Antiretroviral Therapy for HIV-Infected Adults Drug Summary

Last updated: 22 September 2025

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Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)*

Content on this page:

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)*

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)*


Drug Dosage Remarks1
Doravirine (DOR) 100 mg PO 24 hourly Adverse Reactions
  • CNS effects (insomnia, abnormal dreams, nightmare, depression, headache, dizziness, somnolence); GI effects (nausea/vomiting, diarrhea, abdominal pain); Other effects (rash, fatigue)
Special Instructions
  • Concomitant administration with strong CYP450 enzyme inducers (eg anticonvulsants, androgen receptor inhibitor, antimycobacterials, cytotoxic agents) is contraindicated
  • Contraindicated in patients with galactose intolerance, total lactase deficiency or glucose-galactose malabsorption
  • Use with caution in patients with severe hepatic impairment, end-stage renal disease (ESRD) or those in dialysis
Efavirenz (EFV) 600 mg PO 24 hourly Adverse Reactions
  • Dermatologic effects (rash, Stevens-Johnson syndrome, erythema multiforme, pruritus); CNS effects (dizziness, headache, insomnia, somnolence, abnormal dreams, fatigue, impaired concentration, depression, anxiety, psychosis, amnesia, ataxia); GI effects (nausea/vomiting, diarrhea, hepatitis, abdominal pain); Other effects (gynecomastia, blurred vision)
Special Instructions
  • Contraindicated in patients with severe hepatic impairment
  • Use with caution in patients with renal impairment, mild to moderate liver disease, known or suspected hepatitis B infection, history of mental illness and seizures
  • Discontinue use if severe skin rash or fever develops
  • Monitor liver enzymes and cholesterol level
Etravirine (ETV) 200 mg PO 12 hourly Adverse Reactions
  • Dermatologic effect (rash); GI effects (nausea/vomiting, abdominal pain); Metabolic effects (elevated total cholesterol, hyperglycemia, increased ALT and creatinine levels); CV effect (hypertension); CNS effect (peripheral neuropathy)
  • May cause fat redistribution and immune reconstitution syndrome
Special Instructions
  • Should be taken with food
  • Discontinue use if severe skin rash develops
  • Unboosted protease inhibitors (ie without low-dose Ritonavir) should not be used with Etravirine
  • Use with caution in patients with severe hepatic impairment
Nevirapine (NVP) Initial dose: 200 mg PO 24 hourly x 14 days
Maintenance dose: 200 mg PO 12 hourly or 400 mg PO 24 hourly		 Adverse Reactions
  • Dermatologic effect (rash); GI effects (nausea/vomiting, abnormal liver function tests [LFTs], diarrhea, abdominal pain); CNS effects (headache, fatigue)
Special Instructions
  • Re-introduce at a lower dose for the first 14 days if treatment is interrupted for >7 days
  • Contraindicated in patients with moderate to severe hepatic impairment
  • Interrupt treatment if severe hepatotoxicity or life-threatening skin reactions develop
  • Use with caution in patients with renal or hepatic insufficiency; monitor liver function periodically
Rilpivirine (RPV) 25 mg PO 24 hourly or
Oral lead-in therapy: 25 mg PO 24 hourly (+ Cabotegravir 30 mg) x ≥1 month
Every month IM dosing
Initiation dose: 900 mg IM at month 2 (+ Cabotegravir 600 mg) administered on final day of oral lead-in therapy
Continuation dose: 600 mg IM monthly (+ Cabotegravir 400 mg) monthly starting at month 3 onwards, given up to 7 days before or after the date of monthly injection schedule
Every 2-month IM dosing
Initiation dose: 900 mg IM at month 2 (+ Cabotegravir 600 mg) administered on final day of oral lead-in therapy and at month 3
Continuation dose: 900 mg IM monthly (+ Cabotegravir 600 mg) every 2 months starting at month 5 onwards, given up to 7 days before or after the date of every-2-month injection schedule
Switching from monthly to every 2-month IM dosing
Single dose of 900 mg IM 1 month after last 600 mg continuation dose then 900 mg IM every 2 months thereafter
Switching from every 2-month to monthly IM dosing
Single dose of 600 mg IM 2 months after last 900 mg continuation dose then 600 mg IM monthly thereafter		 Adverse Reactions
  • CNS effects (depression, dysphoria, mood changes, negative thoughts, suicidal ideation, headache, insomnia, dizziness, asthenia, anxiety, abnormal dreams); Dermatologic effect (rash); Metabolic effects (increased LDL, total cholesterol/triglyceride levels); Hepatic effects (elevated liver transaminases and bilirubin levels); Renal effect (elevated creatinine level); Injection site reactions (swelling, erythema, pruritus, bruising, warmth, hematoma); GI effects (decreased appetite, nausea/vomiting, abdominal pain, flatulence, diarrhea, dry mouth)
Special Instructions
  • Tablet should be taken with food for optimal absorption
  • IM injection should be co-administered with Cabotegravir injection at separate gluteal injection sites
  • Contraindicated in patients with severe hepatic impairment
  • Concurrent use of Carbamazepine, Dexamethasone (>1 dose), Oxcarbazepine, Phenobarbital, Phenytoin, PPIs, Rifabutin, Rifampin, Rifapentine, St John’s wort are contraindicated
  • Use with caution in patients with mild-moderate hepatic impairment, severe renal impairment or ESRD, depressive disorders
*Combinations of NNRTIs and NRTIs are available. Please see the latest MIMS for specific formulations and prescribing information.
1Drug interactions listed in the remarks section may not be comprehensive. Please see the latest MIMS for complete drug interaction details and full prescribing information.

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)*^


Drug Dosage Remarks1
Abacavir (ABC) 300 mg PO 12 hourly or
600 mg PO 24 hourly		 Adverse Reactions
  • Dermatologic effects (rash, severe/potentially fatal hypersensitivity reactions may occur); GI effects (anorexia, nausea/vomiting, diarrhea, abdominal pain); CNS effects (headache, fatigue, malaise, lethargy); Metabolic effects (elevated blood glucose/triglyceride levels); Other effects (fever, cough, dyspnea)
Special Instructions
  • Contraindicated in patients with moderate to severe renal and hepatic impairment, ESRD
  • Use with caution in patients with mild liver impairment; discontinue when liver function deteriorates or if hepatomegaly and unexplained metabolic acidosis develop
  • Discontinue as soon as hypersensitivity is suspected
Didanosine (ddI) Regular tab/cap or 10 mg/ml oral solution
<60 kg: 125 mg PO 12 hourly or 250 mg PO 24 hourly
≥60 kg: 200 mg PO 12 hourly or 400 mg PO 24 hourly (twice-daily dosing is preferred)
Delayed-release cap:
25 kg to <60 kg: 250 mg PO 24 hourly
≥60 kg: 400 mg PO 24 hourly
With Tenofovir:
<60 kg: 200 mg PO 24 hourly
≥60 kg: 250 mg PO 24 hourly		 Adverse Reactions
  • GI effects (pancreatitis, nausea/vomiting, diarrhea, abdominal pain, hepatic failure); Dermatologic effect (rash); CNS effects (peripheral neuropathy, headache, fatigue); Metabolic effect (increased uric acid levels); Ocular effects (optic neuritis, retinal pigmentation)
  • Patients may develop peripheral neuropathy, immune reconstitution syndrome, redistribution/accumulation of body fat
Special Instructions
  • Take on an empty stomach (1.5 hours before or 2 hours after meals)
  • Use with caution in patients with history of pancreatitis and liver disease, in those with impaired hepatic and renal function, peripheral neuropathy, hyperuricemia
  • Discontinue use in patients with confirmed pancreatitis
  • Consider discontinuation or interruption in patients with worsening liver disease
  • Patients may develop retinal changes and optic neuritis; half to yearly dilated retinal examinations are recommended
Emtricitabine (FTC) 200 mg PO 24 hourly (as capsule) or
240 mg PO 24 hourly (as a 10 mg/ml solution) 		Adverse Reactions
  • GI effects (diarrhea, nausea/vomiting, dyspepsia, abdominal pain); Endocrine and metabolic effects (elevated amylase, lipase, creatine kinase, or LFT levels, hypertriglyceridemia, hypercholesterolemia, hyperglycemia, hyperlactatemia, insulin resistance, hyperbilirubinemia); CNS effects (headache, insomnia, dizziness, abnormal dreams, pain, asthenia); Other effects (anemia, neutropenia, rash, hyperpigmentation)
  • Potentially fatal lactic acidosis and severe hepatomegaly with steatosis have been reported
Special Instructions
  • Use with other Emtricitabine- or Lamivudine-containing preparations are contraindicated
  • Use with caution in patients with renal impairment, hepatomegaly, hepatic steatosis, hepatitis, hepatic impairment or those at risk for liver disease, in patients with hepatitis C coinfection, and patients on alpha-interferon and Ribavirin therapy
  • Test for presence of chronic HBV infection prior to initiating therapy
  • Discontinue use if there is a rapid rise in aminotransferase levels, progressive hepatomegaly or steatosis, metabolic or lactic acidosis of unknown cause
  • Concurrent use of alpha-interferon increases the risk of lactic acidosis
Lamivudine (3TC) 150 mg PO 12 hourly or
300 mg PO 24 hourly 		Adverse Reactions
  • GI effects (abdominal pain, nausea/vomiting, diarrhea); CNS effects (headache, peripheral neuropathy, insomnia); Metabolic effects (elevated creatine phosphokinase and alanine aminotransferase levels); Other effects (fever, cough, muscle pain, rash, alopecia, malaise, paronychia, angioedema, anaphylactoid reaction, urticaria)
  • Potentially fatal lactic acidosis associated with severe hepatomegaly and hepatic steatosis have been reported
Special Instructions
  • Use with caution in patients with renal impairment, hepatomegaly or other risk factors for hepatic impairment
  • Discontinue use if there is rapid rise in aminotransferase levels, progressive hepatomegaly, metabolic or lactic acidosis of unknown cause, if with clinical signs and symptoms or lab abnormalities suggestive of pancreatitis develop
Stavudine (d4T) <60 kg: 30 mg PO 12 hourly
≥60 kg: 40 mg PO 12 hourly
 Adverse Reactions
  • GI effects (nausea/vomiting, abdominal pain, anorexia); CNS effects (headache, asthenia, insomnia, mood changes); Dermatologic effects (skin rashes, pruritus); Hematologic effects (neutropenia, thrombocytopenia); Other effects (arthralgia, myalgia, influenza-like syndrome, dyspnea, pharyngitis)
Special Instructions
  • Use with caution in patients with hepatomegaly or other risk factors for liver disease, with history of peripheral neuropathy, in renal impairment 
  • Discontinue use if peripheral neuropathy develops, if there is rapid rise in aminotransferase levels, progressive hepatomegaly, metabolic or lactic acidosis of unknown cause
  • Monitor for signs of pancreatitis; avoid concurrent administration of drugs that causes pancreatitis (eg IV Pentamidine) and peripheral neuropathy (eg Metronidazole, Isoniazid, Vincristine)
  • Risk of adverse effects (eg hepatotoxicity, peripheral neuropathy, pancreatitis) is increased if used with Didanosine and Hydroxycarbamide
Tenofovir disoproxil fumarate (TDF)
 300 mg PO 24 hourly  Adverse Reactions
  • GI effects (nausea/vomiting, diarrhea, abdominal pain, flatulence, anorexia, dyspepsia, hepatitis); Metabolic effects (hypophosphatemia, increased amylase and liver enzymes, hypertriglyceridemia, hyperglycemia); CNS effects (peripheral neuropathy, headache, depression, asthenia, dizziness, insomnia); Renal effects (nephritis, nephrogenic diabetes insipidus, renal impairment, Fanconi syndrome); Other effects (body fat redistribution, osteomalacia, immune reconstitution syndrome)
Special Instructions
  • Use with caution in patients with renal impairment, hepatomegaly or in those at risk for liver disease
  • Discontinue use if there is rapid rise in aminotransferase levels, progressive hepatomegaly or steatosis, metabolic or lactic acidosis of unknown cause
  • Monitor creatinine clearance and serum phosphorus routinely in patients at risk of renal impairment
  • Bone monitoring for patients with history of pathologic bone fracture or those at risk of osteopenia
Zalcitabine (ddC)
 0.75 mg PO 8 hourly
 Adverse Reactions
  • CNS effects (numbness, sharp shooting pain, asthenia, fatigue, mood changes); CV effects (cardiomyopathy, heart failure, chest pain); GI effects (oral and esophageal ulceration, constipation, diarrhea); Dermatologic effects (rash, alopecia, pruritus); Metabolic effects (elevated LFTs, hyperuricemia); Other effects (arthralgia, myalgia, dyspnea, pharyngitis, hearing, visual/renal disturbances)
  • Potentially fatal hepatic failure, pancreatitis, lactic acidosis and severe hepatomegaly with steatosis have been reported
Special Instructions
  • Should be taken on an empty stomach (at least 1 hour before or 2 hours after meals)
  • Contraindicated in patients with or at risk of peripheral neuropathy
  • Use with caution in patients with history of pancreatitis or increased serum amylase, cardiomyopathy, heart failure, renal or hepatic impairment
  • Discontinue if pancreatitis, lactic acidosis, hepatic dysfunction, or peripheral neuropathy develops
  • Perform baseline serum amylase and triglycerides in patients with previous history of pancreatitis, elevated amylase, or alcohol abuse
Zidovudine (ZDV)
 200 mg PO 8 hourly or
250 mg PO 12 hourly or
300 mg PO 12 hourly or
1-2 mg/kg IV 4 hourly 		 Adverse Reactions
  • GI effects (nausea/vomiting, anorexia, diarrhea, taste perversion, elevated LFT, pancreatitis); CNS effects (severe headache, insomnia, asthenia, convulsions); Dermatologic effects (nail, skin and oral mucosa pigmentation); Hematologic effects (neutropenia, bone marrow depression); Other effects (myalgia, myopathy, fat redistribution)
  • Potentially fatal hepatotoxicity, lactic acidosis and severe hepatomegaly with steatosis, blood dyscrasias (eg serious anemia that may require transfusion, neutropenia, leukopenia) have been reported
Special Instructions
  • Contraindicated in patients with neutrophil count <0.75 x 109/L or hemoglobin <7.5 g/dL
  • Use with caution in patients with renal and hepatic impairment, anemia or myelosuppression
  • Monitor patients with risk factors for liver disease
  • Blood tests should be carried out regularly; decrease dose if neutrophil or hemoglobin count is low
  • Monitor serum creatine kinase every 3 months in patients who have received >6 months of treatment
*Combinations of NNRTIs and NRTIs are available. Please see the latest MIMS for specific formulations and prescribing information.
^Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with NRTIs alone or in combination.
1Drug interactions listed in the remarks section may not be comprehensive. Please see the latest MIMS for complete drug interaction details and full prescribing information.

Combination Products*


Drug Dosage Remarks1
Combination of INSTI-based Regimens
Elvitegravir 150 mg/Cobicistat 150 mg/Emtricitabine 200 mg/Tenofovir alafenamide 10 mg 1 tab PO 24 hourly Adverse Reactions
  • Significant effects: Immune reconstitution inflammatory symptoms, acute renal injury and/or Fanconi syndrome, opportunistic infections, decreased BMD, osteomalacia, severe acute exacerbation of HBV co-infection
  • GI effects (diarrhea, nausea/vomiting, flatulence, abdominal pain); CNS effects (headache, dizziness, abnormal dreams); Metabolic effects (increased LDL, creatine phosphokinase, amylase and LFTs); Other effects (fatigue, rash, hematuria)
Special Instructions
  • Prior to initiating therapy, test for presence of chronic HBV infection
  • Co-administration with drugs that are highly dependent on CYP3A for clearance and strong CYP3A inducers is contraindicated
  • Use with caution in patients with renal and hepatic impairment
  • Monitor CBC, serum phosphorus, renal and hepatic function, urine glucose and urine protein prior to initiation of therapy and periodically during therapy
Elvitegravir 150 mg/Cobicistat 150 mg/Emtricitabine 200 mg/Tenofovir disoproxil fumarate 300 mg
 1 tab PO 24 hourly
Combination of INSTI and 2 NRTIs
Bictegravir (BIC) 50 mg/Emtricitabine (FTC) 200 mg/Tenofovir alafenamide (TAF) 25 mg 1 tab PO 24 hourly

Adverse Reactions

  • CNS effects (headache, dizziness, depression, abnormal dreams); GI effects (diarrhea, nausea); Other effect (fatigue)

Special Instructions

  • May be administered with or without food
  • Co-administration with Rifampicin and St John's Wort is contraindicated and simultaneous administration of Mg/Al-containing antacids or iron supplements must be avoided
  • Contraindicated in patients with severe hepatic impairment and CrCl <30 mL/min
  • Use with caution in patients with hepatic and renal impairment, HBV and HCV co-infection
Dolutegravir 50 mg/Abacavir 600 mg/Lamivudine 300 mg 1 tab PO 24 hourly

Adverse Reactions

  • CNS effects (insomnia, headache, abnormal dreams, depression, anxiety, nightmares, dizziness, somnolence); GI effects (nausea/vomiting, diarrhea, abdominal pain, dyspepsia, gastroesophageal reflux disease, increased LFTs, creatine phosphokinase); Respiratory effects (cough, nasal symptoms); Dermatologic effects (rash, pruritus); Other effects (fatigue, hypersensitivity, anorexia, lethargy, arthralgia, myalgia, fever, malaise)

Special Instructions

  • May be administered with or without food
  • Do not administer in patients with positive HLA-B*5701 status and in those with negative status but with suspected hypersensitivity to Abacavir
  • Co-administration with medicinal products with narrow therapeutic windows that are substrates of organic cation transporter 2 (eg Fampiridine/Dalfampiridine) is contraindicated
  • Monitor hepatic function and markers of HBV infection (if with co-infection) periodically
Dolutegravir 50 mg /Emtricitabine 200 mg/Tenofovir alafenamide 25 mg  1 tab PO 24 hourly  Adverse Reactions
  • CNS effects (insomnia, headache, abnormal dreams, depression, nightmares, dizziness); GI effects (nausea/vomiting, diarrhea, abdominal pain and discomfort, flatulence, increase LFTs, creatine phosphokinase); Dermatologic effects (rash, pruritus)
Special Instructions
  • May be administered with or without food; preferably with food for patients with Integrase class resistance
  • Discontinue if hypersensitivity reaction develops or if there is evidence of worsening liver disease
  • Co-administration with Dofetilide and other organic cation transporter substrates is contraindicated
  • Avoid simultaneous administration with other cytidine analogues or drugs that reduce exposure such as Mg/Al-containing antacids or iron supplements
  • Use with caution in patients with HBV or HCV co-infection
  • Monitor hepatic function (LFTs, aminotransferases, bilirubin) and markers of HBV replication
Dolutegravir 50 mg /Lamivudine 300 mg/Tenofovir disoproxil fumarate 300 mg  1 tab PO 24 hourly   Adverse Reactions
  • CNS effects (insomnia, headache, abnormal dreams, depression, nightmares, dizziness); GI effects (nausea/vomiting, diarrhea, abdominal pain and discomfort, flatulence, elevated LFTs or creatine phosphokinase); Dermatologic effects (rash, pruritus); Respiratory effects (cough, nasal symptoms); Dermatologic effects (rash,pruritus); Other effects (hypophosphatemia, fatigue, arthralgia)
Special Instructions
  • May be administered with or without food
  • Co-administration with Dofetilide is contraindicated
  • Avoid simultaneous administration with other cytidine analogues or drugs that reduce exposure such as Mg/Al-containing antacids or iron supplements
  • Monitor hepatic function (LFTs, aminotransferases, bilirubin) and markers of HBV replication
Combination of INSTI and 1 NRTI
Dolutegravir 50 mg/Lamivudine 300 mg 1 tab PO 24 hourly 

Adverse Reactions

  • CNS effects (headache, suicidal ideation [particularly in patients with pre-existing history of depression or psychiatric illness], depression, anxiety, insomnia, abnormal dreams, dizziness); GI effects (nausea/vomiting, diarrhea, abdominal pain, flatulence); Dermatologic effects (rash, pruritus, alopecia); Other effects (fatigue, malaise, fever, hyperlactataemia, arthralgia, muscle disorders)

Special Instructions

  • May be administered with or without food
  • Co-administration with medicinal products that have narrow therapeutic windows and drugs that are organic cation transporter substrates is contraindicated
  • Monitor hepatic function (LFTs, aminotransferases, bilirubin) and markers of HBV replication
Combination of NNRTI and 2 NRTIs (NNRTI-based Regimens)
Doravirine 100 mg/Lamivudine 300 mg/Tenofovir disoproxil fumarate 300 mg 1 tab PO 24 hourly

Adverse Reactions

Doravirine
  • CNS effects (insomnia, abnormal dreams, nightmare, depression, headache, dizziness, somnolence); GI effects (nausea/vomiting, diarrhea, abdominal pain); Other effects (rash, fatigue)
Efavirenz
  • Dermatologic effects (rash, Stevens-Johnson syndrome, erythema multiforme, pruritus); CNS effects (dizziness, headache, insomnia, somnolence, abnormal dreams, fatigue, impaired concentration, depression, anxiety, psychosis, amnesia, ataxia); GI effects (nausea/vomiting, diarrhea, hepatitis, abdominal pain); Other effects (gynecomastia, blurred vision)
Emtricitabine
  • GI effects (diarrhea, nausea/vomiting, dyspepsia, abdominal pain); Endocrine and metabolic effects (elevated amylase, lipase, creatine kinase, or LFT levels, hypertriglyceridemia, hypercholesterolemia, hyperglycemia, hyperlactatemia, insulin resistance, hyperbilirubinemia); CNS effects (headache, insomnia, dizziness, abnormal dreams, pain, asthenia); Other effects (anemia, neutropenia, rash, hyperpigmentation)
  • Potentially fatal lactic acidosis and severe hepatomegaly with steatosis have been reported

Lamivudine
  • GI effects (abdominal pain, nausea/vomiting, diarrhea); CNS effects (headache, peripheral neuropathy, insomnia); Metabolic effects (elevated creatine phosphokinase and alanine aminotransferase levels); Other effects (fever, cough, muscle pain, rash, alopecia, malaise, paronychia, angioedema, anaphylactoid reaction, urticaria)
  • Potentially fatal lactic acidosis associated with severe hepatomegaly and hepatic steatosis have been reported
Rilpivirine
  • CNS effects (depression, dysphoria, mood changes, negative thoughts, suicidal ideation, headache, insomnia, dizziness, asthenia, anxiety, abnormal dreams); Dermatologic effect (rash); Metabolic effects (increased LDL, total cholesterol/triglyceride levels); Hepatic effects (elevated liver transaminases and bilirubin levels); Renal effect (elevated creatinine level); Injection site reactions (swelling, erythema, pruritus, bruising, warmth, hematoma); GI effects (decreased appetite, nausea/vomiting, abdominal pain, flatulence, diarrhea, dry mouth)

Tenofovir
  • GI effects (nausea/vomiting, diarrhea, abdominal pain, flatulence, anorexia, dyspepsia, hepatitis); Metabolic effects (hypophosphatemia, increased amylase and liver enzymes, hypertriglyceridemia, hyperglycemia); CNS effects (peripheral neuropathy, headache, depression, asthenia, dizziness, insomnia); Renal effects (nephritis, nephrogenic diabetes insipidus, renal impairment, Fanconi syndrome); Other effects (body fat redistribution, osteomalacia, immune reconstitution syndrome)

Special Instructions

  • Doravirine 100 mg/Lamivudine 300 mg/Tenofovir disoproxil fumarate 300 mg: May be administered with or without food
  • Efavirenz 600 mg/ Emtricitabine 200 mg/Tenofovir disoproxil fumarate 300 mg: Should be taken on an empty stomach (dosing at bedtime to improve tolerability of nervous system symptoms) 
Doravirine
  • Concomitant administration with strong CYP450 enzyme inducers (eg anticonvulsants, androgen receptor inhibitor, antimycobacterials, cytotoxic agents) is contraindicated
  • Contraindicated in patients with galactose intolerance, total lactase deficiency or glucose-galactose malabsorption
  • Use with caution in patients with severe hepatic impairment, end-stage renal disease (ESRD) or those in dialysis
Efavirenz
  • Contraindicated in patients with severe hepatic impairment
  • Use with caution in patients with renal impairment, mild to moderate liver disease, known or suspected hepatitis B infection, history of mental illness and seizures
  • Discontinue use if severe skin rash or fever develops
  • Monitor liver enzymes and cholesterol level
Emtricitabine
  • Use with other Emtricitabine- or Lamivudine-containing preparations are contraindicated
  • Use with caution in patients with renal impairment, hepatomegaly, hepatic steatosis, hepatitis, hepatic impairment or those at risk for liver disease, in patients with hepatitis C coinfection, and patients on alpha-interferon and Ribavirin therapy
  • Test for presence of chronic HBV infection prior to initiating therapy
  • Discontinue use if there is a rapid rise in aminotransferase levels, progressive hepatomegaly or steatosis, metabolic or lactic acidosis of unknown cause
  • Concurrent use of alpha-interferon increases the risk of lactic acidosis
Lamivudine
  • Use with caution in patients with renal impairment, hepatomegaly or other risk factors for hepatic impairment
  • Discontinue use if there is rapid rise in aminotransferase levels, progressive hepatomegaly, metabolic or lactic acidosis of unknown cause, if with clinical signs and symptoms or lab abnormalities suggestive of pancreatitis develop
Rilpivirine
  • Tablet should be taken with food for optimal absorption
  • IM injection should be co-administered with Cabotegravir injection at separate gluteal injection sites
  • Contraindicated in patients with severe hepatic impairment
  • Concurrent use of Carbamazepine, Dexamethasone (>1 dose), Oxcarbazepine, Phenobarbital, Phenytoin, PPIs, Rifabutin, Rifampin, Rifapentine, St John’s wort are contraindicated
  • Use with caution in patients with mild-moderate hepatic impairment, severe renal impairment or ESRD, depressive disorders
Tenofovir
  • Use with caution in patients with renal impairment, hepatomegaly or in those at risk for liver disease
  • Discontinue use if there is rapid rise in aminotransferase levels, progressive hepatomegaly or steatosis, metabolic or lactic acidosis of unknown cause
  • Monitor creatinine clearance and serum phosphorus routinely in patients at risk of renal impairment
  • Bone monitoring for patients with history of pathologic bone fracture or those at risk of osteopenia
 
Efavirenz 600 mg/Emtricitabine 200 mg/Tenofovir disoproxil fumarate 300 mg 1 tab PO 24 hourly
Rilpivirine 25 mg/Emtricitabine 200 mg/Tenofovir alafenamide 25 mg  1 tab PO 24 hourly
Rilpivirine 25 mg/Emtricitabine 200 mg/Tenofovir disoproxil fumarate 300 mg  1 tab PO 24 hourly 
Combination of NRTIs
Abacavir 600 mg/Lamivudine 300 mg 1 tab PO 24 hourly

Adverse Reactions

Abacavir

  • Dermatologic effects (rash, severe/potentially fatal hypersensitivity reactions may occur); GI effects (anorexia, nausea/vomiting, diarrhea, abdominal pain); CNS effects (headache, fatigue, malaise, lethargy); Metabolic effects (elevated blood glucose/triglyceride levels); Other effects (fever, cough, dyspnea)
Lamivudine
  • GI effects (abdominal pain, nausea/vomiting, diarrhea); CNS effects (headache, peripheral neuropathy, insomnia); Metabolic effects (elevated creatine phosphokinase and alanine aminotransferase levels); Other effects (fever, cough, muscle pain, rash, alopecia, malaise, paronychia, angioedema, anaphylactoid reaction, urticaria)
  • Potentially fatal lactic acidosis associated with severe hepatomegaly and hepatic steatosis have been reported

Special Instructions

  • May be administered with or without food
Abacavir
  • Contraindicated in patients with moderate to severe renal and hepatic impairment, ESRD
  • Use with caution in patients with mild liver impairment; discontinue when liver function deteriorates or if hepatomegaly and unexplained metabolic acidosis develop
  • Discontinue as soon as hypersensitivity is suspected
Lamivudine
  • Use with caution in patients with renal impairment, hepatomegaly or other risk factors for hepatic impairment
  • Discontinue use if there is rapid rise in aminotransferase levels, progressive hepatomegaly, metabolic or lactic acidosis of unknown cause, if with clinical signs and symptoms or lab abnormalities suggestive of pancreatitis develop
Abacavir 300 mg/Lamivudine 150 mg/Zidovudine 300 mg 1 tab PO 24 hourly
Emtricitabine 200 mg/Tenofovir disoproxil fumarate 300 mg  1 tab PO 24 hourly   Adverse Reactions

Emtricitabine
  • GI effects (diarrhea, nausea/vomiting, dyspepsia, abdominal pain); Endocrine and metabolic effects (elevated amylase, lipase, creatine kinase, or LFT levels, hypertriglyceridemia, hypercholesterolemia, hyperglycemia, hyperlactatemia, insulin resistance, hyperbilirubinemia); CNS effects (headache, insomnia, dizziness, abnormal dreams, pain, asthenia); Other effects (anemia, neutropenia, rash, hyperpigmentation)
  • Potentially fatal lactic acidosis and severe hepatomegaly with steatosis have been reported
Tenofovir
  • GI effects (nausea/vomiting, diarrhea, abdominal pain, flatulence, anorexia, dyspepsia, hepatitis); Metabolic effects (hypophosphatemia, increased amylase and liver enzymes, hypertriglyceridemia, hyperglycemia); CNS effects (peripheral neuropathy, headache, depression, asthenia, dizziness, insomnia); Renal effects (nephritis, nephrogenic diabetes insipidus, renal impairment, Fanconi syndrome); Other effects (body fat redistribution, osteomalacia, immune reconstitution syndrome)
Special Instructions

 

Emtricitabine
  • Use with other Emtricitabine- or Lamivudine-containing preparations are contraindicated
  • Use with caution in patients with renal impairment, hepatomegaly, hepatic steatosis, hepatitis, hepatic impairment or those at risk for liver disease, in patients with hepatitis C coinfection, and patients on alpha-interferon and Ribavirin therapy
  • Test for presence of chronic HBV infection prior to initiating therapy
  • Discontinue use if there is a rapid rise in aminotransferase levels, progressive hepatomegaly or steatosis, metabolic or lactic acidosis of unknown cause
  • Concurrent use of alpha-interferon increases the risk of lactic acidosis
Tenofovir
  • Use with caution in patients with renal impairment, hepatomegaly or in those at risk for liver disease
  • Discontinue use if there is rapid rise in aminotransferase levels, progressive hepatomegaly or steatosis, metabolic or lactic acidosis of unknown cause
  • Monitor creatinine clearance and serum phosphorus routinely in patients at risk of renal impairment
  • Bone monitoring for patients with history of pathologic bone fracture or those at risk of osteopenia
Emtricitabine 200 mg/Tenofovir alafenamide fumarate 25 mg  1 tab PO 24 hourly  Adverse Reactions
  • GI effects (nausea/vomiting, diarrhea, flatulence); CNS effects (insomnia, headache, abnormal dreams, dizziness); Other effects (rash, fatigue)
Special Instructions
  • May be swallowed whole
  • Co-administration with certain anticonvulsants is contraindicated
  • Monitor liver function in patients with significant underlying liver disorders
Lamivudine 150 mg/Zidovudine 300 mg  ≥30 kg: 1 tab PO 12 hourly   Adverse Reactions

Lamivudine
  • GI effects (abdominal pain, nausea/vomiting, diarrhea); CNS effects (headache, peripheral neuropathy, insomnia); Metabolic effects (elevated creatine phosphokinase and alanine aminotransferase levels); Other effects (fever, cough, muscle pain, rash, alopecia, malaise, paronychia, angioedema, anaphylactoid reaction, urticaria)
  • Potentially fatal lactic acidosis associated with severe hepatomegaly and hepatic steatosis have been reported
Zidovudine
  • GI effects (nausea/vomiting, anorexia, diarrhea, taste perversion, elevated LFT, pancreatitis); CNS effects (severe headache, insomnia, asthenia, convulsions); Dermatologic effects (nail, skin and oral mucosa pigmentation); Hematologic effects (neutropenia, bone marrow depression); Other effects (myalgia, myopathy, fat redistribution)
  • Potentially fatal hepatotoxicity, lactic acidosis and severe hepatomegaly with steatosis, blood dyscrasias (eg serious anemia that may require transfusion, neutropenia, leukopenia) have been reported

Special Instructions

Lamivudine

  • Use with caution in patients with renal impairment, hepatomegaly or other risk factors for hepatic impairment
  • Discontinue use if there is rapid rise in aminotransferase levels, progressive hepatomegaly, metabolic or lactic acidosis of unknown cause, if with clinical signs and symptoms or lab abnormalities suggestive of pancreatitis develop
Zidovudine
  • Contraindicated in patients with neutrophil count <0.75 x 109/L or hemoglobin <7.5 g/dL
  • Use with caution in patients with renal and hepatic impairment, anemia or myelosuppression
  • Monitor patients with risk factors for liver diseaseBlood tests should be carried out regularly; decrease dose if neutrophil or hemoglobin count is low
  • Monitor serum creatine kinase every 3 months in patients who have received >6 months of treatment
Combination of PI + 2NRTIs
Darunavir 800 mg/Cobicistat 150 mg/Emtricitabine 200 mg/Tenofovir alafenamide 10 mg
 1 tab PO 24 hourly   Adverse Reactions
  • GI effects (diarrhea, nausea/vomiting, abdominal pain and distension, dyspepsia, flatulence); Endocrine and metabolic effects (increased pancreatic enzymes, DM, increased LDL, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia); CNS effects (headache, anorexia, asthenia, abnormal dreams, dizziness); Dermatologic effects (rash, pruritus, urticaria); Other effects (anemia, increased hepatic enzyme, increased creatinine, arthralgia, myalgia, fatigue) 
Special Instructions
  • Should be administered with food
  • Contraindicated in patients with severe hepatic impairment, eGFR <30 mL/min, treatment-experienced patients with viral load ≥100,000 copies/mL or CD4 count <100 cells x 106/L
  • Concomitant administration with Carbamazepine, Phenobarbital, Phenytoin, Rifampicin, Lopinavir/Ritonavir, St John's wort, Alfuzosin, Amiodarone, Dronedarone, Quinidine, Ranolazine, ergot derivatives is contraindicated
  • Use with caution in patients with pre-existing liver disease, hemophilia, sulfonamide allergy, mild-moderate hepatic impairment
Combination of PI-based Regimens 
Atazanavir 300 mg/Cobicistat 150 mg  1 tab PO 24 hourly  Adverse Reactions
  • Hepatic effects (hyperbilirubinemia, jaundice, scleral icterus); Metabolic effects (elevated LFTs, creatine kinase, lipase); Renal effects (CKD, nephrolithiasis); CV effects (2nd, 3rd degree AV block, QTc prolongation, torsades de pointes)
Special Instructions
  • May be administered with or without food
  • Concurrent use of ergot derivatives, CYP3A4 substrates, drugs highly dependent on UGT1A1 for clearance and narrow therapeutic index, Cisapride, St John's wort are contraindicated
Darunavir 800 mg/Cobicistat 150 mg  1 tab PO 24 hourly   Adverse Reactions
  • GI effects (diarrhea, nausea/vomiting, abdominal pain); CNS effect (headache); Metabolic effects (hyperglycaemia; hyperlactataemia, insulin resistance, elevated LFTs, triglycerides, creatinine, pancreatic amylase, lipase, cholesterol, creatine phosphokinase)
Special Instructions
  • Should be taken with food
Lopinavir 100 mg/Ritonavir 25 mg tab;
Lopinavir 200 mg/Ritonavir 50 mg tab; 
Lopinavir 400 mg/Ritonavir 100 mg (per 5 mL oral solution)
 ART-naive: 400/100 mg PO 12 hourly (two 200/50 mg tab or 5 ml oral solution) or 800/200 mg PO 24 hourly (four 200/50 mg tab or 10 ml oral solution)
ART-experienced: 400/100 mg PO 12 hourly 
Concomitant therapy with APV, EFV, NVP, NFV: 6.5 ml (Lopinavir 533 mg/Ritonavir 133 mg) oral solution 12 hourly or Lopinavir 500 mg/Ritonavir 125 mg PO 12 hourly 		 Adverse Reactions
  • GI effects (diarrhea, nausea/vomiting, abdominal pain, flatulence, dyspepsia); CNS effects (headache, asthenia, paresthesia, insomnia); Endocrine and metabolic effects (elevated liver enzymes, total cholesterol/triglyceride levels, decreased libido, hypogonadism); Other effects (bronchitis, weight loss)
Special Instructions
  • Tab: May be taken with or without food
  • Oral solution: Should be taken with food
  • Once-daily administration is not recommended in therapy-experienced patients
  • Concurrent use of ergot derivatives, Cisapride, Pimozide, sedatives, Rifampicin, HMG Co-A inhibitors are contraindicated
  • Use with caution in patients with pancreatitis, hepatic impairment, hemophilia
  • See also Ritonavir special instructions
*Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with NRTIs alone or in combination.
1Drug interactions listed in the remarks section may not be comprehensive. Please see prescribing information for specific formulations in the latest MIMS for complete drug interaction details.

Protease Inhibitors (PIs)*


Drug Dosage Remarks1
Amprenavir (APV) Capsules
Combined with Ritonavir: 600 mg PO 12 hourly
Combined with other antiretrovirals:
1,200 mg PO 12 hourly
Oral solution
Combined with other antiretrovirals:
17 mg/kg PO 8 hourly 
Max dose: 2.8 g/day		 Adverse Reactions
  • CNS effects (tremors, mood disorders, oral or perioral paresthesia); GI effects (nausea/vomiting, diarrhea); Endocrine effects (dyslipidemia, redistribution of body fat, buffalo hump, facial atrophy, breast enlargement); Dermatologic effect (rash)
Special Instructions
  • May be taken with or without food, but do not take with a high-fat meal
  • Contraindicated in patients with sulfonamide allergy, renal or hepatic failure, concomitant Metronidazole or Disulfiram therapy
  • Use with caution in patients with diabetes mellitus (DM), when patient is on Sildenafil and vitamin E supplement
  • Use oral solution only when capsule and other PIs are not therapeutic options
  • Potentially fatal interactions with drugs with narrow therapeutic index (eg Cisapride, Terfenadine, Pimozide, Guanidine, Rifampicin) 
Atazanavir (ATV) Treatment-naive: 400 mg PO 24 hourly or 300 mg PO 24 hourly with Ritonavir 100 mg
Treatment-experienced: 300 mg PO 24 hourly with Ritonavir 100 mg		 Adverse Reactions
  • GI effects (nausea/vomiting, diarrhea, taste disturbances, abdominal pain, anorexia, flatulence); CNS effects (asthenia, sleep disturbances, headache, dizziness, paresthesia, hypoesthesia); Musculoskeletal effects (myalgia, arthralgia, myositis, rhabdomyolysis); Dermatologic effects (alopecia, pruritus, rash which may be occasionally severe)
  • Potentially fatal: Stevens-Johnson syndrome and erythema multiforme have been reported
  • Redistribution and accumulation of body fat may occur 
  • May prolong PR interval on ECG 
Special Instructions
  • Concurrent administration with Cisapride, ergot derivatives, Rifampin, Irinotecan, Midazolam, Triazolam, Pimozide, Simvastatin, Lovastatin, Indinavir, PPIs, or St John’s wort are contraindicated
  • Contraindicated in patients with severe hepatic impairment
  • Use with caution in patients with mild-moderate hepatic impairment, DM, hemophilia, history of cardiac conduction disorders
  • Discontinue if acute hemolytic anemia occurs
  • Monitor for signs of lipodystrophy
Darunavir (DRV) Treatment-naive: 800 mg with Ritonavir 100 mg or Cobicistat 150 mg 24 hourly 
Treatment-experienced: 600 mg 12 hourly with Ritonavir 100 mg 12 hourly 
Treatment-experienced without DRV resistance and viral load <100,000 copies/mL and CD4 count ≥100 cells x 106/L: 800 mg with Ritonavir 100 mg or Cobicistat 150 mg 24 hourly		 Adverse Reactions
  • GI effects (diarrhea, abdominal pain, nausea/vomiting, constipation); CNS effect (headache); Other effects (nasopharyngitis, lipodystrophy)
  • May exacerbate DM and hyperglycemia 
Special Instructions
  • Contraindicated in patients with severe hepatic impairment
  • Coadministration with Rifampicin, St John's wort, Phenobarbital, Phenytoin, and medicinal products that have narrow therapeutic index (eg Astemizole, Terfenadine, Midazolam, Triazolam, Cisapride, Pimozide, and ergot alkaloids) are contraindicated
  • Use with caution in patients with sulfonamide allergy and hemophilia, pre-existing liver disease, mild-moderate hepatic impairment
Indinavir (IDV) 800 mg PO 8 hourly
Combined with Efavirenz: 1,000 mg PO 8 hourly
Co-administered with Delavirdine, Itraconazole or Ketoconazole: 600 mg PO 8 hourly 
Combined with Lopinavir and Ritonavir:
600 mg PO 12 hourly
Combined with Nelfinavir: 1,200 mg PO 12 hourly
Combined with Nevirapine: 1,000 mg PO 8 hourly
Combined with Rifabutin: 1,000 mg PO 8 hourly (reduce Rifabutin to ½ the standard dose) 		 Adverse Reactions
  • GI effects (abdominal pain, nausea/vomiting, diarrhea, regurgitation, dyspepsia, dry mouth); Metabolic effects (elevated liver enzymes, bilirubin, creatinine, creatine phosphokinase, blood lipid levels); CNS effects (headache, dizziness, somnolence); Renal effects (nephrolithiasis, flank pain); Respiratory effects (cough, dyspnea); Other effects (alopecia, lipodystrophy, back pain)
  • Potentially fatal acute hemolytic anemia and acute hepatitis have been reported 
Special Instructions
  • Take on an empty stomach (best taken with plain water 1 hour before or 2 hours after meals)
  • Ensure adequate hydration
  • Contraindicated in patients with severe hepatic impairment
  • Concurrent administration with Amiodarone, Cisapride, ergot derivatives, Lovastatin, Simvastatin, Alprazolam, Midazolam, Triazolam, Pimozide, Quinidine, Rifampin, Sildenafil, St John’s wort are contraindicated
  • Use with caution in patients with increased risk of urolithiasis/nephrolithiasis, DM, hemophilia
  • Monitor for signs of lipodystrophy
Nelfinavir (NFV) 750 mg PO 8 hourly or 1,250 mg PO 12 hourly Adverse Reactions
  • GI effects (diarrhea, nausea, flatulence); Endocrine and metabolic effects (hyperglycemia, dyslipidemia, lipodystrophy, hypertriglyceridemia, increased creatine kinase, elevated transaminases); Hematologic effects (decreased lymphocyte, neutrophil and hemoglobin counts) 
Special Instructions
  • Concurrent administration with Amiodarone, Cisapride, ergot derivatives, Lovastatin, Simvastatin, Alprazolam, Midazolam, Triazolam, Pimozide, Quinidine, Rifampin, Sildenafil, St John’s wort are contraindicated
  • Use with caution in patients with hepatic and renal impairment, hemophilia A or B, DM
  • Monitor for signs of lipodystrophy
Ritonavir (RTV)
 600 mg PO 12 hourly or 300 mg PO 12 hourly x 3 days then increase dose by 100 mg PO 12 hourly at 2-3 days interval up to recommended dose of 600 mg PO 12 hourly over a period of not >14 days 
Dosing for PI-based regimens, please refer to dosages of other Protease Inhibitors 		 Adverse Reactions
  • CNS effects (asthenia, fatigue, headache, dizziness, seizures, anxiety, sweating, paresthesia); CV effects (syncope, orthostatic hypotension); GI effects (dry mouth, mouth ulcers, dyspepsia, nausea/vomiting, diarrhea, taste disturbance, pancreatitis); Dermatologic effects (skin rashes, pruritus); Other effects (myalgia, renal insufficiency, anemia, elevated WBC count, raised prothrombin time, lipodystrophy, electrolyte imbalance)
  • Potentially fatal hypersensitivity reactions, anaphylaxis, Stevens-Johnson syndrome have been reported 
Special Instructions
  • Contraindicated in patients with severe hepatic impairment
  • Use with caution in patients with DM, hemophilia, pancreatitis
  • Discontinue treatment if patient develops hemolytic anemia
  • Monitor levels of glucose, lipid, uric acid and blood count
  • Ensure adequate hydration to reduce risk of nephrolithiasis
Saquinavir (SQV)  Combined with Ritonavir: 
1,000 mg PO 12 hourly  		 Adverse Reactions
  • GI effects (nausea/vomiting, diarrhea, taste disturbances, abdominal pain, anorexia, flatulence); CNS effects (asthenia, fatigue, sleep disturbances, headache, dizziness, paresthesia, hypoesthesia); Musculoskeletal effects (myalgia, arthralgia, myositis, rhabdomyolysis); Endocrine and metabolic effects (hyperglycemia, onset or exacerbation of DM, irregular and prolonged heavy menstruation, sexual dysfunction); Other effects (lipodystrophy, blood disorders, ingrowing toenails, paronychia of the great toes, acute paranoid reactions)
  • Potentially fatal hypersensitivity reactions, Stevens-Johnson syndrome, photosensitivity, nephrolithiasis, pancreatitis, hemorrhage, hemolytic anemia, intracranial hemorrhage, respiratory disorder have been reported
Special Instructions
  • Take with food (take at the same time as Ritonavir within 2 hours following a meal)
  • Contraindicated in patients with severe hepatic impairment
  • Use with caution in patients with renal and mild-moderate hepatic impairment, DM, hemophilia, underlying hepatitis B or other liver abnormalities
  • Concomitant use with Sildenafil, NRTIs, Pimozide may cause serious arrhythmogenic, neurologic or other toxicities
Tipranavir (TPV)  Combined with Ritonavir: 
500 mg PO 12 hourly 		 Adverse Reactions
  • GI effects (diarrhea, nausea/vomiting, abdominal pain); CNS effects (headache, fatigue); Metabolic effects (elevated transaminases, total cholesterol/triglyceride levels); Other effects (fever, dehydration, weight loss, myalgia, rash, dyspnea, lipodystrophy) 
Special Instructions
  • Contraindicated in patients with moderate-severe hepatic impairment
  • Concurrent use of ergot derivatives, Cisapride, Pimozide, sedatives, Rifampicin, HMG Co-A inhibitors, immunosuppressive agents are contraindicated
  • Use with caution in patients with DM, hemophilia, mild hepatic impairment, chronic hepatitis B or C co-infection, sulfonamide allergy and those who are at increased risk of bleeding
  • Monitor liver function, cholesterol and triglyceride levels before and during therapy 
*PIs cause dyslipidemia including elevated triglycerides and high cholesterol along with a redistribution in body fat. They also cause hyperglycemia.
2Drug interactions listed in the remarks section may not be comprehensive. Please see the latest MIMS for complete drug interaction details and full prescribing information.

Other Antivirals


Drug Dosage Remarks1
Capsid Inhibitor (Long-Acting)
Lenacapavir Maintenance dosing:
600 mg PO plus 927 mg SC on day 1, then 600 mg PO on day 2, followed by 927 mg SC every 6 months or 
600 mg PO on day 1 and 2, 300 mg PO on day 8, then 927 mg SC on day 15, followed by 927 mg SC every 6 months 		 Adverse Reactions
  • GI effects (nausea/vomiting, diarrhea, elevated liver enzymes); CNS effects (dizziness, headache); Local effects (erythema, hematoma, injection site reactions, pruritus, skin necrosis, skin ulcer); GU effects (proteinuria,glycosuria); Other effects (Guillain-Barre syndrome, hyperglycemia, immune reconstitution syndrome, edema)
Special Instructions
  • Contraindicated in patients on strong CYPA3A inducers
CCR5 Antagonist 
Maraviroc (MVC)
 150 mg PO 12 hourly or 
300 mg PO 12 hourly or
600 mg PO 12 hourly

Adverse Reactions

  • GI effects (GI disorders, dysgeusia); CNS effects (dizziness, somnolence, paresthesia, insomnia); Other effects (increased transaminases, rash, pruritus, back pain, muscle spasms) 

Special Instructions

  • Contraindicated in patients on strong CYPA3A inducers
  • Use with caution in patients with mild-moderate renal or hepatic impairment, patients at risk for CV events, history of postural hypotension
Fusion Inhibitor
Enfuvirtide (T20) 90 mg SC 12 hourly 

Adverse Reactions

  • GI effects (diarrhea, nausea, abdominal pain); CNS effects (fatigue, insomnia); Other effects (pain, infection, erythema at injection site)

Special Instructions

  • Local injection site reactions are common. Administration using a needle-free device has been associated with nerve pain, bruising and hematomas at sites when large nerves are close to the skin; administer only in recommended sites
  • Use with caution in patients with coagulation disorders or in those receiving anticoagulants due to increased risk of bleeding at injection site
Integrase Strand Transfer Inhibitors (INSTIs)
Cabotegravir Oral lead-in therapy:
30 mg PO 24 hourly
(+ Rilpivirine 25 mg) x ≥1 month 
Every month IM dosing
Initiation dose: 600 mg IM at month 2 (+ Rilpivirine 900 mg) administered on final day of oral lead-in therapy 
Continuation dose:
400 mg IM monthly (+ Rilpivirine 600 mg) monthly starting at month 3 onwards, given up to 7 days before or after the date of monthly injection schedule 
Every 2-month IM dosing
Initiation dose: 600 mg IM at month 2 (+ Rilpivirine 900 mg) administered on final day of oral lead-in therapy and at month 3 
Continuation dose:
600 mg IM monthly (+ Rilpivirine 900 mg) starting at month 5 onwards, given up to 7 days before or after the date of every-2-month injection schedule 
Switching from monthly to every 2-month IM dosing
Single dose of 600 mg IM 1 month after last 400 mg continuation dose then 600 mg IM every 2 months thereafter 
Switching from every 2-month to monthly IM dosing
Single dose of 400 mg IM 2 months after last 600 mg continuation dose then 400 mg IM monthly thereafter

Adverse Reactions

  • CNS effects (anxiety, depression, abnormal dreams, insomnia, headache, dizziness, asthenia); GI effects (nausea/vomiting, abdominal pain, flatulence, diarrhea); Dermatologic effect (rash); Injection site effects (injection site pain, nodule, induration, swelling, erythema, pruritis, bruising, warmth, hematoma); Other effects (myalgia, fatigue, malaise, increased weight)

Special Instructions

  • Co-administered with Rilpivirine at separate gluteal injection sites
  • Contraindicated in patients with HBV co-infection
  • Tablets are contraindicated in patients with galactose intolerance, total lactase deficiency or glucose-galactose malabsorption
  • Concomitant administration of Rifampicin, Rifapentine, Carbamazepine, Oxcarbazepine, Phenytoin or Phenobarbital is contraindicated
  • Use with caution in patients with severe hepatic impairment and ESRD or renal replacement therapy
  • Periodic monitoring of LFTs is recommended 
Dolutegravir Patients infected with HIV-1 without documented/clinically suspected resistance to the integrase class:
50 mg PO 24 hourly 
Patients infected with HIV-1 with documented/clinically suspected resistance to the integrase class:
50 mg PO 12 hourly

Adverse Reactions

  • GI effects (nausea/vomiting, diarrhea, abdominal pain and discomfort, flatulence); CNS effects (headache, insomnia, abnormal dreams); Dermatologic effects (rash, pruritus); Other effects (fatigue, increased ALT/AST and creatine phosphokinase)

Special Instructions

  • Use with caution in patients with known resistance to integrase class, osteonecrosis and immune reactivation syndrome
  • Discontinue immediately if signs or symptoms of hypersensitivity develops
  • Monitor the liver biochemistries of patients co-infected with hepatitis B or C
  • Possible development of complications of HIV and opportunistic infections
  • In patients with known resistance to integrase class, co-administration with Efavirenz, Nevirapine, Tipranavir/Ritonavir or Rifampicin should be avoided
Raltegravir (RAL) 400 mg PO 12 hourly or
1,200 mg PO 24 hourly in combination with other antiretroviral agents		 Adverse Reactions
  • GI effects (diarrhea, nausea/vomiting, abdominal pain and distension, flatulence, dyspepsia); Respiratory effects (upper respiratory tract infection, nasopharyngitis, bronchitis); CNS effects (headache, asthenia, dizziness, vertigo, abnormal dreams, insomnia, depression); Metabolic effects (increased ALT, AST, triglycerides, lipase, pancreatic amylase); Other effects (pyrexia, fatigue) 
Special Instructions
  • Use with caution in patients with history of myopathy or rhabdomyolysis, with elevations in transaminases, severe hepatic impairment, pre-existing history of depression or psychiatric illness
  • Rifampin may decrease the serum concentration of Raltegravir; increase dose of Raltegravir to 800 mg 12 hourly (adult dose) when used concomitantly with Rifampin
  • PPIs may increase serum concentration of Raltegravir
1Drug interactions listed in the remarks section may not be comprehensive. Please see the latest MIMS for complete drug interaction details and full prescribing information.

Disclaimer

All dosage recommendations are for non-elderly adults with normal renal and hepatic function unless otherwise stated.  
Not all products are available or approved for above use in all countries.  
Products listed in the Drug Summary are based on indications stated in the locally approved product monographs.   
Please refer to local product monographs in Related MIMS Drugs for country-specific prescribing information.  

Related MIMS Drugs