Aluminum hydroxide 320 mg/5 mL oral suspension

640 mg 5-6 times/d after meals and at bedtime x 2 wks

NA

Constipation, hypophosphatemia, anemia, osteomalacia

Increases pH which affects absorption of weak acids (digoxin, phenytoin, isoniazid)

Decreases bioavailability of drugs via adsorption (eg, tetracyclines, fluoroquinolones)

Increases urinary pH, which inhibits excretion of bases (quinidine, amphetamines) and enhances excretion of acidic drugs (salicylates)

Take 1-3 hours after meals

Maintain proper hydration

Magnesium hydroxide

400 mg chewable tablet;

400 mg/5 mL, 1200 mg/15 mL, and 2400 mg/10 mL oral suspension

5-15 mL (2-4 tabs) up to QID

NA

Cathartic colon (chronic abuse), rectal bleeding, tartrazine (FD&C Yellow) sensitivity

Take with full glass of water

Do not use maximum dose longer than 2 wks

Do not use if experiencing abdominal pain, nausea, vomiting

Calcium carbonate 250, 500, 600, 650, 750, 1000, 1250 mg tablets/capsules/chewable tablets; 1250 mg/5 mL oral suspension

1-4 tablets PRN, dosing recommendations vary by product

NA

Tartrazine (FD&C Yellow) sensitivity, GI tract irritation, hypercalcemia, renal calculi

Take with or after meals for best absorption

Take with full glass of water

Avoid excessive use in pregnancy

Bismuth subsalicylate 262 mg caplet/chewable tablet; 262 mg/15 mL, 525 mg/15 mL oral suspension

Bismuth subcitrate potassium

(Pylera)^b

Gas/indigestion/ heartburn/nausea: 2 tablets or 30 mL (524 mg) every 30 min to 1 h, PRN (maximum 8 doses/d)

H pylori

3 capsules (420 mg bismuth subcitrate potassium/375 mg metronidazole/375 mg tetracycline) QID for 10 days with omeprazole 20 mg BID

Nausea and vomiting, fever, tinnitus, fecal impaction

Coadministration with anticoagulants may increase the risk of bleeding

May decrease absorption of tetracyclines

Causes gray-black stool

Potentially toxic if breastfeeding

Cimetidine (Tagamet HB)
200, 300, 400, 800 mg tablet; 300 mg/5 mL oral solution^e

200-400 mg/d

GERD, erosive

1600 mg/d, divided as BID or QID, x 12 wks

Duodenal ulcer

800 mg QHS or

300 mg QID with meals and QHS or

400 mg BID x 8 wks

400 mg QHS (prophylaxis)

Benign Gastric ulcer

800 mg QHS or

300 mg QID with meals and QHS x 8 wks

Headache, gynecomastia

Major CYP inhibitor; increases serum levels and delays elimination of drugs metabolized by CYP, including drugs with narrow therapeutic windows (warfarin, theophylline, phenytoin)

OTC – do not take maximum dose for more than 2 wks

Do not use with other acid reducers

Famotidine (Pepcid, Pepcid AC)
10, 20, 40 mg tablet; 40 mg/5 mL powder for oral suspension^e

10-20 mg/d up to BID as needed (max 40 mg/d)

GERD

20 mg BID x 6 wks

Duodenal ulcer

40 mg QHS x 4-8 wks

20 mg QHS

(maintenance)

Benign Gastric ulcer

40 mg QHS

Headache, dizziness, constipation, diarrhea

No CYP activity

Additive effect with other QT-prolonging drugs

Decreases levels of many drugs via increased gastric pH causing reduced effectiveness (cyclosporine, cefditoren, cefpodoxime, itraconazole, certain ARTs, tyrosine kinase inhibitors)

Nizatidine (Axid)

150, 300 mg capsule;

15 mg/mL oral solution

Rx only

GERD

150 mg BID

Duodenal ulcer

300 mg QHS up to 8 wks

(150 mg BID alternative)

150 mg QHS (maintenance)

Benign Gastric ulcer

300 mg given either as 150 mg BID or 300 mg QHS up to 8 wks

Dizziness, headache

No CYP activity

Absorption decreased by aluminum- and magnesium-containing antacids

Ranitidine (Zantac)

150, 300 mg capsule; 75, 150, 300 mg tablet;

15 mg/mL, 75 mg/5 mL, 150 mg/10 mL oral syrup^e

75-150 mg taken once daily or BID

GERD

150 mg BID x 6 wks

Duodenal/benign gastric ulcer

150 mg BID initial, 150 mg QHS (maintenance)

Rare

No clinical CYP activity

Omeprazole

(Prilosec)

10, 20, 40 mg delayed-release capsule; 2.5, 10 mg powder for delayed-release oral suspension

2 mg/mL oral suspension; 20 mg delayed-release tablet; 20 mg orally disintegrating tablet

20 mg/d

GERD

20 mg/d x 4 wks

Duodenal ulcer

20 mg/d x 4-8 wks

H pylori duodenal ulcer

20-40 mg BID x 2-4 wks

Gastric ulcer

40 mg/d x 4-8 wks

Headache, nausea, vomiting, diarrhea, abdominal pain, flatulence

Antiplatelets: All PPIs have the potential to inhibit conversion of clopidogrel to its active metabolite via CYP 2C19. However, there is no good evidence showing meaningful differences in clinical outcomes.^2,5

Reduced efficacy of drugs that depend on gastric pH, (eg, ketoconazole, ampicillin, iron salts, digoxin, cyanocobalamin)

Drug-lab interaction: false-positive for THC in urine drug test

Can use with antacids

If diarrhea does not improve, rule-out CDI

Take before meals: omeprazole, esomeprazole, lansoprazole

Take without regard to meals: dexlansoprazole, pantoprazole, rabeprazole

Can open and sprinkle over applesauce: dexlansoprazole, esomeprazole, lansoprazole, rabeprazole

Chronic use of PPIs and/or H2RAs can cause decreased absorption of vitamin B₁₂, especially with high doses and in elderly patients. Hypomagnesemia is also possible, but rare.

Pregnancy – most studies have not shown an increased risk for major birth defects; all safe in pregnancy per ACG guideline

Omeprazole/sodium bicarbonate

(Zegerid; Zegerid OTC)

Oral capsule/packet, omeprazole
20, 40 mg/bicarbonate 1100, 1680 mg

20 mg/1100 mg/d

GERD

20 mg/d x 4-8 wks

Duodenal ulcer

20 mg/d x 4 wks

Gastric ulcer

40 mg/d x 4-8 wks

Lansoprazole

(Prevacid)

15, 30 mg delayed-release capsule;

15, 30 mg delayed-release orally disintegrating tablet;

15 mg/d

GERD

15 mg/d x 8 wks

Duodenal ulcer

15 mg/d x 4 wks

15 mg/d

(maintenance)

H pylori duodenal ulcer

30 mg BID x 10-14 days

Gastric ulcer

30 mg/d x 8 wks

NSAID-induced gastric ulcer

30 mg/d x 8 wks (healing)

15 mg/d x 12 wks (risk reduction)

Abdominal pain, nausea, diarrhea, constipation

Esomeprazole

(Nexium; Nexium 24 HR)
20, 40 mg delayed-release oral capsule; 2.5, 5, 10, 20, 40 mg delayed-release powder for oral suspension; 49.3 mg delayed-release capsule^e

20 mg/d

GERD

20 mg/d x 4-8 wks

H pylori eradication

40 mg/d x 10-14 days

NSAID-induced gastric ulcer

20-40 mg/d up to 6 months (risk reduction)

Headache, flatulence, nausea, diarrhea, abdominal pain, dizziness, vertigo, dry mouth

Pantoprazole

(Protonix)
20, 40 mg delayed-release tablet^e

40 mg packet for oral suspension

Rx only

GERD (erosive)

40 mg/d x 8-16 wks

Headache, dizziness, diarrhea, vomiting, arthralgia

Rabeprazole (Aciphex)
20 mg delayed-release tablet

5 and 10 mg capsule sprinkle

Rx only

GERD

20 mg/d x 4-8 wks

Duodenal ulcer

20 mg/d after morning meal x 4 wks

H pylori

20 mg BID with meals x 7 days

Pain, pharyngitis, flatulence, constipation, infection

Dexlansoprazole (Dexilant)
30, 60 mg delayed-release capsule

Rx only

GERD

30 mg/d x 4 wks

Nausea, vomiting, diarrhea, flatulence, upper respiratory tract infection

Amoxicillin (Moxatag, various generics)
Tablet, capsule, chewable tablet, powder for oral suspension

Rx only

1 g BID

All: hypersensitivity reactions, GI, CNS, dermatologic effects

Superinfection possible

CDAD possible

QT prolongation possible with levofloxacin and clarithromycin

Teeth discoloration may occur in children if mother takes tetracycline during last half of pregnancy, or if taken by infants and children up to 8 years of age

Boxed warning for levofloxacin: tendinitis/tendon rupture, peripheral neuropathy, CNS effects, and exacerbation of myasthenia gravis

Decreases effect of oral contraceptives

Pregnancy category B

Do not swallow chewable tablets whole

Store oral suspension at room temperature or refrigerated for 14 days

Clarithromycin (Biaxin)
Tablet, extended-release tablet, powder for oral suspension

500 mg BID

Major CYP3A4 substrate

Weak CYP1A2 inhibitor

Strong CYP3A4 inhibitor

Inhibits P-glycoprotein

Contraindicated with multiple drugs, including QT prolonging drugs

Pregnancy category C

Should not be used in pregnancy except in circumstances when no alternative is appropriateDo not refrigerate reconstituted solution; use within 14 days

Levofloxacin (Levaquin)
Tablet, oral solution, ophthalmic solution^e

500 mg QD

Additive effect with QT-prolonging drugs

Decreased absorption of levofloxacin with concomitant use of antacids

Pregnancy category C

Tetracycline

Oral capsule

500 mg QID

Decreases effect oral contraceptives

Impaired absorption if given with drugs that adsorb tetracycline

Pregnancy category D

 Contraindicated in second and third trimesters

Metronidazole (Flagyl)
Oral capsule, oral tablet, oral suspension, topical cream/gel/lotion, vaginal gel^e

500 mg BID

250 mg QID

Peripheral neuropathy, vaginal candidiasis, GI discomfort

Boxed warning of possible carcinogenesis

Disulfiram reaction with ethanol

Potentiates anticoagulant effect of warfarin

Human data suggest low risk in pregnancy

Avoid alcohol during and for 3 days after therapy

Contraindicated when breastfeeding

Bismuth subsalicylate^g

Refer to antacids section above.

Sucralfate (Carafate)
Oral suspension, tablet

Rx only

Duodenal Ulcer

1 g QID empty stomach

1 g BID (maintenance dose)

Constipation

Bezoars have been reported

Decreased absorption of many drugs

Only minimally absorbed; not likely to increase risks in pregnancy

Misoprostol (Cytotec)
Oral tablet

Ulcer healing

200 mcg QID

Diarrhea

Boxed warning: abortifacient, contraindicated in women of child-bearing potential

Oxytocin,

antacids

Abortifacient and teratogen: follow safe handling procedures

Table 9. Guideline-Recommended Drugs for Ulcerative Colitis and Crohn's Disease^5,14-17*

Drug

Formulation

Induction

Maintenance

Common side effects

Drug interactions

Comments

Sulfasalazine (Azulfidine, Azulfidine EN)

Oral tablet, 500 mg

Delayed-release tablet (EN), 500 mg

UC: 3-4 g/d, divided

CD: 3-6 g/d, divided

UC: 2 g/d

CD: none

Anorexia, gastric pain, headache, nausea, vomiting, reversible oligospermia

Sulfapyridine intolerance results in nausea, vomiting, headache, anorexia

Decreases folate absorption in diet

Minimal hepatic metabolism; extensively metabolized by intestinal tract

Potentiates effect of heparin, LMWH, MTX (hepatotoxicity), prilocaine (methemoglobinemia), Varicella-containing vaccines (Reye's Syndrome)

Decreases concentration of digoxin

Warnings

Irreversible neuromuscular and CNS changes, blood dyscrasias, renal damage, hepatotoxicity, serious infections (eg, pneumonia and sepsis), serious skin reactions, crystalluria, G6PD deficiency at risk for hemolytic anemia, porphyria, oligospermia, hypersensitivity reactions

Mesalamine (Canasa)

Rectal suppository, 1 g

UC: 1 g/d

UC: 1 g/d

Headache, abdominal pain, flatulence, diarrhea, nausea

Inhibits TMPT, which can increase toxicity of AZA and 6-MP

Do not administer antacids, PPIs, H2RAs with formulations with pH-sensitive coatings (Asacol, Lialda, Apriso), which cause early dissolution of coating

Warnings

Worsening of symptoms may occur, including acute intolerance syndrome

Cases of pericarditis, pancolitis, and sulfite sensitivity have been reported

Monitor renal function if pre-existing renal condition

Nephrotoxicity, pancreatitis, hepatotoxicity, and infertility in men have been reported in postmarketing setting

Mesalamine (Rowasa, SF Rowasa)

Rectal enema, 4 g/60 mL

UC: 4 g/d

UC: 2-4 g/d

Mesalamine (Asacol HD)

Delayed-release tablet, 800 mg

UC: 1600 mg TID

UC: Use beyond 6 wks not evaluated

Mesalamine (Apriso)

24-hour extended-release capsule, 0.375 g

None

UC: 1.5 g/d

Mesalamine (Lialda)

Delayed-release tablet, 1.2 g

UC: 2.4 g or 4.8 g/d

UC: 2.4 g/d

Mesalamine (Pentasa)

Extended-release capsule, 250 mg, 500 mg

UC: 1 g QID

UC: Use beyond 8 wks not evaluated

Mesalamine (Delzicol)

Delayed-release capsule, 400 mg

UC: 800 mg TID

UC: 1.6 g/d, divided

Olsalazine (Dipentum)

Oral capsule, 250 mg

UC: 1.5-3 g/d in 2 divided doses

UC: 500 mg BID

Diarrhea, rash, abdominal pain, headache

Increased PT with warfarin

Warnings

Dose-related diarrhea, exacerbation of symptoms, renal tubular damage, carcinogenesis

Balsalazide (Colazal, Giazo)

Oral capsule, 750 mg (Colazal) Oral tablet, 1.1 g (Giazo)

UC: Capsule: 2.25 g TID

Tablet: 3.3 g BID

UC: capsule: use beyond 12 wks has not been evaluated

Tablet: use beyond 8 wks not evaluated

Headache, abdominal pain, diarrhea, nausea, arthralgia, respiratory tract infection, vomiting

Same as mesalamine

Therapeutically active form is mesalamine

Warnings

Renal toxicity and hypersensitivity reactions, exacerbation of UC, pyloric stenosis, hepatic function impairment

Hydrocortisone rectal topical (Colocort, Cortenema, Cortifoam)

Rectal enema, 100 mg/60 mL

10% foam, 90 mg (Cortifoam)

UC: Enema: 1 enema QHS

Foam: 1 applicator full once or twice daily

Not recommended for chronic use

Burning, itching, irritation, dryness, allergic contact dermatitis, secondary infection

Lack of antibody response or neurological complications with vaccination

Warnings

Rectal wall damage possible with improper administration technique, signs of infection may be masked, ocular effects, BP elevation, electrolyte abnormalities, viral infections, reactivation of TB, psychiatric effects, secondary adrenal insufficiency

Budesonide

(Enterocort EC, Uceris)

24-hour extended-release capsule, 3 mg (Entocort EC)

Extended-release tablet, 9 mg (Uceris)

CD & UC: 9 mg/d

UC: Not recommended for chronic use

CD:

Capsules: 6 mg/d, not recommended beyond 4 months

Budesonide rectal

(Uceris)

2 mg/actuation rectal foam

UC: 2 mg BID x 2 wks

UC: 2 mg/d x 4 wks

Prednisone

(Rayos)

Oral tablet, 1 mg, 2.5 mg, 5 mg, 10 mg, 20 mg, 50 mg

Delayed-release tablet: 1 mg, 2 mg, 5 mg

UC & CD: 40-60 mg/d

Not recommended for chronic use

Azathioprine (Imuran, Azasan)

Oral tablet, 50 mg, 75 mg, 100 mg

Not used in induction due to slow onset of action

UC: 1.5-2.5 mg/kg/d

CD: 2-2.5 mg/kg/d

Myelosuppression, nausea, vomiting, diarrhea, hepatotoxicity, rash, pulmonary edema, pancreatitis, hypersensitivity

Increases effect of warfarin

XO inhibitors (allopurinol, febuxostat) may inhibit metabolism of AZA and 6-MP, leading to bone marrow suppression; dose reduction of AZA/6-MP may be necessary

Coadministration with ACEI or TMP/SMX may cause severe leukopenia

Hazardous agent handling precautions

Boxed warning

Increased risk for developing malignancy (skin cancer and lymphoma)

Other warnings: serious infection, hematologic effects, GI hypersensitivity, caution in renal/hepatic insufficiency

Mercaptopurine (Purinethol)

Oral tablet, 50 mg

UC: Not used in induction due to slow onset of action

UC: 1-1.5 mg/kg/d

CD: 0.75-1.5 mg/kg/d

Methotrexate (Otrexup, Rasuvo)

10 mg, 12.5 mg, 15 mg, 17.5 mg, 20 mg, 22.5 mg, 25 mg/ 0.4 mL SC autoinjector (Otrexup)

7.5 mg, 10 mg, 12.5 mg, 15 mg, 17.5 mg, 20 mg, 22.5 mg, 25 mg, 27.5 mg, 30 mg SC autoinjector (supplied as 50 mg/mL)

25 mg/mL vials for injection

CD: 15-25 mg IM or SC once wkly

CD: 15-25 mg IM or SC once wkly

Myelosuppression, vomiting, diarrhea, hepatotoxicity, hypotension, blurred vision, headache, nephropathy, hyperuricemia, serious skin reactions, stomatitis, interstitial pneumonia

Coadministration with NSAIDs and salicylates may increase methotrexate toxicity

TMP/SMX and other folate-related drugs may increase risk for bone marrow suppression

Potential for increased hepatotoxicity when administered with other hepatotoxic drugs

Hazardous agent handling precautions

Boxed warning

Associated with severe toxic reactions (eg, myelosuppression, GI toxicity, hepatotoxicity, lung disease) and embryo-fetal toxicity and death

Other warnings: drug elimination impaired with renal dysfunction, ascites, or pleural effusions; non-Hodgkin’s lymphoma and other tumors have been reported with low-dose oral use

Supplementation with folic acid can help reduce toxicity

Cyclosporine (Sandimmune)

50 mg/mL ampules, IV

UC: 2-4 mg/kg daily

Not recommended for chronic use

Nephrotoxicity, increased risk for infection, diarrhea, nausea, vomiting, headache, tremors, hypertension, hepatotoxicity, paresthesias

Increased risk of nephrotoxicity with other nephrotoxic drugs

Concurrent use with potassium-sparing diuretics increases the risk of hyperkalemia

Use with CYP3A4 inhibitors can increase toxicity

Hazardous agent handling precautions

Has boxed warning regarding its use in organ transplant patients

Other warnings: Increased risk of hepatotoxicity and nephrotoxicity with high doses, increased risk for lymphomas or other malignancies, increased risk for serious infections

Adalimumab (Humira)

10 mg/0.1 mL, 0.2 mL SC

20 mg/0.2 mL, 0.4 mL SC

40 mg/0.4 mL, 0.8 mL SC

80 mg/0.8 mL SC

CD & UC: 160 mg wk 0, 80 mg wk 2

CD & UC: 40 mg every other wk, starting at wk 4

Injection site reactions

Enhances neutropenic effect of other immunosuppressants

Enhances toxic effect of live vaccines

Diminishes therapeutic effect of inactivated vaccines

Boxed warnings

Increased risk of serious infections, including active TB, invasive fungal infections, and opportunistic infections

Malignancy

Warnings

CNS demyelinating disease

Pancytopenia

Worsening of CHF

Hypersensitivity

Autoimmunity

Certolizumab (Cimzia)

200 mg/mL SC

CD: 400 mg at wk 0, 2, 4

CD: 400 mg every 4 wks

URI, rash, UTI

Golimumab (Simponi)

50 mg/0.5 mL SC

100 mg/mL SC

UC: 200 mg at wk 0 and 2

UC: 100 mg every 4 wks

URI, injection site reaction

Infliximab (Remicade, Renflexis, Inflectra)

100 mg reconstituted IV solution

CD & UC: 5 mg/kg IV at wk 0, 2, 6

CD & UC : 5 mg/kg IV every 8 wks

Infusion reactions (dyspnea, flushing, headache, rash)

Natalizumab (Tysabri)

300 mg/15 mL injection solution

CD: 300 mg IV every 4 wks

CD: 300 mg IV every 4 wks

Headache, fatigue, URI, nausea

Boxed warning

Increased risk of opportunistic viral infection of brain, progressive multifocal leukoencephalopathy, leading to potential death or severe disability

REMS

TOUCH program, both patient and prescriber must be enrolled prior to dispensing

Warnings

Herpes encephalitis/

meningitis

Hepatotoxicity

Immunogenicity

Hypersensitivity

Vedolizumab (Entyvio)

300 mg reconstituted IV solution

CD & UC: 300 mg at wk 0, 2, 6

CD & UC : 300 mg every 8 wks

Infusion reactions (dyspnea, flushing, headache, rash)

Warnings

Infusion-related reactions and hypersensitivity

Increased risk for infections

Ustekinumab (Stelara)

45 mg/0.5 mL SC

90 mg/mL SC

130 mg/26 mL IV vial

CD: single IV infusion, dose weight-dependent (260 mg, 390 mg, or 520 mg)

CD: 90 mg SC every 8 wks

Vomiting, nasopharyngitis, injection site reactions, interstitial pneumonia

Warnings

Hypersensitivity reactions

Increased risk for infections

Malignancies

Noninfectious pneumonia

Tofacitinib (Xeljanz)

5 mg, 10 mg tablets

UC: 10 mg BID for at least 8 wks

UC: 5-10 mg BID

Nasopharyngitis, URI, elevated cholesterol levels, diarrhea

Dose adjustments recommended for patients receiving strong CYP3A4 inhibitors or moderate CYP3A4 inhibitor with a strong CYP2C19 inhibitor

Boxed warnings

Increased risk of serious infections, including active TB, invasive fungal infections, and opportunistic infections

Malignancy

Warnings

Gastrointestinal perforations

Dose adjustments recommended for moderate to severe renal impairment, moderate hepatic impairment, and in those with lymphopenia, neutropenia, or anemia

Table 11. Approved Agents for Hepatitis B Virus^5,21,22

Usual dosing

Dosage adjustment

Common side effects/warnings

Drug interactions

Monitoring

Comments^a

Preferred immunomodulators

PEG IFN alfa-2a (Pegasys)

180 mcg SC once wkly

Dose adjustment when CrCl < 30 mL/min or if neutropenia, thrombocytopenia, increased ALT or depression develops

Contraindicated in hepatic decompensation (Child-Pugh B or C) in cirrhotic patients

Hypertension, neuropsychiatric reactions, bone marrow suppression, autoimmune exacerbation, ocular effects, cerebrovascular events, hepatitis B exacerbations, pulmonary effects, pancreatitis, fertility impairment, flu-like symptoms

Combinations with NRTIs may cause hematologic toxicity

Increased methadone and theophylline levels

Baseline:

Standard hematological and biochemical laboratory tests, including CrCl, and an eye examination

Pregnancy screening

Electrocardiograms for patients with preexisting cardiac disease

During therapy:

Hematological/biochemical tests

TSH

Evidence of psychiatric symptoms

Signs/symptoms of toxicity

Administer in abdomen or thigh

Do not shake

Do not leave outside of refrigerator for

> 24 hours

Protect from light

Pregnancy category C

Preferred antivirals [nucleot(s)ide analogs]

Entecavir (Baraclude)

0.5 mg once daily

1 mg once daily^b

Dose adjustment when CrCl < 50 mL/min

Dizziness, fatigue, headache, nausea, ALT elevation associated with VL reduction

Boxed warning

Severe acute exacerbation of HBV may occur if entecavir discontinued

Treatment for HIV/HBV coinfection not recommended due to resistance

Lactic acidosis and hepatomegaly have been reported

Increased levels of entecavir if coadministered with drugs competing for renal tubular secretion, or drugs that reduce renal function

Hepatic function, periodically

Adverse reactions when administered with drugs affecting renal function

Take on an empty stomach 2 hours after a meal and 2 hours before the next meal

Pregnancy category C

Tenofovir disoproxil fumarate (Viread)

300 mg once daily

Dose adjustment when CrCl < 50 mL/min

Fanconi syndrome,

osteomalacia, decreased bone density, renal insufficiency

Boxed warning

Severe acute exacerbation of HBV may occur if tenofovir discontinued

Lactic acidosis and hepatomegaly have been reported

Weak CYP1A2 inhibitor

P-glycoprotein inducer

HIV status

Bone density

Urine SCr, glucose, protein

LFTs

Take with or without food

Pregnancy category B

Tenofovir alafenamide (Vemlidy)

25 mg once daily

No dose adjustment required for renal or hepatic impairment (not recommended in decompensated (Child-Pugh B or C) hepatic dysfunction or in patients with CrCl < 15 mL/min who are not receiving dialysis)

Lactic acidosis, headache

Boxed warning

Severe acute exacerbation of HBV may occur if tenofovir discontinued

Drugs that strongly affect P-gp and BCRP are likely to change absorption of tenofovir

HIV status

Renal function; urine SCr, glucose, protein

Take with food

No adequate human data on pregnancy available

Nonpreferred antivirals (due to higher likelihood of failing therapy and developing a drug-resistant virus)

Lamivudine (Epivir)

100 mg once daily

Dose adjustment when CrCl < 50 mL/min

Well-tolerated;

reports of myopathy, peripheral neuropathy

Boxed warning

Severe acute exacerbation of HBV may occur if lamivudine discontinued

Lamivudine-containing products have lower dose for HBV than HIV

Lactic acidosis and hepatomegaly have been reported

Pancreatitis

Enhances effect/toxicity of emtricitabine and ganciclovir/valganciclovir

Enhances hepatotoxicity of ribavirin

Decreases excretion of trimethoprim

Hematologic labs

Signs/symptoms of pancreatitis

Amylase, bilirubin, LFTs

HIV

Take without regard to meals

Pregnancy category C

Adefovir (Hepsera)

10 mg once daily

Extend dosing interval when CrCl < 50 mL/min

Boxed warning

Severe acute exacerbation of HBV may occur if adefovir discontinued

HIV resistance may develop in patients with HBV/HIV coinfection not being treated for HIV

Lactic acidosis and hepatomegaly have been reported

Nephrotoxicity may occur in patients with underlying renal dysfunction

Fanconi syndrome

Nephrogenic diabetes insipidus

Increased concentration if coadministered with nephrotoxic drugs or drugs that competitively inhibit renal tubular secretion

Renal function; urine SCr, glucose, protein

HIV

Take with or without food

Pregnancy category C

Table 12. Approved Agents for Hepatitis C Virus⁵

Usual dosing

Dosage adjustment

Side effects

Drug interactions

Monitoring

Comments

Daclatasvir (Daklinza)

60 mg once daily

Strong CYP3A inhibitors: reduce dose to 30 mg once daily

Moderate CYP3A inducers: increase dose to 90 mg once daily

Bradycardia, fatigue, headache, diarrhea, nausea

Substrate of CYP3A4, P-glycoprotein; refer to product labeling for specific information

Symptomatic bradycardia can develop when used with amiodarone and sofosbuvir

Boxed warning: test for presence of HBV prior to initiating therapy

Liver enzymes at baseline and periodically when indicated thereafter

Consider testing for NS5A resistance prior to use in genotype 1a patients

Do not use as monotherapy; use only in combination with sofosbuvir

Approved for use in genotype 1 or 3 infection; duration of therapy 12 wks

Administer with or without food

Elbasvir; grazoprevir (Zepatier)

1 tablet once daily

None

Fatigue, headache, nausea, and anemia

ALT elevations; changes have been mostly asymptomatic and resolved with ongoing or completed therapy

Substrate of OATP1B1/3, CYP3A and P-gp; refer to product labeling for specific information

Boxed warning: test for presence of HBV prior to initiating therapy

Hepatic function: monitor at baseline, treatment wk 8, and wk 12 (if treatment duration is 16 wks) and as clinically indicated

Test for NS5A resistance prior to use in genotype 1a patients

May be used in combination with ribavirin in some patients

Approved for use in genotype 1 or 4 infection; duration of therapy 12 or 16 wks

Administer without regard to meals

Contraindicated in moderate or severe hepatic impairment

Glecaprevir/ pibrentasvir (Mavyret)

3 tablets once daily

None

Headache, fatigue, nausea

Substrate of OATP1B1/3, BCRP, and P-gp; refer to product labeling for specific information

Boxed warning: test for presence of HBV prior to initiating therapy

Liver enzymes at baseline and periodically when indicated thereafter

Approved for use in genotypes 1, 2, 3, 4, 5 and 6 infection; duration of therapy 8, 12, or 16 wks

Administer with food

Contraindicated in severe hepatic impairment (not recommended with moderate impairment)

Ledipasvir; sofosbuvir

(Harvoni)

1 tablet once daily

None

Fatigue, headache, insomnia, diarrhea, nausea, increased lipase

Substrate of BCRP and P-gp; refer to product labeling for specific information

Symptomatic bradycardia can develop when used with amiodarone

Boxed warning: test for presence of HBV prior to initiating therapy

Bilirubin, liver enzymes, lipase, and serum creatinine at baseline and periodically when indicated

May be used with ribavirin in some patients

Approved for use in genotype 1, 4, 5, or 6 infection; duration of therapy 12 or 24 wks

Administer with or without food

Ombitasvir; paritaprevir; ritonavir; dasabuvir

(Viekira Pak)

2 ombitasvir, paritaprevir, ritonavir fixed-dose tablets every morning

1 tablet twice daily of dasabuvir

None

Fatigue, headache, insomnia, pruritus, diarrhea, nausea, decreased hemoglobin, muscle spasm, weakness, cough, hepatic effects

Inhibitor of UGT1A1, CYP3A4, OATP1B1/3, and BCRP; refer to product labeling for specific information

Concurrent use of several medications is contraindicated with Viekira Pak; see product labeling for complete list

Boxed warning: test for presence of HBV prior to initiating therapy

Baseline hepatic function tests and for the first 4 wks of therapy, then periodically during therapy

May be used in combination with ribavirin

Approved for use in genotype 1 infection; duration of therapy 12 or 24 wks

Contraindicated in moderate to severe hepatic impairment

Administer with a meal

Sofosbuvir (Sovaldi)

400 mg once daily

Dose reduction is not recommended

Chills, fatigue, headache, insomnia, irritability, pruritis, skin rash, diarrhea, nausea, decreased appetite, decreased neutrophils, thrombocytopenia, anemia, fever, myalgia, flu-like symptoms

Substrate of BCRP and P-gp; refer to product labeling for specific information

Symptomatic bradycardia can develop when used with amiodarone

Boxed warning: test for presence of HBV prior to initiating therapy

Bilirubin, liver enzymes, and serum creatinine at baseline and periodically when indicated

Use only in combination with ribavirin or in combination with pegylated interferon and ribavirin

Approved for use in genotype 1, 2, 3, or 4 infection and in patients with hepatocellular carcinoma patients awaiting transplantation; duration of therapy 12, 24, or 48 wks

Administer with or without food

Sofosbuvir/ velpatasvir (Epclusa)

1 tablet once daily

None

Headache, fatigue, nausea, asthenia, insomnia, diarrhea

Substrate of BCRP and P-gp; refer to product labeling for specific information

Symptomatic bradycardia can develop when used with amiodarone

Boxed warning: test for presence of HBV prior to initiating therapy

Baseline hepatic function tests and as clinically indicated

May be used in combination with ribavirin

Approved for use in genotype 1, 2, 3, 4, 5, or 6; duration of therapy 12 wks

Administer with or without food

Sofosbuvir/ velpatasvir/ voxilaprevir (Vosevi)

1 tablet once daily

None

Headache, fatigue, diarrhea, nausea, asthenia, insomnia

Substrate of BCRP,P-gp, and OATP1B1/3; refer to product labeling for specific information

Symptomatic bradycardia can develop when used with amiodarone

Boxed warning: test for presence of HBV prior to initiating therapy

Baseline hepatic function tests and as clinically indicated

Approved for use in genotype 1, 2, 3, 4, 5, or 6; duration of therapy 12 wks

Administer with food

Not recommender in moderate or severe hepatic impairment