Antiretroviral Drug Classes
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Questions and Answers

Which mechanism do non-nucleoside reverse transcriptase inhibitors (NNRTIs) primarily employ to inhibit HIV replication?

  • They block the HIV protease enzyme from cleaving proteins.
  • They directly bind to and inhibit HIV integrase.
  • They bind to the reverse transcriptase enzyme causing conformational changes. (correct)
  • They prevent the fusion of HIV with host cells.

Which class of antiretroviral drugs does not require intracellular phosphorylation for its activity?

  • Entry/Fusion Inhibitors
  • Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) (correct)
  • Integrase Strand Transfer Inhibitors (INSTIs)
  • Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

Which of the following is NOT a common side effect associated with NNRTIs?

  • Nausea (correct)
  • Rash
  • Hepatotoxicity
  • Dizziness

What is the main function of protease inhibitors (PIs) in antiretroviral therapy?

<p>Block the cleavage of polyprotein precursors into functional proteins. (C)</p> Signup and view all the answers

Which of the following best describes the role of Entry/Fusion Inhibitors?

<p>They prevent HIV from entering cells by blocking attachment or fusion. (B)</p> Signup and view all the answers

What type of HIV do NNRTIs primarily treat?

<p>HIV-1 (D)</p> Signup and view all the answers

Which drug class includes tenofovir and lamivudine?

<p>Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs) (D)</p> Signup and view all the answers

What primary role does the integrase enzyme play in HIV replication?

<p>Integrates viral genetic material into host cell DNA. (B)</p> Signup and view all the answers

What is the main purpose of administering antiviral medications for genital herpes?

<p>To reduce viral shedding and outbreaks (C)</p> Signup and view all the answers

Which of the following is NOT considered a common infectious agent of nongonococcal urethritis (NGU)?

<p>Neisseria gonorrhoeae (D)</p> Signup and view all the answers

When is it essential for patients to abstain from sexual activity after initiating treatment for nongonococcal urethritis?

<p>For 7 days following treatment (B)</p> Signup and view all the answers

What is the recommended first-line antibiotic regimen for treating uncomplicated nongonococcal urethritis in adults?

<p>Doxycycline 100 mg twice daily for 7 days (C)</p> Signup and view all the answers

For pelvic inflammatory disease (PID), which of the following is part of the standard outpatient treatment regimen?

<p>Single dose of Ceftriaxone plus doxycycline for 14 days (A)</p> Signup and view all the answers

What is the role of prompt treatment in cases of pelvic inflammatory disease (PID)?

<p>To prevent complications like infertility (A)</p> Signup and view all the answers

What additional treatment should be considered for sexually acquired proctitis if perianal ulcers are present?

<p>Antiviral treatment for herpes simplex virus (A)</p> Signup and view all the answers

Which of the following antibiotics is recommended for treating acute sexually transmitted epididymitis in men under 35?

<p>Ceftriaxone plus Doxycycline (A)</p> Signup and view all the answers

Sexual partners of patients treated for nongonococcal urethritis should be evaluated and treated primarily to:

<p>Prevent reinfection (C)</p> Signup and view all the answers

What is the standard course of treatment for uncomplicated cases of nongonococcal urethritis in pregnant women who cannot take doxycycline?

<p>Azithromycin 1 g orally once (A)</p> Signup and view all the answers

Which statement about the follow-up care for sexually transmitted infections is accurate?

<p>Testing 3 months after treatment is advised for trichomoniasis and syphilis. (A)</p> Signup and view all the answers

What is the primary bacterial cause of syphilis?

<p>Treponema pallidum (B)</p> Signup and view all the answers

Which treatment is preferred for early syphilis?

<p>A single dose of penicillin G benzathine (B)</p> Signup and view all the answers

Which of the following is true about bacterial vaginosis?

<p>Overgrowth of anaerobic bacteria is a common cause. (B)</p> Signup and view all the answers

What is the alternative treatment for a patient with penicillin allergy who has early syphilis?

<p>Doxycycline for 14 days (B)</p> Signup and view all the answers

Which of the following is a characteristic symptom of genital herpes?

<p>Painful blisters or ulcers (A)</p> Signup and view all the answers

Regarding trichomoniasis, what is the recommended dosage for men?

<p>2 g of metronidazole in a single oral dose (A)</p> Signup and view all the answers

What is a common sign of secondary syphilis?

<p>Skin rashes and lymphadenopathy (A)</p> Signup and view all the answers

Which of the following is true regarding metronidazole and alcohol?

<p>Alcohol should be avoided during treatment and for 3 days after. (C)</p> Signup and view all the answers

What is recommended for the treatment of neurosyphilis?

<p>Aqueous crystalline penicillin G intravenously (D)</p> Signup and view all the answers

Which medication is known for reducing both symptoms and outbreak frequency in genital herpes?

<p>Acyclovir (D)</p> Signup and view all the answers

What is a key preventative measure during outbreaks of genital herpes?

<p>Consistent condom use (D)</p> Signup and view all the answers

What is not a characteristic symptom of bacterial vaginosis?

<p>Painless sore (A)</p> Signup and view all the answers

What is the primary mechanism by which protease inhibitors (PIs) prevent HIV replication?

<p>They bind to the active site of HIV protease and prevent cleavage. (B)</p> Signup and view all the answers

Which of the following statements about enfuvirtide is incorrect?

<p>Enfuvirtide needs to be administered orally. (A)</p> Signup and view all the answers

Before initiating maraviroc therapy, what test is essential?

<p>A tropism test to confirm CCR5 co-receptor use. (C)</p> Signup and view all the answers

Which of the following is NOT a common side effect of protease inhibitors?

<p>Rash (B)</p> Signup and view all the answers

What is the preferred treatment duration for nonoccupational postexposure prophylaxis (nPEP) after potential HIV exposure?

<p>28 days (B)</p> Signup and view all the answers

What alternative treatment might be preferred for severely immunocompromised patients with Pneumocystis pneumonia?

<p>Intravenous pentamidine (A)</p> Signup and view all the answers

Which of the following drugs is NOT commonly used for treating cytomegalovirus retinitis?

<p>Acyclovir (C)</p> Signup and view all the answers

What is the primary reason for using combination therapy with amphotericin B and flucytosine in cryptococcal meningitis treatment?

<p>To decrease treatment failure and relapse rates. (C)</p> Signup and view all the answers

What key strategy complements PrEP in preventing HIV transmission?

<p>Risk reduction counseling and condom use. (A)</p> Signup and view all the answers

Which of the following is a crucial aspect of drug therapy for Mycobacterium infections such as tuberculosis?

<p>Multi-drug regimen for extended duration. (B)</p> Signup and view all the answers

Which of the following is NOT a first-line drug in the treatment regimen for drug-susceptible tuberculosis?

<p>Amikacin (A)</p> Signup and view all the answers

Which statement regarding treatment for varicella zoster virus infection is true?

<p>Oral acyclovir is recommended for children if started within 24 hours. (D)</p> Signup and view all the answers

Which side effect is notably associated with enfuvirtide administration?

<p>Injection site reactions (C)</p> Signup and view all the answers

How is the treatment for herpes simplex virus infections best characterized?

<p>Medications can reduce symptoms but cannot cure the infection. (D)</p> Signup and view all the answers

How is maraviroc primarily metabolized in the body?

<p>By the CYP450 enzyme system, specifically CYP3A4. (A)</p> Signup and view all the answers

What is the standard dosing frequency for enfuvirtide?

<p>Twice daily (B)</p> Signup and view all the answers

What is a key consideration when treating candidiasis in immunocompromised patients?

<p>Chronic suppressive therapy may be necessary for recurrent infections. (B)</p> Signup and view all the answers

Which of the following best describes chlamydial infections?

<p>They can lead to serious complications if left untreated. (A)</p> Signup and view all the answers

Which treatment is typically employed for ganciclovir-resistant CMV retinitis?

<p>Cidofovir (C)</p> Signup and view all the answers

Which HIV treatment strategy focuses on reducing risk before potential exposure?

<p>PrEP (preexposure prophylaxis) (B)</p> Signup and view all the answers

What is the standard treatment for uncomplicated gonococcal infections?

<p>A single intramuscular dose of ceftriaxone. (B)</p> Signup and view all the answers

Why is it crucial to monitor patients receiving amphotericin B for adverse effects?

<p>It can cause serious renal damage. (D)</p> Signup and view all the answers

What is the recommended course of treatment for an initial episode of herpes simplex virus infection?

<p>Oral or IV antivirals for 7-10 days. (A)</p> Signup and view all the answers

What factor is important for treating varicella zoster virus infections in older adults?

<p>Higher doses of oral acyclovir or valacyclovir are recommended. (B)</p> Signup and view all the answers

What condition can cause newborns to develop conjunctivitis during birth due to maternal infection?

<p>Chlamydia trachomatis. (D)</p> Signup and view all the answers

Which of the following statements regarding dual therapy for gonococcal infections is accurate?

<p>Dual therapy is no longer preferred due to microbiome concerns. (D)</p> Signup and view all the answers

What is the appropriate course of action for treating vulvovaginal candidiasis?

<p>Oral fluconazole or topical azoles can be effective. (C)</p> Signup and view all the answers

What is an important consideration for patients with both TB and HIV?

<p>Drug interactions and immune responses must be monitored. (C)</p> Signup and view all the answers

Flashcards

NRTIs

Nucleoside/Nucleotide Reverse Transcriptase Inhibitors that block HIV reverse transcriptase needed for viral replication.

NNRTIs

Non-Nucleoside Reverse Transcriptase Inhibitors that bind directly to and inhibit HIV reverse transcriptase by a different mechanism.

Protease Inhibitors (PIs)

Drugs that block the HIV protease enzyme, preventing the virus from making infectious particles.

Integrase Strand Transfer Inhibitors (INSTIs)

Inhibit the HIV integrase enzyme, preventing viral genetic material integration into host cells.

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Entry/Fusion Inhibitors

Prevent HIV from entering host cells by blocking viral attachment or fusion.

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HIV Reverse Transcriptase

An enzyme needed for HIV to make a DNA copy of its RNA.

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HAART

Highly Active Antiretroviral Therapy, a combination drug regimen for HIV.

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HIV Protease

Enzyme that HIV uses to process its proteins into functional pieces, needed to produce infectious virus.

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Drug-resistant TB treatment

MDR and XDR TB need second-line agents like fluoroquinolones, injectable drugs, and reserve drugs for at least 18-24 months.

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Cryptococcal meningitis treatment

Amphotericin B plus flucytosine are the first-line drugs. Maintenance with fluconazole is also needed.

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Varicella-zoster treatment

Acyclovir is the first-line drug for chickenpox and shingles; oral acyclovir or valacyclovir are commonly used. Intravenous acyclovir for severe cases; early treatment is key.

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Herpes simplex treatment

Acyclovir, valacyclovir, and famciclovir reduce symptoms and viral shedding. Episodic or suppressive therapy may be needed.

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Candidiasis treatment

Topical agents (nystatin, clotrimazole) for mucosal; oral azoles (fluconazole) for systemic infections. Suppressive therapy may be needed.

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Chlamydial infection treatment

Antibiotics (azithromycin or doxycycline) are used to treat the bacterial infection. Prompt treatment is crucial.

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Gonococcal infection treatment

Ceftriaxone is the recommended treatment for uncomplicated gonorrhea. Dual therapy is no longer used due to resistance.

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Standard TB regimen

Isoniazid, rifampin, ethambutol, and pyrazinamide for 2 months (intensive), followed by isoniazid and rifampin for 4 more months.

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TB/HIV co-infection

Requires special considerations for drug interactions and immune reconstitution inflammatory syndrome.

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Directly observed therapy

A crucial method to monitor adherence and prevent resistance in TB treatment.

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Drug interactions

Potential adverse effects from using different drugs together, need careful monitoring.

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Ceftriaxone

Recommended monotherapy for uncomplicated gonorrhea.

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Azithromycin

Antibiotic used for chlamydia and historically part of gonorrhea treatment, but not in current recommended treatment regime.

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Immune reconstitution inflammatory syndrome

Potential inflammatory reaction related to immune system strengthening after antiviral use.

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HIV Protease Inhibitors (PIs)

Drugs that stop HIV from replicating by blocking an enzyme crucial for its life cycle.

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Highly active antiretroviral therapy (HAART)

A combination of antiretroviral drugs used to treat HIV.

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CYP450 enzyme system

Enzyme system that metabolizes many drugs, including PIs.

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Ritonavir boosting

Using a low dose of ritonavir to increase levels of other PIs.

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Enfuvirtide

HIV fusion inhibitor preventing viral entry into cells.

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Fusion inhibitor

Drug that stops the virus from fusing with the host cell.

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Maraviroc

CCR5 co-receptor inhibitor that blocks HIV entry.

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Pre-exposure prophylaxis (PrEP)

Taking antiretrovirals to reduce risk of contracting HIV before exposure.

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Postexposure prophylaxis (nPEP)

Taking antiretrovirals within 72 hours of HIV exposure to reduce infection risk.

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Pneumocystis pneumonia (PCP)

Opportunistic fungal infection; a serious risk for immunocompromised individuals.

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Trimethoprim/sulfamethoxazole (TMP/SMZ)

First-line treatment for PCP.

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Cytomegalovirus (CMV) retinitis

Serious opportunistic infection causing damage to the eye in immunocompromised individuals.

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Ganciclovir/Valganciclovir

First line therapy for CMV retinitis, either IV or oral.

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Mycobacterium Infections

Infections caused by bacteria with multi-drug regimens.

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Genital Herpes Treatment

There's no cure for genital herpes, but antiviral medications like acyclovir, famciclovir, and valacyclovir can help manage the infection. These drugs reduce viral shedding, shorten outbreaks, and decrease recurrence frequency. They can be taken episodically during outbreaks or daily as suppressive therapy, which significantly reduces transmission risk. Severe or complicated cases may require intravenous acyclovir.

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Nongonococcal Urethritis (NGU)

NGU is an inflammatory condition of the urethra caused by organisms other than Neisseria gonorrhoeae. Common culprits include Chlamydia trachomatis, Ureaplasma urealyticum, Trichomonas vaginalis, and Mycoplasma genitalium. Diagnosis involves urethral discharge and polymorphonuclear leukocytes on microscopy, with a negative gonorrhea test.

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NGU Treatment

Doxycycline is the first-line antibiotic for uncomplicated NGU. The standard regimen is 100mg twice daily for 7 days. For patients who can't take doxycycline, azithromycin is an alternative. Sexual partners should be evaluated and treated to prevent reinfection. Abstinence from sexual activity for 7 days after treatment initiation is advised.

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Pelvic Inflammatory Disease (PID)

PID is an infection of the reproductive organs, often caused by sexually transmitted infections like chlamydia and gonorrhea. Treatment usually involves a combination of antibiotics to cover a broad range of potential pathogens.

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PID Treatment

The CDC recommends a single dose of intramuscular ceftriaxone plus 14 days of oral doxycycline, with or without metronidazole for outpatient treatment. Severe cases may require inpatient intravenous antibiotics. Sexual partners should be treated. Prompt treatment is crucial to prevent complications like infertility, ectopic pregnancy, and chronic pelvic pain.

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Acute Sexually Transmitted Epididymitis

This is an inflammation of the epididymis, often caused by chlamydia and gonorrhea, particularly in men under 35. Treatment usually involves a combination of antibiotics to cover both infections.

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Epididymitis Treatment

The CDC recommends ceftriaxone 500mg intramuscularly once plus doxycycline 100mg orally twice daily for 10 days. For those engaging in insertive anal intercourse, levofloxacin 500mg orally once daily for 10 days is added. Analgesics, scrotal support, and abstinence from sexual activity until treatment completion are advised. Prompt treatment helps prevent complications like abscess formation or infertility.

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Proctitis Treatment

The preferred treatment for sexually acquired proctitis is a combination of antibiotics to cover potential causative organisms like Neisseria gonorrhoeae, Chlamydia trachomatis, Treponema pallidum, and herpes simplex virus. The recommended regimen is ceftriaxone plus doxycycline. Prolonged antibiotic courses are required for cases with bloody discharge and positive chlamydia tests. Treatment for herpes simplex virus should also be considered if perianal ulcers are present.

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Sexual Health Reminder

For all sexually transmitted infections, it is crucial to evaluate and treat all sexual partners to prevent reinfection. Prompt treatment is generally recommended to prevent complications and ensure better outcomes. Consistent condom use during sexual activity is important to reduce transmission risk.

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Syphilis

A sexually transmitted infection caused by the bacterium Treponema pallidum, progressing through stages if untreated: primary with painless chancre sore, secondary with skin rashes and flu-like symptoms, latent with no visible symptoms, and tertiary with potentially destructive long-term complications.

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Syphilis Treatment

Penicillin G is the recommended treatment, with dosage based on the stage of the disease. Alternatives like doxycycline may be used for early stages with penicillin allergy, but desensitization is preferred for neurosyphilis or pregnancy.

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Bacterial Vaginosis (BV)

A common vaginal infection characterized by an overgrowth of anaerobic bacteria like Gardnerella vaginalis, leading to a thin, grayish, malodorous discharge, elevated vaginal pH, and clue cells on microscopy.

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Trichomoniasis

A sexually transmitted infection caused by the protozoan Trichomonas vaginalis, primarily affecting the urogenital tract, causing vaginitis in women and urethritis in men, often asymptomatic.

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Trichomoniasis Treatment

Metronidazole is the recommended treatment for both men and women, with dose variations based on gender. Tinidazole is an alternative. Alcohol should be avoided due to a disulfiram-like reaction.

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Genital Herpes

A chronic, lifelong viral infection primarily caused by HSV-2, causing painful blisters or ulcers on the genitals, with possible fever and lymph node swelling during initial infection.

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Syphilis Stages

Syphilis progresses through distinct stages if untreated: Primary with a painless chancre sore, Secondary with skin rashes and flu-like symptoms, Latent without visible symptoms, and Tertiary with potentially destructive long-term complications.

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Penicillin Desensitization

A process to gradually introduce penicillin to a patient with severe allergy, allowing them to receive the necessary treatment for syphilis, especially in cases of neurosyphilis or pregnancy.

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Clue Cells

Vaginal epithelial cells covered in bacteria, indicative of bacterial vaginosis, observed under microscopy.

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Disulfiram-like Reaction

An adverse reaction to alcohol consumption during metronidazole or tinidazole treatment for trichomoniasis, potentially leading to nausea, vomiting, flushing, and headache.

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Asymptomatic BV

Bacterial vaginosis without noticeable symptoms, potentially still requiring treatment or follow-up to prevent complications.

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Test of Cure

Follow-up testing after treatment, crucial to confirm the effectiveness of therapy and identify persistent or recurrent infections, as in trichomoniasis.

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Viral Shedding

The release of herpes simplex virus (HSV) particles from infected cells, even in the absence of symptoms, contributing to transmission.

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Study Notes

Antiretroviral Drug Classes

  • Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs): Inhibit HIV reverse transcriptase, crucial for viral replication. Examples include tenofovir, abacavir, and lamivudine.
  • Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs): Bind to and inhibit HIV reverse transcriptase differently than NRTIs. Examples include efavirenz, rilpivirine, and doravirine. They act by causing conformational changes, inhibiting the enzyme's activity, and blocking viral replication. Generally, NNRTIs are only active against HIV-1, not HIV-2. Side effects include rash, hepatotoxicity, and CNS effects.
  • Protease Inhibitors (PIs): Block viral protease, preventing the production of mature, infectious viral particles. Examples include atazanavir, darunavir, and lopinavir. They are metabolized by the CYP450 enzyme system which leads to drug interactions. Ritonavir often used in low doses to boost other PIs. Side effects include GI intolerance, hyperlipidemia, insulin resistance, and body fat redistribution.
  • Integrase Strand Transfer Inhibitors (INSTIs): Inhibit HIV integrase, crucial for viral integration into host cells. Examples include dolutegravir, raltegravir, and bictegravir.
  • Entry/Fusion Inhibitors: Prevent HIV from entering cells. Examples include enfuvirtide and maraviroc. Enfuvirtide used subcutaneously twice daily, as a last resort, for multiple-drug-resistant HIV. Maraviroc uses CCR5 co-receptor to block CCR5-tropic HIV infection.

NNRTI Pharmacology

  • NNRTIs directly bind to HIV-1 reverse transcriptase, causing changes that halt its activity.
  • Unlike NRTIs, NNRTIs don't need cellular phosphorylation for activity.
  • Used in combination therapy (HAART) against HIV-1.

PI Pharmacology

  • PIs inhibit HIV protease, preventing viral polyprotein cleavage.
  • This leads to non-infectious viral particles.
  • PIs significantly improve HIV outcomes but require careful monitoring due to CYP450 interactions and metabolic side effects.

Enfuvirtide Pharmacology

  • Enfuvirtide is a fusion inhibitor, preventing HIV envelope fusion with host cells.
  • Administered subcutaneously twice daily, reserved for treatment-experienced patients with multidrug-resistant HIV.
  • Often combined with other antiretrovirals to delay resistance.
  • Potential side effects include injection site reactions, hypersensitivity reactions, and rare immune-mediated conditions.

Maraviroc Pharmacology

  • Maraviroc blocks CCR5 co-receptor on CD4 cells, preventing CCR5-tropic HIV entry.
  • Must be used in combination with other antiretrovirals.
  • A tropism test is required before starting maraviroc to confirm CCR5-tropism.
  • Metabolism by CYP3A4 can lead to drug interactions.

HIV Prevention (PrEP and nPEP)

  • PrEP: Daily antiretroviral use to reduce HIV acquisition risk. Regimens include Truvada and Descovy. Cabotegravir (long-acting) is an emerging option. Recommended for high-risk individuals.
  • nPEP: 28-day course of antiretrovirals after potential exposure. Must be initiated within 72 hours of exposure and usually involves a three-drug combination, including an integrase inhibitor. Recommended for single high-risk exposures.

Opportunistic Infections and Drug Therapy

  • Pneumocystis pneumonia (PCP): Trimethoprim/sulfamethoxazole (TMP/SMZ) is the primary treatment. Intravenous pentamidine can be used for severely immunocompromised individuals.
  • Cytomegalovirus (CMV) retinitis: Ganciclovir (or valganciclovir) or foscarnet or cidofovir are first-line treatments. Lifelong maintenance therapy may be needed.
  • Mycobacterium infections (e.g., tuberculosis): Multi-drug regimen required, including isoniazid, rifampin, ethambutol, and pyrazinamide for 2 months (initial), then isoniazid and rifampin for 4 months. MDR/XDR TB require second-line agents. Co-infection requires special consideration.
  • Cryptococcal meningitis: Amphotericin B plus flucytosine is the preferred treatment. Maintenance therapy with fluconazole is generally used after initial treatment.
  • Varicella-zoster virus: Acyclovir is the primary medication for chickenpox and shingles. Early intervention is best, with supportive care.
  • Herpes Simplex Virus (HSV): Acyclovir, valacyclovir, famciclovir are used for symptomatic relief. Suppressive therapy is possible. Topical available for oral herpes.
  • Candidiasis: Topical antifungals (nystatin, clotrimazole, miconazole) for mucosal candidiasis. Oral azoles (fluconazole) for systemic infections.

Bacterial STIs and Drug Therapy

  • Chlamydia: Azithromycin or doxycycline. Early treatment and partner treatment vital.
  • Gonorrhea: Ceftriaxone. Avoiding dual-therapy, for now. Partner treatment essential.
  • Syphilis: Intramuscular penicillin G. Alternatives (doxycycline) for penicillin-allergic patients. Partner treatment and follow-up testing necessary.
  • Bacterial vaginosis (BV): Oral or vaginal metroinidazole or clindamycin. Can use tinidazole.
  • Trichomoniasis: Metronidazole (or tinidazole) for both partners. Alcohol avoidance necessary. Follow-up testing essential.
  • Nongonococcal urethritis (NGU): Doxycycline is first-line therapy. Partner treatment required.
  • Pelvic Inflammatory Disease (PID): Intramuscular cephalosporin (e.g., ceftriaxone) plus oral doxycycline/metronidazole.
  • Acute sexually transmitted epididymitis: Ceftriaxone plus doxycycline (or levofloxacin for anal insertive activity).

Other Conditions and Treatment

  • Genital herpes: Antivirals (acyclovir, famciclovir, valacyclovir) can reduce symptoms and outbreaks, but no cure.
  • Proctitis: Combination of antibiotics to cover multiple organisms.

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This quiz covers key classes of antiretroviral drugs, including NRTIs, NNRTIs, and PIs. Learn about their mechanisms, examples, and side effects. Test your knowledge of how these drugs combat HIV infection and their role in modern treatment regimens.

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