Introduction of Dolutegravir sodium

Dolutegravir sodium (product name:TIVICAY) is an oral, World Health Organisation-recommended first-line antiretroviral drug that belongs to a class of drugs called HIV integrase inhibitors. It is often used in combination with other anti-HIV medications to treat human immunodeficiency virus (HIV) infection in adults and children 4 weeks of age and older who weigh at least 6.6 pounds (3 kg). The combination of dolutegravir and rilpivirine can also be used to treat adult patients with HIV-1 infection for six months.

Mechanisms of action

Dolutegravir binds to the active site of integrase, an HIV enzyme that catalyses the transfer of viral genetic material into the human chromosome. This prevents the integrase from binding to retroviral deoxyribonucleic acid (DNA) and blocks the strand transfer step, which is essential for the HIV replication cycle. This prevents HIV-1 replication. Mean EC50 values for dolutegravir in peripheral blood mononuclear cells (PBMC) and MT-4 cells ranged from 0.5 nM (0.21 ng/mL) to 2.1 nM (0.85 ng/mL).

Adverse effects of Dolutegravir sodium

Commonly there may be headaches, difficulty sleeping, diarrhoea, stomach pains, etc. Severe cases may result in rashes, fever, feeling unwell, excessive fatigue, muscle or joint pains, blistering or peeling of the skin; blisters or ulcers in the mouth, redness or swelling of the eyes; swelling of the eyes, face, lips, mouth, tongue, or throat; difficulty in breathing or swallowing; yellowing of the eyes or skin; dark-coloured urine; pale-coloured bowel movements etc. Contact your doctor if you experience any unusual problems while taking this medication.

References:

[1] MEYERSTAMMY  KrogstadPaul. Dolutegravir for children with HIV-associated tuberculosis.[J]. Lancet Hiv, 2022: e599-e600. DOI:10.1016/S2352-3018(22)00172-2. 

[2] J S. Dolutegravir/Lamivudine Single-Tablet Regimen: A Review in HIV-1 Infection.[J]. Drugs, 2020, 80 1: 61-72. DOI:10.1007/s40265-019-01247-1.