Dolutegravir

Drug #2321

The chemical name of dolutegravir sodium is sodium (4R,12aS)-9-{[(2,4-difluorophenyl)methyl]carbamoyl}- 4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazin-7- olate. Dolutegravir is a human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor (INSTI) indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and children aged 12 years and older and weighing at least 40 kg.

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Primary Characteristics

It is of Synthetic origin.

It belongs to Antiviral Agents pharmacological group on the basis of mechanism of action.

Molecular Weight: 441.36 · Solubility in Water: slightl soluble · Non-proprietary name: Dolutegravir.

Pharmacokinetics

Distribution: Dolutegravir has a volume of distribution is 17.4L. plasma protein binding is greater than 98.9%.

Elimination: it is metabolised via hepatic, plasma half-life is 14hrs, renal excretion is 53% by feces, 31% in urine.

Indications

Dolutegravir is primarily indicated in conditions like HIV infection in combination with other antiretroviral drugs.

Contraindications

None recorded.

Dosage

Dolutegravir's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
0 – 50 mg	—	—	PO	Patients infected with HIV-1 without suspected resistance to the integrase class
50 mg	50 mg	—	PO	patient infected with HIV-1 without suspected resistance to the integrase classwhen co-administered with some medicines (e.g. efavirenz, nevirapine, tipranavir/ritonavir, or rifampicin) i
50 mg	50 mg	—	PO	Patients infected with HIV-1 with resistance to the integrase class
Paediatric Dosage (20kg)
0 – 50 mg	—	—	PO	pediatric patients aged 12 years and older and weighing at least 40 kg
Neonatal Dosage (3kg)
No data.

Drug Interactions

16 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Dolutegravir is known to cause more or less tolerable side effects which are usually transient. These include Headache, Insomnia.

Warnings / Precautions

Hypersensitivity reactions characterized by rash, constitutional findings, and sometimes organ dysfunction, including liver injury.Effects on Serum Liver Biochemistries in Patients With Hepatitis B or C 51 Co-infection, Fat redistribution, immune reconstitution syndrome. caution should be taken in all these conditions.

Available Brands

None recorded.

Storage Conditions

Dolutegravir should be stored Tablet.

Drug Classification

1.6.5.2 — Antiretroviral drugs