. as a PDF file. Combination HIV medicines contain two or more HIV medicines from one or more drug classes. Antiretroviral Drugs Used in the. Currently, 25 single or combination preparations from four classes of drugs are licensed. PDF, 3.7 MB Table 2.1: Antiretroviral agents Trade name Abbrev. • Enlist classes of drugs used for anti retroviral therapy. • Five classes of antiretroviral drugs.
HIV drug classes. Nucleoside Reverse Transcriptase Inhibitors (NRTIs), so called "nukes", interfere with the function of reverse transcriptase, which HIV uses to replicate. Non- Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) block reverse transcriptase by binding to the reverse transcriptase enzyme. With the enzyme blocked, HIV cannot reproduce. Protease Inhibitors (PIs) target the HIV protease enzyme called HIV- 1 protease, which the virus uses to complete viral replication. By binding to this enzyme, PI's inhibit its activity and therefore prevent viral replication.
Fusion Inhibitors (FIs), also known as entry inhibitors, are a class of antiretroviral drugs that interfere with the binding, fusion and entry of an HIV virion to a human cell. Integrase Inhibitors (II) are a new drug class that block the action of integrase, an enzyme that integrates genetic material from the virus into its target cell. CCR5 Antagonists are a new drug class that target the CD4+ co- receptor called CCR5. HIV also binds to this drug class, therefore blocking the HIV from binding to these receptors on the cell. By blocking this receptor, entry of HIV into the cell is inhibited.
Classes Of Antiretroviral Drugs Pdf To Word
HIV Medicine 2. 00. Drug classes and overview of antiretroviral agents.
Currently, 2. 5 single or combination preparations from four classes of drugs are licensed: nucleoside. NRTIs), non- nucleoside reverse transcriptase inhibitors (NNRTIs), protease. PIs) and fusion inhibitors. Further drugs and new classes of drugs can be expected in. The following chapter provides an overview of the individual agents and their specific features. Common combinations are described in the chapter on "Which HAART to Start With".
More? HIV Medicine 2. Chapter 5. 2: Download. HIV Medicine. 15th edition.
There are several classes of antiretroviral agents that act on different. no antiretroviral drugs were available and treatment consisted of treating.
Read about Antiretroviral Agents and Antiretroviral drugs. Read about Antiretroviral Agents and Antiretroviral drugs. There are six antiretroviral classes.
Classes Of Antiretroviral Drugs Pdf Download
Table 2. 1: Antiretroviral agents. Trade name Abbrev. Drug Manufacturer. Nucleoside and Nucleotide Reverse Transcriptase Inhibitors (NRTIs). Combivir CBV AZT+3. TC GSK. Emtriva FTC Emtricitabine Gilead.
Epivir 3. TC Lamivudine GSK. HIVID* dd. C Zalcitabine Roche. Kivexa/Epzicom KVX 3. TC+ABC GSK. Retrovir AZT Zidovudine GSK. Trizivir TZV AZT+3. TC+ABC GSK. Truvada TVD FTC+TDF Gilead. Videx dd. I Didanosine BMS.
Viread TDF Tenofovir Gilead. Zerit d. 4T Stavudine BMS. Ziagen ABC Abacavir GSK. Non- Nucleoside Reverse Transcriptase Inhibitors (NNRTIs). Rescriptor DLV Delavirdine Pfizer. Sustiva/Stocrin EFV Efavirenz BMS/MSD. Viramune NVP Nevirapine Boehringer Ingelheim.
Protease Inhibitors (PIs). Aptivus TPV Tipranavir Boehringer- Ingelheim. Agenerase APV Amprenavir GSK.
Crixivan IDV Indinavir MSD. Invirase 5. 00 SQV Saquinavir Roche. Kaletra LPV Lopinavir/ritonavir Abbott. Norvir RTV Ritonavir Abbott.
Reyataz ATV Atazanavir BMS. Telzir/Lexiva FPV Fosamprenavir GSK. Viracept NFV Nelfinavir Roche/Pfizer. Fusion inhibitors. Fuzeon T- 2. 0 Enfuvirtide Roche.
Entry inhibitors. Celsentri/Selzentry MVC Maraviroc Pfizer. Distribution ceased. Currently, 2. 5 single or combination preparations from four classes of drugs are licensed: nucleoside. NRTIs), non- nucleoside reverse transcriptase inhibitors (NNRTIs), protease. PIs) and fusion inhibitors.
Further drugs and new classes of drugs can be expected in. The following chapter provides an overview of the individual agents and their specific features and. Common combinations are described in the chapter on "Which HAART to Start With". Nucleoside analogs (NRTIs). Mechanism of action. Nucleoside analogs ("nukes") are also referred to as nucleoside reverse transcriptase inhibitors.
Their target is the HIV enzyme reverse transcriptase. Acting as alternative substrates or "false. The incorporation of nucleoside analogs induces the abortion of. DNA synthesis, as phosphodiester bridges can no longer be built to stabilize the double strand.
Nucleoside analogs are "prodrugs", which means that they are absorbed unchanged and only activated. It is the. triphosphate derivative that is efficacious. AZT and d. 4T are thymidine analogs, while FTC and 3. TC. are cytidine analogs. Combinations containing AZT + d. T or FTC + 3. TC are therefore pointless, since. Havlir 2. 00. 2).
I is an inosine analog, which is converted to. There is a high degree of cross- resistance between. Resistance"). Nucleoside analogs were the first drugs to be used in HIV treatment, and therefore, most of the. They are easy to take, and once- daily dosing is sufficient for most. Overall initial tolerability is fairly good. However, frequent complaints during the first weeks are.
The gastrointestinal complaints are easily treated symptomatically. Side Effects"). However, nucleoside analogs can cause a wide variety of long- term side effects, including. Although lipodystrophy was. PIs, many metabolic disorders, and especially.
Galli 2. 00. 2). They are probably related. Brinkmann 1. 99. 9).
Mitochondrial. function requires nucleosides. The metabolism of these important organelles is disrupted by the. There are probably. Mitochondrial toxicity"). Nucleoside analogs are eliminated mainly by renal excretion and do not interact with drugs that are. There is therefore little potential for interaction. However. ribavirin, for example, can also reduce intracellular phosphorylation of AZT or d.
T (Piscitelli. 2. In contrast to the PIs and NNRTIs, the doses have to be adjusted for patients with renal. Individual agents. Abacavir (Ziagen) is a guanosine analog, which can lower viral load by approximately 1. Harrigan 2. 00. 0).
Abacavir is phosphorylated intracellularly to carbovir triphosphate. Harris 2. 00. 2). In October 2. 00. Moyle 2. 00. 5, Sosa 2. It is also a component of Trizivir and. In combination with AZT+3. TC (Trizivir, see also Triple Nuke), abacavir was less effective than.
Gulick 2. 00. 4). The randomized, double blind CNA3. Study also showed lower efficacy in. Staszewski 2. 00.
In contrast. efficacy was comparable to that of nelfinavir (Matheron 2. When combined with 3. TC, the efficacy.
TC plus either AZT (De. Jesus 2. 00. 4) or d. T (Podzamczer 2. 00. A regimen that is failing virologically can be successfully intensified with abacavir if it is added. Katlama 2. 00. 0, Rozenbaum 2. Abacavir is also. HAART. Numerous randomized studies have demonstrated that patients on a successful.
PI- or NNRTI- regimen can switch relatively safely to abacavir plus two NRTIs (Clumeck 2. Katlama. 2. 00. 3, Martinez 2.
Bonjoch 2. 00. 5). However, there is a certain degree of risk associated with this.
Opravil 2. 00. 2. Martinez 2. 00. 3). Caution therefore must be taken when combining tenofovir with 3.
TC as resistance. Triple Nuke"). With respect to mitochondrial toxicity, abacavir is more favorable than several other substances. In. comparison to d. T, the lipoatrophy risk is low (Podczamcer 2. Lipoatrophy improves on changing.
T to abacavir (Carr 2. John 2. 00. 3, Moyle 2. Mc. Comsey 2. 00. This also applies to an. DNA (Hoy 2. 00. 4, Martin 2. Mc. Comsey 2. 00. One drawback to the use of abacavir is the risk of a hypersensitivity reaction (HSR), an allergic.
Side Effects). This occurs in. In acutely infected. Stekler 2. 00. 6). On re- exposure, HSR can even be fatal. Severe HSR can occur after only a single abacavir tablet (De.
Rosa 2. 00. 4) or even after treatment interruption despite prior tolerability (El- Sahly 2. The. combination of strongly worded warnings contained in the package insert and the unspecific symptoms. HSR poses a constant challenge to the physician. A genetic predisposition exists, so that. HLA type B5. 70. 1 are at a higher risk than others - with HSR occurring in up to 8.
Mallal 2. 00. 2, Hetherington 2. However, HSR is also possible in the absence of this HLA. Data from the PREDICT study, in which the predictive value of the HLA type was prospectively. In the future, it may be. HLA type before administration of abacavir, a strategy already practiced in some. AZT (Zidovudine, Retrovir) was the first antiretroviral agent to be put on the market, in 1. An. initial study on AZT monotherapy showed a survival benefit - at least in significantly.
Fischl 1. 98. 7). In contrast, two other early, very large studies, ACTG 0. Fischl 1. 99. 0, Volberding 1. Even at that time. AZT monotherapy was likely to be limited. The. Concorde Study has even brought AZT from time to time into disrepute: it showed that there was no.
AZT treatment. In addition, the higher doses that were given in these first few. Fischl 1. 99. 0a), something which should also not be. Long- term treatment almost. MCV (mean corpuscular volume of erythrocytes), which is useful as a means of. Gastrointestinal complaints, especially initially, may present a further. In contrast, AZT- related myopathy or even cardiomyopathy is quite rare.
A "logical". disadvantage of AZT is that it has to be taken twice daily, disqualifying it as a substance for. Furthermore, AZT finally came under pressure when, in the 9. Severe anemia was. AZT- arm in comparison to tenofovir, causing 5. Gallant 2. 00. 6).
Lack of neurotoxicity and good CNS penetration are some of the advantages of this drug. Therefore. AZT still remains a component of many regimens and transmission prophylaxes.
AZT is also a component. Combivir and Trizivir, at a slightly higher dose (3. It is noteworthy that the US- patent protection of AZT. AZT could soon become much cheaper.
C - Zalcitabine (HIVID) was, in 1. NRTI to reach the market. The weak efficacy as. C being taken from the. HIV medicine. dd. I - (Didanosine, Videx) in 1.
The. introduction of acid- resistant tablets, which, in 2. Early studies showed a survival advantage for.
AZT+dd. I compared to AZT monotherapy. This effect of dd. I was less. marked in AZT- pretreated patients. Therefore, the addition of dd. I in the Delta 2 study led to.
CPCRA0. 07 (Saravolatz 1. In ACTG. 1. 75, monotherapy with dd. I was more potent than AZT, even with regard to disease progression (Hammer. However, this predominance was not confirmed in other studies (Dolin 1. Floridia 1. 99. 7).
Following failure of AZT, dd. I is much more effective than d. T (Havlir 2. 00. 0). In more recent studies, dd. I is only used seldomly. Gastrointestinal complaints and polyneuropathy.
Pancreatitis is more specific, occurring in up to 1. This toxicity is probably dose- dependent (Jablonowski 1. This is possibly. Moyle 2. 00. 4). Special caution should be given to.
Havlir 2. 00. 1, Martinez 2. Concomitant. administration of these drugs should be avoided. Even the combination with d. T, is no longer. recommended, especially in primary therapy (see especially the chapter on "Problematic primary. Patients with a history of pancreatitis should not be treated with dd. I. If the body. weight is less than 6. I has to be. administered on an empty stomach.
In view of its toxicity dd. I has become less popular but is useful. Molina 2. 00. 5). T (Stavudine, Zerit) was the second thymidine analog to be introduced after AZT. Subjectively. d. 4T is often initially tolerated better than AZT (less gastrointestinal side effects and limited. Spruance 1. 99. 7, Squires 2.
HIV drugs. However, several studies have since placed it under a lot. In the Gilead 9. 03 Study, d. T was tested in a double blind design against tenofovir in.