Medications and cautions

Table 7. Specific medications and cautions

Medication Comments and cautions
Tenofovir
  • Daily dosing. Tenofovir disoproxil fumarate/emtricitabine or tenofovir with lamivudine have superior tolerability when compared to zidovudine/ lamivudine or stavudine with lamivudine.
  • Use with caution or avoid in renal disease (eGFR <60), dose reduction required in renal impairment.
  • Use zidovudine/lamivudine where tenofovir is directly contraindicated and seek expert advice.
Dolutegravir
  • Daily dosing. Well tolerated when used in PEP with high rates of adherence and regimen completion rates.
Drugs that are contraindicated
  • Dofetilide (not available in Australia).
Drugs that should be used with caution
  • Phenytoin, phenobarbital, rifampicin, St John’s Wort, carbamazepine - increase dolutegravir dose to 50mg BD or stop St. John’s Wort.
  • Antacids containing polyvalent cations e.g. Mg or Al – use at least 2 hours before or 6 hours after the dolutegravir dose.
  • Products containing calcium or iron – use at least 2 hours before or 6 hours after the dolutegravir dose OR dose concomitantly with food.
  • Metformin – increase monitoring of glycaemic control, adjustment in metformin dose may be required.
Raltegravir
  • BD dosing. Well tolerated when used in PEP with high rates of adherence and regimen completion rates.
  • Small risk of rhabdomyolysis – inform patients about the potential for myalgia and the need to re-present if myalgia occurs.
  • Advise against the use of statins while on PEP containing raltegravir.
  • Caution patients who engage in heavy gym work about the increased risk of rhabdomyolysis, especially when anabolic steroids are used.
  • Consider switching to dolutegravir or rilpivirine (see below) in patients who report myalgia on raltegravir.
  • Check CK, renal function and urinary myoglobin in patients who report myalgia on raltegravir.
Rilpivirine Daily dosing. Well tolerated when used in PEP with high rates of adherence and regimen completion rates.
  • MUST be taken with food. Rilpivirine taken without food results in at least a 40% drop in drug exposure.
Drugs that are contraindicated
  • Carbamazepine, oxcarbazepine, phenobarbital, phenytoin
  • Rifabutin, rifampicin, rifapentine
  • Dexamethasone
  • Omeprazole, lansoprazole, pantoprazole, esomeprazole
  • St. John’s Wort.
Drugs that should be used with caution
  • Famotidine, cimetidine, nizatidine, ranitidine – administer at least 4 hours after rilpivirine dose
  • Aluminium or magnesium hydroxide, calcium carbonate – administer 2 hours before or 4 hours after rilpivirine dose.
Zidovudine BD dosing. Frequent side effects. Not recommended as a first-line agent.
Efavirenz, Nevirapine, Abacavir, Didanosine (or in combination with Stavudine) Are not recommended due to excessive toxicity and/or life-threatening hypersensitivity reaction.20,21
Protease Should be avoided because of high rates of potential drug interactions with other commonly used licit and illicit medications as well as the high rates of gastrointestinal side effects and regimen discontinuation. 22

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