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Pharmacology - NEETMDS- courses
NEET MDS Lessons
Pharmacology

GENERAL ANESTHETICS

General anesthesia often involves more than one drug to get different, favourable effects.
Premedication is often used to:
1. Treat anxiety - Benzodiazapenes
2. Reduce pain - Opiod anaglesics such as morphine
3. Produce muscle paralysis -E.g. Tubocurare
4. Reduce secretions
Induction of anesthesia is often done via intravenous anesthetics, which are quick and easy to administer.
Maintenance of anesthesia involves inhalation agents.

Prototype Agents:
Volatile Anesthetics:
•    Nitrous Oxide
•    Ether
•    Halothane
•    Enflurane
•    Isoflurane

Injectable Anesthetics:
•    Thiopental 
•    Ketamine
•    Etomidate
•    Propofol 
•    Midazolam
 

Propofol -Intravenous Anesthetics

- A nonbarbiturate anesthetic
- It is very lipid-soluble, acts rapidly and has a short recovery time.
- It is associated with less nausea and vomiting than some of the other IV anesthetics.
- Propofol is very similar to thiopental in its effects on the cardiorespiratory system.
- It does not have any analgesic properties but lowers the dose of opioid needed when the two agents are used in combination.

- The most significant adverse cardiovascular effect associated with propofol administration is hypotension. It should be used with caution in patients with cardiac disease.

First Generation Cephalosporins

Prototype Drugs are CEFAZOLIN (for IV use) and CEPHALEXIN (oral use).

1. Staph. aureus - excellent activity against b-lactamase-producing strains
Not effective against methicillin-resistant Staph. aureus & epidermidis

2. Streptococci - excellent activity versus Streptococcus sp.
Not effective against penicillin-resistant Strep. pneumoniae

3. Other Gm + bacteria - excellent activity except for Enterococcus sp.

4. Moderate activity against gram negative bacteria.

Caution: resistance may occur in all cases.
Susceptible organisms include:

E. coli
Proteus mirabilis
Indole + Proteus sp. (many strains resistant)
Haemophilus influenzae (some strains resistant)
Neisseria sp. (some gonococci resistant)


Uses
1. Upper respiratory tract infections due to Staph. and Strep.
2. Lower respiratory tract infections due to susceptible bacteria e.g. Strep.pneumoniae in penicillin-allergic patient (previous rash)
3. Uncomplicated urinary tract infections (Cephalexin)
4. Surgical prophylaxis for orthopedic and cardiovascular operations (cefazolin preferred because of longer half-life)
5. Staphylococcal infections of skin and skin structure

Streptomycin

Streptomycin was the first of a class of drugs called aminoglycosides to be discovered, and was the first antibiotic remedy for tuberculosis. It is derived from the actinobacterium Streptomyces griseus.

Streptomycin cannot be given orally, but must be administered by regular intramuscular injection.

Celecoxib

is a highly selective COX-2 inhibitor and primarily inhibits this isoform of cyclooxygenase, whereas traditional NSAIDs inhibit both COX-1 and COX-2. Celecoxib is approximately 10-20 times more selective for COX-2 inhibition over COX-1.

Being a sulphonamide can cause skin rash &  hypersensitivity rxn., occasional oedema& HT.

Indication

Osteoarthritis ( 100‐200mg BID ) , rheumatoid  arthritis, dysmenorrhea, acute gouty attacks,  acute musculoskeletal pain. 

SULPHONAMIDES

Derivative of  sulphonilamide (Para-amino Benzene (PABA ) sulphonamide).

Anti-bacterial spectrum

Bacteriostatic to gram + and gram - bacteria. but bactericidal concentrations arce attained in urine. S pyogencs. H influenzae.E coli, few- Staph aureus. gonococci. pneumococci, proteus, shigella and Lymphogranuloma venereum.

Mechanism of action

Inhibits bacterial folate synthetase as they compete with PABA

Less soluble in acid urine and may precipitate to cause crystalluria.

Accumulate in patients with renal failure and can cause toxicity

Classification

Shart Acting (4-8 Hrs) sulphadiazine, sulphamethizole.

Intermediate acting(8-16 Hrs): sulphamethoxazole , sulphaphenazole

Long Acting(l-7days): sulphamethoxypyridazine.

Ultralong Acting(3-8days): sulfaline

Adverse effects

I. nausea, vomiting and epigastric pain

2. crystalluria

3. hypersensitivity-like polyarthritis nodosa. Steven-Johnson Syndrome. photosenstivity

4.hemolysis in G-6PD deficiency

5. kernicterus

They inhibit metabolism of phenytoin. tolbutamide. methotrexate

Therapeutic Use

UTI Meningitis, Streptococcal pharyngitis, Bacillary Dysentery

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

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