1. General Pharmacological Principles
    2. 1. Introduction, Routes of Drug Administration
    2. Pharmacokinetics: Membrane Transport, Absorption and Distribution of Drugs
    3. Pharmacokinetics: Metabolism and Excretion of Drugs, Kinetics of Elimination
    4. Pharmacodynamics: Mechanism of Drug Action; Receptor Pharmacology
    5. Aspects of Pharmacotherapy, Clinical Pharmacology and Drug Development
    6. Adverse Drug Effects
  2. Drug Acting on Autonomic Nervous System
    3. 7. Cholinergic Transmission and Cholinergic Drugs
    8. Anticholinergic Drugs and Drugs Acting on Autonomic Ganglia
    9. Adrenergic Transmission and Adrenergic Drugs
    10. Antiadrenergic Drugs (Adrenergic Receptor Antagonists) and Drugs for Glaucoma
  3. Autacoids and Related Drugs
    4. 11. Histamine and Antihistaminics
    12. 5-Hydroxytryptamine, its Antagonists and Drug Therapy of Migraine
    13. Prostaglandins, Leukotrienes (Eicosanoids) and Platelet Activating Factor
    14. Nonsteroidal Antiinflammatory Drugs and Antipyretic-Analgesics
    15. Antirheumatoid and Antigout Drugs
  4. Respiratory System Drugs
    5. 16. Drugs for Cough and Bronchial Asthma
  5. Hormones and Related Drugs
    6. 17. Anterior Pituitary Hormones
    18. Thyroid Hormones and Thyroid Inhibitors
    19. Insulin, Oral Antidiabetic Drugs and Glucagon
    20. Corticosteroids
    21. Androgens and Related Drugs, Drugs for Erectile Dysfunction
    22. Estrogens, Progestins and Contraceptives
    23. Oxytocin and Other Drugs Acting on Uterus
    24. Hormones and Drugs affecting Calcium balance
  6. Drugs acting on Peripheral nervous system
    7. 25. Skeletal muscle relaxants
    26. Local anaesthetics
  7. Drugs acting on Central nervous system
    8. 27. General anaesthetics
    28. Ethyl and Methyl alcohols
    29. Sedative-Hypnotics
    30. Antiepileptic Drugs
    31. Antiparkinsonian Drugs
    32. Drugs used in Mental Illness: Antipsychotic and Antimanic drugs
    33. Drugs used in Mental Illness: Antidepressant and Antianxiety drugs
    34. Opioid analgesics and antagonists
    35. CNS stimulants and Cognitino enhancers
  8. Cardiovascular drugs
    9. 36. Drugs affecting Renin-Angiotensin system
    37. Nitric oxide and Vasoactive peptide signal molecules
    38. Cardiac glycosides and Drugs for Heart failure
    39. Antiarrhythmic drugs
    40. Antianginal and other Anti-ischaemic drugs
    41. Antihypertensive drugs
  9. Drugs acting on Kidney
    10. 42. Diuretics
    43. Antidiuretics
  10. Drugs affecting blood and Blood formation
    11. 44. Haematinics and Erythropoietin
    45. Drugs affecting Coagulation, Bleeding and Thrombosis
    46. Hypolipidaemic drugs
  11. Gastrointestinal drugs
    12. 47. Drugs for Pepric ulcer and gastroesophageal reflux disease
    48. Antiemetic, Prokinetic and Digestant drugs
    49. Drugs for Constipation and Diarrhoea
  12. Antimicrobial drugs
    13. 50. Antimicrobial drugs: General considerations
    51. Sulfonamides, Cotrimoxazole and Quinolones
    52. Beta-lactam antibiotics
    53. Tetracyclines and Chloramphenicol (Broad-spectrum antibiotics)
    54. Aminoglycosides antibiotics
    55. Macrolide, Lincosamide, Glycopeptide and Other antibacterial antibiotics; Urinary antiseptics
    56. Antitubercular Drugs
    57. Antileprotic Drugs
    58. Antifungal drugs
    59. Antiviral drugs (Non-retroviral)
    60. Antiviral drugs (Anti-retrovirus)
    61. Antimalarial drugs
    62. Antiamoebic and Other antiprotozoal drugs
    63. Antihelmintic drugs
  13. Chemotherapy of Neoplastic diseases
    14. 64. Anticancer drugs
  14. Miscellaneous drugs
    15. 65. Immunosuppressant drugs
    66. Drugs acting on Skin and Mucous membranes
    67. Antiseptics, Disinfectants and Ectoparasiticides
    68. Chelating agents
    69. Vitamins
    70. Vaccine, Antisera and Immunoglobulins
    71. Drug interactions
Antimicrobial drugs
51. Sulfonamides, Cotrimoxazole and Quinolones
SULFONAMIDES
▢ MOA: Selectively inhibits Folate reductase enzyme of bacteria.
▢ Classification:
▢ Uses:
❖ Sulfonamide +Pyramethamine:
  1. Toxoplasmosis
  2. Resistant malaria
❖ Sulfonamide + Trimethoprim (@SEPTRAN):
  1. STD's
    1. Chancroid
    2. Lymphogranuloma venereum
  2. Enteritis (Diarrhoea)
    1. E. coli
    2. Shigella
    1. Pneumocystis carina
    2. Pneumocystis jiroveci
  4. Typhoid
  5. Respiratory Tract Infection
  6. Acute uncomplicated UTI
  7. Nocardia
▢ Adverse effects (@ABC RASH):
  1. Aplastic anaemia
  2. Bile salt displacement -> Kernicterus
  3. Crystalluria
  4. Rash
  5. Acetylation
  6. SLE
  7. Haemolysis in G-6-PD deficient individuals
1. Longest acting sulfonamide is
  • Sulfadiazine
  • Sulfadoxine
  • Sulfamethoxazole
  • Sulfamethiazole
2. Mechanism of action of Sulfonamide is
  • Inhibit bacterial cell wall synthesis
  • Inhibits translocation of mRNA
  • Inhibit folate synthesis
  • Inhibits bacterial respiration
3. Sulfonamide injection causes decrease in folic acid by
  • Competitive inhibition
  • Non-competitive inhibition
  • Uncompetitive inhibition
  • Allosteric inhibition
4. Thymidine is responsible for resistance to which antibiotic
  • Erythromycin
  • Sulfonamide
  • Tetracycline
  • Nitrofurantoin
5. All of the following are topically used sulfonamides except
  • Sulfacetamide
  • Sulfadiazine
  • Silver sulfadiazine
  • Mafenide
6. Which of the following is topical sulfonamide
  • Sulfadoxine
  • Mafenide
  • Sulfamethopyrazine
  • None
7. Which of the following is side effect of Sulfonamide
  • Constipation
  • Joint pain
  • Crystalluria
  • Hyperkalamia
8. In unconjugated hyperbilirubinemia, the risk of Kernicterus increases with the use of
  • Ceftriaxone
  • Phenobarbitone
  • Ampicillin
  • Sulfonamide
TRIMETHOPRIM
▢ MOA: Selectively inhibits Dihydrofolate reductase (DHFR) enzyme of bacterial.
COTRIMOXAZOLE
▢ Introduction:
  1. Fixed dose combination of
    1. Sulfamethoxazole and
    2. Trimethoprim
  2. Combination ratio in drugs => Sulfamethoxazole:Trimethoprim=5:1
  3. Combination ratio reached in blood => Sulfamethoxazole:Trimethoprim=20:1
    1. Due to wider volume of distribution of trimethoprim
▢ Reasons for combination:
  1. Same half life of both i.e., ~10 hr.
  2. Synergistic action (Both are bacteriostatic individually but bactericidal in combination).
  3. Sequential blockage of 2 steps of Folic acid synthesis in bacteria.
    4. Image 1
  4. Different bioavailablity of 2 drugs i.e., 20:1.
  5. Slow resistance to the combination.
▢ Uses:
❖ Sulfonamide + Trimethoprim (@SEPTRAN):
  1. STD's
    1. Chancroid
    2. Lymphogranuloma venereum
  2. Enteritis (Diarrhoea)
    1. E. coli
    2. Shigella
    1. Pneumocystis carina
    2. Pneumocystis jiroveci
  4. Typhoid
  5. Respiratory Tract Infection
  6. Acute uncomplicated UTI
  7. Nocardia
▢ Adverse effects:
❖ General:
  1. Nausea, Vomiting, Stomatitis, Headache and Rashes
  2. Megaloblastic anaemia -> Due to folate deficiency
  3. Blood dyscrasias -> Rare
❖ Pregnancy: Teratogenic
❖ Renal disease patient: Uremia
❖ AIDS patient with Pneumocystis jiroveci infection: Fever, Rash, Bone marrow hypoplasia
❖ Elderly patient: Bone marrow toxicity
❖ Used with Diuretics: Thrombocytopenia
Note
  1. Trimethoprim adequately crosses Blood brain barrier and Placenta, while Sulfamethoxazole can't.
  2. Trimetoprim is more rapidly absorbed than Sulfamethoxazole.
  3. It doesn't affect absorption of Sulfamethoxazole.
  4. Plasma protein bound
    1. Trimethoprim → 40%
    2. Sulfamethoxazole → 60%
1. In cotrimoxazole, the ratio of Sulfamethoxazole and Trimethoprim is
  • 2:1
  • 1:1
  • 5:1
  • 1:5
2. Trimethoprim acts by
  • Inhibiting DHFR
  • Inhibiting Protein
  • Inhibiting cell wall
  • Inhibiting cell membrane
QUINOLONES
▢ Introduction:
Image 1
▢ MOA:
  1. Gram +ve bacteria -> Inhbits Topoisomerase IV
  2. Gram -ve bacteria -> Inhibits DNA gyrase (Mostly)
    1. DNA gyrase consists of 2 units A and B
    2. A -> Nicking and Resealing
    3. B -> Unwinding by introducing negative supercoils
    Note
    Mammalian cells possess Topoisomerase II which has low affinity with fluoroquinolones and thus less toxicity to host cells.
▢ Spectrum of activity: Wide spectrum
▢ Classification: