MALARIA
It is an infectious disease of humans caused by parasitis protozoans belonging to the genus plasmodium.
It is endemic in most parts of India and other tropical countries.
As per WHO, malaria causes one death every minute globally and about 40,000 annual deaths in India.
The disease is transmitted by the bite of an infected female Anopheles mosquito.
Four species of protozoa plasmodium can cause malaria which are P. falciparum, P. vivax, P. ovale and P. malariae.
INTRODUCTION
These are the drugs which are used for the treatment, prophylaxis and prevention of relapses of malaria.
The treatment of malaria is available since 17 century. During those times, the bark of Cinchona tree was used in the crude form.
Later in 1820, quinine was isolated from the bark.
Since 1920, quinine and other drugs are commercially available in the market
OBJECTIVES IN USE OF ANTIMALARIAL DRUGS
The various objectives are:
To prevent clinical attack of malaria.
To treat clinical attack of malaria.
To completely eradicate the parasite from the patient’s body.
To cut down human to mosquito transmission.
THERAPEUTIC CLASSIFICATION
1. CAUSAL PROPHYLACTICS: (Destroy parasite in liver cells and prevent invasion of erythrocytes)
e.g. primaquine, pyrimethamine
2.BLOOD SCHIZONTOCIDES SUPPRESIVES (destroy parasites in the RBC and terminate clinical attacks of malaria): e.g. chloroquine, quinine, mefloquine, halofantrine, pyrimethamine
3. TISSUE SCHIZONTOCIDES used to prevent relapse: act vivax and P. ovale that produce replapses. E.g. primaquine
4. GAMETOCIDAL DRUGS: primaquine, chloroquine, quinine.
1. CHLOROQUINE
It acts as erythrocytic schizontocide against all species of plasmodia.
The parasite disappears from peripheral blood in 1-3 days. It control the clinical attacks of malaria within 1-2 days.
It doesn’t have any gametocidal activity.
It is bitter in taste, so patient should be advised ‘not to chew the tablet’ it is used for the treatment of malaria during pregnancy: no teratogenic effects have been reported.
MECHANISM OF ACTION
Its gets concentrated in the infected RBCs and then is actively taken up by the susceptible plasmodia.
The chloroquine binds to the heme and forms chloroquine heme complex.
Complex inhibits the formation of hemozoin and also damages the Plasmodium memberane
PHARMACOKINETICS
It is well absorbed orally.
50% of the drug is plasma protein bound, gets concentrated in liver, spleen, kidneys, lungs, skin and leukocytes.
The plasma half life is 3-10 days, whereas the terminal half life is 1-2 months. On prolonged use, it gets accumulated selectively in the retina and causes ocular toxicity.
It is partially metabolized in liver and slowly excreted in urine.
INDICATIONS ADVERSE EFFECTS
Clinical drug of choice for malaria.
Extraintestinal amoebiasis.
Rheumatoid arthritis
Infectious mononucleosis.
Mil
synthetic antimicrobials having a quinolone structure that are active primarily against gram-negative bacteria, though newer fluorinated compounds also inhibit gram-positive ones.
MALARIA
It is an infectious disease of humans caused by parasitis protozoans belonging to the genus plasmodium.
It is endemic in most parts of India and other tropical countries.
As per WHO, malaria causes one death every minute globally and about 40,000 annual deaths in India.
The disease is transmitted by the bite of an infected female Anopheles mosquito.
Four species of protozoa plasmodium can cause malaria which are P. falciparum, P. vivax, P. ovale and P. malariae.
INTRODUCTION
These are the drugs which are used for the treatment, prophylaxis and prevention of relapses of malaria.
The treatment of malaria is available since 17 century. During those times, the bark of Cinchona tree was used in the crude form.
Later in 1820, quinine was isolated from the bark.
Since 1920, quinine and other drugs are commercially available in the market
OBJECTIVES IN USE OF ANTIMALARIAL DRUGS
The various objectives are:
To prevent clinical attack of malaria.
To treat clinical attack of malaria.
To completely eradicate the parasite from the patient’s body.
To cut down human to mosquito transmission.
THERAPEUTIC CLASSIFICATION
1. CAUSAL PROPHYLACTICS: (Destroy parasite in liver cells and prevent invasion of erythrocytes)
e.g. primaquine, pyrimethamine
2.BLOOD SCHIZONTOCIDES SUPPRESIVES (destroy parasites in the RBC and terminate clinical attacks of malaria): e.g. chloroquine, quinine, mefloquine, halofantrine, pyrimethamine
3. TISSUE SCHIZONTOCIDES used to prevent relapse: act vivax and P. ovale that produce replapses. E.g. primaquine
4. GAMETOCIDAL DRUGS: primaquine, chloroquine, quinine.
1. CHLOROQUINE
It acts as erythrocytic schizontocide against all species of plasmodia.
The parasite disappears from peripheral blood in 1-3 days. It control the clinical attacks of malaria within 1-2 days.
It doesn’t have any gametocidal activity.
It is bitter in taste, so patient should be advised ‘not to chew the tablet’ it is used for the treatment of malaria during pregnancy: no teratogenic effects have been reported.
MECHANISM OF ACTION
Its gets concentrated in the infected RBCs and then is actively taken up by the susceptible plasmodia.
The chloroquine binds to the heme and forms chloroquine heme complex.
Complex inhibits the formation of hemozoin and also damages the Plasmodium memberane
PHARMACOKINETICS
It is well absorbed orally.
50% of the drug is plasma protein bound, gets concentrated in liver, spleen, kidneys, lungs, skin and leukocytes.
The plasma half life is 3-10 days, whereas the terminal half life is 1-2 months. On prolonged use, it gets accumulated selectively in the retina and causes ocular toxicity.
It is partially metabolized in liver and slowly excreted in urine.
INDICATIONS ADVERSE EFFECTS
Clinical drug of choice for malaria.
Extraintestinal amoebiasis.
Rheumatoid arthritis
Infectious mononucleosis.
Mil
synthetic antimicrobials having a quinolone structure that are active primarily against gram-negative bacteria, though newer fluorinated compounds also inhibit gram-positive ones.
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.
Quinolones are synthetic antimicrobials having a quinolone
structure.
Active against gram-ve bacteria, newer fluorinated compounds also inhibit gram +ve bacteria.
First member was nalidixic acid introduced in 1960’s
Their usefulness is limited to urinary and GI tract infections because of
Low potency
Modest blood and tissue levels
Limited spectrum
High frequency of bacterial resistance
In gram negative bacteria –
Inhibition of DNA gyrase enzyme (Inhibit negative super coiling)
In gram positive bacteria –
Inhibition of Topoisomerase IV – Inhibition of nicking and separation of daughter DNA strands after DNA replication
The malformed DNA is digested by Exoneucleases
Urinary Antiseptics, Drugs used in STDs and UTIANUSHA SHAJI
The current presentation includes the pharmacology of urinary antiseptics, Drugs used in STDs and UTI.
Reference: Essentials of Medical Pharmacology, K D Tripathi, Seventh Edition
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.
Quinolones are synthetic antimicrobials having a quinolone
structure.
Active against gram-ve bacteria, newer fluorinated compounds also inhibit gram +ve bacteria.
First member was nalidixic acid introduced in 1960’s
Their usefulness is limited to urinary and GI tract infections because of
Low potency
Modest blood and tissue levels
Limited spectrum
High frequency of bacterial resistance
In gram negative bacteria –
Inhibition of DNA gyrase enzyme (Inhibit negative super coiling)
In gram positive bacteria –
Inhibition of Topoisomerase IV – Inhibition of nicking and separation of daughter DNA strands after DNA replication
The malformed DNA is digested by Exoneucleases
Urinary Antiseptics, Drugs used in STDs and UTIANUSHA SHAJI
The current presentation includes the pharmacology of urinary antiseptics, Drugs used in STDs and UTI.
Reference: Essentials of Medical Pharmacology, K D Tripathi, Seventh Edition
Sulphonamides, MOA, SAR, History of development, Nomenclature of the Sulfonamides, Classification, Spectrum of Action of the Sulfonamides,Structure Activity Relationship, Reducing Toxicity, Cotrimoxazole
nalidixic acid, the quinolones, the naphthyridines & the cinnolines, Classification, ISOSTERIC REPLACEMENT
DNA gyrase (Topo II) SAR- substitution variation, Ciprofloxacin
Penicillin Classification, Mechanism of Action, Structure Activity Relationship, Structure of Penicillins, penicillin-binding proteins (PBPs) functional propertiesCross-linking of the peptidoglycan by transpeptidases, Cross-linking of the peptidoglycan by transpeptidases, Shape of penicillin G Penicillin SAR AcylSide Chain Modifications Instability of β-lactams to nucleophiles
Penicillinase-Resistant Penicillins Protein Binding of Penicillins
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
www.agostodourado.com
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.
- Video recording of this lecture in English language: https://youtu.be/lK81BzxMqdo
- Video recording of this lecture in Arabic language: https://youtu.be/Ve4P0COk9OI
- Link to download the book free: https://nephrotube.blogspot.com/p/nephrotube-nephrology-books.html
- Link to NephroTube website: www.NephroTube.com
- Link to NephroTube social media accounts: https://nephrotube.blogspot.com/p/join-nephrotube-on-social-media.html
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
- Video recording of this lecture in English language: https://youtu.be/kqbnxVAZs-0
- Video recording of this lecture in Arabic language: https://youtu.be/SINlygW1Mpc
- Link to download the book free: https://nephrotube.blogspot.com/p/nephrotube-nephrology-books.html
- Link to NephroTube website: www.NephroTube.com
- Link to NephroTube social media accounts: https://nephrotube.blogspot.com/p/join-nephrotube-on-social-media.html
Basavarajeeyam is a Sreshta Sangraha grantha (Compiled book ), written by Neelkanta kotturu Basavaraja Virachita. It contains 25 Prakaranas, First 24 Chapters related to Rogas& 25th to Rasadravyas.
Muktapishti is a traditional Ayurvedic preparation made from Shoditha Mukta (Purified Pearl), is believed to help regulate thyroid function and reduce symptoms of hyperthyroidism due to its cooling and balancing properties. Clinical evidence on its efficacy remains limited, necessitating further research to validate its therapeutic benefits.
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!
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
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1. ANTIAMEBIC
AGENTS
DR. SHILPA SUDHAKAR HARAK
ASST. PROF., PHARM. CHEM.,
GES SIR DR. M. S. GOSAVI COLLEGE OF PHARMACEUTICAL
EDUCATION AND RESEARCH, NASHIK
2. PARASITIC INFECTIONS
• Affect huge numbers of individuals > 1 billion
• Found in developing nations
• Cost of health care is the dominant factor
• Sometimes can exceed 80% of the population
• Reduced incentive for both the study of the diseases and the development of effective
therapy
• High cost of drug discovery and Lower incidence in affluentWestern countries
• Parasitic infections -
• Protozoal - amebiasis, giardiasis, babesiosis, Chagas disease, leishmaniasis, malaria, sleeping
sickness, toxoplasmosis, trichomoniasis, and pneumocystosis.
• Others - include Helminth infections (worms), scabies, lice (pediculosis), chiggers, and
bedbugs (Cimicidae family), are also considered to be parasitic infections.
3. PROTOZOAL DISEASES
AMEBIASIS
Disease of the large intestine
• caused by Entamoeba histolytica
• The disease occurs mainly in the tropics, but it is also seen in temperate
climates.
Symptoms –
• can be without significant symptoms or
• can lead to severe, life-threatening dysentery.
The organism exists in one of two forms:
• the motile trophozoite form or
• the dormant cyst form.
4. AMOEBA
Trophozoite Form
• found in the intestine or in the wall of the colon
• Expelled from the body with the feces
Cyst Form
• Encased by a chitinous wall that protects the organism from the
environment
• the organism can be transmitted through contaminated water
and foods.
• Responsible for transmission of the disease.
5. AMOEBA
Host
• rendered susceptible to infection by preexisting
conditions viz. Protein malnutrition, Pregnancy, HIV
infection, High-carbohydrate intake.
8. ENTAMOEBA HISTOLYTICA
Invasion of Host
Intestinal form a. Disintegration of cyst wall in small intestine
b. Movement of trophozoites into the colon
c.Adhesion of trophozoite to cells of the host, which
involves a change in composition and production of
mucus
Extraintestinal
form
d. Penetration of intestinal lining and entrance into portal
circulation
e. Invasion of liver tissue
10. ANTIAMOEBIC DRUGS
• These are drugs useful in infection caused by the protozoa
Entamoeba histolytica.
A.Tissue amoebicides
• a) For both intestinal and extraintestinal amoebiasis:
I. Nitroimidazoles: Metronidazole,Tinidazole, Secnidazole,
Ornidazole, Satranidazole
II.Alkaloids: Emetine, Dehydroemetine
• b) For extra intestinal amoebiasis only: Chloroquine
11. ANTIAMOEBIC DRUGS
B. Luminal amoebicides
• a) Amide : Diloxanide furoate, Nitazoxanide
• b) 8-Hydroxyquinolines: Quiniodochlor
(Iodochlorohydroxyquin, Clioquinol),
Diiodohydroxyquin (Iodoquinol)
• (c) Antibiotics:Tetracyclines
13. METRONIDAZOLE
• Flagyl, Metryl, Satric, Dependal, Metrogyl
• Initially introduced for the treatment of vaginal infections
caused by Trichomonas vaginalis
• But is effective against amebiasis, giardiasis, and anaerobic
bacterial infections (Clostridium difficile).
18. METABOLISM
• Liver metabolism
• to two major
metabolites:
• hydroxylation of the 2-
CH3 to 2-CH2OH
metronidazole (HM)
• its oxidation 2-CH2OH
to 2-CH2COOH
(metronidazole acetic
acid)
19. PHARMACOKINETICS
• Dosage forms - IV, oral, rectal, vaginal suppositories.
• Bioavailability ~100% orally but
• 67% to 82% rectal route
• 19% to 56% vaginal route
• Not bound to plasma protein
• Distribution - uniform throughout the body, including
mother’s milk.
20. THERAPEUTIC APPLICATION
• Drug of choice for Protozoal infections:
• Amebiasis (intestinal and extraintestinal),
• Giardiasis, and
• Trichomoniasis
• gram-positive bacilli Clostridium difficile
21. THERAPEUTIC APPLICATION
Combinations
• Helicobacter pylori infections
common side effects
• abdominal distress,
• a metallic taste
• disulfiram-like effect if taken with alcohol
• Reported to be carcinogenic in mice (acetamide metabolite)
• Restrained use during the first trimester of pregnancy
22. TINIDAZOLE
• Treatment of amebiasis, giardiasis, and trichomoniasis.
• Highly effective against Helicobacter pylori infections
(unapproved)
• Rapidly and completely orally
• Administered with food to reduce GI disturbance
23. TINIDAZOLE
Mechanism of action
• parallels to metronidazole
• Similar metabolic pathway
• Mimic the actions of metronidazole,
• Effective against some metronidazole resistant
protozoa
26. NITAZOXANIDE
• NTZ – orphan drug for the treatment of diarrhea in children
(age 1 to 11 years) in giardiasis & also in cryptosporidiosis in
patients with AIDS.
• Cryptosporidiosis is a protozoal infection caused by
Cryptosporidium parvum in HIV infections.
27. NTZ MOA
• Prodrug metabolised to the deacetylated drug tizoxanide (TIZ)
• TIZ then undergoes a four-electron reduction of the 5-nitro group giving
various short-lived intermediates, which can include the hydroxylamine
derivative.
• These reduced products represent the active forms of NTZ.
• NTZ has the same mechanism of action as metronidazole, this does not
appear to be the case.
• NTZ is thought to inhibit the enzyme pyruvate: ferredoxin oxidoreductase
in Trichomonas vaginalis, Entamoeba histolytica, and Clostridium perfringens.
• The result of this inhibition is disruption of the bioenergetics of these
organisms.
28. NTZ MOA
• Unlike metronidazole and tinidazole, which fragment DNA and
are suspected mutagenic agents, NTZ and TIZ do not cause
DNA fragmentation and are not considered to be mutagenic.
• This might be associated with the higher redox potential found
for NTZ, a nitrothiazole, in comparison with very low redox
potential found for the nitroimidazoles, such as metronidazole
and tinidazole.
• Additional metabolites of TIZ include the glucuronide, which
shows some biologic activity, and small amounts of an aromatic
hydroxylation product.
29. DILOXANIDE
• Furamide, or eutamide, is the 2-furoate ester of 2,2-dichloro-4-
hydroxy-N-methylacetanilide
• Result of discovery that various a,a-dichloroacetamides
possessed amebicidal activity in vitro.
• Hydrolysis of the amide is required for the amebicidal effect.
• Nonpolar esters of diloxanide are more potent than polar ones.
• Diloxanide furoate has been used in the treatment of
asymptomatic carriers of E. histolytica.
30. DILOXANIDE
• Treatment of asymptomatic amebiasis
• Its effectiveness against acute intestinal amebiasis or hepatic
abscesses, however, has not been established.
• It is ineffective as a single agent for the extraintestinal form
of the disease.
• Administered orally and is hydrolyzed in the gut to give
diloxanide (active drug)
• Diloxanide is the only form identified in the bloodstream.
• The drug is found in the urine as the glucuronide
32. QUINOPHENOL/ OXINE
• Also known as oxyquinoline
• It is the parent compound of antiprotozoal oxyquinolines
• The antibacterial and antifungal properties of oxine and its derivatives,
which are believed to result from the ability to chelate metal ions, are well
known.
• Aqueous solutions of acid salts of oxine, particularly the sulfate (Chinosol,
Quinosol), in concentrations of 1:3,000 to 1:1,000, have been used as
topical antiseptics.
• The substitution of an iodine atom at the 7-position of 8-
hydroxyquinolines yields compounds with broad-spectrum amebicidal
properties.
33. IODOQUINOL
• 5,7-Diiodo-8-quinolinol, 5,7-diiodo-8-hydroxyquinoline, or
diiodohydroxyquin (Yodoxin, Diodoquin, Diquinol)
• Recommended for acute and chronic intestinal amebiasis
• It is ineffective in extraintestinal disease
• High incidence of optic neuropathy has occurred with its use,
iodoquinol should not be used routinely for traveler’s diarrhea.
34. EMETINE AND DEHYDROEMETINE
• Obtained from extracts of ipecac
• They are levorotatory
• Exert a direct amebicidal action on
various forms of E. histolytica.
• They are protoplasmic poisons that
inhibit protein synthesis in protozoal
and mammalian cells by preventing
protein elongation.
• Their effect in intestinal amebiasis is
solely symptomatic
• Cure rate is only 10% to 15%, hence
used only in combination
Stereochemical variation
35. EMETINE AND DEHYDROEMETINE
• The high concentrations in liver and other tissues after i.m. have high
effectiveness against hepatic abscesses and other extraintestinal
forms of the disease.
• Toxic effects limit the usefulness of emetine.
• high frequency of GI distress (especially nausea and diarrhea),
• cardiovascular effects (hypotension and arrhythmias), and
• neuromuscular effects (pain and weakness).
• A lower incidence of cardiotoxicity has been associated with the use
of dehydroemetine (Mebadin), which is available from the CDC and
is also amebicidal.
36. PENTAMIDINE ISETHIONATE
• 4,4'-(Pentamethylenedioxy) dibenzamidine diisethionate (NebuPent, Pentam 300)
• It is a water-soluble crystalline salt that is stable to light and air.
• The principal use of pentamidine is for the treatment of pneumonia caused by the
opportunistic pathogenic protozoan P. carinii, a frequent secondary invader associated
with AIDS.
• The drug may be administered by slow intravenous infusion or by deep intra- muscular
injection for PCP.
• An aerosol form of pentamidine is used by inhalation for the prevention of PCP in high-
risk patients infected with HIV who have a previous history of PCP infection or a low
peripheral CD4+ lymphocyte count.
37. PENTAMIDINE ISETHIONATE
• Both the inhalant (aerosol) and parenteral dosage forms of pentamidine
isethionate
• Adverse reactions : cough & bronchospasm (inhalation) &
hypertension & hypoglycemia (injection).
• Used for the prophylaxis and treatment of African trypanosomiasis.
• It also has some value for treating visceral leishmaniasis.
• It rapidly disappears from the plasma after IV injection & is distributed
to the tissues, where it is stored for a long period.
• Hence can be used as a prophylactic agent.
38. ATOVAQUONE
• 3-[4-(4-Chlorophenyl)-cyclohexyl]-2-hydroxy-1,4-naphthoquinone (Mepron)
• It is a highly lipophilic, water-insoluble analog of ubiquinone , an essential component of the
mitochondrial electron transport chain in microorganisms.
• The structural similarity between atovaquone and ubiquinone suggests that the former may act as an
antimetabolite for the latter and thereby interfere with the function of electron transport enzymes.
• Atovaquone was originally developed as an antimalarial drug, but Plasmodium falciparum was found
to develop a rapid tolerance to its action.
• More recently, the effectiveness of atovaquone against P. carinii was discovered.
• Alternative to trimethoprim- sulfamethoxazole (TMP-SMX) for the treatment and prophylaxis of PCP
in patients intolerant to this combination.
• Atovaquone was also shown to be effective in eradicating T. gondii in preclinical animal studies.
39. EFLORNITHINE
• Treatment of West African sleeping sickness, caused by Trypanosoma
brucei gambiense.
• Specifically indicated for the meningoencephalitic stage of the disease.
• Is myelosuppressive drug that causes high incidences of anemia,
leukopenia, and thrombocytopenia.
• Complete blood cell counts must be monitored during the course of
therapy.
• Causes irreversible inactivation of ornithine decarboxylase
• It causes decarboxylation & release of fluoride ion from the inhibitor
• It is enzyme- catalyzed activation of the inhibitor
40. EFLORNITHINE
• Only the (-) isomer, stereochemically related to L-ornithine, is
active.
• Eflornithine is supplied as the hydrochloride salt.
• It may be administered either intravenously or orally.
• Approximately 80% of the unchanged drug is excreted in the
urine.
• Penetration of eflornithine into the CSF is facilitated by
inflammation of the meninges.