For short-term hospital use only (max. 15 doses).
USES: *Accelerate the time to upper and lower gastrointestinal recovery following partial large or small bowel resection surgery with primary anastomosis.*
ACTIONS: Opioid (μ) receptor antagonist; selectively binds GI receptors, antagonizes effects of opioids on GI motility/secretion.
DOSE: 12 mg 30 min–5 hr preop PO, then 12 mg BID up to 7 days; max. 15 doses.
W/P: [B,?/−] Not rec in complete bowel obstruction surgery, hepatic/renal impairment.
CI: Therapeutic opioids >7 consecutive days prior.
DISP: Caps 12 mg.
SE: ↓ K+, dyspepsia, urinary retention, anemia, back pain.
NOTES: Hospitals must be registered to use.
AMIFOSTINE (GENERIC)
USES: *Xerostomia prophylaxis during RT (head, neck, etc.) where parotid is in radiation field; ↓ renal tox w/ repeated cisplatin (label specifies ovarian ca).*
ACTIONS: Prodrug, dephosphorylated to active thiol metabolite, free radical scavenger binds cisplatin metabolites.
DOSE: Chemo prevent: 910 mg/m2/d 15-min IV Inf 30 min prechemo; Xerostomia Px: 200 mg/m2 over 2 min 1×/d 15 min prerad.
W/P: [C,?/−].
DISP: 500-mg vials powder, reconstitute in NS.
SE: Transient ↓ BP (>60%), N/V, flushing w/ hot or cold chills, dizziness, ↓ Ca2+, somnolence, sneezing, serious skin infection.
NOTES: Does not ↓ effectiveness of cyclophosphamide + cisplatin chemotherapy.
AMIKACIN (AMIKIN)
WARNING: May cause nephrotoxicity, neuromuscular blockade, & respiratory paralysis.
USES: *Serious gram(−) bacterial infections* & mycobacteria.
ACTIONS: Aminoglycoside; ↓ protein synth. Spectrum: Good gram(−) bacterial coverage: Pseudomonas & Mycobacterium sp.
DOSE:
Adults & Peds: Conventional: 5–7.5 mg/kg/dose q8h; once daily; 15–20 mg/kg q24h; ↑ interval w/ renal impairment. Neonates < 1,200 g, 0–4 wk: 7.5 mg/kg/dose q18–24h. Age <7 d, 1,200–2,000 g: 7.5 mg/kg/dose q12h >2,000 g:7.5–10 mg/kg/dose q12h. Age >7 d, 1,200–2,000 g: 7.5–10 mg/kg/dose q8–12h >2,000 g: 7.5–10 mg/kg/dose q8h.
W/P: [O, +/−] Avoid w/ diuretics.
DISP: Inj 50 & 250 mg/mL.
SE: Renal impairment, oto toxicity.
NOTES: May be effective in gram (−) resistance to gentamicin & tobramycin; follow Cr; Levels: Peak: 30 min after Inf. Trough <0.5 hr before next dose. Therapeutic: Peak 20–30 μg/mL. Trough: <8 μg/mL. Toxic peak >35 μg/mL; half-life: 2 hr.
AMILORIDE (MIDAMOR, GENERIC)
WARNING: ↑ K+ esp renal disease DM, elderly
USES: *HTN, CHF, & thiazide or loop diuretic induced ↓ K+*
ACTIONS: K+-sparing diuretic; interferes w/ K+/Na+ exchange in distal tubule & collecting duct
DOSE:
Adults: 5–10 mg PO daily (max 20 mg/d)
Peds: 0.4–0.625 mg/kg/d; ↓ w/ renal impairment
W/P: [B, ?] avoid CrCl <10 mL/min
CI: ↑ K+, acute or chronic renal disease, diabetic neuropathy, w/ other K+-sparing diuretics
DISP: Tabs 5 mg
SE: ↑ K+; headache, dizziness, dehydration, impotence
NOTES: Check K+
AMINOCAPROIC ACID (AMICAR)
USES: *Excessive bleeding from systemic hyperfibrinolysis & urinary fibrinolysis.*
ACTIONS: ↓ Fibrinolysis; inhibits TPA, inhibits conversion of plasminogen to plasmin.
DOSE:
Adults: 4–5 g IV or PO (1st hr) then 1 g/h IV or 1.25 g/h PO × 8 hr or until bleeding controlled; 30 g/d max.
Peds: 100 mg/kg IV (1st hr) then 1 g/m2/h; max. 18 g/m2/d; ↓ w/ renal insufficiency.
W/P: [C, ?] Not for upper urinary tract bleeding (firm clot obstruction risk).
CI: DIC.
DISP: Tabs 500 mg, syrup 1.25 g/5 mL; Inj 250 mg/mL.
SE: ↓ BP, ↓ HR, dizziness, headache, fatigue, rash, GI disturbance, skelet al muscle weakness, ↓ plt function.
NOTES: Urinary fibrinolysis (a normal physiologic phenomenon), may contribute to excessive urinary tract fibrinolytic bleeding associated with surgical hematuria (eg, following prostatectomy and nephrectomy) or nonsurgical hematuria (polycystic or neoplastic diseases, radiation cystitis). Administer × 8 hr or until bleeding controlled; has also been administered by bladder irrigation; obvious clots should be cleared before stating and saline CBI can help effectiveness.
AMINOGLUTETHIMIDE (CYTADREN)
USES: *Cushing syndrome,* adrenocortical carcinoma, breast cancer & PCa.
ACTIONS: ↓ Adrenal steroidogenesis & conversion of androgens to estrogens; 1st gen aromatase inhibitor.
DOSE: Initial 250 mg PO 4 × d, titrate q1–2wk max. 2 g/d; w/ hydrocortisone 20–40 mg/d; ↓ w/ renal insufficiency.
W/P: [D, ?].
DISP: Tabs 250 mg.
SE: Adrenal insufficiency, hypothyroidism, masculinization, ↓ BP, N/V, rare hepatotox, rash, myalgia, fever, drowsiness, lethargy, anorexia.
NOTES: No longer available in the US.
AMITRIPTYLINE (ELAVIL)
WARNING: Antidepressants may ↑ suicide risk; consider risks/benefits of use. Monitor pts closely.
USES: *Depression (not bipolar depression)* peripheral neuropathy, chronic pain, tension HAs, migraine headache prophylaxis PTSD* enuresis, interstitial cystitis.
ACTIONS: Tricyclic antidepressants; ↓ reuptake of serotonin & norepinephrine by presynaptic neurons.
DOSE:
Adults: Initial: 25–150 mg PO hs; may ↑ to 300 mg hs.
Peds: Do not use if <12 yr unless for chronic pain, Initial: 0.1 mg/kg PO hs, ↑ over 2–3 wk to 0.5–2 mg/kg PO hs; taper to D/C.
W/P: CV disease, seizures [D,+/−] narrow-angle glaucoma, hepatic impairment.
CI: w/ MAOIs or w/in 14 days of use, during AMI recovery.
DISP: Tabs 10, 25, 50, 75, 100, 150 mg; Inj 10 mg/mL.
SE: Strong anticholinergic SEs; OD may be fatal; urine retention, sedation, ECG changes BM suppression, orthostatic ↓ BP, photosensitivity.
NOTES: Levels: Therapeutic: 100–250 ng/mL, Toxic: >500 ng/mL; levels may not correlate w/ effect.
AMLODIPINE (NORVASC)
USES: *HTN, stable or unstable angina,*
ACTIONS: Calcium channel blocker; relaxes coronary vascular smooth muscle.
DOSE: 2.5–10 mg/d PO; ↓ w/ hepatic impairment.
W/P: [C, ?].
DISP: Tabs 2.5, 5, 10 mg.
SE: Edema, headache, palpitations, flushing, dizziness.
NOTES: Take w/o regard to meals.
AMLODIPINE/OLMESARTAN (AZOR)
WARNING: Use of renin–angiotensin agents in PREGNANCY can cause injury and death to fetus, D/C immediately when PREGNANCY detected.
USES: *Hypertension.*
ACTIONS: Calcium channel blocker w/ angiotensin II receptor blocker.
DOSE:
Adults: Initial 5 mg/20 mg, max. 10 mg/40 mg q day.
W/P: [D, −] w/ K+ supl or K+-sparing diuretics, renal impairment, RAS, severe CAD, AS.
CI: PREGNANCY.
DISP: Tabs amlodipine/olmesartan 5 mg/20 mg, 10/20, 5/40, 10/40.
SE: Edema, vertigo, dizziness, ↓ BP.
AMLODIPINE/VALSARTAN (HA EXFORGE)
WARNING: Use of renin–angiotensin agents in PREGNANCY can cause fet al injury and death, D/C immediately when PREGNANCY detected.
USES: *HTN.*
ACTIONS: Calcium channel blocker w/ angiotensin II receptor blocker.
DOSE:
Adults: Initial 5 mg/160 mg, may ↑ after 1–2 wk, max. 10 mg/320 mg q day, start elderly at 1/2 initial dose.
W/P: [D /−] w/ K+ supl or K+-sparing diuretics, renal impairment, RAS, severe CAD.
CI: PREGNANCY.
DISP: Tabs amlodipine/valsartan 5/160, 10/160, 5/320, 10 mg/320 mg.
SE: Edema, vertigo, nasopharyngitis, URI, dizziness, ↓ BP.
AMLODIPINE/VALSARTAN/HCTZ (EXFORGE HCT)
WARNING: Use of renin–angiotensin agents in PREGNANCY can cause fet al injury and death, D/C immediately when PREGNANCY detected.
USES: *Hypertension (not initial Treat).*
ACTIONS: Calcium channel blocker, angiotensin II receptor blocker, & thiazide diuretic.
DOSE: 5–10/160–320/12.5–25 mg 1 tab 1 × day may ↑ dose after 2 wk; max. dose 10/320/25 mg.
W/P: [D, −] w/ severe hepatic or renal impairment.
CI: Anuria, sulfonamide allergy.
DISP: Tabs amlodipine/valsartan/ HCTZ: 5/160/12.5, 10/160/12.5, 5/160/25, 10/160/25, 10/320/25 mg.
SE: Edema, dizziness, headache, fatigue, ↑/↓ K+ ↑ BUN, ↑ SCr, nasopharyngitis, dyspepsia, N, back pain, muscle spasm, ↓ BP.
AMMONIUM ALUMINUM SULFATE [ALUM] [OTC]
USES: *Hemorrhagic cystitis when saline bladder irrigation fails.*
ACTIONS: Astringent, forms precipitates over bleeding surface.
DOSE:
Adult/Peds: 1–4% soln w/ constant NS bladder irrigation 200–250 mL/h.
W/P: [+/−].
DISP: Powder for recons; (typical 50 g in 5 L sterile water).
SE: Encephalopathy possible; check aluminum levels, especially w/ renal insufficiency; spasms; can precipitate & occlude catheters.
NOTES: Safe w/o anesthesia & w/ vesicoureteral reflux; effect often takes several days.
AMOXICILLIN (AMOXIL, MOXATAG, GENERIC)
USES: *Ear, nose, & throat, lower resp, skin, urinary tract infections from susceptible gram(+) bacteria* endocarditis prophylaxis, H. pylori eradication w/ other agents (gastric ulcers).
ACTIONS: β-Lactam antibiotic; ↓ cell wall synth. Spectrum: gram(+) (Streptococcus sp, Enterococcus sp); some gram(−) (H. influenzae, E. coli, N. gonorrhoeae, H. pylori, & P. mirabilis).
DOSE:
Adults: 250–500 mg PO TID or 500–875 mg BID ER 775 mg 1 × d.
Peds: 25–100 mg/kg/24 h PO ÷ q8h, ↓ in renal impairment.
W/P: [B, +].
DISP: Caps 250, 500 mg; chew tabs 125, 200, 250, 400 mg; susp 50, 125, 200, 250 mg/mL & 400 mg/5 mL; tabs 500, 875 mg; tab ER 775 mg.
SE: Diarrhea; rash.
NOTES: Cross-hypersens w/ PCN; many E. coli strains resistant; chew tabs contain phenylalanine.
AMOXICILLIN/CLAVULANIC ACID (AUGMENTIN, AUGMENTIN ES-600, AUGMENTIN XR)
USES: *Ear, lower resp, sinus, urinary tract, skin infections caused by β-lactamase–producing H. influenzae, S. aureus, & E. coli.*
ACTIONS: β-Lactam antibiotic w/ β-lactamase inhibitor. Spectrum: gram(+) same as amoxicillin alone, MSSA; gram(−) as w/ amoxicillin alone, β-lactamase–producing H. influenzae, Klebsiella sp, M. catarrhalis.
DOSE:
Adults: 250–500 mg PO q8h or 875 mg q12h; XR 2,000 mg PO q12h.
Peds: 20–40 mg/kg/d as amoxicillin PO ÷ q8h or 45–90 mg/kg/d ÷ q12h; ↓ in renal impairment; take w/ food.
W/P: [B, enters breast milk].
DISP: Supplied (as amoxicillin/clavulanic): Tabs 250/125, 500/125, 875/125 mg; chew tabs 125/31.25, 200/28.5, 250/62.5, 400/57 mg; susp 125/31.25, 250/62.5, 200/28.5, 400/57 mg/5 mL; susp ES 600/42.9 mg/5 mL; XR tab 1,000/62.5 mg.
SE: Abdominal discomfort, N/V/diarrhea, allergic reaction, vaginitis.
NOTES: Do not substitute two 250-mg tabs for one 500-mg tab (possible OD of clavulanic acid); max. clavulanic acid 125 mg/dose.
AMPHOTERICIN B (FUNGIZONE)
USES: *Severe, systemic fungal infections; oral & cutaneous candidiasis.*
ACTIONS: Binds ergosterol in the fungal membrane to alter permeability.
DOSE:
Adults & Peds: 0.25–1.5 mg/kg/24 h IV over 2–6 h (25–50 mg/d or q other day). Total varies w/ indication ↑ PR, N/V.
W/P: [B, ?].
DISP: Powder (Inj) 50 mg/vial.
SE: ↓ K+/Mg2+ from renal wasting; anaphylaxis, headache, fever, chills, nephrotoxic, ↓ BP, anemia, rigors.
NOTES: Check Cr/LFTs/K+/Mg2+; ↓ in renal impairment; pretreatment w/ acetaminophen & diphenhydramine ± hydrocortisone can ↓ SE.
AMPHOTERICIN B CHOLESTERYL (AMPHOTEC)
USES: *Aspergillosis if intolerant/refractory to conventional amphotericin B*, systemic candidiasis.
ACTIONS: Binds ergosterol in fungal membrane, alters permeability.
DOSE:
Adults & Peds: 3–4 mg/kg/d; 1 mg/kg/h Inf, 7.5 mg/kg/d max.; ↓ w/ renal insufficiency.
W/P: [B, ?].
DISP: Powder for Inj 50, 100 mg/vial.
SE: Anaphylaxis; fever, chills, headache, ↓ PLT, N/V, ↑ HR, ↓ K+, ↓ Mg2+, nephrotoxic, ↓ BP, infusion reactions, anemia.
NOTES: Do not use in-line filter; check LFTs/lytes.
AMPHOTERICIN B LIPID COMPLEX (ABELCET)
USES: *Refractory invasive fungal infection in pts intolerant to conventional amphotericin B.*
ACTIONS: Binds ergosterol in fungal membrane, alters permeability.
DOSE:
Adults & Peds: 2.5–5 mg/kg/d IV × 1 daily.
W/P: [B, ?].
DISP: Inj 5 mg/mL.
SE: Anaphylaxis; fever, chills, headache, ↓ K+, ↑ SCr ↓ Mg2+, nephrotoxic, ↓ BP, anemia.
NOTES: Filter w/ 5-μm needle; do not mix in electrolyte-containing solns; if Inf >2 hr, manually mix bag.
AMPHOTERICIN B LIPOSOMAL (AMBISOME)
USES: *Refractory invasive fungal infection w/ intolerance to conventional amphotericin B; cryptococcal meningitis in HIV; empiric for febrile neutropenia; visceral leishmaniasis.*
ACTIONS: Binds ergosterol in fungal membrane, alters membrane permeability.
DOSE:
Adults & Peds: 3–6 mg/kg/d, Inf 60–120 min; varies by indication; ↓ in renal insufficiency.
W/P: [B, ?].
DISP: Powder Inj 50 mg.
SE: Anaphylaxis, fever, chills, headache, ↓ K+, ↓ Mg2+ peripheral edema, insomnia, rash, ↑ LFTs, nephrotoxic, ↓ BP, anemia.
NOTES: Do not use <. 1-μm filter.
AMPICILLIN (GENERIC)
USES: *Resp, GU, or GI tract infections, meningitis d/t gram(−) & (+) bacteria; SBE prophylaxis.*
ACTIONS: β-Lactam antibiotic; ↓ cell wall synth. Spectrum: gram(+) (Streptococcus sp, Staphylococcus sp, Listeria); gram(−) (Klebsiella sp, E. coli, H. influenzae, P. mirabilis, Shigella sp, Salmonella sp).
DOSE:
Adults: 1,000 mg–2 g IM or IV q4–6h or 250–500 mg PO q6h; varies by indication.
Peds Neonates: <7 days: 50–100 mg/kg/24 h IV ÷ q8h.Term infants: –150 mg/kg/24 h ÷ q6–8h IV or PO. Children >1 mo: 200 mg/kg/24 h ÷ q6h IM or IV; 50–100 mg/kg/24 h ÷ q6h PO up to 250 mg/dose; ↓ w/ renal impairment; take on empty stomach.
W/P: [B, M] Cross-hypersensitivity w/ PCN.
DISP: Caps 250, 500 mg; susp, 125 mg/5 mL, 250 mg/5 mL; powder (Inj) 125, 250, 500 mg, 1, 2, 10 g/vial.
SE: Diarrhea, rash, allergic reaction.
NOTES: Many E. coli resistant.
AMPICILLIN-SULBACTAM (UNASYN, GENERIC)
USES: *Gynecologic, intra-abdominal, skin infections d/t β-lactamase–producing S. aureus, Enterococcus, H. influenzae, P. mirabilis, & Bacteroides sp.*
ACTIONS: β-Lactam antibiotic & β-lactamase inhibitor. Spectrum: gram(+) & (−) as for amp alone; also Enterobacter, Acinetobacter, Bacteroides.
DOSE:
Adults: 1.5–3 g IM or IV q6h.
Peds: 100–400 mg ampicillin/kg/d (150–300 mg Unasyn) q6h; ↓ w/ renal insufficiency.
W/P: [B, M].
DISP: Powder for Inj 1.5, 3 g/vial, 15 g bulk package.
SE: Allergic reactions, rash, diarrhea, Inj site pain.
NOTES: A 2:1 ratio ampicillin:sulbactam.
ANIDULAFUNGIN (ERAXIS)
USES: *Candidemia, esophageal candidiasis, other Candida infections (peritonitis, intra-abdominal abscess).*
ACTIONS: Echinocandin; ↓ cell wall synth. Spectrum: C. albicans, C. glabrata, C. parapsilosis, C. tropicalis.
DOSE: Candidemia, others: 200 mg IV × 1, then 100 mg IV daily [Tx ≥ 4 days after last (+) culture]; 1.1 mg/min max. Inf rate.
W/P: [B, ?/−].
CI: Echinocandin hypersens.
DISP: Powder 50, 100 mg/vial.
SE: Histamine-mediated Inf reactions (urticaria, flushing, ↓ BP, dyspnea, etc.), fever, N/V/diarrhea, ↓ K+, headache, ↑ LFTs, hep, worsening hepatic failure.
NOTES: ↓ Inf rate to <1.1 mg/min w/ Inf reactions.
APIXABAN (ELIQUIS)
WARNING: ↑ Risk of spinal/epidural hematoma w/ paralysis & ↑ thrombotic events w/ D/C in afib pts; monitor closely.
USES: *Prevent CVA/TE in nonvalvular afib.*
ACTIONS: Factor Xa inhibitor.
DOSE: 5 mg BID; 2.5 mg w/2 of the following: >80 yr, Wt <60 kg, SCr ≥1.5; 2.5 mg w/ strong dual inhibitor of CYP3A4 and P-glycoprotein; if on 2.5 mg do NOT use w/ strong dual inhibitor of CYP3A4 and P-glycoprotein.
W/P: [B, −] Do not use w/ prosthetic valves.
CI: Pathologic bleeding & apixaban hypersens.
DISP: Tabs 2.5, 5 mg.
SE: Bleeding.
NOTES: If missed dose, do NOT double next dose; no antidote to reverse; anticoagulant effect can last 24 hr after dose.
APREPITANT (EMEND, ORAL)
USES: *Prevents N/V associated w/ emetogenic cancer chemotherapy (eg, cisplatin) (use in combo w/ other antiemetics)*, postop N/V.*
ACTIONS: Substance P/neurokinin 1 (NK1) receptor antagonist.
DOSE: 125 mg PO day 1, 1 hr before chemotherapy, then 80 mg PO q a.m. days 2 & 3; postop N/V: 40 mg w/in 3 hr of induction.
W/P: [B, ?/−]; substrate & mod CYP3A4 inhibitor; CYP2C9 inducer; ↓ effect OCP and warfarin.
CI: Use w/ pimozide or cisapride.
DISP: Caps 40, 80, 125 mg.
SE: Fatigue, asthenia, hiccups.
NOTES: See also Fosaprepitant (Emend, Injection).
ASPIRIN (BAYER, ECOTRIN, ST. JOSEPH’S) [OTC]
USES: *CABG, PTCA, carotid endarterectomy, ischemic stroke, TIA, ACS/MI, arthritis, pain, headache, fever, inflammation*, Kawasaki disease.
ACTIONS: Prostaglandin inhibitor by COX-2 inhibitor.
DOSE:
Adults: Pain, fever: 325–650 mg q4–6h PO or PR (4 g/d max.). Plt inhibitor: 81–325 mg PO daily.
Peds: Antipyretic: 10–15 mg/kg/dose PO or PR q4–6h; for all uses 4 g/d max.; avoid w/ CrCl <10 mL/min, severe liver disease.
W/P: [C, M] linked to Reye syndrome; avoid w/ viral illness in peds <16 yr.
CI: Allergy to ASA, chickenpox/ flu Sxs, syndrome of nasal polyps, angioedema, & bronchospasm to NSAIDs, bleeding disorder.
DISP: Tabs 325, 500 mg; chew tabs 81 mg; EC tabs 81, 162, 325, 500 mg, effervescent tabs 500 mg; supp 300, 600 mg; caplets 81, 375, 500 mg.
SE: GI upset, erosion, & bleeding.
NOTES: D/C 1 wk preop; avoid/limit EtOH; Salicylate levels: Therapeutic: 100–250 μg/mL; Toxic: >300 μg/mL.
ATENOLOL (TENORMIN, GENERIC)
WARNING: Avoid abrupt withdrawal (esp. CAD pts), gradual taper to ↓, acute ↑ HR, HTN +/− ischemia.
USES: *HTN, angina, post-MI.*
ACTIONS: Selective β-adrenergic receptor blocker.
DOSE: HTN & angina: 25–100 mg/d PO; ↓ in renal impairment.
W/P: [D, M] DM, bronchospasm; abrupt D/C can exacerbate angina & ↑ MI risk.
CI: ↓ HR, cardiogenic shock, cardiac failure, 2nd-/3rd-degree AV block, sinus node dysfunction, pulm edema.
DISP: Tabs 25, 50, 100 mg.
SE: ↓ HR, ↓ BP, 2nd-/3rd-degree AV block, dizziness, fatigue.
ATENOLOL & CHLORTHALIDONE (TENORETIC)
USES: *HTN.*
ACTIONS: β-Adrenergic blockade w/ diuretic.
DOSE: 50–100 mg/d PO based on atenolol; ↓ dose w/ CrCl <35 mL/min.
W/P: [D, ?/−] DM, bronchospasm.
CI: See atenolol; anuria, sulfonamide, cross-sensitivity.
DISP: Atenolol 50 mg/chlorthalidone 25 mg, atenolol 100 mg/chlorthalidone 25 mg.
SE: ↓ HR, ↓ BP, 2nd-/3rd-degree AV block, dizziness, fatigue, ↓ K+, photosensitivity.
ATROPINE, BENZOIC ACID, HYOSCYAMINE SULFATE, METHENAMINE, METHYLENE BLUE, PHENYL SALICYLATE (URISED)
USES: *Lower urinary tract discomfort.*
ACTIONS: Methenamine in acidic urine releases formaldehyde (antiseptic), methylene blue/benzoic acid (mild antiseptic), phenyl salicylate (mild analgesic), hyoscyamine and atropine (parasympatholytic; ↓ muscle spasm).
DOSE:
Adults: 2 tablets PO QID.
Peds: >6 yr: Individualize.
W/P: [C, ?/−]; avoid w/ sulfonamides.
CI: Narrow-angle glaucoma, pyloric/duodenal obstruction, bladder outlet obstruction, coronary artery spasm.
DISP: Tablet; atropine 0.03 mg/benzoic acid 45 mg/hyoscyamine 0.03 mg/methenamine 40.8 mg/methylene blue 5.4 mg/phenyl salicylate 18.1 mg.
SE: Rash, dry mouth, flushing, ↑ pulse, dizziness, blurred vision, urine/feces discoloration, voiding difficulty.
NOTES: Take w/ plenty of fluid; can cause crystalluria; see also hyoscyamine and methenamine listings.
AVANAFIL (STENDRA)
USES: *Erectile dysfunction.*
ACTIONS: ↓ Phosphodiesterase type 5 (PDE5) (responsible for cGMP breakdown); ↑ cGMP activity to relax smooth muscles to ↑ flow to corpus cavernosum; onset 30–45 min (delayed 1–1.25 hr with high fat meal).
DOSE: (Men only) 100 mg PO as early as 15 min before sex activity, no more than 1×/d; ↑/↓ dose 50–200 mg based on effect; do not use w/ strong CYP3A4 inhibitor; use 50 mg w/ mod CYP3A4 inhibitor; w/ or w/o food.
W/P: [C, ?] Priapism risk; hypotension w/ BP meds or substantial alcohol; seek immediate attention w/ hearing loss or acute vision loss (may be NAION; w/ CYP3A4 inhibitor (eg, ketoconazole, ritonavir, erythromycin) ↑ effects; do not use w/ severe renal/ hepatic impairment.
CI: w/ Nitrates or if sex not advised.
DISP: Tabs 50, 100, 200 mg.
SE: Headache, flushing, nasal congestion, nasopharyngitis back pain.
NOTES: More rapid onset than sildenafil (15–30 min).
AXITINIB (INLYTA)
USES: *Advanced RCC.*
ACTIONS: Tyrosine kinase inhibitor.
DOSE:
Adults: 5 mg PO q12h; if tolerated >2 wk, ↑ to 7 mg q12h, then 10 mg q12h; w/ or w/o food; swallow whole; ↓ dose by ½ w/ moderate hepatic impairment; avoid w/ or ↓ dose by ½ if used w/ strong CYP3A4/5 inhibitor.
W/P: [D, ?] w/ brain mets, recent GI bleed.
DISP: Tabs 1, 5 mg.
SE: N/V/diarrhea/C, HTN, fatigue, asthenia, ↓ appetite, ↓ Wt, ↑ LFTs, hand–foot syndrome, venous/arterial thrombosis; hemorrhage, ↓ thyroid, GI perf/ fistula, proteinuria, hypertensive crisis, impaired wound healing, reversible posterior leukoencephalopathy syndrome.
NOTES: Hold 24 hr prior to surgery.
AZATHIOPRINE (AZASAN, IMURAN)
WARNING: May ↑ neoplasia w/ chronic use; mutagenic and hematologic tox possible.
USES: *Adjunct to prevent renal transplant rejection, rheumatoid arthritis*, SLE, Crohn’s disease, ulcerative colitis.
ACTIONS: Immunosuppressive; antagonizes purine metabolism.
DOSE:
Adults: Crohn and ulcerative colitis: Start 50 mg/d, ↑ 25 mg/d q1–2wk, target dose 2–3 mg/kg/d.
Adults & Peds: Renal transplant: 3–5 mg/kg/d IV/PO single daily dose, then 1–3 mg/kg/d maint; rheumatoid arthritis: 1 mg/kg/d once daily or ÷ BID × 6–8 wk, ↑ 0.5 mg/kg/d q4wk to 2.5 mg/kg/d; ↓ w/ renal insufficiency.
W/P: [D, ?/−].
CI: PREGNANCY.
DISP: Tabs 50, 75, 100 mg; powder for Inj 100 mg.
SE: GI intolerance, fever, chills, leukopenia, ↑ LFTs, bilirubin, ↑ risk infections, thrombocytopenia.
NOTES: Handle Inj w/ cytotoxic precautions; interaction w/ allopurinol; do not administer live vaccines on drug; check CBC and LFTs; dose per local transplant protocol, usually start 1–3 days pretransplant.
AZITHROMYCIN (ZITHROMAX)
USES: *Community-acquired pneumonia, pharyngitis, otitis media, skin infections, nongonococcal (chlamydial) urethritis, chancroid & PID; Treat & prevention of MAC in HIV.*
ACTIONS: Macrolide antibiotic; bacteriostatic; ↓ protein synth. Spectrum: Chlamydia, H. ducreyi, H. influenzae, Legionella, M. catarrhalis, M. pneumoniae, M. hominis, N. gonorrhoeae, S. aureus, S. agalactiae, S. pneumoniae, S. pyogenes.
DOSE:
Adults: Resp tract infections: PO: Caps 500 mg day 1, then 250 mg/d PO × 4 days. Nongonococcal urethritis: 1 g PO × 1 Gonorrhea, uncomplicated: 2 g PO × 1; Prevent MAC: 1,200 mg PO once/wk.
Peds: Otitis media: 10 mg/kg PO day 1, then 5 mg/kg/d days 2–5. Pharyngitis (≥2 yr): 12 mg/kg/d PO × 5 days; take susp on empty stomach; tabs OK w/ or w/o food; ↓ w/ CrCl < 0 mL/mg.
W/P: [B, +] May ↑ QTc w/ arrhythmias.
DISP: Tabs 250, 500, 600 mg; Z-Pack (5-day, 250 mg); Tri-Pack (500-mg tabs × 3); susp 2 g; single-dose packet (Zmax) ER susp (2 g); susp 100, 200 mg/5 mL; Inj powder 500 mg; 2.5 mL.
SE: GI upset, met allic taste.
AZTREONAM (AZACTAM)
USES: *Aerobic gram(−) UTIs, lower resp, intra-abdominal, skin, gynecologic infections & septicemia.*
ACTIONS: Monobactam: ↓ Cell wall synth. Spectrum: gram(−) (Pseudomonas, E. coli, Klebsiella, H. influenzae, Serratia, Proteus, Enterobacter, Citrobacter).
DOSE:
Adults: 1–2 g IV/IM q6–12h. UTI: 500 mg–1 g IV q8–12h. Meningitis: 2 g IV q6–8h.
Peds: 90–120 mg/kg/d ÷ q6–8h ↓ in renal impairment.
W/P: [B, +].
DISP: Inj (soln), 1 g, 2 g/50 mL Inj powder for recons 1 g, 2 g.
SE: N/V/diarrhea, rash, pain at Inj site.
NOTES: No gram(+) or anaerobic activity; OK in PCN-allergic pts.