Benzimidazoles
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Benzimidazoles are heterocyclic organic compounds used to treat infections from roundworms, tapeworms, lungworms, and liver flukes. They act by uncoupling oxidative phosphorylation in flukes, inhibiting the fumarate reductase enzyme and impairing glucose uptake, decreasing ATP synthesis and killing the parasite. Common drugs include albendazole, fenbendazole, and triclabendazole, which are dosed based on species and weight. Side effects can include headaches, nausea, and vomiting, while rare but serious effects include acute renal failure and hepatotoxicity. Benzimidazoles are contraindicated during pregnancy, lactation, or for hypersensitive or younger animals.
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The all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
this information is free to use by anyone.
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1) The document describes the procedure for synthesizing benzimidazole from o-phenylenediamine and formic acid.
2) Key steps include heating a mixture of o-phenylenediamine and excess formic acid at 100°C for 2 hours, then making the reaction mixture alkaline with sodium hydroxide to precipitate crude benzimidazole.
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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
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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
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Natural compounds from the bark of the cinchona tree, most notably quinine was observed to exhibit antimalarial activity.
Until the development of synthetic derivatives (ie. 4-aminoquinoline antimalarials), quinine continued to be the first choice to treat malaria.
Quinine is associated with side effects such as diarrhœa.
4-aminoquinoline antimalarials such as amodiaquine and chloroquine largely replaced quinine because of reduced unpleasant side effects.
The life cycle of the parasite and the immunological defence mechanisms against the parasite are complex.
Part of the parasite’s life cycle involves invasion of red blood cells (erythrocytes).
The haemoglobin within the red blood cell is broken down by the parasite and is used as a source of amino acids.
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This document discusses antifungals used in poultry and ruminants. It lists several classes of antifungals including polyene antibiotics, azoles, and those for superficial and systemic fungal infections. It provides details on the chemical composition, mode of action, uses, dosage and pricing for common antifungals like amphotericin B, azoles including fluconazole and ketoconazole, and griseofulvin. It also discusses topical antifungals like nystatin and haloprogin as well as natural antifungals added to animal feed like cloves, ginger, garlic and coconut.
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Anthelmintics (antihelminthics) drugs
The all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
this information is free to use by anyone.
Synthesis of benzimidazole
1) The document describes the procedure for synthesizing benzimidazole from o-phenylenediamine and formic acid.
2) Key steps include heating a mixture of o-phenylenediamine and excess formic acid at 100°C for 2 hours, then making the reaction mixture alkaline with sodium hydroxide to precipitate crude benzimidazole.
3) Benzimidazole has biological applications as an active component in anthelmintic and antiulcer drugs, and its derivatives also show antimicrobial and anticancer properties.
H1and h2 receptors
This document discusses histamine receptors and their antagonists. It begins with an introduction to histamine and its physiological effects. It then describes the three main histamine receptor subtypes (H1, H2, H3) and their locations in the body. The document focuses on H1 and H2 receptor antagonists, classifying and providing examples of different types of antihistamines. It discusses the mechanisms of action and structure-activity relationships of H1 receptor antagonists like mepyramine and H2 receptor antagonists like ranitidine and cimetidine. References are provided at the end.
Macrolide antibiotics
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
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The document discusses various approaches used in drug design, including quantitative structure activity relationship (QSAR) analysis. QSAR uses physicochemical parameters like partition coefficient, electronic parameters, and steric parameters to develop mathematical models correlating a drug molecule's structure to its biological activity. The goal is to predict activity for new compounds and guide drug design. Parameters commonly used in QSAR include log P for hydrophobicity, Hammett constants for electronics, and Taft constants for sterics. Methods involve Hansch analysis, Free Wilson models, and other statistical techniques.
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This document discusses anthelmintic drugs used to treat helminth infections. It begins by describing common types of helminths including tapeworms, roundworms, and flukes. It then discusses ideal properties of anthelmintic drugs and classifications based on mechanism of action, spectrum of activity, and type of helminth targeted. Specific drug classes and examples are provided, including benzimidazoles, tetrahydropyrimidines, piperazine, diethylcarbamazine, ivermectin, and others. Their mechanisms of action, clinical uses, safety profiles and pharmacokinetics are summarized for key anthelmintic drugs.
Antimalarial drugs
Natural compounds from the bark of the cinchona tree, most notably quinine was observed to exhibit antimalarial activity.
Until the development of synthetic derivatives (ie. 4-aminoquinoline antimalarials), quinine continued to be the first choice to treat malaria.
Quinine is associated with side effects such as diarrhœa.
4-aminoquinoline antimalarials such as amodiaquine and chloroquine largely replaced quinine because of reduced unpleasant side effects.
The life cycle of the parasite and the immunological defence mechanisms against the parasite are complex.
Part of the parasite’s life cycle involves invasion of red blood cells (erythrocytes).
The haemoglobin within the red blood cell is broken down by the parasite and is used as a source of amino acids.
The 4-aminoquinolines act at the erythrocytic stage of the parasite.
Doxycycline is a compound used in prophylaxis against plasmodial parasites.
Other compounds associated with treating malaria include halofantrine and lumefantrine, often used in combination with other drugs.
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Albendazole mechanism of action_pdf.pdf
We take albendazole medicine for deworming, get relief and forget. Many people have a curiosity to know the fate of the drug.
Albendazole is a miracle drug because it uniquely kills parasitic worms.
Albendazole medicine is basically used for deworming, and it comes on the essential drugs list of WHO (World Health Organisation).
Here, I have made an easy guide to understanding albendazole mechanism of action (moa) and pharmacokinetics.
After reading this post, you will know how albendazole works and how the body reacts in response to albendazole.
The principal mechanism of action of albendazole is inhibiting polymerization and the cell division process of helminths. But it also depends on the types of parasitic worms –
Albendazole mechanism of action for intestinal worms :
When you take albendazole, it goes to your small intestine and is directly active against intestinal worms.
Albendazole strongly binds to the β-tubulin site of worm parasites. As a result, it inhibits the polymerization process that destroys the assembly of the worm’s microtubules.
You don’t need albendazole in your blood circulation for intestinal helminths (such as hookworm, pinworm, roundworm).
In this condition, you have to take albendazole on an empty stomach so that it can stay for a longer time in your intestine. Albendazole does not absorb on an empty stomach but is rapidly absorbed with a fatty meal.
Albendazole mechanism of action for tissue worms:
Sometimes, parasitic worms penetrate your blood circulation and tissues via intestine to blood or skin to blood. In this condition, Albendazole act as a prodrug.
Suppose you have a neurocysticercosis problem (worms in your brain) and take albendazole with a fatty meal.
Firstly, it goes to your stomach and then the small intestine. From the small intestine, albendazole is rapidly absorbed into your hepatic portal circulation via the inferior mesenteric vein.
As soon as albendazole reaches the liver, it converts into albendazole sulfoxide by First Pass Metabolism. Here, albendazole sulfoxide is a real anthelmintic for systemic worm infections.
After reaching blood circulation, it easily crosses your blood-brain barrier (BBB) and enters cerebrospinal fluid (CSF) because albendazole is a highly lipid-soluble drug.
In your brain, albendazole get accumulates in higher concentrations. It effectively kills Taenia solium worms that cause neurocysticercosis.
Here, albendazole binds on the β-tubulin site of Taenia solium worms, inhibiting polymerization and cell division.
Albendazole medicine effectively works in intestinal and tissue helminths by binding on the β-tubulin site of worm parasites.
It is the safest anthelmintic with minimal side effects.
We should especially focus on the administration of albendazole – with food (for tissue parasites) or without food (intraluminal parasites). It is always best to take albendazole under proper medical supervision.
Albendazole Tablet
Albendazole is an anthelmintic (an-thel-MIN-tik) or anti- worm medication. It prevents newly hatched insect larvae (worms) from growing or multiplying in your body. Albendazole is used to treat certain infections caused by worms such as pork tapeworm and dog tapeworm
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Drugs for helminthiasis.
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ANTIFUNGAL-DRUGS details ofclassificationand adversity.pdf
This document discusses the mechanisms of action and uses of various antifungal drugs. It begins by defining antifungal drugs as those that inhibit or slow fungal growth. It then describes the different sites of action for various antifungal drugs, including the cell membrane, cell wall, and intracellular sites. For each drug class, the document provides details on the mechanism of action, source, spectrum of activity, resistance, pharmacokinetics, adverse effects, drug interactions, and dosages. A wide range of individual antifungal drugs are examined, from amphotericin B to griseofulvin.
Antihelmentic drugs
Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them and without causing significant damage to the host.
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Class antifungal agents
This document discusses various antifungal drugs, their mechanisms of action, and clinical uses. It describes how caspofungin inhibits fungal cell wall synthesis, while amphotericin B and nystatin bind to ergosterol in the fungal cell membrane. Azoles like ketoconazole, fluconazole and itraconazole inhibit ergosterol synthesis. 5-flucytosine inhibits fungal nucleic acid synthesis. It also discusses the antifungals' mechanisms of action, pharmacokinetics, clinical indications, resistance and adverse effects. Superficial and systemic fungal infections are outlined.
Anthelmintic drugs
Albendazole is a broad-spectrum oral anthelmintic drug used to treat various worm infections and parasitic diseases. It works by inhibiting the polymerization of parasite tubulin, which disrupts the formation of microtubules. Common side effects include abdominal pain, headaches, and diarrhea. When used for longer periods, it can potentially cause liver enzyme elevations, neutropenia, and alopecia. Nurses should monitor patients' liver enzymes and blood counts regularly when they are taking albendazole.
Anthelmintic Drugs [Pharmacology]
In this slidashare we have covered the anthelmintic medications.
In this we have covered introduction,classification of the anthelmintic drugs,their mechanism of action,uses,side effects,etc...
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3.15_Drug_Formulary_for_Primates_and_Primate_Sanctuaries.pdf
3.15_Drug_Formulary_for_Primates_and_Primate_Sanctuaries.pdf
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Prostate hyperplasia in dogs is a natural consequence of aging that occurs in most dogs over six years old, as both estrogen and androgen must be present for marked enlargement. The prostate gland is located near the bladder, and an enlarged prostate can be detected during rectal examination, ultrasound, or cytological examination. The most effective treatments are castration to cause involution of the enlarged gland or low dose estrogen treatment to depress hormone secretion.
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Benzimidazoles
- 1. BENZIMIDAZOLES Md. Saheb Ali Faculty of Veterinary Science Bangladesh Agricultural University
- 2. Outline Definition Indication Mode of action Pharmacological dose Available drugs in BD Side effect Contraindication
- 3. BENZIMIDAZOLES Benzimidazoles is a heterocyclic organic compound. This bicyclic compound consists of fusion of benzene and imidazole. It is a colorless solid.
- 4. Indications: Infections against Round worm Tape worm Lung worm Liver fluke
- 5. MODE OF ACTION Acts as a uncoupling oxidative phosphorylation in fluke. They inhibit the fumerate reductase enzyme, impaired glucose uptake thereby decrease ATP synthesis and killed the parasite.
- 6. Pharmacological Dose Albendazole: Cattle: @ 7.5 mg/kg bwt Sheep & Goat @ 5 mg/kg bwt Fenbendazole: Cattle: @ 7.5 mg/kg bwt Dog & Cat: @ 100 mg/kg bwt Horse: @ 5-10 mg/kg bwt Triclabendazole: Cattle: @ 12 mg/kg bwt Sheep & Goat: @10 mg/kg bwt
- 7. Common Trade Names of Benzimidazoles Tab. Albentic vet @ 1 tab/80 kg bwt Bol. Almex @ 1 boli / 80 kg bwt Tab. Helmex @ 1tab/80 kg bwt Bol. Acinex @ 1 tab/75 kg bwt Bol. Endex @ 1 boli/70 kg bwt Bol. Fenvet @ 1 boli/ 50 kg bwt
- 8. Side Effects Common: Headache, Abdominal pain, Nausea, Vomiting. Rare: Fever, skin rash, itching, thining or loss of hair, unusual tiredness and weakness. Serious: Acute renal failure, Granulocytopenia, Hepatotoxicity and leucopenia