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"Macrolides"? Classify Each Drug in This Chapter As a Macrolide Or Azalide, and As an Antibiotic Or Semi-Synthetic Derivative
STUDY GUIDE THE MACROLIDE/AZALIDE ANTIMICROBIAL AGENTS 1. Why are these antibiotics derivatives called "macrolides"? Classify each drug in this chapter as a macrolide or azalide, and as an antibiotic or semi-synthetic derivative. 2. What are the key structural differences between erythromycin, clarithromycin, azithromycin and dirithromycin? 3. Generally how does spiramycin and josamycin differ in structure from the commercial macrolides/azalides (2 reasons)? 4. What are the “ketolides and how do they differ in structure from the commercial macrolides? 5. What is the biosynthetic source of erythromycin? What is the lactone moiety of erythromycin called? What sugar moieties are present and what are their properties? 6. What hydrolysis product forms from erythromycin in aqueous acid or base? What is the significance of this reaction? Can it occur with other macrolides? 7. When does the “intramolecular cyclization” reaction occur with erythromycin? What is it's significance (two reasons) and how does it occur? Which functional groups are important for this reaction? 8. What salt forms of erythromycin are available? Which are water soluble? Which are water-insoluble? How is each salt form formulated and used (oral or parenteral)? 9. What ester and ester salt derivatives of erythromycin are available? What is the estolate? How is each salt form formulated and used (oral or parenteral)? What are the advantages of these esters dosage forms? 10. How does clarithromycin differ in structure from erythromycin? Why was this macrolide developed (the role of the 6-methoxy)? 11. How does azithromycin differ in structure from erythromycin? Why was this macrolide developed? 12. How does dirithromycin differ in structure from erythromycin? Why was this macrolide developed? What is the active form of this prodrug? 13. -
35 Cyproterone Acetate and Ethinyl Estradiol Tablets 2 Mg/0
PRODUCT MONOGRAPH INCLUDING PATIENT MEDICATION INFORMATION PrCYESTRA®-35 cyproterone acetate and ethinyl estradiol tablets 2 mg/0.035 mg THERAPEUTIC CLASSIFICATION Acne Therapy Paladin Labs Inc. Date of Preparation: 100 Alexis Nihon Blvd, Suite 600 January 17, 2019 St-Laurent, Quebec H4M 2P2 Version: 6.0 Control # 223341 _____________________________________________________________________________________________ CYESTRA-35 Product Monograph Page 1 of 48 Table of Contents PART I: HEALTH PROFESSIONAL INFORMATION ....................................................................... 3 SUMMARY PRODUCT INFORMATION ............................................................................................. 3 INDICATION AND CLINICAL USE ..................................................................................................... 3 CONTRAINDICATIONS ........................................................................................................................ 3 WARNINGS AND PRECAUTIONS ....................................................................................................... 4 ADVERSE REACTIONS ....................................................................................................................... 13 DRUG INTERACTIONS ....................................................................................................................... 16 DOSAGE AND ADMINISTRATION ................................................................................................ 20 OVERDOSAGE .................................................................................................................................... -
RIFAMPICIN Productinformation Sigma Prod
RIFAMPICIN ProductInformation Sigma Prod. No. R3501 CH3 CH3 CAS NUMBER: 13292-46-1 HO SYNONYMS: Tubocin; Sinerdol; Rimactan; L-5103; Dione-21 Acetate; Archidyn; Arficin; 3-(4- CH3 O O OH O Methylpiperazinyliminomethyl)-rifamycin SV; NSC 113926; C OH OH CH 1 2 3 H C Rifampin ; Rifaldazine; Rifamycin AMP H3C 3 O NH H3C PHYSICAL PROPERTIES: CH3 N CH N Appearance: Orange-brown to red-brown powder.3 O OH N Molecular formula: C43H58N4O12 O Molecular weight: 823.0 O CH3 CH3 EmM (max absorbance, phosphate buffer, pH 7.38): 33.20 (237 nm); 32.10 (255 nm); 27.00 (334 nm); 15.40 (475 nm)2,4 pKa (in water):1.7 (4-hydroxyl group), 7.9 (4-piperazine nitrogen); in methylcellosolve-water (4:1): 3.6 (4- hydroxyl group), 6.7 (3-piperazine nitrogen)4 pI (in water): 4.84 25° 4 Optical rotation: [α]D =+10.6° (c=0.5% in CDCl3) Melting point: 183-188°C (dec.)2,4 METHOD OF PREPARATION: Methods of preparation have been reported.4,5 The NMR, UV, IR, Mass spectra, Thin-Layer chromatography and HPLC methods of detection have been reported.4,5,6 A colorimetric test for identification was reported.4 STABILITY / STORAGE: Rifampicin (Rif) should be stable for at least two years when stored desiccated at -20°C and protected from light.3 Rif is stable as a solid at temperatures up to 70EC.4 SOLUBILITY / SOLUTION STABILITY: Rif is soluble in dimethylsulfoxide (~100mg/mL), dimethylformamide, methanol (16 mg/ml, 25EC), chloroform (349 mg/ml, 25°C), ethyl acetate (108 mg/ml, 25°C), and acetone (14 mg/ml, 25°C).4,6,7,8,9 Rif is slightly soluble in water at 25°C: 2.5 mg/ml, pH 7.3; 1.3 mg/ml, pH 4.3; and in 95% ethanol (∼10 mg/mL).4 Rif is soluble at 37°C: in 0.1 N HCl, 200 mg/ml and in phosphate buffer pH 7.4, 9.9 mg/ml.4 R3501 Page 1 of 4 03/28/97 - ARO RIFAMPICIN Sigma Prod. -
Erythromycin Versus Tetracycline for Treatment of Mediterranean Spotted Fever
Arch Dis Child: first published as 10.1136/adc.61.10.1027 on 1 October 1986. Downloaded from Archives of Disease in Childhood, 1986, 61, 1027-1029 Erythromycin versus tetracycline for treatment of Mediterranean spotted fever T MUNOZ-ESPIN, P LOPEZ-PARtS, E ESPEJO-ARENAS, B FONT-CREUS, I MARTINEZ- VILA, J TRAVERIA-CASANOVA, F SEGURA-PORTA, AND F BELLA-CUETO Hospital de Sant Llatzer, Terrassa, Clinica Infantil del Nen Jesus, Sabadell, and Hospital Mare de Deu de la Salut, Sabadell, Barcelona, Spain SUMMARY Eighty one children aged between 1 and 13 years participated in a randomised comparative trial of tetracycline hydrochloride and erythromycin stearate for treatment of Mediterranean spotted fever. Both therapeutic regimens proved effective, but in patients treated with tetracycline both clinical symptoms and fever disappeared significantly more quickly. Likewise, when those patients who began treatment within the first 72 hours of illness are considered the febrile period had a significantly shorter duration in the group treated with tetracycline. One patient was switched to tetracycline because there was no improvement of clinical manifestations, with persistence of fever, myalgias, and prostration, after receiving eight days of treatment with erythromycin. These results suggest that tetracyclines are superior to erythromycin in the treatment of Mediterranean spotted fever. copyright. Mediterranean spotted fever is an acute infectious were not included in the trial; neither were those disease caused by Rickettsia conorii. During the -
MIRENA Data Sheet Vx3.0, CCDS 25 1
NEW ZEALAND DATA SHEET 1. PRODUCT NAME MIRENA 52 mg intrauterine contraceptive device (release rate: 20 microgram/24 hours) 2. QUALITATIVE AND QUANTITATIVE COMPOSITION MIRENA is an intrauterine system (IUS) containing 52 mg levonorgestrel. For details of release rates, see Section 5.2. For the full list of excipients, see Section 6.1. 3. PHARMACEUTICAL FORM MIRENA consists of a white or almost white drug core covered with an opaque membrane, which is mounted on the vertical stem of a T-body. The vertical stem of the levonorgestrel intrauterine system is loaded in the insertion tube at the tip of the inserter. Inserter components are an insertion tube, plunger, flange, body and slider. The white T-body has a loop at one end of the vertical stem and two horizontal arms at the other end. Brown coloured removal threads are attached to the loop. The T-body of MIRENA contains barium sulfate, which makes it visible in X-ray examination. The IUS and inserter are essentially free from visible impurities. 4. CLINICAL PARTICULARS 4.1 Therapeutic indications Contraception Treatment of idiopathic menorrhagia provided there is no underlying pathology. Prevention of endometrial hyperplasia during estrogen replacement therapy MIRENA Data Sheet Vx3.0, CCDS 25 1 4.2 Dose and method of administration MIRENA is inserted into the uterine cavity. One administration is effective for five years. The in vivo dissolution rate is approximately 20 microgram/24 hours initially and is reduced to approximately 18 microgram/24 hours after 1 year and to 10 microgram/24 hours after five years. The mean dissolution rate of levonorgestrel is about 15 microgram /24 hours over the time up to five years. -
Supplementary Materials
Supplementary Materials Table S1. The significant drug pairs in potential DDIs examined by the two databases. Micromedex Drugs.com List of drugs paired PK-PD Mechanism details 1. Amiodarone— PD Additive QT-interval prolongation Dronedarone 2. Amiodarone— PK CYP3A inhibition by Ketoconazole Ketoconazole 3. Ciprofloxacin— PD Additive QT-interval prolongation Dronedarone 4. Cyclosporine— PK CYP3A inhibition by Cyclosporine Dronedarone 5. Dronedarone— PK CYP3A inhibition by Erythromycin Erythromycin 6. Dronedarone— PD Additive QT-interval prolongation Flecainide 7. Dronedarone— PK CYP3A4 inhibition by Itraconazole Itraconazole 8. Dronedarone— PK Contraindication Major CYP3A inhibition by Ketoconazole Ketoconazole 9. Dronedarone— PD Additive QT-interval prolongation Procainamide PD 10. Dronedarone—Sotalol Additive QT-interval prolongation 11. Felodipine— PK CYP3A inhibition by Itraconazole Itraconazole 12. Felodipine— PK CYP3A inhibition by Ketoconazole Ketoconazole 13. Itraconazole— PK CYP3A inhibition by Itraconazole Nisoldipine 14. Ketoconazole— PK CYP3A inhibition by Ketoconazole Nisoldipine 15. Praziquantel— PK CYP induction by Rifampin Rifampin PD 1. Amikacin—Furosemide Additive or synergistic toxicity 2. Aminophylline— Decreased clearance of PK Ciprofloxacin Theophylline by Ciprofloxacin 3. Aminophylline— PK Decreased hepatic metabolism Mexiletine 4. Amiodarone— PD Additive effects on QT interval Ciprofloxacin 5. Amiodarone—Digoxin PK P-glycoprotein inhibition by Amiodarone 6. Amiodarone— PD, PK Major Major Additive effects on QT Erythromycin prolongation, CYP3A inhibition by Erythromycin 7. Amiodarone— PD, PK Flecainide Antiarrhythmic inhibition by Amiodarone, CYP2D inhibition by Amiodarone 8. Amiodarone— PK CYP3A inhibition by Itraconazole Itraconazole 9. Amiodarone— PD Antiarrhythmic inhibition by Procainamide Amiodarone 10. Amiodarone— PK CYP induction by Rifampin Rifampin PD Additive effects on refractory 11. Amiodarone—Sotalol potential 12. Amiodarone— PK CYP3A inhibition by Verapamil Verapamil 13. -
PROCUR Why Procur Has Been Prescribed for You
Consumer Medicine Information Ask your doctor if you have any questions about PROCUR why Procur has been prescribed for you. Cyproterone acetate 50 mg and 100 mg tablets This medicine is available only with a doctor's prescription. What is in this leaflet Before you take Procur Please read this leaflet carefully before you start taking Procur When you must not take it This leaflet answers some common questions about Procur. It does not contain all the available Do not take Procur if you have an allergy to: information. It does not take the place of talking • any medicine containing cyproterone acetate to your doctor or pharmacist. • any of the ingredients listed at the end of this leaflet All medicines have risks and benefits. Your doctor has weighed the risks of you taking Procur against Some of the symptoms of an allergic reaction may the benefits they expect it will have for you. include: • difficulty in breathing or wheezing If you have any concerns about taking this • shortness of breath medicine, ask your doctor or pharmacist. • swelling of the face, tongue, lips, or other parts of the body Keep this leaflet with the medicine. You may • hives on the skin, rash, or itching need to read it again. Do not take Procur if: What Procur is used for • you are allergic to cyproterone acetate or any other ingredient listed at the end of this leaflet Procur tablets contain the active ingredient • you are pregnant cyproterone acetate. Cyproterone acetate is an • you are breastfeeding antiandrogen. It works by blocking the actions of • you suffer from liver diseases (including sex hormones (androgens) that are produced previous or existing liver tumours, Dubin- mainly in men but also, to a lesser extent in Johnson syndrome or Rotor syndrome) women. -
Diagnosis and Treatment of Tinea Versicolor Ronald Savin, MD New Haven, Connecticut
■ CLINICAL REVIEW Diagnosis and Treatment of Tinea Versicolor Ronald Savin, MD New Haven, Connecticut Tinea versicolor (pityriasis versicolor) is a common imidazole, has been used for years both orally and top superficial fungal infection of the stratum corneum. ically with great success, although it has not been Caused by the fungus Malassezia furfur, this chronical approved by the Food and Drug Administration for the ly recurring disease is most prevalent in the tropics but indication of tinea versicolor. Newer derivatives, such is also common in temperate climates. Treatments are as fluconazole and itraconazole, have recently been available and cure rates are high, although recurrences introduced. Side effects associated with these triazoles are common. Traditional topical agents such as seleni tend to be minor and low in incidence. Except for keto um sulfide are effective, but recurrence following treat conazole, oral antifungals carry a low risk of hepato- ment with these agents is likely and often rapid. toxicity. Currently, therapeutic interest is focused on synthetic Key Words: Tinea versicolor; pityriasis versicolor; anti “-azole” antifungal drugs, which interfere with the sterol fungal agents. metabolism of the infectious agent. Ketoconazole, an (J Fam Pract 1996; 43:127-132) ormal skin flora includes two morpho than formerly thought. In one study, children under logically discrete lipophilic yeasts: a age 14 represented nearly 5% of confirmed cases spherical form, Pityrosporum orbicu- of the disease.3 In many of these cases, the face lare, and an ovoid form, Pityrosporum was involved, a rare manifestation of the disease in ovale. Whether these are separate enti adults.1 The condition is most prevalent in tropical tiesN or different morphologic forms in the cell and semitropical areas, where up to 40% of some cycle of the same organism remains unclear.: In the populations are affected. -
Erythromycin* Class
Erythromycin* Class: Macrolide Overview Erythromycin, a naturally occurring macrolide, is derived from Streptomyces erythrus. This macrolide is a member of the 14-membered lactone ring group. Erythromycin is predominantly erythromycin A, but B, C, D and E forms may be included in preparations. These forms are differentiated by characteristic chemical substitutions on structural carbon atoms and on sugars. Although macrolides are generally bacteriostatic, erythromycin can be bactericidal at high concentrations. Eighty percent of erythromycin is metabolically inactivated, therefore very little is excreted in active form. Erythromycin can be administered orally and intravenously. Intravenous use is associated with phlebitis. Toxicities are rare for most macrolides and hypersensitivity with rash, fever and eosinophilia is rarely observed, except with the estolate salt. Erythromycin is well absorbed when given orally. Erythromycin, however, exhibits poor bioavailability, due to its basic nature and destruction by gastric acids. Oral formulations are provided with acid-resistant coatings to facilitate bioavailability; however these coatings can delay therapeutic blood levels. Additional modifications produced better tolerated and more conveniently dosed newer macrolides, such as azithromycin and clarithromycin. Erythromycin can induce transient hearing loss and, most commonly, gastrointestinal effects evidenced by cramps, nausea, vomiting and diarrhea. The gastrointestinal effects are caused by stimulation of the gastric hormone, motilin, which -
Drug Delivery Systems on Leprosy Therapy: Moving Towards Eradication?
pharmaceutics Review Drug Delivery Systems on Leprosy Therapy: Moving Towards Eradication? Luíse L. Chaves 1,2,*, Yuri Patriota 2, José L. Soares-Sobrinho 2 , Alexandre C. C. Vieira 1,3, Sofia A. Costa Lima 1,4 and Salette Reis 1,* 1 Laboratório Associado para a Química Verde, Rede de Química e Tecnologia, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, 4050-313 Porto, Portugal; [email protected] (A.C.C.V.); slima@ff.up.pt (S.A.C.L.) 2 Núcleo de Controle de Qualidade de Medicamentos e Correlatos, Universidade Federal de Pernambuco, Recife 50740-521, Brazil; [email protected] (Y.P.); [email protected] (J.L.S.-S.) 3 Laboratório de Tecnologia dos Medicamentos, Universidade Federal de Pernambuco, Recife 50740-521, Brazil 4 Cooperativa de Ensino Superior Politécnico e Universitário, Instituto Universitário de Ciências da Saúde, 4585-116 Gandra, Portugal * Correspondence: [email protected] (L.L.C.); shreis@ff.up.pt (S.R.) Received: 30 October 2020; Accepted: 4 December 2020; Published: 11 December 2020 Abstract: Leprosy disease remains an important public health issue as it is still endemic in several countries. Mycobacterium leprae, the causative agent of leprosy, presents tropism for cells of the reticuloendothelial and peripheral nervous system. Current multidrug therapy consists of clofazimine, dapsone and rifampicin. Despite significant improvements in leprosy treatment, in most programs, successful completion of the therapy is still sub-optimal. Drug resistance has emerged in some countries. This review discusses the status of leprosy disease worldwide, providing information regarding infectious agents, clinical manifestations, diagnosis, actual treatment and future perspectives and strategies on targets for an efficient targeted delivery therapy. -
Managing Drug Interactions in the Treatment of HIV-Related Tuberculosis
Managing Drug Interactions in the Treatment of HIV-Related Tuberculosis National Center for HIV/AIDS, Viral Hepatitis, STD, and TB Prevention Division of Tuberculosis Elimination Managing Drug Interactions in the Treatment of HIV-Related Tuberculosis Centers for Disease Control and Prevention Office of Infectious Diseases National Center for HIV/AIDS, Viral Hepatitis, STD, and TB Prevention Division of Tuberculosis Elimination June 2013 This document is accessible online at http://www.cdc.gov/tb/TB_HIV_Drugs/default.htm Suggested citation: CDC. Managing Drug Interactions in the Treatment of HIV-Related Tuberculosis [online]. 2013. Available from URL: http://www.cdc.gov/tb/TB_HIV_Drugs/default.htm Table of Contents Introduction 1 Methodology for Preparation of these Guidelines 2 The Role of Rifamycins in Tuberculosis Treatment 4 Managing Drug Interactions with Antivirals and Rifampin 5 Managing Drug Interactions with Antivirals and Rifabutin 9 Treatment of Latent TB Infection with Rifampin or Rifapentine 10 Treating Pregnant Women with Tuberculosis and HIV Co-infection 10 Treating Children with HIV-associated Tuberculosis 12 Co-treatment of Multidrug-resistant Tuberculosis and HIV 14 Limitations of these Guidelines 14 HIV-TB Drug Interaction Guideline Development Group 15 References 17 Table 1a. Recommendations for regimens for the concomitant treatment of tuberculosis and HIV infection in adults 21 Table 1b. Recommendations for regimens for the concomitant treatment of tuberculosis and HIV infection in children 22 Table 2a. Recommendations for co-administering antiretroviral drugs with RIFAMPIN in adults 23 Table 2b. Recommendations for co-administering antiretroviral drugs with RIFAMPIN in children 25 Table 3. Recommendations for co-administering antiretroviral drugs with RIFABUTIN in adults 26 ii Introduction Worldwide, tuberculosis is the most common serious opportunistic infection among people with HIV infection. -
WSAVA List of Essential Medicines for Cats and Dogs
The World Small Animal Veterinary Association (WSAVA) List of Essential Medicines for Cats and Dogs Version 1; January 20th, 2020 Members of the WSAVA Therapeutic Guidelines Group (TGG) Steagall PV, Pelligand L, Page SW, Bourgeois M, Weese S, Manigot G, Dublin D, Ferreira JP, Guardabassi L © 2020 WSAVA All Rights Reserved Contents Background ................................................................................................................................... 2 Definition ...................................................................................................................................... 2 Using the List of Essential Medicines ............................................................................................ 2 Criteria for selection of essential medicines ................................................................................. 3 Anaesthetic, analgesic, sedative and emergency drugs ............................................................... 4 Antimicrobial drugs ....................................................................................................................... 7 Antibacterial and antiprotozoal drugs ....................................................................................... 7 Systemic administration ........................................................................................................ 7 Topical administration ........................................................................................................... 9 Antifungal drugs .....................................................................................................................