NEET MDS Lessons
Pharmacology
Carbenicillin
Antibiotic that is chemically similar to ampicillin. Active against gram-negative germs. It is well soluble in water and acid-labile.
NATURAL ANTICOAGULANTS:
1. PGI-2.
2. Antithrombin.
3. Protein-C.
4. TFPI.
5. Heparin.
6. Fibrinolytic system.
PHARYNGEAL DEMULCENTS
Administered in the form of lozenges, cough drops and cough linctus.
Produce soothing action on throat directly and by increasing the flow of saliva and provide symptomatic relief from dry cough.
EXPECTORANT
Expectorants are the drugs which increase the production of bronchial secretion and reduce its viscosity to facilitate its removal by coughing.
ANTITUSSIVES
They are central cough suppressants and act centrally to raise the threshold of cough centre and inhibit the cough reflex by suppressing the coordinating cough centre in the medulla oblongata.
Codeine - it depresses cough centre but is less constipating and abuse liability is low.
Pholcodeine is similar to codeine in efficacy and is longer acting. It has no analgesic or addicting property.
Noscapine is another opium alkaloid of benzylisoquinoline group. It is used as antitussive with no analgesic and drug abuse or drug dependence property.
Dextromethorphan is a synthetic compound and its dextroisomer is used as antitussive and is as effective as codeine
Pipazethate is another synthetic compound of phenothiazine category used as antitussive with little analgesic and sedative properties.
ANTIHISTAMINICS
They do not act on cough centre but provide relief due to their sedative and anticholinergic action.
BRONCHODILATORS
Bronchodilators are helpful in individuals with cough and bronchoconstriction due to bronchial hyperreactivity. They help by improving the effectiveness of cough in clearing secretions.
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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Inhalational Anesthetics
The depth of general anesthesia is directly proportional to the partial pressure of the anesthetic agent in the brain. These agents enter the body through the lungs, dissolve in alveolar blood and are transported to the brain and other tissues.
A. Rate of induction and rate of recovery from anesthesia:
1. The more soluble the agent is in blood, the more drug it takes to saturate the blood and the more time it takes to raise the partial pressure and the depth of anesthesia.
2. The less soluble the agent is in blood, the less drug it takes to saturate the blood and the less time it takes to raise the partial pressure and depth of anesthesia.
B. MAC (minimum alveolar concentration)
The MAC is the concentration of the anesthetic agent that represents the ED50 for these agents. It is the alveolar concentration in which 50% of the patients will respond to a surgical incision.
The lower the MAC the more potent the general anesthetic agent.
C. Inhalation Anesthetic Agents
- Nitrous Oxide
- Ether
- Halothane
- Enflurane
- Isoflurane
Diphenoxylate (present in Lomotil)
- A meperidine congener
- Not absorbed very well at recommended doses.
- Very useful in the treatment of diarrhea.
Meperidine (Demerol)
Meperidine is a phenylpiperidine and has a number of congeners. It is mostly effective in the CNS and bowel
- Produces analgesia, sedation, euphoria and respiratory depression.
- Less potent than morphine, 80-100 mg meperidine equals 10 mg morphine.
- Shorter duration of action than morphine (2-4 hrs).
- Meperidine has greater excitatory activity than does morphine and toxicity may lead to convulsions.
- Meperidine appears to have some atropine-like activity.
- Does not constrict the pupils to the same extent as morphine.
- Does not cause as much constipation as morphine.
- Spasmogenic effect on GI and biliary tract smooth muscle is less pronounced than that produced by morphine.
- Not an effective antitussive agent.
- In contrast to morphine, meperidine increases the force of oxytocin-induced contractions of the uterus.
- Often the drug of choice during delivery due to its lack of inhibitory effect on uterine contractions and its relatively short duration of action.
- It has serotonergic activity when combined with monoamine oxidase inhibitors, which can produce serotonin toxicity (clonus, hyperreflexia, hyperthermia, and agitation)
Adverse reactions to Meperidine
• Generally resemble a combination of opiate and atropine-like effects.
- respiratory depression, - tremors, - delirium and possible convulsions, - dry mouth
• The presentation of mixed symptoms (stupor and convulsions) is quite common in addicts taking large doses of meperidine.