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28 Cards in this Set
- Front
- Back
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Name the groups of drugs used for treatment of HIV?
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- Nucleotide reverse transcriptase inhibitors (NRTIs)
- Non-nucleotide reverse transcriptase inhibitors (NNRTIs) - Protease inhibitors (PIs) - Integrase strand transfer inhibitors (INSTIs) - Entry inhibitors - CCR5-antagonists |
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Name some NRTIs
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Zidovudine, Lamivudine, Abacavir
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Name some NNRTIs
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Nevirapine, efavirenz
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Name some protease inhibitors
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Darunavir, lopinavir, ritonavir
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Name some integrase strand transfer inhibitors (INSTIs)
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Raltegravir, dolutegravir
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Name entry-inhibitors
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Enfuvirtide
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Name CCR5-antagonists
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Maraviroc
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What is the standard regimen for HIV treatment?
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It is called highly active antiretroviral therapy (HAART). Should consist of at least 3 antiretrovirals, where 2 of them should be NRTIs.
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Why do we combine ritonavir with other protease inhibitors?
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Ritonavir boosts the efficacy of the others because it is a strong Pgp and CYP3A4 inhibitor. This decreases the elimination of the other PIs.
Eg. Ritonavir-boosted darunavir |
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Can we treat HIV with monotherapy?
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No. Increases risk of resistance
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Mechanism of action of NRTIs?
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Nucleotide analogues that get phosphorylated inside the cell, which will convert them into false subtrates for reverse transcriptase. This leads to competative antagonism and chain termination.
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Mechanism of NNRTIs?
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They are non-competative inhibitors of reverse transcriptase. Phosphorylation is not needed.
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Mechanism of action of protease inhibitors?
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They inhibit viral protease, which is important for maturing of the viruses. When its inhibited, only immature, non-infective viruses will be formed.
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Mechanism of action of entry inhibitors?
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They bind to the viral gp41 protein, making the HIV virus unable to enter the cell.
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Pharmacokinetics of NNRTIs?
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They have interactions with CYP enzymes. May induce them or inhibit them.
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Adverse effects of Zidovudine?
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- Bone marrow suppression- Mitochondrial toxicity leading to myopathy, neuropathy, lactic acidosis
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Adverse effect of Abacavir?
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It can cause a life-threatening hypersensitivity reaction in HLA-B*5701. Patients should be tested before they are given the drug.
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Adverse effects of NNRTIs?
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- Hepatotoxic, only for Nevirapine
- Mood disorders, psychosis - efavirenz - Hypersensitivity is very common, can lead to Stevens-Johnson syndrome |
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Adverse effects of protease inhibitors?
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- Hyperglycemia due to inhibition of GLUT4
- Hyperlipidema, central shift of adipose tissue |
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Name antivirals against influenza A?
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Amantadine, rimantadine
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Name antivirals against influenza A and B
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Oseltamivir (tamiflu), Zanamivir, baloxavir marboxil (new)
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Indications for amantadine and rimantadine?
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They are used for influenza prophylaxis for those who cant get vaccinated and are prone for complications if they get influenza.
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Indications of oseltamivir, zanamivir and baloxavir marboxil?
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They are used to treat influenza by shortening the duration of the illness.
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Mechanism of action of amantamine and rimantadine?
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They block M2, a viral-encoded ion channel which is necessary for viral replication.
They are also NMDA receptor antagonists, and can have a small role in Parkinsons treatment. |
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Mechanism of action of oseltamivir and zanamivir?
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They inhibit neuroaminidase (NA), an enzyme which needed for the virus to exit the cell.
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How do we administer Zanamivir?
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It must be inhaled due to poor oral absorption
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Adverse effects of amantadine and rimantadine?
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- Neurological symptoms due to NMDA-antagonism.
- QT-elongation, amantadine |
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Indication for use for immunoglobulins as antivirals?
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Post-exposure prophylaxis for rabies, hep A and B, measles.
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