Clinical Pharmacology Details


EFAVIRENZ


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Indications & Dose:

Combination therapy for HIV -1



Adult and Child >40 kg


• 600 mg qd


Child < 40 kg


• 10-< 15 kg: 200 mg qd; 15-<20 kg: 250 mg qd; 20-<25 kg: 300 mg qd; 25-<32.5 kg: 350 mg qd; 32.5<40 kg: 400 mg qd

Contraindications:

Side Effects:

CNS: CNS side effects seen in 52% of patients, abnormal dreams, amnesia, anxiety, confusion, depression, dizziness, impaired concentration, insomnia, tremor


CV: Flushing, palpitations, tachycardia


EENT: Tinnitus


GI: Diarrhea, elevated transaminases, nausea


METAB: Hyperlipidemia


MS: Arthralgia, myalgia


RESP:Asthma


SKIN: Rash (27%) 

Cautions:

Precautions:

Depression, liver disease, pregnancy (fetal malformations observed in monkeys)


 

Interaction:

Drugs


• Amprenavir: Efavirenz decreases amprenavir plasma level; amprenavir dose adjustment recommended


• Barbiturates: Barbiturates decrease plasma efavirenz levels; dose adjustment not recommended


• Carbamazepine: Carbamazepine decreases plasma efavirenz levels; dose adjustment not recommended


• Cisapride: Efavirenz increases cisapride plasma level; coadministratioh not recommended


• Clarithromycin: Efavirenz decreases clarithromycin plasma levels; coadministration not recommended


• Ergotamines: Efavirenz increases ergotamine plasma level; coadministration not recommended


• Ethinyl estradiol: Efavirenz increases ethinyl estradiol plasma levels; dose adjustment not recommended


• lndinavir: Efavirenz reduces indinavir AUC by 31 %; increase indinavir dose to 1000 mg q8h


• Lopinavir: Decreasd plasma lopinavir concentrations; consider increase dose of lopinavir/ ritonavir combination to 533 mg lopinavir and 133 mg ritonavir


• Lovastatin: Efavirenz increases lovastatin plasma level; dose adjustment not recommended


• Midazolam: Efavirenz increases midazolam plasma level; coadministration not recommended


• Nelfinavir: Efavirenz increases nelfinavir AUC by 20%; dose adjustment not recommended


• Phenobarbital: Decreased plasma efavirenz concentrations


• Phenytoin: Phenytoin decreases plasma efavirenz level; dose adjustment not recommended


• Psychoactive drugs: Potential for additive CNS effects


• Rifabutin: Efavirenz decreases plasma rifabutin level by 35%; no change in plasma efavirenz level; increase rifabutin dose to 450 mg qd


• Rifampin: Rifampin decreases plasma efavirenz level by 25%; dose adjustment not recommended


• Ritonavir: Ritonavir increases efavirenz AUC by 21%; efavirenz increases- ritordvir AUC- by 18%; dose-adjustment not recommended


• St. John’s Wort (Hypericum perforatum):Substantial decrease in plasma efavirenz concentrations likely; coadministration not recommended


• Saquinavir: Saquinavir reduces efavirenz AUC by 12%; efavirenz reduces saquinavir AUC by 62%; coadministration not recommended


• Simvastatin: Efavirenz increases simvastatin plasma level; dose adjustment not recommended


• Triazolam: Efavirenz increases triazolam plasma level; coadministration not recommended


• Warfarin: Efavirenz increases warfarin effect


 

Warnings:

Adverse Effects:

Lactations:

Pregnancy category C (fetal malformations observed in monkeys); breast feeding not recommended 

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

Patient And Carer Advice: