Date of Approval: August 12, 2013
Approved by :U.S. Food and Drug Administration
Company: ViiV Healthcare
Generic Name : Dolutegravir
Brand Name: Tivicay
Other Names: DTG
Drug Class: Integrase Inhibitors
Approved Use: Treatment of HIV Infection
Molecular Weight: 419.3821
DOSAGE AND ADMINISTRATION:
TIVICAY tablets may be taken with or without food.
For Adults :
50 mg tablet once a d for people on HIV therapy
for the first time .
Twice-daily dosing in people who have viral
resistance to Isentress and elvitegravir.
Expected to have no food restriction
Alternative combinations that do not include
metabolic inducers should be considered where
Pediatric Patients :
Age 12 years and older and weighing at least 40 kg –
50 mg p/o -OD.
Efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavi
r, or rifampin - 50 mg twice daily.
Safety and efficacy of TIVICAY have not been
established in pediatric patients younger than 12
years or weighing less than 40 kg, or in pediatric
patients who are INSTI-experienced with
documented or clinically suspected resistance to
other INSTIs (raltegravir, elvitegravir).
DOSAGE FORMS AND STRENGTHS
TIVICAY 50-mg tablets are yellow, round, filmcoated, biconvex tablets .
Each tablet contains 50 mg of dolutegravir (as dolutegravir
Peak plasma time: 2-3 hr
Peak plasma concentration: 3.67-4.15 mcg/l
Protein bound: ≥98.9%
Vd : 17.4 L;
4-232 ng/mL (CSF)
Metabolized by UGT1A1 with some contribution from CYP3A
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)
Mechanism of Action
Inhibits catalytic activity of HIV-1 integrase, an HIV encoded
enzyme required for viral replication
Abnormal liver function in participants co-infected with
hepatitis B and / or C
•GI disorders (<2%)
Coadministration of TIVICAY with dofetilide is
contraindicated due to the potential for increased
dofetilide plasma concentrations and the risk for
serious and/or life-threatening events
Pregnancy: Pregnancy category B.
Breastfeeding: Breastfeeding is NOT recommended
Co-administration of TIVICAY with drugs that are strong
inducers of UGT1A1 and/or CYP3A4 may result in reduced
plasma concentrations of dolutegravir and require dose
adjustments of TIVICAY.
-TIVICAY should be taken 2 hours before or 6 hours after
taking cation-containing antacids or laxatives, sucralfate, oral
iron supplements, oral calcium supplements, or buffered
a medicine that contains metformin
There is no known specific treatment for overdose
If overdose occurs, the patient should be monitored
and standard supportive treatment applied as
As dolutegravir is highly bound to plasma proteins, it
is unlikely that it will be significantly removed by
Effects on Serum Liver Biochemistries in Patients With Hepatitis
B or C Co-infection
Patients should be advised to avoid doing things that can spread
HIV-1 infection to others.
• Do not share personal items that can have blood or body fluids
on them, like toothbrushes and razor blades.
• Practice safe sex by using a latex or polyurethane condom to
lower the chance of sexual contact with semen, vaginal
secretions, or blood.
• Female patients should be advised not to breastfeed
To inform their physician or pharmacist if they develop any
unusual symptom, or if any known symptom persists or
If missed a dose - should take it as soon as they remember.
If they do not remember until it is within 4 hours of the
time for the next dose, they should be instructed to skip
the missed dose and go back to the regular schedule.