Antihelminthic and antiprotozoal drugs are used to treat infections caused by helminths (worms) and protozoa. The major classes of antihelminthics discussed are mebendazole, albendazole, pyrantel, levamisole, and piperazine which are used against nematodes, trematodes, and cestodes. Antiprotozoal drugs discussed include metronidazole for amoebiasis, giardiasis, and trichomoniasis. Drugs for malaria discussed are quinine, chloroquine, antifolates, primaquine, and nitrofurans. Melarsoprol
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.
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.
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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.
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Cardiac conduction defects can occur due to various causes.
Atrioventricular conduction blocks ( AV blocks ) are classified into 3 types.
This document describes the acute management of AV block.
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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.
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ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
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Explore natural remedies for syphilis treatment in Singapore. Discover alternative therapies, herbal remedies, and lifestyle changes that may complement conventional treatments. Learn about holistic approaches to managing syphilis symptoms and supporting overall health.
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
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effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
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
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2. • Antihelmintics are drugs that either kill
(vermicide) or expel (vermifuge) infesting
helminths.
• Nematodes, trematodes, and cestodes are three
major groups of helminthes (worms) that infect
humans.
• Nematodes are elongated roundworms that
possess a complete digestive system. They
cause infections of the intestine as well as the
blood and tissues.
• We use: mebendazole, albendazole, pyrantel,
levamisol, piperazine.
3.
4. Mebendazole
• Uses: whipworms (Trichuris trichiura), pinworms
(Enterobius vermicularis), hookworms (Necator
americanus and Ancylostoma duodenale), and
roundworms (Ascaris lumbricoides);
in high doses: extraintestinal helminthiasis
(trichinellosis and echinococcosis)
• It inhibits the assembly of the microtubules and
glucose utilization in helminthes and paralyses them.
It kills ova and larvae of Ascaris.
• Absorption from intestines – 10-15%
• Adverse effects: abdominal pain, diarrhea,
headache, allergic reactions
5. Albendazole
Uses: ascariasis, hookworms and enterobiasis
(a single dose) , toxocariasis, filariasis,
cysticercosis, echinococcosis (long-term
therapy).
It is absorbed from GIT, metabolized in the
liver.
Adverse effects: headache, diarrhea, dizziness,
leucopenia, skin rashes, abdominal pain,
vomiting.
6. Levamisole
Uses: a single dose – ascariasis, less effective
– ankylostomiasis, strongyloidiasis, filariasis.
Mechanism: stimulation of ganglia, drug-
induced paralysis of helminthes due to
depolarization of their muscles, inhibition of
fumarate reductase and metabolism.
Adverse effects: abdominal pain, diarrhea,
nausea
7.
8. • Pyrantel is active against Ascaris, Enterobius,
Ancylostoma, Necator, Strongyloides
• Mechanism: activation of nicotinic cholinergic
receptors in the worms → persistent
depolarization → slowly developing
contracture and spastic paralysis.
• Absorption from GIT – 10-15%.
• Adverse effects: nausea, vomiting, abdominal
pain, headache and dizziness
9. Diethylcarbamazine citrate is
microfilaricidal. It has a highly selective effect
on microfilariae and against adult worms.
It is rapidly absorbed following oral
administration with meals and is excreted
mainly in the urine.
Adverse effects may include fever, nausea,
vomiting, arthralgia, and headache.
10. Niclosamide
• Uses: Taenia saginata, Diphyllobothrium latum
and Hymenolepis nana.
• It inhibits the mitochondrial phosphorylation of
adenosine diphosphate (ADP). Anaerobic
metabolism may also be inhibited.
• In cases of T. solium, digestion of the dead
segments can be hazardous, because the ova
released from them may develop into larvae in the
intestine, penetrate its wall and cause visceral
cysticercosis.
• It is minimally absorbed from GIT.
• Adverse effects: dyspepsia, allergic reactions.
11.
12. Praziquantel
Uses: all forms of schistosomiasis, other
trematode infections, cestode infections such as
taeniasis, cysticercosis (caused by Taenia solium
larvae)
Mechanism: leakage of intracellular calcium from
the membranes → contracture and paralysis.
It is rapidly absorbed after oral administration and
distributes into the cerebrospinal fluid (CSF). It is
extensively metabolized, and the inactive
metabolites are excreted primarily in the urine.
Adverse effects: dizziness, malaise, headache
13. Antiprotozoal drugs are used for the treatment
and prophylaxis of:
Malaria
Amebiasis
Giardiasis (Metronidazole, furazolidone)
Trixomoniasis (Metronidazole, furazolidone,
Diiodohydroxyquin rect.)
16. Antiamoebic drugs - drugs useful in infection
caused by the anaerobic protozoa Entamoeba
histolytica.
17. CLASSIFICATION
1. Tissue amoebicides
For both intestinal and extraintestinal amoebiasis:
Nitroimidazoles: Metronidazole, Tinidazole,
Ornidazole
For extraintestinal amoebiasis only: Chloroquine
2. Luminal amoebicides: Tetracyclines
18. • Nitroimidazoles (Metronidazole) is used for the
treatment of infections caused by:
• Entamoeba histolytica,
• Giardia lamblia,
• Trichomonas vaginalis,
• anaerobic cocci, and anaerobic gram-negative
bacilli (Bacteroides species),
• for the treatment of pseudomembranous colitis
caused by the anaerobic, gram-positive bacillus
Clostridium difficile.
19.
20. • The nitro group of Nitroimidazoles is able to
serve as an electron acceptor, forming reduced
cytotoxic compounds that bind to proteins and
DNA. The drugs disrupt metabolism and cause
death of microorganisms.
• They are absorbed well from GIT, distribute well
throughout body tissues and fluids. Therapeutic
levels can be found in vaginal and seminal fluids,
saliva, breast milk, and cerebrospinal fluid (CSF).
• Tinidazole and ornidazole are well absorbed from
GIT, accumulated in the plasma in higher
concentrations than Metronidazole and provide
longer effect than it.
21. Adverse effects:
nausea, vomiting, epigastric distress, and
abdominal cramps, an unpleasant,
metallic taste,
oral moniliasis (yeast infection of the
mouth),
neurotoxicity (dizziness, vertigo, and
numbness or paresthesia),
a disulfiram-like reaction (if taken with
alcohol).
22. • Malaria is one of the most common diseases
worldwide and a leading cause of death. Plasmodium
species that infect humans (P falciparum, P malariae,
P ovale, P vivax) undergo a primary developmental
stage in the liver and then parasitize erythrocytes. P
falciparum and P malariae have only 1 cycle of liver
cell invasion. The other species have a dormant
hepatic stage responsible for recurrent infections and
relapses. Primary tissue schizonticides (eg,
primaquine) kill schizonts in the liver, whereas
blood schizonticides (eg, chloroquine, quinine) kill
these parasitic forms only in the erythrocyte.
Sporonticides (proguanil, pyrimethamine) prevent
sporogony and multiplication in the mosquito.
24. Principals of antimalarial drugs use
1. Individual chemoprophylaxis: prevention of the
development of malaria in men during the time
of residency in a area which has a high risk of
malaria. We can use drugs influencing on
preerythrocytic forms or hematoshizotropic
drugs (pyrimethamine, chloroquin)
2. The treatment: oral administration of
hematoshizotropic drugs, which influence
erythrocytic forms of plasmodia. These drugs are
used to cure the acute attacks of M.
25. 3. Prevention of delayed relapses: administration
of drugs which have tropism towards
paraerythrocytic forms (primaquine).
4. Social chemoprophylaxis: prevention of the
transmission of the infection by a sick person.
We use gametotropic drugs (primaquine,
pyrimethamine).
26.
27. • Chinine (Quinine) complexes with
doublestranded DNA and prevents strand
separation, blocks DNA replication and
transcription to RNA. It is solely a blood
schizonticide.
• It is rapidly absorbed orally and is metabolized
before renal excretion. Intravenous administration
of quinine is possible in severe infections.
• It is used in the treatment of severe or
complicated falciparum malaria.
• Adverse effects: cinchonism (gastrointestinal
distress, headache, vertigo, blurred vision and
tinnitus).
28. • Chloroquine is rapidly absorbed when given
orally, is widely distributed to tissues.
• It accumulates in the food vacuole of plasmodia
and prevents polymerization of the hemoglobin
breakdown product heme into hemozoin.
Intracellular accumulation of heme is toxic to the
parasite.
• It is the drug of choice for acute attacks of malaria
and for chemoprophylaxis.
• Side effects: gastrointestinal irritation, skin rash,
and headaches; peripheral neuropathies,
myocardial depression, retinal damage, auditory
impairment, and toxic psychosis
29. • Sulfonamides act as antimetabolites of PABA and
block folic acid synthesis by inhibiting
dihydropteroate synthase.
• Pyrimethamine is a selective inhibitor of
protozoan dihydrofolate reductases. The
combination has synergistic antimalarial effects
(blockade of 2 steps in folic acid synthesis).
• The antifols are blood schizonticides that act
mainly against P falciparum.
• Adverse effects: skin rashes, gastrointestinal
distress, hemolysis, kidney damage.
30. • Primaquine is a synthetic 8-aminoquinoline. It
is used orally.
• It forms quinoline- quinone metabolites, which
are electron-transferring redox compounds that
act as cellular oxidants. The drug is a tissue
schizonticide and also limits malaria
transmission by acting as a gametocide.
• Uses: Eradication of liver stages of P vivax and P
ovale, primary prevention
• Adverse effects: GI distress,
methemoglobinemia, hemolysis in G6PD
deficiency
32. Mechanism:
The restoration of the nitro group to the amino
group under the influence of reductase
microbial cells.
The formation of complexes with nucleic acids,
Disruption of the respiratory chain of
microorganisms.
Increase in the body's resistance to infections.
The decline in the production of toxins.
Type of action: bacteriostatic or bactericidal
33. Side effects
Dyspeptic disorders: nausea, vomiting,
diarrhea;
Cholestasis; disorders of liver function;
Allergic reaction;
Headache, dizziness;
Hemolytic anemia,
Methemoglobinemia in children
up to a year;
Arterial hypertension
34. • Melarsoprol is used for the treatment of
trypanosomal infections. The drug reacts with
sulfhydryl groups of various substances, including
enzymes in both the organism and host.
• It is administered by slow IV injection and has
irritating effect. Adequate trypanocidal
concentrations appear in the CSF. The drug has a
very short half-life and is rapidly excreted in urine.
• Adverse effects: CNS toxicity, peripheral
neuropathy, hypertension, albuminuria; allergy,
febrile reactions; hemolytic anemia in patients
with glucose-6-phosphate dehydrogenase
deficiency.
35.
36. Leishmania, transmitted by flesh-eating flies,
cause various diseases ranging from or
mucocutaneous lesions to splenic and hepatic
enlargement with fever.
37. • Solusurminum and Sodium stibogluconate
(pentavalent antimony) kills the parasite by
inhibition of glycolysis or effects on nucleic
acid metabolism.
• Stibogluconate must be administered
parenterally and is potentially cardiotoxic
(QT prolongation). Alternative agents
include fluconazole or metronidazole (for
cutaneous lesions), and amphotericin (for
mucocutaneous leishmaniasis).
38. Literature
1. Tripathi K.D. Essentials of Medical Pharmacology. Eighth Edition. -2019.- Jaypee
Brothers Medical Publishers. The Health Sciences Publisher. -New Delhi. London. Panama
2. D.A.Kharkevich. Pharmacology. Textbook for medical students. Translation of 12th
edition of Russion textbook “Pharmacology” (2017). – М., ГЭОТАР-Медиа, 2017.
3. Review of pharmacology. Gobind Rai Garg, Sparsh Gupta. 13th edition. - 2019.- Jaypee
Brothers Medical Publishers. The Health Sciences Publisher. -New Delhi. London. Panama
4. Whalen Karen. Lippincott Illustrated Reviews: Pharmacology. Sixth Edition. - Wolters
Kluwer. - 2015.-Philadelphia
5. Color Atlas of Pharmacology. 2nd edition, revised and expanded. Heinz Lüllmann.- 2000
Thieme
6. Pharmacology Examination & Board Review. Tenth Edition. Trevor Anthony J.,
Katzung Bertram G., Kruidering-Hall Marieke, Susan B. Masters. - a LANGE medical
book. - 2013.-New York
7. Medical Pharmacology at a Glance. Eighth Edition. Neal Michael J. – 2016. John Wiley
& Sons, Ltd.
8. USMLE Step 1. Lecture Notes. Pharmacology. Lionel P.Raymon and others.- Kaplan
Medical.Inc. -2009