An antifungal medication is a pharmaceutical fungicide used to treat and prevent mycoses such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and others. Such drugs are usually obtained by a doctor's prescription, but a few are available OTC (over-the-counter).
Antifungals work by exploiting differences between mammalian and fungal cells to kill the fungal organism with fewer adverse effects to the host. Unlike bacteria, both fungi and humans are eukaryotes. Thus, fungal and human cells are similar at the biological level. This makes it more difficult to discover drugs that target fungi without affecting human cells. As a consequence, many antifungal drugs cause side-effects. Some of these side-effects can be life-threatening if the drugs are not used properly.
An antifungal medication is a pharmaceutical fungicide used to treat and prevent mycoses such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and others. Such drugs are usually obtained by a doctor's prescription, but a few are available OTC (over-the-counter).
Antifungals work by exploiting differences between mammalian and fungal cells to kill the fungal organism with fewer adverse effects to the host. Unlike bacteria, both fungi and humans are eukaryotes. Thus, fungal and human cells are similar at the biological level. This makes it more difficult to discover drugs that target fungi without affecting human cells. As a consequence, many antifungal drugs cause side-effects. Some of these side-effects can be life-threatening if the drugs are not used properly.
Anthelmintics | B.Pharm 3rd year 2nd Sem | Medicinal Chemistry-III | History, Classification, Structures & Synthesis of anthelmintics, Synthesis of Diethylcarbamazine citrate, Synthesis of Mebendazole
Medicinal Chemistry and Pharmacology of Antifungal Agents and how to take care from fungal infections. Useful Course study material for the undergraduate , postgraduate and aspirants of Pharmacy , Pharmacology and Medicinal Chemistry.
Anthelmintics | B.Pharm 3rd year 2nd Sem | Medicinal Chemistry-III | History, Classification, Structures & Synthesis of anthelmintics, Synthesis of Diethylcarbamazine citrate, Synthesis of Mebendazole
Medicinal Chemistry and Pharmacology of Antifungal Agents and how to take care from fungal infections. Useful Course study material for the undergraduate , postgraduate and aspirants of Pharmacy , Pharmacology and Medicinal Chemistry.
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Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
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Title: Sense of Taste
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the structure and function of taste buds.
Describe the relationship between the taste threshold and taste index of common substances.
Explain the chemical basis and signal transduction of taste perception for each type of primary taste sensation.
Recognize different abnormalities of taste perception and their causes.
Key Topics:
Significance of Taste Sensation:
Differentiation between pleasant and harmful food
Influence on behavior
Selection of food based on metabolic needs
Receptors of Taste:
Taste buds on the tongue
Influence of sense of smell, texture of food, and pain stimulation (e.g., by pepper)
Primary and Secondary Taste Sensations:
Primary taste sensations: Sweet, Sour, Salty, Bitter, Umami
Chemical basis and signal transduction mechanisms for each taste
Taste Threshold and Index:
Taste threshold values for Sweet (sucrose), Salty (NaCl), Sour (HCl), and Bitter (Quinine)
Taste index relationship: Inversely proportional to taste threshold
Taste Blindness:
Inability to taste certain substances, particularly thiourea compounds
Example: Phenylthiocarbamide
Structure and Function of Taste Buds:
Composition: Epithelial cells, Sustentacular/Supporting cells, Taste cells, Basal cells
Features: Taste pores, Taste hairs/microvilli, and Taste nerve fibers
Location of Taste Buds:
Found in papillae of the tongue (Fungiform, Circumvallate, Foliate)
Also present on the palate, tonsillar pillars, epiglottis, and proximal esophagus
Mechanism of Taste Stimulation:
Interaction of taste substances with receptors on microvilli
Signal transduction pathways for Umami, Sweet, Bitter, Sour, and Salty tastes
Taste Sensitivity and Adaptation:
Decrease in sensitivity with age
Rapid adaptation of taste sensation
Role of Saliva in Taste:
Dissolution of tastants to reach receptors
Washing away the stimulus
Taste Preferences and Aversions:
Mechanisms behind taste preference and aversion
Influence of receptors and neural pathways
Impact of Sensory Nerve Damage:
Degeneration of taste buds if the sensory nerve fiber is cut
Abnormalities of Taste Detection:
Conditions: Ageusia, Hypogeusia, Dysgeusia (parageusia)
Causes: Nerve damage, neurological disorders, infections, poor oral hygiene, adverse drug effects, deficiencies, aging, tobacco use, altered neurotransmitter levels
Neurotransmitters and Taste Threshold:
Effects of serotonin (5-HT) and norepinephrine (NE) on taste sensitivity
Supertasters:
25% of the population with heightened sensitivity to taste, especially bitterness
Increased number of fungiform papillae
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Knee anatomy and clinical tests 2024.pdfvimalpl1234
This includes all relevant anatomy and clinical tests compiled from standard textbooks, Campbell,netter etc..It is comprehensive and best suited for orthopaedicians and orthopaedic residents.
New Directions in Targeted Therapeutic Approaches for Older Adults With Mantl...i3 Health
i3 Health is pleased to make the speaker slides from this activity available for use as a non-accredited self-study or teaching resource.
This slide deck presented by Dr. Kami Maddocks, Professor-Clinical in the Division of Hematology and
Associate Division Director for Ambulatory Operations
The Ohio State University Comprehensive Cancer Center, will provide insight into new directions in targeted therapeutic approaches for older adults with mantle cell lymphoma.
STATEMENT OF NEED
Mantle cell lymphoma (MCL) is a rare, aggressive B-cell non-Hodgkin lymphoma (NHL) accounting for 5% to 7% of all lymphomas. Its prognosis ranges from indolent disease that does not require treatment for years to very aggressive disease, which is associated with poor survival (Silkenstedt et al, 2021). Typically, MCL is diagnosed at advanced stage and in older patients who cannot tolerate intensive therapy (NCCN, 2022). Although recent advances have slightly increased remission rates, recurrence and relapse remain very common, leading to a median overall survival between 3 and 6 years (LLS, 2021). Though there are several effective options, progress is still needed towards establishing an accepted frontline approach for MCL (Castellino et al, 2022). Treatment selection and management of MCL are complicated by the heterogeneity of prognosis, advanced age and comorbidities of patients, and lack of an established standard approach for treatment, making it vital that clinicians be familiar with the latest research and advances in this area. In this activity chaired by Michael Wang, MD, Professor in the Department of Lymphoma & Myeloma at MD Anderson Cancer Center, expert faculty will discuss prognostic factors informing treatment, the promising results of recent trials in new therapeutic approaches, and the implications of treatment resistance in therapeutic selection for MCL.
Target Audience
Hematology/oncology fellows, attending faculty, and other health care professionals involved in the treatment of patients with mantle cell lymphoma (MCL).
Learning Objectives
1.) Identify clinical and biological prognostic factors that can guide treatment decision making for older adults with MCL
2.) Evaluate emerging data on targeted therapeutic approaches for treatment-naive and relapsed/refractory MCL and their applicability to older adults
3.) Assess mechanisms of resistance to targeted therapies for MCL and their implications for treatment selection
NVBDCP.pptx Nation vector borne disease control programSapna Thakur
NVBDCP was launched in 2003-2004 . Vector-Borne Disease: Disease that results from an infection transmitted to humans and other animals by blood-feeding arthropods, such as mosquitoes, ticks, and fleas. Examples of vector-borne diseases include Dengue fever, West Nile Virus, Lyme disease, and malaria.
ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
Ozempic: Preoperative Management of Patients on GLP-1 Receptor Agonists Saeid Safari
Preoperative Management of Patients on GLP-1 Receptor Agonists like Ozempic and Semiglutide
ASA GUIDELINE
NYSORA Guideline
2 Case Reports of Gastric Ultrasound
12. Mohamed Bahr; MD, PhD
1. NATURAL PENICILLINS (PENICILLIN G
[BENZYLPENICILLIN], PENICILLIN V)
Narrow spectrum (gram +ve cocci and bacilli and gram -ve
cocci).
Penicillin V is acid-stable (PO); penicillin G is less stable (IM).
Inactivated by β-lactamase.
13. Mohamed Bahr; MD, PhD
2. ANTI-STAPH PENICILLINS
(OXACILLIN, CLOXACILLIN,
FLUCLOXACILLIN, NAFCILLIN)
Narrow spectrum as natural penicillins.
Stable to gastric acidity.
Stable to β-lactamase.
14. Mohamed Bahr; MD, PhD
3. BROAD-SPECTRUM
PENICILLINS (AMPICILLIN AND
AMOXICILLIN)
Broad-spectrum (as natural penicillins plus some gram -ve
bacilli).
Stable to gastric acidity.
Inactivated by β-lactamase.
15. Mohamed Bahr; MD, PhD
4. ANTIPSEUDOMONAL (OR EXTENDED-
SPECTRUM) PENICILLINS
(CARBENICILLIN INDANYL, TICARCILLIN,
PIPERACILLIN)
Broad-spectrum including Pseudomonas and many gram -ve
bacilli. Piperacillin is also active against Klebseilla
pneumonia.
Unstable to gastric acidity (given parenterally).
Inactivated by β-lactamase.
16. Mohamed Bahr; MD, PhD
5. LONG-ACTING PENICILLINS
(BENZATHINE PENICILLIN,
PROCAINE PENICILLIN)
Insoluble salts of penicillin G →
allow slow drug absorption with
long duration of action (penicillin
G is short-acting; 6 hours).
Procaine penicillin: given /12
hours.
Benzathine penicillin: given
once/month.
24. Mohamed Bahr; MD, PhD
COMMON USES
Streptococcal infections:
• Acute throat infections, wound sepsis, puerperal fever.
• Bacterial endocarditis: penicillin is given plus an aminoglycoside
(facilitate penetration of aminoglycosides by interfering with
bacterial cell wall synthesis → synergistic bactericidal effect).
Staphylococcal infections.
Pneumococcal infections.
Diphtheria, tetanus and gas gangrene (penicillin plus specific
antitoxins).
25. Mohamed Bahr; MD, PhD
COMMON USES
Meningococcal meningitis: penicillin G or ampicillin IV plus
chloramphenicol.
Gonorrhea (alternative: fluorinated quinolones).
Typhoid and paratyphoid fever: amoxicillin and ampicillin.
Syphilis
Prophylaxis against:
• Recurrence of rheumatic fever: benzathine penicillin (1.2 million
units/month).
• Bacterial endocarditis (plus an aminoglycoside).
29. Mohamed Bahr; MD, PhD
ADVERSE EFFECTS
Hypersensitivity (most important). Maybe either direct effect,
rashes and phlebitis; or immunological (due to antigenic
metabolites), angioedema (marked swelling of lips, tongue,
periorbital area) and anaphylaxis. This is more with penicillin G,
so its use is restricted. Cross-allergy may occur between β-
lactam antibiotics.
Diarrhea: disruption of normal balance of intestinal flora; more
with incompletely absorbed and broad-spectrum agents.
Seizures: IT - RF.
Cation disturbance: hyperkalemia with penicillin G.
31. Mohamed Bahr; MD, PhD
1st
Generation
Cephalexin
(PO)
Cefazolin (IV)
G +ve cocci (Strept - Staph), some G -ve organisms (E coli -
Klebsiella)
Cephalexin: Broad spectrum in URTI, UTI
Cefazolin: 1st choice in surgical prophylaxis
In orthopedic surgery: penetrates bone well, penicillinase
resistant (Staph)
2nd
Generation
Cefaclor (PO)
Cefuroxime
(IV)
Cephamycins
(cefoxitin,
cefotetan,
cefmetazole)
(IV)
Less active on G +ve, extended spectrum on G -ve organisms
Cephamycins: aerobic and anerobic G –ve bacilli
Oral agents are used in sinusititis, otitis
Cefuroxime: also in community acquired pneumonia (H
influenza).
Cephamycins are structurally related to cephalosporins, used in
mixed anaerobic infections (including B fragillis), e.g., peritonitis
32. Mohamed Bahr; MD, PhD
3rd Generation
Cefoperazone,
Cefotaxime,
Ceftriaxone
(IV)
↑ activity against resistant G -ve organisms (e.g. Pseudomonas)
Used in serious infections
Most agents cross BBB (used in meningitis)
Ceftriaxone (Longest t½): used in gonorrhea (single injection), typhoid (resistant cases)
Bone: good penetration. BBB: crosses BBB, so can be used in meningitis. Bile: excreted
in bile (40%), used in biliary infection and in renal dysfunction.
4th Generation
Cefepime (IV)
Similar spectrum to 3rd generation on G –ve, effective on penicillin-resistant Strept and
Staph
Crosses BBB well
33. Mohamed Bahr; MD, PhD
5th Generation: Ceftarolene fosamil (IV)
Broad spectrum prodrug, effective against MRSA,
VRSA, H influenza, G -ve organisms (plus
aminoglycosides).
Used in skin infections and community-acquired
pneumonia.
Adjust dose in renal impairment.
36. Mohamed Bahr; MD, PhD
ADVERSE EFFECTS
Hypersensitivity: cross-allergy with penicillins → avoided in patients
with serious (immediate) hypersensitivity to penicillin.
Hypoprothrombinemia and bleeding.
Nephrotoxicity especially if used with aminoglycosides.
Local irritation → severe pain after IMI and thrombophlebitis after IVI.
Intolerance to alcohol → disulfiram-like reaction.
Cross-resistance with penicillins: avoided in penicillin-resistant
infections.
37. Mohamed Bahr; MD, PhD
C. CARBAPENEMS:
IMIPENEM (IV) BROADEST
Effective against gram +ve, -ve organisms and anaerobes.
Resistant to β-lactamase.
High cross-allergy with penicillin.
High risk of toxicity:
• Metabolized in the kidney to an inactive nephrotoxic metabolite, thus it is
given with cilastatin to inhibit renal metabolism.
• High risk of convulsion → avoided in meningitis.
Meropenem and ertapenem are similar to imipenem with less renal
degradation (cilastatin is not required) and less risk of convulsions.
38. Mohamed Bahr; MD, PhD
D. MONOBACTAMS:
AZTREONAM (IV & IM)
NARROW
Effective against aerobic gram -ve organisms (as
aminoglycosides).
Resistant to β-lactamase.
No cross-allergy with β-lactams.
41. Mohamed Bahr; MD, PhD
II. VANCOMYCIN G+, IVI
• Staph resistant to penicillin (MRSA): drug of choice. It is used
in serious infections as Staph pneumonia, endocarditis and
osteomyelitis.
• Severe Staph infections in patients allergic to penicillins or
cephalosporins.
• Pseudomembranous colitis following antibiotic use.
44. Mohamed Bahr; MD, PhD
ADVERSE EFFECTS
• Fever, chills, rigors and phlebitis.
• Shock with rapid infusion → red man syndrome (due to
histamine release). Avoided by slow infusion and
pretreatment with antihistamines.
• Ototoxic.
• Nephrotoxic.
55. Mohamed Bahr; MD, PhD
ADVERSE EFFECTS AND
CONTRAINDICATIONS
• Epigastric pain due to gastric irritation (noncompliance).
• Teeth discoloration and bone hypoplasia.
• Hepatotoxicity (in renal failure or pregnancy).
• Phototoxicity (sensitivity of skin to sun light).
• Superinfection with Candida, C difficile or resistant Staph in
intestine.
• Fanconi-like syndrome: renal tubular dysfunction with outdated
tetracyclines.
• Contraindicated in renal dysfunction.
56. Mohamed Bahr; MD, PhD
TIGECYCLINE (SLOW IVI)
• Similar to tetracycline in structure, mechanism, and adverse
effects; with less resistance.
• Effective against gram +ve, gram -ve, and anaerobes; a wide
variety of multidrug-resistant nosocomial infections.
• Causes nausea.
• Adjust in liver impairment.
59. Mohamed Bahr; MD, PhD
SPECTRUM AND
ACTIVITY
• Effective against aerobic organisms.
• Ineffective against anaerobes (requires O2 for transport into
cells).
• Act mainly against gram -ve organisms, e.g., E coli,
Pseudomonas, cholera.
• Gentamycin is also effective against Staph infections.
• Amikacin resists bacterial enzymatic inactivation, thus it is the
most effective aminoglycoside against gram -ve bacilli.
60. Mohamed Bahr; MD, PhD
PHARMACOKINETICS
• Absorption: not absorbed orally thus have to be given
parenterally.
• Distribution: do not cross BBB even when meninges are
inflamed. They are concentrated in renal cortex, perilymph and
endolymph of inner ear → nephrotoxicity and ototoxicity.
• Excretion: unchanged through the kidney (care in renal
dysfunction).
61. Mohamed Bahr; MD, PhD
THERAPEUTIC USES
• Peritonitis, septicemia, pneumonia.
• Complicated UTI.
• Bacterial endocarditis.
• Streptomycin is used in TB.
• Amikacin and netilmicin are reserved for resistant cases.
• Neomycin (too nephrotoxic for systemic use): used orally in
hepatic coma and intestinal antiseptic before surgery (not
absorbed) and topically in infected wounds.
63. Mohamed Bahr; MD, PhD
ADVERSE EFFECTS
Nephrotoxicity: acute tubular necrosis (may be irreversible). Risk
↑ by dehydration, old age, ↑ dose, ↑ duration or concurrent use of
nephrotoxic drugs.
Ototoxicity: may be irreversible. Coadministration of loop
diuretics or quinidine → ↑ risk.
Neuromuscular paralysis (inhibit ACh release), especially after
intraperitoneal or intrapleural infusion of large doses.
Allergy: contact dermatitis with topically applied neomycin.
64. Mohamed Bahr; MD, PhD
SPECTINOMYCIN
Gonorrhea in patients allergic to
penicillin or patients with penicillin-
resistant gonococcal infection
(single deep IMI).
68. Mohamed Bahr; MD, PhD
SPECTRUM AND USES
Chlamydia, Mycoplasma, Spirochetes, gram +ve cocci
and bacilli as an alternative to penicillins and
tetracyclines. They are of choice in:
Patients with allergy to β lactam antibiotics.
Urogenital Chlamydia infection in pregnancy.
Mycoplasma pneumonia in children (tetracyclines are
contraindicated).
69. Mohamed Bahr; MD, PhD
ADVERSE EFFECTS
Epigastric pain and GIT distress (increases bowel
motility).
Cholestatic jaundice (erythromycin estolate). CI in
liver disease.
Ototoxicity and may lead to transient deafness.
Thrombophlebitis if injected IV.
Prolonged QT interval.
70. Mohamed Bahr; MD, PhD
Enzyme inhibitor: ↑ level of theophylline,
warfarin, carbamazepine and terfenadine (→
arrhythmias).
↑ Digoxin level (inhibits intestinal flora that
inactivate digoxin).
73. Mohamed Bahr; MD, PhD
IV. CLINDAMYCIN
Bone
Anaerobic
Pseudomembranous
colitis
74. Mohamed Bahr; MD, PhD
V. CHLORAMPHENICOL
Rarely used
Typhoid fever (not carrier), but replaced by fluoroquinolones.
Bacterial meningitis (e.g., H influenza) plus penicillin.
Anaerobic infection, e.g., anaerobic brain abscess.
Topically in eye infections.
75. Mohamed Bahr; MD, PhD
ADVERSE EFFECTS
GIT upsets and superinfection.
Bone marrow depression: may be dose-independent or
idiosyncratic.
Gray baby syndrome in neonates (↓ drug clearance due to
undeveloped liver and kidney functions).
Optic neuritis.
Enzyme inhibitor: ↑ warfarin, phenytoin and oral hypoglycemics
level.
80. Mohamed Bahr; MD, PhD
VII. OXAZOLIDINONES:
LINEZOLID
Binds to a unique site on the 50S subunit →
inhibits initiation complex → inhibits protein
synthesis.
82. Mohamed Bahr; MD, PhD
SPECTRUM AND USES
(PO, IV; 100% F)
Restricted to serious infections with gram +ve
organisms resistant to vancomycin or MRSA in
patients intolerant to vancomycin or if IV
access is unavailable.
87. Mohamed Bahr; MD, PhD
Inhibit bacterial:
topoisomerase II (DNA gyrase)
topoisomerase IV
88. Mohamed Bahr; MD, PhD
Nonfluorinated
Quinolones
1st - generation
• Nalidixic Acid
• Not used in systemic
infections, as 90% of
drug is bound to
plasma proteins →
insufficient plasma
conc.
• Used only in UTI
with G -ve bacilli
• Rapid resistance
limits its use
Fluorinated
Quinolones
2nd to 4th generation
• 2nd → 4th
Generation
• Newer Fluorinated
derivatives achieving
systemic levels
• Used in systemic
Infections
89. Mohamed Bahr; MD, PhD
GENERATIONS OF
FLUOROQUINOLONES
Originally developed because of their excellent
activity against gram -ve aerobic bacteria; they
had limited activity against gram +ve
organisms.
Several newer agents have improved activity
against … and …
90. Mohamed Bahr; MD, PhD
2ND GENERATION
NORFLOXACIN - CIPROFLOXACIN - OFLOXACIN -
PEFLOXACIN
Norfloxacin
the least active against both gram -ve and gram +ve organisms. Only in UTI
as it does not achieve systemic levels.
Newer agents
excellent gram -ve activity
moderate to good activity against gram +ve bacteria
MRSA?
Ciprofloxacin
the most active fluoroquinolone against gram -ve organisms esp.
Pseudomonas.
91. Mohamed Bahr; MD, PhD
3RD GENERATION
LEVOFLOXACIN
Greater activity on G +ve, including
Streptococcus pneumoniae
92. Mohamed Bahr; MD, PhD
4TH GENERATION
MOXIFLOXACIN - CLINAFLOXACIN
Improved activity against gram +ve organisms,
particularly S pneumoniae and some Staph.
Fluoroquinolones also are active against agents of
atypical pneumonia (e.g., Mycoplasma and
Chlamydiae) and against intracellular pathogens such
as Legionella species and some Mycobacteria.
Potent against anaerobic bacteria.
94. Mohamed Bahr; MD, PhD
THERAPEUTIC USES
UTI (gram -ve bacilli) and prostatitis.
RTI resistant to β-lactams and atypical pneumonia due to chlamydia,
mycoplasma, legionella (levofloxacin- moxifloxacin).
Typhoid and infective diarrhea (ciprofloxacin: 1st choice for empiric
therapy).
Gonorrhea (ofloxacin single dose, levofloxacin).
Bone and soft tissue infection.
Resistant TB.
Anaerobes.
97. Mohamed Bahr; MD, PhD
CI
Quinolones are contraindicated in
pregnancy and lactation.
Not routinely recommended in patients <18
years (→ arthropathy).
101. Mohamed Bahr; MD, PhD
II. RIFAMPIN
Binds and inhibits DNA-dependent RNA polymerase →
inhibition of RNA synthesis.
102. Mohamed Bahr; MD, PhD
SPECTRUM
Effective against mycobacteria at all sites and
leprosy.
Potent broad spectrum bactericidal. Effective
against MRSA.
Antiviral effect.
103. Mohamed Bahr; MD, PhD
PHARMACOKINETICS
Well absorbed after oral administration.
Widely distributed in body tissues and fluids and can reach TB
cavities and sputum and penetrate macrophages killing slowly
growing TB bacilli inside.
Crosses BBB.
Metabolized in the liver and it is a potent enzyme inducer.
Excreted mainly in bile (enterohepatic recycling) and slightly in
urine.
105. Mohamed Bahr; MD, PhD
ADVERSE EFFECTS
Red discoloration of urine, tears, sputum and soft contact
lenses.
Flu-like syndrome (malaise, headache and fever...).
Liver damage and jaundice.
Resistance: rapid (but no cross-resistance with other anti-TB
drugs).
Enzyme induction (serious drug interactions).
112. Mohamed Bahr; MD, PhD
CO-TRIMOXAZOLE
SMX-TMP 400/80
UTI, gonococcal urethritis and prostatitis.
RTI due to H influenza and S pneumoniae.
Typhoid fever.
113. Mohamed Bahr; MD, PhD
ADVANTAGES?
Synergistic combination.
Less and delayed bacterial resistance
More potent (Bactericidal) and wider-spectrum including
Proteus, Salmonella, Shigella, H. influenza and
Gonococcus.
131. Mohamed Bahr; MD, PhD
2. Dapsone
Bacteriostatic. It is related to sulfonamides and achieves ↑ skin
concentration.
Antagonist to PABA → inhibits folate synthesis.
Adverse Effects
Hemolysis (esp. in G6PD deficiency) - methemoglobuinemia.
PN.
Erythema nodosum leprosum (ENL) → suppressed by
corticosteroids.
132. Mohamed Bahr; MD, PhD
3. Clofazimine (PO)
A dye accumulating in phagocytes and skin → bactericidal
effect through:
• Binding to DNA, preventing template formation and DNA
replication.
• Formation of cytotoxic oxygen radicals.
Anti-inflammatory: no ENL → used in patients developing ENL
with dapsone.
Adverse effects: skin discoloration (red-brown) - enteritis.
133. Mohamed Bahr; MD, PhD
REFERENCES
Lippincott’s Illustrated Reviews, 5th ed.
Color Atlas of Pharmacology, 2nd ed.
Goodman and Gilman's The Pharmacological Basis of
Therapeutics, 12th ed.
Editor's Notes
The 70S ribosomal mRNA complex is shown with its 50S and 30S subunits. In step 1, the charged tRNA unit carrying amino acid 6 binds to the acceptor site on the 70S ribosome. The peptidyl tRNA at the donor site, with amino acids 1 through 5, then binds the growing amino acid chain to amino acid 6 (transpeptidation, step 2). The uncharged tRNA left at the donor site is released (step 3), and the new 6-amino acid chain with its tRNA shifts to the peptidyl site (translocation, step 4). The antibiotic binding sites are shown schematically as triangles. Chloramphenicol (C) and macrolides (M) bind to the 50S subunit and block transpeptidation (step 2). The tetracyclines (T) bind to the 30S subunit and prevent binding of the incoming charged tRNA unit (step 1).