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Dr. Ravi Mundugaru
Assistant Professor
Dept. of Pharmacology
AIMS, B.G. Nagar
Karnataka, India
 Derivative of sulphanilamide ( para-
aminobenzene sulphonamide) PABA
 Prontosil Red – first chemical to be effective
against Streptococcal septicemia
 Prontosil Red breaks inside body and release
active sulfonamide - AMA
Sulfonamides
Systemic
Acting
agents
Short
Acting
(4-8 hours)
Sulfadiazine
Intermediate
Acting
(8-12 hours)
Sulfamethoxazole
Long
Acting
(>7 Days)
Sulfadoxine
Sulfamethopyrazine
Local
Acting
agents
Sulfacetamide
Mafenide
Others
Sulfasalazine
 Well absorbed in small intestine
 Bound to plasma proteins (albumin)
 Distribute throughout the body and penetrate well
into CSF
 Pass the placental barrier and
enter fetal tissues.
 Sulfa drugs are acetylated in
the liver
 Eliminated by glomerular filtration
 Crystalluria
 Hypersensitivity
 Hemopoietic disturbances
 Kernicterus in newborns
 Hepatitis
 Sulfadoxine + Pyrimethamine – treat chloroquine resistant
malaria
 Sulfadiazine + Pyrimethamine – drug of choice for
toxoplasmosis
 Sulfamethoxazole +Trimethoprim – treat urinary &
respiratory tract infections
 Sulfacetamide – treat opthalmic infection
 Topical Sulfadiazine & mafenide – prevent infection on burn
surfaces
 Sulfonamides displace these drugs from
protein binding site and increase their free
form in plasma:
 Phenytoin
 Warfarin
 Tolbutamide
 It isWorld Health Organization (WHO)
approved fixed-dose combination of
sulphamethoxazole and trimethoprim in the
ratio 5:1
 >50000 times more active against bactierial
DHFRase
 It produces sequential blockade
 Individually both are
bacteriostatic but the
combination has cidal
effect
 Chances of
development of
bacterial resistance are
also reduced
 Well absorbed after oral administration
 Widely distributed
 Metabolized in liver
 Excreted in urine
 Skin rashes
 GI disturbances
 Megaloblastic anaemia
 Bone marrow suppression
 C/I in pregnancy
 UrinaryTract Infections -Treatment of
uncomplicated lower urinary tract infections
 Respiratory tract infection: Upper and lower
respiratory tract infection, otitis media
caused by Gram+ve cocci and H.influenza
 Pneumocystis jeroveci infection in AIDS
patients
 Bacterial dysentery and diarrhoea caused
by Shigella, E.coli, Campylobacter
 Chancroid
Thankyou

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Sulfonamide- AIMS.pptx

  • 1. Dr. Ravi Mundugaru Assistant Professor Dept. of Pharmacology AIMS, B.G. Nagar Karnataka, India
  • 2.  Derivative of sulphanilamide ( para- aminobenzene sulphonamide) PABA  Prontosil Red – first chemical to be effective against Streptococcal septicemia  Prontosil Red breaks inside body and release active sulfonamide - AMA
  • 3.
  • 4. Sulfonamides Systemic Acting agents Short Acting (4-8 hours) Sulfadiazine Intermediate Acting (8-12 hours) Sulfamethoxazole Long Acting (>7 Days) Sulfadoxine Sulfamethopyrazine Local Acting agents Sulfacetamide Mafenide Others Sulfasalazine
  • 5.  Well absorbed in small intestine  Bound to plasma proteins (albumin)  Distribute throughout the body and penetrate well into CSF  Pass the placental barrier and enter fetal tissues.  Sulfa drugs are acetylated in the liver  Eliminated by glomerular filtration
  • 6.  Crystalluria  Hypersensitivity  Hemopoietic disturbances  Kernicterus in newborns  Hepatitis
  • 7.  Sulfadoxine + Pyrimethamine – treat chloroquine resistant malaria  Sulfadiazine + Pyrimethamine – drug of choice for toxoplasmosis  Sulfamethoxazole +Trimethoprim – treat urinary & respiratory tract infections  Sulfacetamide – treat opthalmic infection  Topical Sulfadiazine & mafenide – prevent infection on burn surfaces
  • 8.  Sulfonamides displace these drugs from protein binding site and increase their free form in plasma:  Phenytoin  Warfarin  Tolbutamide
  • 9.  It isWorld Health Organization (WHO) approved fixed-dose combination of sulphamethoxazole and trimethoprim in the ratio 5:1  >50000 times more active against bactierial DHFRase  It produces sequential blockade
  • 10.
  • 11.  Individually both are bacteriostatic but the combination has cidal effect  Chances of development of bacterial resistance are also reduced
  • 12.  Well absorbed after oral administration  Widely distributed  Metabolized in liver  Excreted in urine
  • 13.  Skin rashes  GI disturbances  Megaloblastic anaemia  Bone marrow suppression  C/I in pregnancy
  • 14.  UrinaryTract Infections -Treatment of uncomplicated lower urinary tract infections  Respiratory tract infection: Upper and lower respiratory tract infection, otitis media caused by Gram+ve cocci and H.influenza  Pneumocystis jeroveci infection in AIDS patients  Bacterial dysentery and diarrhoea caused by Shigella, E.coli, Campylobacter  Chancroid

Editor's Notes

  1. Kernicterus is a bilirubin-induced brain dysfunction. Bilirubin is a highly neurotoxic substance that may become elevated in the serum, a condition known as hyperbilirubinemia. Hyperbilirubinemia may cause bilirubin to accumulate in the gray matter of the central nervous system, potentially causing irreversible neurological damage.  Crystalluria refers to crystals found in the urine when performing a urine test. 
  2. Toxoplasmosis is a parasitic disease caused by the protozoan Toxoplasma gondii.[1] The parasite infects most genera of warm-blooded animals, including humans, but the primary host is the felid (cat) family. Animals are infected by eating infected meat, by ingestion of feces of a cat that has itself recently been infected, and by transmission from mother to fetus. Cats are the primary source of infection to human hosts, although contact with raw meat, especially lamb, is a more significant source of human infections in some countries. Fecal contamination of hands is a significant risk factor.
  3. Megaloblastic anemia (or megaloblastic anaemia) is an anemia (ofmacrocytic classification) that results from inhibition of DNA synthesis duringred blood cell production.[1] When DNA synthesis is impaired, the cell cyclecannot progress from the G2 growth stage to the mitosis (M) stage. This leads to continuing cell growth without division, which presents as macrocytosis. 
  4. Otitis media is the medical term formiddle ear infection. Pneumocystis jirovecii is a yeast-like fungus of the genus Pneumocystis. The causative organism of Pneumocystis pneumonia, it is an important human pathogen, particularly among immunocompromised hosts.  Chancroid (also known as soft chancre[1] and ulcus molle[2]) is a bacterialsexually transmitted infection characterized by painful sores on the genitalia. Chancroid is known to spread from one individual to another solely through sexual contact.