Five-Mark Answer Points: Short Hints for Easy Scoring

Five-Mark Answer Points: Short Hints for Easy Scoring

UNIT 1: DRUGS ACTING ON GIT

1. Classification of anti-ulcer drugs

Anti-ulcer drugs are classified as:

A. Gastric acid secretion inhibitors
-H₂ blockers: Cimetidine, Ranitidine
-Proton pump inhibitors: Omeprazole, Pantoprazole
B. Antacids
-Systemic: Sodium bicarbonate
-Non-systemic: Aluminium hydroxide, Magnesium hydroxide
C. Ulcer protectives
-Sucralfate, Colloidal bismuth subcitrate
D. Prostaglandin analogues
-Misoprostol
-Used in peptic ulcer disease and GERD.

2. H₂-receptor antagonists

Mechanism: Block H₂ receptors on parietal cells → ↓ gastric acid secretion.
Uses: Peptic ulcer, GERD, Zollinger–Ellison syndrome.
Adverse effects: Gynecomastia (cimetidine), diarrhea, headache.
Drugs: Cimetidine, Ranitidine, Famotidine.

3. Proton pump inhibitors (PPIs)

Mechanism: Irreversibly inhibit H⁺/K⁺-ATPase pump → profound acid suppression.
Uses: Peptic ulcer, GERD, H. pylori eradication.
Adverse effects: Hypomagnesemia, osteoporosis, diarrhea.
Examples: Omeprazole, Pantoprazole.

4. Antacids

Neutralize gastric acid and increase pH.
Types:
a) Systemic: Sodium bicarbonate,
b) Non-systemic: Aluminium hydroxide, Magnesium trisilicate
Uses: Acid peptic disorders.
Adverse effects: Constipation (Al), diarrhea (Mg).

5. Prostaglandin analogues

Drug: Misoprostol
Mechanism: ↑ mucus & bicarbonate secretion, ↓ acid secretion.
Uses: NSAID-induced ulcers.
Adverse effects: Diarrhea, uterine contractions.

6. Laxatives

Classification:

a) Bulk forming: Ispaghula

b) Stool softeners: Liquid paraffin

c) Stimulant purgatives: Senna, Bisacodyl

d) Osmotic purgatives: Lactulose

Uses: Constipation, bowel preparation.

7. Osmotic purgatives

Draw water into intestine → bowel distension → peristalsis.
Drugs: Lactulose
Uses: Chronic constipation, hepatic encephalopathy.
Adverse effects: Flatulence, diarrhea.

8. Antidiarrhoeal drugs

Classification:

 a) ORS and Zinc

 b) Opioids: Loperamide

 c) Adsorbents: Ispaghula

 d) ORS: Prevents dehydration. 

 e) Zinc: Reduces duration and severity.

9. Opioid antidiarrhoeals

Mechanism: ↓ intestinal motility.
Drugs: Loperamide, Diphenoxylate
Adverse effects: Constipation, abdominal cramps.

10. Antiemetics (5-HT₃ antagonists)

Mechanism: Block serotonin receptors in CTZ.
Drugs: Ondansetron, Granisetron
Uses: Chemotherapy-induced vomiting.
Adverse effects: Headache, constipation.

11. Prokinetic drugs

Mechanism: ↑ GI motility by dopamine antagonism.
Drugs: Metoclopramide, Domperidone
Uses: GERD, gastroparesis.
Adverse effects: Extrapyramidal symptoms.

12. Antispasmodics

Mechanism: Reduce smooth muscle spasm.
Drugs: Dicyclomine, Drotaverine
Uses: IBS, colic.
Adverse effects: Dry mouth, blurred vision.

UNIT 2: PHARMACOLOGY OF ENDOCRINE DRUGS

13. Antithyroid drugs

Classification:

a) Thioamides: Propylthiouracil, Carbimazole

b) Ionic inhibitors: Thiocyanates

c) Iodides: NaI, KI

d) Radioactive iodine
Uses: Hyperthyroidism.

14. Propylthiouracil

Mechanism: Inhibits thyroid hormone synthesis and T₄→T₃ conversion.
Uses: Thyrotoxicosis.
Adverse effects: Agranulocytosis, hepatitis. 

15. Insulin preparations

Types: 

a) Short acting: Regular insulin

b) Intermediate: NPH

c) Long acting: Glargine

Uses: Type-1 and Type-2 diabetes. 

16. Oral hypoglycaemic agents

Classification:

a) Sulfonylureas: Glibenclamide

b) Biguanides: Metformin

c) Meglitinides: Repaglinide

d) DPP-4 inhibitors: Sitagliptin, Linagliptin

Used in Type-2 diabetes.

17. Sulfonylureas

Mechanism: Stimulate insulin release.
Uses: Type-2 diabetes.
Adverse effects: Hypoglycemia, weight gain.
Drugs: Glibenclamide, Glimepiride.

 

18. Metformin

Mechanism: ↓ hepatic glucose production.
Uses: Type-2 diabetes.
Adverse effects: Lactic acidosis, GI upset.

 

19. Corticosteroids

Classification:

a) Glucocorticoids

b) Mineralocorticoids

Examples: Hydrocortisone, Prednisolone.

20. Glucocorticoids

Uses: Inflammation, autoimmune diseases.
Adverse effects: Osteoporosis, Cushing’s syndrome.

 

21. Androgens and anabolic steroids

Promote male characteristics and protein synthesis.
Uses: Hypogonadism, anemia.
Adverse effects: Virilization, liver toxicity.

 

22. Uterine stimulants

Drugs: Oxytocin, Ergometrine, Misoprostol
Uses: Induction of labor, postpartum hemorrhage.

 

UNIT 3: ANTIMICROBIALS

23. Principles of antimicrobial therapy

Correct diagnosis, appropriate drug selection, correct dose & duration, avoid misuse.

 

24. Mechanism of action of antimicrobials

a) Cell wall synthesis inhibition

b) Protein synthesis inhibition

c) DNA synthesis inhibition

25. Antibiotic resistance

Occurs due to enzyme production, altered targets, decreased permeability.

 

26. Sulfonamides & cotrimoxazole

 Inhibit folic acid synthesis.
 Uses: UTIs, respiratory infections.
 Adverse effects: Stevens-Johnson syndrome.

 

27. Penicillin classification

Natural, semisynthetic, extended-spectrum, β-lactamase inhibitors.

 

28. Penicillin mechanism

Inhibits bacterial cell wall synthesis → bactericidal.

 

29. β-lactamase inhibitors

Clavulanic acid, Sulbactam protect β-lactam antibiotics.

 

30. Cephalosporins

 Classified into generations.
 Third generation: Ceftriaxone used in severe infections.

 

31. Aminoglycosides

 Inhibit protein synthesis.
 Adverse effects: Nephrotoxicity, ototoxicity.

 

32. Tetracyclines

Broad-spectrum antibiotics.
Contraindicated: Pregnancy, children.

 

33. Chloramphenicol

Adverse effects: Aplastic anemia, gray baby syndrome.

 

34. Macrolides

Inhibit protein synthesis.
Drugs: Erythromycin, Azithromycin.

 

35. Quinolones

Inhibit DNA gyrase.
Drugs: Ciprofloxacin, Levofloxacin.

 

36. Antitubercular drugs

INH, Rifampicin, Pyrazinamide, Ethambutol.

 

37. DOTS

Directly Observed Treatment Short-course for TB control.

 

38. Antifungal drugs

Amphotericin-B disrupts fungal cell membrane.

 

39. Antiviral drugs (HIV)

HAART uses combination therapy to suppress viral replication.

 

40. Pharmacology of Antitubercular Drugs

Antitubercular drugs are used in combination to treat tuberculosis and to prevent the development of drug resistance.

Classification:
First-line drugs: Isoniazid, Rifampicin, Pyrazinamide, Ethambutol, Streptomycin
Second-line drugs: Fluoroquinolones, Aminoglycosides (amikacin), Ethionamide, Cycloserine

Mechanism of Action:
Isoniazid: Inhibits mycolic acid synthesis → damages mycobacterial cell wall
Rifampicin: Inhibits DNA-dependent RNA polymerase → blocks RNA synthesis
Pyrazinamide: Active in acidic pH; disrupts membrane energy production
Ethambutol: Inhibits arabinosyl transferase → impairs cell wall synthesis
Streptomycin: Inhibits protein synthesis by acting on 30S ribosomal subunit

Pharmacokinetics (Brief):
Most drugs are well absorbed orally
Distributed widely, including lungs and CSF
Metabolized mainly in the liver and excreted via urine

Adverse Effects:
Hepatotoxicity (isoniazid, rifampicin, pyrazinamide)
Optic neuritis (ethambutol)
Ototoxicity (streptomycin)

Rationale for Combination Therapy:
Prevents resistance
Enhances bactericidal effect
Shortens treatment duration

Antitubercular drugs act at different targets of Mycobacterium tuberculosis and are used in combination for effective and safe TB management.

     

UNIT 4: IMMUNOSUPPRESSANTS & IMMUNOSTIMULANTS

41. Immunosuppressants

Calcineurin inhibitors, antiproliferative drugs, corticosteroids.

 

42. Cyclosporine

Inhibits T-cell activation.
Uses: Organ transplantation.
Adverse effects: Nephrotoxicity.

 

43. Corticosteroids as immunosuppressants

Suppress cytokine production and immune response.

 

44. Antiproliferative drugs

Azathioprine, Methotrexate inhibit lymphocyte proliferation.

 

45. Monoclonal antibodies

Muromonab-CD3 used in transplant rejection.

 

46. Immunostimulants

Enhance immune response.
Examples: BCG, Interferons.

 

47. Interferons

Used in viral infections and cancers.

 

48. BCG vaccine

Used in tuberculosis and bladder cancer.

BCG (Bacillus Calmette–Guérin) vaccine is a live attenuated vaccine used for the prevention of tuberculosis (TB), especially severe forms in children.

Source and Composition:
BCG vaccine is prepared from a weakened strain of Mycobacterium bovis.

Dose and Route: Given intradermally
Dose: 0.05 mL for infants (<1 year) and 0.1 mL for older children and adults
Common site: Left upper arm

Mechanism of Action:
BCG induces cell-mediated immunity, enhancing macrophage activity to protect against TB infection.
Advantages / Uses:
Prevents severe TB forms like tubercular meningitis and miliary TB
Part of national immunization programs in many countries

Adverse Effects:
Local ulcer and scar formation
Rarely lymphadenitis or keloid formation

BCG vaccine is safe and effective in reducing childhood TB morbidity and mortality.

49. Immunosuppressants vs Immunostimulants

Immunosuppressants and immunostimulants differ mainly in their effects on the immune system. Immunosuppressant’s are drugs that suppress or reduce immune responses and are commonly used in organ transplantation to prevent graft rejection and in autoimmune diseases to control excessive immune activity. They act by inhibiting the function of T-cells and B-cells and by reducing cytokine production. Common examples include cyclosporine, tacrolimus, azathioprine, and corticosteroids. Their major adverse effects include increased susceptibility to infections, risk of malignancy, and organ toxicities such as nephrotoxicity and hepatotoxicity. In contrast, immunostimulants are agents that enhance or stimulate the immune system and are used in conditions like immunodeficiency states, chronic infections, and as vaccines. They work by activating immune cells and promoting antibody and cytokine production. Examples include BCG vaccine, levamisole, and interferons. Adverse effects of immunostimulants may include fever, inflammation, and hypersensitivity reactions. Thus, immunosuppressants are used to control overactive immunity, while immunostimulants are used to strengthen weakened immune responses.

50. Adverse effects of immunosuppressants

Adverse Effects and Contraindications of Immunosuppressant Therapy

Immunosuppressant drugs are used to prevent organ transplant rejection and to treat autoimmune disorders by suppressing immune responses.
Adverse Effects:

1. Increased risk of infections due to suppression of immune defenses

2. Malignancies (especially lymphomas and skin cancers) with long-term use

3. Bone marrow suppression causing anemia, leukopenia, and thrombocytopenia

4. Organ toxicity – nephrotoxicity (cyclosporine), hepatotoxicity (azathioprine)

5. Metabolic disturbances such as hypertension, diabetes, osteoporosis (corticosteroids)
Contraindications:

1. Active infections (bacterial, viral, fungal)

2. Malignancy or history of cancer (relative contraindication)

3. Severe hepatic or renal impairment

4. Pregnancy and lactation (with some agents like mycophenolate)

5. Hypersensitivity to the drug Immunosuppressant therapy requires careful patient selection and monitoring due to serious adverse effects and specific contraindications.

51. Classify anticancer drugs with suitable examples.

Classification of Anticancer Drugs:
Alkylating agents Ex. Cyclophosphamide, Chlorambucil, Dacarbazine
Antimetabolites Ex. Methotrexate, 6-Mercaptopurine, 5-Fluorouracil
Plant-derived anticancer drugs Vinca alkaloids: Vincristine, Vinblastine
Taxanes: Paclitaxel
Antitumor antibiotics Ex. Doxorubicin, Daunorubicin, Bleomycin
Miscellaneous agents: Cisplatin, Carboplatin, Etoposide, L-Asparaginase

52. Explain the mechanism of action, therapeutic uses, and adverse effects of alkylating agents.
Mechanism of Action:
Alkylating agents form covalent bonds with DNA, leading to cross-linking of DNA strands, inhibition of DNA replication, and cell death. They are cell-cycle non-specific.

Therapeutic Uses:
Leukemias and lymphomas
Breast cancer
Ovarian cancer
Hodgkin’s and non-Hodgkin’s lymphoma

Adverse Effects:
Bone marrow suppression
Nausea and vomiting
Alopecia
Hemorrhagic cystitis (cyclophosphamide)
Increased risk of secondary malignancy

53. Describe antimetabolite anticancer drugs with special reference to methotrexate.

Antimetabolites:
They are structural analogues of normal metabolites required for DNA synthesis and inhibit cell proliferation during the S-phase.

Methotrexate:
Mechanism of Action:
Inhibits dihydrofolate reductase, preventing formation of tetrahydrofolate → inhibition of thymidine synthesis → impaired DNA synthesis.
Therapeutic Uses:
Acute lymphoblastic leukemia
Breast cancer
Choriocarcinoma
Autoimmune diseases (low dose)
Adverse Effects:
Bone marrow suppression
Oral ulcers
Hepatotoxicity
Nephrotoxicity

54. Discuss plant-derived anticancer drugs (vinca alkaloids and taxanes) with mechanisms and adverse effects.

Vinca Alkaloids (Vincristine, Vinblastine):
Mechanism:
Inhibit microtubule polymerization → arrest cells in M phase.
Uses:
Leukemia, lymphoma, testicular cancer
Adverse Effects:
Peripheral neuropathy (vincristine)
Bone marrow suppression (vinblastine)

Taxanes (Paclitaxel):
Mechanism:
Stabilizes microtubules and prevents depolymerization → inhibits mitosis.
Uses:
Breast cancer
Ovarian cancer
Adverse Effects:
Myelosuppression
Alopecia
Hypersensitivity reactions



55. Explain the pharmacology of antitumor antibiotics, mentioning examples and toxicities.

Antitumor Antibiotics:
These drugs interfere with DNA function and are derived from Streptomyces species.

Examples and Mechanism:
Doxorubicin & Daunorubicin:
Intercalate into DNA and inhibit topoisomerase-II
Bleomycin:
Causes DNA strand breaks via free radical formation

Therapeutic Uses:
Leukemias
Lymphomas
Solid tumors (breast, testicular)

Toxicities:
Cardiotoxicity (doxorubicin)
Bone marrow suppression
Pulmonary fibrosis (bleomycin) Alopecia


                                                   END OF THE DOCUMENT

1. Chapters in Pharmacology

2. Strictly Syllabus-Based 50 Questions (5 marks each) from Pharmacology-III For Practice