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dolutegravir(doe-loo-teg–ra-vir ) ,
Pregnancy Category: B
Pharmacologic: integrase strand transfer inhibitors
Pharmacologic: integrase strand transfer inhibitors
Treatment of HIV-1 infection, in combination with other antiretrovirals
Inhibits HIV-1 integrase, which is required for viral replication.
Evidence of decreased viral replication and reduced viral load with slowed progression of HIV and its sequelae.
Absorption: Absorption follows oral administration; bioavailability is unknown
Distribution: Enters CSF
Protein Binding: >98.9%
Metabolism and Excretion: Metabobolized primarily by the UGT1A1 enzyme system with some metabolism by CYP3A4. 53% excreted unchanged in feces. Metabolites are renally excreted, minimal renal elimination of unchanged drug. genetic implication Poor metabolizers of dolutegravir have ↑ levels and ↓ clearance.
Half-life: 14 hr
Time/action profile (blood levels)
|PO||unk||2–3 hr||12–24 hr†|
Contraindicated in: Concurrent use of dofetilide;Severe hepatic impairment; Lactation: Breast feeding not recommended in HIV-infected patients.
Use Cautiously in: Underlying hepatic disease, including hepatitis B or C (↑ risk fo hepatotoxicity);Severe renal impairment; Geriatric: Consider age-related decrease in cardiac, renal and hepatic function, chronic disease states and concurrent medications; Obstetric: Use during pregnancy only if clearly needed; Pediatric: Patients <12 yr, <49 kg or INSTI-experienced (have received raltegravir or elvitegravir) or resistance documented (safety and effectiveness not established).
Adverse Reactions/Side Effects
Central nervous system
- headache (most frequent)
- insomnia (most frequent)
- hepatic toxicity (↑ with hepatitis B or C)
- renal impairment
- fat accumulation/redistribution
- hypersensitivity reactions (including rash, constitutional symptoms, and liver injury)
- immune reconstitution syndrome
Drug-Drug interactionBlood levels and effectiveness are ↓ by etravirine (should not be used concurrently without atazanavir/ritonavir, darunavir/ritonavir or lopinavir/ritonavir).Blood levels and effectiveness are ↓ by efavirenz, dosage adjustment is recommended.Blood levels and effectiveness may be↓ by nevirapine Blood levels and effectiveness are ↓ by fosamprenavir/ritonavir or tipranavir/ritonavir ; dosage adjustment is recommended.May ↑ blood levels and toxicity from dofetilide (arrhythmias) or metformin (hypoglycemia), concurrent dofetilide should be avoided.Blood levels and effectiveness may be ↓ other metabolic inducers including carbamazepine, oxcarbazepine, phenobarbital, phenytoin, or rifampin ; concurrent use should be avoided and alternative medications considered.Absorption and effectiveness may be ↓ by cation-containing antacids, buffered medications, calcium supplements (oral), iron supplements (oral), laxatives, or sucralfate ; dolutegravir should be taken 2 hr before or 6 hr after.Blood levels and effectiveness may be ↓ St. John's wort ; concurrent use should be avoided.
Oral (Adults) Treatment-naïve or treatment-experienced INSTI-naïve patients—50 mg once daily; Treatment-naïve or treatment-experienced INSTI-naïve patients currently receiving efavirenz, fosamprenavir/ritonavir, tipranvir/ritonavir or rifampin—50 mg twice daily; INSTI-experienced with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance (consider other combinations that do not include metabolic inducers)—50 mg twice daily.
Oral (Children ≥ 12 yr and >40 k g) 50 mg once daily; concurrent efavirenz, fosamprenavir/ritonavir, tipranvir/ritonavir or rifampin—50 mg twice daily.
Tablets: 50 mg
- Assess patient for change in severity of HIV symptoms and for symptoms of opportunistic infections during therapy.
- Monitor for signs and symptoms of hypersensitivity reactions (rash, fever, malaise, fatigue, muscle or joint aches, blisters or peeling of skin, oral blisters or lesions, conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema, difficulty breathing). Discontinue therapy and do not restart.
- Lab Test Considerations: Monitor viral load and CD4 counts regularly during therapy.
- May casue ↓ ANC, hemoglobin, total neutrophils, and platelet counts.
- May cause ↑ serum glucose, lipase, AST, ALT, total bilirubin, creatine kinase concentrations.
Potential Nursing DiagnosesRisk for infection (Indications)
Noncompliance (Patient/Family Teaching)
- Oral: May be administered without regard to food.
- Emphasize the importance of taking dolutegravir as directed. Do not take more than prescribed amount and do not stop taking without consulting health care professional. Take missed doses as soon as remembered unless within 4 hr of next dose; then skip dose. Do not double doses. Advise patient to read Patient Information sheet before starting therapy and with each prescription renewal in case changes have been made.
- Instruct patient that dolutegravir should not be shared with others.
- 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.
- Inform patient that dolutegravir does not cure AIDS or prevent associated or opportunistic infections. Dolutegravir does not reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to use a condom during sexual contact and to avoid sharing needles or donating blood to prevent spreading the AIDS virus to others. Advise patient that the long-term effects of dolutegravir are unknown at this time.
- Advise patient to notify health care professional if signs and symptoms of hypersensitivity or infection occur.
- Inform patient that redistribution and accumulation of body fat may occur, causing central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, breast enlargement, and cushingoid appearance. The cause and long-term effects are not known.
- Advise patients to notify health care professional if pregnancy is planned or suspected. Breast feeding should be avoided during therapy. Pregnant patients should be encouraged to enroll in the Antiretroviral Pregnancy Registry by calling 1-800-258-4263.
- Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects.
- Delayed progression of AIDS and decreased opportunistic infections in patients with HIV.
- Decrease in viral load and improvement in CD4 cell counts.
Drug Guide, © 2015 Farlex and Partners