abacavir--lamivudine-drug-combination and Headache

Integrase inhibitors are the latest drug family to be added to the therapeutic arsenal against human immunodeficiency virus infection. Drugs in this family that do not require pharmacological boosting are characterized by a very good safety profile. The latest integrase inhibitor to be approved for use is dolutegravir. In clinical trials, dolutegravir has shown an excellent tolerability profile, both in antiretroviral-naïve and previously treated patients. Discontinuation rates due to adverse effects were 2% and 3%, respectively. The most frequent adverse effects were nausea, headache, diarrhea and sleep disturbance. A severe hypersensitivity reaction has been reported in only one patient. In patients coinfected with hepatropic viruses, the safety profile is similar to that in patients without coinfection. The lipid profile of dolutegravir is similar to that of raltegravir and superior to those of Atripla® and darunavir/ritonavir. Dolutegravir induces an early, predictable and non-progressive increase in serum creatinine of around 10% of baseline values in treatment-naïve patients and of 14% in treatment-experienced patients. This increase is due to inhibition of tubular creatinine secretion through the OCT2 receptor and does not lead to a real decrease in estimated glomerular filtration rate with algorithms that include serum creatinine. The effect of the combination of dolutegravir plus Kivexa(®) on biomarkers of bone remodeling is lower than that of Atripla(®). Dolutegravir has an excellent tolerability profile with no current evidence of long-term adverse effects. Its use is accompanied by an early and non-progressive increase in serum creatinine due to OCT2 receptor inhibition. In combination with abacavir/lamivudine, dolutegravir has a lower impact than enofovir/emtricitabine/efavirenz on bone remodelling markers.

Topics: Bone Remodeling; Clinical Trials as Topic; Creatinine; Dideoxynucleosides; Drug Combinations; Drug Hypersensitivity; Drug Therapy, Combination; Gastrointestinal Diseases; Headache; Hepatitis, Viral, Human; Heterocyclic Compounds, 3-Ring; HIV Infections; HIV Integrase Inhibitors; Humans; Immune Reconstitution Inflammatory Syndrome; Kidney Tubules; Lamivudine; Lipid Metabolism; Mood Disorders; Organic Cation Transport Proteins; Organic Cation Transporter 2; Oxazines; Piperazines; Pyridones; Respiration Disorders; Sleep Initiation and Maintenance Disorders

Ergotism is an ischaemic complication due to vasoconstriction throughout the body due to ingestion of ergotamine. A 34-year-old Hispanic man with HIV infection treated with saquinavir, ritonavir and abacavir/lamivudine presented to the emergency department complaining of left foot pain 1 week prior to admission. The affected extremity was cold with absence of pedal and tibial pulses. Arterial Doppler revealed absent arterial flow from the popliteal artery later confirmed by arteriography. Medication reconciliation revealed a recent prescription for migraine headache containing ergotamine. Drug was discontinued and the patient was started on cilostazol, enoxaparin and nitroglycerin patches on the affected limb. Complete resolution of symptoms and arteriography findings occurred 2 days after therapy began.

Topics: Adult; Anti-HIV Agents; Anticoagulants; Cilostazol; Cytochrome P-450 CYP3A Inhibitors; Dideoxynucleosides; Drug Combinations; Drug Interactions; Enoxaparin; Ergotamine; Ergotism; Headache; HIV Infections; Humans; Ischemia; Lamivudine; Lower Extremity; Male; Nitroglycerin; Ritonavir; Saquinavir; Tetrazoles; Tibial Arteries; Ultrasonography, Doppler, Color; Vasoconstrictor Agents; Vasodilator Agents