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Pharmacology

VITAMIN -K

  • Group of lipophilic, hydrophobic vitamins.
  • Needed for the post-translational modification of coagulation proteins.
  • Phylloquinone (vitamin K1) is the major dietary form of vitamin K.
  • Vitamin K2 (menaquinone, menatetrenone) is produced by bacteria in the intestines.

Immunosuppressive drugs are essential in managing various medical conditions, particularly in preventing organ transplant rejection and treating autoimmune diseases. They can be classified into five main groups:

  1. Glucocorticoids: These are steroid hormones that reduce inflammation and suppress the immune response. They work by inhibiting the production of inflammatory cytokines and reducing the proliferation of immune cells. Common glucocorticoids include prednisone and dexamethasone. Their effects include:

    • Mechanism of Action: Glucocorticoids inhibit the expression of genes coding for pro-inflammatory cytokines (e.g., IL-1, IL-2, TNF-α).

    • Clinical Uses: They are used in conditions like rheumatoid arthritis, lupus, and to prevent transplant rejection.

    • Side Effects: Long-term use can lead to osteoporosis, weight gain, diabetes, and increased risk of infections.

  2. Cytostatic Drugs: These agents inhibit cell division and are often used in cancer treatment as well as in autoimmune diseases. They include:

    • Examples: Cyclophosphamide, azathioprine, and methotrexate.

    • Mechanism of Action: They interfere with DNA synthesis and cell proliferation, particularly affecting rapidly dividing cells.

    • Clinical Uses: Effective in treating cancers, systemic lupus erythematosus, and other autoimmune disorders.

    • Side Effects: Can cause bone marrow suppression, leading to increased risk of infections and anemia.

  3. Antibodies: This group includes monoclonal and polyclonal antibodies that target specific components of the immune system.

    • Types:

      • Monoclonal Antibodies: Such as basiliximab and daclizumab, which target the IL-2 receptor to prevent T-cell activation.
      • Polyclonal Antibodies: These are derived from multiple B-cell clones and can broadly suppress immune responses.
    • Clinical Uses: Used in organ transplantation and to treat autoimmune diseases.

    • Side Effects: Risk of infections and allergic reactions due to immune suppression.

  4. Drugs Acting on Immunophilins: These drugs modulate immune responses by binding to immunophilins, which are proteins that assist in the folding of other proteins.

    • Examples: Cyclosporine and tacrolimus.

    • Mechanism of Action: They inhibit calcineurin, a phosphatase involved in T-cell activation, thereby reducing the production of IL-2.

    • Clinical Uses: Primarily used in organ transplantation to prevent rejection.

    • Side Effects: Nephrotoxicity, hypertension, and increased risk of infections.

  5. Other Drugs: This category includes various agents that do not fit neatly into the other classifications but still have immunosuppressive effects.

    • Examples: Mycophenolate mofetil and sirolimus.

    • Mechanism of Action: Mycophenolate inhibits lymphocyte proliferation by blocking purine synthesis, while sirolimus inhibits mTOR, affecting T-cell activation and proliferation.

    • Clinical Uses: Used in transplant patients and in some autoimmune diseases.

    • Side Effects: Gastrointestinal disturbances, increased risk of infections, and potential for malignancies.

Estimation of the risk of anesthesia (American Society of Anesthesiologists scale)

• ASA 1: healthy patient.

• ASA 2: patient with stable, treated illness like arterial hypertension, diabetes melitus, asthma bronchiale, obesity

• ASA 3: patient with systemic illness decreasing sufficiency like heart illness, late infarct

• ASA 4: patient with serious illness influencing his state like renal insuficiency, unstable hypertension, circulatory insuficiency

• ASA 5: patient in life treatening illness

• ASA 6: brain death- potential organ donor

Piroxicam:

Half‐life of 45 hrs. Once‐daily dosing. Delay onset of  action.

High doses inhibits PMN migration, decrease oxygen  radical production, inhibits lymphocyte function. 

used to relieve the symptoms of  arthritis, primary dysmenorrhoea, pyrexia; and as an analgesic,non-selective  cyclooxygenase (COX) inhibitor

The risk of adverse side efects is nearly ten times higher than with other NSAIDs. Peptic ulcer (9.5 higher)

Neomycin

used as a topical preparation

Neomycin is not absorbed from the gastrointestinal tract, and has been used as a preventative measure for hepatic encephalopathy and hypercholesterolemia. By killing bacteria in the intestinal tract, it keeps ammonia levels low and prevents hepatic encephalopathy, especially prior to GI surgery. It is not given intravenously, as neomycin is extremely nephrotoxic (it causes kidney damage), especially compared to other aminoglycosides.

Operator position

For the right-handed operator, the 8 and 10 o’clock position and for left-handed operators, the corresponding 2 and 4 o’clock position almost always allows for optimal visualization of the injection field.

Oxyphenbutazone: one of the metabolites of  phenylbutazone. Apazone.  Similar to  phenylbutazone, but less likely to cause  agranulocytosis

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