This document discusses penicillin-G and semisynthetic penicillins. It provides details on the antibacterial spectrum and mechanisms of resistance for penicillin-G. It also describes the pharmacokinetics of penicillin-G and various adverse effects. The document then discusses various semisynthetic penicillins including acid-resistant, penicillinase-resistant, and extended spectrum penicillins. It provides examples like phenoxymethyl penicillin, methicillin, cloxacillin, and ampicillin; and discusses their spectrums of activity, pharmacokinetics, uses, and limitations due to emerging resistance.
This ppt deals with the sulfonamide group of drugs with classification, mechanism, spectrum, resistance, uses and adverse effects discussed in detail. It also discusses in detail about Cotrimoxazole
this presentation gives the knowledge about the decongestants are a type of medication that can provide short relief for a blocked nose ................
This PPT covers drug therapy for tuberculosis. It includes classification of antitubercular drugs, chemotherapy for tuberculosis, strategies for addressing resistance and pharmacotherapy of antitubercular drugs
Pharmacology of Penicllins (Beta lactam antibiotics), description of their mechanism of action, mechanism of resistance, classification, indications and adverse effects
synthetic antimicrobials having a quinolone structure that are active primarily against gram-negative bacteria, though newer fluorinated compounds also inhibit gram-positive ones.
This ppt deals with the sulfonamide group of drugs with classification, mechanism, spectrum, resistance, uses and adverse effects discussed in detail. It also discusses in detail about Cotrimoxazole
this presentation gives the knowledge about the decongestants are a type of medication that can provide short relief for a blocked nose ................
This PPT covers drug therapy for tuberculosis. It includes classification of antitubercular drugs, chemotherapy for tuberculosis, strategies for addressing resistance and pharmacotherapy of antitubercular drugs
Pharmacology of Penicllins (Beta lactam antibiotics), description of their mechanism of action, mechanism of resistance, classification, indications and adverse effects
synthetic antimicrobials having a quinolone structure that are active primarily against gram-negative bacteria, though newer fluorinated compounds also inhibit gram-positive ones.
To enjoy the presentation kindly download it.
For Original view, download "Poetsen One" font style from dafont website.
Here I have discussed pharmacology of penicillin G.
Respiratory stimulants: types, complete discussion on indications, contraindications, assessment, patient notes and examples of stimulants both central and respiratory
Expectorants and Antitussives: types, complete discussion on indications, contraindications, assessment, patient notes and examples of expectorants and antitussives
Complete pharmacology of Non steroidal Anti inflammatory Drugs, classification, Mechanism of action, Pharmacological actions, Indications, Contraindications, Adverse effects
Pharmacology laboratory experiment, both invivo and invitro includes interpolation, matching , bracketing, three point, four point bioassays with a note on hypoglycemic activity, acute skin irritation, acute eye irritaiton, pyrogen test, gastrointestinal motility test, physiological salt solutions
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
micro teaching on communication m.sc nursing.pdfAnurag Sharma
Microteaching is a unique model of practice teaching. It is a viable instrument for the. desired change in the teaching behavior or the behavior potential which, in specified types of real. classroom situations, tends to facilitate the achievement of specified types of objectives.
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
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
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journeygreendigital
Tom Selleck, an enduring figure in Hollywood. has captivated audiences for decades with his rugged charm, iconic moustache. and memorable roles in television and film. From his breakout role as Thomas Magnum in Magnum P.I. to his current portrayal of Frank Reagan in Blue Bloods. Selleck's career has spanned over 50 years. But beyond his professional achievements. fans have often been curious about Tom Selleck Health. especially as he has aged in the public eye.
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Introduction
Many have been interested in Tom Selleck health. not only because of his enduring presence on screen but also because of the challenges. and lifestyle choices he has faced and made over the years. This article delves into the various aspects of Tom Selleck health. exploring his fitness regimen, diet, mental health. and the challenges he has encountered as he ages. We'll look at how he maintains his well-being. the health issues he has faced, and his approach to ageing .
Early Life and Career
Childhood and Athletic Beginnings
Tom Selleck was born on January 29, 1945, in Detroit, Michigan, and grew up in Sherman Oaks, California. From an early age, he was involved in sports, particularly basketball. which played a significant role in his physical development. His athletic pursuits continued into college. where he attended the University of Southern California (USC) on a basketball scholarship. This early involvement in sports laid a strong foundation for his physical health and disciplined lifestyle.
Transition to Acting
Selleck's transition from an athlete to an actor came with its physical demands. His first significant role in "Magnum P.I." required him to perform various stunts and maintain a fit appearance. This role, which he played from 1980 to 1988. necessitated a rigorous fitness routine to meet the show's demands. setting the stage for his long-term commitment to health and wellness.
Fitness Regimen
Workout Routine
Tom Selleck health and fitness regimen has evolved. adapting to his changing roles and age. During his "Magnum, P.I." days. Selleck's workouts were intense and focused on building and maintaining muscle mass. His routine included weightlifting, cardiovascular exercises. and specific training for the stunts he performed on the show.
Selleck adjusted his fitness routine as he aged to suit his body's needs. Today, his workouts focus on maintaining flexibility, strength, and cardiovascular health. He incorporates low-impact exercises such as swimming, walking, and light weightlifting. This balanced approach helps him stay fit without putting undue strain on his joints and muscles.
Importance of Flexibility and Mobility
In recent years, Selleck has emphasized the importance of flexibility and mobility in his fitness regimen. Understanding the natural decline in muscle mass and joint flexibility with age. he includes stretching and yoga in his routine. These practices help prevent injuries, improve posture, and maintain mobilit
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
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Explore natural remedies for syphilis treatment in Singapore. Discover alternative therapies, herbal remedies, and lifestyle changes that may complement conventional treatments. Learn about holistic approaches to managing syphilis symptoms and supporting overall health.
Anti ulcer drugs and their Advance pharmacology ||
Anti-ulcer drugs are medications used to prevent and treat ulcers in the stomach and upper part of the small intestine (duodenal ulcers). These ulcers are often caused by an imbalance between stomach acid and the mucosal lining, which protects the stomach lining.
||Scope: Overview of various classes of anti-ulcer drugs, their mechanisms of action, indications, side effects, and clinical considerations.
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.
3. • Cocci: Streptococci (except viridans, group D or enterococci) are
highly sensitive, so are many pneumococci.
• Staph. aureus, though originally very sensitive, has acquired resistance to
such an extent that it must be counted out of PnG spectrum.
• Gram negative cocci—Neisseria gonorrhoeae and N. meningitidis are
susceptible to PnG, though increasing number of gonococci have
developed partial and others high degree resistance.
4. • Bacilli: Gram-positive bacilli—majority of B. anthracis, Corynebacterium
diphtheriae, and practically all Clostridia (tetani and others), Listeria are
highly sensitive, so are spirochetes (Treponema pallidum, Leptospira, and
others)
• Bacteroides fragilis is largely resistant.
• Actinomyces israelii is only moderately sensitive.
• Majority of aerobic gram-negative bacilli, Mycobacterium tuberculosis,
rickettsiae, chlamydiae, protozoa, fungi and viruses are totally insensitive
to PnG.
5. BACTERIAL RESISTANCE
Many bacteria are inherently insensitive to PnG because in them
the target enzymes and PBPs are located deeper under lipoprotein
barrier where PnG is unable to penetrate or have low affinity for
PnG. The primary mechanism of acquired resistance is
production of penicillinase.
6. PENICILLINASE
• Penicillinase It is a narrow spectrum β-lactamase which opens the β-
lactam ring and inactivates PnG and some closely related congeners.
• Majority of Staphylococci and some strains of gonococci, B. subtilis, E.
coli, H. influenzae and few other bacteria produce penicillinase.
• The gram-positive penicillinase producers elaborate large quantities of the
enzyme which diffuses into the surroundings and can protect other
inherently sensitive bacteria.
• In gram-negative bacteria, penicillinase is found in small quantity, but is
strategically located inbetween the lipoprotein and peptidoglycan layers of
the cell wall.
7. • The gram-negative bacteria have ‘porin’ channels formed by
specific proteins located in their outer membrane.
• Permeability of various β-lactam antibiotics through these
channels differs: ampicillin and other members which are active
against gram-negative bacteria cross the porin channels much
better than PnG.
• Some gram-negative bacteria become resistant by loss or
alteration of porin channels.
8. PHARMACOKINETICS
• Penicillin G is acid labile, therefore destroyed by gastric acid.
• As such, less than 1/3rd of an oral dose is absorbed in the active
form.
• Absorption of sod. PnG from i.m. site is rapid and complete;
peak plasma level is attained in 30 min.
• It is distributed mainly extracellularly; reaches most body fluids,
but penetration in serous cavities and CSF is poor.
• About 60% is plasma protein bound. It is little metabolized
because of rapid excretion.
9. • The pharmacokinetics of PnG is dominated by very rapid renal
excretion; about 10% by glomerular filtration and the rest by
tubular secretion.
• The plasma t½ of PnG in healthy adult is 30 min. Neonates have
slower tubular secretion— t½ of PnG is longer; but approaches
adult value at 3 months and then is even shorter during
childhood.
• Aged and those with renal failure excrete penicillin slowly.
• Tubular secretion of PnG can be blocked by probenecid—higher
and longer lasting plasma concentrations are achieved.
Probenecid also decreases the volume of distribution of
penicillins.
10. ADVERSE EFFECTS
Penicillin G is one of the most nontoxic antibiotics; up to 20
MU has been injected in a day without any organ toxicity.
11. • Local irritancy and direct toxicityPain at i.m. injection site, nausea on
oral ingestion and thrombophlebitis of injected vein are doserelated
expressions of irritancy.
• Toxicity to the brain may be manifested as mental confusion, muscular
twitchings, convulsions and coma, when very large doses (> 20 MU) are
injected i.v.; especially in patients with renal insufficiency.
• Bleeding has also occurred with such high doses due to interference with
platelet function.
• Intrathecal injection of PnG is no longer recommended because it has
caused arachnoiditis and degenerative changes in spinal cord.
• Accidental i.v. injection of procaine penicillin produces CNS stimulation,
hallucinations and convulsions due to procaine. Being insoluble, it may
also cause microembolism.
12. • Hypersensitivity These reactions are the major problem in the use of
penicillins.
• An incidence of 1–10% is reported. Individuals with an allergic diathesis are
more prone to develop penicillin reactions.
• PnG is the most common. Frequent manifestations of penicillin allergy
are—rash, itching, urticaria and fever. Wheezing, angioneurotic edema,
serum sickness and exfoliative dermatitis are less common.
• Anaphylaxis is rare (1 to 4 per 10,000 patients), but may be fatal.
13. SuperinfectionsThese are rare with PnG because of its narrow
spectrum; though bowel, respiratory and cutaneous microflora does undergo
changes.
14. • Jarisch-Herxheimer reaction Penicillin injected in a syphilitic
patient (particularly secondary syphilis) may produce shivering, fever,
myalgia, exacerbation of lesions, even vascular collapse.
• This is due to sudden release of spirochetal lytic products and lasts for
12–72 hours. I
• t does not recur and does not need interruption of therapy.
• Aspirin and sedation afford relief of symptoms.
15. USES
• Penicillin G is the drug of choice for infections caused by
organisms susceptible to it, unless the patient is allergic to this
antibiotic.
• However, use has declined very much due to fear of causing
anaphylaxis.
16. Streptococcal infections
• Like pharyngitis, otitis media, scarlet fever, rheumatic fever respond
to ordinary doses of PnG because Strep. pyogenes has not
developed significant resistance.
• However, the risk of injecting PnG for this infection is seldom
taken now.
• For subacute bacterial endocarditis (SABE) caused by Strep.
viridans or faecalis high doses (10–20 MU i.v. daily) along with
gentamicin given for 2–6 weeks is needed.
17. Pneumococcal infections
• PnG is not used now for empirical therapy of pneumococcal
(lobar) pneumonia and meningitis because many strains have
become highly penicillin resistant.
• However, PnG 3–6 MU i.v. every 6 hours is the drug of choice
if organism is sensitive.
18. Meningococcal infections
• still mostly responsive; meningitis and other infections may be treated with
intravenous injection of high doses.
Gonorrhoea
• PnG has become unreliable for treatment of gonorrhoea due to spread of
resistant strains.
• The treatment of ophthalmia neonatorum due to sensitive N. gonorrhoeae
consists of saline irrigation + sod. PnG 10,00020,000 U/ml 1 drop in each
eye every 1–3 hours. In severe cases, give 50,000 U i.m. BD for 1 week in
addition.
19. Syphilis T. pallidum
• has not shown any resistance and PnG is the drug of choice.
• Early and latent syphilis is treated either with daily i.m. injection of
1.2 MU of procaine penicillin for 10 days or with 1–3 weekly doses
of 2.4 MU benzathine penicillin.
• For late syphilis, benzathine penicillin 2.4 MU weekly for 4 weeks is
recommended.
• Cardiovascular and neurosyphilis requires sod. PnG 5 MU i.m. 6
hourly for 10–14 days followed by the above regimen.
• Leptospirosis: PnG 1.5 MU injected i.v. 6 hourly for 7 days is
curative.
20. Diphtheria Antitoxin therapy
Is of prime importance. Procaine penicillin 1–2 MU daily for 10 days is used
to prevent carrier state.
Tetanus and gas gangrene
Antitoxin and other measures are more important; PnG 6–12 MU/day is used
to kill the causative organism and has adjuvant value.
21. • Penicillin G is the drug of choice for rare infections like
anthrax, actinomycosis, rat bite fever and those caused by
Listeria monocytogenes, Pasteurella multocida.
• For trench mouth or acute necrotizing ulcerative gingivitis
(ANUG) which is a mixed infection caused by spirochetes and
fusobacteria
• PnG (i.m.)/penicillin V (oral) or amoxicillin are generally
combined with metronidazole.
22. PROPHYLACTIC USES
(a)Rheumatic fever: Low concentrations of penicillin prevent colonization by
streptococci that are indirectly responsible for rheumatic fever. Benzathine penicillin
1.2 MU every 4 weeks till 18 years of age or 5 years after an attack, whichever is more.
(b)Bacterial endocarditis: Dental extractions, endoscopies, catheterization, etc.
cause bacteremia which in patients with valvular defects can cause endocarditis. PnG
can afford protection, but amoxicillin is preferred now.
(c)Agranulocytosis patients: Penicillin has been used alone or in combination
with streptomycin to prevent respiratory and other acute infections, but cephalosporins
+ an aminoglycoside or fluoroquinolone are preferred now.
24. SEMISYNTHETIC PENICILLINS
• Semisynthetic penicillins are produced by chemically combining
specific side chains (in place of benzyl side chain of PnG) or by
incorporating specific precursors in the mould cultures.
• Thus, procaine penicillin and benzathine penicillin are salts of
PnG and not semisynthetic penicillins.
25. The aim of producing semisynthetic penicillins has been to overcome the
shortcomings of PnG, which are:
1. Poor oral efficacy.
2. Susceptibility to penicillinase.
3. Narrow spectrum of activity.
4. Hypersensitivity reactions (this has not been overcome in any
preparation).
In addition, some β-lactamase inhibitors have been developed which
themselves are not antibacterial, but augment the activity of penicillins
against β-lactamase producing organisms.
27. ACID-RESISTANT ALTERNATIVE TO PENICILLIN-G
• Phenoxymethyl penicillin (Penicillin V) It differs from PnG only in that it
is acid stable.
• Oral absorption is better; peak blood level is reached in 1 hour and plasma
t½ is 30–60 min.
• The antibacterial spectrum of penicillin V is identical to PnG, but it is
about 1/5 as active against Neisseria, other gram negative bacteria and
anaerobes.
• It cannot be depended upon for more serious infections and is used only
for streptococcal pharyngitis, sinusitis, otitis media, prophylaxis of
rheumatic fever (when an oral drug has to be selected), less serious
pneumococcal infections and trench mouth.
28. PENICILLINASE-RESISTANT PENICILLINS
• Methicillin It is highly penicillinase resistant but not acid resistant—must be injected.
• It is also an inducer of penicillinase production.
• MRSA have emerged in many areas. These are insensitive to all penicillinase-resistant
penicillins and to other β-lactams as well as to erythromycin, aminoglycosides,
tetracyclines, etc.
• The MRSA have altered PBPs which do not bind penicillins.
• The drug of choice for these organisms is vancomycin/linezolid, but ciprofloxacin can
also be used.
• Haematuria, albuminuria and reversible interstitial nephritis are the specific adverse
effects of methicillin. It has been replaced by cloxacillin.
29. Cloxacillin/Dicloxacillin
• It has an isoxazolyl side chain and is highly penicillinase as well as acid
resistant.
• Activity against PnG sensitive organisms is weaker, and it should not be
used as a substitute for PnG.
• It is more active than methicillin against penicillinase producing Staph,
but not against MRSA.
• Cloxacillin/dicloxacillin are incompletely but dependably absorbed from
oral route, especially if taken in empty stomach.
• It is > 90% plasma protein bound. Elimination occurs primarily by kidney,
also partly by liver. Plasma t½ is about 1 hour.
30. EXTENDED SPECTRUM PENICILLINS
• These semisynthetic penicillins are active against a variety of gram-
negative bacilli as well.
• Aminopenicillins This group, led by ampicillin, has an amino substitution
in the side chain. Some are prodrugs and all have quite similar
antibacterial spectra.
• None is resistant to penicillinase or to other β-lactamases.
• Ampicillin It is active against all organisms sensitive to PnG. In addition,
many gram-negative bacilli, e.g. H. influenzae, E. coli, Proteus,
Salmonella Shigella and Helicobacter pylori are inhibited.
• However, due to wide-spread use, many of these have developed
resistance; usefulness of this antibiotic has decreased considerably.
31. • Ampicillin is
• more active than PnG for Strep. viridans, enterococci and Listeria;
• equally active for pneumococci, gonococci and meningococci (penicillin-
resistant strains are resistant to ampicillin as well)
• less active against other gram-positive cocci.
• Penicillinase producing Staph. are not affected, as are other gram-negative
bacilli, such as Pseudomonas, Klebsiella, indole positive Proteus and
anaerobes like Bacteroides fragilis.
32. PHARMACOKINETICS
• Ampicillin is not degraded by gastric acid; oral absorption is incomplete
but adequate.
• Food interferes with absorption.
• It is partly excreted in bile and reabsorbed— enterohepatic circulation
occurs.
• However, primary channel of excretion is kidney, but tubular secretion is
slower than for PnG.
• Plasma t½ is 1 hr.
33. USES
1. Urinary tract infections: Ampicillin has been the drug of choice for
most acute infections, but resistance has increased and
fluoroquinolones/cotrimoxazole are now more commonly used for
empirical therapy.
2. Respiratory tract infections: including bronchitis, sinusitis, otitis
media, etc. are usually treated with ampicillin, but higher doses (50–80
mg/kg/day) are generally required now.
34. 3. Meningitis: Ampicillin has been a first line drug, but a significant
number of meningococci, pneumococci and H. influenzae are now
resistant. For empirical therapy, it is now used only in combination with a
third generation cephalosporin with or without another antibiotic.
4. Gonorrhoea: It is one of the first line drugs for oral treatment of
nonpenicillinase producing gonococcal infections. A single dose of 3.5 g
ampicillin + 1 g probenecid (ROSCIND, DYNACILPRB cap) is adequate and
convenient for urethritis.
35. 5. Typhoid fever: Due to emergence of resistance, it is now
rarely used, only when the organism is shown to be sensitive.
Salmonella diarrhoeas should usually not be treated with
antimicrobials, including ampicillin.
6. Bacillary dysentery: due to Shigella often responds to
ampicillin, but many strains are now resistant; quinolones are
preferred.
36. 7. Cholecystitis: Ampicillin is a good drug because high concentrations
are attained in bile.
8. Subacute bacterial endocarditis: Ampicillin 2 g i.v. 6 hourly is used
in place of PnG. Concurrent gentamicin is advocated.
9. H. pylori: Though amoxicillin is mostly used for eradication of H. pylori
from stomach and duodenum, ampicillin is also active.
37. 10.Septicaemias and mixed infections:
Injected ampicillin may be combined with gentamicin or one of the third
generation cephalosporins.
11.ANUG:
Ampicillin/amoxicillin are generally preferred over penicillin V for
combining with metronidazole in treating this condition.
38. ADVERSE EFFECTS
• Diarrhoea is frequent after oral administration.
• Ampicillin is incompletely absorbed—the unabsorbed drug irritates the
lower intestines as well as causes marked alteration of bacterial flora.
• It produces a high incidence (up to 10%) of rashes, especially in patients
with AIDS, EB virus infections or lymphatic leukaemia.
• Concurrent administration of allopurinol also increases the incidence of
rashes. Sometimes the rashes may not be allergic, but toxic in nature.
• Patients with a history of immediate type of hypersensitivity to PnG
should not be given ampicillin as well.
40. • β-lactamases are a family of enzymes produced by many gram-
positive and gram-negative bacteria that inactivate β-lactam
antibiotics by opening the β-lactam ring.
• Different β-lactamases differ in their substrate affinities.
• Three inhibitors of this enzyme clavulanic acid, sulbactam
and tazobactam are available for clinical use.
41. CLAVULANIC ACID
• Clavulanic acid Obtained from Streptomyces clavuligerus, it has a β-lactam ring but
no antibacterial activity of its own.
• It inhibits a wide variety (class II to class V) of β-lactamases (but not class I
cephalosporinase) produced by both gram-positive and gram-negative bacteria.
• Clavulanic acid is a ‘progressive’ inhibitor: binding with β-lactamase is reversible
initially, but becomes covalent later—inhibition increasing with time.
• Called a ‘suicide’ inhibitor, it gets inactivated after binding to the enzyme.
• It permeates the outer layers of the cell wall of gram-negative bacteria and inhibits the
periplasmically located β-lactamase.
42. USES
• Addition of clavulanic acid re-establishes the activity of amoxicillin
against β-lactamase producing resistant Staph. aureus (but not MRSA
that have altered PBPs), H. influenzae, N. gonorrhoeae, E. coli, Proteus,
Klebsiella, Salmonella and Shigella.
• Though Bact. fragilis and Branhamella catarrhalis are not responsive to
amoxicillin alone, they are inhibited by the combination.
• Clavulanic acid does not potentiate the action of amoxicillin against strains
that are already sensitive to it.
43. Coamoxiclav is indicated for:
• Skin and soft tissue infections, intraabdominal and gynaecological
sepsis, urinary, biliary and respiratory tract infections: especially
when empiric antibiotic therapy is to be given for hospital acquired
infections.
• Gonorrhoea (including PPNG) single dose amoxicillin 3 g +
clavulanic acid 0.5 g + probenecid 1 g is highly curative.
44. ADVERSE EFFECTS
• Same as for amoxicillin alone; but g.i. tolerance is poorer—
especially in children.
• Other adverse effects are Candida stomatitis/vaginitis and
rashes.
• Some cases of hepatic injury have been reported with the
combination.