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Pharmacology

BradyKinin

An endogenous vasodilator occurring in blood vessel walls. 
At least two distinct receptor types, B1 and B2, appear to exist for BradyKinin

Roles of bradykinin:

1) Mediator of inflammation and pain.
2) Regulation of microcirculation.
3) Their production is interrelated with clotting and fibrinolysin systems.
4) Responsible for circulatory change after birth.
5) Involved in shock and some immune reactions.

Neurotransmitters can be classified into:
1. Biogenic amines:
ACh, NA, DA, 5-HT, Histamine
2. Amino acids:
Excitatory (glutamate & asparate)
Inhibitory (GABA& glycine)
3. Others:
Adenosine, melatonin

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

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

Cephalosporins

Produced semisynthetically by chemical attachment of side chains to 7-aminocephalosporanic acid. Same mode of action , same resistance mech. 
But tend to be more resistant than penicillins to certain beta –lactamases .


GENERATION BASED ON :
-- BACTERIAL SUSCEPTIBILITY PATTERNS
-- RESISTANCE TO BETA –LACTAMASES
--NOT EFFECTIVE AGAINST -MRSA , L. MONOCYTOGENES , C. DIFFICLE , ENTEROCOCCI

First Generation 

Parentral

- CEPHALOTHIN
- CEFAZOLIN

Oral

- CEPHALEXIN
- CEPHRADINE
- CEFADROXIL

Second Generation

Parentral

CEFUROXIME
CEFOXITIN

Oral

CEFACLOR
CEFUROXIME AXETIL

Third Generation

Parentral

CEFOTAXIME 
CEFTIZOXIME
CEFTRIAXONE 
CEFTAZIDIME
CEFOPERAZONE

Oral 

CEFIXIME 
CEFPODOXIME
CEFDINIR 
CEFTIBUTEN

Fourth Generation

Parentral

CEFEPIME
CEFPIROME

Hydromorphone

  • About 8-10 times more potent than morphine when given intravenously.
  • Slightly shorter duration of action.
  • More soluble than morphine, thus higher concentrations may be injected if necessary.
  • Better oral/parenteral absorption ratio than morphine, but not as good as codeine or oxycodone.
  • It is used for the treatment of moderate to severe pain

Opiate Antagonists

Opiate antagonists have no agonist properties. They are utilized to reverse opiate induced respiratory depression and to prevent drug abuse.

A. Naloxone

 Pure opiate antagonist , Short duration of action,  Only 1/50th as potent orally as parenterally

B. Naltrexone

Pure opiate antagonist, Long duration of action, Better oral efficacy

 

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