HIV infection

Dolutegravir is an integrase strand transfer inhibitor that blocks retroviral DNA integration in the HIV replication cycle.

Absorption:Bioavailability, Oral: not established
Distribution:
Vd: 17.4 L
Metabolism:
Liver: primary site via UGT1A1 with some contribution from CYP3A,ether glucuronidated dolutegravir (major): activity unknown.
inhibitor of OCT2 renal organic cation transporter
Excretion:
Renal: 31% changed,Dialyzable: No (hemodialysis, peritoneal dialysis).
Elimination Half Life:14 hours.

Concomitant use with dofetilide
Hypersensitivity to dolutegravir

Fetal risk cannot be ruled out. (TH)

Infant risk cannot be ruled out.(MDX)

Common:
Endocrine metabolic: Hyperglycemia (grade 2 to 4, up to 12% )
Hepatic: Increased serum lipase level (grade 3 to 4, 1% to 8% )
Neurologic: Headache (moderate to severe, up to 2% ), Insomnia (grade 1, 1% to 7%; grade 2 to 4, less than 1% to 3% )
Serious:
Hepatic: ALT/SGPT level raised (grade 2 to 4, up to 8%; hepatitis B and/or C coinfection, 8% to 16% (grade 2 to 4) ), AST/SGOT level raised (grade 2 to 4, up to 6% ), Hepatitis (less than 2% ), Serum bilirubin raised (grade 2, up to 2%; grade 3, up to 1% )
Immunologic: Hypersensitivity reaction (up to 1% ), Immune reconstitution syndrome
Renal: Renal impairment (less than 2% )

HIV infection
Treatment-naive or treatment-experienced but integrase strand inhibitor-naive (INSTI-naive), 50 mg orally once daily
INSTI-experienced with certain known or suspected INSTI-associated resistance substitutions, 50 mg orally twice daily
Concomitant use with certain UGT1A or CYP3A inducers (ie, carbamazepine, efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, or rifampin) in treatment-naive or treatment-experienced and INSTI-naive adults: 50 mg orally twice daily
Concomitant use with certain UGT1A or CYP3A inducers (ie, carbamazepine, efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, or rifampin) in INSTI-experienced adults with known or suspected resistance: Use an alternative treatment regimen that does not include metabolic inducers
Concomitant use with certain UGT1A or CYP3A inducers (ie, carbamazepine, efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, or rifampin) in treatment-naive or treatment-experienced and INSTI-naive pediatric patients: Increase dosing frequency to twice daily

HIV infection:
(30 to less than 40 kg) Treatment-naive or treatment-experienced, integrase strand inhibitor-naive, 35 mg orally once daily
(40 kg or greater) Treatment-naive or treatment-experienced, integrase strand inhibitor-naive, 50 mg orally once daily

Renal impairment, mild, moderate, or severe, in treatment-naive or treatment-experienced and integrase strand transfer inhibitor-naive (INSTI-naive) patients: No adjustment necessary
Renal impairment, mild to moderate, in INSTI-experienced patients with known or suspected resistance: No adjustment necessary
Renal impairment, severe, in INSTI-experienced patients with known or suspected resistance: Caution advised

Hepatic impairment, mild to moderate (Child-Pugh score A or B): No adjustment necessary
Hepatic impairment, severe (Child-Pugh score C): Use not recommended