Antiretroviral therapy (ART) targets the replication cycle Cycle The type of signal that ends the inspiratory phase delivered by the ventilator Invasive Mechanical Ventilation of the human immunodeficiency Immunodeficiency Chédiak-Higashi Syndrome virus Virus Viruses are infectious, obligate intracellular parasites composed of a nucleic acid core surrounded by a protein capsid. Viruses can be either naked (non-enveloped) or enveloped. The classification of viruses is complex and based on many factors, including type and structure of the nucleoid and capsid, the presence of an envelope, the replication cycle, and the host range. Virology (HIV) and is classified based on the viral enzyme or mechanism that is inhibited. The goal of therapy is to suppress viral replication to reach the outcome of undetected viral load Viral load The quantity of measurable virus in a body fluid. Change in viral load, measured in plasma, is sometimes used as a surrogate marker in disease progression. HIV Infection and AIDS. Currently, reverse transcriptase Reverse transcriptase A reverse transcriptase encoded by the pol gene of HIV. It is a heterodimer of 66 kda and 51 kda subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse h activity that plays an essential role the viral replication process. HIV Infection and AIDS, protease Protease Enzyme of the human immunodeficiency virus that is required for post-translational cleavage of gag and gag-pol precursor polyproteins into functional products needed for viral assembly. HIV protease is an aspartic protease encoded by the amino terminus of the pol gene. HIV Infection and AIDS, integrase Integrase Enzyme of the human immunodeficiency virus that is required to integrate viral DNA into cellular DNA in the nucleus of a host cell. HIV integrase is a DNA nucleotidyltransferase encoded by the pol gene. HIV Infection and AIDS, and entry inhibitors are used in combined ART (cART) regimens. Combination therapy (3-drug regimen) is used to prevent drug resistance Resistance Physiologically, the opposition to flow of air caused by the forces of friction. As a part of pulmonary function testing, it is the ratio of driving pressure to the rate of air flow. Ventilation: Mechanics of Breathing and cross- resistance Resistance Physiologically, the opposition to flow of air caused by the forces of friction. As a part of pulmonary function testing, it is the ratio of driving pressure to the rate of air flow. Ventilation: Mechanics of Breathing, which develop through genetic mutations Genetic Mutations Carcinogenesis.
Last updated: 5 May, 2022
Contents
HIV replication
HIV replication
Human Immunodeficiency Virus (HIV)
cycle
Cycle
The type of signal that ends the inspiratory phase delivered by the ventilator
Invasive Mechanical Ventilation:
1. Virion binds the CD4
receptor
Receptor
Receptors are proteins located either on the surface of or within a cell that can bind to signaling molecules known as ligands (e.g., hormones) and cause some type of response within the cell.
Receptors and a chemokine
receptor
Receptor
Receptors are proteins located either on the surface of or within a cell that can bind to signaling molecules known as ligands (e.g., hormones) and cause some type of response within the cell.
Receptors, followed by a conformational change that facilitates fusion of the virion and the host cell.
2. A
capsid
Capsid
The outer protein protective shell of a virus, which protects the viral nucleic acid. Capsids are composed of repeating units (capsomers or capsomeres) of capsid proteins which when assembled together form either an icosahedral or helical shape.
Virology protein shell (surrounding the viral
RNA
RNA
A polynucleotide consisting essentially of chains with a repeating backbone of phosphate and ribose units to which nitrogenous bases are attached. RNA is unique among biological macromolecules in that it can encode genetic information, serve as an abundant structural component of cells, and also possesses catalytic activity.
RNA Types and Structure and
proteins
Proteins
Linear polypeptides that are synthesized on ribosomes and may be further modified, crosslinked, cleaved, or assembled into complex proteins with several subunits. The specific sequence of amino acids determines the shape the polypeptide will take, during protein folding, and the function of the protein.
Energy Homeostasis) is uncoated as the virion traverses the cytoplasm.
3.
Reverse transcriptase
Reverse transcriptase
A reverse transcriptase encoded by the pol gene of HIV. It is a heterodimer of 66 kda and 51 kda subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse h activity that plays an essential role the viral replication process.
HIV Infection and AIDS-mediated
synthesis
Synthesis
Polymerase Chain Reaction (PCR) of proviral
DNA
DNA
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
DNA Types and Structure occurs.
4. Viral
DNA
DNA
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
DNA Types and Structure is transported across the
nucleus
Nucleus
Within a eukaryotic cell, a membrane-limited body which contains chromosomes and one or more nucleoli (cell nucleolus). The nuclear membrane consists of a double unit-type membrane which is perforated by a number of pores; the outermost membrane is continuous with the endoplasmic reticulum. A cell may contain more than one nucleus.
The Cell: Organelles and integrated into the host
DNA
DNA
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
DNA Types and Structure, facilitated by
integrase
Integrase
Enzyme of the human immunodeficiency virus that is required to integrate viral DNA into cellular DNA in the nucleus of a host cell. HIV integrase is a DNA nucleotidyltransferase encoded by the pol gene.
HIV Infection and AIDS.
5. Viral
DNA
DNA
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
DNA Types and Structure is transcribed, and multiple copies of new HIV
RNA
RNA
A polynucleotide consisting essentially of chains with a repeating backbone of phosphate and ribose units to which nitrogenous bases are attached. RNA is unique among biological macromolecules in that it can encode genetic information, serve as an abundant structural component of cells, and also possesses catalytic activity.
RNA Types and Structure form and are transported to the cytoplasm. New HIV
RNA
RNA
A polynucleotide consisting essentially of chains with a repeating backbone of phosphate and ribose units to which nitrogenous bases are attached. RNA is unique among biological macromolecules in that it can encode genetic information, serve as an abundant structural component of cells, and also possesses catalytic activity.
RNA Types and Structure becomes the
genome
Genome
The complete genetic complement contained in the DNA of a set of chromosomes in a human. The length of the human genome is about 3 billion base pairs.
Basic Terms of Genetics of a new
virus
Virus
Viruses are infectious, obligate intracellular parasites composed of a nucleic acid core surrounded by a protein capsid. Viruses can be either naked (non-enveloped) or enveloped. The classification of viruses is complex and based on many factors, including type and structure of the nucleoid and capsid, the presence of an envelope, the replication cycle, and the host range.
Virology. Cytokine activation of the cell also occurs.
6. New viral
RNA
RNA
A polynucleotide consisting essentially of chains with a repeating backbone of phosphate and ribose units to which nitrogenous bases are attached. RNA is unique among biological macromolecules in that it can encode genetic information, serve as an abundant structural component of cells, and also possesses catalytic activity.
RNA Types and Structure +
proteins
Proteins
Linear polypeptides that are synthesized on ribosomes and may be further modified, crosslinked, cleaved, or assembled into complex proteins with several subunits. The specific sequence of amino acids determines the shape the polypeptide will take, during protein folding, and the function of the protein.
Energy Homeostasis +
enzymes
Enzymes
Enzymes are complex protein biocatalysts that accelerate chemical reactions without being consumed by them. Due to the body’s constant metabolic needs, the absence of enzymes would make life unsustainable, as reactions would occur too slowly without these molecules.
Basics of Enzymes move to the cell surface and form a
noninfectious
Noninfectious
Febrile Infant particle.
7. Particle (viral
RNA
RNA
A polynucleotide consisting essentially of chains with a repeating backbone of phosphate and ribose units to which nitrogenous bases are attached. RNA is unique among biological macromolecules in that it can encode genetic information, serve as an abundant structural component of cells, and also possesses catalytic activity.
RNA Types and Structure +
proteins
Proteins
Linear polypeptides that are synthesized on ribosomes and may be further modified, crosslinked, cleaved, or assembled into complex proteins with several subunits. The specific sequence of amino acids determines the shape the polypeptide will take, during protein folding, and the function of the protein.
Energy Homeostasis) eventually buds out of the host cell with the immature HIV. Viral protein
protease
Protease
Enzyme of the human immunodeficiency virus that is required for post-translational cleavage of gag and gag-pol precursor polyproteins into functional products needed for viral assembly. HIV protease is an aspartic protease encoded by the amino terminus of the pol gene.
HIV Infection and AIDS (enzyme) then cleaves newly synthesized polyproteins producing a mature HIV.
Type of drug | Mechanism of action |
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Reverse transcriptase
Reverse transcriptase
A reverse transcriptase encoded by the pol gene of HIV. It is a heterodimer of 66 kda and 51 kda subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse h activity that plays an essential role the viral replication process.
HIV Infection and AIDS inhibitors
|
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Integrase Integrase Enzyme of the human immunodeficiency virus that is required to integrate viral DNA into cellular DNA in the nucleus of a host cell. HIV integrase is a DNA nucleotidyltransferase encoded by the pol gene. HIV Infection and AIDS strand transfer inhibitors (INSTIs) |
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Protease Protease Enzyme of the human immunodeficiency virus that is required for post-translational cleavage of gag and gag-pol precursor polyproteins into functional products needed for viral assembly. HIV protease is an aspartic protease encoded by the amino terminus of the pol gene. HIV Infection and AIDS inhibitors (PIs) |
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Entry inhibitors:
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Post- attachment Attachment The binding of virus particles to virus receptors on the host cell surface, facilitating virus entry into the cell. Virology inhibitor | Binds CD4 molecule, blocking entry but not the attachment Attachment The binding of virus particles to virus receptors on the host cell surface, facilitating virus entry into the cell. Virology |
Schematic description of the mechanism of four classes of antiretroviral drugs against HIV:
Fusion or entry inhibitors: interfere with the binding, fusion or entry of the
HIV virion
HIV virion
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human t-lymphotropic virus type iii/lymphadenopathy-associated virus. From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.
Human Immunodeficiency Virus (HIV)
Reverse transcriptase
Reverse transcriptase
A reverse transcriptase encoded by the pol gene of HIV. It is a heterodimer of 66 kda and 51 kda subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse h activity that plays an essential role the viral replication process.
HIV Infection and AIDS inhibitors: interfere with the reverse
transcription
Transcription
Transcription of genetic information is the first step in gene expression. Transcription is the process by which DNA is used as a template to make mRNA. This process is divided into 3 stages: initiation, elongation, and termination.
Stages of Transcription of viral
RNA
RNA
A polynucleotide consisting essentially of chains with a repeating backbone of phosphate and ribose units to which nitrogenous bases are attached. RNA is unique among biological macromolecules in that it can encode genetic information, serve as an abundant structural component of cells, and also possesses catalytic activity.
RNA Types and Structure into
DNA
DNA
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
DNA Types and Structure
Integrase
Integrase
Enzyme of the human immunodeficiency virus that is required to integrate viral DNA into cellular DNA in the nucleus of a host cell. HIV integrase is a DNA nucleotidyltransferase encoded by the pol gene.
HIV Infection and AIDS inhibitor: prevent the insertion of the viral
genome
Genome
The complete genetic complement contained in the DNA of a set of chromosomes in a human. The length of the human genome is about 3 billion base pairs.
Basic Terms of Genetics into the host
DNA
DNA
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
DNA Types and Structure
Protease
Protease
Enzyme of the human immunodeficiency virus that is required for post-translational cleavage of gag and gag-pol precursor polyproteins into functional products needed for viral assembly. HIV protease is an aspartic protease encoded by the amino terminus of the pol gene.
HIV Infection and AIDS inhibitors: block cleavage of protein precursors necessary for the production of
infectious
Infectious
Febrile Infant viral particles
Drug | Adverse effects | Interactions/ contraindications Contraindications A condition or factor associated with a recipient that makes the use of a drug, procedure, or physical agent improper or inadvisable. Contraindications may be absolute (life threatening) or relative (higher risk of complications in which benefits may outweigh risks). Noninvasive Ventilation |
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Zidovudine (AZT):
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Emtricitabine: structurally similar to lamivudine |
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Do not combine with lamivudine (the drugs compete with intracellular phosphorylation Phosphorylation The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety. Post-translational Protein Processing). |
Lamivudine: active against the hepatitis B Hepatitis B Hepatitis B virus (HBV) is a partially double-stranded DNA virus, which belongs to the Orthohepadnavirus genus and the Hepadnaviridae family. Most individuals with acute HBV infection are asymptomatic or have mild, self-limiting symptoms. Chronic infection can be asymptomatic or create hepatic inflammation, leading to liver cirrhosis and hepatocellular carcinoma (HCC). Hepatitis B Virus virus Virus Viruses are infectious, obligate intracellular parasites composed of a nucleic acid core surrounded by a protein capsid. Viruses can be either naked (non-enveloped) or enveloped. The classification of viruses is complex and based on many factors, including type and structure of the nucleoid and capsid, the presence of an envelope, the replication cycle, and the host range. Virology |
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Do not combine with emtricitabine (the drugs compete with intracellular phosphorylation Phosphorylation The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety. Post-translational Protein Processing). |
Abacavir | Hypersensitivity reaction (potentially fatal): fever Fever Fever is defined as a measured body temperature of at least 38°C (100.4°F). Fever is caused by circulating endogenous and/or exogenous pyrogens that increase levels of prostaglandin E2 in the hypothalamus. Fever is commonly associated with chills, rigors, sweating, and flushing of the skin. Fever, rash Rash Rocky Mountain Spotted Fever, abdominal pain Pain An unpleasant sensation induced by noxious stimuli which are detected by nerve endings of nociceptive neurons. Pain: Types and Pathways, vomiting Vomiting The forcible expulsion of the contents of the stomach through the mouth. Hypokalemia, dyspnea Dyspnea Dyspnea is the subjective sensation of breathing discomfort. Dyspnea is a normal manifestation of heavy physical or psychological exertion, but also may be caused by underlying conditions (both pulmonary and extrapulmonary). Dyspnea |
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Tenofovir (NtRTI): TAF and TDF (TAF: active against the hepatitis B Hepatitis B Hepatitis B virus (HBV) is a partially double-stranded DNA virus, which belongs to the Orthohepadnavirus genus and the Hepadnaviridae family. Most individuals with acute HBV infection are asymptomatic or have mild, self-limiting symptoms. Chronic infection can be asymptomatic or create hepatic inflammation, leading to liver cirrhosis and hepatocellular carcinoma (HCC). Hepatitis B Virus virus Virus Viruses are infectious, obligate intracellular parasites composed of a nucleic acid core surrounded by a protein capsid. Viruses can be either naked (non-enveloped) or enveloped. The classification of viruses is complex and based on many factors, including type and structure of the nucleoid and capsid, the presence of an envelope, the replication cycle, and the host range. Virology) |
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Non-competitive inhibitors of reverse transcriptase Reverse transcriptase A reverse transcriptase encoded by the pol gene of HIV. It is a heterodimer of 66 kda and 51 kda subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse h activity that plays an essential role the viral replication process. HIV Infection and AIDS:
Diagram of the mechanism of action of NRTIs and NNRTIs:
A: Note how NRTIs block the growing viral
DNA
DNA
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
DNA Types and Structure
genome
Genome
The complete genetic complement contained in the DNA of a set of chromosomes in a human. The length of the human genome is about 3 billion base pairs.
Basic Terms of Genetics by substituting the naturally occurring
nucleosides
Nucleosides
Purine or pyrimidine bases attached to a ribose or deoxyribose.
Nucleic Acids and functioning as chain terminators.
B: On the other
hand
Hand
The hand constitutes the distal part of the upper limb and provides the fine, precise movements needed in activities of daily living. It consists of 5 metacarpal bones and 14 phalanges, as well as numerous muscles innervated by the median and ulnar nerves.
Hand: Anatomy, NNRTIs
bind
BIND
Hyperbilirubinemia of the Newborn directly to the
reverse transcriptase
Reverse transcriptase
A reverse transcriptase encoded by the pol gene of HIV. It is a heterodimer of 66 kda and 51 kda subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse h activity that plays an essential role the viral replication process.
HIV Infection and AIDS enzyme, directly preventing viral
DNA
DNA
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
DNA Types and Structure
synthesis
Synthesis
Polymerase Chain Reaction (PCR).
NRTI: nucleoside
reverse transcriptase
Reverse transcriptase
A reverse transcriptase encoded by the pol gene of HIV. It is a heterodimer of 66 kda and 51 kda subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse h activity that plays an essential role the viral replication process.
HIV Infection and AIDS inhibitor
NNRTI: non-nucleoside
reverse transcriptase
Reverse transcriptase
A reverse transcriptase encoded by the pol gene of HIV. It is a heterodimer of 66 kda and 51 kda subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse h activity that plays an essential role the viral replication process.
HIV Infection and AIDS inhibitor
RNAseH:
ribonuclease
Ribonuclease
Enzymes that catalyze the hydrolysis of ester bonds within RNA.
Interferons H
Drug | Adverse effects | Interactions/ contraindications Contraindications A condition or factor associated with a recipient that makes the use of a drug, procedure, or physical agent improper or inadvisable. Contraindications may be absolute (life threatening) or relative (higher risk of complications in which benefits may outweigh risks). Noninvasive Ventilation |
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Etravirine: most commonly used NNRTI in resistant HIV cases |
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Can interact with other antiretroviral drugs (e.g., if in combination, dose of maraviroc should be doubled) |
Efavirenz |
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Avoid in long QT syndrome Long QT syndrome Long QT syndrome (LQTS) is a disorder of ventricular myocardial repolarization that produces QT prolongation on electrocardiogram (ECG). Long QT syndrome is associated with an increased risk of developing life-threatening cardiac arrhythmias, specifically torsades de pointes. Long QT Syndrome, liver Liver The liver is the largest gland in the human body. The liver is found in the superior right quadrant of the abdomen and weighs approximately 1.5 kilograms. Its main functions are detoxification, metabolism, nutrient storage (e.g., iron and vitamins), synthesis of coagulation factors, formation of bile, filtration, and storage of blood. Liver: Anatomy disease, psychiatric illness |
Doravirine | CNS/psychiatric effects similar to efavirenz (but much less common) | Use with rifampin Rifampin A semisynthetic antibiotic produced from streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits dna-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. Epiglottitis contraindicated (↓ doravirine exposure Exposure ABCDE Assessment) |
Rilpivirine |
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Nevirapine: not initial treatment of treatment-naive patients Patients Individuals participating in the health care system for the purpose of receiving therapeutic, diagnostic, or preventive procedures. Clinician–Patient Relationship (↑ toxicity Toxicity Dosage Calculation) |
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Drug | Adverse effects | Interactions/ contraindications Contraindications A condition or factor associated with a recipient that makes the use of a drug, procedure, or physical agent improper or inadvisable. Contraindications may be absolute (life threatening) or relative (higher risk of complications in which benefits may outweigh risks). Noninvasive Ventilation |
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Atazanavir |
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Darunavir |
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Ritonavir: booster |
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One of the most potent known inhibitors of CYP3A4 CYP3A4 Class 3 Antiarrhythmic Drugs (Potassium Channel Blockers); avoid taking drugs with narrow therapeutic index Therapeutic Index An indicator of the benefits and risks of treatment. Dosage Calculation. |
Lopinavir: coformulated with ritonavir |
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Not for initial treatment (related to potency and toxicity Toxicity Dosage Calculation) |
Drug | Adverse effects | Interactions/ contraindications Contraindications A condition or factor associated with a recipient that makes the use of a drug, procedure, or physical agent improper or inadvisable. Contraindications may be absolute (life threatening) or relative (higher risk of complications in which benefits may outweigh risks). Noninvasive Ventilation |
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Raltegravir |
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Enzyme inducers (e.g., rifampin Rifampin A semisynthetic antibiotic produced from streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits dna-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. Epiglottitis) increase its metabolism by inducing UDP-glucuronosyltransferase. |
Dolutegravir | Mild reversible creatinine elevation (inhibits the renal transporter, OCT2) |
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Elvitegravir: administered with cobicistat or ritonavir | GI symptoms | Currently available only in a fixed-dose combination with tenofovir, emtricitabine, and cobicistat (which ↑ drug-drug interactions) |
Bictegravir: coformulated with emtricitabine and TAF |
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Intake with rifampin Rifampin A semisynthetic antibiotic produced from streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits dna-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. Epiglottitis or dofetilide Dofetilide Class 3 Antiarrhythmic Drugs (Potassium Channel Blockers) contraindicated |
Schematic diagram of viral entry and steps inhibited by enfuvirtide and maraviroc:
The trimeric
gp120
Gp120
External envelope protein of the human immunodeficiency virus which is encoded by the HIV env gene. It has a molecular weight of 120 kda and contains numerous glycosylation sites. Gp120 binds to cells expressing CD4 cell-surface antigens, most notably t4-lymphocytes and monocytes/macrophages. Gp120 has been shown to interfere with the normal function of CD4 and is at least partly responsible for the cytopathic effect of HIV.
HIV Infection and AIDS subunit of the viral
envelope
Envelope
Bilayer lipid membrane acquired by viral particles during viral morphogenesis. Although the lipids of the viral envelope are host derived, various virus-encoded integral membrane proteins, i.e. Viral envelope proteins are incorporated there.
Virology glycoprotein complex binds CD4 on the target cell surface, triggering a conformational change that promotes interactions with chemokine
receptors
Receptors
Receptors are proteins located either on the surface of or within a cell that can bind to signaling molecules known as ligands (e.g., hormones) and cause some type of response within the cell.
Receptors (in this case
CCR5
CCR5
Ccr receptors with specificity for chemokine ccl3; chemokine ccl4; and chemokine ccl5. They are expressed at high levels in T-lymphocytes; B-lymphocytes; macrophages; mast cells; and nk cells. The ccr5 receptor is used by the human immunodeficiency virus to infect cells.
HIV Infection and AIDS). The trimeric transmembrane subunit
gp41
Gp41
Transmembrane envelope protein of the human immunodeficiency virus which is encoded by the HIV env gene. It has a molecular weight of 41, 000 and is glycosylated. The n-terminal part of gp41 is thought to be involved in cell fusion with the CD4 antigens of T4 lymphocytes, leading to syncytial formation. Gp41 is one of the most common HIV antigens detected by immunoblotting.
HIV Infection and AIDS is activated to mediate membrane fusion so that the viral contents can enter the cell. Maraviroc blocks the
CCR5
CCR5
Ccr receptors with specificity for chemokine ccl3; chemokine ccl4; and chemokine ccl5. They are expressed at high levels in T-lymphocytes; B-lymphocytes; macrophages; mast cells; and nk cells. The ccr5 receptor is used by the human immunodeficiency virus to infect cells.
HIV Infection and AIDS coreceptor. Enfuvirtide binds
gp41
Gp41
Transmembrane envelope protein of the human immunodeficiency virus which is encoded by the HIV env gene. It has a molecular weight of 41, 000 and is glycosylated. The n-terminal part of gp41 is thought to be involved in cell fusion with the CD4 antigens of T4 lymphocytes, leading to syncytial formation. Gp41 is one of the most common HIV antigens detected by immunoblotting.
HIV Infection and AIDS, preventing fusion.