Helicobacter Pylori Agents

  Antimicrobial

• Amoxicillin,

• Clarithromycin,

• Metronidozole

• Tetracycline

 Antisecreteory agents accelerates symptom relief and yield healing (omeprozole)

  Bismuth subsalicylate

Therapy For H. Pylori

  Original

• Tetracycline

• Metronidazole (Flagyl)

• Bismuth subsalicylate

• Given for 14 days

• >90% effective in eradicating microorganisms

 New triple therapy

• Amoxicillin

• Clarithromycin

• Omeprazole (Prilosec)

• Given for 7 days

• >90% effective in eradicating microorganisms

Dual Therapy

  Amoxicillin or clarithromycin

  Omeprazole

  Given for 14 days

  60-80% effective in eradication of H. Pylori

Class II Beta Blockers 

Block SNS stimulation of beta receptors in the heart and decreasing risks of ventricular fibrillation
– Blockage of SA and ectopic pacemakers: decreases automaticity 
– Blockage of AV increases the refractory period
- Increase AV nodal conduction ´ 
- Increase PR interval
- Reduce adrenergic activity

Treatment: Supraventricular tachycardia (AF, flutter, paroxysmal supraventricular tachycardia 
– Acebutolol 
– Esmolol 
– Propanolol 

Contraindications and Cautions 

• Contraindicated in sinus bradycardia P < 45
• Cardiogenic shock,  asthma or respiratory depression which could be made worse by the blocking of Beta receptors. 
• Use cautiously in patients with diabetes and thyroid dysfunction, which could be altered by the blockade of Beta receptors 
• Renal and hepatic dysfunction could alter the metabolism and excretion of these drugs.
 

Ciprofloxacin : Ciprofloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase

Ciprofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and  Gram-negative bacteria.

Enterobacteriaceae, Vibrio,  Hemophilus influenzae, Neisseria gonorrhoeae

 Neisseria menigitidis,  Moraxella catarrhalis,  Brucella, Campylobacter,

 Mycobacterium intracellulare, Legionella sp., Pseudomonas aeruginosa,

Bacillus anthracis - that causes anthrax

Weak activity against: Streptococcus pneumoniae,

No activity against:  Bacteroides,  Enterococcus faecium, Ureaplasma urealyticum  and others

It is contraindicated in children, pregnancy, and epilepsy.

Ciprofloxacin can cause photosensitivity reactions and can elevate plasma

theophylline levels to toxic values. It can also cause  constipation and sensitivity to caffeine.

Dosage in respiratory infections is 500-1500 mg a day in 2 doses.

Pharmacodynamics

Pharmacodynamics is the study of what drugs do to the body and how they do it.

Dose-Response Relationships

- Basic Features of the Dose-Response Relationship:  The dose-response relationship is graded instead of all-or-nothing (as dose increases, response becomes progressively larger).

- Maximal Efficacy and Relative Potency

- Maximal Efficacy: the largest effects that a drug can produce

- Relative Potency:  Potency refers to the amount of drug that must be given to elicit an effect.

- Potency is rarely an important characteristic of a drug.

- Potency of a drug implies nothing about its maximal efficacy.
 

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.

Etomidate  -Intravenous Anesthetics

- A nonbarbiturate anesthetic used primarily to induce surgical anesthesia.
- It does not produce analgesia.
- Etomidate has minimal effect on the cardiovascular system and respiration during induction of anesthesia.
- Like the barbiturates, etomidate decreases cerebral blood flow, cerebral metabolic rate and intracranial pressure.
- No changes in hepatic, renal or hematologic function have been reported.
- Myoclonic muscle movements are relatively common.
- Postoperative nausea and vomiting are more common with etomidate than with barbiturates.