NEET MDS Lessons
Pharmacology
ANTIASTHMATIC AGENTS
Classification for antiasthmatic drugs.
I. Bronchodilators
i. Sympathomimetics (adrenergic receptor agonists)
Adrenaline, ephedrine, isoprenaline, orciprenaline, salbutamol, terbutaline, salmeterol, bambuterol
ii. Methylxanthines (theophylline and its derivatives)
Theophylline
Hydroxyethyl theophylline
Theophylline ethanolate of piperazine
iii. Anticholinergics
Atropine methonitrate
Ipratropium bromide
II. Mast cell stabilizer
Sodium cromoglycate
Ketotifen
III. Corticosteroids
Beclomethasone dipropionate
Beclomethasone (200 µg) with salbutamol
IV. Leukotriene pathway inhibitors
Montelukast
Zafirlukast
Third Generation Cephalosporins
Prototype drugs are CEFOTAXIME (IV) and CEFIXIME (oral). CEFTAZIDIME (for Pseudomonas aeruginosa.).
Further expansion of Gm negative spectrum to include hard to treat organisms such as Enterobacter, Serratia, and Pseudomonas.
In addition to better Gm negative spectrum, this group has improved pharmacokinetic properties (longer half-lives) that allow once daily dosing with some agents. In general, activity toward Gm + bacteria is reduced. These are specialty antibiotics that should be reserved for specific uses.
Enterobacteriaciae that are almost always sensitive (>95% sensitive)
E. coli
Proteus mirabilis (indole –)
Proteus vulgaris (indole +)
Klebsiella pneumoniae
Gram negative bacilli that are generally sensitive (>75% sensitive)
Morganella morganii
Providencia retgerri
Citrobacter freundii
Serratia marcescens
Pseudomonas aeruginosa (Ceftazidime only)
Gram negative bacilli that are sometimes sensitive (<75% sensitive)
Enterobacter
Stenotrophomonas (Xanthomonas) maltophilia (Cefoperazone & Ceftazidime only)
Acinetobacter
--> cefepime & cefpirome are promising for these bacteria
Bacteria that are resistant
Listeria monocytogenes
Pseudomonas cepacia
Enterococcus sp.
Uses
1. Gram negative septicemia & other serious Gm – infections
2. Pseudomonas aeruginosa infections (Ceftazidime - 90% effective)
3. Gram negative meningitis - Cefotaxime, Ceftriaxone, Cefepime. For empiric therapy add vancomycin ± rifampin to cover resistant Strep. pneumoniae
4. Gonorrhea - Single shot of Ceftriaxone is drug of choice. Oral cefixime and ceftibuten are also OK.
5. Complicated urinary tract infections, pyelonephritis
6. Osteomyelitis - Ceftriaxone in home health care situations
7. Lyme disease - ceftriaxone in home health care situations
Calcium Channel Blocking Agents
• Act on contractile and conductive tissues of the heart and on vascular smooth muscles
• Prevent movement of extracellular calcium into the cell
– Coronary and peripheral arteries dilate
– Myocardial contractility decreases
– Depress conduction system
Therapeutic Actions
• Inhibit movement of calcium ions across the membranes of myocardial and arterial muscle cells. Altering the action potential and blocking muscle cell contraction
• Depress myocardial contractility
• Slow cardiac impulse formation in the conductive tissues
• Cause a fall in BP
Miconazole
Miconazole is an imidazole antifungal agent commonly used in topical sprays, creams and ointments applied to the skin to cure fungal infections such as Athlete's foot and Jock itch. It may also be used internally to treat vaginal yeast infection.
When used by a person taking the anticoagulant medication warfarin, Miconazole may cause an adverse reaction which can lead to excessive bleeding or bruising.
Isoflurane (Forane) MAC 1.3%, Blood/gas solubility ratio 1.4
- Better muscle relaxation than with the other halogenated anesthetic agents.
- Isoflurane markedly potentiates the action of the neuromuscular blocking agents.
- Produces rapid onset and recovery of anesthesia.
- Does not sensitize the heart to catecholamines.
- Produces respiratory depression, but produces less cardiovascular depression
- than does halothane.
- It has an extremely low degree of metabolism and is apparently relatively
- nontoxic.
CNS acting drugs are of major therapeutic and clinical importance.
They can produce diverse physiologicaland psychologicaleffects such as:
•Induction of Anesthesia
•Relief of Pain
•Prevention of Epileptic seizures
•Reduction of Anxiety
•Treatment of Parkinsonism
•Treatment of Alzheimer's disease
•Treatment of Depression
•Centrally acting drugs also include drugs that are administered without medical intervention like tea, coffee, nicotine, and opiates.
Classification Based on
a. Chemical structure
I. Sulphonamidcs.and others - c.g.. sulphadiazine. etc.
2. Beta-lactum ring - e.g.. penicillin
3. Tetracycline - e.g.. Oxytetracycline,.doxycycline.etc.
b. Mechanism of action
1. Inhibits cell-wall synthesis - penicillin. cephalosporin..cycloserine. etc.
2. Cause leakage from cell-membrane – polypeptides (polymyxin, Bacitracin), polyenes (Nystatin)
3. Inhibit protein synthesis - tetracyclines. chloramphenicols. erythromycin.
4. Cause mis-reading of mRNA code - aminoglycosides
5. Interfere with DNA function - refampicin.. metronidazole
6. Interfere with intermediary metabolism - sulphonamides. ethambutole
c. Type of organism against which it is primarily activate
I. Antibacterial - penicillin.
2. Antifungal - nystatin.
d. Spectrum of activity
1. Broad spectrum - tetracylines .
2. Narrow spectrum - penicillin G (penG). streptomycin.erythromycin
e. Type of action
I. Bacteriostatic - sulphonamides, erythromycin.tertracyclines
2. Bacteriocidal - penicillin. aminoglycoside
f. Source
I. Fungi - penicillin. cephalosporins
2. Bacteria - Polymyxin B