tenofovir

REMS

HIV infection (with other antiretrovirals).
Chronic hepatitis B.

Contraindicated in:

Hypersensitivity
Concurrent use of antiretroviral combination products containing tenofovir
Concurrent or recent use of NSAIDs (↑ risk of acute renal failure)
Lactation: HIV-infected women should not breast feed.

Use Cautiously in:

Co-infection with HIV and chronic hepatitis B
Obesity, women, prolonged nucleoside exposure (may be risk factors for lactic acidosis/hepatomegaly)
Renal impairment (↑ dosing interval if CCr <50 mL/min)
History of pathologic bone fractures or at risk for osteopenia
OB: Has been used safely
Pedi: Children <2 yr (safety not established).

CNS: depression, headache, weakness.

Endo: fat redistibution.

GI: HEPATOMEGALY, (with steatosis), diarrhea, nausea, abdominal pain, anorexia, vomiting, flatulence.

GU: ACUTE RENAL FAILURE/FANCONI SYNDROME, proximal renal tubulopathy, renal impairment.

F and E: LACTIC ACIDOSIS, hypophosphatemia.

Derm: rash.

MS: bone pain, ↓ bone mineral density, muscle pain, osteomalacia.

Misc: immune reconstitution syndrome.

Drug-Drug:

May ↑ didanosine levels; ↓ didanosine dose.
Blood levels may be ↑ by cidofovir, acyclovir, ganciclovir, or valganciclovir.
Risk of renal toxicity ↑ by other nephrotoxic agents.
Combination therapy with atazanavir may lead to ↓ virologic response and possible resistance to atazanavir (small amounts of ritonavir may be added to boost blood levels); may also ↑ tenofovir levels.
Lopinavir/ritonavir may ↑ levels.
Concurrent use with adefovir for chronic hepatitis B infection should be avoided.
Concurrent use with NSAIDs may ↑ risk of acute renal failure

Tablets: 150 mg; 200 mg; 250 mg; 300 mg;
Oral powder: 40 mg/scoop;
In combination with: emtricitabine (Truvada); emtricitabine and rilpivirine (Complera); efavirenz and emtricitabine (Atripla); elvitegravir, cobicistat, and emtricitabine (Stribild). See Appendix [not included in this PDA edition].

HIV

PO (Adults and Children 12 yr and 35 kg): 300 mg once daily.

Renal Impairment

PO (Adults): CCr 30–49 mL/min — 300 mg every 48 hr; CCr 10–29 mL/min — 300 mg every 72–96 hr; Hemodialysis — 300 mg every 7 days following dialysis.
PO (Children 2–11 yr and 17 kg): Tablets:35 kg — 300 mg once daily; 28–34.9 kg — 250 mg once daily; 22–27.9 kg — 200 mg once daily; 17–21.9 kg — 150 mg once daily;.
PO (Children 2–11 yr): Oral Powder:35 kg — 7.5 scoops (300 mg) once daily; 34–34.9 kg — 7 scoops (280 mg) once daily; 32–33.9 kg — 6.5 scoops (260 mg) once daily; 29–31.9 kg — 6 scoops (240 mg) once daily; 27–28.9 kg — 5.5 scoops (220 mg) once daily; 24–26.9 kg — 5 scoops (200 mg) once daily; 22–23.9 kg — 4.5 scoops (180 mg) once daily; 19–21.9 kg — 4 scoops (160 mg) once daily; 17–18.9 kg — 3.5 scoops (140 mg) once daily; 14–16.9 kg — 3 scoops (120 mg) once daily; 12–13.9 kg — 2.5 scoops (100 mg) once daily; 10–11.9 kg — 2 scoops (80 mg) once daily;.

Chronic Hepatitis B

PO (Adults and Children 12 yr and 35 kg): 300 mg once daily.

Renal Impairment

PO (Adults): CCr 30–49 mL/min — 300 mg every 48 hr; CCr 10–29 mL/min — 300 mg every 72–96 hr; Hemodialysis — 300 mg every 7 days following dialysis.

Active drug (tenofovir) is phosphorylated intracellularly; tenofovir diphosphate inhibits HIV reverse transcriptase resulting in disruption of DNA synthesis.

Therapeutic Effects:

Slowed progression of HIV infection and decreased occurrence of sequelae.
Increased CD4 cell count and decreased viral load.
Decreased progression/sequelae of chronic hepatitis B infection.

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: nucleoside reverse transcriptase inhibitors

Absorption: Tenofovir disoproxil fumarate is a prodrug, which is split into tenofovir, the active component.

Distribution: Absorption is enhanced by food.

Metabolism/Excretion: 70–80% excreted unchanged in urine by glomerular filtration and active tubular secretion.

Half-life: Unknown.

(blood levels)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2 hr*	24 hr

*When taken with food.

Instruct patient on the importance of taking tenofovir as directed, even if feeling better. Do not take more than prescribed amount and do not stop taking without consulting health care professional. Discontinuing therapy may lead to severe exacerbations. Take missed doses as soon as remembered unless almost time for next dose; do not double doses. Caution patient not to share or trade this medication with others.
Inform patient that tenofovir may cause hyperglycemia. Advise patient to notify health care professional if increased thirst or hunger; unexplained weight loss; increased urination; fatigue; or dry, itchy skin occurs.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Caution patient to avoid crowds and persons with known infections.
Inform patient that tenofovir does not cure AIDS and does not reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to use a condom and avoid sharing needles or donating blood to prevent spreading HIV to others.
Advise patient to notify health care professional immediately if symptoms of lactic acidosis (nausea, vomiting, unusual or unexpected stomach discomfort, and weakness) or signs of Immune Reconstitution Syndrome (signs and symptoms of an infection) occur.
Inform patient that changes in body fat distribution (increased fat in upper back and neck, breast, and trunk, and loss of fat from legs, arms, and face) may occur, but may not be related to drug therapy.
Rep: Advise patient taking oral contraceptives to use a nonhormonal method of birth control during tenofovir therapy. If pregnancy is suspected notify health care professional promptly. Encourage pregnant women to enroll in the Antiretroviral Pregnancy Registry by calling 1–800–258–4263. Advise female patient to avoid breast feeding during therapy.
Emphasize the importance of regular exams to monitor for side effects.

NDC Code^*

0904- Major Pharmaceuticals
0904-6821- tenofovir disproxil fumarate 0904-6821-04- 30 BLISTER PACK in 1 CARTON (0904-6821-04) > 1 TABLET in 1 BLISTER PACK

33342- Macleods Pharmaceuticals Limited
33342-096- tenofovir disproxil fumarate 33342-096-07- 30 TABLET in 1 BOTTLE (33342-096-07)

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