NEET MDS Lessons
Pharmacology
Etomidate -Intravenous Anesthetics
- A nonbarbiturate anesthetic used primarily to induce surgical anesthesia.
- It does not produce analgesia.
- Etomidate has minimal effect on the cardiovascular system and respiration during induction of anesthesia.
- Like the barbiturates, etomidate decreases cerebral blood flow, cerebral metabolic rate and intracranial pressure.
- No changes in hepatic, renal or hematologic function have been reported.
- Myoclonic muscle movements are relatively common.
- Postoperative nausea and vomiting are more common with etomidate than with barbiturates.
Fentanyl (Sublimaze)
- Related chemically to meperidine.
- Approximately 80 times more potent than morphine.
- Duration of action very short (t1/2 20 min).
- Used mainly following general anesthesia.
- Neurolept analgesia: Fentanyl & Droperidol (Innovar)
- fentanyl in analgesic (2-10 µg/kg), or anaesthetic (30-100 µg/kg) doses seldom causes significant decreases in blood pressure when given alone, even in patients with poor LV function
- hypotension following fentanyl is mostly due to bradycardia and can be prevented by the use of anticholinergics, sympathomimetics or agents such as pancuronium this is more likely to occur in patients with high pre-existing sympathetic tone
- hypertension is the commonest disturbance with high dose fentanyl anaesthesia, usually accompanying intubation, sternotomy, or aortic root dissection
Lamotrigine (Lamictal): newer; broad spectrum (for most seizure types)
Mechanism: ↓ reactivation of Na channels (↑ refractory period, blocks high frequency cell firing)
Side effects: dizziness, ataxia, fatigue, nausea, no significant drug interactions
Chloramphenicol
derived from the bacterium Streptomyces venezuelae
Chloramphenicol is effective against a wide variety of microorganisms, but due to serious side-effects (e.g., damage to the bone marrow, including aplastic anemia) in humans, it is usually reserved for the treatment of serious and life-threatening infections (e.g., typhoid fever). It is used in treatment of cholera, as it destroys the
vibrios and decreases the diarrhoea. It is effective against tetracycline-resistant vibrios.It is also used in eye drops or ointment to treat bacterial conjunctivitis.
Mechanism and Resistance Chloramphenicol stops bacterial growth by binding to the bacterial ribosome (blocking peptidyl transferase) and inhibiting protein synthesis.
Chloramphenicol irreversibly binds to a receptor site on the 50S subunit of the bacterial ribosome, inhibiting peptidyl transferase. This inhibition consequently results in the prevention of amino acid transfer to growing peptide chains, ultimately leading to inhibition of protein formation.
Spectrum of activity: Broad-spectrum
Effect on bacteria: Bacteriostatic
Meperidine (Demerol)
Meperidine is a phenylpiperidine and has a number of congeners. It is mostly effective in the CNS and bowel
- Produces analgesia, sedation, euphoria and respiratory depression.
- Less potent than morphine, 80-100 mg meperidine equals 10 mg morphine.
- Shorter duration of action than morphine (2-4 hrs).
- Meperidine has greater excitatory activity than does morphine and toxicity may lead to convulsions.
- Meperidine appears to have some atropine-like activity.
- Does not constrict the pupils to the same extent as morphine.
- Does not cause as much constipation as morphine.
- Spasmogenic effect on GI and biliary tract smooth muscle is less pronounced than that produced by morphine.
- Not an effective antitussive agent.
- In contrast to morphine, meperidine increases the force of oxytocin-induced contractions of the uterus.
- Often the drug of choice during delivery due to its lack of inhibitory effect on uterine contractions and its relatively short duration of action.
- It has serotonergic activity when combined with monoamine oxidase inhibitors, which can produce serotonin toxicity (clonus, hyperreflexia, hyperthermia, and agitation)
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
Ciprofloxacin : Ciprofloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase
Ciprofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
Enterobacteriaceae, Vibrio, Hemophilus influenzae, Neisseria gonorrhoeae
Neisseria menigitidis, Moraxella catarrhalis, Brucella, Campylobacter,
Mycobacterium intracellulare, Legionella sp., Pseudomonas aeruginosa,
Bacillus anthracis - that causes anthrax
Weak activity against: Streptococcus pneumoniae,
No activity against: Bacteroides, Enterococcus faecium, Ureaplasma urealyticum and others
It is contraindicated in children, pregnancy, and epilepsy.
Ciprofloxacin can cause photosensitivity reactions and can elevate plasma
theophylline levels to toxic values. It can also cause constipation and sensitivity to caffeine.
Dosage in respiratory infections is 500-1500 mg a day in 2 doses.