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Pharmacology

Quinolone

Quinolones and fluoroquinolones form a group of  broad-spectrum antibiotics. They are derived from nalidixic acid.

Fluoroquinolone antibiotics are highly potent and considered relatively safe.

MOA : Quinolones act by inhibiting the bacterial  DNA gyrase enzyme. This way they inhibit nucleic acid synthesis and act bacteriocidically.

Drugs  :Nalidixic acid, Ciprofloxacin , Levofloxacin,  Norfloxacin ,Ofloxacin,  Moxifloxacin  , Trovafloxacin

Nitrous Oxide (N2O)

MAC 100%, blood/gas solubility ratio 0.47
- An inorganic gas., low solubility in blood, but greater solubility than N2
- Inflammable, but does support combustion.
- Excreted primarily unchanged through the lungs.
- It provides amnesia and analgesia when administered alone.
- Does not produce muscular relaxation.
- Less depressant to both the cardiovascular system and respiratory system than most of the other inhalational anesthetics.
- Lack of potency and tendency to produce anoxia are its primary limitations.
- The major benefit of nitrous oxide is its ability to reduce the amount of the secondary anesthetic agent that is necessary to reach a specified level of anesthesia.

Megltinides

nateglinide
repaglinide

Mechanism

binds to K+ channels on β-cells → postprandial insulin release


Clinical use
type 2 diabetes mellitus
may be used as monotherapy, or in combination with metformin

Glitazones (thiazolidinediones)

Thiazolidinediones, also known as the "-glitazones"

pioglitazone
rosiglitazone

Mechanism

bind to nuclear receptors involved in transcription of genes mediating insulin sensitivity
peroxisome proliferator-activating receptors (PPARs)

↑ insulin sensitivity in peripheral tissue
↓ gluconeogenesis
↑ insulin receptor numbers
↓ triglycerides

Clinical use

type II DM
as monotherapy or in combination with other agents
contraindicated in CHF
associated with increased risk of MI (in particular rosiglitazone)

Azithromycin

Azithromycin is the first macrolide antibiotic belonging to the azalide group. Azithromycin is derived from erythromycin by adding a nitrogen atom into the lactone ring of erythromycin A, thus making lactone ring 15-membered.

Azithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain gram-negative bacteria, particularly Hemophilus influenzae.

azithromycin is acid-stable and can therefore be taken orally without being protected from gastric acids.

Main elimination route is through excretion in to the biliary fluid, and some can also be eliminated through urinary excretion

Thiazide diuretics

Chlorothiazide, Hydrochlorothiazide

Mechanism(s) of Action

1.    Block facilitated Na/Cl co-transport in the early distal tubule. This is a relatively minor Na absorption mechanism and the result is modest diuresis 

2.    Potassium wasting effect 

a.    Blood volume reduction leads to increased production of aldosterone 
b.    Increased distal Na load secondary to diuretic effect 
c.    a + b = increase Na (to blood) for K (to urine) exchange which produces indirect K wasting

3.    Increase distal Ca re-absorption (direct effect) 

o    causes an increase in plasma calcium.This is unimportant NORMALLY but makes thiazides VERY inappropriate choice for hypercalcemic patients.

4.    Anti-diuretic effect in nephrogenic diabetes insipidus patients secondary to depletion of Na and Water. 

Toxicity
 
•    Electrolyte imbalance (particularly hypokalemia) ,Agranulocytosis , Allergic reactions 
•    Hyperuricemia , Thrombocytopenia 
 

Clavulanic acid is often combined with amoxicillin to treat certain infections caused by bacteria, including infections of the ears, lungs, sinus, skin, and urinary tract. It works by preventing bacterium that release beta-lactamases from destroying amoxicillin.

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