NEET MDS Lessons
Pharmacology
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
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
Use of local anesthetics during pregnancy
Local anesthetics (injectable)
Drug FDA category
Articaine C
Bupivacaine C
Lidocaine B
Mepivacaine C
Prilocaine B
Vasoconstrictors
Epinephrine 1:200,000 or 1:100,000 C (higher doses)
Levonordefrin 1:20,000 Not ranked
Local anesthetics (topical)
Benzocaine C
Lidocaine B
Pramlintide -Amylin mimetics
Mechanism
synthetic analogue of human amylin that acts in conjunction with insulin
↓ release of glucagon
delays gastric emptying
Clinical use
type I and II DM
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
Mechanism of Action
When a local anesthetic is injected, it is the ionized [cation] form of the local anesthetic that actually binds to anionic channel receptors in the sodium channel, thus blocking the influx of sodium ions which are responsible for lowering the -70mv resting potential towards the firing threshold of -55mv which then results in depolarization of the nerve membrane. However, only the lipid soluble nonionized [base] form of the local anesthetic can penetrate the various barriers [e.g., nerve membrane, fibrous tissue] between the site of injection and the targeted destination which is the sodium channel.
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