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Exam 4 Pharmacology Pt3 (Protein Synthesis Inhibitors to the Flu
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Protein Synthesis Inhibitors Classes
5 classes
- Tetracyclines
- Aminoglucosides
- Mcrolides
- Clindamycin
- Linezolid
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Protein Synthesis Inhibitors Classes
5 classes
- Tetracyclines
- Aminoglucosides
- Mcrolides
- Clindamycin
- Linezolid
Protein Synthesis MOA
- inhibit protein synthesis and target the bacterial ribosome
- must enter the bacterial cell to be effective
Tetracyclines Drugs
-Doxycycline
-Minocycline
Tetracycline
Tetracyclines MOA
- Used to treat Gram + , -, and atypical.
- Treats Tick-borne diseases, acne,anthrax, gastric infection with H. Pylori
Tetracyclines Adverse Drug Reactions
- photosensitivity
- discoloration of teeth **
- Gi intolerance
- Contraindicted in pregnancy
Tetracyclines Pharmacokinetics
- high concentration are achieved in body organs, skin, bone, and teeth
- Chelation interactions
Tetracyclines Antibacterial Spectrum
- gram +, gram -, atypical
Tetracyclines Therapeutic Uses
- Uncomplicated respiratory tract infections
- tick borne diseases
- acne
-bioterrorism
Aminoglycosides Drugs
- Gentmicin
Aminoglycosides MOA
- Used to treat serious nosocomial, gram-negative infections and serious UTIs
-Hardly any gram-positive coverage
-No anaerobic coverage
Aminoglycosides Pharmacokinetics
- very water soluble
- not absorbed orally
- high concentrations can accumulate in the kidneys and inner ear
Aminoglycosides adverse effects
- nephrotoxicity and ototoxicity
Aminoglycosides Antibacterial Spectrum
-Most active against aerobic gram negative bacteria
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- no anaerobic
Aminoglycosides Drug level monitoring
- routine blood checks
Macrolides Drugs
-Azithromycin
-Clarithromycin
-Erythromycin
Macrolides Pharmacokinetics
- metabolized by cytochrme p450
Macrolides MOA
- Used to treat acne, community-acquired pneumonia and has excellent atypical coverage with broad spectrum
Macrolides Adverse drug reactions
- Gi intolerance
- **Erythromycin and clarithomycin have prolongation of QT interval
-abnormal taste**
Macrolides Antibacterial Spectrum
- broad spectrum
- excellent atypical coverage, some gram +, some gram -
- whopping cough and acne
Macrolides Therapeutic Uses
- whooping cough
- acne **
Clindamycin MOA
- Used to treat diabetic foot ulcers, aspiration pneumonias, acne.
- Coversanaerobic infections.
- Gram-positive cocci and has almost no gram negative coverage
Clindamycin Antibacterial spectrum
- covers anaerobic
- gram positive cocci, strepto, and staph
- has almost no gram -
- used to treat diabetic foot, skin and soft tissue infections
- MRSA**
Clindamycin Adverse Drug Reactions *
- Causes CDIFF
ClinDamycin = C Diff
What is CDIFF?
- superinfection
- watery stools up to 10-20 times a day
- Treatment; start metronidazole or oral vancomycin *
Linezolid MOA
- Primarily reserved for VRE infections and MRSA - Covers gram-positive bacteria and no gram negative coverage.
Linezolid Antibacterial spectrum
- gram positive; strept, staph, entero
- no gram negative
- reserved for VRE and MRSA**
Linezolid Adverse Drug Reactions
- Diarrhea, nausea, headache
Linezolid Drug Interactions **
**- weak MOA inhibitor
- can increase risk of SEROTONIN SYNDROME if taken with SSRI**
DNA Synthesis Inhibitors Drugs
- Fluoroquinolones
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Fluoroquinolones Drugs
- Ciprofloxacin
- Levofloxacin
- ends in FLOXACIN
Fluoroquinolones MOA
- inhibit bacterial DNA replication
Fluoroquinolones Pharmokinetics
- oral absorption is excellent
Fluoroquinolones Drug Interactions
- chelation occurs with anatacids, milk, vitamins
- best absorption if taken with empty stomach
- Some have cytochrome P450 interactions
Fluoroquinolones Adverse Drug Reactions
- TENDON RUPTURES
- prolongation of QT
- contraindicted in pregnancy
Fluoroquinolones Therapeutic indications
- broad spectrum
- gram neg, gram pos, atypical, almost no anaerobic
- used for UTI or respiratory tract infection
Folate Antagonists (sulfa drugs/sulfonamides) Drugs
- sufamethoxazole, bactrim component
- Trimethoprim
- Trimethoprim/sulfamethozazole
Folate Antagonists (sulfa drugs/sulfonamides) MOA
- inhibit folic acid synthesis
-bacteria turn PABA into folic acid
- use up much of enzyme needed to convert PABA to folic acid, decreasing folic acid production
Folate Antagonists (sulfa drugs/sulfonamides) Mechanism of selective toxicity
- fairly specific to bacterial cells
Folate Antagonists (sulfa drugs/sulfonamides) Therapeutic Indications
- UTI
- active against E.Coli and MRSA
Folate Antagonists (sulfa drugs/sulfonamides) Pharmacokinetics
- well absorbed orally
- distributes throughout body water
Folate Antagonists (sulfa drugs/sulfonamides) Adverse Effects
- Allergic reactions
- Nephrotoxicity
- kernicterus
- drug interactions with warfarin
Trimethroprim MOA
- dihydrofolate reductase inhibitor
- resistant in gram negative
Trimethroprim Pharmacokinetics
- similar to sulfonamides
- well absorbed orally
- distributes throughout body water
Trimethroprim Adverse Drug Reactions
- can produce effect of folate deficiency
Trimethroprim/Sulfamethoxazole Drug
- combination of two antibiotics
1) a sulfa drug
2) a folate antagonist (trimethroprim)
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Trimethroprim/Sulfamethoxazole MOA
- inhibits two sequential steps in synthesis of active folic acid
Trimethroprim/Sulfamethoxazole Adverse affects
- nephrotoxicity
-angioedema
-rashes
-steven johnsons syndrome
Trimethroprim/Sulfamethoxazole Therapeutic Indications
- UTI **
- pneumonia
Miscellaneous Drugs
- Nitrofurantoin
- Metronidazole
Nitrofurantoin MOA
- inhbits various enzymes and damages bacterial DNA
Nitrofurantoin Therapeutic Use
- Uncolicated UTIs
Nitrofurantoin Adverse Effects
- turns urine brown/orange**
- take with food or milk
Metronidazole MOA
- damages bacterial DNA
Metronidazole Therapeutic Uses**
- Drug of choice for C diff diarrhea
Metronidazole Adverse Effects
- headache, metallic taste, vertigo
Metronidazole Drug Interactions
- DO NOT TAKE WITH ALCOHOL ****
Two classes of antibiotics with cytochrome p450 drug interactions**
- Fluoroquinolones & Macrolides*
Two classes of antibiotics with chelation interactions**
- Fluoroquinolones & Tetracyclines
Difference between Active and Latent TB**
*- Active TB
Has symptoms
Infection: can be contagious and actively sick
-Latent TB
Has NO symptoms
Infection: Is NOT contagious or sick
Prime directive for TB **
- take two drugs or more
- prevents drug resistance*
Drugs to treat TB
-Isoniazid
-Rifampin
-Pyrazinamide
-Ethambutol
- RIPE
Isoniazid (IHN)
- MOA; targets enzymes responsible for outer layer
- Use; both latent and active TB
- ** Adverse; Liver Failure**
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Rifampin ***
- MOA; Blocks RNA synthesis
- Therapeutic; treatment of TB, MRSA, Meningitis
- Adverse; Liver failure, all body fluids orange-red**
- Drug Int; Cytochrome P450 Inducer ***
Pyrazinamide
-MOA; unknown
- Therapeutic; TB
- Adverse; Liver failure**
Ethambutol
- Therapeutic; TB
- Adverse; Optic nerve, red/green blindness
- REMEMBER EYECHART E
List the medication(s) indicated for treatment of latent TB **
*-Isoniazid (daily x 6-9 months or Twice weekly)
-Isoniazid + Rifapentine (Once weekly x 3 month)*
List the medications indicated for treatment of active TB**
*-Initially: Isoniazid + Rifampin + Pyrazinamide + Ethambutol ( x 2 months)
-Then: Isoniazid + Rifampin ( x 4 months)
OR
-Initially: Isoniazid + Rifampin (x 1 month)
-Then: Isoniazid + Rifampin (Daily or Biweekly x 8 months)
Discuss why patients receiving the common drug regimens for TB treatment must be monitored for liver function changes and why these patients should avoid alcohol**
-to monitor to liver failure
-Alcohol increase the RISK of Liver Failure
Antifungal Drugs MOA
- Bind to sterols in fungal cell membranes
- prevent synthesis of sterols
4 Classes of antifungals
- polyenes
- azoles
-pyrimidine analogs
- echinocandins
Polyenes Drugs
- Amphotericin B
Amphotericin B Therapeutic Use
- serious systemic fungal infections
Amphotericin B Adverse Drug Reactions***
***- SHAKE AND BAKE
- renal damage
- very very toxic**
Azoles Pharmacokinetics
- Broad Spectrum
- Cytochrome P450 Drug interactions
- end in AZOLE
Azole Drugs
- Ketoconazole
- fluconazole
Fluconazole **
- single oral dose is effective for yeast infections
Superficial fungal infections
- tinea = skin, scalp, hair
- candidas = vaginal, oral
- onchomycosis = nails
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Clotrimazole Use**
- superficial fungal and yeast infections**
Nystatin Use**
*- superficial candidal infections
-swish and swallow suspension**
Antiviral Drug MOA
- inhibition of viral replication
- viruses have no cell wall and no cell membrane
Non HIV Antivirals - Influenza inhibitors Drugs
- neuraminidase inhibitors; Oseltamivir and Zanamivir
Oseltamivir and Zanamivir
-Both = Treatment of A and B, expensive, start within 48 hours of symptoms
- osel(oral)
-zana(inhalant/powder )
Herpes Antivirals Drugs
- Acyclovir
-Valacyclovir
Treatment of genital herpes outbreaks**
-Life-long, daily suppressive therapy with antivirals will reduce frequency and viral shedding by 85%-
90%**
Treatment of varicella-zoster virus (herpes zoster), both chicken pox and shingles**
**-Chicken pox- Treatment can reduce severity by 30% if started early; Viravax ® (chicken pox vaccine) + booster vaccination now required for all school age children
-Shingles- latent virus; can flare-up later in life due to stress or immunocompromized conditions; treatment is important to prevent postherpetic neuralgia. Postherpetic neuralgia pain is extremely difficult to treat - occurs when the virus damages the nerves. Zostavax® - shingles vaccine ↓ shingles by 50%.**
Discuss the flu vaccine: when is it given, who should receive it, & who should NOT?**
-Flu vaccine is given in October/November. All people ages 6 months and older should receive it. You should NOT receive it if you have a severe allergy to chicken eggs, People who have had a severe reaction
to the influenza vaccine in the past, People who have experienced Guillain-Barre' syndrome (GBS), and people with moderate or severe illness with fever (these individuals should wait until symptoms resolve).
Compare symptoms of influenza and symptoms of a cold**
*-Both have headache and cough
-Both do not have diarrhea/vomiting as symptoms**
-Influenza is more severe and has more symptoms
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