Integrated Pharmaceutical Sciences 1: Organic Medicinal Chemistry Part 2 Lecture Notes PDF

Integrated Pharmaceutical Sciences 1: Organic Medicinal Chemistry Part 2 David Charles B. Alejandro, PharmD, MSPh, RPh Diuretics  Site 1: Carbonic anhydrase inhibitors They inhibit the enzyme carbonic anhydrase which is found in the proximal convoluted tubule. The net resul...

Integrated Pharmaceutical Sciences 1: Organic Medicinal Chemistry Part 2 David Charles B. Alejandro, PharmD, MSPh, RPh Diuretics  Site 1: Carbonic anhydrase inhibitors They inhibit the enzyme carbonic anhydrase which is found in the proximal convoluted tubule. The net result of carbonic anhydrase inhibition is increased excretion of Na+, K+, HCO3-. Site 1: Carbonic anhydrase inhibitors SAR: The free sulfamoyl nitrogen is essential for diuretic activity. Attachment of the sulfamoyl group to aromatic system Site 2: Loop diuretics High ceiling diuretics Inhibit Co-transport System Onset of action in about 30 minutes and lasts for 6 hours. They cause hypokalemia. Subclasses: 1. 2-Aminobenzoic acid derivatives. (Furosemide and Azosemide) 2. Phenoxyaceticacid derivatives (Ethacrynicacid). Site 2: Loop diuretics 5-Sulfamoyl-2-aminobenzoic Acids 1. Position-1 must be acidic (optimal activity with COOH) 2. SO2NH2 group at position 5 is prerequisite for activity, 3. must be free. Furosemide 4. Activating group at position 4- as Cl or CF3. Site 2: loop diuretics Phenoxyacetic acid -Obsolete Ethacrynic acid Site 3: thiazide and thiazide like activity Site 3: thiazide and thiazide like activity Loss of Double bond between 3 and 4 position increases potency Position 6 must be –Cl, -Br, -CF3, –NO2 or a phenoxy group Sulfamoyl group in position 7 is required 4, 5, and 8 substitution destroys activity MOA:  inhibits reabsorption of Na+ and Cl-  Inhibits electroneutral Na+/Cl- co- transport system Site 4: potassium sparing diuretics Aldosterone antagonist: Spironolactone Inhibits Aldosterone Resembles progesterone Eplerenone, Amiloride and Triamterene (Resembles vitamin B9) Na+ Channel Blockers Miscellaneous class Xanthine Alkaloids Osmotic Diuretics Dextrose Mannose Mercurial Diuretics Mercaptomerin Meralluride Merthoxyline Cardiovascular Agents ANTIHYPERTENSIVE AGENTS HYPERTENSION Blood pressure is a measure of the force of the blood pushing against the walls of the arteries Normal B.P120/80 Hypertension is defined as a repeatedly elevated blood pressure exceeding 140/90 mm Hg. So antihypertensive drugs are medications used to treat High blood pressure. IMIDAZOLINE-1 RECEPTOR AGONISTS Non-adrenergic receptors agonized by Clonidine Structurally related to Clonidine VASODILATORS Arteriolar Vasodilators Minoxidil Diazoxide Potassium channel opener Mechanism VASODILATORS Mixed Arteriolar-Venous Vasodilators Nitrates Na Nitroprusside Glyceryl trinitrate Isosorbide dinitrate Amyl Nitrite inhaler Nitrate donors Molsidomine VASODILATORS PDE5 inhibitors Sildenafil Vardenafil Avanafil Tadalafil Dopamine-1 Agonist Fenoldopam Calcium Channel Blockers Dihydropyridine derivatives e.g. Nefidipine Benthothiazepine derivatives e.g. Diltiazem HCl Phenyl alkylamine derivatives e.g. Verapamil  Calcium Channel Blockers Dihydropyridine derivatives Blocks L-type Ca2+ channels in arteriolar SM Nifedipine Amlodipine Nicardipine Felodipine Calcium Channel Blockers Benzothiazepine derivative Diltiazem The drug is used in patients with variant angina and is used also as antiarrhythmic agent. Calcium Channel Blockers Phenyl alkylamine derivative Active metabolite : norverapamil  RAAS MODIFIERS ACE INHIBITORS ACE is Zinc containing enzyme so according to the group that binds with Zn+2 ACE inhibitors are classified into; Sulhydryl containing inhibitors e.g. Captopril and Lisinopril Carboxylate containing inhibitors e.g. Enalapril Phosphonate containing inhibitors e.g. Fosinopril ACE INHIBITORS ACE inhibitors General Structure ANGIOTENSIN RECEPTOR ANTAGONIST AT-1 Antagonist General Structure ANGIOTENSIN RECEPTOR ANTAGONIST Renin inhibitor Cardiac Glycoside Digoxin, Digitoxin, Inhibition of Na+/K+ ATPase (the “sodium pump”) of the cell membrane  Drugs for Dyslipidemia Dyslipidemia Can lead to negative cardiovascular events like ASCVD and CHD. Primary dyslipidemias = genetic predisposition. Secondary dyslipidemias = lifestyle choices. Hyperlipidemia: elevation of serum cholesterol, cholesterol esters, triglycerides, and/or phospholipids. Increases risk of CHD. Hypertriglyceridemia increases risk of pancreatitis. Hyperlipoproteinemia: elevation of the lipoproteins that transport lipids through the bloodstream. DRUGS USED FOR DYSLIPIDEMIA HMG CoA Reductase Inhibitors Atorvastatin Rosuvastatin Simvastatin Fluvastatin Lovastatin Pivastatin  DRUGS USED FOR DYSLIPIDEMIA Fibrinic acid Derivatives Fenofibrate Gemfibrozil Bezafibrate Ciprofibrate Clofibrate MOA: -Peroxisome proliferator- activated receptor alpha agonist - glycerol-3-phosphate O- acyltransferase inhibitor DRUGS USED FOR DYSLIPIDEMIA Niacin aka Nicotinic acid MOA: Inhibits lipolysis of Fatty acids and glycerol from adipose tissue decreasing reserves in the liver for VLDL synthesis  DRUGS USED FOR DYSLIPIDEMIA Bile acid Sequestrants Cholestyramine Colestipol Colesevelam MOA: Anion exchange for bile acid and reduces bile acid reaborption  DRUGS USED FOR DYSLIPIDEMIA Bile acid Sequestrants Cholestyramine Colestipol Colesevelam MOA: Anion exchange for bile acid and reduces bile acid reabsorption Ezetemibe – inhibits intestinal absorption of cholesterol Anti-Obesity Agent Orlistat saturated derivative of lipstatin, a potent natural inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini Orlistat works by inhibiting gastric and pancreatic lipase  DRUGS USED FOR COAGULATION DISORDERS Parenteral Heparin – Activates Antithrombin III Hirudin, Lepirudin, Bivalirudin, Argatroban and Dabigatran – Direct thrombin inhibitors LMW Heparins: Enoxaparin, Fraxiparin, Tinzaparin, Andeparin, Dalteparin and Danaparoid (Heparoid) - Inactivates Factor X Fondaparinux  DRUGS USED FOR COAGULATION DISORDERS: Anticoagulants Oral Dicumarol Phenprocoumon Anisindione and Phenisindione Warfarin MOA: Blocks carboxylation of glutamate/glutamine residues in prothrombin factors II, VII, IX, and X DRUGS USED FOR COAGULATION DISORDERS: Anti-platelet TXA2 Synthesis Inhibitor – Aspirin PDE inhibitors: Dipyridamole and Cilostazol ADP Antagonist: Thienopyridines: Irriversible -Ticlopidine, Clopidogrel, Prasugrel Triazolopyrimidine: Ticagrelor Glycoprotein IIb/IIIa receptor antagonist -Abciximab, Eptifibatide and Tirofiban  DRUGS USED FOR COAGULATION DISORDERS: Thrombolytics Streptokinase Urokinase Tissue plasminogen activators: Alteplase, Reteplase, and Tenecteplase  DRUGS USED FOR BLEEDING DISORDERS Vitamin K Phytonadione-Vitamin K deficiency Fibrinolytic inhibitors: Aminocaproic acid and tranexamic acid Protamine sulfate – heparin reversal Serine Protease Inhibitor – Aprotinin vasopressin V2 receptor agonist: desmopressin acetate – Increases factor VIII activity DRUGS USED FOR DIABETES HUMAN INSULIN ORAL HYPOGLYCEMIC AGENTS Sulfonylureas Max act: R’ = 3-6 Carbons Stimulate the release of insulin from the functioning beta-cells of the intact pancreas. ORAL HYPOGLYCEMIC AGENTS Sulfonylureas First Gen: Tolbutamide, Chlorpropamide, Acetohexamide Second Gen: Glyburide, Glipizide, Glimepiride ORAL HYPOGLYCEMIC AGENTS Meglitinides/Metaglinides Repaglinide and Nateglinide d-phenylalanine derivatives Also insulin secretagogues and blockers if K+ Channels in Beta cells ORAL HYPOGLYCEMIC AGENTS Biguanides Metformin - Euglycemic stimulation of glucose uptake and glycolysis in peripheral tissues slowing of glucose absorption from the GIT Reduction of plasma glucagon levels ORAL HYPOGLYCEMIC AGENTS Thiazolidinediones (Tzds) Rosiglitazone and Pioglitazone increase target tissue sensitivity to insulin by activating PPAR-γ receptor ORAL HYPOGLYCEMIC AGENTS α-Glucosidase Inhibitors Acarbose, Voglibose, and Miglitol Inhibits alpha glucosidase GLP-1 Agonists (injectables) Incretin mimetic drugs Exenatide Liraglutide Albiglutide Direct stimulation of the GLP-1 receptor Dipeptidyp dipeptidase (DPP-4) Inhibitors Saxagliptin and Sitagliptin MOA: Inhibit GLP-1 degradation → promotes glucose-dependent insulin secretion SGLT-2 inhibitors Canagliflozin Dapagliflozin Empagliflozin MOA: Increased glucosuria through the inhibition of SGLT-2 in the kidney Shown to reduce incidence of HF in patients with or without DM (EMPEROR Trials)  Respiratory and Gastrointestinal Drugs Drugs for Asthma: Sympathomimetics Epinephrine Selective Beta-2 agonists Short acting: Albuterol, Terbutaline, and Metaproterenol Long Acting Salmeterol, Formoterol, Indacaterol and Vilanterol Drugs for Asthma: Methylxanthines Purine derivatives Theophylline, Aminophylline, Doxofylline Inhibitor of PDE IV in the lungs May cause arrhythmia Roflumilast Selective PDE IV inhibitor for COPD with bacterial infection Drugs for Asthma: Antimuscarinics Ipratropium Oxytropium Tiotropium and aclidinium Drugs for Asthma: CORTICOSTEROIDS Prednisone Hydrocortisone Local aerosols: Beclomethasone, Budesonide, Dexamethasone, Flunisolide, Fluticasone, Mometasone common first-line therapy for individuals with moderate to severe asthma Drugs for Asthma: LT ANTAGONISTS Leukotriene Receptor Blockers Montelukast and Zafirlukast (LTD4 antagonists) Lipoxygenase Inhibitor Zileuton effective in preventing exercise-, antigen-, and aspirin-induced bronchospasm Drugs for Asthma: Mast Cell Stabilizers Cromolyn & Nedocromil Via aerosol for asthma no bronchodilator action but can prevent bronchoconstriction Drugs for Asthma: ANTI-IgE ANTIBODY Omalizumab humanized murine monoclonal antibody to human IgE binds to the IgE on sensitized mast cells and prevents activation by asthma trigger antigens and subsequent release of inflammatory mediators.  Cough Medication Expectorants Mucolytics Antitussives Guaifenesin Bromhexine Dextromethorphan Sodium Citrate Ambroxol Levodropropizine Carbocisteine Butamirate citrate Acetylcysteine Erdocysteine Motility Promoters (Prokinetics) Cholinomimetics – Bethanecol Neostigmine Macrolide – Erythromycin D2 Receptor Antagonists – Metoclopramide and Domperidone LAXATIVES Antidiarrheal Agents Piperadines: Diphenoxylate and Loperamide Bismuth compounds Bile acid-Binding Resins Ocreotide Kaolin Drugs Used for Irritable Bowel Syndrome Anticholinergics - Dicyclomine and Hyoscyamine 5HT3 Antagonist: Alosetron TCA – Amitriptyline and Desipramine Mesapride, Lubiprostone, and Linaclotide are used for constipation-predominant IBS ANTIEMETICS 5HT3 Antagonist: Ondansetron and friends Corticosteroids: Dexamethasone and Methylprednisolone NK1 Antagonists: Aprepitant and Fosaprepitant Antimuscarinics: Scopolamine ANTIEMETICS Antipsychotics: Promethazine, Prochorperazine, Thiethylperazine, and Droperidol D2 Antagonists: Metoclopramide, Domperidone, Trimethobenzmine Benzodiazepines: Diazepam and Lorazepam Cannabinoids Drugs Used in Inflammatory Bowel Disease (IBD) Anti-bacterials Antibiotics HISTORY Joseph Lister – Antiseptic Principles Paul Erhlich- Father of Chemotherapy Early Anti-infectives – Hg, Sb and As containing compounds  β-Lactam Antibiotics: Pennicilins Substituted 6-APA NATURAL PENICILINS PENICILLINASE – RESISTANT PENICILLINS Methicillin – Nephrotoxic Nafcillin Isoxazolyl Penicillins: Oxacillin Cloxacillin Dicloxacillin BROAD-SPECTRUM PENICILLINS Aminopenicillin Ampicillins Bacampicillin, Pivampicillin, and hetacillin Amoxicillin Sensitive to Penicillinase Clavulanic acid is a common adjuct against penicillinase EXTENDED SPECTRUM Carboxypenicillin Carbenicillin, Carboxypenicillin Indanyl Sodium, and Ticarcillin Active against ampicillin-sensitive, Gram-negative species and additional Gram-negative bacilli of the genera Pseudomonas, Klebsiella, Enterobacter, indole-producing Proteus, Serratia, and Providencia. Ureidopenicillin Azocillin, Mezlocillin, and Piperacillin + Tazobactam β-LACTAMASE INHIBITORS Class 1: Clavulanic Acid, Sulbactam, and Tazobactam Class 2 Imipenem, Doripenem, Meropenem, and Ertapenem  β-Lactam Antibiotics: Cephalosphorins Substituted 7-ACA  β-Lactam Antibiotics: Cephalosphorins Substituted 7-ACA CEPHALOSPHORINS First Generation cefazolin, cefadroxil, cephalexin, cephalothin, cephapirin, and cephradine Second Generation cefaclor cefamandole, cefonicid, cefuroxime, cefprozil, loracarbef, and ceforanide and the structurally related cephamycins cefoxitin, cefmetazole , and cefotetan CEPHALOSPHORINS Third Generation cefoperazone, cefotaxime, ceftazidime, ceftizoxime, ceftriaxone, cefixime, cefpodoxime proxetil, cefdinir, cefditoren pivoxil, ceftibuten, and moxalactam Fourth Generation cefepime, cefotaxime, and ceftazidime Fifth Generation ceftaroline, ceftobiprole  β-Lactam Antibiotics: Monobactams Substituted 3-amino-4-methylmonobactamic acid Aztreonam and Tigemonam OTHER CELL WALL ACTIVE ANTIBIOTICS Glycopeptides Vancomycin and Teicoplanin Lipoglycopeptide Telvacin and Dalbavancin Daptomycin, Fosfomycin, Polymixins, and Gramicidin PROTEIN SYNTHESIS  Protein Synthesis Inhibitors Tetracycline Octahydronaphthacene derivative PROTEIN SYNTHESIS INHIBITORS: TETRACYCLINE MOA: Binding to 30S Ribosomal Subunit Broad Spectrum Bacteriostatic Tetracycline Minocycline –most potent Tigecycline Demeclocycline Doxycycline Oxytetracycline  Protein Synthesis Inhibitors Aminoglycosides Kanamycin PROTEIN SYNTHESIS INHIBITORS: AMINOGLYCOSIDES MOA: Binding to 30S Ribosomal Subunit Gram (-) bactericidal Classifications: Mycins – Obtained from Streptomyces Micins – Obtained from Microsporon PROTEIN SYNTHESIS INHIBITORS: AMINOGLYCOSIDES Streptomycin – treatment of tuberculosis, plague, and tularemia. Tobramycin Neomycin – Most nephron and ototoxic Kanamycin Spectinomycin Gentamicin Netilmicin Amikacin – Kanamycin analog PROTEIN SYNTHESIS INHIBITORS: LINCOSAMIDES MOA: Binding to 50S Ribosomal Subunit Gram (-) bactericidal/static Lincomycin and Clindamycin PROTEIN SYNTHESIS INHIBITORS: CHLORAMPHENICOL MOA: Binding to 50S Ribosomal Subunit Gram (-) bactericidal/static PROTEIN SYNTHESIS INHIBITORS: MACROLIDES Bacteriostatic Bactericidal at high doses Used for G+ and some G- Bacteria PROTEIN SYNTHESIS INHIBITORS: MACROLIDES MOA is the same as Lincomycins Erythromycin – Saccharopolyspora erythraea Clarithromycin – Methylated erythromycin Roxithromycin and Troleandomycin Telithromycin Azithromycin – more active against G- PROTEIN SYNTHESIS INHIBITORS: Streptogramins and Other drugs Streptogramins Quinupristin-Dalfopristin – a combination of 2 streptogramins used as a bactericidal by binding to 50S Oxazolidinones Linezolid – binds to 23S ribosomal RNA of the 50S subunit, FOLIC ACID SYNTHESIS INHIBITORS: Sulfonamides Broad Spectrum Bacteriostatic MOA: Inhibits Dihydropteroate synthase Given with folate reductase inhibitors (Trimethoprim or Pyrimethamine) FOLIC ACID SYNTHESIS INHIBITORS: Sulfonamides Oral Absorbable Agents: Sulfisoxazole and Sulfamethoxazole Sulfadiazine (+pyrimethamine) Sulfadoxine (+pyrimethamine) Oral Non-Absorbable – Sulfasalazine Topical Agents – Sodium sulfacetamide, Mefenide, and Silver Sulfadiazine DNA GYRASE INHIBITORS: FLUOROQUINOLONES 1st Gen UTI Antibiotic Broad Spec (More G-) Bactericidal MOA: Inhibits super coiling of the DNA DNA GYRASE INHIBITORS: FLUOROQUINOLONES 1st Gen: Nalidixic acid, Norfloxacin, and Cinoxacin 2nd Gen: Ciprofloxacin, Pefloxacin, Comefloxacin, Lomefloxacin, Ofloxacin, Norfloxacin, and Enoxacin 3rd Gen: Levofloxacin, Gatifloxacin, Sparfloxacin, and Gemifloxacin 4th Gen: Trovafloxacin, Alatrofloxacin, and Moxifloxacin ANTI-MYCOBACTERIALS: ANTI-TB DRUGS ANTI-MYCOBACTERIALS: ANTI-TB DRUGS Isoniazid – Inhibits mycolic acid synthesis (waxy substance in cell wall) Rifampicin – Inhibits RNA polymerase Ethambutol – inhibits arabinosyl acyltransferase Causes optic neuritis red-green color blindness ANTI-MYCOBACTERIA: DRUGS FOR LEPROSY Dapsone 4,4-diamine-diphenyl sulfone Same MOA as sulfonamides Combination with: Rifampicin Clofazimine – For dapsone resistant strains of M. leprae ANTIHERPES DRUGS Acyclovir and Valacyclovir guanosine analog against herpes simplex virus and varicella zoster Vidarabine, Famiciclovir, Peniciclovir, Docusanol, Trifluridine, Interferon-α , Idoxuridine/Iododeoxyuridine ANTI-CYTOMEGALOVIRUS Gancyclovir and Valgancyclovir Also a guanosine analog Cidofovir and Foscarnet ANTI-INFLUENZA Amantadine and Rimantadine inhibit an early step in replication of the influenza A (but not influenza B) virus Prevents”uncoating” of viruses Oseltamivir and Zanamivir inhibitors of neuraminidases produced by influenza A and B and are currently active against both H3N2 and H1N1 strains. ANTI-HEPATITIS Interferon-α (IFN-α) - degrades viral mRNA and promotes NK cells Lamivudine and Telbivudine – inhibitor of HIV reverse transcriptase Adefovir dipivoxil and Entacavir – Inhibits HBV DNA polymerase Ribavirin – Inhibits the replication of a wide range of DNA and RNA viruses ANTI-MALARIAL DRUGS CINCHONA ALKALOIDS Quinine and Quinidine 4-AMINOQUINOLINES Chloroquine Hydroxychloroquine Mefloquine ANTI-MALARIAL DRUGS 8-AMINOQUINOLINES Primaquine Polycyclics Doxycycline Halofantrine ANTI-MALARIAL DRUGS Artemisinin Family Artemisinin, Artemether, Artesunate, Dihydroartemisinin, Artemotil Fixed Combinations Sulfadoxine and Pyrimethamine Atovaquone and Proguanil  ANTI-AMEOBIC AGENTS TISSUE AMEBICIDES (Chloroquine, Emetines, Metronidazole, Tinidazole) act on organisms in the bowel wall and the liver LUMINAL AMEBICIDES (Diloxanide Furoate, Iodoquinol, Paromomycin) act only in the lumen of the bowel ANTI-LEISHMANIAL AGENTS Sodium Stibogluconate – DOC for all forms Meglumine Antimonate Pentamidine ANTIFUNGAL SYSTEMIC MYCOSES Ampotericin B Binds to ergosterol and forms pores by disrupting ergosterol synthesis DOC for systemic infections Same MOA as Nystain and Natamycin (Polyene Antibiotics) Flucytosine – Converted to 5-FU that inhibits DNA and RNA symthesis ANTIFUNGAL SYSTEMIC MYCOSES Azoles – Inhibits lanosterol C-14 demethylase Classified as: Imidazoles – Miconazole (+Hydrocortisone), Clotrimoxazole, Ketoconazole, Tioconazole Triazoles – Itraconazole, Voriconazole, Fluconazole, and Posaconazole Antifungals: Systemic Drugs for Mucocutaneous Infections Griseofulvin – Inhibits microtubule synthesis – Source: Pennicillium griseofulvum – DOC: Trichophyton, Epidermophyton, and Microsporum ringworms Terbinafine – Inhibits squalene epoxidase – Same MOA as Allylamines (Naftidfine and Tolnaftate) Antifungals: Topical Agents Nystatin – DOC for local and superficial candidiasis. Natamycin Topical Azoles Whitefield’s Ointment – Benzoic an Salicylic acid Tolnaftate – Squalene epoxidase inhibitor Akapulko Fatty acid Derivatives: Propionic acid, Zn Propionate, Na Caprylate, Zn Caprylate, and Undecylenic acid Anti-typanosomal Agents: African Sleeping Sickness Pentamidine – used in the hemolymphatic stages of disease caused by Trypanosoma gambiense and T rhodesiense Suramin – DOC for for early stages Melarsoprol – For advance stages Eflornithine - This agent, a suicide substrate of ornithine decarboxylase, is effective in some forms of African trypanosomiasis Anti-typanosomal Agents: American Sleeping Sickness Nifurtimox ▪ Alternative agent in African forms of the disease, and has also been effective in mucocutaneous leishmaniasis. ▪ Nitrofurazone derivative ▪ Inhibits the parasite-unique enzyme trypanothione reductase. Benzidazole highly effective in early disease this decreases in those who have long term infection ANTI-HELMINTHICS: Nematodes Mebendazole – selectively inhibits microtubule synthesis and glucose uptake DOC for Nematodes except for S. stercoralis, W. bancrofti, O. volvulus and C. philippinensis Thiabendazole – structural congener of mebendazole and has a similar action on microtubules with inhibition on helminth specific fumarate reductase ANTI-HELMINTHICS: Nematodes Ivermectin – intensifies GABA-mediated neurotransmission in nematodes DOC for S. stercoralis and O. volvulus Albendazole – inhibition of microtubule assembly Diethylcarbamazine – immobilizes microfilariae DOC for several filarial infections except O. volvulus Pyrantel pamoate Piperazine Citrate Pyrivinium Pamoate ANTI-HELMINTHICS: Trematodes Praziquantel – has a wide spectrum including both trematodes and cestodes DOC for trematodes except for Fasciola hepatica Increase calcium permeability Niclosamide – uncoupling oxidative phosphorylation or by activating ATPases. Bithionol – codrug of choice (with triclabendazole) for treatment of F. Hepatica ANTI-HELMINTHICS: Trematodes Metrifonate – organophosphate for urinary schistosomiasis Oxamniquine – effective solely in Schistosoma mansoni infections (intestinal bilharziasis), acting on male immature forms and adult schistosomal forms. ANTI-HELMINTHICS: Cestodes Prazyquantel – DOC for Cestodes except Cysticercosis and Hydatid Disease Albendazole – DOC for Cysticercosis and Hydatid Disease Niclosamide ALCOHOLS Alcohol USP (Ethanol) / Spiritus vini rectificatus/ Wine Spirit/ Grain Alcohol – ≥160 Proof; Potency increases with MW Denatured Alcohol Completely Denatured Alcohol Specialized Denatured Alcohol Isopropyl Alcohol ALDEHYDES AND GAS STERILANTS ALDEHYDES Formaldehyde Glutaraldehyde GAS STERILANTS Ethylene oxide, Propylene oxide, Betapropiolactone and Chlorine dioxide PHENOL DERIVATIVES Phenol – Standard for all disinfectants. – MOA: Precipitates proteins (low conc) and lyse bacterial cell wall (high conc); does not kill spores – Phenol Coefficient: Ratio of disinfectant conc to phenol conc to kill a strain of microorganism (eg. Salmonella typhi) Liquefied Phenol p-chlorophenol p-chloro-m-xylenol Hexachorphene Bisphenol Cresol Thymol, Eugenol, Resorcinol and Hexylresorcinol HALOGEN CONTAINING COMPOUNDS IODOPHORES Iodine Tincture Iodine Solution Strong Iodine Solution/ Lugol’s Solution Povidone-Ioine Chlorine Containing compounds – Releases HOCl Halzone Chlorazodin Oxychlorosene OXIDIZING AGENTS MOA: Generates oxygen and oxygen radicals Weak solutions (3%) Strong solutions (25%) INORGANIC AGENTS - KMnO4, H2O2, NaBO2, Metal peroxides, etc ORGANIC AGENTS – Carbamide and Benzoyl peroxide CATIONIC SURFACTANTS Quaternary Ammonium Compounds MOA: Dissolved in microbial cell membrate causing estabilization and lysis Inactivated by Soaps and anionic detergents Benzalkonium Chloride Benzathonium and Methylbenzationium chloride Cetylpyridinium chloride Chlorhexidine  CATIONIC SURFACTAN TS SOAP, DETERGENTS AND HEAVY METALS SOAPS AND DETERGENTS MOA: Removes soil and grease containing microbes. May also act as surfactants HEAVY METALS – Protein precipitants by binding to SH groups NITROMERAOL AND THIMEROSAL DYES Gentian Violet/ Crystal Violet – For yeast infection Basic Fuchsin – For ringworm and athlete’s foot Methylene Blue – Reducing agent, antidote for CN poisoning, bacteriostatic for urethritis and cystisis. Also used for vital nerve staining Oncology drugs  Rank Cancer (2018 new cases; both sexes) Onlocogy 1 2 Lung Breast 3 Colorectal Worldwide Cancer Data 4 Prostate Most common cancer 5 Stomach worldwide: lung and breast 6 Liver cancer (12.3% each, 2018) 7 Esophagus 3rd most common: colorectal cancer (1.8M cases in 2018) 8 Cervix uteri 9 Thyroid 10 Bladder CANCER Refers to a heterogeneous group of diseases caused by an impairment of the normal functioning of genes, which leads to genetic damage Classification of agents