Mebendazole, albendazole, and pyrantel pamoate are commonly used anthelmintic drugs. Mebendazole and albendazole are benzimidazole compounds that are poorly absorbed but have broad spectrum activity against intestinal nematodes. Pyrantel pamoate acts by stimulating acetylcholine release and inhibiting cholinesterase in helminths, causing paralysis. Diethylcarbamazine is effective against filarial nematodes and works by damaging the microfilariae membranes. Common side effects of these drugs include gastrointestinal issues.
Introduction
Classification of Helminthiasis
Classification of Anthelmintics Drugs
Mebendazole
Albendazole
Pyrentel pamoate
Peperazine
Levamisole
Praziquantel
Niclosamide
Ivermectin
Diethylcarbamazine
Helminthiasis, also known as worm infection, is any macroparasitic disease of humans and other animals in which a part of the body is infected with parasitic worms, known as helminths. There are numerous species of these parasites, which are broadly classified into tapeworms, flukes, and roundworms.
The helminths worms are macroscopic, multicellular organisms having their own digestive, excretory, reproductive and nervous system. The helminths could be nemathelminths (round bodied worms) or platyhelminths (flat bodied worms).
Nematodes (round worms) are long, round bodied segmented worms that are tapered at both ends . In festation occurs if the embryonated eggs or tissues of infested host contain larva of the nematode.
Protozoal infections and antiprotozoal drugs(therapy).Gagandeep Jaiswal
presentation comprising knowledge about various protozoal infections and therapy options available for the treatment of those infections. various different drugs used in the therapy with their proposed mechanism of action. Hope it will be useful for understanding the pharmacology of antiprotozoals.
Prokinetics are the type of drugs which enhances gastrointestinal motility/transit by
increasing the frequency or strength of contractions.
They speed up gastric emptying by enhancing coordinated propulsive motility.
Treat Gastrointestinal symptoms : Abdominal discomfort, Bloating, constipation,
Heart burn, nausea and vomiting. And few gastrointestinal disorders : irritable bowel
Syndrome, gastritis, gastroparesis and functional dyspepsia.
Increases gastric emptying
Relief of gastric stasis
Decreases reflux esophagitis/heart burn
Decreases regurgitation of gastric contents& emesis
Introduction
Classification of Helminthiasis
Classification of Anthelmintics Drugs
Mebendazole
Albendazole
Pyrentel pamoate
Peperazine
Levamisole
Praziquantel
Niclosamide
Ivermectin
Diethylcarbamazine
Helminthiasis, also known as worm infection, is any macroparasitic disease of humans and other animals in which a part of the body is infected with parasitic worms, known as helminths. There are numerous species of these parasites, which are broadly classified into tapeworms, flukes, and roundworms.
The helminths worms are macroscopic, multicellular organisms having their own digestive, excretory, reproductive and nervous system. The helminths could be nemathelminths (round bodied worms) or platyhelminths (flat bodied worms).
Nematodes (round worms) are long, round bodied segmented worms that are tapered at both ends . In festation occurs if the embryonated eggs or tissues of infested host contain larva of the nematode.
Protozoal infections and antiprotozoal drugs(therapy).Gagandeep Jaiswal
presentation comprising knowledge about various protozoal infections and therapy options available for the treatment of those infections. various different drugs used in the therapy with their proposed mechanism of action. Hope it will be useful for understanding the pharmacology of antiprotozoals.
Prokinetics are the type of drugs which enhances gastrointestinal motility/transit by
increasing the frequency or strength of contractions.
They speed up gastric emptying by enhancing coordinated propulsive motility.
Treat Gastrointestinal symptoms : Abdominal discomfort, Bloating, constipation,
Heart burn, nausea and vomiting. And few gastrointestinal disorders : irritable bowel
Syndrome, gastritis, gastroparesis and functional dyspepsia.
Increases gastric emptying
Relief of gastric stasis
Decreases reflux esophagitis/heart burn
Decreases regurgitation of gastric contents& emesis
Toxicity is the science dealing with properties, action, toxicity, fatal dose detection or interpretation of result of toxicological analysis & treatment of poison.
Toxicity studies helps to avoid adverse effect and enhance the safety of drug.
This slide provides the information about toxicity screening on experimental animals.
A brief introduction about Pharmacology of free radicals, generation of free radicals, Antioxidants, Free radicals causing disorders such as cancer diabetes, neuro degenerative disorders such as Parkisonism's Disease
Its a about chrono-pharmacology of diabetes
The accurate and detail information about chrono- pharmacology its not available but this information is sufficient or useful.
The identification of the carcinogenic properties of a chemical, resulting in an increased incidence of neoplasms, increased proportion of malignant neoplasms or a reduction in the time to appearance of neoplasms, compared with concurrent control groups.
The identification of target organ(s) of carcinogenicity.
The identification of the time to appearance of neoplasms.
Characterisation of the tumour dose-response relationship.
Introduction to the endocrine system
Growth hormone: Mechanism of Action, secretion, regulation.
Prolactin
Sex hormones
Oral contraceptives
Corticosteroids
Anthelmintics | B.Pharm 3rd year 2nd Sem | Medicinal Chemistry-III | History, Classification, Structures & Synthesis of anthelmintics, Synthesis of Diethylcarbamazine citrate, Synthesis of Mebendazole
Safety pharmacology is a branch of pharmacology with its aim to predict the potential clinical risk profile of new chemical entities (NCEs).
It has the ability to predict the potential off-target drug effects on major organ systems which are associated with exposure in the therapeutic range and above.
As an essential part of the spectrum of drug discovery and development, safety pharmacology studies are generally conducted to determine the relative drug effect on main organs, including respiratory system, central nervous system, and cardiovascular system.Safety pharmacology is an essential part of the drug development process that aims to identify and predict adverse effects prior to clinical trials.
SP studies are described in the international conference on harmonization (ICH) S7A and S7B Guidelines.
Introduction to chronology, chronotherapy, and chronopharmacology.
How chronopharmacology involved in asthma and helps to manage asthma?.
Biological rhythms in bronchial asthma.
Factors associated with nocturnal exacerbation of bronchial asthma.
Introduction to asthma and their symptoms.
Introduction to Antiasthmatic drugs like beta-blockers, leukotriene antagonists, steroids, etc.
Chronopharmacology division & their examples.
Advantages and disadvantages of chronopharmacology.
Marketed preparation and their images along with the price in India.
Dermal Irritation and Dermal Toxicity Studies Dinesh Gangoda
Dermal irritation and Corrosion test guidelines 204.
Dermal irritation is the production of reversible damage of the skin following the application of a test chemical for up to 4 hours.
Corrosive reactions are typified by ulcers, bleeding, bloody scabs, and, by the end of observation at 14 days, by discolouration due to blanching of the skin, complete areas of alopecia, and scars. Histopathology should be considered to evaluate questionable lesions. [1]
Dermal corrosion is the production of irreversible damage of the skin; namely, visible necrosis through the epidermis and into the dermis, following the application of a test chemical for up to four hours.[2]
REFERENCES
OECD/OCDE, Test No. 404: ‘‘Acute Dermal Irritation/Corrosion’’, 28 July 2015 OECD Publishing, peris, Page no, 1- 8.
Robert A., Turner., Screening Methods in Pharmacology; 1st edition; Academic press an imprint of Elsevier, pp, 279- 281.
OECD Guideline for testing of chemicals (1981). ‘‘Repeated Dose Dermal Toxicity’’, 21/28- day Study.
REPRODUCTIVE TOXICITY STUDIES, Definition
Introduction, OECD guidelines for reproductive toxicity studies
Principle of the test, Description of Method, Procedure, Experimental Schedule, Data and Reporting, Results, Male Fertility Toxicological Studies
Ms. I. Sai Reddemma.
Department of Pharmacology
Toxicity is the science dealing with properties, action, toxicity, fatal dose detection or interpretation of result of toxicological analysis & treatment of poison.
Toxicity studies helps to avoid adverse effect and enhance the safety of drug.
This slide provides the information about toxicity screening on experimental animals.
A brief introduction about Pharmacology of free radicals, generation of free radicals, Antioxidants, Free radicals causing disorders such as cancer diabetes, neuro degenerative disorders such as Parkisonism's Disease
Its a about chrono-pharmacology of diabetes
The accurate and detail information about chrono- pharmacology its not available but this information is sufficient or useful.
The identification of the carcinogenic properties of a chemical, resulting in an increased incidence of neoplasms, increased proportion of malignant neoplasms or a reduction in the time to appearance of neoplasms, compared with concurrent control groups.
The identification of target organ(s) of carcinogenicity.
The identification of the time to appearance of neoplasms.
Characterisation of the tumour dose-response relationship.
Introduction to the endocrine system
Growth hormone: Mechanism of Action, secretion, regulation.
Prolactin
Sex hormones
Oral contraceptives
Corticosteroids
Anthelmintics | B.Pharm 3rd year 2nd Sem | Medicinal Chemistry-III | History, Classification, Structures & Synthesis of anthelmintics, Synthesis of Diethylcarbamazine citrate, Synthesis of Mebendazole
Safety pharmacology is a branch of pharmacology with its aim to predict the potential clinical risk profile of new chemical entities (NCEs).
It has the ability to predict the potential off-target drug effects on major organ systems which are associated with exposure in the therapeutic range and above.
As an essential part of the spectrum of drug discovery and development, safety pharmacology studies are generally conducted to determine the relative drug effect on main organs, including respiratory system, central nervous system, and cardiovascular system.Safety pharmacology is an essential part of the drug development process that aims to identify and predict adverse effects prior to clinical trials.
SP studies are described in the international conference on harmonization (ICH) S7A and S7B Guidelines.
Introduction to chronology, chronotherapy, and chronopharmacology.
How chronopharmacology involved in asthma and helps to manage asthma?.
Biological rhythms in bronchial asthma.
Factors associated with nocturnal exacerbation of bronchial asthma.
Introduction to asthma and their symptoms.
Introduction to Antiasthmatic drugs like beta-blockers, leukotriene antagonists, steroids, etc.
Chronopharmacology division & their examples.
Advantages and disadvantages of chronopharmacology.
Marketed preparation and their images along with the price in India.
Dermal Irritation and Dermal Toxicity Studies Dinesh Gangoda
Dermal irritation and Corrosion test guidelines 204.
Dermal irritation is the production of reversible damage of the skin following the application of a test chemical for up to 4 hours.
Corrosive reactions are typified by ulcers, bleeding, bloody scabs, and, by the end of observation at 14 days, by discolouration due to blanching of the skin, complete areas of alopecia, and scars. Histopathology should be considered to evaluate questionable lesions. [1]
Dermal corrosion is the production of irreversible damage of the skin; namely, visible necrosis through the epidermis and into the dermis, following the application of a test chemical for up to four hours.[2]
REFERENCES
OECD/OCDE, Test No. 404: ‘‘Acute Dermal Irritation/Corrosion’’, 28 July 2015 OECD Publishing, peris, Page no, 1- 8.
Robert A., Turner., Screening Methods in Pharmacology; 1st edition; Academic press an imprint of Elsevier, pp, 279- 281.
OECD Guideline for testing of chemicals (1981). ‘‘Repeated Dose Dermal Toxicity’’, 21/28- day Study.
REPRODUCTIVE TOXICITY STUDIES, Definition
Introduction, OECD guidelines for reproductive toxicity studies
Principle of the test, Description of Method, Procedure, Experimental Schedule, Data and Reporting, Results, Male Fertility Toxicological Studies
Ms. I. Sai Reddemma.
Department of Pharmacology
Anthelmintic.
According to the syllabus based on “PHARMACY COUNCIL OF INDIA”
“I Dedicate this work to all the
Students , Pharmacy Faculty & Family Members .”
Anthelmintic are the drugs that either KILL [vermicide] or Expel [vermifuge] infesting Helminths.
The choice of drug for each worm infestation is based not only on Efficacy, but also on Lack of Side effects/ Toxicity, Ease of administration [preferably single dose] & low cost.
Development of resistance has not been a problem in the clinical use of Anthelmintic.
Anthelmintic
According to the syllabus based on “PHARMACY COUNCIL OF INDIA”
“I Dedicate this work to all the
Students , Pharmacy Faculty & Family Members
Drx. Shubhanshu R.s. Jaiswal
Helminthiasis also known as Worm Infection, is any macro parasitic disease of humans & other animals in which a Part of the body is infected with parasitic worms, known as Helminths.
Acetabularia Information For Class 9 .docxvaibhavrinwa19
Acetabularia acetabulum is a single-celled green alga that in its vegetative state is morphologically differentiated into a basal rhizoid and an axially elongated stalk, which bears whorls of branching hairs. The single diploid nucleus resides in the rhizoid.
Synthetic Fiber Construction in lab .pptxPavel ( NSTU)
Synthetic fiber production is a fascinating and complex field that blends chemistry, engineering, and environmental science. By understanding these aspects, students can gain a comprehensive view of synthetic fiber production, its impact on society and the environment, and the potential for future innovations. Synthetic fibers play a crucial role in modern society, impacting various aspects of daily life, industry, and the environment. ynthetic fibers are integral to modern life, offering a range of benefits from cost-effectiveness and versatility to innovative applications and performance characteristics. While they pose environmental challenges, ongoing research and development aim to create more sustainable and eco-friendly alternatives. Understanding the importance of synthetic fibers helps in appreciating their role in the economy, industry, and daily life, while also emphasizing the need for sustainable practices and innovation.
Macroeconomics- Movie Location
This will be used as part of your Personal Professional Portfolio once graded.
Objective:
Prepare a presentation or a paper using research, basic comparative analysis, data organization and application of economic information. You will make an informed assessment of an economic climate outside of the United States to accomplish an entertainment industry objective.
Biological screening of herbal drugs: Introduction and Need for
Phyto-Pharmacological Screening, New Strategies for evaluating
Natural Products, In vitro evaluation techniques for Antioxidants, Antimicrobial and Anticancer drugs. In vivo evaluation techniques
for Anti-inflammatory, Antiulcer, Anticancer, Wound healing, Antidiabetic, Hepatoprotective, Cardio protective, Diuretics and
Antifertility, Toxicity studies as per OECD guidelines
The Roman Empire A Historical Colossus.pdfkaushalkr1407
The Roman Empire, a vast and enduring power, stands as one of history's most remarkable civilizations, leaving an indelible imprint on the world. It emerged from the Roman Republic, transitioning into an imperial powerhouse under the leadership of Augustus Caesar in 27 BCE. This transformation marked the beginning of an era defined by unprecedented territorial expansion, architectural marvels, and profound cultural influence.
The empire's roots lie in the city of Rome, founded, according to legend, by Romulus in 753 BCE. Over centuries, Rome evolved from a small settlement to a formidable republic, characterized by a complex political system with elected officials and checks on power. However, internal strife, class conflicts, and military ambitions paved the way for the end of the Republic. Julius Caesar’s dictatorship and subsequent assassination in 44 BCE created a power vacuum, leading to a civil war. Octavian, later Augustus, emerged victorious, heralding the Roman Empire’s birth.
Under Augustus, the empire experienced the Pax Romana, a 200-year period of relative peace and stability. Augustus reformed the military, established efficient administrative systems, and initiated grand construction projects. The empire's borders expanded, encompassing territories from Britain to Egypt and from Spain to the Euphrates. Roman legions, renowned for their discipline and engineering prowess, secured and maintained these vast territories, building roads, fortifications, and cities that facilitated control and integration.
The Roman Empire’s society was hierarchical, with a rigid class system. At the top were the patricians, wealthy elites who held significant political power. Below them were the plebeians, free citizens with limited political influence, and the vast numbers of slaves who formed the backbone of the economy. The family unit was central, governed by the paterfamilias, the male head who held absolute authority.
Culturally, the Romans were eclectic, absorbing and adapting elements from the civilizations they encountered, particularly the Greeks. Roman art, literature, and philosophy reflected this synthesis, creating a rich cultural tapestry. Latin, the Roman language, became the lingua franca of the Western world, influencing numerous modern languages.
Roman architecture and engineering achievements were monumental. They perfected the arch, vault, and dome, constructing enduring structures like the Colosseum, Pantheon, and aqueducts. These engineering marvels not only showcased Roman ingenuity but also served practical purposes, from public entertainment to water supply.
2024.06.01 Introducing a competency framework for languag learning materials ...Sandy Millin
http://sandymillin.wordpress.com/iateflwebinar2024
Published classroom materials form the basis of syllabuses, drive teacher professional development, and have a potentially huge influence on learners, teachers and education systems. All teachers also create their own materials, whether a few sentences on a blackboard, a highly-structured fully-realised online course, or anything in between. Despite this, the knowledge and skills needed to create effective language learning materials are rarely part of teacher training, and are mostly learnt by trial and error.
Knowledge and skills frameworks, generally called competency frameworks, for ELT teachers, trainers and managers have existed for a few years now. However, until I created one for my MA dissertation, there wasn’t one drawing together what we need to know and do to be able to effectively produce language learning materials.
This webinar will introduce you to my framework, highlighting the key competencies I identified from my research. It will also show how anybody involved in language teaching (any language, not just English!), teacher training, managing schools or developing language learning materials can benefit from using the framework.
How to Make a Field invisible in Odoo 17Celine George
It is possible to hide or invisible some fields in odoo. Commonly using “invisible” attribute in the field definition to invisible the fields. This slide will show how to make a field invisible in odoo 17.
Unit 8 - Information and Communication Technology (Paper I).pdfThiyagu K
This slides describes the basic concepts of ICT, basics of Email, Emerging Technology and Digital Initiatives in Education. This presentations aligns with the UGC Paper I syllabus.
2. Anthelmintic are drugs used in the
treatment of Infection with helminths in the intestinal tract
or tissues of the body.
Anthelmintics that kill worms are called
vermicides and those that help to expel the worms are
called vermifuges.
2Goodman & Gilman’s. The Pharmacological Basis of Therapeutics. 12th edition.
6. Mebendazole (Mebendazole is a Benzimidazole compound)
It is a Benzimidazole introduced in 1972. This congener of thiabendazole became
very popular because it retained the broad-spectrum anthelmintic activity.
Pharmacokinetics
Mebendazole is administered orally.
poorly absorbed from the GI tract.
highly bound to plasma proteins and.
metabolized in liver.
Absorption of mebendazole from intestines is minimal.
75–90% of an oral dose is passed in the faeces.
The fraction absorbed is excreted mainly as inactive metabolites in urine/faeces.
Adverse effects
Mebendazole is well tolerated even by patients in poor health and rarely causes
GIT side effects anorexia, nausea, vomiting, diarrhea, and abdominal Pain
But occasionally it may cause skin rashes, itching, drug fever, etc.
Dose:- 100mg chewable tablet, 100mg/5ml suspension, 100mg tablet.
6
7. Albendazole (Albendazole is a Benzimidazole compound)
It is benzimidazole and has broad spectrum of anthelmintic activity.
Pharmacokinetics
Absorption of albendazole after oral administration is significant, but inconsistent.
It is enhanced when the drug is taken with fatty meal (this may help in treating
neurocysticercosis and hydatid disease).
Side effects
Albendazole is well tolerated; only gastrointestinal side effects have been
noted. Few patients have felt dizziness.
Prolonged use, as in hydatid or in cysticercosis, has caused headache, fever,
alopecia(loss of hair), jaundice and neutropenia, nausea, vomiting,
epigastric, distress.
Dose and administration
Single oral dose of 400mg for adults and childrens >2 years of age,
200mg of single dose for children between 1 -2 yrs of age. No fasting or purging
required.
Uses
Trichinosis, Neurocysticercosis, Cutaneous larva migrans, Hydatid disease, Filariasis. 7
8. Albendazole
Ascariasis, Trichuriasis, and Hookworm and Pinworm Infections
For adults and children older than 2 years of age with ascariasis and
hookworm infections, the treatment is a single dose of 400 mg orally
(repeated for 2–3 days for heavy ascaris infections and in 2 weeks
for pinworm infections)
Hydatid Disease Dosing is 400 mg twice daily with meals for 1 month
or longer. Daily therapy for up to 6 months has been well tolerated.
Neurocysticercosis Corticosteroids are given with the anthelmintic
drug to decrease inflammation caused by dying organism. Albendazole
is given in a dosage of 400 mg twice a day for up to 21 day.
Other Infections Albendazole is the drug of choice in the treatment of
Cutaneous larva migrans (400 mg daily for 3 days),
Visceral larva migrans (400 mg twice daily for 5 days),
Intestinal capillariasis (400 mg daily for 10 days),
Microsporidial infections (400 mg twice daily for 2 weeks or longer),
Gnathostomiasis (400 mg twice daily for 3 weeks).
It also has activity against trichinosis (400 mg twice daily for 1–2 weeks) &
Clonorchiasis (400 mg twice daily for 1 week).
8
9. Thiabendazole (Thiabendazole is a Benzimidazole compound)
A Benzimidazole, thiabendazole has broad spectrum of anthelmintic activity and
effective against most of the nematodes.
Thiabendazole is an alternative to ivermectin or albendazole for the treatment of
strongyloidiasis and cutaneous larva migrans.
Although it is a chelating agent that forms stable complexes with a number of
metals, including iron, it does not bind calcium.
The drug is almost completely metabolized in the liver to the 5-hydroxy form; 90% is
excreted in the urine in 48 hours, largely as the glucuronide or sulfonate conjugate.
Clinical Uses
The standard dosage, 25 mg/kg twice daily, should be given after meals.
Tablets should be chewed. For strongyloides infection, treatment is for 2 days.
Cure rates are reportedly 93%.
A course can be repeated in 1 week if indicated. In patients with hyperinfection
syndrome, the standard dose is continued twice daily for 5–7 days. For cutaneous
larva migrans, thiabendazole cream can be applied topically, or the oral drug can be
given for 2 days (although albendazole is less toxic and therefore preferred).
9
10. Adverse effects:-
dizziness, anorexia, nausea, and vomiting, epigastric pain, abdominal
cramps, diarrhea, headache, drowsiness, and neuropsychiatric
symptoms.
Irreversible liver failure and fatal Stevens-Johnson syndrome have
been reported.
Experience with thiabendazole is limited in children weighing less
than 15kg. The drug should not be used in pregnancy or in the
presence of hepatic or renal disease.
MOA is similarly to Mebendazole and
Albendazole. rarely used because of
it is toxicity.
10
12. Pyrantel Pamoate
Pyrantel pamoate first was introduced into veterinary practice as a
broad-spectrum anthelmintic directed against pinworm, roundworm,
and hookworm infections.
Its effectiveness and lack of toxicity led to its trial against related
intestinal helminths in humans.
Pharmacokinetics
Pyrantel pamote is given orally but absorbed poorly(10-15%), about
80-90% of oral dose is excreted in faeces.
Side effects
Occasional G.I symptoms, headache and dizziness. It is tasteless,
Nonirritant, abnormal migration of worms is not provoked, nausea,
diarrhea, skin rashes, fever. 12
13. MOA Pyrantel pamoate inhibits cholinesterases in worms
stimulates nicotinic Ach concentration
receptors in the worm
persistent depolarisation(Na+, K+ )
spastic paralysis
worms are expelled(vermifuge)
Use and administration
Single dose of 10/11 mg/kg to maximum of 1g is recommended.
NOTE:- Pyrantel pamoate has not been studied in pregnanat women.
Thus its use in pregnant patients and children <2 years of age is not
recommanded. 13
14. Pyrantel pamoate
By stimulating the release of acetylcholine, inhibiting cholinesterase,
and stimulating ganglionic neurons, pyrantel acts as a depolarizing
neuromuscular blocking agent in helminthes.
These actions cause extensive depolarization of the helminth muscle
membrane, producing tension of the helminth's muscles, which
causes paralysis and release of their hold to the intestinal wall.
This action is unlike piperazine, which is a hyperpolarizing
neuromuscular blocking agent that relaxes helminth muscles, causing
a subsequent detachment from the intestinal wall. Expulsion of the
parasites from the GI tract occurs by normal peristalsis.
Precautions
When given parenterally to experiment animals, pyrantel can
produce complete neuromuscular blockade; only very large oral
doses produces toxic effects. 14
15. Diethylcarbamazine citrate (DEC)
Developed in 1948, it is the first drug for filariasis caused by
the nematodes Wuchereria bancroft (90% cases) and Brugia malayi.
Diethylcarbamazine is most effective drug in the treatment of
filariasis and tropical eosinophilia.
DEC is available as citrate salt.
It acts mainly on microfilaria but the adult worms are killed slowly
only on long-term treatment.
DEC damages the microfilaria membrane structure so that they are
destroyed by host defences.
The MOA of DEC against susceptible filarial species is not well
understood but the drug appears to exert a direct effect on
W. bancrofti microfilariae by causing organelle damage and apoptosis.
The MOA of filaricidal action of DEC against adult worms is unknown.
15
16. Pharmacokinetics
Well absorbed from GI tract,
Widely distributed in body metabolized in liver and excreted
in urine.
Side effects
Drug induced effects- Vomiting, headache, and dizziness
Parasite induced reaction- Due to release of protein from dying
parasites.
Diethylcarbamazine(DEC)- Produce a severe reaction,
characterized by severe itching, fever, skin rashes, nausea,
vomiting, headache, joint pain, lymphadenitis,
keratisis(inflammation of cornea).
Uses
Filariasis, Tropical pulmonary eosinophilia. 16
17. Clinical uses
Wuchereria bancrofti, Brugia malayi, Brugia timori, and Loa loa
These infections are treated for 2 or (for L loa) 3 weeks, with initial
low doses to reduce the incidence of allergic reactions to dying
microfilariae. This regimen is 50 mg (1 mg/kg in children) on day 1,
three 50 mg doses on day 2, three 100 mg doses (2 mg/kg in
children) on day 3, and then 2 mg/kg three times daily to complete
the 2–3 week course. Diethylcarbamazine may also be used for
chemoprophylaxis (300 mg weekly or 300 mg on 3 successive days
each month for loiasis; 50 mg monthly for bancroftian and Malayan
filariasis)
Other uses
Diethylcarbamazine is given orally at a dosage of 2mg/kg 3 times a
daily for 7 days.
17
18. Ivermectin
It is an extremely potent semisynthetic derivative of the
antinematodal principle obtained from Streptomyces avermitilis.
It is the drug of choice in onchocerciasis and strongyloidiasis.
It is effective against microfilaria of W.bacrofti and B.malayi.
MOA
Ivermectin
Activates glutamate-gated chloride channels
Increases GABA(-aminobutyric acid) transmission in worms
Hyperpolarisation and paralysis of worms
Death/phagocytises of worms
18
20. Pharmacokinetics
It is given orally rapidly absorbed widely distributed to various tissues
metabolized in the liver and excreted mainly in faeces
Uses
Onchocerciasis/river blindness(caused by bites of infected simulius blackflies)
Kills microfilaria but has little effective in stronglyoidiasis, ascarais,
and cutaneous larva migrans. Treatment of scabies and pediculosis.
Side effects
Itching, skin rashes, oedema, headache, fever, muscle and joint pain.
Clinical uses
Onchoerciasis Treatment is with a single oral dose of ivermectin,
150 mg/kg, with water on an empty stomach.
Strongyloidiasis Two daily of 200 mg/kg.
20
21. Niclosamide
Niclosamide is a highly effective drug against cestodes infesting man—
Taenia saginata, T. solium, Diphyllobothrium latum and
Hymenolepis nana, as well as pin worm.
The drug MOA appears to act by inhibiting oxidative phosphorylation
in mitochondria and interfering with anaerobic generation of ATP by
the tapeworm.
Adverse effects
Niclosamide is tasteless and nonirritating.
It is minimally absorbed from g.i.t.—no systemic toxicity occurs.
It is well tolerated; minor abdominal symptoms are produced
occasionally.
Malaise(discomfort, illness), pruritus(severe itching of skin) and light
headedness are rare.
Niclosamide is safe during pregnancy and in patients with poor health
21
22. Mitochondria
22
MOA OF NICLOSAMIDE
Clinical Uses
The adult dose of Niclosamide is 2g once, given in the morning on an
empty stomach. The tablets must be chewed thoroughly and then
swallowed with water.
23. Praziquantel
It is effective in the treatment of trematodes and cestodes but
not for Nematodes.
Pharmacokinetics- It is readily absorbed after oral administration
undergoes extensive first-pass metabolism in liver, highly bound to
plasma protein, crosses the BBB and excreted mainly in urine.
AD effects- Dizziness, nausea, vomiting, abdominal discomfort,
headache, drowsiness, skin rashes, itching, muscle and joint pain.
Uses
Schistosomiasis
Tapeworm infection
Neurocysticercosis.
23
24. Clinical Uses
Praziquantel tablets are taken with liquid after a meal they should be
swallowed without chewing because their bitter taste can induce vomiting.
Schistosomiasis
Praziquantel is the drug of choice for all forms of schistosomiasis.
The dosage is 20 mg/kg per dose for two or three doses at intervals of
4–6 hours. High cure rates (75–95%) are achieved when patients are
evaluated at 3–6 months; there is marked reduction in egg counts in
those not cured.
Clonorchiasis, Opisthorchiasis, and Paragonimiasis
Standard dosing is 25 mg/kg three times daily for 2 days for each of these
fluke infections.
Taeniasis and Diphyllobothriasis
A single dose of praziquantel, 5–10 mg/kg, results in nearly 100% cure rates
for T saginata , T solium , and D latum infections. Because praziquantel
does not kill eggs.
24
25. Neurocysticercosis
The praziquantel dosage is 100mg/kg/d in three divided doses for
1 day, then 50mg/kg/d to complete a 2 to 4 week course.
Hymenolepis nana
Praziquantel is the drug of choice for H nana infections and the
first drug to be highly effective.
A single dose of 25 mg/kg is taken initially and repeated in 1 week.
Other Parasites
Limited trials at a dosage of 25 mg/kg three times daily for 1–2 days
indicate effectiveness of praziquantel against fasciolopsiasis,
metagonimiasis, and other forms of heterophyiasis.
Praziquantel was not effective for fascioliasis, however, even at
dosages as high as 25 mg/kg three times daily for 3–7 days.
25
26. Praziquantel
It is effective in the treatment of trematodes and cestodes but not for
Nematodes.
The mode of action is not exactly known at present, but experimental evidence
shows following mechanism.
MOA
Praziquantel
influx of ca2+ into the tegument
increased muscular contraction and spastic paralysis
At higher concentration
damage tegument
death of the parasite
26
28. Metroimdazole:-
Metronidazole is an antibiotic that is used to treat a wide variety of
infections.
It works by stopping the growth of certain bacteria and parasites.
This antibiotic treats only certain bacterial and parasitic infections.
It will not work for viral infections (such as common cold, flu).
Metronidazole is of the nitroimidazole class.
Side effects:-Nausea, a metallic taste, loss of appetite, and
headaches. Occasionally seizures or allergies to the medication may
occur.
28
29. METROIMIDAZOLE
Metronidazole diffuses into the organism, inhibits protein synthesis
by interacting with DNA and causing a loss of helical DNA structure
and strand breakage. Therefore, it causes cell death in susceptible
organisms.
It inhibits nucleic acid synthesis by disrupting the DNA of microbial
cells.
29
30. PIPERAZINE
Piperazine can be used to treat infections with the common
roundworm (Ascaris lumbricoides) and the threadworm (Enterobius
vermicularis).
Piperazine is given orally and some, But not all is absorbed.
It is partly metabolised, and the remainder is eliminated, unchanged,
via the kidney.
The drug has little pharmacological action in the host. When used to
treat roundworm, piperazine is effective in a single dose.
For thread worm, a longer course (7 days) at lower dosage is
necessary.
30
31. Side effects:- gastrointestinal disturbances, and bronchospasm occur
occasionally, and some patients experience dizziness.
The drug should not be given to pregnant patients or to those with
compromised renal or hepatic function.
MOA
It reversibly inhibits neuromuscular transmission in the worm,
probably by acting like GABA, the inhibitory neurotransmitter, or
GABA-gated chloride channels in nematode muscle.
The paralysed worms are expelled alive by normal intestinal
peristaltic movements.
31
32. Reference:-
Essential medical pharamcology 8th edition by KD Tripathi page no
906-914.
Basic & Clinical Pharmacology 12th edition by Bertram G.
Katzung,Susan B. Masters, Anthony J. Trevor. Chapter 53 clinical
pharmacology of the antihelminthic drugs Philip J. Rosenthal MD
page no;937-947.
Goodman & Gilman’s The pharmacological basis of therapeutics
page no;1443-1451.
Modern pharmacology with clinical application 5th edition by
Charles R. Craig & Robert E. Stitzel page no;621.
Rang and Dale’s Pharmacology 6th edition pageno;712-717.
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