dolutegravir (Rx)

Brand and Other Names:Tivicay, Tivicay PD
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet (Ticivay)

  • 10mg
  • 25mg
  • 50mg

HIV Infection

Indicated in combination with other ARTs

  • Integrase strand transfer inhibitor (INSTI) indicated in patients who weigh ≥30 kg
  • Treatment-naïve or treatment-experienced INSTI-naïve: 50 mg PO qDay
  • INSTI-experienced with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance: 50 mg PO BID

Indicated in combination with rilpivirine

  • To replace the current ART regimen in virologically suppressed patients (HIV-1 RNA <50 copies/mL) on a stable ART regimen ≥6 months with no history of treatment failure or known substitutions associated with resistance to dolutegravir or rilpivirine
  • 50 mg PO qDay

Dosage Modifications

Coadministration with potent UGT1A or CYP3A inducers

  • Treatment-naïve or treatment-experienced INSTI-naïve
  • Potent UGT1A/CYP3A inducers (eg, efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, rifampin)
  • Increase dose to 50 mg PO BID

Hepatic impairment

  • Mild-to-moderate hepatic impairment (Child-Pugh A or B): No dosage adjustment required
  • Severe hepatic impairment (Child-Pugh C): Not recommended

Renal impairment

  • Plasma concentrations were decreased in subjects with severe renal impairment
  • No dosage adjustment required for treatment-naïve or treatment-experienced and INSTI-naïve patients with mild, moderate, or severe renal impairment or for INSTI-experienced patients (with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance) with mild or moderate renal impairment
  • Severe renal impairment in for INSTI-experienced patients with resistance: Not recommended; decrease in dolutegravir concentrations may result in loss of therapeutic effect and development of resistance

Dosing Considerations

Dosage forms (ie, Ticivay, Ticivay PD) are not bioequivalent or interchangeable

Poor virologic response was observed in subjects treated with TIVICAY 50 mg BID with an INSTI-resistance Q148 substitution plus 2 or more additional INSTI-resistance substitutions, including L74I/M, E138A/D/K/T, G140A/S, Y143H/R, E157Q, G163E/K/Q/R/S, or G193E/R

In patients with underlying hepatitis B or C, measure hepatic enzymes before initiating therapy and periodically thereafter

Perform pregnancy testing before initiation in females of childbearing potential

Dosage Forms & Strengths

tablet (Tivicay)

  • 10mg
  • 25mg
  • 50mg

tablet for oral suspension (Tivicay PD)

  • 5mg

HIV Infection

Indicated in combination with other ARTs for treatment-naïve or treatment-experienced, but INSTI-naïve children aged ≥4 weeks who weigh ≥3 kg

Weight 3 to <14 kg

  • Tablets for oral suspension
  • 3 to <6 kg: 5 mg PO qDay
  • 6 to <10 kg: 15 mg PO qDay
  • 10 to <14 kg: 20 mg qDay

Weight ≥14 kg

  • Tablets for oral suspension
    • 14 to <20 kg: 25 mg PO qDay
    • ≥20 kg: 30 mg PO qDay
  • Tablets
    • 14 to <20 kg: 40 mg PO qDay
    • ≥20 kg: 50 mg PO qDay

Dosage Modifications

Coadministration with potent UGT1A or CYP3A inducers (eg, efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, rifampin): Increase weight-based dose to twice daily

Dosing Considerations

Dosage forms (ie, Ticivay, Ticivay PD) are not bioequivalent or interchangeable

Perform pregnancy testing before initiation of dolutegravir in females of childbearing potential

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Interactions

Interaction Checker

and dolutegravir

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      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (1)

            • dofetilide

              dolutegravir will increase the level or effect of dofetilide by decreasing renal clearance. Contraindicated. Dolutegravir inhibits the renal organic cation transporter, OCT2; risk of life-threatening arrhythmias caused by increased systemic exposure to dofetilide

            Serious - Use Alternative (19)

            • aluminum hydroxide/magnesium carbonate

              aluminum hydroxide/magnesium carbonate will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations

            • cabotegravir

              dolutegravir, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • carbamazepine

              carbamazepine will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment

            • efavirenz

              efavirenz will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Increase dolutegravir dose to 50 mg BID when coadministered with strong UGT1A/CYP3A inducers

            • etravirine

              etravirine will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Etravirine (a strong UGT1A/CYP3A inducer) significantly reduces dolutegravir plasma concentrations, but the effect of etravirine is mitigated by coadministration of lopinavir/ritonavir or darunavir/ritonavir, and is expected to be mitigated by atazanavir/ritonavir; do not use with etravirine without coadministration of atazanavir/ritonavir, darunavir/ritonavir, or lopinavir/ritonavir

            • fosamprenavir

              fosamprenavir will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Increase dolutegravir dose to 50 mg BID when coadministered with strong UGT1A/CYP3A inducers (eg, fosamprenavir/ritonavir)

            • fosphenytoin

              fosphenytoin will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment

            • magnesium citrate

              magnesium citrate will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations

            • magnesium gluconate

              magnesium gluconate will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations

            • magnesium oxide

              magnesium oxide will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations

            • nevirapine

              nevirapine will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment

            • oxcarbazepine

              oxcarbazepine will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment

            • phenobarbital

              phenobarbital will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment

            • phenytoin

              phenytoin will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment

            • Prussian blue

              Prussian blue will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations

            • rifampin

              rifampin will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Increase dolutegravir dose to 50 mg BID when coadministered with strong UGT1A/CYP3A inducers

            • St John's Wort

              St John's Wort will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Avoid coadministration; insufficient data to recommend dosage adjustment

            • sucralfate

              sucralfate will decrease the level or effect of dolutegravir by cation binding in GI tract. Avoid or Use Alternate Drug. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations

            • tipranavir

              tipranavir will decrease the level or effect of dolutegravir by increasing metabolism. Avoid or Use Alternate Drug. Increase dolutegravir dose to 50 mg BID when coadministered with strong UGT1A/CYP3A inducers (eg, tipranavir/ritonavir)

            Monitor Closely (19)

            • aluminum hydroxide

              aluminum hydroxide will decrease the level or effect of dolutegravir by cation binding in GI tract. Use Caution/Monitor. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations; use alternative therapy if available

            • calcium acetate

              calcium acetate will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.

            • calcium carbonate

              calcium carbonate will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.

            • calcium citrate

              calcium citrate will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.

            • dalfampridine

              dolutegravir will increase the level or effect of dalfampridine by Other (see comment). Modify Therapy/Monitor Closely. dolutegravir inhibits OCT2 and multidrug and toxin extrusion transporter 1

            • eslicarbazepine acetate

              eslicarbazepine acetate will decrease the level or effect of dolutegravir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dose of dolutegravir to 50 mg PO q12hr for treatment naïve or treatment experienced INSTI-naïve.

            • ferric maltol

              ferric maltol will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.

            • ferrous fumarate

              ferrous fumarate will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.

            • ferrous gluconate

              ferrous gluconate will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.

            • ferrous sulfate

              ferrous sulfate will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.

            • magnesium hydroxide

              magnesium hydroxide will decrease the level or effect of dolutegravir by cation binding in GI tract. Use Caution/Monitor. Administer dolutegravir 2 hr before or 6 hr after taking medications containing polyvalent cations; use alternative therapy if available

            • magnesium supplement

              magnesium supplement will decrease the level or effect of dolutegravir by Other (see comment). Modify Therapy/Monitor Closely. Drug may form a chelate with polyvalent cations; may decrease absorption by the intestinal tract; applies to oral forms; may administer under fasting conditions 2 hr before administering polyvalent cation or 6 hr after

            • metformin

              dolutegravir will increase the level or effect of metformin by decreasing renal clearance. Modify Therapy/Monitor Closely. Dolutegravir inhibits the renal organic cation transporter, OCT2; when used with metformin, limit total daily dose of metformin to 1,000 mg either when starting metformin or dolutegravir; when stopping dolutegravir, adjustment of metformin dose may be necessary; monitor blood glucose when initiating concomitant use and after withdrawal of dolutegravir

            • multivitamins

              multivitamins will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.

            • multivitamins, vision

              multivitamins, vision will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir 2 hr (dolutegravir or abacavir/dolutegravir/lamivudine) or 4 hr (dolutegravir/rilpivirine) before or 6 hr after taking medications containing polyvalent cations.

            • orlistat

              orlistat will decrease the level or effect of dolutegravir by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Loss of virological control reported in HIV-infected patients taking orlistat concomitantly. Exact mechanism is unclear, but may include a drug-drug interaction that inhibits systemic absorption of the antiretroviral drug. Monitor HIV RNA levels frequently and if increased HIV viral load confirmed, discontinue orlistat.

            • selenium

              selenium will decrease the level or effect of dolutegravir by cation binding in GI tract. Modify Therapy/Monitor Closely. Administer dolutegravir at least 2 h before or 6 h after polyvalent cations. Administer the dolutegravir/rilpivirine combination at least 4 h before or 6 h after polyvalent cations.

            • sodium sulfate/?magnesium sulfate/potassium chloride

              sodium sulfate/?magnesium sulfate/potassium chloride decreases levels of dolutegravir by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Administer dolutegravir at least 2 hr before or 6 hr after each dose to avoid chelation with magnesium. .

            • sodium sulfate/potassium sulfate/magnesium sulfate

              sodium sulfate/potassium sulfate/magnesium sulfate decreases levels of dolutegravir by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Administer dolutegravir at least 2 hr before or 6 hr after each dose to avoid chelation with magnesium. .

            Minor (0)

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              Adverse Effects

              >10%

              Increased cholesterol and triglycerides (up to 17%)

              1-10%

              Increased lipase (1-8%)

              Hyperglycemia (<1-7%)

              Increased creatinine kinase (3-4%)

              Increased AST (2-3%)

              Insomnia (<1-3%)

              Increased ALT (2%)

              Increased bilirubin (<1-2%)

              Headache (<1-2%)

              GI disorders (<2%)

              Fatigue (<2%)

              Hepatitis (<2%)

              Myositis (<2%)

              Renal impairment (<2%)

              Pruritus (<2%)

              Nausea (<1-1%)

              <1%

              Abnormal dreams

              Dizziness

              Diarrhea

              Rash

              Vertigo

              Postmarketing Reports

              Arthralgia

              Myalgia

              Hepatobiliary

              Disorders

              Acute liver failure, hepatotoxicity

              Musculoskeletal

              Psychiatric

              Anxiety

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              Warnings

              Contraindications

              Documented hypersensitivity

              Coadministration with dofetilide due to the potential for increased dofetilide plasma concentrations and the risk for serious and/or life-threatening events

              Cautions

              Hypersensitivity reactions reported; characterized by rash, constitutional findings, and sometimes organ dysfunction, including liver injury (see Contraindications)

              Hepatic adverse events reported; patients with underlying hepatitis B or C may be at increased risk for worsening or development of transaminase elevations; in some cases, transaminase elevations were consistent with immune reconstitution syndrome or hepatitis B reactivation particularly in the setting where antihepatitis therapy was withdrawn

              Hepatic toxicity, including elevated serum liver biochemistries, hepatitis, and acute liver failure reported without pre-existing hepatic disease or other identifiable risk factors; drug-induced liver injury leading to liver transplant reported; monitoring for hepatotoxicity recommended

              Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy; may develop an inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium infection, cytomegalovirus, Pneumocystis jiroveci pneumonia [PCP], or tuberculosis) or autoimmune disorders (eg, Graves disease, polymyositis, and Guillain-Barré syndrome)

              Dosage forms (ie, tablets and tablets for oral suspension) are not bioequivalent and are not interchangeable on a mg-per-mg basis; if a pediatric patient switches from one formulation to the other, the dose must be adjusted for the new dosage formulation; incorrect dosing of a given formulation may result in underdosing and loss of therapeutic effect and possible resistance or clinically significant adverse reactions from greater exposure of dolutegravir

              Dosage forms are not interchangeable on a milligram per milligram basis; dose must be adjusted for new dosage formulation; incorrect dosing may lead to loss of therapeutic effect when underdosing and clinically significant adverse reactions when overdosing

              Potential risk of neural tube birth defects (see Pregnancy)

              Drug interaction overview

              • Coadministration with certain drugs may result in known or potentially significant drug interactions, some of which may lead to loss of therapeutic effect and possible resistance, or significant adverse reactions of other from increase systemic exposure
              • Inducers of UGT1A1 and CYP3A (eg, oxcarbazepine, phenytoin, phenobarbital, carbamazepine, St John’s wort, rifampin) decrease dolutegravir
              • Coadministration with medications containing polyvalent cations decrease dolutegravir systemic exposure; give dolutegravir 2 hr before or 6 hr after polyvalent cations (eg, antacids, laxatives, sucralfate, iron supplements, calcium supplements, buffered medications)
              • Dolutegravir may increase plasma concentrations of drugs eliminated via OCT2 or MATE1 (dofetilide and metformin)
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              Pregnancy & Lactation

              Pregnancy

              A pregnancy exposure registry monitors pregnancy outcomes in women during pregnancy; healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263

              Based on prospective reports to the APR of exposures to dolutegravir during pregnancy resulting in live births (including over 450 exposed in first trimester and over 280 exposed in second/third trimester), there was no difference between overall risk of birth defects for dolutegravir compared with background birth defect rate of 2.7% in the U.S. reference population of Metropolitan Atlanta Congenital Defects Program (MACDP); the prevalence of defects in live births was 3.5% (95% CI: 2.0% to 5.6%) following first trimester exposure to dolutegravir-containing regimens and 4.2% (95% CI: 2.2% to 7.2%) following second/third trimester exposure to dolutegravir-containing regimens

              Initiation of therapy is not recommended in individuals actively trying to become pregnant unless there is no suitable alternative; a benefit-risk assessment should consider factors such as feasibility of switching, tolerability, ability to maintain viral suppression, and risk of transmission to infant against risk of neural tube defects

              In adolescents and adults of childbearing potential currently receiving therapy who are actively trying to become pregnant, or if pregnancy is confirmed in the first trimester, assess risks and benefits of continuing therapy versus switching to another antiretroviral regimen and consider switching to an alternative regimen

              Advise pregnant adolescents and adults of potential risk to embryo exposed to drug from time of conception through first trimester of pregnancy; a benefit-risk assessment should consider factors such as feasibility of switching, tolerability, ability to maintain viral suppression, and risk of transmission to infant against risk of neural tube defects

              Perform pregnancy testing in adolescents and adults of childbearing potential before initiation of therapy

              In animal reproduction studies, no evidence of adverse developmental outcomes was observed during organogenesis

              Contraception

              • In adolescents and adults of childbearing potential currently receiving therapy who are actively trying to become pregnant, or if pregnancy is confirmed in first trimester, assess risks and benefits of continuing treatment versus switching to another antiretroviral regimen and consider switching to an alternative regimen
              • Counsel adolescents and adults of childbearing potential who are taking drug to consistently use effective contraception

              Potential risk of neural tube birth defects

              • Serious cases of neural tube birth defects involving the brain, spine, and spinal cord reported in babies born to women treated with dolutegravir
              • Data from a birth outcome surveillance study has identified an increased risk of neural tube defects when therapy is administered at time of conception compared with non- dolutegravir-containing antiretroviral regimens
              • As defects related to closure of neural tube occur from conception through the first 6 weeks of gestation, embryos exposed to dolutegravir from the time of conception through first 6 weeks of gestation are at potential risk
              • In addition, 2 of birth defects (encephalocele and iniencephaly), which have been observed with therapy, although often termed neural tube defects, may occur post-neural tube closure, the time period of which may be later than 6 weeks of gestation, but within the first trimester
              • Recommendations
                • Patients should not discontinue dolutegravir without consulting a healthcare professional because stopping your medicine can cause the HIV infection to worsen
                • Pregnant women stopping dolutegravir-containing regimen without switching to alternative HIV medicines could cause the amount of virus to increase and spread HIV to your baby
                • Patients taking a dolutegravir-containing regimen at the time of becoming pregnant and during the first trimester of pregnancy, there is a potential risk of neural tube defects; neural tube defects happen early in pregnancy, before many women even know they are pregnant
                • Inform women of childbearing age about the potential risk of neural tube defects when a dolutegravir-containing regimen is used at the time of conception and early in pregnancy; women of childbearing age should consult their healthcare providers about other non-dolutegravir-containing antiretroviral medicine
                • Healthcare providers should weigh the benefits and the risks of dolutegravir when prescribing antiretroviral medicines to women of childbearing age; consider alternative antiretroviral medicines; discuss the relative risks and benefits of appropriate alternative antiretroviral therapies
                • Women of childbearing age who decide to take a dolutegravir-containing regimen should consistently use effective birth control (contraception) while on HIV treatment; women should discuss their healthcare professionals about an effective birth control method to use while taking a dolutegravir-containing regimen
                • Perform pregnancy testing before initiating a dolutegravir-containing regimen in women of childbearing age to exclude pregnancy

              Lactation

              The Centers for Disease Control and Prevention recommend that HIV-1-infected mothers in the United States not breastfeed infants to avoid risking postnatal transmission of HIV-1 infection; not known whether drug is present in human breast milk, affects human milk production, or has effects on breastfed infant; when administered to lactating rats, dolutegravir was present in milk

              It is not known whether drug is present in human breast milk, affects human milk production, or has effects on breastfed infant; when administered to lactating rats, dolutegravir was present in milk

              Because of potential for (1) HIV-1 transmission (in HIV-negative infants), and (2) developing viral resistance (in HIV-positive infants), instruct mothers not to breastfeed if they are receiving drug therapy

              Pregnancy Categories

              A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

              B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

              C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

              D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

              X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

              NA: Information not available.

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              Pharmacology

              Mechanism of Action

              Integrase strand transfer inhibitor (INSTI); inhibits catalytic activity of HIV-1 integrase, an HIV encoded enzyme required for viral replication

              Absorption

              Peak plasma time: 2-3 hr

              Peak plasma concentration: 3.67-4.15 mcg/mL

              AUC 53.6-75.1 mcg•h/mL

              Distribution

              Protein bound: ≥98.9%

              Vd: 17.4 L; 4-232 ng/mL (CSF)

              Metabolism

              Metabolized by UGT1A1 with some contribution from CYP3A

              Elimination

              Half-life: 14 hr

              Clearance: 1 L/hr

              Excretion: 53% feces (unchanged); 31% urine (as ether glucuronide, benzylic carbon, or N-dealkylation product); <1% urine (unchanged)

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              Administration

              Oral Administration

              May take with or without food

              Dosage forms (ie, tablets and tablets for oral suspension) are not bioequivalent and are not interchangeable on a mg-per-mg basis

              Tablets for oral suspension

              • Do not chew, cut, or crush
              • Swallow tablets for oral suspension whole (if >1 tablet required, swallow 1 tablet at a time to reduce choking risk), or
              • Fully disperse tablets for oral suspension in 5 mL of drinking water (if using 1-3 tablets for oral suspension) or 10 mL (if using 4-6 tablets for oral suspension) in the supplied cup; swirl suspension so that no lumps remain; after full dispersion, administer oral suspension within 30 minutes of mixing
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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              Tivicay oral
              -
              50 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              dolutegravir oral

              DOLUTEGRAVIR TABLET - FOR ORAL SUSPENSION

              (DOE-loo-TEG-ra-vir)

              COMMON BRAND NAME(S): Tivicay PD

              USES: Dolutegravir is used with other HIV medications to help control HIV infection. It helps to decrease the amount of HIV in your body so your immune system can work better. This lowers your chance of getting HIV complications (such as new infections, cancer) and improves your quality of life. Dolutegravir belongs to a class of drugs known as integrase inhibitors. It blocks the virus from growing and infecting more cells.Dolutegravir is not a cure for HIV infection. To decrease your risk of spreading HIV disease to others, continue to take all HIV medications exactly as prescribed by your doctor. Use an effective barrier method (latex or polyurethane condoms/dental dams) during sexual activity as directed by your doctor. Do not share personal items (such as needles/syringes, toothbrushes, and razors) that may have contacted blood or other body fluids. Consult your doctor or pharmacist for more details.

              HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking dolutegravir and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Do not change dosage forms of this medication without checking with your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually 1 to 2 times daily.The tablet(s) may be swallowed whole or mixed in water. Do not chew, cut, or crush the tablet(s).If you are mixing the tablet(s) in water, place the tablet(s) in the supplied cup with a small amount of water. Ask your doctor or pharmacist how much water you should use to dissolve the tablet(s). Do not use any other liquids. Swirl the mixture gently for 1 to 2 minutes, then drink all of the mixture right away. To make sure you have taken all of the medication, add another small amount of water to the cup, swirl it, and drink it right away. Take this medication within 30 minutes of mixing.Take this medication at least 2 hours before or 6 hours after taking sucralfate and products containing aluminum or magnesium (such as antacids, laxatives, buffered medications). These products bind with dolutegravir, decreasing its effectiveness.If you are also taking calcium or iron supplements (including vitamins/minerals that contain calcium or iron), take dolutegravir at least 2 hours before or 6 hours after these products. Or, if you take dolutegravir with food, you can take calcium or iron supplements at the same time.The dosage is based on your medical condition, response to treatment, age, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). In children, the dosage is also based on weight.It is very important to keep taking this medication (and other HIV medications) exactly as prescribed by your doctor. Do not skip any doses.For the best effect, take this medication at evenly spaced times. To help you remember, take this medication at the same time(s) every day.Do not take more or less of this drug than prescribed or stop taking it (or other HIV medicines) even for a short time unless directed to do so by your doctor. Doing so may cause the amount of virus to increase, make the infection more difficult to treat (resistant), or worsen side effects.

              SIDE EFFECTS: Headache and trouble sleeping may occur. If either of these effects lasts or gets worse, tell your doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: symptoms of liver problems (such as nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine), signs of kidney problems (such as change in the amount of urine), mental/mood changes (such as depression, thoughts of suicide).As your immune system gets stronger, it can begin to fight off infections you already had, possibly causing disease symptoms to come back. You could also have symptoms if your immune system becomes overactive. This reaction may happen at any time (soon after starting HIV treatment or many months later). Get medical help right away if you have any serious symptoms, including: unexplained weight loss, severe tiredness, muscle aches/weakness that doesn't go away, headaches that are severe or don't go away, joint pain, numbness/tingling of the hands/feet/arms/legs, vision changes, signs of infection (such as fever, chills, swollen lymph nodes, trouble breathing, cough, non-healing skin sores), signs of an overactive thyroid (such as irritability, nervousness, heat intolerance, fast/pounding/irregular heartbeat, bulging eyes, unusual growth in the neck/thyroid known as a goiter), signs of a certain nerve problem known as Guillain-Barre syndrome (such as trouble breathing/swallowing/moving your eyes, drooping face, paralysis, trouble speaking).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Before taking dolutegravir, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease (such as hepatitis B, hepatitis C), kidney disease.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Before using this medication, women of childbearing age should talk with their doctor(s) about the risks and benefits. Tell your doctor if you are pregnant or if you plan to become pregnant. Your doctor should direct you to get a pregnancy test before starting this medication. During pregnancy, this medication should be used only when clearly needed. It is not recommended for use during the first trimester of pregnancy due to possible harm to the unborn baby. Ask about reliable forms of birth control while using this medication.It is unknown if this medication passes into breast milk. Because breast milk can transmit HIV, do not breast-feed.

              DRUG INTERACTIONS: See also How to Use section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug are: dofetilide, orlistat.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

              NOTES: Do not share this medication with others.Lab and/or medical tests (such as liver/kidney function, viral load, T-cell counts) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.

              MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

              STORAGE: Store at room temperature away from light and moisture. Keep this drug in the original bottle, and keep the bottle tightly closed. The bottle contains a desiccant to help keep your medicine dry. Keep the desiccant in the bottle. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

              Information last revised January 2021. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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              Formulary

              FormularyPatient Discounts

              Adding plans allows you to compare formulary status to other drugs in the same class.

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              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.