Tetracyclines slide contains full information about uses, adverse effect, marketed preparation, precaution, route of drug administration, antimicrobial spectrum, mechanism of action, pharmacokineticks and pharmacodynamics of tetracyclines. This slide is very helpful for pharmacy and pharmacology student for the study about tetracyclines.
Anthelmintics | B.Pharm 3rd year 2nd Sem | Medicinal Chemistry-III | History, Classification, Structures & Synthesis of anthelmintics, Synthesis of Diethylcarbamazine citrate, Synthesis of Mebendazole
Broad Spectrum Antibiotic:Tetracycline,four cyclic rings,Physicochemical Properties,Classification-According to source and Based on Duration of action ,Mechanism of action-30S ribosomes ,Inhibit protein synthesis,Antimicrobial spectrum
Resistance
Adverse effects
Precautions,Uses by snehal chakorkar
These are antibiotics having a macrocyclic
lactone ring with attached sugars. Erythromycin
is the first member discovered in the 1950s,
Roxithromycin, Clarithromycin and Azithromycin
are the later additions. Antimicrobial spectrum is narrow,
includes mostly gram-positive and a few gramnegative
bacteria, and overlaps considerably with
that of penicillin G. Erythromycin is highly active
against Str. pyogenes and Str. pneumoniae, N.
gonorrhoeae, Clostridia, C. diphtheriae and
Listeria, but penicillin-resistant Staphylococci
and Streptococci are now resistant to erythromycin
also.
All cocci readily develop resistance
to erythromycin, mostly by acquiring the
capacity to pump it out. Resistant Enterobacteriaceae
have been found to produce an erythromycin
esterase. Alteration in the ribosomal binding
site for erythromycin by a plasmid encoded
methylase enzyme is an important mechanism of
resistance in gram-positive bacteria. All the above
types of resistance are plasmid mediated. Change
in the 50S ribosome by chromosomal mutation
reducing macrolide binding a
Broad spectrum antibiotics chloramphenicol, anaerobic,soil bacteria. Description includes Physicochemical Properties,Mechanism of action-50S ribosome ,Inhibits Bacterial protein synthesis,Resistance,Interactions,Indications of chloramphenicol-Pyogenic meningitis.
Anaerobic infections.
Intraocular infections.
Enteric fever
Drug of choice in some conditions.
Urinary tract infections
Topically In conjunctivitis & external ear Infections. Snehal chakorkar
These are a class of antibiotics having a nucleus of four cyclic rings. The tetracyclines are primarily bacteriostatic; inhibit protein synthesis by binding to 30S ribosomes in susceptible organism.
Subsequent to such binding, attachment
of aminoacyl-t-RNA to the acceptor (A) site of
mRNA-ribosome complex. The carrier involved
in active transport of tetracyclines is absent in
the host cells. Moreover, protein synthesizing
apparatus of host cells is less susceptible to
tetracyclines. These two factors are responsible
for the selective toxicity of tetracyclines for
the microbes.
Aminoglycosides(medicinal chemistry by p.ravisankar)Dr. Ravi Sankar
Aminoglycosides,Aminocyclitols,Source,Structures of streptomycin,Dihydrostreptomycin,A mention of other aminoglycoside antibiotics,Acid hydrolysis,Mechanism of action,SAR,Dihydrostreptomycin and its importance,therapeutic uses, toxicity.
Tetracyclines slide contains full information about uses, adverse effect, marketed preparation, precaution, route of drug administration, antimicrobial spectrum, mechanism of action, pharmacokineticks and pharmacodynamics of tetracyclines. This slide is very helpful for pharmacy and pharmacology student for the study about tetracyclines.
Anthelmintics | B.Pharm 3rd year 2nd Sem | Medicinal Chemistry-III | History, Classification, Structures & Synthesis of anthelmintics, Synthesis of Diethylcarbamazine citrate, Synthesis of Mebendazole
Broad Spectrum Antibiotic:Tetracycline,four cyclic rings,Physicochemical Properties,Classification-According to source and Based on Duration of action ,Mechanism of action-30S ribosomes ,Inhibit protein synthesis,Antimicrobial spectrum
Resistance
Adverse effects
Precautions,Uses by snehal chakorkar
These are antibiotics having a macrocyclic
lactone ring with attached sugars. Erythromycin
is the first member discovered in the 1950s,
Roxithromycin, Clarithromycin and Azithromycin
are the later additions. Antimicrobial spectrum is narrow,
includes mostly gram-positive and a few gramnegative
bacteria, and overlaps considerably with
that of penicillin G. Erythromycin is highly active
against Str. pyogenes and Str. pneumoniae, N.
gonorrhoeae, Clostridia, C. diphtheriae and
Listeria, but penicillin-resistant Staphylococci
and Streptococci are now resistant to erythromycin
also.
All cocci readily develop resistance
to erythromycin, mostly by acquiring the
capacity to pump it out. Resistant Enterobacteriaceae
have been found to produce an erythromycin
esterase. Alteration in the ribosomal binding
site for erythromycin by a plasmid encoded
methylase enzyme is an important mechanism of
resistance in gram-positive bacteria. All the above
types of resistance are plasmid mediated. Change
in the 50S ribosome by chromosomal mutation
reducing macrolide binding a
Broad spectrum antibiotics chloramphenicol, anaerobic,soil bacteria. Description includes Physicochemical Properties,Mechanism of action-50S ribosome ,Inhibits Bacterial protein synthesis,Resistance,Interactions,Indications of chloramphenicol-Pyogenic meningitis.
Anaerobic infections.
Intraocular infections.
Enteric fever
Drug of choice in some conditions.
Urinary tract infections
Topically In conjunctivitis & external ear Infections. Snehal chakorkar
These are a class of antibiotics having a nucleus of four cyclic rings. The tetracyclines are primarily bacteriostatic; inhibit protein synthesis by binding to 30S ribosomes in susceptible organism.
Subsequent to such binding, attachment
of aminoacyl-t-RNA to the acceptor (A) site of
mRNA-ribosome complex. The carrier involved
in active transport of tetracyclines is absent in
the host cells. Moreover, protein synthesizing
apparatus of host cells is less susceptible to
tetracyclines. These two factors are responsible
for the selective toxicity of tetracyclines for
the microbes.
Aminoglycosides(medicinal chemistry by p.ravisankar)Dr. Ravi Sankar
Aminoglycosides,Aminocyclitols,Source,Structures of streptomycin,Dihydrostreptomycin,A mention of other aminoglycoside antibiotics,Acid hydrolysis,Mechanism of action,SAR,Dihydrostreptomycin and its importance,therapeutic uses, toxicity.
Drugs used in protozoal infections with antiprotozoal drugskhangloo1110
This file includes diseases caused by protozoa like amebiasis, Giardiasis, trypanosomiasis, leishmaniasis with drugs acting on the diseases like Emetine, Metronidazole, clioquinol and iodoquinol with their mechanism of action and their pharmacology.
Similar to Antiamoebic and antiprotozoal drugs - drdhriti (20)
A Power point presentation on Betalactam antibiotics suitable for undergraduate medical students. This Ppt is already presented in theory class lectures to the students of NEIGRIHMS, Shillong, Meghalaya
A Powerpoint presentation on drugs excretion and elimination suitable for UG medical students. This ppt is already presented to my students in one of the theory classes.
A PowerPoint presentation on "NSAIDS" suitable for reading by UG and PG Medical/Paramedical students of Pharmacology and Pharmacy sciences. This Ppt. is prepared for academic purpose only and already presented to my students in one of the theory classes of mine.
Report Back from SGO 2024: What’s the Latest in Cervical Cancer?bkling
Are you curious about what’s new in cervical cancer research or unsure what the findings mean? Join Dr. Emily Ko, a gynecologic oncologist at Penn Medicine, to learn about the latest updates from the Society of Gynecologic Oncology (SGO) 2024 Annual Meeting on Women’s Cancer. Dr. Ko will discuss what the research presented at the conference means for you and answer your questions about the new developments.
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.
Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Ve...kevinkariuki227
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
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.
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
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
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
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
Title: Sense of Smell
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 primary categories of smells and the concept of odor blindness.
Explain the structure and location of the olfactory membrane and mucosa, including the types and roles of cells involved in olfaction.
Describe the pathway and mechanisms of olfactory signal transmission from the olfactory receptors to the brain.
Illustrate the biochemical cascade triggered by odorant binding to olfactory receptors, including the role of G-proteins and second messengers in generating an action potential.
Identify different types of olfactory disorders such as anosmia, hyposmia, hyperosmia, and dysosmia, including their potential causes.
Key Topics:
Olfactory Genes:
3% of the human genome accounts for olfactory genes.
400 genes for odorant receptors.
Olfactory Membrane:
Located in the superior part of the nasal cavity.
Medially: Folds downward along the superior septum.
Laterally: Folds over the superior turbinate and upper surface of the middle turbinate.
Total surface area: 5-10 square centimeters.
Olfactory Mucosa:
Olfactory Cells: Bipolar nerve cells derived from the CNS (100 million), with 4-25 olfactory cilia per cell.
Sustentacular Cells: Produce mucus and maintain ionic and molecular environment.
Basal Cells: Replace worn-out olfactory cells with an average lifespan of 1-2 months.
Bowman’s Gland: Secretes mucus.
Stimulation of Olfactory Cells:
Odorant dissolves in mucus and attaches to receptors on olfactory cilia.
Involves a cascade effect through G-proteins and second messengers, leading to depolarization and action potential generation in the olfactory nerve.
Quality of a Good Odorant:
Small (3-20 Carbon atoms), volatile, water-soluble, and lipid-soluble.
Facilitated by odorant-binding proteins in mucus.
Membrane Potential and Action Potential:
Resting membrane potential: -55mV.
Action potential frequency in the olfactory nerve increases with odorant strength.
Adaptation Towards the Sense of Smell:
Rapid adaptation within the first second, with further slow adaptation.
Psychological adaptation greater than receptor adaptation, involving feedback inhibition from the central nervous system.
Primary Sensations of Smell:
Camphoraceous, Musky, Floral, Pepperminty, Ethereal, Pungent, Putrid.
Odor Detection Threshold:
Examples: Hydrogen sulfide (0.0005 ppm), Methyl-mercaptan (0.002 ppm).
Some toxic substances are odorless at lethal concentrations.
Characteristics of Smell:
Odor blindness for single substances due to lack of appropriate receptor protein.
Behavioral and emotional influences of smell.
Transmission of Olfactory Signals:
From olfactory cells to glomeruli in the olfactory bulb, involving lateral inhibition.
Primitive, less old, and new olfactory systems with different path
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2. Section – 1
Antiamoebic Drugs
Drugs useful in infection caused by the protozoa Entamoeba
histolytica (E. histolytica)
3. Amoebiasis - Epidemiology
• Poor environmental sanitation, low socio-economic status
• Approximately 48 million individuals suffer from amoebiasis
throughout the world
• Endemic in most parts of India
• At least 40 thousand deaths are attributable to amoebiasis
• Ranks third among parasitic causes of deaths, behind only malaria
and schistosomiasis
4. E. Histolytica –
Pathogenesis
• It is a water-borne pathogen transmitted by the fecal-oral route
• Exists in 2 (two) forms:
1. Cyst or the dormant form – can survive outside the body
2. Trophozoite or the dividing form - Non-infective and do not persists outside the body
but invasive
• Two stages of development:
Ingested cyst reaches colon transforms to trophozoites
May live as
commensals
Form cysts that pass
on to stool
1. Form amoebic ulcers (acute dysentery) -
galactose/N- acetyl-galactosamine
(Gal/GalNAc) lectin
2. Chronic amoebic dysentery (vague
symptoms, amoeboma)
5. Pathogenesis of E. Histolytica – contd.
• Trophozoites can also enter the
blood stream and travel to other
parts— commonly the liver, but
sometimes the lungs or brain and
can cause Amoebic liver abscesses
• Remember - In tissues, only
trophozoites are present
6. Available Drugs
1. Tissue amoebicides:
a) Intestinal and extra-intestinal: Nitroimidazoles – Metronidazole, Tinidazole,
Secnidazole, Ornidazole, Satranidazole and Alkaloides – Emetine and
Dihydroemetine
b) Extra-intestinal Only - Chloroquine
2. Luminal amoebicides: Amides – Diloxonide furoate,
Nitazoxamide; 8-Hydroxyquinolines – Quinodochlor,
Diiodohydroxyquin; Antibiotics - Tetracycline
7. Metronidazole –
Prototype
• Originally discovered and used for Trichomoniasis in 1959
• Broad spectrum cidal activity against --- Protozoa – E.
histolytica, T. vaginalis, G. lamblia
• Anaerobic bacteria – B.fragilis, C.perfringes,
Fusobacterium, H.pylori, Cl. Difficile, Campylobacter,
Anaerobic streptococci
• Helminths – Dracunculus medinensis
• Resistance – no significant resistance for E. histolytica till
now, but developed for T. vaginalis
G. lamblia T. vaginalis
8. Metronidazole –
MOA
• Selective Toxicity to anerobic microorganisms
• A system unique to anaerobics - Pyruvate:ferredoxin oxidoreductase pathway
(PFOR) normally generates ATP via oxidative decarboxylation of pyruvate
• Metronidazole: Entry into the microorganism by diffusion (LMW) ---- Reduced to
nitro radical by certain redox proteins in the mitochondria to highly reactive nitro
group --- nitro radicals act as an electron sink --- competes with Biological
acceptor sites of anaerobic organisms for the electrons generated by PFOR
pathway of pyruvate reduction
– Reduction of metronidazole creates a concentration gradient that drives
uptake of more drug, and promotes formation of intermediate compounds and
free radicals
– Cytotoxic intermediate particles interact with host cell DNA, resulting in DNA
strand breakage and fatal destabilization of the DNA helix
• Aerobic environment ??
9. Metronidazole – contd.
• Pharmacokinetics:
Well absorbed from the small intestine
Widely distributed in the body secretions – vaginal secretions, semen, saliva
and CSF
Metabolized in liver by oxidation and glucoronidation
Half life – 8 Hrs
• ADRs:
Most common - Nausea, Vomiting, abdominal cramps and metallic taste
Less frequent – headache, glossitis, rashes and dryness of mouth
Prolonged administration – Peripheral neuropathy and CNS effects
Seizures at high dose
10. Metronidazole
– contd.
• Contraindications:
– First trimester of pregnancy
– Neurological diseases and Blood dyscrasias
– Chronic alcoholism
• Interactions:
– Disulfiram-like intolerance: Symptoms: flushing, burning sensation,
throbbing headache, perspiration, dizziness, vomiting, visual
disturbance, mental confusion, fainting and circulatory collapse
– MOA: Disulfiram irreversibly inhibits the oxidation of acetaldehyde by
competing with the cofactor nicotinamide adenine dinucleotide (NAD)
for binding sites on ALDH
– Enzyme inducers like Phenobarbitone and Rifampicin (reduced
therapeutic effect)
11. Metronidazole - uses
1. Ameobiasis – 1st
line of drug - Kills E. histolytic trophozoites but less cysts.
Treatment of all tissue infections with E histolytica – diff doses – mild
intestinal, invasive dysentery and liver abscess
• Less effects against luminal parasites and so must be used with a luminal
amoebicide – for eradication - dosage
1. Giardiasis
2. Trichomonas vaginitis – DOC - additional intravaginal treatment and both
partners !!
3. Anaerobic bacterial infections
4. Pseudo-membranous enterocolitis: Cl difficile
5. Ulcerative gingivitis, trench mouth – DOC – ulcerative gingivitis
6. Helicobacter pylori
12. Other Nitroimidazoles
• Tinidazole, Secnidazole, Ornidazole, Satranidazole
• Tinidazole:
– Slower metabolism, duration of action longer (t1/2 12 hrs) – single dose
– Higher cure rates (!)
– Better tolerated – lesser incidence of side effects
• Secnidazole: Rapid absorption, but slower metabolism – half life 17-29 hrs
• Ornidazole: 12 -24
• Satranidazole: 14 hrs half life – better tolerated plus no nausea, vomiting and
metallic taste - no disulfiram like reaction and neurological symptoms
13. Emetine and Dehydroemetine
• Emetine, alkaloid derived from Cephaelis ipecacuanha and dehydroemetine, a
synthetic analog – kills trophozoites of E histolytica
• MOA: Inhibiting intra-ribosomal translocation of tRNA-amino acid complex →
inhibition of protein synthesis
• Action: Effects on trophozoites but not on cysts. Potent and rapid action –
symptomatic relief in 1-3 days, but not curative - asymptomatic cyst passing
• Administered SC (preferred) or i.m. (but never i.v. or oral) because oral
preparations are absorbed erratically and vomiting – very slow excretion in urine1
-2 months
• Uses: Seldom used. Reserve drug for severe intestinal and extraintestinal
amoebiasis or for patients not responding to metronidazole. Luminal amoebicide
needed to be added
14. Emetine - ADRs
• Local stimulation: pain and tenderness in the area of injection
• Gastrointestinal tract discomfort: nausea, vomiting– CTZ (oral and
IV)
• Diarrhoea and abdominal cramps
• Neuromuscular blockade: muscle weakness and discomfort
• Cardiac toxicity: arrhythmias, congestive heart failure,
hypotension, ECG changes – bed rest
• Contraindication: Not be used in patients with cardiac or renal
disease, in young children, or in pregnancy
15. Chloroquine
Kills trophozoites of E. histolytica
Concentrates in liver – used in hepatic amoebiasis
Completely absorbed from upper intestine – not effective
in invasive or luminal dysentery
Efficacy in amoebic liver is equal to emetine, but longer
treatment and relapse
Used after a course of Metronidazole – but a luminal
amoebicide must be added
Dose - 600mg stat and next day & 300 mg for 2-3 days
16. Diloxanide furoate (DF)
Highly effective luminal amoebicide
Kills trophozoites responsible for production of cyst – however no
antibacterial action
MOA: Oral DF F hydrolyzed (exerts effects) and D is freed
90% D is absorbed remaining 10% reaches Large intestine and
exerts effects (weaker than F)
Absorbed D – low serum level – no therapeutic effects
Uses: Mild tissue amoebiasis/asymptomatic cyst passers, Tissue
amoebiasis and liver abscess with Metronidazole – no antibacterial
action
ADRs: Well tolerated, only flatulence, nausea, itching and rarely
urticaria
17. Nitazoxanide
• Newer Drug for Giardiasis
• Also effective in E. Histolytica, T. Vaginalis, H. Pylori etc.
• Converted to Tizoxanide after absorption
• MOA: Inhibition of PFOR
• Uses: Giardiasis, aboebiasis as luminal amebicide
• Dose: 500 mg BD for 3 days
18. 8-Hydroxyquinolines
Drugs – Iodoquinol, Clioquinol, Quinodochlor and Iodochlorohydroxyquin
Act against Entamoeba, Giardia, Trichomanas, some fungi and Bacteria
Luminal amoebicidal but no tissue action – not effective in acute dysentery but in
chronic intestinal amebiasis (but lesser than DF)
Absorbed very less amount (10-30%) - therapeutic conc. Is not attained
conjugated and excreted in urine
Once a popular drug – but less now because of ADRs
ADRs – well tolerated – only nausea, green stools pruritus etc. plus Iodism
But Subacute myelo-optic neuropathy (SMON) - the inflammation of the optic
nerve causing a complete or partial loss of vision and also peripheral neuropathy
Uses: Alternative to DF in amoebiasis, Giardia, local treatment of vaginal
Trichomonas and fungal and bacterial infections. 250 to 500 mg tds
19. Choices of Drugs
Asymptomatic cysts carriers Diloxanide furoate or
Metronidazole/Tinidazole or Iodoquinol -
Repeated course
Diarrhoea / Dysentery Metronidazole/Tinidazole or Emetine -
Metronidazole + Diloxanide
Amebic liver abscess Chloroquine - Metronidazole + DF (or
Dehydroemetine)
Giardiasis (Giardia labmlia) Metronidazole or Nitazoxamide or
Quinodochlor or Furazolidone
20. Trichomonas vaginitis treatment
• Metronidazole – 400 mg tds for 7 days or 2 gm single dose,
or
• Tinidazole 600 mg BD for 7 days or 2 gm single dose
• Repeat after 6 weeks
• Additional intravaginal treatment for refractory cases
• Resistance have been reported
• Both partners should be treated
• Local application drugs: Quinodochlor, Clotrimazole,
Natamycin, Povidone Iodine etc.
21. •Section – 2
•Drugs for Leishmaniasis
• Visceral leishmaniasis or kala-azar caused by Leishmania donovani
• Transmitted by bite of female sand fly of genus phlebotomus
• Amastigote and Promastigote
22. Available Drugs
• Antimonial – Sodium stibogluconate (SSG)
• Antifungal – Amphotericin B (AMB), Ketoconazole (KTZ)
• Others – Miltefosine, Mifepristone, Paromomycin and Allopurinol
23. Sodium stibogluconate (SSG)
• The drug of choice in Leishmaniasis – some resistance
• Water soluble pentavalent antimonial compound – 1/3rd
antimony by weight
• MOA: Not clear
-SH dependent enzymes are inhibited – bioenergetics of the parasite
Enzyme in leishmania converts SSG to trivalent compound – causes efflux of glutathione
and thiols – oxidative damage
Not metabolized – excreted unchanged in urine after IM injection
Dose: 20-30 mg/kg deep IM daily in buttock for 20-30 days or more – depends on
response – also IV
Response in Bone marrow and splenic aspirates
Should be give on alternate days in poor health patients
24. SSG - ADRs
• All antimonials are toxic
• Pentavalent compounds are less toxic and better tolerated
• Nausea, vomiting, metallic taste, cough and pain abdomen
• Stiffness and abscess in injected muscles
• Pancreatitis, liver and kidney damage etc.
• Rarely shock and death
25. Amphotericin B (AMB)
• Antifungal effective against Leishmania
• 2 forms – Liposomal AMB and AMB Deoxycholate
• MOA: Ergosterol (Ion channel)
• 99% cure rate
• ADR: Nephrotoxicity
• 1st
line of drug by WHO – but costly
26. Miltefosine – Latest Drug
Alkyl phosphocholine derivative
1st
orally effective anti-leishmaniasis drug
1st
line agent now by NVBDCP – only available
MOA: Not clear –
interferes with lipid metabolism – or,
Prevents synthesis of cell surface molecules - or,
alter signal transduction
Used as combination therapy with L- AMB or Paramomycin
Kinetics: Absorbed orally – Distributed widely - Biphasic elimination
7 days early half-life and total half-live 4 weeks
ADRs: Hepatotoxicity, skin allergy and nephrotoxicity – also teratogenic (3 months)