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Recent Developments in Therapies and Strategies Against COVID-19
Published in Hanadi Talal Ahmedah, Muhammad Riaz, Sagheer Ahmed, Marius Alexandru Moga, The Covid-19 Pandemic, 2023
Misbah Hameed, M. Zia-Ul-Haq, Marius Moga
Lopinavir is a protease inhibitor and is prepared from structurally similar ritonavir antiretroviral agents. Aspartic protease is essential for the cleavage of proteins from precursor polypeptide strand of virus, which is needed for structural and functional proteins. The inhibition of protease results in immature and non-effective virions [20]. Lopinavir is a selective inhibitor of the HIV type 1 (HIV-1), which is required for mature infective virus production. The drug blocks infectivity by blocking the maturation of HIV-1. Lopinavir is a highly potent. These two drugs are available as formulation because when co-administered, ritonavir at low doses improves the pharmacokinetic profile and the activity of lopinavir against HIV-1 protease [21].
Antimicrobials during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Lopinavir is a protease inhibitor used, in combination with ritonavir, for the treatment of HIV-infected women to prevent vertical transmission of HIV. An aggregate analysis of 10 published studies included 2,800 pregnancies exposed to lopinavir reported no increased frequency of birth defects. One study of 267 women who used the drug during the first trimester, the frequency of birth defects was not increased (Roberts et al., 2009). In another study, 270 women used lopinavir during the first trimester, and the frequency of congenital anomalies was not increased (Shapiro et al., 2010). The Antiretroviral Pregnancy Registry reported 1,418 first trimester exposure to lopinavir and the frequency of birth defects was not increased (Antiretroviral Registry, 2018).
Investigational Nanomedicines in 2016: A Review of Nanotherapeutics Currently Undergoing Clinical Trials *
Published in Valerio Voliani, Nanomaterials and Neoplasms, 2021
Joseph M. Caster, Artish N. Patel, Tian Zhang, Andrew Wang
Saint Stephens Aids Trust and the University of Liverpool are investigating polymeric nanoformulations of two antiretroviral agents used for HIV treatment. Efavirenz is a non-nucleoside reverse transcriptase inhibitor clinically used as the preferred first line treatment for HIV infection [70]. Lopinavir is a protease inhibitor commonly utilized in combination therapy. Nano-formulations of these antiretroviral agents aim to reduce total dosage and cost in order to improve patient tolerability while maintaining clinical efficacy. Preclinical studies have demonstrated bioequivalent efficacy in suppressing HIV-1 replication and slower emergence of drug resistance with HIV-IIIB and subtype A virus. Development of NANOEfavirenz and NANOLopinavir has reached phase I trials examining safety and tolerability in HIV negative, healthy patients as well as the bioequivalence of these nanoformulations to the free drugs Sustiva (Efavirenz) and Kaletra (Lopinavir/Ritonavir). Results have yet to be published.
Dried blood spot sampling for therapeutic drug monitoring: challenges and opportunities
Published in Expert Review of Clinical Pharmacology, 2023
Isadora Ritter Müller, Gabriel Linden, Mariele Feiffer Charão, Marina Venzon Antunes, Rafael Linden
Another study that employed DBS for TDM in resource-poor regions is described in the literature, with the aim of quantifying antiretroviral drugs. Plasma and DBS samples were collected from study patients treated with nevirapine, efavirenz or lopinavir in Tanzania. Within the framework of an adherence assessment study, 299 patients were included, and both plasma and DBS samples were collected [45]. The plasma samples were shipped to a specialized bioanalytical laboratory in Switzerland on dry ice, while the DBS samples were shipped at room temperature. During the field study, the level of agreement between plasma and DBS samples was deemed satisfactory for efavirenz. However, the concentration of lopinavir in DBS was found to be lower by an average of 52% compared to plasma, and even after correction, the concentrations were still ~ 30% lower. The authors attribute this result to the prolonged storage and sample shipment, which caused the degradation of lopinavir in DBS samples [46].
Effect of Aspirin Use on clinical Outcome among Critically Ill Patients with COVID- 19
Published in Egyptian Journal of Anaesthesia, 2022
Rania M. Ali, Ayman I. Tharwat, Heba A. Labib
All the critically ill patients admitted to the ICU received full care in accordance with the COVID management protocol at Ain Shams University Hospital. Available antiviral drug was administered, Lopinavir–Ritonavir (200/50 mg) two tablets bid for 5–10 days or Favipiravir if available 1600 mg twice day 1 then 600 mg twice for 9 days. If cytokine storm was diagnosed, tocilizumab was added as 8 mg/kg and the response was assessed, if the patient needed second dose it was calculated as 4 mg/kg after 12 hrs. If tocilizumab was not available, methylprednisolone 1–2 mg/kg/day IV up to 500 mg/day intravenous infusion for 5 days was given, followed by half the previous dose for 2 days then gradual withdrawal in the following days. Self-prone positioning was encouraged for all patients as tolerated unless there was a contraindication. All patients received oxygen therapy, which was escalated depending on the patient’s condition to non-invasive mechanical ventilation (NIMV) for lung recruitment using high-flow nasal oxygen (HFNO) administration or non-invasive positive pressure ventilation (NIPPV) to reach the target oxygen saturation level of greater than 94%. If the tidal volume for patients utilizing NIPPV exceeded 9 ml/kg of predicted body weight or the ROX index score, the ratio of oxygen saturation/fraction of inspired oxygen to respiratory rate fell below 3.85 for patients utilizing HFNO therapy and switch to invasive mechanical ventilation with lung protective methods was decided.
Recent advances in nanoformulation development of Ritonavir, a key protease inhibitor used in the treatment of HIV-AIDS
Published in Expert Opinion on Drug Delivery, 2022
Srinivas Reddy Jitta, Navya Ajitkumar Bhaskaran, Shirleen Miriam Marques, Lalit Kumar
Saquinavir is the first-ever protease inhibitor for the treatment of HIV, approved by the US Food and Drug Administration (US FDA). Saquinavir has very poor solubility in the aqueous phase, and its solubility is highly pH-dependent. Along with poor solubility, metabolism by hepatic and small intestinal enzymes are the main reasons for the poor bioavailability [40–42]. Second-generation protease inhibitors used in the treatment of HIV, such as Darunavir, are associated with low oral bioavailability, adverse effects such as liver toxicity and skin rashes. High lipophilic nature, low water solubility, and first-pass metabolism are the major factors for low oral bioavailability [43,44]. Indinavir, a specific protease inhibitor used to treat HIV infection, belongs to BCS class IV with low permeability and low solubility. Clinical application of this drug is limited by low gastrointestinal absorption, short half-life, and extensive hepatic first-pass metabolism [1,45]. Nelfinavir mesylate is an HIV protease inhibitor and an important integral component of highly active antiretroviral therapy (HAART) used in the treatment of AIDS [46]. Lopinavir, a protease inhibitor used in the treatment of HIV, and this drug block the ability of HIV protease to cleave polyprotein resulting in the formation of noninfectious immature virions [38]. Lopinavir exhibits poor oral bioavailability as it is a substrate for the P-gp system and CYP 3A4 present in both intestine and liver [38,47].