NEET MDS Lessons
Pharmacology
Uses of NSAIDs
NSAIDs are usually indicated for the treatment of acute or chronic conditions where pain and inflammation are present. Research continues into their potential for prevention of colorectal cancer, and treatment of other conditions, such as cancer and cardiovascular disease.
NSAIDs are generally indicated for the symptomatic relief of the following conditions.
rheumatoid arthritis, osteoarthritis, inflammatory arthropathies (e.g. ankylosing spondylitis, psoriatic arthritis, Reiter's syndrome), acute gout, dysmenorrhoea, metastatic bone pain ,headache and migraine, postoperative pain, mild-to-moderate pain due to inflammation and tissue injury, pyrexia, renal colic
Aspirin, the only NSAID able to irreversibly inhibit COX-1, is also indicated for inhibition of platelet aggregation; an indication useful in the management of arterial thrombosis and prevention of adverse cardiovascular events.
SYMPATHOMIMETICS
β2 -agonists are invariably used in the symptomatic treatment of asthma.
Epinephrine and ephedrine are structurally related to the catecholamine norepinephrine, a neurotransmitter of the adrenergic nervous system
Some of the important β 2 agonists like salmeterol, terbutaline and salbutamol are invariably used as bronchodilators both oral as well as
aerosol inhalants
SALBUTAMOL
It is highly selective β2 -adrenergic stimulant h-aving a prominent bronchodilator action.
It has poor cardiac action compared to isoprenaline.
TERBUTALINE
It is highly selective β2 agonist similar to salbutamol, useful by oral as well as inhalational route.
SALMETEROL
Salmeterol is long-acting analogue of salbutamol
BAMBUTEROL
It is a latest selective adrenergic β2 agonist with long plasma half life and given once daily in a dose of 10-20 mg orally.
METHYLXANTHINES (THEOPHYLLINE AND ITS DERIVATIVES)
THEOPHYLLINE
Theophylline has two distinct action:
smooth muscle relaxation (i.e. bronchodilatation) and suppression of the response of the airways to stimuli (i.e. non-bronchodilator prophylactic effects).
ANTICHOLINERGICS
Anticholinergics, like atropine and its derivative ipratropium bromide block cholinergic pathways that cause airway constriction.
MAST CELL STABILIZERS
SODIUM CROMOGLYCATE
It inhibits degranulation of mast cells by trigger stimuli.
It also inhibits the release of various asthma provoking mediators e.g. histamine, leukotrienes, platelet activating factor (PAF) and interleukins (IL’s) from mast cell
KETOTIFEN
It is a cromolyn analogue. It is an antihistaminic (H1 antagonist) and probably inhibits airway inflammation induced by platelet activating factor (PAF) in primate.
It is not a bronchodilator. It is used in asthma and symptomatic relief in atopic dermatitis, rhinitis, conjunctivitis and urticaria.
LEUKOTRIENE PATHWAY INHIBITORS
MONTELUKAST
It is a cysteinyl leukotriene receptor antagonist indicated for the management of persistent asthma.
Aquaretics
An aquaretic is a class of drug that is used to promote aquaresis, the excretion of water without electrolyte loss.
Lithium, demeclocycline
Mechanism of Action
1. Block ADH action on distal tubule and collecting duct. Blocking ADH decreases H2O permeability. H2O is not recovered (distal tubule) using osmotic draw of counter-current multiplier so aquaretics reduce water reabsorption (tubule to blood stream).
2. Net effect is an increase in free water clearance
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:
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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:
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Mechanism of Action: Glucocorticoids inhibit the expression of genes coding for pro-inflammatory cytokines (e.g., IL-1, IL-2, TNF-α).
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Clinical Uses: They are used in conditions like rheumatoid arthritis, lupus, and to prevent transplant rejection.
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Side Effects: Long-term use can lead to osteoporosis, weight gain, diabetes, and increased risk of infections.
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Cytostatic Drugs: These agents inhibit cell division and are often used in cancer treatment as well as in autoimmune diseases. They include:
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Examples: Cyclophosphamide, azathioprine, and methotrexate.
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Mechanism of Action: They interfere with DNA synthesis and cell proliferation, particularly affecting rapidly dividing cells.
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Clinical Uses: Effective in treating cancers, systemic lupus erythematosus, and other autoimmune disorders.
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Side Effects: Can cause bone marrow suppression, leading to increased risk of infections and anemia.
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Antibodies: This group includes monoclonal and polyclonal antibodies that target specific components of the immune system.
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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.
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Clinical Uses: Used in organ transplantation and to treat autoimmune diseases.
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Side Effects: Risk of infections and allergic reactions due to immune suppression.
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Drugs Acting on Immunophilins: These drugs modulate immune responses by binding to immunophilins, which are proteins that assist in the folding of other proteins.
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Examples: Cyclosporine and tacrolimus.
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Mechanism of Action: They inhibit calcineurin, a phosphatase involved in T-cell activation, thereby reducing the production of IL-2.
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Clinical Uses: Primarily used in organ transplantation to prevent rejection.
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Side Effects: Nephrotoxicity, hypertension, and increased risk of infections.
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Other Drugs: This category includes various agents that do not fit neatly into the other classifications but still have immunosuppressive effects.
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Examples: Mycophenolate mofetil and sirolimus.
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Mechanism of Action: Mycophenolate inhibits lymphocyte proliferation by blocking purine synthesis, while sirolimus inhibits mTOR, affecting T-cell activation and proliferation.
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Clinical Uses: Used in transplant patients and in some autoimmune diseases.
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Side Effects: Gastrointestinal disturbances, increased risk of infections, and potential for malignancies.
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Clotrimazole: Clotrimazole is a potent, specific inhibitor of p450 enzymes.
It is used in some antifungal medications, and in the treatment of yeast infections.
Cough is a protective reflex which helps in expulsion of respiratory secretion or foreign particles which are irritant to respiratory
tract. Irritation to any part of respiratory tract starting from pharynx to lungs carried impulses by afferent fibres in vagus and
sympathetic nerve to the cough centre in the medulla oblongata. \
Cough may be dry (without sputum or unproductive) or productive (with sputum production).
Classification for drugs used in cough.
I. Pharyngeal demulcents
Certain lozenges, linctus and cough drops containing glycerine, liquorice and syrups.
II. Expectorants
Sodium and potassium citrate
Sodium and potassium acetate
Potassium iodide
Ammonium chloride & carbonate
Acetylcysteine
Bromhexine
Guaiphenesin
III. Antitussive
i. Opioids
Codeine (as linctus) Pholcodeine
ii. Non-opioids
Noscapine
Dextromethorphan
Pipazethate
iii. Antihistaminics
Chlorpheniramine
Diphenhydramine
Promethazine
Erdosteine is recently introduced mucolytic with unique protective functions for the respiratory tract. It is indicated in the treatment of acute and chronic airway diseases such as bronchitis, rhinitis, sinusitis, laryngopharyngitis and exacerbations of chronic bronchitis.
Midazolam -Intravenous Anesthetics
Midazolam is a benzodiazepine used for preoperative sedation, induction of anesthesia, or maintenance of anesthesia in short procedures.