Adult Dosing

HIV-1 infection

• 400 mg PO bid with or without food
• During coadministration with rifampin: 800 mg PO bid with or without food

Pediatric Dosing

HIV-1 infection

• Tablets
• 12 years: 400 mg PO bid
• 6-12 years; 25 kg: 400 mg PO bid

• Chewable tablets
• 2-<12 yrs: 40kg: 300mg PO bid
• 28-<40kg: 200 mg PO bid
• 20-<28kg: 150 mg PO bid
• 14-<20kg: 100 mg PO bid
• 10-<14kg: 75 mg PO bid
• Max: 300 mg PO bid

[Outline]

• Adult Dosing
• Pediatric Dosing

• In combination with other antiretroviral agents for the treatment of HIV-1 infection in patients 4 weeks of age and older

• Hypersensitivity to any of the ingredients of the product

• N/A

Renal Dose Adjustment

• Renal impairment: No dosage adjustments

Hepatic Dose Adjustment :

• Mild/Moderate hepatic impairment: No dosage adjustments
• Severe hepatic impairment: Use with caution

• Severe, potentially life-threatening, and fatal skin reactions such as Stevens-Johnson syndrome, toxic epidermal necrolysis, and hypersensitivity reactions characterized by rash, constitutional findings, and organ dysfunction, including hepatic failure have been reported with raltegravir. Discontinue therapy and other suspect agents if severe skin reactions or hypersensitivity reactions occur
• Therapy may cause an inflammatory response to indolent or residual opportunistic infections during the initial phase of treatment, which may necessitate further evaluation and treatment
• Autoimmune disorders including Graves disease, polymyositis, and Guillain-Barré syndrome may occur in the setting of immune reconstitution
• Chewable Tablets contain phenylalanine and should be use with caution in patients with phenylketonuria

Cautions: Use cautiously in

• Severe hepatic impairment
• Geriatric population
• Concurrent use of medications associated with rhabomyolysis/myopathy

Pregnancy Category:C

Breastfeeding: Unsafe, breastfeeding is not recommended in HIV infected individuals due to risk of transmission to the infant.

• CNS: Depression, dizziness, headache, asthenia, paranoia
• PSYCHIATRY: Suicidality thoughts, insomnia
• GI: Nausea, gastritis hepatitis
• GU: Renal failure
• DERM: Stevens-Johnson syndrome
• MUSC: Rhabdomyolysis
• HEMA: Neutropenia, anemia, thrombocytopenia
• METABOLIC: Hyperbilirubinemia
• MISC: Immune reconstitution syndrome, hypersensitivity reaction, fatigue

• Integrase strand transfer inhibitor (INSTI); inhibits viral replication by inhibiting HIV-1 integrase
• Metabolized in liver primarily by glucoronidation by the enzyme UDP-glucuronosy transferase (UGT) 1A1;CYP450: None
• Renally excreted 32%; feces 51%
• Half-life: 9 hrs

US Trade Name(s)

• Isentress

US Availability

Isentress

• TABS: 400 mg
• CHEW TABS: 25, 100 mg

Canadian Trade Name(s)

• Isentress

Canadian Availability

Isentress

• TABS: 400 mg

UK Trade Name(s)

• Isentress

UK Availability

Isentress

• TABS: 400 mg

Australian Trade Name(s)

• Isentress

Australian Availability

Isentress

• TABS: 400 mg

[Outline]

Antimicrobials

Antiviral (HIV) Agents

Integrase Inhibitors

Infectious Disease

Antiviral (HIV) Agents

Integrase Inhibitors

Pricing data from www.DrugStore.com in U.S.A.

• Isentress 400 MG TABS [Bottle] (MERCK SHARP & DOHME)
  60 mg = $1030.04
  180 mg = $3030.04

Warning: This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit drugstore.com.

Drug Name: ISENTRESS 400 MG Oral Tablet

Ingredient(s): Raltegravir

Imprint: 227

Color(s): Pink

Shape: Oval

Size (mm): 16.00

Score: 1

Inactive Ingredient(s): ferrosoferric oxide / butylated hydroxytoluene / anhydrous dibasic calcium phosphate / hypromellose / lactose monohydrate / magnesium stearate / cellulose, microcrystalline / poloxamer 407 / polyethylene glycol 3350 / polyvinyl alcohol / ferric oxide red / sodium stearyl fumarate / talc / titanium dioxide

Drug Label Author:
Merck Sharp & Dohme Corp.

DEA Schedule:
Non-Scheduled

Drug Name: Isentress (RALTEGRAVIR 400 mg)

Ingredient(s): N/A

Imprint: 227

Color(s): Pink

Shape: Oval

Size (mm): 16.00

Score: 1

Inactive Ingredient(s): ferrosoferric oxide / butylated hydroxytoluene / anhydrous dibasic calcium phosphate / hypromellose / lactose monohydrate / magnesium stearate / cellulose, microcrystalline / poloxamer 407 / polyethylene glycol 3350 / polyvinyl alcohol / ferric oxide red / sodium stearyl fumarate / talc / titanium dioxide

Drug Label Author:
Physicians Total Care, Inc.

DEA Schedule:
Non-Scheduled