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Sulfonamide

Sulfonamide

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Sulfonamide

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  1. Sulfonamide • Sulfonamide drugs were the first antimicrobial drugs, and paved the way for the antibiotic revolution in medicine. The first sulfonamide was trade named Prontosil, which is a prodrug • Sulfonamidochrysoidine (KI-730), first synthesized by Bayer chemists Josef Klarer and Fritz Mietzsch, was tested and found effective against some important bacterial infections in mice by Gerhard Domagk, who subsequently received the 1939 Nobel Prize in Medicine. Prontosil was the result of five years of research and testing involving thousands of compounds related to azo dyes.

  2. Sulfanilamida • Jacques and Thérèse Trefouel and their team at the French Pasteur Institute found in 1936 that prontosil is metabolized to sulfanilamide (para-aminophenylsulfonamide), a much simpler, colorless molecule, redefining Prontosil as a prodrug. Prontylin became the first oral version of sulfanilamide by Bayer. • Its synthesis had been first reported by Paul Gelmo, a chemistry student working at the University of Vienna in his 1909 thesis, but he had not realized its medical potential.

  3. Acidul folic

  4. Elixir Sulfanilamide - the excipient DEG was responsible for the fatal adverse effects.

  5. Gerhardt Domagk • Born30 October 1895Lagow, Brandenburg • Died24 April 1964 (aged 68) Burgberg • Nationality Germany • Fields bacteriology • Alma materUniversity of Kiel • Known for Prontosil • Notable awards1939, Nobel Prize in Medicine

  6. Medical ethics • Nazi human experimentation was a series of medical experiments on large numbers of prisoners by the GermanNazi regime in its concentration camps during World War II. Prisoners were coerced into participating: they did not willingly volunteer and there was never informed consent. Typically, the experiments resulted in death, disfigurement or permanent disability. • From about July 1942 to about September 1943, experiments to investigate the effectiveness of sulfonamide, a synthetic antimicrobial agent, were conducted at Ravensbrück.[15] Wounds inflicted on the subjects were infected with bacteria such as Streptococcus, Clostridium perfringens (the causative agent in gas gangrene) and Clostridium tetani, the causative agent in tetanus.[16] • After the war, these crimes were tried at what became known as the Doctors' Trial, and revulsion at the abuses perpetrated led to the development of the Nuremberg Code of medical ethics.

  7. Bayer AG has discovered, among others:Aspirin — an analgesic, anti-fever, and anti-coagulant medicine, arguably the most commercially successful drug ever Heroin (diacetylmorphine) — an addictive drug, originally sold as a cough treatment. Heroin was a Bayer trademark, until World War I Prontosil as the first sulfonamide

  8. Sulfamide antidiabetice • Sulfonylurea (UK: Sulphonylurea) derivatives are a class of antidiabetic drugs that are used in the management of diabetes mellitustype 2 ("adult-onset"). They act by increasing insulin release from the beta cells in the pancreas.

  9. Sulfamide diuretice – tiazide, furosemid, indapamida

  10. Sulfamide dermatologice - Sulfacetamida, Mafenid • Sulfacetamide 10% topical lotion, sold under the brand name Klaron or Ovace, is approved for the treatment of acne and seborrheic dermatitis.[1] When combined with sulfur, it is sold under the brand name PLEXION and AVAR, which contain 10% sulfacetamide and 5% sulfur. • Mafenide (INN; usually as mafenide acetate, trade name Sulfamylon) is a sulfonamide. It is used to treat severe burns

  11. Sulfamide antiinflamatoare • Sulfasalazine (brand name Azulfidine in the U.S., Salazopyrin in Europe) is a sulfa drug, a derivative of mesalazine (also called 5-aminosalicylic acid, or 5-ASA), used primarily as an anti-inflammatory agent in the treatment of inflammatory bowel disease as well as for rheumatoid arthritis. It may be abbreviated SSZ. It is not a pain killer. • Celecoxib (INN) (pronounced /sɛlɨˈkɒksɪb/) is a sulfanon-steroidal anti-inflammatory drug (NSAID) used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis. It is marketed by Pfizer. It is known under the brand nameCelebrex or Celebra for arthritis and Onsenal for polyps. Celecoxib is available by prescription in capsule form.

  12. Sulfamide antivirale • Darunavir (brand name Prezista, formerly known as TMC114) is a drug used to treat HIV infection. It is in the protease inhibitor class. Prezista is an OARAC recommended treatment option for treatment-naïve and treatment-experienced adults and adolescents[1]. Developed by pharmaceutical company Tibotec, darunavir is named after Arun K. Ghosh, the chemist who discovered the molecule at the University of Illinois at Chicago. It was approved by the Food and Drug Administration (FDA) on June 23, 2006.[2] • As other antivirals, darunavir does not cure HIV infection or AIDS, and does not prevent passing HIV to others. • The drug costs around $9000 for a one year supply

  13. Sulfamide uricosurice – probenecid(benuril) • Uricosuricmedications (drugs) are substances that increase the excretion of uric acid in the urine, thus reducing the concentration of uric acid in blood plasma. Generally, this effect is achieved by action on the proximal tubule. Drugs that reduce blood uric acid are not all uricosurics; blood uric acid can be reduced by other mechanisms

  14. Sulfamide heteterociclice anticonvulsivante • Acetazolamide, sold under the trade name Diamox, is a carbonic anhydrase inhibitor that is used to treat glaucoma, epileptic seizures, benign intracranial hypertension (pseudotumor cerebri), altitude sickness, cystinuria, and dural ectasia. Acetazolamide is available as a generic drug and is also used as a diuretic. • Acetazolamide is sometimes taken prophylactically, anywhere between 125 milligrams (mg) to 500 mg per day, starting a few days before going to the higher altitude. Such use is recommended for those ascending from sea level to 3000 meters (9800 feet) in one day, or for those ascending more than 600 meters (2000 feet) per day once above an altitude of 2500 meters (8200 feet).[8][9] Also, prophylactic use is recommended for those with a significant history of acute mountain sickness. • The drug forces the kidneys to excrete bicarbonate, the conjugate base of carbonic acid. By increasing the amount of bicarbonate excreted in the urine, the blood becomes more acidic.[9] Acidifying the blood stimulates ventilation, which increases the amount of oxygen in the blood. • Ethoxzolamide (alternatively known as Ethoxyzolamide) is a sulfonamidemedication that functions as a carbonic anhydrase inhibitor. It is used in the treatment of glaucoma, duodenalulcers, and as a diuretic. It may also be used in the treatment of some forms of epilepsy.

  15. Short acting sulfonamide • Sulfisomidine (INN), also known as sulphasomidine (BAN until 2003),[1]sulfamethin and sulfaisodimidine, is a sulfonamideantibacterial. It is closely related to sulfadimidine. • (A British Approved Name (BAN) is the official non-proprietary or generic name given to a pharmaceuticalsubstance, as defined in the British Pharmacopoeia (BP). The BAN is also the official name used in many countries across the world, especially those of the Commonwealth of Nations • Sulfanilamida • Sulfaisodimidine · Sulfamethizole · Sulfadimidine · Sulfapyridine · Sulfafurazole · Sulfanilamide (Prontosil) · Sulfathiazole · Sulfathiourea

  16. Intermediate-acting sulfonamide • Sulfadiazina - Silver sulfadiazine is a sulfa derivative[1]topicalantibacterial historically used as a topical burn cream on second- and third-degree burns • Sulfamethoxazole (abbreviated SMX[1][2] and less reliably[3]SMZ[4][5][6]) is a sulfonamidebacteriostaticantibiotic. It is most often used as part of a synergistic combination with trimethoprim in a 5:1 ratio in co-trimoxazole (abbreviated SXT, SMX-TMP and SMZ-TMP,[7] or TMP-SMX and TMP-SMZ), also known under trade names such as Bactrim, Septrin, or Septra. • Sulfamethoxazole ·Sulfadiazine# ·Sulfamoxole

  17. Long acting sulfonamide • Sulfadimethoxine (trade name Di-Methox, Albon) is a sulfonamideantibiotic. Albon is produced by Pfizer Animal Health and is available as a oral suspension, tablet or bolus. It is used to treat many infections including treatment of respiratory, urinary tract, enteric, and soft tissue infections.[1] It is most frequently used in veterinary medicine. Sulfadimethoxine inhibits bacterial synthesis of folic acid (pteroylglutamic acid) from para-aminobenzoic acid • Sulfadoxine (also spelled sulphadoxine) is an ultra-long-lasting sulfonamide often used in combination with pyrimethamine to treat or prevent malaria.[1] It is also used, usually in combination with other drugs, to treat or prevent various infections in livestock.[ • Sulfadimethoxine ·Sulfalene ·Sulfametomidine ·Sulfametoxydiazine ·Sulfamethoxypyridazine ·Sulfaperin ·Sulfamerazine ·Sulfaphenazole ·Sulfamazone

  18. Sulfatiazol

  19. Sulfafurazol • Sulfafurazole (INN, also known as sulfisoxazole) is a sulfonamideantibacterial with an oxazole substituent. It has antibiotic activity against a wide range of Gram-negative and Gram-positive organisms. It is sometimes given in combination with erythromycin or phenazopyridine. It is used locally in a 4% solution or ointment.

  20. Sulfametoxazol • Sulfamethoxazole (abbreviated SMX[1][2] and less reliably[3]SMZ[4][5][6]) is a sulfonamidebacteriostaticantibiotic. It is most often used as part of a synergistic combination with trimethoprim in a 5:1 ratio in co-trimoxazole (abbreviated SXT, SMX-TMP and SMZ-TMP,[7] or TMP-SMX and TMP-SMZ), also known under trade names such as Bactrim, Septrin, or Septra. Its primary activity is against susceptible forms of Streptococcus, Staphylococcus aureus (including MRSA), Escherichia coli, Haemophilus influenzae, and oralanaerobes. It is commonly used to treat urinary tract infections. In addition can be used as an alternative to amoxicillin-based antibiotics to treat sinusitis.

  21. Trimetoprim • Trimethoprim was commonly (since1969 in the UK-GlaxoSmithKline ) used in a 1:5 combination with sulfamethoxazole, a sulfonamide antibiotic, which inhibits an earlier step in the folate synthesis pathway (see diagram above). This combination, also known as co-trimoxazole, TMP-sulfa, or TMP-SMX, results in an in vitrosynergistic antibacterial effect by inhibiting successive steps in folate synthesis. This claimed benefit was not seen in general clinical use.[2][3]

  22. Biseptol

  23. Trimetoprim –Stenbuck, P.; Hood, H. M.; 1962, U.S. Patent 3,049,544

  24. Mescalina • Mescaline or 3,4,5-trimethoxyphenethylamine is a naturally-occurringpsychedelicalkaloid of the phenethylamine class. It is mainly used as an entheogen, and a tool to supplement various practices for transcendence, including in meditation, psychonautics, art projects, and psychedelic psychotherapy. • It occurs naturally in the peyote cactus (Lophophora williamsii),[1] the San Pedro cactus (Echinopsis pachanoi) and the Peruvian Torch cactus (Echinopsis peruviana), and in a number of other members of the Cactaceae.