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Encyclopedia > Lopinavir
Lopinavir chemical structure
Lopinavir
Systematic (IUPAC) name
(2S)-N-[(2S,4S,5S)-5-{[2-(2,6-dimethylphenoxy)
acetyl]amino}-4-hydroxy-1,6-diphenyl-hexan-2-yl]-
3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide
Identifiers
CAS number  ?
ATC code J05AE06
PubChem 92727
DrugBank EXPT00388
Chemical data
Formula C37H48N4O5 
Mol. weight 628.810 g/mol
Pharmacokinetic data
Bioavailability Unknown
Protein binding 99%
Metabolism Hepatic
Half life 5 to 6 hours
Excretion Mostly fecal
Therapeutic considerations
Pregnancy cat. C (U.S.)
Legal status ℞-only (U.S.), POM (UK)
Routes Oral

Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. It is marketed by Abbott as Kaletra®, a co-formulation with a sub-therapeutic dose of ritonavir, as a component of combination therapy to treat HIV/AIDS. IUPAC nomenclature is a systematic way of naming organic chemical compounds. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules . ... DrugBank is a database available at the University of Alberta that provides information about thousands of products. ... A chemical formula (also called molecular formula) is a concise way of expressing information about the atoms that constitute a particular chemical compound. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Atomic mass 12. ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, Symbol, Number nitrogen, N, 7 Chemical series nonmetals Group, Period, Block 15, 2, p Appearance colorless Atomic mass 14. ... General Name, Symbol, Number oxygen, O, 8 Chemical series Nonmetals, chalcogens Group, Period, Block 16, 2, p Appearance colorless Atomic mass 15. ... The molecular mass of a substance (less accurately called molecular weight and abbreviated as MW) is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... The gram or gramme, symbol g, is a unit of mass. ... The mole and its simple conversions into different units of measurements. ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of medication that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... You may be looking for albumen, or egg white. ... Santorio Santorio (1561-1636) in his steelyard balance, from Ars de statica medecina, first published 1614 Metabolism (from μεταβολισμος (metabolismos)) is the biochemical modification of chemical compounds in living organisms anggjgjhnd cell (b). ... The liver is the largest internal organ of the human body. ... The elimination half-life of a drug (or any xenobiotic agent) refers to the timecourse necessary for the quantity of the xenobiotic agent in the body (or plasma concentration) to be reduced to half of its original level through various elimination processes. ... The hour (symbol: h) is a unit of time. ... Excretion is the biological process by which an organism chemically separates waste products from its body. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother. ... Motto: (traditional) In God We Trust (official, 1956–present) Anthem: The Star-Spangled Banner Capital Washington, D.C. Largest city New York City Official language(s) None at the federal level; English de facto Government Federal Republic  - President George W. Bush (R)  - Vice President Dick Cheney (R) Independence - Declared - Recognized... The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... A prescription drug (or POM Prescription Only Medicine, in UK) is a licensed medicine that is regulated by legislation to require a prescription before it can be obtained. ... In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... Antiretroviral drugs are medications for the treatment of infection by retroviruses, primarily HIV. Different classes of antiretroviral drugs act at different stages of the HIV life cycle. ... Protease inhibitors are a class of medication used to treat or prevent viral infections. ... Abbott Laboratories NYSE: ABT is a pharmaceuticals and health care company. ... Ritonavir is a drug from the protease inhibitor class used to treat AIDS. It is manufactured as Norvir® by Abbott Laboratories. ... Human immunodeficiency virus (commonly known as HIV, and formerly known as HTLV-III and lymphadenopathy-associated virus) is a retrovirus that is the cause of the disease known as AIDS, or Acquired Immunodeficiency Syndrome, a syndrome where the immune system begins to fail, leading to many life-threatening opportunistic infections. ... The Red ribbon is a symbol for solidarity with HIV-positive people and those living with AIDS. Acquired immunodeficiency syndrome or Acquired immune deficiency syndrome (AIDS or Aids) is a collection of symptoms and infections in humans resulting from the specific damage to the immune system caused by infection with...


As of 2006, lopinavir/ritonavir forms part of the preferred combination for first-line therapy recommended by the US DHHS.[1] It is available as capsules, tablets and oral solution. The United States Department of Health and Human Services, often abbreviated HHS, is a Cabinet department of the United States government with the goal of protecting the health of all Americans and providing essential human services. ...

Contents


History

Lopinavir was developed by Abbott in an attempt to improve on the HIV resistance and serum protein-binding properties of the company's earlier protease inhibitor, ritonavir.[2] Administered alone, lopinavir has insufficient bioavailability; however, like several HIV protease inhibitors, its blood levels are greatly increased by low doses of ritonavir, a potent inhibitor of cytochrome P450 3A4.[2] Abbott therefore pursued a strategy of co-administering lopinavir with sub-therapeutic doses of ritonavir, and lopinavir is only marketed as a co-formulation with ritonavir. Abbott Laboratories NYSE: ABT is a pharmaceuticals and health care company. ... Ritonavir is a drug from the protease inhibitor class used to treat AIDS. It is manufactured as Norvir® by Abbott Laboratories. ... Cytochrome P450 Oxidase (CYP2E1) Cytochrome P450 oxidase (commonly abbreviated CYP) is a generic term for a large number of related, but distinct, oxidative enzymes (EC 1. ... Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1. ...


Lopinavir/ritonavir was approved by the US FDA on 15 September 2000, and in Europe in April 2001. United States may refer to: Places: United States of America SS United States, the fastest ocean liner ever built. ... This article or section is in need of attention from an expert on the subject. ...


Adverse effects

The most common adverse effects observed with lopinavir/ritonavir are diarrhoea and nausea. In key clinical trials, moderate or severe diarrhoea occurred in up to 27% of patients, and moderate/severe nausea in up to 16%.[3] Other common adverse effects include abdominal pain, asthenia, headache, vomiting and, particularly in children, rash.[3] Diarrhea or diarrhoea (see spelling differences) is a condition in which the sufferer has frequent watery, loose bowel movements (from the ancient Greek word διαρροή = leakage; lit. ... For other uses, see Nausea (disambiguation). ... Abdominal pain can be one of the symptoms associated with transient disorders or serious disease. ... Asthenia is a medical term denoting weakness, lack of energy and strength. ... A headache (medically known as cephalalgia) is a condition of pain in the head; sometimes neck or upper back pain may also be interpreted as a headache. ... Although it has probably evolved as a mechanism for expelling ingested poisons, vomiting (or emesis)may result from many causes not related to poisoning, ranging from gastritis to brain tumors, or elevated intracranial pressure (ICP). ... A typical rash A rash is a change in the skin which affects its appearance or texture. ...


Raised liver enzymes and hyperlipidemia (both hypertriglyceridemia and hypercholesterolemia) are also commonly observed during lopinavir/ritonavir treatment. Hypercholesterolemia (literally: high blood cholesterol) is the presence of high levels of cholesterol in the blood. ... In medicine, hypertriglyceridemia denotes high (hyper-) blood levels (-emia) of triglycerides, the most abundant fatty molecule in most organisms. ... Hypercholesterolemia (literally: high blood cholesterol) is the presence of high levels of cholesterol in the blood. ...


References

  1. ^ DHHS panel. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (May 4, 2006). (Available for download from AIDSInfo)
  2. ^ a b Sham HL, Kempf DJ, Molla A, et al. (1998) ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob. Agents Chemother. 42: 3218-24
  3. ^ a b KALETRA® (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2005

External link


Antivirals (ATC J05A) edit
Anti-herpesvirus agents   Aciclovir · Cidofovir · Docosanol · Famciclovir · Foscarnet · Fomivirsen · Ganciclovir · Idoxuridine · Penciclovir · Trifluridine · Tromantadine · Valaciclovir · Valganciclovir · Vidarabine
Anti-influenza agents Amantadine · Oseltamivir · Peramivir · Rimantadine · Zanamivir
 
Antiretroviral drugs   NRTIs Zidovudine · Didanosine · Stavudine · Zalcitabine · Lamivudine · Abacavir · Tenofovir · Emtricitabine
NNRTIs   Nevirapine · Efavirenz · Delavirdine
NtRTIs   Tenofovir · Adefovir
PIs Saquinavir · Indinavir · Atazanavir · Ritonavir · Nelfinavir · Amprenavir · Fosamprenavir · Lopinavir · Tipranavir · Darunavir
 
Other antiviral agents Fomivirsen · Enfuvirtide · Imiquimod · Interferon · Ribavirin · Viramidine

  Results from FactBites:
 
Lopinavir - Wikipedia, the free encyclopedia (381 words)
Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class.
Lopinavir was developed by Abbott in an attempt to improve on the HIV resistance and serum protein-binding properties of the company's earlier protease inhibitor, ritonavir.
Administered alone, lopinavir has insufficient bioavailability; however, like several HIV protease inhibitors, its blood levels are greatly increased by low doses of ritonavir, a potent inhibitor of cytochrome P450 3A4.
MedlinePlus Drug Information: Lopinavir and Ritonavir (923 words)
Lopinavir is in a class of medications called protease (pro' tee ace) inhibitors.
Lopinavir and ritonavir is not a cure and may not decrease the number of HIV-related illnesses.
Lopinavir and ritonavir may cause increases in levels of cholesterol and other fats (triglycerides) in the blood.
  More results at FactBites »

 
 

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