Medicinal chemistry iii
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These orally administered drugs attain antibacterial concentrations only in urine, treating lower urinary tract infections locally without systemic effects. Nitrofurantoin and methenamine are examples that are concentrated in kidney tubules. While nitrofurantoin is suitable for oral UTI treatment, it and the nitrofurans are known to be potentially mutagenic and carcinogenic due to metabolic reaction products that can damage DNA. Methenamine releases formaldehyde in acidic urine to inhibit bacteria without bacteriostatic power, making it useful as an internal urinary antiseptic for chronic UTIs.
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This document discusses various classes of anti-fungal drugs including antifungal antibiotics like polyenes such as amphotericin B and nystatin, antimetabolites like flucytosine, and azoles including imidazoles like ketoconazole and triazoles like fluconazole and itraconazole. It provides details on their mechanisms of action, effectiveness against different fungal infections, routes of administration, and common adverse effects.
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Tuberculosis is caused by Mycobacterium tuberculosis and was once incurable but now treatable with anti-tubercular drugs. These drugs are classified as primary/standard or secondary/reserve drugs and include isoniazid, rifampicin, streptomycin, pyrazinamide, ethambutol, para-aminosalicylic acid, thiacetazone, capreomycin, kanamycin, ethionamide, and cycloserine. The primary drugs are bactericidal while the secondary drugs treat multi-drug resistant strains. A standard short-term regimen involves taking isoniazid, rifampicin, ethambutol, and pyrazinamide daily for 2 months
Drugs used in protozoal infections with antiprotozoal drugs
This file includes diseases caused by protozoa like amebiasis, Giardiasis, trypanosomiasis, leishmaniasis with drugs acting on the diseases like Emetine, Metronidazole, clioquinol and iodoquinol with their mechanism of action and their pharmacology.
Pharmacology of antitubercular drugs
This presentation describes epidemiology of tuberculosis, classification of anti-tubercular drugs based on the efficacy and priority and the pharmacology of the anti-tubercular drugs.
Antiamoebic drugs
This document discusses various antiamoebic drugs used to treat protozoal infections caused by Entamoeba histolytica, the parasite that causes amebiasis. It describes the life cycle of E. histolytica and clinical manifestations of amebiasis. Several classes of antiamoebic drugs are outlined, including their mechanisms of action, pharmacokinetics, clinical uses, and adverse effects. The main drugs discussed are metronidazole, tinidazole, diloxanide furoate, iodoquinol, emetine/dehydroemetine, paromomycin, and tetracyclines. Metronidazole is highlighted as the drug of choice for
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The document provides an overview of antimicrobial drugs. It discusses the history of antimicrobial drugs from empirical use in ancient times to the modern era beginning in the 1930s. It then covers various topics related to antimicrobial drugs including classification based on organism targeted, mechanism of action, examples of different drug classes, and properties like spectrum of activity. Specific drugs are discussed in more detail like penicillin, its mechanism of inhibiting cell wall synthesis, examples like benzyl penicillin, and its uses and side effects. Other beta-lactam antibiotics and semisynthetic penicillins are also summarized.
Pharmacology - Antiprotozoals
This document discusses antiprotozoal drugs used to treat various protozoal infections. It focuses on drugs used to treat amebiasis caused by Entamoeba histolytica, including metronidazole and tinidazole as mixed amebicides effective against both luminal and systemic forms of the disease. It also discusses luminal amebicides like iodoquinol and paromomycin. For malaria, it covers antimalarial drugs like primaquine, chloroquine, atovaquone-proguanil, mefloquine, quinine, and artemisinin derivatives.
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Antibiotics and its use in dentistry.
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Medicinal chemistry iii
- 2. •These are orally administeredAMAs which attain antibacterial concentration only in urine , with no systemic antibacterial effect. •Like many other drugs , they are concentrated in the kidney tubules , and are useful in lower UTI. •They have been called “urinary antiseptics” because this may be considered as form of local therapy. •Eg. Nitrofurantoin , methenamine.
- 3. •First nitroheterocyclic compound introduced into chemotherapy . •These are derivative of 5-nitro-2-furaldehyde formed on reaction with hydrazine or amine derivative •Antimicrobial activity present only when the nitro group is in 5 position.
- 4. •The nitrofurans are known to be mutagenic and carcinogenic under certain condition. It thought that DNA damage caused by metabolic reaction products may be involved in these cellular effect •Eg. nitrofurantoin
- 5. Drug Bind to DNA, Ribosome Produce superoxides Damage metabolic pathway Bactericidal action Mechanism of action
- 6. •Nitrofurantoin suitable for oral use. •Treatment of UTI caused by susceptible strains of E.coil , enterococci, s. aureus,and klevsiella , Enterobacter and proteus species
- 7. Compound prepared by evaporating a solution of formaldehyde and strong ammonia water to dryness. methanamine is weak base with pka 4.9.
- 8. methanamine Decompose at acidic urine pH Release formaldehyde Inhibit all bacteria
- 9. •It used internally as a urinary antiseptic for treatment of chronic urinary track infection. •Practically no bacteriostatic power.
- 10. • Nausea • Stomach upset • Epigastric • Distress • Bladder irritation • Rash • Contraindication – in renal insufficiency • Chemical cystitis and haematuria • CNS symptoms
- 11. Foye’s Principle of medicinal chemisty Wilson and Gisvald’s textbook of Organic Chemisty and pharmaceutical chemistry