NEET MDS Lessons
Pharmacology
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
Classification
1. Natural Alkaloids of Opium
Phenanthrenes -> morphine, codeine, thebaine
Benzylisoquinolines -> papaverine, noscapine
2. Semi-synthetic Derivatives
diacetylmorphine (heroin) hydromorphone, oxymorphone hydrocodone, oxycodone
3. Synthetic Derivatives
phenylpiperidines pethidine, fentanyl, alfentanyl, sufentnyl
benzmorphans pentazocine, phenazocine, cyclazocine
propionanilides methadone
morphinans levorphanol
BETA-LACTAM ANTIBIOTICS
β-lactam antibiotics are a broad class of antibiotics including penicillin derivatives, cephalosporins, monobactams, carbapenems and β-lactamase inhibitors; basically any antibiotic agent which contains a β-lactam nucleus in its molecular structure. They are the most widely used group of antibiotics available.
Mode of action All β-lactam antibiotics are bactericidal, and act by inhibiting the synthesis of the peptidoglycan layer of bacterial cell walls.β-lactam antibiotics were mainly active only against Gram-positive bacteria, the development of broad-spectrum β-lactam antibiotics active against various Gram-negative organisms has increased the usefulness of the β-lactam antibiotics.
Common β-lactam antibiotics
Penicillins
Narrow spectrum penicillins:
benzathine penicillin
benzylpenicillin (penicillin G)
phenoxymethylpenicillin (penicillin V)
procaine penicillin
Narrow spectrum penicillinase-resistant penicillins
methicillin
dicloxacillin
flucloxacillin
Moderate spectrum penicillins :
amoxicillin, ampicillin
Broad spectrum penicillins :
co-amoxiclav (amoxycillin+clavulanic acid)
Extended Spectrum Penicillins:
piperacillin
ticarcillin
azlocillin
carbenicillin
Nalidixic acid:
Nalidixic acid is the basis for quinolone antibiotics. It acts bacteriostatically (that is, it inhibits growth and reproduction) or bactericidally (it kills them) on both Gram positive and Gram negative bacteria, depending on the concentration. It is especially used in treating urinary tract infections, caused for example by Escherichia coli, Proteus, Enterobacter and Klebsiella.
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
Antihypertensives Drugs
CATEGORIES
I. Diuretics to reduce blood volume
Chlorothiazide (Diuril)
II. Drugs that interfere with the Renin-Angiotensin System
A. Converting enzyme inhibitors Captopril , enalapril, Lisinopril
B. Angiotensin receptor antagonists Saralasin Losartan
III. Decrease peripheral vascular resistance and/or cardiac output
A. Directly acting vasodilators
1. calcium channel blockers Nifedipine , Diltiazem, amlodipine
2. potassium channel activators Minoxidil
3. elevation of cGMP Nitroprusside
4. others Hydralazin e
B. Sympathetic nervous system depressants
1. α-blockers Prazosin, phentolamine, phenoxybenzamine
2. β-blockers Propranolol ,Metoprolol, atenolol
3. norepinephrine synthesis inhibitors Metyrosine
4. norepinephrine storage inhibitors Reserpine
5. transmitter release inhibitors Guanethidine
6. centrally acting: decrease
sympathetic outflow Clonidine , methyldopa
Barbiturates
1. Long-acting. Phenobarbital is used to treat certain types of seizures (see section on antiepileptic drugs).
2. Intermediate-acting. Amobarbital, pentobarbital (occasionally used for sleep), secobarbital.
3. Short-acting. Hexobarbital, methohexital, thiopental—rarely used as IV anesthetics.